Bromocriptine

PHARMACOLOGY:
  • Stimulates dopamine receptors in brain, relieving parkinsonian symptoms. 
  • Paminergic & Dopamine agonist
  • Inhibits prolactin, which is responsible for lactation, and lowers elevated blood levels of growth hormone in acromegaly. 
  • The mechanism in glycemic control is unknown.
DOSES FORM:
  • Tablet:1 mg,2.5 mg.
  • Capsule: 5 mg ,10 mg .
PHARMACOKINETICS:                                                     

Absorption 28% of oral dose absorbed
Distribution 90 to 96% bound to serum albumin
Metabolism Primarily metabolized in the GI tract and liver (CYP3A4). Undergoes extensive first-pass metabolism
Elimination Major elimination route is hepatic; 6% is renally eliminated. Terminal half-life of 15 h
Onset 1-2 h

INDICATIONS:
  • Treatment of hyperprolactinemia-associated disorders (eg, amenorrhea with or without galactorrhea, infertility, hypogonadism).
  • In patients with prolactin-secreting adenomas treatment of acromegaly
  • Therapy for Parkinson disease (idiopathic or postencephalitic)
  • Therapy for type 2 diabetes
  • Hepatic Coma
  • Cyclical mastalgia
CONTRAINDICATION:
  • Hypersensitivity to bromocriptine, ergot alkaloids or ergot-related drugs, or any component of the product; breast-feeding.
  • They should also be avoided in pre-eclampsia
  • Uncontrolled hypertension; pregnancy postpartum period in women with a history of coronary artery disease or severe CV conditions
ADVERSE REACTION:
  • Cardiovascular
  • Postural/orthostatic hypotension , syncope ,cardiac valvulopathy, hypertension, MI, stroke
CNS
  • Headache, dizziness , fatigue , light-headedness , somnolence ,drowsiness ,confusion, hallucinations, psychomotor agitation, psychotic disorders, seizures
ENT
  • Rhinitis , sinusitis ,amblyopia dry mouth/nasal stuffiness
Metabolic
  • Hypoglycemia
Respiratory
  • Constrictive pericarditis, pleu
  • ral and pericardial effusion, pleural and pulmonary fibrosis, pleural thickening
GI
  • Nausea , constipation , diarrhea ,dyspepsia , vomiting anorexia ,abdominal cramps , GI bleeding
DRUG INTERACTION:
  1. CYP3A4 strong inhibitors (eg, azoleantifungals, protease inhibitors)
  2. Pharmacologic and toxic effects of bromocriptine may beincreased. Coadminister with caution
  3. Dopamine antagonists (eg, butyrophenones, metoclopramide, phenothiazine
  4. Dopamine antagonists may reduce bromocriptine efficacy; bromocriptine may reduce effectiveness of dopamine antagonists. Concurrent use is not recommended
Ergot drugs (eg, ergotamine)
  • Coadministration may increase occurrence of ergot-related side effects (eg, fatigue, nausea, vomiting) and may reduce effectiveness of ergot drugs when used to treat migraines.
  • Concomitant use is not recommended.
Erythromycin, octreotide
  • May increase bromocriptine serum levels
Ethanol
  • May potentiate adverse effects of bromocriptine
  • Highly protein—bound drugs (eg, chloramphenicol, probenecid, salicylates, sulfonamides)
  • Bromocriptine may increase the unbound fraction of other concomitantly used highly protein—bound drugs
  • Methyldopa Hypotensive effects may be increased
  • Triptans (eg,sumatriptan)
  1. May have additive vasoconstrictive effects.
  2. Avoid concomitant use 
Exam Question
  • Prolactinoma is treated with Alpha-Bromocriptine
  • Bromocriptine is paminergic agonists used for parkinsonism which has the potential to cause retroperitoneal fibrosis
  • Bromocriptine therapy for mother is Contraindication to breast milk feeding
  • To suppress lactation in mother with rheumatic fever, Rx of choice is Bromocriptine 
  • Bromocriptine is Dopamine agonist that Decreases prolactin release
  • Bromocriptine is indicated in Prolactin -secreting adenomas,Amenorrhea - Galactorrhea & Acromegaly
  • A young women with secondary amenorrhea and galactorrhea. MRI shows a tumour of < lOmm diameter in the pituitary fossa. Treatment is Bromocriptine 
  • Bromocriptine is used in Type II DM,Hepatic Coma & Cyclical mastalgia
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