Rekvip Modutab, 4 mg 28 pcs

Requip Modutab is an antiparkinsonian drug, a highly selective non-ergoline agonist of dopamine D 2 -, D 3 -receptors, which has peripheral and central action. The drug does not act on disrupting presynaptic dopaminergic 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. Ropinirole compensates for dopamine deficits in the black matter and striatum systems by stimulating dopamine receptors in the striatum.

Ropinirole enhances the effects of levodopa, including the control of on/off frequency phenomenon and “end-of-dose” effects associated with long-term therapy with levodopa drugs, and allows a reduction in the daily dose of levodopa. Ropinirole acts at the hypothalamic and pituitary levels by inhibiting prolactin secretion.

Pharmacokinetics

The pharmacokinetics of ropinirole are similar in healthy subjects, Parkinson’s patients and patients with restless legs syndrome and differ depending on the dosage form.

Intake.

The bioavailability of ropinirole after oral administration is low and is approximately 50% (36%-57%). After oral administration of ropinirole in slow release tablets its concentration in plasma increases slowly, the average time of reaching the maximum concentration (Tmax) is 6 hours. In equilibrium patients with Parkinson’s disease after oral administration of 12 mg ropinirole once daily in combination with fat-rich food, an increase in systemic ropinirole exposure was observed, with the area under “concentration-time” curve (AUC) and maximum concentration (Cmax) increasing by 20% and 44% respectively, Tmax was prolonged by 3 hours. However, in clinical studies of efficacy and safety ropinirole was taken regardless of food intake.

Binding to plasma proteins and distribution. Binding to plasma proteins is low (10-40%). Due to high lipophilicity ropinirole is characterized by high volume of distribution (approximately 7 l/kg).

Metabolism. Ropinirole is mainly metabolized by CYP1A2 isoenzyme.

The metabolite of ropinirole is mainly excreted by the kidneys.

Evacuation. On average, the elimination half-life of ropinirole from the systemic bloodstream is about 6 hours. The increase in the duration of systemic action of ropinirole (Cmax and AUC) is approximately proportional to the increase in dose. There is no difference in excretion of ropinirole after a single oral dose or with regular use.

Special patient groups

Elderly patients

The clearance of ropinirole after oral administration is reduced by approximately 15% in elderly patients aged 65 years and older compared to younger patients. No dose adjustment is required in this category of patients.

Patients with impaired renal function

Pharmacokinetic parameters are not changed in patients with mild to moderate renal impairment and Parkinson’s disease.
In patients with end-stage renal failure who are on permanent hemodialysis, oral ropinirole clearance is reduced by approximately 30%.

Indications

Parkinson’s disease:

Active ingredient

Composition

Active ingredient:

Ropinirole hydrochloride;

Associates:

Hypromellose-2208,

hydrogenated castor oil,

sodium carmellose, povidone-K29-32,

maltodextrin,

magnesium stearate,

lactose monohydrate,

silicon dioxide colloid,

mannitol,

iron [III] oxide (yellow) (E172),

glyceryl dibeugenate

How to take, the dosage

Adults
Orally.
“Rekvip Modutab” should be taken once a day at the same time regardless of meals. Tablets should be taken whole, without chewing or breaking.

The need for dose titration should be considered when missing a dose (one or more).
Dose reduction is recommended if the patient experiences drowsiness at any stage of dose titration.
If other adverse reactions develop, the dose of the drug should be reduced followed by a gradual increase in the dose.
Individual adjustment of the dose according to the effectiveness and tolerability of the drug is recommended.

Monotherapy
Commencement of treatment
The recommended starting dose of Rekvip Modutab is 2 mg once daily for one week. Subsequently, the dose is increased by 2 mg at intervals of at least 1 week to 8 mg/day.

The maintenance dose

If after adjusting the dose the therapeutic effect is not sufficiently pronounced or is unstable, the daily dose of the drug may be increased further by 4 mg at intervals of 1-2 weeks (until the desired therapeutic effect is achieved).
The dose may be changed depending on the therapeutic effect and increased to a maximum dose of 24 mg once a day.

Contraindications

Hypersensitivity

Side effects

CNS disorders: drowsiness, dyskinesia; hallucinations, dizziness (up to severe); confusion, drowsiness, dizziness (up to severe);

Cardiovascular disorders: orthostatic hypotension, decreased BP, orthostatic hypotension, decreased BP;

Digestive system disorders: nausea, abdominal pain, dyspepsia, vomiting, constipation;

General reactions: peripheral edema (including leg edema);

CNS and peripheral nervous system disorders: Psychotic states (including delirium and delirium), perceptual disturbances (including illusions, excluding hallucinations), increased impulsivity, increased libido, including hypersexuality, pathological cravings for gambling; marked somnolence, episodes of sudden falling asleep (as with other dopaminergic agents, these symptoms have very rarely been reported in patients with Parkinson’s disease ). When the dose was reduced or the drug was withdrawn, all symptoms disappeared. In most cases, concomitant sedation was used.

Cardiovascular system: orthostatic hypotension, decreased BP.

Allergic reactions: urticaria, angioedema, rash, itching.

Overdose

Symptoms: mainly the symptoms of ropinirole overdose are related to dopaminergic effects (nausea, vomiting, dizziness, drowsiness).

Treatment: these symptoms can be corrected with appropriate treatment with dopamine antagonists such as typical neuroleptics and metoclopramide.

Pregnancy use

Pregnancy is possible if the expected effect of therapy is greater than the potential risk to the fetus.

The FDA fetal category is C.

Ropinirol inhibits prolactin secretion in humans and can potentially inhibit lactation. Animal studies have shown that ropinirole and/or its metabolites are excreted into the milk of lactating rats. It is not known whether ropinirole is excreted into human breast milk.

Because many drugs are excreted in the milk of women and there may be serious adverse effects of ropinirole on the infant, a decision should be made either to stop breastfeeding or to stop taking ropinirole (given the degree of maternal need for the drug).

Similarities