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- Pharmacology For Pioglitazone + Glimepiride
Pioglitazone + Glimepiride Pharmacology
Pioglitazone + GlimepirideAbout Pioglitazone + GlimepirideN/AMechanism of Action of Pioglitazone + GlimepirideN/APharmacokinets of Pioglitazone + GlimepirideN/AOnset of Action for Pioglitazone + GlimepirideN/ADuration of Action for Pioglitazone + GlimepirideN/AHalf Life of Pioglitazone + GlimepirideN/ASide Effects of Pioglitazone + GlimepirideN/AContra-indications of Pioglitazone + GlimepirideN/ASpecial Precautions while taking Pioglitazone + GlimepirideN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Pioglitazone + GlimepirideN/AInteractions for Pioglitazone + GlimepirideN/ATypical Dosage for Pioglitazone + GlimepirideN/ASchedule of Pioglitazone + GlimepirideN/AStorage Requirements for Pioglitazone + GlimepirideN/AEffects of Missed Dosage of Pioglitazone + GlimepirideN/AEffects of Overdose of Pioglitazone + GlimepirideN/A
PioglitazoneAbout PioglitazoneThiazolidinedione (TZD) derivative, Insulin Sensitizer, Oral anti diabetic.Mechanism of Action of PioglitazoneThe 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.
It also raises HDL level and lowers serum triglyceride level without significant change in LDL level.
Pharmacokinets of PioglitazoneAbsorption: Well absorbed orally, Distribution: Widely distributed in a highly protein bound form, Metabolism: Extensively metabolized in the liver in to metabolites; of which 3 metabolites are active. Excretion: Excreted mainly through faeces and rest is excreted through urine.Onset of Action for PioglitazoneN/ADuration of Action for Pioglitazone24 hoursHalf Life of Pioglitazone3 to 5 hoursSide Effects of Pioglitazone1. Oedema
2. Plasma volume expansion
3. Weight gain
6. Mild anaemia
7. Back pain
10. Upper respiratory tract infections
Contra-indications of Pioglitazone1. 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 Pioglitazone1.Cardiac diseases
2.AlcoholicsPregnancy Related InformationContraindicatedOld Age Related InformationMay be usedBreast Feeding Related InformationContraindicated
Children Related InformationContraindicatedIndications for Pioglitazone1. Non-insulin dependent diabetes mellitus (as adjunct to diet and exercise)
Interactions for PioglitazoneN/ATypical Dosage for PioglitazoneOral: Starts with 15 to 30mg once daily; Increase if required based on patient`s response in increments up to 45mg once daily. Schedule of PioglitazoneN/AStorage Requirements for PioglitazoneStore 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 PioglitazoneTake 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 PioglitazoneProvide 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.
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