Antiemetics Flashcards
Activation of vomit center
Direct - upsetting sights/smells/pain. Direct from sensor organs, fear or anticipation
Indirect - activations of chemoreceptor trigger zone by either stomach/small intestine sending signals or drugs (anticancer/opioids, ipecac) activating CTZ
Receptors involved in emetic response
Serotonin, glucocorticoids, substance P, neurokinin, dopamine, acetylcholine, histamine
Ondansetron
Serotonin receptor antagonist (5-HT3) in the chemoreceptor trigger zone (CTZ) and afferent vagal neurons in upper GI tract.
Even more effective combined with dex
Glucocorticoids as antiemetics
Methylprednisolone (solumedrol) and dex. Mechanism unknown
Aprepitant
Substance P/neurokinin1 antagonist. Prolonged duration of action, but should be combined with other drugs (good with dex or zofran)
Inhibitor and inducer of CYP3A4 so has complicated drug reactions
Benzos for antiemetics
Lorazepam in combo for CINV (chemotherapy induced). Helps sedate, suppress emesis and anterograde amnesia. Also good for EPS from other antiemetics like phenothiazine
Dopamine antagonists
Sides of EPS, antichol effects, hypotension and sedation
Promethazine (phenergan) - resp depression and local tissue injury
Butyrophenones for antiemetic
Haloperidol and droperidol (inapsine)
Also block D2 receptors in CTZ
Metoclopramide
Reglan
Blocks dope receptors in CTZ
Cisplantin
Chemo drug with max N/V 48-72 hours after
Hyperemisis gravidum
Hypokalemia, dehydration, 5% loss of body weight, ketonuria
Doxylamine plus B6 (pyridoxine) is effective without negative fetal outcomes
Scopolamine
Muscarinic antagonist
Blocks neuronal pathway from inner ear to vomit center
Dry mouth, blurred vision, drowsiness, urinary retention, constipation, disorientation
Antihistamines for motion sickness
Dimenhydrinate which block receptors for acteylcholine and histamine which both contribute to antiemetic effects
Two main ways CTZ activated
Signals from stomach and small intestine
Direct action of chemicals
Receptors involved in vomiting
Serotonin (5HT3) Glucocorticoids Substance P Neurokinin Dopamine Histamine ACH
Serotonin receptor antagonists
Zofran, best for chemotherapy, radiation, anesthesia, viral gastritis, preggo
Zofran MOA
Blocks 5ht3 serotonin receptors in CTZ and upper GI
Zofran adverse
Headache, dizzy, Diarrhea, GI, QT prolongation
4mg IV
8mg IM
Peds 0.1mg/kg SIVP max 4mg
Metoclopramide
Blocks dopamine/serotonin receptors in CTZ, also increases upper GI motility by enhancing Ach
Good for post operative procedures, also good for chemo/opioids/toxins
Metoclopramide interactions and adverse
EPS, sedation, diarrhea
Antipsychos and MAOIs may interact
Contras are bowel obstruction/perforation/bleeding, EPS, seizures, hypersens
Metoclopramide dose
10mg IV in 50mL over 15 minutes or 10 IM for migraine
For nausea over 5 minutes or 10mg IM still
No repeats