Peringatan Keamanan

Symptoms of propafenone overdose (usually most severe within the first 3 hours) may include convulsions (rarely), heartbeat irregularities, low blood pressure, and sleepiness.

Propafenone

DB01182

small molecule approved

Deskripsi

An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated.

Struktur Molekul 2D

Berat 341.444
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 2-10 hours
Volume Distribusi * 252 L
Klirens (Clearance) -

Absorpsi

Nearly completely absorbed following oral administration (90%). Systemic bioavailability ranges from 5 to 50%, due to significant first-pass metabolism. This wide range in systemic bioavailability is related to two factors: presence of food (food increases bioavailability) and dosage (bioavailability is 3.4% for a 150-mg tablet compared to 10.6% for a 300-mg tablet).

Metabolisme

Metabolized primarily in the liver where it is rapidly and extensively metabolized to two active metabolites, 5-hydroxypropafenone and N-depropylpropafenone. These metabolites have antiarrhythmic activity comparable to propafenone but are present in concentrations less than 25% of propafenone concentrations.

Rute Eliminasi

Approximately 50% of propafenone metabolites are excreted in the urine following administration of immediate release tablets.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products.
  • 2. Take with or without food. Take consistently at the same time in regard to meals.

Interaksi Obat

1606 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Propafenone.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Propafenone.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Propafenone.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Propafenone.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Propafenone.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Propafenone.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Propafenone.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Propafenone.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Propafenone.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Propafenone.
Silodosin The excretion of Silodosin can be decreased when combined with Propafenone.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Propafenone.
Ceritinib Propafenone may increase the bradycardic activities of Ceritinib.
Ivabradine Propafenone may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Propafenone.
Deferasirox The serum concentration of Propafenone can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Propafenone can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Propafenone can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Propafenone can be decreased when it is combined with Teriflunomide.
Remikiren Propafenone may decrease the antihypertensive activities of Remikiren.
Guanadrel Propafenone may decrease the antihypertensive activities of Guanadrel.
Chlorthalidone Propafenone may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Propafenone may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Propafenone may decrease the antihypertensive activities of Minoxidil.
Metolazone Propafenone may decrease the antihypertensive activities of Metolazone.
Cyclothiazide Propafenone may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Propafenone may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Propafenone may decrease the antihypertensive activities of Mecamylamine.
Nitroglycerin Propafenone may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Propafenone may decrease the antihypertensive activities of Metyrosine.
Hydroflumethiazide Propafenone may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Propafenone may decrease the antihypertensive activities of Cryptenamine.
Fenoldopam Propafenone may decrease the antihypertensive activities of Fenoldopam.
Chlorothiazide Propafenone may decrease the antihypertensive activities of Chlorothiazide.
Trichlormethiazide Propafenone may decrease the antihypertensive activities of Trichlormethiazide.
Pentolinium Propafenone may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Propafenone may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Propafenone may decrease the antihypertensive activities of Diazoxide.
Epoprostenol Propafenone may decrease the antihypertensive activities of Epoprostenol.
Polythiazide Propafenone may decrease the antihypertensive activities of Polythiazide.
Tienilic acid Propafenone may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Propafenone may decrease the antihypertensive activities of Diethylnorspermine.
Hexamethonium Propafenone may decrease the antihypertensive activities of Hexamethonium.
Rauwolfia serpentina root Propafenone may decrease the antihypertensive activities of Rauwolfia serpentina root.
Angiotensin 1-7 Propafenone may decrease the antihypertensive activities of Angiotensin 1-7.
BQ-123 Propafenone may decrease the antihypertensive activities of BQ-123.
Guanoxan Propafenone may decrease the antihypertensive activities of Guanoxan.
Vincamine Propafenone may decrease the antihypertensive activities of Vincamine.
Linsidomine Propafenone may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Propafenone may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Propafenone may decrease the antihypertensive activities of Tolonidine.
Endralazine Propafenone may decrease the antihypertensive activities of Endralazine.
Cadralazine Propafenone may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Propafenone may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Propafenone may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Propafenone may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Propafenone may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Propafenone may decrease the antihypertensive activities of Guanoclor.
Muzolimine Propafenone may decrease the antihypertensive activities of Muzolimine.
Xipamide Propafenone may decrease the antihypertensive activities of Xipamide.
Tocopherylquinone Propafenone may decrease the antihypertensive activities of Tocopherylquinone.
Furosemide Propafenone may decrease the antihypertensive activities of Furosemide.
Torasemide Propafenone may decrease the antihypertensive activities of Torasemide.
Bosentan Propafenone may decrease the antihypertensive activities of Bosentan.
Tadalafil Propafenone may decrease the antihypertensive activities of Tadalafil.
Hydralazine Propafenone may decrease the antihypertensive activities of Hydralazine.
Sitaxentan Propafenone may decrease the antihypertensive activities of Sitaxentan.
Pinacidil Propafenone may decrease the antihypertensive activities of Pinacidil.
Riociguat The serum concentration of Riociguat can be increased when it is combined with Propafenone.
Macitentan Propafenone may decrease the antihypertensive activities of Macitentan.
Ramipril Propafenone may decrease the antihypertensive activities of Ramipril.
Perindopril Propafenone may decrease the antihypertensive activities of Perindopril.
Levamlodipine The risk or severity of bradycardia can be increased when Levamlodipine is combined with Propafenone.
Buthiazide Propafenone may decrease the antihypertensive activities of Buthiazide.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Propafenone.
Dipyridamole Dipyridamole may increase the bradycardic activities of Propafenone.
Fingolimod Propafenone may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Propafenone is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Propafenone.
Methacholine Propafenone may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Propafenone.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Propafenone.
Esmolol The risk or severity of adverse effects can be increased when Propafenone is combined with Esmolol.
Betaxolol The risk or severity of adverse effects can be increased when Propafenone is combined with Betaxolol.
Metoprolol The risk or severity of adverse effects can be increased when Propafenone is combined with Metoprolol.
Atenolol The risk or severity of adverse effects can be increased when Propafenone is combined with Atenolol.
Sotalol The risk or severity of adverse effects can be increased when Propafenone is combined with Sotalol.
Labetalol The risk or severity of adverse effects can be increased when Propafenone is combined with Labetalol.
Alprenolol The risk or severity of adverse effects can be increased when Propafenone is combined with Alprenolol.
Pindolol The risk or severity of adverse effects can be increased when Propafenone is combined with Pindolol.
Carvedilol The risk or severity of adverse effects can be increased when Propafenone is combined with Carvedilol.
Acebutolol The risk or severity of adverse effects can be increased when Propafenone is combined with Acebutolol.
Nadolol The risk or severity of adverse effects can be increased when Propafenone is combined with Nadolol.
Bevantolol The risk or severity of adverse effects can be increased when Propafenone is combined with Bevantolol.
Practolol The risk or severity of adverse effects can be increased when Propafenone is combined with Practolol.
Penbutolol The risk or severity of adverse effects can be increased when Propafenone is combined with Penbutolol.
Oxprenolol The risk or severity of adverse effects can be increased when Propafenone is combined with Oxprenolol.
Dexpropranolol The risk or severity of adverse effects can be increased when Propafenone is combined with Dexpropranolol.
Celiprolol The risk or severity of adverse effects can be increased when Propafenone is combined with Celiprolol.
Nebivolol The risk or severity of adverse effects can be increased when Propafenone is combined with Nebivolol.

Target Protein

Sodium channel protein type 5 subunit alpha SCN5A
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2
Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2

Referensi & Sumber

Synthesis reference: Helmut Lietz, "Preparation of propafenone." U.S. Patent US4474986, issued May, 1974.

Contoh Produk & Brand

Produk: 165 • International brands: 0
Produk
  • Apo-propafenone
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Apo-propafenone
    Tablet • 300 mg • Oral • Canada • Generic • Approved
  • Myl-propafenone
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Myl-propafenone
    Tablet • 300 mg • Oral • Canada • Generic • Approved
  • Mylan-propafenone
    Tablet • 300 mg • Oral • Canada • Generic • Approved
  • Mylan-propafenone
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Nu-propafenone
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • PMS-propafenone
    Tablet • 150 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 165 produk.

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