Mesudipine
Mesudipine is a calcium channel blocker used primarily in the management of hypertension and angina pectoris. It belongs to the dihydropyridine class of calcium channel blockers, which are known for their potent vasodilatory effects.
Mechanism of Action[edit | edit source]
Mesudipine works by inhibiting the influx of calcium ions through L-type calcium channels in the smooth muscle cells of the vascular system. This action leads to relaxation of the vascular smooth muscle, resulting in vasodilation and a subsequent decrease in blood pressure. By reducing the workload on the heart, Mesudipine also helps alleviate symptoms of angina.
Pharmacokinetics[edit | edit source]
Mesudipine is administered orally and is well absorbed from the gastrointestinal tract. It undergoes extensive first-pass metabolism in the liver, which affects its bioavailability. The drug is primarily metabolized by the cytochrome P450 enzyme system, particularly CYP3A4. The metabolites are excreted mainly via the kidneys.
Clinical Uses[edit | edit source]
Mesudipine is indicated for the treatment of:
- Hypertension: As a first-line or adjunctive therapy to lower blood pressure and reduce the risk of cardiovascular events.
- Angina pectoris: To relieve chest pain and improve exercise tolerance in patients with chronic stable angina.
Adverse Effects[edit | edit source]
Common side effects of Mesudipine include:
Less common but serious side effects may include:
Drug Interactions[edit | edit source]
Mesudipine may interact with other medications, including:
- Beta-blockers: May enhance the hypotensive effect.
- CYP3A4 inhibitors: Such as ketoconazole or erythromycin, which can increase plasma concentrations of Mesudipine.
- Grapefruit juice: Can increase the bioavailability of Mesudipine by inhibiting its metabolism.
Contraindications[edit | edit source]
Mesudipine is contraindicated in patients with:
- Severe aortic stenosis
- Unstable angina
- Known hypersensitivity to dihydropyridines
Also see[edit | edit source]
References[edit | edit source]
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