DGIdb - PILOCARPINE Drug Record

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 CYP2A64, 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 (CYP2A618 and CYP2A619) 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 CYP2A67, 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:

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

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

PILOCARPINE Drug Record

PILOCARPINE chembl:CHEMBL550 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9661997

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 842358

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 7747601

Sources: NCI

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 19465517 18824613 11752352

Sources: TdgClinicalTrial TEND

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 6144226

Sources: NCI

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15183516

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15860570

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10101239

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15183516

Sources: NCI

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: None found

Sources: TTD

TdgClinicalTrial: PILOCARPINE

Alternate Names:

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

Publications:

TEND: PILOCARPINE

Alternate Names:

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

Publications:

NCI: PILOCARPINE

Alternate Names: C748 NCI drug code

Drug Info:

DTC: PILOCARPINE

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

Alternate Names:

Drug Info:

TTD: Pilocarpine

Alternate Names: D06HLY TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL550

Alternate Names:

Interaction Types & Directionality:

n/a

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
9661997

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
842358

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
7747601

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name THVD-201

PMIDs:
19465517 18824613 11752352

Sources:
TdgClinicalTrial TEND

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

Interaction Types & Directionality:

n/a

PMIDs:
6144226

Sources:
NCI

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

Interaction Types & Directionality:

n/a

PMIDs:
15183516

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15860570

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
10101239

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15183516

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

PMIDs:
None found

Sources:
TTD

Drug Info:

Drug Indications for treatment of incontinence

Drug Class Small Molecule

FDA Approval approved

Drug Info:

Drug Class anti-glaucomic agents

Drug Class miotics

Year of Approval approved before 1982

Alternate Names:

C748 NCI drug code

Alternate Names:

CHEMBL550 ChEMBL Drug ID

Publications:

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

Alternate Names:

D06HLY TTD Drug ID