Peringatan Keamanan

Intense agitation, convulsions, hypertension, rhythm disturbance, coronary insufficiency, hyperthermia, rhabdomyolysis, and renal impairment. Oral mouse LD50 = 96 mg/kg

Cocaine

DB00907

small molecule approved illicit

Deskripsi

An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.

Struktur Molekul 2D

Berat 303.3529
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 1 hour
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Cocaine is absorbed from all sites of application, including mucous membranes and gastrointestinal mucosa. By oral or intra-nasal route, 60 to 80% of cocaine is absorbed.

Metabolisme

Hepatic. Cocaine is metabolized to benzoylecgonine and ecgonine methyl ester, which are both excreted in the urine. In the presence of alcohol, a further active metabolite, cocaethylene is formed, and is more toxic then cocaine itself.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

1899 Data
Aclidinium The risk or severity of adverse effects can be increased when Cocaine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Cocaine.
Mirabegron The risk or severity of urinary retention can be increased when Cocaine is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Cocaine is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Cocaine.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Cocaine.
Tiotropium The risk or severity of adverse effects can be increased when Cocaine is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Cocaine is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Cocaine is combined with Umeclidinium.
Dronabinol Cocaine may increase the tachycardic activities of Dronabinol.
Nabilone Cocaine may increase the tachycardic activities of Nabilone.
SLV319 Cocaine may increase the tachycardic activities of SLV319.
Rimonabant Cocaine may increase the tachycardic activities of Rimonabant.
Taranabant Cocaine may increase the tachycardic activities of Taranabant.
GW842166 Cocaine may increase the tachycardic activities of GW842166.
Lenabasum Cocaine may increase the tachycardic activities of Ajulemic acid.
Ibipinabant Cocaine may increase the tachycardic activities of Ibipinabant.
Surinabant Cocaine may increase the tachycardic activities of Surinabant.
WIN 55212-2 Cocaine may increase the tachycardic activities of WIN 55212-2.
Nabiximols Cocaine may increase the tachycardic activities of Nabiximols.
Palmidrol Cocaine may increase the tachycardic activities of Palmidrol.
Cannabinol Cocaine may increase the tachycardic activities of Cannabinol.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Cocaine.
Glycopyrronium The risk or severity of adverse effects can be increased when Cocaine is combined with Glycopyrronium.
Pegvisomant Pegvisomant may increase the neuromuscular blocking activities of Cocaine.
Mefloquine The risk or severity of methemoglobinemia can be increased when Mefloquine is combined with Cocaine.
Tacrine Tacrine may increase the neuromuscular blocking activities of Cocaine.
Profenamine Profenamine may increase the neuromuscular blocking activities of Cocaine.
Gallamine triethiodide Gallamine triethiodide may increase the neuromuscular blocking activities of Cocaine.
Triflupromazine Triflupromazine may increase the neuromuscular blocking activities of Cocaine.
Cisplatin The risk or severity of methemoglobinemia can be increased when Cisplatin is combined with Cocaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Cinchocaine is combined with Cocaine.
Pyridostigmine Pyridostigmine may increase the neuromuscular blocking activities of Cocaine.
Nizatidine Nizatidine may increase the neuromuscular blocking activities of Cocaine.
Galantamine Galantamine may increase the neuromuscular blocking activities of Cocaine.
Isoflurophate Isoflurophate may increase the neuromuscular blocking activities of Cocaine.
Diethylcarbamazine Diethylcarbamazine may increase the neuromuscular blocking activities of Cocaine.
Procaine The risk or severity of methemoglobinemia can be increased when Procaine is combined with Cocaine.
Minaprine Minaprine may increase the neuromuscular blocking activities of Cocaine.
Mechlorethamine The risk or severity of methemoglobinemia can be increased when Mechlorethamine is combined with Cocaine.
Hexafluronium Hexafluronium may increase the neuromuscular blocking activities of Cocaine.
Demecarium Demecarium may increase the neuromuscular blocking activities of Cocaine.
Physostigmine Physostigmine may increase the neuromuscular blocking activities of Cocaine.
Rivastigmine Rivastigmine may increase the neuromuscular blocking activities of Cocaine.
Edrophonium Edrophonium may increase the neuromuscular blocking activities of Cocaine.
Memantine Memantine may increase the neuromuscular blocking activities of Cocaine.
Ambenonium Ambenonium may increase the neuromuscular blocking activities of Cocaine.
Tubocurarine Tubocurarine may increase the neuromuscular blocking activities of Cocaine.
Ketamine Ketamine may increase the neuromuscular blocking activities of Cocaine.
Decamethonium Decamethonium may increase the neuromuscular blocking activities of Cocaine.
Pancuronium Pancuronium may increase the neuromuscular blocking activities of Cocaine.
Pipecuronium Pipecuronium may increase the neuromuscular blocking activities of Cocaine.
Ginkgo biloba Ginkgo biloba may increase the neuromuscular blocking activities of Cocaine.
Neostigmine Neostigmine may increase the neuromuscular blocking activities of Cocaine.
Bambuterol Bambuterol may increase the neuromuscular blocking activities of Cocaine.
1,10-Phenanthroline 1,10-Phenanthroline may increase the neuromuscular blocking activities of Cocaine.
Thiotepa The risk or severity of methemoglobinemia can be increased when Thiotepa is combined with Cocaine.
Huperzine A Huperzine A may increase the neuromuscular blocking activities of Cocaine.
Phenserine Phenserine may increase the neuromuscular blocking activities of Cocaine.
Regramostim Regramostim may increase the neuromuscular blocking activities of Cocaine.
Aprotinin Aprotinin may increase the neuromuscular blocking activities of Cocaine.
Betaine Betaine may increase the neuromuscular blocking activities of Cocaine.
Capsaicin The risk or severity of methemoglobinemia can be increased when Cocaine is combined with Capsaicin.
Coumaphos Coumaphos may increase the neuromuscular blocking activities of Cocaine.
Dichlorvos Dichlorvos may increase the neuromuscular blocking activities of Cocaine.
Fenthion Fenthion may increase the neuromuscular blocking activities of Cocaine.
Metrifonate Metrifonate may increase the neuromuscular blocking activities of Cocaine.
Acotiamide Acotiamide may increase the neuromuscular blocking activities of Cocaine.
Methanesulfonyl Fluoride Methanesulfonyl Fluoride may increase the neuromuscular blocking activities of Cocaine.
Paraoxon Paraoxon may increase the neuromuscular blocking activities of Cocaine.
Tyrothricin The risk or severity of methemoglobinemia can be increased when Tyrothricin is combined with Cocaine.
Ipidacrine Ipidacrine may increase the neuromuscular blocking activities of Cocaine.
Distigmine Distigmine may increase the neuromuscular blocking activities of Cocaine.
Tretamine The risk or severity of methemoglobinemia can be increased when Tretamine is combined with Cocaine.
Posiphen Posiphen may increase the neuromuscular blocking activities of Cocaine.
Terbutaline Terbutaline may increase the neuromuscular blocking activities of Cocaine.
Methylphosphinic Acid Methylphosphinic Acid may increase the neuromuscular blocking activities of Cocaine.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Cocaine.
Ioflupane I-123 Cocaine may decrease effectiveness of Ioflupane I-123 as a diagnostic agent.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Cocaine is combined with Botulinum toxin type A.
Glucagon Cocaine may increase the gastrointestinal motility reducing activities of Glucagon.
Sulpiride Cocaine may increase the anticholinergic activities of Sulpiride.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Cocaine is combined with Botulinum toxin type B.
Mirtazapine Cocaine may increase the serotonergic activities of Mirtazapine.
Iobenguane The therapeutic efficacy of Iobenguane can be decreased when used in combination with Cocaine.
Eluxadoline The risk or severity of constipation can be increased when Cocaine is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Cocaine is combined with Ramosetron.
Diamorphine The risk or severity of adverse effects can be increased when Cocaine is combined with Diamorphine.
Desomorphine The risk or severity of adverse effects can be increased when Cocaine is combined with Desomorphine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Cocaine is combined with Carfentanil, C-11.
Methadone The risk or severity of adverse effects can be increased when Cocaine is combined with Methadone.
Alfentanil The risk or severity of adverse effects can be increased when Cocaine is combined with Alfentanil.
Fentanyl The risk or severity of adverse effects can be increased when Cocaine is combined with Fentanyl.
Hydromorphone The risk or severity of adverse effects can be increased when Cocaine is combined with Hydromorphone.
Butorphanol The risk or severity of adverse effects can be increased when Cocaine is combined with Butorphanol.
Pentazocine The risk or severity of adverse effects can be increased when Cocaine is combined with Pentazocine.
Naltrexone The risk or severity of adverse effects can be increased when Cocaine is combined with Naltrexone.
Sufentanil The risk or severity of adverse effects can be increased when Cocaine is combined with Sufentanil.
Nalbuphine The risk or severity of adverse effects can be increased when Cocaine is combined with Nalbuphine.
Levorphanol The risk or severity of adverse effects can be increased when Cocaine is combined with Levorphanol.

Target Protein

Sodium-dependent dopamine transporter SLC6A3
Sodium-dependent noradrenaline transporter SLC6A2
Sodium channel protein SCN1A
Sodium-dependent serotonin transporter SLC6A4
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Sigma non-opioid intracellular receptor 1 SIGMAR1
Liver carboxylesterase 1 CES1

Referensi & Sumber

Synthesis reference: Nobuyuki Shigetoh, Hiroshi Nakayama, Jinsei Miyazaki, Tadayasu Mitsumata, "Labelling colors for detecting cocaine or methamphetamine, method of preparing the same and detector for cocaine or methamphetamine." U.S. Patent US5571727, issued October, 1981.
Artikel (PubMed)
  • PMID: 3940302
    Siegel RK, Elsohly MA, Plowman T, Rury PM, Jones RT: Cocaine in herbal tea. JAMA. 1986 Jan 3;255(1):40.
  • PMID: 10983846
    Volkow ND, Wang GJ, Fischman MW, Foltin R, Fowler JS, Franceschi D, Franceschi M, Logan J, Gatley SJ, Wong C, Ding YS, Hitzemann R, Pappas N: Effects of route of administration on cocaine induced dopamine transporter blockade in the human brain. Life Sci. 2000 Aug 11;67(12):1507-15.
  • PMID: 15262059
    Dimitrijevic N, Dzitoyeva S, Manev H: An automated assay of the behavioral effects of cocaine injections in adult Drosophila. J Neurosci Methods. 2004 Aug 30;137(2):181-4.
  • PMID: 12865893
    Uz T, Akhisaroglu M, Ahmed R, Manev H: The pineal gland is critical for circadian Period1 expression in the striatum and for circadian cocaine sensitization in mice. Neuropsychopharmacology. 2003 Dec;28(12):2117-23.
  • PMID: 15967985
    McClung CA, Sidiropoulou K, Vitaterna M, Takahashi JS, White FJ, Cooper DC, Nestler EJ: Regulation of dopaminergic transmission and cocaine reward by the Clock gene. Proc Natl Acad Sci U S A. 2005 Jun 28;102(26):9377-81. Epub 2005 Jun 20.

Contoh Produk & Brand

Produk: 14 • International brands: 0
Produk
  • Cocaine Hydrochloride
    Solution • 40 mg/1mL • Topical • US
  • Cocaine Hydrochloride
    Solution • 100 mg/1mL • Topical • US
  • Cocaine Hydrochloride
    Solution • 40 mg/1mL • Nasal • US • Generic • Approved
  • Cocaine Hydrochloride
    Solution • 40 mg/1mL • Nasal • US • Generic • Approved
  • Cocaine Hydrochloride Nasal
    Solution • 40 mg/1mL • Topical • US • Generic • Approved
  • Cocaine Hydrochloride Nasal
    Solution • 40 mg/1mL • Topical • US • Generic • Approved
  • Cocaine Hydrochloride Top Sol 40mg/ml
    Liquid • 40 mg / mL • Topical • Canada • Approved
  • Cocaine Hydrochloride Topical Sol 10%
    Liquid • 100 mg / mL • Topical • Canada • Approved
Menampilkan 8 dari 14 produk.

Sekuens Gen/Protein (FASTA)

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