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Details

Stereochemistry RACEMIC
Molecular Formula C21H23Cl2NO6
Molecular Weight 456.316
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CLEVIDIPINE

SMILES

CCCC(=O)OCOC(=O)C1=C(C)NC(C)=C(C1C2=C(Cl)C(Cl)=CC=C2)C(=O)OC

InChI

InChIKey=KPBZROQVTHLCDU-UHFFFAOYSA-N
InChI=1S/C21H23Cl2NO6/c1-5-7-15(25)29-10-30-21(27)17-12(3)24-11(2)16(20(26)28-4)18(17)13-8-6-9-14(22)19(13)23/h6,8-9,18,24H,5,7,10H2,1-4H3

HIDE SMILES / InChI

Molecular Formula C21H23Cl2NO6
Molecular Weight 456.316
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description

Clevidipine is a dihydropyridine calcium channel blocker. Clevidipine is marketed under the trade name Cleviprex, indicated for the reduction of blood pressure (BP) when oral therapy is not feasible or not desirable. Clevidipine is a dihydropyridine L-type calcium channel blocker. L-type calcium channels mediate the influx of calcium during depolarization in arterial smooth muscle. Experiments in anesthetized rats and dogs show that clevidipine reduces mean arterial blood pressure by decreasing systemic vascular resistance. Clevidipine does not reduce cardiac filling pressure (pre-load), confirming lack of effects on the venous capacitance vessels.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
CLEVIPREX

Cmax

ValueDoseCo-administeredAnalytePopulation
3.36 ng/mL
2 mg/h other, intravenous
CLEVIDIPINE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
122 ng × h/mL
2 mg/h other, intravenous
CLEVIDIPINE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
4.18 min
2 mg/h other, intravenous
CLEVIDIPINE plasma
Homo sapiens
15 min
2 mg/h other, intravenous
CLEVIDIPINE plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
0.5%
2 mg/h other, intravenous
CLEVIDIPINE plasma
Homo sapiens

Doses

AEs

OverviewOther

Other InhibitorOther SubstrateOther Inducer


Drug as perpetrator​

Tox targets

PubMed

Sample Use Guides

In Vivo Use Guide
Initial dose: Initiate the intravenous infusion of Cleviprex at 1-2 mg/hour. Dose titration: The dose may be doubled at short (90 second) intervals initially. As the blood pressure approaches goal, the increase in doses should be less than doubling and the time between dose adjustments should be lengthened to every 5-10 minutes. An approximately 1-2 mg/hour increase will generally produce an additional 2-4 mmHg decrease in systolic pressure. Maintenance dose: The desired therapeutic response for most patients occurs at doses of 4-6 mg/hour. Patients with severe hypertension may require doses up to 32 mg/hour, but there is limited experience at this dose rate. Maximum dose: Most patients were treated with maximum doses of 16 mg/hour or less.There is limited short-term experience with doses up to 32 mg/hour. Because of lipid load restrictions, no more than 1000 mL or an average of 21 mg/hour of Cleviprex infusion is recommended per 24 hour period. In clinical trials, 55 hypertensive patients were treated with >500mL of Cleviprex infusion per 24 hour period. There is little experience with infusion durations beyond 72 hours at any dose.
Route of Administration: Intravenous
In Vitro Use Guide
Clevidipine completely reversed U46619-induced contraction (EC50 = 3.88 +/- 0.84 x 10(-6) mol/L) of human internal mammary artery.
Substance Class Chemical
Record UNII
19O2GP3B7Q
Record Status Validated (UNII)
Record Version