nitroglycerin sublingual (Nitrostat, Nitrolingual Pumpspray, GoNitro, NitroQuick, glyceryl trinitrate sublingual, Sublingual Nitroglycerin)
Classes: Nitrates, Angina
Dosing and uses of Nitrostat, NitroQuick (nitroglycerin sublingual)
Adult dosage forms and strengths
tablet, SL
- 0.3mg
- 0.4mg
- 0.6mg
powder, SL (GoNitro)
- 0.4mg
Angina Pectoris (Acute Relief)
0.3-0.6 mg SL q5min up to 3 times; use at first sign of angina
Prompt medical attention needed if no relief
Dissolve under tongue or in buccal pouch; do not rinse mouth or spit for 5 minutes after administration
Angina Pectoris (Prophylaxis)
1 tablet SL 5-10 minutes before activities likely to provoke angina attacks
Renal Failure
CrCl: 10-50 mg/min: Administer q24-72hr for prophylaxis
CrCl <10 mL/min: Administer q72-96hr for prophylaxis
Pediatric dosage forms and strengths
Not FDA approved
Geriatric dosage forms and strengths
Angina Pectoris (Acute Relief)
0.3-0.6 mg SL q5min up to 3 times; use at first sign of angina
Prompt medical attention needed if no relief
Dissolve under tongue or in buccal pouch; do not rinse mouth or spit for 5 minutes after adminstration
Angina Pectoris (Prevention)
1 tablet SL 5-10 minutes before activities likely to provoke angina attacks
Nitrostat, NitroQuick (nitroglycerin sublingual) adverse (side) effects
Common
Headache
Hypotension
Tachycardia
Dizziness
Lightheadedness
Blurred vision
Flushing
N/V
Nervousness
Xerostomia
Serious
Methemoglobinemia (rare)
Syncope
Prolonged bleeding time
Exfoliative dermatitis
Unstable angina
Rebound hypertension
Thrombocytopenia
Warnings
Contraindications
Early myocardial infarction, severe anemia, increased intracranial pressure, and known hypersensitivity to nitroglycerin
Recent use (within several days) of PDE-5 inhibitors (eg, avanafil, sildenafil, tadalafil, or vardenafil) may cause dangerously low hypotension; the time course of the interaction appears to be related to the PDE-5 inhibitor half-life
Riociguat; coadministration may cause hypotension
Narrow angle glaucoma (controversial: may not be clinically significant)
Cautions
Caution in MI or CHF, alcohol use, increased ICP (eg, head trauma, cerebral hemorrhage; potential contraindication), hyperthyroidism, hypertrophic cardiomyopathy, increased IOP, postural hypotension, volume depletion, low systolic Bp
Inability to relieve chest pain after 3 doses indicates acute MI-rush to ER if possible
Lack of burning/tingling does not indicate loss of potency
Store in original container at room temp; protect from moisture
Discard unused tabs 6 months after bottle opened
Do not change brands unintentionally as not all are bioequivalent
Treat drug-induced headache with aspirin or acetaminophen
Provide nitrate-free interval (10-12 hr or overnight) to avoid development of tolerance
Benefits of sublingual nitroglycerin in patients with acute myocardial infarction or congestive heart failure not established; if one elects to use nitroglycerin in these conditions, careful clinical or hemodynamic monitoring must be used because of possibility of hypotension and tachycardia
Use smallest dose required for effective relief acute anginal attack; excessive use may lead to development of tolerance
Sublingual tablets should not be swallowed
Hypotension induced by nitroglycerin may be accompanied by paradoxical bradycardia and increased angina pectoris
May aggravate angina caused by hypertrophic cardiomyopathy
Industrial workers who have had long-term exposure to unknown (presumably high) doses of organic nitrates, tolerance rarely occurs; chest pain, acute myocardial infarction, and even sudden death have occurred during temporary withdrawal of nitrates from these workers, demonstrating existence of true physical dependence
Discontinue drug if blurring of vision or drying of mouth occurs; excessive dosage of nitroglycerin may produce severe headaches
Pregnancy and lactation
Pregnancy category: B
Lactation: Not known whether the drug crosses into breast milk, use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Nitrostat, NitroQuick (nitroglycerin sublingual)
Mechanism of action
Organic nitrate which causes systemic venodilation, decreasing preload
Cellular mechanism: nitrate enters vascular smooth muscle and converted to nitric oxide (NO) leading to activation of cGMP & vasodilation
Relaxes smooth muscle via dose-dependent dilation of arterial and venous beds to reduce both preload and afterload, and myocardial O2 demand
Also improves coronary collateral circulation. Lower BP, increase HR, occasional paradoxical bradycardia
Pharmacokinetics
Half-Life: 1-4 min
Onset: 1-3 min (antianginal and hemodynamic effects)
Duration of antianginal effects: Up to 30 min
Duration of hemodynamic effects: Up to 30 min
Bioavailability: 38.5%
Protein bound: 60%
Vd: 3 L/kg
Metabolism: Mainly in liver, extrahepatic sites (vascular wall, RBC)
Metabolites: 1,3-glyceryl dinitrate, 1,2-glyceryl dinitrate, & glyceryl mononitrate (inactive)
Clearance: 5.5-11 L/min
Excretion: Urine
Dialyzable No