Drug Groups

approved

Description

Adrenergic beta-agonist used to control premature labor. [PubChem]

Indication

For the treatment and prophylaxis of premature labour

Pharmacology

Beta-2 adrenergic receptors are located at sympathetic neuroeffector junctions of many organs, including uterus. Ritodrine is beta-2 adrenergic agonist. It stimulates beta-2 adrenergic receptor, increases cAMP level and decreases intracellular calcium concentration. The decrease of calcium concentration leads to a relaxation of uterine smooth muscle and, therefore, a decrease in premature uterine contractions.

Toxicity

LD₅₀=64mg/kg (mice, IV); LD₅₀=540 mg/kg (mice, oral); LD₅₀=85 mg/kg (rat, IV)

Affected Organisms

Biotransformation

Hepatic, by both the mother and fetus

Half Life

1.7-2.6 hours

Protein Binding

~56%

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