Adult: As pitavastatin calcium: As an adjunct to diet: Initially, 1 mg once daily, adjust dose at intervals of at least 4 weeks according to response. Max: 4 mg daily. Dose is individualised according to LDL-C levels, the goal of therapy, and patient response. Dosage and treatment recommendations may vary between countries (refer to specific local guidelines).
Oral Heterozygous familial hypercholesterolaemia
Child: As pitavastatin calcium: As an adjunct to diet: 6-9 years Initially, 1 mg daily, adjust dose at intervals of at least 4 weeks according to response. Max: 2 mg daily; ≥10 years Initially, 1 mg daily, adjust dose at intervals of at least 4 weeks according to response. Max: 4 mg daily. Dose is individualised according to LDL-C levels, the goal of therapy, and patient response. Dosage and treatment recommendations may vary between countries (refer to specific local guidelines).
What are the brands available for Pitavastatin in Thailand?
The SLCO1B1 gene encodes OATP1B1, an influx transporter that facilitates the hepatic uptake of statins and other exogenous and endogenous compounds into hepatocytes for subsequent clearance. Certain SLCO1B1 gene polymorphisms can produce a less active form of OATP1B1 enzyme. Individuals with genetic variation of SLCO1B1 may have an altered systemic exposure to statins which may lead to increased risk for statin-associated musculoskeletal symptoms (SAMS). Genetic testing may be considered to reduce the incidence of SAMS, identify those at significant risk, and recommend a lower dose or use of an alternative agent with lower risk of SAMS.
Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline as of January 2022:
Phenotype and Genotype
Implications
Recommendations
SLCO1B1 decreased function
Individuals carrying 1 normal or increased functional allele and 1 non-functional allele (e.g. *1/*5, *1/*15)
Increased pitavastatin exposure as compared with normal function resulting to increased risk of myopathy.
Initiate treatment at a dose of ≤2 mg and adjust doses according to disease-specific guidelines. If >2 mg dose is needed for desired efficacy, may consider an alternative statin or combination therapy with non-statin guideline-directed therapy.
Increased pitavastatin exposure as compared with normal function resulting to increased risk of myopathy.
Initiate treatment at a dose of ≤2 mg and adjust doses according to disease-specific guidelines. If >2 mg dose is needed for desired efficacy, may consider an alternative statin or combination therapy with non-statin guideline-directed therapy.
Increased pitavastatin exposure as compared with normal and decreased function resulting to increased risk of myopathy.
Initiate treatment at a dose of ≤1 mg and adjust doses according to disease-specific guidelines. If >1 mg dose is needed for desired efficacy, may consider an alternative statin or combination therapy with non-statin guideline-directed therapy.
Renal Impairment
Moderate to severe (GFR 15-59 mL/min/1.73 m2), ESRD on haemodialysis: Initially, 1 mg once daily. Max: 2 mg once daily.
Administration
Pitavastatin May be taken with or without food.
Contraindications
Active liver disease, unexplained persistent elevations of serum transaminases (>3 times the ULN), decompensated cirrhosis. Concomitant use with ciclosporin, systemic fusidic acid or within 7 days of stopping fusidic acid treatment. Pregnancy and lactation.
Special Precautions
Patient with predisposing factors for myopathy or rhabdomyolysis (e.g. uncontrolled hypothyroidism, personal or family history of hereditary muscular disorders, history of muscular toxicity with fibrates or another statin), history of liver disease, diabetes mellitus, myasthenia gravis. Patient who consumes large quantities of alcoholic beverages. Not recommended for coadministration with gemfibrozil. Patient undergoing major surgery. Patient with known SLCO1B1 gene polymorphism. Renal and hepatic impairment. Children and elderly.
Adverse Reactions
Significant: Myalgia; increased HbA1c, fasting blood glucose, serum transaminases, creatine phosphokinase (CPK); hypersensitivity reactions (e.g. angioedema, rash, pruritus, urticaria). Rarely, immune-mediated necrotising myopathy, worsen or precipitate myasthenia gravis, interstitial lung disease. Gastrointestinal disorders: Constipation, diarrhoea, dyspepsia, nausea, dysgeusia. General disorders and administration site conditions: Asthenia, fatigue, malaise, peripheral oedema. Infections and infestations: Influenza. Musculoskeletal and connective tissue disorders: Arthralgia, muscle spasms, back pain, pain in extremity. Nervous system disorders: Headache, dizziness. Psychiatric disorders: Insomnia, somnolence. Respiratory, thoracic and mediastinal disorders: Nasopharyngitis. Potentially Fatal: Rhabdomyolysis (with or without acute renal failure secondary to myoglobinuria). Rarely, hepatic failure.
This drug may cause dizziness and somnolence, if affected, do not drive or operate machinery. Women of childbearing potential must use appropriate contraception during treatment.
Monitoring Parameters
Obtain lipid profile (fasting or non-fasting) before treatment initiation. Monitor fasting lipid profile during treatment (4-12 weeks after treatment initiation and 3-12 months thereafter); LFTs at baseline and periodically; CPK at baseline (particularly in individuals at risk for myopathy). Assess for signs and symptoms of rhabdomyolysis or myopathy, hepatotoxicity, new-onset diabetes mellitus.
Drug Interactions
Increased risk of myopathy and rhabdomyolysis with erythromycin, rifampicin, colchicine, niacin, gemfibrozil and other fibrates. Increased plasma concentration with glecaprevir/pibrentasvir, lopinavir/ritonavir, darunavir/ritonavir, atazanavir, or efavirenz. Potentially Fatal: Increased risk of rhabdomyolysis with fusidic acid. Ciclosporin significantly increases pitavastatin exposure.
Food Interaction
Increased risk of liver damage with alcohol. Increased risk of adverse effects with red yeast rice.
Action
Description: Mechanism of Action: Pitavastatin is a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate limiting enzyme in cholesterol synthesis, resulting in a compensatory increase in the expression of LDL receptors on hepatocyte membranes and subsequently increase the hepatic clearance of LDL cholesterol (LDL-C). Pharmacokinetics: Absorption: Bioavailability: Approx 51%. Time to peak plasma concentration: Approx 1 hour. Distribution: Volume of distribution: Approx 148 L. Plasma protein binding: >99% (mainly to albumin and α1-acid glycoprotein). Metabolism: Metabolised in the liver by uridine 5'-diphosphate glucuronosyltransferase (e.g. UGT1A3, UGT2B7) via glucuronidation into an inactive lactone metabolite. Undergoes minimal metabolism by CPY2C9 and CYP2C8 isoenzymes. Excretion: Mainly via faeces (79%); urine (15%). Elimination half-life: Approx 12 hours.
Chemical Structure
Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5282452, Pitavastatin. https://pubchem.ncbi.nlm.nih.gov/compound/Pitavastatin. Accessed July 26, 2024.
C10AA08 - pitavastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
References
Cooper-DeHoff R, Niemi M, Ramsey L et al. The Clinical Pharmacogenetics Implementation Consortium Guideline for SLCO1B1, ABCG2, and CYP2C9 Genotypes and Statin-Associated Musculoskeletal Symptoms. Clinical Pharmacology and Therapeutics. 2022 May;111(5):1007-1021. doi: 10.1002/cpt.2557. Accessed 08/07/2024Annotation of CPIC Guideline for Pitavastatin and SLCO1B1. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org. Accessed 08/07/2024.Anon. Pitavastatin. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/07/2024.Brayfield A, Cadart C (eds). Pitavastatin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/07/2024.Livalo Film-coated Tablets 2 mg, 4 mg (DKSH Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 04/07/2024.Livalo Tablet, Film Coated (Kowa Pharmaceuticals America, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/07/2024.Livazo 1 mg Film-coated Tablets (Kowa Pharmaceutical Europe Co. Ltd). MHRA. https://products.mhra.gov.uk. Accessed 04/07/2024.Pitavastatin. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 04/07/2024.SLCO1B1 - Pitavastatin. UpToDate Lexidrug, Pharmacogenomics Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 08/07/2024.The Clinical Pharmacogenetics Implementation Consortium Guideline for Statins and SLCO1B1, ABCG2, and CYP2C9. Clinical Pharmacogenetics Implementation Consortium (CPIC). https://cpicpgx.org. Accessed 08/07/2024.
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