Drug information of Bromocriptine

Bromocriptine


Bromocriptine belongs to the group of medicines known as ergot alkaloids. Bromocriptine blocks the release of a hormone called prolactin from the pituitary gland.
Bromocriptine is used to treat certain menstrual problems (e.g., amenorrhea) in women and stops milk production in some men and women who have abnormal milk leakage.
It is also used to treat infertility in both men and women that occurs because the body is making too much prolactin.
Bromocriptine is also used to treat acromegaly (overproduction of growth hormone) and pituitary prolactinomas (tumors of the pituitary gland).
Bromocriptine is also used to treat the signs and symptoms of Parkinson's disease , often in combination with levodopa .
Bromocriptine is also used together with a proper diet and exercise to treat high blood sugar levels in patients with type 2 diabetes .

Mechanism of effect

Semisynthetic ergot alkaloid, dopamine receptor agonist, inhibits prolactin secretion, and lowers blood levels of growth hormone in acromegaly
Quick-release formulation of bromocriptine (Cycloset) is thought to act on circadian neuronal activities within the hypothalamus to reset abnormally elevated hypothalamic drive for increased plasma glucose, triglyceride, and free fatty acid levels in fasting and postprandial states in patients with insulin-resistant

Pharmacodynamic

Bromocriptine is a dopamine agonist. It works by blocking the release of prolactin from the pituitary gland. It also works by lowering growth hormone levels in patients with acromegaly.
In Parkinson disease , bromocriptine works by stimulating dopamine receptors in certain parts of the brain.

Pharmacokinetics

Half-life elimination : 4-4.5 hr (initial phase); 8-20 hr (terminal phase)
Excretion : 85% feces (via biliary elimination); urine (2.5-5.5%)
Protein bound : 90-96% (to albumin)
Peak plasma time : 1-3 hr
Vd : 61L
Absorption : 28% from GI tract
Bioavailability : 28% (parlodel); 65-95% (cycloset)
Metabolism : Completely in liver, principally by hydrolysis of the amide bond to produce lysergic acid and a peptide fragment

Drug indications

Parkinson's Disease , Acromegaly

Dosage

Hyperprolactinemia
- Initial: 1.25 mg to 2.5 mg orally daily.
- Titration: Add 2.5 mg orally, as tolerated, to the treatment dosage every 2 to 7 days.
- Maintenance: 2.5 mg to 15 mg orally daily.
Acromegaly - Initial: 1.25 mg to 2.5 mg orally once daily, with food, at bedtime for 3 days.
- Titration: Add 1.25 mg to 2.5 mg orally, as tolerated, to the treatment dosage every 3 to 7 days.
- Maintenance: 20 mg to 30 mg orally daily
- The maximum dosage should not exceed 100 mg/day.
Parkinson's Disease
- Initial: 1.25 mg twice daily with meals.
- Titration: Add 2.5 mg/day, with meals, to dosage regimen every 14 to 28 days.
- Maximum dosage: 100 mg/day.
Diabetes Type 2
For the Cycloset (R) trade name of bromocriptine only:
- Initial: 0.8 mg orally daily taken within two hours after waking in the morning with food
- Titration: Increase by 0.8 mg weekly as tolerated
- Maintenance: 1.6 to 4.8 mg orally daily taken within two hours after waking in the morning with food
- The maximum dosage should not exceed 4.8 mg daily.
Neuroleptic Malignant Syndrome (Off-label)
2.5-5 mg PO 2-3 times/day; not to exceed 45 mg/day

Drug contraindications

Lactation , diabetic ketoacidosis

Alerts

• Tell your doctor or pharmacist if you have recently given birth and you also have a history of heart blood vessel problems or other severe heart or blood vessel problems (eg, stroke, high or low blood pressure) ; kidney or liver problems; lung or breathing problems (eg, asthma); stomach ulcers; or stomach or bowel bleeding
• Use with caution in patients with cardiovascular disease, dementia, hepatic impairment, and peptic ulcer disease
• Effectiveness and safety are unknown in patients already taking dopamine receptor agonists for other indications; concomitant use not recommended
Bromocriptine should be used with extreme caution in CHILDREN younger than 11 years old; safety and effectiveness in these children have not been confirmed.
• Bromocriptine may decrease the effectiveness of your birth control pill. To prevent pregnancy, be sure to use an additional form of birth control (eg, condoms) while using bromocriptine.
• Patients with Parkinson disease may have an increased risk of developing a certain type of skin cancer (melanoma). It is not known if bromocriptine also increases the risk of melanoma. You may need to have skin exams while you are using bromocriptine.
• Some people have experienced new, unusual, or increased urges (eg, gambling, sexual urges) while taking bromocriptine. Tell your doctor right away if you notice such effects.

Points of recommendation

• Take bromocriptine with food.
Bromocriptine may cause drowsiness, dizziness, or light-headedness. These effects may be worse if you take it with alcohol or certain medicines. Use bromocriptine with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.
• Do not drink alcohol while you are using bromocriptine.
• Check with your doctor before you use medicines that may cause drowsiness (eg, sleep aids, muscle relaxers) while you are using bromocriptine; it may add to their effects. Ask your pharmacist if you have questions about which medicines may cause drowsiness.
• Do not suddenly stop taking bromocriptine. Some conditions may become worse when bromocriptine is suddenly stopped. Your dose may need to be slowly lowered by your doctor to avoid side effects (eg, fever, stiff muscles, confusion, abnormal thinking, fast or irregular heartbeat, sweating).

Pregnancy level

B


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