(and dosage form):
Each tablet contains 5 mg selegiline hydrochloride: ((R)-(-)-N, alpha-dimethyl-N-2-propynyl-phenethylamine hydrochloride).
A 5.4.1. Anti-Parkinsonism preparations.
Selegiline is a selective MAO-B (monoamine oxidase type B) inhibitor which prevents the breakdown of dopamine in the brain. It also inhibits the re-uptake of dopamine at pre-synaptic dopamine receptors. These effects potentiate dopaminergic function in the brain. Thus selegiline acts in Parkinsonism by potentiating and prolonging the effect of levodopa.
Selegiline is rapidly absorbed from the gastro-intestinal tract.
It crosses the blood-brain barrier.
It is rapidly and completely metabolized to N-desmethyldeprenyl, L-methamphetamine and L-amphetamine. The mean half-lives of the 3 active metabolites that were found in serum and urine following a single dose of selegiline are as follows:
N-desmethyldeprenyl 2 hours
L-methamphetamine 17.7 hours
L-amphetamine 20.5 hours
Selegiline is 94% bound to plasma proteins at therapeutic concentrations.
PARKILYNE is indicated in the management of early morning akinesia and nocturnal akinesia in patients with Parkinsons disease being treated with levodopa alone or levodopa and a peripheral decarboxylase inhibitor. At the end-stage of Parkinsons disease, response may be markedly reduced.
PARKILYNE is contra-indicated in patients with a known hypersensitivity to any of the ingredients.
PARKILYNE should be avoided in patients with active ulceration.
PARKILYNE is contra-indicated in patients receiving serotonin receptor agonists such as sumatriptan.
Safety and efficacy in children have not been established.
PARKILYNE is less likely to interact with tyramine in food; such hypertensive reactions have been reported less frequently at usual doses but its selectivity is lost at higher doses and it must be assumed that PARKILYNE can only be used safely without dietary restrictions at doses of up to 10 mg daily.
Even when given in therapeutic doses, life-threatening interactions can occur between PARKILYNE and pethidine.
Serious reactions, sometimes fatal, have also been reported when PARKILYNE has been used with tricyclic antidepressants or selective serotonin reuptake inhibitors (SSRIs)
It is recommended that 14 days should elapse between discontinuation of PARKILYNE and starting treatment with tricyclic antidepressants or SSRIs. Conversely, PARKILYNE should not be given to patients who have recently received these antidepressants; at least 5 weeks should elapse between discontinuing fluoxetine and starting treatment with PARKILYNE.
MAO-A inhibitors, e.g. moclobemide should not be used with PARKILYNE due to the lack of clinical experience with this combination.
PREGNANCY AND LACTATION:
The safety during pregnancy and lactation has not been established.
DOSAGE AND DIRECTIONS FOR USE:
PARKILYNE should always be given together with existing levodopa therapy.
The initial dose is one tablet (5 mg) in the morning.
If the patient develops side-effects, the dose of levodopa should be reduced.
If no response is achieved with PARKILYNE treatment, e.g. the on-offsymptoms, the dose can be increased to two tablets (10 mg) in the morning.
SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Because PARKILYNE potentiates the effects of levodopa, side-effects of levodopa may be potentiated. Dyskinesias may be aggravated when PARKILYNE is added to levodopa but may clear when the dose of levodopa is reduced.
Less frequent: Hypotension; chest pain.
Frequent: Nausea; vomiting; dry mouth.
Less frequent: Constipation; diarrhoea; stomatitis.
Less frequent: Transient increases in liver enzymes have been reported.
Less frequent: Back pain; muscle cramps; joint pain; myopathy.
Nervous system disorders:
Frequent: Dyskinesias; dizziness; vertigo. (The diskinesias are usually of the cervico-facial lingual type or consist of oscillatory and rocking movements of the arms, legs or trunk. Less frequently, exaggerated respiratory movements can produce an irregular gasping pattern of hyperventilation.
Less frequent: Headache; tremor; agitation.
Frequent: Confusion; psychosis; depression.
Less frequent: Hallucinations; insomnia; abnormal dreams. (Evening doses should be avoided.
Renal and urinary disorders:
Less frequent: Difficulty in micturition.
Less frequent: Sore throat.
Less frequent: Skin reactions.
PARKILYNE should be used with caution in patients with a history of peptic ulceration.
It should also be used with caution in uncontrolled hypertension, arrhythmias, angina, or psychosis.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Overdosage may result in amphetamine-like central nervous system effects including pupil dilation, sweating and agitation.
Treatment is symptomatic and PARKILYNE should be withdrawn.
White, flat, round tablets, notch on the one side, beveled edge.
A carton containing 30 tablets packed in PVC/PVDC/Aluminium foil blister strips.
Store below 25°C and protect from light. Store in original package until required for use.
KEEP OUT OF REACH OF CHILDREN.
NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION:
Generix International SA (Pty) Ltd
Cnr. Pooke and Ester Roads,
Athlone, Industria, Cape Town
DATE OF PUBLICATION OF THE PACKAGE INSERT:
23 September 2005
New addition to this site: January 2007
Source: Pharmaceutical Industry
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