Drug intelligence / Profile preview

midazolam + digoxin

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Intranasal, Rectal
01

Overview

Midazolam + digoxin is a **combination** of two pharmaceutical agents frequently evaluated together in clinical pharmacology studies to detect drug-drug interactions and probe drug metabolism pathways. **Midazolam** is a short-acting benzodiazepine used for its sedative, anxiolytic, muscle relaxant, anticonvulsant, hypnotic, and amnesic effects, acting primarily as a positive allosteric modulator at the gamma-aminobutyric acid type A (GABA(A)) receptor. **Digoxin** is a cardiac glycoside used for the treatment of various heart conditions, especially atrial fibrillation and heart failure, exerting positive inotropic effects by inhibiting sodium/potassium ATPase in cardiac myocytes, thus increasing intracellular calcium. Midazolam is commonly used as a probe for CYP3A-mediated metabolism, while digoxin is used as a probe for P-glycoprotein (P-gp) activity. There is precedent for pharmacokinetic interaction between the two drugs, as benzodiazepines, including midazolam, may increase serum levels and effects of digoxin, requiring monitoring and potential dose adjustments[2][5][4].

02

Targets

ABCB1 (P-glycoprotein)CYP3A4 (Cytochrome P450 3A4)ATP1A (Sodium/potassium-transporting ATPase)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)

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