Medostatin

Lovastatin is butanoic acid 2-methyl-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1-naphthalenyl ester [1S-[1a (R*), 3a, 7β, 8β, (25*, 45*) 8aβ]].

Lovastatin is a cholesterol-lowering agent being a potent inhibitor of endogenous cholesterol synthesis.

Treatment of primary hypercholesterolemia (type IIa and IIb hyperlipoproteinemia) caused by elevated LDL cholesterol concentration in patients unresponsive to diet or non-drug measures. Reduction of elevated LDL in patients with combined hypercholesterolemia and hypertriglyceridemia.

Prior to treatment with lovastatin, the patient should be given a standard cholesterol-lowering diet and this should be continued during treatment with lovastatin.
Adult: Initially 20 mg once daily. Dosage can be adjusted if required but at intervals of not less than 4 weeks reaching a maximum of 80 mg daily given in single or divided doses with the morning and evening meals.
Patients Taking Immunosuppressive Drugs Concomitantly with Lovastatin: Maximum Recommended Dosage:  ≤20 mg daily.
If LDL-cholesterol levels fall <75 mg/100 mL or total plasma cholesterol levels fall <140 mg/100 mL, the dosage of lovastatin should be reduced.
Lovastatin is effective alone or in combination with bile-acid sequestrants.
Renal Insufficiency: Modification of dosage is not necessary in patients with moderate renal insufficiency but in patients with severe renal insufficiency (creatinine clearance <30 mL/min), dosages >20 mg/day should be carefully considered and if necessary, they should be implemented cautiously.

Hypersensitivity to lovastatin or to any other component of Medostatin.
Active liver disease or unexplained persistent elevations of serum transaminases.
Use in pregnancy: Medostatin is contraindicated during pregnancy.
Medostatin should be administered to women of childbearing age only when conceiving is highly unlikely for such patients. In case such a patient becomes pregnant while taking Medostatin, the therapy should be discontinued and the patient apprised of the potential hazard to the fetus.
Use in lactation: As with other drugs, Medostatin is excreted in the human milk and for this reason, women taking Medostatin should not breastfeed their infants.

Hepatic Effects: Before treatment with lovastatin begins, it is recommended that transaminase tests are performed and the tests be repeated periodically during treatment particularly in patients who have abnormal liver function tests and/or consume substantial quantities of alcohol. If serum transaminase levels increase no more than 3 times the upper limit of normal, the potential risk of continuing lovastatin therapy should be carefully studied against the anticipated benefits. Transaminase measurements should be repeated promptly and if these elevations are persistent or progressive, therapy with lovastatin should be discontinued.
Moderate elevation of serum transaminases have been reported soon after initiation of therapy with lovastatin but these were transient and not accompanied by any symptoms. In such cases, discontinuation of therapy is not required.
Lovastatin should be cautiously used in patients with a previous history of liver disease.
Muscle Effects: Mild elevations of creatine phosphokinase levels are frequently observed in patients treated with lovastatin but these are transient having no clinical significance. Myalgia has also been associated with lovastatin therapy.
More rarely, myopathy has occurred and this should be taken into account for any patient with diffuse myalgias, muscle tenderness or weakness and/or marked elevation of creatine phosphokinase in which case, lovastatin therapy should be discontinued.
Ophthalmic Evaluations: There are no indications that lovastatin has an adverse effect on the human lens.
Homozygous Familial Hypercholesterolemia: In patients with the rare homozygous familial hypercholesterolemia, lovastatin was less effective; possible because these patients have no functional LDL receptors.
Lovastatin appears to be more likely to raise serum transaminases.
Hypertriglyceridemia: Lovastatin is not indicated where hypertriglyceridemia is the abnormality of most concern (ie, hyperlipidemia types I, IV and V).
Use in children: Safety and effectiveness in children have not been established.
Use in the elderly: No apparent increase in the adverse effects in elderly patients has been observed.

Use in pregnancy: Medostatin is contraindicated during pregnancy.
Medostatin should be administered to women of childbearing age only when conceiving is highly unlikely for such patients. In case such a patient becomes pregnant while taking Medostatin, the therapy should be discontinued and the patient apprised of the potential hazard to the fetus.
Use in lactation: As with other drugs, Medostatin is excreted in the human milk and for this reason, women taking Medostatin should not breastfeed their infants.

Lovastatin is generally well tolerated; for the most part, adverse reactions have been mild and transient in nature.
Frequently: Flatulence, diarrhoea, constipation, nausea, dyspepsia, dizziness, blurred vision, headache, muscle cramps, myalgia, skin rashes and abdominal pain have been reported. Patient receiving active control agents had a similar or higher incidence of gastrointestinal effects.
Other Adverse Reactions Occurring Less Frequently: Fatigue, pruritus, dry mouth, insomnia, sleep disorders and dysgeusia. Myopathy and rhabdomyolysis have been reported rarely.
The following additional adverse reactions can occur: Hepatitis, cholestatic jaundice, vomiting, anorexia, paresthesia and psychic disturbances including anxiety; erythema multiforme, including Stevens-Johnson syndrome; toxic epidermal necrolysis.
An apparent hypersensitivity syndrome has been reported rarely which has included ≥1 of the following features: Anaphylaxis, angioedema, lupus-like syndrome, polymyalgia rheumatica, thrombocytopenia, leukopenia, hemolytic anemia, increased ESR, arthritis, arthralgia, urticaria, asthenia, photosensitivity, fever, flushing, chills, dyspnea and malaise.

Concomitant administration with immunosuppressive drugs, gemfibrozil, niacin (nicotinic acid) and erythromycin is not recommended.
Coumarin Derivatives: When lovastatin and coumarin anticoagulants are administered concomitantly, prothrombin time may be increased in some patients.
In patients taking anticoagulants, prothrombin time should be determined prior to starting therapy with lovastatin and thereafter, monitored at the intervals usually recommended for patients on coumarin anticoagulants.

Store in a well-closed, light-resistant container at a temperature not exceeding 25°C. Protect from light.

Dyslipidaemic Agents

C10AA02 - lovastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.

POM