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Glibenclamide C23H28ClN3O5S

Molecular Weight: 494g/mol
Dissociation Constant: 4.7
Indication

It is primarily indicated for treating Diabetes Mellitus type 2. Orphan (rare medication use): Acute spinal cord injury, stroke and hemorrhage

Mechanism of Action

It increases B cell insulin secretion, receptors and sensitivity. It also decreases the liver production of glucose

Dosage

Strength: 5mg

Form: tablet

Dosing interval: Every 24 hours usually. Administer every 12 hourly for doses less than 10mg

Maximum Dose: 20mg per day

Dialyzable:The medicine is not dialyzable. Hence, suggested to avoid in renal insufficient patients.

Maintainance dose

Studies suggests to start with a dose of 2.5-5mg per day then adjust up to 7.5-12mg per day.

Hepatic Adjustment

It has been suggested to start with 1.25mg of Glibenclamide initially in patients who have a compromised liver functioning as per studies.

Renal Adjustment

It is not suggested in patients with Creatinine Clearence less than 50ml/min: Suggested to be used with caution.

  • pregnant

    Pregnancy

    Doctors consultation is important before use, as human and animal research is insufficient or animals showed defects and human research hasn?t been conducted.

  • mother

    Lactation

    Insufficient data to prove if the drug enters breast milk, hence not recommended.

ContraIndication
Cautions

Should be taken with great care in patients who have renal and kidney dysfunction. Also it is suggested to observe blood levels for anemic conditions that might develop due to 6-phosphate glucose dehydrogenase deficiency conditions. Pregnant and nursing mothers should be closely monitored for altered glucose levels.

Pharmacokinetics

Time of onset: 1 Hr

Tmax: 9.5 Liters

Bioavailability: Variable

Protein Binding : 99%

Elimination Half Life (t1/2): 1.4-1.8 Hr for active drug. Ten hours for metabolites.

Metabolism: Less metabolites formed through extensive liver metabolism

Volume of Distribution (Vd): 9.5 Liters

Metabolites:

Active: 3-cis-hydroxyglyburide

Disclaimer

Dawaai's intention is to make sure that it's consumers get information that is accurate, reviewed by an expert and error-free. However, the information mentioned here should not be used as a replacement for the advice of a qualified physician. The information given here is for informational purposes only, which may not cover all possible precautions, side effects, contraindications or drug interactions. Consult your doctor and discuss your queries related to any medicine or disease.

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