THERAPEUTICS

Brands

• Reglan, Maxolon, Clopra

Generic?

• Yes

Class

• Antiemetic

Commonly Prescribed for

(FDA approved in bold)

• Diabetic gastroparesis

• Symptomatic gastroesophageal reflux (short-term therapy)

• Nausea and vomiting (postoperative, chemotherapy, pregnancy)

• Small bowel intubation

• Migraine (acute)

• Tics in Gilles de la Tourette syndrome (GTS)

• Hiccup

How the Drug Works

• Antagonism at dopamine receptor (specifically D2) and 5-HT3 (at higher dose) decreases nausea. It may also increase absorption of coadministered drugs. May stimulate GI motility by sensitizing tissues to the actions of muscarinic activity, D2 antagonism, and 5-HT4 receptor agonism

How Long Until It Works

• 30–60 minutes with oral dose for nausea. Gastroparesis improvesmaximally by 3 weeks

If It Works

• Use at lowest effective dose

• Continue to assess effect of the medication and if it is still needed

If It Doesn't Work

• Increase dose, or discontinue and change to another agent

• Migraine: change to another antiemetic (prochlorperazine, droperidol, chlorpromazine) or combine with other agents

• Gastroparesis: domperidone (where available) is an alternative. Smaller, more frequent meals with low fat and fiber might improve symptoms

Best Augmenting Combos for Partial Response or Treatment-Resistance

• Migraine: often combined with NSAIDs, triptans, or ergots. Usually not used as monotherapy

• Gastroparesis: may be combined with erythromycin, botulinum toxin, electrical gastric stimulation

Tests

• None required

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• Motor AEs and prolactinemia: blocking of D2 receptors

Notable AEs

• Most common: sedation, CNS depression

• Fluid retention, bradycardia or superventricular tachycardia, hypo or hypertension, rash, galactorrhea, urinary frequency or incontinence

• Akathisia, parkinsonism (bradykinesia, tremor, rigidity), acute dystonic reactions

Life-Threatening or Dangerous AEs

• Tardive dyskinesias

• Neuroleptic malignant syndrome (rare)

• Hepatotoxicity (rare)

Weight Gain

• Unusual

Sedation

• Not unusual

What to Do About AEs

• Excessive sedation: lower dose or use only as a rescue agent when patient can lie down or sleep