Palonidipine
Palonidipine 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]
Palonidipine 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, Palonidipine also helps alleviate symptoms of angina.
Pharmacokinetics[edit | edit source]
Palonidipine is administered orally and is well absorbed from the gastrointestinal tract. It undergoes extensive first-pass metabolism in the liver, primarily via the cytochrome P450 enzyme system. The drug is highly protein-bound, and its metabolites are excreted primarily through the kidneys.
Clinical Uses[edit | edit source]
Palonidipine 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 Palonidipine include:
Less common but serious side effects may include:
Drug Interactions[edit | edit source]
Palonidipine may interact with other medications, including:
- Beta-blockers: May enhance the hypotensive effect.
- CYP3A4 inhibitors: Such as ketoconazole and itraconazole, which may increase the plasma concentration of Palonidipine.
- Grapefruit juice: Can increase the bioavailability of Palonidipine, leading to increased effects and potential toxicity.
Contraindications[edit | edit source]
Palonidipine is contraindicated in patients with:
- Severe aortic stenosis
- Known hypersensitivity to dihydropyridine calcium channel blockers
Also see[edit | edit source]
References[edit | edit source]
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