Chlorpropamide

Chlorpropamide is oral hypoglycemic agent. Chlorpropamide is used in the treatment of non-insulin dependent diabetes mellitus. Chlorpropamide is used in conjunction with proper diet and exercise to decrease blood sugar levels.


Adult Dose
Dose: 250 mg
Single Dose: 250 (250)
Frequency: 24 hourly
Route: PO
Instructions: With breakfast.
Neonatal
Dose: 125 to 250 mg
Single Dose: 190 (187.5)
Frequency: 24 hourly
Route: For central D.I.
Instructions:
Paedriatic
Dose:
Single Dose:
Frequency:
Route:
Instructions: Not recommended in this age group
Characteristics
chloropropamide, chloropropamide, chloropropamide are the derivatives of Chlorpropamide. It is of Synthetic origin and belongs to Sulfonylurea. It belongs to Potassium Channel (ATP sensitive) antagonist pharmacological group on the basis of mechanism of action and also classified in Drugs Afecting Glucose Metabolism and Antidiabetic Agent, Sulfonylurea pharmacological group.The Molecular Weight of Chlorpropamide is 277.00. Its pKa is 5.0.
Contraindications
Chlorpropamide is contraindicated in conditions like Iddm,Ketosis,Congestive heart failure,Gestational diabetes mellitus,Renal impairment,Hepatic impairment.
Effects
The severe or irreversible adverse effects of Chlorpropamide, which give rise to further complications include Thrombocytopenia, Cholestatic jaundice, Aplastic anemia, Hemolytic anemia, Cholestatic jaundice, Aplastic anemia, Hemolytic anemia, Fictitious hypoglycemia, Agranulocytosis, Exfoliative dermatitis, Eosinophilic pulmonary infiltrates, Hemolytic anemia, Aplastic anemia.Chlorpropamide produces potentially life-threatening effects which include Hypoglycemia, Hypoglycemia, Hypoglycemia. which are responsible for the discontinuation of Chlorpropamide therapy.The signs and symptoms that are produced after the acute overdosage of Chlorpropamide include Coma, Seizures, Hypothermia, Hypoglycemia.The symptomatic adverse reactions produced by Chlorpropamide are more or less tolerable and if they become severe, they can be treated symptomatically, these include Headache, Diarrhea, Abdominal pain, Dyspepsia, Facial flushing, Hyponatremia, dyspepsia.
Indications
Chlorpropamide is primarily indicated in conditions like Diabetes insipidus, Diabetes mellitus, Diabetes mellitus type-ii, and can also be given in adjunctive therapy as an alternative drug of choice in Softening and dilatation of cervix before mechanical cervical dilatation.
Interactions
Chlorpropamide is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAlcoholAllopurinolAllopurinol reduces the renal excretion and prolong the half-life of chlorpropamide.MinorMonitor blood sugar of patient regularly.Amiloride (HCl)CarbamazepineChloramphenicolChloramphenicol reduces the hepatic clearence of chlorpropamide or displaces it from binding siteresult in increase plasma concentration of chlorpropamide which may lead to enhanced hypoglycemic effect.ModerateClosely monitor for level of glucose whenever start or discontinuetherapy with chloramphenicol.Adjust the dose of chlorpropamide if necessary.Cimetidine (HCl)Cimetidine inhibit the hepatic metabolism of chlorpropamide or increase its absorption by altering gastric pH results in increased plasma concentration may lead to enhanced hypoglycemic effect.ModerateClosely monitor blood sugar regularly. Reduce the dose of chlorpropamide if necessary.ClofibrateDesmopressin (Acetate)FluconazoleFluconazole decrease chlorpropamide clearance by inhibiting CYP450 3A4 thus increases its plasma concentration that leads to marked hypoglycemia. ModerateRegular checking of blood glucose level and chlorpropamide dose adjustment is required when given with fluconazole.LypressinMagnesium Oxides and HydroxidesMethyltestosteroneThe hypoglycemic effect of insulin secretagogues (e.g., sulfonylureas, meglitinides) may be potentiated by certain drugs, including ACE inhibitors, anabolic steroids, fibrates, monoamine oxidase inhibitors (MAOIs), nonsteroidal anti-inflammatory drugs (NSAIDs), salicylates, selective serotonin reuptake inhibitors (SSRIs), sulfonamides, disopyramide, propoxyphene, quinine, and quinidine. These drugs may increase the risk of hypoglycemia by enhancing insulin sensitivity (ACE inhibitors, fibrates); stimulating insulin secretion (salicylates, NSAIDs, disopyramide, quinine, quinidine, MAOIs); increasing peripheral glucose utilization (SSRIs, insulin-like growth factor); and/or inhibiting gluconeogenesis (SSRIs, MAOIs, insulin-like growth factor). Or, they may increase plasma concentration of insulin secretagogues by displacing them from plasma protein binding sites and/or inhibiting their metabolism (fibrates, NSAIDs, salicylates, sulfonamides). Clinical hypoglycemia has been reported during use of these agents alone or with insulin and/or sulfonylureas. Use of SSRIs has also been associated with loss of awareness of hypoglycemia in isolated cases.ModerateClose monitoring for the development of hypoglycemia is recommended if these drugs are coadministered with insulin secretagogues, particularly in patients with advanced age and/or renal impairment. The oral antidiabetic dosage(s) may require adjustment if an interaction is suspected. Patients should be apprised of the signs and symptoms of hypoglycemia (e.g., headache, dizziness, drowsiness, nausea, hunger, tremor, weakness, sweating, palpitations), how to treat it, and to contact their doctor if it occurs. Patients should be observed for loss of glycemic control when these drugs are withdrawn.MetipranololInfrequent reports of METIPRANOLOL [EYE] increasing the HYPOGLYCAEMIC effect of CHLORPROPAMIDE. ModerateMiconazole (Nitrate)PerindoprilTheoretical potential for Perindopril Erbumine increasing the HYPOGLYCAEMIC effect of CHLORPROPAMIDE.ModerateMay need to avoid combinationPhenelzinePhenelzine inhibits gluconeogenesis thus potentiate the hypoglycemic effect of chlorpropamide.ModerateAdjust the dose of chlorpropamide if necessary. Closely monitor the blood sugar level especially in patients of advance age or renal impairent.PhenobarbitonePhenylbutazone Phenylbutazone inhibit the metabolism and renal clearence of chlorpropamide and displace it from plasma protein binding site thus potentiate the hypoglycaemic effect.ModerateMonitor blood sugar regularly. Closely monitor for increased hypoglycemic effect. Reduce the dose of chlorpropamide if necessary.Phenytoin (Na)Phenytoin cause hyperlycemia, hypoinsulinemia and glucose intolerance and thus diminishes the hypoglycemic effect of chlorpropamide.While chlorpropamide inhibits the metabolism of phenytoin thus increases its plasma concentration and pharmacological effects.ModerateClosely monitor the level of phenytoin and blood glucose. Patient should notify to physician if experience the symptoms of phenytoin toxiity.ProbenecidProbenecid stimulate the secretion of insulin thus potentiate the hypoglycemic effect of chlorpropamide.ModerateClosely monitor the blood glucose level especially in patients of advanced age or renall impairment. Adjust the dose of chlorpropamide if necessary.Patient should notify to physician if experince the signs of hypoglycemia.Propranolol (HCl)Propranolol inhibits the insulin secretion and hepatic glycogenolysis thus potentiate the hypoglycemic effect of chlorpropamide.ModerateClosely monitor the level of blood glucose regularly.RifampicinSalicylic AcidSodium AcetateAlkalinization of the urine may increase the renal clearance of some sulfonylureas for which renal elimination is pH dependent. The clinical significance of this interaction is unknown. Management consists of monitoring blood glucose frequently during the initial period of coadministration. The sulfonylurea dosage should be adjusted as needed and appropriate.MinorThe sulfonylurea dosage should be adjusted as needed and appropriate.Sodium CitrateSodium Citrate may increase the excretion and decrease the serum levels of Chlorpropamide, possibly decreasing their pharmacologic effects.SulphadiazineTranylcypromine (Sulphate)Tranylcypromine stimulate the secretion of insulin thus potentiate the hypoglycemic effect of chlorpropamide.ModerateClosely monitor for blood glucose level especially in patient with advanced age and renal impairement.VasopressinVORICONAZOLEAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongationWarfarin (Na)Chlorpropamide either enhance or reduce the hypoprothrombinemic effect of warfarin by displacing it from plasma protein binding site. Warfarin also increase the blood level of chlorpropamide by inhibiting hepatic metabolism.ModerateProthrombin time, INR and blood sugar level should be monitor frequently. Patient should report the sign of bleeding to physician. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, Geriatrics, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Tab Store in a well closed container, Below 40°C.
Warnings
Chlorpropamide should be used with caution in patients with medical history, especially if have high blood pressure or liver or kidney disease. Avoid alcohol while taking this medication. Photosensitization may occur, caution patients to take appropriate measure (e.g.wear protective clothing and a sunscreen) against exposure to UV or sunlight. It should be used in pregnancy or lactation only if clearly needed. Insulin therapy may be necessary during pregnancy.
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