Rasagiline – Oral

Rasagiline is a drug used to alter the chemicals in the brain in order to treat the symptoms of Parkinson’s disease.

Overview

Rasagiline is a drug which is taken in the form of a tablet or capsule in order to treat the symptoms of Parkinson’s disease. It belongs to the group of drugs known as MAO inhibitors (monoamine oxidase inhibitors). Monoamine oxidase is a particular enzyme, typically found in neurons in the brain, as well as in the majority of cells throughout the human body. It is an enzyme which works to break down dopamine, tyramine, serotonin and norepinephrine; chemicals which work as neurotransmitters, communicating messages and stimulating responses throughout the nervous system.

There are two classes of MAO enzymes; MAO-A and MAO-B. Rasagiline is designed to inhibit the function of MAO-B enzymes, making them less effective at breaking down certain chemicals, such as serotonin, so that there are higher-than-normal levels of these chemicals throughout the body. It is not definitively known whether rasagiline also inhibits the function of MAO-A enzymes too.

It is still being investigated to determine exactly how rasagiline affects the enzymes and stops them from working as effectively. It is not completely understood how or why they work, but it has been scientifically proven that rasagiline stops MAO-B from breaking down dopamine as well, leading to increased quantities of dopamine which help to reduce the effects of the symptoms associated with Parkinson’s disease.

Parkinson’s disease causes patients to suffer a varied number of symptoms, which increase in quantity and severity as time goes on. The most recognizable of these symptoms are the ones which affect the movement of patients: tremors, slowing down of all movements, muscle and joint rigidity and postural instability.

Parkinson’s disease causes cells in the middle of the brain to die off. This means that cells are unable to produce dopamine, and so in these areas where many of the cells have died, there are very low levels of dopamine within the brain. Rasagiline is used to artificially increase the level of dopamine in the brain, which can alleviate some of the symptoms of Parkinson’s disease, although it cannot reverse the degeneration caused by the death of these cells.

Symptoms such as shaking, stiff muscles and difficulty with movement can all be improved with a prescription of rasagiline.

Conditions treated

  • Parkinson’s Disease

Type of medicine

  • MAO inhibitor

Side Effects

When doctors prescribe a drug to a patient they are well aware of the potential side effects that the drug may cause. If they have prescribed the drug, this is because they believe that the potential benefits of taking the drug will outweigh the risk of possible side effects. Many people who take rasagiline on a regular basis do not experience side effects.

The most common side effects of rasagiline are all relatively minor:

  • Dizziness and light-headedness
  • Unexplained weariness
  • Drowsiness
  • Heartburn
  • Dry mouth
  • Nausea
  • Unexplained weight loss
  • Abdominal cramps
  • Joint pain

The symptoms listed above are all minor side effects which, although they may be uncomfortable, will not cause lasting damage to the patient. These symptoms should all be manageable with over-the-counter remedies and patents do not need to seek medical attention unless any one or more of these symptoms last a long time or is particularly severe. Many patients find that the side effects start to wear off and become less severe as time goes on and the body becomes accustomed to having the drug in its system.

In order to reduce the possibility of dizziness whilst taking rasagiline, patients should take care to stand up slowly if they have been sitting or lying down. Allowing the body time to adjust to a standing position is particularly important at the beginning of treatment, as this is when patients are most likely to experience dizziness.

In rare cases, more serious side effects can be experienced as a result of taking rasagiline. Patients should seek urgent medical attention if they experience any of the following:

  • Fainting
  • Severe or sudden loss of balance
  • Hallucinations
  • Depression
  • Extreme mood changes
  • Unusually strong urges (leading to impulsive behaviour such as gambling or increased sexual advances)
  • Swelling in the legs, ankles and feet
  • Bruising more easily than normal
  • Severe muscle twitches
  • Extreme stiffness

MAO inhibitors increase the levels of serotonin in the brain. If the levels of serotonin become too inflated, this can lead to a very rare but very serious condition known as serotonin syndrome or serotonin toxicity. The risk of developing this condition is greatly increased for patients who are taking more than one form of medication which increases serotonin levels in the brain. The following are all symptoms of serotonin syndrome:

  • Severe nausea
  • Severe vomiting
  • Very fast heartbeat
  • Severe dizziness
  • Sudden and severe loss of coordination
  • Unexplained fever
  • Hallucinations
  • Severe diarrhea
  • Unusual agitation

If one or more of the symptoms listed above are experienced, this could be an indicator of serotonin toxicity and patients should seek immediate medical attention. When speaking to the doctor, make sure it is clear that the patient has been taking MAO inhibitors which can lead to increased serotonin levels.

It is very rare for patients to experience a severe allergic reaction to rasagiline, but it can happen. Symptoms of an allergic reaction include:

  • Itching
  • Rash
  • Difficulty breathing
  • Swollen tongue, face and/or throat
  • Dizziness

If an allergic reaction is suspected, patients should try to seek medical attention before their next dose is due to be taken.

In rare cases, rasagiline can also provoke extremely high blood pressure, known as a hypertensive crisis. This can be fatal. Patients who experience any of the following symptoms could be suffering from sudden increased blood pressure and should seek medical attention immediately:

  • Chest pain
  • Stiff or sore neck
  • Irregular heartbeat
  • Nausea and/or vomiting
  • Changes to eyesight (e.g. Blurred vision)
  • Photo phobia (light sensitivity)
  • Severe headache
  • Sweating

If patients experience any new symptoms whilst taking rasagiline, which are not associated with their condition, it is advisable to contact a doctor straight away. Make sure that they are aware that the patient is taking rasagiline so that they are able to make appropriate recommendations to alleviate, prevent or treat the symptoms.

Dosage

Patients, or their carers, should carefully read the instructions which came with the prescription of rasagiline in order to find specific dosage requirements. Rasagiline can be taken with or without food, but should be swallowed with water.

If patients find that they have missed a dose of rasagiline, they should miss out the missed dose and take the next dose at the normal time. It is important not to take two doses at once, or an extra dose in between normal doses, as this can lead to overdose or increase the severity of side effects.

Usual adult dose

When used as the only drug in a course of treatment for Parkinson’s disease, patients are usually prescribed 1mg to be taken once a day. If the drug is being taken in conjunction with other drugs to treat the symptoms of Parkinson’s Disease, the initial and maintenance doses of rasagiline can range between 0.5 mg to 1 mg to be taken once a day.

The dose may be adjusted if the patient is suffering from kidney or liver disease, in order to reduce the strain on these organs.

There is no dosage recommendation for patients under the age of 18 as it has not been registered as safe for use in children.

Interactions

The combination of two or more different pharmaceuticals in the body can start to cause interactions between the chemicals which can change the way in which the body responds to the drugs. Interactions between drugs can make the medications less effective at treating certain conditions or could increase the possibility or severity of side effects for the patient.

In order to keep track of any potential interactions, patients are advised to keep comprehensive and up-to-date lists of the drugs that they are currently taking, both prescription and non-prescription drugs, so that any interactions can be spotted and prevented ahead of time. Patients should bring this list of drugs to all meetings with their doctor or pharmacist. It is also important not to stop taking a drug, to change the dose or to start taking a new one without first consulting with a doctor or pharmacist.

There are known interactions between rasagiline and the following products:

  • Deutetrabenazine
  • Bupropion
  • Carbamazepine
  • Apraclonidine
  • Dextromethorphan
  • Buspirone
  • Methyldopa
  • Tetrabenazine
  • Cyclobenzaprine
  • Valbenazine
  • Appetite suppressants including diethylpropion
  • Triptans used to treat migraines
  • Food supplements, especially tryptophan and tyramine

MAO inhibitors, such as rasagiline, increase the level of serotonin in the brain. Having too much serotonin in the brain can lead to a condition known as serotonin syndrome. This condition can be fatal if not treated in time. A patient’s risk of developing serotonin syndrome is greatly increased if they are taking more than one drug which is known to increase serotonin levels. Examples of such drugs include:

  • MDMA
  • Ecstasy
  • Tramadol
  • Fentanyl
  • Methadone
  • Tapentadol
  • Meperidine
  • St John’s wort
  • Many antidepressants, including SSRIs, SNRIs and tricyclics

Rasagiline should not be combined with any of the drugs listed above unless specifically advised by a doctor. It is also very unusual to be taking more than one MAO inhibitor at once, due to the increased risk of serotonin syndrome. Again, do not combine MAO inhibitors unless specifically advised by a doctor to do so. It is usually recommended for a period of two weeks to separate courses of different MAO inhibitors in order to reduce the risk of serotonin syndrome.

Rasagiline can cause drowsiness in some of the patients who take the medication. This can become more severe if combined with other drugs which also cause drowsiness. You should tell your doctor or pharmacist if you take other substances which cause you to feel drowsy, including:

  • Codeine
  • Hydrocodone
  • Diazepam
  • Alprazolam
  • Zolpidem
  • Alcohol
  • Antihistamines
  • Marijuana
  • Muscle relaxants

Rasagiline can, in very rare circumstance, cause a hypertensive crisis by increasing the patient’s blood pressure to dangerous levels. When combined with other drugs which can also increase blood pressure, this risk is increased. Patients taking any of the following drugs should report them to their doctor if taking rasagiline alongside them:

  • Stimulants such as ephedrine, phenylalanine, epinephrine and amphetamines
  • Decongestants
  • Dextromethorphan
  • Herbal products which include ephedra and ma Huang

Rasagiline should not be combined with any of these products in the same treatment plan. Patients should speak to their doctor or pharmacist if they are worried about any interactions between different substances they are taking alongside their prescription of rasagiline.

Foods which are rich in tyramine can increase the risk of high blood pressure for patients taking rasagiline. The following foods should, therefore, be avoided where possible:

  • Aged cheeses eg. Extra mature cheddar and blue cheeses
  • Cured and smoked meats and fish eg. Smoked salmon, cured bacon, salami and chorizo
  • Tofu
  • Home-brewed beers
  • Bean curd
  • Draught beers
  • Miso soup
  • Broad beans and fava beans
  • Certain beans, such as fava or broad beans
  • Soy sauce
  • Pickled vegetables
  • Products made with sourdough

Warnings

Sometimes, rasagiline can have an unintended effect on underlying medical conditions which have nothing to do with the symptoms of Parkinson’s disease. Patients should take care to ensure that their doctor always has an up-to-date medical history, as well as a comprehensive record of any drugs that they are currently taking to manage other conditions. When a patient is prescribed rasagiline, it is particularly important to inform their healthcare professional if any of the following statements are true:

  • The patient is allergic to Rasagiline or any of its constituent ingredients
  • The patient has previously had a severe allergic reaction to any other forms of medication
  • The patient currently suffers from, or has ever been diagnosed with, liver disease
  • The patient has taken any medication for depression within the last 2 weeks
  • The patient is taking any of the following drugs; Tramadol, Cyclobenzaprine, Propoxyphene, Dextromethorphan, Meperidine, St. John's Wort or Methadone
  • The patient has taken the drug Fluoxetine within the last 5 weeks
  • The patient suffers from high blood pressure or suffers from attacks of hypertensive crisis

Rasagiline can cause the patient to fall asleep suddenly and without much warning. Patients may find themselves falling asleep whilst eating, talking or performing other normal daily activities. Patients should therefore not drive or operate machinery whilst taking this medication. They should not do anything which requires them to be fully alert at all times.

Rasagiline can cause patients to feel dizzy and in some cases can cause them to faint, especially after standing up. In order to minimize this, patients should stand up slowly after sitting or lying down and should take extra care when using the stairs.

Drinking alcohol is not recommended whilst taking rasagiline. Patients should discuss their condition with their doctor to ascertain whether or not it is safe to drink alcohol whilst receiving treatment.

Storage

As with many forms of medication, rasagiline should be kept in the packaging provided by the pharmacy. It should be closed with an airtight seal in order to protect the drug from external contaminants.

The medication should be clearly labelled so that it cannot be confused with other drugs or supplements. The name on the label should be clearly legible to the patient and any carers who might need access to it. If instructions were provided as to how to take the drug, these should be kept close to the medication at all times in case they need to be used as a reference.

Rasagiline tablets are to be kept somewhere dry, where they cannot be affected by liquid or moisture. This means that they should not be kept in bathrooms or kitchens. Rasagiline should be stored at room temperature, somewhere which is not susceptible to large fluctuations in temperature.

As with all other medications, Rasagiline should be stored somewhere safely out of reach for children and pets, so that they cannot accidentally find and swallow the tablets. Pill boxes and pill minders are not child-resistant in the same way that prescribed containers are. Even very young children can get into most pill boxes quickly and easily. Patients and their carers should be mindful of this when using pill minders to organize medication, especially when children are regularly present in the same house.

Rasagiline is usually only taken once a day, so there is less of a need to carry the medication when out and about for the day. However, if patients do choose to carry their medication with them, the same guidelines should still be followed. The medication should be kept at room temperature, away from moisture and care should be taken to ensure that children and pets are unable to access the drugs.

If the medication reaches its expiry date, or the patient no longer needs it for whatever reason, care should be taken when disposing of the medication. The pills should not be thrown away with household garbage and they should not be flushed down the toilet. Instead, they should be returned to the doctor or pharmacy as part of a medicine take-back program so that they can be disposed of without the risk of harm to others.

Summary

Rasagiline is a form of MAO inhibitor which is used to treat the symptoms of Parkinson’s disease. It is a medication which comes in the form of a tablet, usually taken once a day, and is designed to stop certain enzymes in the body from being able to break down certain chemicals produced in the brain. Many of the symptoms of Parkinson’s disease are caused by low levels of dopamine in the brain, and by stopping enzymes from being able to break down and dispose of dopamine, rasagiline is able to artificially increase dopamine levels and alleviate some of the symptoms associated with Parkinson’s disease.

Rasagiline is not a cure for Parkinson’s, as it is unable to reverse any of the regeneration associated with the disease, but it is able to treat some of the symptoms. By increasing the level of dopamine in the brain, rasagiline can reduce the severity of some of the symptoms associated with motor function and movement, making it easier for patients with Parkinson’s to be more mobile. It can reduce tremors, muscle stiffness and twitches to allow patients to be more comfortable and to regain more control.

As an MAO inhibitor, rasagiline can also increase levels of serotonin in the brain. If combined with other drugs which increase serotonin levels, serious side effects can occur.

 

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Last Reviewed:
January 31, 2018
Last Updated:
January 27, 2018
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