Cabergoline

Indications

• Hyperprolactinemia (may be idiopathic or due to prolactinoma)

Administration

• Type: Dopamine Agonist
• Dosage Forms: Tab 0.5mg
• Routes of Administration: Oral
• Common Trade Names: DOSTINEX

Adult Dosing

Hyperprolactinemia

• 0.25-1 mg PO 2x/wk
  • Start 0.25mg 2x/wk, increase q4wk by 0.25mg 2x/wk
  • Max: 1 mg 2x/wk

Pediatric Dosing

Safety/efficacy not established in pediatric patients

Special Populations

• Pregnancy Rating: B: No teratogenicity at 55x MRHD
• Lactation risk: Avoid use while breastfeeding

Renal Dosing

• Adult: Not defined
• Pediatric: Unavailable

Hepatic Dosing

• Adult:
  • Child-Pugh Class C: Caution advised
• Pediatric: Unavailable

Contraindications

• Allergy to class/drug
• Hypersensitivity to ergot derivatives
• Cardiac valvular fibrosis
• Pericardial fibrosis
• Pulmonary fibrosis
• Retroperitoneal fibrosis
• Hypertension, uncontrolled
• Breastfeeding
• Hepatic impairment

Adverse Reactions

Serious

• Hypotension, orthostatic
• Valvulopathy
• Pleural effusion
• Pulmonary fibrosis, Pericardial fibrosis, retroperitoneal fibrosis
• Depression, aggressive behavior, psychosis

Common

• Nausea, Vomiting, Vertigo
• Headache, Dizziness
• Constipation, abdominal pain, diarrhea
• Asthenia, paresthesia
• Fatigue, Somnolence
• Dyspepsia
• Anxiety, compulsive behaviors
• Hot flashes, breast pain
• Xerostomia

Pharmacology

• Half-life: 63-69 hours
• Metabolism: Liver
• Excretion: Feces 60%, urine 22% (<4% unchanged)

Mechanism of Action

• Stimulates dopamine D2 receptors to inhibit prolactin secretion