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Rosiglitazone C18H19N3O3S

Molecular Weight: 357g/mol
Dissociation Constant: 5.78
Indication

Indicated for treating Diabetes Mellitus type 2.

Mechanism of Action

It is known to activate the perioxisomes-activated receptors gamma (PARR(gamma)) which utilizes the peripheral glucose and lipid metabolism present in the peripheral tissues.

Dosage

Strength: 4mg

Form: tablet

Dosing interval: 12 Hr

Maximum Dose: 8mg per day

Dialyzable:It is not dialysable as per reported data.

Maintainance dose

It is mentioned to initiate with a dose of 4mg twice daily, if found inappropriate then increase upto 8mg once daily

Hepatic Adjustment

Monitor closely liver ALT levels (ALT greater than 2.5 x ULN) don?t initate rosiglitazone (Monitor ALT levels ever month for one year, then every three months thereafter). Sulfonylurea dose need to be adjusted when coadministered.

Renal Adjustment

Study suggests to continue giving prescribed doses as no renal adjustments are required in patients with kidney impairments.

  • pregnant

    Pregnancy

    Doctor 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 efficacy for nursing mothers hence, found to be unsafe.

ContraIndication
Cautions

BLACK BOX WARNING: Pioglitazone and Rosiglitazone are known to cause an exaggeration of cardiovascular cases. It is suggested to be monitored closely with sulfonylureas. Also monitor liver enzyme eg. AST(Aspartate aminotransferase) and ALT (Alanine Aminotransferase) levels before administering.

Pharmacokinetics

Time of onset: Delayed

Tmax: 17.6 Liters

Bioavailability: 99%

Protein Binding : 99.8% to serum albumin

Elimination Half Life (t1/2): 3-4 Hr

Metabolism: The molecule has found to be extensively metabolized by liver

Volume of Distribution (Vd): 17.6 Liters

Metabolites:

Inactive metabolites are usually formed as per studies reported (para, ortho hydroxyrosiglitazone).

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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