Drug reference

Pitavastatin

Statin · Hypolipidemic

StatinHypolipidemic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Avoid in pregnant women.

FDA category + note

Top interactionssee all 12 →

Azole AntifungalsSevereTextbookG&G 14e · p736
Hiv Protease InhibitorSevereTextbookKDT 7e · p637
Hiv Protease InhibitorsSevereTextbookG&G 14e · p736
KetoconazoleSevereTextbookKDT 7e · p637

Mechanism

Statins are cholesterol-lowering agents that reversibly inhibit HMG-CoA reductase, which catalyzes a rate-limiting step in cholesterol biosynthesis. This primarily results in the reduction of cholesterol biosynthesis in the liver, which is the main target organ for their pharmacological effect.

Indications

Reduction of LDLTreatment of hyperlipidemiaDecreased oxidative stressReduction of vascular inflammation with increased stability of atherosclerotic lesionsInitiation of high-dose statin therapy immediately after acute coronary syndromesInhibition of certain viruses (off-label)Mitigation of NAFLD (off-label)Mitigation of irritable bowel disease (off-label)Retardation of the replication of cancer cells in hepatocellular carcinoma (off-label)HypercholesterolemiaReduction of LDL-C levelsTreat dyslipidemias, especially elevated LDL-CPrimary hyperlipidaemias with raised LDL and total CH levels, with or without raised TG levels (Type IIa, IIb, V)Secondary hypercholesterolaemia (e.g., in diabetes, nephrotic syndrome)

Dosing

Adult: carcinoma. It has become standard practice to initiate highdose statin therapy immediately after acute coronary syndromes, regardless of lipid levels. child’s age. Children with homozygous FH or chylomicronemia syndrome must be treated at the time of diagnosis.…

Pharmacokinetics

Half-life

12 hours

Contraindications

Pregnancy
Lactation
Women likely to become pregnant
Children under 8 years of age
Combination with gemfibrozil

Side effects

Common

MyalgiaMuscle sorenessWeaknessGastrointestinal complaintsHeadacheRashes (uncommon)Sleep disturbances (uncommon)Muscle aches (10%)

Serious

Adverse effects due to exposure of extrahepatic cells in smooth muscle
Impairment of central nervous system myelination in children under 8 years of age
Myopathy
Rhabdomyolysis
Hepatotoxicity
Rise in serum transaminase
Liver damage (rare)
Myopathy (rare, < 1 per 1000)
Rhabdomyolysis (fatalities on record)

Pregnancy & lactation

Pregnancy

Avoid in pregnant women.

Lactation

Avoid in lactating women.

Drug interactions

Azole Antifungals

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Hiv Protease Inhibitor

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Hiv Protease Inhibitors

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy. For simvastatin, coadministration is contraindicated.

Source: G&G 14e · p736

Ketoconazole

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Macrolide Antibiotics

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Source: G&G 14e · p736

Nefazodone

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Nicotinic Acid

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

A lower dose of statin is advisable when nicotinic acid is given concurrently. Close monitoring for muscle symptoms is essential.

Source: KDT 7e · p637, p640

Clofibrate

Severe

Database

Clinical effect not specified

Source: DDInter

Colchicine

Severe

Database

Drug interaction classified as: synergy, metabolism

Source: DDInter

Cyclosporine

Severe

Database

Increased risk of myopathy and rhabdomyolysis.

Source: DDInter

Erythromycin

Severe

Database

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: DDInter

Fenofibrate

Severe

Database

Lower risk of statin myopathy compared to other fibrate-statin combinations.

Fenofibrate is the most suitable fibrate for combining with statins due to its minimal impact on statin metabolism and lower myopathy risk. However, continued vigilance for muscle symptoms is prudent.

Source: DDInter