Pramipexole-Teva, pills 1mg, 30pcs

Composition

Active ingredient:

pramipexole dihydrochloride monohydrate 1 mg;

Auxiliary substances:

mannitol;

MCC;

sodium carboxymethyl starch;

povidone K 25;

colloidal silicon dioxide;

magnesium stearate;

sodium stearyl fumarate

Pharmacological action

Pramipexole-Teva – dopaminergic, antiparkinsonian.

Pharmacodynamics

Pramipexole is a dopamine receptor agonist, binds to dopamine D2 receptors with high selectivity and specificity, and has a pronounced affinityfor dopamine D3 receptors.

Reduces motor deficits in Parkinson’s disease by stimulating dopamine receptors in the striatum.

Pramipexole inhibits the synthesis, release and metabolism of dopamine, and protects dopaminergic neurons from degeneration that occurs in response to ischemia or methamphetamine neurotoxicity.

In clinical studies, the effectiveness of pramipexole therapy in the late stages of Parkinson’s disease was shown, in which there was a significant decrease in the number of motor disorders and a significantly later development of complications compared to levodopa monotherapy.

Pharmacokinetics

Suction. Pramipexole is rapidly and completely absorbed after oral use, reaching _Cmax in plasma after approximately 1-3 h. The absolute bioavailability of pramipexole exceeds 90%. The rate of absorption decreases with food intake, but the total volume of absorption is not affected by food intake. Pramipexole is characterized by linear kinetics and relatively small variability in concentrations between individual patients.

Distribution. V_d is 400 liters. Binding to plasma proteins is less than 20%.

Metabolism and elimination. Slightly metabolized in the body. About 90% of the dose is excreted by the kidneys (80% – unchanged) and less than 2% – in the faeces. The total clearance of pramipexole is about 500 ml / min, the renal clearance is about 400 ml/min.

The final T_1/2 value is 8 hours in young healthy volunteers and about 12 hours in the elderly.

Indications

Symptomatic treatment of Parkinson’s disease as monotherapy or in combination with levodopa preparations in the late stage of the disease, when the effects of levodopa are weakened or become unstable and fluctuations in the therapeutic effect occur (on-off).

Contraindications

• hypersensitivity to pramipexole or any of the components of the drug;
• breast-feeding period;
• age up to 18 years.

With caution:  renal failure; arterial hypotension; cardiovascular diseases; concomitant use with dopamine receptor agonists, sedatives, cimetidine, amantadine, ethanol; pregnancy.

Side effects

Nervous system disorders:  often — confusion, insomnia, dizziness, impaired consciousness, depression, anxiety; infrequently-extrapyramidal syndrome, amnesia, hypesthesia, dystonia, myoclonus, tremor, ataxia, hypokinesia, delirium, suicidal mood; rarely-neuroleptic malignant syndrome (hyperthermia, muscle rigidity, akathisia, vegetative lability, thinking disorders).

Musculoskeletal disorders:  rarely — muscle hypertonia, leg muscle cramps, muscle twitching, arthritis, bursitis, myasthenia gravis, pain in the lumbosacral spine, chest pain, neck pain.

From the digestive system:  often — decreased appetite, dysphagia, dyspepsia, abdominal pain, flatulence, diarrhea, dry mouth, vomiting.

Respiratory system disorders:  infrequently-pharyngitis, sinusitis, rhinitis, shortness of breath, increased cough, voice changes; very rarely — flu-like syndrome, pulmonary infiltration, pleural effusion.

From the genitourinary system:  rarely — urinary tract infection, increased urination.

From the CCC side:  often-orthostatic hypotension; infrequently-tachycardia, increased CPK activity, angina pectoris, arrhythmias. In some patients, a decrease in blood pressure may occur at the beginning of treatment, especially if the dose of the drug is increased too quickly.

From the side of the senses:  often — conjunctivitis, paralysis of accommodation, diplopia, cataracts, fever IOP, hearing loss.

Other services:  often-allergic reactions, increased body temperature, weight loss, increased sweating; rarely-retroperitoneal fibrosis. There have been cases of peripheral edema.

Interaction

Pramipexole binds to plasma proteins to a small extent (less than 20%) and undergoes biotransformation. Therefore, interactions with other drugs that affect plasma protein binding or elimination by biotransformation are unlikely.

Selegiline and levodopa do not affect the pharmacokinetics of pramipexole. Pramipexole increases the_cmaxof levodopa by 40% and reduces the tmax from 2.5 to 0.5 hours.

Drugs that inhibit the active secretion of cationic drugs through the renal tubules (for example, cimetidine), or which are themselves eliminated by active secretion through the renal tubules, may interact with pramipexole, which is expressed in a decrease in the clearance of one or both drugs. If amantadine and pramipexole are used concomitantly, attention should be paid to signs of dopamine overstimulation, such as dyskinesia, agitation, or hallucinations. In such cases, it is necessary to reduce the dose.

Diltiazem, triamteren, verapamil, quinidine, quinine reduce the clearance of pramipexole by 20%.

Interaction with anticholinergic drugs and amantadine has not been studied. However, interaction with amantadine is possible, since the drugs have a similar mechanism of elimination. Anticholinergics are mainly metabolically eliminated, so interaction with pramipexole is unlikely.

When increasing the dose of pramipexole, it is recommended to reduce the dose of levodopa, while maintaining the concentration of other antiparkinsonian drugs at a constant level.

Dopamine receptor agonists (derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide) reduce the effectiveness of pramipexole.

Due to possible cumulative effects, patients should be advised to exercise caution when using sedatives or ethanol (alcohol) and pramipexole simultaneously, as well as when taking medications that increase the concentration of pramipexole in plasma (for example, cimetidine).

How to take, course of use and dosage

Inside, regardless of food intake, with a sufficient amount of liquid.

The daily dose should be evenly divided into 3 doses.

The initial daily dose of 264 mcg of pramipexole base (375 mcg of pramipexole dihydrochloride) should be increased every 5-7 days.

Overdose

Symptoms:  nausea, vomiting, hyperkinesia, hallucinations, agitation and decreased blood pressure.

Treatment:  gastric lavage, symptomatic therapy. There is no specific antidote. The effectiveness of hemodialysis has not been established.

Tablet Form of production

Storage conditions

In a dark place, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Pramipexole

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For adults as directed by your doctor

Indications

Parkinson ‘s Disease