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Nimodipine; Mechanism, Uses, Contraindications, Dosage, Side effects,

Nimodipine is a dihydropyridine derivative and an analog of the calcium channel blocker nifedipine, with antihypertensive activity. Nimodipine inhibits the transmembrane influx of calcium ions in response to depolarization in smooth muscle cells, thereby inhibiting vascular smooth muscle contraction and inducing vasodilatation. Nimodipine has a greater effect on cerebral arteries than on peripheral smooth muscle cells and myocardial cells, probably because this agent can cross the blood-brain barrier due to its lipophilic nature. Furthermore, this agent also inhibits the drug efflux pump P-glycoprotein, which is overexpressed in some multi-drug resistant tumors, and may improve the efficacy of some antineoplastic agents.

Nimodipine is a dihydropyridine calcium channel blocker originally developed for the treatment of high blood pressure. It is not frequently used for this indication, but has shown good results in preventing a major complication of subarachnoid hemorrhage (a form of cerebral hemorrhage) termed vasospasm; this is now the main use of nimodipine. Nimodipine is a 1,4-dihydropyridine calcium channel blocker. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, nimodipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction. Compared to other calcium channel blocking agents, nimodipine exhibits greater effects on cerebral circulation than on peripheral circulation.

Mechanism of action of Nimodipine

Nimodipine binds specifically to L-type voltage-gated calcium channels. There are numerous theories about its mechanism in preventing vasospasm, but none are conclusive. Nimodipine has additionally been found to act as an antagonist of the mineralocorticoid receptor, or as an antimineralocorticoid. Although the precise mechanism of action is not known, nimodipine blocks the intracellular influx of calcium through voltage-dependent and receptor-operated slow calcium channels across the membranes of myocardial, vascular smooth muscle, and neuronal cells. Nimodipine binds specifically to L-type voltage-gated calcium channels. The inhibition of calcium ion transfer results in the inhibition of vascular smooth muscle contraction. Evidence suggests that the dilation of small cerebral resistance vessels, with a resultant increase in collateral circulation, and/or a direct effect involving the prevention of calcium overload in neurons may be responsible for nimodipine’s clinical effect in patients with subarachnoid hemorrhage.

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Indications of Nimodipine

Hunt and Hess Grades I-V Subarachnoid hemorrhage
Subarachnoid Hemorrhage
Ischemic Stroke
Migraine Prevention
Treatment of aneurysmal subarachnoid hemorrhage
For use as an adjunct to improve neurologic outcome following subarachnoid hemorrhage (SAH) from ruptured intracranial berry aneurysms by reducing the incidence and severity of ischemic deficits.

Dosage of Nimodipine

Strengths: 30 mg; 60 mg/20 mL; 30 mg/10 mL

Subarachnoid Hemorrhage

60 mg orally, nasogastric, or gastric tube every 4 hours
Duration of therapy: 21 days

Side Effects of Nimodipine

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

Rare

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

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Drug Interactions of Nimodipine

Nimodipine may interact with following drugs, supplements, & may change the efficacy of 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)
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 nimodipine 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.

Lactation

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

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