Article Highlights:

  • Galantamine is one of five FDA-approved drugs for the treatment of Alzheimer’s disease.
  • Other FDA-approved drugs include rivastigmine, memantine, donepezil, and tacrine.
  • These drugs can temporarily boost cognitive function, dementia is still a progressive disease that will eventually get worse.
  • Manageable side effects of Galantamine can include nausea, dizziness and vomiting.
  • More severe side effects can include irregular heartbeat, fainting, and seizures.
  • Symptoms of overdose include chronic vomiting, extreme fatigue, and collapse.
  • Galantamine has interactions with many drugs, however only a few are commonly prescribed.

Overview

Galantamine comes in both an organic and a synthetic form. Galantamine is an organic compound of a plant that derives from Galanthus nivalis, a species of a plant commonly known as the “snowdrop. This compound has been used for many years as anesthesia for surgery and dentistry, as well as for the treatment of neuropathic pain, a chronic pain condition that is associated with damaged nerve fibers often as a result of tissue injury commonly resulting from tissue injury.

The synthetic form of Galantamine was first registered for the treatment of Alzheimer’s disease in Sweden in the year 2000. It has since then been approved for Alzheimer’s treatment in the United States, Europe, Canada, and various other countries around the globe.

Alzheimer’s is a degenerative disease of the brain that gradually impacts a person’s memory, causing confusion, disorientation, problems with communicating, and various other issues associated with diminished mental capacity. Alzheimer’s is a fatal disease that over time affects all parts of the brain. Alzheimer’s Disease International estimates that there are currently nearly 50 million people with AD worldwide, a number that is expected to increase to more than 74 million by 2030, and to 131 million by 2050.

Galantamine is one of five FDA-approved drugs for the treatment of Alzheimer’s disease. Other drugs approved by the FDA include rivastigmine, memantine, donepezil, and tacrine (tacrine is rarely used because of its severe side effects).

Although Galantamine does not cure Alzheimer’s disease or prevent future loss of mental function, when taken under appropriate conditions Galantamine can defer the progression of certain symptoms of mild to moderate Alzheimer’s disease. These include confusion, memory loss, and cognitive function related to performing Activities of Daily Living (ADLs).

Galantamine comes in the form of a tablet, an extended-release capsule, and a liquid solution that can be taken orally. To avoid prescribing confusion between galantamine’s original brand name Reminyl and the diabetes drug Amaryl, the brand name Reminyl was changed in 2005 to RAZADYNE®. Since then, several generic forms of galantamine have been approved by the FDA.

Galantamine can have gastrointestinal-related side effects such as loss of appetite, nausea, and vomiting, as well as more serious side effects such as blood in the urine, fainting, and seizures.

Mechanism of Action: How Galantamine Works

People with Alzheimer’s disease, Parkinson’s disease, and some other types of dementia, are commonly known to have diminished levels of acetylcholine, a neurotransmitter in the brain that enhances synaptic transmissions, particularly those associated with memory and other cognitive functions that relate to the performance of Activities of Daily Living (ADLs).

Galantamine is a part of a class of medication called acetylcholinesterase inhibitors. Its mechanism of action consists of inhibiting the effectiveness of an enzyme, acetylcholinesterase, which lowers the levels of acetylcholine in the brain. It thus benefits individuals with Alzheimer’s by increasing the levels of acetylcholine in their brains and subsequently boosting cognitive function.

Although further research is necessary, Galantamine is thought to be beneficial to the millions of people who have Mild Cognitive Impairment (MCI). MCI goes beyond the normal age-related forgetfulness, but falls short of qualifying as dementia. Although MCI does not necessarily lead to Alzheimer’s disease, it is a very strong risk factor for developing dementia.

Galantamine goes beyond the ability of Donepezil and Rivastigmine in its modulation of nicotinic receptors, molecular receptors that bind to acetylcholine and nicotine. Galantamine modulates these receptors by conserving both their quantity and their functional integrity, thus deferring receptor deterioration in Alzheimer’s disease. Donepezil and Rivastigmine do not present nicotinic receptor action, potentially decreasing the the effectiveness of the drugs over time.

Forms, Dosage, and Usage of Galantamine

Galantamine comes in RAZADYNE® ER capsules, RAZADYNE® tablets, and RAZADYNE® oral solution. The dosages are as follows:

Extended-Release (ER) Capsules

  • 4mg
  • 8mg
  • 12mg

Tablets

  • 8mg
  • 16mg
  • 24mg

Oral Solution

  • 4mg/mL

RAZADYNE® ER capsules are taken once a day and have a 24-hour duration, while RAZADYNE® tablets are taken twice daily (mornings and evenings) and always after meals or with food.

It is common for physicians to start treatment with a low dosage that can then be increased, usually once every 2 to 4 weeks, to reach the desired long-term maintenance level. Doctors refer to this as escalation. Do not take more than the maximum recommended dose of 24 milligrams per day.

Galantamine is taken twice a day, to be taken morning and evening and always with food, as it may cause nausea, vomiting, loss of appetite, and other side effects when taken on an empty stomach. The dosage that your physician may start you off with will depend on your specific condition and other factors that the physician will ascertain after examining you and taking measure of your medical history, family history, age and mental condition.

Patients are advised to drink plenty of fluids with this medication unless instructed otherwise. To lower the risk of side effects, the dosage will likely be gradually increased to the target dose.

When taking RAZADYNE® liquid solution, read the pharmaceutical instruction sheet that comes with the solution. Use the measuring device that comes with the product to measure out your dose. The pharmacist may help with measuring the solution and other administration information. The correct amount of the solution then needs to be mixed with approximately 4 ounces of water or juice, which then needs to stirred and drink the entire mixture.

It may take a few weeks (at least four) of continued use before galantamine takes effect and starts producing the desired long-term benefits. Do not stop taking galantamine or change the prescribed dosage or repetitions without consulting a physician first. If you stop taking RAZADYNE® for 3 days or longer, your doctor may want to start at the low dosage before building up to the long-term maintenance level.

RAZADYNE® as an Alzheimer’s Treatment

In a study of 636 patients with mild to moderate Alzheimer’s that lasted for six months, patients were split up between a group that was given escalated doses of up to 24mg per day, and another group (placebo) that were not given Galantamine. The results over the six-month period were measured per the Alzheimer’s Assessment Scale and the Clinician’s Interview-Based Impression of Change (which includes input from the patients’ close families and caregivers.

The study found that those who were given Galantamine showed enhanced cognitive function compared to those who were not given the drug.

After another six months however, the results on those who had been given Galantamine on 24 mg a day dose for the entire 12-month duration did not show any further improvements from their scores after six months.

In terms of side effects, the most common adverse events, mostly gastrointestinal in nature, decreased in frequency over the course of long-term treatment. There were also no signs of hepatotoxicity, which is a term used for drug-induced liver damage.

The study concluded that Galantamine was effective and safe as a treatment for individuals with Alzheimer’s. At the six-month mark, Galantamine considerably enhanced cognitive faculties and awareness. After 12 months, and with the 24mg a day dose, these cognitive benefits were preserved without adverse reactions.

FDA-Approved Drugs to Treat Alzheimer’s

Five drugs are currently FDA-approved for the treatment of Alzheimer’s; some are also used to treat Parkinson’s disease and other conditions, although they are specifically approved for the treatment of AD. Tacrine is hardly ever used because of its very severe side effects. The five drugs are:

  • Galantamine (RAZADYNE® and RAZADYNE® ER)
  • Rivastigmine (Exelon and Exelon patch)
  • Memantine (Namenda and Namenda XR)
  • Donepezil (Aricept and Aricept dissolvable tablet)
  • Tacrine (Cognex)

Although various other medications are continually being prescribed in attempts to treat dementia symptoms, these are the only ones that have, under the appropriate testing standards, demonstrated to be effective in deferring the onset of Alzheimer’s, or slowing the progression of some of its symptoms

Some other drugs used include anti-inflammatory medications such as Advil, Motrin and Celebrex, Eldepryl (Selegiline) for Parkinson’s, and statins that are prescribed to lower cholesterol levels.

Side Effects of Galantamine (RAZADYNE®)

Many of the side effects of Galantamine are mild and do not require medical attention. Most patients taking RAZADYNE® get used to less severe side effects over a short period of time before they disappear altogether. It is nevertheless important to keep a check on what the person is feeling, just in case one or more of the more severe side effects present, in which case it would be important to address with your loved one’s physician.

The less serious and more common side effects of Galantamine include:

  • Diarrhea, nausea, vomiting, and other symptoms of underlying gastrointestinal issues, upset stomach, or indigestion
  • Headache and shakiness or tremors
  • Dizziness and weakness, i.e. a diminished strength in muscles and muscle groups, and loss of muscle function
  • Weight loss and loss of appetite, medically called anorexia, and frequently of a reversible nature
  • Insomnia and sleep disturbance
  • Swelling in hands and feet, and joint pain
  • Coughing, runny nose, and increased sweating

More serious and far less common potential side effects of Galantamine include:

  • Black or tarry stool, and vomit that looks like coffee grounds, which may indicate there is considerable internal bleeding
  • Slow or irregular heartbeat, lightheadedness, and fainting (syncope), which is a temporary partial or complete loss of consciousness with reflexive recovery
  • Trouble urinating, possible constipation, bloating and full feeling
  • Considerable stomach or abdominal pain, constipation, and unusual fatigue
  • Chest pain, discomfort and seizures (convulsions)
  • Hallucinating, i.e. seeing, hearing, or sensing things or people that are not there
  • Loss of balance control, shuffling walk, twisting movements of the body, difficulty with speech, and drooling
  • Aggression, confusion, depression
  • Uncontrolled movements, particularly of the face, back, and neck

Stuart’s grandmother had mild to moderate Alzheimer’s

Stuart’s grandmother was diagnosed with Alzheimer’s when she was 68 years-old. Once past the initial shock of hearing the diagnosis, Stuart went ahead with having her sign a durable power of attorney for health issues, and another one for financial issues, since she had both checking and savings accounts in her name. By doing those two things, he became her agent for when she would be incapacitated and no longer able to make decisions on her own. Incapacitation indeed came only two short years after the initial diagnosis. She became clinically with “mild to moderate” Alzheimer’s, and while she was still able to dress herself, he had to lay out the desired clothes on her bed and give her cues as to what to do.

When Stuart subsequently started noticing further declines, particularly with confusion when he set a plate with food in front of her, he decided it was time to go to the dementia specialist that her primary care physician had recommended.

After a thorough examination of both her physical and mental conditions, and after doing some tests, including blood tests for kidney and liver function, the specialist prescribed RAZADYNE®, starting her two with 4 mg tablets a day, to be taken after breakfast and dinner, and then escalating that dosage to 8 mgs a day four weeks later. At first there was no reaction. The little nausea Stuart’s grandmother felt initially quickly disappeared, and she seemed to tolerate the drug well.

Weeks passed into two months, then three months and, to Stuart’s amazement, she started showing distinct signs of improvement. When he placed her dinner plate in front of her, she went at it without hesitation, and as for dressing herself, all he then had to do was bring out her clothing hangers from the closet, and she would do the rest.

This kind of improvement in her cognitive faculties lasted several months after that, until he started noticing further declines all over again. The dementia specialist had well prepared him for that, reminding him repeatedly that Galantamine should improve cognitive function for a while, but would not be able to stop further declines in the longer run.

Symptoms of Overdose of Galantamine (RAZADYNE®)

An individual with dementia must not be given more than 24 mgs of Galantamine per day. If that maximum level is exceeded, the person may overdose. Some of the listed less-severe side effects of galantamine may occur although, through a process of escalating the drug over a few weeks, may dissipate entirely. If they do not diminish over time, or if the person has a reaction to Galantamine, then he or she must be quickly referred to emergency medical treatment.

One or more of the following symptoms may additionally indicate an overdose and will also necessitate medical emergency treatment:

  • Dry mouth, shortness of breath, trouble breathing, and slow or irregular heartbeat
  • Pale or discolored (bluish) skin, lips, and fingernails
  • Chest pain or significant discomfort
  • Stomach cramps, severe or chronic vomiting, and severe nausea
  • Increased sweating, increased urination, and increased watering of the mouth or drooling
  • Need to have a bowel movement
  • Teary eyes
  • Lightheadedness, dizziness or unconscious spells (fainting)
  • Extreme fatigue, collapse
  • Hallucinations, i.e. seeing things, hearing voices that do not exist

Galantamine (RAZADYNE®) Warnings and Interactions

People who weigh less than 110 lbs should be monitored closely by their physician when taking Galantamine in any of its forms. The same goes for anyone suffering from the following conditions:

  • Individuals who are pregnant or planning to become pregnant, since there is no proof yet that the drug won’t pass on through breast-feeding
  • People who have a history of liver or kidney problems, heart problems (for example slow or irregular heartbeat, unexplained fainting episodes, stomach or bowel problems, lung or breathing problems (as in chronic obstructive pulmonary disease), urinary blockage or trouble urinating, or seizures
  • People planning to have surgery or dental work with anesthesia
  • Individuals who take any medicine that may slow their heartbeat (such as digoxin, diltiazem, verapamil).

Galantamine interacts with over 500 other drugs, although drugs that are commonly prescribed that have interactions with Galantamine are few and include those in this short summary:

  • Ibuprofen and other nonsteroidal anti-inflammatory drugs (NSAIDs), because of the increased risk of stomach or bowel bleeding
  • Bethanechol and other cholinergic agents, donezil and other cholinesterase inhibitors, ketoconazole, or Paroxetine and other selective serotonin reuptake inhibitors, since SSRIs may increase the risk of galantamine’s severe side effects
  • Scopolamine and other anticholinergics, since their effectiveness may be decreased with galantamine

Final Thoughts

Most caregivers who look after individuals with Alzheimer’s disease and other types of dementia know about medications of the antidepressant or antipsychotic type, or drugs that assuage signs of anxiety, agitation, aggression, or other behavioral challenges. When used thoughtfully, these can be a good help in managing some of the harsher symptoms that Alzheimer’s commonly presents. You should also discuss with your doctor the possibility of taking one of the drugs approved to treat Alzheimer’s. While these drugs do not provide a cure, they may help reduce or delay cognitive symptoms and provide some temporary relief.

In the larger scheme of things, it is important to remember that medications, including RAZADYNE®, are only one component of what it takes to provide quality care for someone with Alzheimer’s or another type of dementia. There is ample research that points to other ways of looking after someone with Alzheimer’s as being just as effective, if not more so, than what these medications offer. Drugs cannot preserve a person’s dignity and sense of well-being, nor do they equal the benefits that affectionate care and support provide. Caregivers have the power to better the lives of individuals with dementia by helping them maintain healthy and engaged lifestyles with good nutrition, exercise, and plentiful support and interaction.

Posted 
August 15, 2017
 in 
Caregiver Resources
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