Requip Modutab
Requip Modutab: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Requip Modutab
ATX code: N04BC04
Active ingredient: ropinirole (ropinirole)
Manufacturer: GLAXO WELLCOME, SA (Spain), SmithKline Beecham, PLC (Great Britain)
Description and photo update: 28.11.2018
Prices in pharmacies: from 1149 rubles.
Buy
Requip Modutab is an antiparkinsonian agent, a stimulant of dopaminergic transmission in the central nervous system (CNS), a dopamine agonist.
Release form and composition
Requip Modutab is available in the form of tablets of prolonged action, film-coated: biconvex, capsule-shaped, engraved "GS" on one side; 2 mg each - pink, on the other side of the tablet is engraved "3V2"; 4 mg each - light brown, “WXG” engraved on the other side of the tablet; 8 mg - red, on the other side of the tablet is engraved "5CC" (in blisters: 2 mg tablets - 14 pcs., in a cardboard box 2 or 6 blisters, or 21 pcs., in a cardboard box 2 blisters; tablets of 4 mg and 8 mg - 14 pcs., in a pack of cardboard 2 or 6 blisters; each pack also contains instructions for the use of Requip Modutab).
Composition of 1 film-coated tablet:
- active substance: ropinirole - 2 mg, 4 mg or 8 mg (equivalent to 2.28 mg, 4.56 mg or 9.12 mg ropinirole hydrochloride, respectively);
- additional components: hypromellose-2208, sodium carmellose, maltodextrin, lactose monohydrate, mannitol, glyceryl dibegenate, hydrogenated castor oil, povidone K29 / 32, magnesium stearate, colloidal silicon dioxide, yellow iron oxide (E172);
- film shell: tablets with a dosage of 2 mg - pink opadry dye QY-S-24900 [hypromellose-2910, macrogol-400, titanium dioxide, yellow iron oxide (E172), red iron oxide (E172)]; tablets with a dosage of 4 mg - light brown opadry dye OY-272Q7 [hypromellose-2910, macrogol-400, titanium dioxide, yellow "Sunset" (E110), indigo carmine]; tablets with a dosage of 8 mg - red dye opadry 03B25227 [hypromellose-2910, macrogol-400, titanium dioxide, yellow iron oxide (E172), black iron oxide (E172), red iron oxide (E172)].
Pharmacological properties
Pharmacodynamics
Requip Modutab is an antiparkinsonian agent, a highly selective non-ergoline agonist of dopamine D2-, D3-receptors with central and peripheral effects.
Requip Modutab has no effect on the disintegrating presynaptic dopaminergic neurons of the substantia nigra and acts directly as a synthetic neurotransmitter. Thus, ropinirole reduces the degree of hypodynamia, tremor and rigidity, which are symptoms of parkinsonism.
Taking the drug allows you to compensate for the dopamine deficiency in the systems of the substantia nigra and striatum by stimulating dopamine receptors in the striatum.
Ropinirole acts at the pituitary and hypothalamic levels to inhibit prolactin secretion.
Requip Modutab enhances the effects of levodopa, including controlling the frequency of the on / off phenomenon and the “end of dose” effect associated with long-term treatment with levodopa, and allows you to reduce its daily dose.
Pharmacokinetics
In healthy people, patients with restless legs syndrome and patients with Parkinson's disease, the pharmacokinetics of ropinirole are similar, the observed differences depend on the dosage form.
The oral bioavailability of ropinirole is low and averages ~ 50% (from 36% to 57%). Since Requip Modutab is available in the form of sustained-release tablets, after oral administration, the concentration of ropinirole in blood plasma increases slowly, the average time to reach the maximum concentration (Tmax) is 6 hours. In patients with Parkinson's disease, after oral administration of Requip Modutab in a daily dose of 12 mg together with food rich in fats, an increase in the systemic exposure of ropinirole was observed in the equilibrium state, while an increase in Cmax and AUC by 44% and 20%, respectively, was recorded, Tmax increased by 3 hours. However, during clinical trials of efficacy and safety, ropinirole was taken regardless of food intake.
The duration of the systemic effect of ropinirole (AUC and Cmax) increases approximately in proportion to the dose increase.
Ropinirole binds to blood plasma proteins at the level of 10-40%. Due to its high lipophilicity, it is characterized by a large volume of distribution (Vd), which is ~ 7 l / kg.
Ropinirole is metabolized primarily by the CYP1A2 isoenzyme.
The half-life (T1 / 2) from the systemic circulation is on average ~ 6 hours. The metabolite ropinirole is excreted mainly in the urine. The elimination of ropinirole after a single oral dose does not differ from that with regular use.
In elderly patients (aged 65 years and older), the clearance of ropinirole after oral administration is reduced by ~ 15% compared to younger patients. No dose adjustment is required in this category of patients.
Pharmacokinetic parameters in patients with mild to moderate renal impairment and Parkinson's disease are not affected. In patients with end-stage renal failure who are indicated for continuous hemodialysis, the clearance of ropinirole when taken orally decreases by ~ 30%.
Indications for use
Requip Modutab is prescribed for patients with Parkinson's disease:
- as a monotherapy drug (in the early stages of the disease in patients who need dopaminergic therapy, in order to delay the appointment of levodopa drugs);
- as part of combination therapy [in patients who are already receiving levodopa drugs, in order to enhance the effectiveness of the latter, including control of changes in the therapeutic effect of levodopa (the phenomenon of "on-off") and the effect of the "end of dose" against the background of prolonged therapy with levodopa, as well as reducing the daily dose of levodopa].
Contraindications
Absolute:
- acute psychosis;
- severe renal failure [creatinine clearance (CC) less than 30 ml / min] in the absence of regular hemodialysis;
- hepatic dysfunction;
- lactase deficiency, lactose intolerance, malabsorption of galactose / glucose;
- age under 18;
- period of pregnancy;
- breast-feeding;
- hypersensitivity to the components present in the composition of the product.
Relative (Requip Modutab tablets are taken with caution):
- severe cardiovascular insufficiency;
- a history of psychotic disorders (prescribed by a doctor only if the expected benefits of therapy exceed the possible risks).
Requip Modutab, instructions for use: method and dosage
Requip Modutab tablets are not chewed or broken; they are taken whole, once a day at the same time, regardless of the meal.
The dose should be selected individually, taking into account the effectiveness and tolerability of the drug in each specific case. If at any stage of dose selection the patient experiences drowsiness, the dose should be reduced. Similarly, it is necessary to proceed with the development of other undesirable reactions; subsequently, the dose should be increased gradually.
Dose titration is necessary if it is missed (if one or more doses have been missed).
With monotherapy, the initial daily dose is 2 mg. In this dose, Requip Modutab is taken for 7 days, after which the daily dose is gradually increased to 8 mg (by 2 mg every week: 1st week - 2 mg, 2nd week - 4 mg, 3rd week - 6 mg, 4th week - 8 mg).
In case of insufficiently expressed therapeutic effect, or its lack of persistence, it is possible to further increase the daily dose of ropinirole by 4 mg at intervals of 1-2 weeks (the dose is increased until the required therapeutic effect is achieved, but not exceeding the maximum daily dose of 24 mg).
In combination therapy, Requip Modutab is taken in doses used for monotherapy, simultaneously with levodopa drugs (depending on the clinical effect, the dose of levodopa can be gradually reduced). In clinical trials, patients simultaneously receiving the drug in the form of sustained-release tablets and levodopa, the dose of the latter was gradually reduced by ~ 30%. In patients with a progressive form of the disease who are taking Requip Modutab in combination with levodopa drugs, dyskinesia may occur during the titration period of ropinirole. To reduce these symptoms, it is recommended to reduce the dose of levodopa drugs.
Like other dopaminergic drugs, Requip Modutab should be withdrawn gradually, reducing the daily dose for at least 1 week. In the case of interruption of therapy for a day or more when resuming treatment, it is necessary to consider the appropriateness of dose titration.
In elderly patients (65 years and older), despite a possible decrease in drug clearance, titration of the ropinirole dose is performed as usual.
Patients with impaired renal function of mild and moderate severity (with CC from 30 to 50 ml / min) do not need to adjust the dose of ropinirole, since its clearance remains unchanged.
Patients with end-stage renal failure on hemodialysis are advised to take Requip Modutab at an initial daily dose of 2 mg. In the future, the dose is increased, taking into account its tolerance and effectiveness.
The maximum daily dose in patients on continuous hemodialysis is 18 mg. Maintenance doses are not required after the hemodialysis procedure.
Side effects
Classification of violations: very often - ≥ 1/10, often - ≥ 1/100 and <1/10, infrequently - ≥ 1/1000 and <1/100, rarely - ≥ 1/10 000 and <1/1000, very rarely - <1/10 000, including isolated cases.
Adverse reactions reported in clinical trials (monotherapy):
- mental disorders: often - hallucinations;
- disorders of the central nervous system: very often - drowsiness; often - dizziness (including vertigo);
- vascular disorders: infrequently - hypotension (including orthostatic);
- disorders of the digestive system: very often - nausea; often - dyspepsia, constipation, vomiting, abdominal pain;
- general disorders and disorders at the injection site: often - peripheral edema (including edema of the legs).
Adverse reactions reported in clinical trials (combination therapy):
- mental disorders: often - confusion, hallucinations;
- disorders of the central nervous system: very often - dyskinesia (in patients with a progressive form of the disease who take Requip Modutab simultaneously with levodopa drugs, during the dose titration period, coordination of movements may be impaired; in order to reduce these symptoms, levodopa drugs are canceled); often - dizziness (including vertigo), drowsiness;
- vascular disorders: often - hypotension (including orthostatic);
- disorders of the digestive system: often - nausea, constipation;
- general disorders and disorders at the injection site: often - peripheral edema.
Adverse reactions recorded during post-registration observations:
- mental disorders: infrequently - psychotic reactions (except for hallucinations), including delirium, delirium, paranoia; impulsive drive syndrome, increased libido, including hypersexuality, an irresistible urge to make purchases, pathological cravings for gambling, overeating, the manifestation of aggression associated with compulsive symptoms and psychotic reactions;
- disorders from the central nervous system: very rarely - severe drowsiness, cases of sudden falling asleep (as with other dopaminergic drugs, reports of severe drowsiness and cases of sudden falling asleep have been reported extremely rarely, primarily these episodes were observed in patients with Parkinson's disease during post-registration observation. There are reports of sudden falling asleep in the absence of any previous or obvious signs of fatigue and drowsiness. Reducing the dose / discontinuation of the drug can eliminate these symptoms. In most cases, concomitant sedatives were used);
- disorders of the immune system: very rarely - hypersensitivity reactions (urticaria, rash, itching, angioedema);
- vascular disorders: often - hypotension (including orthostatic).
Overdose
Symptoms of an overdose of Requip Modutab are due to dopaminergic action and include nausea, vomiting, drowsiness, and dizziness.
Treatment for this condition is with dopamine antagonists (eg, antipsychotics and metoclopramide).
special instructions
When taking Requip Modutab, drowsiness may develop, episodes of sudden falling asleep are not excluded, sometimes not preceded by drowsiness, about which patients should be warned in advance. If such reactions occur, it is advisable to consider discontinuing therapy.
Because of the possible development of orthostatic hypotension, it is recommended to monitor blood pressure (BP).
In patients with restless legs syndrome, ropinirole therapy in some cases led to a paradoxical worsening of the condition (earlier onset, increased intensity of manifestations, or progression of symptoms with seizure of previously unaffected limbs) or the development of rebound syndrome (recurrence of symptoms) in the early morning hours. If these symptoms appear, the tactics of treatment with ropinirole should be reviewed, the dose should be adjusted or Requip Modutab should be completely canceled.
There are reports of the development of impulsive drive syndrome, including compulsive behavior (hypersexuality, pathological gambling, overeating, irresistible urge to buy), in patients who took dopaminergic drugs, including ropinirole. Desire disorders are reversible, for this you need to reduce the dose of the drug or completely cancel it. When using the drug Requip Modutab in some patients, other risk factors may be the combined use of several dopaminergic drugs or reports of compulsive behavior in history.
The drug is produced in the form of prolonged-release film-coated tablets with the ability to release the active substance during the day. In situations where the drug passes through the gastrointestinal tract too quickly, the likelihood of incomplete release of the active substance increases, the remainder of which passes into the stool.
Influence on the ability to drive vehicles and complex mechanisms
During therapy with ropinirole, adverse reactions may occur that affect the speed of psychomotor reactions and concentration of attention, which should be warned the patient in advance. In rare cases, sudden falling asleep was noted, while no previous / obvious signs of daytime sleepiness or dizziness were noticed. In the presence of such manifestations, it is recommended to refuse to engage in potentially hazardous activities, including driving vehicles.
Application during pregnancy and lactation
It is contraindicated to use Requip Modutab for pregnant and breastfeeding women.
Pediatric use
Age under 18 is a contraindication to taking the drug.
With impaired renal function
In case of impaired renal function of mild and moderate severity (CC - 30-50 ml / min), it is not required to adjust the dose of ropinirole.
The recommended initial daily dose of Requip Modutab in patients with end-stage renal failure on hemodialysis is 2 mg. In the future, the dose is increased based on data on its effectiveness and tolerability.
The maximum daily dose in patients on continuous hemodialysis is 18 mg. Maintenance doses are not required after the hemodialysis procedure.
For violations of liver function
For violations of hepatic function, taking Requip Modutab is contraindicated.
Use in the elderly
Despite the possible decrease in drug clearance in elderly patients (65 years and older), titration of the ropinirole dose in this category of patients is carried out as usual.
Drug interactions
- antipsychotics, other dopamine antagonists of central action (for example, metoclopramide, sulpiride): reduce the effectiveness of ropinirole (simultaneous administration is not recommended);
- levodopa, domperidone, digoxin: no pharmacological interaction was observed (dose adjustment is not required);
- ciprofloxacin: increases the Cmax of ropinirole by approximately 60%, AUC - by 84% (it is necessary to adjust the dose of ropinirole; it is recommended to do the same when taking and discontinuing drugs that inhibit the CYP1A2 isoenzyme, including enoxacin, fluvoxamine);
- substrates of the isoenzyme CYP1A2 (for example, theophylline): the pharmacokinetics of the drugs remains unchanged;
- estrogens (high doses): the concentration of ropinirole in plasma increases (for patients who received hormone replacement therapy before starting Requip Modutab, treatment with ropinirole can be prescribed as usual. Dose adjustment may be required for those patients in whom hormone replacement therapy was stopped / started time of ropinirole therapy);
- ethanol: no drug interaction with ropinirole was observed (nevertheless, it is recommended to refrain from drinking alcoholic beverages during drug therapy);
- other drugs taken for parkinsonism: no interaction with ropinirole was found.
Dose adjustment Requip Modutab may be required in patients who have started / stopped smoking during ropinirole therapy, since nicotine is an inducer of the CYP1A2 isoenzyme.
Analogs
Requip Modutab analogs are Rolprina SR, Sindranol, Ropinirole Teva, etc.
Terms and conditions of storage
Store in its original packaging at temperatures up to 25 ° C, out of the reach of children.
Shelf life: tablets with a dosage of 2 mg - 2 years, tablets with a dosage of 4 mg and 8 mg - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Requip Modutab
There are few reviews of Requip Modutab, mostly they are positive. The drug is considered effective, rapidly relieving negative symptoms in patients with Parkinson's disease. When taken, a decrease in tremor and rigidity, which are characteristic symptoms of the disease, was noted. Patients like the convenient method of application (once a day), the absence of dependence on meals.
The disadvantages of Requip Modutab indicate the development of undesirable effects such as drowsiness, constipation, lowering blood pressure, and in some cases, hallucinations.
Price for Requip Modutab in pharmacies
The price for Requip Modutab for a pack containing 28 pieces is:
- tablets with a dosage of 2 mg: 1085-1550 rubles;
- tablets with a dosage of 4 mg: RUB 1,870–2280;
- tablets with a dosage of 8 mg: 3520–4220 rubles.
Requip Modutab: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Requip Modutab 2 mg film-coated tablets of prolonged action 28 pcs. 1149 RUB Buy |
|
Requip Modutab tablets coated captivity. obol. prolonged action 2mg 28 pcs. 1299 RUB Buy |
|
Requip Modutab 4 mg film-coated tablets of prolonged action 28 pcs. 1598 RUB Buy |
|
Requip Modutab 8 mg prolonged-release film-coated tablets 28 pcs. 3477 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
