section name header

Pronunciation

broe-moe-KRIP-teen

Classifications

Therapeutic Classification: antiparkinson agents, antidiabetics

Pharmacologic Classification: dopamine agonists

Indications

REMS


Action

  • 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.

Pharmacokinetics

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.

Time/Action Profile

(suppression of various parameters)

ROUTEONSETPEAKDURATION
PO30–90 min1–2 hr8–12 hr
PO2 hr8 hr24 hr
PO§1–2 hr4–8 wk4–8 hr
POunknownunknownunknown



Effect on parkinsonian symptoms.

Effect on serum prolactin levels.

§Effect on growth hormone.

During chronic therapy.

Effect on blood glucose levels.

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

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)

Interactions

Drug-drug:

Route/Dosage

Parkinsonism

Hyperprolactinemia

Acromegaly

Pituitary Adenomas

Type 2 Diabetes (Cycloset only)

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Cycloset, Parlodel

Code

NDC Code