Peringatan Keamanan

Symptoms of overdose include hypotension, hypoglycemic seizure, restlessness, euphoria, insomnia.L6901 Patients with asthma may develop bronchospasm.L6901 In case of overdose, monitor vital signs, mental status, and blood glucose.L6901 Treat hypotension with intravenous fluids, bradycardia with atropine, and isoproterenol and aminophylline for bronchospasm.L6901 If patients do not respond to intravenous fluids, follow up with glucagon 50-150µg/kg intravenously, then 1-5mg/hour, followed by catecholamines.L6901,L6904,L6907 Dialysis will not be useful as propranolol is highly protein bound.L6901,L6904,L6907

Propranolol

DB00571

small molecule approved investigational

Deskripsi

Propranolol is a racemic mixture of 2 enantiomers where the S(-)-enantiomer has approximately 100 times the binding affinity for beta adrenergic receptors.L6904 Propranolol is used to treat a number of conditions but most commonly is used for hypertension.L6901,L6904,L6907

Propranolol was granted FDA approval on 13 November 1967.L6904

Struktur Molekul 2D

Berat 259.3434
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of propranolol is approximately 8 hours.[L6907] The plasma half-life of propranolol is 3 to 6 hours.[L6901,L6904]
Volume Distribusi The volume of distribution of propranolol is approximately 4L/kg[L6901,L6904] or 320L.[A180289]
Klirens (Clearance) The clearance of propranolol is 2.7±0.03L/h/kg in infants <90 days and 3.3±0.35L/h/kg in infants >90 days.[L6901] Propranolol clearance increases linearly with hepatic blood flow.[A180286] Propranolol has a clearance in hypertensive adults of 810mL/min.[A180289]

Absorpsi

Patients taking doses of 40mg, 80mg, 160mg, and 320mg daily experienced Cmax values of 18±15ng/mL, 52±51ng/mL, 121±98ng/mL, and 245±110ng/mL respectively.A180289 Propranolol has a Tmax of approximately 2 hours, though this can range from 1 to 4 hours in fasting patients.A180295 Taking propranolol with food does not increase Tmax but does increase bioavailability.A180295

Metabolisme

Propranolol undergoes side chain oxidation to ?-naphthoxylactic acid, ring oxidation to 4’-hydroxypropranolol, or glucuronidation to propranolol glucuronide.A36551 It can also be N-desisopropylated to become N-desisopropyl propranolol.A179878 17% of a dose undergoes glucuronidation and 42% undergoes ring oxidation.A180298

Rute Eliminasi

91% of an oral dose of propranolol is recovered as 12 metabolites in the urine.A180298

Interaksi Makanan

3 Data
  • 1. Avoid alcohol. Alcohol increases propranolol plasma concentrations.
  • 2. Avoid natural licorice. Natural licorice inhibits the metabolism of propranolol, increasing drug exposure.
  • 3. Take with food.

Interaksi Obat

2003 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Propranolol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Propranolol is combined with Levodopa.
Risperidone Propranolol may increase the hypotensive activities of Risperidone.
Ceritinib Propranolol may increase the bradycardic activities of Ceritinib.
Ivabradine Propranolol may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Propranolol.
Deferasirox The serum concentration of Propranolol can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Propranolol can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Propranolol can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Propranolol can be decreased when it is combined with Teriflunomide.
Alfuzosin Alfuzosin may increase the hypotensive activities of Propranolol.
Amifostine Propranolol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Propranolol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Propranolol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Propranolol.
Obinutuzumab Propranolol may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Propranolol.
Rituximab Propranolol may increase the hypotensive activities of Rituximab.
Doxapram Doxapram may decrease the antihypertensive activities of Propranolol.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Propranolol.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Propranolol.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Propranolol.
Amineptine Amineptine may decrease the antihypertensive activities of Propranolol.
Naluzotan Naluzotan may decrease the antihypertensive activities of Propranolol.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Propranolol.
Cinitapride Cinitapride may decrease the antihypertensive activities of Propranolol.
Tyramine Tyramine may decrease the antihypertensive activities of Propranolol.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Propranolol.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Propranolol.
Atipamezole Atipamezole may decrease the antihypertensive activities of Propranolol.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Propranolol.
Piclozotan Piclozotan may decrease the antihypertensive activities of Propranolol.
Idazoxan Idazoxan may decrease the antihypertensive activities of Propranolol.
Tramazoline Tramazoline may decrease the antihypertensive activities of Propranolol.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Propranolol.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Propranolol.
Quinupramine Quinupramine may decrease the antihypertensive activities of Propranolol.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Propranolol.
Fenozolone Fenozolone may decrease the antihypertensive activities of Propranolol.
Melitracen Melitracen may decrease the antihypertensive activities of Propranolol.
Lofepramine Lofepramine may decrease the antihypertensive activities of Propranolol.
Xenon Xenon may decrease the antihypertensive activities of Propranolol.
Iprindole Iprindole may decrease the antihypertensive activities of Propranolol.
Buflomedil Buflomedil may decrease the antihypertensive activities of Propranolol.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Propranolol.
Mefenorex Mefenorex may decrease the antihypertensive activities of Propranolol.
5-methoxy-N,N-dimethyltryptamine 5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Propranolol.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Propranolol.
Remifentanil Remifentanil may decrease the antihypertensive activities of Propranolol.
Sufentanil Sufentanil may decrease the antihypertensive activities of Propranolol.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Propranolol.
Halothane Halothane may decrease the antihypertensive activities of Propranolol.
Cariprazine Cariprazine may decrease the antihypertensive activities of Propranolol.
Tianeptine Tianeptine may decrease the antihypertensive activities of Propranolol.
Siponimod Siponimod may decrease the antihypertensive activities of Propranolol.
Flibanserin Flibanserin may decrease the antihypertensive activities of Propranolol.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Propranolol.
Alfentanil Alfentanil may decrease the antihypertensive activities of Propranolol.
Fentanyl Fentanyl may decrease the antihypertensive activities of Propranolol.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Propranolol.
Opipramol Opipramol may decrease the antihypertensive activities of Propranolol.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Propranolol.
Naxitamab Naxitamab may decrease the antihypertensive activities of Propranolol.
Protriptyline Protriptyline may decrease the antihypertensive activities of Propranolol.
Isoflurane Isoflurane may decrease the antihypertensive activities of Propranolol.
Propofol Propofol may decrease the antihypertensive activities of Propranolol.
Desflurane Desflurane may decrease the antihypertensive activities of Propranolol.
Sevoflurane Sevoflurane may decrease the antihypertensive activities of Propranolol.
Solifenacin Solifenacin may decrease the antihypertensive activities of Propranolol.
Lurasidone Lurasidone may decrease the antihypertensive activities of Propranolol.
Butriptyline Butriptyline may decrease the antihypertensive activities of Propranolol.
Amiodarone The therapeutic efficacy of Propranolol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Propranolol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Propranolol.
Disopyramide Disopyramide may increase the bradycardic activities of Propranolol.
Dronedarone Dronedarone may increase the bradycardic activities of Propranolol.
Fingolimod Propranolol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Propranolol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Propranolol.
Methacholine Propranolol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Propranolol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Propranolol.
Regorafenib Regorafenib may increase the bradycardic activities of Propranolol.
Reserpine Reserpine may increase the hypotensive activities of Propranolol.
Deserpidine Deserpidine may increase the hypotensive activities of Propranolol.
Guanethidine Guanethidine may increase the hypotensive activities of Propranolol.
Rivastigmine Propranolol may increase the bradycardic activities of Rivastigmine.
Dabrafenib The serum concentration of Propranolol can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Propranolol can be increased when it is combined with Luliconazole.
Zolmitriptan The serum concentration of the active metabolites of Zolmitriptan can be reduced when Zolmitriptan is used in combination with Propranolol resulting in a loss in efficacy.
Colestipol Colestipol can cause a decrease in the absorption of Propranolol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Propranolol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Propranolol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Propranolol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Propranolol.
Quinine The serum concentration of Propranolol can be increased when it is combined with Quinine.
Quinidine The serum concentration of Propranolol can be increased when it is combined with Quinidine.
Mirabegron The serum concentration of Propranolol can be increased when it is combined with Mirabegron.
Abiraterone The serum concentration of Propranolol can be increased when it is combined with Abiraterone.
Nicorandil Nicorandil may increase the hypotensive activities of Propranolol.

Target Protein

Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
Beta-3 adrenergic receptor ADRB3
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 1B HTR1B

Referensi & Sumber

Artikel (PubMed)
  • PMID: 4066876
    Harrison PM, Tonkin AM, Cahill CM, McLean AJ: Rapid and simultaneous extraction of propranolol, its neutral and basic metabolites from plasma and assay by high-performance liquid chromatography. J Chromatogr. 1985 Oct 11;343(2):349-58.
  • PMID: 29846253
    Hagen R, Ghareeb E, Jalali O, Zinn Z: Infantile hemangiomas: what have we learned from propranolol? Curr Opin Pediatr. 2018 Aug;30(4):499-504. doi: 10.1097/MOP.0000000000000650.
  • PMID: 656285
    Weiss YA, Safar ME, Lehner JP, Levenson JA, Simon A, Alexandre JM: (+)-Propranolol clearance, an estimation of hepatic blood flow in man. Br J Clin Pharmacol. 1978 May;5(5):457-60. doi: 10.1111/j.1365-2125.1978.tb01655.x.
  • PMID: 1149212
    Chidsey CA, Morselli P, Bianchetti G, Morganti A, Leonetti G, Zanchetti A: Studies of the absorption and removal of propranolol in hypertensive patients during therapy. Circulation. 1975 Aug;52(2):313-8. doi: 10.1161/01.cir.52.2.313.
  • PMID: 378502
    Routledge PA, Shand DG: Clinical pharmacokinetics of propranolol. Clin Pharmacokinet. 1979 Mar-Apr;4(2):73-90. doi: 10.2165/00003088-197904020-00001.
  • PMID: 2859169
    Walle T, Walle UK, Olanoff LS: Quantitative account of propranolol metabolism in urine of normal man. Drug Metab Dispos. 1985 Mar-Apr;13(2):204-9.
  • PMID: 8062488
    Walle T, Walle K, Mathur RS, Palesch YY, Conradi EC: Propranolol metabolism in normal subjects: association with sex steroid hormones. Clin Pharmacol Ther. 1994 Aug;56(2):127-32.

Contoh Produk & Brand

Produk: 576 • International brands: 11
Produk
  • Apo-propranolol
    Tablet • 40 mg • Oral • Canada • Generic • Approved
  • Apo-propranolol
    Tablet • 80 mg • Oral • Canada • Generic • Approved
  • Apo-propranolol
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-propranolol
    Tablet • 120 mg • Oral • Canada • Generic • Approved
  • Apo-propranolol
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Detensol Tab 10mg
    Tablet • 10 mg • Oral • Canada • Approved
  • Detensol Tab 120mg
    Tablet • 120 mg • Oral • Canada • Approved
  • Detensol Tab 40mg
    Tablet • 40 mg • Oral • Canada • Approved
Menampilkan 8 dari 576 produk.
International Brands
  • Angilol
  • Bedranol SR
  • Cardinol
  • Ciplar
  • Deralin
  • Dociton
  • Duranol
  • Indobloc
  • INNOPRAN
  • Prophylux

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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