HYDRALAZINE Powder for concentrate for solution for injection/infusion Ref.[8220] Active ingredients: Hydralazine

Source: Medicines & Healthcare Products Regulatory Agency (GB)  Revision Year: 2019  Publisher: Amdipharm UK Limited, Capital House, 85 King William Street, London, EC4N 7BL, United Kingdom

Pharmacodynamic properties

Pharmacotherapeutic group: Hydrazinophthalazine derivatives
ATC code: C02DB02

Mechanism of action

Hydralazine is a direct acting vasodilator which exerts its effects principally on the arterioles. Its precise mode of action is not known.

Pharmacodynamic effects

Administration of hydralazine produces a fall in peripheral resistance and a decrease in arterial blood pressure, effects which induce reflex sympathetic cardiovascular responses. The concomitant use of a beta-blocker will reduce these reflex effects. and enhance the anti-hypertensive effect. The use of hydralazine can result in sodium and fluid retention, producing oedema and reduced urinary volume. These effects can be prevented by concomitant administration of a diuretic.

Pharmacokinetic properties

Absorption

None stated.

Distribution

Hydralazine is rapidly distributed in the body and displays a particular affinity for the blood-vessel walls. Plasma protein binding is of the order of 90%.

Biotransformation

None stated.

Elimination

Plasma half-life averages 2-3 hours but is prolonged up to 16 hours in severe renal failure (creatinine clearance less than 20 ml/min) and shortened to approximately 45 minutes in rapid acetylators.

Characteristics in patients

None stated.

Preclinical safety data

Hydralazine has been found to be teratogenic in mice producing a small incidence of cleft palate and certain other bony malformations, in oral doses ranging from 20-120mg/kg i.e. 20-30 times the maximum human daily dose. It was not teratogenic in rats or rabbits.

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