Requipip Modules Tablet 4 mg 28 pcs
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Active ingredients
Ropinirol
Release form
Pills
Composition
Ropinirole hydrochloride * 4.56 mg,; which corresponds to the content of ropinirole 4 mg; Excipients: upper barrier layer **: hypromellose 2208 - 62.83 mg, glyceryl dibeganate - 35 mg, mannitol - 33.04 mg, povidone K29-32 - 7 mg, magnesium stearate - 1.4 mg, colloidal silicon dioxide - 0.56 mg, iron (III) oxide (yellow) - 0.17 mg; active layer: hypromellose 2208 - 61.5 mg, lactose monohydrate - 44.04 mg, carmellose sodium - 15 mg, castor oil, hydrogenated - 15 mg, maltodextrin - 7.5 mg, magnesium stearate - 1.5 mg, colloidal silicon dioxide - 0.9 mg; lower barrier layer **: hypromellose 2208 - 76.29 mg, glyceryl dibeganate - 42.5 mg, mannitol - 40.12 mg, povidone K29-32 - 8.5 mg, magnesium stearate - 1.7 mg, colloidal silicon dioxide - 0.68 mg, iron (III) oxide ( yellow) - 0.21 mg.; Film coating composition: Opydray OY-27207 dye light brown - 13.8 mg (hypromellose 2910 - 62.5%, titanium dioxide - 21.25%, macrogol 400 - 6.25%, sunset sunflower yellow - 9%, indigo carmine - one%).
Pharmacological effect
An anti-parkinsonian drug, a highly selective non-ergoline agonist of dopamine D2, D3 receptors, which has a peripheral and central action.; The drug does not act on decaying presynaptic black matter neurons and acts directly as a synthetic neurotransmitter. Thus, ropinirole reduces the degree of hypodynamia, rigidity and tremor, which are symptoms of parkinsonism.; Ropinirol compensates for dopamine deficiency in the black and striatal systems by stimulating the dopamine receptors in the banded body; and the effect of "end of dose" associated with long-term therapy with levodopa, and allows to reduce the daily dose of levodopa.; Ropinirol has an effect at the level of hypothesis ADR and pituitary to inhibit the secretion of prolactin.
Pharmacokinetics
The pharmacokinetics of ropinirole is similar in healthy people, patients with Parkinson's disease and patients with restless legs syndrome and varies depending on the dosage form.; Absorption; After oral administration, bioavailability of ropinirole is low and is approximately 50% (36-57%). After ingestion of ropinirole in sustained release pills, its concentration in plasma increases slowly, the average time Tmax is 6 hours.Patients with Parkinson's disease after ingestion of ropinirole at a dose of 12 mg 1 time / day in combination with food rich in fats, in an equilibrium state, increased systemic exposure of ropinirole was observed, with an increase in AUC and Cmax by 20% and 44% respectively, Tmax lengthened by 3 hours. However, in clinical studies of the efficacy and safety, ropinirole was taken regardless of the meal.; The increase in the duration of the systemic action of ropinirole (Cmax and AUC) is approximately proportional to the dose increase;; Distribution; Linkage Blood plasma protein levels are low (10–40%). Due to its high lipophilicity, ropinirole is characterized by a high Vd (approximately 7 l / kg); Metabolism; Ropinirol is mainly metabolized by the CYP1A2 isoenzyme; There is no difference in the removal of ropinirole after a single dose by mouth or with regular use.; Pharmacokinetics in special clinical situations; The clearance of ropinirole after oral administration is reduced by approximately 15% in elderly patients (65 years and older) compared with younger patients. Dose adjustment in this category of patients is not required.; Pharmacokinetic parameters do not change in patients with impaired mild to moderate renal function and Parkinson's disease. In patients with end-stage renal failure who are on constant hemodialysis, the clearance of ropinirole when administered orally is reduced by about 30%.
Indications
Parkinson's disease: - monotherapy for the early stages of the disease in patients who need dopaminergic therapy in order to delay the administration of levodopa drugs; - as part of combination therapy in patients receiving levodopa preparations in order to increase the effectiveness of levodopa, including the control of fluctuations of the therapeutic effect of levodopa (on-off phenomenon) and the “end of dose” effect against the background of chronic therapy with levodopa doses of levodopa.
Contraindications
- acute psychosis; - abnormal liver function; - severe renal dysfunction (CC less than 30 ml / min), which is not carried out regular hemodialysis; - rare hereditary diseases: lactose intolerance, lactase deficiency,impaired glucose or galactose absorption; - pregnancy; - lactation; - children's and teenage age up to 18 years; - hypersensitivity to the drug components.; The drug should be used with caution in patients with severe cardiovascular insufficiency. Ropinirol can be prescribed to patients with a history of psychotic disorders only in cases where the expected benefit from its use outweighs the potential risk.
Use during pregnancy and lactation
Contraindicated use during pregnancy and lactation (breastfeeding).
Dosage and administration
The drug is administered orally 1 time / day at the same time, regardless of the meal. The pills are taken whole without chewing, without breaking.; It is recommended that the individual selection of the dose in accordance with the effectiveness and tolerability of the drug.; It is recommended to reduce the dose if the patient is drowsy at any stage of the selection of the dose. With the development of other adverse reactions it is necessary to reduce the dose of the drug, followed by a gradual increase in the dose. It should be borne in mind the need for dose titration when skipping a dose (one or more); Monotherapy; Start of treatment; Recommended initial dose of the drug Requip Modoutab; is 2 mg 1 time per day for one week. Subsequently, the dose is increased by 2 mg at intervals of at least 1 week to 8 mg / day; Maintenance dose; If the therapeutic effect after dose adjustment is not sufficiently pronounced or unstable, you can continue to increase the daily dose of the drug by 4 mg at intervals of 1-2 weeks ( to achieve the desired therapeutic effect). The dose can be changed depending on the therapeutic effect and increased to a maximum dose of 24 mg 1 time / day; Combination therapy; When using the drug Requip Modoutab; in doses used in monotherapy, in combination with levodopa preparations, the dose of levodopa can be gradually reduced (depending on the clinical effect). In clinical studies in patients simultaneously receiving Requipip Modutab; in sustained release pills, the dose of levodopa was gradually reduced by approximately 30%. In patients with a progressive form of the disease, taking Requip Modutab; in combination with levodopa preparations, dyskinesia may occur during the dose titration period of ropinirole. Reducing the dose of levodopa drugs can lead to a reduction of these symptoms. Cancellation of therapy.Requipo Modutab; (like other dopaminergic drugs) should be abolished, gradually reducing the daily dose for at least 1 week. If treatment was interrupted for 1 day or more, when therapy is resumed, the need for dose titration should be considered. Despite the possible reduction in clearance of the drug in patients aged 65 years and older, dose ropinirole is titrated in this category of patients as usual .; In patients with impaired renal mild and moderate severity (CC 30-50 ml / min), ropinirole clearance does not change, dose adjustment of ropinirole is not required. For patients with end-stage renal failure on hemodia Liza, the recommended initial dose of ropinirole is 2 mg 1 time / day. A subsequent increase in dose should be based on an assessment of tolerability and effectiveness. The maximum daily dose in patients on permanent hemodialysis is 18 mg. Administration of maintenance doses after hemodialysis is not required.
Side effects
The adverse reactions listed below are listed according to the damage to organ systems and the frequency of occurrence. The frequency of occurrence is determined as follows: very often (≥1 / 10); often (≥1 / 100, <1/10); sometimes (≥1 / 1000, <1/100); rarely (≥1 / 10,000, <1/1000); very rarely (<1/10 000, including isolated cases) .; Clinical data; The table lists adverse reactions that occur with a higher frequency when using ropinirole compared with placebo or a higher or comparable frequency of occurrence with respect to the comparator drug .; In patients with a progressive form of the disease, taking Requip Modutab, in combination with levodopa preparations, during the period of dose titration, the development of impaired coordination of movements is possible. It was shown that the elimination of levodopa drugs can lead to a reduction in these symptoms.; Post-observation observations; From the immune system: very rarely - hypersensitivity reactions, including urticaria, angioedema, rash, itching.; Mental disorders: infrequently - psychotic reactions (excluding hallucinations), including delirium, paranoia, delirium; Immune drive syndrome, increased libido, including hypersexuality,pathological craving for gambling, irresistible craving for shopping, overeating, aggression *; From the nervous system: very rarely - severe drowsiness, episodes of sudden sleep **; From the side of the cardiovascular system: often - orthostatic hypotension, hypotension *** .; Allergic reactions: very rarely - urticaria, angioedema, rash, itching; * Aggression is associated with psychotic reactions and compulsive symptoms. ** As with the use of other dopaminergic drugs, severe sinusitis and episodes with communicated very rarely, primarily in patients with Parkinson's disease during post-registration follow-up. There are cases of sudden sleep without any previous or obvious signs of drowsiness and fatigue. With a decrease in the dose or withdrawal of the drug, all the symptoms disappeared. In most cases, concomitant sedatives were used. *** As in the case of using other dopamiaergic drugs, hypotension was observed in the treatment with ropinirole, including orthostatic hypotension.
Overdose
Symptoms: mainly due to dopaminergic effects - nausea, vomiting, dizziness, drowsiness. Treatment: use of dopamine antagonists, such as typical antipsychotics and metoclopramide.
Interaction with other drugs
Typical antipsychotics and other centrally acting dopamine antagonists, such as sulpiride or metoclopramide, can reduce the effectiveness of ropinirole (simultaneous administration should be avoided); no pharmacokinetic interaction between ropinirole and levodopa or domperidone was noted, which would require dose adjustment of these drugs. with other drugs that are often used to treat Parkinson's disease. In patients with Parkinson's disease who took both digoxys n, no interaction of digoxin with ropinirole was found, which would require dose adjustment.; Ropinirole is mainly metabolized by the CYP1A2 isoenzyme. Pharmacokinetic studies in patients with Parkinson's disease have shown that ciprofloxacin increases Cmax and AUC of ropinirole by approximately 60% and 84%, respectively.In this regard, in patients receiving ropinirol, its dose should be adjusted when prescribing and discontinuing drugs that inhibit CYP1A2 isoenzyme, for example, ciprofloxacin, enoxacin or fluvoxamine; substrate of the isoenzyme CYP1A2, showed that the pharmacokinetics of drugs does not change. With the simultaneous use of ropinirole with other substrates of CYP1A2 isoenzyme, the pharmacokinetics of ropinirole does not change. An increase in plasma ropinirole concentration was observed in patients who received estrogens in high doses. In patients receiving hormone replacement therapy before starting treatment with ropinirole, treatment with ropinirole can be initiated as usual. However, in case of termination of hormone replacement therapy or its initiation during ropinirole therapy, dose adjustment may be required. There is no information on the possibility of interaction between ropinirole and ethanol. As with other centrally acting drugs, patients should be warned to refrain from taking alcohol during treatment with ropinirole. Nicotine is known to induce the CYP1A2 isoenzyme, so if the patient starts or stops smoking during treatment with ropinirole, need to adjust its dose.
special instructions
Patients should be warned about the possible development of drowsiness or episodes of sudden sleep, sometimes not preceded by drowsiness. In the event of such reactions, the possibility of discontinuation of therapy should be considered. Blood pressure monitoring is recommended because of the possibility of developing orthostatic hypotension. In patients taking dopaminergic drugs, including ropinirole, impulse impulses syndrome, including compulsive behavior, including pathological craving for gambling, hypersexuality, irresistible craving for shopping, overeating. Disorders of desire, as a rule, are reversible after dose reduction or drug withdrawal. In some cases, when using the drug Requip Modutab; other risk factors may be a history of compulsive behavior or the combined use of several dopaminergic drugs. Paradoxical deterioration of the condition in restless legs syndrome was noted during ropinirole therapy (an earlier onset, an increase in the intensity of manifestations,either progression of symptoms with involvement of previously unaffected extremities), or rebound syndrome in the early morning hours (recurrence of symptoms in the early morning hours). With the appearance of these symptoms, it is necessary to revise the tactics of treatment with ropinirole, to clarify the dose up to the possible discontinuation of the drug. Prenarate Requip Modutab; available in the form of sustained-release pills, film-coated, with the property of releasing the active substance within 24 hours ; Patients should be warned of possible adverse reactions during ropinirole therapy. Patients should be informed that there are very rare au episodes of sudden sleep without any previous or obvious signs of daytime sleepiness and cases of dizziness (sometimes pronounced). If the patient has developed daytime sleepiness or episodes of falling asleep during the day, requiring active intervention, the patient should be warned about the need to abandon driving vehicles and avoid other activities that require high concentration of attention and speed of psychomotor reactions.