Peringatan Keamanan

Symptoms of overdose include drowsiness, vertigo, headache, and atriventricular block.

Penbutolol

DB01359

small molecule approved investigational

Deskripsi

Penbutolol is a drug in the beta-blocker class used to treat hypertension. Penbutolol binds both beta-1 and beta-2 adrenergic receptors, rendering it a non-selective beta-blocker. Penbutolol can act as a partial agonist at beta adrenergic receptors, since it is a sympathomimetric drug. Penbutolol also demonstrates high binding affinity to the 5-hydroxytryptamine receptor 1A with antagonistic effects. This binding characteristic of penbutolol is being investigated for its implications in Antidepressant Therapy. Penbutolol is contraindicated in patients with cardiogenic shock, sinus bradycardia, second and third degree atrioventricular conduction block, bronchial asthma, and those with known hypersensitivity.

Struktur Molekul 2D

Berat 291.4284
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Plasma= approximately 5h Conjugated= approximately 20h in healthy persons, 25h in healthy elderly persons, and 100h in patients on renal dialysis.
Volume Distribusi -
Klirens (Clearance) Approximately 90% of the metabolites are excreted in the urine.

Absorpsi

>90%.

Metabolisme

Metabolized in the liver by hydroxylation and glucuroconjugation forming a glucuronide metabolite and a semi-active 4-hydroxy metabolite.

Rute Eliminasi

The metabolites are excreted principally in the urine.

Interaksi Obat

2013 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Penbutolol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Penbutolol is combined with Levodopa.
Risperidone Penbutolol may increase the hypotensive activities of Risperidone.
Ceritinib Penbutolol may increase the bradycardic activities of Ceritinib.
Ivabradine Penbutolol may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Penbutolol.
Alfuzosin Alfuzosin may increase the hypotensive activities of Penbutolol.
Amifostine Penbutolol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Penbutolol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Penbutolol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Penbutolol.
Obinutuzumab Penbutolol may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Penbutolol.
Rituximab Penbutolol may increase the hypotensive activities of Rituximab.
Doxapram Doxapram may decrease the antihypertensive activities of Penbutolol.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Penbutolol.
Dutasteride Dutasteride may decrease the antihypertensive activities of Penbutolol.
Finasteride Finasteride may decrease the antihypertensive activities of Penbutolol.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Penbutolol.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Penbutolol.
Tyramine Tyramine may decrease the antihypertensive activities of Penbutolol.
Atipamezole Atipamezole may decrease the antihypertensive activities of Penbutolol.
Siponimod Siponimod may decrease the antihypertensive activities of Penbutolol.
Idazoxan Idazoxan may decrease the antihypertensive activities of Penbutolol.
Tramazoline Tramazoline may decrease the antihypertensive activities of Penbutolol.
Fenozolone Fenozolone may decrease the antihypertensive activities of Penbutolol.
Xenon Xenon may decrease the antihypertensive activities of Penbutolol.
Buflomedil Buflomedil may decrease the antihypertensive activities of Penbutolol.
Mefenorex Mefenorex may decrease the antihypertensive activities of Penbutolol.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Penbutolol.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Penbutolol.
Naxitamab Naxitamab may decrease the antihypertensive activities of Penbutolol.
Buprenorphine Penbutolol 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 Penbutolol.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Penbutolol.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Penbutolol.
Hydrocodone Penbutolol 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 Penbutolol.
Magnesium sulfate The therapeutic efficacy of Penbutolol can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Penbutolol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Penbutolol may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Penbutolol.
Mirtazapine Penbutolol 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 Penbutolol.
Orphenadrine Penbutolol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Penbutolol 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 Penbutolol.
Pramipexole Penbutolol may increase the sedative activities of Pramipexole.
Ropinirole Penbutolol may increase the sedative activities of Ropinirole.
Rotigotine Penbutolol may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Penbutolol.
Sodium oxybate Penbutolol may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Penbutolol 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 Penbutolol.
Thalidomide Penbutolol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Penbutolol may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Amiodarone The therapeutic efficacy of Penbutolol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Penbutolol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Penbutolol.
Disopyramide Disopyramide may increase the bradycardic activities of Penbutolol.
Dronedarone Dronedarone may increase the bradycardic activities of Penbutolol.
Fingolimod Penbutolol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Penbutolol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Penbutolol.
Methacholine Penbutolol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Penbutolol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Penbutolol.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Penbutolol.
Regorafenib Regorafenib may increase the bradycardic activities of Penbutolol.
Reserpine Reserpine may increase the hypotensive activities of Penbutolol.
Deserpidine Deserpidine may increase the hypotensive activities of Penbutolol.
Guanethidine Guanethidine may increase the hypotensive activities of Penbutolol.
Rivastigmine Penbutolol may increase the bradycardic activities of Rivastigmine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Penbutolol.
Dicoumarol The risk or severity of adverse effects can be increased when Penbutolol is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Penbutolol is combined with Phenindione.
Phenprocoumon The risk or severity of adverse effects can be increased when Penbutolol is combined with Phenprocoumon.
Acenocoumarol The risk or severity of adverse effects can be increased when Penbutolol is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Penbutolol is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of adverse effects can be increased when Penbutolol is combined with Coumarin.
(R)-warfarin The risk or severity of adverse effects can be increased when Penbutolol is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Penbutolol is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Penbutolol is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Penbutolol is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Penbutolol is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Penbutolol is combined with Tioclomarol.
(S)-Warfarin The risk or severity of adverse effects can be increased when Penbutolol is combined with (S)-Warfarin.
Mirabegron The serum concentration of Penbutolol can be increased when it is combined with Mirabegron.
Nicorandil Nicorandil may increase the hypotensive activities of Penbutolol.
Molsidomine Molsidomine may increase the hypotensive activities of Penbutolol.
Insulin argine Penbutolol may increase the hypoglycemic activities of Insulin argine.
Carteolol Carteolol may increase the hypotensive activities of Penbutolol.
Dorzolamide Dorzolamide may increase the hypotensive activities of Penbutolol.
Bimatoprost Bimatoprost may increase the hypotensive activities of Penbutolol.
Metipranolol Metipranolol may increase the hypotensive activities of Penbutolol.
Unoprostone Penbutolol may increase the hypotensive activities of Unoprostone.
Minoxidil Minoxidil may increase the hypotensive activities of Penbutolol.
Nitroglycerin Nitroglycerin may increase the hypotensive activities of Penbutolol.
Bretylium Bretylium may increase the hypotensive activities of Penbutolol.
Remikiren Remikiren may increase the hypotensive activities of Penbutolol.

Target Protein

Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 1B HTR1B

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15595665
    Maurer HH, Tenberken O, Kratzsch C, Weber AA, Peters FT: Screening for library-assisted identification and fully validated quantification of 22 beta-blockers in blood plasma by liquid chromatography-mass spectrometry with atmospheric pressure chemical ionization. J Chromatogr A. 2004 Nov 26;1058(1-2):169-81.
  • PMID: 8174208
    Aguirre C, Rodriguez-Sasiain JM, Calvo R: Decrease in penbutolol protein binding as a consequence of treatment with some alkylating agents. Cancer Chemother Pharmacol. 1994;34(1):86-8.
  • PMID: 1468487
    Hjorth S: (-)-Penbutolol as a blocker of central 5-HT1A receptor-mediated responses. Eur J Pharmacol. 1992 Nov 3;222(1):121-7.
  • PMID: 2359502
    Pepe S, Scalici G, D'Angelo A, Curiale B, Corrao S, Agnello C: Validity of the use of penbutolol in essential arterial hypertension. Minerva Med. 1990 Jun;81(6):471-3.
  • PMID: 2189902
    Frishman WH, Covey S: Penbutolol and carteolol: two new beta-adrenergic blockers with partial agonism. J Clin Pharmacol. 1990 May;30(5):412-21.
  • PMID: 1974610
    Martinez Jorda R, Aguirre C, Calvo R, Rodriguez-Sasiain JM, Erill S: Decrease in penbutolol central response as a cause of changes in its serum protein binding. J Pharm Pharmacol. 1990 Mar;42(3):164-6.

Contoh Produk & Brand

Produk: 2 • International brands: 2
Produk
  • Levatol
    Tablet • 20 mg/1 • Oral • US • Approved
  • Levatol
    Tablet • 20 mg/1 • Oral • US • Approved
International Brands
  • Betapressin — Hoechst Ltd.
  • Lobeta — Sanofi-Aventis

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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