| Acarbose Pharmacology |
| Acarbose |
| About Acarbose |
| Alpha-Glucosidase Inhibitor, Antidiabetic Agent. |
| Mechanism of Action of Acarbose |
| The 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 Acarbose |
| Absorption: 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 Acarbose |
| N/A |
| Duration of Action for Acarbose |
| 2 to 4 hours |
| Half Life of Acarbose |
| About 2 hours |
| Side Effects of Acarbose |
| 1 Flatulence 2.Loose stools 3.Abdominal pain 4.Diarrhoea 5.Elevated serum transaminase levels (rare) |
| Contra-indications of Acarbose |
| 1 Hypersensitivity to the drug 2.Diabetic ketoacidosis 3.Cirrhosis 4.Ulcerative colitis 5.Partial intestinal obstruction 6.Chronic intestinal diseases 7.Hepatic impairment 8.Severe renal impairment 9.History of abdominal surgery 10.Hernia. |
| Special Precautions while taking Acarbose |
| 1.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 Information |
| Contraindicated. |
| Old Age Related Information |
| Use with caution |
| Breast Feeding Related Information |
| Contraindicated. |
| Children Related Information |
| Contraindicated. |
| Indications for Acarbose |
| 1. Non-insulin dependent diabetes mellitus (as adjunct to diet and exercise) |
| Interactions for Acarbose |
| Sucrose: 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 Acarbose |
| Oral: 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 Acarbose |
| H |
| Storage Requirements for Acarbose |
| Store at room temperature below 25 degree C in a well closed container. Protect from moisture. Keep out of reach of children |
| Effects of Missed Dosage of Acarbose |
| 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 Acarbose |
| Provide symptomatic treatment and supportive measures. |
| Acamprosate Pharmacology |
| Acamprosate |
| About Acamprosate |
| Sulfonic Acids and Derivatives, for management of chronic alcoholism (drug depenance) and maintain balance. |
| Mechanism of Action of Acamprosate |
| Acamprosate may interact with glutamate and GABA neurotransmitter systems centrally, and has led to the hypothesis that acamprosate restores the balance. It seems to inhibit NMDA receptors while activating GABA receptors. (Chronic alcohol exposure is hypothesized to alter the normal balance between neuronal excitation and inhibition). |
| Pharmacokinets of Acamprosate |
| Absorptiom: Absorbed after oral administration Distribution: Volume of distribution estimated to be 72 to 109 L (1 L/kg). Protein binding is negligible. Metabolism: Acamprosate does not undergo metabolism. Excretion: Major route of excretion is via kidneys. |
| Onset of Action for Acamprosate |
| N/A |
| Duration of Action for Acamprosate |
| N/A |
| Half Life of Acamprosate |
| 20 – 33 hours |
| Side Effects of Acamprosate |
| 1.Nausea 2.Vomiting 3.Abdominal pain 4.Hypertension 5.Cough 6.Headaches 7.Insomnia 8.Impotence |
| Contra-indications of Acamprosate |
| Hypersensitivity to drug. Severe renal impairment. |
| Special Precautions while taking Acamprosate |
| 1.Mild to moderate renal impairment 2.Suicidal ideation or behavior 3.Elderly patients 4.Breastfeeding patients 5.Children. |
| Pregnancy Related Information |
| Contraindicated |
| Old Age Related Information |
| Use with caution |
| Breast Feeding Related Information |
| Contraindicated |
| Children Related Information |
| Contraindicated |
| Indications for Acamprosate |
| To maintain abstinence from alcohol in patients with alcohol dependence who are abstinent when treatment begins. |
| Interactions for Acamprosate |
| Antidepressants : Weight gain and loss reported more frequently compared with either agent alone. Naltrexone: Acamprosate levels may be increased; however, no dosage adjustment is recommended. |
| Typical Dosage for Acamprosate |
| Adults: PO Two 333 mg tablets 3 times daily. |
| Schedule of Acamprosate |
| N/A |
| Storage Requirements for Acamprosate |
| Store tablets at controlled room temperature (59? to 86?F). Keep out of the reach of children. |
| Effects of Missed Dosage of Acamprosate |
| N/A |
| Effects of Overdose of Acamprosate |
| N/A |