Lipirose 5

Lipirose 5 contains 5 mg of the statin called Rosuvastatin which is an HMG-CoA Reductase Inhibitor belonging to an Antilipidemic Agent.

Lipirose 5 is an HMG-CoA reductase inhibitor used to lower lipid levels and reduce the risk of cardiovascular disease including myocardial infarction and stroke.

The peak plasma concentrations of Lipirose 5 were reached 3 to 5 hours following oral dosing. Both Cmax and AUC increased in approximate proportion to the Lipirose 5 doses. The absolute bioavailability of Lipirose 5 is approximately 20%. The mean volume of distribution at the steady state of Lipirose 5 is approximately 134 liters. Lipirose 5 is 88% bound to plasma proteins, mostly albumin. Lipirose 5 is not extensively metabolized; approximately 10% of a radiolabeled dose is recovered as a metabolite. Following oral administration, Lipirose 5 and its metabolites are primarily excreted in the feces (90%). The elimination half-life (t1/2) of Lipirose 5 is approximately 19 hours. After an intravenous dose, approximately 28% of total body clearance was via the renal route, and 72% by the hepatic route.

Lipirose 5 shows common side effects like Constipation, stomach pain, Dizziness, difficulty falling asleep or staying asleep, Depression, joint pain, Headache, memory loss or forgetfulness, and confusion.

Lipirose 5 is available in the form of a film-coated Oral Tablet and Oral Capsule.

Rosuvastatin is available in India, the US, Singapore, the UK, Malaysia, Spain, Canada, Russia, Japan, China, and Australia.

Lipirose 5 contains 5 mg of the statin called Rosuvastatin belonging to the Antilipidemic Agent and acts as an HMG-CoA Reductase Inhibitor.

Lipirose 5 is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis (reduces the production of mevalonic acid from HMG-CoA); this then results in a compensatory increase in the expression of LDL receptors on hepatocyte membranes and stimulation of LDL catabolism. In addition to the ability of HMG-CoA reductase inhibitors to decrease levels of high-sensitivity C-reactive protein (hsCRP), they also possess pleiotropic properties including improved endothelial function, reduced inflammation at the site of the coronary plaque, inhibition of platelet aggregation, and anticoagulant effects.

The Data on the onset and duration of action of Lipirose 5 is not clinically established.

The Tmax of Lipirose 5 is approximately 3-5 hours.

Lipirose 5 contains 5 mg of the statin called Rosuvastatin and is used in the treatment of high blood cholesterol and triglycerides (fats) levels. This medicine works by blocking the production of unhealthy fats in your body and prevents the risk of heart problems and stroke (a condition that causes reduced oxygen supply to the brain).

Lipirose 5 contains 5 mg of the statin called Rosuvastatin and is used in the treatment of high blood cholesterol and triglycerides (fats) levels. This medicine works by blocking the production of unhealthy fats in your body and prevents the risk of heart problems and stroke (a condition that causes reduced oxygen supply to the brain).

Lipirose 5 contains 5 mg of the statin called Rosuvastatin and is available in the form of Oral Tablets and Oral capsules.

• Dosage Adjustment in Kidney Patient

CrCl ≥30 mL/minute/1.73 m²: No dosage adjustment necessary.

CrCl <30 mL/minute/1.73 m²: 5 to 10 mg once daily.

• Dosage Adjustment in Hepatic Impairment Patient

There are no specific dosage adjustments provided.

Lipirose 5 contains 5 mg of the statin called Rosuvastatin and is available in the form of Oral Tablets and Oral capsules.

• Dosage Adjustment in Kidney Patient

CrCl ≥30 mL/minute/1.73 m²: No dosage adjustment necessary.

CrCl <30 mL/minute/1.73 m²: 5 to 10 mg once daily.

• Dosage Adjustment in Hepatic Impairment Patient

There are no specific dosage adjustments provided.

Lipirose 5 contains 5 mg of the statin called Rosuvastatin and is used in the treatment of high blood cholesterol and triglycerides (fats) levels. This medicine works by blocking the production of unhealthy fats in your body and prevents the risk of heart problems and stroke (a condition that causes reduced oxygen supply to the brain).

Lipirose 5 contains 5 mg of the statin called Rosuvastatin and is used in the treatment of high blood cholesterol and triglycerides (fats) levels. This medicine works by blocking the production of unhealthy fats in your body and prevents the risk of heart problems and stroke (a condition that causes reduced oxygen supply to the brain).

Lipirose 5 contains 5 mg of the statin called Rosuvastatin and is used in the treatment of high blood cholesterol and triglycerides (fats) levels. This medicine works by blocking the production of unhealthy fats in your body and prevents the risk of heart problems and stroke (a condition that causes reduced oxygen supply to the brain).

It is not known whether Lipirose 5 is excreted in human milk, but a small amount of another drug in this class does pass into breast milk. In rats, breast milk concentrations of Lipirose 5 are three times higher than plasma levels; however, animal breast milk drug levels may not accurately reflect human breast milk levels. Because another drug in this class passes into human milk and because HMG-CoA reductase inhibitors have the potential to cause serious adverse reactions in nursing infants, women who require Lipirose 5 treatment should be advised not to nurse their infants.

Adverse events have been observed in some animal reproduction studies. There are reports of congenital anomalies following maternal use of HMG-CoA reductase inhibitors in pregnancy; however, maternal disease, differences in specific agents used, and the low rates of exposure limit the interpretation of the available data. Cholesterol biosynthesis may be important in fetal development; serum cholesterol and triglycerides increase normally during pregnancy. The discontinuation of lipid-lowering medications temporarily during pregnancy is not expected to have a significant impact on the long-term outcomes of primary hypercholesterolemia treatment. Lipirose 5 should be discontinued immediately if an unplanned pregnancy occurs during treatment.

Common Adverse effects

• Myalgia, diabetes mellitus, constipation, nausea, cystitis, increased serum alanine aminotransferase, increased serum transaminases (including increased serum alkaline phosphatase, increased serum bilirubin), dizziness, headache, arthralgia, asthenia, increased creatine phosphokinase in a blood specimen, Abnormal thyroid function test, increased gamma-glutamyl transferase, increased serum glucose, Abdominal pain, Hematuria, proteinuria, Elevated glycosylated hemoglobin (HbA_1c), Hypersensitivity reaction.

Rare Adverse effects

• Gynecomastia, Pancreatitis, Thrombocytopenia, Autoimmune hepatitis, hepatic failure, hepatitis, jaundice, Angioedema, Drug reaction with eosinophilia and systemic symptoms, immune-mediated necrotizing myopathy, Cognitive dysfunction (reversible; includes amnesia, confusion, memory impairment), depression, peripheral neuropathy, sleep disorder (including insomnia, nightmares), Myoglobinuria, myopathy, myositis, rhabdomyolysis, Renal failure syndrome, Interstitial pulmonary disease.

• Cyclosporine

Cyclosporine increased Lipirose 5 exposure and may result in an increased risk of myopathy. Therefore, in patients taking cyclosporine, the dose of Lipirose 5 should not exceed 5 mg once daily.

• Gemfibrozil

Gemfibrozil significantly increased Lipirose 5 exposure. Due to an observed increased risk of myopathy/rhabdomyolysis, combination therapy with Lipirose 5 and gemfibrozil should be avoided. If used together, the dose of Lipirose 5 should not exceed 10 mg once daily.

• Protease Inhibitors

Coadministration of Lipirose 5 with certain protease inhibitors has differing effects on Lipirose 5 exposure and may increase the risk of myopathy. Simeprevir, which is a hepatitis C virus (HCV) protease inhibitor, or combinations of atazanavir/ritonavir or lopinavir/ritonavir, which are HIV-1 protease inhibitors, increase Lipirose 5 exposure. For these protease inhibitors, the dose of Lipirose 5 should not exceed 10 mg once daily. The combinations of fosamprenavir/ritonavir or tipranavir/ritonavir, which are HIV-1 protease inhibitors, produce little or no change in Lipirose 5 exposure. Caution should be exercised when Lipirose 5 is coadministered with protease inhibitors.

• Coumarin Anticoagulants

Lipirose 5 significantly increased INR in patients receiving coumarin anticoagulants. Therefore, caution should be exercised when coumarin anticoagulants are given in conjunction with Rosuvastatin. In patients taking Coumarin anticoagulants and Lipirose 5 concomitantly, INR should be determined before starting Lipirose 5 and frequently enough during early therapy to ensure that no significant alteration of INR occurs.

• Niacin

The risk of skeletal muscle effects may be enhanced when Lipirose 5 is used in combination with lipid-modifying doses (≥1 g/day) of niacin; caution should be used when prescribing with Rosuvastatin.

• Fenofibrate

When Lipirose 5 was coadministered with fenofibrate, no clinically significant increase in the AUC of Lipirose 5 or fenofibrate was observed. Because it is known that the risk of myopathy during treatment with HMG-CoA reductase inhibitors is increased with concomitant use of fenofibrate, caution should be used when prescribing fenofibrate with Rosuvastatin.

• Colchicine

Cases of myopathy, including rhabdomyolysis, have been reported with HMG-CoA reductase inhibitors, including rosuvastatin, coadministered with colchicine, and caution should be exercised when prescribing Lipirose 5 with colchicine.

The common side effects of Lipirose 5 which contains 5 mg of a statin called Rosuvastatin include the following-

Common

● Constipation, stomach pain, Dizziness, difficulty falling asleep or staying asleep, Depression, joint pain, Headache, memory loss or forgetfulness, confusion.

Rare

● Muscle pain, tenderness, or weakness (or if these symptoms continue after stopping rosuvastatin), lack of energy, fever, chest pain, dark, reddish urine; decreased amount of urine; weakness; and muscle aches, yellowing of the skin or eyes, dark colored urine, pain in the upper right part of the abdomen, nausea, extreme tiredness, weakness, unusual bleeding or bruising, loss of appetite, flu-like symptoms, rash, hives, itching, difficulty breathing or swallowing, swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs, hoarseness.

The common side effects of Lipirose 5 which contains 5 mg of a statin called Rosuvastatin include the following-

Common

● Constipation, stomach pain, Dizziness, difficulty falling asleep or staying asleep, Depression, joint pain, Headache, memory loss or forgetfulness, confusion.

Rare

● Muscle pain, tenderness, or weakness (or if these symptoms continue after stopping rosuvastatin), lack of energy, fever, chest pain, dark, reddish urine; decreased amount of urine; weakness; and muscle aches, yellowing of the skin or eyes, dark colored urine, pain in the upper right part of the abdomen, nausea, extreme tiredness, weakness, unusual bleeding or bruising, loss of appetite, flu-like symptoms, rash, hives, itching, difficulty breathing or swallowing, swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs, hoarseness.

There is no specific treatment in the event of an overdose. In the event of an overdose, the patient should be treated symptomatically, and supportive measures instituted as required. Hemodialysis does not significantly enhance the clearance of rosuvastatin.

Pharmacodynamics

Lipirose 5 dose-dependently reduces elevated LDL cholesterol and reduces total cholesterol and triglycerides and increases HDL cholesterol. A therapeutic response to Lipirose 5 is evident within 1 week of commencing therapy and 90% of the maximum response is usually achieved in 2 weeks. The maximum response is usually achieved within 4 weeks and is maintained after that. Individualization of drug dosage should be based on the therapeutic response.

Pharmacokinetics

• Absorption

In clinical pharmacology studies in men, peak plasma concentrations of Lipirose 5 were reached 3 to 5 hours following oral dosing. Both Cmax and AUC increased in approximate proportion to the Lipirose 5 dose. The absolute bioavailability of Lipirose 5 is approximately 20%. Administration of Lipirose 5 with food did not affect the AUC of rosuvastatin. The AUC of Lipirose 5 does not differ following evening or morning drug administration.

• Distribution

The mean volume of distribution at the steady state of Lipirose 5 is approximately 134 liters. Lipirose 5 is 88% bound to plasma proteins, mostly albumin. This binding is reversible and independent of plasma concentrations.

• Metabolism

Lipirose 5 is not extensively metabolized; approximately 10% of a radiolabeled dose is recovered as a metabolite. The major metabolite is N-desmethyl rosuvastatin, which is formed principally by cytochrome P450 2C9, and in vitro, studies have demonstrated that N-desmethyl Lipirose 5 has approximately one-sixth to one-half the HMG-CoA reductase inhibitory activity of the parent compound. Overall, greater than 90% of active plasma HMG-CoA reductase inhibitory activity is accounted for by the parent compound.

• Excretion

Following oral administration, Lipirose 5 and its metabolites are primarily excreted in the feces (90%). The elimination half-life (t1/2) of Lipirose 5 is approximately 19 hours. After an intravenous dose, approximately 28% of total body clearance was via the renal route, and 72% by the hepatic route.