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- Pharmacology For Metformin + Glibenclamide
Metformin + Glibenclamide Pharmacology
Metformin + GlibenclamideAbout Metformin + GlibenclamideN/AMechanism of Action of Metformin + GlibenclamideN/APharmacokinets of Metformin + GlibenclamideN/AOnset of Action for Metformin + GlibenclamideN/ADuration of Action for Metformin + GlibenclamideN/AHalf Life of Metformin + GlibenclamideN/ASide Effects of Metformin + GlibenclamideN/AContra-indications of Metformin + GlibenclamideN/ASpecial Precautions while taking Metformin + GlibenclamideN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Metformin + GlibenclamideN/AInteractions for Metformin + GlibenclamideN/ATypical Dosage for Metformin + GlibenclamideN/ASchedule of Metformin + GlibenclamideN/AStorage Requirements for Metformin + GlibenclamideN/AEffects of Missed Dosage of Metformin + GlibenclamideN/AEffects of Overdose of Metformin + GlibenclamideN/A
MetforminAbout MetforminBiguanide derivative, Oral anti-diabetic.Mechanism of Action of MetforminIt is a biguanide which exerts antidiabetic action. The drug suppresses gluconeogenesis in liver and thus suppresses hepatic glucose output. It enhance insulin mediated glucose disposal in muscle and adipose tissue. It enhance GLUT1 (glucose transporter-1) transport from intracellular site to plasma membrane. It also interferes with respiratory chain in mitochondria and promotes peripheral glucose utilization by increasing anaerobic glycolysis. It inhibits intestinal absorption of glucose, other hexose sugars, amino acids and vitamin B12. It also improves lipid profile in type-2 diabetics.Pharmacokinets of MetforminAbsorption: Absorbed orally and bioavailability is about 50% to60%. Distribution: It is distributed in to erythrocytes, Metabolism: Not metabolized in the body, Excretion: Excreted mainly through urine.Onset of Action for MetforminN/ADuration of Action for Metformin6 to 8 hoursHalf Life of Metformin1.5 to 3hoursSide Effects of Metformin1. Abdominal pain
5. Metalic taste
6. Mild diarrhea
8. Small increase in blood lactate
9. Lactic acidosis (rare)
10. Vitamin B12 deficiency
11. Megaloblastic anaemia
Contra-indications of Metformin1. Hypersensitivity to the drug
2. Renal impairment
3. Hepatic impairment
4. Diabetic ketoacidosis
5. Cardiovascular collapse
6. Hypotensive states
7. Respiratory disease
Special Precautions while taking Metformin1. Alcohol intake can precipitate severe lactic acidosis
2. Vitamin B12deficiency
3. In malnourished and deliberate individuals
4. Adrenal insufficiency
5. Pituitary insufficiency.
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationContraindicatedIndications for MetforminNon-insulin dependent diabetes mellitus (as adjunct to diet and exercise).Interactions for MetforminN/ATypical Dosage for MetforminAdults: Initial dose: 250mg twice or thrice daily with meals. Increase gradually at 2 week intervals, if required to a maximum of 3g daily.
Children: Not applicable. Schedule of MetforminGStorage Requirements for MetforminStore at room temperature at a range of 15 to 30 degree C. in a well closed container.Keep out of reach of children.
Effects of Missed Dosage of MetforminTake 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 doseEffects of Overdose of MetforminProvide supportive measures and symptomatic treatment. Remove accumulated drug from the body by haemodialysis.
GlibenclamideAbout GlibenclamideSecond generation sulfonylurea, Oral anti-diabetic.Mechanism of Action of GlibenclamideThe drug exerts it`s 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 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 GlibenclamideAbsorption: Well absorbed orally
Distribution: Distributed in a protein bound form
Metabolism: Completely metabolized in to inactive metabolites in liver
Excretion: Excreted through urine and faeces as metabolites.
Onset of Action for Glibenclamide30 to 60 minutesDuration of Action for Glibenclamide18 to 24 hoursHalf Life of Glibenclamide4 to 6 hoursSide Effects of Glibenclamide1. Hypoglycemia
8. Weight gain
9. Hypersensitivity reactions
13. Transient leucopenia
Contra-indications of Glibenclamide1. Hypersensitivity to the drug
2. Diabetic ketoacidosis
3. Diabetic coma
4. Renal impairment
Special Precautions while taking Glibenclamide1. Hepatic impairment
2. Malnourished and deliberate individuals
3. Strenous exercise and irregular meals may leads to hypoglycemia
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationContraindicatedIndications for Glibenclamide1. Non insulin dependent diabetes mellitus.
Interactions for GlibenclamideHypoglycaemic effect of glibenclamide is enhanced by: Anticoagulants, Androgens, Chloramphenicol, Clofibrate, Fenfluramine, Fluconazole, Gemfibrozil, Histamine H2 antagonists, Magnesium Salts, Methyldopa, MAOIs, Phenylbutazone, Probenecid, Salicylates, Sulfinpyrazone, Sulfonamides, TCAs, & Urinary acidifiers.
Hypoglycemic effect of glibenclamide inhibited by the following drugs: Beta-blockers, Cholestyramine, Diazoxide, Hydantoins, Rifampicin, Thiazide diuretics & Urinary alkalisers.
Charcoal: Reduces the absorption of glibenclamide thus reducing its efficacy or toxicity.
Digitalis glycosides: Co-administration results in increased digitalis serum levels.
Typical Dosage for GlibenclamideOral: Starts with 2.5mg once daily with breakfast. Adjust the dosage by increments of 2.5mg daily.
Maximum dose: 15mg/day
Maintenance dosage: 1.25 to 15mg once daily with breakfast or in divided doses; if gastrointestinal disturbances occur.
Schedule of GlibenclamideGStorage Requirements for GlibenclamideStore at room temperature below 25 degree C.in a well closed container. Protect from light. Keep out of reach of children.Effects of Missed Dosage of GlibenclamideTake 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 GlibenclamideMild hypoglycemia can be treated with oral glucose and dosage adjustment. If 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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