Omitting (Oprimea)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
Read on
Similar drugsTo uncover
Dosage form: & nbsppills
Composition:

1 tablet contains:

Active substance:

Pramipexole dihydrochloride monohydrate:

0.125 mg

0.25 mg

1.00 mg

which corresponds to pramipexole

0.088 mg

0.18 mg

0.7 mg

Excipients: mannitol, corn starch, pregelatinized starch, povidone K25, silicon dioxide colloid, anhydrous, magnesium stearate.

Description:

Tablets 0.088 mg: round tablets of white color with a facet and with engraving "P6" on one side.

Tablets 0.18 mg: Oval white tablets with bevel, with a risk on both sides, with engraving "P7" on both halves of one side of the tablet.

Tablets 0,7 mg: round tablets of white color with a bevel, with a risk on both sides, with engraving "P9" on both halves of one side of the tablet.

Pharmacotherapeutic group:dopamine receptor agonist
Pharmacodynamics:

Pramipexole, a dopamine receptor agonist, with high selectivity and specificity binds to subgroup dopamine receptors D2, of which the most pronounced affinity for D3receptors. Reduces the lack of motor activity in Parkinson's disease by stimulating dopamine receptors in the striatum. Pramipexole inhibits the synthesis, release and metabolism of dopamine. Pramipexole in vitro protects dopaminergic neurons from the neurotoxicity of levodopa.

Reduces the secretion of prolactin (dose-dependent).

Pharmacokinetics:

Pramipexole is rapidly and completely absorbed after ingestion. Absolute bioavailability is more than 90%, and the maximum concentration in the blood plasma (CmOh) is achieved in 1-3 hours.

The rate of absorption decreases with food intake, but the total intake is not affected by food intake. Pramipexole is characterized by linear kinetics and a relatively small variability in the concentrations between individual patients.

Pramipexole binds to plasma proteins to a very small extent (less than 20%) and has a large volume of distribution (400 liters). It is exposed to a metabolism to an insignificant degree. About 90% of the dose is excreted through the kidneys (80% unchanged) and less than 2% is excreted through the intestine. The total clearance of pramipexole is about 500 ml / min, the renal clearance is 400 ml / min. The half-life (T1/2) ranges from 8 h in young and up to 12 h in the elderly.

Indications:

Symptomatic treatment of idiopathic Parkinson's disease (monotherapy or in combination with levodopa) at a late stage of the disease, when the effects of levodopa are weakened or become unstable.

Contraindications:

- Hypersensitivity to pramipexole or to one of the components

preparation;

- age under 18 years (effectiveness and safety not studied);

- simultaneous reception with neuroleptics.

Carefully:

Renal failure, arterial hypotension,

psychotic disorders, visual impairment, severe cardiovascular diseases.

Pregnancy and lactation:

The effect of the drug on pregnancy and lactation in humans has not been investigated.

Oprimea should not be used during pregnancy, except in cases of extreme necessity, if the potential benefit to the mother significantly exceeds the potential risk to the fetus.

The drug should not be used during breastfeeding. If therapy is necessary, breastfeeding should be discontinued.

Dosing and Administration:

Inside, regardless of food intake, with a small amount of water. The daily dose should be divided into 3 divided doses.

Initial therapy

The dose of the drug should be increased gradually, every 5-7 days, starting with 0.375 mg per day. To reduce the risk of side effects, the dose should be selected gradually until the maximum therapeutic effect is achieved.

Scheme of increasing the dose of Oprimeia

A week

Single dose (mg)

Total daily dose (mg)

1

3x0,125

0,375

2

3 x 0.25

0,75

3

3 x 0.5

1,5

If you need to further increase the daily dose, add 0.75 mg per week to a maximum dose of 4.5 mg per day.

It should be borne in mind that when taking doses over 1.5 mg / day, the incidence of drowsiness increases.

Supportive therapy

The individual dose should be in the range of 0.375 mg to 4.5 mg per day. Both at the early and late stages of the disease the drug is effective, starting with a daily dose of 1.5 mg. Further dose changes should depend on the patient's response to treatment and on the development of unwanted effects. It is not excluded that in some patients, a dose of more than 1.5 mg per day can provide an additional therapeutic effect, especially at a late stage of the disease, when a reduction in the dose of levodopa is indicated.

Discontinuation of therapy

A sudden cessation of therapy with dopamine receptor agonists can lead to the development of a malignant neuroleptic syndrome.

Pramipexole must be withdrawn gradually, at 0.75 mg per day, until the drug is completely discontinued (see section "Special instructions").

Patients with renal insufficiency

Dose pramipexole but depends on the clearance of creatinine (CC):

Initial therapy:

- patients with QC greater than 50 ml / min: a decrease in the daily dose of the drug is not required;

- patients with KK 20 - 50 ml / min: 0,125 mg twice a day (0.25 mg per day);

- Patients with SC less than 20 ml / min: 0.125 mg once a day.

If during maintenance therapy the function of the kidneys is reduced, then the daily dose of the drug is reduced by the same percentage, to which the QC is reduced, i.e. If the QC is reduced by 30%, then the daily dose of the drug should be reduced by 30%. The daily dose can be divided into two doses if the SC is in the range of 20-50 ml / min, or taken once a day, if the SC is less than 20 ml / min.

Patients with hepatic insufficiency

In patients with hepatic insufficiency, there is no need to change the dose of the drug.

Patients receiving concurrent therapy with levodopa

At simultaneous therapy with levodopa, it is recommended to reduce the dose of levodopa as the dose increases, and during maintenance therapy with pramipexole. This is necessary to avoid excessive dopamine stimulation.

Side effects:

Classification of the incidence of adverse events (WHO): Often (≥ 1/10); often (≥ 1/100, <1/10); infrequently (≥ 1 / 1,000, <1/100); rarely (≥ 1 / 10,000, <1 / 1,000); very rarely (<1 / 10,000), VCindividual messages.

From the central (CNS) and peripheral nervous system: very often - dyskinesia, dizziness, drowsiness; often - insomnia, gullycognition, headache, atypical dreams, anxiety; infrequently - paranoia, hyperkinesia, sudden falling asleep, confusion, fainting; very rarely hypersexuality, pathological gambling.

From the digestive system: very often - nausea; often - constipation, vomiting.

From the side of the cardiovascular system: very often - a decrease in blood pressure (at the beginning of therapy, if the dose of the drug is increased too quickly).

From the genitourinary system: infrequently - violations of libido (increase (0.1%) or decrease (0.4%)).

From the respiratory system: infrequently - shortness of breath.

From the sense organs: visual impairment (visual acuity reduction).

Allergic reactions: infrequently - itchy skin, skin rash.

Other: often - general weakness, peripheral edema, weight loss; infrequently - weight gain; very rarely - increased appetite.

Overdose:

Presumptive symptoms, characteristic of the pharmacodynamic profile of dopamine receptor agonists: nausea, vomiting, hyperkinesia, hallucinations, agitation, lowering blood pressure.

Treatment: there is no specific antidote; symptomatic therapy: gastric lavage, activated charcoal and ECG monitoring are recommended. Also, an intravenous injection of 0.9% sodium chloride solution is necessary. When there are signs of stimulation of the central nervous system, neuroleptics may be recommended. The effectiveness of hemodialysis is not established.

Interaction:

Pramipexole to a minor extent (less than 20%) binds to plasma proteins and undergoes biotransformation. Therefore, interaction with other drugs that affect the binding to plasma proteins or excretion due to biotransformation is unlikely.

Selegiline and levodopa do not affect the pharmacokinetics of pramipexole.

Cimetidine reduces the renal clearance of pramipexole by approximately 34%, mainly due to the inhibition of the cationic secretory transport system of the renal tubules. Drugs that inhibit this mechanism of excretion through the renal tubules (for example, cimetidine and amantadine), or which are themselves excreted in this way, can interact with pramipexole, which is manifested in a decrease in the clearance of one or both drugs.In case of simultaneous use of such drugs, it is necessary to reduce the dose of pramipexole.

With combsandMr.the drug Oprimeja with levodopa it is recommended to reduce the dose of levodopa, and the dose of other antiparkinsonian drugs should be maintained at a constant level with an increase in the dose of pramipexole.

It is necessary to use with caution other sedative drugs or alcohol in combination with pramipexole, t. additive effect is possible.

It should avoid simultaneous use of antipsychotics and pramipexole (possibly antagonistic action).

Blockers of dopamine receptors (derivatives of phenothiazine, butyrophenone, thioxanthene; metoclopramide) reduce the effectiveness of treatment.

Special instructions:

When prescribing the drug Oprimeja patients with Parkinson's disease and renal dysfunction is recommended to reduce the dose in accordance with the recommendations (see section "Method of administration and dose").

Patients should be warned about the possibility of developing hallucinations.

When using Oprimea in combination with levodopa, in the late stages of Parkinson's disease, at the initial stage of dose selection, dyskinesias can develop.When dyskinesias appear, it is necessary to reduce the dose of levodopa.

Against the background of the use of pramipexole, there were cases of sudden falling asleep, in particular in patients with Parkinson's disease. Cases falling asleep during daily activities, sometimes without any previous signs, were noted infrequently. Because of the possibility of developing an additive effect, it is necessary to take with caution simultaneously with pramipexole other sedatives or alcohol

During the treatment of Parkinson's disease, dopamine receptor agonists, including pramipexole, cases of pathological excitement, increased libido and the development of hypersexuality were noted. Patients and caregivers should be informed of possible changes in behavior. In such cases, the question of reducing the dose of the drug or its withdrawal should be decided.

Patients with psychotic disorders can receive therapy with dopamine receptor agonists after a preliminary benefit / risk assessment.

It should avoid simultaneous use of antipsychotics and pramipexole (see section "Interaction with other drugs").

When developing visual disorders, it is recommended that an ophthalmic examination be performed on a regular basis.

In connection with the risk of developing orthostatic hypotension, it is recommended to control blood pressure, especially at the beginning of treatment.

Effect on the ability to drive transp. cf. and fur:

Oprimea's preparation can have a significant impact on the ability to drive or work with technical devices. In connection with the possibility of developing drowsiness and hallucinations, in order to avoid episodes of falling asleep, patients taking the drug should refuse for the period of treatment from driving and working with technical devices related to the concentration of attention and the speed of psychomotor reactions.

Form release / dosage:Tablets, 0.088 mg, 0.18 mg, 0.7 mg.
Packaging:

10 tablets per blister.

By 2, 3, 6, 9 or 10 blisters are placed in a pack of cardboard along with instructions for use.

Storage conditions:

At a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

2 of the year.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription
Registration number:LSR-007999/10
Date of registration:12.08.2010
The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
Manufacturer: & nbsp
KRKA, d.d. Slovenia
Representation: & nbspKRKA KRKA Slovenia
Information update date: & nbsp27.08.2015
Illustrated instructions
    Instructions
    Up