nitroglycerin translingual (Nitrolingual, glyceryl trinitrate translingual spray, NitroMist)

Dosing and uses of Nitrolingual, glyceryl trinitrate translingual spray (nitroglycerin translingual)

• Adult
• Pediatric
• Geriatric

 

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