Tolbutamide: Difference between revisions

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'''Tolbutamide''' is an [[Oral hypoglycemic agent|oral hypoglycemic agent]] used for the treatment of [[Diabetes mellitus type 2|type 2 diabetes]]. It belongs to the [[Sulfonylurea|sulfonylurea]] class of drugs, which are insulin secretagogues. Tolbutamide works by stimulating the release of insulin from the [[Pancreas|pancreas]], thereby lowering blood glucose levels.
== Tolbutamide ==


==Pharmacology==
[[File:Tolbutamide.svg|thumb|right|Chemical structure of Tolbutamide]]
Tolbutamide is a [[Sulfonylurea|sulfonylurea]] oral hypoglycemic agent. It works by stimulating the release of insulin from the [[Pancreas|pancreas]]. This action is dependent upon functioning beta cells in the pancreatic islets. Tolbutamide is extensively metabolized in the liver, primarily to hydroxytolbutamide.


==Clinical Use==
'''Tolbutamide''' is an [[oral hypoglycemic agent]] belonging to the class of [[sulfonylureas]]. It is primarily used in the management of [[type 2 diabetes mellitus]] to help control blood sugar levels. Tolbutamide works by stimulating the release of [[insulin]] from the [[beta cells]] of the [[pancreas]].
Tolbutamide is used in the management of [[Diabetes mellitus type 2|type 2 diabetes]] when diet alone is not adequate to control blood sugar levels. It is usually used in conjunction with a proper diet and exercise program to control high blood sugar in patients with type 2 diabetes.


==Side Effects==
== Mechanism of Action ==
Common side effects of tolbutamide include nausea, upset stomach, and skin rash or itching. More serious side effects can include low blood sugar (hypoglycemia), jaundice, and thrombocytopenia.


==Contraindications==
Tolbutamide acts by binding to the sulfonylurea receptor on the surface of pancreatic beta cells. This binding leads to the closure of [[ATP-sensitive potassium channels]], resulting in the depolarization of the cell membrane. The depolarization opens [[voltage-gated calcium channels]], allowing calcium ions to enter the cell. The increase in intracellular calcium concentration triggers the exocytosis of insulin-containing granules, thereby increasing insulin secretion.
Tolbutamide is contraindicated in patients with known hypersensitivity to sulfonylureas, in patients with type 1 diabetes or diabetic ketoacidosis, and in patients with severe renal or hepatic insufficiency.


==Interactions==
== Pharmacokinetics ==
Tolbutamide may interact with other drugs, including beta blockers, which can mask the symptoms of hypoglycemia, and certain antibiotics, which can increase the risk of hypoglycemia.
 
Tolbutamide is rapidly absorbed from the [[gastrointestinal tract]] after oral administration. It has a relatively short half-life, which necessitates multiple daily dosing. The drug is metabolized in the [[liver]] to inactive metabolites and is excreted primarily in the [[urine]].
 
== Clinical Use ==
 
Tolbutamide is indicated for the treatment of type 2 diabetes mellitus in patients who cannot achieve adequate glycemic control with [[diet]] and [[exercise]] alone. It is often used in combination with other antidiabetic agents such as [[metformin]] or [[insulin]] to achieve better glycemic control.
 
== Side Effects ==
 
Common side effects of tolbutamide include [[hypoglycemia]], [[nausea]], and [[skin rash]]. Hypoglycemia is the most serious side effect and can occur if the drug is taken without adequate food intake or if the patient engages in excessive physical activity. Other potential side effects include [[weight gain]] and [[gastrointestinal disturbances]].
 
== Contraindications ==
 
Tolbutamide is contraindicated in patients with [[type 1 diabetes mellitus]], [[diabetic ketoacidosis]], and those with known hypersensitivity to sulfonylureas. It should be used with caution in patients with [[renal]] or [[hepatic impairment]].
 
== Related Pages ==


==See Also==
* [[Sulfonylurea]]
* [[Sulfonylurea]]
* [[Diabetes mellitus type 2]]
* [[Type 2 diabetes mellitus]]
* [[Oral hypoglycemic agent]]
* [[Insulin]]
 
* [[Hypoglycemia]]
[[Category:Drugs]]
[[Category:Diabetes]]
[[Category:Pharmacology]]


{{stub}}
[[Category:Antidiabetic drugs]]

Latest revision as of 03:50, 13 February 2025

Tolbutamide[edit]

Chemical structure of Tolbutamide

Tolbutamide is an oral hypoglycemic agent belonging to the class of sulfonylureas. It is primarily used in the management of type 2 diabetes mellitus to help control blood sugar levels. Tolbutamide works by stimulating the release of insulin from the beta cells of the pancreas.

Mechanism of Action[edit]

Tolbutamide acts by binding to the sulfonylurea receptor on the surface of pancreatic beta cells. This binding leads to the closure of ATP-sensitive potassium channels, resulting in the depolarization of the cell membrane. The depolarization opens voltage-gated calcium channels, allowing calcium ions to enter the cell. The increase in intracellular calcium concentration triggers the exocytosis of insulin-containing granules, thereby increasing insulin secretion.

Pharmacokinetics[edit]

Tolbutamide is rapidly absorbed from the gastrointestinal tract after oral administration. It has a relatively short half-life, which necessitates multiple daily dosing. The drug is metabolized in the liver to inactive metabolites and is excreted primarily in the urine.

Clinical Use[edit]

Tolbutamide is indicated for the treatment of type 2 diabetes mellitus in patients who cannot achieve adequate glycemic control with diet and exercise alone. It is often used in combination with other antidiabetic agents such as metformin or insulin to achieve better glycemic control.

Side Effects[edit]

Common side effects of tolbutamide include hypoglycemia, nausea, and skin rash. Hypoglycemia is the most serious side effect and can occur if the drug is taken without adequate food intake or if the patient engages in excessive physical activity. Other potential side effects include weight gain and gastrointestinal disturbances.

Contraindications[edit]

Tolbutamide is contraindicated in patients with type 1 diabetes mellitus, diabetic ketoacidosis, and those with known hypersensitivity to sulfonylureas. It should be used with caution in patients with renal or hepatic impairment.

Related Pages[edit]