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Identification
NamePethidine
Accession NumberDB00454  (APRD00074)
TypeSmall Molecule
GroupsApproved
Description

A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration. [PubChem]

Structure
Thumb
Synonyms
Isonipecaïne
Meperidine
Pethidin
Péthidine
Pethidine dbl
Pethidinum
Petidina
Petydyna
Sauteralgyl
Spasmedal
Spasmodolin
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Demerolinjection, solution50 mg/mLintramuscular; intravenous; subcutaneousPhysicians Total Care, Inc.2007-08-212016-04-05Us
Demerolinjection, solution25 mg/.5mLintramuscular; intravenous; subcutaneousHospira, Inc.1942-11-102016-04-23Us
Demeroltablet50 mg/1oralSanofi Aventis U.S. Llc1942-11-102016-04-23Us
Demeroltablet50 mg/1oralbryant ranch prepack2013-04-012016-04-05Us
Demerolinjection, solution100 mg/mLintramuscular; intravenous; subcutaneousPhysicians Total Care, Inc.2003-03-112016-04-05Us
Demerolinjection, solution100 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1942-11-102016-04-23Us
Demerolinjection, solution50 mg/mLintramuscular; intravenous; subcutaneousPhysicians Total Care, Inc.1994-04-112016-04-05Us
Demerolinjection, solution50 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1942-11-102016-04-23Us
Demerolinjection, solution100 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1942-11-102016-04-23Us
Demerolinjection, solution100 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1942-11-102016-04-23Us
Demerolinjection, solution75 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1942-11-102016-04-23Us
Demerolinjection, solution100 mg/2mLintramuscular; intravenous; subcutaneousHospira, Inc.1942-11-102016-04-23Us
Demerolinjection, solution50 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1942-11-102016-04-23Us
Demerolinjection, solution75 mg/1.5mLintramuscular; intravenous; subcutaneousHospira, Inc.1942-11-102016-04-23Us
Demerolinjection, solution25 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1942-11-102016-04-23Us
Demerolinjection, solution50 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.1942-11-102016-04-23Us
Demeroltablet100 mg/1oralSanofi Aventis U.S. Llc1942-11-102016-04-23Us
Demeroltablet50 mgoralSanofi Aventis Canada Inc1944-12-31Not applicableCanada
Demerol 50mg - Liq Im IV Sc 50mg/mlliquid50 mgintramuscular; intravenous; subcutaneousSanofi Canada, Inc.1944-12-312001-08-10Canada
Demerol 50mg - Liq Im Sc 50mg/mlliquid50 mgintramuscular; subcutaneousSanofi Canada, Inc.1944-12-312001-08-10Canada
Demerol 10%-liq Im IV Scliquid100 mgintramuscular; intravenous; subcutaneousSanofi Canada, Inc.1944-12-312001-08-10Canada
Demerol 10%-liq Im Sc 100mg/mlliquid100 mgintramuscular; subcutaneousSanofi Canada, Inc.1944-12-312001-08-17Canada
Demerol 100 mg/mlsolution100 mgintramuscular; subcutaneousHospira Healthcare Corporation2000-05-01Not applicableCanada
Demerol 100 mg/mlsolution100 mgintramuscular; intravenous; subcutaneousHospira Healthcare Corporation2000-08-15Not applicableCanada
Demerol 50 mg/ml (multiple Dose With Metacresol As Preservative)solution50 mgintramuscular; subcutaneousHospira Healthcare Corporation2000-12-012012-08-03Canada
Demerol 50 mg/ml (single Use, Preservative Free)solution50 mgintramuscular; intravenous; subcutaneousHospira Healthcare Corporation2000-12-01Not applicableCanada
Demerol 75 mg/mlsolution75 mgintramuscular; intravenous; subcutaneousHospira Healthcare Corporation2000-12-01Not applicableCanada
Demerol 75mg - Liq Im IV Sc 75mg/mlliquid75 mgintramuscular; intravenous; subcutaneousSanofi Canada, Inc.1969-12-312001-08-10Canada
Meperidine HClinjection, solution10 mg/mLintravenousCantrell Drug Company2012-01-232016-04-05Us
Meperidine HCl Injection 100mg/mlsolution100 mgintramuscular; intravenous; subcutaneousHospira Healthcare Corporation1981-12-312012-08-03Canada
Meperidine HCl Injection 10mg/mlsolution10 mgintramuscular; intravenous; subcutaneousHospira Healthcare Corporation1981-12-312012-08-03Canada
Meperidine HCl Injection 25mg/mlsolution25 mgintramuscular; intravenous; subcutaneousHospira Healthcare Corporation1981-12-312012-08-03Canada
Meperidine HCl Injection 50mg/mlsolution50 mgintramuscular; intravenous; subcutaneousHospira Healthcare Corporation1981-12-312012-08-03Canada
Meperidine HCl Injection 75mg/mlsolution75 mgintramuscular; intravenous; subcutaneousHospira Healthcare Corporation1981-12-312012-08-03Canada
Meperidine Hydrochloride Injection 10mg/ml USPsolution10 mgintravenousHospira Healthcare Corporation1986-12-31Not applicableCanada
Meperidine Hydrochloride Injection USPsolution50 mgintramuscular; intravenous; subcutaneousSandoz Canada Incorporated1987-12-31Not applicableCanada
Meperidine Hydrochloride Injection USPsolution75 mgintramuscular; intravenous; subcutaneousSandoz Canada Incorporated1987-12-31Not applicableCanada
Meperidine Hydrochloride Injection USPsolution100 mgintramuscular; intravenous; subcutaneousSandoz Canada Incorporated1988-12-31Not applicableCanada
Pethidine Injection B.P.solution10 mgintravenousHospira Healthcare Corporation1998-09-242012-08-03Canada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Meperidine Hydrochloridetablet75 mg/1oralMikart, Inc.2009-06-242016-04-05Us
Meperidine Hydrochloridetablet50 mg/1oralQualitest Pharmaceuticals1998-12-172016-04-23Us
Meperidine Hydrochloridesolution50 mg/5mLoralRoxane Laboratories, Inc1985-01-302016-04-23Us
Meperidine Hydrochloridetablet100 mg/1oralMikart, Inc.2009-06-242016-04-05Us
Meperidine Hydrochloridetablet50 mg/1oralMikart, Inc.2009-06-242016-04-05Us
Meperidine Hydrochloridetablet100 mg/1oralBarr Laboratories Inc.2015-02-242016-04-23Us
Meperidine Hydrochloridetablet100 mg/1oralEpic Pharma, LLC2011-05-052016-04-05Us
Meperidine Hydrochloridetablet100 mg/1oralBarr Laboratories Inc.1996-10-112016-07-31Us
Meperidine Hydrochloridetablet50 mg/1oralbryant ranch prepack1998-12-172016-04-05Us
Meperidine Hydrochloridetablet50 mg/1oralEpic Pharma, LLC2011-05-052016-04-05Us
Meperidine Hydrochloridetablet50 mg/1oralBarr Laboratories Inc.1997-02-032016-04-23Us
Meperidine Hydrochloridetablet100 mg/1oralCaraco Pharmaceutical Laboratories, Ltd.2007-01-042016-04-05Us
Meperidine Hydrochlorideinjection100 mg/mLintramuscular; intravenous; subcutaneousWest Ward Pharmaceutical Corp.1975-01-222016-04-23Us
Meperidine Hydrochlorideinjection, solution10 mg/mLintravenousHospira, Inc.1984-08-162016-04-23Us
Meperidine Hydrochloridetablet50 mg/1oralCaraco Pharmaceutical Laboratories, Ltd.2007-01-042016-04-05Us
Meperidine Hydrochlorideinjection50 mg/mLintramuscular; intravenous; subcutaneousWest Ward Pharmaceutical Corp.1975-01-222016-04-23Us
Meperidine Hydrochloridetablet50 mg/1oralRoxane Laboratories, Inc1997-03-122016-04-23Us
Meperidine Hydrochlorideinjection50 mg/mLintramuscularPhysicians Total Care, Inc.2010-03-042016-04-05Us
Meperidine Hydrochloridetablet50 mg/1oralPhysicians Total Care, Inc.2009-09-142016-04-05Us
Meperidine Hydrochlorideinjection25 mg/mLintramuscular; intravenous; subcutaneousWest Ward Pharmaceutical Corp.1975-01-222016-04-23Us
Meperidine Hydrochloridetablet100 mg/1oralRoxane Laboratories, Inc1997-03-122016-04-23Us
Meperidine Hydrochloridetablet100 mg/1oralQualitest Pharmaceuticals1998-12-172016-04-23Us
Meperidine Hydrochloridetablet50 mg/1oralRoxane Laboratories, Inc1997-03-122016-04-23Us
Meperidine Hydrochloridetablet150 mg/1oralMikart, Inc.2009-06-242016-04-05Us
Over the Counter ProductsNot Available
International Brands
NameCompany
Dolantinsanofi-aventis
Dolcontralmibe
DolosalCristália
DolsinBiotika
LydolSopharma
MialginZentiva
PetidinNycomed
Brand mixtures
NameLabellerIngredients
Meperidine Hydrochloride and Promethazine HydrochlorideEci Pharmaceuticals Llc
Salts
Name/CASStructureProperties
Meperidine hydrochloride
ThumbNot applicableDBSALT001046
Pethidine hydrochloride
Thumb
  • InChI Key: WCNLCIJMFAJCPX-UHFFFAOYSA-N
  • Monoisotopic Mass: 283.13390666
  • Average Mass: 283.794
DBSALT000628
Categories
UNII9E338QE28F
CAS number57-42-1
WeightAverage: 247.3327
Monoisotopic: 247.157228921
Chemical FormulaC15H21NO2
InChI KeyInChIKey=XADCESSVHJOZHK-UHFFFAOYSA-N
InChI
InChI=1S/C15H21NO2/c1-3-18-14(17)15(9-11-16(2)12-10-15)13-7-5-4-6-8-13/h4-8H,3,9-12H2,1-2H3
IUPAC Name
ethyl 1-methyl-4-phenylpiperidine-4-carboxylate
SMILES
CCOC(=O)C1(CCN(C)CC1)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpiperidines. These are compounds containing a phenylpiperidine skeleton, which consists of a piperidine bound to a phenyl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPiperidines
Sub ClassPhenylpiperidines
Direct ParentPhenylpiperidines
Alternative Parents
Substituents
  • Phenylpiperidine
  • Phenylacetate
  • Piperidinecarboxylic acid
  • Aralkylamine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxylic acid ester
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationUsed to control moderate to severe pain.
PharmacodynamicsMeperidine is a synthetic opiate agonist belonging to the phenylpiperidine class. Meperidine may produce less smooth muscle spasm, constipation, and depression of the cough reflex than equivalent doses of morphine. The onset of action is lightly more rapid than with morphine, and the duration of action is slightly shorter. The chemical structure of meperidine is similar to local anesthetics. Meperidine is recommended for relief of moderate to severe acute pain and has the unique ability to interrupt postoperative shivering and shaking chills induced by amphotericin B. Meperidine has also been used for intravenous regional anesthesia, peripheral nerve blocks and intraarticular, epidural and spinal analgesia. Meperidine is considered a second-line agent for the treatment of acute pain.
Mechanism of actionMeperidine is primarily a kappa-opiate receptor agonist and also has local anesthetic effects. Meperidine has more affinity for the kappa-receptor than morphine. Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Related Articles
AbsorptionThe oral bioavailability of meperidine in patients with normal hepatic function is 50-60% due to extensive first-pass metabolism. Bioavailability increases to 80-90% in patients with hepatic impairment (e.g. liver cirrhosis). Meperidine is less than half as effective when administered orally compared to parenteral administration. One study reported that 80-85% of the drug administered intramuscularly was absorbed within 6 hours of intragluteal injection in health adults; however, inter-individual variation and patient-specific variable appear to cause considerable variations in absorption upon IM injection.
Volume of distribution

Meperidine crosses the placenta and is distributed into breast milk.

Protein binding60-80% bound to plasma proteins, primarily albumin and α1-acid glycoprotein. The presence of cirrhosis or active viral hepatitis does not appear to affect the extent of protein binding.
Metabolism

Meperidine is metabolized in the liver by hydrolysis to meperidinic acid followed by partial conjugation with glucuronic acid. Meperidine also undergoes N-demethylation to normeperidine, which then undergoes hydrolysis and partial conjugation. Normeperidine is about half as potent as meperidine, but it has twice the CNS stimulation effects.

Route of eliminationExcreted in the urine. The proportion of drug that is excreted unchanged or as metabolites is dependent on pH. When urine pH is uncontrolled, 5-30% of the meperidine dose is excreted as normeperidine and approximately 5% is excreted unchanged. Meperidine and normeperidine are found in acidic urine, while the free and conjugated forms of meperidinic and normperidinic acids are found in alkaline urine.
Half lifeInitial distribution phase (t1/2 α) = 2-11 minutes; terminal elimination phase (t1/2 β) = 3-5 hours. In patients with hepatic dysfunction (e.g. liver cirrhosis or active viral hepatitis) the t1/2 β is prolonged to 7-11 hours.
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9947
Blood Brain Barrier+0.9876
Caco-2 permeable+0.6683
P-glycoprotein substrateSubstrate0.7821
P-glycoprotein inhibitor IInhibitor0.5174
P-glycoprotein inhibitor IIInhibitor0.5401
Renal organic cation transporterInhibitor0.6375
CYP450 2C9 substrateNon-substrate0.8593
CYP450 2D6 substrateSubstrate0.8826
CYP450 3A4 substrateSubstrate0.5073
CYP450 1A2 substrateNon-inhibitor0.6897
CYP450 2C9 inhibitorNon-inhibitor0.6691
CYP450 2D6 inhibitorInhibitor0.7415
CYP450 2C19 inhibitorNon-inhibitor0.7635
CYP450 3A4 inhibitorNon-inhibitor0.6876
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5547
Ames testNon AMES toxic0.8694
CarcinogenicityNon-carcinogens0.8355
BiodegradationNot ready biodegradable0.9145
Rat acute toxicity3.1526 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8593
hERG inhibition (predictor II)Inhibitor0.5813
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Hospira inc
  • Sanofi aventis us llc
  • Abbott laboratories pharmaceutical products div
  • Astrazeneca lp
  • Baxter healthcare corp anesthesia and critical care
  • Baxter healthcare corp anesthesia critical care
  • Elkins sinn div ah robins co inc
  • International medication systems ltd
  • Parke davis div warner lambert co
  • Watson laboratories inc
  • International medication system
  • Mallinckrodt chemical inc
  • Roxane laboratories inc
  • Barr laboratories inc
  • Caraco pharmaceutical laboratories ltd
  • Duramed pharmaceuticals inc sub barr laboratories inc
  • Mallinckrodt inc
  • Mikah pharma llc
  • Mikart inc
  • Mutual pharmaceutical co inc
  • Vintage pharmaceuticals inc
  • Wyeth ayerst laboratories
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintramuscular; intravenous; subcutaneous100 mg/mL
Injection, solutionintramuscular; intravenous; subcutaneous100 mg/2mL
Injection, solutionintramuscular; intravenous; subcutaneous25 mg/.5mL
Injection, solutionintramuscular; intravenous; subcutaneous25 mg/mL
Injection, solutionintramuscular; intravenous; subcutaneous50 mg/mL
Injection, solutionintramuscular; intravenous; subcutaneous75 mg/mL
Injection, solutionintramuscular; intravenous; subcutaneous75 mg/1.5mL
Tabletoral100 mg/1
Tabletoral50 mg/1
Tabletoral50 mg
Liquidintramuscular; intravenous; subcutaneous50 mg
Liquidintramuscular; subcutaneous50 mg
Liquidintramuscular; intravenous; subcutaneous100 mg
Liquidintramuscular; subcutaneous100 mg
Solutionintramuscular; intravenous; subcutaneous100 mg
Solutionintramuscular; subcutaneous100 mg
Solutionintramuscular; subcutaneous50 mg
Solutionintramuscular; intravenous; subcutaneous50 mg
Solutionintramuscular; intravenous; subcutaneous75 mg
Liquidintramuscular; intravenous; subcutaneous75 mg
Solutionintramuscular; intravenous; subcutaneous10 mg
Solutionintramuscular; intravenous; subcutaneous25 mg
Injectionintramuscular50 mg/mL
Injectionintramuscular; intravenous; subcutaneous100 mg/mL
Injectionintramuscular; intravenous; subcutaneous25 mg/mL
Injectionintramuscular; intravenous; subcutaneous50 mg/mL
Injection, solutionintravenous10 mg/mL
Solutionoral50 mg/5mL
Tabletoral150 mg/1
Tabletoral75 mg/1
Capsuleoral
Solutionintravenous10 mg
Prices
Unit descriptionCostUnit
Meperidine HCl 100 mg/ml vial33.99USD vial
Meperidine hcl powder10.51USD g
Demerol 100 mg tablet3.33USD tablet
Demerol 100 mg/ml vial1.79USD ml
Demerol 50 mg tablet1.71USD tablet
Meperidine HCl 100 mg tablet1.33USD tablet
Meperidine 100 mg tablet1.31USD tablet
Demerol 100 mg/ml ampul1.1USD ml
Meperidine Hydrochloride 100 mg/ml1.1USD ml
Meperidine Hydrochloride 75 mg/ml1.04USD ml
Meperidine Hydrochloride 50 mg/ml0.98USD ml
Meperidine HCl 50 mg tablet0.93USD tablet
Demerol 50 mg/ml vial0.85USD ml
Meperidine 10 mg/ml syringe0.85USD ml
Meperidine 50 mg tablet0.69USD tablet
Demerol 50 mg/ml ampul0.58USD ml
Meperidine 10 mg/ml cartrdge0.3USD ml
Demerol 50 mg Tablet0.16USD tablet
Meperidine HCl 50 mg/5ml Solution0.14USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point270 °CPhysProp
water solubility3220 mg/L (at 30 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.72SANGSTER (1994)
logS-1.89ADME Research, USCD
pKa8.59SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility1.11 mg/mLALOGPS
logP2.9ALOGPS
logP2.46ChemAxon
logS-2.4ALOGPS
pKa (Strongest Basic)8.16ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area29.54 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity72.48 m3·mol-1ChemAxon
Polarizability28.09 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-zo80000000-7309f4ee3918ea05f00dView in MoNA
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesN02AB02N02AB52N02AB72N02AG03
AHFS Codes
  • 28:08.08
PDB EntriesNot Available
FDA labelDownload (173 KB)
MSDSDownload (6.6 KB)
Interactions
Drug Interactions
Drug
AcepromazineAcepromazine may increase the hypotensive activities of Pethidine.
AcetazolamideThe risk or severity of adverse effects can be increased when Pethidine is combined with Acetazolamide.
AcetophenazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Acetophenazine.
AlvimopanThe risk or severity of adverse effects can be increased when Pethidine is combined with Alvimopan.
AmilorideThe risk or severity of adverse effects can be increased when Pethidine is combined with Amiloride.
AmisulprideThe risk or severity of adverse effects can be increased when Pethidine is combined with Amisulpride.
Ammonium chlorideAmmonium chloride may increase the excretion rate of Pethidine which could result in a higher serum level.
AmobarbitalAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
AmphetamineAmphetamine may increase the analgesic activities of Pethidine.
AripiprazoleThe risk or severity of adverse effects can be increased when Pethidine is combined with Aripiprazole.
AtazanavirThe risk or severity of adverse effects can be increased when Atazanavir is combined with Pethidine.
AzelastinePethidine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Pethidine.
BatimastatThe risk or severity of adverse effects can be increased when Batimastat is combined with Pethidine.
BendroflumethiazideThe risk or severity of adverse effects can be increased when Pethidine is combined with Bendroflumethiazide.
BenzquinamideThe risk or severity of adverse effects can be increased when Pethidine is combined with Benzquinamide.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
BumetanideThe risk or severity of adverse effects can be increased when Pethidine is combined with Bumetanide.
ButabarbitalButabarbital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
ButethalButethal may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
ButorphanolButorphanol may decrease the analgesic activities of Pethidine.
CarphenazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Carphenazine.
CathinoneCathinone may increase the analgesic activities of Pethidine.
ChlormezanoneThe risk or severity of adverse effects can be increased when Pethidine is combined with Chlormezanone.
ChlorothiazideThe risk or severity of adverse effects can be increased when Pethidine is combined with Chlorothiazide.
ChlorpromazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Pethidine is combined with Chlorprothixene.
ChlorthalidoneThe risk or severity of adverse effects can be increased when Pethidine is combined with Chlorthalidone.
CimetidineThe serum concentration of Pethidine can be increased when it is combined with Cimetidine.
ClozapineThe risk or severity of adverse effects can be increased when Pethidine is combined with Clozapine.
CyclothiazideThe risk or severity of adverse effects can be increased when Pethidine is combined with Cyclothiazide.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Pethidine.
DarunavirThe risk or severity of adverse effects can be increased when Darunavir is combined with Pethidine.
DesmopressinThe risk or severity of adverse effects can be increased when Pethidine is combined with Desmopressin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
EluxadolinePethidine may increase the activities of Eluxadoline.
Etacrynic acidThe risk or severity of adverse effects can be increased when Pethidine is combined with Ethacrynic acid.
EthanolPethidine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthoxzolamideThe risk or severity of adverse effects can be increased when Pethidine is combined with Ethoxzolamide.
FencamfamineThe risk or severity of adverse effects can be increased when Pethidine is combined with Fencamfamine.
FlupentixolThe risk or severity of adverse effects can be increased when Pethidine is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Pethidine is combined with Fluspirilene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Pethidine.
FosamprenavirThe risk or severity of adverse effects can be increased when Fosamprenavir is combined with Pethidine.
FosphenytoinThe serum concentration of Pethidine can be decreased when it is combined with Fosphenytoin.
FurosemideThe risk or severity of adverse effects can be increased when Pethidine is combined with Furosemide.
GranisetronGranisetron may increase the serotonergic activities of Pethidine.
HaloperidolThe risk or severity of adverse effects can be increased when Pethidine is combined with Haloperidol.
HeptabarbitalHeptabarbital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
HexobarbitalHexobarbital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Pethidine is combined with Hydrochlorothiazide.
HydrocodonePethidine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroflumethiazideThe risk or severity of adverse effects can be increased when Pethidine is combined with Hydroflumethiazide.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
IndapamideThe risk or severity of adverse effects can be increased when Pethidine is combined with Indapamide.
IndinavirThe risk or severity of adverse effects can be increased when Indinavir is combined with Pethidine.
IsocarboxazidIsocarboxazid may increase the serotonergic activities of Pethidine.
IsoflurophateThe risk or severity of adverse effects can be increased when Isoflurophate is combined with Pethidine.
LinezolidLinezolid may increase the serotonergic activities of Pethidine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Pethidine.
LoxapineThe risk or severity of adverse effects can be increased when Pethidine is combined with Loxapine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
MesoridazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Mesoridazine.
MethohexitalMethohexital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Methotrimeprazine.
MetoclopramideThe risk or severity of adverse effects can be increased when Pethidine is combined with Metoclopramide.
MetolazoneThe risk or severity of adverse effects can be increased when Pethidine is combined with Metolazone.
MetyrosinePethidine may increase the sedative activities of Metyrosine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
MoclobemideMoclobemide may increase the serotonergic activities of Pethidine.
MolindoneThe risk or severity of adverse effects can be increased when Pethidine is combined with Molindone.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
NaltrexoneThe therapeutic efficacy of Pethidine can be decreased when used in combination with Naltrexone.
NelfinavirThe risk or severity of adverse effects can be increased when Nelfinavir is combined with Pethidine.
OlanzapineThe risk or severity of adverse effects can be increased when Pethidine is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Pethidine is combined with Ondansetron.
OrphenadrinePethidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PaliperidoneThe risk or severity of adverse effects can be increased when Pethidine is combined with Paliperidone.
ParaldehydePethidine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
PegvisomantThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Pethidine.
PentobarbitalPentobarbital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
PerphenazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Perphenazine.
PhenelzinePhenelzine may increase the serotonergic activities of Pethidine.
PhenobarbitalPhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
PhenytoinThe serum concentration of Pethidine can be decreased when it is combined with Phenytoin.
PimozideThe risk or severity of adverse effects can be increased when Pethidine is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Piperacetazine.
PramipexolePethidine may increase the sedative activities of Pramipexole.
PrimidonePrimidone may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
ProcarbazineProcarbazine may increase the serotonergic activities of Pethidine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Prochlorperazine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Pethidine.
PromazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Pethidine is combined with Quetiapine.
RamosetronPethidine may increase the activities of Ramosetron.
RasagilineRasagiline may increase the serotonergic activities of Pethidine.
RemoxiprideThe risk or severity of adverse effects can be increased when Pethidine is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Pethidine is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Pethidine is combined with Risperidone.
RitonavirThe risk or severity of adverse effects can be increased when Ritonavir is combined with Pethidine.
RopinirolePethidine may increase the sedative activities of Ropinirole.
RotigotinePethidine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pethidine.
SaquinavirThe risk or severity of adverse effects can be increased when Saquinavir is combined with Pethidine.
SecobarbitalSecobarbital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
SelegilineSelegiline may increase the serotonergic activities of Pethidine.
SertindoleThe risk or severity of adverse effects can be increased when Pethidine is combined with Sertindole.
SimeprevirThe risk or severity of adverse effects can be increased when Simeprevir is combined with Pethidine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
SpironolactoneThe risk or severity of adverse effects can be increased when Pethidine is combined with Spironolactone.
SuccinylcholineSuccinylcholine may increase the bradycardic activities of Pethidine.
SulpirideThe risk or severity of adverse effects can be increased when Pethidine is combined with Sulpiride.
SuvorexantPethidine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Pethidine.
ThalidomidePethidine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Pethidine is combined with Thiothixene.
TicrynafenThe risk or severity of adverse effects can be increased when Pethidine is combined with Ticrynafen.
TipranavirThe risk or severity of adverse effects can be increased when Tipranavir is combined with Pethidine.
TorasemideThe risk or severity of adverse effects can be increased when Pethidine is combined with Torasemide.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Pethidine.
TranylcypromineTranylcypromine may increase the serotonergic activities of Pethidine.
TriamtereneThe risk or severity of adverse effects can be increased when Pethidine is combined with Triamterene.
TrichlormethiazideThe risk or severity of adverse effects can be increased when Pethidine is combined with Trichlormethiazide.
TrifluoperazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Pethidine is combined with Triflupromazine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Pethidine is combined with Ziprasidone.
ZolpidemPethidine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Pethidine is combined with Zuclopenthixol.
Food Interactions
  • Take without regard to meals. Avoid alcohol.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
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 synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates th...
Gene Name:
OPRK1
Uniprot ID:
P41145
Molecular Weight:
42644.665 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Voltage-gated cation channel activity
Specific Function:
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. It mediates neuronal functions in glutamate neurotransmission. Is involved in the cell surface targeting of NMDA receptors (...
Gene Name:
GRIN1
Uniprot ID:
Q05586
Molecular Weight:
105371.945 Da
References
  1. Yamakura T, Sakimura K, Shimoji K: N-methyl-D-aspartate receptor channel block by meperidine is dependent on extracellular pH. Anesth Analg. 2000 Apr;90(4):928-32. [PubMed:10735801 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. In concert with DAPK1 at extrasynaptic sites, acts as a central mediator for stroke damage. Its phosphorylation at Ser-1303 by DAPK1 enhances synaptic NMDA receptor channel activity inducing injurious Ca2+ influx through them, resulting in an ...
Gene Name:
GRIN2B
Uniprot ID:
Q13224
Molecular Weight:
166365.885 Da
References
  1. Yamakura T, Sakimura K, Shimoji K: N-methyl-D-aspartate receptor channel block by meperidine is dependent on extracellular pH. Anesth Analg. 2000 Apr;90(4):928-32. [PubMed:10735801 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Activation requires binding of agonist to both types of subunits.
Gene Name:
GRIN2A
Uniprot ID:
Q12879
Molecular Weight:
165281.215 Da
References
  1. Yamakura T, Sakimura K, Shimoji K: N-methyl-D-aspartate receptor channel block by meperidine is dependent on extracellular pH. Anesth Analg. 2000 Apr;90(4):928-32. [PubMed:10735801 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Nmda glutamate receptor activity
Specific Function:
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine.
Gene Name:
GRIN2C
Uniprot ID:
Q14957
Molecular Weight:
134207.77 Da
References
  1. Yamakura T, Sakimura K, Shimoji K: N-methyl-D-aspartate receptor channel block by meperidine is dependent on extracellular pH. Anesth Analg. 2000 Apr;90(4):928-32. [PubMed:10735801 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Nmda glutamate receptor activity
Specific Function:
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine.
Gene Name:
GRIN2D
Uniprot ID:
O15399
Molecular Weight:
143750.685 Da
References
  1. Yamakura T, Sakimura K, Shimoji K: N-methyl-D-aspartate receptor channel block by meperidine is dependent on extracellular pH. Anesth Analg. 2000 Apr;90(4):928-32. [PubMed:10735801 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
binder
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 action of G proteins. Primary transducing effect is Pi turnover.
Components:
NameUniProt IDDetails
Muscarinic acetylcholine receptor M1P11229 Details
Muscarinic acetylcholine receptor M2P08172 Details
Muscarinic acetylcholine receptor M3P20309 Details
Muscarinic acetylcholine receptor M4P08173 Details
Muscarinic acetylcholine receptor M5P08912 Details
References
  1. Hustveit O: Binding of fentanyl and pethidine to muscarinic receptors in rat brain. Jpn J Pharmacol. 1994 Jan;64(1):57-9. [PubMed:8164394 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
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. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociati...
Gene Name:
OPRM1
Uniprot ID:
P35372
Molecular Weight:
44778.855 Da
References
  1. Poulain R, Horvath D, Bonnet B, Eckhoff C, Chapelain B, Bodinier MC, Deprez B: From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands. J Med Chem. 2001 Oct 11;44(21):3378-90. [PubMed:11585443 ]
  2. Bryant, Bronwen (2010). Pharmacology for Health Professionals (Paperback) (3rd ed.). Chatswood: Mosby Australia. [ISBN:978-0-7295-3929-6 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Monoamine transmembrane transporter activity
Specific Function:
Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A3
Uniprot ID:
Q01959
Molecular Weight:
68494.255 Da
References
  1. Lomenzo SA, Izenwasser S, Gerdes RM, Katz JL, Kopajtic T, Trudell ML: Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine. Bioorg Med Chem Lett. 1999 Dec 6;9(23):3273-6. [PubMed:10612583 ]
  2. Lomenzo SA, Rhoden JB, Izenwasser S, Wade D, Kopajtic T, Katz JL, Trudell ML: Synthesis and biological evaluation of meperidine analogues at monoamine transporters. J Med Chem. 2005 Mar 10;48(5):1336-43. [PubMed:15743177 ]
  3. Gu X, Izenwasser S, Wade D, Housman A, Gulasey G, Rhoden JB, Savoie CD, Mobley DL, Lomenzo SA, Trudell ML: Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands. Bioorg Med Chem. 2010 Dec 1;18(23):8356-64. doi: 10.1016/j.bmc.2010.09.060. Epub 2010 Sep 29. [PubMed:20980153 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Norepinephrine:sodium symporter activity
Specific Function:
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A2
Uniprot ID:
P23975
Molecular Weight:
69331.42 Da
References
  1. Lomenzo SA, Rhoden JB, Izenwasser S, Wade D, Kopajtic T, Katz JL, Trudell ML: Synthesis and biological evaluation of meperidine analogues at monoamine transporters. J Med Chem. 2005 Mar 10;48(5):1336-43. [PubMed:15743177 ]
  2. Gu X, Izenwasser S, Wade D, Housman A, Gulasey G, Rhoden JB, Savoie CD, Mobley DL, Lomenzo SA, Trudell ML: Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands. Bioorg Med Chem. 2010 Dec 1;18(23):8356-64. doi: 10.1016/j.bmc.2010.09.060. Epub 2010 Sep 29. [PubMed:20980153 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binding
General Function:
Serotonin:sodium symporter activity
Specific Function:
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
Molecular Weight:
70324.165 Da
References
  1. Lomenzo SA, Rhoden JB, Izenwasser S, Wade D, Kopajtic T, Katz JL, Trudell ML: Synthesis and biological evaluation of meperidine analogues at monoamine transporters. J Med Chem. 2005 Mar 10;48(5):1336-43. [PubMed:15743177 ]
  2. Gu X, Izenwasser S, Wade D, Housman A, Gulasey G, Rhoden JB, Savoie CD, Mobley DL, Lomenzo SA, Trudell ML: Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands. Bioorg Med Chem. 2010 Dec 1;18(23):8356-64. doi: 10.1016/j.bmc.2010.09.060. Epub 2010 Sep 29. [PubMed:20980153 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Ramirez J, Innocenti F, Schuetz EG, Flockhart DA, Relling MV, Santucci R, Ratain MJ: CYP2B6, CYP3A4, and CYP2C19 are responsible for the in vitro N-demethylation of meperidine in human liver microsomes. Drug Metab Dispos. 2004 Sep;32(9):930-6. [PubMed:15319333 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Ramirez J, Innocenti F, Schuetz EG, Flockhart DA, Relling MV, Santucci R, Ratain MJ: CYP2B6, CYP3A4, and CYP2C19 are responsible for the in vitro N-demethylation of meperidine in human liver microsomes. Drug Metab Dispos. 2004 Sep;32(9):930-6. [PubMed:15319333 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Ramirez J, Innocenti F, Schuetz EG, Flockhart DA, Relling MV, Santucci R, Ratain MJ: CYP2B6, CYP3A4, and CYP2C19 are responsible for the in vitro N-demethylation of meperidine in human liver microsomes. Drug Metab Dispos. 2004 Sep;32(9):930-6. [PubMed:15319333 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Ramirez J, Innocenti F, Schuetz EG, Flockhart DA, Relling MV, Santucci R, Ratain MJ: CYP2B6, CYP3A4, and CYP2C19 are responsible for the in vitro N-demethylation of meperidine in human liver microsomes. Drug Metab Dispos. 2004 Sep;32(9):930-6. [PubMed:15319333 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Edwards DJ, Svensson CK, Visco JP, Lalka D: Clinical pharmacokinetics of pethidine: 1982. Clin Pharmacokinet. 1982 Sep-Oct;7(5):421-33. [PubMed:6754208 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da
References
  1. Edwards DJ, Svensson CK, Visco JP, Lalka D: Clinical pharmacokinetics of pethidine: 1982. Clin Pharmacokinet. 1982 Sep-Oct;7(5):421-33. [PubMed:6754208 ]
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Drug created on June 13, 2005 07:24 / Updated on April 21, 2016 10:37