Lipvar 10

Print
Lipid-lowering agent - Statin group
Barcode: 8936007614198
Description

COMPOSITION:
Atorvastatin (as calcium) .......................................................................10 mg
Excipients  q.s .....................................................................................1 tablet
(Lactose monohydrate, avicel M101, calcium carbonate, hydroxypropyl cellulose, croscarmellose sodium, polysorbate 80, magnesium stearate).
DOSAGE FORM: Tablet.
PRESENTATION: Box of 3 blisters x 10 tablets
PHARMACODYNAMICS: Lipvar is a synthetic lipid-lowering agent including active ingredient Atorvastatin calcium. It is a competitive inhibitor of 3-hydroxy-3-methyglutaryl-coenzyme A (HMG-CoA) reductase, which prevents the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. Atorvastatin lowers the plasma cholesterol and lipoprotein levels by inhibiting hepatic cholesterol synthesis and by increasing the amount of hepatic LDL (Low-Density Lipoprotein) receptors on the cell surface, resulting in enhancing the uptake and catabolism of LDL.
Atorvastatin enhances HDL (High-Density Lipoprotein) cholesterol (5% - 15%) and consequently lowers LDL /HDL and total cholesterol /HDL. Besides, Atorvastatin reduces the plasma triglyceride (10 - 30%) by increasing the clearance of surplus VLDL (Very Low-Density Lipoprotein) by LDL receptor.
In clinical studies, the evidences have showed that statins remarkably reduce coronary arterial accidents, every known cardiovascular accidents, and total of death in patients with coronary arterial disease.
PHARMACOKINETICS: Atorvastatin is rapidly absorbed after oral administration; maximum plasma concentrations (Cmax) occur within 1 to 2 hours. Extent of absorption increases in proportion to atorvastatin dose. The absolute bioavailability of atorvastatin is approximately 12% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%. Although food decreases the rate and extent of drug absorption, the therapeutic effect is unchangeable whether atorvastatin is given with or without food. Plasma atorvastatin concentrations are lower following evening drug administration compared with morning. However, the effect of drug is the same whatever the time of day for drug.
Atorvastatin is ≥ 98% bound to plasma proteins. Mean volume of distribution of atorvastatin is approximately 381L. Atorvastatin is metabolised by CPY 3A4 to ortho- and parahydroxylated derivatives and various beta-oxidation products. Approximately 70% of circulating inhibitory activity for HMG-CoA reductase is attributed to active metabolites. Atorvastatin is eliminated primarily in bile. Mean plasma elimination half-life of atorvastatin in humans is approximately 14 hours. The half-life of inhibitory activity for HMG-CoA reductase is approximately 20 to 30 hours.
Special populations
Elderly: Plasma concentrations of atorvastatin are higher in healthy elderly subjects than in young adults. These differences were of no clinical significance.
Paediatric population: Same as in adults
Gender: Concentrations of atorvastatin and its active metabolites in women differ from those in men. These differences were of no clinical significance.
Renal impairment: Renal disease has no influence on the plasma concentrations or lipid effects of atorvastatin.
Hepatic impairment: Plasma concentrations of atorvastatin and its active metabolites are markedly increased in patients with chronic alcoholic liver disease.
INDICATIONS: Lipvar is used in the following cases: elevated total cholesterol, LDL-cholesterol, (LCL-C) apolipoprotein B, and triglycerides in patients with primary hypercholesterolaemia including heterozygous familial and non-familial hypercholesterolaemia, combined (mixed) hyperlipidaemia (corresponding to Types IIa and IIb of the Fredrickson classification), hypertriglyceridemia (Type IV of the Fredrickson classification) when response to diet is inadequate.
Lipvar is also indicated to reduce total cholesterol and LDL-cholesterol in patients with homozygous familial hypercholesterolaemia.
Lipvar is used in primary prevention of cardiovascular events: slowing the progression of coronary atherosclerosis, reducing the risk of myocardial infarction, reducing the risk of procedures of coronary arteries reproduction, the risk of stroke, the risk of death from cardiovascular disease.
CONTRAINDICATIONS: Hypersensitivity to any components of the drug.
Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels.
Unexplained persistent elevations of serum transaminases exceeding 3 times the upper limit of normal.
Patients receiving treatment of tipranavir and ritonavir, or telaprevir.
During pregnancy, while breast-feeding and in women of child-bearing potential not using appropriate contraceptive measures.
PRECAUTIONS: Before starting on the atorvastatin treatment, blood cholesterol should be coordinately controlled by diet, weight loss, exercise, treatment of diseases associated with elevated lipid.  Lipid assay should be periodically tested and the dosage can be adjusted according to patient's response to the drug. Using LDL-C concentration to start treatment and assess treatment response.
It is recommended that liver enzyme tests be performed before the initiation of statin and as clinically indicated.
Liver effects: Liver function tests should be performed before the initiation of treatment and periodically thereafter. Patients who develop any signs or symptoms suggestive of liver injury should have liver function tests performed. Patients who develop increased transaminase levels should be monitored until the abnormality(ies) resolve. Should an increase in ALT or AST of greater than 3 times the upper limit of normal (ULN) persist, reduction of dose or withdrawal of atorvastatin is recommended. Atorvastatin should be used with caution in patients who consume substantial quantities of alcohol and/or have a history of liver disease.
Hemorrhagic stroke: For patients with prior hemorrhagic stroke, the balance of risks and benefits of atorvastatin 80 mg is uncertain, and the potential risk of hemorrhagic stroke should be carefully considered before initiating treatment.
Skeletal muscle effects: Atorvastatin, like other HMG-CoA reductase inhibitors, may in rare occasions affect the skeletal muscle and cause myalgia, myositis, and myopathy that may progress to rhabdomyolysis, a potentially life-threatening condition characterised by markedly elevated creatine kinase (CK) levels (> 10 times ULN), myoglobinaemia and myoglobinuria which may lead to renal failure.
A creatine kinase (CK) level should be measured in the following situations:
+ Before starting treatment: A CK level should be measured in the following situations: renal impairment, hypothyroidism, personal or family history of hereditary muscular disorders, previous history of muscular toxicity with a statin or fibrate, previous history of liver disease and/or where substantial quantities of alcohol are consumed, In elderly (age > 70 years) according to the presence of other predisposing factors for rhabdomyolysis, situations where an increase in plasma levels may occur, such as interactions and special populations. In such situations, the risk of treatment should be considered in relation to possible benefit, and clinical monitoring is recommended. If CK levels are significantly elevated (> 5 times ULN) at baseline, treatment should not be started.
+ Whilst on statin treatment: Patients must be asked to promptly report muscle pain, cramps, or weakness. If such symptoms occur whilst a patient is receiving treatment with atorvastatin, their CK levels should be measured.
Concomitant treatment with other medicinal products: Risk of rhabdomyolysis is increased when atorvastatin is administered concomitantly with inhibitors of CYP3A4 or transport proteins or HIV protease inhibitors including ciclosporin, clarithromycin, ketoconazole, indinavir, darunavir, etc). The risk of myopathy may also be increased with the concomitant use of gemfibrozil and other fibric acid derivates. If possible, alternative therapies should be considered instead of these medicinal products. In cases where co-administration of these medicinal products with atorvastatin is necessary, the benefit and the risk of concurrent treatment should be carefully considered (in the case of potent CYP3A4 inhibitors, a lower starting dose of atorvastatin should be considered).
Interstitial lung disease: Exceptional cases of interstitial lung disease have been reported with some statins, especially with long-term therapy. Presenting features can include dyspnoea, cough and deterioration in general health (fatigue, weight loss and fever). If it is suspected a patient has developed interstitial lung disease, statin therapy should be discontinued.
Diabetes mellitus:
Some evidence suggests that statins as a class raise blood glucose and in some patients, at high risk of future diabetes. This risk, however, is outweighed by the reduction in vascular risk with statins and therefore should not be a reason for stopping statin treatment. Patients at risk (fasting glucose 5.6 to 6.9 mmol/L, BMI > 30, raised triglycerides, hypertension) should be monitored.
Excipients: Lipvar contains lactose. Patients with rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
PREGNANCY AND LACTATION:
Women of childbearing potential: Women of child-bearing potential should use appropriate contraceptive measures during treatment
Pregnancy: Atorvastatin is contraindicated during pregnancy. Safety in pregnant women has not been established. No controlled clinical trials with atorvastatin have been conducted in pregnant women. Rare reports of congenital anomalies following intrauterine exposure to HMG-CoA reductase inhibitors have been received. Studies in animals have shown toxicity to reproduction. Maternal treatment with atorvastatin may reduce the fetal levels of mevalonate which is a precursor of cholesterol biosynthesis.
Atherosclerosis is a chronic process, and ordinarily discontinuation of lipid-lowering medicinal products during pregnancy should have little impact on the long-term risk associated with primary hypercholesterolaemia.
For these reasons, atorvastatin should not be used in women who are pregnant, trying to become pregnant or suspect they are pregnant. Treatment with atorvastatin should be suspended for the duration of pregnancy or until it has been determined that the woman is not pregnant.
Breast-feeding: It is unknown whether atorvastatin or its metabolites are excreted in human milk. In rats, plasma concentrations of atorvastatin and its active metabolites are similar to those in milk. Because of the potential for serious adverse reactions, women taking atorvastatin should not breast-feed their infants. Atorvastatin is contraindicated during breast-feeding.
Fertility: In animal studies atorvastatin had no effect on male or female fertility.
EFFECTS ON ABILITY TO DRIVE AND USE MACHINES:
The drug should be used with caution in drivers and machinery operators because of possibility of headache, dizziness.
INTERACTIONS:
Effect of co-administered medicinal products on atorvastatin
CYP3A4 inhibitors
Potent CYP3A4 inhibitors have been shown to lead to markedly increased concentrations of atorvastatin (e.g. ciclosporin, clarithromycin, delavirdine, ketoconazole, voriconazole, itraconazole, posaconazole and HIV protease inhibitors including ritonavir, lopinavir, atazanavir, indinavir, darunavir, etc.). In cases where co-administration of these medicinal products with atorvastatin cannot be avoided lower starting and maximum doses of atorvastatin should be considered and appropriate clinical monitoring of the patient is recommended
Moderate CYP3A4 inhibitors (e.g. erythromycin, diltiazem, verapamil and fluconazole) may increase plasma concentrations of atorvastatin. An increased risk of myopathy has been observed with the use of erythromycin in combination with statins. Therefore, a lower maximum dose of atorvastatin should be considered and appropriate clinical monitoring of the patient is recommended when concomitantly used with moderate CYP3A4 inhibitors. Appropriate clinical monitoring is recommended after initiation or following dose adjustments of the inhibitor.
CYP3A4 inducers
Concomitant administration of atorvastatin with inducers of cytochrome CYP3A4 (e.g. efavirenz, rifampin, etc.) can lead to variable reductions in plasma concentrations of atorvastatin. Due to the dual interaction mechanism of rifampin, simultaneous co-administration of atorvastatin with rifampin is recommended, as delayed administration of atorvastatin after administration of rifampin has been associated with a significant reduction in atorvastatin plasma concentrations. The effect of rifampin on atorvastatin concentrations in hepatocytes is, however, unknown and if concomitant administration cannot be avoided, patients should be carefully monitored for efficacy.
Transport protein inhibitors
Inhibitors of transport proteins (e.g. ciclosporin) can increase the systemic exposure of atorvastatin. The effect of inhibition of hepatic uptake transporters on atorvastatin concentrations in hepatocytes is unknown. If concomitant administration cannot be avoided, a dose reduction and clinical monitoring for efficacy is recommended.
Gemfibrozil, fibric acid derivatives, ezetimibe, colestipol, fusidic acid, and colchicine
The use of fibrates, ezetimibe alone is occasionally associated with muscle related events, including rhabdomyolysis. The risk of these events may be increased with the concomitant use of fibrates, ezetimibe and atorvastatin. If concomitant administration cannot be avoided, appropriate clinical monitoring of these patients is recommended. Plasma concentrations of atorvastatin were lower (by approx. 25%) when colestipol was co-administered with atorvastatin. However, lipid effects were greater when atorvastatin and colestipol were co-administered than when either medicinal product was given alone. Interaction studies with atorvastatin and fusidic acid have not been conducted. Muscle related events have been reported with atorvastatin and fusidic acid given concurrently. The mechanism of this interaction is not known. Patients should be closely monitored and temporary suspension of atorvastatin treatment may be appropriate. Although no studies on interactions between atorvastatin and colchicine have been reported, myopathy has been there have been case reports of patients with diseases of the body as atorvastatin combination therapy with colchicine. Therefore caution should be exercised when prescribing two drugs
Effect of atorvastatin on co-administered medicinal products
Digoxin
When multiple doses of digoxin and 10 mg atorvastatin were co-administered, steady-state digoxin concentrations increased slightly. Patients taking digoxin should be monitored appropriately.
Oral contraceptives
Co-administration of atorvastatin with an oral contraceptive produced increases in plasma concentrations of norethindrone and ethinyl oestradiol.
Warfarin
In a clinical study in patients receiving chronic warfarin therapy, co-administration of atorvastatin 80 mg daily with warfarin caused a small decrease in prothrombin time during the first 4 days of dosing which returned to normal within 15 days of atorvastatin treatment. Although only very rare cases of clinically significant anticoagulant interactions have been reported, prothrombin time should be determined before starting atorvastatin in patients taking coumarin anticoagulants. Atorvastatin therapy has not been associated with bleeding or with changes in prothrombin time in patients not taking anticoagulants.
ADVERSE EFFECTS:
Common: Infections: nasopharyngitis. Immune system disorders: allergic reactions. Metabolism and nutrition disorders: hyperglycaemia. Respiratory disorders: pharyngolaryngeal pain, epistaxis. Gastrointestinal disorders: constipation, flatulence, dyspepsia, nausea, diarrhoea. Nervous system disorders: headache, dizziness, blurred vision, insomnia, asthesia. Musculoskeletal disorders: myalgia, arthralgia, muscle spasms, back pain.
Uncommon: Metabolism and nutrition disorders: hypoglycaemia, weight gain, anorexia. Psychiatric disorders: nightmare, insomnia. Nervous system disorders: dizziness, paraesthesia, dysgeusia, amnesia. Eye disorders: vision blurred. Ear disorders: tinnitus. Gastrointestinal disorders: vomiting, abdominal pain, eructation, pancreatitis. Hepatic disorders: hepatitis. Skin and subcutaneous tissue disorders: urticaria, skin rash, pruritus, alopecia. Muscular disorders: neck pain, muscle fatigue.
Rare: thrombocytopenia, peripheral neuropathy, visual disturbance, cholestasis, angioneurotic oedema, Stevens- Johnson syndrome, myopathy, rhabdomyolysis, herniation. 
Very rare: anaphylaxis, hearing loss, hepatic failure, gynecomastia.
Some other adverse effects include impaired awareness (e.g., amnesia, confusion), increases in HbA1c, transamine.
Inform your physician about any adverse effects occur during the treatment.
OVERDOSAGE: There is no specific treatment for atorvastatin overdosage. In the event of an overdose, the patient should be treated symptomatically, and supportive measures institutes as required. Due to extensive drug binding to plasma proteins, hemodialysis is not expected to significantly enhance atorvastatin clearance.
DOSAGE & ADMINISTRATION: Atorvastatin may be given at any time of day with or without food.
Before therapy with atorvastatin, blood cholesterol should be controlled by a reasonable diet, exercise and weight loss in obese patients, and treatment of underlying pathology. Patients should maintain a standard cholesterol-lowering diet during treatment.
The dose should be individualised according to baseline LDL-C levels, the g

Reviews

There are yet no reviews for this product.