Identification

Name
Cyproheptadine
Accession Number
DB00434  (APRD00033)
Type
Small Molecule
Groups
Approved
Description

A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc. [PubChem]

Structure
Thumb
Synonyms
  • 1-methyl-4-(5-dibenzo(a,e)cycloheptatrienylidene)piperidine
  • 1-Methyl-4-(5H-dibenzo(a,d)cycloheptenylidene)piperidine
  • 4-(5-Dibenzo(a,D)cyclohepten-5-ylidine)-1-methylpiperidine
  • 4-(5H-Dibenzo(a,D)cyclohepten-5-ylidene)-1-methylpiperidine
  • 4-Dibenzo[a,D]cyclohepten-5-ylidene-1-methyl-piperidine
  • 5-(1-methylpiperidylidene-4)-5H-dibenzo(a,d)cyclopheptene
  • Axoprol
  • Ciproheptadina
  • Cyproheptadin
  • Cyproheptadine
  • Cyproheptadinum
  • Dihexazin
  • Glutodina
External IDs
Fl 5967 / HSp 1229
Product Ingredients
IngredientUNIICASInChI Key
Cyproheptadine Hydrochloride0S9323MCT0969-33-5ZPMVNZLARAEGHB-UHFFFAOYSA-N
Product Images
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CyproheptadineSyrup2 mg/5mLOralPharmaceutical Associates, Inc.2013-07-29Not applicableUs
CyproheptadineSyrup2 mg/5mLOralPharmaceutical Associates, Inc.2013-07-29Not applicableUs
Cyproheptadine HydrochlorideTablet4 mg/1OralAv Kare, Inc.2010-06-15Not applicableUs
Cyproheptadine HydrochlorideTablet4 mg/1OralDash Pharmaceuticals Llc2017-02-21Not applicableUs
Cyproheptadine HydrochlorideTablet4 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-01-08Not applicableUs
Cyproheptadine HydrochlorideTablet4 mg/1OralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Cyproheptadine HydrochlorideSyrup2 mg/5mLOralRising Pharmaceuticals2006-07-10Not applicableUs
Cyproheptadine HydrochlorideTablet4 mg/1OralCadila Pharnmaceuticals2017-07-20Not applicableUs
Cyproheptadine HydrochlorideTablet4 mg/1OralAppco Pharma Llc2016-12-142017-01-16Us
Cyproheptadine HydrochlorideTablet4 mg/1OralRemedy Repack2012-08-162016-10-13Us
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cyproheptadine 4mg TabletsTablet4 mgOralJamp Pharma Corporation2010-05-03Not applicableCanada
Euro-cyproheptadine 2mg/5mlSyrup2 mgOralSandoz Canada Incorporated2003-05-27Not applicableCanada
Euro-cyproheptadine 2mg/5mlSyrup2 mgOralEuro Pharm International Canada IncNot applicableNot applicableCanada
Euro-cyproheptadine 4 Mg/tabletTablet4 mgOralEuro Pharm International Canada IncNot applicableNot applicableCanada
Euro-cyproheptadine 4mg/tabletTablet4 mgOralSandoz Canada Incorporated2006-06-05Not applicableCanada
Jamp Cyproheptadine SyrupSyrup0.4 mgOralJamp Pharma CorporationNot applicableNot applicableCanada
Periactin Syr 2mg/5mlSyrup2 mgOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1961-12-312002-07-29Canada
Periactin Tab 4mgTablet4 mgOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1961-12-312002-07-29Canada
PMS-cyproheptadine HCl Tab 4mgTablet4 mgOralPharmascience Inc1996-10-16Not applicableCanada
International/Other Brands
Apeplus (Radicura) / Apitup (Universal) / Biohept (Biofarm) / Ciplactin (Cipla) / Cipractine (Teriak) / Ciproheptadina (Arena) / Ciprovit / Ciptadine (IBN) / Cyheptine (Greater Pharma) / Cyllermin (CCPC) / Periactin (Merck) / Periactine (Teofarma) / Periatin (Apex) / Reactin (Orion)
Categories
UNII
2YHB6175DO
CAS number
129-03-3
Weight
Average: 287.3981
Monoisotopic: 287.167399677
Chemical Formula
C21H21N
InChI Key
JJCFRYNCJDLXIK-UHFFFAOYSA-N
InChI
InChI=1S/C21H21N/c1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21/h2-11H,12-15H2,1H3
IUPAC Name
1-methyl-4-{tricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,9,11,13-heptaen-2-ylidene}piperidine
SMILES
CN1CCC(CC1)=C1C2=CC=CC=C2C=CC2=CC=CC=C12

Pharmacology

Indication

For treatment of perennial and seasonal allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis due to inhalant allergens and foods, mild uncomplicated allergic skin manifestations of urticaria and angioedema, amelioration of allergic reactions to blood or plasma, cold urticaria, dermatographism, and as therapy for anaphylactic reactions adjunctive to epinephrine.

Structured Indications
Pharmacodynamics

Cyproheptadine is a piperidine antihistamine. Unlike other antihistamines, this drug also antagonizes serotonin receptors. This action makes Cyproheptadine useful in conditions such as vascular headache and anorexia. Cyproheptadine does not prevent the release of histamine but rather competes with free histamine for binding at HA-receptor sites. Cyproheptadine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. Most antihistamines possess significant anticholinergic properties, but Cyproheptadine exerts only weak anticholinergic actions. Blockade of central muscarinic receptors appears to account for Cyproheptadine's antiemetic effects, although the exact mechanism is unknown. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite. Cyproheptadine also has been used to counter vascular headaches, which many believe are caused by changes in serotonin activity, however it is unclear how Cyproheptadine exerts a beneficial effect on this condition.

Mechanism of action

Cyproheptadine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite.

TargetActionsOrganism
AHistamine H1 receptor
antagonist
Human
A5-hydroxytryptamine receptor 2A
antagonist
Human
A5-hydroxytryptamine receptor 2C
antagonist
Human
UMuscarinic acetylcholine receptor M1
antagonist
Human
UMuscarinic acetylcholine receptor M2
antagonist
Human
UMuscarinic acetylcholine receptor M3
antagonist
Human
U5-hydroxytryptamine receptor 7Not AvailableHuman
Absorption

Well absorbed after oral administration.

Volume of distribution
Not Available
Protein binding

96 to 99%

Metabolism

Hepatic (cytochrome P-450 system) and some renal.

Route of elimination

After a single 4 mg oral dose of14C-labelled cyproheptadine HCl in normal subjects, given as tablets 2% to 20% of the radioactivity was excreted in the stools. At least 40% of the administered radioactivity was excreted in the urine.

Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Cyproheptadine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Cyproheptadine.Experimental, Illicit
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Cyproheptadine.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Cyproheptadine.Experimental, Illicit
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Cyproheptadine.Experimental
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the anticholinergic activities of Cyproheptadine.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Cyproheptadine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Cyproheptadine.Approved
AdipiplonThe risk or severity of adverse effects can be increased when Adipiplon is combined with Cyproheptadine.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Cyproheptadine.Approved, Investigational
AlaproclateThe therapeutic efficacy of Alaproclate can be decreased when used in combination with Cyproheptadine.Experimental
AlfaxaloneThe risk or severity of adverse effects can be increased when Alfaxalone is combined with Cyproheptadine.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Cyproheptadine.Approved, Illicit
AllopregnanoloneThe risk or severity of adverse effects can be increased when Allopregnanolone is combined with Cyproheptadine.Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Cyproheptadine.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Alphaprodine is combined with Cyproheptadine.Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Cyproheptadine.Approved, Illicit, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Amisulpride is combined with Cyproheptadine.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Cyproheptadine.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Cyproheptadine.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Amperozide is combined with Cyproheptadine.Experimental
AmphetamineAmphetamine may increase the anticholinergic activities of Cyproheptadine.Approved, Illicit
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Cyproheptadine.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Articaine is combined with Cyproheptadine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Cyproheptadine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Azaperone is combined with Cyproheptadine.Investigational, Vet Approved
AzelastineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Cyproheptadine.Approved
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Cyproheptadine.Illicit
BenmoxinBenmoxin may increase the anticholinergic activities of Cyproheptadine.Withdrawn
BenperidolThe risk or severity of adverse effects can be increased when Benperidol is combined with Cyproheptadine.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Cyproheptadine.Approved
BenzphetamineBenzphetamine may decrease the sedative activities of Cyproheptadine.Approved, Illicit
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Cyproheptadine.Approved
Benzylpenicilloyl PolylysineCyproheptadine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Cyproheptadine.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Brexpiprazole.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved
BrofaromineBrofaromine may increase the anticholinergic activities of Cyproheptadine.Experimental
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Cyproheptadine.Approved, Illicit
BromisovalThe risk or severity of adverse effects can be increased when Bromisoval is combined with Cyproheptadine.Experimental
BromperidolThe risk or severity of adverse effects can be increased when Bromperidol is combined with Cyproheptadine.Investigational
BrompheniramineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Brotizolam is combined with Cyproheptadine.Approved, Investigational, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Cyproheptadine.Approved, Investigational
BuprenorphineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Cyproheptadine.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Cyproheptadine.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Butacaine is combined with Cyproheptadine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Butalbital is combined with Cyproheptadine.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Butamben is combined with Cyproheptadine.Approved
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Cyproheptadine.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Cyproheptadine.Approved, Illicit, Vet Approved
CanertinibThe risk or severity of adverse effects can be increased when Canertinib is combined with Cyproheptadine.Investigational
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Cyproheptadine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Cyproheptadine.Illicit, Investigational, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Carisoprodol is combined with Cyproheptadine.Approved
CaroxazoneCaroxazone may increase the anticholinergic activities of Cyproheptadine.Withdrawn
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Cyproheptadine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Cyproheptadine.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Cyproheptadine.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Cyproheptadine.Approved, Investigational, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Cyproheptadine.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Chlorphenamine.Approved
ChlorphentermineChlorphentermine may decrease the sedative activities of Cyproheptadine.Illicit, Withdrawn
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Cyproheptadine.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Cyproheptadine.Approved, Investigational, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Cyproheptadine.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Cyproheptadine.Approved, Vet Approved
CitalopramThe therapeutic efficacy of Citalopram can be decreased when used in combination with Cyproheptadine.Approved
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with Cyproheptadine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Clobazam is combined with Cyproheptadine.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when clomethiazole is combined with Cyproheptadine.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Clomipramine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Clonazepam.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Clonidine.Approved
ClopenthixolThe risk or severity of adverse effects can be increased when Clopenthixol is combined with Cyproheptadine.Experimental
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Cyproheptadine.Approved, Illicit
ClothiapineThe risk or severity of adverse effects can be increased when Clothiapine is combined with Cyproheptadine.Experimental
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Cyproheptadine.Approved
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Cyproheptadine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Cyproheptadine.Approved, Illicit
CyclizineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Cyproheptadine.Approved
DantroleneThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Dantrolene.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Cyproheptadine.Approved
DapoxetineThe therapeutic efficacy of Dapoxetine can be decreased when used in combination with Cyproheptadine.Investigational
DeramciclaneThe risk or severity of adverse effects can be increased when Deramciclane is combined with Cyproheptadine.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Cyproheptadine.Approved
DesipramineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Desipramine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe therapeutic efficacy of Desvenlafaxine can be decreased when used in combination with Cyproheptadine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Detomidine is combined with Cyproheptadine.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Cyproheptadine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Cyproheptadine.Approved, Vet Approved
DextroamphetamineDextroamphetamine may decrease the sedative activities of Cyproheptadine.Approved, Illicit
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Cyproheptadine.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Cyproheptadine.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Cyproheptadine.Approved, Investigational
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Cyproheptadine.Approved, Illicit, Vet Approved
Diethyl etherThe risk or severity of adverse effects can be increased when Diethyl ether is combined with Cyproheptadine.Experimental
DiethylpropionDiethylpropion may decrease the sedative activities of Cyproheptadine.Approved, Illicit
DifenoxinThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Cyproheptadine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Cyproheptadine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Cyproheptadine.Experimental, Illicit
DimenhydrinateThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Dimenhydrinate.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Cyproheptadine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Cyproheptadine.Approved, Illicit
DixyrazineThe risk or severity of adverse effects can be increased when Dixyrazine is combined with Cyproheptadine.Experimental
DoramectinThe risk or severity of adverse effects can be increased when Doramectin is combined with Cyproheptadine.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Doxepin.Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Cyproheptadine.Experimental
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved, Illicit
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Cyproheptadine.Experimental, Illicit
DuloxetineThe therapeutic efficacy of Duloxetine can be decreased when used in combination with Cyproheptadine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Cyproheptadine.Approved
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Cyproheptadine.Experimental, Illicit
EcopipamThe risk or severity of adverse effects can be increased when Ecopipam is combined with Cyproheptadine.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Efavirenz.Approved, Investigational
EltanoloneThe risk or severity of adverse effects can be increased when Eltanolone is combined with Cyproheptadine.Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Cyproheptadine.Approved, Investigational, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Entacapone.Approved, Investigational
EscitalopramThe therapeutic efficacy of Escitalopram can be decreased when used in combination with Cyproheptadine.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Cyproheptadine.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Cyproheptadine.Approved
EthanolCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Cyproheptadine.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Cyproheptadine.Withdrawn
Ethyl chlorideThe risk or severity of adverse effects can be increased when Ethyl chloride is combined with Cyproheptadine.Experimental, Investigational
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Cyproheptadine.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Cyproheptadine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Etidocaine is combined with Cyproheptadine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Etifoxine is combined with Cyproheptadine.Investigational, Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Etizolam is combined with Cyproheptadine.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Cyproheptadine.Approved
EtoperidoneThe therapeutic efficacy of Etoperidone can be decreased when used in combination with Cyproheptadine.Withdrawn
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Cyproheptadine.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Ezogabine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Felbamate.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Cyproheptadine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Cyproheptadine.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Fexofenadine.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Flibanserin.Approved
FluanisoneThe risk or severity of adverse effects can be increased when Fluanisone is combined with Cyproheptadine.Experimental
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Cyproheptadine.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Cyproheptadine.Approved, Illicit
FluoxetineThe therapeutic efficacy of Fluoxetine can be decreased when used in combination with Cyproheptadine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Cyproheptadine.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Cyproheptadine.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Cyproheptadine.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Cyproheptadine.Approved, Investigational
Fluticasone propionateThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Fluticasone propionate.Approved
FluvoxamineThe therapeutic efficacy of Fluvoxamine can be decreased when used in combination with Cyproheptadine.Approved, Investigational
FosphenytoinThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Fosphenytoin.Approved
FospropofolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Cyproheptadine.Approved, Illicit, Investigational
FurazolidoneFurazolidone may increase the anticholinergic activities of Cyproheptadine.Approved, Investigational, Vet Approved
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Cyproheptadine.Approved, Investigational
Gabapentin EnacarbilThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Gabapentin Enacarbil.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Cyproheptadine.Approved, Illicit, Investigational
GepefrineGepefrine may decrease the sedative activities of Cyproheptadine.Experimental
GepironeThe risk or severity of adverse effects can be increased when Gepirone is combined with Cyproheptadine.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Cyproheptadine.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Guanfacine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Cyproheptadine.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Cyproheptadine.Approved
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Cyproheptadine.Approved, Vet Approved
HarmalineHarmaline may increase the anticholinergic activities of Cyproheptadine.Experimental
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Cyproheptadine.Approved, Illicit, Investigational
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Cyproheptadine.Approved
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Cyproheptadine.Approved, Investigational
HydracarbazineHydracarbazine may increase the anticholinergic activities of Cyproheptadine.Experimental
HydrocodoneCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Cyproheptadine.Approved, Illicit
HydroxyamphetamineHydroxyamphetamine may decrease the sedative activities of Cyproheptadine.Approved
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Iloperidone.Approved
ImipramineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Imipramine.Approved
IndalpineThe therapeutic efficacy of Indalpine can be decreased when used in combination with Cyproheptadine.Investigational, Withdrawn
IndiplonThe risk or severity of adverse effects can be increased when Indiplon is combined with Cyproheptadine.Investigational
Iofetamine I-123Iofetamine I-123 may decrease the sedative activities of Cyproheptadine.Approved
IproclozideIproclozide may increase the anticholinergic activities of Cyproheptadine.Withdrawn
IproniazidIproniazid may increase the anticholinergic activities of Cyproheptadine.Withdrawn
IsocarboxazidIsocarboxazid may increase the anticholinergic activities of Cyproheptadine.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Cyproheptadine.Approved, Vet Approved
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Cyproheptadine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Cyproheptadine.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Cyproheptadine.Approved, Investigational
LamotrigineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Lamotrigine.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Cyproheptadine.Approved, Investigational
LevocabastineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Cyproheptadine.Approved, Investigational
LevomilnacipranThe therapeutic efficacy of Levomilnacipran can be decreased when used in combination with Cyproheptadine.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Cyproheptadine.Approved
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Cyproheptadine.Approved, Vet Approved
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Cyproheptadine.Approved, Investigational
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Cyproheptadine.Approved
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Cyproheptadine.Illicit
LoprazolamThe risk or severity of adverse effects can be increased when Loprazolam is combined with Cyproheptadine.Experimental
LoratadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Loratadine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Cyproheptadine.Approved
LormetazepamThe risk or severity of adverse effects can be increased when Lormetazepam is combined with Cyproheptadine.Approved
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Cyproheptadine.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Cyproheptadine.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Maprotiline.Approved
MebanazineMebanazine may increase the anticholinergic activities of Cyproheptadine.Withdrawn
MebicarThe risk or severity of adverse effects can be increased when Mebicar is combined with Cyproheptadine.Experimental
MeclizineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Meclizine.Approved
MedazepamThe risk or severity of adverse effects can be increased when Medazepam is combined with Cyproheptadine.Experimental
MedetomidineThe risk or severity of adverse effects can be increased when Medetomidine is combined with Cyproheptadine.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Cyproheptadine.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Melperone is combined with Cyproheptadine.Approved, Investigational
MephedroneMephedrone may decrease the sedative activities of Cyproheptadine.Investigational
MephentermineMephentermine may decrease the sedative activities of Cyproheptadine.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Cyproheptadine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Cyproheptadine.Approved, Illicit
MeptazinolThe risk or severity of adverse effects can be increased when Meptazinol is combined with Cyproheptadine.Experimental
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Cyproheptadine.Approved, Investigational
MetaxaloneThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Metaxalone.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Cyproheptadine.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Cyproheptadine.Approved, Illicit
MethamphetamineMethamphetamine may decrease the sedative activities of Cyproheptadine.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Cyproheptadine.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Cyproheptadine.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Methocarbamol is combined with Cyproheptadine.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Cyproheptadine.Approved
MethotrimeprazineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Cyproheptadine.Approved, Investigational, Vet Approved
MethoxyphenamineMethoxyphenamine may decrease the sedative activities of Cyproheptadine.Experimental
MethsuximideThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Methsuximide.Approved
MethylecgonineThe risk or severity of adverse effects can be increased when Methylecgonine is combined with Cyproheptadine.Experimental
Methylene blueMethylene blue may increase the anticholinergic activities of Cyproheptadine.Approved, Investigational
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Cyproheptadine.Approved
MetyrosineCyproheptadine may increase the sedative activities of Metyrosine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Cyproheptadine.Approved, Illicit
MidomafetamineMidomafetamine may decrease the sedative activities of Cyproheptadine.Experimental, Illicit, Investigational
MilnacipranThe therapeutic efficacy of Milnacipran can be decreased when used in combination with Cyproheptadine.Approved
MinaprineMinaprine may increase the anticholinergic activities of Cyproheptadine.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved, Investigational
MirtazapineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MMDAMMDA may decrease the sedative activities of Cyproheptadine.Experimental, Illicit
MoclobemideMoclobemide may increase the anticholinergic activities of Cyproheptadine.Approved
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Cyproheptadine.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Cyproheptadine.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Cyproheptadine.Approved
NefazodoneThe therapeutic efficacy of Nefazodone can be decreased when used in combination with Cyproheptadine.Approved, Withdrawn
NialamideNialamide may increase the anticholinergic activities of Cyproheptadine.Withdrawn
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Cyproheptadine.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Cyproheptadine.Approved, Vet Approved
NorfluraneThe risk or severity of adverse effects can be increased when Norflurane is combined with Cyproheptadine.Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Cyproheptadine.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Nortriptyline.Approved
OctamoxinOctamoxin may increase the anticholinergic activities of Cyproheptadine.Withdrawn
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Cyproheptadine.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Olopatadine.Approved
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Cyproheptadine.Approved
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Cyproheptadine.Approved, Illicit
OrphenadrineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Cyproheptadine.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Cyproheptadine.Approved
OxethazaineThe risk or severity of adverse effects can be increased when Oxethazaine is combined with Cyproheptadine.Approved, Investigational
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Cyproheptadine.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Cyproheptadine.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Cyproheptadine.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Cyproheptadine.Approved, Investigational, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Cyproheptadine.Approved
ParaldehydeCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved, Investigational
PargylinePargyline may increase the anticholinergic activities of Cyproheptadine.Approved
ParoxetineThe therapeutic efficacy of Paroxetine can be decreased when used in combination with Cyproheptadine.Approved, Investigational
PenfluridolThe risk or severity of adverse effects can be increased when Penfluridol is combined with Cyproheptadine.Experimental
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Cyproheptadine.Approved, Vet Approved
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Cyproheptadine.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved
PerazineThe risk or severity of adverse effects can be increased when Perazine is combined with Cyproheptadine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Perospirone is combined with Cyproheptadine.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Cyproheptadine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Cyproheptadine.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Phenazocine is combined with Cyproheptadine.Experimental
PhenelzinePhenelzine may increase the anticholinergic activities of Cyproheptadine.Approved
PhenibutThe risk or severity of adverse effects can be increased when Phenibut is combined with Cyproheptadine.Experimental
PheniprazinePheniprazine may increase the anticholinergic activities of Cyproheptadine.Withdrawn
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Cyproheptadine.Approved
PhenoperidineThe risk or severity of adverse effects can be increased when Phenoperidine is combined with Cyproheptadine.Experimental
PhenoxyethanolThe risk or severity of adverse effects can be increased when Phenoxyethanol is combined with Cyproheptadine.Approved
PhenoxypropazinePhenoxypropazine may increase the anticholinergic activities of Cyproheptadine.Withdrawn
PhenterminePhentermine may decrease the sedative activities of Cyproheptadine.Approved, Illicit
PhenytoinThe risk or severity of adverse effects can be increased when Phenytoin is combined with Cyproheptadine.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Cyproheptadine.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with Cyproheptadine.Approved, Investigational
PipotiazineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Pipotiazine.Approved, Investigational
PiritramideThe risk or severity of adverse effects can be increased when Piritramide is combined with Cyproheptadine.Investigational
PirlindolePirlindole may increase the anticholinergic activities of Cyproheptadine.Approved
PivhydrazinePivhydrazine may increase the anticholinergic activities of Cyproheptadine.Withdrawn
PizotifenThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Pomalidomide.Approved
PramipexoleCyproheptadine may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Pramocaine is combined with Cyproheptadine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Cyproheptadine.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Cyproheptadine.Approved, Illicit, Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Cyproheptadine.Approved
PrimidoneThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Primidone.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Cyproheptadine.Approved, Investigational, Vet Approved
ProcarbazineProcarbazine may increase the anticholinergic activities of Cyproheptadine.Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Cyproheptadine.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Cyproheptadine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Promethazine.Approved
PropanididThe risk or severity of adverse effects can be increased when Propanidid is combined with Cyproheptadine.Experimental
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Cyproheptadine.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Cyproheptadine.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Propoxycaine is combined with Cyproheptadine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Cyproheptadine.Approved
ProxibarbalThe risk or severity of adverse effects can be increased when Proxibarbal is combined with Cyproheptadine.Experimental
PSD502The risk or severity of adverse effects can be increased when PSD502 is combined with Cyproheptadine.Investigational
PseudoephedrinePseudoephedrine may decrease the sedative activities of Cyproheptadine.Approved
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Cyproheptadine.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Cyproheptadine.Approved
QuinisocaineThe risk or severity of adverse effects can be increased when Quinisocaine is combined with Cyproheptadine.Experimental
RacloprideThe risk or severity of adverse effects can be increased when Raclopride is combined with Cyproheptadine.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Ramelteon.Approved, Investigational
RasagilineRasagiline may increase the anticholinergic activities of Cyproheptadine.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Cyproheptadine.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Cyproheptadine.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Cyproheptadine.Approved, Investigational
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Cyproheptadine.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Ritanserin is combined with Cyproheptadine.Investigational
RitobegronRitobegron may decrease the sedative activities of Cyproheptadine.Investigational
RomifidineThe risk or severity of adverse effects can be increased when Romifidine is combined with Cyproheptadine.Vet Approved
RopiniroleCyproheptadine may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Cyproheptadine.Approved
RotigotineCyproheptadine may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Cyproheptadine.Approved
SafrazineSafrazine may increase the anticholinergic activities of Cyproheptadine.Withdrawn
ScopolamineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Scopolamine.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Cyproheptadine.Approved, Vet Approved
SelegilineSelegiline may increase the anticholinergic activities of Cyproheptadine.Approved, Investigational, Vet Approved
SepranoloneThe risk or severity of adverse effects can be increased when Sepranolone is combined with Cyproheptadine.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Cyproheptadine.Approved, Investigational, Withdrawn
SertralineThe therapeutic efficacy of Sertraline can be decreased when used in combination with Cyproheptadine.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Cyproheptadine.Approved, Vet Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved
StiripentolThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Cyproheptadine.Approved, Investigational
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Cyproheptadine.Approved, Investigational
SultoprideThe risk or severity of adverse effects can be increased when Sultopride is combined with Cyproheptadine.Experimental
SuvorexantCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Tandospirone is combined with Cyproheptadine.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Tasimelteon.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Cyproheptadine.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Tetrabenazine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Tetracaine is combined with Cyproheptadine.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Tetrahydropalmatine is combined with Cyproheptadine.Investigational
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Cyproheptadine.Investigational
ThalidomideCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Cyproheptadine.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Cyproheptadine.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Cyproheptadine.Approved, Withdrawn
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Cyproheptadine.Approved
TiagabineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Tiagabine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Tiapride is combined with Cyproheptadine.Approved, Investigational
TiletamineThe risk or severity of adverse effects can be increased when Tiletamine is combined with Cyproheptadine.Vet Approved
TilidineThe risk or severity of adverse effects can be increased when Tilidine is combined with Cyproheptadine.Experimental
TizanidineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Tizanidine.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Tolcapone is combined with Cyproheptadine.Approved, Withdrawn
ToloxatoneToloxatone may increase the anticholinergic activities of Cyproheptadine.Approved
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with Cyproheptadine.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Cyproheptadine.Approved, Investigational
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the anticholinergic activities of Cyproheptadine.Experimental
TranylcypromineTranylcypromine may increase the anticholinergic activities of Cyproheptadine.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Cyproheptadine.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Cyproheptadine.Approved
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Tricaine methanesulfonate is combined with Cyproheptadine.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Trichloroethylene is combined with Cyproheptadine.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Cyproheptadine.Approved
TrifluperidolThe risk or severity of adverse effects can be increased when Trifluperidol is combined with Cyproheptadine.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Cyproheptadine.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Triprolidine is combined with Cyproheptadine.Approved
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Cyproheptadine.Approved, Investigational
VenlafaxineThe therapeutic efficacy of Venlafaxine can be decreased when used in combination with Cyproheptadine.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Veralipride is combined with Cyproheptadine.Experimental
VigabatrinThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Vigabatrin.Approved
Vinyl etherThe risk or severity of adverse effects can be increased when Vinyl ether is combined with Cyproheptadine.Experimental
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Cyproheptadine.Approved
XenonThe risk or severity of adverse effects can be increased when Xenon is combined with Cyproheptadine.Experimental
XylazineThe risk or severity of adverse effects can be increased when Xylazine is combined with Cyproheptadine.Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Cyproheptadine.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Ziconotide.Approved
ZimelidineThe therapeutic efficacy of Zimelidine can be decreased when used in combination with Cyproheptadine.Withdrawn
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Cyproheptadine.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Zolazepam is combined with Cyproheptadine.Vet Approved
ZolpidemCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Cyproheptadine.Approved
ZotepineThe risk or severity of adverse effects can be increased when Zotepine is combined with Cyproheptadine.Approved, Investigational
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Cyproheptadine.Approved, Investigational
Food Interactions
  • Avoid alcohol.
  • Take with food.

References

Synthesis Reference

Engelhardt, E.L.; U S . Patent 3,014,911; December 26, 1961; assigned to Merck & Co., Inc.

General References
  1. Tokunaga S, Takeda Y, Shinomiya K, Hirase M, Kamei C: Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats. J Pharmacol Sci. 2007 Feb;103(2):201-6. Epub 2007 Feb 8. [PubMed:17287588]
External Links
Human Metabolome Database
HMDB14578
KEGG Compound
C06935
PubChem Compound
2913
PubChem Substance
46508613
ChemSpider
2810
BindingDB
50017721
ChEBI
4046
ChEMBL
CHEMBL516
Therapeutic Targets Database
DAP000103
PharmGKB
PA164749366
IUPHAR
277
Guide to Pharmacology
GtP Drug Page
HET
C7H
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cyproheptadine
ATC Codes
R06AX02 — Cyproheptadine
AHFS Codes
  • 04:04.92 — Miscellaneous Derivatives
PDB Entries
5ayf
MSDS
Download (74.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedBasic ScienceStrokes1
2CompletedSupportive CareCachexia / Leukemias / Malignant Lymphomas / Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Diseases / Neoplasms, Brain / Tumors, Central Nervous System / Unspecified Childhood Solid Tumor, Protocol Specific1
2CompletedTreatmentAlcoholism1
2TerminatedSupportive CareLeukemias / Malignant Lymphomas / Malnutrition / Myelodysplastic Syndromes / Unspecified Childhood Solid Tumor, Protocol Specific / Weight Changes1
2Unknown StatusTreatmentFunctional Abdominal Pain1
3TerminatedSupportive CareCancers1
4CompletedTreatmentAdhd / Attention Deficit and Disruptive Behavior Disorders / Attention Deficit Disorder With Hyperactivity / Attention Deficit Hyperactivity Disorder (ADHD) / Mental Disorders Diagnosed in Childhood1
4Not Yet RecruitingTreatmentFeeding Behaviors1
4Unknown StatusTreatmentFailure to Thrive1
Not AvailableCompletedBasic ScienceSpinal Cord Injuries (SCI)1
Not AvailableRecruitingTreatmentHemiparesis / Muscle Spasticity / Strokes1

Pharmacoeconomics

Manufacturers
  • Merck and co inc
Packagers
Dosage forms
FormRouteStrength
SolutionOral2 mg/5mL
SyrupOral2 mg/5mL
TabletOral4 mg/1
SyrupOral0.4 mg
SyrupOral2 mg
TabletOral4 mg
Prices
Unit descriptionCostUnit
Cyproheptadine hcl powder7.34USD g
Cyproheptadine HCl 4 mg tablet0.47USD tablet
Cyproheptadine 4 mg tablet0.43USD tablet
Cyproheptadine HCl 2 mg/5ml Syrup0.16USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)112.3-113-3Engelhardt, E.L.; U S . Patent 3,014,911; December 26, 1961; assigned to Merck & Co., Inc.
water solubilitySolubleNot Available
logP4.69SANGSTER (1993)
Predicted Properties
PropertyValueSource
Water Solubility0.0136 mg/mLALOGPS
logP5.02ALOGPS
logP4.38ChemAxon
logS-4.3ALOGPS
pKa (Strongest Basic)8.05ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area3.24 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity105.17 m3·mol-1ChemAxon
Polarizability34.17 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.986
Caco-2 permeable+0.8038
P-glycoprotein substrateSubstrate0.8598
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IINon-inhibitor0.5315
Renal organic cation transporterInhibitor0.8303
CYP450 2C9 substrateNon-substrate0.8127
CYP450 2D6 substrateNon-substrate0.6719
CYP450 3A4 substrateSubstrate0.6092
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9082
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.902
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5433
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.9511
BiodegradationNot ready biodegradable0.8349
Rat acute toxicity2.9576 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5429
hERG inhibition (predictor II)Inhibitor0.7423
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (10 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-00kr-2290000000-a17c27a9f171b058f2c3
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-0290000000-964629904e89d79568d8

Taxonomy

Description
This compound belongs to the class of organic compounds known as dibenzocycloheptenes. These are compounds containing a dibenzocycloheptene moiety, which consists of two benzene rings connected by a cycloheptene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Dibenzocycloheptenes
Sub Class
Not Available
Direct Parent
Dibenzocycloheptenes
Alternative Parents
Piperidines / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Dibenzocycloheptene / Piperidine / Tertiary aliphatic amine / Tertiary amine / Azacycle / Organoheterocyclic compound / Organic nitrogen compound / Organopnictogen compound / Hydrocarbon derivative / Organonitrogen compound
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
piperidines, tertiary amine (CHEBI:4046)

Targets

Details
1. Histamine H1 receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. 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
Antagonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Rashid M, Nakazawa M, Nagatomo T: Effects of sarpogrelate, a novel 5-HT2 antagonist, on 5-HT-induced endothelium-dependent relaxations in porcine coronary artery. Jpn J Pharmacol. 2002 Aug;89(4):405-12. [PubMed:12233819]
  2. Honda M, Nishida T, Ono H: Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol. 2003 Jan 1;458(1-2):91-9. [PubMed:12498911]
  3. Callaway CW, Rempel N, Peng RY, Geyer MA: Serotonin 5-HT1-like receptors mediate hyperactivity in rats induced by 3,4-methylenedioxymethamphetamine. Neuropsychopharmacology. 1992 Sep;7(2):113-27. [PubMed:1358088]
  4. Hoenicke EM, Vanecek SA, Woods JH: The discriminative stimulus effects of clozapine in pigeons: involvement of 5-hydroxytryptamine1C and 5-hydroxytryptamine2 receptors. J Pharmacol Exp Ther. 1992 Oct;263(1):276-84. [PubMed:1403790]
  5. Calka O, Metin A, Dulger H, Erkoc R: Effect of cyproheptadine on serum leptin levels. Adv Ther. 2005 Sep-Oct;22(5):424-8. [PubMed:16418149]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Honda M, Nishida T, Ono H: Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol. 2003 Jan 1;458(1-2):91-9. [PubMed:12498911]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. Eltze M, Lambrecht G, Mutschler E: Cyproheptadine displays high affinity for muscarinic receptors but does not discriminate between receptor subtypes. Eur J Pharmacol. 1989 Dec 7;173(2-3):219-22. [PubMed:2625138]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. Eltze M, Lambrecht G, Mutschler E: Cyproheptadine displays high affinity for muscarinic receptors but does not discriminate between receptor subtypes. Eur J Pharmacol. 1989 Dec 7;173(2-3):219-22. [PubMed:2625138]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. Eltze M, Lambrecht G, Mutschler E: Cyproheptadine displays high affinity for muscarinic receptors but does not discriminate between receptor subtypes. Eur J Pharmacol. 1989 Dec 7;173(2-3):219-22. [PubMed:2625138]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. Teitler M, Toohey N, Knight JA, Klein MT, Smith C: Clozapine and other competitive antagonists reactivate risperidone-inactivated h5-HT7 receptors: radioligand binding and functional evidence for GPCR homodimer protomer interactions. Psychopharmacology (Berl). 2010 Dec;212(4):687-97. doi: 10.1007/s00213-010-2001-x. Epub 2010 Sep 9. [PubMed:20827463]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A3
Uniprot ID
P35503
Uniprot Name
UDP-glucuronosyltransferase 1-3
Molecular Weight
60337.835 Da
References
  1. Green MD, King CD, Mojarrabi B, Mackenzie PI, Tephly TR: Glucuronidation of amines and other xenobiotics catalyzed by expressed human UDP-glucuronosyltransferase 1A3. Drug Metab Dispos. 1998 Jun;26(6):507-12. [PubMed:9616184]

Drug created on June 13, 2005 07:24 / Updated on December 10, 2017 17:18