Legal category: POM.
Active ingredient: Rotigotine 2 mg, 4 mg, 6 mg, 8 mg per 24 hours.
Description: Thin, matrix-type, square, tan coloured, transdermal patches marked with name and strength.
Treatment Initiation Pack: £110.34.
2mg Continuation Pack of 28 patches: £77.24.
4mg Continuation Pack of 28 patches: £88.28.
6mg Continuation Pack of 28 patches: £110.34.
8mg Continuation Pack of 28 patches: £142.79.
Indication: For the treatment of the signs and symptoms of early idiopathic Parkinson's disease as monotherapy.
Pharmacology: Rotigotine is a non-ergoline dopamine agonist that is thought to activate D3, D2 and D1 receptors in the caudate putamen to alleviate the symptoms of Parkinson's disease.
It has been formulated as a transdermal patch, a route of administration that offers many advantages. Unlike oral preparations, rotigotine is continuously released over the 24-hour patch application period, thus delivering constant dopamine stimulation to the brain. Rotigotine patches, therefore, provide a short-term immediate symptomatic benefit and may offer long-term reduction in the risk of complications such as motor fluctuations and dyskinesias.
Transdermal rotigotine delivery also avoids GI absorption problems and first pass metabolism, simplifying titration and dose ranging. Moreover, once daily application reduces pill burden and may improve compliance. Once removed, (due to its short plasma elimination half-life) rotigotine "wash-out" is more rapid than with the long-acting or controlled release preparations often used to treat Parkinson's disease.
Following transdermal application, rotigotine is continuously absorbed through the skin. Steady state concentrations are reached after one to two days and are maintained at a stable level with once daily dosing. Approximately 45% of the active ingredient is released over the 24-hour application period and although rotation of patch sites may produce day-to-day differences in plasma levels this is not thought to affect the overall clinical outcome. Rotigotine undergoes extensive metabolism and is excreted primarily via the urine with a smaller proportion of the dose being excreted in the faeces.
The safety and efficacy of rotigotine has been investigated in multi-national, double-blind, placebo-controlled studies of patients who were either L-dopa naïve or who had previously been given L-dopa for no more than six months. The primary outcome assessment for these studies was based on the Activities of Daily Life and Motor Examination components of the Unified Parkinson's Disease Rating Scale. In one of the studies, a 20% improvement in primary outcome was seen in 48% of subjects given rotigotine, which compared favourably with the placebo group, where a 20% improvement was seen in only 19% of patients.
In the second study, a 20% improvement was observed in 52% of those given rotigotine as opposed to 68% of those given ropinirole and 30% of the placebo group. In this study patients were titrated up to a maximum of 8 mg/24 hours of rotigotine and up to a maximum of 24 mg/day of ropinirole. The usual therapeutic dose for ropinirole is 3-9mg per day when used as monotherapy.
Rotigotine was generally well tolerated and was described as a safe, effective treatment for early-stage Parkinson's disease.
Adult Dose: Initially, one 2 mg/24 hour patch per day. Increase in weekly steps of 2 mg/24 hours up to a maximum daily dose of 8 mg/24 hours. Patches should be applied at the same time each day and removed after 24 hours. Patch sites should be rotated each day so that same site is not used within 14 days.
Child Dose: Not recommended.
Contraindications: Pregnancy, lactation.
Special precautions: Severe hepatic impairment. Assess for drowsiness or sleepiness - reduce dose if necessary - advise patients against driving or operating machinery. Monitor blood pressure due to the risk of orthostatic hypotension. Monitor for signs of neuroleptic malignancy syndrome and for signs of visual abnormality. Warn patients that hallucinations may occur and advise them to avoid applying any external heat to the patch. Withdraw gradually - reducing the dose in increments of 2 mg/24 hours every other day.
Interactions: Neuroleptic anti-emetics. Dopamine agonists or antagonists. Sedatives, CNS depressants, alcohol.
Adverse reactions: Anorexia. Sleep attacks, hallucinations, anxiety, abnormal dreams, insomnia. Somnolence, dizziness, headache, dyskinesia, lethargy. Orthostatic hypotension, hypertension. Cough, hiccup. GI disturbance, dry mouth. Hyperhydrosis, erythema, pruritus. Patch site reactions, peripheral oedema, asthenia.
? Report any adverse reactions to CSM.
Further information: Schwarz Pharma Ltd, East Street, Chesham, Buckinghamshire HP5 1DG. Tel: (01494) 797500.