HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Rotigotine
Neupro · CS-110 · N 0923 · SPM 962 · Rotigotine · S(-)-N-0437 · ROTIGOTINE USP · 14C]-Rotigotine
Identifikatoren & physikalische Daten
| CAS No. | 99755-59-6 |
|---|---|
| Summenformel | C19H25NOS |
| Durchschnittliche Molmasse | 315,5 g/mol |
| Monoisotopische Masse | 315,16568542 g/mol |
| SMILES | CCCN(CCc1cccs1)[C@H]1CCc2c(O)cccc2C1 |
| InChIKey | KFQYTPMOWPVWEJ-INIZCTEOSA-N |
| PubChem CID | 59227 |
| ChEMBL | CHEMBL1303 |
| ChEBI | CHEBI:135351 |
| EC No. | 619-458-3 |
| DTXSID | DTXSID5046772 |
Chemische & physikalische Eigenschaften
| XLogP | 4,9 |
|---|---|
| Polarare Oberfläche (TPSA) | 51,7 |
| H-Brücken-Donoren | 1 |
| H-Brücken-Akzeptoren | 3 |
| Frei drehbare Bindungen | 6 |
| Schwere Atome | 22 |
| Formalladung | 0 |
| Komplexität | 337 |
| Arzneimittel | Pharmaceuticals -> Listed in ZINC15 |
| Color/Form | White to off-white powder |
| Löslichkeit | Lipophilic and poorly soluble in water at neutral pH. Solubility increases at more acidic pH.Insoluble in waterDMF: 30 mg/mlDMF:PBS(pH7.2) (1:2): 0.33 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml |
| Human Drugs | Breast FeedingLactationMilk, HumanDopamine AgonistsFDA approved drugs -> Active ingredientEMA approved medicines: Human medicine |
| Optical Rotation | White crystalline solid. Specific optical rotation: -55.79 deg at 25 °C/578 °C (c = 0.99 in methanol) /Rotigotine hydrochloride/ |
| Stability/Shelf Life | Stable under recommended storage conditions. /Rotigotine hydrochloride/ |
| Other Experimental Properties | Non-hygroscopic. Sensitive to oxidation |
| Schmelzpunkt | 78 °C |
| Siedepunkt | 470.1±45.0 °C(Predicted) |
| Dichte | 1.15±0.1 g/cm3(Predicted) |
| Lagerbedingungen | room temp |
| Aggregatzustand | powder to crystal |
| pKa (Säurekonstante) | 10.49±0.40(Predicted) |
| Farbe | White to Almost white |
| Hauptanwendungen | pharmaceuticalpharmaceutical small molecule |
| InChI | InChI=1S/C19H25NOS/c1-2-11-20(12-10-17-6-4-13-22-17)16-8-9-18-15(14-16)5-3-7-19(18)21/h3-7,13,16,21H,2,8-12,14H2,1H3/t16-/m0/s1 |
| InChIKey | KFQYTPMOWPVWEJ-INIZCTEOSA-N |
| SMILES | C1(O)=C2C(C[C@@H](N(CCC)CCC3SC=CC=3)CC2)=CC=C1 |
Sicherheit & Vorschriften
| GHS-Einstufung | WarningH302 (50%): Harmful if swallowed [Warning Acute toxicity, oral]P203, P260, P261, P263, P264, P270, P271, P273, P280, P301+P317, P304+P340, P318, P319, P330, P403+P233, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 4 reports by companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.H302: Harmful if swallowed [Warning Acute toxicity, oral] |
|---|---|
| FDA-Anforderungen | The Approved Drug Products with Therapeutic Equivalence Evaluations identifies currently marketed prescription drug products, including rotigotine, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act. |
| Toxic Combustion Products | Special hazards arising from the substance or mixture: Carbon oxides, nitrogen oxides (NOx), Sulphur oxides, Hydrogen chloride gas. /Rotigotine hydrochloride/ |
| Hazard Classes and Categories | Acute Tox. 4 (50%) |
| Brandbekämpfungsverfahren | Advice for firefighters: Wear self contained breathing apparatus for fire fighting if necessary. /Rotigotine hydrochloride/Suitable extinguishing media: Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide. /Rotigotine hydrochloride/ |
| Lagerbedingungen | Conditions for safe storage, including any incompatibilities: Keep container tightly closed in a dry and well-ventilated place. /Rotigotine hydrochloride/Store at 20 deg - 25 °C (68 deg - 77 °F)excursions permitted between 15 deg - 30 °C (59 deg - 86 °F).Neupro should be stored in the original pouch. Do not store outside of pouch. |
| Reinigungsverfahren | Accidental Release Measures. Personal precautions, protective equipment and emergency procedures: Use personal protective equipment. Avoid dust formation. Avoid breathing vapors, mist or gas. Ensure adequate ventilation. Avoid breathing dust. Methods and materials for containment and cleaning up: Pick up and arrange disposal without creating dust. Sweep up and shovel. Keep in suitable, closed containers for disposal. /Rotigotine hydrochloride/ |
| Entsorgungsverfahren | SRP: Expired or waste pharmaceuticals shall carefully take into consideration applicable DEA, EPA, and FDA regulations. It is not appropriate to dispose by flushing the pharmaceutical down the toilet or discarding to trash. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.Discard used systems in household trash in a manner that prevents accidental application or ingestion by children, pets, or others.Product: Offer surplus and non-recyclable solutions to a licensed disposal company. Contaminated packaging: Dispose of as unused product. /Rotigotine hydrochloride/ |
| Preventive Measures | Appropriate engineering controls: Handle in accordance with good industrial hygiene and safety practice. Wash hands before breaks and at the end of workday. /Rotigotine hydrochloride/Precautions for safe handling: Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Provide appropriate exhaust ventilation at places where dust is formed. Normal measures for preventive fire protection. /Rotigotine hydrochloride/Gloves must be inspected prior to use. Use proper glove removal technique (without touching glove's outer surface) to avoid skin contact with this product. Dispose of contaminated gloves after use in accordance with applicable laws and good laboratory practices. Wash and dry hands. /Rotigotine hydrochloride/ |
| Personal Protective Equipment (PPE) | Skin protection: Handle with gloves. /Rotigotine hydrochloride/Eye/face protection: Safety glasses with side-shields conforming to EN166 Use equipment for eye protection tested and approved under appropriate government standards such as NIOSH (US) or EN 166(EU). /Rotigotine hydrochloride/Respiratory protection: For nuisance exposures use type P95 (US) or type P1 (EU EN 143) particle respirator.For higher level protection use type OV/AG/P99 (US) or type ABEK-P2 (EU EN 143) respirator cartridges. Use respirators and components tested and approved under appropriate government standards such as NIOSH (US) or CEN (EU). /Rotigotine hydrochloride/Body Protection: Complete suit protecting against chemicals. The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace. /Rotigotine hydrochloride/ |
| Wechselwirkungen | Concurrent oral administration of levodopa/carbidopa (100/25 mg twice daily) and transdermal rotigotine (4 mg/24 hours) in patients with restless legs syndrome had no effect on the steady-state pharmacokinetics of any of the drugs. Transdermal rotigotine may potentiate the therapeutic effects of levodopa as well as its adverse dopaminergic effects (including dyskinesia).Concurrent administration of transdermal rotigotine (3 mg/24 hours) did not substantially affect the pharmacodynamics or pharmacokinetics of an oral estrogen-progestin combination contraceptive (ethinyl estradiol 0.03 mg with 0.15 mg levonorgestrel) in healthy females. Possible interactions with rotigotine and other forms of hormonal contraceptives have not been evaluated to date.Dopamine antagonists (e.g., antipsychotic agents, metoclopramide) may diminish the effectiveness of rotigotine.Transdermal rotigotine may potentiate the therapeutic and/or adverse dopaminergic effects (including dyskinesia) of other dopamine agonists used in the treatment of parkinsonian syndrome and restless legs syndrome.Alcohol and other CNS depressants (e.g., sedatives, anxiolytics, antidepressants, antipsychotics, opiate analgesics) may increase the risk of additive effects, including somnolence and falling asleep during activities of daily living, in patients receiving transdermal rotigotine, and should therefore be used concomitantly with caution. |
| Hepatotoxicity | In multiple, controlled trials in Parkinson disease and restless leg syndrome, rotigotine transdermal patches were not associated with serum enzyme elevations, liver related severe adverse events or instances of clinically apparent liver injury. Since the approval and more wide scale use of rotigotine, there have been no published case reports of liver injury associated with its use and hepatotoxicity is not mentioned in the product label. |
| Toxizitätsübersicht | IDENTIFICATION AND USE: Rotigotine is a white to off white powder formulated into a transdermal system (patch). It is a nonergot-derivative dopamine receptor agonist used for the symptomatic management of idiopathic parkinsonian syndrome. It is also used for the symptomatic management of moderate-to-severe primary restless legs syndrome. HUMAN EXPOSURE AND TOXICITY: The most likely symptoms of overdose would be those related to the pharmacodynamic profile of a dopamine agonist, including nausea, vomiting, hypotension, involuntary movements, hallucinations, confusion, convulsions, and other signs of excessive dopaminergic stimulation. Post-marketing reports indicate that patients may experience new or worsening mental status and behavioral changes, which may be severe, including psychotic behavior during rotigotine treatment or after starting or increasing the dose of rotigotine. Other drugs prescribed to improve the symptoms of Parkinson's disease can have similar effects on thinking and behavior. This abnormal thinking and behavior may consist of one or more of the following: paranoid ideation, delusions, hallucinations, confusion, disorientation, aggressive behavior, agitation, and delirium. These various manifestations of psychotic behavior were also observed during the clinical development of rotigotine for early- and advanced-stage Parkinson's disease and Restless Legs Syndrome. Patients may experience intense urges to gamble, increased sexual urges, intense urges to spend money, binge eating, and/or other intense urges, and the inability to control these urges while taking one or more of the medications, including rotigotine, that increase central dopaminergic tone and that are generally used for the treatment of Parkinson's disease. In some cases, although not all, these urges were reported to have stopped when the dose was reduced or the medication was discontinued. ANIMAL STUDIES: Two-year carcinogenicity studies of rotigotine were conducted in mice at doses of 0, 3, 10, and 30 mg/kg and in rats at doses of 0, 0.3, 1, and 3 mg/kgin both studies rotigotine was administered subcutaneously once every 48 hours. No significant increases in tumors occurred in mice at doses up to 9 times the maximum recommended human dose (MRHD) in Parkinson's disease (8 mg/24 hours). In rats, there were increases in Leydig cell tumors and in uterine tumors (adenocarcinomas, squamous cell carcinomas) at all doses. The endocrine mechanisms believed to be involved in the production of these tumors in rats are not considered relevant to humans. Therefore, there were no tumor findings considered relevant to humans at plasma exposures (AUC) up to 4 to 6 times that in humans at the MRHD. Rotigotine administered subcutaneously (10, 30, or 90 mg/kg/day) to pregnant mice during organogenesis resulted in increased incidences of delayed skeletal ossification and decreased fetal body weights at the two highest doses and an increase in embryo-fetal death at the high dose. Rotigotine administered subcutaneously (0.5, 1.5, or 5 mg/kg/day) to pregnant rats during organogenesis resulted in increased embryo-fetal death at all doses. When rotigotine was administered subcutaneously (5, 10, or 30 mg/kg/day) to pregnant rabbits during organogenesis, an increase in embryo-fetal death occurred at the two highest doses tested. In a study in which rotigotine was administered subcutaneously (0.1, 0.3, or 1 mg/kg/day) to rats throughout pregnancy and lactation, impaired growth and development during lactation and long-term neurobehavioral abnormalities were observed in the offspring at the highest dose testedwhen those offspring were mated, growth and survival of the next generation were adversely affected. When rotigotine was administered subcutaneously (1.5, 5, or 15 mg/kg/day) to female rats prior to and during mating and continuing through gestation day 7, an absence of implantation was observed at all doses. In male rats treated from 70 days prior to and during mating, there was no effect on fertilityhowever, a decrease in epididymal sperm motility was observed at the highest dose tested. When rotigotine was administered subcutaneously to female mice at doses of 10, 30, and 90 mg/kg/day from 2 weeks until 4 days before mating and then at a dose of 6 mg/kg/day (all groups) from 3 days before mating until gestation day 7, a markedly reduced (low dose) or complete absence of implantation (mid and high doses) was observed. The effects on implantation in rodents are thought to be due to the prolactin-lowering effect of rotigotine. In humans, chorionic gonadotropin, not prolactin, is essential for implantation. Rotigotine was negative in the in vitro bacterial reverse mutation (Ames) and in the in vivo micronucleus assays. Rotigotine was mutagenic and clastogenic in the in vivo mouse lymphoma tk assay |
| Human Toxicity Excerpts | /HUMAN EXPOSURE STUDIES/ The aim of this study was to evaluate in a group of patients with psychosis the effect of the dopamine agonist rotigotine on neuroleptic-induced extrapyramidal symptoms (EPSs), a set of movement disorders such as pseudoparkinsonism, dyskinesias, akinesia, and akathisia that occur as result of taking drugs that block dopamine receptors. Twenty patients with psychosis with EPSs were clinically evaluated before and after the administration of rotigotine. The drug was started at a dosage of 2 mg daily and gradually increased until the best clinical benefit was achieved (mean + or - SD, dosage, 3.2 + or - 1.8 mgrange, 2-8 mg). The neurological status was assessed using the Unified Parkinson's Disease Rating Scale (UPDRS) total and UPDRS section III, the Simpson-Angus Scale, and the Barnes Akathisia Rating Scale. The Positive and Negative Syndrome Scale and the Hamilton Depression Rating Scale were used to appraise possible modifications of the psychiatric conditions. Compared with baseline, there was a significant improvement in the UPDRS total, the UPDRS section III, the Simpson-Angus Scale (P < 0.0001), and the Barnes Akathisia Rating Scale (P < 0.05), without changes in the Positive and Negative Syndrome Scale and the Hamilton Depression Rating Scale (P < 0.05). All patients tolerated rotigotine well, except 1 who dropped out of the trial because of the recurrence of his psychotic symptoms. The results of this observational study suggest that low doses of rotigotine are well tolerated in patients with psychosis and are effective in neuroleptic-induced EPSs./SIGNS AND SYMPTOMS/ Post-marketing reports indicate that patients may experience new or worsening mental status and behavioral changes, which may be severe, including psychotic behavior during Neupro treatment or after starting or increasing the dose of Neupro. Other drugs prescribed to improve the symptoms of Parkinson's disease can have similar effects on thinking and behavior. This abnormal thinking and behavior may consist of one or more of the following: paranoid ideation, delusions, hallucinations, confusion, disorientation, aggressive behavior, agitation, and delirium. These various manifestations of psychotic behavior were also observed during the clinical development of Neupro for early- and advanced-stage Parkinson's disease and Restless Legs Syndrome./SIGNS AND SYMPTOMS/ Patients may experience intense urges to gamble, increased sexual urges, intense urges to spend money, binge eating, and/or other intense urges, and the inability to control these urges while taking one or more of the medications, including Neupro, that increase central dopaminergic tone and that are generally used for the treatment of Parkinson's disease. In some cases, although not all, these urges were reported to have stopped when the dose was reduced or the medication was discontinued. Because patients may not recognize these behaviors as abnormal, it is important for prescribers to specifically ask patients or their caregivers about the development of new or increased gambling urges, sexual urges, uncontrolled spending, or other urges while being treated with Neupro. Physicians should consider dose reduction or stopping the medication if a patient develops such urges while taking Neupro./SIGNS AND SYMPTOMS/ The most likely symptoms of overdose would be those related to the pharmacodynamic profile of a dopamine agonist, including nausea, vomiting, hypotension, involuntary movements, hallucinations, confusion, convulsions, and other signs of excessive dopaminergic stimulation.For more Human Toxicity Excerpts (Complete) data for ROTIGOTINE (9 total), please visit the HSDB record page. |
| Non-Human Toxicity Excerpts | /LABORATORY ANIMALS: Acute Exposure/ The local/tumorigenic effects of the patch itself have also been analysed in a repeated application study in mini pigs. The study revealed that there is a potential for some inflammatory reaction when the patch is applied successively in the same site, but this reaction is reduced when sites of application are changed at every application. Neoplastic lesions at the site of application were not observed./LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ The aim of the study is to evaluate the neuroprotective effects of continuous dopaminergic stimulation (CDS) by rotigotine-loaded microspheres (RoMS) in a mouse model of MPTP-induced Parkinson's disease (PD) and to elucidate the potential mechanism underlying these effects. Male C57BL/6 mice were treated either intramuscularly once with RoMS or twice daily for two weeks with rotigotine, and from the 9th day, MPTP (30 mg/kg, i.p.) was injected for the last 5 days. Following treatment, Parkinsonism scores were calculated and oxidative stress-related indicators in the striatum were performed. Neuroinflammatory cytokines, such as tumor necrosis factor-a (TNF-a), interleukin-1beta (IL-1beta), and interleukin-6 (IL-6) were detected in the striatum. Expression of apoptosis-related proteins B-cell leukemia/lymphoma 2 (Bcl-2) and Bcl-2-associated X protein (BAX) was measured in the striatum by Western blot. Nigral tyrosine hydroxylase (TH)-positive neurons and microglial cell markers, i.e., ionized calcium binding adaptor molecule-1 (Iba-1) and neuronal synaptosomes, were quantified to assess the neuroprotective efficacy of RoMS. KEY FINDINGS: The administration of rotigotine significantly improved the Parkinsonism score, protected dopaminergic neurons with antioxidants, reduced microglial cell activation and the release of neuroinflammatory cytokines, and balanced the expression of Bcl-2 and Bax in MPTP-treated mice. Interestingly, the neuroprotective properties of rotigotine were remarkably amplified by CDS treatment with RoMS. These results suggest that CDS therapy can play a neuroprotective role in an MPTP mouse model. Neuroprotective disease-modifying therapy may have the potential benefits of early treatment by normalizing compensatory mechanisms and may also help to delay dyskinesia in the later stages of PD./LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ Continuous dopaminergic stimulation (CDS) has been an important strategy of drug development for the treatment of Parkinson's disease (PD). Rotigotine is a non-ergoline D3/D2/D1 dopamine agonist for treating PD. As a new treatment option for CDS, rotigotine-loaded microspheres (RoMS), a long-acting sustained-release microspheres for injection with poly(lactide-co-glycolide) as drug carrier, are now being evaluated in clinical trial. In this study, subchronic toxicity of RoMS in SD rats has been characterized via intramuscular administration with RoMS (0-240 mg/kg/week) on a consecutive weekly dosing schedule for 3 months followed by 1-month recovery period. The No Observed Adverse Effect Level (NOAEL) was 45 mg/kg/week. One male at 240 mg/kg died from an extensive pulmonary embolism. The major toxicological effects were associated with the dopamine agonist-related pharmacodynamic properties of rotigotine (e.g. hyperactivity and stereotype, enlarged ovary, sporadic gastric mucous membrane lesions, decreased body weight, food consumption and prolactin, and increased mononuclear cell, neutrophil granulocyte, aspartate aminotransferase and alanine aminotransferase) and foreign body removal reaction induced by poly(lactide-co-glycolide) and carboxymethycellulose sodium. At the end of recovery period, all findings had recovered to a normal level or to a certain degree except foreign body reaction at injection sites. RoMS has exhibited high safety on SD rats./LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ Continuous dopaminergic stimulation (CDS) is an important drug development strategy in the treatment of Parkinson's disease (PD). Rotigotine is a non-ergoline D(3)/D(2)/D(1) dopamine receptor agonist for treating PD. As a new treatment option for CDS, rotigotine-loaded microspheres (RoMS), long-acting sustained-release microspheres with poly(lactide-co-glycolide) as drug carrier, are now being evaluated in clinical trial. In the present study, the subchronic toxicity in Cynomolgus monkeys has been characterized via intramuscular administration with RoMS at 0, 10, 40 and 160 mg/kg, weekly for 3 months with a 1-month recovery period. The NOAEL was 10 mg/kg/week. One male at 160 mg/kg died from an extensive pulmonary embolism. The major toxicological effects were associated with dopamine agonist-related pharmacodynamic properties of rotigotine (e.g., hyperactivity and stereotype, decreased serum prolactin level) and foreign body removal reaction induced by poly(lactide-co-glycolide) and carboxymethycellulose sodium (e.g., increased mononuclear cells and neutrophils, thymus atrophy and vacuolar degeneration of adrenal cortex, foreign body granuloma with foam cells accumulation at injection sites and foam cells accumulation in spleen and multiple lymph sinuses). At the end of recovery period, above findings recovered to a normal level or to a certain degree except vacuolar degeneration of adrenal gland. RoMS has exhibited high safety on monkeys.For more Non-Human Toxicity Excerpts (Complete) data for ROTIGOTINE (15 total), please visit the HSDB record page. |
| Populations at Special Risk | Patients with a major psychotic disorder should ordinarily not be treated with Neupro because of the risk of exacerbating psychosis. |
| Antidote and Emergency Treatment | /SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B//SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B//SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W TKO /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's (LR) if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/There is no known antidote for overdosage of dopamine agonists. In case of suspected overdose, the excess transdermal system(s) should immediately be removed from the patient. Concentrations of rotigotine decrease after patch removal. The terminal half-life of rotigotine is 5 to 7 hours. The pharmacokinetic profile showed a biphasic elimination with an initial half-life of 3 hours. The patient's heart rate, heart rhythm, and blood pressure should be monitored. As shown in a study of renally impaired patients, dialysis is not expected to be beneficial. Treatment of overdose may require general supportive measures to maintain vital signs. If it is necessary to discontinue use of rotigotine after overdose, it should be discontinued gradually to prevent hyperpyrexia and confusion. |
| Effects During Pregnancy and Lactation | ◉ Summary of Use during Lactation |
| Wassergefährdungsklasse (WGK) | WGK 3 |
| Zollcode | 2934990002 |
| R-Sätze (R) | 22 |
| Gefahrensymbole | Xn |
| Lagerklasse | 11 - Combustible Solids |
| Gefahrstoffdaten | 99755-59-6(Hazardous Substances Data) |
Anwendungen & Verwendung
Beschreibung
While levodopa is still considered the cornerstone of treatment of Parkinson’s disease, many patients begin to experience treatment-related problems, such as a wearing-off phenomenon and the development of dyskinesias as the disease progresses. Continuous dopaminergic stimulation by means of a dopamine agonist has been recognized as being associated with a lower incidence of dyskinesias. Using a selective dopamine agonist as monotherapy in early disease may delay the onset of levodopa therapy, or at a minimum, lower its dose in adjunctive situations to minimize the adverse neurotoxic effects of levodopa. Rotigotine is a nonergolinic dopamine D3/D2/D1 receptor agonist, and it is the first dopamine agonist to be launched as a transdermal patch.
Verwenden
It is a non-ergot dopamine agonist drug and is indicated for the treatment of Parkinson disease.