Nisoldipine
Nisoldipine Uses, Dosage, Side Effects, Food Interaction and all others data.
Nisoldipine 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, nisoldipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction. Nisoldipine may be used in alone or in combination with other agents in the management of hypertension.
Nisoldipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nisoldipine is similar to other peripheral vasodilators. Nisoldipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
| Trade Name | Nisoldipine |
| Availability | Prescription only |
| Generic | Nisoldipine |
| Nisoldipine Other Names | Nisoldipin, Nisoldipina, Nisoldipine, Nisoldipino, Nisoldipinum |
| Related Drugs | amlodipine, aspirin, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide, atenolol, diltiazem, nitroglycerin |
| Weight | 17mg, 20mg, 25.5mg, 30mg, 34mg, 40mg, 8.5mg |
| Type | Oral tablet, extended release |
| Formula | C20H24N2O6 |
| Weight | Average: 388.4144 Monoisotopic: 388.16343651 |
| Protein binding | 99% |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Nisoldipine is a calcium channel blocker used as monotherapy or combined with other drugs for the treatment of hypertension.
For the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.
Nisoldipine is also used to associated treatment for these conditions: High Blood Pressure (Hypertension)
How Nisoldipine works
By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Nisoldipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Food Interaction
- Avoid grapefruit products.
[Moderate] GENERALLY AVOID: The consumption of grapefruit juice may be associated with significantly increased plasma concentrations of some calcium channel blockers (CCBs) when they are administered orally.
The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.
The interaction has been reported with the dihydropyridine CCBs (in roughly decreasing order of magnitude) felodipine, nisoldipine, nifedipine, and nimodipine, often with a high degree of interindividual variability.
Grapefruit juice caused more than twofold increases in felodipine, nifedipine, and nisoldipine AUCs.
MANAGEMENT: The manufacturers of nifedipine and nisoldipine recommend avoiding grapefruit juice.
Patients treated orally with other calcium channel blockers should be advised to avoid consumption of large amounts of grapefruits and grapefruit juice to prevent any undue fluctuations in serum drug levels.
Increased effects on blood pressure may persist for up to 4 days after the consumption of grapefruit juice.
Monitoring for calcium channel blocker adverse effects (e.g., headache, hypotension, syncope, tachycardia, edema) is recommended.
Nisoldipine multivitamins interaction
[Moderate] Calcium-containing products may decrease the effectiveness of calcium channel blockers by saturating calcium channels with calcium.
Calcium chloride has been used to manage acute severe verapamil toxicity.
Management consists of monitoring the effectiveness of calcium channel blocker therapy during coadministration with calcium products.
Nisoldipine Drug Interaction
Moderate: aspirin, aspirin, nebivolol, metoprololUnknown: amoxicillin / clavulanate, dutasteride, olmesartan, ciprofloxacin, ubiquinone, rosuvastatin, apixaban, insulin glargine, atorvastatin, bimatoprost ophthalmic, pregabalin, esomeprazole, levothyroxine, ascorbic acid, cholecalciferol, ezetimibe / simvastatin
Nisoldipine Disease Interaction
Major: cardiogenic shock/hypotension, coronary artery disease, liver diseaseModerate: CHF/AMI
Elimination Route
Relatively well absorbed into the systemic circulation with 87% of the radiolabeled drug recovered in urine and feces. The absolute bioavailability of nisoldipine is about 5%.
Half Life
7-12 hours
Elimination Route
Although 60-80% of an oral dose undergoes urinary excretion, only traces of unchanged nisoldipine are found in urine.
Innovators Monograph
You find simplified version here Nisoldipine
