ANTI-EMETIC

&
ANTI-NAUSEA AGENTS
Prof. Lopez
NUR 103: Pharmacology
 Definitions
■ Nausea
■ Emesis (vomiting)
■ Antiemetic agents
VC and CTZ

■ Vomiting center (VC)

■ Chemoreceptor trigger
zone (CTZ)
■ Neurotransmitters
– Acetylcholine
– Dopamine
– Histamine
– Prostaglandins
– Serotonin (5-HT3)
– Substance P (Neurokinin
1)
Anti-emetics
and Anti-
nausea Drugs

■ Anticholinergic drugs
■ Antihistamines
(histamine 1 [H1]
receptor blockers)
■ Antidopaminergic drugs
■ Neurokinin Antagonists
■ Prokinetic drugs
■ Serotonin blockers
■ Tetrahydrocannabinoids

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Anticholinergics
(Acetylcholine blockers)
■ MOA
– Blocks Ach receptors deep in the brain
– Dry up GI secretions, reduce smooth muscle spasms
■ Drug
■ SCOPOLAMINE [C]: Belladonna alkaloid
– Use: Motion sickness prophylaxis & postop n/v
– Contraindicated: narrow angle glaucoma
– AE: related to anticholinergic properties
– Formulation: ____________
– Dose: Apply 1 patch to hairless area behind 1 ear every 3
days, 4 hours before travel
Antihistamines (H-1 Receptor
Blockers)
■ Block H-1 receptors to prevent Ach from binding to
receptors
■ Anticholinergic properties
■ Drugs
– Diphenhydramine, dimenhydrinate, meclizine,
hydroxyzine-Anticholinergic antihistamine
■ Uses: Motion sickness, n/v
– AE: Drowsiness, dizziness, confusion, Anticholinergic
effects
– Contra: shock and lactation [meclizine]-B
– Dosing: 25-50 mg 1 hours before travel & repeat daily
during travel; PO: 25-100 mg/day, divided 1-4 times
daily
Anti-dopaminergics
■ MOA:
– Block dopamine receptors in the CTZ
– Also used for psychotic disorders, intractable hiccups
– Drugs: Phenothiazine
– Prochlorperazine: PO, IM, PR, IV [c]
– Promethazine: IM, IV, PO [c]
■ Sedation common

– Droperidol: BLACK BOX WARNING

■ Wide/Prolonged QT interval on EKG
 Neurokinin Inhibitor
[Substance P]
■ Aprepitant [B] ■ Fosaprepitant
■ MOA: inhibits Substance – IV form of aprepitant
P/neurotkinin 1 receptors ■ Akynzeo
■ Uses: prevents n/v associated – New combo: 5-HT3
with high emetogenic [palonsetron] & substance P
chemotherapy Rx: high dose inhibitor [netupitant
cisplatin; postop n/v
■ Interaction
– Warfarin, oral contraceptives
– Cytochrome P-450 enzyme
inhibitor
■ Route: PO
Prokinetic
MOA: promote movement of substances via GI
tract & increase GI motility
Drug: metocloperamide [B]-Dopamine antagonist
Uses: delayed gastric emptying &
Gastroesophageal reflux, anti-emetic
Contra: seizures, pheochromocytoma, Breast Ca
or GI obstruction, allergy to procaine or
procainamide
AE TREMORS: [Extrapyramidal effects}, tardive
dyskinesia [long-term use]
 Serotonin Blockers [5-HT3
receptor blockers]
Block serotonin receptors in the
GI tract, CTZ, and VC
Used for nausea and vomiting in
patients receiving chemotherapy
and for postoperative nausea and
vomiting
Examples
■ Dolasetron- no longer
recommended
■ granisetron [patch]
■ ondansetron (Zofran)-[B]
prototype
■ palonosetron
■ Ondansetron
– Chemo-induced n/v, postop n/v;
hyperemesis gravidarum
– Form: PO, Parenteral & PO
disintegrating
– IV: 8 mcg can be given IVP over
2-5 minutes
– Concern: cleft palate
deverlopment in fetus 1st
trimester
– *Potential for
__PROLONGED/WIDE QT
Tetrahydrocannabinoids
■ Dronabinol
■ Synthetic derivative of THC
■ Uses: n/v from chemo; anorexia: appetite
enhancer & weight gain
– Cancer and HIV patients benefit
■ Route: PO
■ Controlled Substance
Miscellaneous

■ Phosphorated cabohydrate solution

■ MOA: local action on walls of GI tract
■ Uses: control mild cases n/v; morning
sickness {unlabeled use}
■ Route: PO solution
Herbal Products: Ginger
[Zingiber officinate
■ Uses: antioxidant & relief of nausea and vomiting,
(chemotherapy, morning sickness, and motion
sickness
■ Adverse effects
– Anorexia, nausea and vomiting, skin reactions
■ Drug interactions
– May decrease absorption of oral medications
– Increase bleeding risk with anticoagulants &
antiplateltets: warfarin, clopidrogel

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Pediatric Consideration

■ Syrup of Ipecac & Poisoning

■ NO LONGER USED as home treatment for
poisoning (aap, 2003)
■ Parent must call PCC hotline @ 800-222-
1222
Nursing Considerations
■ Assess complete nausea and vomiting history, including
precipitating factors.
■ Assess current medications.
■ Assess for contraindications and potential drug interactions
■ Many of these drugs cause severe drowsiness; warn patients
about driving or performing any hazardous tasks.
■ Taking anti-emetics with alcohol may cause severe central
nervous system depression.
■ Teach patients to change positions slowly to avoid
hypotensive effects
Nursing Considerations
■ Chemotherapy: given _30-60 minutes before chemotherapy
begins
■ Surgical procedures: 30 before end
■ Peds: cautious use-paradoxical reaction
■ Older: CNS changes, hypotension, psychotic-type reaction
■ Antidopaminergics:
– Cautious assessment for signs and symptoms of dehydration
or electrolyte imbalance with checking skin turgor and
examining the tongue for the presence of longitudinal
furrows.
– Monitor vital signs, especially blood pressure and pulse rate
– Monitor EKG: Seronton 5-HT: Ondestron: QT wide/prolonged
Nursing Considerations
■ Undiluted forms of diphenhydramine: cautious
IV use at rate of 25 mg/min
■ Aprepitant: Monitor INR before each cycle
■ Promethazine: give without regard to meals
■ Metoclopramide given orally is best taken 30
minutes before meals and at bedtime
■ Metoclopramide: EPS reactions: report
immeditely
■ Educate pt regarding long-term use effects
Nursing Considerations
■ Scopolamine: apply patch behind ear as directed
– Instruct regarding activities that require mental
alertness
– Instruct to leave patch in place for 72 as indicated
■ Instruct to AVOID alcohol
■ Dronabinol: give 1-3 hours before chemo; can take
at home before treatment appointment
■ Antihistamines: Think safety: Drowsiness, dizzines,
sedation