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Pitavastatin Brand Names
Livalo | NIKITA | Zypitamag
What is Pitavastatin
Pitavastatin is a member of the HMG-CoA reductase inhibitor (‘statin’) class of lipid-lowering drugs with moderately potent LDL-lowering effects.
In patients with primary hypercholesterolemia, doses of 1 mg, 2 mg, and 4 mg PO daily reduce LDL-cholesterol by 32%, 36%, and 43%, respectively; doses of 1 to 4 mg/day lower triglycerides by 15% to 19%.
Similar to other statins, pitavastatin produces modest increases in HDL (5% to 8%).
Clinical trials have been conducted to compare pitavastatin with atorvastatin and simvastatin in patients with hypercholesterolemia, dyslipidemia, type 2 diabetes, and acute coronary syndrome (ACS).
When compared to atorvastatin and simvastatin, pitavastatin was shown to be not inferior to either agent for reduction of LDL-C in patients with primary hyperlipidemia or mixed dyslipidemia, but when compared to equivalent doses of pravastatin, pitavastatin therapy resulted in a significantly greater reduction in LDL-C in patients with primary hyperlipidemia or mixed dyslipidemia.
In a 12 week comparative trial with atorvastatin, pitavastatin did not reach the noninferiority objective for the treatment of patients with type 2 diabetes and combined dyslipidemia.
Treatment with pitavastatin 4 mg/day has been shown to be as effective as atorvastatin 20 mg/day in patients with ACS for the regression of atherosclerosis.
The catabolism of pitavastatin is not significantly mediated by the cytochrome P450 system or P-glycoprotein, thus reducing the potential for drug-drug interactions involving these enzyme systems; however, the uptake of pitavastatin into hepatocytes is primarily facilitated by organic anion transporting polypeptide (OATP)1B1, creating the potential for drug interactions with inhibitors of OATP1B1 (e.g., cyclosporine, gemfibrozil).
Pitavastatin has high oral bioavailability in contrast to most commercially available statins which have low bioavailability due to extensive first-pass metabolism (e.g., simvastatin, lovastatin).
The extensive first pass metabolism of other statins is hypothesized to be an advantage since drug delivery is targeted to the liver, the site of action for HMG-CoA reductase inhibitors.
The clinical relevance of low or high bioavailability for statin drugs is unknown.
Indications
- atherosclerosis
- hypercholesterolemia
- hyperlipoproteinemia
- hypertriglyceridemia
For the treatment of hypercholesterolemia, hyperlipoproteinemia, and/or hypertriglyceridemia as an adjunct to dietary control
Side Effects
- abdominal pain
- amnesia
- angioedema
- arthralgia
- asthenia
- back pain
- cholestasis
- cirrhosis
- Co-Enzyme Q-10 deficiency
- confusion
- constipation
- depression
- diabetes mellitus
- diarrhea
- dizziness
- dyspepsia
- elevated hepatic enzymes
- fatigue
- headache
- hepatic failure
- hepatic necrosis
- hepatitis
- hyperglycemia
- hypoesthesia
- immune-mediated necrotizing myopathy
- impotence (erectile dysfunction)
- influenza
- insomnia
- interstitial lung disease
- jaundice
- malaise
- memory impairment
- muscle cramps
- myalgia
- myopathy
- nausea
- pancreatitis
- peripheral neuropathy
- pharyngitis
- pruritus
- rash
- renal failure (unspecified)
- rhabdomyolysis
- urticaria
Hypersensitivity reactions including angioedema, rash, pruritus, and urticaria have been reported with pitavastatin.
Monitoring Parameters
- creatine phosphokinase (CPK)
- LFTs
- serum cholesterol profile
- serum creatinine
Contraindications
- alcoholism
- breast-feeding
- children
- cholestasis
- contraception requirements
- diabetes mellitus
- dialysis
- electrolyte imbalance
- endocrine disease
- geriatric
- hepatic disease
- hepatic encephalopathy
- hepatitis
- hypotension
- hypothyroidism
- hypovolemia
- infants
- infection
- jaundice
- myopathy
- pregnancy
- renal disease
- renal failure
- renal impairment
- rhabdomyolysis
- seizure disorder
- sepsis
- shock
- surgery
- trauma
Interactions
- Abiraterone
- Aprepitant, Fosaprepitant
- Atazanavir; Cobicistat
- Bortezomib
- Cimetidine
- Clofarabine
- Cobicistat
- Colchicine
- Colchicine; Probenecid
- Cyclosporine
- Daclatasvir
- Daptomycin
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Elexacaftor; tezacaftor; ivacaftor
- Eltrombopag
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
- Erythromycin
- Erythromycin; Sulfisoxazole
- Everolimus
- Fenofibrate
- Fenofibric Acid
- Fostemsavir
- Gemfibrozil
- Glecaprevir; Pibrentasvir
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Lanthanum Carbonate
- Leflunomide
- Letermovir
- Lovastatin; Niacin
- Niacin, Niacinamide
- Niacin; Simvastatin
- Ombitasvir; Paritaprevir; Ritonavir
- Oritavancin
- Raltegravir
- Red Yeast Rice
- Rifampin
- Simeprevir
- Sirolimus
- Sofosbuvir; Velpatasvir; Voxilaprevir
- Tacrolimus
- Telaprevir
- Telbivudine
- Telithromycin
- Teriflunomide
- Tolvaptan
- Warfarin
