Syndranol
Syndranol: 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: Sindranol
ATX code: N04BC04
Active ingredient: ropinirole (Ropinirole)
Manufacturer: Pharmaten International S. A. (Greece)
Description and photo updated: 30.11.2018
Prices in pharmacies: from 477 rubles.
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Sindranol is an antiparkinsonian drug, a dopamine agonist.
Release form and composition
The drug is produced in the form of tablets of prolonged action, film-coated: biconvex, the core of the tablet is almost white; dosage of 2 mg - round, pink; dosage 4 mg - oblong, light brown; dosage 8 mg - oblong, reddish-brown color (14 pcs. in blisters, in a cardboard box 2, 4 or 6 packages and instructions for use of Syndranol).
1 tablet contains:
- active substance: ropinirole hydrochloride - 2.28; 4.56 or 9.121 mg, which is equivalent to 2, 4 or 8 mg of ropinirole, respectively;
- auxiliary components: methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer (2: 0.1: 1), sodium lauryl sulfate, hypromellose, magnesium stearate, copovidone.
The composition of the film coating of tablets:
- dosage 2 mg: Opadry II pink 32K14834 [hypromellose 2910 (hypromellose 15cP), lactose monohydrate, triacetin, iron oxide red dye, titanium dioxide];
- dosage 4 mg: Opadry yellowish brown OY-27207 [hypromellose 2910 (hypromellose 6cP), macrogol 400, yellow sunset dye aluminum, indigo carmine aluminum varnish (E132), titanium dioxide];
- dosage of 8 mg: Opadry red 03B25227 [hypromellose 2910 (hypromellose 6cP), macrogol 400, iron oxide black, iron oxide red, iron oxide yellow, titanium dioxide].
Pharmacological properties
Pharmacodynamics
Sindranol is an antiparkinsonian drug with dopaminomimetic action. Its active substance, ropinirole, is a highly selective non-ergoline agonist of D 2 -, D 3 -dopamine receptors, has a peripheral and central effect. The action of a direct synthetic neurotransmitter inherent in ropinirole excludes its effect on the decaying presynaptic dopaminergic neurons of the substantia nigra. Thanks to this, the degree of manifestation of such symptoms of Parkinson's disease as inactivity, rigidity and tremor is reduced.
By stimulating dopamine receptors in the striatum, the drug compensates for the dopamine deficiency in the systems of the substantia nigra and striatum. The action of ropinirole at the level of the hypothalamus and pituitary gland is aimed at inhibiting the secretion of prolactin.
Against the background of the use of Syndranol, such effects of levodopa as control of the effect of the end of the dose and the frequency of the "on-off" phenomenon that occur during prolonged therapy with levodopa are enhanced.
When ropinirole is used in daily doses up to 4 mg, there is no risk of prolongation of the QT interval on the electrocardiogram (ECG). It is impossible to exclude the prolongation of the QT interval on the ECG when taking higher doses due to the lack of clinical trial results.
Pharmacokinetics
After oral administration of a prolonged-release tablet, a slow increase in plasma ropinirole is observed. Its maximum plasma concentration (C max) is reached after 6-10 hours. Taking Syndranol at a dose of 12 mg once a day simultaneously with fatty foods causes an increase in the systemic exposure of ropinirole compared to taking it on an empty stomach. At the same time, there is an increase in C max in blood plasma by an average of 44% and AUC (total concentration in blood plasma) by 20%, the time to reach the maximum concentration is extended by 3 hours. Bioavailability is approximately 50%. The systemic exposure of ropinirole when taking extended-release tablets at the same daily doses of the active substance corresponds to the systemic exposure of ropinirole in immediate-release tablets.
Plasma protein binding is 10-40%.
The volume of distribution (V d) is approximately 7 l / kg.
Ropinirole is extensively metabolized in the liver, predominantly with the participation of the CYP1A2 isoenzyme. As a result of biotransformation, N-depropyl is formed, which is the main metabolite. It has no activity and is further converted to carbamylglucuronide, carboxylic acid and N-depropyl hydroxymetabolites.
T 1/2 (half-life) from the systemic circulation is about 6 hours.
The duration of the systemic action of ropinirole increases in proportion to the dose increase.
The drug is excreted mainly through the kidneys in the form of metabolites.
There is a high degree of variability in pharmacokinetics and a linear character of ropinirole.
With mild and moderate renal impairment, the pharmacokinetic parameters of Syndranol do not change. With end-stage renal failure in patients with Parkinson's disease who are on hemodialysis, the clearance of ropinirole is reduced by approximately 30%, and its metabolites by 60 to 80%. The maximum daily dose in this category of patients is 18 mg.
No dose adjustment is required for patients 65 years of age or older.
Indications for use
The use of Syndranol is indicated for patients with Parkinson's disease in the following cases:
- monotherapy of an early stage of the disease in patients who need dopaminergic therapy, in order to delay the appointment of levodopa drugs;
- Combination therapy with levodopa drugs to reduce the daily dose of levodopa, as well as to increase its effectiveness, including control of fluctuations in the therapeutic effect of levodopa (the phenomenon of "on-off") and the effect of the end of the dose that occurs against the background of its long-term regular use.
Contraindications
Absolute:
- severe renal failure with creatinine clearance (CC) less than 30 ml / min in the absence of treatment with programmed hemodialysis;
- liver dysfunction;
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
- breast-feeding;
- age up to 18 years;
- hypersensitivity to drug components.
With caution, Syndranol should be prescribed for severe diseases of the cardiovascular system, severe cardiovascular failure.
With a history of psychotic disorders or during pregnancy, the use of Syndranol is indicated only in cases where the expected effect of therapy outweighs the potential risk.
Syndranol, instructions for use: method and dosage
Syndranol tablets are taken orally, swallowing whole (membrane damage violates the prolonged release of ropinirole), regardless of the meal, but always at the same time of day.
For treatment, it is recommended to use tablets in the dosage of Syndranol, which allows you to take the required dose of ropinirole using the minimum number of tablets.
The selection of the dose should be made taking into account the individual tolerance and effectiveness of the drug. If a patient develops drowsiness, the dose of ropinirole should be reduced at any stage of its selection. A temporary decrease in the dose of Syndranol is also shown with the development of other undesirable phenomena. If one or more doses are missed, it may be necessary to adjust the dose.
The prescribed dose of the drug is taken 1 time per day.
The recommended dosing regimen for Syndranol monotherapy: the initial dose is 2 mg for 7 days. Starting from the eighth day, the daily dose is increased to 4 mg (taking the drug at this dose can provide a therapeutic effect).
It should be borne in mind that treatment must be carried out in the minimum effective dose. If necessary, the dose of Syndranol is adjusted to 8 mg, increasing by 2 mg at intervals of at least 7 days. If the therapeutic effect against the background of taking Syndranol 8 mg per day is unstable or insufficiently pronounced, an increase in the daily dose by 2-4 mg can be continued with an interval of at least 14 days until the desired therapeutic effect is achieved.
The maximum daily dose is 24 mg at a time.
When using Syndranol in doses used for monotherapy against the background of combination therapy with levodopa drugs, a gradual decrease in the dose of levodopa (up to 30%) is possible, taking into account the clinical effect. Dyskinesia may develop in patients with progressive Parkinson's disease receiving levodopa during the selection of the dose of extended-release ropinirole. In this case, a decrease in the dose of levodopa is indicated.
If Sindranol is prescribed as replacement therapy for other dopamine receptor agonists, then the switch to ropinirole is made in strict accordance with the recommendations regarding the cancellation of the previous antiparkinsonian drug.
Cancellation of Syndranol therapy should be made by gradually reducing the daily dose for at least 7 days.
When switching from immediate-release tablets to extended-release tablets, therapy can be started immediately with a dose of ropinirole equivalent to the daily dose of ropinirole in immediate-release tablets.
Resume therapy after interruption (skipping one or more doses) should be repeated with dose selection.
It is advisable to select a dose of Syndranol in patients aged 75 and older more slowly. No dose adjustment is required in elderly patients.
With a mild or moderate degree of renal dysfunction (CC 30-50 ml / min), dose adjustment of Syndranol is not required.
For patients with end-stage renal disease who are on hemodialysis, the initial daily dose should be 2 mg. Further, it can be increased, taking into account the tolerability and effectiveness of the drug. The maximum daily dose of Syndranol for this category of patients is 18 mg. An additional dose of ropinirole is not required after hemodialysis.
If, with renal failure with CC less than 30 ml / min, the patient does not receive treatment with programmed hemodialysis, the use of Syndranol is contraindicated.
Side effects
The undesirable disorders described below are classified as follows: 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, the frequency is unknown - it is not possible to estimate the incidence of violations.
Monotherapy
Adverse reactions recorded during clinical trials:
- from the nervous system: very often - drowsiness; often - dizziness (including vertigo);
- from the side of the vessels: infrequently - orthostatic hypotension, hypotension;
- from the gastrointestinal tract: very often - nausea; often - dyspepsia, abdominal pain, vomiting, constipation;
- mental disorders: often - hallucinations;
- general disorders: often - peripheral edema (including edema of the legs).
Side effects established during post-registration observations:
- from the immune system: very rarely - urticaria, skin rash, pruritus, angioedema and other hypersensitivity reactions;
- mental disorders: infrequently - delirium, delirium, paranoia and other psychotic reactions (except for hallucinations); the frequency has not been established - aggression, increased libido, hypersexuality, impulsive drive syndrome (including pathological craving for purchases, gambling), compulsive overeating;
- from the nervous system: very often - fainting; very rarely - sudden falling asleep, severe drowsiness;
- from the side of the vessels: often - orthostatic hypotension, hypotension;
- from the gastrointestinal tract: often - abdominal pain, vomiting, heartburn;
- from the hepatobiliary system: the frequency has not been established - liver dysfunction (more often manifested by an increase in the activity of liver enzymes);
- general disorders: often - edema of the lower extremities.
Combination therapy
Adverse reactions recorded during clinical trials in combination therapy with levodopa drugs:
- on the part of the nervous system: very often - dyskinesia (during the titration of the ropinirole dose, the development of impaired coordination of movements is possible, to reduce the severity of dyskinesia, a decrease in the dose of levodopa is indicated); often - dizziness (including vertigo), drowsiness;
- from the side of the vessels: often - hypotension, orthostatic hypotension;
- from the gastrointestinal tract: often - constipation, nausea;
- mental disorders: often - confusion, hallucinations;
- general disorders: often - peripheral edema.
Side effects established during post-registration observations in combination therapy with levodopa drugs:
- from the immune system: very rarely - urticaria, skin rash, pruritus, angioedema and other hypersensitivity reactions;
- mental disorders: often - confusion; infrequently - delirium, delirium, paranoia and other psychotic reactions (except hallucinations); the frequency has not been established - aggression, increased libido, hypersexuality, impulsive drive syndrome (including pathological craving for purchases, gambling), compulsive overeating;
- from the nervous system: very often - drowsiness; very rarely - sudden falling asleep, severe drowsiness;
- from the side of the vessels: often - orthostatic hypotension, hypotension;
- from the gastrointestinal tract: very often - nausea; often - heartburn;
- from the hepatobiliary system: the frequency has not been established - liver dysfunction (more often manifested by an increase in the activity of liver enzymes).
Overdose
Symptoms: nausea, vomiting, dizziness, drowsiness.
Treatment: the appointment of neuroleptics, metoclopramide.
special instructions
For patients with psychotic disorders (including a history), the appointment of Syndranol is indicated only in cases where the expected clinical effect of therapy with a dopamine receptor agonist outweighs the potential risk.
Treatment of patients with severe cardiovascular insufficiency (including ischemic heart disease) should be accompanied by regular monitoring of blood pressure, especially at the initial stage of therapy.
Caution should be exercised with the simultaneous use of antihypertensive and antiarrhythmic drugs in connection with the possible risk of arterial hypotension, bradycardia and other arrhythmias.
When prescribing Syndranol, patients should be informed about such side effects of the drug as drowsiness and episodes of sudden falling asleep (including without previous drowsiness). The occurrence of these reactions requires consideration of the question of the abolition of ropinirole.
Caregivers need to carefully monitor the condition of patients for habit disorder and the development of compulsive behavior, impulsive drive syndrome. Desire disorders are usually reversible and can be controlled by reducing the dose or stopping the pill.
Drinking alcohol during treatment with ropinirole is contraindicated.
During Syndranol therapy, cases of paradoxical deterioration of the condition in patients with restless legs syndrome have been observed. They are characterized by an earlier onset, an increase in the intensity of manifestations, the progression of symptoms covering previously unaffected limbs, or the development of a ricochet syndrome in the early morning hours. The appearance of the listed symptoms indicates the need to revise the tactics of treatment, to clarify the dose of Syndranol, up to its possible cancellation.
In prolonged-release tablets, the duration of the release of ropinirole is 24 hours. It should be borne in mind that with the rapid passage of the drug through the gastrointestinal tract, the release of the drug may be incomplete.
Influence on the ability to drive vehicles and complex mechanisms
The use of Syndranol can cause the development of undesirable reactions that affect the speed of psychomotor reactions, including dizziness, vertigo, drowsiness and sudden falling asleep without any precursors, therefore, patients should refuse to drive vehicles and engage in other potentially hazardous activities if drowsiness occurs during the day. …
Application during pregnancy and lactation
The use of Syndranol is contraindicated during breastfeeding.
During gestation, the administration of the drug is possible only in cases where the expected clinical effect for the mother outweighs the potential risk of toxicity to the fetus.
Pediatric use
The appointment of Syndranol is contraindicated for the treatment of children and adolescents under the age of 18 years.
With impaired renal function
The use of Syndranol is contraindicated in severe renal failure (CC less than 30 ml / min) in the absence of programmed hemodialysis treatment.
With mild or moderate renal impairment (CC 30-50 ml / min), dose adjustment is not required.
For patients with end-stage renal disease who are on hemodialysis, the initial daily dose should be 2 mg. Further, it can be increased, taking into account the tolerability and effectiveness of the drug. The maximum daily dose of Syndranol for this category of patients is 18 mg. An additional dose of ropinirole is not required after hemodialysis.
For violations of liver function
The appointment of Syndranol is contraindicated in patients with impaired liver function.
Use in the elderly
No dose adjustment is required for patients 65 years of age or older. In patients aged 75 years and older, it is recommended to select the dose of Syndranol more slowly.
Drug interactions
- levodopa, domperidone: no pharmacokinetic interaction was observed, therefore dose adjustment is not required;
- antipsychotics and other centrally acting dopamine receptor antagonists (sulpiride, metoclopramide): a decrease in the effectiveness of ropinirole is possible, and therefore combined use should be avoided;
- estrogens (in high doses): there is an increase in the level of ropinirole in the blood plasma. If HRT (hormone replacement therapy) was carried out before starting treatment with ropinirole, no dose adjustment is required. It is necessary to adjust the dose of ropinirole in cases when the appointment / cancellation of HRT is performed while taking the drug;
- ciprofloxacin, enoxacin, fluvoxamine and other inhibitors of the isoenzyme CYP1A2: may cause a clinically significant increase in the C max and AUC of ropinirole, so a dose adjustment of the drug may be required;
- digoxin, theophylline: no interaction detected;
- nicotine: increases the activity of the CYP1A2 isoenzyme, therefore, cessation or initiation of tobacco smoking during treatment may require a dose adjustment of ropinirole.
Analogs
Analogues of Sindranol are: Mirapex, Piribedil, Mipexol, Parlodel, Bromocriptine, Pronoran, Bromergon, Requip Modutab, Azilekt, Nyupro, Oprimaea, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Sindranol
There are currently no reviews for Sindranol.
Price for Syndranol in pharmacies
The price of Syndranol for a package containing 28 tablets of prolonged release, film-coated, can be:
- dosage of 2 mg - 485-630 rubles;
- dosage 4 mg - from 867 rubles.
Sindranol: prices in online pharmacies
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Drug name Price Pharmacy |
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Syndranol 2 mg film-coated tablets of prolonged action 28 pcs. 477 r 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!
