Bromocriptine

Trade name: parlodelClass: Antiparkinson agent

Dosage form availableDosage form available

TabletTablet:1 mg,2.5 mg:1 mg,2.5 mg . .

CapsuleCapsule: 5 mg ,10 mg: 5 mg ,10 mg. .

Pharmacology

Stimulates dopamine receptors in brain, relieving parkinsonian symptoms. Inhibits prolactin, which is responsible for lactation, and lowers elevated blood levels of growth hormone in acromegaly. The mechanism in glycemic control is unknown..

Pharmacokinetic data

Absorption of oral dose absorbed 28%

Distribution

to 96% bound to serum albumin 90

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 and Usage

*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

Dose

 1 -Prevention or suppression of lactation 2.5 mg on day 1 (prevention) or daily for 2–3 days (suppression); then 2.5 mg twice daily for 14 days

2-Hypogonadism, galactorrhoea, infertility,

initially 1–1.25 mg at bedtime, increased gradually; usual dose 7.5 mg daily in divided doses, increased if necessary to max. 30 mg daily, usual dose in infertility without hyperprolactinaemia, 2.5 mg twice daily.

3-Acromegaly, initially 1–1.25 mg at bedtime, increase gradually to 5 mg every 6 hours

4-Prolactinoma, initially 1–1.25 mg at bedtime; increased gradually to 5 mg every 6 hours (occasional patients may require up to 30 mg daily)

5-child under 15 years, not recommended

Contraindications

*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 Reactions

CardiovascularPostural/orthostatic hypotension , syncope ,cardiac valvulopathy, hypertension, MI,

stroke CNSHeadache, dizziness , fatigue , light-headedness , somnolence ,drowsiness ,confusion, hallucinations, psychomotor agitation,

psychotic disorders, seizures EENTRhinitis , sinusitis ,amblyopia dry mouth/nasal stuffiness

MetabolicHypoglycemia

RespiratoryConstrictive pericarditis, pleural and pericardial effusion, pleural and pulmonary fibrosis, pleural thickening GINausea , constipation , diarrhea ,dyspepsia , vomiting anorexia ,abdominal cramps , GI bleeding

Drugs ineraction

CYP3A4 strong inhibitors (eg, azole antifungals, protease inhibitors) Pharmacologic and toxic effects of bromocriptine may beincreased. Coadminister with caution

Dopamine antagonists (eg, butyrophenones, metoclopramide, phenothiazine 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

May have additive vasoconstrictive effects.

Avoid concomitant use

General Advice

**Give with milk or meals to reduce gastric distress……

**Initial dose of Parlodel is usually given at bedtime because of adverse CNS reactions (eg,

dizziness, fainting).