Vomiting is coordinated by the vomiting center in the medulla, which receives input from the chemoreceptor trigger zone (CTZ) (dopamine D2, serotonin 5-HT3, neurokinin-1 receptors — senses drugs and toxins in blood), the GI tract (5-HT3 receptors on vagal nerves, released by chemotherapy and radiation), the vestibular system (histamine H1 and muscarinic receptors — motion sickness), and the cortex (anxiety, anticipation). Antiemetics are chosen by the receptor that drives the cause.
| Antiemetic class | Receptor blocked | Best for |
|---|
| 5-HT3 antagonists (ondansetron, granisetron, palonosetron) | Serotonin 5-HT3 (gut and CTZ) | Chemotherapy, postoperative, gastroenteritis |
| Dopamine antagonists (metoclopramide, prochlorperazine, droperidol) | D2 in the CTZ; metoclopramide also speeds gastric emptying | Postoperative, migraine-associated, gastroparesis |
| NK1 antagonists (aprepitant, fosaprepitant) | Substance P/neurokinin-1 | Acute and delayed chemotherapy nausea |
| Antihistamines/anticholinergics (meclizine, dimenhydrinate, promethazine, scopolamine) | H1 and muscarinic | Motion sickness, vertigo |
| Corticosteroid (dexamethasone) | Uncertain | Added to chemotherapy and postoperative regimens |
| Cannabinoids (dronabinol) | CB1 | Refractory chemotherapy nausea, appetite |
Laxatives increase stool water or bowel movement.
- Bulk-forming (psyllium, methylcellulose) — absorb water, enlarge stool; slowest, most physiologic (12–72 hours)
- Osmotic (polyethylene glycol [PEG], lactulose, magnesium hydroxide or citrate, sodium phosphate) — draw water into the bowel
- Stimulant (senna, bisacodyl) — stimulate the myenteric plexus and increase secretion (6–12 hours orally; suppository within an hour)
- Stool softener (docusate) — surfactant; weak evidence alone
- Lubricant (mineral oil)
- Secretagogues (lubiprostone, linaclotide, plecanatide) — increase intestinal fluid secretion
- Peripherally acting mu-opioid receptor antagonists (PAMORAs) (methylnaltrexone, naloxegol, naldemedine) — block opioid effects in the gut without reversing analgesia
Antidiarrheals
- Loperamide and diphenoxylate — opioid agonists acting on gut receptors → slow motility; loperamide barely enters the brain at normal doses
- Bismuth subsalicylate — antisecretory and antimicrobial
- Octreotide — somatostatin analog; reduces secretory diarrhea (carcinoid, VIPoma, high-output ostomy)
- Oral rehydration solution (ORS) — glucose–sodium cotransport restores fluid; the most important treatment of acute diarrhea
| Drug (generic) | Key use | Key point |
|---|
| Ondansetron (prototype 5-HT3) | Chemotherapy, postoperative, gastroenteritis nausea | QT prolongation; constipation, headache |
| Metoclopramide | Gastroparesis, postoperative nausea | Boxed warning: tardive dyskinesia — avoid longer than 12 weeks |
| Prochlorperazine | Nausea, migraine | Boxed warning: increased mortality in older adults with dementia-related psychosis; EPS, sedation, hypotension |
| Promethazine | Nausea, motion sickness, allergy | Boxed warnings: respiratory death under age 2; severe tissue injury/gangrene with injection |
| Droperidol | Postoperative nausea | Boxed warning: QT prolongation, torsades |
| Aprepitant/fosaprepitant | Highly emetogenic chemotherapy (with a 5-HT3 antagonist and dexamethasone) | CYP3A4 interactions |
| Scopolamine patch | Motion sickness, postoperative nausea | Behind the ear 4 hours before travel |
| Meclizine, dimenhydrinate | Motion sickness, vertigo | Drowsiness; anticholinergic |
| Doxylamine–pyridoxine | Nausea and vomiting of pregnancy (first-line drug) | Drowsiness |
| Psyllium | Chronic constipation, IBS | Full glass of fluid |
| PEG 3350 | Constipation; bowel preparation | Well tolerated |
| Lactulose | Constipation; hepatic encephalopathy | Bloating, diarrhea, electrolyte loss |
| Senna, bisacodyl | Constipation; opioid-induced constipation | Cramping |
| Docusate | Softening stool (limited benefit) | Not enough alone for opioid constipation |
| Methylnaltrexone, naloxegol | Opioid-induced constipation not helped by laxatives | Contraindicated in bowel obstruction |
| Linaclotide, lubiprostone | Chronic idiopathic constipation, IBS-C | Diarrhea; linaclotide contraindicated under age 2 |
| Loperamide (prototype antidiarrheal) | Non-infectious acute or chronic diarrhea, traveler's diarrhea without fever or blood | Cardiac toxicity at high doses |
| Diphenoxylate–atropine | Diarrhea | US Schedule V; atropine discourages misuse |
| ORS | Dehydration from diarrhea | First-line in all ages |
Ondansetron: headache, constipation, dizziness, QT prolongation (dose-related; the single IV dose is limited to 16 mg), serotonin syndrome with other serotonergic drugs.
Dopamine antagonists: extrapyramidal symptoms (acute dystonia, akathisia — especially in children and young adults), tardive dyskinesia (metoclopramide), sedation, orthostatic hypotension, neuroleptic malignant syndrome (rare), QT prolongation (droperidol).
Promethazine: sedation, respiratory depression, anticholinergic effects; injection causes severe chemical irritation — gangrene with extravasation or intra-arterial injection.
Antihistamines/anticholinergics (scopolamine, meclizine): dry mouth, drowsiness, blurred vision, urinary retention, constipation, confusion in older adults.
Dexamethasone: hyperglycemia, insomnia. Dronabinol: dizziness, euphoria, tachycardia.
Laxatives
- Bulk-forming: bloating; esophageal or bowel obstruction if taken with too little water
- Osmotic: cramping, gas, diarrhea, dehydration and electrolyte loss (hypokalemia, hypernatremia with lactulose); hypermagnesemia from magnesium salts in kidney disease; sodium phosphate — hyperphosphatemia and acute phosphate nephropathy
- Stimulant: cramping, diarrhea; long-term overuse can cause electrolyte loss
- Mineral oil: lipoid pneumonia if aspirated, reduced absorption of fat-soluble vitamins, anal leakage
- Secretagogues: diarrhea; lubiprostone — nausea, dyspnea
- PAMORAs: abdominal pain, diarrhea, GI perforation (rare), opioid withdrawal symptoms
Antidiarrheals
- Loperamide: constipation, abdominal cramps; high doses (misuse) → QT prolongation, torsades, syncope, cardiac arrest
- Diphenoxylate–atropine: dry mouth, drowsiness, tachycardia; respiratory depression in children
- Octreotide: gallstones, glucose changes (hypo- or hyperglycemia), bradycardia, injection-site pain
Antiemetics
- QT-prolonging drugs (ondansetron, droperidol, prochlorperazine) — avoid with congenital long QT, hypokalemia or hypomagnesemia, and other QT drugs (some antiarrhythmics, macrolides, fluoroquinolones, antipsychotics, methadone)
- Metoclopramide: contraindicated in GI obstruction, perforation, or bleeding, pheochromocytoma, seizure disorders, and with other drugs causing EPS; reduce dose in kidney impairment; avoid in Parkinson disease
- Promethazine: contraindicated under 2 years; caution with respiratory disease; the preferred injection route is deep IM; IV use (December 2023 label) requires dilution to no more than 1 mg/mL and slow infusion over 20–40 minutes through a large vein (preferably a central line), never through hand or wrist veins; subcutaneous and intra-arterial injection are contraindicated
- Anticholinergics: narrow-angle glaucoma, urinary retention, prostatic hyperplasia; high-risk in older adults (Beers Criteria)
- Aprepitant: CYP3A4 interactions; reduces hormonal contraceptive effectiveness (backup for 1 month) and warfarin effect (check INR)
- Additive CNS depression with opioids, alcohol, benzodiazepines
Laxatives
- Do not give any laxative with undiagnosed abdominal pain, nausea and vomiting, suspected appendicitis, or bowel obstruction, or with fecal impaction above the rectum (manual removal or enema first)
- Magnesium and phosphate products: avoid in kidney impairment, heart failure; sodium phosphate enemas are avoided in young children and in kidney disease or dehydration
- Bisacodyl enteric-coated tablets: do not crush or chew; do not take within 1 hour of milk or antacids (early dissolution → gastric irritation)
- Mineral oil: avoid in clients at risk of aspiration (dysphagia, bedbound, young children)
- PAMORAs: contraindicated in known or suspected mechanical GI obstruction
- Psyllium separate from other drugs (can reduce absorption)
Antidiarrheals
- Avoid loperamide and diphenoxylate with bloody diarrhea, high fever, or suspected C. difficile or invasive bacterial infection (toxic megacolon, prolonged infection)
- Loperamide: not for children under 2; avoid with QT risk factors
- Diphenoxylate–atropine: contraindicated under 6 years (label); caution with liver disease; MAOIs
- Bismuth subsalicylate: avoid in children and teens with viral illness (Reye syndrome), with aspirin allergy or anticoagulants
- Assess the cause first — nausea from bowel obstruction, raised intracranial pressure, pregnancy, or drug toxicity needs different management; constipation or diarrhea needs a cause assessment before drugs
- Fluid and electrolyte status: vital signs, orthostatic changes, mucous membranes, urine output, daily weight, potassium, sodium, magnesium (normal potassium 3.5–5.0 mEq/L (mmol/L)); correct low potassium and magnesium before QT-prolonging antiemetics
- Aspiration safety for vomiting clients with reduced alertness: side-lying position, suction ready
- ECG when giving QT-prolonging antiemetics to clients with risk factors
- Time antiemetics before the trigger: 30–60 minutes before chemotherapy; scopolamine patch at least 4 hours before travel
- Watch for dystonia after metoclopramide or prochlorperazine; treat with diphenhydramine or benztropine as ordered; give IV metoclopramide slowly (over 1–2 minutes for a 10 mg bolus, or diluted) to reduce akathisia
- Promethazine injection: preferred deep IM; if IV is ordered, dilute and infuse over 20–40 minutes through a large vein (not the hand or wrist); stop at once for pain or burning at the site
- Bowel regimen with every opioid order (stimulant with or without softener); do not rely on bulk-forming laxatives alone for opioid constipation
- Record stool frequency, consistency, blood; C. difficile testing for new diarrhea after antibiotics, with contact precautions and soap-and-water hand hygiene
- Take bulk-forming laxatives with a full glass (240 mL) of water and drink fluids through the day
- Increase fiber (gradually), fluids, and activity; respond to the urge to defecate
- Avoid long-term routine stimulant laxative use unless advised (for example, with ongoing opioid therapy)
- Scopolamine patch: apply to clean, hairless skin behind the ear; wash hands after touching (pupil dilation and blurred vision if rubbed into the eye); remove before MRI
- Antiemetics and antihistamines cause drowsiness — no driving or alcohol
- Loperamide: do not exceed the label dose (8 mg/day over the counter unless a provider directs up to 16 mg/day); stop and seek care for fever, blood in stool, or diarrhea beyond 48 hours
- Oral rehydration solution is the key treatment of diarrhea in children and adults; sports drinks and sodas are not substitutes
- Report severe abdominal pain, abdominal distension, vomiting with no stool or gas passing (possible obstruction)
| Problem | Signs | Management |
|---|
| Acute dystonia (metoclopramide, prochlorperazine) | Neck twisting, oculogyric crisis, jaw spasm | Diphenhydramine or benztropine IV/IM; stop the drug |
| Tardive dyskinesia | Lip smacking, tongue movements | Stop metoclopramide; may be irreversible |
| QT prolongation/torsades (ondansetron, droperidol, loperamide misuse) | Palpitations, syncope | Stop the drug; ECG; IV magnesium sulfate for torsades; correct potassium |
| Loperamide or diphenoxylate overdose | CNS and respiratory depression, miosis, ileus | Naloxone (may need repeat doses); cardiac monitoring for loperamide |
| Anticholinergic toxicity (scopolamine, antihistamines) | Hot, dry, flushed skin; dilated pupils; delirium; urinary retention; tachycardia | Supportive; physostigmine in selected severe cases per toxicology |
| Serotonin syndrome (5-HT3 with other serotonergic drugs) | Agitation, hyperthermia, clonus, diarrhea | Stop the drugs; supportive; cyproheptadine per order |
| Laxative misuse | Dehydration, hypokalemia, weakness, dysrhythmia | Stop; fluid and electrolyte replacement; assess for eating disorder |
| Promethazine extravasation | Burning, pain, blanching, gangrene | Stop injection; notify at once |
- Match antiemetic to cause: 5-HT3 for chemo/postop; anticholinergic/antihistamine for motion sickness
- Ondansetron: QT prolongation, constipation; correct K⁺ and Mg²⁺
- Metoclopramide: tardive dyskinesia (boxed), no longer than 12 weeks; not in GI obstruction or seizures
- Promethazine: never under 2 years; deep IM preferred; tissue injury with IV
- Dystonia → diphenhydramine or benztropine
- No laxatives with undiagnosed abdominal pain or obstruction
- Bulk-forming laxatives need a full glass of water
- Opioids → start a stimulant laxative; PAMORAs contraindicated in obstruction
- No loperamide with bloody diarrhea, fever, or C. difficile; high doses → cardiac toxicity
- ORS is first-line for dehydration from diarrhea
- Magnesium and phosphate laxatives: avoid in kidney disease
Country Notes
United States
- The FDA limited the single IV dose of ondansetron to 16 mg (2012) because of QT prolongation, and added warnings about serious cardiac events with high-dose loperamide misuse (2016).
- Loperamide, bismuth subsalicylate, senna, bisacodyl, PEG 3350, and meclizine are sold over the counter.
Philippines
- Oral rehydration solution (locally called Oresol) and zinc supplementation for children with diarrhea are part of WHO/UNICEF-supported national child health programs; antidiarrheal drugs are not recommended for young children.
- Drugs are prescribed and labeled by generic name (Generics Act of 1988, RA 6675).