Metformin + Glibenclamide Pharmacology

Metformin + Glibenclamide

About Metformin + Glibenclamide
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Mechanism of Action of Metformin + Glibenclamide
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Pharmacokinets of Metformin + Glibenclamide
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Onset of Action for Metformin + Glibenclamide
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Duration of Action for Metformin + Glibenclamide
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Half Life of Metformin + Glibenclamide
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Side Effects of Metformin + Glibenclamide
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Contra-indications of Metformin + Glibenclamide
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Special Precautions while taking Metformin + Glibenclamide
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Metformin + Glibenclamide
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Interactions for Metformin + Glibenclamide
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Typical Dosage for Metformin + Glibenclamide
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Schedule of Metformin + Glibenclamide
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Storage Requirements for Metformin + Glibenclamide
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Effects of Missed Dosage of Metformin + Glibenclamide
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Effects of Overdose of Metformin + Glibenclamide
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Metformin

About Metformin
Biguanide derivative, Oral anti-diabetic.
Mechanism of Action of Metformin
It 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 Metformin
Absorption: 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 Metformin
N/A
Duration of Action for Metformin
6 to 8 hours
Half Life of Metformin
1.5 to 3hours
Side Effects of Metformin
1. Abdominal pain
2. Nausea
3. Vomiting
4. Anorexia
5. Metalic taste
6. Mild diarrhea
7. Tiredness
8. Small increase in blood lactate
9. Lactic acidosis (rare)
10. Vitamin B12 deficiency
11. Megaloblastic anaemia
12. Diarrhoea
13. Flatulence
14. Dermatitis
15. Rashes.
Contra-indications of Metformin
1. Hypersensitivity to the drug
2. Renal impairment
3. Hepatic impairment
4. Diabetic ketoacidosis
5. Cardiovascular collapse
6. Hypotensive states
7. Respiratory disease
8. Alcoholics.
Special Precautions while taking Metformin
1. Alcohol intake can precipitate severe lactic acidosis
2. Vitamin B12deficiency
3. In malnourished and deliberate individuals
4. Adrenal insufficiency
5. Pituitary insufficiency.
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Contraindicated
Indications for Metformin
Non-insulin dependent diabetes mellitus (as adjunct to diet and exercise).
Interactions for Metformin
N/A
Typical Dosage for Metformin
Adults: 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 Metformin
G
Storage Requirements for Metformin
Store 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 Metformin
Take 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 Metformin
Provide supportive measures and symptomatic treatment. Remove accumulated drug from the body by haemodialysis.

Glibenclamide

About Glibenclamide
Second generation sulfonylurea, Oral anti-diabetic.
Mechanism of Action of Glibenclamide
The 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 Glibenclamide
Absorption: 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 Glibenclamide
30 to 60 minutes
Duration of Action for Glibenclamide
18 to 24 hours
Half Life of Glibenclamide
4 to 6 hours
Side Effects of Glibenclamide
1. Hypoglycemia
2. Nausea
3. Vomiting
4. Diarrhoea
5. Constipation
6. Headache
7. Presthesia
8. Weight gain
9. Hypersensitivity reactions
10. Rashes
11. Photosensitivity
12. Purpura
13. Transient leucopenia
14. Agranulocytosis
Contra-indications of Glibenclamide
1. Hypersensitivity to the drug
2. Diabetic ketoacidosis
3. Diabetic coma
4. Renal impairment
Special Precautions while taking Glibenclamide
1. Hepatic impairment
2. Malnourished and deliberate individuals
3. Strenous exercise and irregular meals may leads to hypoglycemia
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Contraindicated
Indications for Glibenclamide
1. Non insulin dependent diabetes mellitus.
Interactions for Glibenclamide
Hypoglycaemic 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 Glibenclamide
Oral: 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 Glibenclamide
G
Storage Requirements for Glibenclamide
Store 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 Glibenclamide
Take 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 Glibenclamide
Mild 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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Metformin + Glibenclamide is a generic medicine name and there are several brands available for it. Some of the brands for metformin + glibenclamide might be better known than metformin + glibenclamide itself. If the pharmacy that's willing to deliver medicines to your home doesn't have metformin + glibenclamide in stock, you can ask for one of the branded alternatives for metformin + glibenclamide.