Livalo (Pitavastatin) Alnajah University Pharm_D Livalo (Pitavastatin) By: Rayah M. M. Yahya

Livalo (pitavastatin) Company: Kowa Company Approval Status: Approved August 2009 Treatment for: primary hyperlipidemia and mixed dyslipidemia Areas: Cardiology/Vascular Diseases

Mechanism of Action Livalo -Livalo is a HMG-CoA reductase inhibitor. -It differs from other statins in that it has a unique cyclopropyl group on the base structure. -This cyclopropyl group contributes to a more effective inhibition of the HMG-CoA reductase enzyme to inhibit cholesterol production, and potentially affords greater low-density lipoprotein cholesterol (LDL-C) clearance and reduction of plasma cholesterol Livalo

-The enzyme that catalyzes the conversion of HMG-CoA to mevanolate. Target: HMG-CoA Reductase (HMGR) -The enzyme that catalyzes the conversion of HMG-CoA to mevanolate. -This reaction is the rate-determining step in the synthetic pathway.

How Livalo Works : Livalo blocks an enzyme called 3-hydroxy-3methylglutaryl coenzyme A (HMG CoA) reductase, which is an important protein needed in the production of cholesterol

Dosing -Livalo is supplied as a tablet (1, 2 and 4 mg) for oral administration. -The recommended initial dose of the drug is 2 mg and the maximum dose is 4 mg. After initiation or upon titration of Livalo, lipid levels should be analyzed after 4 weeks and the dosage adjusted accordingly.

Livalo Side Effects -Back pain-Muscle pain -Diarrhea-Constipation -Pain in the legs or arms -Hives or welts-itching skin -Rash-redness of the skin -headache-loss of appetite

Pharmacokinetic profile of LIVALO shows potential advantage over other statins *Many statins, such as atorvastatin and simvastatin, are metabolized by the cytochrome P450 system, particularly through the 3A4 pathway. *strong inhibitors of this pathway, such as itraconazole and grapefruit juice, can influence drug exposure levels that may result in other clinical complications, such as hospitalizations due to severe muscle problems. *LIVALO is a clinically effective and well-tolerated statin that has less potential for these types of interactions."

The open-label study was conducted to determine the potential pharmacokinetic interaction of itraconazole (200 mg), an antifungal agent that strongly inhibits CYP3A4, on the pharmacokinetics of LIVALO (4 mg) Additionally, LIVALO was shown to be well tolerated both as monotherapy and when combined with itraconazole and was not associated with any moderate or severe adverse events or clinically relevant changes in laboratory, vital or physical signs or ECG. compared with other commonly prescribed statins, LIVALO's metabolic route may offer a favorable tolerability profile when administered with drugs that inhibit CYP3A4,"

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