bromocriptine (Rx)

Brand and Other Names:Cycloset, Parlodel
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet (Parlodel)

  • 2.5mg

capsule (Parlodel)

  • 5mg

tablet (Cycloset)

  • 0.8mg
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Hyperprolactinemia-Associated Dysfunctions (Parlodel)

Indicated for treatment of dysfunctions associated with hyperprolactinemia including amenorrhea with or without galactorrhea, infertility or hypogonadism; also indicated in patients with prolactin-secreting adenomas

1.25-2.5 mg PO qDay initially; may increase by 2.5 mg/day q2-7Days until optimal therapeutic response achieved

Usual therapeutic dosage ranges from 2.5-15 mg/day

Up to 30 mg/day has been used in some patients with amenorrhea and/or galactorrhea

Parkinson Disease (Parlodel)

Indicated as adjunctive treatment to levodopa for the signs and symptoms of idiopathic/postencephalitic Parkinson disease

1.25 mg PO q12hr initially; may increase dose by 2.5 mg/day q2-4Weeks until optimal therapeutic response achieved

Safety >100 mg/day not established

Acromegaly (Parlodel)

Indicated for acromegaly

1.25-2.5 mg PO qHS for 3 days initially; may increase by 1.25-2.5 mg/day q3-7Days until optimal therapeutic response achieved

Not to exceed 100 mg/day

Type 2 Diabetes Mellitus (Cycloset)

Quick release formulation (Cycloset) is the only bromocriptine product indicated for diabetes mellitus type 2 as adjunct to diet and exercise to improve glycemic control

0.8 mg PO qDay initially; may increase by 0.8-mg increments qWeek as tolerated

Usual dosage ranges between 1.5-4.8 mg PO qDay; not to exceed 4.8 mg (6 tablets)/day

Note: Cycloset is not indicated for hyperprolactinemia, Parkinson disease, or acromegaly

see Dosage Modifications (Cycloset) and Administratio (Cycloset)

Neuroleptic Malignant Syndrome (Off-label, Parlodel)

2.5-5 mg PO 2-3 times/day; not to exceed 45 mg/day

[Strawn JR, Keck PE Jr, and Caroff SN, "Neuroleptic Malignant Syndrome," Am J Psychiatry, 2007, 164(6):870-6]

Dosage Modifications

Hepatic impairment: Safety and efficacy has not been established; dosage adjustment may be necessary due to extensive hepatic metabolism; use with caution

Renal impairment: Safety and efficacy has not been established

Cycloset

  • Concomitant use with CYP3A4 inhibitor
    • Strong CYP3A4 inhibitor (eg, azole antimycotics, HIV protease inhibitors): Avoid use; ensure adequate washout of the strong CYP3A4 inhibitor drug before initiating Cycloset treatment
    • Moderate CYP3A4 inhibitor (eg, erythromycin): Dose should not exceed 1.6 mg PO qDay

Dosing Considerations

Dosage forms for Cycloset and Parlodel and not interchangeable

Cycloset

  • Limitations of use
    • Not for treatment of type 1 diabetes or diabetic ketoacidosis
    • Limited efficacy data in combination with thiazolidinediones
    • Efficacy has not been confirmed in combination with insulin

Parlodel

  • Patients treated with pituitary irradiation should be withdrawn from Parlodel therapy on a yearly basis to assess both the clinical effects of radiation on the disease process and effects of Parlodel therapy; usual withdrawal period range, 4-8 weeks; recurrence of the signs/symptoms or increases in growth hormone indicate the disease is still active and further courses of Parlodel should be considered

Dosage Forms & Strengths

tablet (Parlodel)

  • 2.5mg

capsule (Parlodel)

  • 5mg
more...

Hyperprolactinemia (Parlodel)

≤10 years: Safety and efficacy not established

11-15 years: 1.25-2.5 mg PO qDay initially; therapeutic dosage ranges from 2.5-10 mg/day; may need to increase dose for optimal therapeutic response

≥16 years: Safety and efficacy not established

see Administration (Parlodel)

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Interactions

Interaction Checker

and bromocriptine

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            Adverse Effects

            >10%

            Cycloset

            • Monotherapy
              • Nausea (32.5 %)
              • Rhinitis (13.8%)
              • Headache (12.5%)
              • Asthenia (12.5%)
              • Dizziness (12.5%)
              • Constipation (11.3%)
            • Adjunct to sulfonylurea
              • Nausea (25.4%)
              • Asthenia (18.9%)
              • Headache (16.8%)
              • Dizziness (11.9%)
              • Rhinitis (10.7%)
            • Adjunct to diet or ≤2 antidiabetic medications (eg, metformin, insulin secretagogues, and/or insulin)
              • Nausea (32.2%)
              • Dizziness (14.8%)
              • Fatigue (13.9%)
              • Headache (11.4%)

            Parlodel

            • Hyperprolactinemic indications
              • Nausea (49%)
              • Headache (19%)
              • Dizziness (17%)
            • Acromegaly
              • Nausea (18%)
              • Constipation (14%)

            1-10%

            Cycloset

            • Monotherapy
              • Sinusitis (10%)
              • Diarrhea (8.8%)
              • Amblyopia (7.5%)
              • Dyspepsia (7.5%)
              • Vomiting (6.3%)
              • Infection (6.3%)
              • Anorexia (5%)
            • Adjunct to sulfonylurea
              • Constipation (9.8%)
              • Flu syndrome (9.4%)
              • Cold (8.2%)
              • Sinusitis (7.4%)
              • Somnolence (6.6%)
              • Vomiting (5.3%)
              • Amblyopia (5.3%)
            • Adjunct to diet or ≤2 antidiabetic medications (eg, metformin, insulin secretagogues, and/or insulin)
              • Vomiting (8.1%)
              • Diarrhea (8.1%)
              • Constipation (5.8%)

            Parlodel

            • Hyperprolactinemic indications
              • Fatigue (7%) Lightheadedness (5%) Vomiting (5%) Abdominal cramps (4%) Nasal congestion (3%) Constipation (3%) Diarrhea (3%) Drowsiness (3%)
            • Acromegaly
              • Postural/orthostatic hypotension (6%)
              • Anorexia (4%)
              • Dry mouth/nasal stuffiness (4%)
              • Indigestion/dyspepsia (4%)
              • Digital vasospasm (3%)
              • Drowsiness/tiredness (3%)
              • Vomiting (2%)
              • Gastrointestinal bleeding (<2%)
              • Dizziness (<2%)
              • Exacerbation of Raynaud syndrome (<2%)
              • Headache (<2%)
              • Syncope (<2%)
            • Postpartum
              • Headache (10%)
              • Dizziness (8%)
              • Nausea (7%)
              • Vomiting (3%)
              • Fatigue (1%)

            <1%

            Parlodel

            • Postpartum
              • Syncope (0.7%)
              • Diarrhea (0.4%)
              • Cramps (0.4%)

            Frequency Not Defined

            Parlodel

            • Parkinson disease
              • Most common: Nausea, abnormal involuntary movements, hallucinations, confusion, “on-off’’ phenomenon, dizziness, drowsiness, faintness/fainting, vomiting, asthenia, abdominal discomfort, visual disturbance, ataxia, insomnia, depression, hypotension, shortness of breath, constipation, and vertigo
              • Less common: Anorexia, anxiety, blepharospasm, dry mouth, dysphagia, edema of the feet and ankles, erythromelalgia, epileptiform seizure, fatigue, headache, lethargy, mottling of skin, nasal stuffiness, nervousness, nightmares, paresthesia, skin rash, urinary frequency, urinary incontinence, urinary retention, and rarely, signs and symptoms of ergotism such as tingling of fingers, cold feet, numbness, muscle cramps of feet and legs or exacerbation of Raynaud syndrome

            Postmarketing Experience

            Cycloset

            • Hallucinations
            • Fibrotic-related complications (eg, retroperitoneal fibrosis, pulmonary fibrosis, pleural effusion, pleural thickening, pericarditis, and pericardial effusions)
            • Psychotic and psychiatric disorders
            • Stroke
            • Neuroleptic-like malignant syndrome

            Parlodel

            • Psychiatric disorders: Confusion, psychomotor agitation/excitation, hallucinations, psychotic disorders, insomnia, libido increase, hypersexuality
            • Nervous system disorders: Headache, drowsiness, dizziness, dyskinesia, somnolence, paraesthesia, excess daytime somnolence, sudden onset of sleep
            • Eye disorders: Visual disturbance, vision blurred
            • Ear and labyrinth disorders: Tinnitus
            • Cardiac disorders: Pericardial effusion, constrictive pericarditis, tachycardia, bradycardia, arrhythmia, cardiac valve fibrosis
            • Vascular disorders: Hypotension, orthostatic hypotension (very rarely leading to syncope), reversible pallor of fingers and toes induced by cold (especially in patients with history of Raynaud phenomenon)
            • Respiratory, thoracic and mediastinal disorders: Nasal congestion, pleural effusion, pleural fibrosis, pleurisy, pulmonary fibrosis, dyspnea
            • Gastrointestinal disorders: Nausea, constipation, vomiting, dry mouth, diarrhoea, abdominal pain, retroperitoneal fibrosis, gastrointestinal ulcer, gastrointestinal hemorrhage
            • Skin and subcutaneous tissue disorders: Allergic skin reactions, hair loss
            • Musculoskeletal and connective tissue disorders: Leg cramps
            • General disorders and administration site conditions: Fatigue, peripheral edema, a syndrome resembling Neuroleptic Malignant Syndrome (NMS) on abrupt withdrawal of Parlodel
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            Warnings

            Contraindications

            Parlodel

            • Hypersensitivity to bromocriptine, ergot-related drugs, or to any of the excipients in Parlodel
            • Uncontrolled hypertension
            • Pregnancy in patients treated for hyperprolactinemia (see Pregnancy)
            • Postpartum period in women with a history of coronary artery disease and other severe cardiovascular conditions

            Cycloset

            • Hypersensitivity to bromocriptine, ergot-related drugs, or any of the excipients in Cycloset
            • Syncopal migraine
            • Women who are nursing (see Lactation)

            Cautions

            Dosage forms for Cycloset and Parlodel and not interchangeable

            Avoid abrupt withdrawal (associated with neuroleptic malignant syndrome-like symptoms); discontinue gradually

            Use with caution in patients with cardiovascular disease, dementia, hepatic impairment, and peptic ulcer disease

            Somnolence

            • Somnolence, and episodes of sudden sleep onset has been reported, particularly in patients with Parkinson’s disease
            • Inform and advise not to drive or operate machines during treatment; dose reduction or termination of therapy may be considered
            • During the first days of treatment, hypotensive reactions may occasionally occur and result in reduced alertness, particular care should be exercised when driving a vehicle or operating machinery

            Parlodel

            • Avoid use in patients with galactose intolerance, severe lactase deficiency, or glucose-galactose malabsorption
            • Used with caution in patients with a history of psychosis or cardiovascular disease
            • In patients undergoing treatment for macroadenoma-related hyperprolactinemia or who have undergone transsphenoidal surgery, a persistent watery nasal discharge may be sign of CSF rhinorrhea
            • Visual field impairment is a known complication of macroprolactinoma; Parlodel therapy may lead to a reduction in hyperprolactinemia and often to a resolution of the visual impairment; monitor visual fields in patients with macroprolactinoma
            • Cold-sensitive digital vasospasm has been observed in some acromegalic patients; response is reversible by dose reduction of Parlodel and may be prevented by keeping the fingers warm
            • Cases of severe gastrointestinal bleeding from peptic ulcers have been reported; patients with a history of peptic ulcer or gastrointestinal bleeding should be observed carefully during treatment with Parlodel
            • Possible tumor expansion while receiving Parlodel therapy has been reported; all patients should be carefully monitored and, if evidence of tumor expansion develops, discontinuation of treatment and alternative procedures considered
            • High doses of Parlodel may be associated with confusion and mental disturbances; parkinsonian patients may manifest mild degrees of dementia, caution should be used when treating such patients
            • Auditory or visual hallucinations may occur when administered alone or concomitantly with levodopa; hallucinations usually resolve with dosage reduction; occasionally, discontinue therapy
            • Postmarketing reports suggest that patients treated with anti-Parkinson medications can experience intense urges to gamble, increased sexual urges, intense urges to spend money uncontrollably, and other intense urges
            • History of MI and a residual atrial, nodal or ventricular arrhythmia, especially with Parkinson disease
            • Retroperitoneal fibrosis has been reported in a few patients receiving long-term therapy
            • Hypertension
              • Hypertension have been reported, sometimes at the initiation of therapy, but often developing in the second week of therapy; periodic blood pressure monitoring, during the first weeks of therapy is prudent
              • Seizures have also been reported both with and without the prior development of hypertension; stroke have been reported mostly in postpartum patients whose prenatal and obstetric courses had been uncomplicated
              • Use of the drug in patients with uncontrolled hypertension is not recommended (see Contraindications [Parlodel])
              • Exercise caution when administering Parlodel therapy concomitantly with other medications known to lower blood pressure
              • If hypertension, severe, progressive, or unremitting headache (with or without visual disturbance), or evidence of CNS toxicity develops, evaluate patient and therapy should be discontinued

            Cycloset

            • Somnolence may occur; inform patients should be made aware of this potential side effect, particularly when initiating therapy; patients experiencing somnolence should refrain from driving or operating heavy machinery
            • Fibrotic valve thickening (eg, aortic, mitral, tricuspid), possibly due to excess serotonin activity, usually associated with long-term, chronic use of ergot alkaloids and derivatives reported
            • Dopamine receptor antagonists
              • Dopamine receptor antagonists, including neuroleptic agents that have dopamine D2 receptor antagonist properties (eg, clozapine, olanzapine, ziprasidone), may reduce the effectiveness of Cycloset and Cycloset may reduce the effectiveness of these agents; concomitant use with dopamine receptor antagonists, including neuroleptic drugs, is not recommended
              • Other dopamine receptor agonists are indicated for the treatment of Parkinson’s disease, hyperprolactinemia, restless leg syndrome, acromegaly, and other disorders; effectiveness and safety of Cycloset in patients currently treated with other dopamine receptor agonists is unknown; concomitant use is not recommended
            • Hypotension
              • Hypotension, including orthostatic hypotension, can occur, particularly upon Cycloset initiation and with dose escalation
              • Assess orthostatic vital signs prior to initiation of Cycloset and periodically thereafter; during early treatment, patients should be advised to make slow postural changes and to avoid situations that could lead to serious injury if syncope was to occur
              • Use caution in patients taking anti-hypertensive medication
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            Pregnancy & Lactation

            Pregnancy

            Parlodel

            • Safety of Parlodel treatment during pregnancy to the mother and fetus has not been established
            • If pregnancy occurs during Parlodel administration, careful observation of these patients is mandatory
            • Prolactin-secreting adenomas may expand and compression of optic/other cranial nerves may occur, emergency pituitary surgery becoming necessary; in most cases, the compression resolves following delivery
            • Reinitiation of Parlodel treatment has been reported to produce improvement in the visual fields of patients in whom nerve compression has occurred during pregnancy
            • In patients being treated for hyperprolactinemia, Parlodel should be withdrawn when pregnancy is diagnosed
            • Acromegaly, prolactinoma, or Parkinson disease
              • Patients who subsequently become pregnant, determine whether continuing therapy is medically necessary or can discontinues
              • If it is continued, discontinue therapy in those who may experience hypertensive disorders of pregnancy (including eclampsia, preeclampsia, or pregnancy-induced hypertension) unless withdrawal of Parlodel is considered to be medically contraindicated

            Cycloset

            • Because human studies cannot rule out the possibility of harm, Cycloset should be used during pregnancy only if clearly necessary

            Lactation

            Parlodel: Avoid use during lactation in postpartum women

            Cycloset

            • Cycloset is contraindicated in women who are nursing
            • Cycloset contains bromocriptine which inhibits lactation; use of bromocriptine for inhibition of postpartum lactation was withdrawn based on postmarketing reports of stroke in this setting

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Parlodel: Semisynthetic ergot alkaloid, dopamine receptor agonist, inhibits prolactin secretion, and lowers blood levels of growth hormone in acromegaly

            Cycloset: Mechanism of action is unknown; bromocriptine is believed 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

            Absorption

            Peak plasma concentration (Parlodel): 465 pg/mL (2 doses of 2.5 mg); 628 pg/mL (steady state)

            AUC steady state (Parlodel): 2377 pg·hr/mL

            Peak plasma time (Cycloset): 53 minutes (fasted); 90-120 minutes (high-fat meal)

            Bioavailability (Cycloset): 55-66%

            Distribution

            Protein bound (Parlodel): 90-96% (to albumin)

            Vd (Cycloset): 61L

            Metabolism

            Parlodel: Primarily hepatic via CYP3A; extensive first-pass biotransformation

            Cycloset: Metabolism by; absorbed dose (~93%) undergoes first-pass metabolism and the remaining reaches the systemic circulation

            Elimination

            Half-life: 4.85 hr (Parlodel); 6 hr (Cycloset)

            Excretion: Feces (~82%); urine (2-6%)

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            Administration

            Oral Administration

            Parlodel

            • Take with food

            Cycloset

            • Take with food; administer within 2 hours after waking in the morning
            • If dose missed, wait until the next morning to take medication

            Storage

            Cycloset and Parlodel: Store ≤25°C (77°F)

            Parlodel: Store in tight, light-resistant container

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
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