Usage
Clinidipine is primarily prescribed for the treatment of essential hypertension (high blood pressure). It belongs to the pharmacological classification of calcium channel blockers, specifically dihydropyridine calcium channel blockers. Clinidipine works by blocking L-type calcium channels in vascular smooth muscle, leading to vasodilation (widening of blood vessels) and a reduction in blood pressure.
Alternate Names
While “cilnidipine” is the generic name, there are various brand names under which it’s marketed internationally, including Cilren, Cinod, and Cilacar.
How It Works
Pharmacodynamics: Clinidipine primarily affects the vascular smooth muscle, causing relaxation and vasodilation. This reduces peripheral vascular resistance, leading to a decrease in blood pressure. It has minimal effect on cardiac contractility or heart rate.
Pharmacokinetics:
- Absorption: Clinidipine is well-absorbed after oral administration, with peak plasma concentrations reached in approximately 1-2 hours. Food does not significantly affect its absorption.
- Metabolism: Clinidipine is extensively metabolized in the liver, primarily by CYP3A4 and CYP2C19 enzymes.
- Elimination: The majority of the drug and its metabolites are excreted in the urine, with a small portion eliminated in the feces. The elimination half-life is around 6-10 hours, allowing for once-daily dosing.
Mode of Action: Clinidipine selectively blocks L-type calcium channels in vascular smooth muscle. This inhibits calcium influx into the cells, preventing smooth muscle contraction and promoting vasodilation.
Dosage
Standard Dosage
Adults:
The initial dose is typically 5-10 mg once daily, preferably after breakfast. If necessary, the dose can be increased to a maximum of 20 mg once daily.
Children:
The safety and efficacy of cilnidipine in children under 18 years of age have not been established. Use is generally not recommended unless specifically prescribed by a doctor.
Special Cases:
- Elderly Patients: An initial dose of 5 mg is recommended, with careful titration based on response and tolerability.
- Patients with Renal Impairment: Dose adjustment may be necessary in patients with moderate to severe renal impairment.
- Patients with Hepatic Dysfunction: Caution is advised, and dose adjustment may be required in patients with severe hepatic impairment.
- Patients with Comorbid Conditions: Careful monitoring is essential for patients with heart failure, severe aortic stenosis, or other cardiovascular conditions.
Clinical Use Cases
Clinidipine is primarily used for chronic hypertension management. Its use in acute clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations is not routinely indicated. Other medications may be more appropriate for these scenarios.
Dosage Adjustments
Dose adjustments should be individualized based on patient-specific factors such as age, renal function, hepatic function, and concomitant medications.
Side Effects
Common Side Effects:
Headache, dizziness, flushing, peripheral edema (swelling of ankles or feet), palpitations, and gastrointestinal disturbances (nausea, vomiting, abdominal pain).
Rare but Serious Side Effects:
Hypotension (low blood pressure), angina (chest pain), myocardial infarction (heart attack), and allergic reactions.
Long-Term Effects:
Long-term use may be associated with gingival hyperplasia (gum overgrowth) in some cases. Regular monitoring is recommended.
Adverse Drug Reactions (ADR):
Severe hypotension, angioedema (swelling of face, lips, or tongue), and hepatotoxicity (liver damage).
Contraindications
- Hypersensitivity to cilnidipine.
- Cardiogenic shock.
- Severe aortic stenosis.
- Unstable angina or recent myocardial infarction.
- Heart failure.
- Hypotension.
Drug Interactions
Clinidipine interacts with various medications, including:
- CYP3A4 inhibitors (e.g., ketoconazole, erythromycin): May increase cilnidipine levels.
- CYP3A4 inducers (e.g., rifampin, phenytoin): May decrease cilnidipine levels.
- Grapefruit juice: May increase cilnidipine levels.
- Other antihypertensives: May enhance the blood pressure-lowering effect.
- Antidiabetic drugs: May alter glucose levels.
Pregnancy and Breastfeeding
Clinidipine is generally not recommended during pregnancy or breastfeeding due to potential risks to the fetus or neonate. The safety and efficacy have not been established in these populations.
Drug Profile Summary
- Mechanism of Action: Calcium channel blocker, inhibits calcium influx into vascular smooth muscle, causing vasodilation.
- Side Effects: Headache, dizziness, flushing, peripheral edema, palpitations, GI disturbances. Rarely: hypotension, angina, MI.
- Contraindications: Hypersensitivity, cardiogenic shock, severe aortic stenosis, unstable angina/MI, heart failure, hypotension.
- Drug Interactions: CYP3A4 inhibitors/inducers, grapefruit juice, other antihypertensives, antidiabetic drugs.
- Pregnancy & Breastfeeding: Not recommended.
- Dosage: Adults: 5-10 mg once daily, up to 20 mg. Elderly: start with 5 mg.
- Monitoring Parameters: Blood pressure, heart rate, signs of peripheral edema, liver function tests.
Popular Combinations
Clinidipine is often combined with other antihypertensive medications, such as thiazide diuretics or ACE inhibitors, to achieve better blood pressure control.
Precautions
- Monitor for hypotension, especially in elderly patients.
- Avoid abrupt withdrawal.
- Caution in patients with hepatic or renal impairment.
- Avoid grapefruit juice.
- Monitor blood glucose levels in patients with diabetes.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Clinidipine?
A: Adults: Initially 5-10 mg once daily, up to a maximum of 20 mg/day. Elderly patients: Initiate at 5mg once daily.
Q2: What are the common side effects of Clinidipine?
A: Headache, dizziness, flushing, peripheral edema, palpitations, and gastrointestinal upset.
Q3: How does Clinidipine work?
A: It blocks calcium channels in blood vessels, leading to vasodilation and lowering blood pressure.
Q4: Can Clinidipine be used during pregnancy?
A: Clinidipine is generally not recommended during pregnancy due to potential risks to the fetus. Consult a doctor for alternative options.
Q5: What are the contraindications for Clinidipine?
A: Hypersensitivity to cilnidipine, cardiogenic shock, severe aortic stenosis, unstable angina, heart failure, and hypotension.
Q6: Does Clinidipine interact with other medications?
A: Yes, it interacts with CYP3A4 inhibitors/inducers, grapefruit juice, other antihypertensives, and antidiabetic medications.
Q7: What should patients be advised regarding lifestyle while taking Clinidipine?
A: Patients should limit alcohol intake, avoid grapefruit juice, and incorporate lifestyle modifications such as a low-salt diet and regular exercise.
Q8: How should Clinidipine be taken?
A: Orally, once daily, preferably after breakfast. Swallow the tablet whole with water. Do not crush or chew.
Q9: What should be done in case of a missed dose?
A: Take the missed dose as soon as remembered, unless it’s almost time for the next dose. Do not double the dose.
Q10: Can Cilnidipine be used in children?
A: The safety and effectiveness in children haven’t been established, and it’s generally not recommended.
