Bromocriptinum

General characteristics. Structure:

Active agent: Bromocriptinum мезилат 2,87 mg in terms of Bromocriptinum of 2,5 mg.

Excipients: lactoses monohydrate of-55,63 mg, cellulose microcrystallic - 20,0 mg, potato starch - 15,0 mg, sodium carboxymethylstarch - 2,0 mg, povidone (polyvinylpirrolidone) - 3,5 mg, magnesium stearate of-1,0 mg.

Pharmacological properties:

Stimulator of the central and peripheral 02-dopamine receptors (derivative ergot alkaloid). Inhibiting prolactin secretion, suppresses a physiological lactation, contributes to normalization of menstrual function, oppresses growth hormone hypersecretion, reduces the sizes and number of cysts in a mammary gland (due to elimination of an imbalance between progesterone and estrogen).
Stimulates dopamine receptors of a striate body, black kernel of a brain, a hypothalamus and mesolimbic system in high doses. Has protivoparkinso-nichesky effect, suppresses secretion of somatotropic (STG) and adrenocorticotropic (AKTG) of hormones. After reception of a single dose decrease in level of prolactin of a blood plasma occurs in 2 hours, the maximum effect - in 8 hours, protivoparkinsonichesky effect - in 30-90 min., maximum - in 2 hours, decrease in the STG level - in 1-2 hours, the maximum effect is reached in 4-8 weeks of therapy.

Pharmacokinetics. Absorption - 28% (25-30%), the semi-absorption period - 20 min. Gets into breast milk. Has effect of "the first passing" through a liver, bioavailability of-6%.
Communication with proteins of plasma (albumine) - 90-96%. Time of achievement of the maximum concentration (Tsglakh) - 1-3 hours. The elimination half-life is two-phase: 4-4,5 hours - and - a phase, 15 hours - a final phase. It is removed with bile in the form of metabolites, through kidneys - 6%.

Indications to use:

Disturbances of a menstrual cycle, female infertility:
- the prolaktinzavisimy diseases and states which are followed or not followed by a giperprolaktinemiya: the amenorrhea (which is followed and not followed by a galactorrhoea); oligomenorrhea; insufficiency of a lyuteinovy phase; a secondary giperprolaktinemiya against the background of reception of medicines (for example, some psychoactive or hypotensive medicines);
- prolaktinnezavisimy female infertility: syndrome of polycystic ovaries; anovulatory cycles (in addition to anti-estrogen, for example clomifene). A premenstrual syndrome - morbidity of mammary glands; the hypostases connected with a cycle phase; meteorism; disturbances of mood.
Giperprolaktinemiya at men: prolaktinzavisimy hypogonadism (oligospermatism, loss of a libido, impotence).
Prolaktinoma: conservative treatment prolaktinsekre-tiruyushchy micro and macroadenomas of a hypophysis; preoperative preparation for reduction of volume of a tumor and simplification of its removal; postoperative treatment if the level of prolactin remains raised. Acromegalia: as additional medicine in a complex with radiation therapy and operational treatment or, in special cases, as an alternative to surgical or beam treatment. Suppression of a lactation: prevention or the termination of a puerperal lactation on medical indications: prevention of a lactation after abortion; puerperal nagrubaniye of mammary glands; the beginning lactational mastitis. Benign diseases of mammary glands: a mastalgiya (in the isolated look, and also in combination with a premenstrual syndrome), a mastalgiya with high-quality nodal or cystous changes of gland; high-quality nodal and/or cystous changes, especially fibrous and cystous mastopathy. Parkinson's disease: all stages of an idiopathic disease of Parkinson and postencephalitic parkinsonism (in the form of monotherapy, or in a combination with other protivoparkinsonichesky medicines).

Route of administration and doses:

Inside, during food, the maximum daily dose of-100 mg.
Disturbances of a menstrual cycle, female infertility - on 1,25 mg 2-3 times a day; if the effect is insufficient, the dose is gradually increased to 5-7,5 mg/days (frequency rate of reception 2-3 times/days). Treatment is continued before normalization of a menstrual cycle and/or recovery of an ovulation. If necessary for prevention of a recurrence, treatment can be continued during several cycles.
Premenstrual syndrome - treatment is begun for the 14th day of a cycle with 1,25 mg/days. Gradually increase a dose by 1,25 mg/days to 5 mg/days (before periods).
Giperprolaktinemiya at men - on 1,25 mg 2-3 times a day, gradually increasing a dose to 5-10 mg/days. Prolaktinoma - on 1,25 mg 2-3 times a day, with gradual increase in a dose up to several tablets in days, necessary for maintenance of adequate decrease in concentration of prolactin in plasma. The acromegalia - an initial dose makes 1,25 mg 2-3 times a day, further, depending on clinical effect and side effects, the daily dose is gradually increased to 10-20 mg. Suppression of a lactation - in 1 day 2 times (appoint 1,25 mg during food at breakfast and a dinner), then within 14 days - on 2,5 mg 2 times a day. For prevention of the beginning of a lactation administration of drug should be begun in several hours after the delivery or abortion (after stabilization of the vital functions). In 2-3 days after drug withdrawal sometimes there is an insignificant secretion of milk. It can be eliminated, having resumed administration of drug in the same dose within 1 more week.
The puerperal nagrubaniye of mammary glands - is appointed once in a dose by 2,5 mg, in 6-12 hours if necessary repeat reception (it is not followed by undesirable suppression of a lactation). The beginning lactational mastitis - the mode of dosing same, as well as in case of suppression of a lactation. If necessary add an antibiotic to treatment.
Benign diseases of mammary glands - on 1,25 mg 2-3 times a day. The daily dose is gradually increased to 5-7,5 mg. Parkinson's disease - for ensuring optimum portability treatment should be begun with use of a small dose of drug: 1,25 mg of 1 times a day (it is more preferable in the evening) within 1 week. The daily dose of drug is raised gradually, every week on 1,25 mg, the daily dose is divided into 2-3 receptions. The adequate therapeutic result can be achieved within 6-8 weeks of treatment. If it does not occur, the daily dose can be raised further - every week on 2,5 mg/days. Average therapeutic doses of Bromocriptinum for mono-or a combination therapy make 10-30 mg/days. The maximum daily dose - 30 mg. If at selection of a dose there are by-effects, the daily dose should be reduced and supported at lower level within not less than 1 week. If by-effects disappear, the dose of drug can be raised again. Patients with the motive disturbances which are noted against the background of reception of a levodopa are recommended to lower a levodopa dose prior to use of Bromocriptinum. After achievement of satisfactory effect it is possible to undertake further gradual reduction of a dose of a levodopa. At some patients full cancellation of a levodopa is possible.

Features of use:

For the prevention of nausea and vomiting in an initiation of treatment it is reasonable to appoint antiemetic medicines in 1 hour prior to administration of drug. Periodic control of arterial pressure, function of a liver and kidneys is recommended. At use of drug in high doses during the long period the risk of development of cardial fibrosis is increased.
Treatment can cause the accelerated resuming of function of ovaries after the delivery in this connection, the warning of women of a possibility of early puerperal conception is necessary. At the women accepting Bromocriptinum at pregnancy approach treatment is stopped, except for cases when the possible positive effect of treatment outweighs potential risk for a fruit. During therapy use of non-hormonal contraception is reasonable.
In case of pregnancy against the background of hypophysis adenoma after cancellation systematic control of its state, including a research of fields of vision is necessary. Before an initiation of treatment of benign diseases of mammary glands it is necessary to exclude existence of a malignant tumor of the same localization. At treatment of an acromegalia if in the anamnesis there is an instruction on existence of a peptic ulcer of a stomach, it is better to refuse treatment. If treatment is necessary, to draw the attention of patients to need to inform the doctor at emergence of frustration from digestive tract.
It is necessary to observe carefully hygiene of an oral cavity, at the remaining dryness of an oral cavity more than 2 weeks it is necessary to consult with the doctor. The patients accepting drug should abstain  from occupations   the types of activity  requiring special  attention  and  bystry  physical  and mental reactions.

Side effects:

Nausea, vomiting, dizziness; seldom - orthostatic hypotension. Myocardial infarction, stroke. A lock, drowsiness, a headache, psychomotor excitement, hallucinations, psychoses, a liskineziya, decrease in visual acuity, dryness in a mouth (caries, diseases of a parodont, орокандидоз, discomfort), a nose congestion, allergic reactions, skin rash, spasms in gastrocnemius muscles.
At prolonged use - Reynaud's syndrome; at treatment by high doses (parkinsonism) - confusion of consciousness, release of cerebrospinal liquid from the nasal courses, unconscious states, a round ulcer, gastrointestinal bleeding (black kcal, blood in emetic masses), retroperitoneal fibrosis (an abdominal pain, a loss of appetite, a dorsodynia, nausea, vomiting, weakness, the speeded-up urination).

Interaction with other medicines:

Reduces efficiency of oral contraceptives. Strengthens effect of a levodopa, hypotensive medicines.
 Monoamine oxidase inhibitors,    furasolidone, Procarbazinum, селегилин, ergot alkaloids, a haloperidol, локсапин, Methyldopum, метокпопрамид, молиндон, Reserpinum, thioxanthines and fenotiazina increase concentration in plasma and risk of development of side effects. Erythromycin, кларитромицин, тролеандомицин increase bioavailability and the maximum concentration, phenyl propyl ketones reduce efficiency. The concomitant use of ethanol leads to development of disulfiramopodobny reactions (a stethalgia, a hyperemia of integuments, tachycardia, nausea, vomiting, reflex cough, the pulsing headache, indistinct sight, weakness, судорош).
At joint appointment with ritonaviry 50% a dose decline are recommended.

Contraindications:

Hypersensitivity to Bromocriptinum and other alkaloids of an ergot; gestosis; arterial hypertension in a puerperal period; diseases of cardiovascular system (including arterial hypertension, hypotension); essential, family tremor; psychoses; liver failure; chorea of Gettington; digestive tract cankers; children's age.
WITH CARE
Parkinsonism with dementia symptoms; pregnancy; lactation period; simultaneous performing hypotensive therapy.

Overdose:

Symptoms: headache, hallucinations, lowering of arterial pressure.
Treatment: parenteral administration of Metoclopramidum.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets on 2,5 mg.
On 10,30 tablets in a blister strip packaging from a film of the polivinilkhporidny and printing aluminum foil varnished.
On   10, 20, 30, 40, 50 or 100 tablets in a container polymeric for medicines. One container or 1, 2, 3, 4, 5, 6, 8 or 10 blister strip packagings together with the application instruction place in a pack from a cardboard.