GI Drugs - Kumar TS Flashcards
Which appetite stimulant is used in cats and acts through GABA?
diazepam (valium)
What neurotransmitter stimulates appetite? Which one inhibits appetite?
Stimulated by GABA
inhibited by serotonin
Which appetite stimulant for cats is an antihistaminic and antiserotonin agent?
cyproheptadine
What is the anti obesity drug used for dogs?
dirlotapide
What animals are NOT able to vomit effectively?
horses, ruminants, rodents
What are the the 4 afferent sources that can stimulate vomiting?
CTZ
vestibular
peripheral sensory receptors
higher CNS
What are the 5 neurotransmitters involved in vomiting?
dopamine, histamine, serotonin, Ach, substance P
What is the most important neurotransmitter for the CTZ to initiate vomiting?
dopamine
What is the neurotransmitters used to cause vomiting in the vestibular system?
Histamine and muscarinic
What is the primary neurotransmitter for peripheral sensory receptors?
acetylcholinne
What are the transmtters used for higher CNS centres for vomiting?
cholinergic and histamine
What pathway initiates emesis from increased intracranial pressure?
limbic pathway
What is the primary neurotransmitter used in psychogenic vomiting?
acetylcholine
Where are NK-1 receptors found?
emetic center and CTZ
Which peripheral acting emetic should not be dosed twice in cats?
ipecac
What are the 3 peripheral acting/reflex emetics?
salt water, hydrogen peroxide, ipecac
What are the 2 centrally acting emetics?
apomorphine
xylazine
Which centrally acting emetic is used in cats?
xylazine
What is the MOA for apomorphine?
opiod - dopaminergic receptors in CTZ`
How is apomorphine adminisstered?
subq or conjuctival
What is the contraindication of apomorphine?
animals with existing central depression because it depresses respiratory centers
What is the MOA of xylazine?
stimulates alpha 2 receptors in CTZ
What are the side effects of xylazine?
bradycardia
What can be used to prevent emesis at the vestibular apparatus?
anti histamines
What antimuscarinic can cross the BBB in dogs to prevent emesis?
scopolamine
What are the SE of antimuscarinics?
xerostomia, drowsiness, constipation, urine retention
What are the 5 anti emetic drugs acting on the CTZ?
- phenothiazines
- butyrophenone derivatives
- metoclopramide
- peripheral serotonin antagonists
- Nk1 receptor blockers - cerenia
What antiemetic drugs are “broad” spectrum?
phenothiazines
What should be done before giving animals phenothiazines (ace)?
fluid replacement
What are the contraindications of phenothiazines?
animals with seizures
What anti emetic effectively antagonizes apomorphine induced emesis?
metoclopramide
What is the MOA for metoclopramide?
dopamine antagonist, serotonin agonist and serotonin receptor antagoonist to CTZ
What CTZ anti emetic blocks transmission to CTZ an interferes with action of serotonin on peripheral receptors in GI tract?
peripheral serotonin antagonists (cyproheptadine)
What drug acts by blocking NK-1 receptor?
maropitant citrate (cerenia)
Why can’t cerenia be used in puppies less than 11 weeks of age?
can induce bone marrow hypocellularity
What are the 3 ways anticholinergic drugs exert its antiemetic activity?
inhibit vagus
relax GI smooth muscle
inhibit GI secretions
What receptors do butyrophenone derivatives act on?
antidopaminergic
What are the 2 SE of butyrophenone derivatives?
sedation and hypotension
What drug effectively antagonizes apomorphine induced emesis?
metoclopramide (reglan)
Why is the bioavailability of metclopramide only 50%?
extensive hepatic first pass metabolism
What are the SE of metclopramide in horses and cats?
hyperactivity, restlessness, tremors
What group of drugs are indicated for emesis induced by chemotherapeutic agents?
peripheral serotonin antagonists
What peripheral serotonin antagonist is used in small animals?
cyproheptadine (periactin)
What are some other examples of peripheral serotonin antagonists?
granisetron, palonosetron, ondansetron
What anti emetic is a NK-1 receptor blocker?
maropitant citrate (cerenia)
What is the contraindication of maropitant citrate (cerenia)?
puppies less than 11 weeks - bone marrow hypocellularity
What are the 3 ways anticholinergics exert antimetic activity?
inhibit vagus
relax GI spasm
inhibit GI secretions
What is the one drawback of anticholinergic drugs?
delays gastric emptying - dont use for more than 3 days
What are the 3 MOA for drugs to modulate gastric acid secretion?
block endogenous secretagogues
block proton pump
enhance cytoprotective effect
Which antisecretory drug is anticholinergic and selective for gastric M1 receptors?
pirenzepine
Which H2 receptor antagonist (of the antisecretory drugs) has the longest duration of action?
famotidine
What is the order of potency for H2 receptor antagonists of the antisecretory drugs?
famotidine>ranitidine>nizatidine>cimetidine