SELEGILINE

COMMON BRAND NAME(S): Eldepryl

GENERIC NAME(S): SELEGILINE HCL

 

Description: Selegiline is a monoamine oxidase (MAO) , type B inhibitor.  It is believed to prevent tyramine and other indirect acting sympathomimetics from displacing norepinephrine from adrenergic neurons. This mechanism helps to slow the progression of Parkinson’s disease.

Pharmacokinetics:

Absorption: Approximately 10% of the drug is absorbed in the gastrointestinal tract

Distribution: Rapidly distributed throughout the body and crosses the blood-brain barrier.

Metabolism: Extensive hepatic first-pass effect

Excretion: Mainly as metabolites in the urine; about 15% is excreted via faeces. Elimination half-life: about 10 hr.

Indications:

Used in combination with levodopa or carbidopa to control symptoms of movement disorders caused by Parkinson’s disease. It may improve shakiness (tremor), muscle stiffness, loss of normal movement as your dose of other Parkinson’s medication wears off (end-of-dose failure), and sudden switching between normal movement and stiffness (“on-off” problems). It may improve your range of motion and ability to walk, dress, and exercise.

OTHER USES:

May also be given for adult depression.

Contraindications:

Should not be given to patients who had known allergic reaction with this drug.

Should not be given with drugs such as meperidine and opioids.

How to use selegiline:

Dosage (depends on the condition):

Parkinson’s disease- Take 5 mg of this medication by mouth, usually twice daily with breakfast and lunch.

Adult Depression- Apply one 6 mg/24 hours transdermal patch to intact skin once every 24 hours

  • Taking selegiline late in the day may cause trouble sleeping.
  • After you have been taking selegiline for 2 or 3 days, your doctor may direct you to lower your levodopa dose. Follow your doctor’s instructions closely.
  • It may take a few weeks for the full benefits of the drug to be noticed. Do not stop taking this drug without first consulting your doctor. Talk with your doctor if the medication stops working well or if your condition worsens.

Availability: This is a prescription only drug.

Severe CNS toxicity associated with hyperpyrexia and death have been reported with selegiline.

Another patient receiving protriptyline and selegiline hcl developed tremors, agitation, and restlessness followed by unresponsiveness and death two weeks after selegiline hcl was added.

Related adverse events including hypertension, syncope, asystole, diaphoresis, seizures, changes in behavioral and mental status, and muscular stiffness have also been reported in some patients receiving selegiline hcl and various tricyclic antidepressants.

Serious, sometimes fatal, reactions with signs and symptoms that may include hyperthermia, rigidity, myoclonus, autonomic instability with rapid fluctuations of the vital signs, and mental status changes that include extreme agitation progressing to delirium and coma have been reported with patients receiving a combination of fluoxetine hydrochloride and nonselective MAOIs. Similar signs have been reported in some patients on the combination of selegiline hcl (10 mg a day) and selective serotonin reuptake inhibitors including fluoxetine, sertraline and paroxetine.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

It is advised to consult your doctor or pharmacist when any of these side effect manifest.

Most common side effects:

  • dizziness,
  • abdominal pain,
  • dry mouth,
  • nausea,
  • stomach upset,
  • trouble sleeping, and
  • headache may occur

Side effects from the levodopa when taking selegiline. Tell your doctor immediately if any of these side effects occur:

  • nausea,
  • shakiness,
  • muscle stiffness,
  • mental/mood changes such as hallucinations/abnormal dreams.

Some people taking selegiline have fallen asleep suddenly during their usual daily activities (such as talking on the phone, driving). If you experience increased sleepiness or fall asleep during the day, do not drive or take part in other possibly dangerous activities until you have discussed this effect with your doctor. Your risk of this sleep effect is increased by using alcohol or other medications that can make you drowsy. See also Precautions section.

Tell your doctor right away if you have any serious side effects, including:

  • Fainting, loss of balance, mental/mood changes (e.g., agitation, confusion, depression, hallucinations), unusual strong urges (such as increased gambling, increased sexual urges), worsening muscle stiffness/twitching, changes in sexual ability/interest, increased shaking (tremor), swollen ankles/legs, difficulty urinating, unusual weight gain, easy bleeding/bruising, black/tarry stools, vomit that looks like coffee grounds.
  • This drug may rarely cause an attack of extremely high blood pressure (hypertensive crisis), which may be fatal. Many drug and food interactions can increase this risk. (See also Drug Interactions section.) Get medical help right away if any of these serious side effects occur: frequent/severe headache, fast/slow/irregular/pounding heartbeat, chest pain, neck stiffness/soreness, severe nausea/vomiting,sweating/clammy skin (sometimes with fever), widened pupils, vision changes (e.g., double/blurred vision), sudden sensitivity to light (photophobia).
  • This medication may increase serotonin and rarely cause a very serious condition called serotonin syndrome. The risk increases if you are also taking other drugs that increase serotonin, so tell your doctor or pharmacist of all the drugs you take. Get medical help right away if you develop some of the following symptoms: hallucinations, unusual restlessness, loss of coordination, fast heartbeat, severe dizziness, unexplained fever, severe nausea/vomiting/diarrhea, twitching muscle.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Precautions:

General:

This drug may make you dizzy or drowsy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages. See also Side Effects section.

To minimize dizziness and the risk of fainting, get up slowly when rising from a sitting or lying position.

Before having surgery, tell your doctor or dentist you are taking this medication. You may need to stop taking this drug beforehand. Follow your doctor’s instructions carefully.

  • Allergy: Before taking selegiline, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies.
  • Medical History: Before using this medication, tell your doctor or pharmacist if you had:a certain kind of adrenal gland tumor (pheochromocytoma), cerebrovascular disease (e.g., stroke), heart problems (e.g., congestive heart failure, heart attack), bleeding problems, history of severe/frequent headaches, peptic ulcer, diabetes, personal/family history of mental/mood disorders (e.g., schizophrenia,bipolar disorder), personal/family history of high blood pressure, liver disease,overactive thyroid (hyperthyroidism).

Pregnancy Risk: Categoy C- Selegiline should be used only when clearly needed during pregnancy.

Breastfeeding: It is not known if this drug passes into breast milk. Consult your doctor before breast-feeding.

Interactions

  • Some products that may interact with selegiline include: antidepressants (including bupropion, maprotiline, mirtazapine), other MAO inhibitors (isocarboxazid, linezolid, methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, tranylcypromine), appetite suppressants (such as diethylpropion), drugs for attention deficit disorder (such as atomoxetine, methylphenidate), apraclonidine, buspirone, carbamazepine/oxcarbazepine, cyclobenzaprine, certain herbal products (such as ephedra/ma huang), cold medications/nasal decongestants (such as phenylephrine, phenylpropanolamine, pseudoephedrine), fentanyl, street drugs (such as LSD, mescaline), stimulants (such as amphetamines, ephedrine), supplements (such as tryptophan, tyramine), tetrabenazine, certain “triptans” used to treat migraine headaches (such as rizatriptan, sumatriptan, zolmitriptan).
  • The risk of serotonin syndrome/toxicity increases if you are also taking other drugs that increase serotonin. Examples include street drugs such as MDMA/”ecstasy,” St. John’s wort, dextromethorphan, certain antidepressants (including SSRIs such as fluoxetine/paroxetine, SNRIs such as duloxetine/venlafaxine, TCAs such as amitriptyline/doxepin), certain narcotic medications (such as meperidine, methadone, pentazocine, propoxyphene, tramadol, tapentadol), among others. The risk of serotonin syndrome/toxicity may be more likely when you start or increase the dose of these drugs.
  • Tell your doctor or pharmacist if you are using any of these medications before, during, or within 2 weeks after treatment with selegiline. Tell your doctor or pharmacist if you have taken fluoxetine during at least 5 weeks before starting selegiline. Discuss with your doctor how much time to wait between starting or stopping any of these drugs and taking selegiline.
  • Check the labels on all your medicines (such as allergy, cough-and-cold products, diet pills) because they may contain dextromethorphan, decongestants, or stimulants. Ask your pharmacist about the safe use of those products.
  • To prevent a very serious high blood pressure reaction, it is very important that you follow a special diet recommended by your doctor or dietician in order to limit your intake of tyramine while you are taking this medicine. Avoid foods and beverages that are high in tyramine, including: aged cheeses (e.g., bleu, cheddar, parmesan), dried/aged/fermented meats and sausages (e.g., salami, liverwurst), preserved fish (e.g., pickled herring), products containing large amounts of yeast (e.g., concentrated yeast extract, bouillon cubes, powdered soup/gravy, homemade or sourdough bread), fermented foods (e.g., sauerkraut, kim chee), most soybean products (e.g., soy sauce, tofu), broad/fava beans, red wine, sherry, tap beers, vermouth. Limit or avoid foods that are moderate in tyramine, including: avocados, bananas, eggplant, green beans, raisins, raspberries, red plums, spinach, tomatoes, chocolate, cultured dairy products (e.g., buttermilk, yogurt, sour cream), fish eggs, pate, peanuts, coffee, cola, alcohol-free beer, bottled beer, distilled spirits, port, white wine. Consult your doctor or dietician for more details and a complete list of other tyramine-containing foods you should limit or avoid. Seek immediate medical attention if you notice symptoms of very high blood pressure such as unusually fast/slow heartbeat, vomiting, unexplained sweating, headache, chest pain, sudden vision changes, weakness on one side of the body, slurred speech.

This medication may interfere with certain medical/laboratory tests (including brain scan for Parkinson’s disease), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

Overdose

If overdose is suspected, contact a poison control center or emergency room immediately.

Symptoms of overdose may be not appear for up to 12 hours and may include:

  • excitement,
  • irritability,
  • restlessness,
  • dizziness,
  • weakness,
  • drowsiness,
  • flushing,
  • sweating,
  • fast heartbeat,
  • headache,
  • confusion, and
  • seizures.

Notes

Do not share this medication with others.

People with Parkinson’s disease may have an increased risk for developing skin cancer (melanoma). Tell your doctor promptly if you notice a change in the appearance or size of moles or other unusual skin changes. Ask your doctor if you should have regular skin exams.

Missed Dose

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

Storage

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Brands:

Available Brands

  • Selegos [ Medochemie ]

Also marketed as

  • Jumex [ sanofi-aventis ]

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