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ETC / RX - Anti-diabetics - Rosuliptin

COMPOSITION:

Film-coated caplet ROSULIPTIN® 10

  • Active ingredient: Rosuvastatin (as Rosuvastatin calcium)  10 mg
  • Other ingredients: Lactose monohydrate, cellulose microcrystalline, crospovidone, dicalcium hydrophosphate, magnesium stearate, opadry II white

Film-coated caplet ROSULIPTIN® 20

  • Active ingredient: Rosuvastatin (as Rosuvastatin calcium)  20 mg
  • Other ingredients: Lactose monohydrate, cellulose microcrystalline, crospovidone, dicalcium hydrophosphate, magnesium stearate, opadry pink.

PHARMACODYNAMICS:

Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that 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 reducing the total number of VLDL and LDL particles.

Rosuvastatin reduces elevated LDL-cholesterol, total cholesterol and triglycerides and increases HDL-cholesterol. It also lowers ApoB, nonHDL-C, VLDL-C, VLDL-TG and increases ApoA-I. Rosuvastatin also lowers the LDL-C/HDL-C, total C/HDL-C and nonHDL-C/HDL-C and the ApoB/ApoA-I ratios.

A therapeutic effect is obtained within 1 week following treatment initiation and 90% of maximum response is achieved in 2 weeks. The maximum response is usually achieved by 4 weeks and is maintained after that.


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. Approximately 90% of rosuvastatin is bound to plasma proteins, mainly to albumin.

Metabolism: Rosuvastatin undergoes limited metabolism (approximately 10%). The main metabolites identified are the N-desmethyl and lactone metabolites. The N-desmethyl metabolite is approximately 50% less active than rosuvastatin whereas the lactone form is considered clinically inactive. Rosuvastatin accounts for greater than 90% of the circulating HMG-CoA reductase inhibitor activity.

Excretion: Approximately 90% of the rosuvastatin dose is excreted unchanged in the faeces (consisting of absorbed and non-absorbed active substance) and the remaining part is excreted in urine. Approximately 5% is excreted unchanged in urine. The plasma elimination half-life is approximately 19 hours. The elimination half-life does not increase at higher doses.


INDICATIONS:

  • Rosuvastatin is indicated for patients with primary hypercholesterolaemia (heterozygous familial and nonfamilial) or mixed dyslipidaemia (Fredrickson type IIa and IIb) as an adjunct to diet when response to diet and exercise has been inadequate.
  • Rosuvastatin reduces elevated total cholesterol, LDL – cholesterol, triglycerides and apolipoprotein B, and increases HDL – cholesterol.
  • Rosuvastatin is also indicated in patients with homozygous familial hypercholesterolaemia, either alone or as an adjunct to diet and other lipid lowering treatments (e.g LDL apheresis).

ADMINISTRATION AND DOSAGE:

Rosuvastatin may be administered as a single dose at any time of day and without regard to meals.

Adults:

Recommend to start from the lowest dosage which is still effective. After that, if needed, it can be adjusted the dosage that is based on individual response by increasing dosage periodically (interval time for each wave is at least 4 weeks) and is recommended to monitor its adverse effects, especially, the adverse effects to muscle.

Heterozygous familial and nonfamilial hypercholesterolemia; mixed dyslipidemia:

Oral: The recommended starting dose of Rosuvastatin is 5 mg once daily

A dose adjustment to 10 – 20 mg once daily can be made after 2- 4 weeks, if necessary.

Rosuvastatin 40 should only be used for patient with severe hypercholesterolaemia who do not achieve their treatment goal on a dose of 20 mg/day.

Homozygous familial hypercholesterolemia (HFH): Initial: Take orally 20 mg once daily (maximum dose: 40 mg/day).

Dosage in patients with renal insufficiency:

No dose adjustment is necessary in patients with mild to moderate renal impairment. The 40 mg dose is contraindicated in patients with moderate renal impairment. The use of Rosuvastatin in patients with severe renal impairment is contraindicated.

Children: Not recommended.

Note: 

  • Relation between the dose of rosuvastatin and rhabdomyolysis should note that all patients must start with dose 10mg once daily and only increase to 20mg if necessary after 4 weeks. Close monitoring for situations using the dose 40mg.
  • Pharmacokinetic studies in United State show an approximate 2-fold elevation in absorption of Rosuvastatin in Asian subjects compared with Caucasians, therefore the 5mg initial dosage should be considered with Asian.

CONTRAINDICATIONS:

  • Hypersensitivity to any component of this product.
  • Active liver disease or unexplained persistent elevations of serum transaminases.
  • Severe renal impairment (creatinine clearance lesser than 30ml/ min.)
  • Patients with myopathy.
  • Patients receiving ciclosporin.
  • Pregnancy and lactation, and women of childbearing potential not using appropriate contraceptive measures.

WARNINGS AND PRECAUTIONS:

  • Should consider when use the statin drugs in patients with predisposing factors to muscle injury. The statin drugs may cause the adverse effects to muscle system such as myasthenia, myositis, especially to patients with factors of risk as patients over 65 years, patients with uncontrolled hypothyroidism, patients with renal impairment. Close monitoring the side effects during the therapy.
  • Patients should immediately inform physician about signs or symptoms of muscle pain, fatigue, fever, dark urine, nausea or vomiting during the treatment.
  • Liver function test should be performed prior to and periodically during therapy with Rosuvastatin.
  • Use with caution in patient who consume large amount of alcohol or have a history of liver disease.
  • Temporarily withhold in any patient with an acute or serious condition predisposing to renal failure secondary to rhabdomyolysis (sepsis, hypotension, major surgery, trauma, severe metabolic, endocrine, or electrolyte disorders, uncontrolled seizures).
  • Safety and efficacy have not been established in children.
  • Women of child bearing potential should use appropriate contraceptive measures.

SIDE EFFECTS:

Headache, dizziness, hypertension, palpitation, pharyngitis, diarrhea, constipation, nausea, abdominal pain, myalgia, myopathy, asthenia of body.

In case of an unexpected reaction, consult your physician.


INTERACTIONS:

  • Plasma concentrations of rosuvastatin decreased when given with antacids. Antacids should be administered at least 2 hours after rosuvastatin.
  • Cyclosporine may increase serum concentrations of rosuvastatin (up to 10 times usual concentrations). Limit dose of rosuvastatin to 5 mg/day.
  • Gemfibrozil: may be increased (doubled) serum concentrations of rosuvastatin during concurrent administration; Combination should be avoided. Limit dose of rosuvastatin to 10 mg/day.
  • Clofibrate, fenofibrate, and niacin may increase the risk of myopathy and rhabdomyolysis
  • Plasma concentrations of oral contraceptive increased when given with rosuvastatin.
  • Warfarin: Effects may be increased by rosuvastatin.
  • Alcohol and rosuvastatin can both be damaging to the liver.

OVERDOSAGE:

There is no specific treatment in the event of overdose. 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. Hemodialysis does not significantly enhance clearance of rosuvastatin.


PRESENTATION:

Box of 1 blister x 10 tablets.

Storage: Store at temperature from 150C to 300C, in a dry place, protect from light.

Shelf-life: 36 months from manufacturing date. Do not use after expiry date.