cabergoline

Absorption: Well absorbed but undergoes extensive first-pass hepatic metabolism.

Distribution: Widely distributed; concentrates in pituitary.

Metabolism/Excretion: Extensively metabolized by the liver; <4% excreted unchanged in urine.

Protein Binding: 40–42%.

Half-Life: 63–69 hr.

Time/Action Profile ⬆ ⬇

(effect on serum prolactin levels)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2–3 hr	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to cabergoline or ergot alkaloids;
Uncontrolled hypertension;
History of pulmonary, pericardial, or retroperitoneal fibrotic disorders;
History of cardiac valvular disease;
Lactation: Has been associated with hypertension, stroke, and seizures. Not to be used for suppression of physiologic lactation.

Use Cautiously in:

Hepatic impairment;
Patients who have received medications associated with valvular disorders;
OB: Use only if clearly needed;
Pedi: Safety not established.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hot flashes, PERICARDIAL FIBROSIS, postural hypotension, VALVULAR DISORDERS

EENT: abnormal vision

Endo: breast pain

GI: constipation, nausea, abdominal pain, dyspepsia, RETROPERITONEAL FIBROSIS, vomiting

GU: dysmenorrhea

Neuro: dizziness, headache, depression, drowsiness, fatigue, impulse control disorders (gambling, sexual), nervousness, paresthesia, vertigo, weakness

Resp: pleural effusion, PULMONARY FIBROSIS

Interactions ⬆ ⬇

Drug-drug:

↑risk of hypotension with antihypertensives.
May ↑ the effects of SSRIs and other serotonin agonists (induces serotonin syndrome).
Effectiveness may be ↓ by phenothiazines, butyrophenones (haloperidol), thioxanthenes, or metoclopramide (avoid concurrent use).

Route/Dosage ⬆ ⬇

PO (Adults ): 0.25 mg twice weekly; may be ↑ at 4-wk intervals up to 1 mg twice weekly.

Availability ⬆ ⬇

(Generic available)

Tablets: 0.5 mg

Assessment ⬆ ⬇

Monitor BP before and frequently during initial therapy. Initial doses >1 m g may cause orthostatic hypotension. Use with caution when administering concurrently with other medications that lower BP. Supervise ambulation and transfer during initial dosing to prevent injury from hypotension.
Evaluate the cardiac status and monitor echocardiography at baseline and every 6–12 mo after initiation of therapy or as indicated clinically by signs and symptoms of valvular disease (dyspnea, edema, HF, new cardiac murmur). Use lowest dose and reassess need for therapy periodically.
Monitor for signs and symptoms of pulmonary fibrosis (dyspnea, persistent coughing, difficulty with breathing while lying down, peripheral edema) periodically during therapy. Obtain chest x-ray prior to therapy and chest x-ray and CT scan periodically during therapy to assess for pulmonary fibrosis.

Lab Test Considerations:

Monitor serum prolactin concentrations monthly until normalized (<20 mcg/L in women and <15 mcg/L in men).
- Monitor erythrocyte sedimentation rate (ESR) and creatinine at baseline and as needed during therapy.

Implementation ⬆ ⬇

PO: May be taken without regard to food.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed. Take missed doses as soon as possible within 1 or 2 days. If not remembered until time of next dose, double dose. If nausea occurs, discuss with health care professional.
May cause drowsiness and dizziness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
Advise patient to change positions slowly to minimize orthostatic hypotension.
Caution patient to avoid concurrent use of alcohol during therapy.
Instruct patients taking cabergoline for pituitary tumors to inform health care professional immediately if signs of tumor enlargement occur (blurred vision, sudden headache, severe nausea, and vomiting).
Advise patient to notify health care professional if signs of valvular disorders (shortness of breath, swelling in extremities) occurs.
Advise patient to notify health care professional if new or increased gambling, sexual, or other impulse control disorders occur.
Advise women to consult with health care professional regarding a nonhormonal method of birth control. Women should contact health care professional promptly if pregnancy is planned or suspected.
Emphasize the importance of regular follow-up exams to determine effectiveness and monitor side effects.

Evaluation/Desired Outcomes ⬆ ⬇

Decrease in galactorrhea in patients with hyperprolactinemia.
- After a normal serum prolactin level has been maintained for more than 6 mo, cabergoline may be discontinued. Serum prolactin levels should be monitored periodically to determine necessity of reinstituting cabergoline.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇