Active Pharmaceutical Ingredients

Catalog ID80017671

CAS NO.103890-78-4

Purity 99%

MDL NumberMFCD00865936

Molecular FormulaC26H33NO6

Molecular Weight455.5433

Melting point: 174~175°C

Aspect	Details
Mechanism of Action	Lacidipine is a selective and potent calcium antagonist that primarily targets L-type calcium channels in vascular smooth muscle cells. By blocking these channels, it inhibits calcium influx, leading to vasodilation and reduced blood pressure. Additionally, it has antioxidant properties and may reduce atherosclerosis by inhibiting the formation of reactive oxygen species and inflammatory pathways.
Indications	– Treatment of hypertension (high blood pressure) in adults.<br>- Potential use in slowing the progression of atherosclerosis.<br>- Investigated for its potential anti-tumor effects in cancer immunotherapy.
Pharmacokinetics	– Absorption: Rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations reached within 30 to 150 minutes.<br>- Distribution: Highly lipophilic, with extensive first-pass metabolism in the liver.<br>- Metabolism: Metabolized by CYP3A4, with no active metabolites detected.<br>- Excretion: Approximately 70% excreted in feces and 30% in urine.<br>- Half-Life: Average terminal half-life is 13 to 19 hours.
Adverse Effects	– Common: Headache, flushing, ankle edema, dizziness, palpitations.<br>- Rare: Depression, tremor, syncope, hypotension, angioedema.<br>- Potential for increased blood alkaline phosphatase levels.
Contraindications	– Hypersensitivity to lacidipine or any of its components.<br>- Severe hypotension.<br>- Acute myocardial infarction (within 1 month) without concurrent treatment with other antihypertensive agents.
Storage Conditions	Store in a cool place, with the container tightly closed in a dry and well-ventilated area. Recommended storage temperature is 2 to 8 °C.
Special Considerations	– Monitor blood pressure regularly, especially at the start of treatment.<br>- Use with caution in patients with severe renal or hepatic impairment.<br>- May interact with other antihypertensive agents, CYP3A4 inhibitors, or inducers.<br>- Potential for QTc interval prolongation, though this is generally minimal.<br>- In cancer immunotherapy, lacidipine may be investigated for its ability to reprogram tryptophan metabolism and enhance T-cell activity

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