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BEZACHOLESR (Film-coated Tablets)
BEZACHOLESR (Film-coated Tablets)
SCHEDULING STATUS:
S3
PROPRIETARY NAME
(and dosage form):
BEZACHOLESR (Film-coated Tablets)
COMPOSITION:
Each slow release tablet contains 400mg of bezafibrate.
PHARMACOLOGICAL CLASSIFICATION:
A 7.5 Serum cholesterol reducers.
PHARMACOLOGICAL ACTION:
Bezafibrate, a fibric acid derivative, lowers triglyceride and low density lipoprotein (LDL) cholesterol; and may raise high density lipoprotein (HDL) cholesterol levels. The effects of bezafibrate on blood lipids are probably mediated by its interaction with peroxisome proliferator-activated receptors (PPARs), which regulate gene transcription. LDL levels remain unchanged or fall, especially when triglyceride levels are not elevated.
Pharmacokinetics:
Absorption from the gastrointestinal tract is virtually complete and there is no pre-systemic metabolism. In a study of 24healthy volunteers the peak levels of the drug in plasma have occurred between 3 and 6hours and the mean plasma half-life was in the order of 6 to 11hours.
More than 95%of bezafibrate in plasma is bound to protein, almost exclusively to albumin.
Bezafibrate is excreted predominantly as glucuronide conjugates; 60% to 90% of an oral dose is excreted in the urine, with smaller amounts appearing in the faeces. Excretion of bezafibrate is impaired in renal failure (see "Warnings and Precautions").
INDICATIONS:
BEZACHOLESR is indicated for the use in patients with increased triglycerides, increased LDL cholesterol or a combination of these who have failed to respond adequately to diet, weight loss and increased physical activity. BEZACHOLESR is also indicated for use with secondary hyperlipoproteinaemias that persist despite the appropriate treatment of the underlying disease (e.g. Diabetes Mellitus)
It has not been firmly established whether the drug-induced lowering of serum cholesterol or lipid levels has detrimental, beneficial or no effect on the morbidity or mortality due to atherosclerosis or coronary heart disease.
CONTRA-INDICATIONS:
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Hypersensitive to BEZACHOLESR or the constituents. |
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Severe hepatic impairment. |
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Primary biliary cirrhosis. |
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Gallstones or gallbladder disorders. |
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Hypoalbuminaemic states such as nephrotic syndrome. |
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Patients undergoing dialysis and with impaired renal function (serum creatinine >1.5mg/100mL i.e. >135micromols/L or creatinine clearance <60mL/min.). |
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Pregnancy and lactation. |
WARNINGS:
BEZACHOLESR should be used with caution in patients with renal impairment (see "Dosage and Directions for Use").
Elevated creatine phosphokinase concentrations during BEZACHOLESR therapy may be associated with a syndrome of myositis, myopathy, and rarely rhabdomyolysis; patients with hypoalbuminaemia resulting from nephrotic syndrome or with renal impairment may be at increased risk.
Patients treated with BEZACHOLESR should consult their doctor if they develop muscle pain, tenderness, or weakness, and treatment should be stopped if muscle toxicity is suspected clinically or if creatine phosphokinase is markedly raised or progressively rising.
Other lipid regulating medicines, particularly the statins, have also been associated with myopathy and the risk of muscle toxicity is increased if BEZACHOLESR and statins are taken together. Combination therapy may be necessary in some patients but careful monitoring is required (see "INTERACTIONS").
BEZACHOLESR may increase the lithogenic index, and there have been reports of gallstones. BEZACHOLESR should not be used by children or pregnant women. (See "Pregnancy and Lactation")
INTERACTIONS:
BEZACHOLESR potentiates the action of warfarin, in part by displacing warfarin from its binding sites on albumin. Careful monitoring at the INR and reduction in dosage of the anticoagulant may be appropriate when treatment with BEZACHOLESR is begun.
A number of other medicines that may be displaced from plasma proteins by BEZACHOLESR include:
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sufionylurea antidiabetics |
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phenytoin |
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furosemide in patients with hypoalbuminaemia |
When BEZACHOLESR is used concurrently with cholestyramine, an interval of 2hours should be maintained between taking the two medicines, since the absorption of BEZACHOLESR is impaired by cholestyramine. The interaction with antidiabetic oral medication is complex since BEZACHOLESR alters glucose tolerance in diabetic and non-diabetic patients. The dosage of oral antidiabetic medication may need adjusting during BEZACHOLESR therapy.
There is an increased risk of myopathy if BEZACHOLESR is used with statins. (See "Warnings and Precautions").
Increased ciclosporin concentrations and associated nephrotoxicity have been reported when taken together with BEZACHOLESR.
PREGNANCY AND LACTATION:
It is recommended that BEZACHOLESR not be administered to pregnant or breast-feeding women (see "Warnings and Precautions").
DOSAGE AND DIRECTIONS FOR USE:
The basis of the treatment of all disorders of lipid metabolism is by diet in the first instance. This should be prescribed by a medical practitioner. Obese patients should lose weight.
The dose is generally one tablet taken in the evening, as determined by the doctor. The tablet should be swallowed whole, with a little fluid, after the evening meal.
The dosage in patient, with renal insufficiency must be adjusted according to serum creatinine levels. Treatment with BEZACHOLESR should be monitored over the first 8 weeks of treatment by determination of the triglyceride, total cholesterol and HDL-cholesterol levels at least three times. If no significant reduction of triglyceride and total cholesterol is obtained, treatment should be discontinued.
SIDE EFFECTS AND SPECIAL PRECAUTIONS:
SIDE EFFECTS:
Gastrointestinal disorders
Frequent: Anorexia, nausea and gastric discomfort.
Nervous system disorders
Less frequent: Headache, dizziness, vertigo, fatigue.
Skin and subcutaneous tissue disorders
Less frequent: Skin rashes, pruritis, photosentivity, alopecia.
Blood and lymphatic disorders
Less frequent: Leucopenia, anaemia, thrombocytopenia, raised serum-aminotransferase concentrations.
Musculoskeletal disorders
The following side-effects have been reported and frequencies are unknown:
Myositis, myopathy and rhabdomyolysis associated with elevated creatine phosphokinase has been reported (see "Warnings and Precautions").
Hepatobiliary disorders
Less frequent: Abnormalities of liver function tests and hepatomegaly, which are apparently not indicative of hepatoxicity, have occasionally been reported. Liver function should be monitored.
Other
Less frequent: Impotence
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Symptoms of overdose include gastric pain, nausea and vomiting. Treatment consists of dose reduction.
IDENTIFICATION:
White, round, bi-convex, film-coated tablets.
PRESENTATION:
A blister made up of an opaque, white PVC foil, coated with PVdC. Blister strips consists of 10 tablets which are packed in cartons of 30 or 100.
STORAGE INSTRUCTIONS:
Store in a dry place below 25ºC. Protect from moisture and light.
KEEP OUT OF REACH OF CHILDREN.
REGISTRATION NUMBER:
36/7.5/0281
NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION:
Pharmacare Limited
Building 12
Healthcare Park
Woodlands Drive
Woodmead
Sandton
2148
DATE OF PUBLICATION OF THIS PACKAGE INSERT:
19 April 2006
308646 020207
Harry's Printers K00000 D07
New addition to this site: February 2010
Source: Pharmaceutical Industry |
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