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Clevidipine; Uses, Dosage, Side effects, Interactions

Clevidipine is a dihydropyridine L-type calcium channel blocker that is selective for vascular smooth muscle and is indicated for blood pressure reduction when oral therapy is not an option. Clevidipine is a dihydropyridine calcium channel blocker indicated for the reduction of blood pressure when oral therapy is not feasible or not desirable. Clevidipine is a dihydropyridine L-type calcium channel blocker that is selective for vascular smooth muscle and is indicated for blood pressure reduction when oral therapy is not an option.

Mechanism of Action of Clevidipine

Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, clevidipine inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue.

Indications of Clevidipine

Contra-Indications of Clevidipine

Severe heart failure
Abnormally low blood pressure
Kidney disease with a reduction in kidney function
Fluid Retention in the Legs, arms or hands
Blood Circulation Failure due to Serious Heart Condition
Chronic idiopathic constipation
The high amount of triglyceride in the blood
Excessive fat in the blood
Severe Narrowing of the Aortic Heart valve
Acute Inflammation of the pancreas
Fast heartbeat
Minimal Change glomerulonephritis
Stomach or intestine blockage
Narrowing of the intestines
Decreased motility function of stomach or intestines

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Dosage of Clevidipine

Strengths: 1 mg, 2 mg, 0.5 mg/mL

Hypertension

Initial dose: IV infusion of 1 to 2 mg/hour (2 to 4 mL/hour)
Dose titration: Dose may be doubled at short (90 seconds) intervals initially. As blood pressure approaches the goal, increase in doses should be less than doubling and intervals between dose adjustments should increase to every 5 to 10 minutes. An increase of approximately 1 to 2 mg/hour generally produces an additional 2 to 4 mmHg decrease in systolic pressure.
Maintenance dose: The desired therapeutic response for most patients occurs at doses of 4 to 6 mg/hour (8 to 12 mL/hour). Patients with severe hypertension may require doses up to 32 mg/hour (64 mL/hour).
Maximum dose: Most patients were treated with maximum doses of 16 mg/hour (32 mL/hour) or less; however, there is limited short-term experience with doses up to 32 mg/hour (64 mL/hour). Due to lipid load restrictions, no more than 1000 mL (or an average of 21 mg/hour) of clevidipine infusion is recommended per 24 hour period. There is little experience with infusion durations beyond 72 hours at any dose.

Side Effects of Clevidipine

The most common

a severe headache, rapid heartbeat, stiffness in your neck,
chest pain, fast or slow heart rate;
swelling, rapid weight gain;
Xerostomia (dry mouth)
A headache
Fatigue
Skin reactions
Hypotension
Anxiety
Constipation
Nausea/vomiting
Weight gain/loss
Erectile dysfunction

More common

Abdominal or stomach pain, discomfort, or tenderness
chills or fever
difficulty with moving
a headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
discomfort in arms, shoulders, neck or upper back
excessive sweating
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
rust colored urine
decreased amount of urine

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Rare

Anxiety
change in vision
chest pain or tightness
confusion
a cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
fainting
hallucinations
a headache
irritability
lightheadedness
mood or mental changes
muscle pain or cramps
muscle spasm or jerking of all extremities
nervousness

Drug Interactions of Clevidipine

Clevidipine may interact with the following drugs, supplements, & may change the efficacy of the drug

alpha blockers (e.g., alfuzosin, doxazosin, tamsulosin)
alpha agonists (e.g., clonidine, methyldopa)
angiotensin II receptor blockers (ARBs; e.g., candesartan, losartan)
antidiabetes medications (e.g., insulin, metformin, glyburide)
atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine, risperidone)
azathioprine
barbiturates (e.g., butalbital, pentobarbital phenobarbital)
beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
“azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
canagliflozin
ciprofloxacin
calcium supplements (e.g., calcium carbonate, calcium citrate)
carbamazepine
clopidogrel
cyclosporine
diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
duloxetine
“gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
guanfacine
heparin
levodopa
medications that increase potassium levels (e.g., potassium supplements, spironolactone, amiloride, and salt substitutes containing potassium)
metformin
nonsteroidal anti-inflammatory drugs (NSAIDs; e.g., ibuprofen, indomethacin, naproxen)
other angiotensin-converting-enzyme inhibitors (ACEIs; e.g., captopril, ramipril)
pentoxifylline
macrolide antibiotics (e.g., clarithromycin, erythromycin)
methylphenidate
monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine)
phosphodiesterase-5 inhibitors (e.g., sildenafil, tadalafil, vardenafil)
pregabalin
sodium phosphates
tizanidine
trimethoprim
valproic acid
warfarin

Pregnancy Category

FDA Pregnancy Category C

Pregnancy

This medication should not be taken by women who are or may become pregnant, as clevidipine may cause harm to the developing baby if it is taken by the mother during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

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Lactation

This medication should not be taken by women who are breastfeeding. The safety and effectiveness of using this medication have not been established for children.