Sifrol 0.75mg Boehringer treatment for Parkinson's disease (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Pramipexole dihydrochloride monohydrate

Ingredient

Composition information	Content
Pramipexole dihydrochloride monohydrate	0.75mg

Uses

indicated

Sifrol ER is indicated in case of:

Treatment of signs and symptoms of innocent Parkinson's disease in adults: Use single therapy (not with levodopa) or combined with Levodopa, meaning it can be used during the treatment, until the late period when Levodopa has gradually lost the effect (Wear Off) or becomes unstable and appears oscillation in treatment effect (at the end of the dose or the "on off".

Pharmacokology

Pharmacological group: Dopamine homogeneous substance.

ATC code: N04BC05.

Pramipexole is a selective and highly specific dopamine dopamine with Dopamine D2 receptor group, which has priority affinity with D3 receptor; This active ingredient has a complete intrinsic activity.

Pramipexole reduces patients' movement defects in Parkinson's disease by stimulating dopamine receptors in the pattern. Animal studies have shown pramipexole inhibiting synthesis, release and metabolism of dopamine.

Dynamic pharmacokinetics

pramipexole are absorbed quickly and completely after drinking. Absolute bioavailability is greater than 90%.

Use 1 time/day Sifrol ER reduces the frequent oscillation of plasma pramipexole content for 24 hours compared to Sifrol released quickly 3 times/day.

Peak concentration in plasma is achieved after about 6 hours after using Sifrol ER 1 time/day. The equilibrium achieved at the latest after 5 days of continuous treatment.

Use with food generally does not affect the bioavailability of pramipexole.

Eating high -fat food increases the peak concentration (CMAX) about 24% after single dose and about 20% after multiple doses and slow time to achieve peak concentration in healthy volunteers about 2 hours. The area under the total curve (AUC) is not affected when used with food. Increasing CMAX is considered to have no clinical significance.

The body weight does not affect AUC, but the impact on the distribution is and thus affects the cmax peak concentration. Reducing body weight by about 30 kg, resulting in an increase in CMAX by about 45%. However, in phase III clinical studies in Parkinson patients, there is no clinical significance of weight on the effectiveness of treatment and the ability to tolerate Sifrol ER.

Pramipexole shows that the livel pharmacokinetics and plasma concentrations are less changing in patients. In humans, Pramipexole binds to protein at a very low rate (

On humans, pramipexole is only transformed at a small level.

Pramipexole is excreted mainly through the kidneys in non -metabolic form. About 90% of the drug is marked with 14C excreted through the kidneys, while less than 2% is found in the feces. The total clearance of Pramipexole is about 500 ml/minute and the renal clearance is about 400 ml/min. The sale time (t leave) changes from 8 hours in young people to 12 hours in the elderly.

Before taking Sifrol 0.75mg Boehringer treatment for Parkinson's disease (3 blisters x 10 tablets)

How to use

Sifrol ER is the oral dosage form of PramipExole used only a day of the day. Should drink whole tablet with water, do not chew, split or crushed. Can be used with or not with food and should be used daily at a certain time.

Dosage

Starting treatment

Starting dose: 0.375 mg/day, then increasing the dose gradually every 5-7 days. If the patient does not experience uncomfortable side effects, gradually adjust the dose until the maximum treatment is achieved.

Sifrol ER increasing schedule

Week 1: 0.375 mg (½ Sifrol ER 0.75).

week 2: 0.75 mg (1 sifrol ER 0.75).

Week 3: 1.50 mg (2 tablets of Sifrol ER 0.75).

If an additional dose is needed, every week should increase the daily dose by 0.75 mg to a maximum dose of 4.5 mg a day. However, it should be noted that the drowsiness rate will increase when the dose is higher than 1.5 mg/day.

Patients who have used Sifrol quickly release can switch to using Sifrol ER after only 1 night, with the same daily dosage. After switching to Sifrol ER, the dosage can be adjusted based on the patient's treatment response.

Maintain treatment

Dosage for each patient should be from 0.375 mg to a maximum of 4.5 mg per day. In the process of increasing the dose in key studies, the effectiveness is started at a dose of 1.5 mg. Additional dose adjustment should be based on clinical response and the appearance of adverse effects. In the treatment of Parkinson's disease, the dose is higher than 1.5 mg/day, which may be helpful for patients when planning to reduce the dose of Levodopa. Levodopa dose reduction is recommended in both cases of increasing dose or sifted seal ER maintenance depending on the reaction of each patient.

Stop treatment

Sudden stopping dopaminergic therapy can lead to malignant syndrome due to anti -psychotic drugs. Therefore, Pramipexole should be reduced slowly at 0.75 mg/day until the daily dose decreases to 0.375 mg/day.

Patients with renal failure

Pramipexole elimination depends on the kidney function. Sifrol ER dosage is suggested at the beginning of treatment:

Patients with Creatinin clearance> 50 ml/min: No need to reduce the dose or frequency of daily drugs.

Patients with creatinine clearance 30 - 50 ml/min: start at a dose of 0.375 mg/day. Be careful and carefully assess the treatment and tolerance level before increasing the daily dose after a week. If necessary, the dose should be increased by 0.375 mg per week to a maximum dose of 2.25 mg/day.

Patients with creatinine clearance

Patients with liver failure

No need to reduce the dose in patients with liver failure because about 90% of the active ingredient is absorbed will be excreted through the kidneys. However, the effect of liver failure on pharmacokinetics of Sifrol ER has not been studied.

Pediatric patients

Do not use Sifrol ER for indications for treatment of Parkinson's disease in children.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What to do when overdose? The disadvantaged events may be encountered are manifestations related to the pharmacological properties of dopamine, including nausea, vomiting, hyperactivity, hallucinations, agitation, and hypotension.

There is no antidote for dopamine overdose. If there are signs of central nerve stimulation, sedative can be used. Overdose management by general support measures such as gastric lavage, infusion, active carbon and ECG monitoring.

What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.

Side Effects

Common, ADR> 1/100

Mental: Abnormal dreams, expression of behavior of impulse control disorders and forced impulses, confusion, hallucinations, insomnia.

Neurological: Drowsiness, dysfunction, dizziness, headache. Eye: vision disorders including one -sided vision, blurred vision and vision loss. blood vessels: Hypotenem pressure. digestive: Nausea, vomiting, constipation.

Body and on -site: Fatigue, peripheral edema.

Uncommon, 1/1000

Infection: pneumonia.

Endocrinology: Animal hormones are inappropriate.

Mental: Invisible eating, excessive shopping, illusion, eating a lot, increasing libido, sexual desire, paranoia, pathological gambling, restless restlessness, delusion. Neurology: forget, increase dynamic, sudden falling, fainting. Heart: heart failure.

Chest, respiration and mediastinum: Difficulty breathing, hiccups.

Skin and subcutaneous tissue: increased sensitive, itchy, rash.

Rare, 1/10,000

Mental: Hung Cam.

Unknown frequency

Neurological: head and neck (Antollis).

Systemic and on -site: CLASS syndrome (Dopamine co -shipping syndrome).

Instructions on how to handle ADR

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Warnings

Contraindicated

sensitive to the active ingredient or any component of the product.

Be cautious when using

kidney failure

When prescribing Sifrol ER for Parkinson patients with renal failure, the dose should be reduced as instructions in the dosage and usage section.

Illusion

The illusion is the known side effect of Dopamine and Levodopa. Patients need to be notified that the illusion may occur (mostly virtual market).

movement disorders

In Parkinson patients with progression, when treatment combined with Levodopa, dynamic disorders may encounter when starting the standard Sifrol ER. If this happens, levodopa dose should be reduced.

muscle disorders

Parkinson patients may appear muscle disorders around the shaft such as bending heads and neck (Antullis), abnormal spinal bend when standing and walking (Camptocormia) or rare neurological disorders due to prolonged contact with anti -psychotic drugs (Pleurothototus) (PISA syndrome). Sometimes, the muscular disorder is noticed after starting treatment with dopamine agreed drugs including pramipexole, although there is no clear causal relationship. Muscle disorders can also occur several months after the beginning of treatment or adjustment of the drug. If the muscle hypertension occurs, it is necessary to reconsider and consider adjusting the dopaminergic medication regime.

Drowsy and drowsiness

Pramipexole is involved in drowsiness and sudden drowsiness, especially in Parkinson's patient. There is rarely falling off in daily activities that in some cases of unknown or no warning signs. Patients need to be notified and carefully advised when driving or operating machinery when treated with Sifrol ER. Patients who have manifested drowsiness or falling asleep need to limit driving or operating machinery or need to consider reducing the dose or may stop treatment.

Due to the combination effect, it is recommended that patients if they use sedatives or alcohol (alcohol) with pramipexole.

Pulse control disorders and coercive behaviors

Pathological gambling, increased sexual desire and sexual activity are also recorded in dopamine bronze treatment for Parkinson's patients, including Sifrol ER. Therefore, it is necessary to recommend that patients and caregivers know about the possibility of acts of impulse control disorders and coercive acts such as excessive eating and compulsive shopping. Should consider reducing the dose/stopped drugs slowly.

Halfy and delirium

Should check periodically to detect the impellance and delirium in the patient. Patients and caregivers should be noted that the impellance and delusion may occur in patients treated with Pramipexole. Can consider reducing the dose/stop slowly if these symptoms start.

Patients with mental disorders

Should only treat dopamine bronze drugs for patients with mental disorders if the benefits are higher than the risk.

It is not recommended to simultaneously use anti -psychotic drugs with pramipexole for example if the dopamine inhibitor effect is predictable.

Monitoring vision

It is necessary to check your vision periodically or when there is an abnormal vision.

Severe cardiovascular disease

Be careful in case of severe cardiovascular disease. Blood pressure monitoring should be monitored, especially when starting treatment, because of the general risk of hypotension posture related to dopaminergic therapy.

Malignant syndrome caused by psychotic drugs

The appearance of symptoms in malignant syndrome caused by psychotic drugs is also recorded when suddenly stopping dopaminergic therapy.

Cowdown syndrome

Certygia syndrome has been reported during or after stopping dopamine, including pramipexole. Risk factors may include high dopaminergic accumulation. The symptoms of quitting do not respond to Levodopa, and may include indifference, anxiety, depression, fatigue, sweating and pain. Before stopping the drug, it is advisable to notify the patient about the likelihood of cessation symptoms and need to closely monitor during and after the drug stopped. In the case of serious cessation symptoms, temporary reuse can be considered for the lowest doser at the lowest doses.

Traces in feces

Some patients have reported a trace of Sifrol ER in the feces. If the patient has such an observation report, the medical staff should re -evaluate the patient's response to the treatment.

The ability to drive and operate machinery

Sifrol ER has a great impact on the ability to drive and operate machinery.

illusion or drowsiness may occur.

Patients using Sifrol ER have drowsiness and/or sudden fall asleep should be warned to stop driving or participate in activities that if lacking alertness can cause serious injury or death for themselves or others (for example, when operating machinery) until resolving drowsiness and sudden sleep.

Pregnancy

influence on pregnant and lactating women has not been studied in humans. Sifrol ER should not be used during pregnancy unless it is necessary, which is only treatment if the benefits are higher than the risk for the fetus.

The period of breastfeeding

Because Pramipexole inhibits prolactin secretion on humans, can inhibit milk secretion. Pramipexole in breast milk has not been studied. Therefore, Sifrol ER should not be used during breastfeeding. However, if it is necessary to use the drug during this time, stop breastfeeding.

Interactive drug

cohesion with plasma proteins

Pramipexole is associated with plasma proteins with very low rate (

Although interacting with anti -cholinergic drugs have not been studied, because cholinergic drugs have been eliminated due to biological changes, the ability to interact is very low. There is no pharmacokinetic interaction with Selegiline and Levodopa.

Inhibition/competition of active excretion lines through the kidneys

Cimetidine reduces the renal disposal of pramipexole by about 34%, perhaps due to inhibition of the transportation system of the cations (positive ions) in the renal tubules. Therefore, inhibitors or reducing the active excretion through the kidneys such as cimetidine, amantadine and mexiletine, can interact with pramipexole, result in reducing one or both medication clearance. It is necessary to consider reducing the dose of pramipexole when these drugs are used with Sifrol ER.

Simultaneously used with levodopa

When using Sifrol ER along with Levodopa, Levodopa is required, keeping the dose of other Parkinson's medications while increasing the sifrol er.

Due to the possibility of a combination effect, careful recommendations for patients when using pramipexole simultaneously with other sedatives or alcohol.

Anti -psychotic drugs

It is not recommended to simultaneously use psychotic drugs with pramipexole, for example if the effects of antagonistic effects may occur.

Storage

Store under 30 ° C.

Store in the packaging to avoid light.

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