Index of drugs

Treatment of signs and symptoms in early idiopathic Parkinson's disease as monotherapy (ie without concomitant administration of levodopa) or in combination with levodopa, i.e. for the duration of the disease, through its late periods when the effect of levodopa weakens or becomes incompatible and occurs variations in the therapeutic effect (end-dose effect or on-off fluctuations.) In addition, a dose of 2 mg / 24 h is indicated for the treatment of moderate to severe moderate idiopathic Restless Legs Syndrome in adults.

1 transdermal patch releases 2 mg, 4 mg, 6 mg or 8 mg of rotigotine within 24 hours. 1 transdermal system contains rotigotine in an amount of 4.5 mg in 10 cm, respectively², 9 mg in 20 cm², 13.5 mg in 30 cm²18 mg in 40 cm².

Dopaminergic receptor agonist, not derived from ergot alkaloids. The beneficial effects of rotigotine in the treatment of Parkinson's disease is due to the activation of D-receptors₃, D₂ and D₁ the caudate nucleus in the brain. The precise mechanism of action of rotigotine in the treatment of restless legs syndrome is unknown. Rotigotine is a D-receptor agonist₂ and D₃, also acting on D-receptors₁, D₄ and D₅. Within the non-dopaminergic receptors rotigotine showed an antagonistic effect on alpha2B and agonistic receptors on 5HT1A receptors, however, it did not affect the 5HT2B receptor. After applying the patch, the rotigotine is continuously released from the transdermal patch and absorbed through the skin. Steady-state concentrations are reached after 1-2 days and remain constant if the patch is applied for 24 h once a day. About 45% of the active substance is released from the patch into the skin within 24 hours. Absolute bioavailability is about 37%. Binding of rotigotine to plasma proteinsin vitro is around 92%. Rotigotine is extensively metabolised by N-dealkylation and direct and indirect conjugation. Different CYP isoforms can catalyze the N-dealkylation process. Approximately 71% of the dose of rotigotine is excreted in the urine, while the smaller part (approximately 23%) is excreted in the faeces. T_0,5 in the elimination phase is 5-7 h.

Hypersensitivity to rotigotine or to any of the excipients. Magnetic resonance imaging or cardioversion.

If satisfactory control of disease symptoms has not been achieved during the treatment of a patient with Parkinson's disease, switching to another Dopamine agonist may provide additional benefits. Before magnetic resonance imaging or cardioversion, the patch should be removed to avoid skin burns, as the cover layer of the patch contains aluminum. It is recommended to monitor blood pressure, especially at the beginning of treatment, due to the general risk of postural hypotension associated with dopaminergic therapy. The use of the preparation is associated with somnolence and cases of sudden fall asleep - patients should be continuously evaluated for drowsiness or drowsiness and, if necessary, consider a dose reduction or termination of treatment. Patients should be regularly monitored for possible disturbances in the control of habits and drives. Patients and their carers should be advised that behavioral symptoms of libido disorders may occur, including: pathological gambling, increased libido, hypersexuality, compulsive spending or buying, and compulsive or paroxysmal overeating. In such cases, it is recommended to consider a dose reduction or gradual discontinuation of the drug. After sudden discontinuation of dopaminergic therapy, symptoms resembling neuroleptic malignant syndrome may occur - a gradual withdrawal of the preparation is recommended. Neuroleptics should not be used as antiemetics in patients using dopamine agonists. Ophthalmologic monitoring is recommended at regular intervals or when visual disturbances occur.Do not expose the place where the patch is applied to external heat sources (excessive sunlight, heating pads and other heat sources, such as a sauna, hot bath). If there are reactions lasting longer than a few days where the patch is affixed, if the skin gets worse or if the skin reaction gets wider than the area where the patch is applied, the risk-benefit ratio should be assessed for the patient. If skin rashes or irritations occur, avoid exposure to direct sunlight until skin heals, as exposure to sunlight may change its color. If generalized skin reaction related to the treatment is observed during treatment (eg allergic rash, including erythematous, macular, papular rash or pruritus), treatment should be discontinued. The incidence of some dopaminergic side effects, such as hallucinations, dyskinesia and peripheral edema, is usually higher when used in combination with levodopa in patients with Parkinson's disease. Patients with restless leg syndrome may experience worsening of symptoms. The severity refers to their earlier occurrence in the evening (or even in the afternoon), increased severity of symptoms and the extension of symptoms to other parts of the body. Use with caution in patients with severe hepatic impairment. acute deterioration of renal function may cause unexpected accumulation of rotigotine. Do not use the patch on the skin red, irritated or damaged. The product contains sodium metabisulphite, which can cause allergic reactions, including anaphylactic symptoms and life-threatening or moderate asthmatic episodes. The safety and efficacy of rotigotine in children and adolescents has not been established.

The preparation should not be used during pregnancy. Due to the reduction of prolactin by rotigotine in humans, inhibition of lactation should be expected. Breastfeeding should be discontinued when starting treatment with the product - no data are available on the excretion of rotigotine and / or its metabolites in breast milk. Women of childbearing age should use effective methods of contraception.

Parkinson's disease. Very common: drowsiness, pain and dizziness, nausea, vomiting, reactions at the site of patch (including erythema, pruritus, irritation, rash, inflammation of the skin, inflammation, swelling, skin discoloration, papules, scratches, bubbles, urticaria, pain , eczema, hypersensitivity). Common: perceptual disorders (including hallucinations, visual hallucinations, auditory hallucinations, illusions, sleep disorders, nightmares, unusual dreams, impulse control disorders (including pathological gambling, stereotypes, compulsive buying), ungraded consciousness disorders (including fainting, vasovagal syncope, loss of consciousness), dyskinesia, dizziness associated with a change in body position, lethargy, palpitations, orthostatic hypotension, hypertension, hiccups, constipation, dry mouth, dyspepsia, erythema, excessive sweating, pruritus, peripheral edema , weakness (including fatigue, weakness, bad mood), weight loss, falls. Uncommon: hypersensitivity (including angioneurotic edema, swelling of the tongue and lips), sudden sleep bouts / sudden falling asleep, paranoia, sexual desire disorder (including hypersexuality, increased libido), confusion, confusion, agitation, blurred vision, blurred vision, photopsy, atrial fibrillation, hypotension, abdominal pain, pruritus, skin irritation, contact dermatitis, erectile dysfunction, increased liver enzymes (including AST, ALT, GGT), weight gain, increased heart rate. Rare: psychotic disorders, obsessive-compulsive disorder, aggressive behavior / aggression, paroxysmal overeating / eating disorders, convulsions, supraventricular tachycardia, generalized rash, irritability.Restless legs syndrome. Very common: headache, nausea, reactions at the site of application (including erythema, pruritus, irritation, rash, dermatitis, vesicles, pain, eczema, inflammation, swelling, discoloration, papules, clash of skin, urticaria, hypersensitivity), conditions weakness (including fatigue, weakness, bad mood).Common: vomiting, dyspepsia; irritability, hypersensitivity (including angioneurotic edema, swelling of the tongue and lips), sudden sleep bouts / sudden falling asleep, sexual desire disorders (including hypersexuality, increased libido), insomnia, sleep disorders, unusual dreams, impulse control disorders (including pathological gambling) , stereotypes, compulsive buying), drowsiness, hypertension, vomiting, dyspepsia, pruritus, irritability, peripheral edema. Uncommon: obsessive-compulsive disorder, disorientation, agitation, orthostatic hypotension. Rare: aggressive behavior / aggression, paralysis, eating disorders. In some patients treated with ergot alkaloids, cases of retroperitoneal fibrosis, pulmonary infiltrates, exudate to the pleural cavity, thickening of the pleura, pericarditis and damage to the heart valves have been reported; these symptoms may go away after discontinuation of treatment, but not always completely resolves.

Early form of Parkinson's disease. The starting dose is 2 mg / 24 h once daily, then it should be increased to an effective dose at weekly intervals of 2 mg / 24 h. In some patients, the effective dose can be 4 mg / 24 h. In most patients the effective dose is reached within 3-4 weeks and is respectively 6 mg / 24 h or 8 mg / 24 h. The maximum dose is 8 mg / 24 h.An advanced form of Parkinson's disease with fluctuations.The starting dose is 4 mg / 24 h once daily, then it should be increased to an effective dose at weekly intervals of 2 mg / 24 h. The maximum dose is 16 mg / 24 h. In some patients, doses of 4 mg / 24 h may be effective. or 6 mg / 24 h. In most patients, the effective dose is reached within 3-7 weeks for doses of 8-16 mg / 24 h. The maximum dose is 16 mg / 24 h. For doses above 8 mg / 24 h, several patches may be used to obtain the target dose. The preparation should be discontinued gradually. The daily dose should be reduced gradually by 2 mg / 24 h, preferably every second day, until the end of treatment.Restless legs syndrome. The starting dose is 1 mg / 24 h once a day. Depending on the patient's individual response, the dose can be increased at 1-weekly intervals up to 1 mg / 24 h for a maximum dose of 3 mg / 24 h. Every 6 months, the need for continuing treatment should be reconsidered. The preparation should be discontinued gradually. The daily dose should be reduced gradually by 1 mg / 24 h, preferably every other day, until the end of treatment.Special groups of patients. No dosage adjustment is necessary in patients with mild or moderate hepatic impairment. Caution should be exercised in patients with severe hepatic impairment. If your liver gets worse, you may need a dose reduction.Method of application. The patch is applied once a day, more or less at the same time each day and leaves on the skin for 24 hours, after which it is replaced by a new patch stuck elsewhere. The patch should be applied to clean, dry, undamaged and healthy skin of the abdomen, thigh, hip, lateral torso, shoulder or shoulder. It is recommended that the place of sticking the patch be changed every day (eg from the right to the left and from the upper part of the body to the lower one). Avoid re-sticking the patch in the same place for 14 days. If the patient forgets to apply the patch at the usual time or when the patch comes off, a new patch should be applied for the remainder of the day. Do not cut the patch into parts.