LIPTRUZET Rx
Pharmacological Class:
Cholesterol absorption inhibitor + HMG-CoA reductase inhibitor.

Active Ingredient(s):
Ezetimibe/atorvastatin; 10mg/10mg, 10mg/20mg, 10mg/40mg, 10mg/80mg; tabs.

Company
Merck & Co., Inc.

Indication(s):

To reduce elevated total-C, LDL-C, Apo B, TG, and non-HDL-C, and to increase HDL-C in primary (heterozygous familial and non-familial) or mixed hyperlipidemia. To reduce elevated total-C and LDL-C in homozygous familial hypercholesterolemia (HoFH), as an adjunct to other lipid-lowering treatments (eg, LDL apheresis) or if such treatments are unavailable. Limitations of use: No incremental benefit on cardiovascular morbidity/mortality over and above that demonstrated for atorvastatin has been established. Not studied in Fredrickson type I, III, IV, and V dyslipidemias.

Pharmacology:

Ezetimibe reduces blood cholesterol by inhibiting cholesterol absorption by the small intestine. Atorvastatin lowers plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholesterol synthesis.

Clinical Trials:

In a clinical study, 628 patients were randomized to placebo, ezetimibe, atorvastatin, or coadminstered ezetimibe and atorvastatin equivalent to Liptruzet in a 12-week study.
 
Patients receiving all doses of the ezetimibe/atorvastatin combination were compared to those receiving all doses of atorvastatin. Results at 12 weeks demonstrated that the ezetimibe/atorvastatin combination treatment significantly reduced total-C (-41% vs. -32%), LDL-C (-56% vs. -44%), Apo B (-45% vs. -36%), TG (-33% vs. -24%), and non-HDL-C (-52% vs. -41%), and significantly increased HDL-C (7% vs. 4%) compared to all doses of atorvastatin pooled, respectively.

For more information on clinical studies: see full labeling.
 

Legal Classification:

Rx

Adults:

Swallow whole. Usual range: 10mg/10mg to 10mg/80mg. Initially 10mg/10mg or 10mg/20mg; for LDL-C reduction >55%: may start at 10mg/40mg; monitor lipids within ≥2wks and adjust dose as needed. HoFH: 10mg/40mg or 10mg/80mg. Concomitant bile acid sequestrants: give Liptruzet dose either ≥2hrs before or ≥4hrs after bile acid sequestrant administration. Concomitant lopinavir/ritonavir: use lowest dose. Concomitant clarithromycin, itraconazole, saquinavir/ritonavir, darunavir/ritonavir, fosamprenavir, or fosamprenavir/ritonavir: max 10mg/20mg. Concomitant nelfinavir or boceprevir: max 10mg/40mg.

Children:

Not established.

Contraindication(s):

Active liver disease. Unexplained persistent elevated hepatic transaminases. Pregnancy (Category X). Nursing mothers.

Warnings/Precautions:

Increased risk of myopathy/rhabdomyolysis (with high doses). Discontinue if elevated CPK (>10 X ULN) levels occur or myopathy is diagnosed or suspected; withhold if a predisposition in renal failure secondary to rhabdomyolysis develops. Monitor liver function prior to starting therapy and repeat as clinically indicated. History of liver disease or renal impairment; monitor closely. Substantial alcohol consumption. Elderly.

Interaction(s)

See Adult dose. Avoid with concomitant cyclosporine, tipranavir/ritonavir, telaprevir, gemfibrozil. Potentiated by strong CYP3A4 inhibitors, grapefruit juice (>1.2L/day). Caution with lopinavir/ritonavir, colchicine, fenofibrates, niacin ≥1g/day; consider dose reduction of Liptruzet. May increase serum levels of digoxin (monitor), oral contraceptives. May be antagonized by cholestyramine, CYP3A4 inducers (eg, efavirenz, rifampin); coadminister rifampin simultaneously. Monitor oral anticoagulants. Caution with drugs that decrease levels or activity of endogenous steroid hormones (eg, ketoconazole, spironolactone, cimetidine).

Adverse Reaction(s)

Increased ALT/AST, musculoskeletal pain, arthralgia, abdominal pain, nausea; increased in HbA1c or fasting serum glucose; myopathy, rhabdomyolysis; rare: immune-mediated necrotizing myopathy.

How Supplied:

Tabs—30, 90

LAST UPDATED:

6/7/2013
2013年5月7日讯 /生物谷BIOON/ --默沙东（Merck & Co）日前宣布，降胆固醇新药Liptruzet(ezetimibe/ atorvastatin,依替米贝/阿托伐他汀)已获FDA批准，作为一种辅助药物用于单靠饮食无法充分控制的原发性高脂血症（primary hyperlipidemia）或混合型高脂血症（mixed hyperlipidemia）患者低密度脂蛋白（LDL）胆固醇升高的治疗。
 
该药为默沙东降胆固醇药物Zetia（ezetimibe，依替米贝）和辉瑞降胆固醇药物Lipitor仿制药atorvastatin （阿托伐他汀）的复合药物。Zetia是一种有效的降LDL胆固醇药物，能够抑制消化道中胆固醇的吸收，atorvastatin则是目前在美国最广泛处方的一种他汀类药物，能够抑制肝脏中胆固醇的产生。
 
默沙东称，将于本周开始向批发商发货。
 
默沙东已经在销售一种重磅降胆固醇复合药物Vytorin，该药由Zetia和默沙东的降LDL老药Zocor（舒降之，simvastatin，辛伐他汀）组成。2012年，Vytorin的销售额达17.5亿美元，Zetia的销售额则达到了26.7亿美元。Lipitor(阿托伐他汀)被认为是比Zocor更为强大的一种他汀类药物。
 
目前，默沙东正在开展一项长期试验，来证明Vytorin比Zocor单药能更好地降低心脏病发作和中风。该项试验的结果无疑将会决定Zetia在患者中的价值。