Clinical and pharmacological group: & nbsp

Anti-Parkinsonics

Dopaminomimetics

Included in the formulation
  • Newpro®
    patch through. 
  • АТХ:

    N.04.B.C   Stimulants of dopamine receptors

    N.04.B.C.09   Rotigotine

    Pharmacodynamics:

    Rotigotine is nonergolin D3/ D2/ D1 dopamine agonist for the treatment of Parkinson's disease. The mechanism of action is to effect a beneficial effect by activating D3-, D2-and D1receptors of the caudato-putamenal complex of the brain.

    Pharmacokinetics:

    The drug is quickly absorbed through the skin and distributed in the blood. It penetrates the blood-brain barrier, accumulates in the brain tissues: the concentration in them is about 5 times higher than in other tissues and blood. After attaching the plaster rotigotine It is constantly released from the transdermal patch and absorbed through the skin. The equilibrium concentration is achieved 1 to 2 days after the application of the patch and is maintained at a stable level with a single, daily plaster application for a period of 24 hours. Approximately 45% of the active substance of the patch is released through the skin in 24 hours. Absolute bioavailability after transdermal application is about 37%. Changing the location of the patch can lead to daily fluctuations in the level of the drug in the blood plasma.Approximately 71% of the dose of rotigotine is excreted in the urine, approximately 23% - with feces. Half-life from 5 to 7 hours.

    Indications:Monotherapy of idiopathic Parkinson's disease at an early stage (without the use of levodopa).

    VI.G20-G26.G20   Parkinson's disease

    Contraindications:
    • Hypersensitivity to the active substance or any other component of the drug.
    • Pregnancy.
    • The period of breastfeeding.
    • Children under 18 years.
    • Conduction of magnetic resonance imaging or cardioversion.
    Carefully:

    Caution should be given to patients with severe hepatic impairment, as this may lead to a decrease in the clearance of rotigotine. The drug was studied in this group of patients. In the case of increased hepatic insufficiency, the dose is reduced. In acute deterioration of liver function, the cumulative effect of rotigotine may develop.

    Pregnancy and lactation:

    Do not use during pregnancy. Rotigotine is excreted in breast milk, so if you need to use the drug for the mother, breast-feeding should be stopped.

    Category of recommendations for FDA is not defined.

    Dosing and Administration:

    The patch is applied to a clean, dry, undamaged area of ​​the skin of the anterior wall of the abdomen, shoulder or forearm, anterior or external surface of the thigh, the lateral surface of the lumbar region. It is necessary to avoid repeated application of the patch to the same place within 14 days. Do not stick a patch on the red, irritated or damaged skin.

    Side effects:

    From the side immune system: sometimes - hypersensitivity.

    From the side GIT: often - nausea, vomiting, constipation or diarrhea, dry mouth, indigestion; sometimes - abdominal pain, stomach discomfort, anorexia, decreased appetite.

    From the side nervous system and psyche: often - drowsiness, hallucinations (including visual and auditory), anxiety, pathological dreams, insomnia, dizziness, headache, dyskinesia, lethargy; rarely - confusion, sleep disturbance, nightmares, tremor, imbalance, dyskinetic disorders, loss of consciousness, impaired attention, paresthesia, memory impairment, vasovagal syncope, loss of consciousness; psychotic disorders (including paranoid psychosis),increased libido (including hypersexuality), compulsive disorders (including pathological attraction to gambling), very rarely - convulsions.

    From the side organs of sight, hearing: sometimes - visual impairment, photopsy, vertigo (including positional).

    From the side of cardio-vascular system: often - orthostatic hypotension, arterial hypertension; sometimes - palpitation, tachycardia.

    From the side respiratory system: often - cough, hiccough; sometimes - shortness of breath.

    From the side digestive system: sometimes - an increase in the level of hepatic transaminases.

    From the side leather: often - hyperhidrosis, erythema, sometimes itching - rash (including allergic), skin irritation, exanthema, generalized itching.

    From the side soft tissues and bones: sometimes swelling of the joints.

    From the side reproductive system: sometimes erectile dysfunction.

    Other: often - reactions at the place of fixing the plaster (including erythema, pruritus, irritation, burning, dermatitis, inflammation, papules, blisters, pain); sometimes - peripheral edema, asthenia (including fatigue, malaise), rarely - poor health, decreased attention, upset gait.

    Overdose:

    Symptoms: increased major adverse reactions, especially nausea, vomiting, hypotension, involuntary movements, hallucinations, confusion, convulsions and other signs of central dopaminergic stimulation.

    Treatment symptomatic: stopping the receipt of the drug in the body (remove plaster), carrying out general supportive measures to ensure physiological functions. The level of rotigotine decreases after removal of the patch. The patient needs constant monitoring. For correction of arterial pressure apply phenylephrine, epinephrine and other vasoconstrictors. Effectively conducting oxygen therapy. Due to rotigotine more than 90% associated with proteins, dialysis is ineffective. Antidote in case of an overdose of dopamine agonists is unknown.

    Interaction:

    Proceeding from the fact that rotigotine is a dopamine agonist, it can be assumed that dopamine antagonists, such as neuroleptics (eg, phenothiazine, butyrofenone, thioxanthin) or metoclopramide, can reduce the effectiveness of the drug. Therefore, it is advisable to avoid their simultaneous application.Because of possible additive effects, caution should be used rotigotine patients who take sedative medications or other central nervous system depressants (eg, benzodiazepines, antipsychotics, antidepressants).

    Avoid combination with alcohol!

    There are no studies of simultaneous application of rotigotine with substances - inductors of enzyme activity (for example, rifampicin, phenobarbital, carbamazepine, phenytoin, St. John's wort pitted).

    Simultaneous application of L-dopa (levodopa) and carbidopa with rotigotine has no effect on the pharmacokinetics of rotigotine, and it, in turn, does not affect the pharmacokinetics of L-dopa and carbidopa.

    The drug is not intended for combined use with L-dopa in the treatment of Parkinson's disease at an early stage, so when used concomitantly it can provoke a dopaminergic L-dopa reaction and, as with other dopamine agonists, cause or exacerbate pre-existing dyskinesia.

    Special instructions:

    If the patient can not adequately control his behavior (the onset of psychotic disorders) with rotigotine, it is advisable to transfer it to therapy with another dopamine agonist.The protective layer of the patch contains aluminum. To avoid burns to the skin while performing a magnetic resonance imaging or cardioversion, the patch should be removed. As with other dopamine agonists, systemic regulation of blood pressure may worsen, leading to postural / orthostatic hypotension. When using the drug in patients with Parkinson's disease at an early stage who did not receive L-tolerance (levodopa), loss of consciousness was observed. It is recommended to control blood pressure, especially at the beginning of treatment in connection with the general risk of development of orthostatic hypotension associated with dopaminergic therapy. When using the drug, there was increased drowsiness and attacks of sudden falling asleep, especially in patients with Parkinson's disease. There were cases of sudden falling asleep during the day, in some cases without any preliminary signs. Doctors who prescribe the drug should necessarily re-examine patients, assessing drowsiness or sleepiness of patients because patients may not be aware of the presence of drowsiness until they are directly asked about it.In such cases it is advisable to revise the question of reducing the dose or even stopping therapy. In patients who used the drug, there were manifestations of compulsive disorders, including pathological attraction to gambling, hypersexuality, increased libido, repeated meaningless actions (pandering). In cases of abrupt discontinuation of dopaminergic therapy, the development of symptoms resembling a malignant neuroleptic syndrome, not noted with the use of the drug, was observed. Therefore, you must gradually reduce the dose of the drug. Patients should be informed about the possibility of developing hallucinations. In some patients who took dopaminergic derivatives ergolin, there were cases of development of fibrosis of the abdominal space, pulmonary infiltrates, pleural effusion, pericarditis, cardiac valvulopathy. Although these complications may disappear when the drug is withdrawn, there is not always a complete recovery. Such complications are most likely related to the ergoline structure of such compounds, but it is not known whether other dopaminergic agonists (of a non -ergoline nature) can cause such reactions.Patients who use dopamine agonists should not prescribe antipsychotics as antiemetics. It is recommended to conduct regular ophthalmological monitoring. Do not expose to external heating (excessive exposure to sunlight, a heating pad or other heat sources such as a sauna, a hot bath), a patch with an attached patch. Reactions may develop on the skin at the attachment site of the patch. To prevent this, it is recommended to change the place of attachment of the patch daily (for example, from the right side to the left and upper body to the lower part). The same place should not be used within 14 days. If reactions develop at the attachment site of the patch that do not disappear within a few days, or if the severity of these reactions increases or the skin reaction spreads beyond the attachment site, an assessment of the risk / benefit ratio for the individual patient should be made. In the event that the transdermal system leads to rashes or irritations on the skin, direct exposure to sunlight should be avoided until the skin is healed.The drug may cause discoloration of the skin at the site of application. With the advent of a generalized skin reaction (for example, allergic rash, including erythematous blotchiness, papular eruptions or itching) associated with the use of rotigotine, it is advisable to stop using the patch. Caution should be given to patients with severe hepatic impairment, as this may lead to a decrease in the clearance of rotigotine. The drug was studied in this group of patients. In the case of increased hepatic insufficiency, the dose is reduced. In acute deterioration of liver function, the cumulative effect of rotigotine may develop.

    Rotigotine can significantly affect the ability to drive and work with machinery. Patients receiving rotigotine and who have drowsiness and / or sudden sleep attacks, it is necessary to warn about the danger associated with driving or working with those activities (for example, production mechanisms), in which the reduction of attention can expose themselves or others to the risk of serious injury or even cause death.

    Instructions
    Up