Index of drugs

Treatment of Parkinson's disease in accordance with the following principles: initial treatment as monotherapy to delay the introduction of levodopa for treatment; combined treatment with levodopa during the disease period, when the effect of levodopa extinguishes or becomes variable and fluctuations of the therapeutic effect appear (end-dose effect or "on-off" fluctuations).

1 tabl sustained release contains 2 mg, 4 mg or 8 mg of ropinirole hydrochloride. The tablets contain lactose and castor oil.

Nonergoline Dopamine agonist D2 / D3. It reduces the dopamine deficiency characteristic of Parkinson's disease by stimulation of dopamine receptors in the striatum. It works on the hypothalamus and pituitary gland, inhibiting the secretion of prolactin. The bioavailability of ropinirole is approximately 50% (36-57%). After oral administration of C_max is achieved within 6-10 h. In patients receiving the drug in the form of tablets. about release, a high-fat meal may increase systemic exposure to ropinirole (increased AUC by 20% on average,_max 44% on average, T-delay_max by 3 hours). Ropinirole 10-40% bound to plasma proteins. It is metabolized mainly via CYP1A2 and excreted as metabolites in the urine. T_0,5 is about 6 hours.

Hypersensitivity to the active substance or to any of the excipients. Severe renal impairment (creatinine clearance <30 ml / min) without regular hemodialysis. Hepatic dysfunction.

Dopamine agonist medicines should not be used in patients with a history of serious psychiatric or psychotic disorders or such disorders unless the potential benefit outweighs the risk. Patients should be warned about the possibility of sudden sleep attacks (without any warning signals). In these patients, a dose reduction or complete termination of therapy may be considered. Patients should be monitored regularly for the development of impulse control disorders. Patients and their carers should be advised that in patients treated with dopamine agonists, behavioral symptoms of impulse control disorders may occur, including: addiction to 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. These disorders were especially observed in patients treated with high doses of the drug and usually resolved after a dose reduction or discontinuation of the drug. In some cases, a history of risk has occurred, such as pre-existing compulsive behaviors. Due to the risk of hypotension, it is recommended to control blood pressure, especially at the beginning of treatment and with particular attention to patients with severe cardiovascular diseases (especially coronary insufficiency). It is not recommended for use in children and adolescents <18 years. Due to the lactose content, the preparation should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. The tablets contain castor oil, which can cause stomach upset and diarrhea.

Pregnancy is not recommended unless the expected benefits to the patient outweigh the risks to the fetus. The drug can inhibit lactation - do not use during breastfeeding.

Side effects in patients with Parkinson's disease treated with ropinirole in the form of prolonged release (up to 24 mg / day).monotherapy. Very often: drowsiness, nausea. Common: hallucinations, dizziness (including labyrinthine origin), constipation, peripheral edema. Uncommon: orthostatic hypotension, hypotension.Combination therapy. Very often: dyskinesias. Common: hallucinations, drowsiness, dizziness (including labyrinthine origin), orthostatic hypotension, hypotension, nausea, constipation, peripheral edema.
In addition, in patients with Parkinson's disease treated with ropinirole in the form ofof immediate release (up to 24 mg / day) the following side effects have been observed.monotherapy. Very often: fainting. Common: vomiting, heartburn, abdominal pain, swelling of the legs. Uncommon: psychotic reactions (other than hallucinations) including delirium, delusions, paranoia, sudden sleep bouts, excessive daytime sleepiness, orthostatic hypotension, hypotension (rarely severe). Frequency unknown: hypersensitivity reactions (including urticaria, angioneurotic edema, rash, pruritus), addiction to gambling, increased libido, hypersexuality, compulsive spending or buying, compulsive or paroxysmal overeating, liver reactions (mainly increased liver enzymes).Combination therapy. Very often: drowsiness, nausea. Common: confusion, heartburn. Uncommon: psychotic reactions (other than hallucinations) including delirium, delusions, paranoia, sudden sleep bouts, excessive daytime sleepiness, orthostatic hypotension, hypotension (rarely severe). Frequency unknown: hypersensitivity reactions (including urticaria, angioneurotic edema, rash, pruritus), addiction to gambling, increased libido, hypersexuality, compulsive spending or buying, compulsive or paroxysmal overeating, liver reactions (mainly increased liver enzymes).

Orally. Adults. Individual dose selection is recommended depending on the efficacy and tolerability of the drug. The starting dose is 2 mg once a day for 1 week of treatment; Starting from the second week, the dose should be increased to 4 mg once a day. The response to treatment may be seen with a 4 mg dose once a day. Patients who started treatment with a dose of 2 mg drug in the form of tablets. about once a day, if you experience side effects that you are not able to tolerate, you may benefit from switching to ropinirole in the form of tablets. with immediate release at a lower daily dose, divided into 3 equal doses. Treatment should be continued with the lowest dose in the form of tablets. about release allowing control of clinical symptoms. If the 4 mg dose once a day administered in the form of about release is not sufficient to achieve or maintain control of symptoms, then the daily dose may be increased by 2 mg at weekly or longer intervals up to a dose of 8 mg once a day. If this dose is not enough to achieve or maintain control of symptoms then the dose can be increased by 2-4 mg at 2-week intervals. or longer. The maximum daily dose of ropinirole in the form of sustained release is 24 mg. It is recommended to prescribe the smallest possible number of tablets to the patients, which is necessary to achieve the recommended dose, by using the highest available power of ropinirole in the form of tablets. about release.Specific recommendations for treatment with ropinirole. If the treatment is discontinued daily or longer, consider re-starting with a gradual increase in dose until the therapeutic dose is reached. The use of ropinirole in combination with levodopa may allow a gradual reduction in the dose of levodopa, depending on the clinical response. In clinical trials, the dose of levodopa was reduced by approximately 30%. In advanced Parkinson's disease in combination with levodopa, dyskinesias may occur during the initial titration increase, reducing the dose of levodopa may reduce dyskinesias. If treatment with another dopamine agonist is changed to ropinirole, the instructions of the MAH should be followed before discontinuation of the medicine. Change of treatment with ropinirole in the form of tablets of immediate release on the preparation in the form of about release can be done overnight. The dose of ropinirole in the form of about release is calculated on the basis of the total daily dose of ropinirole in the form of about the immediate release that the patient has taken so far. If the patient took 0.75-2.25 mg daily - the dose of the preparation about the 2 mg / day, 3-4 mg / day - 4 mg, 6 mg - 6 mg, 7.5-9 mg - 8 mg, 12 mg - 12 mg, dose of 15-18 mg - 16 mg, at a dose of 21 mg - 20 mg, at a dose of 24 mg - 24 mg. After switching to ropinirole treatment in the form of With prolonged release, the total daily dose may be adjusted depending on the clinical response to treatment.Special groups of patients. In patients ≥65 years, the clearance of ropinirole is reduced by approximately 15%, the dose should be individually adjusted depending on the response to treatment; in patients ≥75 years, a slower dose increase when starting treatment may be considered. No dose adjustment is required in patients with mild to moderate renal impairment (creatinine clearance 30-50 ml / min). In patients with end stage renal disease (undergoing hemodialysis) the following dose adjustments are required: initial dose - 2 mg once a day; further dose increases should be based on tolerability and efficacy; maximum dose of ropinirole - 18 mg / day in patients receiving regular hemodialysis.
The tablets should be taken once a day, at the same time each day, regardless of the meal, swallowed whole, must not be chewed, crushed or divided.