Alzheimer's And Parkinson'sAzilect (Generic)
Generic drugs, marketed without brand names, contain the exact same active ingredients used in their brand-name counterparts, but cost significantly less. The drugs are required to meet US Food and Drug Administration (FDA) standards for safety, purity and effectiveness.
Azilect
MAO-B is an enzyme that breaks down monoamines, and azilect blocks that enzyme. It accomplishes its purpose by elevating particular chemical concentrations in the brain. The symptoms of Parkinson's disease can be managed using the medication Azilect (stiffness, tremors, spasms, poor muscle control). Levodopa is another medication that is occasionally used with azilect in treatment.
Azilect, known generically as rasagiline, is a medication primarily used in the treatment of Parkinson's disease. It belongs to a class of drugs called monoamine oxidase-B (MAO-B) inhibitors, which work by increasing the levels of certain chemicals in the brain that are involved in the regulation of movement and mood. Azilec is widely recognized for its efficacy in managing the symptoms of Parkinson's disease, both as a monotherapy in early stages and as an adjunct therapy in more advanced stages of the disease. This article delves into the pharmacology, therapeutic uses, clinical efficacy, safety profile, and other relevant aspects of Azilect.
Pharmacology
Mechanism of Action
Azilect exerts its therapeutic effects primarily through the inhibition of monoamine oxidase-B (MAO-B), an enzyme responsible for the breakdown of dopamine in the brain. By inhibiting MAO-B, rasagiline increases the availability of dopamine, a neurotransmitter that is critically involved in the regulation of movement. Dopamine levels are significantly reduced in Parkinson's disease due to the degeneration of dopaminergic neurons in the substantia nigra, a region of the brain. By enhancing dopaminergic activity, Azilect helps to alleviate the motor symptoms associated with Parkinson's disease, such as bradykinesia (slowness of movement), rigidity, and tremors.
In addition to its MAO-B inhibitory activity, rasagiline has been suggested to have neuroprotective properties. Preclinical studies have indicated that rasagiline may protect neurons from oxidative stress and apoptosis (programmed cell death), although the clinical significance of these effects in humans remains to be fully elucidated.
Pharmacokinetics
Absorption: Rasagiline is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 0.5 to 1 hour. The bioavailability of rasagiline is approximately 36%, and food does not significantly affect its absorption.
Distribution: Rasagiline is widely distributed throughout the body and readily crosses the blood-brain barrier, which is essential for its action in the central nervous system. The drug is highly bound to plasma proteins (approximately 88-94%).
Metabolism: Rasagiline undergoes extensive hepatic metabolism, primarily via cytochrome P450 1A2 (CYP1A2). The major metabolite is 1-aminoindan, which is pharmacologically inactive.
Excretion: The elimination half-life of rasagiline is approximately 1.5 to 3.5 hours. The drug and its metabolites are primarily excreted in the urine, with a smaller portion eliminated in the feces.
Therapeutic Uses
Parkinson's Disease
Azilect is indicated for the treatment of Parkinson's disease, both as monotherapy in early-stage disease and as an adjunct to levodopa in more advanced stages. Parkinson's disease is a progressive neurodegenerative disorder characterized by the loss of dopaminergic neurons in the substantia nigra, leading to motor and non-motor symptoms.
Monotherapy: In early-stage Parkinson's disease, Azilect can be used as a standalone treatment to manage motor symptoms. Clinical trials have demonstrated that rasagiline monotherapy significantly improves motor function and delays the need for levodopa therapy.
Adjunct Therapy: In patients with more advanced Parkinson's disease who are experiencing motor fluctuations (e.g., "wearing-off" phenomena) despite levodopa therapy, Azilect can be added to the treatment regimen. Rasagiline has been shown to reduce "off" time (periods when levodopa is not effective) and improve motor function during "on" time (periods when levodopa is effective).
Clinical Efficacy
The efficacy of Azilect in the treatment of Parkinson's disease has been demonstrated in several large-scale clinical trials.
TEMPO Study: The TEMPO trial was a pivotal study that evaluated the efficacy of rasagiline in early-stage Parkinson's disease. Patients treated with rasagiline experienced significant improvements in motor function compared to placebo. The study also suggested that early initiation of rasagiline therapy may have long-term benefits in slowing disease progression.
PRESTO and LARGO Studies: These trials evaluated the use of rasagiline as an adjunct to levodopa in patients with advanced Parkinson's disease. Both studies demonstrated that rasagiline significantly reduced "off" time and improved motor function compared to placebo.
Safety and Tolerability
Azilect is generally well-tolerated, with most adverse effects being mild to moderate in severity. However, as with any medication, there are potential risks and side effects that need to be considered.
Common Side Effects
Gastrointestinal: Nausea, vomiting, and abdominal pain are among the most commonly reported gastrointestinal side effects.
Neurological: Dizziness, headache, and somnolence (drowsiness) may occur, particularly during the initial stages of treatment.
Psychiatric: Some patients may experience hallucinations, confusion, or depression, although these side effects are less common.
Serious Side Effects
Hypertensive Crisis: Although rare, rasagiline can potentially cause a hypertensive crisis if taken with tyramine-rich foods or other medications that increase serotonin levels (e.g., selective serotonin reuptake inhibitors, SSRIs). This is due to the drug's MAO-B inhibitory activity, which can also inhibit MAO-A at higher doses, leading to an accumulation of tyramine and serotonin.
Serotonin Syndrome: The combination of rasagiline with other serotonergic agents (e.g., SSRIs, SNRIs, tricyclic antidepressants) can increase the risk of serotonin syndrome, a potentially life-threatening condition characterized by hyperthermia, muscle rigidity, autonomic instability, and mental status changes.
Contraindications
Azilect is contraindicated in patients with a known hypersensitivity to rasagiline or any of its components. It should also be avoided in patients taking other MAO inhibitors, meperidine, or certain other medications that can interact with rasagiline and increase the risk of adverse effects.
Drug Interactions
Azilect has the potential to interact with several other medications, which can alter its efficacy or increase the risk of adverse effects.
MAO Inhibitors: Concurrent use of other MAO inhibitors (e.g., phenelzine, tranylcypromine) is contraindicated due to the increased risk of hypertensive crisis.
Serotonergic Agents: As mentioned earlier, the combination of rasagiline with serotonergic agents (e.g., SSRIs, SNRIs, tricyclic antidepressants) can increase the risk of serotonin syndrome.
CYP1A2 Inhibitors: Medications that inhibit CYP1A2 (e.g., ciprofloxacin, fluvoxamine) can increase the plasma concentration of rasagiline, potentially leading to an increased risk of adverse effects.
Tyramine-Rich Foods: Although the risk is lower with selective MAO-B inhibitors like rasagiline, patients are generally advised to avoid excessive consumption of tyramine-rich foods (e.g., aged cheeses, cured meats) to reduce the risk of hypertensive crisis.
Special Populations
Elderly: The elderly population may be more susceptible to the side effects of rasagiline, particularly dizziness and hallucinations. Dose adjustments may be necessary based on the patient's overall health and renal/hepatic function.
Renal Impairment: No significant dose adjustments are required for patients with mild to moderate renal impairment. However, caution is advised in patients with severe renal impairment, as there is limited data on the safety and efficacy of rasagiline in this population.
Hepatic Impairment: Rasagiline is metabolized in the liver, and patients with hepatic impairment may require dose adjustments. The drug is contraindicated in patients with severe hepatic impairment.
Pregnancy and Lactation: There is limited data on the use of rasagiline in pregnant or breastfeeding women. The drug should be used during pregnancy only if the potential benefits outweigh the risks. It is not recommended for use in breastfeeding women due to the potential for adverse effects in the infant.
Conclusion
Azilect (rasagiline) is a valuable therapeutic option for the management of Parkinson's disease, offering both symptomatic relief and potential neuroprotective benefits. Its efficacy as both monotherapy and adjunct therapy has been well-established in clinical trials, making it a versatile option for patients at different stages of the disease. While generally well-tolerated, healthcare providers must be vigilant about potential drug interactions and contraindications to ensure the safe and effective use of Azilect. As with any medication, individualized treatment plans should be developed based on the patient's specific needs, medical history, and overall health status. Ongoing research continues to explore the full potential of rasagiline in the treatment of Parkinson's disease and other neurodegenerative disorders, offering hope for improved outcomes and quality of life for patients.
Rasagiline tablet
What is this medicine?
Rasagiline is a monoamine oxidase-B (MAO-B) inhibitor. It accomplishes its purpose by elevating particular chemical concentrations in the brain. The signs and symptoms of Parkinson's disease can be alleviated with the help of rasagiline (stiffness, tremors, spasms, poor muscle control). In rare cases, rasagiline is used with another medication known as levodopa. Rasagiline may also be used for uses not included in this pharmaceutical guide.
Before I start using this medication, what should I discuss with my health care providers?
If you have an allergy to rasagiline, you should not take the medication. There are a number of medications that are known to interact negatively with rasagiline and should not be used at the same time. If you take any of the following medications, including cyclobenzaprine (a muscle relaxer), dextromethorphan (which is found in many over-the-counter cough medicines), meperidine (Demerol), methadone, St. John's wort, or tramadol, your doctor may need to make adjustments to the treatment plan he or she has devised for you (Ultram, Ultracet).
Do not take rasagiline if you have used any other MAO inhibitor in the prior 14 days. There is a possibility of a potentially lethal interaction between drugs. Isocarboxazid, linezolid, methylene blue injection, phenelzine, selegiline, and tranylcypromine are some examples of MAO inhibitors. Other examples include phenelzine. To be sure rasagiline is safe for you, notify your doctor if you have:\shigh or low blood pressure;\sliver disease;\sif you take an antidepressant; or\sif you take ciprofloxacin (an antibiotic) (an antibiotic).
Individuals with Parkinson's disease may have an increased risk of skin cancer (melanoma) (melanoma). Discuss this risk and the skin signs you should look out for with your primary care physician. It is not known whether rasagiline will damage an unborn fetus. Inform your doctor if you are pregnant or intend to become pregnant while using this prescription. It is not known whether rasagiline goes into breast milk or if it might affect a breastfeeding infant. If you are breastfeeding a child, you should let your doctor know about it.
What is the correct way to take this medication?
Always make sure to follow all of the instructions on the label of your medication. In order to optimize your treatment and provide the best possible outcomes, your physician may adjust your dosage on occasion. Do not use this medication in greater or lower doses than indicated, nor for a longer period of time than specified. If you are using rasagiline by itself, rather than in combination with other Parkinson's drugs, your dose may be adjusted accordingly. Always adhere to the dose directions provided by your physician.
Rasagiline is simply one component of a comprehensive treatment program that may also involve the formulation of a personalized food plan by your attending physician or nutritionist. When taking rasagiline, if your Parkinson's symptoms do not improve or if they become worse, you should make an appointment with your primary care physician. Do not abruptly stop taking rasagiline or you risk experiencing withdrawal symptoms, which can be quite uncomfortable. Ask your healthcare provider how you can discontinue using rasagiline in a secure manner.
What should I do if I forget a dose?
When you realize you missed a dosage, take it as soon as you can. If it is almost time for your next scheduled dosage, you should skip the dose that you missed. It is not necessary to take additional medication in order to make up for a missed dosage.
What other substances could react with this medication?
If you are also taking an antidepressant, using rasagiline might cause your body to produce an abnormally high amount of serotonin. Agitation, hallucinations, fever, rapid heart rate, hyperactive reflexes, nausea, vomiting, diarrhea, lack of coordination, and fainting are some of the symptoms of this illness. Inform your doctor if you have taken an antidepressant during the 2-week period before you start taking rasagiline.
When used with other sedative medications, rasagiline's drowsiness-inducing properties can become even more pronounced. Inquire with your physician before using rasagiline with a medication for sleeping aids, narcotic pain relievers, muscle relaxants, or medications for anxiety or seizures.
Rasagiline can interact with a wide variety of other medications, and certain medications should never be used together. This include both prescription and over-the-counter medications, in addition to herbal and vitamin supplements. This drug guide does not provide a description of all potentially harmful interactions. Talk to your primary care physician about any and all medications you take, including those that you begin or discontinue taking while you are receiving rasagiline therapy. Provide any healthcare practitioner who is treating you with a list of all the medications you are currently taking.
What potential negative reactions may I have to this medication?
You should seek immediate medical attention if you experience any of the following symptoms of an allergic reaction: hives, difficulty breathing, and swelling of the face, lips, tongue, or neck are all symptoms of anaphylaxis.
If you experience extreme drowsiness, falling asleep suddenly, even after feeling alert; unusual changes in mood or behavior; a lightheaded feeling, like you might pass out; worsening symptoms of Parkinson's disease (especially uncontrolled muscle movements); or dangerously high blood pressure, you should immediately stop using rasagiline and call your doctor.
�severe chest discomfort, shortness of breath, irregular heartbeats, seizures, blurred vision, severe headache, pounding in the neck or ears, nosebleed, anxiety, disorientation, and severe headache, blurred vision, pounding in the neck or ears.
Several persons who use rasagiline in conjunction with levodopa have reported falling asleep during routine daily activities such as working, chatting, eating, or driving while they were taking the combination medication. If you find that you are falling asleep during the day, it is important that you discuss this issue with your primary care physician.
When you are on this medication, you can experience heightened sexual impulses, unexpected cravings to gamble, or other powerful urges. These side effects are possible. If this happens, you should consult with your physician.
Dizziness, drowsiness, trouble sleeping (insomnia), strange dreams, depression, upset stomach, nausea, vomiting, stomach pain, loss of appetite, weight loss, constipation, joint pain or stiffness, swelling in your hands or feet, dry mouth, cough, or symptoms of the common cold are some of the common side effects that may occur (fever, chills, body aches).
This list of potential adverse effects is not exhaustive; additional symptoms may also surface.
What side effects should I be on the lookout for when using this medication?
It's possible that rasagiline will affect either your thoughts or your emotions. It is best not to drive a vehicle or operate heavy machinery until you have a better idea of how this medication may effect you. If you have been sitting or lying down, you should avoid getting up too quickly because you may have dizziness. In order to avoid falling, carefully stand up while keeping your balance.
It's possible that drinking alcohol will make certain rasagiline adverse effects worse.
Additionally, stay away from foods that are rich in tyramine, such as aged cheeses, sour cream, yogurt, avocados, bananas, and soy sauce, as well as pepperoni and other dried meats. Consuming tyramine while also taking rasagiline might cause your blood pressure to rise to potentially harmful levels, which can lead to other adverse consequences that could endanger your life.
Where should I store this prescription medication?
Keep at room temperature and away from heat and moisture when storing.
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try out a different kind and see if it was a better fit for my needs. Which it was!
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crossed my mind how much cheaper the generic versions were. When I started browsing the
items I couldn’t believe the price difference! This is my go to shop right now.
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always bought it in store. I spoke to one of their support reps and they were really nice
and helped to explain how it works and made me feel much more comfortable with my order!
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and it definitely won’t be my last! They had all the items I needed in one place and the
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