with hyperprolactinemia (amenorrhea, galactorrhea, hypogonadism, infertility), parkinsonism, acromegaly. **Cycloset:** Control of blood glucose in type 2 diabetes. **OFF-LABEL:** Neuroleptic malignant syndrome.

#####  PRECAUTIONS

**Contraindications:** Hypersensitivity to bromocriptine; peripheral vascular disease, pregnancy, severe ischemic heart disease, uncontrolled hypertension. **Cycloset:** Syncopal migraine, breastfeeding. **Cautions:** Impaired hepatic, renal, or cardiac function; hypertension, dementia, psychosis, peptic ulcer disease.

#####  ACTION

Activates dopamine receptors in tuberoinfundibular process (inhibits prolactin secretion), stimulates dopamine receptors in corpus striatum (benefits Parkinson's disease). Mechanism for type 2 diabetes unknown. **Therapeutic Effect:** Improves symptoms of parkinsonism, suppresses galactorrhea, reduces glucose production/decreases insulin resistance.

#####  PHARMACOKINETICS

Indication| Onset| Peak| Duration  
---|---|---|---  
Prolactin lowering| 1–2 hrs| 5–10 hrs| 8–12 hrs

Minimally absorbed from GI tract. Protein binding: 90%–96%. Metabolized in liver. Excreted in feces by biliary secretion. **Half-life:** 15 hrs.

#####  ADMINISTRATION/HANDLING

PO

• Give without regard to food (give with food if GI irritation occurs). • Give at least 4-hr interval for immediate onset and 8-hr interval for sustained-release tablet to avoid seizures. • Give Aplenzin once daily in the morning. • Avoid bedtime dosage (decreases risk of insomnia). • Do not break, crush, dissolve, or divide sustained-, extended-release preparations.

#####  INDICATIONS/ROUTES/DOSAGE

Depression

**PO _(Immediate-Release)_** **: ADULTS:** Initially, 100 mg twice daily. May increase to 100 mg 3 times/day no sooner than 3 days after beginning therapy. **Maximum:** 150 mg 3 times/day. **ELDERLY:** Initially, 50–100 mg/day. May increase by 50–100 mg/day q3–4 days. **Maintenance:** Lowest effective dosage.

**PO _(Sustained-Release)_** **:** **ADULTS:** Initially, 150 mg/day as a single dose in the morning. May increase to 150 mg twice daily as early as day 4