Newpro transderm patch 4mg 24h N28
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Active ingredients
Rotigotine
Release form
Patch
Composition
1 mn 24 h system contains: Active substance: rotigotine 4 mg.
Pharmacological effect
Rotigotine is a non-ergolin D3 / D2 / D1 dopamine agonist for the treatment of Parkinson's disease. The mechanism of action is the implementation of a beneficial effect by activating the D3, D2 and D1 receptors of the caudato-putamenal complex of the brain.
Pharmacokinetics
The drug is rapidly 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. Absorption. After attaching the patch, rotigotine is constantly released from the transdermal patch and absorbed through the skin. Equilibrium concentration is achieved in 1 - 2 days after applying the patch and is maintained at a stable level with a single, daily application of the patch for a period of 24 hours. The pharmacokinetic profile of rotigotine has a dose-proportional relationship in the dose range from 2 mg / day (10 cm2) to 8 mg / day (40 cm2). 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 place of application of the patch can lead to daily fluctuations in the level of the drug in the blood plasma. The differences in bioavailability of rotigotine ranged from 1% (hip versus abdomen) to 41% (shoulder versus hip). However, there are no indications regarding the appropriate effect on the clinical outcome. Distribution. In vitro, the binding of rotigotine to plasma proteins is approximately 92%, the distribution volume in humans is approximately 82 l / kg. Metabolism. Rotigotine is metabolized mainly by N-de-alkylation partially direct and secondary conjugation. In vitro results show that various CYP isoforms of cytochrome are capable of catalyzing N-de-alkylation of rotigotine. The main metabolites are sulfates and glucuronide conjugates of the original substance, as well as biologically inactive N-dezalkyl-metabolites. Excretion. Approximately 71% of the dose of rotigotine is excreted in the urine, approximately 23% in feces.The clearance of rotigotine after transdermal application is approximately 10 l / min, and the period of its elimination is from 5 to 7 hours. Since the patch is used transdermally, it is highly likely that the food and the condition of the digestive tract will not affect the effectiveness of the drug.
Indications
- monotherapy of idiopathic Parkinson’s disease at an early stage (without the use of levodopa).
Contraindications
- hypersensitivity to the active substance or any other component of the drug; - pregnancy; - breastfeeding period; - children under the age of 18; - magnetic resonance imaging or cardioversion.
Use during 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, breastfeeding should be stopped.
Dosage and administration
The patch is applied to a clean, dry, intact skin area of the front wall of the abdomen, shoulder, or forearm, front or outer surface of the thigh, the lateral surface of the lumbar region. Repeated plastering should be avoided at the same place within 14 days. Do not stick the patch on reddened, irritated or damaged skin. Application and processingEach patch is packed in a sachet (small bag), after opening which you must immediately use a patch. To do this: - remove one half of the protective layer and stick the adhesive to the application site with sticky side, pressing it tightly against the skin; - bend the adhesive and remove the second part of the protective layer. It is not advisable to touch the sticky part of the patch. The plaster should be pressed tightly with the palm of your hand for 20-30 seconds so that it is well fixed. In case of plaster sticking out during the period remaining from the 24-hour treatment interval, it is necessary to use a new plaster. The plaster should be cut into pieces.
Side effects
At the beginning of therapy, dopaminergic reactions may develop, such as nausea and vomiting, dizziness, drowsiness, and reactions at the patch site. They are usually weak or moderate in severity, pass quickly without discontinuation of the drug and do not require additional therapy. From the immune system: sometimes - hypersensitivity. From the gastrointestinal tract: often - nausea, vomiting,constipation or diarrhea, dry mouth, dyspepsia; sometimes - abdominal pain, stomach discomfort, anorexia, loss of appetite. From the 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, attention disorder, paresthesia, memory impairment, vasovagal syncope, loss of consciousness; psychotic disorders (including paranoid psychosis), increased libido (including hypersexuality), compulsive disorders (including a pathological attraction to gambling), very rarely - convulsions. On the part of the organs of sight, hearing: sometimes - visual disturbances, photopsia , vertigo (including positional). From the cardiovascular system: often - orthostatic hypotension, arterial hypertension; sometimes - a feeling of heartbeat, tachycardia. On the part of the respiratory system: often - cough, hiccups; sometimes - shortness of breath. From the digestive system: sometimes - increased levels of hepatic transaminases. From the skin: often - hyperhidrosis, erythema, itching sometimes - rash (including allergies), skin irritation, exanthema, generalized itching. From the side of soft tissues and bones: sometimes - swelling of the joints. From the reproductive system: sometimes - erectile dysfunction. Others: often - reactions at the site of the patch (including erythema, itching, irritation, burning, dermatitis, inflammation, papules, blisters, pain); sometimes - peripheral edema, asthenia (including fatigue, malaise), rarely - poor health, loss of attention, gait disorder.
Overdose
Symptoms: increased main adverse reactions, especially nausea, vomiting, hypotension, involuntary movements, hallucinations, confusion, convulsions and other signs of central dopaminergic stimulation. Treatment is symptomatic: stopping the drug in the body (removing the patch), carrying out general supportive measures to ensure physiological functions. The level of rotigotine decreases after removal of the patch. The patient must be continuously monitored.Phenylephrine, epinephrine and other vasoconstrictors are used to correct blood pressure. Effectively conducting oxygen therapy. Due to the fact that rotigotine is more than 90% bound to proteins, dialysis is ineffective. The antidote for dopamine agonist overdose is unknown.
Interaction with other drugs
Based on the fact that rotigotine is a dopamine agonist, it can be assumed that dopamine antagonists, such as antipsychotics (for example, phenothiazine, butyrophenone, thioxanthin) or metoclopramide, may reduce the effectiveness of the drug. Therefore, it is advisable to avoid their simultaneous use. Because of the possible additive effects, rotigotine should be carefully prescribed to patients who are taking sedatives or other central nervous system depressants (for example, benzodiazepines, antipsychotics, antidepressants). Avoid combination with alcohol! There are no studies on the simultaneous use of rotigotine with substances - enzyme activity inducers (for example, rifampicin, phenobarbital, carbamazepine, phenytoin, and St. John's wort),. 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, the poet That while the application it may provoke dopaminergic reacting L-dopa and as well as the use of other dopamine agonists, cause or exacerbate preexisting dyskinesia.
special instructions
If the patient cannot adequately control his behavior (the occurrence of psychotic disorders) when using rotigotine, it is advisable to transfer it to therapy with another dopamine agonist. The protective layer of the patch contains aluminum. To avoid burns on the skin when a patient is undergoing magnetic resonance imaging (MRI) or cardioversion, the patch must be removed. As with other dopamine agonists, systemic arterial pressure may be impaired, resulting in postural / orthostatic hypotension.When using the drug in patients with Parkinson's disease at an early stage, not receiving L-dopa (levodopa), loss of consciousness was observed. It is recommended to control blood pressure, especially at the beginning of treatment, due to the general risk of orthostatic hypotension associated with dopaminergic therapy. When using the drug, increased drowsiness and attacks of sudden sleep were observed, 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 a drug must necessarily re-examine patients, assessing the drowsiness or drowsiness of patients, since patients may not be aware of the presence of drowsiness until they are directly asked about it. In such cases, it is advisable to reconsider the question of reducing the dose or even stopping the therapy. Patients who used Newpro had manifestations of compulsive disorders, including a pathological craving for gambling, hypersexuality, increased libido, repeated meaningless actions (panding). In cases of sharp the abolition of dopaminergic therapy was observed the development of symptoms resembling malignant neuroleptic syndrome, not marked when using the drug. Therefore, it is necessary to gradually reduce the dose of the drug. Patients need to be informed about the possibility of developing hallucinations. Fibrous complications: in some patients who took ergoline dopaminergic drugs, there were cases of fibrosis in the abdominal space, pulmonary infiltrates, pleural effusion, pericarditis, cardiac valvulopathy. Although these complications can disappear when you stop taking the drug, it does not always come full recovery. Such complications are rather related to the ergoline structure of such compounds, however, it is not known whether other dopaminergic agonists (of non-ergoline nature) can lead to similar reactions. Patients who use dopamine agonists should not be prescribed antipsychotics as antiemetic agents. It is recommended to regularly monitor ophthalmic. Do not expose to external heat (excessive exposure to sunlight, heating pads or other sources of heat, such as a sauna, hot bath). On the skin, at the site of the patch, reactions may develop.To prevent this, it is recommended to change the location of the patch on a daily basis (for example, from the right side to the left and upper parts of the body to the lower parts). The same place should not be used within 14 days. If reactions have developed at the patch site, which do not disappear within a few days, or if the severity of these reactions has increased, or the skin reaction has spread beyond the patch site, it is necessary to evaluate the risk / benefit ratio for the individual patient. In case the transdermal system has caused a rash or irritation on the skin, direct exposure to the sun's rays should be avoided until the skin heals. The drug can cause discoloration of the skin at the site of application. With the advent of a generalized skin reaction (for example, an allergic rash, including erythematous, spotting, papular rash or itching) associated with the use of rotigotine, it is advisable to stop the use of the patch. Rotigotine clearance. The drug was studied in this group of patients. In the case of increased liver failure, the dose is reduced. With an acute deterioration in liver function, the cumulative effect of rotigotine may develop. The ability to influence the reaction rate when driving vehicles or other mechanisms. Rotigotine can significantly affect the ability to drive and work with mechanisms. Patients who take rotigotine and who experience drowsiness and / or fits of sudden sleep should be warned of the dangers associated with driving or working in those activities (for example, production mechanisms) that may reduce their attention or other people. serious injury or even death.