Nitroglycerin
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Nitroglycerin (glyceryl trinitrate, GTN)
Nitrostat, Nitrolingual, NitroMist, Nitro-Bid, Nitro-Dur, Minitran, Rectiv
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Summary
Classes
Common uses
Acute angina relief (SL, lingual spray)0, Angina prophylaxis (oral ER, transdermal)0, Acute cardiogenic pulmonary edema (IV)0, Hypertensive emergency (IV)0, Chronic anal fissure (topical Rectiv 0.4%)0
Pharmacy
Starting dose
SL 0.3-0.6 mg every 5 minutes up to 3 doses for acute angina (call EMS if not resolved after the third); IV infusion 5-10 mcg/min titrated; transdermal patch 0.2-0.4 mg/hr for 12-14 hours daily (nitrate-free interval prevents tolerance)
Preparations
SL 0.3, 0.4, 0.6 mg tablets; lingual spray 0.4 mg/spray; ER 2.5-9 mg capsules; transdermal patch 0.1-0.8 mg/hr; 2% ointment; 0.4% rectal ointment; 5 mg/mL IV
US FDA Max
Indication-specific; titrated to effect
Pharmacology
Routes
Sublingual, lingual spray, oral ER, transdermal, topical, rectal, IV
Onset
SL/spray: 1-3 minutes; IV: minutes; patch: 30-60 minutes
Duration
SL: 30 minutes; patch: 12-14 hours; IV continuous
Half-life
1-3 minutes (very short)[1]
Bioavailability
Highly route-dependent: SL bypasses first-pass; oral has extensive first-pass (used only for chronic ER preparations); transdermal predictable[1]
Pregnancy
Used in obstetric emergencies (uterine relaxation, severe hypertension) when needed; otherwise limited routine use.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Nitroglycerin is enzymatically denitrated (largely by mitochondrial aldehyde dehydrogenase, ALDH2) to release nitric oxide (NO), which activates soluble guanylyl cyclase, raises cGMP, and relaxes vascular smooth muscle predominantly in the venous capacitance bed (preload reduction) at low doses, with arterial vasodilation at higher doses.0 Phosphodiesterase-5 inhibitors (sildenafil, tadalafil, vardenafil) catastrophically potentiate nitrate-induced hypotension — concurrent use is absolutely contraindicated. Tolerance develops rapidly with continuous exposure; daily nitrate-free intervals (typically 8-12 hours) restore responsiveness[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Nitrostat (nitroglycerin sublingual tablets), Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021134s006lbl.pdf