Pitavastatin

Oral
Hyperlipidaemias, Mixed dyslipidaemia

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.

May be taken with or without food.

Active liver disease including unexplained, persistent elevations in serum aminotransferase (transaminase) concentrations. Pregnancy and lactation. Concomitant use w/ ciclosporin.

Patient w/ predisposing factors for myopathy; alcoholism. Renal impairment.

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.

PO: Z (Avoid)

Monitor lipid panel (total cholesterol, HDL, LDL, triglycerides), hepatic transaminase levels; creatine phosphokinase (CPK).

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.

Increased risk of liver damage w/ alcohol.

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.

Store between 15-30°C. Protect from light.

Dyslipidaemic Agents

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.