Peringatan Keamanan

Overdosage may occur from rapid or repeated injections. Too rapid injection may be followed by an alarming fall in blood pressure even to shock levels. Apnea, occasional laryngospasm, coughing and other respiratory difficulties with excessive or too rapid injections may occur. Lethal blood levels may be as low as 1 mg/100 mL for short-acting barbiturates; less if other depressant drugs or alcohol are also present.

Thiopental

DB00599

small molecule approved vet_approved

Deskripsi

A barbiturate that is administered intravenously for the induction of general anesthesia or for the production of complete anesthesia of short duration. It is also used for hypnosis and for the control of convulsive states. It has been used in neurosurgical patients to reduce increased intracranial pressure. It does not produce any excitation but has poor analgesic and muscle relaxant properties. Small doses have been shown to be anti-analgesic and lower the pain threshold. (From Martindale, The Extra Pharmacopoeia, 30th ed, p920)

Struktur Molekul 2D

Berat 242.338
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 3-8 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Rapidly absorbed.

Metabolisme

Thiopental is extensively metabolized, primarily in the liver, resulting in only 0.3% of an administered dose being excreted unchanged in the urine.L32434 Ring desulfuration leads to the generation of an active metabolite, pentobarbital, that exists in concentrations approximately 3-10% that of the parent concentration.A35309 Thiopental and pentobarbital are also subject to both oxidation and hydroxylation to carboxylic acids and alcohols, respectively, all of which are pharmacologically inert.A35309 While many of the specifics regarding thiopental biotransformation have not been elucidated, including the enzymes responsible, the oxidation of thiopental to its carboxylic acid may be the major driver of thiopental detoxification as this product appears to account for 10-25% of renally excreted drug.A35309

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Additive CNS depression may occur if alcohol is consumed with thiopental.

Interaksi Obat

1433 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Thiopental is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Thiopental is combined with Levodopa.
Risperidone Thiopental may increase the hypotensive activities of Risperidone.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Thiopental.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Thiopental.
Buprenorphine Thiopental 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 Thiopental.
Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Thiopental.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Thiopental.
Hydrocodone Thiopental 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 Thiopental.
Magnesium sulfate The therapeutic efficacy of Thiopental can be increased when used in combination with Magnesium sulfate.
Metyrosine Thiopental may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Thiopental.
Mirtazapine Thiopental 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 Thiopental.
Orphenadrine Thiopental may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Thiopental may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole Thiopental may increase the sedative activities of Pramipexole.
Ropinirole Thiopental may increase the sedative activities of Ropinirole.
Rotigotine Thiopental may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Thiopental.
Suvorexant Thiopental 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 Thiopental.
Thalidomide Thiopental may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Thiopental may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Dabrafenib The serum concentration of Thiopental can be decreased when it is combined with Dabrafenib.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Thiopental.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Thiopental.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Thiopental.
Luliconazole The serum concentration of Thiopental can be increased when it is combined with Luliconazole.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Thiopental.
Colchicine The metabolism of Colchicine can be decreased when combined with Thiopental.
Fentanyl The risk or severity of adverse effects can be increased when Thiopental is combined with Fentanyl.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Thiopental.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Thiopental.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Thiopental.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Thiopental.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Thiopental.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Thiopental.
Mefloquine The therapeutic efficacy of Thiopental can be decreased when used in combination with Mefloquine.
Orlistat Orlistat can cause a decrease in the absorption of Thiopental resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetaminophen The metabolism of Acetaminophen can be increased when combined with Thiopental.
Propacetamol The metabolism of Propacetamol can be increased when combined with Thiopental.
Chloramphenicol The metabolism of Thiopental can be decreased when combined with Chloramphenicol.
Doxycycline The serum concentration of Doxycycline can be decreased when it is combined with Thiopental.
Felbamate The serum concentration of Thiopental can be increased when it is combined with Felbamate.
Griseofulvin The serum concentration of Griseofulvin can be decreased when it is combined with Thiopental.
Lamotrigine The serum concentration of Lamotrigine can be decreased when it is combined with Thiopental.
Mianserin The therapeutic efficacy of Thiopental can be decreased when used in combination with Mianserin.
Methylphenobarbital The risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Thiopental.
Pyridoxine The metabolism of Thiopental can be increased when combined with Pyridoxine.
Teniposide The serum concentration of Teniposide can be decreased when it is combined with Thiopental.
Ulipristal The serum concentration of Ulipristal can be decreased when it is combined with Thiopental.
Voriconazole The serum concentration of Voriconazole can be decreased when it is combined with Thiopental.
Topotecan Thiopental may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Thiopental.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Thiopental.
Sodium oxybate Thiopental may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Thiopental.
Thiethylperazine The risk or severity of adverse effects can be increased when Thiethylperazine is combined with Thiopental.
Promazine The risk or severity of adverse effects can be increased when Promazine is combined with Thiopental.
Prochlorperazine The risk or severity of adverse effects can be increased when Prochlorperazine is combined with Thiopental.
Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Thiopental.
Triflupromazine The risk or severity of adverse effects can be increased when Triflupromazine is combined with Thiopental.
Fluphenazine The risk or severity of adverse effects can be increased when Fluphenazine is combined with Thiopental.
Thioridazine The risk or severity of adverse effects can be increased when Thioridazine is combined with Thiopental.
Moricizine The risk or severity of adverse effects can be increased when Moricizine is combined with Thiopental.
Trifluoperazine The risk or severity of adverse effects can be increased when Trifluoperazine is combined with Thiopental.
Perphenazine The risk or severity of adverse effects can be increased when Perphenazine is combined with Thiopental.
Mesoridazine The risk or severity of adverse effects can be increased when Mesoridazine is combined with Thiopental.
Acetophenazine The risk or severity of adverse effects can be increased when Acetophenazine is combined with Thiopental.
Promethazine The risk or severity of adverse effects can be increased when Promethazine is combined with Thiopental.
Alimemazine The risk or severity of adverse effects can be increased when Alimemazine is combined with Thiopental.
Methotrimeprazine The risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Thiopental.
Periciazine The risk or severity of adverse effects can be increased when Periciazine is combined with Thiopental.
Acepromazine The risk or severity of adverse effects can be increased when Acepromazine is combined with Thiopental.
Aceprometazine The risk or severity of adverse effects can be increased when Aceprometazine is combined with Thiopental.
Pipotiazine The risk or severity of adverse effects can be increased when Pipotiazine is combined with Thiopental.
Thioproperazine The risk or severity of adverse effects can be increased when Thioproperazine is combined with Thiopental.
BL-1020 The risk or severity of adverse effects can be increased when BL-1020 is combined with Thiopental.
Cyamemazine The risk or severity of adverse effects can be increased when Cyamemazine is combined with Thiopental.
Methylene blue The risk or severity of adverse effects can be increased when Methylene blue is combined with Thiopental.
Propiopromazine The risk or severity of adverse effects can be increased when Propiopromazine is combined with Thiopental.
Perazine The risk or severity of adverse effects can be increased when Perazine is combined with Thiopental.
Butaperazine The risk or severity of adverse effects can be increased when Butaperazine is combined with Thiopental.
Chlorproethazine The risk or severity of adverse effects can be increased when Chlorproethazine is combined with Thiopental.
Thiazinam The risk or severity of adverse effects can be increased when Thiazinam is combined with Thiopental.
Dixyrazine The risk or severity of adverse effects can be increased when Dixyrazine is combined with Thiopental.
Perphenazine enanthate The risk or severity of adverse effects can be increased when Perphenazine enanthate is combined with Thiopental.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Thiopental.
Perampanel The metabolism of Perampanel can be increased when combined with Thiopental.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Thiopental.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Thiopental.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Thiopental.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Thiopental.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Thiopental.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Thiopental.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Thiopental.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Thiopental.

Target Protein

Gamma-aminobutyric acid receptor subunit alpha-1 GABRA1
Gamma-aminobutyric acid receptor subunit alpha-2 GABRA2
Gamma-aminobutyric acid receptor subunit alpha-3 GABRA3
Gamma-aminobutyric acid receptor subunit alpha-4 GABRA4
Gamma-aminobutyric acid receptor subunit alpha-5 GABRA5
Gamma-aminobutyric acid receptor subunit alpha-6 GABRA6
Neuronal acetylcholine receptor subunit alpha-4 CHRNA4
Neuronal acetylcholine receptor subunit alpha-7 CHRNA7
Glutamate receptor 2 GRIA2
Glutamate receptor ionotropic, kainate 2 GRIK2
Fatty-acid amide hydrolase 1 FAAH
Muscarinic acetylcholine receptor M3 CHRM3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 7235275
    Morgan DJ, Blackman GL, Paull JD, Wolf LJ: Pharmacokinetics and plasma binding of thiopental. II: Studies at cesarean section. Anesthesiology. 1981 Jun;54(6):474-80.
  • PMID: 13243246
    WINTERS WD, SPECTOR E, WALLACH DP, SHIDEMAN FE: Metabolism of thiopental-S35 and thiopental-2-C14 by a rat liver mince and identification of pentobarbital as a major metabolite. J Pharmacol Exp Ther. 1955 Jul;114(3):343-57.
  • PMID: 3093002
    Bory C, Chantin C, Boulieu R, Cotte J, Berthier JC, Fraisse D, Bobenrieth MJ: Use of thiopental in man. Determination of this drug and its metabolites in plasma and urine by liquid phase chromatography and mass spectrometry. C R Acad Sci III. 1986;303(1):7-12.
  • PMID: 19213
    Carroll FI, Smith D, Mark LC, Brand L, Perel JM: Determination of optically active thiopental, thiamylal, and their metabolites in human urine. Drug Metab Dispos. 1977 Jul-Aug;5(4):343-54.
  • PMID: 9739479
    Russo H, Bressolle F: Pharmacodynamics and pharmacokinetics of thiopental. Clin Pharmacokinet. 1998 Aug;35(2):95-134. doi: 10.2165/00003088-199835020-00002.
  • PMID: 29763050
    Suddock JT, Cain MD: Barbiturate Toxicity .

Contoh Produk & Brand

Produk: 7 • International brands: 17
Produk
  • Pentothal Inj 25mg/ml
    Powder, for solution • 25 mg / mL • Intravenous • Canada • Approved
  • Pentothal Inj 500mg/syr
    Powder, for solution • 500 mg • Intravenous • Canada • Approved
  • Pentothal Ready To Mix Syringe 250mg
    Powder, for solution • 250 mg / syr • Intravenous • Canada • Approved
  • Pentothal Sodium Inj 1gm Sterile
    Powder, for solution • 1 g / vial • Intravenous • Canada • Approved
  • Pentothal Sodium Pws 5gm
    Powder, for solution • 5 g / bottle • Intravenous • Canada • Approved
  • Thiopental Sodium
    Injection, powder, for solution • 25 mg/1mL • Intravenous • US
  • Thiopental Sodium
    Injection, powder, for solution • 50 mg/1mL • Intravenous • US
International Brands
  • Anestho — Incepta
  • Bensulf — Fada
  • Bitol Sodium — Brookes
  • Ekipental — Tüm Ekip
  • Farmotal — Marvecs Pharma Services
  • Intraval Sodium — Abbott
  • Pental Sodyum — I.E. Ulagay
  • Pentazol — Swiss Parenterals
  • Penthal — Oboi
  • Penthotal Sodium — Abbott

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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