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USP DI Vol. II - ANTIGLAUCOMAAGENTS, CHOLINERGIC, LONG-ACTING (Ophthalmic)

ANTIGLAUCOMAAGENTS, CHOLINERGIC, LONG-ACTING (Ophthalmic)


Some commonly used brand names are:

In the U.S.?

  • Humorsol 1
  • Phospholine Iodide 2

In Canada?

  • Phospholine Iodide 2
  • Diflupyl 3
  • Other commonly used names are: DFP, difluorophate, dyflos, and ecothiopate

    Note:

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

    This information applies to the following medicines:
    1.Demecarium (dem-e-KARE-ee-um)?
    2.Echothiophate (ek-oh-THYE-oh-fate)
    3.Isoflurophate (eye-soe-FLURE-oh-fate)*?
    * Not commercially available in the U.S.
    ? Not commercially available in Canada

    Category

    • Antiglaucoma agent, ophthalmic?Demecarium; Echothiophate; Isoflurophate
    • Cyclostimulant, accommodative esotropia?Demecarium; Echothiophate; Isoflurophate
    • Diagnostic aid, accommodative esotropia?Demecarium; Echothiophate; Isoflurophate

    Description

    Demecarium, echothiophate, and isoflurophate are used in theeye to treat certain types of glaucoma and other eye conditions, such as accommodativeesotropia. They may also be used in the diagnosis of certain eye conditions,such as accommodative esotropia.

    These medicines are available only with your doctor's prescription, inthe following dosage forms:

      Ophthalmic
    • Demecarium
      • Ophthalmic solution (eye drops) (U.S.)
    • Echothiophate
      • Ophthalmic solution (eye drops) (U.S. and Canada)
    • Isoflurophate
      • Ophthalmic ointment (eye ointment) (France)


    Before Using This Medicine

    In deciding to use a medicine,the risks of using the medicine must be weighed against the good it will do.This is a decision you and your doctor will make. For demecarium, echothiophate,or isoflurophate, the following should be considered:

    Allergies?Tell your doctor if you have ever had any unusual orallergic reaction to demecarium, echothiophate, or isoflurophate. Also tellyour health care professional if you are allergic to any other substances,such as preservatives.

    Pregnancy?Because of the toxicity of these medicines in general,demecarium, echothiophate, and isoflurophate are not recommended during pregnancy.

    Breast-feeding?Demecarium, echothiophate, and isoflurophate maybe absorbed into the body. These medicines are not recommended during breast-feeding,because they may cause unwanted effects in nursing babies. It may be necessaryfor you to use another medicine or to stop breast-feeding during treatment.Be sure you have discussed the risks and benefits of the medicine with yourdoctor.

    Children?Demecarium, echothiophate, or isoflurophate can causeserious side effects in any patient. When this medicine is used for a longtime, eye cysts may occur. These eye cysts occur more often in children thanin adults. Therefore, it is especially important that you discuss with thechild's doctor the good that this medicine may do as well as the risks ofusing it.

    Older adults?Many medicines have not been studied specificallyin older people. Therefore, it may not be known whether they work exactlythe same way they do in younger adults or if they cause different side effectsor problems in older people. There is no specific information comparing useof these medicines in the elderly with use in other age groups. However, demecarium,echothiophate, or isoflurophate can cause serious side effects in any patient.

    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 takingdemecarium, echothiophate, or isoflurophate, it is especially important thatyour health care professional know if you are taking any of the following:

    • Amantadine (e.g., Symmetrel) or
    • Anticholinergics (medicine for abdominal or stomach spasms or cramps)or
    • Antidepressants (medicine for depression) or
    • Antidyskinetics (medicine for Parkinson's disease or other conditionsaffecting control of muscles) or
    • Antihistamines or
    • Antimyasthenics (ambenonium [e.g., Mytelase], neostigmine [e.g.,Prostigmin], pyridostigmine [e.g., Mestinon]) or
    • Antipsychotics (medicine for mental illness) or
    • Buclizine (e.g., Bucladin) or
    • Carbamazepine (e.g., Tegretol) or
    • Cyclizine (e.g., Marezine) or
    • Cyclobenzaprine (e.g., Flexeril) or
    • Disopyramide (e.g., Norpace) or
    • Flavoxate (e.g., Urispas) or
    • Ipratropium (e.g., Atrovent) or
    • Meclizine (e.g., Antivert) or
    • Methylphenidate (e.g., Ritalin) or
    • Orphenadrine (e.g., Norflex) or
    • Oxybutynin (e.g., Ditropen) or
    • Procainamide (e.g., Pronestyl) or
    • Promethazine (e.g., Phenergan) or
    • Quinidine (e.g., Quinidex) or
    • Trimeprazine (e.g., Temaril)?May increase the possibility ofside effects or toxic effects; use of these medicines with demecarium, echothiophate,or isoflurophate is not recommended except under close supervision by yourdoctor
    • Malathion (topical) (e.g., Prioderm)?May increase the possibilityof side effects or toxic effects, especially if large amounts of malathionare used

    Pesticides or insecticides?Make sure you tell your doctor if you have been exposed recently to pesticidesor insecticides.

    Other medical problems?The presence of other medical problems may affectthe use of demecarium, echothiophate, or isoflurophate. Make sure you tellyour doctor if you have any other medical problems, especially:

    • Asthma or
    • Epilepsy or
    • Heart disease or
    • High or low blood pressure (severe) or
    • Myasthenia gravis or
    • Overactive thyroid or
    • Parkinsonism or
    • Stomach ulcer or other stomach problems or
    • Urinary tract blockage?If this medicine is absorbed into thebody, it may make the condition worse
    • Down's syndrome (mongolism)?This medicine may cause these childrento become hyperactive
    • Eye disease or problems (other)?May increase absorption ofthis medicine into the body or this medicine may make the condition worse

    Proper Use of This Medicine

    To use the ophthalmic solution (eye drops) form of this medicine:

    • First, wash your hands. Tilt the head back and, pressing your fingergently on the skin just beneath the lower eyelid, pull the lower eyelid awayfrom the eye to make a space. Drop the medicine into this space. Let go ofthe eyelid and gently close the eyes. Do not blink. Keep the eyes closed andapply pressure to the inner corner of the eye with your finger for 1 or 2minutes to allow the medicine to be absorbed by the eye.
    • Remove any excess solution around the eye with a clean tissue, beingcareful not to touch the eye.
    • Immediately after using the eye drops, wash your hands to removeany medicine that may be on them.
    • To keep the medicine as germ-free as possible, do not touch the applicatortip to any surface (including the eye). Also, keep the container tightly closed.
    • The preservative in the eye drops containing the medicine, demecarium,may be absorbed by soft contact lenses. If you wear soft contact lenses, andyour doctor has informed you that you can wear them while taking this medication,you should wait at least 15 minutes after applying the eye drops before insertingyour lenses.

    To use the ophthalmic ointment (eye ointment) form of this medicine:

    • First, wash your hands. Tilt the head back and, pressing your fingergently on the skin just beneath the lower eyelid, pull the lower eyelid awayfrom the eye to make a space. Squeeze a thin strip of ointment into this space.A 1/2-cm (approximately 1/4-inch) strip of ointment is usually enough,unless you have been told by your doctor to use a different amount. Let goof the eyelid and gently close the eyes. Keep the eyes closed for 1 to 2 minutesto allow the medicine to be absorbed by the eye.
    • Immediately after using the eye ointment, wash your hands to removeany medicine that may be on them.
    • Since isoflurophate loses its effectiveness when exposed to moisture,do not wash the tip of the ointment tube or allow it to touch any moist surface(including the eye).
    • To keep the medicine as germ-free as possible, do not touch the applicatortip to any surface (including the eye). After using this eye ointment, wipethe tip of the ointment tube with a clean tissue and keep the tube tightlyclosed.

    It is very important that you use this medicine onlyas directed. Do not use more of it and do not use it more often thanyour doctor ordered. To do so may increase the chance of too much medicinebeing absorbed into the body and the chance of side effects.

    If the applicator tip touches any surface (including the eye), it may becomecontaminated with bacteria, which may increase the chance of developing aneye infection. If you think the applicator has become contaminated, notifyyour doctor immediately.

    Eye ointment usually causes blurred vision for a short time after you useit, and eye drops containing these medicines may affect your vision for severalhours after you use them. Therefore, ask your doctor if the dose (or one ofthe doses if you use more than 1 dose a day) can be used at bedtime.

    Dosing?The doses of these medicines will be differentfor different patients. Follow your doctor's orders orthe directions on the label. The following information includes onlythe average doses of these medicines. If your dose isdifferent, do not change it unless your doctor tells you to do so.

      For demecarium
    • For ophthalmic solution (eye drops) dosageform:
      • For glaucoma:
        • Adults and older children?Use one drop in the eye one or twotimes a day.
        • Infants and young children?Use and dose must be determinedby your doctor.
      • For treatment of accommodative esotropia:
        • Adults and older children?Use one drop in the eye once a dayfor two to three weeks, then one drop in the eye once every two days for threeto four weeks, then use as determined by the doctor.
        • Infants and young children?Use and dose must be determinedby your doctor.
      • For diagnosis of accommodative esotropia:
        • Adults and older children?Use one drop in the eye once a dayfor two weeks, then one drop in the eye once every two days for two to threeweeks.
        • Infants and young children?Use and dose must be determinedby your doctor.
      For echothiophate
    • For ophthalmic solution (eye drops) dosageform:
      • For glaucoma:
        • Adults and older children?Use one drop in the eye one or twotimes a day.
        • Infants and younger children?Use and dose must be determinedby your doctor.
      • For treatment of accommodative esotropia:
        • Adults and older children?Use one drop in the eye once a dayor one drop in the eye once every two days.
        • Infants and young children?Use and dose must be determinedby your doctor.
      • For diagnosis of accommodative esotropia:
        • Adults and older children?Use one drop in the eye once a dayat bedtime for two to three weeks.
        • Infants and young children?Use and dose must be determinedby your doctor.
      For isoflurophate
    • For ophthalmic ointment dosage form:
      • For glaucoma:
        • Adults and older children?Use the ointment in the eyes onceevery three days or as often as three times a day as directed by the doctor.
        • Infants and young children?Use and dose must be determinedby your doctor.
      • For treatment of accommodative esotropia:
        • Adults and older children?Use the ointment in the eyes oncea day at bedtime for two weeks, then once a week or as often as once everytwo days as directed by the doctor.
        • Infants and young children?Use and dose must be determinedby your doctor.
      • For diagnosis of accommodative esotropia:
        • Adults and older children?Use the ointment in the eyes oncea day at bedtime for two weeks.
        • Infants and young children?Use and dose must be determinedby your doctor.

    Missed dose?If you miss a dose of this medicine and your dosingschedule is:

    • One dose every other day?Use the missed dose as soon as possibleif you remember it on the day it should be used. However, if you do not rememberthe missed dose until the next day, use it at that time. Then skip a day andstart your dosing schedule again. Do not double doses.
    • One dose a day?Use the missed dose as soon as possible. However,if you do not remember the missed dose until the next day, skip the misseddose and go back to your regular dosing schedule. Do not double doses.
    • More than one dose a day?Use the missed dose as soon as possible.However, if it is almost time for your next dose, skip the missed dose andgo back to your regular dosing schedule. Do not double doses.

    If your dosing schedule is different from all of the above and you missa dose of this medicine, or if you have any questions about this, check withyour doctor.

    Storage?To store this medicine:

    • Keep out of the reach of children. Overdose of demecarium, echothiophate,or isoflurophate is very dangerous in young children.
    • Store away from heat and direct light.
    • Keep this medicine from freezing.
    • 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

    If youare using this medicine for glaucoma, your doctor should check your eye pressureat regular visits to make sure the medicine is working.

    If you will be using this medicine for a long time, your doctor shouldexamine your eyes at regular visits to make sure this medicine does not causeunwanted effects.

    Before you have any kind of surgery (including eyesurgery), dental treatment, or emergency treatment, tell the medicaldoctor or dentist in charge and the anesthesiologist or anesthetist (the personwho puts you to sleep) that you are using this medicine or have used it withinthe past month.

    These medicines should not be used if an eye infection is present, or ifthe eye is wounded or injured. If redness, pain, or discharge develops, orif a foreign object becomes lodged in one or both eyes, or if you suffer ablow to the eye or eye area, notify your doctor immediately.

    Avoid breathing in even small amounts of carbamate-or organophosphate-type insecticides or pesticides (for example, carbaryl[Sevin], demeton [Systox], diazinon, malathion, parathion, ronnel [Trolene],or TEPP). They may add to the effects of this medicine. Farmers, gardeners,residents of communities undergoing insecticide or pesticide spraying or dusting,workers in plants manufacturing such products, or other persons exposed tosuch poisons should protect themselves by wearing a mask over the nose andmouth, changing clothes frequently, and washing hands often.

    Make sure your vision is clear before you drive, usemachines, or do anything else that could be dangerous if you are not ableto see well. This is because:

    • After you apply this medicine to your eyes, your pupils may becomeunusually small. This may cause you to see less well at night or in dim light.
    • After you begin using this medicine, your vision may be blurred orthere may be a change in your near or distance vision.
    • The eye ointment form of this medicine usually causes blurred visionfor a short time after you apply it.


    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 doctorimmediately if any of the following side effects occur:

        Rare

          Burning, redness, stinging, or other eye irritation; eye pain; veil or curtain appearingacross part of vision

        Symptoms of too much medicine being absorbed into the body

          Increased sweating; loss of bladdercontrol; muscle weakness; nausea, vomiting, diarrhea, or stomach cramps or pain; shortness of breath, tightness in chest, or wheezing; slow or irregular heartbeat; unusual tiredness orweakness; watering of mouth

          Note:

          The most common of these symptoms, especially in children, are nausea, vomiting, diarrhea, and stomach cramps or pain.Your doctor may tell you to stop taking the medicine if any of these sideeffects occur.

          Too much medicine being absorbed is rare with the eye ointment form ofthis medicine.

    Other side effects may occur that usually do not need medical attention.These side effects may go away during treatment as your body adjusts to themedicine. However, check with your doctor if any of the following side effectscontinue or are bothersome:

    Blurred vision or change in near or distance vision; difficulty in seeing at night or in dim light; headache or browache; twitching of eyelids; watering of eyes

    Other sideeffects not listed above may also occur in some patients. If you notice anyother effects, check with your doctor.


    Revised: 06/15/99