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Rasagiline; Indications, Dosage, Side effects, Drug Interaction ,Pregnancy

Rasagiline is only found in individuals that have used or taken this drug. It is an irreversible inhibitor of monoamine oxidase and is used as a monotherapy in early Parkinson’s disease or as an adjunct therapy in more advanced cases. The precise mechanisms of action of rasagiline is unknown. One mechanism is believed to be related to its MAO-B inhibitory activity, which causes an increase in extracellular levels of dopamine in the striatum. The elevated dopamine level and subsequent increased dopaminergic activity are likely to mediate rasagiline’s beneficial effects seen in models of dopaminergic motor dysfunction.

Mechanism of action of Rasagiline

The anti-Parkinson drug rasagiline an irreversible and selective monoamine oxidase (MAO)-B inhibitor, was shown to possess neuroprotective activities, involving multiple survival pathways among them the up-regulation of protein kinase C (PKC)alpha, PKCepsilon, the anti-apoptotic Bcl-2, Bcl-xL, and Bcl-w and the induction of brain-derived- and glial cell line-derived neurotrophic factors (BDNF, GDNF). More recently, employing conventional neurochemical techniques, as well as transcriptomic and proteomic screening tools, combined with a biology-based clustering method, it was shown that rasagiline also possesses neurorescue/neurogenesis activity in mice midbrain dopaminergic neurons when given chronically, post-MPTP (N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine). This action was attributed to the activation of cell signaling mediators associated with neurotrophic factors responsive-tyrosine kinase receptor (Trk) pathway, including ShcC, SOS, AF6, Rin1, and Ras and the increase in the Trk-downstream effecter phosphatidylinositol 3 kinase (PI3K) protein and its substrate, Akt/PKB.

Rasagiline mesylate, a propargylamine, is an irreversible monoamine oxidase-B (MAO-B) inhibitor. MAO is a mitochondrial enzyme that regulates the metabolic degradation of catecholamines and serotonin in the CNS and peripheral tissues. There appear to be at least 2 isoforms of MAO, MAO-A, and MAO-B, which differ in localization and substrate specificity. MAO-A, predominantly found in the GI tract and liver, regulates the metabolic degradation of circulating catecholamines and dietary amines (e.g., tyramine). MAO-B, predominantly found in the brain, regulates the metabolic degradation of dopamine and phenylethylamine. Inhibition of MAO-A in the periphery results in systemic absorption of dietary amines (e.g., tyramine), which, in substantial amounts, can cause the release of norepinephrine and subsequent substantial increases in blood pressure. Inhibition of MAO-B results in increased extracellular concentrations of dopamine and, therefore, enhanced dopaminergic activity in the striatum. While the precise mechanisms of action of rasagiline have not been fully characterized, data from ex vivo animal studies indicate that the drug potently and irreversibly inhibits MAO-B in brain, liver, and intestinal tissues; the selectivity of rasagiline in inhibiting MAO-B (and not MAO-A) in humans has not been fully elucidated to avoid restriction of dietary tyramine and sympathomimetic amines.

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Indications of Rasagiline

Parkinson’s Disease
For the treatment of the signs and symptoms of idiopathic Parkinson’s disease as initial monotherapy and as the adjunct therapy to levodopa.
indicated for the treatment of idiopathic Parkinson’s disease (PD) as monotherapy (without levodopa) or as adjunct therapy (with levodopa) in patients with end of dose fluctuations.
Rasagiline Mylan is indicated for the treatment of idiopathic Parkinson’s disease (PD) as monotherapy (without levodopa) or as adjunct therapy (with levodopa) in patients with end of dose fluctuations.
Rasagiline Ratiopharm is indicated for the treatment of idiopathic Parkinson’s disease (PD) as monotherapy (without levodopa) or as adjunct therapy (with levodopa) in patients with end of dose fluctuations.
Rasagiline is used as initial monotherapy or as adjunctive therapy to levodopa for the symptomatic treatment of the idiopathic parkinsonian syndrome.

Contra-Indications of Rasagiline

Malignant melanoma
Severe mental disorder with loss of personality & reality
Abnormal movements of facial muscles and tongue
Abnormal heart rhythm
Blood pressure drop upon standing
Liver problems
Kidney disease with a reduction in kidney function
Allergies to monoamine oxidase inhibitors

Dosage of Rasagiline

Strengths: 0.5 mg; 1 mg

Parkinson’s Disease

Recommended dose: 1 mg orally once a day

Adjunct therapy

Initial dose (in patients on concomitant levodopa): 0.5 mg orally once a day
Initial dose (in patients not on concomitant levodopa): 1 mg orally once a day
Maintenance dose: 0.5 mg to 1 mg orally once a day
Maximum dose: 1 mg orally once a day

Side Effects of Rasagiline

The most common

Dizziness
Orthostatic hypotension
Xerostomia (dry mouth)
A headache
Fatigue
Skin reactions
Hypotension
Anxiety
Constipation
Sedation (dose-dependent)
Nausea/vomiting
Weight gain/loss
Pain below the ear (from salivary gland)
Erectile dysfunction

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More common

Abdominal or stomach pain, discomfort, or tenderness
chills or fever
difficulty with moving
headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
discomfort in arms, shoulders, neck or upper back
excessive sweating
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
rust colored urine
decreased amount of urine

Rare

Anxiety
change in vision
chest pain or tightness
confusion
a cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
fainting
hallucinations
a headache
irritability
lightheadedness
mood or mental changes
muscle pain or cramps
muscle spasm or jerking of all extremities
nervousness

Drug Interactions of Rasagiline

Rasagiline may interact with the following drug, supplements, & may change the efficacy of drugs

benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
cyclobenzaprine
levodopa
MAO inhibitors (e.g., phenelzine, tranylcypromine, )
beta-agonists (e.g., formoterol, salbutamol, salmeterol)
other beta-blockers (e.g., propranolol, metoprolol)
calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
carbamazepine
cyclosporine
dexamethasone
diuretics (water pills; e.g., furosemide, hydrochlorothiazide)
duloxetine
levodopa
sympathomimetic medications (e.g., pseudoephedrine, phenylephrine, ephedrine)
tramadol
lidocaine
MAO inhibitors (e.g., phenelzine, moclobemide, )
macrolide antibiotics (e.g., azithromycin, clarithromycin, erythromycin)
nilotinib
nonsteroidal anti-inflammatory drugs (NSAIDs; e.g., ibuprofen, naproxen)
pentoxifylline
phosphodiesterase-5-inhibitors (e.g., sildenafil, tadalafil)
selective serotonin reuptake inhibitors (SSRI; e.g., fluoxetine, paroxetine, sertraline)
tricyclic antidepressants (e.g., amitriptyline, doxepin, nortriptyline)

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Pregnancy Catagory of Rasagiline

FDA Pregnancy Category C

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

It is not known if rasagiline passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children.