Peringatan Keamanan

Preclinical studies related to the blocking of NMDA receptors have shown an increase in apoptosis in the developing brain which results in cognitive deficits when used for longer than 3 hours. Toxicity studies regarding carcinogenesis have not been performed. Regarding mutagenesis and fertility, ketamine showed to be clastogenic and to not have effects on fertility.FDA label

Ketamine

DB01221

small molecule approved vet_approved

Deskripsi

Ketamine is an NMDA receptor antagonist with a potent anesthetic effect.A31869 It was developed in 1963 as a replacement for phencyclidine (PCP) by Calvin Stevens at Parke Davis Laboratories. It started being used for veterinary purposes in Belgium and in 1964 was proven that compared to PCP, it produced minor hallucinogenic effects and shorter psychotomimetic effects. It was FDA approved in 1970, and from there, it has been used as an anesthetic for children or patients undergoing minor surgeries but mainly for veterinary purposes.L1332

Struktur Molekul 2D

Berat 237.725
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The reported half-life in preclinical studies for ketamine is 186 min.[A31883]
Volume Distribusi The apparent volume of distribution of the central compartment and at steady-state are 371.3 ml/kg and 4060.3 ml/kg, respectively.[A31889]
Klirens (Clearance) The clearance rate of ketamine is high and of around 95 L/h/70kg.[A31885]

Absorpsi

Ketamine absorption is very rapid and the bioavailability is around 93%. After the first pass metabolism, only 17% of the administered dose is absorbed.A31883 It distributes very rapidly and presents a distribution half-life of 1.95 min.A31887 The Cmax levels at peak reach 0.75 mcg/ml in plasma and 0.2 mcg/ml in cerebrospinal fluid.L1336

Metabolisme

Ketamine presents a mainly hepatic metabolism and its major metabolite is norketamine. The biotransformation of ketamine corresponds to N-dealkylation, hydroxylation of the cyclohexone ring, conjugation to glucuronic acid and dehydration of the hydroxylated metabolites for the formation of cyclohexene derivatives.A31883

Rute Eliminasi

Pharmacokinetic studies have resulted in the recovery of 85-95% of the administered dose in urine mainly in the form of metabolites. Some other routes of elimination of ketamine are bile and feces. When administered intravenously the resultant recovery is distributed by 91% of the administered dose in urine and 3% in feces.L1336

Interaksi Makanan

1 Data
  • 1. Avoid alcohol.

Interaksi Obat

1850 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Ketamine.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Ketamine.
Buprenorphine Ketamine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Ketamine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Ketamine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Ketamine.
Hydrocodone Ketamine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Ketamine.
Magnesium sulfate The therapeutic efficacy of Ketamine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Ketamine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Ketamine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Ketamine.
Mirtazapine Ketamine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Ketamine.
Orphenadrine Ketamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Ketamine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole Ketamine may increase the sedative activities of Pramipexole.
Ropinirole Ketamine may increase the sedative activities of Ropinirole.
Rotigotine Ketamine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Ketamine.
Sodium oxybate The risk or severity of CNS depression can be increased when Ketamine is combined with Sodium oxybate.
Suvorexant Ketamine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Ketamine.
Thalidomide Ketamine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Ketamine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Ketamine.
Mifepristone The serum concentration of Ketamine can be increased when it is combined with Mifepristone.
Memantine The risk or severity of adverse effects can be increased when Ketamine is combined with Memantine.
Dipyridamole The therapeutic efficacy of Ketamine can be decreased when used in combination with Dipyridamole.
Ephedrine Ketamine may increase the neuromuscular blocking activities of Ephedrine.
Bambuterol Ketamine may increase the neuromuscular blocking activities of Bambuterol.
Sar9, Met (O2)11-Substance P Ketamine may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P.
Procaine Ketamine may increase the neuromuscular blocking activities of Procaine.
Cocaine Ketamine may increase the neuromuscular blocking activities of Cocaine.
Trimethaphan Ketamine may increase the neuromuscular blocking activities of Trimethaphan.
Doxacurium Ketamine may increase the neuromuscular blocking activities of Doxacurium.
Chloroprocaine Ketamine may increase the neuromuscular blocking activities of Chloroprocaine.
Tubocurarine Ketamine may increase the neuromuscular blocking activities of Tubocurarine.
Aclidinium Ketamine may increase the neuromuscular blocking activities of Aclidinium.
Propacetamol Ketamine may increase the neuromuscular blocking activities of Propacetamol.
Clevidipine Ketamine may increase the neuromuscular blocking activities of Clevidipine.
Mirabegron Ketamine may increase the neuromuscular blocking activities of Mirabegron.
Moxisylyte Ketamine may increase the neuromuscular blocking activities of Moxisylyte.
Butyrylthiocholine Ketamine may increase the neuromuscular blocking activities of Butyrylthiocholine.
Oxybuprocaine Ketamine may increase the neuromuscular blocking activities of Oxybuprocaine.
Benzonatate Ketamine may increase the neuromuscular blocking activities of Benzonatate.
Irinotecan The metabolism of Ketamine can be decreased when combined with Irinotecan.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Ketamine.
Perampanel The metabolism of Perampanel can be increased when combined with Ketamine.
Warfarin The metabolism of Warfarin can be increased when combined with Ketamine.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Ketamine.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Ketamine.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Ketamine.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Ketamine.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Ketamine.
Succinylcholine The metabolism of Succinylcholine can be decreased when combined with Ketamine.
Ethanol Ketamine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Ketamine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Ketamine.
Fluvoxamine The risk or severity of adverse effects can be increased when Ketamine is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Ketamine is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Ketamine is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Ketamine is combined with Trazodone.
Sibutramine The risk or severity of adverse effects can be increased when Ketamine is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Ketamine is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Ketamine is combined with Dapoxetine.
Desvenlafaxine The risk or severity of adverse effects can be increased when Ketamine is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Ketamine is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Ketamine is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Ketamine is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Ketamine is combined with Alaproclate.
Escitalopram The risk or severity of adverse effects can be increased when Ketamine is combined with Escitalopram.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Ketamine.
Mecamylamine The therapeutic efficacy of Mecamylamine can be decreased when used in combination with Ketamine.
Amantadine The therapeutic efficacy of Amantadine can be decreased when used in combination with Ketamine.
Pentolinium The therapeutic efficacy of Pentolinium can be decreased when used in combination with Ketamine.
Fenoterol The therapeutic efficacy of Fenoterol can be decreased when used in combination with Ketamine.
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione The therapeutic efficacy of Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione can be decreased when used in combination with Ketamine.
Agmatine The therapeutic efficacy of Agmatine can be decreased when used in combination with Ketamine.
Esmolol Ketamine may increase the bradycardic activities of Esmolol.
Betaxolol Ketamine may increase the bradycardic activities of Betaxolol.
Atenolol Ketamine may increase the bradycardic activities of Atenolol.
Sotalol Ketamine may increase the bradycardic activities of Sotalol.
Acebutolol Ketamine may increase the bradycardic activities of Acebutolol.
Bevantolol Ketamine may increase the bradycardic activities of Bevantolol.
Practolol Ketamine may increase the bradycardic activities of Practolol.
Dexpropranolol Ketamine may increase the bradycardic activities of Dexpropranolol.
Celiprolol Ketamine may increase the bradycardic activities of Celiprolol.
Bufuralol Ketamine may increase the bradycardic activities of Bufuralol.
Bopindolol Ketamine may increase the bradycardic activities of Bopindolol.
Bupranolol Ketamine may increase the bradycardic activities of Bupranolol.
Indenolol Ketamine may increase the bradycardic activities of Indenolol.
Levobetaxolol Ketamine may increase the bradycardic activities of Levobetaxolol.
Talinolol Ketamine may increase the bradycardic activities of Talinolol.
Anisodamine Ketamine may increase the bradycardic activities of Anisodamine.
Bucindolol Ketamine may increase the bradycardic activities of Bucindolol.
Esatenolol Ketamine may increase the bradycardic activities of Esatenolol.
Cloranolol Ketamine may increase the bradycardic activities of Cloranolol.
Mepindolol Ketamine may increase the bradycardic activities of Mepindolol.
Epanolol Ketamine may increase the bradycardic activities of Epanolol.

Target Protein

Glutamate receptor ionotropic, NMDA 3A GRIN3A
5-hydroxytryptamine receptor 3A HTR3A
Neuronal acetylcholine receptor subunit alpha-7 CHRNA7
Cholinesterase BCHE
Nitric oxide synthase 1 NOS1
Substance-P receptor TACR1
D(2) dopamine receptor DRD2
Delta-type opioid receptor OPRD1
Sodium-dependent noradrenaline transporter SLC6A2
Kappa-type opioid receptor OPRK1
Mu-type opioid receptor OPRM1
Muscarinic acetylcholine receptor CHRM1
5-hydroxytryptamine receptor 2 HTR2A
5-hydroxytryptamine receptor 1 HTR1A

Referensi & Sumber

Synthesis reference: John A. Flores, Kenton L. Crowley, "Process for the preparation of ketamine ointment." U.S. Patent US5817699, issued June, 1995.
Artikel (PubMed)
  • PMID: 2858237
    Harrison NL, Simmonds MA: Quantitative studies on some antagonists of N-methyl D-aspartate in slices of rat cerebral cortex. Br J Pharmacol. 1985 Feb;84(2):381-91.
  • PMID: 10551055
    Bergman SA: Ketamine: review of its pharmacology and its use in pediatric anesthesia. Anesth Prog. 1999 Winter;46(1):10-20.
  • PMID: 12091028
    Bonanno FG: Ketamine in war/tropical surgery (a final tribute to the racemic mixture). Injury. 2002 May;33(4):323-7.
  • PMID: 16979848
    Lankenau SE, Sanders B, Bloom JJ, Hathazi D, Alarcon E, Tortu S, Clatts MC: First injection of ketamine among young injection drug users (IDUs) in three U.S. cities. Drug Alcohol Depend. 2007 Mar 16;87(2-3):183-93. Epub 2006 Sep 18.
  • PMID: 10228376
    Reboso Morales JA, Gonzalez Miranda F: Ketamine. Rev Esp Anestesiol Reanim. 1999 Mar;46(3):111-22.
  • PMID: 12768186
    Ivani G, Vercellino C, Tonetti F: Ketamine: a new look to an old drug. Minerva Anestesiol. 2003 May;69(5):468-71.
  • PMID: 29446381
    Yang Y, Cui Y, Sang K, Dong Y, Ni Z, Ma S, Hu H: Ketamine blocks bursting in the lateral habenula to rapidly relieve depression. Nature. 2018 Feb 14;554(7692):317-322. doi: 10.1038/nature25509.
  • PMID: 26360893
    Kirby T: Ketamine for depression: the highs and lows. Lancet Psychiatry. 2015 Sep;2(9):783-4. doi: 10.1016/S2215-0366(15)00392-2.
Menampilkan 8 dari 13 artikel.

Contoh Produk & Brand

Produk: 62 • International brands: 2
Produk
  • Ketalar
    Injection • 10 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Ketalar
    Injection • 50 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Ketalar
    Injection • 100 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Ketalar
    Injection • 10 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Ketalar
    Injection • 50 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Ketalar
    Injection • 100 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Ketalar
    Injection • 10 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Ketalar
    Solution • 50 mg / mL • Intramuscular; Intravenous • Canada • Approved
Menampilkan 8 dari 62 produk.
International Brands
  • Ketaject — Bristol-Myers Squibb
  • Ketanest — Parke Davis

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