Peringatan Keamanan

The oral LD50 value in mice for pilocarpine hydrochloride are 200 mg/kg. The intraperitoneal and subcutaneous LD50 values in rats for pilocarpine hydrochloride are 203 mg/kg and 230 mg/kg, respectively.L48721

Overdosage can produce sweating, salivation, nausea, tremors, slowing of the pulse, and decreased blood pressure.L48561 Fatal overdosage with pilocarpine has been reported in the scientific literature at doses presumed to be greater than 100 mg. Severe overdosage should be treated with titrated atropine (0.5 mg to 1.0 mg given subcutaneously or intravenously), which is a muscarinic antagonist. Supportive measures should be initiated to maintain respiration and circulation. Epinephrine (0.3 mg to 1.0 mg, subcutaneously or intramuscularly) may also be used in response to severe cardiovascular depression or bronchoconstriction. It is not known if pilocarpine is dialyzable.L48566 Systemic toxicity following ophthalmic use of pilocarpine is rare, but some patients may experience sweating and gastrointestinal overactivity at therapeutic doses.L48561

Pilocarpine

DB01085

small molecule approved investigational

Deskripsi

A naturally occurring alkaloid derived from the Pilocarpus plants, pilocarpine is a muscarinic acetylcholine agonist.A262016, A262036 Pilocarpine is associated with parasympathomimetic effects by selectively working on muscarinic receptors.A262036 Pilocarpine is used to treat dry mouth and various ophthalmic conditions, including elevated intraocular pressure and glaucoma. The usage of glaucoma by pilocarpine dates back to 1875.A262041

Struktur Molekul 2D

Berat 208.2569
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life was 0.76 and 1.35 hours following administration of a 5mg or lOmg dose 3 times daily, respectively.[A262036] Following ophthalmic administration in healthy subjects, the half-life was 3.96 hours.[L48556]
Volume Distribusi There is no information available.
Klirens (Clearance) There is no information available.

Absorpsi

Following oral administration of pilocarpine 5mg three times daily in healthy male subjects, peak plasma drug concentrations of 15?g/L were reached in 1.25 hours. At the dose of pilocarpine 10mg three times daily, peak plasma drug concentrations of 41?g/L were reached in 0.85 hours. The rate of absorption is increased when taken with food.A262036 Following ophthalmic administration in healthy subjects, the overall median Tmax was 2.2 hours. The mean (SD) Cmax and AUC0-t were 897.2 (287.2) pg/mL and 2699 (741.4) hr x pg/mL, respectively.L48556 In patients with presbyopia, the mean Cmax and AUC0-t,ss values were 1.95 ng/mL and 4.14 ng x hr/mL, respectively. The median Tmax was 0.3 hours postdose with a range from 0.2 to 0.5 hours post-dose.L48631

Metabolisme

There is limited information available about the metabolism of pilocarpine in humans. Inactivation of pilocarpine can occur at neuronal synapses and probably in plasma.L48566 Pilocarpine is reported to undergo CYP2A6-mediated 3-hydroxylation to form stereoisomers of 3-hydroxypilocaripine.A262091 Pilocaripine also undergoes hydrolysis mediated by paraoxonase 1, a calcium-dependent esterase in plasma and the human liver.A262091 Pilocarpic acid is a possible metabolic product of hydrolysis.A184409 Pilocarpine metabolites are reported to possess negligible or no pharmacological activity.L48566

Rute Eliminasi

Pilocarpine and its degradation products are eliminated predominantly in the urine.A262036

Interaksi Makanan

1 Data
  • 1. Take with or without food. A high fat meal decreases Cmax and the time to reach Cmax, but not to a clinically significant extent.

Interaksi Obat

121 Data
Esmolol The risk or severity of adverse effects can be increased when Esmolol is combined with Pilocarpine.
Betaxolol The risk or severity of adverse effects can be increased when Betaxolol is combined with Pilocarpine.
Atenolol The risk or severity of adverse effects can be increased when Atenolol is combined with Pilocarpine.
Timolol The risk or severity of adverse effects can be increased when Timolol is combined with Pilocarpine.
Sotalol The risk or severity of adverse effects can be increased when Sotalol is combined with Pilocarpine.
Labetalol The risk or severity of adverse effects can be increased when Labetalol is combined with Pilocarpine.
Alprenolol The risk or severity of adverse effects can be increased when Alprenolol is combined with Pilocarpine.
Pindolol The risk or severity of adverse effects can be increased when Pindolol is combined with Pilocarpine.
Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Pilocarpine.
Nadolol The risk or severity of adverse effects can be increased when Nadolol is combined with Pilocarpine.
Bevantolol The risk or severity of adverse effects can be increased when Bevantolol is combined with Pilocarpine.
Practolol The risk or severity of adverse effects can be increased when Practolol is combined with Pilocarpine.
Penbutolol The risk or severity of adverse effects can be increased when Penbutolol is combined with Pilocarpine.
Oxprenolol The risk or severity of adverse effects can be increased when Oxprenolol is combined with Pilocarpine.
Dexpropranolol The risk or severity of adverse effects can be increased when Dexpropranolol is combined with Pilocarpine.
Celiprolol The risk or severity of adverse effects can be increased when Celiprolol is combined with Pilocarpine.
Bufuralol The risk or severity of adverse effects can be increased when Bufuralol is combined with Pilocarpine.
Bopindolol The risk or severity of adverse effects can be increased when Bopindolol is combined with Pilocarpine.
Bupranolol The risk or severity of adverse effects can be increased when Bupranolol is combined with Pilocarpine.
Indenolol The risk or severity of adverse effects can be increased when Indenolol is combined with Pilocarpine.
Arotinolol The risk or severity of adverse effects can be increased when Arotinolol is combined with Pilocarpine.
Levobetaxolol The risk or severity of adverse effects can be increased when Levobetaxolol is combined with Pilocarpine.
Talinolol The risk or severity of adverse effects can be increased when Talinolol is combined with Pilocarpine.
Anisodamine The risk or severity of adverse effects can be increased when Anisodamine is combined with Pilocarpine.
Bucindolol The risk or severity of adverse effects can be increased when Bucindolol is combined with Pilocarpine.
Esatenolol The risk or severity of adverse effects can be increased when Esatenolol is combined with Pilocarpine.
Cloranolol The risk or severity of adverse effects can be increased when Cloranolol is combined with Pilocarpine.
Mepindolol The risk or severity of adverse effects can be increased when Mepindolol is combined with Pilocarpine.
Epanolol The risk or severity of adverse effects can be increased when Epanolol is combined with Pilocarpine.
Tertatolol The risk or severity of adverse effects can be increased when Tertatolol is combined with Pilocarpine.
Propranolol The risk or severity of adverse effects can be increased when Propranolol is combined with Pilocarpine.
Bisoprolol The risk or severity of adverse effects can be increased when Bisoprolol is combined with Pilocarpine.
Carvedilol The risk or severity of adverse effects can be increased when Carvedilol is combined with Pilocarpine.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Pilocarpine.
Nebivolol The risk or severity of adverse effects can be increased when Nebivolol is combined with Pilocarpine.
Landiolol The risk or severity of adverse effects can be increased when Landiolol is combined with Pilocarpine.
Metoprolol The risk or severity of adverse effects can be increased when Metoprolol is combined with Pilocarpine.
Cimetropium Pilocarpine may decrease the anticholinergic activities of Cimetropium.
Pegvisomant The risk or severity of adverse effects can be increased when Pegvisomant is combined with Pilocarpine.
Tacrine The risk or severity of adverse effects can be increased when Tacrine is combined with Pilocarpine.
Sulpiride The risk or severity of adverse effects can be increased when Sulpiride is combined with Pilocarpine.
Profenamine The risk or severity of adverse effects can be increased when Profenamine is combined with Pilocarpine.
Gallamine triethiodide The risk or severity of adverse effects can be increased when Gallamine triethiodide is combined with Pilocarpine.
Triflupromazine The risk or severity of adverse effects can be increased when Triflupromazine is combined with Pilocarpine.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Pilocarpine.
Cinchocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Pilocarpine.
Pyridostigmine The risk or severity of adverse effects can be increased when Pyridostigmine is combined with Pilocarpine.
Nizatidine The risk or severity of adverse effects can be increased when Nizatidine is combined with Pilocarpine.
Isoflurophate The risk or severity of adverse effects can be increased when Isoflurophate is combined with Pilocarpine.
Diethylcarbamazine The risk or severity of adverse effects can be increased when Diethylcarbamazine is combined with Pilocarpine.
Procaine The risk or severity of adverse effects can be increased when Procaine is combined with Pilocarpine.
Minaprine The risk or severity of adverse effects can be increased when Minaprine is combined with Pilocarpine.
Terbutaline The risk or severity of adverse effects can be increased when Terbutaline is combined with Pilocarpine.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Pilocarpine.
Hexafluronium The risk or severity of adverse effects can be increased when Hexafluronium is combined with Pilocarpine.
Demecarium The risk or severity of adverse effects can be increased when Demecarium is combined with Pilocarpine.
Physostigmine The risk or severity of adverse effects can be increased when Physostigmine is combined with Pilocarpine.
Edrophonium The risk or severity of adverse effects can be increased when Edrophonium is combined with Pilocarpine.
Procainamide The risk or severity of adverse effects can be increased when Procainamide is combined with Pilocarpine.
Memantine The risk or severity of adverse effects can be increased when Memantine is combined with Pilocarpine.
Ambenonium The risk or severity of adverse effects can be increased when Ambenonium is combined with Pilocarpine.
Tubocurarine The risk or severity of adverse effects can be increased when Tubocurarine is combined with Pilocarpine.
Decamethonium The risk or severity of adverse effects can be increased when Decamethonium is combined with Pilocarpine.
Pancuronium The risk or severity of adverse effects can be increased when Pancuronium is combined with Pilocarpine.
Pipecuronium The risk or severity of adverse effects can be increased when Pipecuronium is combined with Pilocarpine.
Ginkgo biloba The risk or severity of adverse effects can be increased when Ginkgo biloba is combined with Pilocarpine.
Neostigmine The risk or severity of adverse effects can be increased when Neostigmine is combined with Pilocarpine.
Bambuterol The risk or severity of adverse effects can be increased when Bambuterol is combined with Pilocarpine.
1,10-Phenanthroline The risk or severity of adverse effects can be increased when 1,10-Phenanthroline is combined with Pilocarpine.
Huperzine A The risk or severity of adverse effects can be increased when Huperzine A is combined with Pilocarpine.
Phenserine The risk or severity of adverse effects can be increased when Phenserine is combined with Pilocarpine.
Regramostim The risk or severity of adverse effects can be increased when Regramostim is combined with Pilocarpine.
Aprotinin The risk or severity of adverse effects can be increased when Aprotinin is combined with Pilocarpine.
Betaine The risk or severity of adverse effects can be increased when Betaine is combined with Pilocarpine.
Capsaicin The risk or severity of adverse effects can be increased when Capsaicin is combined with Pilocarpine.
Coumaphos The risk or severity of adverse effects can be increased when Coumaphos is combined with Pilocarpine.
Dichlorvos The risk or severity of adverse effects can be increased when Dichlorvos is combined with Pilocarpine.
Fenthion The risk or severity of adverse effects can be increased when Fenthion is combined with Pilocarpine.
Metrifonate The risk or severity of adverse effects can be increased when Metrifonate is combined with Pilocarpine.
Acotiamide The risk or severity of adverse effects can be increased when Acotiamide is combined with Pilocarpine.
Methanesulfonyl Fluoride The risk or severity of adverse effects can be increased when Methanesulfonyl Fluoride is combined with Pilocarpine.
Paraoxon The risk or severity of adverse effects can be increased when Paraoxon is combined with Pilocarpine.
Tyrothricin The risk or severity of adverse effects can be increased when Tyrothricin is combined with Pilocarpine.
Ipidacrine The risk or severity of adverse effects can be increased when Ipidacrine is combined with Pilocarpine.
Distigmine The risk or severity of adverse effects can be increased when Distigmine is combined with Pilocarpine.
Tretamine The risk or severity of adverse effects can be increased when Tretamine is combined with Pilocarpine.
Posiphen The risk or severity of adverse effects can be increased when Posiphen is combined with Pilocarpine.
Rivastigmine The risk or severity of adverse effects can be increased when Rivastigmine is combined with Pilocarpine.
Methylphosphinic Acid The risk or severity of adverse effects can be increased when Methylphosphinic Acid is combined with Pilocarpine.
Mefloquine The risk or severity of adverse effects can be increased when Mefloquine is combined with Pilocarpine.
Galantamine The risk or severity of adverse effects can be increased when Galantamine is combined with Pilocarpine.
Ketamine The risk or severity of adverse effects can be increased when Ketamine is combined with Pilocarpine.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Pilocarpine.
Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Pilocarpine.
Thiotepa The risk or severity of adverse effects can be increased when Thiotepa is combined with Pilocarpine.
Capreomycin The therapeutic efficacy of Pilocarpine can be decreased when used in combination with Capreomycin.
Framycetin The therapeutic efficacy of Pilocarpine can be decreased when used in combination with Framycetin.
Amikacin The therapeutic efficacy of Pilocarpine can be decreased when used in combination with Amikacin.
Tobramycin The therapeutic efficacy of Pilocarpine can be decreased when used in combination with Tobramycin.
Gentamicin The therapeutic efficacy of Pilocarpine can be decreased when used in combination with Gentamicin.

Target Protein

Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M5 CHRM5
Muscarinic acetylcholine receptor M4 CHRM4

Referensi & Sumber

Synthesis reference: Gerhard R. Reuther, "Process for the preparation of pilocarpine from in vitro cultures of pilocarpus." U.S. Patent US5059531, issued June, 1987.
Artikel (PubMed)
  • PMID: 32310588
    Panarese V, Moshirfar M: Pilocarpine. .
  • PMID: 7705213
    Wiseman LR, Faulds D: Oral pilocarpine: a review of its pharmacological properties and clinical potential in xerostomia. Drugs. 1995 Jan;49(1):143-55. doi: 10.2165/00003495-199549010-00010.
  • PMID: 28893976
    Pronin AN, Wang Q, Slepak VZ: Teaching an Old Drug New Tricks: Agonism, Antagonism, and Biased Signaling of Pilocarpine through M3 Muscarinic Acetylcholine Receptor. Mol Pharmacol. 2017 Nov;92(5):601-612. doi: 10.1124/mol.117.109678. Epub 2017 Sep 11.
  • PMID: 9257905
    Belmonte KE, Jacoby DB, Fryer AD: Increased function of inhibitory neuronal M2 muscarinic receptors in diabetic rat lungs. Br J Pharmacol. 1997 Aug;121(7):1287-94. doi: 10.1038/sj.bjp.0701274.
  • PMID: 21521796
    Hioki T, Fukami T, Nakajima M, Yokoi T: Human paraoxonase 1 is the enzyme responsible for pilocarpine hydrolysis. Drug Metab Dispos. 2011 Aug;39(8):1345-52. doi: 10.1124/dmd.111.038141. Epub 2011 Apr 26.
  • PMID: 17178767
    Endo T, Ban M, Hirata K, Yamamoto A, Hara Y, Momose Y: Involvement of CYP2A6 in the formation of a novel metabolite, 3-hydroxypilocarpine, from pilocarpine in human liver microsomes. Drug Metab Dispos. 2007 Mar;35(3):476-83. doi: 10.1124/dmd.106.013425. Epub 2006 Dec 18.

Contoh Produk & Brand

Produk: 128 • International brands: 5
Produk
  • Betoptic Pilo
    Kit • - • Ophthalmic • US • Approved
  • Betoptic/pilo
    Suspension • - • Ophthalmic • Canada • Approved
  • E-pilo 1 Ophthalmic Solution
    Solution / drops • - • Ophthalmic • Canada • Approved
  • E-pilo 2 Ophthalmic Solution
    Solution / drops • - • Ophthalmic • Canada • Approved
  • E-pilo 4 Ophthalmic Solution
    Solution / drops • - • Ophthalmic • Canada • Approved
  • E-pilo 6 Ophthalmic Solution
    Solution / drops • - • Ophthalmic • Canada • Approved
  • E-pilo-1 Oph Soln
    Solution / drops • - • Ophthalmic • Canada • Approved
  • E-pilo-2 Oph Soln
    Solution / drops • - • Ophthalmic • Canada • Approved
Menampilkan 8 dari 128 produk.
International Brands
  • Diocarpine
  • Miocarpine
  • Pilostat
  • Pilovisc
  • Timpilo

Sekuens Gen/Protein (FASTA)

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