Peringatan Keamanan

The mean seizure dosage of bupivacaine in rhesus monkeys was found to be 4.4 mg/kg with mean arterial plasma concentration of 4.5 mcg/mL. The intravenous and subcutaneous LD 50 in mice is 6 to 8 mg/kg and 38 to 54 mg/kg respectively. Recent clinical data from patients experiencing local anesthetic induced convulsions demonstrated rapid development of hypoxia, hypercarbia, and acidosis with bupivacaine within a minute of the onset of convulsions. These observations suggest that oxygen consumption and carbon dioxide production are greatly increased during local anesthetic convulsions and emphasize the importance of immediate and effective ventilation with oxygen which may avoid cardiac arrest.

Bupivacaine

DB00297

small molecule approved investigational

Deskripsi

Bupivacaine is a widely used local anesthetic agent.

Struktur Molekul 2D

Berat 288.4277
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 2.7 hours in adults and 8.1 hours in neonates. Bupivacaine applied together with [meloxicam] for postsurgical analgesia had a median half-life of 15-17 hours, depending on dose and application site.[L34100]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Systemic absorption of local anesthetics is dose- and concentration-dependendent on the total drug administered. Other factors that affect the rate of systemic absorption include the route of administration, blood flow at the administration site, and the presence or absence of epinephrine in the anesthetic solution. Bupivacaine formulated for instillation with meloxicam produced varied systemic measures following a single dose of varying strength. In patients undergoing bunionectomy, 60 mg of bupivacaine produced a Cmax of 54 ± 33 ng/mL, a median Tmax of 3 h, and an AUC? of 1718 ± 1211 ng\*h/mL. For a 300 mg dose used in herniorrhaphy, the corresponding values were 271 ± 147 ng/mL, 18 h, and 15,524 ± 8921 ng\*h/mL. Lastly, a 400 mg dose used in total knee arthroplasty produced values of 695 ± 411 ng/mL, 21 h, and 38,173 ± 29,400 ng\*h/mL.L34100

Metabolisme

Amide-type local anesthetics such as bupivacaine are metabolized primarily in the liver via conjugation with glucuronic acid. The major metabolite of bupivacaine is 2,6-pipecoloxylidine, which is mainly catalyzed via cytochrome P450 3A4.

Rute Eliminasi

Only 6% of bupivacaine is excreted unchanged in the urine.

Interaksi Obat

1978 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Bupivacaine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Bupivacaine is combined with Levodopa.
Risperidone Bupivacaine may increase the hypotensive activities of Risperidone.
Buprenorphine Bupivacaine 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 Bupivacaine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Bupivacaine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Bupivacaine.
Hydrocodone Bupivacaine 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 Bupivacaine.
Magnesium sulfate The therapeutic efficacy of Bupivacaine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Bupivacaine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Bupivacaine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Bupivacaine.
Mirtazapine Bupivacaine 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 Bupivacaine.
Orphenadrine Bupivacaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Bupivacaine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Bupivacaine.
Pramipexole Bupivacaine may increase the sedative activities of Pramipexole.
Ropinirole Bupivacaine may increase the sedative activities of Ropinirole.
Rotigotine Bupivacaine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Bupivacaine.
Sodium oxybate The risk or severity of CNS depression can be increased when Bupivacaine is combined with Sodium oxybate.
Suvorexant Bupivacaine 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 Bupivacaine.
Thalidomide Bupivacaine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Bupivacaine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Esmolol The serum concentration of Bupivacaine can be increased when it is combined with Esmolol.
Betaxolol The serum concentration of Bupivacaine can be increased when it is combined with Betaxolol.
Metoprolol The serum concentration of Bupivacaine can be increased when it is combined with Metoprolol.
Atenolol The serum concentration of Bupivacaine can be increased when it is combined with Atenolol.
Timolol The serum concentration of Bupivacaine can be increased when it is combined with Timolol.
Sotalol The serum concentration of Bupivacaine can be increased when it is combined with Sotalol.
Propranolol The serum concentration of Bupivacaine can be increased when it is combined with Propranolol.
Labetalol The serum concentration of Bupivacaine can be increased when it is combined with Labetalol.
Bisoprolol The serum concentration of Bupivacaine can be increased when it is combined with Bisoprolol.
Alprenolol The serum concentration of Bupivacaine can be increased when it is combined with Alprenolol.
Pindolol The serum concentration of Bupivacaine can be increased when it is combined with Pindolol.
Carvedilol The serum concentration of Bupivacaine can be increased when it is combined with Carvedilol.
Propafenone The serum concentration of Bupivacaine can be increased when it is combined with Propafenone.
Acebutolol The serum concentration of Bupivacaine can be increased when it is combined with Acebutolol.
Nadolol The serum concentration of Bupivacaine can be increased when it is combined with Nadolol.
Bevantolol The serum concentration of Bupivacaine can be increased when it is combined with Bevantolol.
Practolol The serum concentration of Bupivacaine can be increased when it is combined with Practolol.
Penbutolol The serum concentration of Bupivacaine can be increased when it is combined with Penbutolol.
Oxprenolol The serum concentration of Bupivacaine can be increased when it is combined with Oxprenolol.
Dexpropranolol The serum concentration of Bupivacaine can be increased when it is combined with Dexpropranolol.
Celiprolol The serum concentration of Bupivacaine can be increased when it is combined with Celiprolol.
Nebivolol The serum concentration of Bupivacaine can be increased when it is combined with Nebivolol.
Bufuralol The serum concentration of Bupivacaine can be increased when it is combined with Bufuralol.
Bopindolol The serum concentration of Bupivacaine can be increased when it is combined with Bopindolol.
Bupranolol The serum concentration of Bupivacaine can be increased when it is combined with Bupranolol.
Indenolol The serum concentration of Bupivacaine can be increased when it is combined with Indenolol.
Arotinolol The serum concentration of Bupivacaine can be increased when it is combined with Arotinolol.
Levobetaxolol The serum concentration of Bupivacaine can be increased when it is combined with Levobetaxolol.
Talinolol The serum concentration of Bupivacaine can be increased when it is combined with Talinolol.
Anisodamine The serum concentration of Bupivacaine can be increased when it is combined with Anisodamine.
Bucindolol The serum concentration of Bupivacaine can be increased when it is combined with Bucindolol.
Esatenolol The serum concentration of Bupivacaine can be increased when it is combined with Esatenolol.
Cloranolol The serum concentration of Bupivacaine can be increased when it is combined with Cloranolol.
Mepindolol The serum concentration of Bupivacaine can be increased when it is combined with Mepindolol.
Epanolol The serum concentration of Bupivacaine can be increased when it is combined with Epanolol.
Tertatolol The serum concentration of Bupivacaine can be increased when it is combined with Tertatolol.
Landiolol The serum concentration of Bupivacaine can be increased when it is combined with Landiolol.
Prilocaine The risk or severity of methemoglobinemia can be increased when Bupivacaine is combined with Prilocaine.
Hyaluronidase (ovine) Hyaluronidase (ovine) can cause an increase in the absorption of Bupivacaine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Hyaluronidase (human recombinant) Hyaluronidase (human recombinant) can cause an increase in the absorption of Bupivacaine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Hyaluronidase Hyaluronidase can cause an increase in the absorption of Bupivacaine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Bupivacaine.
Mirabegron The serum concentration of Bupivacaine can be increased when it is combined with Mirabegron.
Nicorandil Nicorandil may increase the hypotensive activities of Bupivacaine.
Ethanol Bupivacaine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Bupivacaine 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 Bupivacaine.
Sertraline The risk or severity of adverse effects can be increased when Bupivacaine is combined with Sertraline.
Desvenlafaxine The serum concentration of Bupivacaine can be increased when it is combined with Desvenlafaxine.
Sibutramine The risk or severity of adverse effects can be increased when Bupivacaine is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Bupivacaine is combined with Zimelidine.
Milnacipran The risk or severity of adverse effects can be increased when Bupivacaine is combined with Milnacipran.
Seproxetine The risk or severity of adverse effects can be increased when Bupivacaine is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Bupivacaine is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Bupivacaine is combined with Alaproclate.
Dapoxetine The risk or severity of adverse effects can be increased when Bupivacaine is combined with Dapoxetine.
Trazodone The risk or severity of adverse effects can be increased when Bupivacaine is combined with Trazodone.
Dapsone The risk or severity of methemoglobinemia can be increased when Dapsone is combined with Bupivacaine.
Technetium Tc-99m tilmanocept Bupivacaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Linezolid The risk or severity of methemoglobinemia can be increased when Linezolid is combined with Bupivacaine.
Furazolidone Furazolidone may increase the orthostatic hypotensive activities of Bupivacaine.
Phenelzine Phenelzine may increase the orthostatic hypotensive activities of Bupivacaine.
Minaprine Minaprine may increase the orthostatic hypotensive activities of Bupivacaine.
Selegiline Selegiline may increase the orthostatic hypotensive activities of Bupivacaine.
Procarbazine The risk or severity of methemoglobinemia can be increased when Procarbazine is combined with Bupivacaine.
Moclobemide Moclobemide may increase the orthostatic hypotensive activities of Bupivacaine.
Isocarboxazid Isocarboxazid may increase the orthostatic hypotensive activities of Bupivacaine.
Rasagiline Rasagiline may increase the orthostatic hypotensive activities of Bupivacaine.
Pargyline Pargyline may increase the orthostatic hypotensive activities of Bupivacaine.
Clorgiline Clorgiline may increase the orthostatic hypotensive activities of Bupivacaine.
Iproniazid Iproniazid may increase the orthostatic hypotensive activities of Bupivacaine.
Nialamide Nialamide may increase the orthostatic hypotensive activities of Bupivacaine.
Safinamide Safinamide may increase the orthostatic hypotensive activities of Bupivacaine.

Target Protein

Sodium channel protein type 10 subunit alpha SCN10A
Prostaglandin E2 receptor EP1 subtype PTGER1

Referensi & Sumber

Synthesis reference: Thuresson, B. and Egner, B.P.H.; U.S. Patent 2,792,399; May 14, 1957; assigned to AB Bofors, Sweden. Thuresson, B. and Pettersson, B.G.; US. Patent 2,955.1 11; October 4,1960; assigned to AB Bofors, Sweden.
Artikel (PubMed)
  • PMID: 16810015
    Rosenblatt MA, Abel M, Fischer GW, Itzkovich CJ, Eisenkraft JB: Successful use of a 20% lipid emulsion to resuscitate a patient after a presumed bupivacaine-related cardiac arrest. Anesthesiology. 2006 Jul;105(1):217-8.
  • PMID: 16430560
    Picard J, Meek T: Lipid emulsion to treat overdose of local anaesthetic: the gift of the glob. Anaesthesia. 2006 Feb;61(2):107-9.
  • PMID: 25008571
    Zhang H, Ji H, Liu Z, Ji Y, You X, Ding G, Cheng Z: Voltage-dependent blockade by bupivacaine of cardiac sodium channels expressed in Xenopus oocytes. Neurosci Bull. 2014 Aug;30(4):697-710. doi: 10.1007/s12264-013-1449-1. Epub 2014 Jul 9.
  • PMID: 11524330
    Honemann CW, Heyse TJ, Mollhoff T, Hahnenkamp K, Berning S, Hinder F, Linck B, Schmitz W, van Aken H: The inhibitory effect of bupivacaine on prostaglandin E(2) (EP(1)) receptor functioning: mechanism of action. Anesth Analg. 2001 Sep;93(3):628-34. doi: 10.1097/00000539-200109000-00019.
  • PMID: 20685573
    Sheets MF, Fozzard HA, Lipkind GM, Hanck DA: Sodium channel molecular conformations and antiarrhythmic drug affinity. Trends Cardiovasc Med. 2010 Jan;20(1):16-21. doi: 10.1016/j.tcm.2010.03.002.

Contoh Produk & Brand

Produk: 363 • International brands: 7
Produk
  • 0.25% BUPIVACAINE HCl
    Injection, solution • 2.5 mg/1mL • Infiltration; Perineural • US • Generic • Approved
  • Bl
    Kit • - • Epidural; Infiltration; Topical • US • Generic • Approved
  • BLT-25 Kit
    Kit • - • Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Perineural; Topical • US
  • Bt
    Cloth; Injection, solution; Kit; Solution • - • Epidural; Infiltration; Intra-articular; Intramuscular; Topical • US • Approved
  • Bupivacaine
    Injection, suspension, liposomal • 13.3 mg/1mL • Infiltration • US • Generic • Approved
  • Bupivacaine
    Injection, suspension, liposomal • 13.3 mg/1mL • Infiltration • US • Generic • Approved
  • Bupivacaine Hci
    Injection, solution • 2.5 mg/1mL • Infiltration; Perineural • US • Generic • Approved
  • Bupivacaine Hci and Epinephrine
    Injection, solution • - • Perineural • US • Generic • Approved
Menampilkan 8 dari 363 produk.
International Brands
  • Bupivan — Sun
  • Carbostesin — AstraZeneca
  • Marcain — AstraZeneca
  • Marcaina — AstraZeneca
  • Posimir — Durect
  • Sensorcaine-MPF — Astra Zeneca
  • Xaracoll — Innocoll Holdings Limited

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul