nitroglycerin sublingual (Nitrostat, Nitrolingual Pumpspray, GoNitro, NitroQuick, glyceryl trinitrate sublingual, Sublingual Nitroglycerin)

Dosing and uses of Nitrostat, NitroQuick (nitroglycerin sublingual)

• Adult
• Pediatric
• Geriatric

 

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