Peringatan Keamanan

Oral LD50 is 540 mg/kg in rats and 350 mg/kg in mice.L32499 There is limited information on drotaverine overdose and toxicity.

Drotaverine

DB06751

small molecule approved investigational

Deskripsi

Drotaverine is an antispasmodic drug that works by inhibiting phosphodiesterase-4 (PDE4).A231619 It is a benzylisoquinoline derivative that is structurally related to papaverine, although it displays more potent antispasmodic activities than papaverine. Drotaverine has been used in the symptomatic treatment of various spastic conditions, such as gastrointestinal diseases, biliary dyskinesia, and vasomotor diseases associated with smooth muscle spasms.A7036 It also has been investigated in dysmenorrhea, abortion, A231609 and augmentation of labour.A231614 More recently, drotaverine gained attention in the treatment of benign prostatic hyperplasia, parainfluenza, and avian influenza viruses.A231619

Drotaverine is not approved by the FDA, European Medicines Agency, or Health Canada. It is approved for use in Thailand as oral tablets or intramuscular injections.L22689

Struktur Molekul 2D

Berat 397.5072
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following oral administration of a single 80 mg dose, the mean half-life was 9.11 ± 1.29 hours. Following an intravenous dose of 80 mg, the mean half-life 9.33 ± 1.02 hours.[A7036]
Volume Distribusi Following oral administration of a single 80 mg dose, the mean volume of distribution was 193 ± 48 L. Following an intravenous dose of 80 mg, the mean volume of distribution was 195 ± 48 L.[A7036]
Klirens (Clearance) Following oral administration of a single 80 mg dose, the mean renal clearance was 0.59 ± 0.18 mL/min. Following an intravenous dose of 80 mg, the mean renal clearance was 0.73 ± 0.29 mL/min.[A7036]

Absorpsi

Drotaverine is not completely absorbed following oral administration and its bioavailability is highly variable. Following oral administration of a single 80 mg dose, the absolute bioavailability ranged between 24.5 and 91 % with a mean of 58.2 ± 18.2%. Mean Cmax was 292 ± 88 ng/mL. Mean AUC was 3251 ± 950 ng*h/mL. Mean Tmax was 1.9 ± 0.54 hours.A7036

Metabolisme

Drotaverine is reported to undergo extensive hepatic metabolism, which is its main route of elimination. It may also undergo biliary excretion to form conjugated metabolites.A7036 Proposed metabolic pathways and metabolites are based on limited animal studies: in rats, the major identified metabolites of drotaverine are 4'-desethyl-drotaverine, 6-desethyl-drotaverine, drotaveraldine, and 4'-desethyl-drotaveraldine, all of which are glucuronidated in the bile. 4'-desethyl-drotaveraldine was the most predominant metabolite eliminated into the bile.A231634

Rute Eliminasi

Drotaverine is mainly eliminated via hepatic metabolism.A7036 About 67% of the drug is found in feces and 20% of the drug was eliminated with urine.A231644

Interaksi Obat

4 Data
Riociguat Drotaverine may increase the hypotensive activities of Riociguat.
Patent Blue The therapeutic efficacy of Drotaverine can be decreased when used in combination with Patent Blue.
Isosorbide mononitrate Drotaverine may increase the vasodilatory activities of Isosorbide mononitrate.
Iloprost Iloprost may increase the hypotensive activities of Drotaverine.

Target Protein

3',5'-cyclic-AMP phosphodiesterase 4A PDE4A
Voltage-dependent L-type calcium channel CACNA1C

Referensi & Sumber

Artikel (PubMed)
  • PMID: 8980918
    Bolaji OO, Onyeji CO, Ogundaini AO, Olugbade TA, Ogunbona FA: Pharmacokinetics and bioavailability of drotaverine in humans. Eur J Drug Metab Pharmacokinet. 1996 Jul-Sep;21(3):217-21.
  • PMID: 25434320
    Rai RR, Dwivedi M, Kumar N: Efficacy and safety of drotaverine hydrochloride in irritable bowel syndrome: a randomized double-blind placebo-controlled study. Saudi J Gastroenterol. 2014 Nov-Dec;20(6):378-82. doi: 10.4103/1319-3767.145331.
  • PMID: 26185766
    Tomaszewski D, Balkota M: Intramuscular Administration of Drotaverine Hydrochloride Decreases Both Incidence of Urinary Retention and Time to Micturition in Orthopedic Patients under Spinal Anesthesia: A Single Blinded Randomized Study. Biomed Res Int. 2015;2015:926953. doi: 10.1155/2015/926953. Epub 2015 Jun 21.
  • PMID: 19644697
    Madhu C, Mahavarkar S, Bhave S: A randomised controlled study comparing Drotaverine hydrochloride and Valethamate bromide in the augmentation of labour. Arch Gynecol Obstet. 2010 Jul;282(1):11-5. doi: 10.1007/s00404-009-1188-8. Epub 2009 Jul 31.
  • PMID: 27879007
    Pavel IZ, Heller L, Sommerwerk S, Loesche A, Al-Harrasi A, Csuk R: Drotaverine - a Concealed Cytostatic! Arch Pharm (Weinheim). 2017 Jan;350(1). doi: 10.1002/ardp.201600289. Epub 2016 Nov 23.
  • PMID: 7398679
    Vargay Z, Simon G, Winter M, Szuts T: Qualitative and quantitative determination of drotaverine metabolites in rat bile. Eur J Drug Metab Pharmacokinet. 1980;5(2):69-74. doi: 10.1007/BF03189448.
  • PMID: 754481
    Magyar K, Lengyel M, Knoll J: Absorption, distribution and elimination of drotaverine. Acta Physiol Acad Sci Hung. 1978;51(4):401-11.
  • PMID: 27738091
    Patai Z, Guttman A, Mikus EG: Potential L-Type Voltage-Operated Calcium Channel Blocking Effect of Drotaverine on Functional Models. J Pharmacol Exp Ther. 2016 Dec;359(3):442-451. doi: 10.1124/jpet.116.237271. Epub 2016 Oct 13.

Contoh Produk & Brand

Produk: 0 • International brands: 3
International Brands
  • Drotin
  • No-Spa — Sanofi-Aventis
  • Taverin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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