Products
Clevidipine is marketed as an oil-in-water emulsion for intravenous injection (Cleviprex). It was approved in the United States in 2008 and in many countries in 2010. It is also registered in several European countries.
Structure and properties
Clevidipine (C21H23Cl2NO6, Mr = 456.32 g/mol) is a racemate of – and -levidipine. Both enantiomers are involved in the action. Clevidipine is practically insoluble in water and is therefore formulated as a milky white emulsion. Clevidipine has an identical structure to felodipine but is esterified differently, which is the basis for its short duration of action. Like esmolol, it belongs to the so-called soft drugs, a group of drugs that are rapidly and predictably metabolized and inactivated after they have produced the desired effect.
Effects
Clevidipine (ATC C08CA16) has vasodilator and antihypertensive properties. It has a rapid onset of action in the range of minutes. After cessation of administration, the effects wear off within about 5 to 15 minutes because the drug is rapidly hydrolyzed by esterases in the blood and tissues to inactive metabolites. The effects are due to blockade of L-type calcium channels. This reduces the influx of calcium ions into vascular smooth muscle cells and decreases peripheral vascular resistance.
Indications
For rapid reduction of blood pressure in perioperative situations.
Dosage
According to the SmPC. The drug is administered intravenously.
Contraindications
For complete precautions, see the drug label.
Interactions
Pharmacokinetic interactions are considered unlikely because clevidipine does not interact with CYP450 isozymes.
Adverse effects
The most common potential adverse effects include headache.