Pitavastatin


Generic Medicine Info
Indications and Dosage
Oral
Hyperlipidaemias, Mixed dyslipidaemia
Adult: 1-4 mg once daily. If given w/ erythromycin or rifampicin, max dose of 1 mg or 2 mg respectively.
Renal Impairment
Moderate to severe (CrCl 15-60 mL/min, not on haemodialysis) and ESRD (on haemodialysis): Initial: 1 mg once daily. Max: 2 mg once daily.
Administration
May be taken with or without food.
Contraindications
Active liver disease including unexplained, persistent elevations in serum aminotransferase (transaminase) concentrations. Pregnancy and lactation. Concomitant use w/ ciclosporin.
Special Precautions
Patient w/ predisposing factors for myopathy; alcoholism. Renal impairment.
Adverse Reactions
Liver enzyme abnormalities, myalgia, muscle spasm, back pain, diarrhoea, constipation, pain in extremities, arthralgia, headache, dizziness, influenza, nasopharyngitis, abdominal discomfort, abdominal pain, dyspepsia, nausea, asthenia, malaise, fatigue, hepatitis, jaundice, hypoaesthesia, insomnia, depression, interstitial lung disease, erectile dysfunction, cognitive impairment (e.g. memory loss and impairment, confusion, forgetfulness, amnesia).
Potentially Fatal: Myopathy and rhabdomyolysis w/ acute renal failure secondary to myoglobinuria; hepatic failure.
MonitoringParameters
Monitor lipid panel (total cholesterol, HDL, LDL, triglycerides), hepatic transaminase levels; creatine phosphokinase (CPK).
Drug Interactions
Increased bioavailability w/ erythromycin and rifampicin. Increased risk of myopathy/rhabdomyolysis w/ gemfibrozil, colchicine, niacin and other fibrates.
Potentially Fatal: Ciclosporin significantly increases pitavastatin exposure.
Food Interaction
Increased risk of liver damage w/ alcohol.
Action
Description: Pitavastatin, an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis (reduces the production of mevalonic acid from HMG-CoA), resulting in a compensatory increase in the expression of LDL receptors on hepatocyte membranes and a stimulation of LDL catabolism.
Pharmacokinetics:
Absorption: Bioavailability: Approx 51%. Time to peak plasma concentration: Approx 1 hr.
Distribution: Plasma protein binding: >99%.
Metabolism: Hepatic, mainly via glucuronidation to a lactone metabolite; marginally metabolised by CYP2C9 and to a lesser extent by CYP2C8 isoenzyme.
Excretion: Mainly via faeces; urine (approx 15%). Elimination half-life: 12 hr.
Storage
Store between 15-30°C. Protect from light.
References
Anon. Pitavastatin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/08/2014.

Buckingham R (ed). Pitavastatin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/08/2014.

Livalo Tablet, Film Coated (Eli Lilly and Company). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/08/2014.

Livalo Tablets. U.S. FDA. https://www.fda.gov/. Accessed 06/08/2014.

McEvoy GK, Snow EK, Miller J et al (eds). Pitavastatin Calcium. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 06/08/2014.

Disclaimer: This information is independently developed by MIMS based on Pitavastatin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com
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