Class: Nitrate, Antianginal
Dosage Forms. Capsule (Extended Release): 2.5 mg, 6.5 mg, 9 mg; Sublingual Tablet: 0.3 mg, 0.4 mg, 0.6 mg; Patch: 0.1 mg/h, 0.2 mg/h, 0.4 mg/h, 0.6 mg/h, 0.8 mg/h; Sublingual Spray: 0.4 mg/actuation; Ointment: 2%
Common FDA Label Indication, Dosing, and Titration.
1. Angina, prophylaxis: Extended release, 2.5-6.5 mg po tid-qid; Sublingual: 1 tab or 1-2 sprays 5-10 min before activity, which may induce angina; Transdermal 0.2-0.4 mg/h worn topically 12-14 h per day, may titrate to 0.8 mg/h worn topically
2. Angina, acute: Sublingual, 1 tab or 1-2 sprays at first sign of angina, repeat every 5 min if needed for total of 3 tabs in 15 min
Off-Label Uses. None
MOA. Nitroglycerin is believed to be converted to nitric oxide (NO) by vascular endothelium. NO activates guanylate cyclase, increasing cyclic GMP that in turn decreases intracellular calcium, resulting in direct relaxation of vascular smooth muscle. In myocardial ischemia, nitrates dilate large epicardial vessels, enhance collateral size and flow, and reduce coronary vasoconstriction.
Drug Characteristics: Nitroglycerine
Medication Safety Issues: Nitroglycerine
Drug Interactions: Nitroglycerine
Adverse Reactions: Nitroglycerine
Efficacy Monitoring Parameters. Decreased use of sublingual nitroglycerin to treat anginal episodes, reduction in angina episodes, reduction in anginal pain.
Toxicity Monitoring Parameters. Signs/symptoms of hypotension, problematic headaches, or decreasing efficacy (drug tolerance).
Key Patient Counseling Points. Sit prior to using sublingual tablets, lingual aerosol, or spray. Tablet should be dissolved under tongue or in buccal pouch at first sign of angina; do not swallow. Spray should be sprayed onto or under tongue; do not inhale; do not spit out or rinse mouth after use. Rise slowly from a sitting position in order to prevent lightheadedness. Allow a 10- to 12-h/d drug-free interval to avoid development of nitrate tolerance for both patches and extended-release capsules. Avoid concurrent use of alcohol, CNS depressants, antihypertensives, or other drugs which cause hypotension. Do not use with phosphodiesterase inhibitors, which may result in hypotension.
Clinical Pearls. Safety and efficacy not established in children. Patch contains aluminum, remove before MRI.