Peringatan Keamanan

The oral LD50 in mice is 600mg/kg and in rats is >2g/kg.L7727,L7730 The intravenous LD50 in mice and rats is 50-60mg/kg.L7727,L7730

Patients experiencing an overdose may present with excessive hypotension and bradycardia.L7727,L7730 Patients should be placed on their back with their legs raised to maintain perfusion of the brain.L7727,L7730 Oral overdoses may be treated with gastric lavage or emesis, bradycardia may be treated with atropine or epinephrine, cardiac failure may be treated with digitalis and a diuretic, hypotension may be treated with vasopressors, bronchospasms may be treated with epinephrine or a beta2 agonist, and seizures may be treated with diazepam.L7727,L7730

Labetalol

DB00598

small molecule approved

Deskripsi

Labetalol is a racemic mixture of 2 diastereoisomers where dilevalol, the R,R' stereoisomer, makes up 25% of the mixture.L7730 Labetalol is formulated as an injection or tablets to treat hypertension.L7727,L7730

Labetalol was granted FDA approval on 1 August 1984.L7724

Struktur Molekul 2D

Berat 328.4055
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Labetalol has a half life of 1.7-6.1 hours.[A181853]
Volume Distribusi In normotensive patients, the volume of distribution is 805L.[A181853] In hypertensive patients, the volume of distribution is between 188-747L with an average of 392L.[A181853]
Klirens (Clearance) Labetalol has a plasma clearance of approximately 1500mL/min and a whole blood clearance of 1100mL/min.[A181853]

Absorpsi

100mg and 200mg oral doses of labetalol have a Tmax of 20 minutes to 2 hours.A181853 Bioavailability may be as low as 11% or as high as 86% and may increase in older patients or when taken with food.A181853

Metabolisme

The metabolism of labetalol has not been fully described in the literature but studies in sheep show an N-dealkylation to 3-amino-1-phenyl butane.A181835 This metabolite may be further metabolized to benzylacetone and 3-amino-(4-hydroxyphenyl)butane.A181835 Labetalol in humans is mainly metabolized to glucuronide metabolites such as the O-phenyl-glucuronide and the N-glucuronide.A181853,L7727,L7730

Rute Eliminasi

Radiolabelled doses of labetalol are 55-60% recovered in the urine and 12-27% recovered in the feces.A181853

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1855 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Labetalol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Labetalol is combined with Levodopa.
Risperidone Labetalol may increase the hypotensive activities of Risperidone.
Ceritinib Labetalol may increase the bradycardic activities of Ceritinib.
Ivabradine Labetalol may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Labetalol.
Amifostine Labetalol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Labetalol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Labetalol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Labetalol.
Obinutuzumab Labetalol may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Labetalol.
Rituximab Labetalol may increase the hypotensive activities of Rituximab.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Labetalol.
Doxapram Doxapram may decrease the antihypertensive activities of Labetalol.
Atropine Atropine may decrease the antihypertensive activities of Labetalol.
Naratriptan Naratriptan may decrease the antihypertensive activities of Labetalol.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Labetalol.
Dutasteride Dutasteride may decrease the antihypertensive activities of Labetalol.
Finasteride Finasteride may decrease the antihypertensive activities of Labetalol.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Labetalol.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Labetalol.
Amineptine Amineptine may decrease the antihypertensive activities of Labetalol.
Flibanserin Flibanserin may decrease the antihypertensive activities of Labetalol.
Naluzotan Naluzotan may decrease the antihypertensive activities of Labetalol.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Labetalol.
Cinitapride Cinitapride may decrease the antihypertensive activities of Labetalol.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Labetalol.
Butriptyline Butriptyline may decrease the antihypertensive activities of Labetalol.
Tianeptine Tianeptine may decrease the antihypertensive activities of Labetalol.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Labetalol.
Atipamezole Atipamezole may decrease the antihypertensive activities of Labetalol.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Labetalol.
Piclozotan Piclozotan may decrease the antihypertensive activities of Labetalol.
Siponimod Siponimod may decrease the antihypertensive activities of Labetalol.
Idazoxan Idazoxan may decrease the antihypertensive activities of Labetalol.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Labetalol.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Labetalol.
Quinupramine Quinupramine may decrease the antihypertensive activities of Labetalol.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Labetalol.
Melitracen Melitracen may decrease the antihypertensive activities of Labetalol.
Lofepramine Lofepramine may decrease the antihypertensive activities of Labetalol.
Xenon Xenon may decrease the antihypertensive activities of Labetalol.
Iprindole Iprindole may decrease the antihypertensive activities of Labetalol.
Buflomedil Buflomedil may decrease the antihypertensive activities of Labetalol.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Labetalol.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Labetalol.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Labetalol.
Sufentanil Sufentanil may decrease the antihypertensive activities of Labetalol.
Isoflurane Isoflurane may decrease the antihypertensive activities of Labetalol.
Remifentanil Remifentanil may decrease the antihypertensive activities of Labetalol.
Halothane Halothane may decrease the antihypertensive activities of Labetalol.
Desflurane Desflurane may decrease the antihypertensive activities of Labetalol.
Sevoflurane Sevoflurane may decrease the antihypertensive activities of Labetalol.
Fentanyl Fentanyl may decrease the antihypertensive activities of Labetalol.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Labetalol.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Labetalol.
Naxitamab Naxitamab may decrease the antihypertensive activities of Labetalol.
Protriptyline Protriptyline may decrease the antihypertensive activities of Labetalol.
Opipramol Opipramol may decrease the antihypertensive activities of Labetalol.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Labetalol.
Amiodarone The therapeutic efficacy of Labetalol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Labetalol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Labetalol.
Disopyramide Disopyramide may increase the bradycardic activities of Labetalol.
Dronedarone Dronedarone may increase the bradycardic activities of Labetalol.
Fingolimod Labetalol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Labetalol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Labetalol.
Methacholine Labetalol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Labetalol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Labetalol.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Labetalol.
Regorafenib Regorafenib may increase the bradycardic activities of Labetalol.
Reserpine Reserpine may increase the hypotensive activities of Labetalol.
Deserpidine Deserpidine may increase the hypotensive activities of Labetalol.
Guanethidine Guanethidine may increase the hypotensive activities of Labetalol.
Rivastigmine Labetalol may increase the bradycardic activities of Rivastigmine.
Dabrafenib The serum concentration of Labetalol can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Labetalol can be increased when it is combined with Luliconazole.
Dapoxetine Dapoxetine may increase the orthostatic hypotensive activities of Labetalol.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Labetalol.
Nelfinavir The metabolism of Labetalol can be increased when combined with Nelfinavir.
Phenytoin The metabolism of Labetalol can be increased when combined with Phenytoin.
Desogestrel The metabolism of Labetalol can be increased when combined with Desogestrel.
Zidovudine The metabolism of Labetalol can be increased when combined with Zidovudine.
Efavirenz The metabolism of Labetalol can be increased when combined with Efavirenz.
Ethinylestradiol The metabolism of Labetalol can be increased when combined with Ethinylestradiol.
Testosterone propionate The metabolism of Labetalol can be increased when combined with Testosterone propionate.
Lamotrigine The metabolism of Labetalol can be increased when combined with Lamotrigine.
Lurasidone Labetalol may increase the hypotensive activities of Lurasidone.
Mirabegron The serum concentration of Labetalol can be increased when it is combined with Mirabegron.
Tedizolid phosphate Tedizolid phosphate may increase the hypertensive activities of Labetalol.
Nicorandil Nicorandil may increase the hypotensive activities of Labetalol.
Molsidomine Molsidomine may increase the hypotensive activities of Labetalol.
Insulin argine Labetalol may increase the hypoglycemic activities of Insulin argine.
Carteolol Carteolol may increase the hypotensive activities of Labetalol.
Dorzolamide Labetalol may increase the hypotensive activities of Dorzolamide.
Bimatoprost Labetalol may increase the hypotensive activities of Bimatoprost.
Metipranolol Labetalol may increase the hypotensive activities of Metipranolol.

Target Protein

Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
Alpha-1 adrenergic receptors ADRA1A

Referensi & Sumber

Synthesis reference: U.S. Patent 4,012,444.
Artikel (PubMed)
  • PMID: 8097698
    Yeleswaram K, Rurak DW, Kwan E, Hall C, Doroudian A, Abbott FS, Axelson JE: Disposition, metabolism, and pharmacodynamics of labetalol in adult sheep. Drug Metab Dispos. 1993 Mar-Apr;21(2):284-92.
  • PMID: 6370541
    McNeil JJ, Louis WJ: Clinical pharmacokinetics of labetalol. Clin Pharmacokinet. 1984 Mar-Apr;9(2):157-67. doi: 10.2165/00003088-198409020-00003.
  • PMID: 3154919
    Opie LH: Role of vasodilation in the antihypertensive and antianginal effects of labetalol: implications for therapy of combined hypertension and angina. Cardiovasc Drugs Ther. 1988 Sep;2(3):369-76.
  • PMID: 6354658
    Carter BL: Labetalol. Drug Intell Clin Pharm. 1983 Oct;17(10):704-12.
  • PMID: 6310529
    MacCarthy EP, Bloomfield SS: Labetalol: a review of its pharmacology, pharmacokinetics, clinical uses and adverse effects. Pharmacotherapy. 1983 Jul-Aug;3(4):193-219.

Contoh Produk & Brand

Produk: 319 • International brands: 4
Produk
  • Apo-labetalol
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Apo-labetalol
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Labetalol
    Injection, solution • 5 mg/1mL • Intravenous • US • Generic • Approved
  • Labetalol
    Tablet, film coated • 100 mg/1 • Oral • US • Generic • Approved
  • Labetalol
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
  • Labetalol
    Tablet, film coated • 300 mg/1 • Oral • US • Generic • Approved
  • Labetalol
    Tablet, film coated • 100 mg/1 • Oral • US • Generic • Approved
  • Labetalol
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 319 produk.
International Brands
  • Albetol — Leiras
  • Latol — Standard
  • Normadate — GlaxoSmithKline
  • Normodyne — Schering

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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