Cilnidipine is a dihydropyridine calcium channel blocker that has been extensively used in the management of hypertension. It is a third-generation calcium channel blocker that has both L-type and N-type calcium channel-blocking actions. This article aims to provide a comprehensive review of cilnidipine’s pharmacology, clinical uses, adverse effects, and drug interactions.

Pharmacology

Cilnidipine blocks L-type calcium channels in the heart and vascular smooth muscle, leading to vasodilation and a decrease in blood pressure. It also blocks N-type calcium channels in the sympathetic nervous system, leading to a reduction in sympathetic tone. This dual action results in a reduction in peripheral resistance and an improvement in cardiac function.

Cilnidipine has a half-life of 7–12 hours and is primarily metabolised in the liver. Its bioavailability ranges from 15%–60%, and it is excreted mainly in the urine. The recommended starting dose of cilnidipine is 5 mg/day, which can be increased to 10 mg/day after 2–4 weeks.

Clinical uses

Cilnidipine has been extensively used in the management of hypertension, either alone or in combination with other antihypertensive agents. It has been shown to be effective in reducing both systolic and diastolic blood pressure in patients with mild to moderate hypertension. Cilnidipine has also been found to have renoprotective effects in patients with diabetic nephropathy and chronic kidney disease.

In addition, cilnidipine has been shown to have beneficial effects in the management of heart failure. It has been found to improve left ventricular ejection fraction and reduce the incidence of hospitalization due to heart failure.

Adverse effects

Like other calcium channel blockers, cilnidipine may cause peripheral oedema, flushing, and headache. These adverse effects are usually mild and transient and do not require discontinuation of the drug. Rarely, cilnidipine may cause serious adverse effects such as angioedema, Stevens-Johnson syndrome, and toxic epidermal necrolysis. Therefore, cilnidipine should be used with caution in patients with a history of hypersensitivity reactions to other calcium channel blockers.

Drug interactions

Cilnidipine may interact with other drugs that are metabolized in the liver, such as cytochrome P450 inhibitors and inducers. It may also interact with other antihypertensive agents, such as beta-blockers and ACE inhibitors. Therefore, it is essential to monitor blood pressure and adjust the dose of cilnidipine when it is co-administered with other drugs.

Conclusion

Cilnidipine is a third-generation calcium channel blocker that has both L-type and N-type calcium channel-blocking actions. It has been extensively used in the management of hypertension, either alone or in combination with other antihypertensive agents. Cilnidipine has also been found to have renoprotective effects in patients with diabetic nephropathy and chronic kidney disease. In addition, it has been shown to have beneficial effects in the management of heart failure. Although cilnidipine is generally well-tolerated, it may cause peripheral oedema, flushing, and headache. Therefore, it should be used with caution in patients with a history of hypersensitivity reactions to other calcium channel blockers. Finally, cilnidipine may interact with other drugs that are metabolised in the liver, and therefore, it is essential to monitor blood pressure and adjust the dose of cilnidipine when it is co-administered with other drugs.

Ellen Diamond, a psychology graduate from the University of Hertfordshire, has a keen interest in the fields of mental health, wellness, and lifestyle.