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CARDIOVASCULAR SYSTEM › CARDIAC THERAPY › VASODILATORS USED IN CARDIAC DISEASES › Organic nitrates
glyceryl trinitrate, combinations
C01DA52
Forms & Strengths
- Transdermal patches: 0.1 mg/hr, 0.2 mg/hr, 0.4 mg/hr, 0.8 mg/hr
- Sublingual tablets: 0.3 mg, 0.4 mg, 0.6 mg
- Sublingual spray: 0.4 mg/actuation
- Intravenous infusion: 5 mg/mL, 10 mg/mL, 25 mg/mL
- Ointment: 2% (15 mg/inch)
Adult Dosing
- Angina pectoris (Sublingual): 0.3 to 0.6 mg sublingually every 5 minutes as needed for up to 3 doses
- Angina prophylaxis (Patch): Apply 1 patch daily, remove after 10-12 hours to maintain nitrate-free interval
- Heart failure/ACS (IV infusion): Start at 5-10 mcg/min, titrate up by 5-20 mcg/min every 3-5 minutes as clinically indicated
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
- IV infusion (off-label for heart failure/hypertension): 0.25 to 5 mcg/kg/min titrated to response
Indications
- Acute relief of an anginal attack
- Prophylaxis of angina pectoris due to coronary artery disease
- Adjunctive treatment of heart failure associated with acute myocardial infarction
- Control of perioperative hypertension and induction of intraoperative hypotension
Mechanism of Action
- Converted to nitric oxide (NO) in vascular smooth muscle
- Activates intracellular guanylyl cyclase, increasing cyclic GMP
- Dephosphorylates myosin light chains, leading to vascular smooth muscle relaxation
- Preferentially dilates capacitance vessels (veins > arteries), reducing preload and myocardial oxygen demand
Contraindications
- Hypersensitivity to organic nitrates or formulation components
- Concurrent use with phosphodiesterase-5 (PDE-5) inhibitors (e.g., sildenafil, tadalafil, vardenafil)
- Concurrent use with soluble guanylate cyclase (sGC) stimulators (e.g., riociguat)
- Severe hypotension, uncorrected hypovolemia, or increased intracranial pressure
Adverse Reactions
- Common: Headache, dizziness, flushing, orthostatic hypotension, tachycardia
- Serious: Severe paradoxical bradycardia, profound hypotension, methemoglobinemia (high doses)
- Dermatologic: Contact dermatitis (transdermal patches)
- Tolerance: Diminished anti-anginal efficacy with continuous 24-hour administration
Drug Interactions
- PDE-5 inhibitors: Severe, potentially fatal hypotension due to synergistic vasodilation
- sGC stimulators: Contraindicated due to risk of severe hypotension
- Antihypertensive agents, alcohol, and beta-blockers: Additive hypotensive effects
- Dihydroergotamine: Increased bioavailability and hypertensive potential of ergotamine
Curated Content: Needs Vetting Before Put to Clinical Use