Peringatan Keamanan

Patients experiencing an overdose may experience excessive bradycardia, cardiac failure, hypotension, and bronchospasm.L32353 Initiate treatment with symptomatic and supportive measures.L32353

Pindolol

DB00960

small molecule approved investigational

Deskripsi

Pindolol is a first generation non-selective beta blocker used in the treatment of hypertension.L32353 Early research into the use of pindolol found it had chronotropic effects, and so further investigation focused on the treatment of arrhythmia.A231059 Research into pindolol's use in the treatment of hypertension began in the early 1970s.A231064

Pindolol was granted FDA approval on 3 September 1982.L32348

Struktur Molekul 2D

Berat 248.3208
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of pindolol varies from 3-4 hours[L32388] but can be as high as 30 hours in patients with cirrhosis of the liver.[L32353]
Volume Distribusi The volume of distribution of pindolol is approximately 2-3 L/kg.[L32353,L32388]
Klirens (Clearance) In otherwise healthy patients, the systemic clearance of pindolol is 400-500 mL/min.[L32388] In patients with cirrhosis, the clearance of pindolol varies from 50-300 mL/min.[L32353]

Absorpsi

The mean oral bioavailability of pindolol is 87-92%.L32388 A 5 mg oral dose reaches a Cmax of 33.1 ± 5.2 ng/mL, with a Tmax of 1-2 hours.L32388

Metabolisme

30-40% of a dose of pindolol is not metabolized.L32388 The remainder is hydroxylated and subsequently undergoes glucuronidation or sulfate conjugation.L32388

Rute Eliminasi

80% of an oral dose is eliminated in the urine,L32388 with 25-40% of the dose as the unchanged parent compound.L32353 6-9% of an intravenous dose is eliminated in the feces.L32353 Overall, 60-65% of a dose is eliminated as glucuronide and sulfate metabolites.L32353

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Alcohol may aggravate signs and symptoms of overdose.
  • 2. Take with or without food. Food does not significantly affect absorption.

Interaksi Obat

2016 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Pindolol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Pindolol is combined with Levodopa.
Risperidone Pindolol may increase the hypotensive activities of Risperidone.
Ceritinib Pindolol may increase the bradycardic activities of Ceritinib.
Ivabradine Pindolol may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Pindolol.
Alfuzosin Alfuzosin may increase the hypotensive activities of Pindolol.
Amifostine Pindolol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Pindolol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Pindolol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Pindolol.
Obinutuzumab Pindolol may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Pindolol.
Rituximab Pindolol may increase the hypotensive activities of Rituximab.
Doxapram Doxapram may decrease the antihypertensive activities of Pindolol.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Pindolol.
Dutasteride Dutasteride may decrease the antihypertensive activities of Pindolol.
Finasteride Finasteride may decrease the antihypertensive activities of Pindolol.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Pindolol.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Pindolol.
Tyramine Tyramine may decrease the antihypertensive activities of Pindolol.
Atipamezole Atipamezole may decrease the antihypertensive activities of Pindolol.
Siponimod Siponimod may decrease the antihypertensive activities of Pindolol.
Idazoxan Idazoxan may decrease the antihypertensive activities of Pindolol.
Tramazoline Tramazoline may decrease the antihypertensive activities of Pindolol.
Fenozolone Fenozolone may decrease the antihypertensive activities of Pindolol.
Xenon Xenon may decrease the antihypertensive activities of Pindolol.
Buflomedil Buflomedil may decrease the antihypertensive activities of Pindolol.
Mefenorex Mefenorex may decrease the antihypertensive activities of Pindolol.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Pindolol.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Pindolol.
Naxitamab Naxitamab may decrease the antihypertensive activities of Pindolol.
Buprenorphine Pindolol 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 Pindolol.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Pindolol.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Pindolol.
Hydrocodone Pindolol 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 Pindolol.
Magnesium sulfate The therapeutic efficacy of Pindolol can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Pindolol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Pindolol may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Pindolol.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Pindolol.
Orphenadrine Pindolol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Pindolol 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 Pindolol.
Pramipexole Pindolol may increase the sedative activities of Pramipexole.
Ropinirole Pindolol may increase the sedative activities of Ropinirole.
Rotigotine Pindolol may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Pindolol.
Sodium oxybate Pindolol may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Pindolol 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 Pindolol.
Thalidomide Pindolol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Pindolol may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Amiodarone The therapeutic efficacy of Pindolol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Pindolol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Pindolol.
Disopyramide Disopyramide may increase the bradycardic activities of Pindolol.
Dronedarone Dronedarone may increase the bradycardic activities of Pindolol.
Fingolimod Pindolol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Pindolol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Pindolol.
Methacholine Pindolol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Pindolol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Pindolol.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Pindolol.
Regorafenib Regorafenib may increase the bradycardic activities of Pindolol.
Reserpine Reserpine may increase the hypotensive activities of Pindolol.
Deserpidine Deserpidine may increase the hypotensive activities of Pindolol.
Guanethidine Guanethidine may increase the hypotensive activities of Pindolol.
Rivastigmine Pindolol may increase the bradycardic activities of Rivastigmine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Pindolol.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Pindolol.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Pindolol.
Dicoumarol The risk or severity of adverse effects can be increased when Pindolol is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Pindolol is combined with Phenindione.
Phenprocoumon The risk or severity of adverse effects can be increased when Pindolol is combined with Phenprocoumon.
Acenocoumarol The risk or severity of adverse effects can be increased when Pindolol is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Pindolol is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of adverse effects can be increased when Pindolol is combined with Coumarin.
(R)-warfarin The risk or severity of adverse effects can be increased when Pindolol is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Pindolol is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Pindolol is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Pindolol is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Pindolol is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Pindolol is combined with Tioclomarol.
(S)-Warfarin The risk or severity of adverse effects can be increased when Pindolol is combined with (S)-Warfarin.
Mirabegron The serum concentration of Pindolol can be increased when it is combined with Mirabegron.
Mirtazapine Pindolol may increase the serotonergic activities of Mirtazapine.
Nicorandil Nicorandil may increase the hypotensive activities of Pindolol.
Molsidomine Molsidomine may increase the hypotensive activities of Pindolol.
Insulin argine Pindolol may increase the hypoglycemic activities of Insulin argine.
Carteolol Carteolol may increase the hypotensive activities of Pindolol.
Dorzolamide Dorzolamide may increase the hypotensive activities of Pindolol.
Bimatoprost Bimatoprost may increase the hypotensive activities of Pindolol.
Metipranolol Pindolol may increase the hypotensive activities of Metipranolol.
Unoprostone Pindolol may increase the hypotensive activities of Unoprostone.
Minoxidil Minoxidil may increase the hypotensive activities of Pindolol.
Nitroglycerin Nitroglycerin may increase the hypotensive activities of Pindolol.

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: 30422499
    Alhayek S, Preuss CV: Beta 1 Receptors .
  • PMID: 10342782
    Blumenfeld JD, Sealey JE, Mann SJ, Bragat A, Marion R, Pecker MS, Sotelo J, August P, Pickering TG, Laragh JH: Beta-adrenergic receptor blockade as a therapeutic approach for suppressing the renin-angiotensin-aldosterone system in normotensive and hypertensive subjects. Am J Hypertens. 1999 May;12(5):451-9. doi: 10.1016/s0895-7061(99)00005-9.
  • PMID: 7049208
    Clark BJ, Menninger K, Bertholet A: Pindolol--the pharmacology of a partial agonist. Br J Clin Pharmacol. 1982;13(Suppl 2):149S-158S. doi: 10.1111/j.1365-2125.1982.tb01904.x.
  • PMID: 24685403
    Ferguson SS, Feldman RD: beta-adrenoceptors as molecular targets in the treatment of hypertension. Can J Cardiol. 2014 May;30(5 Suppl):S3-8. doi: 10.1016/j.cjca.2014.01.017. Epub 2014 Feb 12.
  • PMID: 6125395
    Belpaire FM, Bogaert MG, Rosseneu M: Binding of beta-adrenoceptor blocking drugs to human serum albumin, to alpha 1-acid glycoprotein and to human serum. Eur J Clin Pharmacol. 1982;22(3):253-6. doi: 10.1007/BF00545224.
  • PMID: 4398866
    Robak J, Gryglewski R: Influence of INPEA, pindolol and propranolol on the chronotropic and metabolic responses to -adrenergic stimulation in intact rats. Biochem Pharmacol. 1971 Oct;20(10):2749-58. doi: 10.1016/0006-2952(71)90184-5.
  • PMID: 5156091
    Walter I, Kusus T, Lydtin H: Clinical test of a new beta-receptor blockader in labile hypertension. Verh Dtsch Ges Inn Med. 1971;77:940-3.

Contoh Produk & Brand

Produk: 57 • International brands: 11
Produk
  • Apo-pindol Tab 10mg
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-pindol Tab 15mg
    Tablet • 15 mg • Oral • Canada • Generic • Approved
  • Apo-pindol Tab 5mg
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Dom-pindolol
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Dom-pindolol
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Dom-pindolol
    Tablet • 15 mg • Oral • Canada • Generic • Approved
  • Gen-pindolol Tab 15mg
    Tablet • 15 mg • Oral • Canada • Generic • Approved
  • Mylan-pindolol
    Tablet • 5 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 57 produk.
International Brands
  • Betapindol
  • Blockin L
  • Blocklin L
  • Calvisken
  • Decreten
  • Durapindol
  • Glauco-Visken
  • Pectobloc
  • Pinbetol
  • Prinodolol

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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