Antiemetics, Laxatives, and Antidiarrheals | MyMerci
제안하기
0 / 2000

Antiemetics, Laxatives, and Antidiarrheals

Unit 9 · Topic 47Antiemetics, Laxatives, and Antidiarrheals
1.Mechanism of Action

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 classReceptor blockedBest 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 emptyingPostoperative, migraine-associated, gastroparesis
NK1 antagonists (aprepitant, fosaprepitant)Substance P/neurokinin-1Acute and delayed chemotherapy nausea
Antihistamines/anticholinergics (meclizine, dimenhydrinate, promethazine, scopolamine)H1 and muscarinicMotion sickness, vertigo
Corticosteroid (dexamethasone)UncertainAdded to chemotherapy and postoperative regimens
Cannabinoids (dronabinol)CB1Refractory 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
2.Indications & Key Drugs
Drug (generic)Key useKey point
Ondansetron (prototype 5-HT3)Chemotherapy, postoperative, gastroenteritis nauseaQT prolongation; constipation, headache
MetoclopramideGastroparesis, postoperative nauseaBoxed warning: tardive dyskinesia — avoid longer than 12 weeks
ProchlorperazineNausea, migraineBoxed warning: increased mortality in older adults with dementia-related psychosis; EPS, sedation, hypotension
PromethazineNausea, motion sickness, allergyBoxed warnings: respiratory death under age 2; severe tissue injury/gangrene with injection
DroperidolPostoperative nauseaBoxed warning: QT prolongation, torsades
Aprepitant/fosaprepitantHighly emetogenic chemotherapy (with a 5-HT3 antagonist and dexamethasone)CYP3A4 interactions
Scopolamine patchMotion sickness, postoperative nauseaBehind the ear 4 hours before travel
Meclizine, dimenhydrinateMotion sickness, vertigoDrowsiness; anticholinergic
Doxylamine–pyridoxineNausea and vomiting of pregnancy (first-line drug)Drowsiness
PsylliumChronic constipation, IBSFull glass of fluid
PEG 3350Constipation; bowel preparationWell tolerated
LactuloseConstipation; hepatic encephalopathyBloating, diarrhea, electrolyte loss
Senna, bisacodylConstipation; opioid-induced constipationCramping
DocusateSoftening stool (limited benefit)Not enough alone for opioid constipation
Methylnaltrexone, naloxegolOpioid-induced constipation not helped by laxativesContraindicated in bowel obstruction
Linaclotide, lubiprostoneChronic idiopathic constipation, IBS-CDiarrhea; linaclotide contraindicated under age 2
Loperamide (prototype antidiarrheal)Non-infectious acute or chronic diarrhea, traveler's diarrhea without fever or bloodCardiac toxicity at high doses
Diphenoxylate–atropineDiarrheaUS Schedule V; atropine discourages misuse
ORSDehydration from diarrheaFirst-line in all ages
3.Adverse Effects

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
4.Contraindications, Cautions & Interactions

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
5.Monitoring & Nursing Interventions
  1. 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
  2. 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
  3. Aspiration safety for vomiting clients with reduced alertness: side-lying position, suction ready
  4. ECG when giving QT-prolonging antiemetics to clients with risk factors
  5. Time antiemetics before the trigger: 30–60 minutes before chemotherapy; scopolamine patch at least 4 hours before travel
  6. 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
  7. 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
  8. Bowel regimen with every opioid order (stimulant with or without softener); do not rely on bulk-forming laxatives alone for opioid constipation
  9. Record stool frequency, consistency, blood; C. difficile testing for new diarrhea after antibiotics, with contact precautions and soap-and-water hand hygiene
6.Client Education
  • 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)
7.Toxicity, Overdose & Antidotes
ProblemSignsManagement
Acute dystonia (metoclopramide, prochlorperazine)Neck twisting, oculogyric crisis, jaw spasmDiphenhydramine or benztropine IV/IM; stop the drug
Tardive dyskinesiaLip smacking, tongue movementsStop metoclopramide; may be irreversible
QT prolongation/torsades (ondansetron, droperidol, loperamide misuse)Palpitations, syncopeStop the drug; ECG; IV magnesium sulfate for torsades; correct potassium
Loperamide or diphenoxylate overdoseCNS and respiratory depression, miosis, ileusNaloxone (may need repeat doses); cardiac monitoring for loperamide
Anticholinergic toxicity (scopolamine, antihistamines)Hot, dry, flushed skin; dilated pupils; delirium; urinary retention; tachycardiaSupportive; physostigmine in selected severe cases per toxicology
Serotonin syndrome (5-HT3 with other serotonergic drugs)Agitation, hyperthermia, clonus, diarrheaStop the drugs; supportive; cyproheptadine per order
Laxative misuseDehydration, hypokalemia, weakness, dysrhythmiaStop; fluid and electrolyte replacement; assess for eating disorder
Promethazine extravasationBurning, pain, blanching, gangreneStop injection; notify at once
8.High-Yield Points
  • 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).

다음 이론을 계속 학습하려면 로그인하세요.

로그인하고 계속 학습
컨텐츠를 그만볼래?

필기노트, 하이라이터, 메모는 잘 쓰고 있어?

내보내줘
어떤 폴더에 저장할래?

컨텐츠 노트에는 총 0개의 폴더가 있어!

폴더 만들기
컨텐츠 만들기
만들기
신고했어요.

운영진이 검토할게요!

해당 유저를 차단했어요.

마이페이지에서 차단한 회원을 관리할 수 있어요.