ROSUVASTATIN ELSaad 40
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Chemical Name:
Rosuvastatin -
Therapeutic Category:
Cardiovascular drugs -
Pharmacologic Category:
Antilipemic Agent, HMG-CoA Reductase Inhibitor -
Pharmaceutical Form:
Tablets -
Composition:
Rosuvastatin 40mg
ROSUVASTATIN ElSaad
Film Coated Tablets
Rosuvaststin (Calcium)
1-COMPOSITION:
ROSUVASTATIN ElSaad 5- F.C.Tablet: Each film coated tablet contains Rosuvaststin (Calcium) 5mg.
ROSUVASTATIN ElSaad 10 –F.C.Tablet: Each film coated tablet contains Rosuvaststin (Calcium) 10mg.
ROSUVASTATIN ElSaad 20 –F.C.Tablet: Each film coated tablet contains Rosuvaststin (Calcium) 20mg.
ROSUVASTATIN ElSaad 40 –F.C.Tablet: Each film coated tablet contains Rosuvaststin (Calcium) 40mg.
Excipient:
ROSUVASTATIN ElSaad 5:
Lactose monohydrate, Microcrystalline cellulose, Tricalcium Phosphate, Crospovidone, Magnesium Stearate, Hydroxy Propyl Methyl Cellulose, Titanium Dioxide, Quinoline Yellow, Triacetine, Ethanol 97%.
ROSUVASTATIN ElSaad 10:
Lactose monohydrate, Microcrystalline cellulose, Tricalcium Phosphate, Crospovidone, Magnesium Stearate, Hydroxy Propyl Methyl Cellulose, Titanium Dioxide, Erythrosine, Triacetine, Ethanol 97%.
ROSUVASTATIN ElSaad 20:
Lactose monohydrate, Microcrystalline cellulose, Tricalcium Phosphate, Crospovidone, Magnesium Stearate, Hydroxy Propyl Methyl Cellulose, Titanium Dioxide, Dibutylphtalate, Triacetine, Ethanol 97%.
ROSUVASTATIN ElSaad 40:
Lactose monohydrate, Microcrystalline cellulose, Tricalcium Phosphate, Crospovidone, Magnesium Stearate, Hydroxy Propyl Methyl Cellulose, Titanium Dioxide, Red Iron Oxide, Yellow Iron Oxide, Triacetine, Ethanol 97%.
2-MECHANISM of ACTION:
Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, Which converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, (a precursor for cholesterol). The primary site of action of Rosuvastatin is the liver, the target organ for cholesterol lowering.
Rosuvastatin increases the number of hepatic LDL receptors on the cell-surface, enhancing uptake and catabolism of LDL and it inhibits the hepatic synthesis of VLDL, thereby it reduces elevated VLDL, LDL-cholesterol, total cholesterol and triglycerides and increases HDL-cholesterol.
3-PHARMACOKINETICS:
Absorption: Maximum Rosuvastatin plasma concentrations are achieved approximately 5 hours after oral administration. The absolute bioavailability is approximately 20%.
Distribution: Rosuvastatin is taken up extensively by the liver, The volume of distribution is approximately 134 L, Approximately 90% is bound to plasma proteins, mainly to albumin.
Metabolism: Rosuvastatin undergoes limited metabolism (approximately 10%), it is metabolised in the liver.
Excretion: Approximately 90% of the Rosuvastatin dose is excreted unchanged in the faeces, and the remaining part is excreted in urine. The plasma elimination half-life is approximately 19 hours.
4-INDICATIONS:
Rosuvastatin is indicated for the following cases:
- Treatment of primary hypercholesterolaemia (type IIa including heterozygous familial hypercholesterolaemia) or mixed dyslipidaemia (type IIb) as an adjunct to diet when response to diet or exercise and weight reduction is inadequate.
- Treatment of Homozygous familial hypercholesterolaemia as an adjunct to diet and other lipid lowering treatments.
- Prevention of major cardiovascular events in patients who are estimated to have a high risk for a first cardiovascular event as an adjunct to correction of other risk factors.
5-CONTRAINDICATIONS:
- Hypersensitivity to Rosuvastatin or to any of the excipients.
- In patients with active liver disease, with severe renal impairment (creatinine clearance <30 ml/min), with myopathy.
- The 40 mg dose is contraindicated in patients with pre-disposing factors for myopathy/rhabdomyolysis. Such factors include:
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Moderate renal impairment (creatinine clearance < 60 ml/min).
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Hypothyroidism.
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Personal or family history of hereditary muscular disorders.
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Previous history of muscular toxicity with another HMG-CoA reductase inhibitor or fibrate.
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Alcohol abuse.
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Situations where an increase in plasma levels may occur.
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Age >70 years.
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Concomitant use of Fibrates.
6-ADVERSE REACTIONS:
Common adverse reactions include: Diabetes mellitus, Headache, Dizziness, Constipation, Nausea, Abdominal pain, Myalgia, Asthenia.
7-DRUG INTERACTIONS:
- Very rare cases of rhabdomyolysis have been reported with the use of Ezetimibe in combination with HMG-CoA reductase inhibitors.
- Concomitant administration of Rosuvastatin with drugs that are inhibitors of hepatic uptake transporter OATP1B1 and efflux transporter BCRP increased risk of myopathy by increasing Rosuvastatin plasma concentrations.
- Concomitant administration of Rosuvastatin with Ciclosporin is contraindicated.
- Fibrates and Niacin increase the risk of myopathy when given concomitantly with HMG-CoA reductase inhibitors.
- Concomitant administration of Rosuvastatin with antacid containing Aluminium and Magnesium Hydroxide decreases Rosuvastatin plasma concentration.
- Erythromycin increases gut motility which results in decreased concentration of Rosuvastatin.
- Concomitant of administration of Rosuvastatin with oral contraceptives increased plasma levels of Ethinyl Estradiol and Norgestrel.
- Combination of Rosuvastatin and Fusidic Acid is not recommended.
- Concomitant administration of Rosuvastatin with Warfarin or another coumarin anticoagulant may result in an increase in International Normalised Ratio (INR).
8-WARNINGS and PRECAUTIONS:
- An assessment of renal function should be considered during routine follow-up of patients treated with a dose of 40 mg Rosuvastatin.
- Rosuvastatin should be prescribed with caution in patients with pre-disposing factors formyopathy/rhabdomyolysis.
- Patients should be asked to report inexplicable muscle pain, weakness or cramps immediately, particularly if associated with malaise or fever and CK levels should be measured in these patients, therapy should be discontinued if CK levels are markedly elevated (>5xULN).
- Rosuvastatin should be used with caution in patients who consume excessive quantities of alcohol and / or have a history of liver diseases.
- The concomitant use of Rosuvastatin and certain protease inhibitors in HIV patients is not recommended unless the dose of Rosuvastatin is adjusted.
- Statin therapy should be discontinued in patient who developed interstitial lung disease.
- In some patients, at high risk of future diabetes they should take into account that Statins raise blood glucose and may produce a level of hyperglycaemia.
- Rosuvastatin contains lactose monohydrate, patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this drug.
- When driving vehicles or operating machines, it should be taken into account that dizziness may occur during treatment.
9-PREGNANCY and LACTATION:
Rosuvastatin is contraindicated in pregnancy and lactation.
10-DOSAGE and ADMINISTRATION:
Before treatment initiation the patient should be placed on a standard cholesterol-lowering diet that should continue during treatment.
Rosuvastatin may be given at any time of day, with or without food, and the dose should be individualized according to the goal of therapy and patient response.
Treatment of hypercholesterolaemia: The recommended start dose is 5 or 10 mg orally once daily, and A dose adjustment to the next dose level can be made after 4 weeks, if necessary. a final titration to the maximum dose of 40 mg should only be considered in patients with severe hypercholesterolaemia at high cardiovascular risk and with Specialist supervision.
Prevention of cardiovascular events: The recommended dose is 20 mg daily.
In children 6 to 9 years of age with heterozygous familial hypercholesterolaemia, the usual dose range is 5-10 mg orally once daily. and In children 10 to 17 years of age the usual dose range is 5-20 mg orally once daily.
Children and adolescents should be placed on standard cholesterol-lowering diet before rosuvastatin treatment initiation this diet should be continued during rosuvastatin treatment.
Rosuvastatin tablet 40 mg is not suitable for use in paediatric patients.
Rosuvastatin is not recommended for use in children younger than 6 years.
In the elderly >70 years: A start dose of 5 mg is recommended.
Patients with moderate renal impairment (creatinine clearance of < 60 mL / min): The recommended start dose is 5 mg, The 40 mg dose is contraindicated in them, and The use of ROSUVASTATIN in patients with severe renal impairment is contraindicated for all doses
11-OVERDOSAGE:
In the event of overdose, the patient should be treated symptomatically and supportive measures instituted as required. Liver function and CK levels should be monitored. Haemodialysis is unlikely to be of benefit
12-PACKAGE:
ROSUVASTATIN ElSaad 5 –F.C.Tablet: Carton package of 10 or 30 F.C.Tablets.
ROSUVASTATIN ElSaad 10 –F.C.Tablet: Carton package of 10 or 30 F.C.Tablets.
ROSUVASTATIN ElSaad 20 –F.C.Tablet: Carton package of 10 or 30 F.C.Tablets.
ROSUVASTATIN ElSaad 40 –F.C.Tablet: Carton package of 10 or 30 F.C.Tablets.
13-STORAGE CONDIIONS:
Store ROSUVASTATIN ElSaad- Film coated tablets at temperature between (15-30)°C, Protect from moisture.
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