Glyceryl Trinitrate

Indications
Oral
Management of stable angina
Adult: As modified-release preparation: Up to 12.8 mg tid.
Sublingual
Acute angina
Adult: As tablet: 300-600 mcg, repeated if necessary. Seek medical help if pain persists after a total of 3 doses within 15 minutes. As aerosol spray: 1-2 sprays of 400 mcg each directed onto or under the tongue, closing the mouth after spraying. No more than 3 metered-doses to be taken at any one time and min of 15 minutes interval between consecutive treatments.
Buccal
Acute angina
Adult: 2-5 mg tid, placed between the gum and upper lip, increased if necessary. If the buccal tablet is accidentally swallowed, place another tablet in the buccal cavity.
Buccal
Heart failure
Adult: 5 mg placed between the gum and upper lip, repeated until symptoms are controlled. For chronic heart failure: 5-10 mg tid may be used.
Transdermal
Management of stable angina
Adult: Apply 1 patch (releasing 2.5-20 mg/24 hr) onto the chest, upper arms, thigh, abdomen or shoulder. Replace with a new patch every 24 hr and rotate sites of application with every new patch. Max: 20 mg daily.
Transdermal
Prophylaxis of phlebitis and extravasation secondary to venous cannulation
Adult: Apply one 5-mg patch distal to the IV site, replace patch at a different skin site either daily or after 3-4 days depending on the patch; continue for as long as the IV infusion is maintained.
Intravenous
Unstable angina
Adult: Initially, 5-10 mcg/minute. Usual range: 10-200 mcg/minute.
Intravenous
Heart failure
Adult: Initially, 5-25 mcg/minute.
Intravenous
Acute myocardial infarction
Adult: Initially, 5-25 mcg/minute, adjust according to patient's response. Usual range: 10-200 mcg/minute. Max: 400 mcg/minute.
Intravenous
Induction of hypotension or control of hypertension during surgery
Adult: Initially, 5-25 mcg/minute, adjust according to patient's response. Usual range: 10-200 mcg/minute. Max: 400 mcg/minute.
Topical/Cutaneous
Management of stable angina
Adult: As 2% ointment: Apply 0.5-2 inches (to the chest, arm, thigh or back) 3-4 times daily or every 3-4 hr, if necessary.
Rectal
Pain due to chronic anal fissure
Adult: As a 0.4% ointment: Apply 1.5 mg intra-anally every 12 hr for up to 8 wk.

Incompatibility: Y-site admin: Alteplase, levofloxacin. Admixture: Hydralazine, phenytoin.
Contraindications
Hypersensitivity. Severe hypotension, heart failure, marked anaemia, hypertrophic obstructive cardiomyopathy, cerebral haemorrhage or head trauma, low cardiac output secondary to hypovolaemia, inferior MI with right ventricular involvement, raised intracranial pressure. Concomitant use with phosphodiesterase type-5 inhibitors.
Warnings / Precautions
Severe hepatic or renal impairment, hypothyroidism, malnutrition, hypothermia. Cerebrovascular disease, lung disease or cor pulmonale. Pregnancy, lactation, glaucoma, mitral valve prolapse, cardiac tamponade, syncope. Gradual withdrawal in patients who have received prolonged high dose infusions. Avoid prolonged excessive hypotension. Nitrate-free interval is recommended in patients on continuous treatment with nitrates to reduce risk of tolerance.
Adverse Reactions
Facial flushing, dizziness, tachycardia, throbbing headache and tolerance. Large doses can cause vomiting, restlessness, hypotension, syncope, rarely cyanosis and methaemoglobinaemia, impaired respiration, bradycardia. IV admin: IV preparation contains substantial quantities of alcohol and alcohol intoxication can occur. Sublingual Tabs/Spray: Dry mouth, localised burning sensation. Topical: Contact dermatitis, erythema, local irritation. Transdermal patches: Contact dermatitis, metal-containing patches should be removed before cardioversion, defibrillation, diathermy. Buccal tablets: Delayed dissolution, may be swallowed by mistake.
Potentially Fatal: Hypotension, paradoxical bradycardia, impaired respiration, syncope and collapse.
Overdose Reactions
Symptoms include vasodilatation, venous pooling, reduced cardiac output and hypotension. May also include increased intracranial pressure, throbbing headache, confusion and moderate fever; vertigo; palpitation; visual disturbances; nausea, vomiting; syncope; air hunger and dyspnoea.
Drug Interactions
Enhances bioavailability of dihydroergotamine. Glyceryl trinitrate infusion may prolong pancuronium-induced neuromuscular blockade. May reduce the efficacy of heparin, alteplase and noradrenaline when used together. Efficacy of buccal and sublingual preparations may be reduced by drugs that can cause dry mouth due to decreased dissolution. Aspirin and other NSAIDs may reduce the therapeutic response to glyceryl trinitrate.
Potentially Fatal: Orthostatic hypotension may be produced by combined use of calcium channel blockers, antihypertensives, phenothiazines and TCAs. Alcohol may cause severe hypotension and collapse.
See Below for More glyceryl trinitrate Drug Interactions
Lab Interactions
May interfere with Zlatkis-Zak colour reaction, resulting in false report of decreased serum cholesterol.
Mechanism of Actions
Glyceryl trinitrate acts on the enzyme nitric oxide stimulating guanylate cyclase in the vascular smooth muscle cells resulting in the relaxation of smooth muscles. It reduces venous return (preload) and facilitates subendocardial blood flow with redistribution into ischaemic areas. It relieves coronary vasospasm and dilates arterioles reducing afterload. It is useful for relief and prevention of anginal attacks.
Onset: 1-3 minutes (sublingual, buccal); 30-60 minutes (transdermal, topical); 1-2 minutes (IV).
Duration: 30-60 minutes (sublingual); 3-5 hr (buccal, as modified-release preparations); 24 hr (transdermal); 8 hr (topical, as ointment); 3-5 minutes (IV).
Absorption: Rapidly absorbed from oral mucosa (sublingual), well absorbed from the GI tract (oral), well absorbed from the skin (topical, transdermal).
Distribution: Widely distributed: Smooth muscles of the blood vessels.
Metabolism: Extensive hepatic 1st pass metabolism by glutathione-organic nitrate reductase (yielding dinitrates and mononitrates); also undergoes hydrolysis in the plasma.
Excretion: Urine (as inactive metabolites).
Storage Conditions
Buccal: Store at 15-30°C. Intravenous: Store at 15-30°C. Oral: Store at 15-30 °C. Rectal: Store at 15-30°C. Sublingual: Store at 15-30 °C. Topical/Cutaneous: Store at 15-30°C. Transdermal: Store at 15-30°C.
ATC Classification
C01DA02 - glyceryl trinitrate ; Belongs to the class of organic nitrate vasodilators. Used in the treatment of cardiac disease.
C05AE01 - glyceryl trinitrate ; Belongs to the class of muscle relaxants. Used in the topical treatment for the treatment of hemorrhoids and anal fissures.
Storage
Buccal: Store at 15-30°C. Intravenous: Store at 15-30°C. Oral: Store at 15-30 °C. Rectal: Store at 15-30°C. Sublingual: Store at 15-30 °C. Topical/Cutaneous: Store at 15-30°C. Transdermal: Store at 15-30°C.
Available As
  • Glyceryl Trinitrate 0.2% w/w
  • Glyceryl Trinitrate 0.4 mg
  • Glyceryl Trinitrate 0.5 gm
  • Glyceryl Trinitrate 0.5 mg
  • Glyceryl Trinitrate 10 mg
  • Glyceryl Trinitrate 2%
  • Glyceryl Trinitrate 2.5 mg
  • Glyceryl Trinitrate 2.6 mg
  • Glyceryl Trinitrate 5 mg
  • Glyceryl Trinitrate 6.4 mg
  • Glyceryl Trinitrate 6.5 mg
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