API Lercanidipine hydrochloride

Lercanidipine hydrochloride More Info

Lercanidipine hydrochloride is a calcium channel blocker.

1. Chemical structure and formula

Its chemical name is (±)-2 - [(3,3 - diphenylpropyl)methylamino] - 1,1 - dimethylethyl methyl 1,4 - dihydro - 2,6 - dimethyl - 4 - (3 - nitro - phenyl) - 3,5 - pyridinedicarboxylate hydrochloride. The chemical formula is C₃₆H₄₁N₃O₆·HCl.

2. Mechanism of action

Lercanidipine hydrochloride acts by selectively blocking the L - type calcium channels in vascular smooth muscle cells. By doing so, it inhibits the influx of calcium ions into these cells. As a result, it causes relaxation of the arterial smooth muscle, leading to vasodilation. This helps in reducing peripheral vascular resistance and subsequently lowering blood pressure. For example, in the arterioles of the systemic circulation, it works to widen the blood vessels, allowing blood to flow more easily and reducing the pressure exerted on the vessel walls.

3. Pharmacokinetic properties

Absorption: It is rapidly and almost completely absorbed after oral administration. However, it undergoes extensive first - pass metabolism in the liver. The bioavailability of lercanidipine hydrochloride is relatively low, usually around 10% - 15%.

Distribution: It is highly protein - bound (more than 98%) in the plasma. This high protein - binding property affects its distribution in the body and its interaction with other drugs that also bind to plasma proteins.

Metabolism: The drug is mainly metabolized in the liver through the cytochrome P450 system, specifically CYP3A4 isoenzyme. The metabolites are then excreted mainly in the feces, with a small portion excreted in the urine.

Elimination: The elimination half - life of lercanidipine hydrochloride is approximately 8 - 10 hours, which means it takes this amount of time for half of the drug to be removed from the body.

4. Therapeutic uses

Lercanidipine hydrochloride is primarily used in the treatment of hypertension. By reducing blood pressure, it helps to decrease the risk of various cardiovascular complications such as heart attacks, strokes, and kidney damage associated with high blood pressure. It can be used alone or in combination with other antihypertensive drugs depending on the severity of the hypertension and the patient's response to treatment.

5. Side effects and precautions

Side effects: Common side effects may include headache, flushing (a feeling of warmth and redness in the skin, usually in the face and neck), ankle edema (swelling of the ankles due to fluid accumulation), and dizziness. These side effects are usually mild and transient. In some cases, more severe side effects such as palpitations (irregular or rapid heartbeats) and gastrointestinal disturbances (such as nausea, vomiting, or abdominal pain) may occur.

Precautions: It should be used with caution in patients with hepatic impairment because of its extensive liver metabolism. Also, interactions with other drugs that affect the cytochrome P450 system, especially CYP3A4 inhibitors or inducers, need to be considered. For example, concurrent use of strong CYP3A4 inhibitors like ketoconazole can increase the plasma concentration of lercanidipine hydrochloride, increasing the risk of side effects.