Universal reference book for medicines
Product name: OPRIMEYA

Active substance: pramipexole

Type: antiparkinsonian drug - a stimulant of dopaminergic transmission in the central nervous system

Manufacturer: KRKA (Slovenia)
Composition, form of production and packaging
Tablets
1 tab.

pramipexole dihydrochloride monohydrate 1 mg

10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (3) - packs cardboard.
10 pieces.
- packings cellular planimetric (6) - packs cardboard.
10 pieces.
- packings cellular planimetric (9) - packs cardboard.
10 pieces.
- packings cellular planimetric (10) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Pramipexole, a dopamine receptor agonist, binds with dopamine receptors of the D2 subgroup with high selectivity and selectivity, of which it has the most pronounced affinity for D 3 receptors.
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 invitro 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 C max in blood plasma 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 V d (400 L).
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 output through the bowel. The total clearance of pramipexole is about 500 ml / min, the renal clearance is 400 ml / min. The half-life (T 1/2 ) ranges from 8 hours in young and up to 12 hours in the elderly.
INDICATIONS

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

DOSING MODE

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 at 0.375 mg per day.

To reduce the risk of side effects, the dose should be selected

gradually to achieve maximum therapeutic effect.

Scheme of increasing the dose of Oprimeia

Week Single dose (mg) Total daily dose (mg)

1 3 x 0.125 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 noted that when taking doses above 1.5 mg / day, the incidence of drowsiness increases.

Supportive therapy

Individual dose should be in the range from 0.375 mg to 4.5 mg per day.
Both at an early and late stage 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 the dose above 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 should be withdrawn gradually, at 0.75 mg per day until the drug is completely discontinued (see section "Special instructions").

Patients with renal insufficiency

The dose of pramipexole depends on the creatinine clearance (CC):

Initial therapy:

- Patients with QC greater than 50 ml / min: a decrease in daily medication is not required;

- patients with KK 20 - 50ml / min;
on 0.125 mg 2 times a day (0.25 mg per day);
- Patients with SC less than 20 ml / min: 0.125 mg 1 time per day.

If during the maintenance therapy the kidney function decreases, the daily dose of the drug is reduced by the same percentage, to which the QC decreases, ie,
if the QC
decreases 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 QC is in the range of 20-50 ml / min or taken once a day if the SC is less than 20 ml / million.
Patients with hepatic insufficiency

Patients with hepatic insufficiency do not 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 EFFECT

Classification of the incidence of adverse events (WHO):

very often> 1/10%;
often from> 1/100 to <1/10; infrequently from> 1/1000 to 1/100; rarely from> 1/10000 to <1/1000; very rarely from <1/10000; including individual messages.
From the central (CNS) and peripheral nervous systems: very often - dyskinesia, dizziness, drowsiness;
often - insomnia, hallucinations, headache, atypical dreams, anxiety; infrequently - paranoia, hyperkinesia, sudden falling asleep, confusion, fainting; very rarely - hypersexuality, pathological gambling.
From the side of the digestive system: very often - nausea;
often - constipation, vomiting.
From 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);

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

On the part of the respiratory system: infrequently - shortness of breath.

From the sense organs: a visual impairment (reduced visual acuity).

Allergic reactions: infrequently - itchy skin, skin rash.

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

- hypersensitivity to pramipexole or to one of the components of the drug;

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

- simultaneous reception with neuroleptics.

With caution: renal failure, arterial hypotension, psychotic disorders, visual impairment, severe diseases of the cardiovascular system.

PREGNANCY AND LACTATION

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

The use of the drug during pregnancy is possible only if the intended benefit for the mother exceeds the potential risk to the fetus.

The drug should not be used during breastfeeding.
If therapy is necessary, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER

Use this medication with caution in case of kidney failure.
In case of impaired renal function, it is recommended to reduce the dose in accordance with the recommendations (see section "Method of administration and dose").
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Patients with hepatic insufficiency do not need to change the dose of the drug


APPLICATION FOR CHILDREN

Contraindicated at the age of 18 years (efficacy and safety not studied).

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, dyskinesia 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 of falling asleep during everyday 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 other pills and sedatives or alcohol simultaneously with pramipexole.
During the treatment of Parkinson's disease dopamine receptor agonists, including pramipexole, there are cases of pathological excitement, increased libido and the development of hypersexuality.
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 is necessary to avoid the simultaneous use of neuroleptics and pramipexole (see the 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 monitor blood pressure, especially at the beginning of treatment.

Impact on the ability to manage motor transport and other technical devices

Oprimea's drug 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.
OVERDOSE

Presumptive symptoms inherent in 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.

A 0.9% solution of sodium chloride is also needed.
When there are signs of stimulation of the central nervous system, neuroleptics may be recommended.
The effectiveness of hemodialysis is not established.

DRUG 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.
When combining Oprimei 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 promipexol.

It is necessary to use with caution other sedatives or alcohol in combination with pramipexole, t.
additive effect is possible.
It should avoid simultaneous use of antipsychotics and pramipexole (possibly antagonistic action).

Dopamine receptor blockers (derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide) reduce the effectiveness of treatment.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life - 2 years.

Do not use the drug after the expiration date.

Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y
Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!