Tolbutamide

Tolbutamide is a sulfonylurea compound. Tolbutamide is oral anti-diabetic agent, acts by increasing pancreatic insulin secretion. Tolbutamide is used in the treatment of non-insulin dependent diabetes. Tolbutamide is recommended when there is great danger of hypoglycemia (in elderly).


Brands
Adult Dose
Dose: 2.38 to 9.52 mg/kg
Single Dose: 6 (5.95)
Frequency: 8 hourly
Route: PO
Instructions: -
Neonatal
Dose:
Single Dose:
Frequency:
Route:
Instructions: Not recommended in this age group
Paedriatic
Dose:
Single Dose:
Frequency:
Route:
Instructions: Not recommended in this age group
Characteristics
Tolbutamide also known as Butamidum. . It is of Synthetic origin and belongs to Sulphonyl Urea. It belongs to Potassium Channel (ATP sensitive) antagonist pharmacological group on the basis of mechanism of action and also classified in Antidiabetic Agent, Sulfonylurea pharmacological group.The Molecular Weight of Tolbutamide is 270.40. Its pKa is 5.3.
Contraindications
Tolbutamide is contraindicated in conditions like Adrenal insufficiency,Thyroid disease,Renal diseases,Hepatic disease,Iddm,Diabetic ketoacidosis.
Effects
The severe or irreversible adverse effects of Tolbutamide, which give rise to further complications include Thrombocytopenia, Hyponatremia, Pancytopenia, Hepatosplenomegaly.Tolbutamide produces potentially life-threatening effects which include Hypoglycemia, Hepatic dysfunction. which are responsible for the discontinuation of Tolbutamide therapy.The signs and symptoms that are produced after the acute overdosage of Tolbutamide include Vomiting.The symptomatic adverse reactions produced by Tolbutamide are more or less tolerable and if they become severe, they can be treated symptomatically, these include Nausea and vomiting, Skin sensitization, Increased intracranial pressure.
Indications
Tolbutamide is primarily indicated in conditions like NIDDM, Softening and dilatation of cervix before mechanical cervical dilatation.
Interactions
Tolbutamide is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAdrenalineChloramphenicolHalf life and serum concentration of tolbutamide is increased when given with chloramphenicol.ChloramphenicolClofibrateClofibrateCyclophosphamideGemfibrozilKetoconazoleMetformin (HCl)MetipranololInfrequent reports of METIPRANOLOL [EYE] increasing the HYPOGLYCAEMIC effect of TOLBUTAMIDEModeratePerindoprilTheoretical potential for Perindopril Erbumine increasing the HYPOGLYCAEMIC effect of TOLBUTAMIDE. ModerateMay need to avoid combinationPhenylbutazone Phenylbutazone Phenytoin (Na)Silver SulphadiazineSulfadimidine Sulfadimidine inhibits the metabolism of Tolbutamide and enhances their action.SulphadiazineSulphinpyrazoneTeniposideConcurrent use may result in potentiation of drug toxicity.TorasemideTolbutamide, and Sitaxsentan are strong CYP2C9 inhibitors, may increase the serum concentration of Torasemide, a CYP2C9 substrate, by decreasing Torasemide metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Torasemide if Tolbutamide, and Sitaxsentan is initiated, discontinued or dose changed.VORICONAZOLETolbutamide may decrease the metabolism and clearance of Voriconazole. Consider alternate therapy or monitor for changes in Voriconazole therapeutic and adverse effects 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
False +ve reaction for Albumin determination
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, patients suffering from Kidney dysfunction, patients suffering from Liver Malfunction, 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 Below 40°C. Protect from Sunlight and Moisture.
Warnings
Tolbutamide should be used with caution in patients with high blood pressure or liver or kidney disease. This medication may make person more prone to sunburn, wear protective clothing and sunscreen. It should be used with extreme caution during pregnancy or lactation. Insulin therapy may be necessary during pregnancy.
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