What are the characteristics of Dihydropyridine (DHP) calcium channel blockers, including their names, mechanism of action, route of administration, dosage, half-life, adverse effects, and contraindications?

From the Guidelines

Dihydropyridine calcium channel blockers, such as Amlodipine and Nifedipine, are primarily used to treat hypertension and angina by selectively blocking L-type calcium channels in vascular smooth muscle, causing vasodilation and reducing peripheral vascular resistance. The main medications in this group include Amlodipine, Nifedipine, Felodipine, Nicardipine, Nisoldipine, and Lercanidipine. These drugs are administered orally, with dosages ranging from 5-10 mg once daily for Amlodipine 1 to 30-90 mg daily for Nifedipine 1. The half-life of these medications varies, with Amlodipine having a half-life of 30-50 hours and Nifedipine having a half-life of 2-5 hours 1.

Mechanism of Action and Route of Administration

• Dihydropyridines work by selectively blocking L-type calcium channels in vascular smooth muscle, causing vasodilation and reducing peripheral vascular resistance 1
• These drugs are administered orally, with dosages ranging from 5-10 mg once daily for Amlodipine to 30-90 mg daily for Nifedipine 1
• The route of administration is oral, and the dosage forms include immediate-release and extended-release formulations 1

Dosage and Half-Life

• Amlodipine is typically administered orally at 5-10 mg once daily with a half-life of 30-50 hours 1
• Nifedipine is given at 30-90 mg daily (extended-release) with a half-life of 2-5 hours 1
• Felodipine dosage ranges from 2.5-10 mg once daily with a half-life of 11-16 hours 1
• Nicardipine is dosed at 20-40 mg three times daily (immediate-release) or 30-60 mg twice daily (sustained-release) with a half-life of 2-4 hours 1
• Nisoldipine is given at 17-34 mg once daily with a half-life of 7-12 hours 1
• Lercanidipine is administered at 10-20 mg once daily with a half-life of 8-10 hours 1

Adverse Effects and Contraindications

• Common side effects include peripheral edema, headache, dizziness, flushing, and gingival hyperplasia 1
• These medications are contraindicated in patients with severe aortic stenosis, cardiogenic shock, unstable angina, and hypersensitivity to dihydropyridines 1
• Caution should be exercised when using these medications in patients with heart failure, severe hepatic impairment, or during pregnancy 1
• Immediate-release nifedipine should not be administered to patients with NSTE-ACS in the absence of beta-blocker therapy 1

From the FDA Drug Label

Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Felodipine is a member of the dihydropyridine class of calcium channel antagonists (calcium channel blockers) It reversibly competes with nitrendipine and/or other calcium channel blockers for dihydropyridine binding sites, blocks voltage-dependent Ca ++ currents in vascular smooth muscle and cultured rabbit atrial cells, and blocks potassium-induced contracture of the rat portal vein

The characteristics of Dihydropyridine (DHP) calcium channel blockers are:

• Names: Amlodipine, Felodipine
• Mechanism of action: Inhibition of transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle, blocking voltage-dependent Ca++ currents
• Route of administration: Oral (PO)
• Dosage: Not specified in the provided text
• Half-life:
  • Amlodipine: Not specified in the provided text
  • Felodipine: 11 to 16 hours (terminal half-life)
• Adverse effects: Not specified in the provided text
• Contraindications: Not specified in the provided text 2 3

From the Research

Characteristics of Dihydropyridine (DHP) Calcium Channel Blockers

• Names: Examples of Dihydropyridine calcium channel blockers include amlodipine and nifedipine 4
• Mechanism of Action: Dihydropyridine calcium channel blockers work by reducing calcium flux into cells, which dilates arteries and lowers blood pressure 5
• Route of Administration: The route of administration for Dihydropyridine calcium channel blockers is oral 6
• Dosage: The dosage of Dihydropyridine calcium channel blockers varies depending on the specific medication and the patient's condition, but they are often taken once daily 6
• Half-life: The half-life of Dihydropyridine calcium channel blockers can vary, with long-acting agents like amlodipine having a longer half-life than intermediate-acting agents 6
• Adverse Effects: Common adverse effects of Dihydropyridine calcium channel blockers include edema, headache, flushing, and tachycardia, while high doses of verapamil can cause constipation 5
• Contraindications: Dihydropyridine calcium channel blockers are contraindicated in patients with congestive heart failure 4

Pharmacological Differences

• Dihydropyridine vs Non-Dihydropyridine: Dihydropyridine calcium channel blockers are more vascular selective, while non-dihydropyridine calcium channel blockers are more myocardial selective and tend to reduce heart rate 4
• Short-acting vs Long-acting: Short-acting and long-acting forms of calcium channel antagonists have different clinical effects, with long-acting agents like amlodipine offering greater protection against major complications of hypertension 6

Therapeutic Applications

• Cardiovascular Disease: Dihydropyridine calcium channel blockers are used to treat cardiovascular disease, including hypertension, angina pectoris, and vasodilator activities 7
• Other Therapeutic Applications: Dihydropyridine derivatives have also shown antibacterial, anticancer, antileishmanial, anticoagulant, anticonvulsant, antitubercular, antioxidant, antiulcer, and neuroprotection properties, among others 7