Calcium channel blocker · Antihypertensive
Clevidipine (Cleviprex)
Also called Cleviprex
Indications
- Lowering BP when oral therapy is not feasible or not desirable
- Perioperative hypertension, especially cardiac surgery
- Hypertensive emergencies, including hypertensive acute heart failure
- Acute ischemic stroke around reperfusion, and intracerebral hemorrhage
- Aortic dissection, after beta-blockade
- Pheochromocytoma or stimulant crisis
Dosing
Clevidipine drip card and mL/h converterStart: 1–2 mg/h
Mechanism of action
Clevidipine is a dihydropyridine L-type (Cav1.2) calcium channel blocker that works like nicardipine: it binds the α1C subunit, favors inactivated channels in depolarized arteriolar smooth muscle and blocks calcium entry, so arterioles relax and SVR falls. It spares veins, so preload is kept. Esterases in blood and tissue split its butyroxymethyl ester within about a minute, so the effect tracks the pump rate.
Pharmacology
- Cardiovascular: arteriolar dilation lowers SVR and BP without reducing preload
- Cardiovascular: reflex tachycardia; it can depress contractility and worsen heart failure
- Cardiovascular: the effect plateaus near a 25% fall in systolic pressure, with no tolerance during 72-h infusions
- Metabolic: 0.2 g of fat (2 kcal) per mL; triglycerides can rise during long infusions
- Other: headache, nausea and vomiting are most common
Pharmacokinetics
| Onset | 2–4 min |
|---|---|
| Duration | Full BP recovery 5–15 min after stopping |
| Context-sensitive half-time | Under 1 min, whatever the infusion length (Ericsson 2000) |
| Half-life | Initial about 1 min (85–90% of elimination); terminal about 15 min |
| Distribution | Small Vd at steady state, 0.17–0.19 L/kg |
| Protein binding | Over 99.5% |
| Metabolism | Hydrolyzed by esterases in blood (mostly red cells) and tissues to an inactive acid and formaldehyde; plasma cholinesterase deficiency barely slows it |
| Clearance | About 0.07 L/kg/min, several times liver blood flow |
| Elimination | Metabolites in urine (63–74%) and feces (7–22%) |
| Organ failure | Not expected to change with liver or kidney failure |
Chemistry
- Dihydropyridine with a 2,3-dichlorophenyl ring at C4 and a butyroxymethyl ester, the link blood esterases cleave
- Racemic; both enantiomers are hydrolyzed at similar rates
- Practically insoluble in water (log P about 4.3), so it comes as a milky 0.5 mg/mL emulsion in 20% soybean oil with glycerin, egg yolk phospholipids, oleic acid and EDTA, pH 6–8
- Refrigerate (up to 2 months at room temperature); keep vials in the carton against light, though the running infusion needs no cover
- Supports microbial growth: aseptic technique, discard 12 h after puncture, no dilution, no other drug in the line
Adverse effects and cautions
In the one-pagers
Practice Aortic Dissection and Hypertensive Emergency questions free19 exam-style questions with rationales on the topic where Clevidipine comes up most. No account or download needed.
In the algorithms
Other calcium channel blocker drugs
Practice free in your browser2,450+ exam-style questions with rationales. No account, no ads. Also free on the App Store and Google Play.
Sources
- FDA label: Cleviprex (2022)
- Ericsson 2000 (kinetics)
- Ericsson 1999 (in vitro hydrolysis)
- PubChem: clevidipine
For education and exam preparation only. Follow your institution’s protocols. Typical adult values for study. Follow your local protocols and medical direction.