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Alzheimer's disease medications.


Fact Sheet

Five prescription drugs prescription drug Prescription medication Pharmacology An FDA-approved drug which must, by federal law or regulation, be dispensed only pursuant to a prescription–eg, finished dose form and active ingredients subject to the provisos of the Federal Food, Drug,  currently are approved by the U.S. Food and Drug Administration (FDA FDA
abbr.
Food and Drug Administration


FDA,
n.pr See Food and Drug Administration.

FDA,
n.pr the abbreviation for the Food and Drug Administration.
) to treat people who have been diagnosed with Alzheimer's disease Alzheimer's disease (ăls`hī'mərz, ôls–), degenerative disease of nerve cells in the cerebral cortex that leads to atrophy of the brain and senile dementia.  (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 cholinesterase inhibitor
n.
A drug, such as neostigmine, that restores myoneural function by inhibiting the biodegradation of acetylcholine. Also called acetylcholinesterase inhibitor.
, and are prescribed pre·scribe  
v. pre·scribed, pre·scrib·ing, pre·scribes

v.tr.
1. To set down as a rule or guide; enjoin. See Synonyms at dictate.

2. To order the use of (a medicine or other treatment).
 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 behavioral symptom Neurology In Alzheimer's disease, any of the Sx that relate to action or emotion, such as wandering, depression, anxiety, hostility, sleep disturbances. See Alzheimer's disease. . The medications are: Razadyne[R] (galantamine galantamine /ga·lan·ta·mine/ (gah-lan´tah-men) a reversible competitive inhibitor of acetylcholinesterase used as the hydrobromide salt in the treatment of Alzheimer's disease. , previously known as Reminyl Reminyl®  1 Sabeluzole, see there. 2. Galanthamine [R]), Exelon[R] (rivastigmine rivastigmine /riv·a·stig·mine/ (riv?ah-stig´men) a cholinesterase inhibitor used as the tartrate salt as an adjunct in the treatment of dementia of the Alzheimer type. ), Aricept Ar·i·cept

A trademark for the drug donepezil hydrochloride.


donepezil hydrochloride

Aricept

Pharmacologic class: Acetylcholinesterase inhibitor

Therapeutic class:
[R] (donepezil donepezil /do·nep·e·zil/ (do-nep´e-zil) an acetylcholinesterase inhibitor used as the hydrochloride salt for the treatment of mild to moderate symptoms of dementia of the Alzheimer type; administered orally. ), and Cognex Cog·nex

A trademark for the drug tacrine hydrochloride.


tacrine hydrochloride

Cognex

Pharmacologic class: Cholinergic (cholinesterase inhibitor)

Therapeutic class:
[R] (tacrine tacrine /tac·rine/ (tak´ren) a cholinesterase inhibitor used to improve cognitive performance in dementia of the Alzheimer type; used as the hydrochloride salt. ). Scientists do not yet fully understand how cholinesterase inhibitors work to treat AD, but current research indicates that they prevent the breakdown of acetylcholine acetylcholine (əsēt'əlkō`lēn), a small organic molecule liberated at nerve endings as a neurotransmitter. It is particularly important in the stimulation of muscle tissue. , 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 NMDA

N-methyl-D-asparate
) antagonist antagonist /an·tag·o·nist/ (an-tag´o-nist)
1. a substance that tends to nullify the action of another, as a drug that binds to a cell receptor without eliciting a biological response, blocking binding of substances that could
. 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 glutamate /glu·ta·mate/ (gloo´tah-mat) a salt of glutamic acid; in biochemistry, the term is often used interchangeably with glutamic acid.

glu·ta·mate
n.
1. A salt of glutamic acid.
, another important brain chemical that, when produced in excessive amounts, may lead to brain cell death. Because NMDA antagonists NMDA antagonist Neurology Any of a number of agents that protect against brain damage in neurologic disorders–eg, stroke; PCP–phencyclidine and ketamine are effective, but have psychotomimetic effects or damage neurons in the cerebral cortex; diazepam  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 dosage /dos·age/ (do´saj) the determination and regulation of the size, frequency, and number of doses.

dos·age
n.
1. Administration of a therapeutic agent in prescribed amounts.
 and Side Effects Side effects

Effects of a proposed project on other parts of the firm.
 

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 herbal, early botanical book containing descriptions and illustrations of herbs and plants with their properties, chiefly those qualities that made them useful as medicines or condiments. Most of the herbals were written between c.1470 and c.  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 ADEAR Alzheimer's Disease Education And Referral Center ) 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 The National Institute on Aging is a division of the U.S. National Institutes of Health, located in Bethesda, Maryland.

Formed in 1974, NIA's mission is to improve the health and well-being of older Americans through research. It is the primary U.S.
 offers information and publications on diagnosis, treatment, patient care, caregiver care·giv·er
n.
1. An individual, such as a physician, nurse, or social worker, who assists in the identification, prevention, or treatment of an illness or disability.

2.
 needs, longterm care, and research.

Alzheimer's Association The Alzheimer's Association, incorportated on April 10, 1980 as the Alzheimer’s Disease and Related Disorders Association, Inc., is a non-profit American voluntary health organization which focuses on care, support and research for Alzheimer's disease.  

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
No portion of this article can be reproduced without the express written permission from the copyright holder.
Copyright 2007, Gale Group. All rights reserved.

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Publication:Pamphlet by: National Institute on Aging
Date:Nov 1, 2007
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