Nisoldipine

Drug Information: Nisoldipine

Nisoldipine is a dihydropyridine calcium channel blocker used primarily in the treatment of hypertension. It selectively blocks calcium influx into vascular smooth muscle cells, leading to vasodilation and a reduction in blood pressure. Nisoldipine is available in extended-release formulations to provide a consistent and prolonged antihypertensive effect. It’s important to note that Nisoldipine, like other dihydropyridine calcium channel blockers, may cause peripheral edema as a side effect.

Category

Antihypertensive

Mechanism of Action

Nisoldipine belongs to the dihydropyridine class of calcium channel blockers (DHP-CCBs). Its primary mechanism of action involves selectively blocking L-type calcium channels in vascular smooth muscle cells. These voltage-dependent calcium channels are crucial for the influx of calcium ions into cells, which triggers muscle contraction. By inhibiting the entry of calcium, Nisoldipine promotes vasodilation, particularly in the peripheral arterioles. This reduction in peripheral vascular resistance leads to a decrease in systemic blood pressure. Unlike some other calcium channel blockers, Nisoldipine exhibits greater selectivity for vascular smooth muscle than for cardiac muscle. This selectivity minimizes its direct effects on heart rate and contractility at therapeutic doses. However, the reduction in blood pressure can trigger a reflex increase in heart rate in some individuals. The drug’s extended-release formulation ensures a gradual and sustained reduction in blood pressure over 24 hours.

Clinical Uses

Nisoldipine is primarily indicated for the treatment of hypertension. Its effectiveness in lowering blood pressure has been demonstrated in numerous clinical trials. Due to its long-acting nature, the extended-release formulation is often preferred for once-daily administration, which improves patient compliance. It may be used as monotherapy or in combination with other antihypertensive agents, such as diuretics, ACE inhibitors, or beta-blockers, to achieve optimal blood pressure control. While primarily used for hypertension, Nisoldipine, like other calcium channel blockers, has been investigated for potential use in other cardiovascular conditions such as angina. However, its primary approved indication remains the management of high blood pressure. Clinical studies have also explored its effects on specific populations, such as patients with diabetes and hypertension, and those with renal impairment. In such cases, careful monitoring of blood pressure and renal function is warranted.

Dosage

Adults: The usual starting dose of Nisoldipine extended-release tablets is 17 mg once daily. The dosage may be increased gradually, typically every 7-14 days, to a maximum of 34-68 mg once daily, depending on the patient’s blood pressure response and tolerability. Nisoldipine ER should be taken orally, and it’s important to swallow the tablet whole; do not crush, chew, or break it. Food can significantly increase Nisoldipine levels, it should be consistently administered either with food or on an empty stomach.

Pediatrics: The safety and effectiveness of Nisoldipine in pediatric patients have not been established. Dosage adjustments may be necessary in elderly patients or those with hepatic impairment.

Indications

* Hypertension (high blood pressure)

Contraindications

* Hypersensitivity to nisoldipine or other dihydropyridine calcium channel blockers.
* Severe hypotension (systolic blood pressure less than 90 mmHg).
* Advanced aortic stenosis.
* Cardiogenic shock.
* Use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole) is generally not recommended.

FAQ

Q: What is Nisoldipine used for?
A: Nisoldipine is primarily used to treat hypertension (high blood pressure).

Q: How does Nisoldipine work?
A: Nisoldipine is a calcium channel blocker. It works by relaxing blood vessels so blood can flow more easily.

Q: What are the common side effects of Nisoldipine?
A: Common side effects may include headache, flushing, peripheral edema (swelling of ankles and feet), and dizziness.

Q: Can I take Nisoldipine with food?
A: Food can significantly increase Nisoldipine levels, it should be consistently administered either with food or on an empty stomach. Consult your doctor or pharmacist.

Q: What should I do if I miss a dose of Nisoldipine?
A: If you miss a dose, take it as soon as you remember. If it’s almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not double the dose to catch up.

Q: Are there any drug interactions with Nisoldipine?
A: Yes, Nisoldipine can interact with other medications, including other blood pressure medications, certain antifungals, and some antibiotics. Always inform your doctor about all the medications you are taking.

Q: Can I drink alcohol while taking Nisoldipine?
A: Alcohol can increase the blood-pressure-lowering effect of Nisoldipine and may increase the risk of dizziness. It’s best to avoid or limit alcohol consumption while taking this medication.

Q: Is Nisoldipine safe to take during pregnancy?
A: You should discuss the risks and benefits of taking Nisoldipine during pregnancy with your doctor. It should be used during pregnancy only if clearly needed.