What is Zypitamag and how does it work?
Zypitamag (pitavastatin) tablets are an HMG-CoA reductase inhibitor indicated for patients with primary hyperlipidemia or mixed dyslipidemia as an adjunctive therapy to diet to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C).
Zypitamag (pitavastatin) is an inhibitor of HMG-CoA reductase. It is a synthetic lipid-lowering agent for oral administration.
Limitations Of Use
The effect of Zypitamag on cardiovascular morbidity and mortality has not been determined.
What are the side effects of Zypitamag?
Common side effects of Zypitamag include:
- muscle pain,
- back pain,
- pain in extremities,
- joint pain,
- influenza, and
- runny or stuffy nose.
The following serious adverse reactions are discussed in other sections of the labeling:
- Myopathy and Rhabdomyolysis
- Immune-Mediated Necrotizing Myopathy
- Hepatic Dysfunction
- Increases in HbA1c and Fasting Serum Glucose Levels
Clinical Studies Experience
Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of one drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice.
Adverse Reactions In Adults With Primary Hyperlipidemia And Mixed Dyslipidemia
In 10 controlled clinical studies and 4 subsequent open-label extension studies, 3,291 adult patients with primary hyperlipidemia or mixed dyslipidemia were administered pitavastatin 1 mg to 4 mg daily. The mean continuous exposure of pitavastatin (1 mg to 4 mg) was 36.7 weeks (median 51.1 weeks).
The mean age of the patients was 60.9 years (range; 18 years - 89 years) and the gender distribution was 48% males and 52% females. Approximately 93% of the patients were Caucasian, 7% were Asian/Indian, 0.2% were African American and 0.3% were Hispanic and other.
In controlled clinical studies and their open-label extensions, 3.9% (1 mg), 3.3% (2 mg), and 3.7% (4 mg) of pitavastatin-treated patients were discontinued due to adverse reactions.
The most common adverse reactions that led to treatment discontinuation were:
- elevated creatine phosphokinase (0.6% on 4 mg) and
- myalgia (0.5% on 4 mg).
Adverse reactions reported in ≥ 2% of patients in controlled clinical studies and at a rate greater than or equal to placebo are shown in Table 1. These studies had treatment duration of up to 12 weeks.
Table 1: Adverse Reactions (≥ 2% and ≥ placebo) in Adult Patients with Primary Hyperlipidemia and Mixed Dyslipidemia in Studies up to 12 Weeks
|Pitavastatin 1 mg|
|Pitavastatin 2 mg|
|Pitavastatin 4 mg|
|Pain in Extremity||1.9||2.3||0.6||0.9|
Other adverse reactions reported from clinical studies were
Hypersensitivity reactions including
The following laboratory abnormalities have been reported:
Adverse Reactions In Adult HIV-Infected Patients With Dyslipidemia
- In a double-blind, randomized, controlled, 52-week trial, 252 HIV-infected patients with dyslipidemia were treated with either pitavastatin 4 mg once daily (n=126) or another statin (n=126).
- All patients were taking antiretroviral therapy (excluding darunavir) and had HIV-1 RNA less than 200 copies/mL and CD4 count greater than 200 cell/μL for at least 3 months prior to randomization.
- The safety profile of pitavastatin was generally consistent with that observed in the clinical trials described above. One patient (0.8%) treated with pitavastatin had a peak creatine phosphokinase value exceeding 10 times the upper limit of normal (ULN), which resolved spontaneously.
- Four patients (3%) treated with pitavastatin had at least one ALT value exceeding 3 times but less than 5 times the ULN, none of which led to drug discontinuation.
- Virologic failure was reported for four patients (3%) treated with pitavastatin, defined as a confirmed measurement of HIV-1 RNA exceeding 200 copies/mL that was also more than a 2-fold increase from baseline.
Pediatric use information is approved for Kowa Co Ltd's LIVALO (pitavastatin) tablets. However, due to Kowa Co Ltd's marketing exclusivity rights, this drug product is not labeled with that information.
What is the dosage for Zypitamag?
General Dosage And Administration Information
Take Zypitamag orally once daily with or without food at the same time each day. Individualize the dose of Zypitamag according to patient characteristics, goal of therapy, and response. After initiation or upon titration of Zypitamag, analyze lipid levels after 4 weeks and adjust the dosage accordingly.
Recommended Dosage For Adults
The recommended starting Zypitamag dosage is 2 mg once daily.
The maximum recommended dosage is Zypitamag 4 mg once daily.
Recommended Dosage In Patients With Renal Impairment
- The recommended starting dose for patients with moderate and severe renal impairment (estimated glomerular filtration rate 30 mL/min/1.73 m2 to 59 mL/min/1.73 m 2 and 15 mL/min/1.73 m2 to 29 mL/min/1.73 m2 not receiving hemodialysis, respectively) and patients with end-stage renal disease receiving hemodialysis is pitavastatin 1 mg once daily. Zypitamag is not available in a 1 mg dose; use an alternative formulation of pitavastatin for the 1 mg dose.
- The maximum recommended dose for these patients is Zypitamag 2 mg once daily.
Zypitamag Dosage Adjustments Due To Drug Interactions
- In patients taking erythromycin, do not exceed pitavastatin 1 mg once daily. Zypitamag is not available in a 1 mg dose; use an alternative formulation of pitavastatin for the 1 mg dose.
- In patients taking rifampin, do not exceed Zypitamag 2 mg once daily.
What drugs interact with Zypitamag?
Drug Interactions That Increase The Risk Of Myopathy And Rhabdomyolysis With Zypitamag
Table 2: Drug Interactions that Increase the Risk of Myopathy and Rhabdomyolysis with Zypitamag
|Clinical Impact:||Cyclosporine significantly increases pitavastatin exposure and increases the risk of myopathy and rhabdomyolysis.|
|Intervention:||Concomitant use of cyclosporine with Zypitamag is contraindicated.|
|Clinical Impact:||Gemfibrozil may cause myopathy when given alone. The risk of myopathy and rhabdomyolysis is increased with concomitant use of gemfibrozil with statins, including pitavastatin.|
|Intervention:||Avoid concomitant use of gemfibrozil with Zypitamag.|
|Clinical Impact:||Erythromycin significantly increases pitavastatin exposure and increases the risk of myopathy and rhabdomyolysis.|
|Intervention:||In patients taking erythromycin, do not exceed pitavastatin 1 mg once daily. Zypitamag is not available in a 1 mg dose; use an alternative formulation of pitavastatin for the 1 mg dose.|
|Clinical Impact:||Rifampin significantly increases peak pitavastatin exposure and increases the risk of myopathy and rhabdomyolysis.|
|Intervention:||In patients taking rifampin, do not exceed Zypitamag 2 mg once daily.|
|Clinical Impact:||Fibrates may cause myopathy when given alone. The risk of myopathy and rhabdomyolysis is increased with concomitant use of fibrates with statins, including pitavastatin.|
|Intervention:||Consider if the benefit of using fibrates concomitantly with Zypitamag outweighs the increased risk of myopathy and rhabdomyolysis.|
|Clinical Impact:||The risk of myopathy and rhabdomyolysis may be increased with concomitant use of lipid-modifying doses (≥1 g/day) of niacin with pitavastatin.|
|Intervention:||Consider if the benefit of using lipid-modifying doses (>1 g/day) of niacin concomitantly with Zypitamag outweighs the increased risk of myopathy and rhabdomyolysis.|
|Clinical Impact:||Cases of myopathy and rhabdomyolysis have been reported with concomitant use of colchicine with statins, including pitavastatin.|
|Intervention:||Consider the risk/benefit of concomitant use of colchicine with Zypitamag.|
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Is Zypitamag safe to take when pregnant or breastfeeding?
- Zypitamag is contraindicated for use in pregnant women since safety in pregnant women has not been established and there is no apparent benefit to therapy with pitavastatin during pregnancy.
- Because HMG-CoA reductase inhibitors decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, Zypitamag may cause fetal harm when administered to pregnant women.
- Zypitamag should be discontinued as soon as pregnancy is recognized. Zypitamag is contraindicated during breastfeeding.
- There is no available information on the effects of the drug on the breastfed infant or the effects of the drug on milk production. However, it has been shown that another drug in this class passes into human milk.
- Because of the potential for serious adverse reactions in a breastfed infant, advise patients that breastfeeding is not recommended during treatment with Zypitamag.
Zypitamag (pitavastatin) tablets are an HMG-CoA reductase inhibitor indicated for patients with primary hyperlipidemia or mixed dyslipidemia as an adjunctive therapy to diet to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C). It is a synthetic lipid-lowering agent for oral administration.
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