Peringatan Keamanan

The reported LD50 of oral ranolazine in the rat is 980 mg/kg.MSDS High oral doses of ranolazine have led to dizziness, nausea, and vomiting. These effects have been shown to be dose related. High intravenous doses can cause diplopia, confusion, paresthesia, in addition to syncope. In
the case of an overdose, provide supportive therapy accompanied by continuous ECG monitoring for QT interval prolongation.L3580

Ranolazine

DB00243

small molecule approved investigational

Deskripsi

Chronic angina is a common cardiovascular condition affecting millions worldwide and causes significant disability while interfering with daily activities.A189234 Ranolazine is a well-tolerated piperazine derivative used for the management of this condition, offering relief from uncomfortable and debilitating symptoms.L3580 With a mechanism of action different from drugs used to treat the same condition, ranolazine is a promising anti-anginal therapy. It was originally approved by the FDA in 2006.L5440

Struktur Molekul 2D

Berat 427.5365
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The apparent terminal half-life of ranolazine is 7 hours.[A175030,L3580]
Volume Distribusi The mean apparent volume of distribution of ranolazine is reported to be 53.2 L[L5473] and the average steady-state volume of distribution is estimated to range from 85 to 180 L.[A38645]
Klirens (Clearance) The reported clearance rate of orally administered ranolazine is of 45 L/h when administered at a dose of 500 mg twice daily.[A38645] The clearance rate of ranolazine is dose-dependent and renal impairment can increase ranolazine serum concentration by 40-50%.[A174946]

Absorpsi

The time to reach peak serum concentration is quite variable but has been observed to be in the range of 2-6 hours, with steady-state within 3 days.A174898 The FDA indicates a Tmax of 3-5 hours.L3580 The average steady-state Cmax is about 2600 ng/mL. Absorption of ranolazine is not significantly affected by food consumption.A174940 The bioavailability of ranolazine taken in the tablet form compared to that from a solution of ranolazine is about 76%.L3580

Metabolisme

Ranolazine is rapidly heavily metabolized in the liver an gastrointestinal tract through the activity of the CYP3A4 enzyme with minor contributions from CYP2D6.A174898,A174913,L3580 More than 40 ranolazine metabolites have been found in plasma and more than 100 metabolites have been identified in the urine.A174946 Ranolazine and some of its metabolites are known to weakly inhibit CYP3A4. However, the activity of the metabolites of ranolazine has not been fully elucidated.L5473

Rute Eliminasi

From the administered dose, about 3/4 of the dose is excreted renally, while 1/4 of the dose is excreted in the feces. An estimated 5% of an ingested dose is excreted as unchanged drug.A174898,L3580

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1532 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Ranolazine.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Ranolazine.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Ranolazine.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Ranolazine which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Ranolazine which could result in a higher serum level.
Ethinylestradiol Ethinylestradiol may decrease the excretion rate of Ranolazine which could result in a higher serum level.
Glyburide Glyburide may decrease the excretion rate of Ranolazine which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Ranolazine which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Ranolazine which could result in a higher serum level.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Ranolazine.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Ranolazine.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Ranolazine.
Lomitapide The metabolism of Lomitapide can be decreased when combined with Ranolazine.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Ranolazine.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Ranolazine.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Ranolazine.
Loxapine The serum concentration of Ranolazine can be increased when it is combined with Loxapine.
Zonisamide The serum concentration of Ranolazine can be increased when it is combined with Zonisamide.
Carvedilol The serum concentration of Ranolazine can be increased when it is combined with Carvedilol.
Propafenone The serum concentration of Ranolazine can be increased when it is combined with Propafenone.
Lapatinib The serum concentration of Ranolazine can be increased when it is combined with Lapatinib.
Mibefradil The serum concentration of Ranolazine can be increased when it is combined with Mibefradil.
Biricodar The serum concentration of Ranolazine can be increased when it is combined with Biricodar.
Elacridar The serum concentration of Ranolazine can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Ranolazine can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Ranolazine can be increased when it is combined with Vandetanib.
Zosuquidar The serum concentration of Ranolazine can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Ranolazine can be increased when it is combined with Tariquidar.
Brefeldin A The serum concentration of Ranolazine can be increased when it is combined with Brefeldin A.
Ivacaftor The serum concentration of Ranolazine can be increased when it is combined with Ivacaftor.
Vorapaxar The serum concentration of Ranolazine can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Ranolazine can be increased when it is combined with Suvorexant.
Daclatasvir The serum concentration of Ranolazine can be increased when it is combined with Daclatasvir.
Niguldipine The serum concentration of Ranolazine can be increased when it is combined with Niguldipine.
Rolapitant The serum concentration of Ranolazine can be increased when it is combined with Rolapitant.
Neratinib The serum concentration of Ranolazine can be increased when it is combined with Neratinib.
Sarecycline The serum concentration of Ranolazine can be increased when it is combined with Sarecycline.
Laniquidar The serum concentration of Ranolazine can be increased when it is combined with Laniquidar.
Dexniguldipine The serum concentration of Ranolazine can be increased when it is combined with Dexniguldipine.
ONT-093 The serum concentration of Ranolazine can be increased when it is combined with ONT-093.
Istradefylline The serum concentration of Ranolazine can be increased when it is combined with Istradefylline.
Erythromycin The serum concentration of Ranolazine can be increased when it is combined with Erythromycin.
Reserpine The serum concentration of Ranolazine can be increased when it is combined with Reserpine.
Sorafenib The serum concentration of Ranolazine can be increased when it is combined with Sorafenib.
Verapamil The serum concentration of Ranolazine can be increased when it is combined with Verapamil.
Tacrolimus The serum concentration of Ranolazine can be increased when it is combined with Tacrolimus.
Carfilzomib The serum concentration of Ranolazine can be increased when it is combined with Carfilzomib.
Entrectinib The serum concentration of Ranolazine can be increased when it is combined with Entrectinib.
Erdafitinib The serum concentration of Ranolazine can be increased when it is combined with Erdafitinib.
Regorafenib The serum concentration of Ranolazine can be increased when it is combined with Regorafenib.
Palbociclib The serum concentration of Ranolazine can be increased when it is combined with Palbociclib.
Mefloquine The serum concentration of Ranolazine can be increased when it is combined with Mefloquine.
Arsenic trioxide The serum concentration of Ranolazine can be increased when it is combined with Arsenic trioxide.
Favipiravir The serum concentration of Ranolazine can be increased when it is combined with Favipiravir.
Ixabepilone The serum concentration of Ranolazine can be increased when it is combined with Ixabepilone.
Clofazimine The serum concentration of Ranolazine can be increased when it is combined with Clofazimine.
Ponatinib The serum concentration of Ranolazine can be increased when it is combined with Ponatinib.
Cethromycin The serum concentration of Ranolazine can be increased when it is combined with Cethromycin.
Voclosporin The serum concentration of Ranolazine can be increased when it is combined with Voclosporin.
Umbralisib The serum concentration of Ranolazine can be increased when it is combined with Umbralisib.
Diosmin The serum concentration of Ranolazine can be increased when it is combined with Diosmin.
Sapropterin The serum concentration of Ranolazine can be increased when it is combined with Sapropterin.
Levoketoconazole The metabolism of Ranolazine can be decreased when combined with Levoketoconazole.
Belumosudil The serum concentration of Ranolazine can be increased when it is combined with Belumosudil.
Cyclosporine The serum concentration of Ranolazine can be increased when it is combined with Cyclosporine.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Ranolazine.
Sildenafil The serum concentration of Ranolazine can be increased when it is combined with Sildenafil.
Morphine The serum concentration of Morphine can be increased when it is combined with Ranolazine.
Tenofovir disoproxil The serum concentration of Tenofovir disoproxil can be increased when it is combined with Ranolazine.
Toremifene The serum concentration of Ranolazine can be increased when it is combined with Toremifene.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Ranolazine.
Bisoprolol The serum concentration of Bisoprolol can be increased when it is combined with Ranolazine.
Mannitol The serum concentration of Mannitol can be increased when it is combined with Ranolazine.
Vardenafil The serum concentration of Ranolazine can be increased when it is combined with Vardenafil.
Sirolimus The serum concentration of Sirolimus can be increased when it is combined with Ranolazine.
Clomifene The serum concentration of Clomifene can be increased when it is combined with Ranolazine.
Quinidine The serum concentration of Ranolazine can be increased when it is combined with Quinidine.
Fexofenadine The serum concentration of Fexofenadine can be increased when it is combined with Ranolazine.
Dactinomycin The serum concentration of Dactinomycin can be increased when it is combined with Ranolazine.
Tegaserod The serum concentration of Tegaserod can be increased when it is combined with Ranolazine.
Dasatinib The serum concentration of Dasatinib can be increased when it is combined with Ranolazine.
Sitagliptin The serum concentration of Sitagliptin can be increased when it is combined with Ranolazine.
Paliperidone The serum concentration of Ranolazine can be increased when it is combined with Paliperidone.
Digitoxin The serum concentration of Digitoxin can be increased when it is combined with Ranolazine.
Belinostat The serum concentration of Belinostat can be increased when it is combined with Ranolazine.
Indacaterol The serum concentration of Indacaterol can be increased when it is combined with Ranolazine.
Cobimetinib The serum concentration of Cobimetinib can be increased when it is combined with Ranolazine.
Trastuzumab emtansine The serum concentration of Trastuzumab emtansine can be increased when it is combined with Ranolazine.
Inotuzumab ozogamicin The risk or severity of QTc prolongation can be increased when Ranolazine is combined with Inotuzumab ozogamicin.
Romidepsin The serum concentration of Romidepsin can be increased when it is combined with Ranolazine.
Tolvaptan The serum concentration of Tolvaptan can be increased when it is combined with Ranolazine.
Rivaroxaban The serum concentration of Rivaroxaban can be increased when it is combined with Ranolazine.
Temsirolimus The serum concentration of Ranolazine can be increased when it is combined with Temsirolimus.
Simeprevir The serum concentration of Ranolazine can be increased when it is combined with Simeprevir.
Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Ranolazine.
Panobinostat The serum concentration of Panobinostat can be increased when it is combined with Ranolazine.
Apixaban The serum concentration of Apixaban can be increased when it is combined with Ranolazine.
Odanacatib The serum concentration of Odanacatib can be increased when it is combined with Ranolazine.
Dabigatran etexilate The serum concentration of Dabigatran etexilate can be increased when it is combined with Ranolazine.
Cabazitaxel The metabolism of Cabazitaxel can be decreased when combined with Ranolazine.

Target Protein

Plasminogen PLG
Sodium channel protein SCN1A
Inward rectifier potassium channel KCNJ12
Voltage gated L-type calcium channel CACNA1C
Alpha-1 adrenergic receptors ADRA1A
Beta-1 adrenergic receptor ADRB1
Fatty acid

Referensi & Sumber

Synthesis reference: Gilla Goverdhan, Anumula Raghupathi, Reddy Aalla, Sampath Kurella, Srinivas Vurimidi, Himabindu Ghanta, Mahesh Reddy.(2019).Improved Process for Ranolazine. Organic Process Research & Development 2009, 13, 1, 67-72
Artikel (PubMed)
  • PMID: 26979079
    Rayner-Hartley E, Sedlak T: Ranolazine: A Contemporary Review. J Am Heart Assoc. 2016 Mar 15;5(3):e003196. doi: 10.1161/JAHA.116.003196.
  • PMID: 26459200
    Saad M, Mahmoud A, Elgendy IY, Richard Conti C: Ranolazine in Cardiac Arrhythmia. Clin Cardiol. 2016 Mar;39(3):170-8. doi: 10.1002/clc.22476. Epub 2015 Oct 13.
  • PMID: 29939605
    Reed M, Nicolas D: Ranolazine .
  • PMID: 29666676
    Mezincescu A, Karthikeyan VJ, Nadar SK: Ranolazine: A true pluripotent cardiovascular drug or jack of all trades, master of none? Sultan Qaboos Univ Med J. 2018 Feb;18(1):e13-e23. doi: 10.18295/squmj.2018.18.01.003. Epub 2018 Apr 4.
  • PMID: 25028555
    Codolosa JN, Acharjee S, Figueredo VM: Update on ranolazine in the management of angina. Vasc Health Risk Manag. 2014 Jun 24;10:353-62. doi: 10.2147/VHRM.S40477. eCollection 2014.
  • PMID: 16640453
    Jerling M: Clinical pharmacokinetics of ranolazine. Clin Pharmacokinet. 2006;45(5):469-91. doi: 10.2165/00003088-200645050-00003.
  • PMID: 16787254
    Thomas D, Karle CA, Kiehn J: The cardiac hERG/IKr potassium channel as pharmacological target: structure, function, regulation, and clinical applications. Curr Pharm Des. 2006;12(18):2271-83. doi: 10.2174/138161206777585102.
  • PMID: 28082152
    Balestrini S, Sisodiya SM: Pharmacogenomics in epilepsy. Neurosci Lett. 2018 Feb 22;667:27-39. doi: 10.1016/j.neulet.2017.01.014. Epub 2017 Jan 10.
Menampilkan 8 dari 13 artikel.

Contoh Produk & Brand

Produk: 88 • International brands: 0
Produk
  • Aspruzyo Sprinkle
    Granule • 500 mg/1 • Oral • US • Approved
  • Aspruzyo Sprinkle
    Granule • 1000 mg/1 • Oral • US • Approved
  • Corzyna
    Tablet, extended release • 500 mg • Oral • Canada • Approved
  • Corzyna
    Tablet, extended release • 1000 mg • Oral • Canada • Approved
  • Ranexa
    Tablet, film coated, extended release • 500 mg/1 • Oral • US • Approved
  • Ranexa
    Tablet, film coated, extended release • 1000 mg/1 • Oral • US • Approved
  • Ranexa
    Tablet, film coated, extended release • 500 mg/1 • Oral • US • Approved
  • Ranexa
    Tablet, film coated, extended release • 1000 mg/1 • Oral • US • Approved
Menampilkan 8 dari 88 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul