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Antiemetic drugs

Phenothiazines Benzodiazepines
-Prochlorperazine act by blocking dopamine -antiemetic potency of lorazepam and alprazolam is
receptors low
-effective against low or moderately emetogenic -beneficial effects may be due to their sedative,
chemotherapeutic agents anxiolytic, and amnesic properties
5-HT3 receptor blockers -useful in treating anticipatory vomiting
-ondansetron, granisetron, palonosetron , and Corticosteroids
dolasetron -Dexamethasone and methylprednisolone used
-selectively block 5-HT3 receptors in the alone, are effective against mildly to moderately
periphery (visceral vagal afferent fibers) and in the emetogenic chemotherapy
brain (CTZ) -Most frequently,they are used in combination
-longer duration of action and superior efficacy -mechanism is not known (maybe PG)
-also useful in the management of postoperative Substance P/neurokinin-1 receptor blocker
nausea and vomiting -Aprepitant targets the neurokinin receptor in the
Substituted benzamides brain and blocks the actions of the natural substance
-metoclopramide is effective at high doses against -indicated only for highly or moderately emetogenic
the emetogenic cisplatin->inhibition of dopamine in chemotherapy
the CTZ -usually with dexamethasone and a 5-HT3 anta.
-extrapyramidal symptoms, limit long-term high- Combination regimens
dose use -to increase antiemetic activity or decrease toxicity
Butyrophenones -dexamethasone, increase antiemetic activity when
-Droperidol and haloperidol act by blocking given with high-dose metoclopramide, a
dopamine receptors 5-HT3 antagonist, phenothiazine, butyrophenone, or
-moderately effective antiemetics a benzodiazepine
-may prolong the QTc interval

Antidiarrheals

Antimotility agents Adsorbents


-diphenoxylate and loperamide -aluminum hydroxide and methylcellulose
-analogs of meperidine and have opioid-like are used to control diarrhea
actions on the gut -adsorbing intestinal toxins or microorganisms
-activate presynaptic opioid receptors in the and/or by coating or protecting the intestinal
enteric nervous system to inhibit acetylcholine mucosa (less effectiva than antimot. agents)
release and decrease peristalsis Agents that modify fluid and electrolyte trans.
-can contribute to toxic megacolon, they should -Bismuth subsalicylate, used for traveler’s
not be used in young children or in patients diarrhea->decreases fluid secretion in bowel
with severe colitis -action may be due to its salicylate component
as well as its coating action
-Adverse effects may include black tongue and
black stools

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