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- Pharmacology For Acarbose + Metformin
Acarbose + Metformin Pharmacology
Acarbose + MetforminAbout Acarbose + MetforminN/AMechanism of Action of Acarbose + MetforminN/APharmacokinets of Acarbose + MetforminN/AOnset of Action for Acarbose + MetforminN/ADuration of Action for Acarbose + MetforminN/AHalf Life of Acarbose + MetforminN/ASide Effects of Acarbose + MetforminN/AContra-indications of Acarbose + MetforminN/ASpecial Precautions while taking Acarbose + MetforminN/APregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationContraindicatedIndications for Acarbose + MetforminType II diabetes mellitusInteractions for Acarbose + MetforminN/ATypical Dosage for Acarbose + MetforminN/ASchedule of Acarbose + MetforminN/AStorage Requirements for Acarbose + MetforminN/AEffects of Missed Dosage of Acarbose + MetforminN/AEffects of Overdose of Acarbose + MetforminN/A
AcarboseAbout AcarboseAlpha-Glucosidase Inhibitor, Antidiabetic Agent.Mechanism of Action of AcarboseThe drug exerts it`s antihyperglycaemic action by causing reversible competitive inhibition of pancreatic alpha-amylase and membrane bound intestinal alpha-glucosidase hydrolase enzymes; which are the final enzymes in the carbohydrate digestion in the brush border of small intestinal mucosa. It reduces digestion and absorption of polysaccharides and sucrose, lowers HbA1c, body weight and serum triglyceride levels. It delays and reduces glucose absorption and lowers postprandial hyperglycaemia.
Pharmacokinets of AcarboseAbsorption: Less than 2%absorbed orally, Distribution: It acts locally within the gastrointestinal tract, Metabolism: Exclusively metabolized within the gastrointestinal tract mainly by intestinal bacteria and to a little extend by digestive enzymes. Excretion: Excreted mainly through faeces as unabsorbed drug; and the fraction absorbed (less than 2%) is excreted through urine.Onset of Action for AcarboseN/ADuration of Action for Acarbose2 to 4 hoursHalf Life of AcarboseAbout 2 hoursSide Effects of Acarbose1 Flatulence
5.Elevated serum transaminase levels (rare)
Contra-indications of Acarbose1 Hypersensitivity to the drug
5.Partial intestinal obstruction
6.Chronic intestinal diseases
8.Severe renal impairment
9.History of abdominal surgery
Special Precautions while taking Acarbose1.Mild to moderate renal impairment
2.Monitor hepatic function tests during therapy
3.Enhance hypoglycaemic effects of sulfonylureas. Give glucose in such situations.
Pregnancy Related InformationContraindicated.Old Age Related InformationUse with cautionBreast Feeding Related InformationContraindicated.Children Related InformationContraindicated.Indications for Acarbose1. Non-insulin dependent diabetes mellitus (as adjunct to diet and exercise)Interactions for AcarboseSucrose: Abdominal discomfort or diarrhoea.
Digestive enzymes (amylase, pancreatin) and intestinal adsorbents (charcoal): Reduce efficacy of acarbose.
Sulphonylureas, biguanides: Acarbose increases their efficacy.
Insulin: In IDDM, insulin requirement is reduced.
Typical Dosage for AcarboseOral: Start with 25mg thrice daily with the 1st bite of each main meal. Increased to 50mg thrice daily; at 4 to 8 week intervals based on 1st hour postprandial glucose levels and tolerance. Then increased to 100mg thrice daily if required.
Maintenance dosage: 50mg to 100mg thrice daily; depending up on the patient`s weight.
Maximum dose: 200mg thrice daily.
Schedule of AcarboseHStorage Requirements for AcarboseStore at room temperature below 25 degree C in a well closed container. Protect from moisture. Keep out of reach of childrenEffects of Missed Dosage of AcarboseTake 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 AcarboseProvide symptomatic treatment and supportive measures.
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.
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