Pergolide

Chemical name

(8бета)-8-[(Метилтио)мет��л]-6-пропилэрголин (and in the form of nelfinavir)

Gross

C19-H26-N2-S

Of drugs

The drugs - противопаркинсоничес кое. Ergolinovy agonist dofamine receptors. Does postsinapticalkie dofaminove receptors (D_1 and D_2) nigro-striarna the brain. Suppress the secretion of prolactin is tranzithornoe the concentration of growth hormone in serum (in patients with akromegaliei-down), a reduced standard luteinizirutego hormone in Krovi.horosho drawn from the blood was linked to the blood supply by 90%. Metabolised to form at least 10 metabolites, including pergolida sulfoxida and pergolida sulfona (agonisticescuu been active in tests on animals), as well as N-despropil-pergolida. Report predominantly Pockami.v biennial study carcinogenicity pergolida when imposing with their food mice (in doses 340 times MRDC), and rats (in doses 12 times higher than MRDC) have reported cases of uterine tumors (in mice, endometrium sarcoma, in rats, adenoma and carcinoma Oxytocics), due probably high estrogena / progesterone, which in rodents is the result �ролактинингибирующе��о the Pergolida.otsenka mutagennosti potential, and a number of tests in vitro and in vivo revealed weak mutagennouu activity in the analysis of point mutations after metabolic activation mikrosom liver rats. In imposing samzam and Female mice doses of 0.6 and 1.7 mg / kg / day influence fertility. However, with the increasing dose to 5.6 mg / kg / day cut fertility (possibly as a result of the reduction in serum hormone needed to maintain a certain level of progesterone, a normal implantation in mice). The mice and rabbits at doses exceeding MRDC 375, and 133 times, respectively, have been identified adverse action Plod.adekwatnykh and well-controlled studies on the use during pregnancy in humans did not. But there is evidence that women who received pergolid if there is a violation of endocrine status, 33 pregnancies resulted birth of healthy children, and six pregnancies accompanied by the emergence of birth defects in development, including 3 heavy.

Indications

Parkinson's disease (as a complement to the treatment of levodopa / carbidopa).

Restrictions on the use of

Pleurisy, plevralny fibrosis, pericardit, availability or pleural effusion pericardialland, retroperitonealny fibrosis in history, pregnancy, breast-feeding, child age (safety and efficacy of the use of children to be determined).

Pregnancy and lactation

Perhaps if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breast-feeding (ability excretirovtsa in breast milk is not known and, in addition, there is a likelihood of birth).

Contraindications

Гиперчувствительност ь (incl. other derivative LPV).

Side-Effects

From the nervous system and sensory organs : psoriasis, distonia, fatigue, dizziness, headache, hallucinations, sputannosti consciousness, drowsiness or insomnia, nightmares, anxiety, tremor, depression, personality changes, depression, the gait, and / or coordination of movements akatizia, ekstrapiramidnyi syndrome, paresthesia, akinesia, nevralgia, disorders of speech, visual impairment, including diplopia, violations Vkusa.so the circulatory system and blood (blood, gemostaz) : ortostatical gipotenzia, vazodilatation, demotion AD hypertension, fear, palpitations, irregular, myocardial infarction, pericardit, pericardialny vpot, Anemia.so the respiratory system : rhinitis, active bleeding, pharyngitis, increased cough, despnoe, pleurisy, plevralny vpot, plevralny Fibros.so part of the intestine : nausea, vomiting, dry mouth, neuralgia, constipation or diarrhoea, Anorexia.so the urogenital system : frequent urination, infections of the urinary tract, gematuria, Dismenorea.so the musculoskeletal system : artralgia, bursitis, mialgia, increasing muscle strength, apnoea Podergivania.prochie : pain syndrome (pain in the thorax, in the neck, abdominalnaya pain, pain in the back, etc.), grippopodobnyy syndrome, oedema, including peripheral, oedema; sweating, increases or decreases body weight, retroperitonealny fibrosis and skin rashes.

Patient interaction

Do effects of levodopa, incl. side (hallucinations, sputannosti consciousness psoriasis). Dopamine antagonists, including neiroleptiki (fenotiazina, butirofenona, tioksantena) and metoclopramide reduce effectiveness.

Overdosing

Symptoms : nausea, vomiting, loss AD convulsions, bringing Zns.lechenie : application of activated carbon (instead of or after gastric lavage); AD normalization, the maintenance functions of the heart, including complications of funds; in initiating CNS-appointment doses (from the group fenotiazina or butirofenon); necessary to monitor respiratory function, ensuring adequate ventilation, light, the maintenance of normal levels of gases and electrolytes blood.

Precautions

To use caution when in the history of pleurisy, plevralny vpot, plevralny fibrosis, pericardit, pericardialny vpot, retroperitonealny fibrosis, and other similar types of pathology (this category of patients must be carefully monitored clinical, which includes X-ray and laboratory studies). Caution is needed in patients with Aritmiami.v the likely (especially at the beginning of therapy) gipotenziei to start treatment with low doses and gradually increase them. Dose appointed a levodopa / carbidopa can be reduced (up to the average daily dose of levodopa-650 mg). Lifting перголида lower dose or change regimens should be implemented in a gradual manner (perhaps the нейролептического malignant syndrome).

Dosing and Administration

Inside, 3 times a day. Initial dose 0.05 mg / day within two days, then dose gradually increased at 0.1-015 mg / day every third day for 12 days, followed by 0.25 mg (every third day) to achieve an optimal therapeutic effect. Average daily intake to 3 mg.

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