CLEVIPREX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CLEVIPREX (CLEVIPREX).
Cleviprex (clevidipine) is a dihydropyridine L-type calcium channel blocker with high vascular selectivity. It inhibits calcium influx into vascular smooth muscle cells, causing arterial vasodilation and reduced peripheral vascular resistance.
| Metabolism | Rapidly metabolized by esterases in the blood and extravascular tissues to an inactive carboxylic acid metabolite (H152/81). Not primarily dependent on hepatic CYP450 enzymes. |
| Excretion | Renal: 63–73% as metabolites, fecal: 7–10%, unchanged drug in urine: <1% |
| Half-life | Terminal elimination half-life: 2.7 minutes (dihydropyridine ring reduction) and 15 minutes (ester hydrolysis); clinical context: rapid offset allows precise titration |
| Protein binding | 87–97% bound to plasma proteins (primarily albumin) |
| Volume of Distribution | 0.32 L/kg (approx. 22 L for 70 kg); indicates limited extravascular distribution |
| Bioavailability | Intravenous: 100% (only route administered) |
| Onset of Action | Intravenous: 2–4 minutes |
| Duration of Action | Infusion rate-dependent; steady-state achieved within 5–10 min; effects dissipate within 5–15 min after infusion stop due to rapid metabolism |
Initiate intravenous infusion at 1-2 mg/kg/hr, titrate by 0.5-1 mg/kg/hr every 90 minutes up to maximum 32 mg/kg/hr. Maintenance dose: 4-6 mg/kg/hr. Route: IV. Frequency: continuous infusion.
| Dosage form | EMULSION |
| Renal impairment | No dose adjustment required for renal impairment. Clevidipine is not removed by dialysis. |
| Liver impairment | Contraindicated in patients with severe hepatic impairment (Child-Pugh Class C). Use with caution in moderate impairment (Child-Pugh B); consider lower initial doses and titrate slowly. |
| Pediatric use | Safety and efficacy not established in pediatric patients. No FDA-approved dosing recommendations. |
| Geriatric use | No specific dose adjustment required. Elderly patients may be more sensitive to hypotensive effects; use lower initial doses and titrate cautiously. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CLEVIPREX (CLEVIPREX).
| Breastfeeding | No data on presence in human milk or effects on breastfed infants. Clevidipine is highly protein-bound (>99%) and rapidly metabolized, suggesting minimal excretion into milk. However, caution is advised. M/P ratio: not determined. |
| Teratogenic Risk | Cleviprex (clevidipine) is a calcium channel blocker. No adequate and well-controlled studies in pregnant women. In animal studies, no teratogenic effects were observed at clinically relevant doses. However, maternal toxicity at high doses led to fetal effects (reduced fetal weight, delayed ossification). First trimester: limited data; risk cannot be excluded. Second and third trimesters: may cause fetal acidosis, hypotension, and bradycardia due to maternal hypotension. Use only if potential benefit justifies potential risk. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to clevidipine or any component of the formulation (including soybean oil or egg lecithin)","Severe aortic stenosis (may reduce cardiac output and worsen symptoms)","Patients with defective lipid metabolism (e.g., hyperlipoproteinemia, lipoid nephrosis, acute pancreatitis with hyperlipidemia)"]
| Precautions | ["Use caution in patients with heart failure, as beta-blocker withdrawal may exacerbate angina; continue beta-blocker therapy.","Hypotension and reflex tachycardia may occur; monitor blood pressure and heart rate closely.","Can cause acute kidney injury or worsening of renal function in at-risk patients.","Lipid emulsion formulation; use caution in patients with severe hypertriglyceridemia or lipid metabolism disorders.","Contains soybean oil and egg lecithin; contraindicated in patients with allergies to soybeans or eggs.","Not recommended for use in pediatric patients due to lack of safety and efficacy data."] |
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| Fetal Monitoring | Continuous monitoring of maternal blood pressure and heart rate during infusion. Fetal heart rate monitoring recommended due to risk of fetal bradycardia. Maternal acid-base status and venous pH monitoring in prolonged use or high doses. |
| Fertility Effects | No human data on fertility. Animal studies (rats) showed no impairment of fertility at doses up to 10 times the maximum recommended human dose based on body surface area. |