Bromocriptine

Pronunciation

(broe moe KRIP teen)

U.S. Brand Names

Parlodel®

Synonyms

Bromocriptine Mesylate

Generic Available

Yes: Tablet

Canadian Brand Names

Apo-Bromocriptine®; Parlodel®; PMS-Bromocriptine

Use

Amenorrhea with or without galactorrhea; infertility or hypogonadism; prolactin-secreting adenomas; acromegaly; Parkinson's disease

A previous indication for prevention of postpartum lactation was withdrawn voluntarily by Sandoz Pharmaceuticals Corporation.

Use - Unlabeled/Investigational

Neuroleptic malignant syndrome

Pregnancy Risk Factor

Lactation

Enters breast milk/contraindicated

Contraindications

Hypersensitivity to bromocriptine, ergot alkaloids, or any component of the formulation; ergot alkaloids are contraindicated with potent inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics); uncontrolled hypertension; severe ischemic heart disease or peripheral vascular disorders; pregnancy (risk to benefit evaluation must be performed in women who become pregnant during treatment for acromegaly, prolactinoma, or Parkinson's disease - hypertension during treatment should generally result in efforts to withdraw)

Warnings/Precautions

Use with caution in patients with impaired renal or hepatic function, a history of psychosis, or cardiovascular disease (myocardial infarction, arrhythmia). Patients who receive bromocriptine during and immediately following pregnancy as a continuation of previous therapy (ie, acromegaly) should be closely monitored for cardiovascular effects. Discontinuation of bromocriptine in patients with macroadenomas has been associated with rapid regrowth of tumor and increased prolactin serum levels. Use with caution in patients with a history of peptic ulcer disease, dementia, or concurrent antihypertensive therapy. Pleural and peritoneal fibrosis have been reported with prolonged daily use. Cardiac valvular fibrosis has also been associated with ergot alkaloids. Safety and effectiveness in patients <15 years of age have not been established.

Adverse Reactions

>10%:

Central nervous system: Headache, dizziness

Gastrointestinal: Nausea

1% to 10%:

Cardiovascular: Orthostatic hypotension

Central nervous system: Fatigue, lightheadedness, drowsiness

Gastrointestinal: Anorexia, vomiting, abdominal cramps, constipation

Respiratory: Nasal congestion

<1%: Arrhythmias, hair loss, insomnia, paranoia, visual hallucinations

Overdosage/Toxicology

Symptoms of overdose include nausea, vomiting, and hypotension. Treatment is symptomatic and supportive.

Drug Interactions

Substrate of CYP3A4 (major); Inhibits CYP1A2 (weak), 3A4 (weak)

Antifungals, azole derivatives (itraconazole, ketoconazole) increase levels of ergot alkaloids by inhibiting CYP3A4 metabolism, resulting in toxicity; concomitant use is contraindicated.

Antipsychotics: May diminish the effects of bromocriptine (due to dopamine antagonism); these combinations should generally be avoided.

CYP3A4 inhibitors: May increase the levels/effects of bromocriptine. Example inhibitors include azole antifungals, ciprofloxacin, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, and verapamil.

Macrolide antibiotics: Erythromycin, clarithromycin, and troleandomycin may increase levels of ergot alkaloids by inhibiting CYP3A4 metabolism, resulting in toxicity (ischemia, vasospasm); concomitant use is contraindicated.

MAO inhibitors: The serotonergic effects of ergot derivatives may be increased by MAO inhibitors. Monitor for signs and symptoms of serotonin syndrome.

Metoclopramide: May diminish the effects of bromocriptine (due to dopamine antagonism); concurrent therapy should generally be avoided.

Protease inhibitors (ritonavir, amprenavir, indinavir, nelfinavir, and saquinavir) increase blood levels of ergot alkaloids by inhibiting CYP3A4 metabolism, acute ergot toxicity has been reported; concomitant use is contraindicated.

Serotonin agonists: Concurrent use with bromocriptine may increase the risk of serotonin syndrome (includes buspirone, SSRIs, TCAs, nefazodone, sumatriptan, and trazodone).

Sibutramine: May cause serotonin syndrome; concurrent use with ergot alkaloids is contraindicated.

Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may increase GI side effects or ethanol intolerance).

Herb/Nutraceutical: St John's wort may decrease bromocriptine levels.

Mechanism of Action

Semisynthetic ergot alkaloid derivative and a dopamine receptor agonist which activates postsynaptic dopamine receptors in the tuberoinfundibular and nigrostriatal pathways

Pharmacodynamics/Kinetics

Protein binding: 90% to 96%

Metabolism: Primarily hepatic

Half-life elimination: Biphasic: Initial: 6-8 hours; Terminal: 50 hours

Time to peak, serum: 1-2 hours

Excretion: Feces; urine (2% to 6% as unchanged drug)

Dosage

Oral:

Children: Prolactin-secreting adenoma:

11-15 years (based on limited information): Initial: 1.25-2.5 mg daily; dosage may be increased as tolerated to achieve a therapeutic response (range 2.5-10 mg daily).

16 years: Refer to Adults dosing

Adults:

Parkinsonism: 1.25 mg 2 times/day, increased by 2.5 mg/day in 2- to 4-week intervals (usual dose range is 30-90 mg/day in 3 divided doses), though elderly patients can usually be managed on lower doses

Neuroleptic malignant syndrome: 2.5-5 mg 3 times/day

Hyperprolactinemia: 2.5 mg 2-3 times/day

Acromegaly: Initial: 1.25-2.5 mg increasing as necessary every 3-7 days; usual dose: 20-30 mg/day

Prolactin-secreting adenomas: Initial: 1.25-2.5 mg/day; may be increased as tolerated every 2-7 days until optimal response (range: 2.5-15 mg/day)

Dosing adjustment in hepatic impairment: No guidelines are available, however, may be necessary

Monitoring Parameters

Monitor blood pressure closely as well as hepatic, hematopoietic, and cardiovascular function

Dietary Considerations

May be taken with food to decrease GI distress.

Patient Education

Take exactly as directed (may be prescribed in conjunction with levodopa/carbidopa); do not change dosage or discontinue without consulting prescriber. Therapeutic effects may take several weeks or months to achieve and you may need frequent monitoring during first weeks of therapy. Take with meals if GI upset occurs, before meals if dry mouth occurs, after eating if drooling or if nausea occurs. Take at the same time each day. Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake; void before taking medication. Do not use alcohol, prescription or OTC sedatives or CNS depressants without consulting prescriber. Urine or perspiration may appear darker. You may experience drowsiness, dizziness, confusion, or vision changes (use caution when driving, climbing stairs, or engaging in tasks requiring alertness until response to drug is known); orthostatic hypotension (use caution when rising from sitting or lying position); constipation (increased exercise, fluids, fruit, or fiber may help); nasal congestion (consult prescriber for appropriate relief); or nausea, vomiting, loss of appetite, or stomach discomfort (small, frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help). Report unresolved constipation or vomiting; chest pain or irregular heartbeat; acute headache or dizziness; CNS changes (eg, hallucination, loss of memory, seizures, acute headache, nervousness), painful or difficult urination; increased muscle spasticity, rigidity, or involuntary movements; skin rash; or significant worsening of condition. Breast-feeding precaution: Do not breast-feed.

Additional Information

Usually used with levodopa or levodopa/carbidopa to treat Parkinson's disease. When adding bromocriptine, the dose of levodopa/carbidopa can usually be decreased.

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Orthostatic hypotension.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

Drowsiness is common; may cause hallucinations

Mental Health: Effects on Psychiatric Treatment

Used to treat neuroleptic malignant syndrome and cocaine abuse; fluvoxamine and nefazodone may increase bromocriptine concentrations; monitor for hypotension, headache, nausea

Dosage Forms

Capsule, as mesylate: 5 mg

Tablet, as mesylate: 2.5 mg

References

Dackis CA and Gold MS, "Bromocriptine as Treatment of Cocaine Abuse," Lancet , 1985, 1(8438):1151-2.

de Groot AN, van Dongen PW, Vree TB, et al, "Ergot Alkaloids. Current Status and Review of Clinical Pharmacology and Therapeutic Use Compared With Other Oxytocics in Obstetrics and Gynaecology," Drugs , 1998, 56(4):523-35.

Koller WC, Silver DE, and Lieberman A, "An Algorithm for the Management of Parkinson's Disease," Neurology , 1994, 44(12 Suppl 10):1-52.

Lejoyeux M, et al, "Serotonin Syndrome: Incidence, Symptoms, and Treatment," CNS Drugs , 1994, 2:132-43.

Melmed S and Braunstein GD, "Bromocriptine and Pleuropulmonary Disease," Arch Intern Med , 1989, 149(2):258-9.

Morgans D, "Re: Parlodel," Aust N Z J Obstet Gynaecol , 1995, 35(2):228-9.

Mueller PS, Vester JW, and Fermaglich J, "Neuroleptic Malignant Syndrome. Successful Treatment With Bromocriptine," JAMA , 1983, 249(3):386-8.

Parkes D, "Drug Therapy: Bromocriptine," N Engl J Med , 1979, 301(16):873-8.

Stern MB, "Contemporary Approaches to the Pharmacotherapeutic Management of Parkinson's Disease: An Overview," Neurology , 1997, 49(1 Suppl 1):2-9.

Watts RL, "The Role of Dopamine Agonists in Early Parkinson's Disease," Neurology , 1997, 49(1 Suppl 1):34-48.

International Brand Names

Alpha-Bromocriptine® (NZ); Apo-Bromocriptine® (CA, NZ, SG, TR, ZA); Axialit® (AR); Bagren® (BR); Brameston® (CY, EC); Brocriptin® (RO); Bromcriptin® (RO); Bromed® (AT); Bromergon® (DK, HR, PL, RU, SI, TH); Bromocorn® (PL); Bromocrel® (DE); Bromocriptin AbZ® (DE); Bromocriptina Dorom® (IT, RO); Bromocriptin AZU® (DE); Bromocriptin beta® (DE); Bromocriptin® (DE, RO, RU); Bromocriptine-BC (AU); Bromocriptine® (GB); Bromocriptine-Richter® (BD); Bromocriptin-ratiopharm® (DE); Bromocriptin-Richter® (HU, SG); Bromocriptin Sandoz® (DE); bromocriptin-TEVA® (DE); bromocriptin von ct® (DE); Bromohexal® (AU); Bromo-Kin® (FR); Bromokriptin® (YU); Bromolactin® (AU); Bromtine® (BD); Butin YSP® (SG); Criten® (CL); Elkrip® (ID); Ergolaktyna® (PL); Galaktomin® (TR); Grifocriptina® (CL); Gynodel® (TR); kirim® (DE); kirim gyn® (DE); Kriptonal® (CL); Kripton® (AU); Medocriptine® (BG, CZ, HK, RO); Met. Sulf. Bromergocriptina® (RO); Parilac® (IL); Parlodel® (AR, AT, AU, BD, BE, BG, BR, CA, CH, CL, CO, CZ, DK, ES, FI, FR, GB, HK, HR, ID, IE, IL, IT, LK, MT, MX, NL, NO, NZ, PL, PT, RO, RU, SG, TH, TR); Patrinel® (AR); PMS-Bromocriptine (CA); Pravidel® (DE, SE); Ronalin® (EG, JO, KW, LB, RO, SY); Serocryptin® (AR, HK, HU, ID, MX, RO, RU); Sicriptin® (IN); Sintiacrin® (AR); Suplac® (SG, TH); Syntocriptine® (HK); Umprel® (AT, CL)

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