Bromocriptinum

General characteristics. Structure:

Active ingredient: Bromocriptinum of 2,5 mg (in the form of 2,87 mg of Bromocriptinum of a mezilat).

Excipients: silicon dioxide of colloid 0,65 mg, magnesium stearate of 1,30 mg, talc of 3,90 mg, povidone of 5,20 mg, starch of corn 35,08 mg, cellulose of microcrystallic 40,00 mg, lactoses monohydrate of 41,00 mg.

Pharmacological properties:

Pharmacodynamics. Derivative an ergot, a stimulator of the central and peripheral D2 - dopamine receptors. Inhibiting prolactin secretion, suppresses a physiological lactation, contributes to normalization of menstrual function, reduces the sizes and quantity of cysts in a mammary gland due to elimination of an imbalance of levels of progesterone and estrogen. Does not influence puerperal involution of a uterus and does not increase risk of development of thromboembolisms. Normalizes secretion of luteinizing hormone, reduces expressiveness of a syndrome of polycystic ovaries. Stops growth and reduces the sizes of prolaktinsekretiruyushchy adenomas of a hypophysis.
Stimulates dopamine receptors of a striate body and black kernel of a brain, a hypothalamus and mesolimbic system in high doses and recovers neurochemical balance in these structures. Has protivoparkinsonichesky effect (reduces a tremor, rigidity and slowness of movements in all stages of a disease of Parkinson), weakens expressiveness of the accompanying depression, keeping efficiency for many years.
Suppresses secretion of somatotropic and adrenocorticotropic hormones of a hypophysis, without exerting impacts on other hormones of a hypophysis if their concentration is in norm limits.
After reception of a single dose decrease in level of prolactin in blood occurs in 2 h, the maximum effect is observed in 8 h; protivoparkinsonichesky effect – in 30-90 min., the maximum effect – in 2 h; decrease in somatotropic hormone – in 1-2 h. The maximum effect is reached in 4-8 weeks of therapy.

 Pharmacokinetics. Absorption makes of digestive tract ~ 30%, the semi-absorption period – 20 min. Biological availability ~ 6% as a result of primary metabolism in a liver. Communication with proteins (albumine) of plasma – 90 - 96%. Gets into breast milk. The maximum concentration in blood is reached in 1-3 h. The elimination half-life is two-phase: an alpha phase – 4-4,5 h, a final phase – 15 h. Removal is carried out in the form of metabolites, also 6% - kidneys are preferential with bile.

Indications to use:

Disturbances of a menstrual cycle, female infertility:

- The Prolaktinzavisimy diseases and states which are followed or not followed by a giperprolaktinemiya: an amenorrhea with a galactorrhoea or without it; oligomenorrhea; insufficiency of a lyuteinovy phase; the secondary giperprolaktinemiya connected with reception of medicines (some psychostimulants, antihypertensives).
- Prolaktinnezavisimy female infertility: a syndrome of polycystic ovaries, anovulatory cycles (in addition to therapy with anti-estrogen, for example clomifene).
- Premenstrual syndrome (morbidity of mammary glands, hypostases, meteorism, disturbances of mood).
- Giperprolaktinemiya at men: prolaktinzavisimy hypogonadism (oligospermatism, decrease in a libido, impotence).
- Prolaktinoma: conservative treatment prolaktinsekretiruyushchy micro and macroadenomas of a hypophysis; preoperative preparation for reduction of volume of a tumor; postoperative treatment if the level of prolactin remains raised.
- Acromegalia: as an additional tool in complex therapy together with beam and operational treatment, or, in special cases, as an alternative to surgical or beam treatment.
- Suppression of a lactation: prevention or suppression of a puerperal lactation on medical indications: after abortion; puerperal nagrubaniye of mammary glands; the beginning lactational mastitis.
- Benign diseases of mammary glands: a mastalgiya at a premenstrual syndrome or without it; a mastalgiya with high-quality nodal or cystous changes of gland; high-quality nodal or cystous changes, especially, fibrous and cystous mastopathy.
- All stages of an idiopathic disease of Parkinson and postentsefalitny parkinsonism (monotherapy or in a combination with other protivoparkinsonichesky medicines).

Route of administration and doses:

Inside, during food.
Disturbances of a menstrual cycle, female infertility: on 1,25 mg 2-3 times in days, in case of need a dose gradually increase up to 5-7,5 mg/days. Treatment is continued before normalization of a menstrual cycle and/or recovery of an ovulation. For prevention of a recurrence treatment can be continued during several menstrual cycles.
Premenstrual syndrome: to begin treatment for the 14th day of a menstrual cycle with 1,25 mg/days, the dose is gradually increased 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 in days, gradually increasing a dose to several tablets a day providing the desirable level of prolactin in blood.
Acromegalia: an initial dose on 1,25 mg 2-3 times a day, then, depending on clinical and side effects, a daily dose it is possible to increase gradually to 10-20 mg.
Termination of a lactation: in the first day on 1,25 mg 2 times (in the morning and in the evening), then within 14 days on 2,5 mg 2 times a day. Treatment needs to be begun in several hours after the delivery or abortion, but not in the first 4 hours after them – after stabilization of the vital functions of an organism. In 2-3 days after drug withdrawal insignificant secretion of milk is possible, resuming of administration of drug within 1 more week in the same dose leads to the secretion termination.
The beginning lactational mastitis: see the section the termination of a lactation. In case of need begin treatment with an antibiotic.

Puerperal nagrubaniye of mammary glands: 2,5 mg once, later 6-12 h a dose it is possible to repeat, the undesirable stop of a lactation at the same time does not arise.
Benign diseases of mammary glands: on 1,25 mg 2-3 times a day, gradually increase a dose to 5-7,5 mg/days.
Parkinson's disease: for ensuring optimum portability treatment is begun with a small dose: 1,25 mg of 1 times in days, are desirable in the evening, within 1 week. The dose gradually, is weekly raised on 1,25 mg, distributing on 2-3 receptions a day.
The therapeutic effect occurs within 6-8 weeks of treatment, otherwise it is possible to continue to raise a daily dose, weekly increasing it by 2,5 mg/days.

Average therapeutic doses of Bromocriptinum for mono - and a combination therapy – 10-30 mg/days. The maximum daily dose – 30 mg. In case of development of side effects the daily dose is subject to decrease, after each next decrease the dose is appointed within not less than 1 week. At disappearance of undesirable reactions, the dose can be increased 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. In case of satisfactory therapeutic effect it is possible to continue a further gradual dose decline of a levodopa, sometimes up to its full cancellation. Treatment by Bromocriptinum should be begun along with development of side effects of a levodopa, for example, of dyskinesia, aggravations of symptoms by the end of the action of a dose of a levodopa connected with reduction of duration of action of a single dose (effect of "end of dose") since Bromocriptinum minimal effective dose. Higher doses apply in exceptional cases.

Features of use:

For prevention of dizziness, nausea and vomiting in an initiation of treatment it is reasonable to appoint antiemetics in 1 hour prior to administration of drug.
Periodic control of arterial pressure, function of kidneys and a liver, at parkinsonism – in addition is recommended to function of cardiovascular system, a blood picture.
It is necessary to remember a possibility of approach of pregnancy after the delivery against the background of treatment by drug owing to bystry recovery of ovulatory cycles in this connection use of non-hormonal contraception is reasonable.
In case of pregnancy against the background of hypophysis adenoma, after the treatment termination by Bromocriptinum regular control of a condition of adenoma, including a research of fields of vision is necessary.

At suppression of a puerperal lactation, regular control of arterial pressure, especially, on the first week of treatment by Bromocriptinum 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 arterial hypertension, a sharp, persistent headache with disturbance of visual acuity or without vision disorder it is necessary to stop treatment by Bromocriptinum and to conduct examination of the patient.
In the presence in the anamnesis of a peptic ulcer of a stomach it is desirable to refuse treatment of an acromegalia Bromocriptinum and to apply, whenever possible, other therapy. In case treatment by Bromocriptinum is carried out nevertheless, it is necessary to warn the patient about possible development of gastrointestinal frustration and about importance of the address in such cases to the attending physician.
Careful respect for hygiene of an oral cavity is necessary. At the remaining dryness of an oral cavity more than 2 weeks it is necessary to consult with the doctor.
In the presence of mental disorders purpose of high doses demands extra care.
In case of the expressed increase in the sizes of a prolaktinoma it is necessary to start treatment again.

At treatment of the diseases which are not followed by a giperprolaktinemiya appoint the smallest effective dose of Bromocriptinum.
At development of plevro-pulmonic symptoms (infiltrate in lungs, a pleural exudate) it is necessary to stop treatment and to conduct careful medical examination of the patient.

Influence on ability to drive the car and other mechanisms:
It is necessary to abstain from driving of the car and occupations the types of activity requiring special attention and speed of physical and psychomotor reactions (sudden backfilling, decrease in visual acuity are possible). These restrictions have individual character.

Side effects:

Nausea, vomiting, headache, dizziness, it is rare – orthostatic hypotension, fatigue (these by-effects do not demand the treatment termination), a myocardial infarction, a stroke, obstipation, drowsiness, sudden backfilling, psychomotor excitement, hallucinations, psychoses, dyskinesia, decrease in visual acuity, dryness in a mouth, caries, diseases of a parodont, орокандиоз, a nose congestion, allergic skin rash, spasms in gastrocnemius muscles.

At long therapy – Reynaud's syndrome; at treatment of parkinsonism high doses – confusion of consciousness, release of cerebrospinal fluid from the nasal courses, faints, a round ulcer, gastrointestinal bleeding, retroperitoneal fibrosis (an abdominal pain, spin, a loss of appetite, nausea, vomiting, the speeded-up urination).

Interaction with other medicines:

Reduces efficiency of oral contraceptives.
Strengthens effects of a levodopa, hypotensive medicines.
Erythromycin, кларитромицин, тролеандомицин increase bioavailability and the maximum concentration in plasma.
At appointment with ritonaviry 50% a dose decline are recommended.
Monoamine oxidase inhibitors, furasolidone, Procarbazinum, селегилин, ergot alkaloids (it is impossible to apply together), локсапин, Methyldopa, Metoclopramidum, молиндон, Reserpinum, thioxanthines increase concentration in plasma and promote development of side reactions.

The drugs possessing anti-dopamine action: phenyl propyl ketones, fenotiazina can weaken action of Bromocriptinum.
Reception of ethanol leads to development of disulfiramopodobny reactions: a stethalgia, a hyperemia, tachycardia, nausea, vomiting, reflex cough, the pulsing headache, decrease in visual acuity, weakness, spasms.

Contraindications:

- Hypersensitivity to Bromocriptinum and other alkaloids of an ergot;
- diseases of valves of heart;
- gestosis;
- arterial hypertension in a puerperal period;
- essential and family tremor;
- chorea of Gettington;
- psychoses;
- cardiovascular diseases (including arterial hypertension; hypotension);
- liver failure;
- digestive tract cankers;
- children's age (up to 15 years, in view of lack of sufficient clinical experience).

With care: parkinsonism with dementia symptoms; pregnancy; lactation period; simultaneous performing hypotensive therapy.

Pregnancy and period of a lactation
Pregnancy: Women of childbearing age during treatment by Bromocriptinum need to provide reliable, whenever possible non-hormonal contraception. In case of desire of the patient to keep pregnancy it is necessary to stop treatment by Bromocriptinum, except for cases when advantage of use of Bromocriptinum for mother more, than the harm done to a fruit. Reception of Bromocriptinum in the first 8 weeks of pregnancy does not make harmful effects on a current and the result of pregnancy. After drug withdrawal abortions do not become frequent.
In the period of a lactation apply only according to indications.

Overdose:

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

Storage conditions:

To store in the place protected from light at a temperature not above 30 °C. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Tablets of 2,5 mg.
On 30 tablets in a brown glass bottle of the III hydrolytic class. 1 bottle in a cardboard pack with the enclosed application instruction.