Here is a comprehensive overview of antiemetic (anti-vomiting) pharmacotherapy, drawn from Katzung's Basic and Clinical Pharmacology (16th ed.) and supporting emergency medicine sources:
Antiemetic Drug Classes & Their Prescriptions
1. 5-HT₃ Receptor Antagonists (First-line for most settings)
| Drug | Dose | Notes |
|---|
| Ondansetron | 4–8 mg PO/IV/ODT q6–8h | Drug of choice; ODT formulation preferred for active vomiting |
| Granisetron | 1 mg PO/IV | Chemotherapy-induced N/V |
| Palonosetron | 0.25 mg IV (single dose) | Long half-life; CINV prevention |
Mechanism: Block 5-HT₃ receptors in the gut and chemoreceptor trigger zone (CTZ).
2. Dopamine (D₂) Antagonists / Prokinetics
| Drug | Dose | Notes |
|---|
| Metoclopramide | 10 mg PO/IV/IM q6h | Also a prokinetic; first-line in pregnancy (oral preferred) |
| Prochlorperazine | 5–10 mg PO/IV/IM q6h; 25 mg PR | Phenothiazine; useful 2nd line; rectal suppository available |
| Promethazine | 12.5–25 mg PO/IV/IM/PR q4–6h | Sedating; IV carries vascular damage risk — prefer IM or PR |
| Haloperidol | 0.5–2 mg PO/SC | Useful when phenothiazines fail |
Mechanism: Block D₂ receptors in the CTZ; some also block muscarinic/histamine receptors.
Risk: All D₂ antagonists can cause extrapyramidal side effects (EPS), including acute dystonia — treat with diphenhydramine 25–50 mg IV.
3. Antihistamines (H₁ Blockers)
| Drug | Dose | Notes |
|---|
| Dimenhydrinate (Dramamine) | 25–50 mg IV/PO q4–6h | Motion sickness, vestibular causes |
| Diphenhydramine | 25–50 mg PO/IV/IM q6h | Also used for EPS prophylaxis |
| Meclizine | 25 mg PO q6h | Motion sickness |
Mechanism: H₁ + muscarinic blockade in the vestibular pathway.
4. NK1 (Neurokinin) Receptor Antagonists (Chemotherapy-induced)
| Drug | Dose | Notes |
|---|
| Aprepitant | 125 mg PO day 1, then 80 mg/day × 2 days | CYP3A4 inhibitor — check interactions |
| Fosaprepitant | 115 mg IV (single dose, day 1) | IV prodrug of aprepitant |
| Rolapitant | 180 mg PO (single dose) | 180-hr half-life |
| Netupitant/palonosetron | 300/0.5 mg PO (single dose) | Combo product (Akynzeo) |
Mechanism: Block NK1 receptors in the area postrema centrally.
Combined NK1 + 5-HT₃ antagonist + dexamethasone prevents acute emesis in 80–90% of patients on highly emetogenic chemotherapy.
5. Corticosteroids (Adjunct, especially for CINV)
| Drug | Dose |
|---|
| Dexamethasone | 8–20 mg IV/PO before chemotherapy, then 8 mg/day × 2–4 days |
Mechanism: Unknown; synergistic with 5-HT₃ antagonists.
6. Olanzapine (Adjunct for refractory/CINV)
- Dose: 10 mg PO on days 1–4 of chemotherapy
- Reduces acute and delayed N/V by an additional 15–30% on top of triple therapy.
7. Anticholinergics (Motion sickness / vestibular)
| Drug | Dose | Notes |
|---|
| Scopolamine (hyoscine) | 1.5 mg transdermal patch q72h | Motion sickness; apply behind ear |
Quick Clinical Guide by Etiology
| Cause | Preferred Agent(s) |
|---|
| Postoperative N/V | Ondansetron, dexamethasone, prochlorperazine |
| Chemotherapy (CINV) | Ondansetron + dexamethasone + aprepitant ± olanzapine |
| Pregnancy (hyperemesis) | Metoclopramide IV, dimenhydrinate, pyridoxine (B6) |
| Gastroenteritis/ED | Ondansetron ODT, metoclopramide IV |
| Motion sickness / vestibular | Scopolamine patch, meclizine, dimenhydrinate |
| Opioid-induced | Metoclopramide, ondansetron, prochlorperazine |
| Refractory (all others failed) | Haloperidol 0.5–2 mg PO/SC |
Key point on route of administration: When patients are actively vomiting, prefer IV, ODT (orally disintegrating tablet), or IM/PR routes. Ondansetron ODT has largely replaced rectal suppositories as the preferred out-of-IV option. — Katzung's Basic and Clinical Pharmacology, 16th Ed.; Roberts and Hedges' Clinical Procedures in Emergency Medicine