Nitrendipine

Nitrendipine is a dihydropyridine-type calcium channel blocker that has been particularly well studied for the treatment of isolated systolic hypertension in older patients. The Syst-Eur trial showed that nitrendipine can reduce strokes by 42% and dementia by 50% in this patient group.

Nitrendipine is taken once or twice daily depending on the dose and is available as a generic and under the brand name Bayotensin®. It has an intermediate half-life and acts predominantly on the vascular muscle.

Nitrendipine blocks L-type calcium channels in the vascular muscle:

Mechanism of action:

• Blocks the influx of calcium into vascular smooth muscle cells
• Arteries and arterioles dilate
• Peripheral vascular resistance decreases
• Blood pressure falls – especially the systolic value

Special features:

• High vascular selectivity
• Little effect on the heart
• Intermediate half-life (8-12 hours)
• Taken once or twice daily, depending on the dose

Clinical significance: The Syst-Eur trial showed that in older patients with isolated systolic hypertension, nitrendipine:

• Reduces strokes by 42%
• Reduces dementia by 50%
• Lowers cardiovascular events by 31%

Onset of action: After 1-2 hours. Maximum effect after 1-2 weeks of regular use.

Nitrendipine is suitable for:

• Adults with high blood pressure
• In particular: isolated systolic hypertension in older patients

Especially recommended for:

• Older patients (over 60 years) with elevated systolic blood pressure
• When stroke prevention is the priority
• In combination with other blood pressure-lowering drugs

Not suitable:

• Unstable angina pectoris
• Acute myocardial infarction (first 4 weeks)
• Severe heart failure
• Severe aortic stenosis
• Pregnancy and breastfeeding

High blood pressure:

• Starting dose: 10 mg twice daily (morning and evening) or 20 mg once daily (morning)
• Usual dose: 10-20 mg twice daily
• Maximum dose: 20 mg twice daily (40 mg/day)

Older patients:

• Your doctor sets the dose individually. The lowest dose is 10 mg
• Slow dose increase

Available strengths:

• 10 mg, 20 mg tablets

How to take:

• Once or twice daily (morning and evening)
• Regardless of meals
• With sufficient water
• Avoid grapefruit juice

Notes:

• Regular blood pressure checks
• Headache and flushing may occur at the start – these usually improve
• Inform your doctor if facial redness is severe
• Do not stop abruptly (consult your doctor)

Nitrendipine must not be taken in cases of:

• Hypersensitivity to nitrendipine or other dihydropyridines
• Unstable angina pectoris
• Acute myocardial infarction (first 4 weeks)
• Severe heart failure
• Severe aortic stenosis
• Cardiogenic shock

Caution in:

• Hepatic impairment (slowed breakdown)
• Tachycardia (reflex increase in heart rate)
• Severe renal impairment

Pregnancy: Contraindicated. Not sufficiently studied in pregnancy.

Common (1-10%):

• Headache
• Facial redness (flushing)
• Dizziness
• Palpitations
• Ankle edema

Uncommon (0.1-1%):

• Gastrointestinal complaints
• Fatigue
• Tachycardia
• Skin rash

Rare:

• Gum overgrowth (gingival hyperplasia)
• Elevated liver enzymes
• Allergic reactions
• Chest pain
• Paresthesias

Note: Flushing and headache are common at the start of therapy, but usually improve after 1-2 weeks. Consult a doctor if symptoms persist.

Caution with:

• Grapefruit juice → increased nitrendipine levels (CYP3A4 inhibition)
• CYP3A4 inhibitors (ketoconazole, erythromycin) → enhanced effect
• CYP3A4 inducers (rifampicin, phenytoin) → reduced effect
• Other blood pressure-lowering drugs → increased hypotension
• Digoxin → slight increase in levels possible
• Cimetidine → increased nitrendipine levels

Combines well with:

• ACE inhibitors and sartans
• Beta blockers (prevent reflex tachycardia)
• Diuretics

Alcohol: Increases the blood pressure-lowering effect. Use caution with concurrent consumption.