Statin (HMG-CoA reductase inhibitor)
Brand names: Livazo, Livalo
Updated · Methodology
Second line
Second-line for hypercholesterolemia per 2019. Advantage over atorvastatin in patients on polytherapy with CYP3A4-metabolized drugs (cyclosporine post-transplant, antiretrovirals, azole antifungals) – fewer interactions. Dose 2–4 mg once daily. In pre-diabetes or T2D, preferred over atorvastatin due to less glycemic impact.
Sources
ICD-10: E78.0 · ICD-11: 5C80.00
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Pitavastatin is a new-generation statin with minimal CYP3A4 interaction. It is prescribed for hyperlipidemia and for primary/secondary CV prevention in high-risk patients ( 2019). In anti-aging and longevity communities, pitavastatin is promoted as a means for life extension and vessel protection in healthy adults. In people with normal lipid profile and low CV risk, no clinical studies of prophylactic use exist, and meta-analyses do not confirm benefit. The drug causes myalgia, elevated liver enzymes, risk of rhabdomyolysis (rare but dangerous), elevated glucose, and new-onset diabetes risk. If pitavastatin was prescribed at a normal lipid profile, consider seeking a second opinion.
A competitive HMG-CoA reductase inhibitor. Mainly UGT-glucuronidation metabolism, minor CYP2C9 – no significant CYP3A4 interactions (differs from atorvastatin and simvastatin). reduction 35–45% at 2–4 mg – moderate-to-high intensity at low doses. Lower glycemia rise than rosuvastatin and atorvastatin (J-PREDICT data).
Contraindicated. Stop 1–3 months before planned conception.
Contraindicated during lactation.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
1 pair found. Sorted from critical to minor.
Mechanism
Cyclosporine inhibits OATP1B1 – pitavastatin rises 5-7 fold. Livalo contraindication.
Symptoms
Myalgia, weakness, dark urine, rising CK within 5-10 days.
Management
Combination contraindicated.
Sources
Verbatim lines from the interaction sections, in the language of the label
«en pacientes con tratamiento concomitante con ciclosporina»AEMPS, section 4.3 · Open on CIMA
«Otros efectos: Se recomienda suspender temporalmente el tratamiento con pitavastatina durante el tratamiento con eritromicina, otros antibióticos macrólidos o ácido fusídico (ver sección 4.5)…»AEMPS, section 4.4 · Open on CIMA
«DRUG INTERACTIONS: Intervention: In patients taking erythromycin, do not exceed pitavastatin tablets 1 mg once daily [see Dosage and Administration (2.4) ] .»FDA, section 7 · Open on DailyMed
«DRUG INTERACTIONS: Intervention: Avoid concomitant use of gemfibrozil with pitavastatin tablets.»FDA, section 7 · Open on DailyMed
«Otros efectos: Se recomienda suspender temporalmente el tratamiento con pitavastatina durante el tratamiento con eritromicina, otros antibióticos macrólidos o ácido fusídico (ver sección 4.5)…»AEMPS, section 4.4 · Open on CIMA
«DRUG INTERACTIONS: Intervention: Consider the risk/FDA, section 7 · Open on DailyMed
«DRUG INTERACTIONS: Intervention: Consider if the benefit of using fibrates concomitantly with pitavastatin tablets outweighs the increased risk of myopathy and rhabdomyolysis.»FDA, section 7 · Open on DailyMed
«Gemfibrozilo y otros fibratos: El uso de fibratos solos se asocia ocasionalmente a miopatía. La coadministración de fibratos con estatinas se ha asociado a un aumento de miopatía y rabdomiólisis…»AEMPS, section 4.5 · Open on CIMA
«Gemfibrozilo y otros fibratos: El uso de fibratos solos se asocia ocasionalmente a miopatía. La coadministración de fibratos con estatinas se ha asociado a un aumento de miopatía y rabdomiólisis…»AEMPS, section 4.5 · Open on CIMA
«Inhibidores de la proteasa e inhibidores no nucleosídicos de la transcriptasa inversa : La coadministración de lopinavir/AEMPS, section 4.5 · Open on CIMA
«Inhibidores de la proteasa e inhibidores no nucleosídicos de la transcriptasa inversa : La coadministración de lopinavir/AEMPS, section 4.5 · Open on CIMA
«La digoxina , un sustrato conocido de glicoproteína-P, no mostró ninguna interacción con pitavastatina. Durante la coadministración, no hubo ningún cambio significativo en las concentraciones de…»AEMPS, section 4.5 · Open on CIMA
«Inhibidores de la proteasa e inhibidores no nucleosídicos de la transcriptasa inversa : La coadministración de lopinavir/AEMPS, section 4.5 · Open on CIMA
«La ezetimiba y su metabolito glucurónido inhiben la absorción del colesterol alimentario y biliar. La coadministración de pitavastatina no tuvo ningún efecto en las concentraciones plasmáticas de…»AEMPS, section 4.5 · Open on CIMA
«Inhibidores de CYP3A4: Los estudios de interacción con itraconazol y zumo de pomelo, inhibidores conocidos de CYP3A4, no mostraron ningún efecto clínicamente significativo en las concentraciones…»AEMPS, section 4.5 · Open on CIMA
«Inhibidores de CYP3A4: Los estudios de interacción con itraconazol y zumo de pomelo, inhibidores conocidos de CYP3A4, no mostraron ningún efecto clínicamente significativo en las concentraciones…»AEMPS, section 4.5 · Open on CIMA
«Rifampicina: La coadministración con pitavastatina al mismo tiempo produjo un aumento de 1,3 veces en el AUC de la pitavastatina debido a la reducción de la captación hepática.»AEMPS, section 4.5 · Open on CIMA
«Inhibidores de la proteasa e inhibidores no nucleosídicos de la transcriptasa inversa : La coadministración de lopinavir/AEMPS, section 4.5 · Open on CIMA
«Transporters: Use caution when concomitantly administering eltrombopag and drugs that are substrates of OATP1B1 (e.g., atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan…»FDA, section 7 · Open on DailyMed
«Número de veces que cambia la exposición con ciclosporina: Pitavastatina»AEMPS, section 4.5 · Open on CIMA
«Drugs without Clinically Significant Interactions with Darunavir: No dosage adjustments are recommended when darunavir/FDA, section 7 · Open on DailyMed
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Pitavastatin is evaluated for the following indications with varying evidence strength: Primary hypercholesterolemia (evidence tier A), Anti-aging and longevity (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Pitavastatin (≥ 1 in 100): Myalgia, Headache, Back pain, Constipation, Elevated ALT. See the Safety section for uncommon and serious reactions.
Contraindicated. Stop 1–3 months before planned conception.
Contraindicated during lactation.
Pitavastatin is contraindicated in: Hypersensitivity to pitavastatin or other statins; Active hepatic disease or transaminase elevation over 3× upper limit; Pregnancy and lactation; Concomitant cyclosporine; Age under 18. Full list in the Safety section.
Direct links to regulator labels. Open in a new tab.
Pravastatin, Rosuvastatin, Rosuvastatin + Ezetimibe, Simvastatin, Atorvastatin, Ezetimibe, Krill oil, Simvastatin + Ezetimibe