Mirapex PD, 3 mg 30 pcs

Mirapex PD is an antiparkinsonian drug – dopamine receptor agonist. With high selectivity and specificity it binds to dopamine receptors of subgroup D2, of which it has the most pronounced affinity for D3 receptors.

It reduces motor deficits in Parkinson’s disease by stimulating dopamine receptors in the striatum. Pramipexole inhibits the synthesis, release and metabolism of dopamine. In vitro, pramipexole protects dopamine neurons from degeneration occurring in response to ischemia or methamphetamine neurotoxicity.

Pramipexole in vitro protects neurons from levodopa neurotoxicity.

Decreases prolactin secretion (dose-dependent).

In clinical studies in healthy volunteers in whom the dose of Mirapex PD was increased faster than necessary (every 3 days) up to 4.5 mg/day, an increase in BP and HR was observed. This effect was not observed in patient studies.

Pharmacokinetics

Intake and distribution

Pramipexole is quickly and completely absorbed after oral administration. Absolute bioavailability is greater than 90% and Cmax in plasma is reached after approximately 6 h. As a rule, food intake does not affect the bioavailability of pramipexole.

A slight increase, approximately 20%, in Cmax and a delay, approximately 2 h, in time to reach Cmax after a fatty meal are not clinically significant.

Pramipexole exhibits linear kinetics and relatively little variability in plasma levels between patients, regardless of pharmaceutical form. Pramipexole binds very little to plasma proteins.

Metabolism and excretion

It is metabolized to a negligible degree.

About 90% of the dose is excreted through the kidneys (80% unchanged) and less than 2% is found in the feces. Total clearance of pramipexole is about 500 ml/min, renal clearance is about 400 ml/min. T1/2 fluctuates from 8 h in young adults to 12 h in the elderly.

Indications

Parkinson’s disease.

Active ingredient

Composition

Active ingredient:

pramipexole dihydrochloride monohydrate 3 mg;

Excipients:

Hypromellose 2208,

Corn starch,

carbomer 941,

colloidal silicon dioxide,

magnesium stearate.

How to take, the dosage

Long-acting tablets should be taken once a day, at approximately the same time of day. The tablets should be swallowed whole with water and should not be chewed, crushed or crushed. The tablets may be taken with or without food.

If the time of the next dose has been missed, the daily dose should be taken if no more than 12 hours have passed since the usual time of taking the medicine. If more than 12 hours have passed, you should not take the medication; the next dose should be taken the next day at the usual time.

Patients who are already taking Mirapex tablets may be switched to taking Mirapex PD long-acting tablets overnight, at the same dose.

Interaction

Pramipexole to a small degree

Drugs that inhibit active renal tubular secretion of cationic drugs (e.g., cimetidine), or that are themselves excreted by active renal tubular secretion, may interact with pramipexole, which is reflected in decreased clearance of one or both drugs.

If such drugs (including amantadine) and pramipexole are used concomitantly, watch out for signs of excessive dopamine stimulation such as dyskinesia, agitation or hallucinations. In such cases, the dose should be reduced.

Selegyline and levodopa do not affect the pharmacokinetics of pramipexole. Pramipexole does not affect the overall absorption or elimination of levodopa. Interaction with anticholinergic drugs and amantadine has not been studied.

However, interaction with amantadine is possible because the drugs have a similar excretion mechanism. Anticholinergic drugs are mostly excreted metabolically, so interactions with pramipexole are unlikely.

Lower doses of levodopa are recommended when increasing the dose in patients with Parkinson’s, and the dose of other antiparkinsonian medications must be maintained at a constant level.

Because of possible cumulative effects, patients should be advised to exercise caution when taking other sedative medications or alcohol in combination with Mirapex PD, as well as when taking concomitant medications that increase plasma concentrations of pramipexole (e.g., cimetidine).

Special Instructions

Since treatment with pramipexole, episodes of sudden falling asleep while awake during the day have been reported. Sleepiness usually develops when using Mirapex in doses greater than 1.5 mg/day. Episodes of falling asleep suddenly during daytime wakefulness occur against a background of already developed somnolence.

The factors increasing the risk of drowsiness include: concomitant use of sedatives, sleep disorders, concomitant use of drugs that increase plasma levels of pramipexole (e.g., cimetidine). Before prescribing Mirapex, the physician should determine the presence of these risk factors. During therapy, the patient’s condition should be monitored to detect a tendency to drowsiness.

In case of pronounced somnolence during daytime or episodes of sudden falling asleep during daytime wakefulness that require active intervention, Mirapex should be discontinued. If continuation of therapy is necessary, the drug dose should be reduced and the patient should be advised to refrain from driving and other potentially dangerous activities.

The incidence of arterial hypotension has generally not increased with therapy with Mirapex compared to placebo.
Patients of advanced age (65 years and older) require dose adjustment of Mirapex.

Because pramipexole is excreted by the kidneys, patients with kidney disease may need to adjust the dose of the drug.

Impact on driving and operating machinery

The patient should refrain from driving and other potentially hazardous activities until the effect of the drug on the ability to concentrate and the speed of psychomotor reactions has been determined.

Paediatric use

The safety and effectiveness of Mirapex in children has not been established.

Contraindications

Hypersensitivity

Side effects

Nervous system and sensory organs: Asthenia, somnolence/insomnia, hallucinations, delusions, amnesia, confusion, dizziness, anxiety, depression, dysphagia, dystonia, akathisia, thought disorders, suicidal tendencies, extrapyramidal syndrome, dyskinesia, tremor, hyposthesia, hypokinesia, myoclonus, ataxia, movement coordination disorders, diplopia, accommodation paralysis, conjunctivitis, impaired hearing; in isolated cases (with rapid dose reduction or abrupt withdrawal) – malignant neuroleptic syndrome (hyperthermia, muscle rigidity, impaired consciousness, autonomic lability).

Cardiovascular system and blood (hematopoiesis, hemostasis): orthostatic hypotension, tachycardia, arrhythmia.

Respiratory system: shortness of breath, rhinitis, pharyngitis, sinusitis, flu-like syndrome, increased coughing.

Gastrointestinal system disorders: nausea, vomiting, dyspepsia, flatulence, diarrhea, dry mouth, anorexia, constipation.

Motor system disorders: muscle hypertonicity, leg muscle cramps, muscle twitching, myasthenia gravis, arthritis, bursitis.

Others: fever; peripheral edema, sweating, increased intraocular pressure, decreased libido, impotence, weight loss; increased frequency of urination, urinary tract infections; pain syndrome, including chest pain.including chest pain, abdominal pain, lumbosacral pain, neck pain; voice changes; increased CPK activity; allergic reactions.

Overdose

Symptoms: not established. There is no clinical experience with a significant overdose of Mirapex. One patient with a 10-year history of schizophrenia took 11 mg/d of pramipexole for 2 days; this is 2-3 times the daily dose recommended by the protocol.

There were no adverse effects associated with the increased dose. BP remained stable, although HR increased to 100-120 bpm.
Treatment: The antidote for pramipexole is unknown.

Phenothiazine or butyrophenone derivatives neuroleptics may be used if symptoms of CNS stimulation occur, but the effectiveness of these drugs in reversing the effects of Mirapex overdose has not been evaluated.

The treatment of overdose may require supportive therapy, gastric lavage, use of means for rehydration and detoxification of the body, ECG monitoring.

Pregnancy use

Possible if the expected effect of therapy exceeds the potential risk to the fetus (no adequate and well-controlled studies on use in pregnancy have been conducted).

The FDA fetal category is C.

Breastfeeding should be discontinued during treatment (no data on penetration into human milk).

Similarities