bromocriptine

broe-moe-KRIP-teen

Therapeutic Classification: antiparkinson agents, antidiabetics

Pharmacologic Classification: dopamine agonists

REMS

Parlodel

Treatment of the following conditions:
- Parkinsonism (as adjunct to levodopa),
- Hyperprolactinemia (amenorrhea/galactorrhea), including associated female infertility,
- Prolactin-secreting adenomas,
- Acromegaly.

Cycloset

Type 2 diabetes (as adjunct to diet and exercise).

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 1st-pass metabolism; only 7% of dose reaches systemic circulation).

Distribution: Well distributed to tissues.

Protein Binding: 90–96%

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme. Primarily excreted in bile; 2–6% excreted unchanged in urine.

Half-Life: 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 concentrations.

§Effect on growth hormone.

¶During chronic therapy.

‡‡Effect on blood glucose concentrations.

Contraindicated in:

Hypersensitivity to bromocriptine, ergot alkaloids, or bisulfites;
Severe cardiovascular disease or peripheral vascular disease;
History of syncopal migraines (↑ risk of syncope) (Cycloset);
Type 1 diabetes (Cycloset);
Diabetic ketoacidosis (Cycloset);
Impulsive control/compulsive behaviors;
OB: Postpartum patients (↑ risk of hypertension, MI, seizures, stroke, and psychosis);
Lactation: Lactation.

Use Cautiously in:

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

CV: orthostatic hypotension, digital vasospasm (acromegaly only), MI

Derm: melanoma, urticaria

EENT: burning eyes, nasal stuffiness, visual disturbances

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

MS: leg cramps

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

Resp: pulmonary effusion, pulmonary infiltrates

Drug-drug:

↑risk of 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 toxicity when used with ergot derivatives ; do not use within 6 hr of each other.
Strong CYP3A4 inhibitors, including itraconazole, ketoconazole, and protease inhibitors, and moderate CYP3A4 inhibitors, including erythromycinmay ↑ levels and risk of toxicity; avoid concurrent use.
CYP3A4 inducers may ↓ levels and effectiveness.

Parlodel

Parkinsonism

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).

Hyperprolactinemia

PO (Adults ): 1.25–2.5 mg/day initially; may gradually ↑ every 3–7 days up to 2.5 mg 2–3 times daily.

Acromegaly

PO (Adults ): 1.25–2.5 mg/day for 3 days; ↑ by 1.25–2.5 mg every 3–7 days until optimal response obtained (usual range 10–30 mg/day; up to 100 mg/day).

Pituitary Adenomas

PO (Adults ): 1.25 mg 2–3 times daily; may ↑ over several weeks (range 2.5–20 mg/day).
Cycloset

Type 2 Diabetes

PO (Adults ): 0.8 mg once daily; may ↑ by 0.8 mg every 7 days (range 1.6–4.8 mg/day). Concurrent use of moderate CYP3A4 inhibitor: Not to exceed 1.6 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 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 signs/symptoms of withdrawal fever, muscular rigidity, altered consciousness, respiratory distress, tachycardia, convulsions, diaphoresis, hypertension, hypotension, pallor, and tiredness upon discontinuation of bromocriptine.
Parkinson’s Disease: Assess signs/symptoms of Parkinson's disease (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: Assess ring size, heel pad thickness, and soft-tissue volume 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/symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety) during therapy.

Lab Test Considerations:

Hyperprolactinemia: Measure serum prolactin concentrations monthly during initial therapy and twice yearly during maintenance therapy to determine effectiveness of therapy. Pregnancy test recommended at least every 4 wk during the amenorrheic period and every time a patients misses a menstrual period.
Acromegaly: Monitor serum growth hormone and insulin-like growth factor-1 concentrations monthly during therapy.
Type 2 Diabetes: Monitor A1c twice yearly, every 3 mo when not meeting glycemic goals, or with change in therapy.

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

Explain the purpose and side effects of bromocriptine. Instruct patient to take as directed. Take missed doses ≤ 4 hr of the scheduled dose or omit. Do not double doses. Caution patient to avoid abrupt discontinuation to prevent withdrawal syndrome. Advise patient to read the Patient Information before taking and with each Rx refill, in case of changes.
- Emphasize the importance of regular follow-up examinations to determine effectiveness and monitor side effects.
- 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, ↑ sweating, continuing or severe nausea and vomiting, nervousness, shortness of breath, weakness) or ↑ 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 ↑ gambling, sexual, binge eating or other intense urges occur.
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/symptoms 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/symptoms of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to drink a glass of orange juice or ingest 2–3 teaspoons 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.
Rep: Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. Advise women of reproductive potential to use a nonhormonal method of birth control during therapy. If bromocriptine is used during pregnancy, notify health care professional if signs and symptoms of high BP, heart attack, seizures, stroke, or psychosis 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.

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.

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 ⬆