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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyButorphanol
Identification
- Name
- Butorphanol
- Accession Number
- DB00611 (APRD00835)
- Type
- Small Molecule
- Groups
- Approved, Illicit, Vet approved
- Description
A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain. [PubChem]
- Structure
Structure for DB00611 (Butorphanol)
- Synonyms
- (-)-17-(Cyclobutylmethyl)morphinan-3,14-diol
- (-)-Butorphanol
- (-)-N-Cyclobutylmethyl-3,14-dihydroxymorphinan
- Butorfanol
- Butorphanol
- Butorphanolum
- External IDs
- BC-2627 / levo-BC 2627 / LEVO-BC-2627
- Product Ingredients
Ingredient UNII CAS InChI Key Butorphanol Tartrate 2L7I72RUHN 58786-99-5 GMTYREVWZXJPLF-AFHUBHILSA-N - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Butorphanol Nasal Spray Solution 10 mg Nasal Aa Pharma Inc 2000-08-01 Not applicable Canada 
Stadol NS - 10mg/ml Aem-liq Aerosol, metered; Liquid 10 mg Nasal Bristol Myers Squibb 1994-12-31 2004-08-04 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Butorphanol Tartrate Spray, metered 10 mg/mL Nasal A S Medication Solutions 2002-03-12 2017-06-20 US 
Butorphanol Tartrate Injection, solution 2 mg/mL Intramuscular; Intravenous West Ward Pharmaceutical 2009-05-01 Not applicable US Butorphanol Tartrate Injection 1 mg/mL Intramuscular; Intravenous Cardinal Health 1998-10-15 2017-12-22 US Butorphanol Tartrate Injection, solution 1 mg/mL Intramuscular; Intravenous Hospira, Inc. 1997-01-23 Not applicable US Butorphanol Tartrate Injection, solution 1 mg/mL Intramuscular; Intravenous West Ward Pharmaceutical 2009-05-01 Not applicable US Butorphanol Tartrate Injection, solution 2 mg/mL Intramuscular; Intravenous General Injectables & Vaccines 2013-08-14 Not applicable US Butorphanol Tartrate Injection 2 mg/mL Intramuscular; Intravenous Cardinal Health 1998-10-15 2017-12-22 US Butorphanol Tartrate Spray 10 mg/mL Nasal Mylan Pharmaceuticals 2011-01-21 Not applicable US Butorphanol Tartrate Spray, metered 10 mg/mL Nasal West Ward Pharmaceutical 2002-03-12 Not applicable US Butorphanol Tartrate Injection, solution 2 mg/mL Intramuscular; Intravenous Hospira, Inc. 1997-01-23 Not applicable US - International/Other Brands
- Butaro (Lotus Pharmaceuticals) / Butrum (Aristo) / Stadol (Bristol-Myers Squibb) / Stadol NS (Cephalon)
- Categories
- Alkaloids
- Analgesics
- Analgesics, Opioid
- Antitussive Agents
- Central Nervous System Agents
- Central Nervous System Depressants
- Mixed Agonist / Antagonist Opioids
- Morphinan Derivatives
- Morphinans
- Narcotic Antagonists
- Narcotics
- Nervous System
- Opiate Alkaloids
- Opiate Partial Agonists
- Opioid Agonist/Antagonist
- Peripheral Nervous System Agents
- Phenanthrenes
- Respiratory System Agents
- Sensory System Agents
- UNII
- QV897JC36D
- CAS number
- 42408-82-2
- Weight
- Average: 327.4605
Monoisotopic: 327.219829177 - Chemical Formula
- C21H29NO2
- InChI Key
- IFKLAQQSCNILHL-QHAWAJNXSA-N
- InChI
- InChI=1S/C21H29NO2/c23-17-7-6-16-12-19-21(24)9-2-1-8-20(21,18(16)13-17)10-11-22(19)14-15-4-3-5-15/h6-7,13,15,19,23-24H,1-5,8-12,14H2/t19-,20+,21-/m1/s1
- IUPAC Name
- (1S,9R,10S)-17-(cyclobutylmethyl)-17-azatetracyclo[7.5.3.0¹,¹⁰.0²,⁷]heptadeca-2(7),3,5-triene-4,10-diol
- SMILES
- [H][[email protected]@]12CC3=C(C=C(O)C=C3)[[email protected]]3(CCCC[[email protected]@]13O)CCN2CC1CCC1
Pharmacology
- Indication
For the relief of moderate to severe pain.
- Structured Indications
- Pharmacodynamics
Butorphanol is a synthetic opioid agonist-antagonist analgesic with a pharmacological and therapeutic profile that has been well established since its launch as a parenteral formulation in 1978. The introduction of a transnasal formulation of butorphanol represents a new and noninvasive presentation of an analgesic for moderate to severe pain. This route of administration bypasses the gastrointestinal tract, and this is an advantage for a drug such as butorphanol that undergoes significant first-pass metabolism after oral administration. The onset of action and systemic bioavailability of butorphanol following transnasal delivery are similar to those after parenteral administration. Butorphanol blocks pain impulses at specific sites in the brain and spinal cord.
- Mechanism of action
The exact mechanism of action is unknown, but is believed to interact with an opiate receptor site in the CNS (probably in or associated with the limbic system). The opiate antagonistic effect may result from competitive inhibition at the opiate receptor, but may also be a result of other mechanisms. Butorphanol is a mixed agonist-antagonist that exerts antagonistic or partially antagonistic effects at mu opiate receptor sites, but is thought to exert its agonistic effects principally at the kappa and sigma opiate receptors.
Target Actions Organism AKappa-type opioid receptor agonistHuman ADelta-type opioid receptor agonistHuman AMu-type opioid receptor partial antagonistHuman - Absorption
Rapidly absorbed after intramuscular injection and peak plasma levels are reached in 20-40 minutes. The absolute bioavailability is 60-70% and is unchanged in patients with allergic rhinitis. In patients using a nasal vasoconstrictor (oxymetazoline) the fraction of the dose absorbed was unchanged, but the rate of absorption was slowed. Oral bioavailability is only 5-17% because of extensive first-pass metabolism.
- Volume of distribution
- 305 to 901 L
- Protein binding
Serum protein binding is approximately 80%.
- Metabolism
Extensively metabolized in the liver. The pharmacological activity of butorphanol metabolites has not been studied in humans; in animal studies, butorphanol metabolites have demonstrated some analgesic activity.
- Route of elimination
Butorphanol is extensively metabolized in the liver. Elimination occurs by urine and fecal excretion.
- Half life
The elimination half-life of butorphanol is about 18 hours. In renally impaired patients with creatinine clearances <30 mL/min the elimination half-life is approximately doubled. After intravenous administration to patients with hepatic impairment, the elimination half-life of butorphanol was approximately tripled.
- Clearance
- 99 +/- 23 L/h [Young with IV 2 mg]
- 82 +/- 21 [Eldery with IV 2 mg]
- Toxicity
The clinical manifestations of butorphanol overdose are those of opioid drugs in general. The most serious symptoms are hypoventilation, cardiovascular insufficiency, coma, and death.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Drug group 2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may increase the analgesic activities of Butorphanol. Experimental, Illicit 2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may increase the analgesic activities of Butorphanol. Experimental 3,4-Methylenedioxyamphetamine 3,4-Methylenedioxyamphetamine may increase the analgesic activities of Butorphanol. Experimental, Illicit 4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may increase the analgesic activities of Butorphanol. Experimental, Illicit 7-Nitroindazole The risk or severity of adverse effects can be increased when Butorphanol is combined with 7-Nitroindazole. Experimental 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline The risk or severity of adverse effects can be increased when Butorphanol is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline. Experimental Acepromazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Acepromazine. Approved, Vet Approved Aceprometazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Aceprometazine. Approved Acetazolamide The risk or severity of adverse effects can be increased when Butorphanol is combined with Acetazolamide. Approved, Vet Approved Aclidinium The risk or severity of adverse effects can be increased when Aclidinium is combined with Butorphanol. Approved Adipiplon The risk or severity of adverse effects can be increased when Butorphanol is combined with Adipiplon. Investigational Agomelatine The risk or severity of adverse effects can be increased when Butorphanol is combined with Agomelatine. Approved, Investigational Alaproclate Butorphanol may increase the serotonergic activities of Alaproclate. Experimental Alcuronium The risk or severity of adverse effects can be increased when Alcuronium is combined with Butorphanol. Experimental Alfaxalone The risk or severity of adverse effects can be increased when Butorphanol is combined with Alfaxalone. Vet Approved Alfentanil Butorphanol may decrease the analgesic activities of Alfentanil. Approved, Illicit Alimemazine Alimemazine may increase the hypotensive activities of Butorphanol. Approved, Vet Approved Allopregnanolone The risk or severity of adverse effects can be increased when Butorphanol is combined with Allopregnanolone. Investigational Alphacetylmethadol Butorphanol may decrease the analgesic activities of Alphacetylmethadol. Experimental, Illicit Alphaprodine Butorphanol may decrease the analgesic activities of Alphaprodine. Illicit Alprazolam The risk or severity of adverse effects can be increased when Alprazolam is combined with Butorphanol. Approved, Illicit, Investigational Alvimopan The risk or severity of adverse effects can be increased when Butorphanol is combined with Alvimopan. Approved, Investigational Amiloride The risk or severity of adverse effects can be increased when Butorphanol is combined with Amiloride. Approved Amisulpride The risk or severity of adverse effects can be increased when Butorphanol is combined with Amisulpride. Approved, Investigational Amitriptyline The risk or severity of adverse effects can be increased when Butorphanol is combined with Amitriptyline. Approved Ammonium chloride Ammonium chloride may increase the excretion rate of Butorphanol which could result in a lower serum level and potentially a reduction in efficacy. Approved, Investigational, Vet Approved Amobarbital The risk or severity of adverse effects can be increased when Butorphanol is combined with Amobarbital. Approved, Illicit Amoxapine The risk or severity of adverse effects can be increased when Butorphanol is combined with Amoxapine. Approved Amperozide The risk or severity of adverse effects can be increased when Butorphanol is combined with Amperozide. Experimental Amphetamine The risk or severity of adverse effects can be increased when Butorphanol is combined with Amphetamine. Approved, Illicit, Investigational Anisotropine Methylbromide The risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Butorphanol. Approved Aripiprazole The risk or severity of adverse effects can be increased when Butorphanol is combined with Aripiprazole. Approved, Investigational Articaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Articaine. Approved Asenapine The risk or severity of adverse effects can be increased when Butorphanol is combined with Asenapine. Approved Atracurium The risk or severity of adverse effects can be increased when Atracurium is combined with Butorphanol. Approved, Experimental, Investigational Atracurium besylate The risk or severity of adverse effects can be increased when Atracurium besylate is combined with Butorphanol. Approved Atropine The risk or severity of adverse effects can be increased when Atropine is combined with Butorphanol. Approved, Vet Approved Azaperone The risk or severity of adverse effects can be increased when Butorphanol is combined with Azaperone. Investigational, Vet Approved Azelastine Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Azelastine. Approved Azosemide The risk or severity of adverse effects can be increased when Butorphanol is combined with Azosemide. Investigational Baclofen The risk or severity of adverse effects can be increased when Butorphanol is combined with Baclofen. Approved Barbital The risk or severity of adverse effects can be increased when Butorphanol is combined with Barbital. Illicit Benactyzine The risk or severity of adverse effects can be increased when Benactyzine is combined with Butorphanol. Withdrawn Bendroflumethiazide The risk or severity of adverse effects can be increased when Butorphanol is combined with Bendroflumethiazide. Approved Benmoxin The risk or severity of adverse effects can be increased when Butorphanol is combined with Benmoxin. Withdrawn Benperidol The risk or severity of adverse effects can be increased when Butorphanol is combined with Benperidol. Approved, Investigational Benzatropine The risk or severity of adverse effects can be increased when Benzatropine is combined with Butorphanol. Approved Benzocaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Benzocaine. Approved, Investigational Benzphetamine Benzphetamine may increase the analgesic activities of Butorphanol. Approved, Illicit Benzyl alcohol The risk or severity of adverse effects can be increased when Butorphanol is combined with Benzyl alcohol. Approved Bezitramide Butorphanol may decrease the analgesic activities of Bezitramide. Experimental, Illicit, Withdrawn Biperiden The risk or severity of adverse effects can be increased when Biperiden is combined with Butorphanol. Approved, Investigational BL-1020 BL-1020 may increase the hypotensive activities of Butorphanol. Investigational Bornaprine The risk or severity of adverse effects can be increased when Bornaprine is combined with Butorphanol. Experimental Brexpiprazole The risk or severity of adverse effects can be increased when Butorphanol is combined with Brexpiprazole. Approved, Investigational Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Butorphanol. Approved Brofaromine The risk or severity of adverse effects can be increased when Butorphanol is combined with Brofaromine. Experimental Bromazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Bromazepam. Approved, Illicit, Investigational Bromisoval The risk or severity of adverse effects can be increased when Butorphanol is combined with Bromisoval. Experimental Bromotheophylline The risk or severity of adverse effects can be increased when Butorphanol is combined with Bromotheophylline. Approved Bromperidol The risk or severity of adverse effects can be increased when Butorphanol is combined with Bromperidol. Approved, Investigational Brompheniramine The risk or severity of adverse effects can be increased when Butorphanol is combined with Brompheniramine. Approved Brotizolam The risk or severity of adverse effects can be increased when Butorphanol is combined with Brotizolam. Approved, Investigational, Withdrawn Bumetanide The risk or severity of adverse effects can be increased when Butorphanol is combined with Bumetanide. Approved Bupivacaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Bupivacaine. Approved, Investigational Buprenorphine Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine. Approved, Illicit, Investigational, Vet Approved Buspirone The risk or severity of adverse effects can be increased when Buspirone is combined with Butorphanol. Approved, Investigational Butabarbital The risk or severity of adverse effects can be increased when Butabarbital is combined with Butorphanol. Approved, Illicit Butacaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Butacaine. Vet Approved Butalbital The risk or severity of adverse effects can be increased when Butorphanol is combined with Butalbital. Approved, Illicit Butamben The risk or severity of adverse effects can be increased when Butorphanol is combined with Butamben. Approved, Withdrawn Butethal The risk or severity of adverse effects can be increased when Butorphanol is combined with Butethal. Approved, Illicit Butylscopolamine The risk or severity of adverse effects can be increased when Butylscopolamine is combined with Butorphanol. Approved, Investigational, Vet Approved Canertinib The risk or severity of adverse effects can be increased when Butorphanol is combined with Canertinib. Investigational Canrenoic acid The risk or severity of adverse effects can be increased when Butorphanol is combined with Canrenoic acid. Approved, Withdrawn Canrenone The risk or severity of adverse effects can be increased when Butorphanol is combined with Canrenone. Investigational Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Butorphanol. Approved, Investigational Carbinoxamine The risk or severity of adverse effects can be increased when Butorphanol is combined with Carbinoxamine. Approved Carfentanil Butorphanol may decrease the analgesic activities of Carfentanil. Illicit, Investigational, Vet Approved Carisoprodol The risk or severity of adverse effects can be increased when Butorphanol is combined with Carisoprodol. Approved Caroxazone The risk or severity of adverse effects can be increased when Butorphanol is combined with Caroxazone. Withdrawn Cetirizine The risk or severity of adverse effects can be increased when Butorphanol is combined with Cetirizine. Approved Chloral hydrate The risk or severity of adverse effects can be increased when Butorphanol is combined with Chloral hydrate. Approved, Illicit, Investigational, Vet Approved Chlordiazepoxide The risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Butorphanol. Approved, Illicit, Investigational Chlormezanone The risk or severity of adverse effects can be increased when Butorphanol is combined with Chlormezanone. Approved, Investigational, Withdrawn Chloroprocaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Chloroprocaine. Approved Chlorothiazide The risk or severity of adverse effects can be increased when Butorphanol is combined with Chlorothiazide. Approved, Vet Approved Chlorphenamine The risk or severity of adverse effects can be increased when Butorphanol is combined with Chlorphenamine. Approved Chlorphenoxamine The risk or severity of adverse effects can be increased when Chlorphenoxamine is combined with Butorphanol. Withdrawn Chlorphentermine Chlorphentermine may increase the analgesic activities of Butorphanol. Illicit, Withdrawn Chlorproethazine Chlorproethazine may increase the hypotensive activities of Butorphanol. Experimental Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Butorphanol. Approved, Investigational, Vet Approved Chlorprothixene The risk or severity of adverse effects can be increased when Butorphanol is combined with Chlorprothixene. Approved, Investigational, Withdrawn Chlorthalidone The risk or severity of adverse effects can be increased when Butorphanol is combined with Chlorthalidone. Approved Chlorzoxazone The risk or severity of adverse effects can be increased when Butorphanol is combined with Chlorzoxazone. Approved Cicletanine The risk or severity of adverse effects can be increased when Butorphanol is combined with Cicletanine. Investigational Cinchocaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Cinchocaine. Approved, Vet Approved Citalopram Butorphanol may increase the serotonergic activities of Citalopram. Approved Clemastine The risk or severity of adverse effects can be increased when Butorphanol is combined with Clemastine. Approved, Investigational Clidinium The risk or severity of adverse effects can be increased when Butorphanol is combined with Clidinium. Approved Clobazam The risk or severity of adverse effects can be increased when Butorphanol is combined with Clobazam. Approved, Illicit Clofenamide The risk or severity of adverse effects can be increased when Butorphanol is combined with Clofenamide. Experimental clomethiazole The risk or severity of adverse effects can be increased when Butorphanol is combined with clomethiazole. Investigational Clomipramine The risk or severity of adverse effects can be increased when Butorphanol is combined with Clomipramine. Approved, Investigational, Vet Approved Clonazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Clonazepam. Approved, Illicit Clonidine The risk or severity of adverse effects can be increased when Butorphanol is combined with Clonidine. Approved Clopamide The risk or severity of adverse effects can be increased when Butorphanol is combined with Clopamide. Experimental Clopenthixol The risk or severity of adverse effects can be increased when Butorphanol is combined with Clopenthixol. Experimental Clorazepate The risk or severity of adverse effects can be increased when Butorphanol is combined with Clorazepate. Approved, Illicit Clorexolone The risk or severity of adverse effects can be increased when Butorphanol is combined with Clorexolone. Experimental Clothiapine The risk or severity of adverse effects can be increased when Butorphanol is combined with Clothiapine. Experimental Clozapine The risk or severity of adverse effects can be increased when Clozapine is combined with Butorphanol. Approved Cocaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Cocaine. Approved, Illicit Codeine Butorphanol may decrease the analgesic activities of Codeine. Approved, Illicit Conivaptan The risk or severity of adverse effects can be increased when Butorphanol is combined with Conivaptan. Approved, Investigational Cyclizine The risk or severity of adverse effects can be increased when Butorphanol is combined with Cyclizine. Approved Cyclobenzaprine The risk or severity of adverse effects can be increased when Butorphanol is combined with Cyclobenzaprine. Approved Cyclopenthiazide The risk or severity of adverse effects can be increased when Butorphanol is combined with Cyclopenthiazide. Experimental Cyclopentolate The risk or severity of adverse effects can be increased when Cyclopentolate is combined with Butorphanol. Approved Cyclopropane The risk or severity of adverse effects can be increased when Butorphanol is combined with Cyclopropane. Experimental Cyclothiazide The risk or severity of adverse effects can be increased when Butorphanol is combined with Cyclothiazide. Approved Cyproheptadine The risk or severity of adverse effects can be increased when Butorphanol is combined with Cyproheptadine. Approved Dantrolene The risk or severity of adverse effects can be increased when Butorphanol is combined with Dantrolene. Approved, Investigational Dapiprazole The risk or severity of adverse effects can be increased when Butorphanol is combined with Dapiprazole. Approved Dapoxetine Butorphanol may increase the serotonergic activities of Dapoxetine. Investigational Darifenacin The risk or severity of adverse effects can be increased when Darifenacin is combined with Butorphanol. Approved, Investigational Deramciclane The risk or severity of adverse effects can be increased when Butorphanol is combined with Deramciclane. Investigational Desflurane The risk or severity of adverse effects can be increased when Butorphanol is combined with Desflurane. Approved Desipramine The risk or severity of adverse effects can be increased when Butorphanol is combined with Desipramine. Approved, Investigational Desloratadine The risk or severity of adverse effects can be increased when Desloratadine is combined with Butorphanol. Approved, Investigational Desmopressin The risk or severity of adverse effects can be increased when Butorphanol is combined with Desmopressin. Approved Desvenlafaxine Butorphanol may increase the serotonergic activities of Desvenlafaxine. Approved, Investigational Detomidine The risk or severity of adverse effects can be increased when Butorphanol is combined with Detomidine. Vet Approved Dexbrompheniramine The risk or severity of adverse effects can be increased when Butorphanol is combined with Dexbrompheniramine. Approved Dexetimide The risk or severity of adverse effects can be increased when Dexetimide is combined with Butorphanol. Withdrawn Dexmedetomidine The risk or severity of adverse effects can be increased when Butorphanol is combined with Dexmedetomidine. Approved, Vet Approved Dextroamphetamine Dextroamphetamine may increase the analgesic activities of Butorphanol. Approved, Illicit Dextromoramide Butorphanol may decrease the analgesic activities of Dextromoramide. Experimental, Illicit Dextropropoxyphene Butorphanol may decrease the analgesic activities of Dextropropoxyphene. Approved, Illicit, Investigational, Withdrawn Dezocine Butorphanol may decrease the analgesic activities of Dezocine. Approved, Investigational Diazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Diazepam. Approved, Illicit, Investigational, Vet Approved Dicyclomine The risk or severity of adverse effects can be increased when Dicyclomine is combined with Butorphanol. Approved Diethyl ether The risk or severity of adverse effects can be increased when Butorphanol is combined with Diethyl ether. Experimental Diethylpropion Diethylpropion may increase the analgesic activities of Butorphanol. Approved, Illicit Difenoxin The risk or severity of adverse effects can be increased when Butorphanol is combined with Difenoxin. Approved, Illicit Dihydrocodeine Butorphanol may decrease the analgesic activities of Dihydrocodeine. Approved, Illicit Dihydroetorphine Butorphanol may decrease the analgesic activities of Dihydroetorphine. Experimental, Illicit Dihydromorphine Butorphanol may decrease the analgesic activities of Dihydromorphine. Experimental, Illicit Dimenhydrinate The risk or severity of adverse effects can be increased when Butorphanol is combined with Dimenhydrinate. Approved Diphenhydramine The risk or severity of adverse effects can be increased when Butorphanol is combined with Diphenhydramine. Approved, Investigational Diphenoxylate Butorphanol may decrease the analgesic activities of Diphenoxylate. Approved, Illicit Dixyrazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Dixyrazine. Experimental Doramectin The risk or severity of adverse effects can be increased when Butorphanol is combined with Doramectin. Vet Approved Doxepin The risk or severity of adverse effects can be increased when Butorphanol is combined with Doxepin. Approved, Investigational Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Butorphanol. Approved, Vet Approved DPDPE Butorphanol may decrease the analgesic activities of DPDPE. Experimental Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Butorphanol. Approved, Illicit Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Butorphanol. Approved, Vet Approved Drospirenone The risk or severity of adverse effects can be increased when Butorphanol is combined with Drospirenone. Approved Drotebanol The risk or severity of adverse effects can be increased when Butorphanol is combined with Drotebanol. Experimental, Illicit Duloxetine Butorphanol may increase the serotonergic activities of Duloxetine. Approved Dyclonine The risk or severity of adverse effects can be increased when Butorphanol is combined with Dyclonine. Approved Ecgonine The risk or severity of adverse effects can be increased when Butorphanol is combined with Ecgonine. Experimental, Illicit Ecopipam The risk or severity of adverse effects can be increased when Butorphanol is combined with Ecopipam. Investigational Efavirenz The risk or severity of adverse effects can be increased when Butorphanol is combined with Efavirenz. Approved, Investigational Efonidipine The risk or severity of adverse effects can be increased when Butorphanol is combined with Efonidipine. Approved, Investigational Eltanolone The risk or severity of adverse effects can be increased when Butorphanol is combined with Eltanolone. Investigational Eluxadoline Butorphanol may increase the constipating activities of Eluxadoline. Approved, Investigational Emepronium The risk or severity of adverse effects can be increased when Emepronium is combined with Butorphanol. Experimental Enflurane The risk or severity of adverse effects can be increased when Butorphanol is combined with Enflurane. Approved, Investigational, Vet Approved Entacapone The risk or severity of adverse effects can be increased when Butorphanol is combined with Entacapone. Approved, Investigational Epitizide The risk or severity of adverse effects can be increased when Butorphanol is combined with Epitizide. Experimental Eplerenone The risk or severity of adverse effects can be increased when Butorphanol is combined with Eplerenone. Approved Escitalopram Butorphanol may increase the serotonergic activities of Escitalopram. Approved, Investigational Estazolam The risk or severity of adverse effects can be increased when Butorphanol is combined with Estazolam. Approved, Illicit Eszopiclone The risk or severity of adverse effects can be increased when Eszopiclone is combined with Butorphanol. Approved, Investigational Etacrynic acid The risk or severity of adverse effects can be increased when Butorphanol is combined with Etacrynic acid. Approved, Investigational Etanautine The risk or severity of adverse effects can be increased when Etanautine is combined with Butorphanol. Experimental Ethanol Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Ethanol. Approved Ethchlorvynol The risk or severity of adverse effects can be increased when Butorphanol is combined with Ethchlorvynol. Approved, Illicit, Withdrawn Ethopropazine The risk or severity of adverse effects can be increased when Ethopropazine is combined with Butorphanol. Approved Ethosuximide The risk or severity of adverse effects can be increased when Butorphanol is combined with Ethosuximide. Approved Ethotoin The risk or severity of adverse effects can be increased when Butorphanol is combined with Ethotoin. Approved Ethoxzolamide The risk or severity of adverse effects can be increased when Butorphanol is combined with Ethoxzolamide. Withdrawn Ethyl carbamate The risk or severity of adverse effects can be increased when Butorphanol is combined with Ethyl carbamate. Withdrawn Ethyl chloride The risk or severity of adverse effects can be increased when Butorphanol is combined with Ethyl chloride. Approved, Experimental, Investigational Ethyl loflazepate The risk or severity of adverse effects can be increased when Butorphanol is combined with Ethyl loflazepate. Approved, Illicit Ethylmorphine Butorphanol may decrease the analgesic activities of Ethylmorphine. Approved, Illicit Etidocaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Etidocaine. Approved Etifoxine The risk or severity of adverse effects can be increased when Butorphanol is combined with Etifoxine. Investigational, Withdrawn Etizolam The risk or severity of adverse effects can be increased when Butorphanol is combined with Etizolam. Approved Etomidate The risk or severity of adverse effects can be increased when Butorphanol is combined with Etomidate. Approved Etoperidone Butorphanol may increase the serotonergic activities of Etoperidone. Withdrawn Etorphine Butorphanol may decrease the analgesic activities of Etorphine. Illicit, Vet Approved Etybenzatropine The risk or severity of adverse effects can be increased when Etybenzatropine is combined with Butorphanol. Experimental Ezogabine The risk or severity of adverse effects can be increased when Butorphanol is combined with Ezogabine. Approved, Investigational Felbamate The risk or severity of adverse effects can be increased when Butorphanol is combined with Felbamate. Approved Fencamfamine The risk or severity of adverse effects can be increased when Butorphanol is combined with Fencamfamine. Approved, Illicit, Withdrawn Fenquizone The risk or severity of adverse effects can be increased when Butorphanol is combined with Fenquizone. Experimental Fentanyl Butorphanol may decrease the analgesic activities of Fentanyl. Approved, Illicit, Investigational, Vet Approved Fesoterodine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Butorphanol. Approved Fexofenadine The risk or severity of adverse effects can be increased when Butorphanol is combined with Fexofenadine. Approved, Investigational Flibanserin The risk or severity of adverse effects can be increased when Butorphanol is combined with Flibanserin. Approved, Investigational Fluanisone The risk or severity of adverse effects can be increased when Butorphanol is combined with Fluanisone. Experimental Fludiazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Fludiazepam. Approved, Illicit Flunarizine The risk or severity of adverse effects can be increased when Butorphanol is combined with Flunarizine. Approved Flunitrazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Flunitrazepam. Approved, Illicit Fluoxetine Butorphanol may increase the serotonergic activities of Fluoxetine. Approved, Vet Approved Flupentixol The risk or severity of adverse effects can be increased when Butorphanol is combined with Flupentixol. Approved, Investigational, Withdrawn Fluphenazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Fluphenazine. Approved Flurazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Flurazepam. Approved, Illicit, Investigational Fluspirilene The risk or severity of adverse effects can be increased when Butorphanol is combined with Fluspirilene. Approved, Investigational Fluticasone propionate The risk or severity of adverse effects can be increased when Butorphanol is combined with Fluticasone propionate. Approved Fluvoxamine The risk or severity of adverse effects can be increased when Butorphanol is combined with Fluvoxamine. Approved, Investigational Fosphenytoin The risk or severity of adverse effects can be increased when Butorphanol is combined with Fosphenytoin. Approved, Investigational Fospropofol The risk or severity of adverse effects can be increased when Butorphanol is combined with Fospropofol. Approved, Illicit, Investigational Furazolidone The risk or severity of adverse effects can be increased when Butorphanol is combined with Furazolidone. Approved, Investigational, Vet Approved Furosemide The risk or severity of adverse effects can be increased when Butorphanol is combined with Furosemide. Approved, Vet Approved Gabapentin The risk or severity of adverse effects can be increased when Butorphanol is combined with Gabapentin. Approved, Investigational Gabapentin Enacarbil The risk or severity of adverse effects can be increased when Butorphanol is combined with Gabapentin Enacarbil. Approved, Investigational Gallamine The risk or severity of adverse effects can be increased when Gallamine is combined with Butorphanol. Experimental Gallamine Triethiodide The risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Butorphanol. Approved Gamma Hydroxybutyric Acid The risk or severity of adverse effects can be increased when Butorphanol is combined with Gamma Hydroxybutyric Acid. Approved, Illicit, Investigational Gepefrine Gepefrine may increase the analgesic activities of Butorphanol. Experimental Gepirone The risk or severity of adverse effects can be increased when Butorphanol is combined with Gepirone. Investigational Glutethimide The risk or severity of adverse effects can be increased when Butorphanol is combined with Glutethimide. Approved, Illicit Glycopyrronium The risk or severity of adverse effects can be increased when Glycopyrronium is combined with Butorphanol. Approved, Investigational, Vet Approved Guanfacine The risk or severity of adverse effects can be increased when Butorphanol is combined with Guanfacine. Approved, Investigational Halazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Halazepam. Approved, Illicit, Withdrawn Haloperidol The risk or severity of adverse effects can be increased when Haloperidol is combined with Butorphanol. Approved Halothane The risk or severity of adverse effects can be increased when Butorphanol is combined with Halothane. Approved, Vet Approved Harmaline The risk or severity of adverse effects can be increased when Butorphanol is combined with Harmaline. Experimental Heroin Butorphanol may decrease the analgesic activities of Heroin. Approved, Illicit, Investigational Hexamethonium The risk or severity of adverse effects can be increased when Hexamethonium is combined with Butorphanol. Experimental Hexobarbital The risk or severity of adverse effects can be increased when Butorphanol is combined with Hexobarbital. Approved Homatropine The risk or severity of adverse effects can be increased when Homatropine is combined with Butorphanol. Approved Hydracarbazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Hydracarbazine. Experimental Hydrochlorothiazide The risk or severity of adverse effects can be increased when Butorphanol is combined with Hydrochlorothiazide. Approved, Vet Approved Hydrocodone Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone. Approved, Illicit Hydroflumethiazide The risk or severity of adverse effects can be increased when Butorphanol is combined with Hydroflumethiazide. Approved, Investigational Hydromorphone Butorphanol may decrease the analgesic activities of Hydromorphone. Approved, Illicit Hydroxyamphetamine Hydroxyamphetamine may increase the analgesic activities of Butorphanol. Approved Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Butorphanol. Approved Hyoscyamine The risk or severity of adverse effects can be increased when Hyoscyamine is combined with Butorphanol. Approved Ibopamine The risk or severity of adverse effects can be increased when Butorphanol is combined with Ibopamine. Experimental Iloperidone The risk or severity of adverse effects can be increased when Butorphanol is combined with Iloperidone. Approved Imipramine The risk or severity of adverse effects can be increased when Butorphanol is combined with Imipramine. Approved Indalpine Butorphanol may increase the serotonergic activities of Indalpine. Investigational, Withdrawn Indapamide The risk or severity of adverse effects can be increased when Butorphanol is combined with Indapamide. Approved Indiplon The risk or severity of adverse effects can be increased when Butorphanol is combined with Indiplon. Investigational Iofetamine I-123 Iofetamine I-123 may increase the analgesic activities of Butorphanol. Approved Ipratropium bromide The risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Butorphanol. Approved Iproclozide The risk or severity of adverse effects can be increased when Butorphanol is combined with Iproclozide. Withdrawn Iproniazid The risk or severity of adverse effects can be increased when Butorphanol is combined with Iproniazid. Withdrawn Isocarboxazid The risk or severity of adverse effects can be increased when Butorphanol is combined with Isocarboxazid. Approved Isoflurane The risk or severity of adverse effects can be increased when Butorphanol is combined with Isoflurane. Approved, Vet Approved Isosorbide The risk or severity of adverse effects can be increased when Butorphanol is combined with Isosorbide. Approved, Investigational Ketamine The risk or severity of adverse effects can be increased when Butorphanol is combined with Ketamine. Approved, Vet Approved Ketazolam The risk or severity of adverse effects can be increased when Butorphanol is combined with Ketazolam. Approved Ketobemidone Butorphanol may decrease the analgesic activities of Ketobemidone. Approved, Investigational Lamotrigine The risk or severity of adverse effects can be increased when Butorphanol is combined with Lamotrigine. Approved, Investigational Levetiracetam The risk or severity of adverse effects can be increased when Butorphanol is combined with Levetiracetam. Approved, Investigational Levobupivacaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Levobupivacaine. Approved, Investigational Levocabastine The risk or severity of adverse effects can be increased when Butorphanol is combined with Levocabastine. Approved, Investigational Levocetirizine The risk or severity of adverse effects can be increased when Butorphanol is combined with Levocetirizine. Approved Levodopa The risk or severity of adverse effects can be increased when Butorphanol is combined with Levodopa. Approved Levomethadyl Acetate Butorphanol may decrease the analgesic activities of Levomethadyl Acetate. Approved, Investigational Levomilnacipran Butorphanol may increase the serotonergic activities of Levomilnacipran. Approved, Investigational Levorphanol Butorphanol may decrease the analgesic activities of Levorphanol. Approved Lidocaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Lidocaine. Approved, Vet Approved Lisdexamfetamine Lisdexamfetamine may increase the analgesic activities of Butorphanol. Approved, Investigational Lithium The risk or severity of adverse effects can be increased when Butorphanol is combined with Lithium. Approved Lofentanil Butorphanol may decrease the analgesic activities of Lofentanil. Illicit Lofexidine The therapeutic efficacy of Butorphanol can be increased when used in combination with Lofexidine. Approved, Investigational Loprazolam The risk or severity of adverse effects can be increased when Butorphanol is combined with Loprazolam. Experimental Loratadine The risk or severity of adverse effects can be increased when Butorphanol is combined with Loratadine. Approved, Investigational Lorazepam The risk or severity of adverse effects can be increased when Lorazepam is combined with Butorphanol. Approved Lormetazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Lormetazepam. Approved Loxapine The risk or severity of adverse effects can be increased when Loxapine is combined with Butorphanol. Approved Lurasidone The risk or severity of adverse effects can be increased when Butorphanol is combined with Lurasidone. Approved, Investigational Magnesium sulfate The therapeutic efficacy of Butorphanol can be increased when used in combination with Magnesium sulfate. Approved, Investigational, Vet Approved Mannitol The risk or severity of adverse effects can be increased when Butorphanol is combined with Mannitol. Approved, Investigational Maprotiline The risk or severity of adverse effects can be increased when Butorphanol is combined with Maprotiline. Approved, Investigational Mazaticol The risk or severity of adverse effects can be increased when Mazaticol is combined with Butorphanol. Experimental Mebanazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Mebanazine. Withdrawn Mebicar The risk or severity of adverse effects can be increased when Butorphanol is combined with Mebicar. Experimental Mebutizide The risk or severity of adverse effects can be increased when Butorphanol is combined with Mebutizide. Experimental Mecamylamine The risk or severity of adverse effects can be increased when Mecamylamine is combined with Butorphanol. Approved, Investigational Meclizine The risk or severity of adverse effects can be increased when Butorphanol is combined with Meclizine. Approved Medazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Medazepam. Experimental Medetomidine The risk or severity of adverse effects can be increased when Butorphanol is combined with Medetomidine. Vet Approved Mefruside The risk or severity of adverse effects can be increased when Butorphanol is combined with Mefruside. Experimental Melatonin The risk or severity of adverse effects can be increased when Butorphanol is combined with Melatonin. Approved, Nutraceutical, Vet Approved Melperone The risk or severity of adverse effects can be increased when Butorphanol is combined with Melperone. Approved, Investigational Mephedrone Mephedrone may increase the analgesic activities of Butorphanol. Investigational Mephentermine Mephentermine may increase the analgesic activities of Butorphanol. Approved Mepivacaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Mepivacaine. Approved, Vet Approved Meprobamate The risk or severity of adverse effects can be increased when Meprobamate is combined with Butorphanol. Approved, Illicit Meptazinol Butorphanol may decrease the analgesic activities of Meptazinol. Experimental Mersalyl The risk or severity of adverse effects can be increased when Butorphanol is combined with Mersalyl. Approved Mesoridazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Mesoridazine. Approved, Investigational Metaxalone The risk or severity of adverse effects can be increased when Butorphanol is combined with Metaxalone. Approved Methadone Butorphanol may decrease the analgesic activities of Methadone. Approved Methadyl Acetate Butorphanol may decrease the analgesic activities of Methadyl Acetate. Approved, Illicit Methamphetamine Methamphetamine may increase the analgesic activities of Butorphanol. Approved, Illicit Methantheline The risk or severity of adverse effects can be increased when Methantheline is combined with Butorphanol. Approved, Investigational Methapyrilene The risk or severity of adverse effects can be increased when Butorphanol is combined with Methapyrilene. Withdrawn Methaqualone The risk or severity of adverse effects can be increased when Butorphanol is combined with Methaqualone. Illicit, Withdrawn Methazolamide The risk or severity of adverse effects can be increased when Butorphanol is combined with Methazolamide. Approved Methocarbamol The risk or severity of adverse effects can be increased when Butorphanol is combined with Methocarbamol. Approved, Vet Approved Methohexital The risk or severity of adverse effects can be increased when Methohexital is combined with Butorphanol. Approved Methotrimeprazine Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine. Approved, Investigational Methoxyflurane The risk or severity of adverse effects can be increased when Butorphanol is combined with Methoxyflurane. Approved, Investigational, Vet Approved Methoxyphenamine Methoxyphenamine may increase the analgesic activities of Butorphanol. Experimental Methscopolamine The risk or severity of adverse effects can be increased when Methscopolamine is combined with Butorphanol. Approved Methsuximide The risk or severity of adverse effects can be increased when Butorphanol is combined with Methsuximide. Approved Methyclothiazide The risk or severity of adverse effects can be increased when Butorphanol is combined with Methyclothiazide. Approved Methylecgonine The risk or severity of adverse effects can be increased when Butorphanol is combined with Methylecgonine. Experimental Methylene blue The risk or severity of adverse effects can be increased when Butorphanol is combined with Methylene blue. Approved, Investigational Methylnaltrexone The risk or severity of adverse effects can be increased when Butorphanol is combined with Methylnaltrexone. Approved Methylphenobarbital The risk or severity of adverse effects can be increased when Butorphanol is combined with Methylphenobarbital. Approved Methylscopolamine bromide The risk or severity of adverse effects can be increased when Methylscopolamine bromide is combined with Butorphanol. Approved Meticrane The risk or severity of adverse effects can be increased when Butorphanol is combined with Meticrane. Experimental Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Butorphanol. Approved Metolazone The risk or severity of adverse effects can be increased when Butorphanol is combined with Metolazone. Approved Metyrosine Butorphanol may increase the sedative activities of Metyrosine. Approved Midazolam The risk or severity of adverse effects can be increased when Butorphanol is combined with Midazolam. Approved, Illicit Midomafetamine Midomafetamine may increase the analgesic activities of Butorphanol. Experimental, Illicit, Investigational Milnacipran Butorphanol may increase the serotonergic activities of Milnacipran. Approved, Investigational Minaprine The risk or severity of adverse effects can be increased when Butorphanol is combined with Minaprine. Approved Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Butorphanol. Approved, Investigational Mirtazapine Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine. Approved MMDA MMDA may increase the analgesic activities of Butorphanol. Experimental, Illicit Moclobemide The risk or severity of adverse effects can be increased when Butorphanol is combined with Moclobemide. Approved, Investigational Molindone The risk or severity of adverse effects can be increased when Butorphanol is combined with Molindone. Approved Moricizine Moricizine may increase the hypotensive activities of Butorphanol. Approved, Investigational, Withdrawn Morphine Butorphanol may decrease the analgesic activities of Morphine. Approved, Investigational Muzolimine The risk or severity of adverse effects can be increased when Butorphanol is combined with Muzolimine. Experimental Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Butorphanol. Approved, Investigational Nalbuphine Butorphanol may decrease the analgesic activities of Nalbuphine. Approved Naloxegol The risk or severity of adverse effects can be increased when Butorphanol is combined with Naloxegol. Approved Naltrexone The therapeutic efficacy of Butorphanol can be decreased when used in combination with Naltrexone. Approved, Investigational, Vet Approved Nefazodone Butorphanol may increase the serotonergic activities of Nefazodone. Approved, Withdrawn Nialamide The risk or severity of adverse effects can be increased when Butorphanol is combined with Nialamide. Withdrawn Nicomorphine Butorphanol may decrease the analgesic activities of Nicomorphine. Experimental Nitrazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Nitrazepam. Approved Nitrous oxide The risk or severity of adverse effects can be increased when Butorphanol is combined with Nitrous oxide. Approved, Vet Approved Norflurane The risk or severity of adverse effects can be increased when Butorphanol is combined with Norflurane. Approved, Investigational Normethadone Butorphanol may decrease the analgesic activities of Normethadone. Approved, Illicit Nortriptyline The risk or severity of adverse effects can be increased when Butorphanol is combined with Nortriptyline. Approved Octamoxin The risk or severity of adverse effects can be increased when Butorphanol is combined with Octamoxin. Withdrawn Olanzapine The risk or severity of adverse effects can be increased when Olanzapine is combined with Butorphanol. Approved, Investigational Olopatadine The risk or severity of adverse effects can be increased when Butorphanol is combined with Olopatadine. Approved Ondansetron The risk or severity of adverse effects can be increased when Butorphanol is combined with Ondansetron. Approved Opium Butorphanol may decrease the analgesic activities of Opium. Approved, Illicit Orphenadrine Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine. Approved Osanetant The risk or severity of adverse effects can be increased when Butorphanol is combined with Osanetant. Investigational Otilonium The risk or severity of adverse effects can be increased when Otilonium is combined with Butorphanol. Experimental, Investigational Oxazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Oxazepam. Approved Oxetacaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Oxethazaine. Approved, Investigational Oxitropium The risk or severity of adverse effects can be increased when Oxitropium is combined with Butorphanol. Investigational Oxprenolol The risk or severity of adverse effects can be increased when Butorphanol is combined with Oxprenolol. Approved Oxybuprocaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Oxybuprocaine. Approved, Investigational Oxybutynin The risk or severity of adverse effects can be increased when Oxybutynin is combined with Butorphanol. Approved, Investigational Oxycodone Butorphanol may decrease the analgesic activities of Oxycodone. Approved, Illicit, Investigational Oxymorphone Butorphanol may decrease the analgesic activities of Oxymorphone. Approved, Investigational, Vet Approved Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Butorphanol. Approved Paliperidone The risk or severity of adverse effects can be increased when Butorphanol is combined with Paliperidone. Approved Pancuronium The risk or severity of adverse effects can be increased when Pancuronium is combined with Butorphanol. Approved Paraldehyde Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde. Approved, Investigational Pargyline The risk or severity of adverse effects can be increased when Butorphanol is combined with Pargyline. Approved Paroxetine Butorphanol may increase the serotonergic activities of Paroxetine. Approved, Investigational Pegvisomant The therapeutic efficacy of Pegvisomant can be decreased when used in combination with Butorphanol. Approved Penfluridol The risk or severity of adverse effects can be increased when Butorphanol is combined with Penfluridol. Experimental Pentazocine Butorphanol may decrease the analgesic activities of Pentazocine. Approved, Vet Approved Pentobarbital The risk or severity of adverse effects can be increased when Pentobarbital is combined with Butorphanol. Approved, Investigational, Vet Approved Pentolinium The risk or severity of adverse effects can be increased when Pentolinium is combined with Butorphanol. Approved Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Butorphanol. Approved Perazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Perazine. Approved, Investigational Perospirone The risk or severity of adverse effects can be increased when Butorphanol is combined with Perospirone. Approved Perphenazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Perphenazine. Approved Pethidine Butorphanol may decrease the analgesic activities of Pethidine. Approved Phenazocine Butorphanol may decrease the analgesic activities of Phenazocine. Experimental Phenelzine The risk or severity of adverse effects can be increased when Butorphanol is combined with Phenelzine. Approved Phenglutarimide The risk or severity of adverse effects can be increased when Phenglutarimide is combined with Butorphanol. Experimental Phenibut The risk or severity of adverse effects can be increased when Butorphanol is combined with Phenibut. Experimental Pheniprazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Pheniprazine. Withdrawn Phenobarbital The risk or severity of adverse effects can be increased when Butorphanol is combined with Phenobarbital. Approved, Investigational Phenoperidine Butorphanol may decrease the analgesic activities of Phenoperidine. Experimental Phenoxyethanol The risk or severity of adverse effects can be increased when Butorphanol is combined with Phenoxyethanol. Approved Phenoxypropazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Phenoxypropazine. Withdrawn Phentermine Phentermine may increase the analgesic activities of Butorphanol. Approved, Illicit Phenytoin The risk or severity of adverse effects can be increased when Butorphanol is combined with Phenytoin. Approved, Vet Approved Pimozide The risk or severity of adverse effects can be increased when Butorphanol is combined with Pimozide. Approved Pipamperone The risk or severity of adverse effects can be increased when Butorphanol is combined with Pipamperone. Approved, Investigational Pipecuronium The risk or severity of adverse effects can be increased when Pipecuronium is combined with Butorphanol. Approved Pipotiazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Pipotiazine. Approved, Investigational Pirenzepine The risk or severity of adverse effects can be increased when Pirenzepine is combined with Butorphanol. Approved Piretanide The risk or severity of adverse effects can be increased when Butorphanol is combined with Piretanide. Approved Piritramide Butorphanol may decrease the analgesic activities of Piritramide. Approved, Investigational Pirlindole The risk or severity of adverse effects can be increased when Butorphanol is combined with Pirlindole. Approved Pivhydrazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Pivhydrazine. Withdrawn Pizotifen The risk or severity of adverse effects can be increased when Butorphanol is combined with Pizotifen. Approved Polythiazide The risk or severity of adverse effects can be increased when Butorphanol is combined with Polythiazide. Approved Pomalidomide The risk or severity of adverse effects can be increased when Butorphanol is combined with Pomalidomide. Approved Potassium The risk or severity of adverse effects can be increased when Butorphanol is combined with Potassium. Approved, Investigational Potassium Citrate The risk or severity of adverse effects can be increased when Butorphanol is combined with Potassium Citrate. Approved, Investigational, Vet Approved Pramipexole Butorphanol may increase the sedative activities of Pramipexole. Approved, Investigational Pramocaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Pramocaine. Approved Prazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Prazepam. Approved, Illicit Pregabalin The therapeutic efficacy of Butorphanol can be increased when used in combination with Pregabalin. Approved, Illicit, Investigational Prilocaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Prilocaine. Approved Primidone The risk or severity of adverse effects can be increased when Butorphanol is combined with Primidone. Approved, Vet Approved Procaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Procaine. Approved, Investigational, Vet Approved Procarbazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Procarbazine. Approved, Investigational Prochlorperazine The risk or severity of adverse effects can be increased when Prochlorperazine is combined with Butorphanol. Approved, Vet Approved Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Butorphanol. Approved Promazine The risk or severity of adverse effects can be increased when Promazine is combined with Butorphanol. Approved, Vet Approved Promethazine Promethazine may increase the hypotensive activities of Butorphanol. Approved, Investigational Propanidid The risk or severity of adverse effects can be increased when Butorphanol is combined with Propanidid. Experimental Propantheline The risk or severity of adverse effects can be increased when Propantheline is combined with Butorphanol. Approved Proparacaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Proparacaine. Approved, Vet Approved Propericiazine Propericiazine may increase the hypotensive activities of Butorphanol. Approved, Investigational Propiopromazine Propiopromazine may increase the hypotensive activities of Butorphanol. Vet Approved Propiverine The risk or severity of adverse effects can be increased when Propiverine is combined with Butorphanol. Approved, Investigational Propofol The risk or severity of adverse effects can be increased when Butorphanol is combined with Propofol. Approved, Investigational, Vet Approved Propoxycaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Propoxycaine. Approved Protriptyline The risk or severity of adverse effects can be increased when Butorphanol is combined with Protriptyline. Approved Proxibarbal The risk or severity of adverse effects can be increased when Butorphanol is combined with Proxibarbal. Experimental PSD502 The risk or severity of adverse effects can be increased when Butorphanol is combined with PSD502. Investigational Pseudoephedrine Pseudoephedrine may increase the analgesic activities of Butorphanol. Approved Quazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Quazepam. Approved, Illicit Quetiapine The risk or severity of adverse effects can be increased when Butorphanol is combined with Quetiapine. Approved Quinethazone The risk or severity of adverse effects can be increased when Butorphanol is combined with Quinethazone. Approved Quinidine The risk or severity of adverse effects can be increased when Quinidine is combined with Butorphanol. Approved, Investigational Quinisocaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Quinisocaine. Experimental Raclopride The risk or severity of adverse effects can be increased when Butorphanol is combined with Raclopride. Investigational Ramelteon The risk or severity of adverse effects can be increased when Butorphanol is combined with Ramelteon. Approved, Investigational Ramosetron Butorphanol may increase the constipating activities of Ramosetron. Approved, Investigational Rasagiline The risk or severity of adverse effects can be increased when Butorphanol is combined with Rasagiline. Approved Remifentanil Butorphanol may decrease the analgesic activities of Remifentanil. Approved Remoxipride The risk or severity of adverse effects can be increased when Butorphanol is combined with Remoxipride. Approved, Withdrawn Reserpine The risk or severity of adverse effects can be increased when Reserpine is combined with Butorphanol. Approved, Investigational Rilpivirine The serum concentration of Butorphanol can be decreased when it is combined with Rilpivirine. Approved Risperidone The risk or severity of adverse effects can be increased when Butorphanol is combined with Risperidone. Approved, Investigational Ritanserin The risk or severity of adverse effects can be increased when Butorphanol is combined with Ritanserin. Investigational Ritobegron Ritobegron may increase the analgesic activities of Butorphanol. Investigational Rolofylline The risk or severity of adverse effects can be increased when Butorphanol is combined with Rolofylline. Investigational Romifidine The risk or severity of adverse effects can be increased when Butorphanol is combined with Romifidine. Vet Approved Ropinirole Butorphanol may increase the sedative activities of Ropinirole. Approved, Investigational Ropivacaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Ropivacaine. Approved Rotigotine Butorphanol may increase the sedative activities of Rotigotine. Approved Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Butorphanol. Approved Safrazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Safrazine. Withdrawn Scopolamine The risk or severity of adverse effects can be increased when Scopolamine is combined with Butorphanol. Approved, Investigational Secobarbital The risk or severity of adverse effects can be increased when Secobarbital is combined with Butorphanol. Approved, Vet Approved Selegiline The risk or severity of adverse effects can be increased when Butorphanol is combined with Selegiline. Approved, Investigational, Vet Approved Sepranolone The risk or severity of adverse effects can be increased when Butorphanol is combined with Sepranolone. Investigational Sertindole The risk or severity of adverse effects can be increased when Butorphanol is combined with Sertindole. Approved, Investigational, Withdrawn Sertraline Butorphanol may increase the serotonergic activities of Sertraline. Approved Sevoflurane The risk or severity of adverse effects can be increased when Butorphanol is combined with Sevoflurane. Approved, Vet Approved Sodium oxybate Sodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Butorphanol. Approved Solifenacin The risk or severity of adverse effects can be increased when Solifenacin is combined with Butorphanol. Approved Spiradoline The risk or severity of adverse effects can be increased when Butorphanol is combined with Spiradoline. Investigational Spironolactone The risk or severity of adverse effects can be increased when Butorphanol is combined with Spironolactone. Approved Stiripentol The risk or severity of adverse effects can be increased when Butorphanol is combined with Stiripentol. Approved Succinylcholine Succinylcholine may increase the bradycardic activities of Butorphanol. Approved Sufentanil Butorphanol may decrease the analgesic activities of Sufentanil. Approved, Investigational Sulpiride The risk or severity of adverse effects can be increased when Butorphanol is combined with Sulpiride. Approved, Investigational Sultopride The risk or severity of adverse effects can be increased when Butorphanol is combined with Sultopride. Experimental Suvorexant Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant. Approved, Investigational Tandospirone The risk or severity of adverse effects can be increased when Butorphanol is combined with Tandospirone. Investigational Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Butorphanol. Approved Tasimelteon The risk or severity of adverse effects can be increased when Butorphanol is combined with Tasimelteon. Approved, Investigational Temazepam The risk or severity of adverse effects can be increased when Temazepam is combined with Butorphanol. Approved, Investigational Tetrabenazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Tetrabenazine. Approved, Investigational Tetracaine The risk or severity of adverse effects can be increased when Butorphanol is combined with Tetracaine. Approved, Vet Approved Tetrahydropalmatine The risk or severity of adverse effects can be increased when Butorphanol is combined with Tetrahydropalmatine. Investigational Tetrodotoxin The risk or severity of adverse effects can be increased when Butorphanol is combined with Tetrodotoxin. Investigational Thalidomide Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide. Approved, Investigational, Withdrawn Theobromine The risk or severity of adverse effects can be increased when Butorphanol is combined with Theobromine. Approved, Investigational Thiamylal The risk or severity of adverse effects can be increased when Butorphanol is combined with Thiamylal. Approved, Vet Approved Thiazinam Thiazinam may increase the hypotensive activities of Butorphanol. Experimental Thiethylperazine Thiethylperazine may increase the hypotensive activities of Butorphanol. Withdrawn Thiopental The risk or severity of adverse effects can be increased when Butorphanol is combined with Thiopental. Approved, Vet Approved Thioproperazine Thioproperazine may increase the hypotensive activities of Butorphanol. Approved Thioridazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Thioridazine. Approved, Withdrawn Thiothixene The risk or severity of adverse effects can be increased when Butorphanol is combined with Thiothixene. Approved Tiagabine The risk or severity of adverse effects can be increased when Butorphanol is combined with Tiagabine. Approved, Investigational Tiapride The risk or severity of adverse effects can be increased when Butorphanol is combined with Tiapride. Approved, Investigational Ticrynafen The risk or severity of adverse effects can be increased when Butorphanol is combined with Ticrynafen. Withdrawn Tiletamine The risk or severity of adverse effects can be increased when Butorphanol is combined with Tiletamine. Vet Approved Tilidine Butorphanol may decrease the analgesic activities of Tilidine. Experimental Tiotropium The risk or severity of adverse effects can be increased when Tiotropium is combined with Butorphanol. Approved Tizanidine The risk or severity of adverse effects can be increased when Butorphanol is combined with Tizanidine. Approved, Investigational Tolcapone The risk or severity of adverse effects can be increased when Butorphanol is combined with Tolcapone. Approved, Withdrawn Toloxatone The risk or severity of adverse effects can be increased when Butorphanol is combined with Toloxatone. Approved Tolterodine The risk or severity of adverse effects can be increased when Tolterodine is combined with Butorphanol. Approved, Investigational Tolvaptan The risk or severity of adverse effects can be increased when Butorphanol is combined with Tolvaptan. Approved Topiramate The risk or severity of adverse effects can be increased when Butorphanol is combined with Topiramate. Approved Torasemide The risk or severity of adverse effects can be increased when Butorphanol is combined with Torasemide. Approved Tramadol Butorphanol may decrease the analgesic activities of Tramadol. Approved, Investigational Tranylcypromine The risk or severity of adverse effects can be increased when Butorphanol is combined with Tranylcypromine. Approved, Investigational Trazodone The risk or severity of adverse effects can be increased when Butorphanol is combined with Trazodone. Approved, Investigational Triamterene The risk or severity of adverse effects can be increased when Butorphanol is combined with Triamterene. Approved Triazolam The risk or severity of adverse effects can be increased when Butorphanol is combined with Triazolam. Approved, Investigational Tricaine methanesulfonate The risk or severity of adverse effects can be increased when Butorphanol is combined with Tricaine methanesulfonate. Vet Approved Trichlormethiazide The risk or severity of adverse effects can be increased when Butorphanol is combined with Trichlormethiazide. Approved, Vet Approved Trichloroethylene The risk or severity of adverse effects can be increased when Butorphanol is combined with Trichloroethylene. Approved Trifluoperazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Trifluoperazine. Approved, Investigational Trifluperidol The risk or severity of adverse effects can be increased when Butorphanol is combined with Trifluperidol. Experimental Triflupromazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Triflupromazine. Approved, Vet Approved Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Butorphanol. Approved Trimethaphan The risk or severity of adverse effects can be increased when Trimethaphan is combined with Butorphanol. Approved, Investigational Trimipramine The risk or severity of adverse effects can be increased when Butorphanol is combined with Trimipramine. Approved Triprolidine The risk or severity of adverse effects can be increased when Butorphanol is combined with Triprolidine. Approved Tropatepine The risk or severity of adverse effects can be increased when Tropatepine is combined with Butorphanol. Experimental Tropicamide The risk or severity of adverse effects can be increased when Tropicamide is combined with Butorphanol. Approved, Investigational Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Butorphanol. Approved Tubocurarine The risk or severity of adverse effects can be increased when Tubocurarine is combined with Butorphanol. Approved Ularitide The risk or severity of adverse effects can be increased when Butorphanol is combined with Ularitide. Investigational Umeclidinium The risk or severity of adverse effects can be increased when Umeclidinium is combined with Butorphanol. Approved Valproic Acid The risk or severity of adverse effects can be increased when Butorphanol is combined with Valproic Acid. Approved, Investigational Vecuronium The risk or severity of adverse effects can be increased when Vecuronium is combined with Butorphanol. Approved Vemurafenib The risk or severity of QTc prolongation can be increased when Vemurafenib is combined with Butorphanol. Approved Venlafaxine Butorphanol may increase the serotonergic activities of Venlafaxine. Approved Veralipride The risk or severity of adverse effects can be increased when Butorphanol is combined with Veralipride. Experimental Vigabatrin The risk or severity of adverse effects can be increased when Butorphanol is combined with Vigabatrin. Approved Vinyl ether The risk or severity of adverse effects can be increased when Butorphanol is combined with Vinyl ether. Experimental Vortioxetine The risk or severity of adverse effects can be increased when Butorphanol is combined with Vortioxetine. Approved, Investigational Xenon The risk or severity of adverse effects can be increased when Butorphanol is combined with Xenon. Experimental Xipamide The risk or severity of adverse effects can be increased when Butorphanol is combined with Xipamide. Experimental Xylazine The risk or severity of adverse effects can be increased when Butorphanol is combined with Xylazine. Vet Approved Zaleplon The risk or severity of adverse effects can be increased when Butorphanol is combined with Zaleplon. Approved, Illicit, Investigational Ziconotide The risk or severity of adverse effects can be increased when Butorphanol is combined with Ziconotide. Approved Zimelidine Butorphanol may increase the serotonergic activities of Zimelidine. Withdrawn Ziprasidone The risk or severity of adverse effects can be increased when Ziprasidone is combined with Butorphanol. Approved Zolazepam The risk or severity of adverse effects can be increased when Butorphanol is combined with Zolazepam. Vet Approved Zolpidem Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Zolpidem. Approved Zonisamide The risk or severity of adverse effects can be increased when Butorphanol is combined with Zonisamide. Approved, Investigational Zopiclone The risk or severity of adverse effects can be increased when Butorphanol is combined with Zopiclone. Approved Zotepine The risk or severity of adverse effects can be increased when Butorphanol is combined with Zotepine. Approved, Investigational, Withdrawn Zuclopenthixol The risk or severity of adverse effects can be increased when Butorphanol is combined with Zuclopenthixol. Approved, Investigational - Food Interactions
- Avoid alcohol.
References
- Synthesis Reference
Monkovic, I. and Conway, T.T.; U.S. Patent 3,775,414; November 27,1973; Monkovic, I.,Wong, H. and Lim, G.; U.S. Patent 3,980,641; September 14, 1976; Pachter, IJ., Belleau, B.R. and Monkovic, I.; U.S. Patent 3,819,635; June 25,1974; and Lim, G. and Hooper, J.W.; U.S. Patent 4,017,497; April 12,1977; all assigned to Bristol-Myers Company.
- General References
- Gear RW, Miaskowski C, Gordon NC, Paul SM, Heller PH, Levine JD: The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain. Pain. 1999 Nov;83(2):339-45. [PubMed:10534607]
- Fan LW, Tanaka S, Tien LT, Ma T, Rockhold RW, Ho IK: Withdrawal from dependence upon butorphanol uniquely increases kappa(1)-opioid receptor binding in the rat brain. Brain Res Bull. 2002 Jun;58(2):149-60. [PubMed:12127012]
- External Links
- KEGG Drug
- D00837
- KEGG Compound
- C06863
- PubChem Compound
- 6916249
- PubChem Substance
- 46507553
- ChemSpider
- 16735714
- BindingDB
- 50240437
- ChEBI
- 3242
- ChEMBL
- CHEMBL33986
- Therapeutic Targets Database
- DAP000214
- PharmGKB
- PA164745398
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Butorphanol
- ATC Codes
- N02AF01 — Butorphanol
- AHFS Codes
- 28:08.12 — Opiate Partial Agonists
- FDA label
- Download (320 KB)
- MSDS
- Download (60.6 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 1 Recruiting Treatment Anxiety, Preoperative 1 4 Completed Treatment Curettage / Pregnancy termination therapy 1 4 Completed Treatment Hysterectomy / Postoperative pain 1 4 Completed Treatment Postoperative pain 1 Not Available Completed Prevention Anaesthesia therapy / Pain 1 Not Available Recruiting Prevention Acute Agitation 1 Not Available Unknown Status Treatment Labour Pain 1
Pharmacoeconomics
- Manufacturers
- Bedford laboratories div ben venue laboratories inc
- Claris lifesciences ltd
- Hikma farmaceutica (portugal) sa
- Hikma farmaceutica sa
- Hospira inc
- Apothecon inc div bristol myers squibb
- Mylan pharmaceuticals inc
- Novex pharma
- Roxane laboratories inc
- Bristol myers squibb co pharmaceutical research institute
- Packagers
- Apotex Inc.
- A-S Medication Solutions LLC
- Bedford Labs
- Ben Venue Laboratories Inc.
- Bristol-Myers Squibb Co.
- Cardinal Health
- Dispensing Solutions
- Hikma Pharmaceuticals
- Hospira Inc.
- Intervet International
- Mead Johnson and Co.
- Meridian Medical Technologies Inc.
- Mylan
- Novex Pharma
- Patheon Inc.
- Physicians Total Care Inc.
- Roxane Labs
- West-Ward Pharmaceuticals
- Dosage forms
Form Route Strength Solution Nasal 10 mg Injection Intramuscular; Intravenous 1 mg/mL Injection Intramuscular; Intravenous 2 mg/mL Injection, solution Intramuscular; Intravenous 1 mg/mL Injection, solution Intramuscular; Intravenous 2 mg/mL Spray Nasal 10 mg/mL Spray, metered Nasal 10 mg/mL Spray Nasal 10 mg Aerosol, metered; liquid Nasal 10 mg - Prices
Unit description Cost Unit Butorphanol Tartrate 10 mg/ml Solution 2.5ml Bottle 56.99USD bottle Butorphanol 10 mg/ml spray 39.63USD ml Stadol 2 mg/ml vial 10.11USD ml Butorphanol 2 mg/ml vial 7.2USD ml Butorphanol 1 mg/ml vial 3.6USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 272-274 Monkovic, I. and Conway, T.T.; U.S. Patent 3,775,414; November 27,1973; Monkovic, I.,Wong, H. and Lim, G.; U.S. Patent 3,980,641; September 14, 1976; Pachter, IJ., Belleau, B.R. and Monkovic, I.; U.S. Patent 3,819,635; June 25,1974; and Lim, G. and Hooper, J.W.; U.S. Patent 4,017,497; April 12,1977; all assigned to Bristol-Myers Company. water solubility Moderate Not Available logP 3.3 Not Available - Predicted Properties
Property Value Source Water Solubility 0.16 mg/mL ALOGPS logP 3.65 ALOGPS logP 2.89 ChemAxon logS -3.3 ALOGPS pKa (Strongest Acidic) 9.86 ChemAxon pKa (Strongest Basic) 10.7 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 43.7 Å2 ChemAxon Rotatable Bond Count 2 ChemAxon Refractivity 95.92 m3·mol-1 ChemAxon Polarizability 37.94 Å3 ChemAxon Number of Rings 5 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9798 Blood Brain Barrier + 0.9463 Caco-2 permeable + 0.6844 P-glycoprotein substrate Substrate 0.8494 P-glycoprotein inhibitor I Inhibitor 0.5 P-glycoprotein inhibitor II Inhibitor 0.5667 Renal organic cation transporter Inhibitor 0.6508 CYP450 2C9 substrate Non-substrate 0.8248 CYP450 2D6 substrate Substrate 0.509 CYP450 3A4 substrate Substrate 0.5842 CYP450 1A2 substrate Non-inhibitor 0.6532 CYP450 2C9 inhibitor Non-inhibitor 0.9094 CYP450 2D6 inhibitor Inhibitor 0.6572 CYP450 2C19 inhibitor Non-inhibitor 0.8456 CYP450 3A4 inhibitor Non-inhibitor 0.8744 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9017 Ames test Non AMES toxic 0.7587 Carcinogenicity Non-carcinogens 0.9573 Biodegradation Not ready biodegradable 0.9368 Rat acute toxicity 2.6466 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.5378 hERG inhibition (predictor II) Inhibitor 0.5983
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Phenanthrenes and derivatives
- Sub Class
- Not Available
- Direct Parent
- Phenanthrenes and derivatives
- Alternative Parents
- Benzazocines / Tetralins / Aralkylamines / 1-hydroxy-2-unsubstituted benzenoids / Piperidines / Tertiary alcohols / Trialkylamines / Cyclic alcohols and derivatives / 1,2-aminoalcohols / Azacyclic compounds show 2 more
- Substituents
- Phenanthrene / Benzazocine / Tetralin / 1-hydroxy-2-unsubstituted benzenoid / Aralkylamine / Piperidine / Cyclic alcohol / Tertiary alcohol / 1,2-aminoalcohol / Tertiary amine show 12 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
Targets
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
- Gene Name
- OPRK1
- Uniprot ID
- P41145
- Uniprot Name
- Kappa-type opioid receptor
- Molecular Weight
- 42644.665 Da
References
- Vivian JA, DeYoung MB, Sumpter TL, Traynor JR, Lewis JW, Woods JH: kappa-Opioid receptor effects of butorphanol in rhesus monkeys. J Pharmacol Exp Ther. 1999 Jul;290(1):259-65. [PubMed:10381785]
- Park Y, Jang CG, Ho IK, Ko KH: kappa-opioid agonist stimulated regional distribution of [(35)S]GTPgammas binding in butorphanol continuously infused rat. Brain Res Bull. 2000 May 1;52(1):17-20. [PubMed:10779697]
- Fan LW, Tanaka S, Tien LT, Ma T, Rockhold RW, Ho IK: Withdrawal from dependence upon butorphanol uniquely increases kappa(1)-opioid receptor binding in the rat brain. Brain Res Bull. 2002 Jun;58(2):149-60. [PubMed:12127012]
- Fan LW, Tanaka S, Park Y, Sasaki K, Ma T, Tien LT, Rockhold RW, Ho IK: Butorphanol dependence and withdrawal decrease hippocampal kappa 2-opioid receptor binding. Brain Res. 2002 Dec 27;958(2):277-90. [PubMed:12470863]
- Commiskey S, Fan LW, Ho IK, Rockhold RW: Butorphanol: effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors. J Pharmacol Sci. 2005 Jun;98(2):109-16. Epub 2005 Jun 8. [PubMed:15942128]
- Picker MJ, Benyas S, Horwitz JA, Thompson K, Mathewson C, Smith MA: Discriminative stimulus effects of butorphanol: influence of training dose on the substitution patterns produced by Mu, Kappa and Delta opioid agonists. J Pharmacol Exp Ther. 1996 Dec;279(3):1130-41. [PubMed:8968334]
- Wakabayashi H, Tokuyama S, Ho IK: Simultaneous measurement of biogenic amines and their metabolites in rat brain regions after acute administration of and abrupt withdrawal from butorphanol or morphine. Neurochem Res. 1995 Oct;20(10):1179-85. [PubMed:8746803]
- Narita M, Feng Y, Makimura M, Hoskins B, Ho IK: Repeated administration of opioids alters characteristics of membrane-bound phorbol ester binding in rat brain. Eur J Pharmacol. 1994 Dec 27;271(2-3):547-50. [PubMed:7705457]
- Ohta S, Niwa M, Nozaki M, Tsurumi K, Shimonaka H, Tanahashi T, Uematsu H, Yamamoto M, Fujimura H: [Kappa-type opioid receptor in human placental membrane]. Masui. 1989 Oct;38(10):1293-300. [PubMed:2555580]
- Walsh SL, Chausmer AE, Strain EC, Bigelow GE: Evaluation of the mu and kappa opioid actions of butorphanol in humans through differential naltrexone blockade. Psychopharmacology (Berl). 2008 Jan;196(1):143-55. Epub 2007 Oct 2. [PubMed:17909753]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
- Gene Name
- OPRD1
- Uniprot ID
- P41143
- Uniprot Name
- Delta-type opioid receptor
- Molecular Weight
- 40368.235 Da
References
- Fan LW, Tanaka S, Tien LT, Ma T, Rockhold RW, Ho IK: Withdrawal from dependence upon butorphanol uniquely increases kappa(1)-opioid receptor binding in the rat brain. Brain Res Bull. 2002 Jun;58(2):149-60. [PubMed:12127012]
- Fan LW, Tanaka S, Park Y, Sasaki K, Ma T, Tien LT, Rockhold RW, Ho IK: Butorphanol dependence and withdrawal decrease hippocampal kappa 2-opioid receptor binding. Brain Res. 2002 Dec 27;958(2):277-90. [PubMed:12470863]
- Commiskey S, Fan LW, Ho IK, Rockhold RW: Butorphanol: effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors. J Pharmacol Sci. 2005 Jun;98(2):109-16. Epub 2005 Jun 8. [PubMed:15942128]
- Picker MJ, Benyas S, Horwitz JA, Thompson K, Mathewson C, Smith MA: Discriminative stimulus effects of butorphanol: influence of training dose on the substitution patterns produced by Mu, Kappa and Delta opioid agonists. J Pharmacol Exp Ther. 1996 Dec;279(3):1130-41. [PubMed:8968334]
- Wakabayashi H, Tokuyama S, Ho IK: Simultaneous measurement of biogenic amines and their metabolites in rat brain regions after acute administration of and abrupt withdrawal from butorphanol or morphine. Neurochem Res. 1995 Oct;20(10):1179-85. [PubMed:8746803]
- Narita M, Feng Y, Makimura M, Hoskins B, Ho IK: Repeated administration of opioids alters characteristics of membrane-bound phorbol ester binding in rat brain. Eur J Pharmacol. 1994 Dec 27;271(2-3):547-50. [PubMed:7705457]
- Walsh SL, Chausmer AE, Strain EC, Bigelow GE: Evaluation of the mu and kappa opioid actions of butorphanol in humans through differential naltrexone blockade. Psychopharmacology (Berl). 2008 Jan;196(1):143-55. Epub 2007 Oct 2. [PubMed:17909753]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Partial antagonist
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
- Gene Name
- OPRM1
- Uniprot ID
- P35372
- Uniprot Name
- Mu-type opioid receptor
- Molecular Weight
- 44778.855 Da
References
- Vivian JA, DeYoung MB, Sumpter TL, Traynor JR, Lewis JW, Woods JH: kappa-Opioid receptor effects of butorphanol in rhesus monkeys. J Pharmacol Exp Ther. 1999 Jul;290(1):259-65. [PubMed:10381785]
- Fan LW, Tanaka S, Tien LT, Ma T, Rockhold RW, Ho IK: Withdrawal from dependence upon butorphanol uniquely increases kappa(1)-opioid receptor binding in the rat brain. Brain Res Bull. 2002 Jun;58(2):149-60. [PubMed:12127012]
- Fan LW, Tanaka S, Park Y, Sasaki K, Ma T, Tien LT, Rockhold RW, Ho IK: Butorphanol dependence and withdrawal decrease hippocampal kappa 2-opioid receptor binding. Brain Res. 2002 Dec 27;958(2):277-90. [PubMed:12470863]
- Commiskey S, Fan LW, Ho IK, Rockhold RW: Butorphanol: effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors. J Pharmacol Sci. 2005 Jun;98(2):109-16. Epub 2005 Jun 8. [PubMed:15942128]
- Picker MJ, Benyas S, Horwitz JA, Thompson K, Mathewson C, Smith MA: Discriminative stimulus effects of butorphanol: influence of training dose on the substitution patterns produced by Mu, Kappa and Delta opioid agonists. J Pharmacol Exp Ther. 1996 Dec;279(3):1130-41. [PubMed:8968334]
- Wakabayashi H, Tokuyama S, Ho IK: Simultaneous measurement of biogenic amines and their metabolites in rat brain regions after acute administration of and abrupt withdrawal from butorphanol or morphine. Neurochem Res. 1995 Oct;20(10):1179-85. [PubMed:8746803]
- Picker MJ: Discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine: cross-substitution by mu and delta opioid agonists. J Pharmacol Exp Ther. 1997 Dec;283(3):1009-17. [PubMed:9399970]
- Narita M, Feng Y, Makimura M, Hoskins B, Ho IK: Repeated administration of opioids alters characteristics of membrane-bound phorbol ester binding in rat brain. Eur J Pharmacol. 1994 Dec 27;271(2-3):547-50. [PubMed:7705457]
- Walsh SL, Chausmer AE, Strain EC, Bigelow GE: Evaluation of the mu and kappa opioid actions of butorphanol in humans through differential naltrexone blockade. Psychopharmacology (Berl). 2008 Jan;196(1):143-55. Epub 2007 Oct 2. [PubMed:17909753]
Drug created on June 13, 2005 07:24 / Updated on May 21, 2018 17:37