Pharm 2 - GI 1

acramer's version from 2016-10-11 14:29

Appetite stimulants and suppressants

Question Answer
appetite stimulents are called ___ agentsOrexigenic agents
what is the neurotransmitter responsible for appetite stimulation, and is it excitatory or inhibitory?GABA, inhibitory
what main group of drugs which work as orexigenic agents?benzodiazepines
which two benzodiazepines are use as appetite stimulants? In who? how do benzos work?Diazepam (and oxazepam). (review said works as a serotonergic antagonist. Notes say "GABA-induced action and central inhibition of the satiety center"). Most effective in CATS.
how does Cyproheptadine work? WHO is this used in?serotonergic antagonist. CATS. (if you dont give kitty liver it will antagonize his happiness, ie, serotonin)
which appetite stimulants are used in both dogs AND cats?glucocorticoids, B-vitamins, anabolic steroids(Megestrolacetate)
which appetite stimulants are used in just cats (usually)?benzodiazepines and cyproheptadine (kitty wants to eat liver)
what is the neurotransmitter responsible for appetite inhibition?serotonin (you're happy and full so you stop eating)
appetite suppressants are called ___ agentsanorectic agents
what is the anorectic agent?Slentrol = Dirlotapide ( DIRL wont get TAPed because he's too fat!!)
what is Dirlotapide and what is its MOA? explain how it works.anorectic(appetite suppressent) agent. MOA= inhibitor of microsomal triglyceride transfer protein which means it interferes with absorption of fat from sm intestine.
Dirlotapide is used in who? Contraindictions?DOGS. Don't use in patients with Liver Disease, Cushing's Disease, corticosteroid use, or growing pups


Question Answer
Name the 5 neurotransmitters involved in emesisdopamine, histamine, serotonin, acetylcholine, and substance P
in emesis, what is the receptor dopamine is acting on?D2 (muscarinic receptor) (vomit is closer to D #2 than it is to D #1)
in emesis, what is the receptor histamine is acting on?H1
in emesis, what is the receptor serotonin is acting on?5-HT(3) (three for e... e as in emesis)
in emesis, what is the receptor acetylcholine is acting on?M1
in emesis, what is the receptor substance P is acting on?Neurokinin NK-1 receptor
what is the "higher emetic center"? what is a unique property about it, as a structure of the brain?CTZ (chemoreceptor trigger zone). No protected by blood brain barrier!--> so chemicals in the blood can affect the CTZ to trigger vomiting
explain the main neurotransmission associated with CTZ, and then the other which also contributeMAINLY DOPAMINE but also serotonin (5-HT3), cholinergic (M1), histamine (H1), and adrenergic (alpha 2).
how does the vestibular system relate to emesis? What are the neurotransmitters involved?info from inner ear or changes in movement (leading to motion sickness) can trigger the CTZ. The main NTs involved in this are histamine (H1, histaminergic) and Acetylcholine (M1, muscarinic) (hear a HM in your ear)
based on what you know about the neutrotransmitters involved in vestibular-system induced emesis (motion sickness), what kind of drugs do you use to treat this?antihistiminergics! (because NTs involved are histamine and acetylcholine)
peripheral sensory receptors of emesis are mediated by which NTs?acetylcholine and serotonin are what mediate the impulses (Ace's limbs were happy even though he had just vomited)
higher CNS center neurotransmission of emesis occurs from what two places?cerebral cortex and limbic system
what are the PERIPHERALLY acting emetics? (basis on how peripherally acting emetics work?) (3)(work by irritating GI mucosa) (1) saline solution (2) 3% hydrogen peroxide solution (3) Syrup of Ipecac
what type of emetic is Syrup of Ipecac, and how does it work?PERIPHERALLY acting emetic, active principle emetine –an irritant alkaloid (emetine looks like emetic)
what is emetine?active ingredient of syrup of ipecac, is an irritant alkaloid
what is the PD characteristic necessary for a emetic to be centrally acting?must be able to cross BBB
what are the centrally acting emetics? WHO is each one used in?Apomorphine hydrochloride (DOGS) and xylazine (CATS)
what is Apomorphine hydrochloride? WHO do you use it in? MOA? contraindications? route of admin?centrally acting emetic for DOGS. MOA=stimulation of dopaminergic(D2receptors) in the CTZ (remember D vomit is closer to D#2, and of course morphine would be DOPE). Is an opioid (morphine derivative) so DON'T use in centrally depressed dogs (or they will stop breathing). Admin (sub?)conjunctivally
dont use in centrally depressed dogsApomorphine hydrochloride
(sub)conjunctival administrationApomorphine hydrochloride
what is xylazine? who do you use it in? MOA?centrally acting emetic for CATS. MOA= Acts by stimulating alpha-2 receptors in CTZ
antihistiminergics are used for what? MOA?centrally acting anti-emetics, blocks H1 receptors in CTZ and in vestibular apparatus (1 in the brain, bc brain most important, H2 in the belly, because less important)
what are the antihistiminergics used for centrally acting anti-emetics?cyclizine hydrochloride, dimenhydrinate, diphenhydramine hydrochloride (vicious cycle of benadryl)
what are Antimuscarinics used for? (what is their MOA?) centrally acting anti-emetics (blocks M1 receptors)
what are the antimuscarinics used for centrally acting anti-emetics, and which is the preferred one?Belladonna alkaloids--> atropine, scopolamine(preferred), isopropamide iodide ( Mother belladonna will SCOPE you out)
scopolamine is a what, used for what?antimuscarinic, anti-emetic, for MOTION SICKNESS (you can then scope out whats out the window of the car without barfing)
what is the group of drugs which act as antidopaminergics? what are these used for?Phenothiazine derivatives, as centrally-acting anti-emetics
what are the Phenothiazine derivatives? what is their MOA/ what should you know about them? side effects?chlorpromazine, triflupromazine, prochlorperazine, promethazine (ALL END IN ZINE). Work as antidopaminergics, HOWEVER, you should know that they are BROAD SPECTRUM and so they are alpha-1 adrenergic receptor antagonist and weak antihistamine and anticholinergic ALSO! NOTE-- because of blocking of alpha-1 receptor, hypotension is a side effect (my thighs so broad you'd faint)
what are Butyrophenones used for? what are they (drugs) and what is their MOA?Centrally acting anti-emetics, Haloperidol, droperidol, antagonizes dopamine receptors (the but is a drop of halo in my dope)
Haloperidol- is what? for what?Centrally acting anti-emetics, antagonizes dopamine receptors (that halo looks dope on you)
droperidol- is what? for what?Centrally acting anti-emetics, antagonizes dopamine receptors (drop that (anti)dopamine right onto my brain)
Metoclopramide's MOA? is used as a what? Any special properities, and any special uses?dopominergic antagonist used as a centrally- acting anti-emetic. PROKINETIC agent (inc stomach emptying mvt) and also it antagonizes apomorphine-induced emesis
antagonizes apomorphine-induced emesisMetoclopramide (Clop right down on your dope party)
prokinetic agent which is also an anti-emetic?Metoclopramide (clop is a pro at being a prokinetic AND an antiemetic)
Peripheral 5-HT3 serotonin antagonists--> what are they? What are they used for?Granisetron, Ondansetron–control emesis induced by chemotherapeutic agents/radiation therapy in small animals ( A grani on dan makes him SO HAPPY in all of his limbs)
control emesis induced by chemotherapeutic agents/radiation therapy in small animalsGranisetron, Ondansetron
what is the NK-1 receptor blocker drug? what is it used for? what should you know about it? Side effects?Maropitant citrate, centrally acting anti-emetic, FDA approved. Bone marrow hypocellularity in young puppies
FDA approved drugMaropitant citrate
Bone marrow hypocellularity in young puppiesMaropitant citrate (citric acid will burn out your bone marrow)
Broad spectrum antiemetic?Phenothiazine (my thighs are so broad)
drugs to tx emesis associated with labyrinthine inflammationanti-histamines
NK-1 receptor blocker and its significanceMaropitant citrate, blocks substance P action in CNS and is FDA approved ( the FDA NowKills oranges Painfully via GMOs)
SO, what are the 4(5) main groups of drugs used as centrally-acting anti-emetics?(1) Antihistaminergics (2) Antimuscarinics(scopolamine) (3) Antidopaminergics(Phenothiazine derivatives, Butyrophenones, Metoclopramide) (4) NK-1 receptor blockers (Maropitant citrate) ( (5)Peripheral 5-HT3 serotonin antagonists (Granisetron+Ondansetron) )
Peripherally acting anti-emetics work in what ways? (3)relieve gastric irritations, reduce excess secretion of gastric acid, modulate GI motility
Anticholinergics/antimuscarinics acting peripherally as anti-emetics are? MOA?Glycopyrrolate, propantheline, methscopolamine. MOA= (modulators of gastric motility!) inhibiting vagal afferent impulses, and also inhibition of GI smooth muscle spasms (glycogen and propane together make meth-scopolamine which will stop your GI from spaseming REALLY fast)
prokinetic agents (inc gastric emptying) used as peripheral anti-emetics? (2)metoclopramide, domperidone (clop clop into your sm intestine, push it along with some domperidone)
what are the GI cytoprotectants used as peripheral anti-emetics?kaolin, pectin and bismuth salts
why are anti-ulcer drugs used as peripherally acting anti-emetics?dec acid secretion which dec irritation (irritation causes vomiting)

Gastric acid secretion/Gastric anti-secretorydrugs

Question Answer
gastric acid is secreted by what, and is dependent on what endogenous agonists for it's production?produced by parietal cells (oxyntic) cells. Agonists are: Histamine(H2!!, Gs proteins), Acetylcholine, Gastrin(hormone made in G cells in stomach)
how do prostaglandins relate to gastric acid secretion?they DEC amount of gastric acid made and INC mucous and bicard formation (cytoprotective)
what are the main categories of Gastric anti-secretorydrugs?(1) anticholinergics (2) H2 receptor antagonists (3) Proton pump inhibitors (4) Prostaglandin E1 analogue
what are big complications of inhibiting gastric acid secretion?Achlorhydria(on chronic use), and malabsorption of certain nutrients (vit.B12and iron). REBOUND HYPERSECRETION OF ACID (except for misoprostol) will cause possible RELAPSE of GASTRODUODEINAL ULCERS! Also dec acid will dec acid barrier to kill unwanted bacteria (prolif of bacteria) and if lots of bact, possible to develop aspiration pneumonia from bact then
what is the preferred anticholinergic (antimuscarinic) anti-secretory drug? what are the others? (why this distinction?)Pirenzepine is the preferred drug because it is selective for the M1 receptor! the other two are Atropine and propantheline, which are non-selective (target M1, 2, and 3). (Pi goes in the belly and you say M!)
which H-receptor do you antagonize to dec gastric secretions? what are the drugs in this category? what should you know about these drugs?Target H2. Know that they VARY IN POTENTCY! the drugs are Famotidine>Ranitidine=Nizatidine>Cimetidine (I dine on antihistimines)
list the H2 recetor antagonists from most to least potentFamotidine>Ranitidine=Nizatidine>Cimetidine
which H2 receptor antagonist is preferred for liver dz pts, and why?Nizatidine, because there is no hepatic metabolism (renal excretion) (for nizzle my lizzle)
which H2 receptor antagonist inhibits CYP450, and what implication can this have?Cimetidine, preferred for acetminophen tox (also might cause thrombocytopenia)
preferred for acetminophen tox, and why?Cimetidine, bc inhibits CYP450 (CIM and aCET)
no hepatic metabolism Nizatidine
what is the "proton pump" pumping?H+/K+-ATPasepump
what is the proton pump inhibitor drug? how does it work and what should you know about it?Omeprazole. IRREVERSIBLE inhibition--> so most powerful gastric acid secretion inhibitor (NOTE: side effects are suppression of acid barrier for bact invasion, and aspiration pneumonia due to inc bact in stomach)
most powerful gastric acid secretion inhibitor?omeprazole (irreversible) (oh me oh my, kristen needs omeprazole)
best drug to combine with antibiotics to fight helicobacter pylori infectionomeprazole (usually combined with clarithromycin or ampicillin/amoxicillin etc) (most powerful stop for the most powerful abx arent deactivated)
what is the Prostaglandin E analogue drug? what is important to know about this drug?(PGE1) Misoprostol- undergoes hepatic first-pass effect to form active misoprostol acid, SO does not alter serum gastrinlevels -->no rebound acid hypersecretion (miso soup on my prostate)
no rebound acid hypersecretionmisoprostol (miso soup is perfect for your tummy probs)