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Nitroglycerin (GTN)

Antianginal / Vasodilatorprescriptionsublingual · inferred

Organic nitrate prodrug requiring mitochondrial ALDH2-mediated bioactivation to release nitric oxide (NO), activating soluble guanylyl cyclase → cGMP → smooth muscle relaxation. Potent venodilator at low doses, arteriolar dilator at higher doses. Extremely short half-life (1-4 min) due to rapid extrahepatic ALDH2 metabolism. Extensive first-pass (oral F ~1%); sublingual route bypasses first-pass (F ~40%). Absolute contraindication with PDE5 inhibitors (sildenafil, tadalafil) — fatal hypotension due to synergistic cGMP accumulation.

Projected serum levels — 0.40 mg, as needed (shown daily)

Nitroglycerin (GTN)
Nitroglycerin (GTN) modeled serum levels, 0.40 mg as needed (shown daily) over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 0.25 0.50 0.75 1 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1

Maintenance schedule: 0.40 mg as needed (shown daily) (sublingual).

Modeled steady state after ~1 days: peak ≈ 0.000 mg, trough ≈ 0.000 mg body load. Population-based estimate over 15 days for a 0.40 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Antianginal / Vasodilator
Route modeled
Sublingual
Model confidence
inferred
Half-life
3 min
Common dose
0.40 mg
Suggested maximum
2.4 mg/day
Reference dose range
0.30–2.4 mg (single dose)
Suggested cadence
as needed (shown daily)
Validated against
0.40 mg sublingual — Cmax 0.002 mg/L at 0.080 h

Research behind this entry

  1. GISSI-3: effects of lisinopril and transdermal glyceryl trinitrate singly and together on 6-week mortality and ventricular function after acute myocardial infarction Gruppo Italiano per lo Studio della Sopravvivenza nell'Infarto Miocardico · The Lancet, 1994 DOI

    Landmark 19,394-patient RCT in acute MI showing transdermal nitroglycerin produced no significant reduction in 6-week mortality (6.5% vs 6.9% control). Changed clinical practice by demonstrating routine nitrate use…

  2. Identification of the enzymatic mechanism of nitroglycerin bioactivation Chen Z, Zhang J, Stamler JS · Proceedings of the National Academy of Sciences, 2002 DOI

    Landmark discovery that mitochondrial aldehyde dehydrogenase (ALDH2) is the primary enzyme responsible for nitroglycerin bioactivation to NO. Explained the mechanism of nitrate tolerance (ALDH2 inactivation by oxidative…

2 published studies referenced in the app, each with a plain-language summary.