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USP DI Vol. II - NITRATES Oral (Systemic)

NITRATES Oral (Systemic)


Some commonly used brand names are:

In the U.S.?

  • Dilatrate-SR 1
  • IMDUR 2
  • ISDN 1
  • ISMO 2
  • Isordil Tembids 1
  • Isordil Titradose 1
  • Monoket 2
  • Nitrocot 3
  • Nitroglyn E-R 3
  • Nitro-par 3
  • Nitro-time 3
  • Nitrong 3
  • Sorbitrate 1

In Canada?

  • Apo-ISDN 1
  • Cedocard-SR 1
  • Coradur 1
  • Coronex 1
  • IMDUR 2
  • ISMO 2
  • Isordil Titradose 1
  • Nitrong SR 3

Another commonly used name is:

  • Glyceryl trinitrate

Note:

For quick reference, the following nitrates are numbered to matchthe corresponding brand names.

This information applies to the following medicines:
1.Isosorbide Dinitrate (eye-soe-SOR-bide dye-NYE-trate)??
2.Isosorbide Mononitrate (eye-soe-SOR-bide mon-oh-NYE-trate)
3.Nitroglycerin (nye-troe-GLI-ser-in)?
? Generic name product may be available in the U.S.
? Generic name product may be available in Canada

Note:

This information does not apply to amylnitrite or mannitol hexanitrate.


Category

  • Antianginal?IsosorbideDinitrate; Isosorbide Mononitrate; Nitroglycerin
  • Vasodilator,congestive heart failure?Isosorbide Dinitrate; Nitroglycerin

Description

Nitrates (NYE-trates) are used to treat the symptomsof angina (chest pain). Depending on the type of dosage form and how it istaken, nitrates are used to treat angina in three ways:

  • to relieve an attack that is occurring by using the medicine whenthe attack begins;
  • to prevent attacks from occurring by using the medicine just beforean attack is expected to occur; or
  • to reduce the number of attacks that occur by using the medicineregularly on a long-term basis.

When taken orally and swallowed, nitrates are used to reduce the numberof angina attacks that occur. They do not act fast enough to relieve the painof an angina attack.

Nitrates work by relaxing blood vessels and increasing the supply of bloodand oxygen to the heart while reducing its work load.

Nitrates may also be used for other conditions as determined by your doctor.

The nitrates discussed here are available only with your doctor's prescription,in the following dosage forms:

    Oral
  • Isosorbide dinitrate
    • Extended-release capsules (U.S.)
    • Tablets (U.S. and Canada)
    • Chewable tablets (U.S.)
    • Extended-release tablets (U.S. and Canada)
  • Isosorbide mononitrate
    • Extended-release tablets (U.S.)
    • Tablets (U.S.)
  • Nitroglycerin
    • Extended-release capsules (U.S.)
    • Extended-release tablets (U.S. and Canada)


Before Using This Medicine

In deciding to use a medicine,the risks of taking the medicine must be weighed against the good it willdo. This is a decision you and your doctor will make. For nitrates, the followingshould be considered:

Allergies?Tell your doctor if you have ever had any unusual orallergic reaction to nitrates or nitrites. Also tell your health care professionalif you are allergic to any other substances, such as certain foods, preservatives,or dyes.

Pregnancy?Nitrates have not been studied in pregnant women.However, studies in rabbits given large doses of isosorbide dinitrate haveshown adverse effects on the fetus. Before taking these medicines, make sureyour doctor knows if you are pregnant or if you may become pregnant.

Breast-feeding?It is not known whether these medicines pass intobreast milk. Although most medicines pass into breast milk in small amounts,many of them may be used safely while breast-feeding. Mothers who are takingthese medicines and who wish to breast-feed should discuss this with theirdoctor.

Children?Studies on these medicines have been done only inadult patients, and there is no specific information comparing use of nitratesin children with use in other age groups.

Older adults?Dizziness or lightheadedness may be more likely tooccur in the elderly, who may be more sensitive to the effects of nitrates.

Other medicines?Although certain medicines should not be usedtogether at all, in other cases two different medicines may be used togethereven if an interaction might occur. In these cases, your doctor may want tochange the dose, or other precautions may be necessary. When you are takingnitrates, it is especially important that your health care professional knowif you are taking any of the following:

  • Antihypertensives (high blood pressure medicine) or
  • Other heart medicine?May increase the effects of nitrates onblood pressure
  • Sildenafil (e.g., Viagra) or
  • Tadalafil (e.g., Cialis) or
  • Vardenafil (e.g., Levitra)?These medicines which treat sexualimpotence should not be used together with nitrates.You should tell your doctor right away if you are taking one of these drugs.

Other medical problems?The presence of other medicalproblems may affect the use of nitrates. Make sure you tell your doctor ifyou have any other medical problems, especially:

  • Anemia (severe)
  • Glaucoma?May be worsened by nitrates
  • Head injury (recent) or
  • Stroke (recent)?Nitrates may increase pressure in the brain,which can make problems worse
  • Heart attack (recent)?Nitrates may lower blood pressure, whichcan aggravate problems associated with heart attack
  • Kidney disease or
  • Liver disease?Effects may be increased because of slower removalof nitroglycerin from the body
  • Overactive thyroid

Proper Use of This Medicine

Take this medicine exactly as directed by your doctor. It will workonly if taken correctly.

This form of nitrate is used to reduce the number ofangina attacks. In most cases, it will not relieve an attack that has alreadystarted because it works too slowly (the extended-release form releasesmedicine gradually over a 6-hour period to provide its effect for 8 to 10hours). Check with your doctor if you need a fast-acting medicine to relievethe pain of an angina attack.

Take this medicine with a full glass (8 ounces) ofwater on an empty stomach. If taken either 1 hour before or 2 hoursafter meals, it will start working sooner.

Extended-release capsules and tablets are not to bebroken, crushed, or chewed before they are swallowed. If broken up,they will not release the medicine properly.

Dosing?The dose of nitrates will be different fordifferent patients. Follow your doctor's orders or thedirections on the label. The following information includes only theaverage doses of nitrates. If your dose is different,do not change it unless your doctor tells you to do so.

The number of capsules or tablets that you take depends on the strengthof the medicine. Also, the number of doses you take eachday, the time allowed between doses, and the length of time you take the medicinedepend on the medical problem for which you are taking nitrates.

    For isosorbide dinitrate
  • For angina (chest pain):
    • For regular (short-acting) oral dosageforms (capsules or tablets):
      • Adults?5 to 40 mg four times a day.
      • Children?Dose must be determined by your doctor.
    • For long-acting oral dosage forms (extended-releasecapsules or tablets):
      • Adults?20 to 80 mg every eight to twelve hours.
      • Children?Dose must be determined by your doctor.
    For isosorbide mononitrate
  • For angina (chest pain):
    • For regular (short-acting) oral dosageform (tablets):
      • Adults?20 mg two times a day. The two doses should be takenseven hours apart.
      • Children?Use and dose must be determined by your doctor.
    • For long-acting oral dosage forms (extended-releasetablets):
      • Adults?30 to 240 mg once a day.
      • Children?Use and dose must be determined by your doctor.
    For nitroglycerin
  • For angina (chest pain):
    • For long-acting oral dosage forms (capsulesor tablets):
      • Adults?2.5 to 9.0 mg every eight to twelve hours.
      • Children?Dose must be determined by your doctor.

Missed dose?If you are taking this medicine regularly and youmiss a dose, take it as soon as possible. However, if the next scheduled doseis within 2 hours (or within 6 hours for extended-release capsules or tablets),skip the missed dose and go back to your regular dosing schedule. Do not doubledoses.

Storage?To store this medicine:

  • Keep out of the reach of children.
  • Store away from heat and direct light.
  • Do not store in the bathroom, near the kitchen sink, or in otherdamp places. Heat or moisture may cause the medicine to break down.
  • Do not keep outdated medicine or medicine no longer needed. Be surethat any discarded medicine is out of the reach of children.

Precautions While Using This Medicine

Do nottake sildenafil (e.g., Viagra), tadalafil (e.g., Cialis), or vardenafil (e.g.,Levitra) if you are taking this medicine. When sildenafil, tadalafil, or vardenafilare taken with nitrates, the combination can lower blood pressure and causedizziness, lightheadedness, or fainting. In some cases,sildenafil, tadalafil, or vardenafil taken with nitrates has caused death. If you are taking sildenafil, tadalafil, or vardenafil and you experiencean angina attack, you must go to the hospital right away.

If you have been taking this medicine regularly forseveral weeks or more, do not suddenly stop using it. Stopping suddenlymay bring on attacks of angina. Check with your doctor for the best way toreduce gradually the amount you are taking before stopping completely.

Dizziness, lightheadedness, or faintness may occur, especially when you get up quickly from a lying or sitting position.Getting up slowly may help. If you feel dizzy, sit or lie down.

The dizziness, lightheadedness, or fainting is also more likely to occurif you drink alcohol, stand for long periods of time, exercise, or if theweather is hot. While you are taking this medicine, becareful to limit the amount of alcohol you drink. Also, use extra care duringexercise or hot weather or if you must stand for long periods of time.

After taking a dose of this medicine you may get aheadache that lasts for a short time. This is a common side effect,which should become less noticeable after you have taken the medicine fora while. If this effect continues, or if the headaches are severe, check withyour doctor.

For patients taking the extended-release dosage formsof isosorbide dinitrate:

  • Partially dissolved tablets have been found in the stools of a fewpatients taking the extended-release tablets. Be alert to this possibility,especially if you have frequent bowel movements, diarrhea, or digestive problems.Notify your doctor if any such tablets are discovered. The tablets must beproperly digested to provide the correct dose of medicine.


Side Effects of This Medicine

Along with its needed effects, a medicine may cause some unwanted effects.Although not all of these side effects may occur, if they do occur they mayneed medical attention.

Check with your doctor as soon as possible if any of the following sideeffects occur:

    Rare

      Blurred vision; dryness of mouth; headache (severe or prolonged); skinrash

    Signs and symptoms of overdose (in the order in which they may occur)

      Bluish-colored lips, fingernails, or palms of hands; dizziness (extreme) or fainting; feelingof extreme pressure in head; shortness of breath; unusual tiredness or weakness; weak and fast heartbeat; fever; convulsions (seizures)

Other side effects may occur that usually do not need medicalattention. These side effects may go away during treatment as your body adjuststo the medicine. However, check with your doctor if any of the following sideeffects continue or are bothersome:

    More common

      Dizziness or lightheadedness, especially when getting up froma lying or sitting position; fast pulse; flushing of face and neck; headache; nausea or vomiting; restlessness

Other side effects notlisted above may also occur in some patients. If you notice any other effects,check with your doctor.


Revised: 10/14/2004