Bioavailability after oral administration of 4 and 8 mg of rosiglitazone was 99%. The maximum concentration dianabol dosage in blood is achieved within 1 hour after ingestion. At therapeutic doses, the plasma concentration is proportional to the dose.
Food does not affect the area under the concentration-time curve in plasma of rosiglitazone, although several decreases, increases slightly (1.75 hours) as compared to fasting state. These changes have little or no clinical significance. Increased gastric pH does not affect the absorption of rosiglitazone. Distribution: the volume of distribution -14 l. Contact with the blood supply is very high (~ 99.8%) and is not dependent on age or on the concentration of rosiglitazone. The extent of the entry in connection with the proteins of the main metabolite (para-hydroxy-sulphate) is very high (> 99.99%). Metabolism: undergoes extensive metabolism and unchanged is not excreted from the body. The main metabolic pathway, hydroxylation, lead to the formation of sulfate or glucuronic conjugates. The role of the main metabolite of rosiglitazone in the manifestation of a hypoglycemic action is not fully understood, and it is possible that he also has a hypoglycemic activity.
Excretion: total plasma clearance of rosiglitazone ~ 3 l / h, while the terminal half-life of ~ 3-4 hours. In one double-reception is not cumulated per day. Derived exclusively in modified form, mainly in the urine (3.2 dose) – with a 25% stool. The elimination of metabolites is very slow: a dianabol dosage terminal half-life of ~ 130 hours. In repeated receptions sometimes possible 8-fold accumulation of metabolites in the plasma, particularly para-hydroxy-sulphate.
Special patient groups: sex differences, age does not significantly affect the pharmacokinetics.
Liver damage: at moderate cirrhosis of free drug in 2-3 times higher than in the normal population. Individual differences are significant: the difference in the AUC of free drug can reach 7 times the size.
Renal impairment: the pharmacokinetics of rosiglitazone with impaired renal function does not differ from that in underlying chronic dialysis end-stage renal failure.
Diabetes mellitus type 2:
- as monotherapy after failure of dietetics;
- in combination with metformin in patients with overweight;
- in combination with a sulfonylurea exclusively in patients not undergoing metformin, metformin is contraindicated or which;
- in combination with insulin.
DOSAGE AND ADMINISTRATION
Ingest, while eating or independently of food intake, 1-2 times a day.
The initial dose of 4 mg.
In combination with metformin: initial dose of 4 mg / day, if necessary after 8 weeks of treatment, the dose can be increased to 8 mg / day.
In combination with sulfonylureas: experience in the use of doses higher than 4 mg / day, no.
In combination with insulin: initial dose of 4 mg / day, can be increased to 8 mg / day, if necessary.
Elderly patients administered dianabol dosage the same dose.
When kidney disease: a dose adjustment is not required for mild and moderate renal insufficiency severity, in severe renal insufficiency rosiglitazone is not applicable.
When liver disease: use is contraindicated.
Children’s age: data on the use of the drug to children 18 years of age are not available, the use of rosiglitazone is not recommended.
Data on the use of rosiglitazone during pregnancy and lactation are not available, so the use is contraindicated.
- Hypersensitivity to rosiglitazone or to any other component of the drug;
- heart failure I-IV Art. by NYHA (including history);
- liver disease;
- severe renal impairment;
- pregnancy, breast-feeding;
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