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- Pharmacology For Phenformin + Chlorpropamide
Phenformin + Chlorpropamide Pharmacology
Phenformin + ChlorpropamideAbout Phenformin + ChlorpropamideN/AMechanism of Action of Phenformin + ChlorpropamideN/APharmacokinets of Phenformin + ChlorpropamideN/AOnset of Action for Phenformin + ChlorpropamideN/ADuration of Action for Phenformin + ChlorpropamideN/AHalf Life of Phenformin + ChlorpropamideN/ASide Effects of Phenformin + ChlorpropamideN/AContra-indications of Phenformin + ChlorpropamideN/ASpecial Precautions while taking Phenformin + ChlorpropamideN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Phenformin + ChlorpropamideN/AInteractions for Phenformin + ChlorpropamideN/ATypical Dosage for Phenformin + ChlorpropamideN/ASchedule of Phenformin + ChlorpropamideN/AStorage Requirements for Phenformin + ChlorpropamideN/AEffects of Missed Dosage of Phenformin + ChlorpropamideN/AEffects of Overdose of Phenformin + ChlorpropamideN/A
PhenforminAbout PhenforminBiguanide derivative ,Insulin Sensitizer, Oral Anti-diabetic.Mechanism of Action of PhenforminIt 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.
Pharmacokinets of PhenforminAbsorption: Incompletely but adequately absorbed orally, Excretion: Excreted through faeces and urine.
Onset of Action for PhenforminN/ADuration of Action for Phenformin8 to 12 hoursHalf Life of Phenformin3 to 10 hoursSide Effects of Phenformin1. Abdominal pain
5. Metalic taste
6. Mild diarrhea
8. Lactic acidosis
Contra-indications of Phenformin1. 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 Phenformin1. 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 InformationContraindicated
Indications for Phenformin1.Non insulin dependent diabetes mellitus (as adjunct to diet and exercise)Interactions for PhenforminN/ATypical Dosage for PhenforminOral: 25 to 50mg 1 to 4 times daily; maximum up to 100mg/daySchedule of PhenforminGStorage Requirements for PhenforminStore 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 PhenforminTake 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 PhenforminProvide supportive measures and symptomatic treatment.
ChlorpropamideAbout ChlorpropamideAntidiabetic Agent, Sulfonylurea derivative, Oral hypoglycemic agent for type ? II diabetes.Mechanism of Action of ChlorpropamideThe 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 ChlorpropamideAbsorption: Well absorbed orally, Distribution: Distributed in a protein bound form, Metabolism: About 80% of the drug is metabolized in to metabolites, Excretion: Excreted through urine.Onset of Action for ChlorpropamideWithin 60minutesDuration of Action for Chlorpropamide36 to 48hoursHalf Life of Chlorpropamide30 to 36 hoursSide Effects of Chlorpropamide1.Hypoglycaemia
Contra-indications of Chlorpropamide1.Hypersensitivity to the drug
2.Type1 diabetes mellitus
3.Diabetes that can be adequately controlled by diet
10.Renal impairmentSpecial Precautions while taking Chlorpropamide1.Hepatic impairment
4.Ischaemic vascular disease
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationContraindicatedIndications for Chlorpropamide1.Maturity onset non ketotic diabetes
2.Neurogenic diabetes insipidus.
Interactions for ChlorpropamideAlcohol: Dilsulfiram like reaction - flushing of face and neck region.
Androgens, Anticoagulants, Chloramphenicol, Clofibrate, Fenfluramine, Fluconazole, Gemfibrozil, Histamine H2 antagonists, Magnesium salts, Methyldopa, MAOIs, Phenylbutazone, Probenecid, Salicylates, Sulfinpyrazone, Sulfonamides, TCAs, Urinary acidifiers: Enhance the hypoglycemic effect of chlorpropamide due to various mechanisms.
Beta-Blockers, Cholestyramine, Diazoxide, Hydantoins, Rifampicin, Thiazide diuretics & Urinary alkalizers: Decrease hypoglycemic effect of chlorpropamide due to various mechanisms.
Charcoal: Reduces the absorption of chlorpropamide leading to decrease in efficacy or toxicity.
Digitalis Glycosides: Increase serum levels.Typical Dosage for ChlorpropamideOral: Starts with 100 to 250mg once daily with breakfast or in divided doses; if gastrointestinal disturbances occur. Adjust the dosage by increments of 50 to 125mg daily at every 3 to 5 days.
Maximum dose: 500mg/day
Schedule of ChlorpropamideGStorage Requirements for ChlorpropamideStore at room temperature at a range of 15 to 30 degree C.in a well closed container. Protect from excess heat and moisture. Keep out of reach of children.Effects of Missed Dosage of ChlorpropamideTake 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 ChlorpropamideMild 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 3 to 5 days.
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