2010/06/05

Abergin (Bromocriptine)

Trade name:
Abergin

International name:
Bromocriptine (Bromocriptine)

Group Affiliation:
Dopamine receptor agonist

Description of the active substance (INN):
Bromocriptine

Dosage form:
Tablets

Mode of action:
Stimulants of the central and peripheral D2-dopamine receptors (a derivative of ergot alkaloids). Inhibiting prolactin secretion, suppresses the physiological lactation, promotes the normalization of menstrual function, inhibits the increased secretion of growth hormone, reduces the size and number of cysts in the breast (at the expense of redressing the imbalance between progesterone and estrogen). In high doses stimulates dopamine receptors in the striatum, black nucleus of the brain , hypothalamus and Mesolimbic system. Has antiparkinsonian action, suppresses the secretion of GH and ACTH. After receiving a single dose reduction of prolactin plasma occurs after 2 h, the maximum effect - after 8 h, antiparkinsonian effect - after 30-90 minutes, maximum - 2 hours, the decline in ST - after 1-2 h, Tried effect is achieved after 4-8 weeks of therapy.

Indications:
Menstrual irregularities, female infertility: - prolaktinzavisimye diseases and conditions, accompanied or not by hyperprolactinemia: amenorrhea (accompanied and unaccompanied by galactorrhea) oligomenorrhea, luteal phase defect, hyperprolactinemia secondary against the admission of drugs (eg some psychoactive or hypotensive drugs) - prolaktinnezavisimoe female infertility: polycystic ovary syndrome; anovulyatornye cycles (in addition to antiestrogens such klomifenu). Premenstrual syndrome - breast tenderness, swelling, associated with the phase of the cycle, bloating, mood disorder. hyperprolactinemia in men: prolaktinzavisimy hypogonadism (oligospermia, loss of libido , impotence). Prolaktinomy: conservative treatment prolaktinsekretiruyuschih micro-and makroadenom pituitary; preoperative preparation to reduce the tumor volume and facilitating its removal, postoperative treatment if prolactin levels remain elevated. acromegaly: as an additional drug in combination with radiation therapy and surgery or in special cases, as an alternative to surgery or radiation therapy. suppression of lactation: the prevention or termination of postpartum lactation for medical reasons: to prevent lactation after an abortion, postpartum breast engorgement; beginning of postpartum mastitis. Benign breast diseases: mastalgia (in isolation or in combined with premenstrual syndrome or benign nodular or cystic changes); benign node and / or cystic changes, particularly of fibro-cystic breast. Parkinson's disease: all the stages of idiopathic Parkinson's disease and parkinsonism postentsefaliticheskogo (as monotherapy or in combination with other antiparkinsonian drugs ).

Contraindications:
Hypersensitivity, preeclampsia, hypertension in the postpartum period, essential tremor and family, chorea Gettingtona diseases CAS, endogenous psychosis, hypertension, hypotension, liver failure, ulcerative lesions ZHKT.C caution. Parkinsonism with signs of dementia, pregnancy, lactation period (excreted in milk), the simultaneous holding of antihypertensive therapy.

Side effects:
Nausea, vomiting, dizziness, rarely - orthostatic hypotension. Myocardial infarction, stroke. Constipation, drowsiness, headache, psychomotor agitation, hallucinations, psychosis, dyskinesia, reduced visual acuity, dry mouth (dental caries, periodontal diseases, orokandidoz, discomfort), nasal congestion, allergic reactions, skin rashes, cramps in the calf muscles. Prolonged application - Raynaud syndrome, the treatment with high doses (parkinsonism) - confusion, the selection of CSF from the nasal passages, fainting, peptic ulcers, gastrointestinal bleeding (black stool, blood in vomit), retroperitoneal fibrosis (abdominal pain, decrease appetite, back pain, nausea, vomiting, weakness, frequent urination). Overdosage. Symptoms: headache, hallucinations, decrease blood pressure. Treatment: parenteral administration of metoclopramide.

Dosage and administration:
Inside, during the meal, the maximum daily dose - 100 mg. Menstrual irregularities, female infertility - at 1.25 mg 2-3 times a day if the effect is insufficient, the dose gradually increased to 5-7.5 mg / d (multiplicity of reception 2-3 times / day). Treatment is continued until the normalization of the menstrual cycle and / or restore ovulation. If necessary to prevent a recurrence, treatment can continue for several cycles. Premenstrual syndrome - treatment begins on day 14 of cycle with 1.25 mg / day. Gradually increase the dose to 1.25 mg / day to 5 mg / day (before the onset of menstruation). Hyperprolactinemia in men - at 1.25 mg 2-3 times daily, gradually increasing the dose of 5-10 mg / day. Prolaktinomy - at 1.25 mg 2 -3 times a day, with a gradual increase in dose up to a few pills a day needed to maintain an adequate reduction of the concentration of prolactin in plasma. acromegaly - the initial dose is 1.25 mg 2-3 times a day in the future, depending on the clinical effect and side action, the daily dose gradually increased to 10-20 mg. suppression of lactation - 1 day appointed for the 1.25 mg 2 times (during meals at breakfast and dinner), then within 14 days - 2.5 mg 2 times a day. To prevent early lactation receiving the drug should be started within a few hours after birth or abortion (after stabilization of vital functions). 2-3 days after discontinuation of the drug is sometimes a slight secretion of milk. It can eliminate the resumption of receiving the drug at the same dose for 1 week. Postpartum breast engorgement - designate a single dose of 2.5 mg in 6-12 hours if necessary, repeat the reception (it is not accompanied by an undesirable suppression of lactation). Incipient puerperal mastitis - dosing regimen is the same as in the case of suppression of lactation. If you want to add the antibiotic treatment. Benign breast diseases - at 1.25 mg 2-3 times a day. The daily dose gradually increased to 5-7.5 mg. Parkinson's disease - for optimal portability, treatment should be started with the application of a small dose: 1.25 mg 1 time a day (preferably in the evening) for 1 week. The daily dose of the drug increases gradually each week by 1.25 mg daily dose is divided into 2-3 reception. Adequate therapeutic result can be achieved within 6-8 weeks of treatment. If not, the daily dose can be increased further - each week by 2.5 mg / day. The average therapeutic doses of bromocriptine for mono-or combination therapy are 10-40 mg / day, but some patients may require higher doses. If the selection of doses side effects occur, the daily dose should be reduced and maintained at a lower level for at least 1 week. If the side effects disappear, the dose of the drug can again increase. Patients with movement disorders, taking place against a background of reception of levodopa is recommended prior to the application of bromocriptine to reduce the dose of levodopa. After achieving a satisfactory effect can be taken further gradual reduction in dose of levodopa. Some patients can complete abolition of levodopa.

Cautions:
To prevent nausea and vomiting in early treatment appropriate to appoint antiemetic drugs for 1 h prior to treatment. It is recommended that periodic monitoring of blood pressure, liver and kidney function. Patients taking the drug, should refrain from training activities that require increased attention and rapid physical and mental reactions . The treatment can cause a rapid resumption of ovarian function after childbirth, and therefore the need to alert women about the possibility of early postpartum conception. In women taking bromocriptine when pregnancy occurs treatment ceased except in cases where a possible positive effect of treatment outweigh the potential risk to the fetus. During treatment it is expedient to use non-hormonal contraception. In case of pregnancy with pituitary adenoma, after the cancellation is necessary systematic condition monitoring adenomas, including the study of visual fields. Before starting the treatment of benign breast diseases is necessary to exclude the presence of a malignant tumor of the same location. In the treatment of acromegaly, If history is an indication of the presence of gastric ulcer, from the treatment should be abandoned. If treatment requires patients to pay attention to the need to put a doctor in popularity in the event of disorders of the gastrointestinal tract. We must carefully observe good oral hygiene, with the persistent dryness of the mouth more than 2 weeks consult a doctor.

Interaction:
Reduces effectiveness of oral contraceptives. Enhances effect of levodopa, antihypertensive drugs. MAO inhibitors, furazolidone, procarbazine, selegiline, ergot alkaloids, haloperidol, loksapin, metildofa, metoclopramide, molindon, reserpine, and phenothiazines tioksantiny increase the concentration in plasma and risk of side effects. Erythromycin , clarithromycin, troleandomitsin increase the bioavailability and Cmax, butyrophenones reduce efficiency. Simultaneous reception of ethanol leads to the development disulfiramopodobnyh reactions (chest pain, flushing of skin, tachycardia, nausea, vomiting, cough reflex, throbbing headache, blurred vision, weakness, convulsions) . In a joint appointment with ritonavir is recommended 50% reduction in dose.