Acarbose C₂₅H₄₃NO₁₈

Indication

It is primarily indicated for treating Diabetes Mellitus type 2, used in combination with other line agents.

Mechanism of Action

Acarbose is known to be pseudotetrasacchride that inhibits absorption of glucose by delayed ingestion by inhibiting the pancreatic aplha amylase enzyme and alpha glucosidase enzyme present in the brush border of the intestine which prevents the breakdown of complex carbohydrates into monosacchride and starch

Dosage

Strength: 100mg

Form: tablet

Dosing interval: 8 Hr

Maximum Dose: Research suggests that the maximum dose given to an individual of 60kg or less should be 50 mg (8-hourly) and above 60kg should be 100mg (8-hourly)

Dialyzable:Data not available, so not recommended or monitor with care.

Maintainance dose

It is suggested to start the dose with 25mg three times a day and can be increased upto 50-100mg three times a day depending upon tolerance and glucose levels (HbA1C, random and fasting blood glucose test)

Hepatic Adjustment

It is suggested to obtain transaminase level before initiation in liver insufficiency to prevent worsened conditions.

Renal Adjustment

It is advised to take cautiously when serum creatinine levels are less than 2mg/dl

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  Pregnancy

  Can be used but doctor consultation is important before use, as human and animal research is insufficient or animals showed defects and human research hasn?t been conducted.
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  Lactation

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

ContraIndication

Pharmacokinetics

Time of onset: 1 Hr

T_max: 0.32 Litres per kg

Bioavailability: less than 2%

Protein Binding : It is known to be greater than 99% as per reported data.

Elimination Half Life (t_1/2): 2 Hr

Metabolism: By digestive system as per researches.

Volume of Distribution (V_d): 0.32 Litres per kg

Metabolites:

4-Methylpyrgallol derivatives as inactive metabolite