Peringatan Keamanan

Quinidine overdoses have been well described. The ingestion of 5 g of quinidine resulted in the death of a toddler, while an adolescent was reported to survive after ingesting 8 g of quinidine.L42420,L3719 A 16-month that ingested quinidine tablets developed a concretion of bezoar in the stomach, which led to non-declining toxic levels of quinidine. A gastric aspirate revealed that quinidine levels were 50 times higher than the ones detected in plasma. In cases of massive overdose, it may be appropriate to perform an endoscopy.L42420 Acute quinidine overdoses are characterized by ventricular arrhythmias and hypotension. Other signs and symptoms of quinidine overdose may include vomiting, diarrhea, tinnitus, high-frequency hearing loss, vertigo, blurred vision, diplopia, photophobia, headache, confusion and delirium.L42420,L3719

Quinidine

DB00908

small molecule approved investigational

Deskripsi

Quinidine is a D-isomer of quinine present in the bark of the Cinchona tree and similar plant species. This alkaloid was first described in 1848 and has a long history as an antiarrhythmic medication.A38016,A250050 Quinidine is considered the first antiarrhythmic drug (class Ia) and is moderately efficacious in the acute conversion of atrial fibrillation to normal sinus rhythm.A38016 It prolongs cellular action potential by blocking sodium and potassium currents. A phenomenon known as “quinidine syncope” was first described in the 1950s, characterized by syncopal attacks and ventricular fibrillation in patients treated with this drug.A38016 Due to its side effects and increased risk of mortality, the use of quinidine was reduced over the next few decades. However, it continues to be used in the treatment of Brugada syndrome, short QT syndrome and idiopathic ventricular fibrillation.A250050

Struktur Molekul 2D

Berat 324.4168
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of quinidine is 6-8 hours in adults and 3-4 hours in pediatric patients.[L42420,L3719]
Volume Distribusi Quinidine has a volume of distribution of 2-3 L/kg in healthy young adults, 0.5 L/kg in patients with congestive heart failure, and 3-5 L/kg in patients with liver cirrhosis.[L42420,L3719]
Klirens (Clearance) The clearance of quinidine ranges from 3 to 5 mL/min/kg in adults. In pediatric patients, quinidine clearance may be two or three times as rapid.[L42420,L3719]

Absorpsi

The absolute bioavailability of quinidine sulfate is approximately 70%, but it ranges from 45% to 100%. The less-than-complete quinidine sulfate bioavailability is a result of first-pass metabolism in the liver.L42420 In contrast, the absolute bioavailability of quinidine gluconate ranges from 70% to 80%, and relative to quinidine sulfate, quinidine from quinidine gluconate has a bioavailability of 1.03.L3719 The tmax of quinidine sulfate extended-release tablets is approximately 6 hL42420, while the tmax of quinidine gluconate goes from 3 to 5 h.L3719 The peak serum concentration reached with immediate-release quinidine sulfate is delayed for about an hour when taken with food. Furthermore, the ingestion of grapefruit juice may decrease the rate of absorption of quinidine.L42420,L3719

Metabolisme

Quinidine is mainly metabolized in the liver by cytochrome P450 enzymes, specifically CYP3A4. The major metabolite of quinidine is 3-hydroxy-quinidine, which has a volume of distribution larger than quinidine and an elimination half-life of about 12 hours.L42420,L3719 Non-clinical and clinical studies suggest that 3-hydroxy-quinidine has approximately half the antiarrhythmic activity of quinidine; therefore, this metabolite is partly responsible for the effects detected with the chronic use of quinidine.L42420,L3719

Rute Eliminasi

The elimination of quinidine is achieved by the renal excretion of the unchanged drug (15 to 40% of total clearance) and its hepatic biotransformation to a variety of metabolites (60 to 85% of total clearance).A250080 When urine has a pH lower than 7, 20% of administered quinidine appears in urine unchanged. However, this proportion decreases to as little as 5% as it becomes more alkaline. The renal clearance of quinidine involves both glomerular filtration and active tubular secretion, moderated by pH-dependent tubular reabsorption.L42420,L3719

Interaksi Makanan

4 Data
  • 1. Exercise caution with grapefruit products. Grapefruit may delay the absorption of quinidine, and inhibit its metabolism through CYP3A4.
  • 2. Exercise caution with St. John's Wort.
  • 3. Take separate from antacids. Antacids may reduce the absorption of quinidine.
  • 4. Take with or without food. Taking quinidine with food may slow its absorption.

Interaksi Obat

2361 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Quinidine.
Modafinil The metabolism of Quinidine can be increased when combined with Modafinil.
Armodafinil The metabolism of Quinidine can be increased when combined with Armodafinil.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Quinidine.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Quinidine.
Glycochenodeoxycholic Acid Quinidine may decrease the excretion rate of Glycochenodeoxycholic Acid which could result in a higher serum level.
Pravastatin Quinidine may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Fluorescein Quinidine may decrease the excretion rate of Fluorescein which could result in a higher serum level.
Indocyanine green acid form Quinidine may decrease the excretion rate of Indocyanine green acid form which could result in a higher serum level.
Glycyrrhizic acid Quinidine may decrease the excretion rate of Glycyrrhizic acid which could result in a higher serum level.
Repaglinide Quinidine may decrease the excretion rate of Repaglinide which could result in a higher serum level.
Ezetimibe Quinidine may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Spironolactone Quinidine may decrease the antihypertensive activities of Spironolactone.
Loratadine Quinidine may decrease the excretion rate of Loratadine which could result in a higher serum level.
Telmisartan Quinidine may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Disulfiram Quinidine may decrease the excretion rate of Disulfiram which could result in a higher serum level.
Ursodeoxycholic acid Quinidine may decrease the excretion rate of Ursodeoxycholic acid which could result in a higher serum level.
Benzbromarone Quinidine may decrease the excretion rate of Benzbromarone which could result in a higher serum level.
Belantamab mafodotin Quinidine may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Quinidine.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Quinidine.
Lomitapide The metabolism of Lomitapide can be decreased when combined with Quinidine.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Quinidine.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Quinidine.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Quinidine.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Quinidine.
Silodosin The excretion of Silodosin can be decreased when combined with Quinidine.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Quinidine.
Remikiren Quinidine may decrease the antihypertensive activities of Remikiren.
Guanadrel Quinidine may decrease the antihypertensive activities of Guanadrel.
Minoxidil Quinidine may decrease the antihypertensive activities of Minoxidil.
Trandolapril Quinidine may decrease the antihypertensive activities of Trandolapril.
Benazepril Quinidine may decrease the antihypertensive activities of Benazepril.
Candoxatril Quinidine may decrease the antihypertensive activities of Candoxatril.
Nitroglycerin Quinidine may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Quinidine may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Quinidine may decrease the antihypertensive activities of Cryptenamine.
Eprosartan Quinidine may decrease the antihypertensive activities of Eprosartan.
Deserpidine Quinidine may decrease the antihypertensive activities of Deserpidine.
Saprisartan Quinidine may decrease the antihypertensive activities of Saprisartan.
Spirapril Quinidine may decrease the antihypertensive activities of Spirapril.
Diethylnorspermine Quinidine may decrease the antihypertensive activities of Diethylnorspermine.
Rauwolfia serpentina root Quinidine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Angiotensin 1-7 Quinidine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Quinidine may decrease the antihypertensive activities of Imidapril.
BQ-123 Quinidine may decrease the antihypertensive activities of BQ-123.
Zofenopril Quinidine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Quinidine may decrease the antihypertensive activities of Guanoxan.
Delapril Quinidine may decrease the antihypertensive activities of Delapril.
Vincamine Quinidine may decrease the antihypertensive activities of Vincamine.
Linsidomine Quinidine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Quinidine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Quinidine may decrease the antihypertensive activities of Tolonidine.
Endralazine Quinidine may decrease the antihypertensive activities of Endralazine.
Cadralazine Quinidine may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Quinidine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Quinidine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Quinidine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Quinidine may decrease the antihypertensive activities of Guanoclor.
Benazeprilat Quinidine may decrease the antihypertensive activities of Benazeprilat.
Ramiprilat Quinidine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Quinidine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Quinidine may decrease the antihypertensive activities of Quinaprilat.
Pinacidil Quinidine may decrease the antihypertensive activities of Pinacidil.
Riociguat The serum concentration of Riociguat can be increased when it is combined with Quinidine.
Aliskiren Quinidine may decrease the antihypertensive activities of Aliskiren.
Cilazapril Quinidine may decrease the antihypertensive activities of Cilazapril.
Ramipril Quinidine may decrease the antihypertensive activities of Ramipril.
Azilsartan medoxomil Quinidine may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Quinidine may decrease the antihypertensive activities of Diazoxide.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Quinidine.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Quinidine.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Quinidine.
Erythromycin The risk or severity of QTc prolongation can be increased when Erythromycin is combined with Quinidine.
Azithromycin The serum concentration of Quinidine can be increased when it is combined with Azithromycin.
Sirolimus The serum concentration of Quinidine can be increased when it is combined with Sirolimus.
Dirithromycin The serum concentration of Quinidine can be increased when it is combined with Dirithromycin.
Telithromycin The metabolism of Quinidine can be decreased when combined with Telithromycin.
Candicidin The serum concentration of Quinidine can be increased when it is combined with Candicidin.
Clarithromycin The metabolism of Quinidine can be decreased when combined with Clarithromycin.
Josamycin The serum concentration of Quinidine can be increased when it is combined with Josamycin.
Epothilone D The serum concentration of Quinidine can be increased when it is combined with Epothilone D.
Patupilone The serum concentration of Quinidine can be increased when it is combined with Patupilone.
6-Deoxyerythronolide B The serum concentration of Quinidine can be increased when it is combined with 6-Deoxyerythronolide B.
Ixabepilone The serum concentration of Quinidine can be increased when it is combined with Ixabepilone.
KOS-1584 The serum concentration of Quinidine can be increased when it is combined with KOS-1584.
Ridaforolimus The serum concentration of Quinidine can be increased when it is combined with Ridaforolimus.
Temsirolimus The serum concentration of Quinidine can be increased when it is combined with Temsirolimus.
AVE9633 The serum concentration of Quinidine can be increased when it is combined with AVE9633.
Coltuximab ravtansine The serum concentration of Quinidine can be increased when it is combined with Coltuximab ravtansine.
Cethromycin The serum concentration of Quinidine can be increased when it is combined with Cethromycin.
Mitemcinal The serum concentration of Quinidine can be increased when it is combined with Mitemcinal.
Brefeldin A The serum concentration of Quinidine can be increased when it is combined with Brefeldin A.
Solithromycin The serum concentration of Quinidine can be increased when it is combined with Solithromycin.
Kitasamycin The serum concentration of Quinidine can be increased when it is combined with Kitasamycin.
Carbomycin The serum concentration of Quinidine can be increased when it is combined with Carbomycin.
Doramectin The serum concentration of Quinidine can be increased when it is combined with Doramectin.
Eprinomectin The serum concentration of Quinidine can be increased when it is combined with Eprinomectin.
Oleandomycin The serum concentration of Quinidine can be increased when it is combined with Oleandomycin.
Selamectin The serum concentration of Quinidine can be increased when it is combined with Selamectin.

Target Protein

Sodium channel protein type 5 subunit alpha SCN5A
Potassium channel subfamily K member 1 KCNK1
Potassium channel subfamily K member 6 KCNK6
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2
Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
Alpha-1D adrenergic receptor ADRA1D

Referensi & Sumber

Synthesis reference: Jean Paul REMON, Chris Vervaet, "QUININE AND QUINIDINE SALTS, METHODS FOR MAKING THEM, AND PHARMACEUTICAL FORMULATIONS COMPRISING THEM." U.S. Patent US20090239900, issued September 24, 2009.
Artikel (PubMed)
  • PMID: 19249010
    Yang F, Hanon S, Lam P, Schweitzer P: Quinidine revisited. Am J Med. 2009 Apr;122(4):317-21. doi: 10.1016/j.amjmed.2008.11.019. Epub 2009 Feb 25.
  • PMID: 31026503
    Vitali Serdoz L, Rittger H, Furlanello F, Bastian D: Quinidine-A legacy within the modern era of antiarrhythmic therapy. Pharmacol Res. 2019 Jun;144:257-263. doi: 10.1016/j.phrs.2019.04.028. Epub 2019 Apr 23.
  • PMID: 24011539
    Priori SG, Wilde AA, Horie M, Cho Y, Behr ER, Berul C, Blom N, Brugada J, Chiang CE, Huikuri H, Kannankeril P, Krahn A, Leenhardt A, Moss A, Schwartz PJ, Shimizu W, Tomaselli G, Tracy C: HRS/EHRA/APHRS expert consensus statement on the diagnosis and management of patients with inherited primary arrhythmia syndromes: document endorsed by HRS, EHRA, and APHRS in May 2013 and by ACCF, AHA, PACES, and AEPC in June 2013. Heart Rhythm. 2013 Dec;10(12):1932-63. doi: 10.1016/j.hrthm.2013.05.014. Epub 2013 Aug 30.
  • PMID: 6988137
    Ochs HR, Greenblatt DJ, Woo E: Clinical pharmacokinetics of quinidine. Clin Pharmacokinet. 1980 Mar-Apr;5(2):150-68. doi: 10.2165/00003088-198005020-00003.

Contoh Produk & Brand

Produk: 37 • International brands: 7
Produk
  • Apo Quinidine Tab 200mg
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Apo-quin-G Tab 325mg
    Tablet • 325 mg • Oral • Canada • Generic • Approved
  • Cardioquin Tablets
    Tablet • 275 mg / tab • Oral • Canada • Approved
  • Novo-quinidin 200mg
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Nuedexta
    Capsule, gelatin coated • - • Oral • US • Approved
  • Nuedexta
    Capsule, gelatin coated • - • Oral • US • Approved
  • Quinate Tab 325mg
    Tablet • 325 mg • Oral • Canada • Approved
  • Quinidex Extentabs Srt 300mg
    Tablet, extended release • 300 mg • Oral • Canada • Approved
Menampilkan 8 dari 37 produk.
International Brands
  • Cardioquin
  • Kinidin
  • Quin-Release
  • Quinaglute
  • Quinalan
  • Quinicardine
  • Quinidex

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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