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Bromocriptine is a D2 receptor agonist, which activates postsynaptic dopamine receptors and partially antagonizes the D1 receptor. Bromocriptin drug is indicated in many diseases such as prolactin-secreting adenomas, acromegaly, Parkinson's,...
1. Uses of Bromocriptin
Bromocriptin (an ergot derivative) is a D2 receptor agonist, which activates postsynaptic dopamine receptors and partially antagonizes the D1 receptor. Bromocriptin has the ability to decrease prolactin levels by inhibiting prolactin secretion from the anterior pituitary by direct action on the pituitary gland and/or stimulation of dopamine receptors in the hypothalamus. Bromocriptin reduces prolactin levels in the blood, thereby restoring ovulation and ovarian function in patients with amenorrhea, and inhibits physiological and pathological lactation in patients with gonadotropin levels and ovarian function. full.
In addition, Bromocriptin also reduces the rate of prolactin-dependent tumor growth. The drug temporarily increases the secretion of growth hormone in subjects with normal levels but rapidly decreases in acromegaly.
In the treatment of Parkinson's disease, Bromocriptin's effectiveness is due to direct stimulation of dopamine receptors in the striatum. For the treatment of type 2 diabetes, the mechanism of action of Bromocriptin is still unknown. However, Bromocriptin is thought to be able to affect the body's circadian rhythms. Bromocriptin (when administered in the morning and rapidly released into the systemic circulation) can re-establish the biological activities of the hypothalamus that are altered by obesity, thereby leading to a reversal of insulin resistance. , reducing glucose production without increasing serum insulin levels
2. Indications for Bromocriptine
Bromocriptin is indicated in the following cases:
Patients with dysfunction associated with hyperprolactinemia (including amenorrhea), with or without lactation, infertility or hypogonadism in both men and women; prolactin-secreting gland tumor. The patient has acromegaly. Patients with Parkinson's disease. Relieves premenstrual symptoms such as swelling, breast discomfort, weight gain, migraines, mood swings. Treatment of infertility in men with low semen volume but no hyperprolactinemia. Note that Bromocriptin should not be used if the patient is still responding to conventional treatments. Combination with tranquilizers (Haloperidol) for the treatment of neuroleptic malignant syndrome.
3. Contraindications of Bromocriptine
Bromocriptin is contraindicated in the following cases:
Uncontrolled hypertension and hypersensitivity to ergot alkaloids. Patients being treated for hyperprolactinemia must discontinue bromocriptin during pregnancy. If bromocriptin is reintroduced to control fast-growing adenomas in pregnant women with hypertension, the benefits and risks must be weighed before deciding whether to use the drug.
4. Dosage of Bromocriptine
Bromocriptine dose depends on the type of disease and the severity of the disease. The following is a reference dose in some cases:
Hyperprolactinemia: The recommended initial dose of Bromocriptin is 1.25-2.5 mg/day, which can be increased by 2.5 mg/day, every 3-7 days, for until the optimal treatment effect is achieved. The usual dose is 5-7.5mg/day. In some patients with amenorrhea and/or increased lactation, a dose of 30 mg/day may be required.
Parkinson's syndrome: The starting dose is 1.25mg / time x 2 times / day. During titration, results should be evaluated every 2 weeks to determine the lowest effective dose. If necessary, the dose may be increased every 14-28 days in increments of 2.5 mg/day to a maximum of 100 mg/day. The usual dose in the treatment of Parkinson's is 30-90mg/day, divided into 3 doses, elderly patients need a lower dose.
Acromegaly: The recommended starting dose is 1.25-2.5mg daily for 3 days. The dose may be increased by 1.25-2.5 mg/day, every 3-7 days until the desired therapeutic effect is achieved. The usual dose of Bromocriptine is 20-30 mg/day in most patients.
Reduce premenstrual symptoms: Use 2.5-7.5mg / time x 2 times / day from the 14th day of the cycle until menstruation.
Neuroleptic malignant syndrome: Dose 2.5-5mg/time x 2-6 times/day in combination with other neuroleptic drugs.
5. Bromocriptine side effects
Patients using Bromocriptin may experience the following side effects:
Frequency > 10%:
Gastrointestinal: Constipation, nausea; Nervous system: Dizziness, headache; Neuromuscular: Asthenia; Respiratory: Rhinitis. Frequency 1 to 10%:
Cardiovascular: Orthostatic hypotension, Raynaud's disease, syncope, vasospasm; Endocrine and metabolic: Hypoglycemia; Gastrointestinal: Abdominal cramps, bloating, anorexia, diarrhea, dyspepsia, gastrointestinal bleeding, vomiting, digestive disorders; Nervous system: Drowsiness; Ophthalmology: Decreased vision ; Respiratory: Nasal congestion, sinusitis. Frequency <1%:
Cardiovascular: Arrhythmia, syncope, ventricular tachycardia; Dermatology: Hair loss, paleness; Nervous system: Delusions, heaviness in the head, insomnia, lethargy, coma, paranoia, paresthesia, sleep disturbance, ear tingling, hallucinations; Neuromuscular: Muscle cramps; Respiratory: Difficulty breathing. Frequency not determined:
Cardiovascular: Neuropathic pain, hypotension; Dermatology: Spotty skin, skin rash; Genitourinary: Frequent urination, urinary incontinence, urinary retention; Nervous system: Ataxia, auditory hallucinations, confusion, depression, fatigue, involuntary body movements, nervousness, nightmares, sudden sleep.
6. Notes when using Bromocriptin
When using Bromocriptin, patients should be aware of the following issues:
Fibrosis of the heart valves: Erectile dysfunction derivatives have been associated with valve thickening, often associated with long-term, chronic use count. Cardiovascular effects: Hypotension, including orthostatic hypotension and syncope, may occur, particularly at initiation and dose increases. In addition, hypertension, seizures, and stroke have been reported. Severe headaches or visual changes may precede these events. Use with caution in patients with cardiovascular disease (myocardial infarction, atrial, nodal or ventricular arrhythmias). Central nervous system depression: May cause CNS depression, reduce physical or mental capacity, cause sudden sleep episodes especially in Parkinson's patients. Hallucinations: Visual or auditory hallucinations may occur when used alone or concurrently with Levodopa. Symptoms may persist for several weeks after stopping the drug. Impulse Control Disorders: Dopamine agonists used for Parkinson's disease or restless legs syndrome are associated with compulsive behavior and/or loss of impulse control, manifesting as an appearance or increase gambling, sexual desire, uncontrolled spending or other intense urges. Reducing the dose or stopping treatment will reverse these behaviors in some cases. Pleural fibrosis: Cases of pleural and pericardial effusion, as well as pleural and/or retroperitoneal fibrosis have been reported with prolonged, high-dose daily use. Discontinue treatment if the above events are suspected. Dementia: Use with caution in patients with dementia as high doses may be associated with confusion and psychosis. Hepatic impairment: Use with caution in patients with hepatic impairment. Peptic ulcer disease: Use with caution in patients with peptic ulcer disease because serious gastrointestinal bleeding has been reported (some fatal). Prolactin-secreting adenomas: CSF bleeding has been observed in some of these patients. Psychiatric Disorders: Use with caution in psychotic patients. Dopamine agonists may worsen the disorder or reduce the effectiveness of medications used to treat psychosis. Not recommended for use in patients with severe mental disorders. Pregnancy: Bromocriptine is not recommended during pregnancy. However, in patients with pituitary tumors, some evidence supports the use of bromocriptin for the prevention or treatment of tumors that develop during pregnancy. Lactation: Bromocriptine has an inhibitory effect on lactation. Therefore, the drug should not be used during lactation. Above is information about uses, dosage and precautions when using Bromocriptine. Patients should not self-medicate, but should consult a doctor or pharmacist before use.
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