nitroglycerin translingual (Nitrolingual, glyceryl trinitrate translingual spray, NitroMist)
Classes: Nitrates, Angina; Antianginal Agents
- Dosing and uses of Nitrolingual, glyceryl trinitrate translingual spray (nitroglycerin translingual)
- Nitrolingual, glyceryl trinitrate translingual spray (nitroglycerin translingual) adverse (side) effects
- Warnings
- Pregnancy
- Pharmacology of Nitrolingual, glyceryl trinitrate translingual spray (nitroglycerin translingual)
Dosing and uses of Nitrolingual, glyceryl trinitrate translingual spray (nitroglycerin translingual)
Adult dosage forms and strengths
spray
- 0.4mg/spray
Angina
1-2 spray(s) PRN for angina, may repeat q3-5min, not to exceed 3 sprays in 15 minutes
Spray onto or under tongue; do not inhale, expectorate or rinse mouth for 5-10 minutes
Seek medical attention if pain persists after 3 doses in 15 minutes
Angina, Prophylaxis
1-2 sprays 5-10 minutes before activities likely to cause angina
Renal Failure
CrCl: 10-50 mg/min: Administer q24-72hr
CrCl<10 mL/min: Administer q72-96hr
Pediatric dosage forms and strengths
Not approved
Geriatric dosage forms and strengths
Angina
Angina1-2 spray(s) PRN for angina, may repeat q3-5min, not to exceed 3 sprays in 15 minutes
Spray onto or under tongue; do not inhale, expectorate or rinse mouth for 5-10 minutes
Seek medical attention if pain persists after 3 doses in 15 minutes
Angina, prophylaxis
1-2 sprays 5-10 minutes before activities likely to cause angina
Nitrolingual, glyceryl trinitrate translingual spray (nitroglycerin translingual) 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
Hypersensitivity
AMI, severe anemia
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
Soluble guanylate cyclase (sGC) stimulator, riociguat; coadministration may cause hypotension
Narrow angle glaucoma (controversial: may not be clinically significant)
Increased intracranial pressure
Circulatory failure or shock
Cautions
CHF, alcohol use, glaucoma, hyperthyroidism, hypertrophic cardiomyopathy, increased ICP (eg, head trauma, cerebral hemorrhage; potential contraindication), increased IOP, postural hypotension, volume depletion, low systolic Bp
Severe hypotension may occur with small doses especially in patients with constrictive pericarditis, aortic or mitral stenosis, volume depleted patients or that are already hypotensive; hypotension may be accompanied by paradoxical bradycardia and/or increased angina pectoris
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; excessive use my lead to development of tolerance
Inability to relieve chest pain after 3 doses may mean AMI-rush to ER if possible
Discontinue if blurred vision develops
Prime pump prior to first use or after prolonged nonuse
Use supportive treatment in overdose
May aggravate the angina caused by hypertrophic obstructive cardiomyopathy
Nitroglycerin produces dose-related headaches, especially at the start of nitroglycerin therapy, which may be severe and persistent but usually subside with continued use
Dose selection for elderly should start at low end of dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy
Pregnancy and lactation
Pregnancy category: C
Lactation: not known whether 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 Nitrolingual, glyceryl trinitrate translingual spray (nitroglycerin translingual)
Mechanism of action
Organic nitrate which causes systemic venodilation, decreasing preload
Cellular mechanism: nitrate enters vascular smooth muscle & converted to nitric oxide (NO) leading to production 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: 2 min
Duration: Up to 1 hr
Protein Bound: 11-60%
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