What are the uses and mechanism of action of Benidipine (Benidipine hydrochloride)?

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From the Guidelines

Benidipine is a calcium channel blocker that should be used to treat hypertension and angina pectoris due to its ability to selectively block L-type and N-type calcium channels, leading to vasodilation and reduced peripheral vascular resistance and myocardial oxygen demand. The mechanism of action of benidipine involves preventing calcium influx into vascular smooth muscle and cardiac tissue, resulting in vasodilation of peripheral and coronary blood vessels 1.

Key Uses of Benidipine

  • Hypertension
  • Angina pectoris

Mechanism of Action

  • Selectively blocks L-type and N-type calcium channels
  • Prevents calcium influx into vascular smooth muscle and cardiac tissue
  • Leads to vasodilation of peripheral and coronary blood vessels
  • Reduces peripheral vascular resistance and myocardial oxygen demand

Dosage and Administration

  • Typical dosage ranges from 2-8 mg once daily
  • Treatment usually starts at 2-4 mg and adjusts based on blood pressure response
  • Benidipine has a long duration of action, allowing for once-daily dosing and improving patient compliance

Benefits and Side Effects

  • Demonstrates renoprotective effects by dilating both afferent and efferent arterioles in the kidneys
  • Common side effects include headache, dizziness, flushing, and peripheral edema
  • Should be used cautiously in patients with severe liver dysfunction, and dose adjustments may be necessary for elderly patients
  • Unlike some other calcium channel blockers, benidipine has minimal negative inotropic effects, making it relatively safer for patients with heart failure 1.

Clinical Considerations

  • Benidipine can be used in combination with other antihypertensive agents, such as ACE inhibitors, beta-blockers, and diuretics, to achieve better blood pressure control 1.
  • The choice of benidipine as a calcium channel blocker should be based on its efficacy, safety, and tolerability profile, as well as the individual patient's needs and medical history 1.

From the Research

Mechanism of Action

  • Benidipine is a dihydropyridine calcium channel blocker that works by blocking L, N, and T-type calcium channels with a membrane approach 2
  • It has relatively high vascular selectivity and is expected to show protective effects on vascular endothelial cells 2
  • Benidipine also has anti-oxidative action and enhances nitric oxide production, which contributes to its cardio-protective effects in patients with ischemic heart diseases 2
  • The blockade of T-type voltage-dependent Ca2+ channels by benidipine inhibits aldosterone production in human adrenocortical cell line NCI-H295R 3

Uses

  • Benidipine is used in the treatment of hypertension and angina pectoris 4, 2, 3
  • It is also used to reduce the risk of cardiovascular events, including stroke and end-stage renal disease, in patients with angina pectoris 5
  • Benidipine has renoprotective effects and can be used in combination with angiotensin II type 1 receptor blockers (ARBs) to achieve adequate anti-hypertensive effects 2, 6
  • It can also be used to treat patients with stage 3-5 chronic kidney disease (CKD) who are already being administered ARBs 6

Pharmacological Effects

  • Benidipine has a long-acting pharmacological effect and is well-tolerated by patients 4, 2
  • It has a smooth and sustained effect on blood pressure, with a high trough-to-peak ratio (T/P ratio) 4
  • Benidipine can reduce systolic and diastolic blood pressure, as well as urinary albumin, in patients with essential hypertension 4
  • It can also reduce the systolic morning blood pressure surge and has a protective effect on vascular endothelial cells 4, 2

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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