Generic Name: Order eldepryl
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Dry mouth, transient rise of serum alanine aminotransferase ALAT values and sleeping disorders have been reported more frequently than in patients receiving placebo. In combination with levodopaSince selegiline potentiates the effect of levodopa, side effects of levodopa restlessness, hyperkinesis, abnormal movements, agitation, confusion, hallucination, postural hypotension, cardiac arrhythmias may be enhanced in combined therapy levodopa should be usually given in association with a peripheral decarboxylase inhibitor.
Micturition difficulties and skin reactions have also been reported during selegiline treatment. It also inhibits the reuptake of dopamine at the presynaptic dopamine receptor. These effects potentiate dopaminergic function in the brain and help to even out and prolong the effect of exogenous and endogenous dopamine. Thus, selegiline potentiates and prolongs the effect of levodopa in the treatment of parkinsonism.
Double-blind studies on early phase Parkinsonian patients showed that patients receiving selegiline monotherapy manage significantly longer without levodopa therapy than controls receiving placebo.
These patients could also maintain their ability to work longer. The addition of selegiline to levodopa with or without decarboxylase inhibitor therapy helps to alleviate dose related fluctuations and end of dose deterioration. Unlike conventional MAO-inhibitors, which inhibit both the MAO-A and MAO-B enzyme, selegiline is a specific MAO-B inhibitor and can be given safely with levodopa.
Selegiline does not cause the so called "cheese effect" either when used alone as monotherapy, or when used with other drugs, except for moclobemide or nonselective MAO-inhibitors.
Treatment of overdose with non-selective MAOIs is symptomatic and supportive. Hypotension and vascular collapse should be treated with intravenous fluids and, if necessary, blood pressure titration with an intravenous infusion of a dilute pressor agent. It should be noted that adrenergic agents may produce a markedly increased pressor response.
Respiration should be supported by appropriate measures, including management of the airway, use of supplemental oxygen, and mechanical ventilatory assistance, as required. The recommended regimen for the administration of ELDEPRYL is 10 mg per day administered as divided doses of 5 mg each taken at breakfast and lunch. There is no evidence that additional benefit will be obtained from the administration of higher doses.
Moreover, higher doses should ordinarily be avoided because of the increased risk of side effects. Eldepryl may also be used in the management of patients with Parkinson's disease not adequately controlled by conventional therapy or in whom on-off symptoms or other dyskinesias develop during maximal levodopa therapy.
Method of administration Eldepryl may be administered either as a single dose in the morning or in two divided doses of 5 mg, taken at breakfast and lunch. Special PopulationsNo data are known on dose adjustment in patients with mild hepatic impairment.
Renal impairmentNo data are known on dose adjustment in patients with mild renal impairment. Selegiline should not be used in combination with selective serotonin reuptake inhibitors SSRIserotonin noradrenaline reuptake inhibitor SNRI venlafaxinetricyclic antidepressants, sympathomimetics, monoamine oxidase inhibitors e. Selegiline should not be used in patients with active duodenal or gastric ulcer. When selegiline is prescribed in combination with levodopa, the contraindications which apply to levodopa must be taken into account.
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Acutely, reserpine can increase the risk of hypertensive crisis by causing an initial release of catecholamines from bound stores. During chronic administration, additive CNS depressant effects and hypotension are possible. Ritonavir: Concurrent administration of selegiline with ritonavir may result in elevated selegiline plasma concentrations.
Rizatriptan: Rizatriptan is partially metabolized by MAO-A, and is contraindicated for use with non-selective MAOIs, including selegiline in its transdermal form, which inhibits both MAO-A and MAO-B at antidepressant doses.
Serotonin syndrome has been reported during co-administration of serotonin-receptor agonists and monoamine oxidase inhibitors MAOIsdue to the inhibitory effects of MAOIs on MAO-A, which decreases central serotonin degradation. Since oral selegiline selectively inhibits MAO-B at recommended doses, no interaction with serotonin-receptor agonists is expected with usual prescription use.
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Patients should be cautioned about operating hazardous machinery, including automobiles, until they are reasonably certain that selegiline transdermal therapy does not impair their ability to engage in such activities. Advise patients to avoid alcohol during treatment for depression. There have been reports of patients with Parkinson's disease who have fallen asleep while performing activities of daily living, including driving, while receiving drugs that increase dopaminergic tone, including oral selegiline products.
Excessive drowsiness has, in some cases, occurred as late as one year after the initiation of treatment. In some cases excessive drowsiness has resulted in auto accidents or other harmful events in the course of daily living. Symptoms of excessive drowsiness may not be preceded by warning signs such as somnolence.
Before initiating treatment with selegiline, patients should be advised about the potential to develop drowsiness and specifically asked about factors that may increase this risk, such as concomitant use of sedating medications and the presence of sleep disorders.
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Careful monitoring of blood pressure is suggested during concurrent therapy with antihypertensives such as alpha-blockers. Alpha-glucosidase Inhibitors: Animal data indicate that monoamine oxidase inhibitors MAO inhibitors may stimulate insulin secretion. Alprazolam: The CNS-depressant effects of MAOIs can be potentiated with concomitant administration of other drugs known to cause CNS depression including benzodiazepines. Altretamine: Avoid concomitant use of antidepressant MAOIs during altretamine therapy whenever possible.
Concurrent administration of altretamine and antidepressants of the monoamine oxidase MAO inhibitor class may cause severe orthostatic hypotension. Four patients, all over 60 years of age, were reported to have experienced symptomatic hypotension after 4 to 7 days of concomitant therapy with altretamine and MAO inhibitors MAOIs. The mechanism of the interaction is not clear.
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Selegiline should not be used in animals with known hypersensitivity or allergy to the drug.
Isavuconazonium: Concomitant use of isavuconazonium with selegiline may result in increased serum concentrations of selegiline.
It is not known if the higher doses are more effective than the lowest dose.
During concurrent use of other CNS depressants, additive respiratory or CNS depressant effects, hypotension, profound sedation, coma, or death may occur.
Buprenorphine: Concurrent use of opioids with other drugs that modulate serotonergic function, such as monoamine oxidase inhibitors MAOIshas resulted in serotonin syndrome in some cases. In addition, both MAOIs and buprenorphine have CNS depressant effects which may be additive during combination therapy.
Patients should be advised to avoid driving or other tasks requiring mental alertness until the effects of the combination are known. Bupropion: Monoamine oxidase inhibitors MAOIs intended to treat psychiatric disorders are contraindicated for use with bupropion or within 14 days of discontinuing treatment with bupropion.
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Distribution Selegiline is rapidly distributed throughout the body, the apparent volume of distribution being 500 1 after an intravenous 10 mg dose.
In the rat study, there was a decrease in fetal body weight at the highest dose tested.