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PILOCARPINE Drug Record

  • Summary
  • Interactions
  • Claims
  • PILOCARPINE chembl:CHEMBL550 Approved

    Alternate Names:

    PILOCARPINE
    OCUSERT PILO
    OCUSERT PILO-20
    OCUSERT PILO-40
    (3S,4R)-3-ETHYLDIHYDRO-4-((1-METHYL-1H-IMIDAZOL-5-YL)METHYL)-2(3H)-FURANONE
    (3S-CIS)-3-ETHYLDIHYDRO-4-[(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-2(3H)-FURANONE
    SALAGEN®
    PILOCARPINE HYDROCHLORIDE
    PILOCARPINE NITRATE
    (+)-PILOCARPINE
    PILOKARPIN
    drugbank:01085
    rxcui:8328
    pubchem.compound:5910
    chembl:CHEMBL550
    chemidplus:92-13-7

    Drug Info:

    Year of Approval approved before 1982
    Drug Class miotics
    Drug Class anti-glaucomic agents
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications for treatment of incontinence
    (4 More Sources)

    Publications:

    Lindholm et al., 1994, Brain-derived neurotrophic factor and neurotrophin-4 increase neurotrophin-3 expression in the rat hippocampus., Int. J. Dev. Neurosci.
    Ekström, 1977, Choline acetyltransferase activity in parotid glands of rats after prolonged treatment with pilocarpine., Acta Physiol. Scand.
    Poulsen et al., 2004, Differential expression of brain-derived neurotrophic factor transcripts after pilocarpine-induced seizure-like activity is related to mode of Ca2+ entry., Neuroscience
    Figueroa et al., 2009, Selectivity of agonists for the active state of M1 to M4 muscarinic receptor subtypes., J. Pharmacol. Exp. Ther.
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Chen X et al., 2015, Rational design of partial agonists for the muscarinic m1 acetylcholine receptor., J Med Chem
    Sykes et al., 2009, Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor., Mol. Pharmacol.
    Moreno-Vinasco et al., 2009, Retinoic acid prevents virus-induced airway hyperreactivity and M2 receptor dysfunction via anti-inflammatory and antiviral effects., Am. J. Physiol. Lung Cell Mol. Physiol.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Hall et al., 1984, Serotonin and acetylcholine affect the release of prolactin and growth hormone from pituitary glands of domestic fowl in vitro in the presence of hypothalamic tissue., Acta Endocrinol.
    Clinckers et al., 2005, Quantitative in vivo microdialysis study on the influence of multidrug transporters on the blood-brain barrier passage of oxcarbazepine: concomitant use of hippocampal monoamines as pharmacodynamic markers for the anticonvulsant activity., J. Pharmacol. Exp. Ther.
    Bucci et al., Effects of age on pilocarpine-induced c-fos expression in rat hippocampus and cortex., Neurobiol. Aging
    Kitagawa K et al., 1999, The significance of the homozygous CYP2A6 deletion on nicotine metabolism: a new genotyping method of CYP2A6 using a single PCR-RFLP., Biochem Biophys Res Commun
    Wang H et al., 2011, Association analysis of CYP2A6 genotypes and haplotypes with 5-fluorouracil formation from tegafur in human liver microsomes., Pharmacogenomics
    Tanii H et al., 2011, Population pharmacokinetic analysis of letrozole in Japanese postmenopausal women., Eur J Clin Pharmacol
    Elens L et al., 2010, Influence of host genetic factors on efavirenz plasma and intracellular pharmacokinetics in HIV-1-infected patients., Pharmacogenomics
    Hirose T et al., 2010, Pharmacokinetics of S-1 and CYP2A6 genotype in Japanese patients with advanced cancer., Oncol Rep
    Djordjevic N et al., 2010, In vivo evaluation of CYP2A6 and xanthine oxidase enzyme activities in the Serbian population., Eur J Clin Pharmacol
    Tan L et al., 2010, The influence of cytochrome oxidase CYP2A6, CYP2B6, and CYP2C9 polymorphisms on the plasma concentrations of valproic acid in epileptic patients., Clin Neurol Neurosurg
    Ishii Y et al., 2010, Can the 2-(13)C-uracil breath test be used to predict the effect of the antitumor drug S-1?, Cancer Chemother Pharmacol
    Murai K et al., 2009, Deactivation of anti-cancer drug letrozole to a carbinol metabolite by polymorphic cytochrome P450 2A6 in human liver microsomes., Xenobiotica
    Kong SY et al., 2009, Association of CYP2A6 polymorphisms with S-1 plus docetaxel therapy outcomes in metastatic gastric cancer., Pharmacogenomics
    di Iulio J et al., 2009, In vivo analysis of efavirenz metabolism in individuals with impaired CYP2A6 function., Pharmacogenet Genomics
    Arab-Alameddine M et al., 2009, Pharmacogenetics-based population pharmacokinetic analysis of efavirenz in HIV-1-infected individuals., Clin Pharmacol Ther
    Endo T et al., 2008, Genetic polymorphisms of CYP2A6 affect the in-vivo pharmacokinetics of pilocarpine., Pharmacogenet Genomics
    Fujita K et al., 2008, CYP2A6 and the plasma level of 5-chloro-2, 4-dihydroxypyridine are determinants of the pharmacokinetic variability of tegafur and 5-fluorouracil, respectively, in Japanese patients with cancer given S-1., Cancer Sci
    Kaida Y et al., 2008, The CYP2A6*4 allele is determinant of S-1 pharmacokinetics in Japanese patients with non-small-cell lung cancer., Clin Pharmacol Ther
    Peamkrasatam S et al., 2006, In vivo evaluation of coumarin and nicotine as probe drugs to predict the metabolic capacity of CYP2A6 due to genetic polymorphism in Thais., Drug Metab Pharmacokinet
    Endo T et al., 2007, Involvement of CYP2A6 in the formation of a novel metabolite, 3-hydroxypilocarpine, from pilocarpine in human liver microsomes., Drug Metab Dispos
    Audrain-McGovern J et al., 2007, The role of CYP2A6 in the emergence of nicotine dependence in adolescents., Pediatrics
    Benowitz NL et al., 2006, CYP2A6 genotype and the metabolism and disposition kinetics of nicotine., Clin Pharmacol Ther
    Nakajima M et al., 2006, Comprehensive evaluation of variability in nicotine metabolism and CYP2A6 polymorphic alleles in four ethnic populations., Clin Pharmacol Ther
    Nurfadhlina M et al., 2006, CYP2A6 polymorphisms in Malays, Chinese and Indians., Xenobiotica
    Minematsu N et al., 2006, Limitation of cigarette consumption by CYP2A6*4, *7 and *9 polymorphisms., Eur Respir J
    Malaiyandi V et al., 2006, Impact of CYP2A6 genotype on pretreatment smoking behaviour and nicotine levels from and usage of nicotine replacement therapy., Mol Psychiatry
    Huang S et al., 2005, CYP2A6, MAOA, DBH, DRD4, and 5HT2A genotypes, smoking behaviour and cotinine levels in 1518 UK adolescents., Pharmacogenet Genomics
    Kimura M et al., 2005, Cyp2a6 is a principal enzyme involved in hydroxylation of 1,7-dimethylxanthine, a main caffeine metabolite, in humans., Drug Metab Dispos
    Gambier N et al., 2005, Association of CYP2A6*1B genetic variant with the amount of smoking in French adults from the Stanislas cohort., Pharmacogenomics J
    Fukami T et al., 2005, Characterization of novel CYP2A6 polymorphic alleles (CYP2A6*18 and CYP2A6*19) that affect enzymatic activity., Drug Metab Dispos
    Gyamfi MA et al., 2005, High prevalence of cytochrome P450 2A6*1A alleles in a black African population of Ghana., Eur J Clin Pharmacol
    Schoedel KA et al., 2004, Ethnic variation in CYP2A6 and association of genetically slow nicotine metabolism and smoking in adult Caucasians., Pharmacogenetics
    Fujieda M et al., 2004, Evaluation of CYP2A6 genetic polymorphisms as determinants of smoking behavior and tobacco-related lung cancer risk in male Japanese smokers., Carcinogenesis
    Yamanaka H et al., 2004, Metabolic profile of nicotine in subjects whose CYP2A6 gene is deleted., Eur J Pharm Sci
    Iwahashi K et al., 2004, Whole deletion of CYP2A6 gene (CYP2A6AST;4C) and smoking behavior., Neuropsychobiology
    Yoshida R et al., 2003, Effects of polymorphism in promoter region of human CYP2A6 gene (CYP2A6*9) on expression level of messenger ribonucleic acid and enzymatic activity in vivo and in vitro., Clin Pharmacol Ther
    Ando M et al., 2003, Association of CYP2A6 gene deletion with cigarette smoking status in Japanese adults., J Epidemiol
    Ariyoshi N et al., 2002, Genetic polymorphism of CYP2A6 gene and tobacco-induced lung cancer risk in male smokers., Cancer Epidemiol Biomarkers Prev
    Daigo S et al., 2002, A novel mutant allele of the CYP2A6 gene (CYP2A6*11 ) found in a cancer patient who showed poor metabolic phenotype towards tegafur., Pharmacogenetics
    Xu C et al., 2002, An in vivo pilot study characterizing the new CYP2A6*7, *8, and *10 alleles., Biochem Biophys Res Commun
    Zhang X et al., 2001, Lack of association between smoking and CYP2A6 gene polymorphisms in A Japanese population., Nihon Arukoru Yakubutsu Igakkai Zasshi
    Pitarque M et al., 2001, Identification of a single nucleotide polymorphism in the TATA box of the CYP2A6 gene: impairment of its promoter activity., Biochem Biophys Res Commun
    Tan W et al., 2001, Frequency of CYP2A6 gene deletion and its relation to risk of lung and esophageal cancer in the Chinese population., Int J Cancer
    Ariyoshi N et al., 2001, A novel single nucleotide polymorphism altering stability and activity of CYP2a6., Biochem Biophys Res Commun
    Rao Y et al., 2000, Duplications and defects in the CYP2A6 gene: identification, genotyping, and in vivo effects on smoking., Mol Pharmacol
    Oscarson M et al., 1999, Identification and characterisation of novel polymorphisms in the CYP2A locus: implications for nicotine metabolism., FEBS Lett
    French et al., 1999, Hippocampal neurotrophin and trk receptor mRNA levels are altered by local administration of nicotine, carbachol and pilocarpine., Brain Res. Mol. Brain Res.
  • PILOCARPINE   CYP2A6

    Interaction Score: 8.72

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10448083 21521021 21494765 20860463 20596643 20155256 20089352 19921195 19845430 19604090 19238117 19225447 18698229 18380793 18212800 17220563 17178767 17130279 17112802 16952495 16891249 16452582 16402128 16272956 15980104 15940289 15900015 15660270 15475735 15308589 15265511 14981342 12844137 12749606 12223434 12042667 11779172 11725533 11394901 11241319 11237731 10999944 10544257


    Sources:
    PharmGKB

  • PILOCARPINE   FOS

    Interaction Score: 0.95

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9661997


    Sources:
    NCI

  • PILOCARPINE   CHAT

    Interaction Score: 0.95

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    842358


    Sources:
    NCI

  • PILOCARPINE   NTF3

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    7747601


    Sources:
    NCI

  • PILOCARPINE   CHRM2

    Interaction Score: 0.47

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name THVD-201

    PMIDs:
    19465517 18824613 11752352


    Sources:
    TdgClinicalTrial TEND

  • PILOCARPINE   CHRM1

    Interaction Score: 0.45

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Muscarinic acetylcholine receptor M1 agonist
    Direct Interaction yes
    Trial Name THVD-201

    PMIDs:
    18824613 17016423 17139284 25478907


    Sources:
    DTC TdgClinicalTrial ChemblInteractions TEND

  • PILOCARPINE   PRL

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    6144226


    Sources:
    NCI

  • PILOCARPINE   CHRM3

    Interaction Score: 0.27

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name THVD-201
    Mechanism of Interaction Muscarinic acetylcholine receptor M3 agonist

    PMIDs:
    18824613 19498041


    Sources:
    TdgClinicalTrial ChemblInteractions

  • PILOCARPINE   NTRK2

    Interaction Score: 0.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15183516


    Sources:
    NCI

  • PILOCARPINE   ABCC1

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15860570


    Sources:
    NCI

  • PILOCARPINE   NTRK1

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10101239


    Sources:
    NCI

  • PILOCARPINE   BDNF

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15183516


    Sources:
    NCI

  • PILOCARPINE   CHRM5

    Interaction Score: 0.12

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • TdgClinicalTrial: PILOCARPINE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications for treatment of incontinence
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • TEND: PILOCARPINE

    • Version: 01-August-2011

    Alternate Names:

    Drug Info:
    Drug Class anti-glaucomic agents
    Drug Class miotics
    Year of Approval approved before 1982

    Publications:

  • NCI: PILOCARPINE

    • Version: 14-September-2017

    Alternate Names:
    C748 NCI drug code

    Drug Info:

    Publications:
    Poulsen et al., 2004, Differential expression of brain-derived neurotrophic factor transcripts after pilocarpine-induced seizure-like activity is related to mode of Ca2+ entry., Neuroscience
    French et al., 1999, Hippocampal neurotrophin and trk receptor mRNA levels are altered by local administration of nicotine, carbachol and pilocarpine., Brain Res. Mol. Brain Res.
    Lindholm et al., 1994, Brain-derived neurotrophic factor and neurotrophin-4 increase neurotrophin-3 expression in the rat hippocampus., Int. J. Dev. Neurosci.

  • DTC: PILOCARPINE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL550 ChEMBL Drug ID

    Drug Info:

    Publications:
    Chen X et al., 2015, Rational design of partial agonists for the muscarinic m1 acetylcholine receptor., J Med Chem

  • PharmGKB: pilocarpine

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Pitarque M et al., 2001, Identification of a single nucleotide polymorphism in the TATA box of the CYP2A6 gene: impairment of its promoter activity., Biochem Biophys Res Commun
    Malaiyandi V et al., 2006, Impact of CYP2A6 genotype on pretreatment smoking behaviour and nicotine levels from and usage of nicotine replacement therapy., Mol Psychiatry
    Gambier N et al., 2005, Association of CYP2A6*1B genetic variant with the amount of smoking in French adults from the Stanislas cohort., Pharmacogenomics J

  • TTD: Pilocarpine

    • Version: 2020.06.01

    Alternate Names:
    D06HLY TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL550

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL550

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21