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Woman with Alzheimer's Disease

When someone has Alzheimer’s disease, nerve cells and vital chemicals in the brain are lost over time. This occurs in parts of the brain that are vital to memory and other mental processes.

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Let’s look at several of the most common medications approved by the FDA for treatment of the symptoms associated with Alzheimer’s disease. These medications work in specific ways to boost memory or slow down the progression of Alzheimer’s.

 

Types of Alzheimer’s Disease Medications

  1. Acetylcholinesterace Inhibitors
  2. Antidepressant Medications
  3. Other Medications Used with Alzheimer’s Disease

 

Acetylcholinesterace Inhibitors

Acetylcholinesterace inhibitors, including Aricept, Exelon, and Razadyne/ER, reduce the destruction of acetylcholine after it’s been excreted, thereby leaving it around for longer periods of time. The rationale behind the use of acetylcholinesterase inhibitors is that it has been noticed in Alzheimer’s disease that there was a decrease in acetylcholine at the receptor site. Therefore, anything that would increase the amount of acetylcholine would improve memory. While acetylcholinesterase inhibitors may temporarily improve the patient’s symptoms, these medications do absolutely nothing to rectify the disease process. While definitely not a cure, there’s some inclination that acetylcholinesterase inhibitors may delay the disease process.

Donepezil (Aricept)

How It Works: Aricept is a cholinesterase inhibitor that stops the breakdown of acetylcholine, a chemical in the brain used for memory and other mental functions. In Alzheimer’s disease, there is a deficiency in acetlycholine in some areas of the brain, which accounts for some symptoms of the disease. Cholinesterase inhibitors also help increase the levels of acetylcholine in the brain. By increasing the amount of acetylcholine, it’s thought that communication between cells should improve and thus increase memory. The problem is that Alzheimer’s causes a loss of the communication wires and neuron cells. Adding more transmitters (acetylcholine) will only provide temporary help. It does not fix the problem.

Possible Side Effects: Aricept has the least side effects of all the anticholinergic drugs. About 5 to 10 percent of patients may have mild side effects such as nausea, vomiting, and diarrhea. Some patients experience weight loss and insomnia.
 

Ribastigmine (Exelon)

How It Works: Exelon is thought to maximally decrease the progression of Alzheimer’s disease, by blocking acetylcholine and butyrocholinesterase. Of all the medications for Alzheimer’s disease so far, Exelon seems to be the only one that works in this way. This medication also affects butyrocholine, which is another type of cholinergic transmitter in the brain.

Possible Side Effects: With Exelon, side effects might include muscarinic effects such as sweating, diarrhea, and nausea. Other less common side effects include seizures and arrhythmias.
 

Galantamine (Razadyne)

How It Works: Razadyne blocks acetylcholine but not butryocholinesterase. Razadyne also binds to nicotine receptors, which increases neurotransmitters for brain activity. Razadyne may also block cell death in Alzheimer’s disease, which might slow the progression of Alzheimer’s more than Exelon. However, no recent study has shown that any of these combinations actually reduce a patient from going to a nursing home by even a single day.

Possible Side Effects: Side effects with Razadyne include upset stomach, vomiting, diarrhea, and urinary tract infections (UTI). Other problems include arrhythmias and seizures.
 

Memantine HCL (Namenda)

How It Works: Namenda is approved by the FDA for treating moderate and severe Alzheimer’s disease. Namenda works by blocking n-methyl D-aspartate (NMDA) receptors to reduce the entry of calcium into the neurons, which may protect it from damage. The NMDA receptor binds the neurotransmitter glutamate, thus increasing its charge and making it more widely to transmit its message to the next neuron. Namenda may also block programmed cell death. I have seen Namenda improve speech, learning, and recent memory in Alzheimer’s patients, and I highly recommend this one.

Possible Side Effects: Some side effects associated with Namenda include dizziness, headache, confusion, Stevens-Johnson syndrome (a life-threatening allergic reaction) and seizures.
 

Antidepressant Medications

Depression is seen in over 70 percent of Alzheimer’s patients and complicates the disease by interfering with sleep and energy. Antidepressants are commonly prescribed to alleviate the signs and symptoms of depression and, thus, improve the quality of the person’s life in spite of the Alzheimer’s disease.

Antidepressants are effective in the early stages of Alzheimer’s when patients recognize their cognitive loss and the loss of their mental abilities cause stress with consequent increase in cortisol levels that eventually produces a decrease in serotonin, dopamine, and even adrenaline. Patient’s first symptoms include difficulty with sleep, early morning awakening, increased fatigue, severe anxiety, and finally weight loss and anhedonia (a complete loss of pleasure). The patient can get to the point where they are immobile and appear to be severely demented. Severe depression can mask as Alzheimer’s. I have had at least one hundred cases where severe endogenous depression was the primary cause of memory loss. Antidepressants, of which there are tricyclics, SSRIs, SNRIs, are the primary antidepressants used. There’s also another category of antidepressants that contains bupropian (Wellbutrin), trazedone (Desyrel), and duloxetine (Cymbalta).

Tricyclics:

  • Amitriptyline (Elavil) 
  • Doxepin (Sinequan)
  • Nortriptyline (Pamelor)

The tricyclics were the first generation of antidepressants, including amitriptyline (Elavil), doxepin (Sinequan), and nortriptyline (Pamelor). These are drugs that reuptake serotonin, increasing the amount available for use. Serotonin is the calmative neurotransmitter that also enhances dopamine production (the feel good transmitter). Initially, these drugs were to be used as antihistamines for allergies until it was found that people who took the tricyclics received a great antidepressant effect. Their sleeping habits improved, their energy levels increased, as did their appetite. Today, the tricyclics are used as both antidepressants and pain relieving modulators. In particular, amitriptyline is used for general neuropathic pain, migraines, arthralgias, and myalgias.
 

Selective Serotonin Reuptake Inhibitors (SSRIs)

In the mid to late 1980s, the second generation of antidepressants, the selective serotonin reuptake inhibitors or SSRIs was formulated. These started with Prozac and then moved to sertraline (Zoloft), paroxetine (Paxil), and fluvoxamine maleate (Luvox). Other antidepressants with different mechanisms of action from the SSRIs were also developed during that same time, including bupropion (Wellbutrin), venlafaxine (Effexor), and mirtazapine (Remeron).

Antidepressants launched in the 1990s have completely different biochemical effects from the drugs of the past. This is important because we have made progress in diagnosing new subtypes of depression and have also arrived at new genetic findings, leading to the new field of pharmacogenetics where a given drug’s metabolism and clinical effects may be genetically determined. Most of the new antidepressants, such as SSRIs, can be used with no dietary restrictions. They are safe even for cardiovascular patients, including those with cardiac arrhyth-mias and blood pressure changes.

I believe that the selective serotonin reupdate inhibitors (SSRIs) may decrease the chance of Alzheimer’s as they elevate serotonin levels in the brain while also suppressing dopaminergic pathways. Many patients who take antidepressants report more refreshing sleep and clarity of mind. Because they feel relaxed, in control, and rested, they can make healthy lifestyle choices and deal with life’s challenges in a much healthier manner.
 

Some Commonly Prescribed Antidepressants in Alzheimer’s Disease
 

Generic Name Brand Name Common Usage
amitriptyline Elavil Sleep
doxepin Sinequan Sleep stage
escitalopram Lexapro Anti-anxiety
fluoxetine Prozac Mood enhancer
sertraline Zoloft Mood enhancer
paroxetine Paxil Mood enhancer
venlafaxine Effexor Anti-anxiety
duloxetine Cymbalta Anti-anxiety
trazadone Desyrel Sleep enhancer
bupropion Wellbutrin Mood enhancer

 

Neuroleptics, such as Haloperidol (Haldol)

In Alzheimer’s patients, the neuroleptics are given to control serious psychological behavior as combativeness, illusions, hallucinations and delusions. Ideas of reference, such as when a patient believes that someone is out to get them, are also treated with neuroleptics.

How They Work: Haldol is a commonly used neuroleptic. Haldol is considered to be particularly effective in the management of hyperactivity, agitation, and mania and is used to treat acute and chronic psychosis, including schizophrenia and manic states. Haldol is also used in the management of aggressive and agitated behavior.

Possible Side Effects: Haldol can cause insomnia, headaches, cerebral seizures, and tardive dyskinesia or involuntary movements of the lips, tongue, face, trunk and extremities.
 

Atypical Neuroleptics such as Quetiapine (Seroquel)

How They Work: The atypical neuroleptics are prescribed for psychosis, severe anxiety, and wandering, While Seroquel is not indicated for the treatment of dementia-related psychosis, it is used at low doses to offset behavioral/psychosis problems with Alzheimer’s.

Possible Side Effects: Side effects of Seroquel include headache, somnolence, hypertriglyceridemia (high levels of triglycerides), severe hypotension, tardive dykenesia, neuroleptic malignant syndrome (NMS), a life-threatening, neurological disorder often caused by an adverse reaction to a neuroleptic or antipsychotic medication. (This is rare at low doses).
 

 

Other Medications Used with Alzheimer’s Disease

Olanzapine (Zyprexa)

How It Works: Olanzapine is a selective monoaminergic antagonist that’s normally prescribed for schizophrenia, or manic episodes of bipolar disorder. It helps in controlling symptoms such as hallucinations and delusions, as well as social withdrawal and apathy.

Possible Side Effects: Some possible side effects of Zyprexa include dizziness, daytime sleepiness, weight gain, neuroleptic malignant syndrome, diabetes mellitus, and extrapyramidal symptoms such as tremors, rigidity, drooping, rolling eyes, and a masked- like expression.
 

Benzodiazepines:

  • Alprazolam (Xanax)
  • Diazepam (Valium)
  • Lorazepam (Ativan)
  • Oxazepam (Serax)
  • Temazepam (Restroil)
  • Triazolam (Halcion)

How They Work: The benzodiazepines belong to a group of medications called central nervous system (CNS) depressants. These medications act on neurotransmitters to slow down normal brain function. CNS depressants are commonly used to treat anxiety and sleep disorders. These drugs are all habit-forming or addictive.

With Alzheimer’s disease, I avoid the use of benzodiazepines to ameliorate symptoms, even anxiety and agitation.

I advise this for the following reasons:

  1. Patients can develop a tolerance to daily use of benzodiazepines within a month.
  2. Patients become addicted so when the drug is withdrawn, they will have increased agitation.
  3. Increased doses of benzodiazepines are required to have the same effect. With an increased dosage, the patient may have increased confusion and a deterioration of both recent and past memory. Functional MRIs have shown that the use of benzodiazepines show an overall decrease in brain activity.

Possible Side Effects: Side effects of benzodiazepines may include memory impairment, psychomotor retardation, toxicity, depression and emotional blunting. These drugs may also give rise to physiologic and physiologic dependence.
 

Medications Used to Treat Insomnia

Initially, I may prescribe eszopicione (Lunesta), zaleplon (Sonata), zolpidem (Ambien), or ramelteon (Rozerem) for minor sleep disturbance. If these don’t work, I often recommend an antidepressant such as sinequan, trazadone, and amitriptyline. Amitriptyline, due to its arrhythmic effects, is not advised in patients with coronary artery disease or over 60 years of age.

Medications to induce sleep should be monitored and discontinued when feasible. Unfortunately, in many nursing homes that I attend, the patients with dementias such as Alzheimer’s often take many sedatives, antidepressants, and antipsychotic medications-without one doctor reviewing this list. As an example, one elderly man was on 17 medications because of his wandering, aggressiveness, and psychotic behaviors. The medications had accumulated in his system, causing liver failure and death. Make sure one doctor sees all the medications you take to avoid serious complications or toxicity.

 

Sleep Medicines That are Purported to be Non-Habit Forming
 

Generic Name Brand Name
eszopicione Lunesta
zaleplon Sonata
ramelteon Rozerem
Non-Habit Forming
mirtazapine Remeron (atypical antipsychotic)
quetiapine fumarate Serequel (atypical antipsychotic)
trazadone Dyserel (antidepressant)

       

 

alzheimer's disease expert

About the Author: Dr. Vincent Fortanasce is a renowned bio-ethicist, author, and radio show host with twenty years experience dealing with medical issues on a national and international level. His rehabilitation center was ranked in the top 10 on the West Coast in 2003, and Dr. Fortanasce was selected as in the top 100 physicians in Los Angeles County and Best Physicians in the USA in 1998. Over the past decade, he has treated such notables as the Dali Lama and Pope John Paul II.
 


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