Peringatan Keamanan

The oral LD50 of benztropine is reported to be of 940 mg/kg in rats.MSDS In the presence of overdose with benztropine, it has been observed symptoms of circulatory collapse, cardiac arrest, respiratory depression, respiratory arrest, psychosis, shock, coma, seizure, ataxia, combativeness, anhidrosis, hyperthermia, fever, dysphagia, decreased bowel sounds and sluggish pupils.F3682

Benzatropine

DB00245

small molecule approved

Deskripsi

Benztropine, with the chemical formula 3alpha-diphenylmethoxytropane, is a tropane-based dopamine inhibitor used for the symptomatic treatment of Parkinson's disease. It is a combination molecule between a tropane ring, similar to cocaine, and a diphenyl ether from the dialkylpiperazines determined to be a dopamine uptake inhibitor since 1970. The generation of structure-activity relationships proved that benztropine derivatives with the presence of a chlorine substituent in the para position in one of the phenyl rings produces an increased potency for dopamine uptake inhibition as well as a decreased inhibition of serotonin and norepinephrine.A37914 Benztropine was developed by USL Pharma and officially approved by the FDA on 1996.L5500

Struktur Molekul 2D

Berat 307.4293
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 of benztropine is very variable and it is reported to be of around 36 hours.[F3682]
Volume Distribusi Benztropine is expected to present a large volume of distribution between 12-30 L/kg.[A175126]
Klirens (Clearance) Extensive pharmacodynamic or pharmacokinetic studies have not been performed.

Absorpsi

Oral administration of 1.5 mg of benztropine is slowly absorbed in the gastrointestinal tract and it reaches a peak concentration of 2.5 ng/ml in about 7 hours.A175087 It has an approximate oral bioavailability of 29%.T445

Metabolisme

Benztropine has been shown to undergo metabolism mainly marked by N-oxidation, N-dealkylation and ring hydroxylation.A175087 The extensive metabolism of benztropine produces eight phase-I metabolites plus four glucuronide conjugates.A1628

Rute Eliminasi

Benztropine is mainly excreted in the urine but it is also found in the feces unchanged.A1628

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with food. Food reduces irritation.

Interaksi Obat

1588 Data
Aclidinium The risk or severity of adverse effects can be increased when Benzatropine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Benzatropine.
Mirabegron The risk or severity of urinary retention can be increased when Benzatropine is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Benzatropine is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Benzatropine.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Benzatropine.
Tiotropium The risk or severity of adverse effects can be increased when Benzatropine is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Benzatropine is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Benzatropine is combined with Umeclidinium.
Ioflupane I-123 Benzatropine may decrease effectiveness of Ioflupane I-123 as a diagnostic agent.
Methylphenidate The risk or severity of adverse effects can be increased when Methylphenidate is combined with Benzatropine.
Dexmethylphenidate The risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with Benzatropine.
Benzylpenicilloyl polylysine Benzatropine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Benzatropine.
Hyaluronidase (ovine) The therapeutic efficacy of Hyaluronidase (ovine) can be decreased when used in combination with Benzatropine.
Hyaluronidase (human recombinant) The therapeutic efficacy of Hyaluronidase (human recombinant) can be decreased when used in combination with Benzatropine.
Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Benzatropine.
Glycopyrronium The risk or severity of adverse effects can be increased when Benzatropine is combined with Glycopyrronium.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Benzatropine is combined with Botulinum toxin type A.
Glucagon Benzatropine may increase the gastrointestinal motility reducing activities of Glucagon.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Benzatropine is combined with Botulinum toxin type B.
Eluxadoline The risk or severity of constipation can be increased when Benzatropine is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Benzatropine is combined with Ramosetron.
Amphetamine Amphetamine may decrease the sedative activities of Benzatropine.
Phentermine Phentermine may decrease the sedative activities of Benzatropine.
Pseudoephedrine Pseudoephedrine may decrease the sedative activities of Benzatropine.
Benzphetamine Benzphetamine may decrease the sedative activities of Benzatropine.
Diethylpropion Diethylpropion may decrease the sedative activities of Benzatropine.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Benzatropine.
Mephentermine Mephentermine may decrease the sedative activities of Benzatropine.
MMDA MMDA may decrease the sedative activities of Benzatropine.
Midomafetamine Midomafetamine may decrease the sedative activities of Benzatropine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Benzatropine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Benzatropine.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Benzatropine.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Benzatropine.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Benzatropine.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Benzatropine.
Metamfetamine Metamfetamine may decrease the sedative activities of Benzatropine.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Benzatropine.
Ritobegron Ritobegron may decrease the sedative activities of Benzatropine.
Mephedrone Mephedrone may decrease the sedative activities of Benzatropine.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Benzatropine.
Gepefrine Gepefrine may decrease the sedative activities of Benzatropine.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Benzatropine.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Benzatropine.
Naltrexone The risk or severity of adverse effects can be increased when Benzatropine is combined with Naltrexone.
Bezitramide The risk or severity of adverse effects can be increased when Benzatropine is combined with Bezitramide.
Tramadol The risk or severity of adverse effects can be increased when Benzatropine is combined with Tramadol.
Morphine The risk or severity of adverse effects can be increased when Benzatropine is combined with Morphine.
Hydromorphone The risk or severity of adverse effects can be increased when Benzatropine is combined with Hydromorphone.
Oxycodone The risk or severity of adverse effects can be increased when Benzatropine is combined with Oxycodone.
Butorphanol The risk or severity of adverse effects can be increased when Benzatropine is combined with Butorphanol.
Pentazocine The risk or severity of adverse effects can be increased when Benzatropine is combined with Pentazocine.
Sufentanil The risk or severity of adverse effects can be increased when Benzatropine is combined with Sufentanil.
Alfentanil The risk or severity of adverse effects can be increased when Benzatropine is combined with Alfentanil.
Nalbuphine The risk or severity of adverse effects can be increased when Benzatropine is combined with Nalbuphine.
Levorphanol The risk or severity of adverse effects can be increased when Benzatropine is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Benzatropine is combined with Remifentanil.
Buprenorphine The risk or severity of adverse effects can be increased when Benzatropine is combined with Buprenorphine.
Hydrocodone The risk or severity of adverse effects can be increased when Benzatropine is combined with Hydrocodone.
Diphenoxylate The risk or severity of adverse effects can be increased when Benzatropine is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Benzatropine is combined with Oxymorphone.
Dezocine The risk or severity of adverse effects can be increased when Benzatropine is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Benzatropine is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Benzatropine is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Benzatropine is combined with Diamorphine.
Ethylmorphine The risk or severity of adverse effects can be increased when Benzatropine is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Benzatropine is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Benzatropine is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Benzatropine is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Benzatropine is combined with Carfentanil.
Dihydrocodeine The risk or severity of adverse effects can be increased when Benzatropine is combined with Dihydrocodeine.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Benzatropine is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Benzatropine is combined with Dihydromorphine.
Ketobemidone The risk or severity of adverse effects can be increased when Benzatropine is combined with Ketobemidone.
DPDPE The risk or severity of adverse effects can be increased when Benzatropine is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Benzatropine is combined with Lofentanil.
Opium The risk or severity of adverse effects can be increased when Benzatropine is combined with Opium.
Normethadone The risk or severity of adverse effects can be increased when Benzatropine is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Benzatropine is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Benzatropine is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Benzatropine is combined with Nicomorphine.
Meptazinol The risk or severity of adverse effects can be increased when Benzatropine is combined with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Benzatropine is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Benzatropine is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Benzatropine is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Benzatropine is combined with Carfentanil, C-11.
Levacetylmethadol The risk or severity of adverse effects can be increased when Benzatropine is combined with Levacetylmethadol.
Codeine The risk or severity of adverse effects can be increased when Benzatropine is combined with Codeine.
Fentanyl The risk or severity of adverse effects can be increased when Benzatropine is combined with Fentanyl.
Methadone The risk or severity of adverse effects can be increased when Benzatropine is combined with Methadone.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Benzatropine is combined with Dextropropoxyphene.
Tapentadol The risk or severity of urinary retention and constipation can be increased when Benzatropine is combined with Tapentadol.
Meperidine The risk or severity of adverse effects can be increased when Benzatropine is combined with Meperidine.
Benzhydrocodone The risk or severity of adverse effects can be increased when Benzatropine is combined with Benzhydrocodone.
Naloxegol The risk or severity of adverse effects can be increased when Benzatropine is combined with Naloxegol.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Benzatropine.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Benzatropine.
Metixene The risk or severity of adverse effects can be increased when Benzatropine is combined with Metixene.

Target Protein

Muscarinic acetylcholine receptor M1 CHRM1
Sodium-dependent dopamine transporter SLC6A3
Histamine H1 receptor HRH1
Sodium-dependent serotonin transporter SLC6A4
Sodium-dependent noradrenaline transporter SLC6A2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17897630
    Rothman RB, Baumann MH, Prisinzano TE, Newman AH: Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addiction. Biochem Pharmacol. 2008 Jan 1;75(1):2-16. doi: 10.1016/j.bcp.2007.08.007. Epub 2007 Aug 9.
  • PMID: 25548026
    Reith ME, Blough BE, Hong WC, Jones KT, Schmitt KC, Baumann MH, Partilla JS, Rothman RB, Katz JL: Behavioral, biological, and chemical perspectives on atypical agents targeting the dopamine transporter. Drug Alcohol Depend. 2015 Feb 1;147:1-19. doi: 10.1016/j.drugalcdep.2014.12.005. Epub 2014 Dec 18.
  • PMID: 10952768
    Brocks DR: Anticholinergic drugs used in Parkinson's disease: An overlooked class of drugs from a pharmacokinetic perspective. J Pharm Pharm Sci. 1999 May-Aug;2(2):39-46.
  • PMID: 1359485
    Blair DT, Dauner A: Extrapyramidal symptoms are serious side-effects of antipsychotic and other drugs. Nurse Pract. 1992 Nov;17(11):56, 62-4, 67.
  • PMID: 11978145
    Deleu D, Northway MG, Hanssens Y: Clinical pharmacokinetic and pharmacodynamic properties of drugs used in the treatment of Parkinson's disease. Clin Pharmacokinet. 2002;41(4):261-309.
  • PMID: 12966155
    Raje S, Cao J, Newman AH, Gao H, Eddington ND: Evaluation of the blood-brain barrier transport, population pharmacokinetics, and brain distribution of benztropine analogs and cocaine using in vitro and in vivo techniques. J Pharmacol Exp Ther. 2003 Nov;307(2):801-8. doi: 10.1124/jpet.103.053504. Epub 2003 Sep 9.
Textbook
  • Troy B. and Beringer P. (2006). Remington: The Science and Practice of Pharmacy (21st ed.). Lippincott Williams & Wilkins.
  • ISBN: 978-0-8261-2858-4
    Hale T. and Rowe H. (2017). MEdications & mothers' milk (17th ed.). Springer publishing company.

Contoh Produk & Brand

Produk: 229 • International brands: 3
Produk
  • Bensylate Tab 2mg
    Tablet • 2 mg • Oral • Canada • Approved
  • Benztropine
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
  • Benztropine
    Solution • 2 mg / 2 mL • Intramuscular; Intravenous • Canada • Approved
  • Benztropine 2 Tab 2mg
    Tablet • 2 mg • Oral • Canada • Approved
  • Benztropine mesylate
    Tablet • 0.5 mg/1 • Oral • US • Generic • Approved
  • Benztropine mesylate
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
  • Benztropine mesylate
    Tablet • 2 mg/1 • Oral • US • Generic • Approved
  • Benztropine Mesylate
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 229 produk.
International Brands
  • Apo-Benztropine — Apotex
  • Cogentinol — Astra (Germany, discontinued)
  • PMS Benztropine — Pharmascience

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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