2 Description of bromocriptine 2. 1 Drug name bromocriptine
2.2 English name Bromocription Pavilion, PARLODOL
2.3 Another name of bromocriptine ergotamine; Bromochlorocycline methanesulfonate; Bromergot cyclic peptide; Bromination treatment; Stop breastfeeding; Breast-conserving tone; Bromergocryptine; Bromocriptine; Bromocriptine mesylate; Bromocriptine a; α ergocryptine; Bromergol; Bromocriptine; Lysergic lactogen; Parlodel Pra Widdel
2.4 classification of drugs in endocrine system > hypothalamus and drugs affecting endocrine.
2.5 dosage form 1. Tablets: 1mg, 2mg, 5 mg;
2. Capsule: 5mg, 10mg.
2.6 pharmacological effects of bromocriptine bromocriptine is a specific dopamine receptor agonist in hypothalamus and pituitary gland, which can directly act on adenohypophysis and inhibit the secretion of prolactin. Like other dopamine receptor agonists, it can slightly increase hormone secretion in normal people, but it has the opposite effect on acromegaly patients, that is, it reduces growth hormone for a much longer time than levodopa, so it is valuable for treating this disease. It can also stimulate dopamine receptors in the extrapyramidal system, and effectively alleviate the tremor caused by surgical injury to the ventral median area of the tegmental part of the monkey brain stem, so it can be used to treat tremor paralysis. Bromocriptine can also stimulate dopamine receptors in organs innervated by autonomic nerves to play a corresponding role. However, unlike levodopa and dopamine, bromocriptine can stimulate not only dopamine receptors, but also adrenergic receptors A and B. Bromocriptine only specifically acts on dopamine receptors, but has no effect on adrenergic receptors A and B. Bromocriptine has little effect on uterus, but its vasoconstrictive effect is only 0.5% of ergotamine. In addition, bromocriptine can reduce the production of aldosterone. Bromocriptine can prevent and stop physiological lactation by antagonizing prolactin, accompanied by amenorrhea or anovulation and pathological prolactin increase. Bromocriptine is a dopamine receptor agonist. It mainly acts on D2 receptor, and has the functions of anti-tremor, inhibiting prolactin secretion and inhibiting growth hormone release. Low dose bromocriptine combined with compound levodopa can achieve good results in the treatment of early tremor paralysis. When they are used together, they have effects on presynaptic and postsynaptic neurons of DA system in substantia nigra and striatum, and can also excite synaptic receptors, so that the receptors can maintain normal functions, thus reducing the fluctuation of symptoms. When bromocriptine is used alone, the curative effect is not as good as levodopa, but better than diphenhydramine. It can also be used when levodopa is ineffective.
2.7 Pharmacokinetics of bromocriptine Oral absorption is rapid and good, and the absorption rate is about 28%. Due to extensive first-pass metabolism, the bioavailability is only 6%. The peak time of plasma concentration was 1 ~ 3h, and the concentration was directly proportional to the dose. After oral administration,1~ 2 hours played a prolactin-lowering role, and the duration was 8 ~1~ 3 hours, which was longer than that of levodopa. The plasma half-life is biphasic, 6.5 hours and 67.9 hours respectively. Almost all of them are metabolized by the liver in vivo, and the metabolic rate is 94%. After administration 120h, only a small amount (2.62%) was excreted in urine, and most (86.3%) was excreted in feces.
2.8 Indications of bromocriptine 1. Postpartum, spontaneous, neoplastic and drug-induced amenorrhea.
2. Menstrual disorder, infertility, secondary amenorrhea and ovulation reduction caused by prolactin.
3. Restrain lactation and prevent postpartum lactation and premature delivery.
4. postpartum * * * congestion, * * tenderness, * * * swelling pain, irritability.
5. Hypoandrogenemia caused by prolactin, such as erectile dysfunction and infertility caused by decreased * * *.
6. Adjuvant treatment of acromegaly and gigantism.
7. Bromocriptine is mainly used to fight Parkinson's disease. Treatment of early Parkinson's disease with compound levodopa. Used when levodopa is ineffective.
8. Adjuvant treatment of pituitary adenoma with acromegaly.
9. Used for hyperprolactinemia caused by prolactin tumor.
2.9 bromocriptine 1 contraindication. Those who are allergic to ergot preparations are prohibited.
2. Those with severe ischemic heart disease and peripheral vascular disease are prohibited.
3./kloc-Children under 0/5 are not allowed to enter.
4. Pregnant women and lactating women are prohibited.
5. It is forbidden to have a serious history of mental illness.
6. Have a history of hypertension or hypertension, and a past history of pregnancy-induced hypertension syndrome or pregnancy-induced hypertension.
7 acromegaly with ulcer or bleeding history.
2. 10 notes 1. After the pregnancy is confirmed, the drug should generally be stopped, but in the treatment of pregnant women with pituitary prolactin's tumor, the drug can still be continued to prevent the tumor from increasing during pregnancy.
2. Long-term and extensive research has not found that bromocriptine will increase the teratogenic rate of fetus.
3. The influence of drugs on the elderly: Clinical observation shows that the elderly are prone to adverse reactions of the central nervous system, which should be paid attention to.
4. Examination or monitoring before and after medication: (1) All patients with hyperprolactinemia should be examined by X-ray, CT or MRI before treatment to determine whether there is pituitary adenoma. If there is pituitary adenoma, we should follow up regularly (such as every year) during the treatment to understand the changes of pituitary adenoma. After 2 ~ 3 years of treatment, the follow-up interval of asymptomatic patients can be appropriately extended. (2) When it is used to inhibit mammary gland secretion after delivery, we should pay attention to the change of blood pressure, which is prone to hypotension. (3) When used to treat amenorrhea patients, pregnancy tests should be conducted regularly, especially for women who have stopped menstruation after menstruation recovery, and more attention should be paid to whether they are pregnant. (4) When treating infertility, female patients need to measure their basal body temperature every day, and the levels of serum follicle stimulating hormone, luteinizing hormone, urinary estrogen and urinary pregnane every month to monitor whether ovulation or pregnancy occurs. In addition, the basic level of serum prolactin should be determined regularly. Male patients, in addition to regularly measuring the serum levels of follicle stimulating hormone, luteinizing hormone and prolactin, should also measure the serum testosterone concentration every 3-6 months, and start to regularly detect the * * * number and * * * activity after 3 months of treatment. (5) When treating acromegaly, the concentration of serum growth hormone and/or serum insulin-like growth factor ⅰ should be determined, and the changes of related signs should be noted.
5. When taking large doses of drugs, it can reduce saliva secretion, and it is easy to suffer from dental caries, periodontitis and oral candida infection.
6. Taking it with food or after meals can reduce gastrointestinal adverse reactions.
7. Non-steroidal contraceptive methods should be used when contraception is needed during medication; If you suspect that you are pregnant, you should see a doctor immediately.
8. Those who are used to inhibit milk secretion after delivery are more prone to hypotension, so it is advisable to take medicine at least 4 hours after delivery, after the heart rate, blood pressure and breathing are stable.
9. When liver function damage occurs, reduce it.
10. When used to treat infertility, pituitary adenoma should be excluded first, because pituitary adenoma will expand in the sella turcica during pregnancy.
1 1. Used to treat amenorrhea or galactorrhea, it can produce short-term curative effect and should not be used for a long time.
12. Use with caution in patients with pituitary adenoma that has developed to the upper part of sella turcica, patients with obvious visual impairment, pregnant or possibly pregnant women, patients with liver injury, patients with peptic ulcer and previous gastrointestinal bleeding, and patients with mental illness.
13. if it is combined with levodopa, the curative effect can be improved, but when 10mg bromocriptine is used, the dosage of levodopa should be reduced by 12.5%.
14. bromocriptine can restore the normal ovulation function of women, and contraception should be paid attention to during medication.
15. At the initial stage of medication, blood pressure may drop, and attention should be paid to mechanical operation and application by vehicle drivers.
16. Adverse drug reactions are dose-related and vary greatly among individuals. After reducing the dose or stopping the drug, all the reactions can disappear. Therefore, it is necessary to observe closely after taking the medicine and adjust the dose at any time.
17. The combination of bromocriptine and ethanol can improve the body's sensitivity to ethanol and increase gastrointestinal adverse reactions. It is not advisable to drink alcohol during medication.
2. 1 1 bromocriptine adverse reactions 1. The incidence of adverse reactions of bromocriptine is above 60%, which is related to dose. With food, it may be reduced.
2. Nausea, vomiting, dizziness, orthostatic hypotension and even syncope can be seen at the beginning of medication.
3. It will cause vasospasm of lower limbs. Nasal congestion, erythematous limb pain, arrhythmia, angina pectoris, dry mouth, constipation, diarrhea, headache, drowsiness, hallucination, mania, depression, etc.
4. Parkinson's disease patients may have dyskinesia, and acromegaly patients may have gastrointestinal bleeding.
5. Long-term medication can cause reticular green spots on the skin, peritoneal fibrosis, pleural thickening and edema.
6. Mental illness, hallucination, delusion and insanity may occur when using a higher dose, but it may also occur when using a low dose.
2. The usage and dosage of 1 2 bromocriptine is1. Used to treat hypogonadism caused by postpartum lactation and hyperprolactinemia: at first, 2.5mg/kloc-0 once a day, taken after meals, gradually increased to 5-7.5 mg per day according to the clinical efficacy, taken 2-3 times after meals, and continued to treat until milk secretion stopped.
2. Used for postpartum mastitis: 2.5mg each time, twice a day, for 14 days.
3. For amenorrhea, functional menstrual disease and low fertility caused by galactorrhea or prolactin, 0. 125mg is given at first, 2-3 times a day, and if the effect is not obvious, it can be gradually increased to 0.25mg, 2-3 times a day after meals. Continue treatment until milk secretion stops. For amenorrhea, functional menstrual disease and low fertility, treatment should continue until menstruation returns to normal. If necessary, the treatment can last for several cycles to prevent recurrence.
4. For acromegaly: at first, take 1.25mg, 2-3 times a day after meals, and gradually increase to 5- 10 mg a day.
5. Used for paralysis agitans: the dosage varies greatly, and the dosage should be based on the decrease of growth hormone blood concentration. Take 1.25mg at first, 1 time a day after meals, and then increase 1.25mg every week. Generally, 10 ~ 40mg per day will achieve the maximum effect, and a comprehensive laboratory examination will be done every three months.
6. Inhibition of lactation: 0.25mg, twice a day, taken with food in the morning and evening, for a total of 14 days. Occasionally, a small amount of milk will be secreted after stopping taking the drug for 2-3 days, and it will stop after taking the same dose for several days.
7.* * * Postpartum congestion: Mild patients take 0.25mg orally, 1 hour, and repeat 1 time if they do not stop breastfeeding.
8. Hypoandrogenemia caused by prolactin: 5 ~ 10 mg per day.
9. Acromegaly: at first, it is 2.5mg per day, and after 7 ~ 14 days, it can be gradually increased to 10 ~ 20 mg per day according to the clinical efficacy, and taken with food for 4 times.
10. Premenstrual syndrome caused by prolactin increase: oral administration was started on the fourth day of menstrual cycle, with a daily dose of 1.25mg, and gradually increased to 2.5mg per day until menstrual cramps.
1 1. Postpartum lactation or lactation stop: 2.5mg each time, twice a day, continuously taking 14 days.
12. pituitary prolactin's adenoma (microadenoma, huge adenoma without surgical resection or postoperative residual adenoma): Take it from a small dose and gradually increase it. The general effective dose is 7.5 ~ 60 mg per day.
2. 13 drug interaction 1. When combined with levodopa in the treatment of Parkinson's disease, the curative effect of bromocriptine can be enhanced, so it should be reduced appropriately.
2. When it is combined with macrolides, the plasma concentration of bromocriptine can be increased, and symptoms of dopamine overdose can occur.
3. When combined with antihypertensive drugs, the antihypertensive effect can be enhanced, and the dosage of antihypertensive drugs should be reduced as appropriate.
4. Oral hormonal contraceptives can lead to amenorrhea or galactorrhea, which will interfere with the effect of bromocriptine and should not be used at the same time.
5. Haloperidol, methyldopa, monoamine oxidase inhibitor, metoclopramide, phenothiazine, reserpine and thiamine can increase the serum prolactin concentration and interfere with the effect of bromocriptine. When it is necessary to use together, the dosage of bromocriptine should be adjusted appropriately.
6. When combined with other ergot derivatives, it can aggravate the hypertension occasionally caused by bromocriptine, but it is rare.
7. When it is combined with alcohol, it may reduce the tolerance to drugs, so it is forbidden to drink alcohol during medication.
8. Styrene-butadiene antipsychotics or H2 receptor blockers combined with bromocriptine can increase the concentration of prolactin and decrease the curative effect.
2. 14 expert comments on bromocriptine's specific dopamine receptor agonist, which has dopamine-like effect and its function is similar to that of prolactin inhibitor secreted by hypothalamus, and can directly act on pituitary prolactin secretory cells, thus inhibiting prolactin secretion and reducing the prolactin level secreted by blood and breast. Clinically, it is used to prevent and terminate physiological lactation and accompanying amenorrhea and anovulation. When treating tremor paralysis, it has obvious effect on tremor, but its effect on reducing exercise and rigidity is far less than that of levodopa, so it is often used in combination with dopa preparation. Low dose bromocriptine combined with dopa preparation can achieve satisfactory curative effect in the early stage of tremor paralysis, and can also improve the curative effect in the late stage, reducing the dosage and adverse reactions of dopa preparation. The drug has the function of protecting neurons, and rarely produces motion fluctuation when used. Parkinson's disease is better than amantadine and trihexyphenidyl, and it is effective for rigidity and hyperactivity, and also for severe patients. It is often used in patients with poor efficacy or intolerance of levodopa. It is characterized by quick response and long duration. It can be used as a first-line drug for elderly patients with Parkinson's disease who are generally in good condition. However, due to its obvious adverse reactions, it was gradually replaced by other drugs.
3 bromocriptine poisoning bromocriptine (bromocriptine, bromocriptine, bromoergot cyclic peptide) is a polypeptide ergot alkaloid, semi-synthetic ergot alkaloid, which can excite the central dopamine D2 receptor at a general dose. Oral absorption is rapid, the plasma half-life is 15h, and the plasma protein binding rate is 90% ~ 96%. Can be used for treating Parkinson's disease, amenorrhea or galactorrhea, acromegaly, female infertility, etc. Bromocriptine is not the first choice when acute drug-induced extrapyramidal symptoms appear. When treating Parkinson's disease, 1.25mg, twice a day, and gradually increase the dose within 2 weeks to find the minimum dose with the best curative effect. Generally, the daily therapeutic dose is 20mg. If it is combined with levodopa, the anti-tremor effect can be improved. [ 1]
3. 1 clinical manifestations [2]
1. Adverse reactions include nausea, epigastric pain, dyspepsia and diarrhea.
2. In large doses, nervous system manifestations include headache, blurred vision, diplopia, lethargy, fatigue, hallucinations, mania, irritability, seizures and individual cerebrovascular accidents.
3. Occasional pulmonary infiltrative lesions, pleural effusion and thickening; Myopia and retroperitoneal fibrosis have been reported. Occasionally, cerebrospinal fluid rhinorrhea occurs. Rare leukopenia and thrombocytopenia.
4. About 10% have calf spasms, while those have erythromelalgia.
3.2 The diagnostic points of bromocriptine poisoning are [2]:
1. Have a history of taking bromine or taking it by mistake, and have the above clinical manifestations.
2. Eliminate the possibility of poisoning by other drugs.
3.3 treatment of bromocriptine poisoning treatment points for [2]:
1. When taking bromocriptine excessively, take medicinal charcoal orally and conduct catharsis treatment.
2. There is no specific antidote, mainly symptomatic and supportive treatment.
3. When impotence occurs, reducing or stopping drugs can restore sexual function as usual.