Glyceryl Trinitrate

Cardiac Therapy · Nitrate

Indications

Cap/Tab/Aerosol/Patch: Treatment and prophylaxis of angina, including variant angina. Injection: For the control of hypertension during cardiac surgery. Treatment of peri-operative myocardial ischaemia. Unresponsive congestive cardiac failure secondary to acute myocardial infarction. Unstable angina refractory to treatment with standard therapy.

Dosage

AEROSOL (Sprays: Translingual): Acute attack: Adults: 1 or 2 doses; max 3 per attack. Exercise-induced angina: Adults: 1 or 2 doses before exertion. Hold canister to mouth, spray under tongue and close mouth immediately. Precautions: Patients should not inhale spray. Children: Not recommended. INJECTION: IV: Adults: 5 mcg/min, increase by 5 mcg/min every 3-5 min to 20 mcg/min; if no response at 20 mcg/min increase by 10 mcg/min every 3-5 min, up to 200 mcg/min. Pulmonary hypertension: Children: Continuous infusion: Start 0.25-0.5 mcg/kg/min and titrate by 1 mcg/kg/min at 20 to 60 min intervals to desired effect. Usual dose: 1-3 mcg/kg/min; max 5 mcg/kg/min. ORAL: Adults: 2.5-9 mg 2-4 times daily up to 26 mg 4 times/day. Children: Not recommended. ORAL: BUCCAL: Adults: Initial 1 mg every 3-5 hr while awake (3 times day); titrate dosage upward if angina occurs with tablet in place.…

Administration

IV: Must be prepared in glass bottles & use special sets intended for nitroglycerin glass IV bottles & administration sets provided by manufacturer. Reconstitution: Standard diluent: 50 mg/250 mL D5W; 50 mg/500 mL D5W. Minimum volume: 100 mg/250 mL D5W, concentration should not exceed 400 mcg/mL. Compatibility: Stable in D5LR, D5 ½NS, D5NS, LR, ½ NS. Y-site administration: Drug to Drug IV Compatibility: Acyclovir, amikacin, amiodarone, aztreonam, bumetanide, calcium gluconate, cephazolin, ceftriaxone, cisatracurium, dexamethasone, diltiazem, diphenhydramine, dobutamine, dopamine, enalapril, epinephrine, esmolol, famotidine, fentanyl, fluconazole, furosemide, gentamicin, heparin, hydrocortisone, hydromorphone, imipenem, insulin regular, labetalol, linezolid, lorazepam, magnesium sulphate, methylprednisolone, metoclopramide, midazolam, milrinone, morphine, nitroprusside, norepinephrine,…

Adverse Effects

Postural hypotension, tachycardia (but paradoxical bradycardia also reported); throbbing headache, dizziness; less commonly nausea, vomiting, heartburn, flushing, asthaenia, fainting, tachycardia, GI upset, syncope, temporary hypoxaemia, rash, application site reactions with transdermal patches; very rarely angle-closure glaucoma. Injection specific side-effects include severe hypotension, diaphoresis, apprehension, restlessness, muscle twitching, retrosternal discomfort, palpitation, abdominal pain; prolonged administration has been associated with methaemoglobinaemia.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Risk cannot be ruled out. Lactation: Caution advised or effect undetermined. Contraindications: Hypersensitivity to nitrates, hypotensive conditions and hypovolaemia, hypertrophic cardiomyopathy, aortic stenosis, cardiac tamponade, constrictive pericarditis, mitral stenosis, toxic pulmonary oedema, head trauma, cerebral haemorrhage, cerebrovascular disease, marked anaemia, raised intracranial pressure, extreme bradycardia, closed-angle glaucoma, G6PD deficiency. Precautions: Hypothyroidism; malnutrition; hypothermia; recent history of myocardial infarction; heart failure due to obstruction; hypoxaemia or other ventilation and perfusion abnormalities, severe renal or hepatic impairment, orthostatic dysfunction, susceptibility to angle-closure glaucoma; metal-containing transdermal systems should be removed before magnetic resonance imaging procedures, cardioversion, or…

Interactions

Sildenafil, tadalafil, vardenafil, ethanol, heparin, alteplase, ergot alkaloids, PDE5 inhibitors, other vasodilators, hypotensive agents, NSAIDs, alcohol, TCADs, antipsychotics, opioid analgesics, sapropterin, riociguat.

Advice to Patient

Swallow E.R tablets or capsules with a full glass of water. Do not break, crush or chew them. For sublingual or buccal use, place tablet under tongue or in buccal pouch when angina starts and then sit or lie down. Do not swallow drug, let it dissolve. If angina is not relieved, place another tablet under tongue or in buccal pouch after 5 minutes and repeat if needed, for three doses total. If pain is not relieved after 20 minutes, seek emergency service. Do not inhale translingual spray. Before first use, press actuator button 10 times to prime container and then hold container upright with forefinger on top of actuator button. Open mouth, bring container as close as possible, press actuator button firmly to release spray onto or under tongue, and release button and immediately close mouth. Replace plastic cover on container and do not spit out the drug or rinse mouth for 5-10…

Pharmacokinetics

Onset of action: Sublingual tab: 1-3 min. Translingual spray: Similar to sublingual tab. Extended release: Approx. 60 min. Topical: 15-30 min. Transdermal: Approx. 30 min. IV: Immediate. Peak effect: Sublingual powd: 7 min. Sublingual tab: 5 min. Translingual spray: 4-15 min. Extended release: 2.5-4 hrs. Topical: Approx. 60 min. Transdermal: 120 min. IV: Immediate. Duration: Sublingual tab: At least 25 min. Translingual spray: Similar to sublingual tab. Extended release: 4-8 hrs. Topical: 7 hrs. Transdermal: 10-12 hrs. IV: 3-5 min. Metabolism: Extensive first-pass effect, hepatic as well as non-hepatic. Nonhepatic metabolism occurs via RBCs and vascular walls. Half-life elimination: Approx. 1-4 min. Excretion: Urine.

Brands with this active ingredient

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