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Identification
NameMefloquine
Accession NumberDB00358  (APRD00300)
TypeSmall Molecule
GroupsApproved
Description

A phospholipid-interacting antimalarial drug (antimalarials). It is very effective against plasmodium falciparum with very few side effects. [PubChem]

Structure
Thumb
Synonyms
[(R*,S*)-2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol
alpha-2-Piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol
Mefloquin
Mefloquina
Méfloquine
Mefloquine
Mefloquinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Lariam Tab 250mgtablet250 mgoralHoffmann La Roche Limited1993-12-312013-05-02Canada
Mefloquinetablet250 mgoralAa Pharma Inc2002-07-23Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mefloquine Hydrochloridetablet250 mg/1oralRoxane Laboratories, Inc.2004-10-01Not applicableUs
Mefloquine Hydrochloridetablet250 mg/1oralH.J. Harkins Company, Inc.2010-04-21Not applicableUs
Mefloquine Hydrochloridetablet250 mg/1oralRebel Distributors Corp2010-04-21Not applicableUs
Mefloquine Hydrochloridetablet250 mg/1oralRebel Distributors Corp2003-12-29Not applicableUs
Mefloquine Hydrochloridetablet250 mg/1oralSandoz Inc2002-02-202016-03-31Us
Mefloquine Hydrochloridetablet250 mg/1oralBarr Laboratories Inc.2004-01-06Not applicableUs
Mefloquine Hydrochloridetablet250 mg/1oralWest ward Pharmaceutical Corp2010-04-21Not applicableUs
Mefloquine Hydrochloridetablet250 mg/1oralPhysicians Total Care, Inc.2005-09-26Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
EloquineUnifarm
FacitalZydus Cadila
FalcitalCadila HC
LariamHoffmann–La Roche
LarimefIpca
MefaxAlkem
MefliamCipla Medpro
MeflonACI
MefloquinaAC Farma
MefqueZydus Cadila
MephaquinHisamitsu Seiyaku
Mephaquin LactabMepha
MequinAtlantic
MqfSun
SutonNewai Chem
TropicurInvesti
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Mefloquine Hydrochloride
Thumb
  • InChI Key: WESWYMRNZNDGBX-YLCXCWDSSA-N
  • Monoisotopic Mass: 414.093360113
  • Average Mass: 414.773
DBSALT000311
Categories
UNIITML814419R
CAS number53230-10-7
WeightAverage: 378.3122
Monoisotopic: 378.116682374
Chemical FormulaC17H16F6N2O
InChI KeyInChIKey=XEEQGYMUWCZPDN-UHFFFAOYSA-N
InChI
InChI=1S/C17H16F6N2O/c18-16(19,20)11-5-3-4-9-10(15(26)12-6-1-2-7-24-12)8-13(17(21,22)23)25-14(9)11/h3-5,8,12,15,24,26H,1-2,6-7H2
IUPAC Name
[2,8-bis(trifluoromethyl)quinolin-4-yl](piperidin-2-yl)methanol
SMILES
OC(C1CCCCN1)C1=CC(=NC2=C1C=CC=C2C(F)(F)F)C(F)(F)F
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as quinolines and derivatives. These are compounds containing a quinoline moiety, which consists of a benzene ring fused to a pyrimidine ring to form benzo[b]azabenzene.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassQuinolines and derivatives
Sub ClassNot Available
Direct ParentQuinolines and derivatives
Alternative Parents
Substituents
  • Quinoline
  • Aralkylamine
  • Benzenoid
  • Pyridine
  • Piperidine
  • Heteroaromatic compound
  • Secondary alcohol
  • 1,2-aminoalcohol
  • Azacycle
  • Secondary amine
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Aromatic alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Amine
  • Alkyl halide
  • Alkyl fluoride
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of mild to moderate acute malaria caused by Mefloquineuine-susceptible strains of Plasmodium falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax. Also for the prophylaxis of Plasmodium falciparum and Plasmodium vivax malaria infections, including prophylaxis of chloroquine-resistant strains of Plasmodium falciparum.
PharmacodynamicsMefloquine is an antimalarial agent which acts as a blood schizonticide. Mefloquine is active against the erythrocytic stages of Plasmodium species. However, the drug has no effect against the exoerythrocytic (hepatic) stages of the parasite. Mefloquine is effective against malaria parasites resistant to chloroquine. Mefloquine is a chiral molecule. According to some research, the (+) enantiomer is more effective in treating malaria, and the (-) enantiomer specifically binds to adenosine receptors in the central nervous system, which may explain some of its psychotropic effects.
Mechanism of actionMefloquine has been found to produce swelling of the Plasmodium falciparum food vacuoles. It may act by forming toxic complexes with free heme that damage membranes and interact with other plasmodial components.
Related Articles
AbsorptionWell absorbed from the gastrointestinal tract. The presence of food significantly enhances the rate and extent of absorption.
Volume of distribution
  • 20 L/kg [healthy adults]
Protein binding98%
Metabolism

Hepatic. Two metabolites have been identified in humans. The main metabolite, 2,8-bis-trifluoromethyl-4-quinoline carboxylic acid, is inactive against Plasmodium falciparum. The second metabolite, an alcohol, is present in minute quantities.

SubstrateEnzymesProduct
Mefloquine
Not Available
2,8-bis-trifluoromethyl-4-quinoline carboxylic acidDetails
Route of eliminationThere is evidence that mefloquine is excreted mainly in the bile and feces. Urinary excretion of unchanged mefloquine and its main metabolite under steady-state condition accounted for about 9% and 4% of the dose, respectively.
Half life2 to 4 weeks
Clearance
  • 30 mL/min
ToxicityOral, rat: LD50 = 880 mg/kg. Symptoms of overdose include nausea, vomiting, and weight loss.
Affected organisms
  • Plasmodium
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9959
Blood Brain Barrier+0.9445
Caco-2 permeable-0.5753
P-glycoprotein substrateSubstrate0.6796
P-glycoprotein inhibitor INon-inhibitor0.7395
P-glycoprotein inhibitor IIInhibitor0.5419
Renal organic cation transporterNon-inhibitor0.6446
CYP450 2C9 substrateNon-substrate0.8711
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6524
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8533
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9163
Ames testNon AMES toxic0.809
CarcinogenicityNon-carcinogens0.9437
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.9133 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9035
hERG inhibition (predictor II)Inhibitor0.8204
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Hoffmann la roche inc
  • Barr laboratories inc
  • Roxane laboratories inc
  • Sandoz inc
  • United states army walter reed army institute research
  • West ward pharmaceutical corp
Packagers
Dosage forms
FormRouteStrength
Tabletoral250 mg
Tabletoral250 mg/1
Prices
Unit descriptionCostUnit
Lariam 25 250 mg tablet Box322.77USD box
Lariam 250 mg tablet12.41USD tablet
Mefloquine hcl 250 mg tablet10.8USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility5000 mg/L (HCl salt)Not Available
logP3.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.038 mg/mLALOGPS
logP3.1ALOGPS
logP4.11ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)13.79ChemAxon
pKa (Strongest Basic)9.46ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area45.15 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity82.58 m3·mol-1ChemAxon
Polarizability31.73 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

US4507482
General ReferencesNot Available
External Links
ATC CodesP01BC02P01BF02
AHFS Codes
  • 08:30.08
PDB Entries
FDA labelDownload (394 KB)
MSDSDownload (107 KB)
Interactions
Drug Interactions
Drug
AcepromazineThe serum concentration of Acepromazine can be increased when it is combined with Mefloquine.
AcetazolamideThe therapeutic efficacy of Acetazolamide can be decreased when used in combination with Mefloquine.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Mefloquine.
AmodiaquineThe risk or severity of adverse effects can be increased when Amodiaquine is combined with Mefloquine.
AprepitantThe serum concentration of Mefloquine can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Mefloquine.
ArtemetherThe risk or severity of adverse effects can be increased when Artemether is combined with Mefloquine.
BexaroteneThe serum concentration of Mefloquine can be decreased when it is combined with Bexarotene.
BosentanThe serum concentration of Mefloquine can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Mefloquine.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Mefloquine.
CarbamazepineThe therapeutic efficacy of Carbamazepine can be decreased when used in combination with Mefloquine.
ChloroquineThe risk or severity of adverse effects can be increased when Chloroquine is combined with Mefloquine.
CitalopramMefloquine may increase the QTc-prolonging activities of Citalopram.
ClobazamThe therapeutic efficacy of Clobazam can be decreased when used in combination with Mefloquine.
ClonazepamThe therapeutic efficacy of Clonazepam can be decreased when used in combination with Mefloquine.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Mefloquine.
ConivaptanThe serum concentration of Mefloquine can be increased when it is combined with Conivaptan.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Mefloquine.
DabrafenibThe serum concentration of Mefloquine can be decreased when it is combined with Dabrafenib.
DapsoneThe risk or severity of adverse effects can be increased when Mefloquine is combined with Dapsone.
DasatinibThe serum concentration of Mefloquine can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Mefloquine can be decreased when it is combined with Deferasirox.
DelorazepamThe therapeutic efficacy of Delorazepam can be decreased when used in combination with Mefloquine.
DiazepamThe therapeutic efficacy of Diazepam can be decreased when used in combination with Mefloquine.
DofetilideMefloquine may increase the QTc-prolonging activities of Dofetilide.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Mefloquine.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Mefloquine.
Eslicarbazepine acetateThe therapeutic efficacy of Eslicarbazepine acetate can be decreased when used in combination with Mefloquine.
EthosuximideThe therapeutic efficacy of Ethosuximide can be decreased when used in combination with Mefloquine.
EthotoinThe therapeutic efficacy of Ethotoin can be decreased when used in combination with Mefloquine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Mefloquine.
EzogabineThe therapeutic efficacy of Ezogabine can be decreased when used in combination with Mefloquine.
FelbamateThe therapeutic efficacy of Felbamate can be decreased when used in combination with Mefloquine.
FluconazoleThe metabolism of Mefloquine can be decreased when combined with Fluconazole.
FlunarizineThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Mefloquine.
FosaprepitantThe serum concentration of Mefloquine can be increased when it is combined with Fosaprepitant.
FosphenytoinThe therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Mefloquine.
Fusidic AcidThe serum concentration of Mefloquine can be increased when it is combined with Fusidic Acid.
GabapentinThe therapeutic efficacy of Gabapentin can be decreased when used in combination with Mefloquine.
GoserelinMefloquine may increase the QTc-prolonging activities of Goserelin.
HalofantrineMefloquine may increase the QTc-prolonging activities of Halofantrine.
HydroxychloroquineThe risk or severity of adverse effects can be increased when Hydroxychloroquine is combined with Mefloquine.
IdelalisibThe serum concentration of Mefloquine can be increased when it is combined with Idelalisib.
IvacaftorThe serum concentration of Mefloquine can be increased when it is combined with Ivacaftor.
LacosamideThe therapeutic efficacy of Lacosamide can be decreased when used in combination with Mefloquine.
LamotrigineThe therapeutic efficacy of Lamotrigine can be decreased when used in combination with Mefloquine.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Mefloquine.
LeuprolideMefloquine may increase the QTc-prolonging activities of Leuprolide.
LevetiracetamThe therapeutic efficacy of Levetiracetam can be decreased when used in combination with Mefloquine.
LuliconazoleThe serum concentration of Mefloquine can be increased when it is combined with Luliconazole.
LumefantrineThe risk or severity of adverse effects can be increased when Mefloquine is combined with Lumefantrine.
Magnesium SulfateThe therapeutic efficacy of Magnesium Sulfate can be decreased when used in combination with Mefloquine.
MephenytoinThe therapeutic efficacy of Mephenytoin can be decreased when used in combination with Mefloquine.
MeprobamateThe therapeutic efficacy of Meprobamate can be decreased when used in combination with Mefloquine.
MethsuximideThe therapeutic efficacy of Methsuximide can be decreased when used in combination with Mefloquine.
MethylphenobarbitalThe therapeutic efficacy of Methylphenobarbital can be decreased when used in combination with Mefloquine.
MifepristoneThe serum concentration of Mefloquine can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Mefloquine can be decreased when it is combined with Mitotane.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Mefloquine.
NelfinavirThe metabolism of Mefloquine can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Mefloquine can be increased when it is combined with Netupitant.
NitrazepamThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Mefloquine.
OxcarbazepineThe therapeutic efficacy of Oxcarbazepine can be decreased when used in combination with Mefloquine.
PalbociclibThe serum concentration of Mefloquine can be increased when it is combined with Palbociclib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Mefloquine.
PentobarbitalThe therapeutic efficacy of Pentobarbital can be decreased when used in combination with Mefloquine.
PerampanelThe therapeutic efficacy of Perampanel can be decreased when used in combination with Mefloquine.
PhenobarbitalThe therapeutic efficacy of Phenobarbital can be decreased when used in combination with Mefloquine.
PhensuximideThe therapeutic efficacy of Phensuximide can be decreased when used in combination with Mefloquine.
PhenytoinThe therapeutic efficacy of Phenytoin can be decreased when used in combination with Mefloquine.
PregabalinThe therapeutic efficacy of Pregabalin can be decreased when used in combination with Mefloquine.
PrimaquineThe risk or severity of adverse effects can be increased when Primaquine is combined with Mefloquine.
PrimidoneThe therapeutic efficacy of Primidone can be decreased when used in combination with Mefloquine.
ProgabideThe therapeutic efficacy of Progabide can be decreased when used in combination with Mefloquine.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Mefloquine.
QuinidineThe risk or severity of adverse effects can be increased when Quinidine is combined with Mefloquine.
QuinineThe risk or severity of adverse effects can be increased when Quinine is combined with Mefloquine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Mefloquine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Mefloquine.
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Mefloquine.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Mefloquine.
SiltuximabThe serum concentration of Mefloquine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Mefloquine can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Mefloquine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Mefloquine can be increased when it is combined with Stiripentol.
TalampanelThe therapeutic efficacy of Talampanel can be decreased when used in combination with Mefloquine.
ThiopentalThe therapeutic efficacy of Thiopental can be decreased when used in combination with Mefloquine.
TiagabineThe therapeutic efficacy of Tiagabine can be decreased when used in combination with Mefloquine.
TizanidineThe therapeutic efficacy of Tizanidine can be decreased when used in combination with Mefloquine.
TocilizumabThe serum concentration of Mefloquine can be decreased when it is combined with Tocilizumab.
TopiramateThe therapeutic efficacy of Topiramate can be decreased when used in combination with Mefloquine.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Mefloquine.
tramiprosateThe therapeutic efficacy of tramiprosate can be decreased when used in combination with Mefloquine.
TrimethadioneThe therapeutic efficacy of Trimethadione can be decreased when used in combination with Mefloquine.
Valproic AcidThe therapeutic efficacy of Valproic Acid can be decreased when used in combination with Mefloquine.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Mefloquine.
VigabatrinThe therapeutic efficacy of Vigabatrin can be decreased when used in combination with Mefloquine.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Mefloquine.
ZonisamideThe therapeutic efficacy of Zonisamide can be decreased when used in combination with Mefloquine.
Food Interactions
  • Avoid alcohol.
  • Take with a full glass of water.
  • Take with food.

Targets

1. Fe(II)-protoporphyrin IX
Kind
Small molecule
Organism
Plasmodium falciparum
Pharmacological action
yes
Actions
antagonist
References
  1. Fitch CD: Ferriprotoporphyrin IX, phospholipids, and the antimalarial actions of quinoline drugs. Life Sci. 2004 Mar 5;74(16):1957-72. [PubMed:14967191 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Oxygen transporter activity
Specific Function:
Involved in oxygen transport from the lung to the various peripheral tissues.
Gene Name:
HBA1
Uniprot ID:
P69905
Molecular Weight:
15257.405 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:
Identical protein binding
Specific Function:
Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
ADORA2A
Uniprot ID:
P29274
Molecular Weight:
44706.925 Da
References
  1. Gillespie RJ, Adams DR, Bebbington D, Benwell K, Cliffe IA, Dawson CE, Dourish CT, Fletcher A, Gaur S, Giles PR, Jordan AM, Knight AR, Knutsen LJ, Lawrence A, Lerpiniere J, Misra A, Porter RH, Pratt RM, Shepherd R, Upton R, Ward SE, Weiss SM, Williamson DS: Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives. Bioorg Med Chem Lett. 2008 May 1;18(9):2916-9. doi: 10.1016/j.bmcl.2008.03.075. Epub 2008 Mar 30. [PubMed:18406614 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Identical protein binding
Specific Function:
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name:
BCHE
Uniprot ID:
P06276
Molecular Weight:
68417.575 Da
References
  1. Lim LY, Go ML: The anticholinesterase activity of mefloquine. Clin Exp Pharmacol Physiol. 1985 Sep-Oct;12(5):527-31. [PubMed:3878759 ]
  2. Zhou C, Xiao C, McArdle JJ, Ye JH: Mefloquine enhances nigral gamma-aminobutyric acid release via inhibition of cholinesterase. J Pharmacol Exp Ther. 2006 Jun;317(3):1155-60. Epub 2006 Feb 24. [PubMed:16501066 ]
  3. McArdle JJ, Sellin LC, Coakley KM, Potian JG, Quinones-Lopez MC, Rosenfeld CA, Sultatos LG, Hognason K: Mefloquine inhibits cholinesterases at the mouse neuromuscular junction. Neuropharmacology. 2005 Dec;49(8):1132-9. Epub 2005 Aug 2. [PubMed:16081111 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxygen binding
Specific Function:
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name:
CYP19A1
Uniprot ID:
P11511
Molecular Weight:
57882.48 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Serine hydrolase activity
Specific Function:
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. Role in neuronal apoptosis.
Gene Name:
ACHE
Uniprot ID:
P22303
Molecular Weight:
67795.525 Da
References
  1. Lim LY, Go ML: The anticholinesterase activity of mefloquine. Clin Exp Pharmacol Physiol. 1985 Sep-Oct;12(5):527-31. [PubMed:3878759 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Fujita R, Ishikawa M, Takayanagi M, Takayanagi Y, Sasaki K: Enhancement of doxorubicin activity in multidrug-resistant cells by mefloquine. Methods Find Exp Clin Pharmacol. 2000 Jun;22(5):281-4. [PubMed:11031728 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on October 08, 2013 14:24