General Information

Nitrostat is an acceptable form of therapy for various circulatory disorders including angina, pulmonary hypertension, and congestive heart failure (administered as an intravenous drug). Nitrostat relaxes smooth muscle, which causes venous dilation and results in decreased stress on the heart. It also dilates the arteries leading to the heart which help to improve oxygen supply to the heart.

One tablet should be dissolved under the tongue or in the buccal pouch at the first sign of an acute anginal attack. The dose may be repeated approximately every five minutes until relief is obtained, up to a total of three tablets in a fifteen minute period. If pain persists past the fifteen minutes, a physician should be notified. These tablets may be used prophylactically five to ten minutes before engaging in activities which might precede an acute attack.

Clinical Results

Regimens in which nitroglycerin patches were worn for twelve hours daily have been studied in well-controlled trials for up to four weeks in duration. Beginning about two hours after application and continuing 10-12 hours after application, patches delivering at least 0.4 mg of nitroglycerin per hour consistently demonstrated greater antianginal activity than placebo. Low-dose patches have not been extensively studied, but in a large, well-controlled trial in which higher-dose patches were also studied, patches delivering 0.2 mg/hr had significantly less antianginal activity than placebo.

It is reasonable to believe that the rate of nitroglycerin absorption from patches may vary with the site of application, but this relationship has not been adequately studied.

Mechanism of Action

Nitroglycerin forms free radical nitric oxide (NO) which activates guanylate cyclase, resulting in an increase of guanosine 3'5' monophosphate (cyclic GMP) in smooth muscle and other tissues. These events lead to dephosphorylation of myosin light chains, which regulate the contractile state in smooth muscle, and result in vasodilation.

Additional Information

Patient Information:

When using the sublingual tablets - those placed under the tongue - you should feel a burning or tingling. This indicates the drug is effective. You should replace these tablets every six months to ensure they are effective. When using the paste or the patch, make sure to wash your hands after applying the medication to avoid getting the medication into the eyes. You may be asked to remove the patch during the night to provide a drug-free period for your body. When changing from one formulation to another, consult with your pharmacist or physician for proper dosage changes. (from RxList)