Peringatan Keamanan

The reported oral LD50 of pravastatin in mice is of 8939 mg/kg.MSDS There haven't been significant overdosage reports however, in the case of overdosage, symptomatic treatment is recommended along with laboratory monitoring and supportive measures.FDA label

In carcinogenic studies, high dose administration of pravastatin has been reported to increase the incidence of hepatocellular carcinomas in males and lung carcinomas in females. There is no evidence relating the administration of pravastatin with mutagenicity in different assays not to produce effects in fertility or reproductive potential.FDA label

Pravastatin

DB00175

small molecule approved

Deskripsi

Pravastatin is the 6-alpha-hydroxy acid form of mevastatin.T303 Pravastatin was firstly approved in 1991 becoming the second available statin in the United States. It was the first statin administered as the active form and not as a prodrug.T274 This drug was developed by Sankyo Co. Ltd.; however, the first approved pravastatin product was developed by Bristol Myers Squibb and FDA approved in 1991.L6142

Pravastatin is made through a fermentation process in which mevastatin is first obtained. The manufacturing process is followed by the hydrolysis of the lactone group and the biological hydroxylation with Streptomyces carbophilus to introduce the allylic 6-alcohol group.T239

Struktur Molekul 2D

Berat 424.5277
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The reported elimination half-life of pravastatin is reported to be of 1.8 hours.[A34502]
Volume Distribusi The reported steady-state volume of distribution of pravastatin is reported to be of 0.5 L/kg.[A177913] This pharmacokinetic parameter in children was found to range from 31-37 ml/kg.[A177907]
Klirens (Clearance) The reported clearance rate of pravastatin ranges from 6.3-13.5 ml.min/kg in adults[A177913] while in children it has been reported to be of 4-11 L/min.[A177907]

Absorpsi

Pravastatin is absorbed 60-90 min after oral administration and it presents a low bioavailability of 17%.A34502 This low bioavailability can be presented due to the polar nature of pravastatin which produces a high range of first-pass metabolism and incomplete absorption.T239 Pravastatin is rapidly absorbed from the upper part of the small intestine via proton-coupled carrier-mediated transport to be later taken up in the livery by the sodium-independent bile acid transporter.A39676 The reported time to reach the peak serum concentration in the range of 30-55 mcg/L is of 1-1.5 hours with an AUC ranging from 60-90 mcg.h/L.A177907

Metabolisme

After initial administration, pravastatin undergoes extensive first-pass extraction in the liver.A34502 However, pravastatin's metabolism is not related to the activity of the cytochrome P-450 isoenzymes and its processing is performed in a minor extent in the liver. Therefore, this drug is highly exposed to peripheral tissues.A177682 The metabolism of pravastatin is ruled mainly by the presence of glucuronidation reactions with very minimal intervention of CYP3A enzymes. After metabolism, pravastatin does not produce active metabolites.A34502 This metabolism is mainly done in the stomach followed by a minor portion of renal and hepatic processing.A39676 The major metabolite formed as part of pravastatin metabolism is the 3-alpha-hydroxy isomer. The activity of this metabolite is very clinically negligible.F4603

Rute Eliminasi

From the administered dose of pravastatin, about 70% is eliminated in the feces while about 20% is obtained in the urine.T357 When pravastatin is administered intravenously, approximately 47% of the administered dose is eliminated via the urine with 53% of the dose eliminated either via biotransformation of biliary.F4603

Farmakogenomik

2 Varian
KIF6 (rs20455)

Patients with this genotype have a greater reduction in risk of a major cardiovascular event with high dose pravastatin.

HMGCR (rs17244841)

Patients with this genotype have a lesser reduction in LDL cholesterol with pravastatin.

Interaksi Makanan

1 Data
  • 1. Take with or without food. Lipid lowering effects are similar in the fasting and fed state.

Interaksi Obat

590 Data
Troglitazone Troglitazone may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Reserpine Reserpine may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Chlorpromazine Chlorpromazine may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Cimetidine Cimetidine may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Tamoxifen Tamoxifen may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Quinidine Quinidine may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Tipranavir Tipranavir may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Ethinylestradiol Ethinylestradiol may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Glyburide Glyburide may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Letermovir The excretion of Pravastatin can be decreased when combined with Letermovir.
Valinomycin Valinomycin may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Nifedipine Pravastatin may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Cyclosporine The serum concentration of Pravastatin can be increased when it is combined with Cyclosporine.
Ranolazine The serum concentration of Pravastatin can be increased when it is combined with Ranolazine.
Acipimox Acipimox may increase the myopathic rhabdomyolysis activities of Pravastatin.
Bezafibrate Bezafibrate may increase the myopathic rhabdomyolysis activities of Pravastatin.
Boceprevir The serum concentration of Pravastatin can be increased when it is combined with Boceprevir.
Ciprofibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ciprofibrate is combined with Pravastatin.
Colchicine Colchicine may increase the myopathic rhabdomyolysis activities of Pravastatin.
Daptomycin The risk or severity of myopathy can be increased when Pravastatin is combined with Daptomycin.
Darunavir The serum concentration of Pravastatin can be increased when it is combined with Darunavir.
Efavirenz The serum concentration of Pravastatin can be decreased when it is combined with Efavirenz.
Gemfibrozil The risk or severity of rhabdomyolysis, myoglobinuria, and elevated creatine kinase (CPK) can be increased when Gemfibrozil is combined with Pravastatin.
Nelfinavir The serum concentration of Pravastatin can be decreased when it is combined with Nelfinavir.
Niacin The risk or severity of myopathy and rhabdomyolysis can be increased when Niacin is combined with Pravastatin.
Paroxetine The risk or severity of increased glucose can be increased when Pravastatin is combined with Paroxetine.
Pazopanib Pravastatin may increase the hepatotoxic activities of Pazopanib.
Raltegravir The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Pravastatin.
Saquinavir The serum concentration of Pravastatin can be decreased when it is combined with Saquinavir.
Simeprevir The serum concentration of Pravastatin can be increased when it is combined with Simeprevir.
Telaprevir The serum concentration of Pravastatin can be increased when it is combined with Telaprevir.
Telithromycin The serum concentration of Pravastatin can be increased when it is combined with Telithromycin.
Trabectedin The risk or severity of myopathy and rhabdomyolysis can be increased when Pravastatin is combined with Trabectedin.
Erythromycin The risk or severity of myopathy and rhabdomyolysis can be increased when Erythromycin is combined with Pravastatin.
Amiodarone The metabolism of Pravastatin can be increased when combined with Amiodarone.
Bosentan The serum concentration of Pravastatin can be decreased when it is combined with Bosentan.
Danazol The serum concentration of Pravastatin can be increased when it is combined with Danazol.
Colestipol Colestipol can cause a decrease in the absorption of Pravastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Pravastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Pravastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Pravastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aspartame The excretion of Pravastatin can be decreased when combined with Aspartame.
Succinic acid The excretion of Succinic acid can be decreased when combined with Pravastatin.
Citrulline The excretion of Citrulline can be decreased when combined with Pravastatin.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Pravastatin.
Cefotiam The excretion of Cefotiam can be decreased when combined with Pravastatin.
Piperacillin The excretion of Piperacillin can be decreased when combined with Pravastatin.
Aminohippuric acid The excretion of Aminohippuric acid can be decreased when combined with Pravastatin.
Trifluridine The excretion of Trifluridine can be decreased when combined with Pravastatin.
Cefdinir The excretion of Cefdinir can be decreased when combined with Pravastatin.
Cephalexin The excretion of Cephalexin can be decreased when combined with Pravastatin.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Pravastatin.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Pravastatin.
Leucovorin The excretion of Leucovorin can be decreased when combined with Pravastatin.
Fluorescein The excretion of Fluorescein can be decreased when combined with Pravastatin.
Acyclovir The excretion of Acyclovir can be decreased when combined with Pravastatin.
Cefaclor The excretion of Cefaclor can be decreased when combined with Pravastatin.
Quinapril The excretion of Quinapril can be decreased when combined with Pravastatin.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Pravastatin.
Famotidine The excretion of Famotidine can be decreased when combined with Pravastatin.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Pravastatin.
Cefazolin The excretion of Cefazolin can be decreased when combined with Pravastatin.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Pravastatin.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Pravastatin.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Pravastatin.
Tazobactam The excretion of Tazobactam can be decreased when combined with Pravastatin.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Pravastatin.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Pravastatin.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Pravastatin.
Doripenem The excretion of Doripenem can be decreased when combined with Pravastatin.
Saxagliptin The excretion of Saxagliptin can be decreased when combined with Pravastatin.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Pravastatin.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Pravastatin.
Avibactam The excretion of Avibactam can be decreased when combined with Pravastatin.
Eluxadoline The excretion of Eluxadoline can be decreased when combined with Pravastatin.
Silibinin The excretion of Silibinin can be decreased when combined with Pravastatin.
Relebactam The excretion of Relebactam can be decreased when combined with Pravastatin.
Liothyronine The excretion of Pravastatin can be decreased when combined with Liothyronine.
Cefalotin The excretion of Pravastatin can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Pravastatin can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Pravastatin can be decreased when combined with Cefotaxime.
Guanidine The excretion of Pravastatin can be decreased when combined with Guanidine.
Piroxicam The excretion of Pravastatin can be decreased when combined with Piroxicam.
Oxytetracycline The excretion of Oxytetracycline can be decreased when combined with Pravastatin.
Furosemide The excretion of Pravastatin can be decreased when combined with Furosemide.
Phenylbutazone The excretion of Pravastatin can be decreased when combined with Phenylbutazone.
Salicylic acid The excretion of Pravastatin can be decreased when combined with Salicylic acid.
Acetylsalicylic acid The excretion of Pravastatin can be decreased when combined with Acetylsalicylic acid.
Ketoprofen The excretion of Pravastatin can be decreased when combined with Ketoprofen.
Probenecid The excretion of Pravastatin can be decreased when combined with Probenecid.
Melatonin The excretion of Pravastatin can be decreased when combined with Melatonin.
Ouabain The excretion of Pravastatin can be decreased when combined with Ouabain.
Cefadroxil The excretion of Pravastatin can be decreased when combined with Cefadroxil.

Target Protein

3-hydroxy-3-methylglutaryl-coenzyme A reductase HMGCR
Histone deacetylase 2 HDAC2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28831316
    Salna MP, Singer HM, Dana AN: Pravastatin-Induced Eczematous Eruption Mimicking Psoriasis. Case Rep Dermatol Med. 2017;2017:3418204. doi: 10.1155/2017/3418204. Epub 2017 Jul 31.
  • PMID: 29067253
    Chastain DB, Stover KR, Riche DM: Evidence-based review of statin use in patients with HIV on antiretroviral therapy. J Clin Transl Endocrinol. 2017 Feb 22;8:6-14. doi: 10.1016/j.jcte.2017.01.004. eCollection 2017 Jun.
  • PMID: 28213601
    Fitzpatrick T, Perrier L, Tricco AC, Straus SE, Juni P, Zwarenstein M, Lix LM, Smith M, Rosella LC, Henry DA: Protocol for a scoping review of post-trial extensions of randomised controlled trials using individually linked administrative and registry data. BMJ Open. 2017 Feb 17;7(2):e013770. doi: 10.1136/bmjopen-2016-013770.
  • PMID: 11192473
    Hatanaka T: Clinical pharmacokinetics of pravastatin: mechanisms of pharmacokinetic events. Clin Pharmacokinet. 2000 Dec;39(6):397-412. doi: 10.2165/00003088-200039060-00002.
  • PMID: 25591572
    Ye YC, Zhao XL, Zhang SY: Use of atorvastatin in lipid disorders and cardiovascular disease in Chinese patients. Chin Med J (Engl). 2015 Jan 20;128(2):259-66. doi: 10.4103/0366-6999.149226.
  • PMID: 28613530
    McIver LA, Siddique MS: Atorvastatin .
  • PMID: 11298482
    Ray SK, Rege NN: Atorvastatin: in the management of hyperlipidaemia. J Postgrad Med. 2000 Jul-Sep;46(3):242-3.
  • PMID: 17516697
    Wiersma HE, Wiegman A, Koopmans RP, Bakker HD, Kastelein JJ, van Boxtel CJ: Steady-state pharmacokinetics of pravastatin in children with familial hypercholesterolaemia. Clin Drug Investig. 2004;24(2):113-20. doi: 10.2165/00044011-200424020-00006.
Menampilkan 8 dari 9 artikel.
Textbook
  • ISBN: 1-57340-221-4
    Frishman W., Cheng-Lai A. and Nawarskas J. (2005). Current cardiovascular drugs (4th ed.). Current medicine LLC.
  • ISBN: 9781935395621
    William H. Frishman, MD, Domenic A. Sica, MD (2011). Cardiovascular Pharmacotherapeutics. Cardiotext Publishing.
  • Taylor JB, Triggle DJ. (2007). Comprehensive Medicinal Chemistry II. Elsevier.
  • ISBN: 978-0-7817-6879-5
    Lemke T., Williams D., Roche V. and Zito W. (2008). Foye's Principles of Medicinal Chemistry (6th) (6th ed.). Lippincott Williams & Wilkins.

Contoh Produk & Brand

Produk: 557 • International brands: 5
Produk
  • Ach-pravastatin
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ach-pravastatin
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Ach-pravastatin
    Tablet • 40 mg • Oral • Canada • Generic • Approved
  • Act Pravastatin
    Tablet • 10 mg • Oral • Canada • Approved
  • Act Pravastatin
    Tablet • 20 mg • Oral • Canada • Approved
  • Act Pravastatin
    Tablet • 40 mg • Oral • Canada • Approved
  • Ag-pravastatin
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ag-pravastatin
    Tablet • 20 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 557 produk.
International Brands
  • Elisor — Baowei Technology Group
  • Lipostat — Bristol-Myers Squibb
  • Mevalotin — Daiichi Sankyo
  • Pravaselect
  • Selipran — Bristol-Myers Squibb

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