Vascor
SIMVASTATIN 20mg/40mgPRODUCT
DESCRIPTION
Vascor Tablet 20: An oval, scored and marked "UP 20" orange film coated
tablet.
Vascor Tablet 40: An oval, scored and marked "UP 40" pink film coated
tablet.
COMPOSITION
Vascor Tablet 20: Each tablet contains 20 mg of Simvastatin.
Vascor Tablet
40: Each tablet contains 40 mg of Simvastatin.
PHARMACOLOGY
Simvastatin is absorbed from the GI tract and is hydrolysed to its active
metabolite, Beta-hydroxyacid form. Simvastatin undergoes extensive first
pass metabolism in the liver. Both drug and the active metabolite are about
95% protein bound. It is mainly excreted in the faeces via bile as
metabolites. About 10 to 15% is recovered in the urine, mainly in inactive
form. The half life of the active metabolite is 1.9 hours.
INDICATIONS
Simvastatin is used for primary hypercholesterolaemia, heterozygous familial
hypercholesterolaemia or combined (mixed) hyperlipidaemia in patients who
have not responded to diet and appropriate measures; to reduce the incidence
of clinical coronary events end slow progression of coronary atherosclerosis
in patients with coronary heart disease.
MECHANISMS OF ACTION
Simvastatin belongs to the lipid regulating drug class commonly known as
statins. Its pharmacological class is 3hydroxy-3-methylglutaryl coenzyme A (HMG
Co-A) reductase inhibitor. Simvastatin competitively inhibits the HMG Co-A
reductase, the enzyme involved in cholesterol synthesis. Simvastatin reduces
total cholesterol, low density lipoprotein (LDL) cholesterol, very low
density lipoprotein (VLDL) cholesterol and triglycerides. It also increases
high density lipoprotein (HDL) cholesterol. They are considered to exert
beneficial effects by stimulating an increase in LDL receptors on hepatocyte
membranes thereby increasing the clearance of LDL from the circulation.
SIDE EFFECTS
Myositis is a rare but significant clinical adverse effect. Other common
side-effects include headache, altered liver-function tests and GI
disturbances such as vomiting and nausea. Rare side effects include rash,
alopecia, anaemia, dizziness, depression, paraesthesia, peripheral
neuropathy, hepatitis, jaundice, pancreatitis, hypersensitivity syndrome (angioedema).
Counselling: Advise patients to report any unexplained muscle pain,
tenderness and weakness promptly.
PRECAUTIONS
Simvastatin should be used with caution in those with a history of liver
disease or those with high intake of alcohol. The manufacturer advises liver
function test be carried out before and within 1-3 months of starting
treatment and thereafter at intervals of 6 months for 1 year, unless
indicated sooner by signs and symptoms of hepatotoxicity. Treatment should
be discontinued if serum transaminase concentration rises to, and persist
at, 3 times the upper limit of reference range. Patients should be advised
to report any muscle pain.
Use in pregnancy and nursing mothers: Refer
contraindications.
Use in paediatric: It is not recommended as the safety and effectiveness
study has not yet been established.
Use in elderly: The efficacy assessment
by the reduction in total-C and LDL-C, appeared to be the same in the whole
population and the group of elderly who were given simvastatin in controlled
clinical studies. Moreover, the frequency of laboratory or clinical adverse
investigations shown no apparent increase.
Laboratory findings: Occasionally, serum transaminases have been reported to
increase persistently. Alkaline phosphate and g-glutemyl trenspeptidese have
been reported to be raised. Mild and transient abnormalities in liver
function test. Increased serum CK levels, derived from skeletal muscle have
been reported.
CONTRAINDICATIONS
Porphyria, pregnancy, breast-feeding and active liver disease. (Female
patients taking Simvastatin should be counselled to have adequate
contraception during and at least 1 month after discontinuing treatment).
Hypersensitivity to any component of this preparation.
DRUG INTERACTIONS
Increased risk of myopathy with clarithromycin, erythromycin, nefadazone,
itraconazole, ketoconazole, and possibly other imidazoles and triazoles,
cyclosporin, other statins, fibrate and nicotinic acid. Simvastatin enhances
effect of warfarin and nicoumalone.
DOSAGE AND ADMINISTRATION
Hyperlipidaemia: 10 mg daily at night adjusted at intervals of not less than
4 weeks; usual range is 10 to 40 mg daily at night.
Coronary heart disease: Initially 20 mg daily at night.
Renal Insufficiency: If moderate, modification is unnecessary. If severe
with creatinine clearance < 30 mL/min, it is advised to carefully monitor
especially with dosage > 10 mg a day.
Dose Adjustment: If necessary, should be adjusted to a maximum of 40 mg per
day and made at intervals of et least 4 weeks.
SYMPTOMS AND TREATMENT OF OVERDOSAGE
There are few reports on patients with maximum dose of 450 mg, none had
typical symptoms and all recovered. Should adopt general measures.
PHARMACEUTICAL INFORMATION
Storage conditions
Store in a dry place below 30°C.
Protect from light.
Keep medicines out of reach of children.
Shelf Life
Please refer to outer package
Pack sizes/package
Blister packs of 30's, 90's, 100's and 120's. |
