Drug Class Description

Generic Name

Drug Description

Presentation

Indications

Adjunctive therapy in combination with levodopa (with a peripheral decarboxylase inhibitor) in the treatment of Parkinson's disease. Zelapar in combination with maximal levodopa therapy is indicated particularly in patients who experience fluctuations in their condition such as 'end-dose' type fluctuations, 'on-off' symptoms or other dyskinesias. Zelaparmay be used alone in early Parkinson's disease for symptomatic relief and/or to delay the need for levodopa.

Adult Dosage

When prescribed as monotherapy for the first time in the early stage of Parkinson's disease or as an adjuvant to levodopa, the dose of Zelaparis one 1.25 mg unit placed on the tongue in the morning, at least five minutes before breakfast and allowed to dissolve. The unit will dissolve rapidly (in less than 10 seconds) in the mouth. The patient should not eat, drink, rinse or wash-out out their mouth for five minutes after taking their medicine to enable selegiline to be absorbed pre-gastrically.

When Zelapa adjunctive therapy is prescribed a reduction (10 to 30%) in the dose of levodopa is usually required. Reduction of the levodopa dose should be gradual in steps of 10% every 3 to 4 days.

No dosage adjustment is required for patients with renal or hepatic impairment.

Do not push the Zelapar tablet through the foil blister. Peel back the foil and carefully remove the unit.

Unused tablets must be disposed of after three months of a sachet opening.

Child Dosage

Contra Indications

Zelapar is contra-indicated in patients with known hypersensitivity (including severe dizziness or hypotension) to conventional selegiline tablets or liquid or any of the excipients used in this product.

Zelapar is contra-indicated in patients receiving treatment with serotonin-agonists (e.g. sumatriptan, naratriptan, zolmitriptan and rizatriptan).

Zelapar is contra-indicated in patients with phenylketonuria due to the content of aspartame, a source of phenylalanine.

Selegiline is also contra-indicated for concomitant use with pethidine and other opioids.

Selegiline should not be used in patients with other extrapyramidal disorders not related to dopamine deficiency.

Selegiline should not be used in patients with active duodenal or gastric ulcer.

Selegiline should not be used in patients who are being treated with antidepressant drugs, including MAO inhibitors and selective serotonin reuptake inhibitors (e.g citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline and venlafaxine.

Selegiline should also not be used with other drugs which are also monoamine oxidase inhibitors, e.g. linezolid.

Selegiline in combination with levodopa is contra-indicated in severe cardiovascular disease, arterial hypertension, hyperthyroidism, phaeochromocytoma, narrow-angle glaucoma, prostatic adenoma with appearance of residual urine, tachycardia, arrhythmias, severe angina pectoris, psychoses, advanced dementia and thyrotoxicosis.

Special Precautions

One unit of Zelapar contains 1.25 mg selegiline. It is recommended that patients be warned that the correct dose of Zelapar is one oral lyophilisate.

Special care should be taken when administering selegiline to patients who have labile hypertension, cardiac arrhythmias, severe angina pectoris, psychosis or a history of peptic ulceration.

Although serious hepatic toxicity has not been observed, caution is recommended in patients with a history of hepatic dysfunction. Transient or continuing abnormalities with a tendency for elevated plasma concentrations of liver enzymes have been described during long-term therapy with conventional tablets of selegiline.

The selectivity for MAO-B following administration of conventional selegiline tablets may be diminished with doses above 10 mg/day. A non-selective dose of Zelapar above 10 mg/day has not been determined. The precise dose at which selegiline becomes a non-selective inhibitor of all MAO has not been determined, but with doses higher than 10 mg/day there is a theoretical risk of hypertension after ingestion of tyramine-rich food.

Concomitant treatment with medicines which inhibit MAO-A, (or non-selective MAO inhibitors) can cause hypotensive reactions. Hypotension, sometimes sudden in onset, has been reported with conventional selegiline.

Since selegiline potentiates the effects of levodopa, the adverse effects of levodopa may be increased. When selegiline is added to the maximum tolerated dose of levodopa, involuntary movements and agitation may occur. Levodopa should be reduced by about 10 to 30% when selegiline is added to the treatment. When an optimum dose of levodopa is reached, adverse effects from the combination are less than those observed with levodopa on its own.

Although conventional tablets of selegiline, at doses of 5 to 10 mg/day, have been in widespread use for many years, the full spectrum of possible responses to Zelapar may not have been observed to date. Therefore patients should be observed closely for atypical responses.

Doping screening tests

The use of selegiline may produce a positive result in doping screening tests.

Mouth ulcers may occur during treatment with Zelapar 1.25 mg oral lyophilisate.

Interactions

Adjunctive therapy in combination with levodopa (with a peripheral decarboxylase inhibitor) in the treatment of Parkinson's disease. Zelapar in combination with maximal levodopa therapy is indicated particularly in patients who experience fluctuations in their condition such as 'end-dose' type fluctuations, 'on-off' symptoms or other dyskinesias.

Zelaparmay be used alone in early Parkinson's disease for symptomatic relief and/or to delay the need for levodopa.

Adverse Reactions

One unit of Zelapar contains 1.25 mg selegiline. It is recommended that patients be warned that the correct dose of Zelapar is one oral lyophilisate.

Special care should be taken when administering selegiline to patients who have labile hypertension, cardiac arrhythmias, severe angina pectoris, psychosis or a history of peptic ulceration.

Although serious hepatic toxicity has not been observed, caution is recommended in patients with a history of hepatic dysfunction. Transient or continuing abnormalities with a tendency for elevated plasma concentrations of liver enzymes have been described during long-term therapy with conventional tablets of selegiline.

The selectivity for MAOB following administration of conventional selegiline tablets may be diminished with doses above 10 mg/day. A non-selective dose of Zelapar above 10 mg/day has not been determined. The precise dose at which selegiline becomes a non-selective inhibitor of all MAO has not been determined, but with doses higher than 10 mg/day there is a theoretical risk of hypertension after ingestion of tyramine-rich food.

Concomitant treatment with medicines which inhibit MAOA, (or non-selective MAO inhibitors) can cause hypotensive reactions. Hypotension, sometimes sudden in onset, has been reported with conventional selegiline.

Since selegiline potentiates the effects of levodopa, the adverse effects of levodopa may be increased. When selegiline is added to the maximum tolerated dose of levodopa, involuntary movements and agitation may occur. Levodopa should be reduced by about 10 to 30% when selegiline is added to the treatment. When an optimum dose of levodopa is reached, adverse effects from the combination are less than those observed with levodopa on its own.

Although conventional tablets of selegiline, at doses of 5 to 10 mg/day, have been in widespread use for many years, the full spectrum of possible responses to Zelapar may not have been observed to date. Therefore patients should be observed closely for atypical responses.

Mouth ulcers may occur during treatment with Zelapar 1.25 mg oral lyophilisate.

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