1. NAME OF THE MEDICINAL PRODUCT

Ropinirole Tablets USP 0.25mg Taj Pharma
Ropinirole Tablets USP 0.5mg Taj Pharma
Ropinirole Tablets USP 1mg Taj Pharma
Ropinirole Tablets USP 2mg Taj Pharma
Ropinirole Tablets USP 3mg Taj Pharma
Ropinirole Tablets USP 4mg Taj Pharma
Ropinirole Tablets USP 5mg Taj Pharma

  1. QUALITATIVE AND QUANTITATIVE COMPOSITION

a) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole        0.25mg
Excipients                                q.s

b) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole         0.5mg
Excipients                                q.s

c) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole          1mg
Excipients                                 q.s

d) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole        2mg
Excipients                              q.s

e) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole       3mg
Excipients                             q.s

f) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole      4mg
Excipients                             q.s

g) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole      5mg
Excipients                            q.s

For the full list of excipients, see section 6.1.

  1. PHARMACEUTICAL FORM

Film-coated tablet.

  1. CLINICAL PARTICULARS

4.1 Therapeutic indications

Ropinirole is indicated for the symptomatic treatment of moderate to severe idiopathic Restless Legs Syndrome (see section 5.1).

4.2 Posology and method of administration

Oral use.

Adults

Individual dose titration against efficacy and tolerability is recommended. Ropinirole should be taken just before bedtime, however the dose can be taken up to 3 hours before retiring. Ropinirole may be taken with food, to improve gastrointestinal tolerance.

Treatment initiation (week 1)

The recommended initial dose is 0.25 mg once daily (administered as above) for 2 days. If this dose is well tolerated the dose should be increased to 0.5 mg once daily for the remainder of week 1.

Therapeutic regimen (week 2 onwards)

Following treatment initiation, the daily dose should be increased until optimal therapeutic response is achieved. The average dose in clinical trials, in patients with moderate to severe Restless Legs Syndrome, was 2 mg once a day.

The dose may be increased to 1 mg once a day at week 2. The dose may then be increased by 0.5 mg per week over the next two weeks to a dose of 2 mg once a day. In some patients, to achieve optimal improvement, the dose may be increased gradually up to a maximum of 4 mg once a day. In clinical trials the dose was increased by 0.5 mg each week to 3 mg once a day and then by 1 mg up to the maximum recommended dose of 4 mg once a day as shown in table 1.

Doses above 4 mg once daily have not been investigated in Restless Legs Syndrome patients.

Table 1 Dose titration

Week2345*6*7*
Dose (mg)/once daily11.522.534

* To achieve optimal improvement in some patients.

The efficacy of ropinirole treatment has not been shown beyond 12 weeks (see Section 5.1). Patient response should be evaluated after 12 weeks treatment and the need for treatment continuation reconsidered. If treatment is interrupted for more than a few days it should be re-initiated by dose titration as noted above.

When switching treatment from another dopamine agonist to ropinirole, the marketing authorisation holder’s guidance on discontinuation should be followed before initiating ropinirole.

As with other dopamine agonists, it is necessary to discontinue ropinirole treatment gradually by reducing the daily dose over the period of one week (see section 4.4).

Children and adolescents

Ropinirole is not recommended for use in children below 18 years of age due to a lack of data on safety and efficacy.

Elderly

The clearance of ropinirole is decreased by approximately 15% in patients aged 65 years or above. Although a dose adjustment is not required, ropinirole dose should be individually titrated, with careful monitoring of tolerability, to the optimal clinical response.

Renal impairment

No dosage adjustment is necessary in patients with mild to moderate renal impairment (creatinine clearance between 30 and 50 ml/min).

A study into the use of ropinirole in patients with end stage renal disease (patients on haemodialysis) has shown that a dose adjustment in these patients is required as follows: the recommended initial dose of Ropinirole is 0.25 mg once daily. Further dose escalations should be based on tolerability and efficacy. The recommended maximum dose of Ropinirole is 3 mg/day in patients receiving regular haemodialysis. Supplemental doses after haemodialysis are not required (see section 5.2).

The use of ropinirole in patients with severe renal impairment (creatinine clearance less than 30 ml/min) without regular haemodialysis has not been studied.

4.3 Contraindications

Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.

Severe renal impairment (creatinine clearance <30 ml/min) without regular haemodialysis.

Severe hepatic impairment.

4.4 Special warnings and precautions for use

Ropinirole should not be used to treat neuroleptic akathisia, tasikinesia (neuroleptic-induced compulsive tendency to walk), or secondary Restless Legs Syndrome (e.g. caused by renal failure, iron deficiency anaemia or pregnancy).

Paradoxical worsening of Restless Legs Syndrome symptoms described as augmentation (either earlier onset, increased intensity, or spread of symptoms to previously unaffected limbs), or early morning rebound (reoccurrence of symptoms in the early morning hours), have been observed during treatment with ropinirole. If this occurs, the adequacy of ropinirole treatment should be reviewed and dosage adjustment or discontinuation of treatment may be considered (see section 4.8).

In Parkinson’s disease, ropinirole has been associated uncommonly with somnolence and episodes of sudden sleep onset (see section 4.8) however, in Restless Legs Syndrome, this phenomenon is very rare. Nevertheless, patients must be informed of this phenomenon and advised to exercise caution while driving or operating machines during treatment with ropinirole. Patients who have experienced somnolence and/or an episode of sudden sleep onset must refrain from driving or operating machines. A reduction of dosage or termination of therapy may be considered.

Patients with major psychotic disorders should not be treated with dopamine agonists unless the potential benefits outweigh the risks.

Impulse control disorders

Patients should be regularly monitored for the development of impulse control disorders. Patients and carers should be made aware that behavioural symptoms of impulse control disorders including pathological gambling, increased libido, hypersexuality, compulsive spending or buying, binge eating and compulsive eating can occur in patients treated with dopamine agonists including Adartrel. Dose reduction/tapered discontinuation should be considered if such symptoms develop.

Neuroleptic malignant syndrome

Symptoms suggestive of neuroleptic malignant syndrome have been reported with abrupt withdrawal of dopaminergic therapy. Therefore it is recommended to taper treatment (see section 4.2).

Dopamine agonist withdrawal syndrome

Non-motor adverse effects may occur when tapering or discontinuing dopamine agonists including ropinirole. Symptoms include apathy, anxiety, depression, fatigue, sweating and pain which may be severe. Patients should be informed about this before tapering the dopamine agonist, and monitored regularly thereafter. In case of persistent symptoms, it may be necessary to increase the ropinirole dose temporarily (see section 4.8).

Hallucinations

Hallucinations are known as a side effect of treatment with dopamine agonists and levodopa. Patients should be informed that hallucinations can occur.

Ropinirole should be administered with caution to patients with moderate hepatic impairment. Undesirable effects should be closely monitored.

Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Due to the risk of hypotension, patients with severe cardiovascular disease (in particular coronary insufficiency) should be treated with caution.

4.5 Interaction with other medicinal products and other forms of interaction

Ropinirole is principally metabolised by the cytochrome P450 isoenzyme CYP1A2. A pharmacokinetic study (with a ropinirole dose of 2 mg, three times a day) revealed that ciprofloxacin increased the Cmax and AUC of ropinirole by 60% and 84% respectively, with a potential risk of adverse events. Hence, in patients already receiving ropinirole, the dose of ropinirole may need to be adjusted when medicinal products known to inhibit CYP1A2, e.g. ciprofloxacin, enoxacin or fluvoxamine, are introduced or withdrawn.

A pharmacokinetic interaction study between ropinirole (at a dose of 2 mg, three times a day) and theophylline, a substrate of CYP1A2, revealed no change in the pharmacokinetics of either ropinirole or theophylline. Therefore, it is not expected that ropinirole will compete with the metabolism of other medicinal products which are metabolised by CYP1A2.

Based on in-vitro data, ropinirole has little potential to inhibit cytochrome P450 at therapeutic doses. Hence, ropinirole is unlikely to affect the pharmacokinetics of other medicinal products, via a cytochrome P450 mechanism.

Smoking is known to induce CYP1A2 metabolism, therefore if patients stop or start smoking during treatment with ropinirole, dose adjustment maybe required.

Increased plasma concentrations of ropinirole have been observed in patients treated with hormone replacement therapy. In patients already receiving hormone replacement therapy, ropinirole treatment may be initiated in the usual manner. However, it may be necessary to adjust the ropinirole dose, in accordance with clinical response, if hormone replacement therapy is stopped or introduced during treatment with ropinirole.

No pharmacokinetic interaction has been seen between ropinirole and domperidone (a medicinal product used to treat nausea and vomiting) that would necessitate dosage adjustment of either medicinal product. Domperidone antagonises the dopaminergic actions of ropinirole peripherally and does not cross the blood-brain barrier. It may therefore have value as an anti-emetic in patients treated with centrally acting dopamine agonists.

Neuroleptics and other centrally active dopamine antagonists, such as sulpiride or metoclopramide, may diminish the effectiveness of ropinirole and, therefore, concomitant use of these medicinal products with ropinirole should be avoided.

In patients receiving the combination of vitamin K antagonists and ropinirole, cases of unbalanced INR have been reported. Increased clinical and biological surveillance (INR) is warranted.

4.6 Fertility, pregnancy and lactation

Pregnancy

There are no adequate data from the use of ropinirole in pregnant women. Ropinirole concentrations may gradually increase during pregnancy (see section 5.2).

Studies in animals have shown reproductive toxicity (see section 5.3). As the potential risk for humans is unknown, it is recommended that ropinirole is not used during pregnancy unless the potential benefit to the patient outweighs the potential risk to the foetus.

Breastfeeding

Ropinirole-related material was shown to transfer into the milk of lactating rats. It is unknown whether ropinirole and its metabolites are excreted in human milk. A risk to the suckling child cannot be excluded.

Ropinirole should not be used in nursing mothers as it may inhibit lactation.

Fertility

There are no data on the effects of ropinirole on human fertility. In female fertility studies in rats, effects were seen on implantation but no effects were seen on male fertility (see Section 5.3).

4.7 Effects on ability to drive and use machines

Patients being treated with ropinirole and presenting with hallucinations, somnolence and/or sudden sleep episodes must be informed to refrain from driving or engaging in activities where impaired alertness may put themselves or others at risk of serious injury or death (e.g. operating machines) until such effects have resolved (see section 4.4).

4.8 Undesirable effects

Adverse drug reactions are listed below by system organ class and frequency. Frequencies from clinical trials are determined as excess incidence over placebo and are classed as very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000); not known (cannot be estimated from the available data).

Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.

Use of ropinirole in Restless Legs Syndrome

In Restless Legs Syndrome clinical trials the most common adverse drug reaction was nausea (approximately 30% of patients). Undesirable effects were normally mild to moderate and experienced at the start of therapy or on increase of dose and few patients withdrew from the clinical studies due to undesirable effects.

Table 2 lists the adverse drug reactions reported for ropinirole in the 12-week clinical trials at ≥1.0% above the placebo rate or those reported uncommonly but known to be associated with ropinirole.

Table 2 Adverse drug reactions reported in 12-week Restless Legs Syndrome clinical trials (ropinirole n=309, placebo n=307)

Psychiatric disorders
CommonNervousness
UncommonConfusion
Nervous system disorders
CommonSyncope, somnolence, dizziness (including vertigo)
Vascular disorders
UncommonPostural hypotension, hypotension
Gastrointestinal disorders
Very commonVomiting, nausea
CommonAbdominal pain
General disorders and administration site conditions
CommonFatigue

Table 3 Adverse drug reactions reported in other Restless Legs Syndrome clinical trials

Psychiatric Disorders
UncommonHallucinations
Nervous system disorders
CommonAugmentation, Early morning rebound (see section 4.4)

Management of undesirable effects

Dose reduction should be considered if patients experience significant undesirable effects. If the undesirable effect abates, gradual up-titration can be re-instituted. Anti-nausea medicinal products that are not centrally active dopamine antagonists, such as domperidone, may be used, if required.

Other experience with ropinirole

Ropinirole is also indicated for the treatment of Parkinson’s disease. The adverse drug reactions reported in patients with Parkinson’s disease on ropinirole monotherapy and adjunct therapy at doses up to 24 mg/day at an excess incidence over placebo are described below.

Table 4 Adverse drug reactions reported in Parkinson’s disease clinical trials at doses up to 24 mg/day

Psychiatric disorders
CommonHallucinations, confusion
UncommonIncreased libido
Nervous system disorders
Very commonSyncope, dyskinesia, somnolence
Gastrointestinal disorders
Very commonNausea
CommonVomiting, abdominal pain, heartburn
General disorders and administration site conditions
CommonOedema peripheral (including leg oedema)

Post marketing reports

Hypersensitivity reactions (including urticaria, angioedema, rash, pruritus)

Psychotic reactions (other than hallucinations) including delirium, delusion and paranoia have been reported.

Aggression* (frequency not known)

*Aggression has been associated with psychotic reactions as well as compulsive symptoms.

Psychiatric disorders: Dopamine dysregulation syndrome (frequency not known).

Impulse control disorders (frequency not known)

Pathological gambling, increased libido, hypersexuality, compulsive spending or buying, binge eating and compulsive eating can occur in patients treated with dopamine agonists including Ropinirole. (see section 4.4. ‘Special warnings and precautions for use’).

Dopamine agonist withdrawal syndrome (frequency not known)

Including apathy, anxiety, depression, fatigue, sweating and pain. Non-motor adverse effects may occur when tapering or discontinuing dopamine agonists including ropinirole (see section 4.4).

In Parkinson’s disease, ropinirole is associated with somnolence and has been associated uncommonly (≥1/1,000 to <1/100) with excessive daytime somnolence and sudden sleep onset episodes, however, in Restless Legs Syndrome, this phenomenon is very rare (<1/10,000).

Following ropinirole therapy, postural hypotension or hypotension has been reported uncommonly (≥1/1,000 to <1/100), rarely severe.

Very rare cases of hepatic reactions (<1/10,000), mainly increase of liver enzymes, have been reported.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product.

4.9 Overdose

The symptoms of ropinirole overdose are related to its dopaminergic activity. These symptoms may be alleviated by appropriate treatment with dopamine antagonists such as neuroleptics or metoclopramide.

  1. PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: Dopamine agonist.

Mechanism of action

Ropinirole is a non ergoline D2/D3 dopamine agonist which stimulates striatal dopamine receptors.

Clinical efficacy

Ropinirole should only be prescribed to patients with moderate to severe idiopathic Restless Legs Syndrome. Moderate to severe idiopathic Restless Legs Syndrome is typically represented by patients who suffer with insomnia or severe discomfort in the limbs.

In the four 12-week efficacy studies, patients with Restless Legs Syndrome were randomised to ropinirole or placebo, and the effects on the IRLS scale scores at week 12 were compared to baseline. The mean dose of ropinirole for the moderate to severe patients was 2.0 mg/day. In a combined analysis of moderate to severe Restless Legs Syndrome patients from the four 12-week studies, the adjusted treatment difference for the change from baseline in IRLS scale total score at week 12 Last Observation Carried Forward (LOCF) Intention To Treat population was -4.0 points (95% CI -5.6, -2.4, p<0.0001; baseline and week 12 LOCF mean IRLS points: ropinirole 28.4 and 13.5; placebo 28.2 and 17.4).

A 12-week placebo-controlled polysomnography study in Restless Legs Syndrome patients examined the effect of treatment with ropinirole on periodic leg movements of sleep. A statistically significant difference in the periodic leg movements of sleep was seen between ropinirole and placebo from baseline to week 12.

A combined analysis of data from moderate to severe Restless Legs Syndrome patients, in the four 12-week placebo-controlled studies, indicated that ropinirole-treated patients reported significant improvements over placebo on the parameters of the Medical Outcome Study Sleep Scale (scores on 0-100 range except sleep quantity). The adjusted treatment differences between ropinirole and placebo were: sleep disturbance (-15.2, 95% CI -19.37, -10.94; p<0.0001), sleep quantity (0.7 hours, 95% CI 0.49, 0.94); p<0.0001), sleep adequacy (18.6, 95% CI 13.77, 23.45; p<0.0001) and daytime somnolence (-7.5, 95% CI -10.86, -4.23; p<0.0001).

Long term efficacy was evaluated in a randomised, double-blind, placebo-controlled clinical trial of 26 weeks. Overall results were difficult to interpret due to significant centre treatment interaction and the high proportion of missing data. No maintenance of efficacy at 26 weeks compared to placebo could be shown.

Study of the effect of ropinirole on cardiac repolarisation

A thorough QT study conducted in male and female healthy volunteers who received doses of 0.5, 1, 2 and 4 mg of ropinirole film-coated (immediate release) tablets once daily showed a maximum increase of the QT interval duration at the 1mg dose of 3.46 milliseconds (point estimate) as compared to placebo. The upper bound of the one sided 95% confidence interval for the largest mean effect was less than 7.5 milliseconds. The effect of ropinirole at higher doses has not been systematically evaluated.

The available clinical data from a thorough QT study do not indicate a risk of QT prolongation at doses of ropinirole up to 4 mg /day.

In clinical studies most patients were of Caucasian origin.

5.2 Pharmacokinetic properties

Absorption

The bioavailability of ropinirole is about 50% (36% to 57%), with Cmax reached on average 1.5 hours after the dose. A high fat meal decreases the rate of absorption of ropinirole, as shown by a delay in median Tmax by 2.6 hours and an average 25% decrease in Cmax

Distribution

Plasma protein binding of ropinirole is low (10 – 40%). Consistent with its high lipophilicity, ropinirole exhibits a large volume of distribution (approx. 7 l/kg).

Biotransformation

Ropinirole is primarily cleared by the cytochrome P450 enzyme, CYP1A2, and its metabolites are mainly excreted in the urine. The major metabolite is at least 100 times less potent than ropinirole in animal models of dopaminergic function.

Elimination

Ropinirole is cleared from the systemic circulation with an average elimination half-life of approximately 6 hours. No change in the oral clearance of ropinirole is observed following single and repeated oral administration. Wide inter-individual variability in the pharmacokinetic parameters has been observed.

Linearity/non-linearity

The pharmacokinetics of ropinirole are linear overall (Cmax and AUC) in the therapeutic range between 0.25 mg and 4 mg, after a single dose and after repeated dosing.

Population-related characteristics

Oral clearance of ropinirole is reduced by approximately 15% in elderly patients (65 years or above) compared to younger patients. Dosage adjustment is not necessary in the elderly.

Renal Impairment

In patients with mild to moderate renal impairment (creatinine clearance between 30 and 50 ml/min), no change in the pharmacokinetics of ropinirole is observed.

In patients with end stage renal disease receiving regular haemodialysis, oral clearance of ropinirole is reduced by approximately 30%. Oral clearance of the metabolites SKF-104557 and SKF-89124 were also reduced by approximately 80% and 60%, respectivelyTherefore, the recommended maximum dose is limited to 3 mg/day in these patients with RLS (see section 4.2).

Paediatric population

Limited pharmacokinetic data obtained in adolescents (12-17 years, n=9) showed that the systemic exposure following single doses of 0.125 mg and 0.25 mg was similar to that observed in adults (see also section 4.2; subparagraph “Children and adolescents”)

Pregnancy

Physiological changes in pregnancy (including decreased CYP1A2 activity) are predicted to gradually lead to an increased maternal systemic exposure of ropinirole (see also section 4.6).

5.3 Preclinical safety data

Toxicology

The toxicology profile is principally determined by the pharmacological activity of ropinirole: behavioural changes, hypoprolactinaemia, decrease in blood pressure and heart rate, ptosis and salivation. In the albino rat only, retinal degeneration was observed in a long term study at the highest dose (50 mg/kg/day), and was probably associated with an increased exposure to light.

Genotoxicity

Genotoxicity was not observed in the usual battery of in vitro and in vivo tests.

Carcinogenicity

From two-year studies conducted in the mouse and rat at dosages up to 50 mg/kg/day there was no evidence of any carcinogenic effect in the mouse. In the rat, the only ropinirole-related lesions were Leydig cell hyperplasia and testicular adenoma resulting from the hypoprolactinaemic effect of ropinirole. These lesions are considered to be a species specific phenomenon and do not constitute a hazard with regard to the clinical use of ropinirole.

Reproductive Toxicity

In fertility studies in female rats, effects were seen on implantation due to the prolactin-lowering effect of ropinirole. It should be noted that prolactin is not essential for implantation in humans.

Administration of ropinirole to pregnant rats at maternally toxic doses resulted in decreased foetal body weight at 60 mg/kg/day (mean AUC in rats approximately 15 times the highest AUC at the Maximum Recommended Human Dose (MRHD)), increased foetal death at 90 mg/kg/day (approximately 25 times the highest AUC at the MRHD) and digit malformations at 150 mg/kg/day (approximately 40 times the highest AUC at the MRHD). There were no teratogenic effects in the rat at 120 mg/kg/day (approximately 30 times the maximum AUC at the MRHD) and no indication of an effect during organogenesis in the rabbit when given alone at 20 mg/kg (60 times the mean human Cmax at the MRHD). However, ropinirole at 10 mg/kg (30 times the mean human Cmax at the MRHD) administered to rabbits in combination with oral L-dopa produced a higher incidence and severity of digit malformations than L-dopa alone.

Safety Pharmacology

In vitro studies have shown that ropinirole inhibits hERG-mediated currents. The IC50 is at least 30-fold higher than the expected maximum plasma concentration in patients treated at the highest recommended dose (4 mg/day) (see section 5.1).

  1. PHARMACEUTICAL PARTICULARS

6.1 List of excipients

Tablet cores: Lactose monohydrate, Microcrystalline cellulose, Croscarmellose sodium & Magnesium stearate.

Film coating: Hypromellose, Macrogol, Titanium dioxide, Polysorbate.

6.2 Incompatibilities

Not applicable.

6.3 Shelf life

3 years.

6.4 Special precautions for storage

Do not store above 25 °C.

Store in the original package.

For storage conditions after first opening of the medicinal product, see section 6.3.

6.5 Nature and contents of container

PVC/Aluminium Blister Pack.

Available in pack of: 7, 14, 28, 30, 50, 60, 90, 100, 200 & 500 tablets.

Not all pack sizes may be marketed.

6.6 Special precautions for disposal and other handling

No special requirements for disposal.

7.Manufactured in India by:
TAJ PHARMACEUTICALS LTD.
Mumbai, India
Unit No. 214.Old Bake House,
Maharashtra chambers of  Commerce Lane,
Fort, Mumbai – 400001
at:Gujarat, INDIA.
Customer Service and Product Inquiries:
1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
E-mail: tajgroup@tajpharma.com

Ropinirole Tablets USP 0.25mg/0.5mg/1mg/2mg/3mg/4mg/5mg Taj Pharma
(Ropinirole)

Package Leaflet: Information For The User

Read all of this leaflet carefully before you start taking this medicine because it contains important information for you.

  • Keep this leaflet. You may need to read it again.
  • If you have any further questions, ask your doctor or pharmacist.
  • This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
  • If you get any side effects talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet (see section 4).

What is in this leaflet:

  1. What Ropinirole is and what it is used for
  2. What you need to know before you take Ropinirole
  3. How to take Ropinirole
  4. Possible side effects
  5. How to store Ropinirole
  6. Contents of the pack and other information

 

  1. WHAT ROPINIROLE IS AND WHAT IT IS USED FOR

Ropinirole is used to treat Parkinson’s disease.

The active ingredient in Ropinirole 5 mg film-coated tablets is ropinirole, which belongs to a group of medicines called dopamine agonists. Dopamine agonists affect the brain in a similar way to a natural substance called dopamine.

People with Parkinson’s disease have low levels of dopamine in some parts of their brains. Ropinirole has effects similar to those of natural dopamine, so it helps to reduce the symptoms of Parkinson’s disease.

  1. WHAT YOU NEED TO KNOW BEFORE YOU TAKE ROPINIROLE

Do not take Ropinirole

  • if you are allergic to ropinirole, or any of the other ingredients of this medicine (listed in section 6).
  • if you have serious kidney disease
  • if you have serious liver disease.

Tell your doctor if you think any of these may apply to you.

Warnings and precautions

Tell your doctor or pharmacist before you start to taking Ropinirole if you:

  • are pregnant or think you may be pregnant
  • are breast-feeding
  • are under 18 years old
  • have liver disease
  • have a serious heart complaint.
  • have a serious mental health problem
  • if you have experienced any unusual urges and / or behaviors (such as excessive gambling or excessive sexual behaviors)
  • if you have an intolerance to some sugars (such as lactose)

Talk to your doctor if you think any of these may apply to you. If you and your doctor decide that you can take ropinirole, your doctor will probably ask you to have extra check-ups while you are taking it.

Tell your doctor if you experience symptoms such as depression, apathy, anxiety, fatigue, sweating or pain after stopping or reducing your Ropinirole treatment. If the problems persist more than a few weeks, your doctor may need to adjust your treatment.

Take special care with this medicine

Tell your doctor if you or your family/carer notices that you are developing urges or cravings to behave in ways that are unusual for you or you cannot resist the impulse, drive or temptation to carry out certain activities that could harm yourself or others. These are called impulse control disorders and can include behaviors such as addictive gambling, excessive eating or spending, an abnormally high sex drive or an increase in sexual thoughts or feelings. Your doctor may need to adjust or stop your dose.

Tell your doctor if you think any of these may apply to you. Your doctor may decide that Ropinirole isn’t suitable for you or that you need extra check-ups while you’re taking it.

Children

Do not give Ropinirole to children. Ropinirole is not normally prescribed for people under 18.

Other medicines and Ropinirole

Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines including any herbal remedies or other medicines you bought without a prescription.

Some medicines can affect the way Ropinirole works, or make it more likely that you will have side effects. Ropinirole can also affect how some other medicines work. These include:

  • the anti-depressant fluvoxamine
  • HRT (hormone replacement therapy)
  • the antibiotics ciprofloxacin or enoxacin
  • medication for other mental health problems, for example sulpiride
  • metoclopramide, which is used to treat nausea and heartburn
  • cimetidine, used in the treatment of stomach ulcers
  • any other medicine for Parkinson’s disease

Tell your doctor if you’re taking, or have recently taken any of these medicines.

Remember to tell your doctor if you start taking any other medicine while taking Ropinirole.

Ropinirole with food and drink

If you take this medicine with food, you may be less likely to feel sick or be sick (vomit). So it’s best to take it with food if you can.

Pregnancy and breast-feeding

If you are pregnant or breast-feeding, think you may be pregnant or planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine. Your doctor may advise you to stop taking Ropinirole.

Ropinirole is not recommended if you are pregnant, unless your doctor advises that the benefit to you taking Ropinirole is greater than the risk to your unborn baby.

Ropinirole is not recommended if you are breast feeding, as it can affect your milk production.

Driving and using machines

Ropinirole can make you feel drowsy. It can make people feel extremely sleepy and it sometimes makes people fall asleep very suddenly without warning.

If you could be affected: don’t drive, don’t operate machines and don’t put yourself in any situation where feeling sleepy or falling asleep could put you (or other people) at risk of serious injury or death. Don’t take part in these activities until you are no longer affected.

Talk to your doctor if this causes problems for you.

Ropinirole can cause hallucinations (seeing, hearing or feeling things that are not there). If affected do not drive or use machines.

Ropinirole contains lactose

This medicinal product contains lactose. If you have an intolerance to lactose or any other sugars, ask your doctor for advice before you take this medicine.

Smoking and Ropinirole

Tell your doctor or nurse if you start smoking, or give up smoking, while you’re taking Ropinirole. Your doctor or nurse may need to adjust your dose.

  1. HOW TO TAKE ROPINIROLE

Always take this medicine exactly as your doctor has told you or pharmacist has told you. Check with your doctor or pharmacist if you are not sure.

You may be given Ropinirole on its own to treat the symptoms of your Parkinson’s disease, or you may be given Ropinirole as well as another medicine called L-dopa (also called levodopa). If you are taking L-dopa you may experience some uncontrollable movements (dyskinesias) when you first start taking Ropinirole. Tell your doctor if this happens, as your doctor may need to adjust the dose of the medicines you are taking.

Tell your doctor if you or your family notices that you are developing any unusual behaviorss (such as an unusual urge to gamble or increased sexual urges and/or behaviorss) while you are taking Ropinirole. Your doctor may need to adjust or stop your dose.

How much Ropinirole will you need to take?

It may take a while to find out the best dose of Ropinirole for you.

The usual starting dose is 0.25 mg ropinirole three times each day for the first week. Then your doctor will increase your dose each week, for the next three weeks.

After that, your doctor will gradually increase the dose until you are taking the dose that is best for you. The usual is 1 mg to 3 mg three times each day (making a total daily dose of 3 mg to 9 mg). If your Parkinson’s disease symptoms have not improved enough, your doctor may decide to gradually increase your dose some more.

Some people take up to 8 mg of Ropinirole three times a day (24 mg daily altogether).

If you are also taking other medicines for Parkinson’s disease, your doctor may advise you to gradually reduce the dose of the other medicine.

Don’t take any more Ropinirole than your doctor has recommended. It may take a few weeks for Ropinirole to work for you.

Take Ropinirole 3 times a day.

Swallow the Ropinirole tablet(s) whole with a glass of water. It’s best to take Ropinirole with food, because that makes it less likely that you’ll feel sick (nauseous).

If you take more Ropinirole than you should

Contact a doctor or pharmacist immediately. If possible, show them the Ropinirole pack.

Someone who has taken an overdose of Ropinirole may have any of these symptoms: feeling sick (nausea) or being sick (vomiting), dizziness (a spinning sensation), feeling drowsy, mental or physical tiredness, fainting and hallucinations.

If you forget to take Ropinirole

Do not take a double dose to make up for a forgotten dose. Just take your next dose at the usual time.

If you have missed taking Ropinirole for more than a few days, ask your doctor for advice on how to start taking Ropinirole again.

If you stop taking Ropinirole

Do not stop taking Ropinirole suddenly without talking to your doctor.

A sudden stop could cause you to develop a medical condition called neuroleptic malignant syndrome which may represent a major health risk. The symptoms include: akinesia (loss of muscle movement), rigid muscles, fever, unstable blood pressure, tachycardia (increased heart rate), confusion, depressed level of consciousness (e.g. coma).

If you suddenly stop taking Ropinirole your Parkinson’s disease symptoms may quickly get much worse.

If you need to stop taking Ropinirole your doctor will reduce your dose gradually.

If you have any further questions on the use of this product , ask your doctor or pharmacist.

  1. POSSIBLE SIDE EFFECTS

Like all medicines, this medicine can cause side effects, although not everybody gets them.

The side effects of Ropinirole are more likely to happen when you first start taking it, or when your dose has just been increased. They are usually mild, and may become less troublesome after you have taken the dose for a while.

If you are worried about side effects, talk to your doctor.

Very common: may affect more than 1 in 10 people

  • fainting
  • feeling drowsy
  • feeling sick (nausea)

Common: may affect up to 1 in 10 people

  • hallucinations (sensing things that are not real)
  • being sick (vomiting)
  • feeling dizzy (a spinning sensation)
  • heartburn
  • stomach pain
  • swelling of the legs, feet or hands.

Uncommon: may affect up to 1 in 100 people

  • feeling dizzy or faint, especially when you stand up suddenly (this is caused by a drop in blood pressure)
  • feeling very sleepy during the day (extreme somnolence)
  • falling asleep very suddenly without feeling sleepy first (sudden sleep onset episodes)
  • mental problems such as delirium (severe confusion), delusions (unreasonable ideas) or paranoia (unreasonable suspicions)

You may experience the following side effects:

  • inability to resist the impulse, drive or temptation to perform an action that could be harmful to you or others, which may include:
    • strong impulse to gamble excessively despite serious personal or family consequences
  • altered or increased sexual interest and behaviors of significant concern to you or to others, for example, an increased sexual drive
  • uncontrollable excessive shopping or spending
  • binge eating (eating large amounts of food in a short time period) or compulsive eating (eating more food than normal and more than is needed to satisfy your hunger).

Tell your doctor if you experience any of these behaviorss; they will discuss ways of managing or reducing the symptoms.

Very rare side effects: may affect up to 1 in 10,000 people

  • changes in liver function, which have shown up in blood tests
  • allergic reactions such as red, itchy swellings on the skin (hives), swelling of the face, lips, mouth, tongue or throat which may cause difficulty in swallowing or breathing, rash or intense itching.

Some patients may have the following side effects (frequency not known; cannot be estimated from the available data):

  • aggression
  • excessive use of ropinirole (craving for large doses of dopaminergic drugs in excess of that required to control motor symptoms, known as dopamine dysregulation syndrome)
  • After stopping or reducing your Ropinirole treatment: Depression, apathy, anxiety, fatigue, sweating or pain may occur (called dopamine agonist withdrawal syndrome or DAWS).

People who are taking Ropinirole with L-dopa may develop other side effects over time:

  • uncontrollable movements (dyskinesias) are a very common side effect. Tell your doctor if this happens, as your doctor may need to adjust the doses of the medicines you are taking
  • feeling confused is a common side effect.

Reporting of side effects

If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet.

  1. HOW TO STORE ROPINIROLE

Keep this medicine out of the sight and reach of children.

Do not use this medicine after the expiry date which is stated on the blister/bottle and the outer carton after Exp. The expiry date refers to the last day of that month.

Do not store above 30°C.

Blisters:

Store in the original package in order to protect from moisture.

Bottles:

Keep the bottle tightly closed in order to protect from moisture.

Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. These measures will help to protect the environment.

  1. CONTENTS OF THE PACK AND OTHER INFORMATION

What Ropinirole contains

The active substance is ropinirole.

a) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole        0.25mg
Excipients                                q.s

b) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole         0.5mg
Excipients                                q.s

c) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole          1mg
Excipients                                 q.s

d) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole        2mg
Excipients                              q.s

e) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole       3mg
Excipients                             q.s

f) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole      4mg
Excipients                             q.s

g) Each film-coated tablet contains:
Ropinirole Hydrochloride
Equivalent to Ropinirole      5mg
Excipients                            q.s

The other ingredients are:

Tablet cores: Lactose monohydrate, Microcrystalline cellulose, Croscarmellose sodium & Magnesium stearate.

Film coating: Hypromellose, Macrogol, Titanium dioxide, Polysorbate.

What Ropinirole looks like and contents of the pack

PVC/Aluminium Blister Pack.

Available in pack of: 7, 14, 28, 30, 50, 60, 90, 100, 200 & 500 tablets.

Not all pack sizes may be marketed.

7.Manufactured in India by:
TAJ PHARMACEUTICALS LTD.
Mumbai, India
Unit No. 214.Old Bake House,
Maharashtra chambers of  Commerce Lane,
Fort, Mumbai – 400001
at:Gujarat, INDIA.
Customer Service and Product Inquiries:
1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
E-mail: tajgroup@tajpharma.com