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- Pharmacology For Rosiglitazone + Glimepiride
Rosiglitazone + Glimepiride Pharmacology
Rosiglitazone + GlimepirideAbout Rosiglitazone + GlimepirideN/AMechanism of Action of Rosiglitazone + GlimepirideN/APharmacokinets of Rosiglitazone + GlimepirideN/AOnset of Action for Rosiglitazone + GlimepirideN/ADuration of Action for Rosiglitazone + GlimepirideN/AHalf Life of Rosiglitazone + GlimepirideN/ASide Effects of Rosiglitazone + GlimepirideN/AContra-indications of Rosiglitazone + GlimepirideN/ASpecial Precautions while taking Rosiglitazone + GlimepirideN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Rosiglitazone + GlimepirideN/AInteractions for Rosiglitazone + GlimepirideN/ATypical Dosage for Rosiglitazone + GlimepirideN/ASchedule of Rosiglitazone + GlimepirideN/AStorage Requirements for Rosiglitazone + GlimepirideN/AEffects of Missed Dosage of Rosiglitazone + GlimepirideN/AEffects of Overdose of Rosiglitazone + GlimepirideN/A
RosiglitazoneAbout RosiglitazoneThiazolidinedione derivative, Oral anti-diabetic.Mechanism of Action of RosiglitazoneThe drug exerts antidiabetic action by acting as a selective agonist for the nuclear "peroxisome proliferator-activated receptor Gama (PPAR Gama); which enhances the transcription of several insulin responsive genes. It reverses insulin resistance by stimulating GLUT4 (glucose transporter 4) expression and translocation and improves entry of glucose in to muscle and adipose tissue. It also suppresses hepatic gluconeogenesis. Activation of genes regulating fatty acid metabolism and lipogenesis in adipose tissue also contributes to the insulin sensitizing action of drug. It reduces blood glucose and HbA1c; improves glycaemic control and lowers circulating levels of Insulin.
Pharmacokinets of RosiglitazoneAbsorption: Well absorbed orally and bioavailability is about 99%, Distribution: Widely distributed in a highly protein bound form, Metabolism: Extensively metabolized in the body. Primarily metabolized through N-demethylation and hydroxylation; with subsequent conjugation, Excretion: Excreted mainly through urine (64%) and rest is excreted through faeces.Onset of Action for RosiglitazoneN/ADuration of Action for Rosiglitazone12 to 24 hoursHalf Life of Rosiglitazone3 to 4 hoursSide Effects of Rosiglitazone1. Oedema
2. Plasma volume expansion
3. Weight gain
6. Mild anaemia
7. Back pain
Contra-indications of Rosiglitazone1. Hypersensitivity to the drug
2. Hepatic impairment
3. Cogestive heart failure
4. Patients with moderately severe to severe cardiac disease (New York Heart Association class III and class IV cardiac diseases)
5. Incresed liver enzyme levels(ALT level greater than 2. 5 times than normal)
6. Type 1 diabetes mellitus
7. Diabetic ketoacidosis.
Special Precautions while taking Rosiglitazone1.Cardiac diseases
2.AlcoholicsPregnancy Related InformationContraindicatedOld Age Related InformationMay be usedBreast Feeding Related InformationContraindicatedChildren Related InformationContraindicatedIndications for Rosiglitazone1. Non-insulin dependent diabetes mellitus (as adjunct to diet and exercise)Interactions for RosiglitazoneMetformin: The pharmacokinetics of rosiglitazone was not altered following its concurrent administration in healthy volunteers.
Acarbose: Coadministration had no clinically relevant effect on the pharmacokinetics of rosiglitazone.Typical Dosage for RosiglitazoneOral: Starts with 4mg once daily in the morning or as two divided doses in the morning and evening. Increases the dose to 8mg once daily or as two divided doses; If fasting glucose levels does not improves after 12 weeks. Schedule of RosiglitazoneN/AStorage Requirements for RosiglitazoneStore at controlled room temperature at a range of 15 to 30 degree C.; in a well closed container. Protect from moisture. Keep out of reach of children.Effects of Missed Dosage of RosiglitazoneTake the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.Effects of Overdose of RosiglitazoneProvide symptomatic treatment and supportive measures.
GlimepirideAbout GlimepirideThird-generation sulfonylurea, Oral Antidiabetic Agent.Mechanism of Action of GlimepirideIt is a potent antidiabetic drug which exerts its action by increasing insulin release from the pancreas and by improving glucose tolerance. It acts on the "sulfonylurea receptors" on pancreatic ?-cell membrane and reduces conductance of ATP sensitive K+ channels and thus causes depolarization. This enhances Ca2+ influx and degranultion and thus increases insulin secretion rate at any glucose concentration. It primarily increases 2nd phase insulin secretion and has little effect on 1st phase. It also slows hepatic degradation of insulin and minor action of reducing glucagon release and increasing Somatostatin release. It also exerts stronger extrapancreatic action; by sensitizing the target tissues such as liver to insulin action. It increases the number of insulin receptors and through a post receptor action improving translation of receptor activation.Pharmacokinets of GlimepirideAbsorption: Well absorbed orally
Distribution: Distributed in a highly protein bound form
Metabolism: Completely metabolized in to inactive metabolites in liver
Excretion: Excreted mainly through urine and also through faeces as metabolites.
Onset of Action for GlimepirideN/ADuration of Action for Glimepiride>24 hoursHalf Life of Glimepiride5 to 7 hoursSide Effects of Glimepiride1. Hypoglycemia
8. Hypersensitivity reactions
12. Transient leucopenia
14.Temporary visual impairment
Contra-indications of Glimepiride1. Hypersensitivity to the drug
2. Diabetic ketoacidosis
3. Diabetic coma
4. Juvenile diabetes mellitus
Special Precautions while taking Glimepiride1. Malnourished and deliberate individuals
2. Strenous exercise and irregular meals may leads to hypoglycemia
3. Hepatic impairment
4. Renal impairment
5. Monitor glucose levels during therapy
6. Adrenal insufficiency
7. Pituitary insufficiency
8. Any work requiring mental alertness such as operating a vehicle or machine
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationContraindicatedIndications for Glimepiride1. Non insulin dependent diabetes mellitus.Interactions for GlimepirideHypoglycaemic effect of glimepiride is enhanced by : Anticoagulants, Androgens, Chloramphenicol, Clofibrate, Fenfluramine, Fluconazole, Gemfibrozil, Histamine H2 anta-gonists, Magnesium Salts, Methyldopa, MAOIs, Phenylbutazone, Probenecid, Salicylates, Sulfinpyrazone, Sulfonamides, TCAs, & Urinary acidifiers.
Hypoglycemic effect of glimepiride inhibited by the following drugs : Beta-blockers, Cholestyramine, Diazoxide, Hydantoins, Rifampicin, Thiazide diuretics & Urinary alkalisers.
Charcoal : Reduces the absorption of glimepiride thus reducing its efficacy or toxicity.
Digitalis glycosides : Coadministration results in increased digitalis serum levels.
Typical Dosage for GlimepirideOral: Starts with 1mg daily; immediately before 1st main meals. Adjust the dosage by increments of 1to 2mg at 1 to 2week intervals based on patients response up to 6mg/day as required.
Maintenance dosage: 1 to 4mg once daily
Maximum dose: 8mg once daily
Schedule of GlimepirideN/AStorage Requirements for GlimepirideStore at room temperature at a range of 15 to 30 degree C. in a well closed container away from light. Protect from excess heat and moisture. Keep out of reach of children.Effects of Missed Dosage of GlimepirideTake the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.Effects of Overdose of GlimepirideMild hypoglycemia can be treated with oral glucose and dosage adjustment. It there is loss of consciousness or neurological findings the patient should receive rapid injection of dextrose 50%; followed by continuous infusion of dextrose 10% at a rate to maintain blood glucose levels greater than 100mg/dl. Monitor patient for 24 to 48 hours.
Home Delivery for Rosiglitazone + Glimepiride in Your City
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Rosiglitazone + Glimepiride is a generic medicine name and there are several brands available for it. Some of the brands for rosiglitazone + glimepiride might be better known than rosiglitazone + glimepiride itself. If the pharmacy that's willing to deliver medicines to your home doesn't have rosiglitazone + glimepiride in stock, you can ask for one of the branded alternatives for rosiglitazone + glimepiride.