bromocriptine

broe-moe-KRIP-teen

Therapeutic Classification: antiparkinson agents, antidiabetics

Pharmacologic Classification: dopamine agonists

REMS

Parkinsonism (as adjunct to levodopa) (Parlodel only).
Hyperprolactinemia (amenorrhea/galactorrhea), including associated female infertility (Parlodel only).
Prolactin-secreting adenomas (Parlodel only).
Acromegaly (Parlodel only).
Type 2 diabetes (as adjunct to diet and exercise) (Cycloset only).

Activates dopamine receptors in the CNS.
Decreases prolactin secretion.
Reduces fasting and postprandial blood glucose concentrations by increasing insulin sensitivity.

Therapeutic effects:

Relief of rigidity and tremor in parkinsonism.
Restoration of fertility in hyperprolactinemia.
Reduction in tumor size.
Decreased growth hormone in acromegaly.
Lowering of blood sugar in patients with diabetes.

Absorption: Parlodel is poorly absorbed (30%) from the GI tract; 65–95% of Cycloset dose is absorbed (undergoes extensive first-pass metabolism; only 7% of dose reaches systemic circulation).

Distribution: 90–96% protein bound.

Metabolism/Excretion: Completely metabolized by the liver (metabolized by CYP3A4); primarily excreted in bile (2–6% excreted unchanged in urine).

Half-Life: Biphasic—initial phase 4–4.5 hr, terminal phase 8–20 hr.

(suppression of various parameters)

ROUTE	ONSET	PEAK	DURATION
PO‡	30–90 min	1–2 hr	8–12 hr
PO‡	2 hr	8 hr	24 hr
PO§	1–2 hr	4–8 wk¶	4–8 hr
PO‡‡	unknown	unknown	unknown

‡Effect on parkinsonian symptoms.

‡Effect on serum prolactin levels.

§Effect on growth hormone.

¶During chronic therapy.

‡‡Effect on blood glucose levels.

Contraindicated in:

Hypersensitivity to bromocriptine, ergot alkaloids, or bisulfites;
Severe cardiovascular disease or peripheral vascular disease;
History of syncopal migraines (↑ risk of syncope) (Cycloset only);
Concurrent use of dopamine antagonists (e.g., clozapine, olanzapine, ziprasidone) or other dopamine agonists (e.g., ropinirole);
Type 1 diabetes (Cycloset only);
Diabetic ketoacidosis (Cycloset only);
Impulsive control/compulsive behaviors;
OB: Postpartum patients ( risk of hypertension, MI, seizures, stroke, and psychosis);
Lactation: Lactation (inhibits lactation).

Use Cautiously in:

Cardiac disease;
Mental disturbances;
May restore fertility (additional contraception may be required if pregnancy is undesirable);
Hepatic impairment;
Concurrent antihypertensive therapy (↑ risk of hypotension);
OB: Safety not established in pregnancy;
Pedi: Safety and effectiveness not established in children.

CV: orthostatic hypotension, MI

Derm: melanoma, urticaria

EENT: burning eyes, nasal stuffiness, visual disturbances

GI: nausea, abdominal pain, anorexia, dry mouth, metallic taste, vomiting

MS: leg cramps

Neuro: dizziness, drowsiness, confusion, hallucinations, headache, impulse control disorders (gambling, sexual, uncontrolled spending, binge/compulsive eating), insomnia, nightmares

Resp: effusions, pulmonary infiltrates

Misc: digital vasospasm (acromegaly only)

Drug-drug:

Additive hypotension with antihypertensives.
Additive CNS depression with antihistamines, alcohol, opioid analgesics, and sedative/hypnotics.
Additive neurologic effects with levodopa.
Effects may be antagonized by phenothiazines, haloperidol, clozapine, olanzapine, ziprasidone, aripiprazole, and metoclopramide.
↑risk of side effects when used with ergot derivatives (do not use within 6 hours of each other).
CYP3A4 inhibitors may ↑ effects.
CYP3A4 inducers may ↓ effects.

Parkinsonism

Hyperprolactinemia

Acromegaly

Pituitary Adenomas

Type 2 Diabetes (Cycloset only)

PO (Adults ): 1.25 mg 1–2 times daily, ↑ by 2.5 mg/day in 2–4 wk intervals (range is 2.5–100 mg/day in divided doses; up to 40 mg/day have been used).
PO (Adults ): 1.25–2.5 mg/day initially, may be gradually ↑ every 3–7 days up to 2.5 mg 2–3 times daily.
PO (Adults ): 1.25–2.5 mg/day for 3 days, ↑ by 1.25–2.5 mg every 3–7 days until optimal response is obtained (usual range 10–30 mg/day; up to 100 mg/day).
PO (Adults ): 1.25 mg 2–3 times daily, may be ↑ over several wk (range 2.5–20 mg/day).
PO (Adults ): 0.8 mg once daily; may be ↑ by 0.8 mg every 7 days (range 1.6–4.8 mg/day).

(Generic available)

Tablets: 0.8 mg; 2.5 mg
Capsules: 5 mg

Assess patient for allergy to ergot derivatives.
- Monitor BP before and frequently during drug therapy. Instruct patient to remain supine during and for several hours after 1st dose; severe hypotension may occur. Supervise ambulation and transfer during initial dosing to prevent injury from hypotension.
Monitor for symptoms (fever, muscular rigidity, altered consciousness, respiratory distress, tachycardia, convulsions, diaphoresis, hypertension, hypotension, pallor, tiredness) upon discontinuation of bromocriptine.
Parkinson’s Disease: Assess symptoms (restlessness or desire to keep moving, rigidity, tremors, pill rolling, masklike face, shuffling gait, muscle spasms, twisting motions, difficulty speaking or swallowing, loss of balance control) before and during therapy.
Acromegaly: Physical examination including ring size, heel pad thickness, and soft-tissue volume should be assessed periodically during therapy.
Hyperprolactinemia: Sella turcica should be evaluated before therapy and yearly with CT scan or MRI scan.
Type 2 Diabetes: Observe for signs and symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety) during therapy.

Lab Test Considerations:

May cause ↑ serum BUN, AST, ALT, CK, alkaline phosphatase, and uric acid levels; usually transient and clinically insignificant.
- Female infertility: Measure serum prolactin concentrations and anterior pituitary function before therapy. Monitor ovulation during therapy.
- Acromegaly: Monitor serum growth hormone and insulin-like growth factor (IGF-1) concentrations periodically during therapy.
- Hyperprolactinemia: Measure serum prolactin concentrations monthly during initial therapy and twice yearly during maintenance therapy to determine effectiveness of therapy.
- Type 2 Diabetes: Monitor serum glucose and glycosylated hemoglobin periodically during therapy to evaluate effectiveness of treatment.

This medication is often given concurrently with levodopa or a levodopa-carbidopa combination in the treatment of Parkinson’s disease.
PO: Administer with food or milk to minimize gastric distress. Tablets may be crushed if patient has difficulty swallowing. Taking at bedtime may decrease nausea.
Type 2 Diabetes: Take with food within 2 hrs of waking in the morning.

Instruct patient to take medication as directed. Take missed doses within 4 hr of the scheduled dose or omit. Do not double doses. Caution patient to avoid abrupt discontinuation to prevent withdrawal syndrome (apathy, anxiety, depression, fatigue, insomnia, sweating, pain). Advise patient to read the Patient Package Insert before taking and with each Rx refill, in case of changes.
- May cause drowsiness and dizziness. Caution patients to avoid driving and other activities requiring alertness until response to medication is known.
- Caution patient to change positions slowly to minimize orthostatic hypotension. Health care professional should be notified if orthostatic hypotension occurs.
- Caution patient to avoid concurrent use of alcohol during the course of therapy.
- Instruct patient to inform health care professional immediately if signs of MI (severe chest pain, fainting, fast heartbeat, increased sweating, continuing or severe nausea and vomiting, nervousness, shortness of breath, weakness) or increasing shortness of breath is noted; pulmonary infiltrates and pleural effusions may occur with long-term therapy.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any Rx, OTC, or herbal products.
- Advise patient to notify health care professional if new or increased gambling, sexual, binge eating or other intense urges occur.
- Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. Advise women to consult with health care professional regarding a nonhormonal method of birth control. If bromocriptine is used during pregnancy, notify health care professional if signs and symptoms of high blood pressure, heart attack, seizures, stroke or psychosis (losing touch with reality) occur during postpartum period. If bromocriptine is used for infertility, since pregnancy may occur prior to reinitiation of menses, advise patient to take a pregnancy test at least every 4 wk during amenorrheic period, and, once menses are reinitiated, every time a menstrual period is missed. Discontinue therapy as soon as pregnancy has been established.
- Emphasize the importance of regular follow-up examinations to determine effectiveness and monitor side effects.
Infertility: Instruct women treated for infertility to obtain daily basal body temperatures to determine when ovulation occurs.
Pituitary Tumors: Instruct patients taking bromocriptine for pituitary tumors to inform health care professional immediately if signs of tumor enlargement (blurred vision, sudden headache, severe nausea, and vomiting) occur.
Type 2 Diabetes: Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long term.
- Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to drink a glass of orange juice or ingest 2–3 tsp of sugar, honey, or corn syrup dissolved in water or an appropriate number of glucose tablets and notify health care professional.
- Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
- Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness and health care professional notified if significant changes occur.
- Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.

Decrease in tremor, rigidity, and bradykinesia.
- Improvement in balance and gait in patients with Parkinson’s disease.
Decrease in galactorrhea in patients with hyperprolactinemia.
Resumption of normal ovulatory menstrual cycles with restoration of fertility (in patients with amenorrhea and galactorrhea, menses usually resume within 6–8 wk, and galactorrhea subsides within 8–12 wk).
Decreased serum levels of growth hormone in patients with acromegaly.
Decrease in the symptoms of neuroleptic malignant syndrome.
Lowering of blood sugar in diabetic patients.

Cycloset, Parlodel

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆