VASODILATOR DOSING





Acronyms



Hydralazine
Apresoline®

Dosage forms

Tablet
  • 10 mg
  • 25 mg
  • 50 mg
  • 100 mg

Dosing

Hypertension
  • Starting: 40 - 100 mg/day given in 3 - 4 divided doses
  • Maintenance: 100 - 200 mg/day given in 3 - 4 divided doses
  • Max: 300 mg/day
  • Increase dose at an interval of 3 - 5 days
  • Food increases absorption. Take consistently either with or without food. [2,3]
Heart failure
  • In the V-HeFT I and II trials, hydralazine was dosed 37.5 mg four times a day for 2 weeks, then 75 mg four times a day
  • In the A-HeFT trial, hydralazine was initially dosed 37.5 mg three times a day, then increased to 75 mg three times a day if tolerated
  • Food increases absorption. Take consistently either with or without food. [2,3]
Kidney disease
  • Hydralazine has not been studied extensively in kidney disease. In one small study (N=49), severe kidney disease (CrCl 5 - 28 ml/min) did not affect hydralazine pharmacokinetics. Dose adjustments do not appear to be necessary in kidney disease. [9]
Liver disease
  • Hydralazine undergoes extensive liver metabolism. The effects of hepatic impairment on hydralazine have not been studied. Use caution.

Generic / Price

  • YES/$

Minoxidil
Loniten®

Dosage forms

Tablet
  • 2.5 mg
  • 10 mg
Topical

Dosing

Hypertension
  • Starting: 5 mg once daily
  • Maintenance: 10 - 40 mg/day
  • Max: 100 mg/day
  • May be given in 1 or 2 divided doses
  • Increase dose at intervals of 3 days
  • It is recommended that minoxidil be taken with a diuretic and beta blocker (see minoxidil side effects)
  • May take without regard to food
Hair loss (off-label)
Kidney disease
  • Minoxidil can exacerbate fluid retention in kidney disease. Start with lower doses and titrate slowly.
Liver disease
  • Minoxidil can exacerbate fluid retention in liver disease. Start with lower doses and titrate slowly.

Generic / Price

  • YES/$

Nitroglycerin aerosol spray
Nitromist®

Dosage forms

Aerosol
  • 0.4 mg/spray
  • Comes in 4.1g (90 sprays) and 8.5g (230 sprays) bottle

Dosing

Acute angina (chest pain)
  • 1 - 2 sprays on or under the tongue at the onset of pain. May repeat in 5 minutes if needed.
  • No more than 3 sprays are recommended within a 15-minute period
  • See quick-acting nitroglycerin dosing
  • May take without regard to food
Prevention of angina
  • 1 spray 5 - 10 minutes prior to engaging in activity
  • May take without regard to food
Kidney disease
  • No dose adjustment is necessary in kidney disease
Liver disease
  • Nitroglycerin undergoes metabolism in the liver and at sites outside of the liver. It has not been studied in liver disease.

Generic / Price

  • NO/$$$$

Other

  • Do not shake container
  • Spray onto or under the tongue
  • Prime bottle with 10 sprays initially. It will remain primed for 6 weeks. May be re-primed with 2 sprays if not used within 6 weeks.
  • Do not rinse mouth for 5 - 10 minutes following spray

Nitroglycerin SL powder
GoNitro™

Dosage forms

Sublingual powder
  • 400 mcg per packet
  • Comes in box with 12, 36, or 96 packets

Dosing

Acute angina (chest pain)
  • Administer one or two packets (400 mcg of NTG) under the tongue at the onset of an attack
  • One additional packet may be administered every five minutes as needed
  • No more than three packets are recommended within a 15-minute period
  • See quick-acting nitroglycerin dosing
Prevention of angina
  • 1 packet 5 - 10 minutes prior to engaging in activity
Kidney disease
  • No dose adjustment is necessary in kidney disease
Liver disease
  • Nitroglycerin undergoes metabolism in the liver and at sites outside of the liver. It has not been studied in liver disease.

Generic / Price

  • NO/$$$$

Other

  • Administer at rest, ideally in the sitting position
  • To administer, empty the contents of a packet under the tongue, close mouth and breath normally. Allow powder to dissolve without swallowing.
  • Do not rinse or spit for 5 minutes after dosing

Nitroglycerin SL tablet
Nitrostat®

Dosage forms

Sublingual tablet
  • 0.3 mg
  • 0.4 mg
  • 0.6 mg
  • Comes in bottle with 25 tablets

Dosing

Acute angina (chest pain)
Prevention of angina
  • 1 tablet 5 - 10 minutes prior to engaging in activity
  • May take without regard to food
Kidney disease
  • No dose adjustment is necessary in kidney disease
Liver disease
  • Nitroglycerin undergoes metabolism in the liver and at sites outside of the liver. It has not been studied in liver disease.

Generic / Price

  • YES/$

Other

  • Store in original container with cap screwed on tightly
  • Drug will lose potency when exposed to light and air

Nitroglycerin spray
Nitrolingual®

Dosage forms

Spray
  • 0.4 mg/spray
  • Comes in 4.9g (60 sprays) and 12g (200 sprays) bottle

Dosing

Acute angina (chest pain)
  • 1 - 2 sprays onto or under the tongue at the onset of pain. May repeat in 5 minutes if needed.
  • No more than 3 sprays are recommended within a 15-minute period
  • See quick-acting nitroglycerin dosing
  • May take without regard to food
Prevention of angina
  • 1 spray 5 - 10 minutes prior to engaging in activity
  • May take without regard to food
Kidney disease
  • No dose adjustment is necessary in kidney disease
Liver disease
  • Nitroglycerin undergoes metabolism in the liver and at sites outside of the liver. It has not been studied in liver disease.

Generic / Price

  • YES/$$

Other

  • Do not shake container
  • Spray onto or under the tongue
  • Avoid swallowing immediately after spray
  • Prime bottle with 5 sprays. It will remain primed for 6 weeks.
  • Do not rinse mouth for 5 - 10 minutes following spray

Isosorbide dinitrate IR
Isordil®

Dosage forms

Tablet
  • 5 mg
  • 10 mg
  • 20 mg
  • 30 mg
  • 40 mg

Dosing

Prevention of angina
  • Starting: 5 - 20 mg two to three times a day
  • Maintenance: 10 - 40 mg two to three times a day
  • Max: 160 mg/day
  • Daily dose free interval of at least 14 hours is advised to minimize tolerance
  • May take without regard to food
Heart failure
  • In the V-HeFT I and II trials, isosorbide dinitrate was dosed 20 mg four times a day for 2 weeks, then 40 mg four times a day
  • In the A-HeFT trial, isosorbide dinitrate was initially dosed 20 mg three times a day, then increased to 40 mg three times a day if tolerated
  • May take without regard to food
Kidney disease
  • No dose adjustment is necessary in kidney disease
Liver disease
  • Isosorbide dinitrate undergoes extensive first-pass metabolism in the liver and considerable extrahepatic metabolism. It has not been studied in liver disease. Use caution.

Generic / Price

  • YES/$

Isosorbide mononitrate IR
Monoket®, ISMO®

Dosage forms

Tablet, immediate-release
  • 10 mg
  • 20 mg

Dosing

Prevention of angina
  • Dosing: 20 mg twice a day with the doses given 7 hours apart
  • Max: 40 mg/day
  • A starting dose of 5 mg twice a day may be appropriate in smaller patients. This dose should be increased to 10 mg by the second or third day of therapy.
  • Tablets are scored
  • May take without regard to food
Kidney disease
  • No dose adjustment is necessary in kidney disease
Liver disease
  • No dose adjustment is necessary in liver disease

Generic / Price

  • YES/$

Isosorbide mononitrate ER
IMDUR®

Dosage forms

Tablet, extended-release
  • 30 mg
  • 60 mg
  • 120 mg

Dosing

Prevention of angina
  • Starting: 30 - 60 mg once daily
  • Maintenance: 60 - 120 mg once daily
  • Max: 240 mg/day
  • Take dose in morning
  • Tablets should not be chewed or crushed
  • May take without regard to food
Kidney disease
  • No dose adjustment is necessary in kidney disease
Liver disease
  • No dose adjustment is necessary in liver disease

Generic / Price

  • YES/$

Nitroglycerin ointment
Nitro-bid®

Dosage forms

Ointment
  • 2% ointment
  • Comes in 30 g and 60 g tube
  • Comes in box of 48 one gram foilpacs (one pack is equivalent to one inch of ointment)

Dosing

Prevention of angina
  • Starting: Apply 1/2 inch over area of truncal skin in morning and 6 hours later
  • Max: 2 inches per dose
  • Typically applied to chest. Do not rub into the skin. Coverage of an area approximately the size of the dose-measuring applicator (3 1/2" by 2 1/4") should be sufficient to obtain the desired clinical effects. A larger area may be used. Tape applicator in place.
  • Effective for about 7 hours
  • A 10 - 12 hour nitrate-free interval per day is recommended to prevent tolerance
Kidney disease
  • No dose adjustment is necessary in kidney disease
Liver disease
  • Nitroglycerin undergoes metabolism in the liver and at sites outside of the liver. It has not been studied in liver disease.

Generic / Price

  • Tube - NO/$
  • Foilpac (#48) - NO/$$

Nitroglycerin patch
Nitro-Dur®, Minitran®

Dosage forms

Patch
  • 0.1 mg/hr
  • 0.2 mg/hr
  • 0.3 mg/hr
  • 0.4 mg/hr
  • 0.6 mg/hr
  • 0.8 mg/hr
  • Comes in carton with 30 patches

Dosing

Prevention of angina
  • Starting: 0.2 - 0.4 mg/hr patch applied for 12 - 14 hours a day
  • Max: 0.8 mg/hr patch
  • A 10 - 12 hour patch-free interval per day is recommended to prevent tolerance
  • Apply to reasonably hair-free site. Typically applied to trunk. Avoid extremities below the knee or elbow, skin folds, scar tissue, burned or irritated areas. May shower with patch on.
  • After removing patch, skin may feel warm and appear red. This is normal.
Kidney disease
  • No dose adjustment is necessary in kidney disease
Liver disease
  • Nitroglycerin undergoes metabolism in the liver and at sites outside of the liver. It has not been studied in liver disease.

Generic / Price

  • 0.1, 0.2, 0.4, 0.6 mg/hr - YES/$
  • 0.3, 0.8 mg/hr - NO/$$$$

Bidil®
Hydralazine + isosorbide dinitrate

Dosage forms

Tablet
  • Isosorbide dinitrate - Hydralazine
    • 20 mg - 37.5 mg

Dosing

Heart failure in black patients
  • Starting: 1 tablet three times a day
  • Target: 2 tablets three times a day
  • Max: 2 tablets three times a day
  • Titrate dose as tolerated
  • See A-HeFT trial for more
  • Effect of food on absorption is unknown

Generic / Price

  • NO/$$$$

Other

  • Tablets are scored

NITRATE PHARMACOKINETICS

  • In chronic dosing, duration of effect is much shorter due to tolerance
Drug Onset of action Duration of effect
Nitroglycerin spray, tablet, powder 1 - 3 minutes around 25 minutes
Isosorbide dinitrate about 1 hour up to 8 hours after one dose
Isosorbide mononitrate about 1 hour up to 12 hours after one dose
Nitroglycerin ointment not rapid enough for acute angina up to 12 hours
Nitroglycerin patch steady-state reached in 2 hours up to 12 hours
QUICK-ACTING NITROGLYCERIN DOSING





DRUG INTERACTIONS


PRICE ($) INFO

  • $ = 0 - $50
  • $$ = $51 - $100
  • $$$ = $101 - $150
  • $$$$ = > $150
  • Pricing based on one month of therapy at standard dosing in an adult
  • Pricing based on information from GoodRX.com®
  • Pricing may vary by region and availability

BIBLIOGRAPHY