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Tolbutamide

ORINASE

Pronunciation: toel-BYOO-ta-mide

Tolbutamide ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Tolbutamide ballicule

What it isFirst-generation sulfonylurea; type 2 diabetes.

Why this oneShort-acting and hepatically cleared, so it was once favored in renal impairment.

What limits itThe UGDP trial suggested excess cardiovascular mortality, which shaped sulfonylurea labeling for decades. Obsolete.

Tolbutamide molecular structure (skeletal formula)
Molecular structure: Tolbutamide

FDA-approved for

⚠ BOXED WARNING

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4
Overdose danger3 / 4
Weight-gain liability2 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk3 / 4

Legacy pregnancy categoryC

Defining liabilityProlonged severe hypoglycemia

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Memory aids: interaction avatars

Tolbutamide CYP2C9 substrate avatar mnemonic
CYP2C9 substrate

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