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Alzheimer's disease medications.

Fact Sheet

Five prescription drugs currently are approved by the U.S. Food and Drug Administration (FDA) to treat people who have been diagnosed with Alzheimer's disease (AD). Treating the symptoms of AD can provide patients with comfort, dignity, and independence for a longer period of time and can encourage and assist their caregivers as well.

It is important to understand that none of these medications stops the disease itself.

Treatment for Mild to Moderate AD

Four of these medications are called cholinesterase inhibitors, and are prescribed for mild to moderate AD. These drugs may help delay or prevent symptoms from becoming worse for a limited time and may help control some behavioral symptoms. The medications are: Razadyne[R] (galantamine, previously known as Reminyl[R]), Exelon[R] (rivastigmine), Aricept[R] (donepezil), and Cognex[R] (tacrine). Scientists do not yet fully understand how cholinesterase inhibitors work to treat AD, but current research indicates that they prevent the breakdown of acetylcholine, a brain chemical believed to be important for memory and thinking. As AD progresses, the brain produces less and less acetylcholine; therefore, cholinesterase inhibitors may eventually lose their effect.

No published study directly compares these drugs. Because they work in a similar way, it is not expected that switching from one of these drugs to another will produce significantly different results. However, an AD patient may respond better to one drug than another. Cognex[R] is no longer actively marketed.

Treatment for Moderate to Severe AD

The fifth approved medication, known as Namenda[R] (memantine), is an Nmethyl D-aspartate (NMDA) antagonist. It is prescribed for the treatment of moderate to severe AD. Studies have shown that the main effect of Namenda[R] is to delay progression of some of the symptoms of moderate to severe AD. The medication may allow patients to maintain certain daily functions a little longer. For example, Namenda[R] may help a patient in the later stages of AD maintain his or her ability to go to the bathroom independently for several more months, a benefit for both patients and caregivers.

Namenda[R] is believed to work by regulating glutamate, another important brain chemical that, when produced in excessive amounts, may lead to brain cell death. Because NMDA antagonists work very differently from cholinesterase inhibitors, the two types of drugs can be prescribed in combination. The FDA has also approved Aricept[R] for the treatment of moderate to severe AD.

Dosage and Side Effects

Doctors usually start patients at low drug doses and gradually increase the dosage based on how well a patient tolerates the drug. There is some evidence that certain patients may benefit from higher doses of the cholinesterase inhibitor medications. However, the higher the dose, the more likely are side effects. The recommended effective dosage of Namenda[R] is 20 mg/day after the patient has successfully tolerated lower doses. Some additional differences among these medications are summarized in the table on the other side.

Patients may be drug-sensitive in other ways, and they should be monitored when a drug is started. Report any unusual symptoms to the prescribing doctor right away. It is important to follow the doctor's instructions when taking any medication, including vitamins and herbal supplements. Also, let the doctor know before adding or changing any medications.

For More Information

To learn about support groups and publications about AD, contact:

Alzheimer's Disease Education and Referral (ADEAR) Center

P.O. Box 8250

Silver Spring, MD 20907-8250

1-800-438-4380

Website: www.alzheimers.nia.nih.gov

This service of the National Institute on Aging offers information and publications on diagnosis, treatment, patient care, caregiver needs, longterm care, and research.

Alzheimer's Association

225 N. Michigan Avenue, Floor 17

Chicago, IL 60601-7633

1-800-272-3900

Website: www.alz.org

This non-profit association supports AD research and families and caregivers of patients with AD. Nationwide chapters provide referrals to local resources.
Medications to Treat Alzheimer's Disease

Note: The brief summary provided below does not include all information
important for patient use and should not be used as a substitute for
professional medical advice. Consult the prescribing doctor
and read the package insert before using these or any other medications
or supplements. Drugs are listed in order, as approved by the U.S. Food
and Drug Administration, starting with the most recent.

 DRUG TYPE AND
DRUG NAME TREATMENT

Namenda[R] (memantine) N-methyl D-aspartate
Blocks the toxic effects (NMDA) antagonist prescribed
associated with excess to treat symptoms of moderate
glutamate and regulates to severe AD
glutamate activation.

Razadyne[R] (galantamine, Cholinesterase inhibitor prescribed
formerly known as to treat symptoms of mild to
Reminyl[R]) moderate AD
Prevents the breakdown
of acetylcholine and
stimulates nicotinic
receptors to release
more acetylcholine in
the brain.

Exelon[R] (rivastigmine) Cholinesterase inhibitor prescribed
Prevents the breakdown of to treat symptoms of mild to moderate
acetylcholine and AD
butyrylcholine (a brain
chemical similar to
acetylcholine) in the
brain.

Aricept[R] (donepezil) Cholinesterase inhibitor prescribed
Prevents the breakdown of to treat symptoms of mild to
acetylcholine in the moderate, and moderate to severe AD
brain.

Cognex[R] (tacrine) Cholinesterase inhibitor prescribed
Prevents the breakdown of to treat symptoms of mild to moderate
acetylcholine in the AD
brain. Note: Cognex
is still available
but no longer actively
marketed by the
manufacturer.

 MANUFACTURER'S RECOMMENDED COMMON SIDE
DRUG NAME DOSAGE EFFECTS

Namenda[R] (memantine) * 5 mg, once a day, Dizziness,
Blocks the toxic effects available in tablet form headache,
associated with excess * Increase to 10 mg/day constipation,
glutamate and regulates (5 mg twice a day), confusion
glutamate activation. 15 mg/day(5 mg and 10 mg
 as separate doses), and
 20 mg/day (10 mg twice
 a day) at minimum of one
 week intervals if well
 tolerated.

Razadyne[R] (galantamine, * 4mg, twice a day Nausea,
formerly known as (8mg/day), available in vomiting,
Reminyl[R]) tablet or capsule form diarrhea,
Prevents the breakdown * Increase by 8mg/day weight loss
of acetylcholine and after 4 weeks to 8mg,
stimulates nicotinic twice a day (16mg/day)
receptors to release if well tolerated.
more acetylcholine in * After another 4 weeks,
the brain. increase to 12mg, twice
 a day (24mg/day) if well
 tolerated.

Exelon[R] (rivastigmine) * 1.5mg, twice a day Nausea,
Prevents the breakdown of (3mg/day), available in vomiting,
acetylcholine and capsule and liquid form weight loss,
butyrylcholine (a brain * Increase by 3mg/day upset stomach,
chemical similar to every 2 weeks to 6mg, muscle
acetylcholine) in the twice a day (12mg/day) weakness
brain. if well tolerated.

Aricept[R] (donepezil) * 5mg, once a day, Nausea,
Prevents the breakdown of available in tablet diarrhea,
acetylcholine in the form vomiting
brain. * Increase after 4-6 weeks
 to 10mg, once a day if
 well tolerated.

Cognex[R] (tacrine) * 10mg, four times a day Nausea,
Prevents the breakdown of (40mg/day), in capsule diarrhea,
acetylcholine in the form possible
brain. Note: Cognex * Increase by 40mg/day liver
is still available every 4 weeks to 40mg, damage
but no longer actively four times a day
marketed by the (160mg/day), if
manufacturer. liver enzyme functions
 remain normal and if
 well tolerated.

 POSSIBLE DRUG
DRUG NAME INTERACTIONS

Namenda[R] (memantine) Other NMDA antagonist medications,
Blocks the toxic effects including amantadine, an antiviral used to
associated with excess treat the flu, dextromethorphan, prescribed
glutamate and regulates to relieve coughs due to colds or flu, and
glutamate activation. ketamine, sometimes used as an anesthetic,
 have not been systematically evaluated and
 should be used with caution in combination
 with this medication.

Razadyne[R] (galantamine, Some antidepressants such as paroxetine,
formerly known as amitriptyline, fluoxetine, fluvoxamine,
Reminyl[R]) and other drugs with anticholinergic
Prevents the breakdown action may cause retention of excess
of acetylcholine and Reminyl in the body, leading to
stimulates nicotinic complications; NSAIDs should be used with
receptors to release caution in combination with this
more acetylcholine in medication. *
the brain.

Exelon[R] (rivastigmine) None observed in laboratory studies; NSAIDs
Prevents the breakdown of should be used with caution in combination
acetylcholine and with this medication. *
butyrylcholine (a brain
chemical similar to
acetylcholine) in the
brain.

Aricept[R] (donepezil) None observed in laboratory studies; NSAIDs
Prevents the breakdown of should be used with caution in combination
acetylcholine in the with this medication. *
brain.

Cognex[R] (tacrine) NSAIDs should be used with caution in
Prevents the breakdown of combination with this medication. *
acetylcholine in the
brain. Note: Cognex
is still available
but no longer actively
marketed by the
manufacturer.

* Use of cholinesterase inhibitors can increase risk of stomach ulcers,
and because prolonged use of non-steroidal anti-inflammatory drugs
(NSAIDs) such as aspirin or ibuprofen can also cause stomach ulcers,
NSAIDs should be used with caution in combination with these
medications.
COPYRIGHT 2007 National Institute on Aging
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Publication:Pamphlet by: National Institute on Aging
Date:Nov 1, 2007
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