DYNA-BEZAFIBRATE SR 400 mg - Pharma Dynamics

SCHEDULING STATUS:
S3
DYNA-BEZAFIBRATE SR 400 mg
PROPRIETARY NAME AND DOSAGE FORM:
DYNA-BEZAFIBRATE SR 400 mg slow release tablets
COMPOSITION:
Each slow release tablet contains 400 mg of bezafibrate.
PHARMACOLOGICAL CLASSIFICATION:
A 7.5 Serum-cholesterol reducers.
PHARMACOLOGICAL ACTION:
DYNA-BEZAFIBRATE SR 400 mg lowers elevated blood lipids (triglycerides and
cholesterol). DYNA-BEZAFIBRATE SR 400 mg lowers VLDL (very low density
lipoproteins) and LDL (low density lipoproteins) and modestly raises HDL (high density
lipoproteins) levels. Bezafibrate increases the lipoprotein lipase activity.
DYNA-BEZAFIBRATE SR 400 mg has a significant ability to reduce platelet reactivity
and aggregation.
Pharmacokinetics:
DYNA-BEZAFIBRATE SR 400 mg is readily absorbed from the gastrointestinal tract.
Plasma protein binding is about 95%. The plasma elimination half-life is about 2 hours.
Most of a dose is excreted in the urine, about half as unchanged drug, the remainder as
metabolites including the glucuronide conjugate. A small proportion of the dose appears
in the faeces.
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INDICATIONS:
DYNA-BEZAFIBRATE SR 400 mg is indicated for use in patients with primary
hyperlipidaemia type IIa, IIb and IV. (see table below)
Table: Classification of hyperlipoproteinaemias:
This method, devised by Fredrickson, was adapted by the WHO.
The WHO classification defines 6 types.
WHO
classification
Lipoproteins
elevated
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Plasma lipids affected
Cholesterol Triglyceride
I Chylomicrons Normal or elevated Elevated
IIa LDL Elevated Normal
IIb LDL and VLDL Elevated Elevated
III VLDL with
Abnormally high
Cholesterol content
Elevated Elevated
IV VLDL Normal or elevated Elevated
V Chylomicrons and VLDL Elevated Elevated
CONTRA-INDICATIONS:
Hypersensitivity to bezafibrate. Bezafibrate should not be given to patients with severe
liver or kidney dysfunction, primary biliary cirrhosis, or gallstones or gallbladder
disorders. Caution has also been advised in patients with hypoalbuminaemic states
such as nephrotic syndrome. In patients taking oral anticoagulant therapy, the dose of
anticoagulant should be reduced by up to 50% and then adjusted as necessary. A
number of other drugs may be displaced from plasma proteins by Bezafibrate, including
tolbutamide and other sulphonylurea anti-diabetic agents, phenytoin and, in patients with
hypoalbuminaemia, furosemide. The interaction with antidiabetic agents is complex
since bezafibrate has been shown to alter glucose tolerance in both diabetic and non-
diabetic patients. The dosage of antidiabetic agents may need adjusting during

concomitant bezafibrate therapy. The safety in pregnancy and lactation has not been
established.
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 the doctor. Obese patients should lose weight.
THE DOSE IS GENERALLY 1 (ONE) TABLET TAKEN IN THE EVENING OR AS
DETERMINED BY THE DOCTOR. THE TABLET SHOULD BE SWALLOWED WHOLE,
WITH A LITTLE FLUID, AFTER THE EVENING MEAL.
Treatment with DYNA-BEZAFIBRATE SR 400 mg 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:
Gastrointestinal complaints such as nausea, vomiting, diarrhoea, dyspepsia, flatulence
and abdominal discomfort can occur and generally disappear after 1 to 2 weeks without
having to stop treatment. A few reports of weight gain, headache, dizziness, fatigue or
drowsiness, skin rashes, pruritis, alopecia, impotence, anaemia and leucopenia have
been reported. Occasionally slight abnormalities of liver function test and hepatomegaly
occur.
WARNINGS:
Patients developing muscle pain, tenderness or weakness should stop therapy and
consult their doctor. Elevated creatine phosphokinase concentrations may cause this
syndrome; which occurs particularly in patients with hypoalbuminaemia resulting from
the nephrotic syndrome or other renal impairment. Serum aminotransferase
concentrations may also be raised.
INTERACTIONS:
When DYNA-BEZAFIBRATE SR 400 mg is used concurrently with colestyramine, an
interval of 2 hours should be maintained between taking the two medicaments, since the
absorption of bezafibrate is impaired by colestyramine.
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DYNA-BEZAFIBRATE SR 400 mg may interact with oral coumarin anti-coagulants and
the dosage of these agents may have to be reduced. Readjustments should be made by
means of checks on the blood clotting status.
Bezafibrate may potentiate the action of sulphonylureas and insulin.
MAO-inhibitors with hepatotoxic potential must not be administered together with
bezafibrate.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Symptoms of overdosage include gastric pain, nausea and vomiting.
Treatment consists of dose reduction.
IDENTIFICATION:
White, round, bi-convex tablet.
PRESENTATION:
White polypropylene securitainer with a white polyethylene snap-on cap containing 30
tablets.
STORAGE INSTRUCTIONS:
Store below 25°C.
KEEP OUT OF REACH OF CHILDREN.
REGISTRATION NUMBER:
36/7.5/0280
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NAME AND BUSINESS ADDRESS OF APPLICANT:
Marketed by Pharma Dynamics (Pty) Ltd for:
CompuPharm (Pty) Ltd
476 Kings Highway
Lynnwood
Pretoria
DATE AND PUBLICATION OF THIS PACKAGE INSERT:
29 July 2005
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SKEDULERINGSTATUS:
S3
EIENDOMSNAAM EN DOSEERVORM:
DYNA-BEZAFIBRATE SR 400 mg
DYNA-BEZAFIBRATE SR 400 mg stadige-vrystelling tablette
SAMESTELLING:
Elke stadige-vrystelling tablet bevat 400 mg besafibraat.
FARMAKOLOGIESE KLASSIFISERING:
A 7.5 Serumcholesterolverlagende middels.
FARMAKOLOGIESE WERKING:
DYNA-BEZAFIBRATE SR 400 mg verlaag verhoogde bloedlipiede (trigliseriede en
cholesterol). DYNA-BEZAFIBRATE SR 400 mg verlaag VLDL (baie-lae-densiteit-
lipoproteïene) en LDL (lae-densiteit-lipoproteïene) en veroorsaak 'n matige verhoging in
HDL-(hoë-densiteit-lipoproteïene) vlakke. Besafibraat verhoog die aktiwiteit van
lipoproteïenlipase.
DYNA-BEZAFIBRATE SR 400 mg besit 'n beduidende vermoë om plaatjie-reaktiwiteit
en - aggregasie te verminder.
Farmakokinetika:
DYNA-BEZAFIBRATE SR 400 mg word maklik uit die spysverteringskanaal
geabsorbeer. Plasmaproteïenbinding is ongeveer 95%. Die plasma-eliminasie halfleeftyd
is ongeveer 2 uur. Die grootste deel van 'n dosis word in die urine uitgeskei, waarvan
ongeveer die helfte onveranderde geneesmiddel, terwyl die res as metaboliete insluitend
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die glukuroniedkonjugaat uitgeskei word. 'n Klein proporsie van die dosis verskyn in die
faeces.
INDIKASIES:
DYNA-BEZAFIBRATE SR 400 mg word aangedui vir gebruik by pasiënte met primêre
hiperlipemie tipe IIa, IIb, en IV (sien Tabel hierna).
Tabel: Klassifisering van hiperlipoproteïenemieë:
Hierdie metode wat deur Frederickson ontwikkel is, is deur die WGO aangepas.
Die WGO-klassifisering definieer 6 tipes
WGO-klassifisering Lipoproteïene wat
verhoog is
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Plasmalipiede wat aangetas word
Cholesterol Trigliseriede
I Chilomikrone Normaal of verhoog Verhoog
IIa LDL Verhoog Normaal
IIb LDL en VLDL Verhoog Verhoog
III VLDL met abnormaal
hoë cholesterolinhoud
Verhoog Verhoog
IV VLDL Normaal of verhoog Verhoog
V Chilomikrone en VLDL Verhoog Verhoog
KONTRA-INDIKASIES:
Hipersensitiwiteit teenoor besafibraat. Besafibraat moet nie vir pasiënte met ernstige
nier- of lewerdisfunksie, primêre biliêre sirrose, of galstene of galblaasversteurings
toegedien word nie. Omsigtigheid word ook by pasiënte met hipoalbuminemiese
toestande, soos die nefrotiese sindroom, aangeraai. By pasiënte wat orale
antikoagulante terapie neem, moet die dosis antikoagulant met soveel as 50%
verminder, en dan soos nodig aangepas word. Verskeie ander geneesmiddels mag uit
plasmaproteïene deur Besafibraat verplaas word, insluitend tolbutamied en ander
sulfonilurea antidiabetiese middels, fenitoïen, en furosemied by pasiënte met

hipoalbuminemie. Die interaksie met antidiabetiese middels is kompleks aangesien daar
aangedui kon word dat besafibraat glukosetoleransie in beide diabetiese en nie-
diabetiese pasiënte verander. Dit mag nodig word om die dosering van antidiabetiese
middels tydens gelyktydige terapie met besafibraat aan te pas. Die veiligheid tydens
swangerskap en laktasie is nie vasgestel nie.
DOSERING EN GEBRUIKSAANWYSINGS:
Die grondslag van behandeling van alle versteurings in lipiedmetabolisme is in die eerste
instansie, dieet. Dit behoort deur die dokter voorgeskryf te word. Vetsugtige pasiënte
behoort gewig te verloor.
DIE DOSIS IS GEWOONLIK 1 (EEN) TABLET WAT IN DIE AAND OF SOOS DEUR DIE
DOKTER BEPAAL, GENEEM MOET WORD. DIE TABLET MOET HEEL, MET 'N
BIETJIE VLOEISTOF, NA AANDETE INGESLUK WORD.
Behandeling met DYNA-BEZAFIBRATE SR 400 mg moet oor die eerste 8 weke van
behandeling gemoniteer word deur bepaling van die trigliseried-, totale cholesterol-, en
HDL-cholesterolvlakke ten minste drie keer. Indien geen beduidende verlaging van
trigliseriede en totale cholesterol bereik word nie, behoort behandeling gestaak te word.
NEWE-EFFEKTE EN SPESIALE VOORSORGMAATREËLS:
Gastroïntestinale klagtes soos naarheid, braking, diarree, dispepsie, winderigheid en
abdominale ongemak kan voorkom en verdwyn gewoonlik na 1 tot 2 weke sonder dat
terapie gestaak moet word nie. 'n Paar berigte van gewigstoename, hoofpyn,
duiseligheid, moegheid of slaperigheid, veluitslae, pruritus, alopesie, impotensie, anemie
en leukopenie is aangemeld. Soms kom effense abnormaliteite by lewerfunksietoeste,
en hepatomegalie voor.
WAARSKUWINGS:
Pasiënte wat spierpyn, -teerheid of -swakheid ontwikkel, behoort terapie te staak en
hulle geneesheer te raadpleeg. Verhoogde kreatienfosfokinasekonsentrasies mag
hierdie sindroom veroorsaak; dit kom veral voor by pasiënte met hipoalbuminemie wat
deur die nefrotiese sindroom of ander nierinkorting veroorsaak word.
Serumkonsentrasies van aminotransferase mag ook verhoog wees.
INTERAKSIES:
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As DYNA-BEZAFIBRATE SR 400 mg saam met cholestiramien gebruik word, moet 'n
tussenpose van 2 uur tussen die neem van die twee medikamente gebruik word,
aangesien die absorpsie van besafibraat deur cholestiramien belemmer word.
DYNA-BEZAFIBRATE SR 400 mg mag met orale kumarien antikoagulante reageer en
dit mag nodig wees om die dosering van hierdie middels te verminder. Aanpassings
moet gedoen word deur monitering van die bloedstollingstatus.
Besafibraat mag die werking van sulfonilureamiddels en insulien versterk.
MAO-inhibeerders met hepatotoksiese potensiaal moet nie saam met besafibraat
toegedien word nie.
BEKENDE SIMPTOME VAN OORDOSERING EN BESONDERHEDE VAN DIE
BEHANDELING DAARVAN:
Simptome van oordosering sluit maagpyn, naarheid en braking in.
Behandeling bestaan uit dosisvermindering.
IDENTIFIKASIE:
Wit, ronde, bikonvekse tablet.
AANBIEDING:
Wit polipropileen veiligheidshouer met 'n wit poliëtileen wip-dop wat 30 tablette bevat.
BERGINGSAANWYSINGS:
Bewaar onder 25 o C.
HOU BUITE BEREIK VAN KINDERS.
REGISTRASIENOMMER:
36/7.5/0280
NAAM EN BESIGHEIDSADRES VAN DIE APPLIKANT:
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Bemark deur Pharma Dynamics (Edms) Bpk vir:
CompuPharm (Edms) Bpk
Kings Highway 476
Lynnwood
Pretoria
DATUM VAN PUBLIKASIE VAN HIERDIE VOUBILJET:
29 Julie 2005
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