Bezafibrate (Bezalip) is a fibrate drug that reduces the synthesis of triglycerides and cholesterol. It is used as an adjunct to diet and exercise for the treatment of Type IIa and IIb mixed hyperlipidemia. It regulates the lipids and apoprotein levels by reducing serum triglyceride levels, LDL cholesterol levels, apolipoprotein A and B levels, and increases HDL levels. It is used to treat high levels of triglycerides, especially who are at risk of developing complications from dyslipidemias.
Bezafibrate Dose in Adults
Use in th treatment of Dyslipidemia:
- 400 mg orally once a day
Bezafibrate Dose in Childrens
Dose in the treatment of Dyslipidemia:
- Children and Adolescents:
- 10 - 20 mg/kg/day orally to a maximum of 400 mg per day.
Pegnancy Risk Factor: X
- Pregnant women should not use it.
- Women in their reproductive years should stop taking hormone therapy at least six months before conceiving and use effective birth control methods.
- As soon as the pregnancy is confirmed, it is important to stop all treatment.
Bezafibrate use during breastfeeding:
- It is not recommended for use during breastfeeding.
Bezafibrate dose in kidney disease:
- CrCl of more than 60 mL/minute:
- Adjustment in dose is not required.
- CrCl of less than 60 mL/minute or a serum creatinine of more than 1.5 mg/dL [>135 micromol/L]:
- Use is contraindicated
- Dialysis:
- Use is contraindicated.
Bezafibrate Dose in Liver Disease:
- It is contraindicated in hepatic impairment.
Frequency not defined.
- Central Nervous System:
- Headache
- Dizziness
- Insomnia
- Migraine
- Pain
- Dermatologic:
- Pruritus
- Eczema
- Erythema
- Urticaria
- Gastrointestinal:
- Gastritis
- Flatulence
- Dyspepsia
- Constipation
- Diarrhea
- Epigastric Distress
- Nausea
- Hematologic & Oncologic:
- Anemia
- Hepatic:
- Increased Serum ALT
- Increased Serum AST
- Hypersensitivity:
- Hypersensitivity Reaction
- Neuromuscular & Skeletal:
- Increased Creatine Phosphokinase
- Respiratory:
- Bronchitis
- Pharyngitis
Contraindication to Bezafibrate Include:
- Allergies to fibrates, bezafibrate or any other component of the formulation
- Photoallergic reactions to fibrates
- Hepatic impairment
- Primary biliary dysfunction
- Renal impairment is a higher level of creatinine than 1.5 mg/dL (>135 micromol/L), a lower CrCl than 60 mL/minute or patients on dialysis.
- Gallbladder disease that is pre-existing
- Patients at high risk for myopathy may also be taking statins (HMG CoA reductase inhibits).
- Pregnancy and breastfeeding
- Treatment of type I hyperlipoproteinemia is not recommended
Warnings and Precautions
- Hematologic effects
- After therapy is initiated, cytopenias can occur.
- Hepatic effects
- It is hepatotoxic.
- If the target goals are not met within 3 months, treatment should be stopped.
- Patients who have a history of jaundice, liver disease or other hepatic disorders should not use it.
- It may increase the risk for gall stones
- Myopathy and rhabdomyolysis
- Myositis and rhabdomyolysis can occur in patients. Patients should report any unresolved muscle pain, tenderness or brown urine.
- Monitor Creatine phosphokinase levels and discontinue therapy if there is a marked increase in CPK (more than 10 times the normal limit).
Monitoring Parameters:
- Serum lipids
- Cholesterol
- Triglycerides
- LFTs after 3-6 months of therapy and then at least annually
- CBC particularly during the first one year
- Fasting glucose
- Serum creatinine
- CPK (creatine phosphokinase levels)
How to take Bezafibrate?
- It may be taken in the morning or evening with meals.
- The drug should be swallowed whole.
- It should not be crushed or chewed and administered with a sufficient amount of fluid.
Mechanism of action of Bezafibrate:
- Its mechanism of action is unclear. It is believed to increase lipoprotein activity and hepatic triglyceride lipase activities.
- It can also inhibit the enzyme acetylCoA carboxylase, reducing the synthesis of triglycerides.
- It inhibits 3-hydroxy-3-methyl glutaryl coenzyme A reductase, which reduces cholesterol synthesis.
94-96% of the drug isprotein-boundIt is.
It has been ahalf-life eliminationbetween 1 and 2 hours, depending on how long you need.
peak serum concentrationIt takes between 3 and 4 hours.
It isexcretedPrimarily via urine
International Brands of Bezafibrate:
- Bezalip SR
- JAMP-Bezafibrate SR
- PMS-Bezafibrate
- Befibrat
- Befizal
- Bezacur
- Bezafibrat
- Bezalip
- Bezalip PR
- Bezalip Rwetard
- Bezamil
- Bezastad
- Bezatol SR
- Cedur
- Clofibral
- Decrilip
- Difaterol
- Elpilip
- Etifibrat
- Eulip
- Lacromid
- Lipitrol
- Lipocin
- Lipocor
- Nimus
- Norlip
- Oralipin
- Oralipin Retard
- Polyzalip
- Regadrin B
- Zafibral
- Zafular
Bezafibrate brands in Pakistan:
|
Bezafibrate [Tabs 200 mg] |
|
| Benzalip | Roche Pakistan Ltd. |
| Bezalip | Roche Pakistan Ltd. |
| Lipocor | Efroze Chemical Industries (Pvt) Ltd. |