Dosing & Uses
Dosage Forms & Strengths
capsule, extended release
- 2.5mg
- 6.5mg
- 9mg
Angina Pectoris (Prophylaxis)
ER capsule: Initial 2.5-6.5 mg PO q6-8hr
Titrate up to effect dose until limited by SE
Renal Failure
CrCl: 10-50 mg/min: Administer q24-72hr
CrCl<10 mL/min: Administer q72-96hr
Not FDA approved
Angina Pectoris (Prophylaxis)
ER capsule: Initial 2.5-6.5 mg PO q6-8hrTitrate up to effec dose until limited by SE
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse 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
Hypersensitivity, acute MI, severe anemia
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
Coadministration with soluble guanylate cyclase stimulators, including riociguat
Cautions
Use caution in increased ICP (eg, head trauma, cerebral hemorrhage; potential contraindication), hyperthyroidism, increased IOP, postural hypotension, volume depletion, low systolic BP
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
Angina long term prophylaxis, NOT for acute relief
Lack of burning/tingling does not indicate loss of potency
Discontinue if blurred vision occurs
Use supportive treatment in overdose
Benefits of oral nitroglycerin in patients with acute myocardial infarction or congestive heart failure not established; if administered in these conditions, use careful clinical or hemodynamic monitoring to avoid hazards of hypotension and tachycardia; because effects of capsules are so difficult to terminate rapidly, not recommended in these settings
Severe hypotension, particularly with upright posture, may occur with even small doses; should be used with caution in patients who may be volume depleted or who, for whatever reason, are already hypotensive; hypotension induced by therapy may be accompanied by paradoxical bradycardia and increased angina pectoris
Therapy may aggravate angina caused by hypertrophic cardiomyopathy
As tolerance to other forms of nitroglycerin develops, effect of sublingual nitroglycerin on exercise tolerance, although still observable, is somewhat blunted
In industrial workers who have had long-term exposure to unknown (presumably high) doses of organic nitrates, tolerance clearly 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
Some clinical trials in angina patients have provided nitroglycerin for about 12 continuous hours of every 24-hour day; during nitrate-free intervals in some of these trials, anginal attacks have been more easily provoked than before treatment, and patients have demonstrated hemodynamic rebound and decreased exercise tolerance; importance of these observations not known
Pregnancy & 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
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
onset: within 1- hr4
Duration antianginal effects: Up to 12 hr
Bioavailability: 38.5%
Protein Bound: 11-60%
Vd: 3 L/kg
Metabolism: 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
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Formulary
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