Sunday, March 5, 2017

Bromocriptine

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 Bromocriptine  Dopamine receptor agonists. The active ingredient is a derivative of ergot alkaloid and stimulates the central and peripheral D2-dopamine receptors. The basic principle is aimed at suppressing effects physiological lactation Inhibition of secretion of the hormone prolactin, normalization menstrual cycle , Reducing the number and size of cysts in the breast (achieved by eliminating the imbalance between estrogen levels and prostesterona), inhibition of increased secretion of growth hormone. Bromocriptine in large doses is able to stimulate dopamine receptors in the black core of the brain, the corpus striatum, mesolimbic system, the hypothalamus. The drug inhibits the secretion of hormones ACTH and growth hormone, has antiparkinsonian effects. Administration of a single dose causes a decrease in prolactin in 2 hours, antiparkinsonian effect   registered through 30-90minut, declines in growth hormone - 2 hours. Bromocriptine is available in tablet dosage form.

Indications:

Instructions for use of the drug bromocriptine recommends prescribers at prolaktinzavisimyh conditions and diseases: if amenorrhea   (including background galaktorei ), Failure of the luteal phase, oligomenoree , Drug hyperprolactinemia (antihypertensive effect and substance). The drug is prescribed for prolaktinnezavisimom female infertility : Anovulatory cycles (in addition to antiestrogen treatment) polycystic ovary syndrome . The premenstrual syndrome drug prescribed for breast tenderness, with swelling, caused by a specific phase of the menstrual cycle, mood disorders, flatulence. Bromocriptine in hyperprolactinemia shown in males: prolaktinzavisimy hypogonadism   (loss of libido, oligospermia, impotence).


When prolactinoma medication is prescribed in complex therapy of prolactin macro- and microadenomas in the pituitary gland; preoperatively to reduce the volume of tumors that can facilitate its subsequent removal. Postoperatively, bromocriptine is used at a high level of prolactin. Acromegaly medicament administered in special cases as an alternative to radiation therapy or surgery. The drug inhibits lactation, it can be used to stop or prevent postpartum lactation after an abortion at puerperal mastitis , For medical reasons, under the postpartum breast engorgement. Bromocriptine is prescribed for benign breast pathology: shotty breast , Cystic and nodular changes benign nature, mastalgia . The drug is indicated for Parkinson's disease (parkinsonism postentsefaliticheskogo all stages and idiopathic Parkinson's disease).

Contraindications:

Bromocriptine is not prescribed for hypertension in the postpartum period, gestosis, intolerance to the active substance, diseases of the cardiovascular system, chorea Gettingtona , Familial tremor, hypotension, endogenous psychosis Ulcerative diseases of the digestive tract, liver disease, essential tremor . At the time of antihypertensive therapy, breastfeeding, parkinsonism   with signs of dementia, while carrying a pregnancy bromocriptine is prescribed with caution.

Side effect:

Constipation, nausea, orthostatic hypotension , Dizziness, vomiting, increased drowsiness, headache, allergic reactions, dry mouth, dyskinesia , Hallucinations, agitation, disturbance of vision, cramps in the calf muscles, skin rashes, orokandidoz , Periodontal disease, and allergic reactions. Long-term therapy can cause fainting, confusion, gastrointestinal bleeding   (presence of blood in vomit, black stools), peptic ulcer, retroperitoneal fibrosis   (weakness, loss of appetite, epigastric pain, nausea, vomiting, frequent urination).

Overdose:

Manifested by hallucinations, headaches, a fall in blood pressure. It is recommended that parenteral administration of metoclopramide.

Mode of application:

Bromocriptine tablets administered by mouth, while eating; per day not exceeding 100 mg. When female infertility, menstrual irregularities   - 2-3 times a day for 1, 25 mg; the ineffectiveness of the amount of medicament increased to 5-7 and 5 mg per day (multiple - 2-3). The therapy is carried out to the full restoration of ovulation or before the normalization of the menstrual cycle. To prevent a recurrence treatment may comprise several successive cycles. When premenstrual syndrome   Richter bromocriptine administered on the 14th day of the menstrual cycle in a dose of 1, 25 mg. Prior to the onset of menstruation amount of the drug is gradually increased up to 5 mg per day. When hyperprolactinemia in males   medicament is administered 2-3 times a day for 1, 25 mg, with a gradual increase to 5-10mg per day. With prolactinoma 2-3 times per day for 1, 25 mg to achieve adequate reduction of prolactin in the blood.

With acromegaly   initial treatment regimen includes a three-time taking the drug at a dose of 1, 25 mg; may further increase to 20 mg. For suppression of lactation on the first day of bromocriptine administered twice at 1, 25 mg, followed by 2 5 mg 2 times a day for two weeks. To stop the lactation, the drug is prescribed for a few hours before the abortion or childbirth. Possible slight secretion of milk in 2-3 days after discontinuation of the drug.

Bromocriptine take a dose of 2, 5 mg during the postpartum breast engorgement; possible repetition of the procedure in 6-12 hours as needed .  When starting postpartum mastitis treatment regimen is identical scheme in the suppression of lactation, further prescribe antibiotics .  In benign breast disease bromocriptine take three times a day 1, 25 mg, with a gradual increase in the daily dose to 5-7, 5 mg .  In Parkinson's disease ensure optimal tolerability of the medicament is achieved designation minimum dosages on the first day - 1, 25 mg .  Gradually increase the amount of the drug, an adequate therapeutic effect is achieved in 6-8 weeks .  In the absence of the desired effect may increase the daily amount of medication to 2 5 mg per day .  When registering significant side effects of the drug reduced the number of daily .  After stabilization may return to initial dosage .  Patients with movement disorders characteristic of receiving levodopa, it is recommended to reduce the dose of levodopa in the treatment of bromocriptine .  Thus it is possible to achieve the complete abolition of levodopa .

Special instructions:

Early treatment for the prevention of nausea and vomiting is recommended to prescribe an antiemetic medication 1 hour before receiving Bromocriptine. It requires regular monitoring of indicators of the functional state of the hepatic system, the level of blood pressure. The drug affects the performance of complex activities, management of vehicles, concentration. The treatment may accelerate the process of resumption of work ovary   after delivery, as the attending doctor must notify the patient in order to avoid early postpartum conception. In the event of pregnancy medication therapy is stopped, unless the necessity of the treatment outweigh the potential risk to the fetus. During treatment recommended bromocriptine non-hormonal contraception .

When the diagnosis of pregnancy on the background pituitary adenoma After cessation of treatment requires regular monitoring of adenomas, including necessarily the study of the visual fields. Before treatment of benign tumors of the mammary glands is necessary to eliminate the malignant nature of the tumor and any cancerous processes in the body. Bromocriptine in the treatment of acromegaly with concomitant ulcer disease of the digestive tract is not appointed. The treating physician should explain to patients about the need to inform the doctor and inform medical personnel in the event of a variety of disorders of the gastrointestinal tract. During treatment requires a thorough oral care. When the dryness in the mouth, do not stop for more than 2 weeks, a doctor should be consulted. Responses to the drug bromocriptine show the effectiveness of the drug.

Drug Interactions:

Bromocriptine is able to enhance the effect of antihypertensive drugs, levodopa ; reduce the effectiveness of oral contraceptives. Haloperidol Selegiline, procarbazine, furazolidone, MAO inhibitors, loxapine, metoclopramide, methyldopa, ergot alkaloids, phenothiazines, thioxanthine, reserpine, molindone increase the risk of side effects by increasing the concentration in the blood plasma. Recommended a 50% reduction in drug dosage while therapy ritonavir . Admission disulfiramopodobnye ethanol causes reactions such as skin redness, pain chest, vomiting, tachycardia , Nausea, blurred vision, cough reflex, throbbing headache, seizures .

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