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Pharmacology - Anti-emetics (dropped image link (dropped image link…
Pharmacology - Anti-emetics
*Motion sickness (Non-Chemotherapy)
H1 M1 receptor antagonists
"H1 N1 Virus makes you sick"
"H1 N1 Virus makes you sick"
H1 M1 receptors in vestibular system
cause of motion sickness
H1 Histamine blockers
= DIPHEN and DIMEN
--> these can cause anti-ACH S/Es
--> benadryl vs dramamine for sleeping/motion sickness
diphenhydramine
= Benadryl
--> more severe allergies
dimenhydrinate
= dramamine/Gravol
--> motion sickness
chlorpheniramine
= Chlor-Trimeton
--> more for less severe allergies
--> allergic rhinitis (hay fever etc.)
M1 muscarinic blockers
= Amines
scopalamine
*M1 Anticholinergic Antiemetics
H1 - M1 antiemetics
--> think
"STOP CHOLINE M1"
-->
scopalamine
*H1 Frst generation Antihistamine Antiemetics
"DIPHEN DIMEN CHLORPHEN"
diphenhydramine
= Benadryl
dimenhydramine
= dramamine/Gravol
chlorpheniramine
-->
"CHLOR"
= high anticholinergic S/E's
--> CN 3 block = blurred vision and mydriasis
high side effects with FGA antihistamines
--> these can cause anti-ACH S/Es
*Histamine receptor Subtypes
H1 --> H4
H1
= smooth muscle and Central Vomiting Centre of brain
--> First generation Antihistamines - antiemetics
--> large anti-ACHS sideeffects
H2
= stomach and mast cells
--> ECL cells (Enterochromaffin-like cells) bind CCK on parietal cells to increaase gastric acid secretion
--> mast cells release histamine in Hhypersensitivity Type 1
*Gastric Infection EMESIS (Non-Chemotherapy)
5HT3 serotonin blockers
--> 5HT3s increase vagal tone back to the vomiting centre
--> think in the stomach there are 1,2,3 that affect
Ondanestron
= 5ht3 blocker = antiemetic
*Ondanestron
= 5ht3 blocker = antiemetic
1,2,3 receptors for GASTRIC ACID and EMESIS
ONLY 1 PUMP = H+/K+ ATPase for gastric acid
--> controlled by 3 different receptors
1,2,3 RECEPTORS for H+/K+ ATPase for gastric acid
1 PUMP
2 = H2 histamine
3 = M3 Ach for vagus
--> also 5HT3 serotonin at the vagus here for vomitting
--> target for serotonin blocker antiemetics
CHEMO
= D2 and 5ht3
motion sickness vestibular
= H1 M1
gastric sickness
= 5ht3
*Chemotherapy antiemetics
Monoamine blockers = Dopamine and Serotonin 5ht3 and
also Neurokinin 1 receptor blockers
*Chemotherapy type Antiemetics
note some of these can be used outside of chemo however
metaclopramide
--> can be used for gastroparesis and as a general anti emetic
*metaclopramide
note that metaclopramide is very strong since it has a double action
--> blocks D2 in the chemo trigger zone
--> blocks D2 in the stomach directly
note that metaclopramide also has a slight block on 5ht receptors in both
can be used for gastroparesis and as a general anti emetic
inhibits D2 receptors in the stomach
contraindicated in parkinson syndrome
*Pathophys of Nausea
vommiting reflex
mouth and stomach through CN9 = mouth and CN 10 = stomach
CTZ = chemo trigger zone
NTS = nucleus tractus soltaris
--> combines all the information for the body
--> the TRUE vomiting centre