Nitrates

Mechanism of Action

Works by relaxation of smooth muscle, producing a vasodilator effect on the peripheral veins and arteries with more prominent effects on the veins. Primarily reduces cardiac oxygen demand by decreasing preload (left ventricular end-diastolic pressure); may modestly reduce afterload; dilates coronary arteries and improves collateral flow to ischemic regions

Pharmacokinetics

Onset of action: Sublingual tablet: 1-3 minutes; Translingual spray: 2 minutes; Buccal tablet: 2-5 minutes; Sustained release: 20-45 minutes; Topical: 15-60 minutes; Transdermal: 40-60 minutes; I.V. drip: Immediate

Peak effect: Sublingual tablet: 4-8 minutes; Translingual spray: 4-10 minutes; Buccal tablet: 4-10 minutes; Sustained release: 45-120 minutes; Topical: 30-120 minutes; Transdermal: 60-180 minutes; I.V. drip: Immediate

Duration: Sublingual tablet: 30-60 minutes; Translingual spray: 30-60 minutes; Buccal tablet: 2 hours; Sustained release: 4-8 hours; Topical: 2-12 hours; Transdermal: 18-24 hours; I.V. drip: 3-5 minutes

Half-life elimination: 1-4 minutes

Isosorbide dinitrate (Isordil ®)	Isosorbide mononitrate (Ismo ®, Monoket ® )
Nitroglycerin ointment	Nitrobid
Nitroglycerin transdermal

Isosorbide dinitrate (Isordil ®)

Angina prophylaxis: 5 to 40 mg orally four times daily or 40 mg (sustained release) orally every 8 to 12 hours.

Congestive heart failure: Oral: Initial: 10 mg 3 times/day. Target: 40 mg 3 times/day. Maximum: 80 mg 3 times/day. Sublingual: 2.5-10 mg every 4-6 hours. Chewable tablet: 5-10 mg every 2-3 hours.

Supplied:
Capsule, sustained release (Dilatrate®-SR): 40 mg
Tablet: 5 mg, 10 mg, 20 mg, 30 mg, 40mg
Tablet, extended release (Isochron™): 40 mg
Sublingual tablet: 2.5 mg, 5 mg

Note: Tolerance to nitrate effects develops with chronic exposure. Dose escalation does not overcome this effect. Tolerance can only be overcome by short periods of nitrate absence from the body. Short periods (10-12 hours) of nitrate withdrawal help minimize tolerance. General recommendations are to take the last dose of short-acting agents no later than 7 PM; administer 2-3 times/day rather than 4 times/day. Sustained release preparations could be administered at times to allow a 15- to 17-hour interval between first and last daily dose. Example: Administer sustained release at 8 AM and 2 PM for a twice daily regimen.

Isosorbide mononitrate (Ismo ®, Monoket ® )

Dosing:
Angina:
Regular release tablet: 5-10 mg twice daily with the two doses given 7 hours apart (8am and 3pm) to decrease tolerance development - then titrate to 10 mg twice daily in first 2-3 days. Extended release tablet: Initial: 30-60 mg given in the morning as a single dose. Titrate upward as needed, giving at least 3 days between increases. Maximum daily single dose: 240 mg

Tolerance to nitrate effects develops with chronic exposure. Dose escalation does not overcome this effect. Tolerance can only be overcome by short periods of nitrate absence from the body. Short periods (10-12 hours) of nitrate withdrawal help minimize tolerance.

Supplied:
Regular release tablets: 10 mg, 20 mg. Extended release tablets: 30 mg, 60 mg, 120 mg

Nitroglycerin ointment:

Dosing:
Initially 0.5 inches q8h. Maintenance: 0.5 to 2 inches every 6 to 8 hours. Maximum: 4 inches every 4 to 6 hours. [0.5 inches = @ 7.5 mg]

Supplied:
Ointment, topical:
Nitro-Bid®: 2% [20 mg/g] (30 g, 60 g)

Nitrobid Extended Release Capsules

Dosing:
Initially 2.5mg orally 2 to 3 times daily. Titrate upward as needed. Usual dose: 2.5 to 9mg 2 to 4 times daily. Maximum: 26mg orally 4 times daily.

Supplied:
Capsule, extended release: 2.5 mg, 6.5 mg, 9 mg

Nitroglycerin transdermal

Dosing:
Initial: 0.2 to 0.4 mg/hour, titrate to doses of 0.4 to 0.8 mg/hour; tolerance is minimized by using a patch-on period of 12-14 hours and patch-off period of 10-12 hours

Supplied:
Transdermal system [once daily patch]: 0.1 mg/hour (30s); 0.2 mg/hour (30s); 0.4 mg/hour (30s); 0.6 mg/hour (30s)

Minitran™: 0.1 mg/hour (30s); 0.2 mg/hour (30s); 0.4 mg/hour (30s); 0.6 mg/hour (30s)

Nitrek®: 0.2 mg/hour (30s); 0.4 mg/hour (30s); 0.6 mg/hour (30s)

Nitro-Dur®: 0.1 mg/hour (30s); 0.2 mg/hour (30s); 0.3 mg/hour (30s); 0.4 mg/hour (30s); 0.6 mg/hour (30s); 0.8 mg/hour (30s)

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph. GlobalRPh Inc.

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