INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo BAYCOL 0,1 Tablet
BAYCOL 0,2 Tablet
BAYCOL 0,3 Tablet

SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):

BAYCOL 0,1 Tablet
BAYCOL 0,2 Tablet
BAYCOL 0,3 Tablet

COMPOSITION:
BAYCOL 0,1:        Each tablet contains 0,1 mg
cerivastatin sodium
BAYCOL 0,2:        Each tablet contains 0,2 mg cerivastatin sodium
BAYCOL 0,3:        Each tablet contains 0,3 mg cerivastatin sodium

PHARMACOLOGICAL CLASSIFICATION:
A 7.5 Serum-cholesterol reducers.

PHARMACOLOGICAL ACTION:
Cerivastatin sodium is a synthetic, pure enantiomeric competitive cholesterol synthesis inhibitor which inhibits the enzyme HMG-CoA reductase (hydroxy-methyl-glutaryl coenzyme A) This enzyme catalyses the rate-determining step in the synthesis of cholesterol, the conversion of HMG-CoA to mevalonic acid. The primary site of action of cerivastatin sodium is the liver. By reducing intracellular cholesterol content, cerivastatin sodium causes secondary up-regulation of the hepatic LDL receptors with increased LDL cholesterol clearance and reduction of both total and LDL cholesterol in the serum. Cerivastatin sodium is readily absorbed from the gastrointestinal tract, reaching maximum plasma concentrations (C
max) 2-3 hours after oral administration. The absolute bioavailability of cerivastatin sodium is about 60%. The pharmacokinetics of cerivastatin sodium are not influenced by concomitant administration of food. Cerivastatin sodium is highly bound to plasma proteins (99,1-99,5%). The drug penetrates only moderately into tissues. No accumulation is observed on repeated administration. With a clearance of about 13 L/hour, cerivastatin sodium can be regarded as a low clearance drug. Cerivastatin sodium is eliminated by cytochrome P450 mediated biotransformation with a plasma elimination half-life of approximately 2-3 hours. Thirty percent of the dose is excreted as metabolites in urine, and 70% via the faeces. Age and gender have no clinically significant effects on the pharmacokinetics of cerivastatin sodium.

INDICATIONS:
Reduction of elevated total and LDL-cholesterol levels in patients with primary hypercholesterolaemia (Types IIA + IIB) who have not responded adequately to an appropriate diet and weight loss.

CONTRA-INDICATIONS:
Known hypersensitivity to any component of BAYCOL. Hepatic impairment or unexplained, persistent elevation in serum transaminases.
Pregnancy, lactation or women of childbearing potential unless adequately protected by non-hormonal contraceptive methods.

WARNINGS:
Liver function
Increases in liver enzymes have occurred during therapy with BAYCOL. It is recommended that liver function tests be performed before treatment begins and periodically thereafter. Attention should be paid to patients who develop increased transaminase levels and therapy should be discontinued if increases in ALT and AST exceed three times the upper limit of normal (ULN). Caution should be exercised when BAYCOL is administered to patients with a history of heavy alcohol ingestion or a past history of liver disease (active liver disease or unexplained transaminase elevations are contra-indications to the use of BAYCOL).
Muscle
Increased creatine phosphokinase (CPK) may occur in patients receiving BAYCOL. Myopathy, associated with marked elevations of CPK ( >10 times the ULN) and/or with diffuse myalgias, muscle tenderness or weakness, has been reported with HMG-CoA reductase inhibitors. Patients should be asked to report promptly muscle pain, tenderness or weakness especially if accompanied by malaise or fever. BAYCOL should be discontinued if markedly elevated CPK levels occur, or if myopathy is diagnosed or suspected. The risk of myopathy is known to increase in those patients receiving HMG-CoA reductase inhibitors who are concomitantly treated with cyclosporin fibric acid derivatives and nicotinic acid. There have been rare cases of renal dysfunction secondary to rhabdomyolysis with drugs of this class. Hence therapy with BAYCOL should be temporarily withheld in any patient experiencing a condition pre-disposing to the development of renal failure secondary to rhabdomyolysis.
Ophthalmological
Nuclear, anterior and posterior subcapsular opacities have been reported in patients treated with BAYCOL. It is recommended that an ophthalmological assessment is performed before initiating treatment and periodically thereafter.

DOSAGE AND DIRECTIONS FOR USE:
Prior to initiating BAYCOL, secondary causes of hypercholesterolaemia should be excluded. Patients should continue on their standard cholesterol-lowering diet during treatment.
Adults
BAYCOL should be taken once a day in the evening (at dinner or bedtime). The initial dose is 0,1 mg once daily. At intervals of at least 4 weeks, the dosage may be increased by increments of 0,1 mg depending on the response. The maximum recommended dose is 0,3 mg once daily. Administration with food does not influence the effect of cerivastatin sodium. A response to BAYCOL is seen within two weeks and the maximum therapeutic response occurs within four weeks. The response is maintained during continuation of therapy.
Elderly patients
There is no clinical evidence to suggest the dosage needs to be different in these patients. Treatment should be initiated at the lower end of the dosage range.
Renal impairment
Dose adjustment is not necessary in patients with renal impairment. Nevertheless, owing to limited clinical experience in this patient group, careful monitoring should be performed, particularly on initiation of treatment and where the creatinine clearance is less than 30 mL/min. A maximum dose of 0,2 mg once daily for patients with moderate to severe renal impairment is recommended.
Children
Owing to an absence of clinical experience, use in children is not recommended.
Concomitant administration
Whilst BAYCOL is effective in lowering total and LDL cholesterol as monotherapy, efficacy may be enhanced when combined with a bile-acid sequestrant (e.g. cholestyramine, see Interactions).

SIDE EFFECTS AND SPECIAL PRECAUTIONS:
Headache, pharyngitis, upper respiratory tract symptoms (including rhinitis, sinusitis, bronchitis, increased cough), flu syndrome, arthralgia, back pain, diarrhoea, nausea, abdominal pain, constipation, flatulence, myalgia, rash, dizziness, vertigo, dyspepsia, asthenia, urinary tract infection, somnolence and insomnia.
Interactions
Bile-acid sequestering agents: BAYCOL should be administered at least one hour after the resin (e.g. cholestyramine) to avoid an interaction due to drug binding to the resin. No clinically significant effects were seen in a range of other interaction studies with drugs commonly prescribed in hypercholesterolaemic patients (e.g. warfarin, digoxin, antacids, cimetidine). Insufficient evidence exists to support the efficacy and safety of BAYCOL in combination with nicotinic acid, fibrates or cyclosporin.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
No specific antidotes to cerivastatin sodium are known. Should overdose occur, treat symptomatically and institute appropriate supportive measures as required.

IDENTIFICATION:
BAYCOL 0,1: Round, biconvex pale yellow film-coated tablets with Bayer cross on one side and 100 on the other side.
BAYCOL 0,2: Round, biconvex light yellow-brown film-coated tablets with a Bayer cross on one side and 200 on the other side.
BAYCOL 0,3: Round, biconvex yellow-brown film-coated tablets with a Bayer cross on one side and 300 on the other side.

PRESENTATION:
Blister packs of 28 tablets.

STORAGE INSTRUCTIONS:
Store below 25°C. Protect from light and moisture.
Store in the manufacturers original container.
Keep out of reach of children.

REGISTRATION NUMBERS:
BAYCOL 0,1:         31/7.5/0604
BAYCOL 0,2..         31/7.5/0605
BAYCOL 0,3:         31/7.5/0606

NAME AND BUSINESS ADDRESS OF THE APPLICANT:
Bayer (Pty) Ltd
27 Wrench Road
1600 ISANDO

DATE OF PUBLICATION OF PACKAGE INSERT:
July 1997

Baycol/O/0/SA6        07D/0699

        Davbar Dbn.
Updated on this site: March 2001

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