Adult: Initially, 15-20 mcg/min via slow infusion, then increased gradually by increments of 10-15 mcg/min until an adequate response is achieved.
Intravenous Unstable angina
Adult: Initially, 10 mcg/min via slow infusion, may increase in increments of 10 mcg/min at approx 30-minutes intervals according to patient response.
Intravenous Induction of hypotension or control of hypertension during surgery
Adult: Initially, 25 mcg/min via slow infusion, may be increased in increments of 25 mcg/min at 5-minute intervals. Usual dose range: 10-200 mcg/min, adjusted according to patient response. Max: 400 mcg/min.
Intravenous Congestive heart failure
Adult: Initially, 20-25 mcg/min via slow infusion, may be decreased to 10 mcg/min, or increased in increments of 20-25 mcg/min every 15-30 minutes until desired response is achieved.
Oral Angina pectoris
Adult: Prophylaxis: As extended-release cap: Initially, 2.5-6.5 mg 3-4 times daily, may be increased up to 26 mg 4 times daily if necessary.
Rectal Chronic anal fissure
Adult: As 0.2% ointment: Apply 1-1.5 cm strip of ointment into the anal canal tid. As 0.4% ointment: Apply 2.5 cm (approx 1.5 mg) 12 hourly for up to 8 weeks.
Sublingual Angina pectoris
Adult: Treatment for acute attacks: As tab: 300-600 mcg placed under the tongue; dose may be repeated at 5-minute intervals for a total of 3 doses. As aerosol spray (400 mcg/spray): 1-2 sprays under the tongue, then close the mouth, dose may be repeated at 5-minute intervals if require. Max: 3 doses. Prophylaxis: As tab: 300-600 mcg, 5-10 minutes prior to activities that may precipitate an attack. As aerosol spray (400 mcg/spray): 1 or 2 sprays, 5-10 minutes prior to activities that may precipitate an attack. Seek medical care if symptoms are not resolved after a total of 3 doses.
Topical/Cutaneous Angina pectoris
Adult: Prophylaxis: As 2% ointment: Apply 1-2 inches 3-4 hourly as necessary, onto convenient area of the skin (e.g. chest, thigh, or arm), spread thinly without rubbing in. May cover the area after application. Dose may be titrated according to patient tolerance.
Transdermal Angina pectoris
Adult: Prophylaxis: As monotherapy or in combination with other anti-anginal treatment: As patch releasing 5 or 10 mg/24 hours: Apply 1 patch daily onto a fresh area of skin (e.g. chest, upper arms, thigh or shoulder). Max: 20 mg daily. Alternatively, 0.2-0.4 mg/hour initially then titrate to 0.4-0.8 mg/hour. Patch may remain on skin for 12-14 hours, followed by 10-12 hours patch-off period.
Transdermal Extravasation injury, Phlebitis
Adult: Prophylaxis secondary to venous cannulation: As patch releasing 5 mg/24 hours: Apply 1 patch distal to the IV site, remove patch after 3-4 days, then apply replacement patch to a different area of the skin. Continue for as long as IV infusion is maintained.
Hướng dẫn pha thuốc
IV infusion: Dilute a vial labeled as containing 50 mg/50 mL to 450 mL NaCl 0.9% inj or dextrose 5% inj to provide a solution containing 100 mcg/mL.
Tương kỵ
Incompatible with phenytoin, alteplase, levofloxacin.
Chống chỉ định
Hypertrophic obstructive cardiomyopathy, increased intracranial pressure (e.g. cerebral haemorrhage, head trauma), inadequate cerebral circulation, severe anaemia, closed-angle glaucoma, severe hypotension (systolic blood pressure <90 mmHg), arterial hypoxaemia, severe/uncontrolled hypovolaemia, extreme bradycardia, migraine or recurrent headache, acute circulatory failure and shock, cardiogenic shock with inadequate end-diastolic pressure, myocardial insufficiency due to obstruction, aortic or mitral stenosis, pericardial tamponade, constrictive pericarditis, toxic pulmonary oedema. Concomitant use with phosphodiesterase type 5 inhibitors (e.g. sildenafil), and riociguat.
Thận trọng
Patients with cerebrovascular disease, lung disease or cor pulmonale, recent history of MI, hypothyroidism, hypoxaemia or ventilation/perfusion imbalance due to lung disease or ischaemic heart failure, hypothermia, malnutrition, volume depletion, pre-existing hypotension, orthostatic dysfunction. Patch/topical ointment: Not indicated for treatment of acute angina attacks. Avoid abrupt withdrawal. Severe renal and hepatic impairment. Elderly. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Severe hypotension, shock, paradoxical bradycardia, increased intracranial pressure, dose-related headache, methaemoglobinaemia, drug tolerance, hypoxaemia.
Ear and labyrinth disorders: Vertigo. Cardiac disorders: Tachycardia. Gastrointestinal disorders: Nausea, vomiting. General disorders and administration site conditions: Asthenia; application site reactions (e.g. irritation, rash, pruritus, erythema, burning or stinging sensation). Nervous system disorders: Dizziness, drowsiness, paraesthesia. Rarely, cerebral ischaemia. Psychiatric disorders: Restlessness. Vascular disorders: Orthostatic hypotension, flushing, syncope.
This drug may cause dizziness, light-headedness, headache, blurred vision, and postural hypotension; if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor blood pressure and heart rate.
Quá liều
Symptoms: Increased intracranial pressure with cerebral symptoms, colicky pain, diarrhoea, flushing, severe headache, dizziness, vertigo, reflex tachycardia, feeling of suffocation, hypotension, weak pulse, asthenia, pallor. Rarely, cyanosis, methaemoglobinaemia, shock with nausea, vomiting, weakness, sweating, syncope. Management: Supportive and symptomatic treatment. Assess vital signs and mental status. Elevate leg and/or lower the head of the patient to promote venous return during mild hypotension. Perform arterial blood gas estimation if patient is clinically cyanosed or if acidosis is present. Administer 1-2 mg/kg methylene blue IV over 5 minutes to treat methaemoglobinaemia (except for patient with G6PD deficiency or methaemoglobin reductase deficiency); oxygen if necessary.
Tương tác
Enhanced hypotensive effects with other vasodilators and antihypertensives (e.g. ACE inhibitors, β-blockers, calcium channel blockers, diuretics), neuroleptics, TCAs, MAOIs, sapropterin, sublingual apomorphine. Increased vasodilating effects with N-acetylcysteine. Reduced absorption of sublingual nitrates with drugs that cause dry mouth (e.g. anticholinergics). May increase serum concentrations of ergot derivatives (e.g. dihydroergotamine). May diminish anticoagulant effect of heparin. May accelerate plasma clearance of tissue plasminogen activators (IV). Potentially Fatal: Potentiated hypotensive effects with phosphodiesterase type 5 inhibitors (e.g. sildenafil, vardenafil, tadalafil) and riociguat.
Tương tác với thức ăn
Enhanced hypotensive effect with alcohol.
Ảnh hưởng đến kết quả xét nghiệm
May interfere with catecholamines and vanilmandelic acid measurement in the urine. May falsely elevate triglyceride assays dependent on glycerol oxidase (IV). May cause false decreased serum cholesterol with Zlatkis-Zak colour reaction.
Tác dụng
Description: Mechanism of Action: Glyceryl trinitrate forms free radical nitric oxide (NO) that stimulates guanylate cyclase which increases guanosine 3’5’ monophosphate (cGMP) in the smooth muscle, resulting in dephosphorylation of myosin light chains and relaxation of smooth muscles. It reduces cardiac oxygen demand by decreasing preload and may modestly reduce afterload; dilates coronary arteries and improves collateral flow to ischaemic regions. It also decreases sphincter tone and intra-anal pressure when administered rectally.
Synonym: Nitroglycerin. Onset: 1-3 minutes (sublingual); approx 60 minutes (modified-release cap); immediate (IV); 15-30 minutes (topical); approx 30 minutes (transdermal). Duration: Approx 25 minutes (sublingual); 4-8 hours (modified-release cap); 3-5 minutes (IV); 7 hours (topical); 10-12 hours (transdermal). Pharmacokinetics: Absorption: Rapidly absorbed from sublingual mucosa. Well absorbed from the gastrointestinal tract and through the skin. Absolute bioavailability: Approx 40% (sublingual). Distribution: Widely distributed into the body. Crosses placenta. Volume of distribution: Approx 3 L/kg. Plasma protein binding: 60%. Metabolism: Rapidly metabolised in the liver by reductase enzyme to glycerol di- and mononitrate metabolites, further metabolised to glycerol and organic nitrate; undergoes extensive first-pass effect and nonhepatic metabolism via RBCs and vascular walls. Excretion: Via urine (as inactive metabolites). Elimination half-life: Approx 1-4 minutes.
Đặc tính
Glyceryl trinitrate Source: National Center for Biotechnology Information. PubChem Database. Nitroglycerin, CID=4510, https://pubchem.ncbi.nlm.nih.gov/compound/Nitroglycerin (accessed on Jan. 23, 2020)
Bảo quản
Sublingual tab, rectal or topical ointment, transdermal patch, solution for infusion: Store below 25°C. Protect from light. Sublingual spray: Store between 20-25°C. Do not refrigerate or freeze. Modified-release cap: Store between 15-30°C. Protect from moisture.
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.
Tài liệu tham khảo
Anon. Nitroglycerin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 09/01/2020.Buckingham R (ed). Glyceryl Trinitrate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/01/2020.Glyceryl Trinitrate Tablets BP 600 mcg (Accord-UK Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 09/01/2020.Joint Formulary Committee. Glyceryl Trinitrate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/01/2020.Nitro-Time Capsule (Major Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/03/2020.Nitroglycerin Lingual Spray (Allegis Pharmaceuticals, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/01/2020.Nitroglycerin Tablet (Alvogen Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/01/2020.Nitroglycerin Transdermal System (Major Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/01/2020.Pharmacy Retailing (NZ) Ltd. Rectogesic 0.2% Ointment data sheet 20 January 2017. Medsafe. http://www.medsafe.govt.nz/. Accessed 09/01/2020.Rectogesic 4 mg/g Rectal Ointment (Kyowa Kirin Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 09/03/2020.Transiderm Nitro 5 (Novartis Pharmaceuticals UK Limited). MHRA. https://products.mhra.gov.uk/. Accessed 09/03/2020.
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