nitroglycerin transdermal (NitroDur, Minitran, Deponit, Transdermal Nitroglycerin, Nitrocine, glyceryl trinitrate transdermal)
Classes: Nitrates, Angina; Antianginal Agents; Vasodilators
Dosing and uses of NitroDur, Minitran (nitroglycerin transdermal)
Adult dosage forms and strengths
patch
- 0.1mg/hr
- 0.2mg/hr
- 0.3mg/hr
- 0.4mg/hr
- 0.6mg/hr
- 0.8mg/hr
Angina Pectoris
1 Patch qDay; Start with smallest unit in series & titrate
Patches may be applied to any skin surface, except on extremities below the knees or elbows
Nitrate-free period of 10-12 hours duration (overnight) needed to prevent tolerance
Minitran 0.1, 0.2, 0.4, 0.6 mg/hr
Nitro-Dur 0.1, 0.2, 0.3, 0.4, 0.6, 0.8 mg/hr
Transdermal-nitroglyderin 0.1, 0.2, 0.4, 0.6 mg/hr
Pediatric dosage forms and strengths
Not FDA approved in children
Geriatric dosage forms and strengths
Angina pectoris
1 Patch qDay; Start with smallest unit in series & titrate
Patches may be applied to any skin surface, except on extremities below the knees or elbows
Nitrate-free period of 10-12 hours duration (overnight) needed to prevent tolerance
Minitran 0.1, 0.2, 0.4, 0.6 mg/hr
Nitro-Dur 0.1, 0.2, 0.3, 0.4, 0.6, 0.8 mg/hr
Transdermal-nitroglyderin 0.1, 0.2, 0.4, 0.6 mg/hr
NitroDur, Minitran (nitroglycerin transdermal) adverse (side) effects
Common
Headache
Hypotension
Tachycardia
Dizziness
Lightheadedness
Blurred vision
Flushing
N/V
Nervousness
Xerostomia
Topical allergic reactions
Serious
Methemoglobinemia (rare)
Syncope
Prolonged bleeding time
Exfoliative dermatitis
Unstable angina
Rebound hypertension
Thrombocytopenia
Warnings
Contraindications
Hypersensitivity to organic nitrates or adhesives
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
Concomitant administration with guanylate stimulator riociguat (may cause hypotension)
Severe anemia
Cautions
Alcohol use, increased ICP (eg, head trauma, cerebral hemorrhage-potential contraindication), hyperthyroidism, hypertrophic cardiomyopathy, increased IOP, postural hypotension, volume depletion, low systolic Bp
Benefits of transdermal nitroglycerin in patients with acute myocardial infarction or congestive heart failure have not been established
Transdermal system should not be used to treat acute angina attacks
Severe hypotension, particularly with upright posture, may occur with even small doses of nitroglycerin, particularly in the elderly; use caution
Nitrate therapy may aggravate angina caused by hypertrophic cardiomyopathy, particularly in the elderly
Arcing may occur if defibrillator discharged through paddle electrode overlying transdermal patch
Discarded patches should be kept out of reach of children and pets
Chest pain, acute myocardial infarction, and even sudden death reported during temporary withdrawal of nitrates from industrial workers with long-term exposure to unknown high doses of organic nitrates
Pregnancy and lactation
Pregnancy category: C
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 NitroDur, Minitran (nitroglycerin transdermal)
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 activation of cGMP & vasodilation
Pharmacokinetics
Half-Life: 12-33 min
Onset: 60 min
Duration: 10-12 hr
Bioavailability: 75%
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, and glyceryl mononitrate (inactive)
Clearance: 5.5-11 L/min
Excretion: Urine
Dialyzable: No
