GI therapy Flashcards

1
Q

Drugs affecting appetite

A

-dirlotapide, anabolic steroids, benzodiazepines (valium, oxazepam), cyproheptadine,mirtazapine, megestrol acetate.
-also B vitamines and glucocorticoids (increase gluconeogenesis and antagonize insulin for hyperglycaemic effect)(steroid euphoria -increases appetite)
(catabolic efffect)

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2
Q

Dirlotapide (Sientrol)

A
  • microsomal triglyceride transfer protein (MTP) inhibitor developed to help dogs lose weight
  • reduced fat absorption and satiety signal from lipid filled enterocytes and reduced appetite by increase peptide YY release into circulation
  • not used in cats
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3
Q

Anabolic steroids

A
  • synthetic derivatives of testosterone that have enhanced anabolic effects with reduced androgenic effects
  • antagonize catabolic effect of glucocorticoids and the negative nitrogen balance (need increase protein calories to improve N balance)
  • stimulate hematopoiesis, appetite and weight gain.
  • controlled, compounding pharmacy
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4
Q

Benzodiazepines

A
  • GABA induced effects and central inhibition of satiety centre in hypothalamus make it an effective appetite stimulant in cats.
  • not effective appetite stimulants in dogs
  • diazepam: IV, IM or oral. Cats will eat within a few sec of IV so have food ready
  • Oxazepam: -less sedative then diazepam but also less effective at stimulating appetite
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5
Q

Cyproheptadine (Periactin)

A
  • antihistamine with serotonin antagonist action. also blocks Ca channels
  • increase appetite by inhibiting serotonergic receptors that control satiety
  • used in cats (may get CNS excitement and aggression and decrease seizure threshold)
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6
Q

Mirtazapine (Remeron)

A
  • antidepressant
  • {NASSA) antagonist of presynaptic alpha 2 adrenergic receptors on NE and serotonin presynaptic neurons plus antagonist of post synaptic serotonin receptors (and H1).==>INCREASED NE and serotonin activity
  • used for disease cans where appetite loss and nausea go together
  • dogs and cats
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7
Q

Megestrol acetate

A
  • synthetic progestin
  • significan anti-estrogen and glucocorticoid activity –> adrenal suppression.
  • stimulates appetiite and promotes weight gain
  • dont use in preg animals, uterine disease diabetes or mammary neoplasia
  • toxicity in cats (adrenocortical suppression, adrenal atrophy, diabetes)
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8
Q

Emetic drugs

A
  • emergency situations following ingested toxin
  • best act central at vomiting centre (directly or thro CRTZ)
  • includes apomorphine, xylazine, hydrogen peroxide.
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9
Q

Apomorphine

A
  • most effective emetic drug
  • opioid that acts as potent central dopamine agonist and directly stimulates CRTZ.
  • more effective in dogs than cats
  • oral or subq, or conjunctival or gingival membranes (not IM)
  • can also get depressant effect on vomit centre, so if doesn’t work the first time then prob won’t work.
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10
Q

Xylazine

A

Rompun

  • alpha 2 adrenergic agonist
  • reliable emetic, esp in cats
  • stimulates the CRTZ
  • can give sedation and hypotension too
  • parenteral (IV or IM)
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11
Q

Hydrogen peroxide

A
  • stimulates vomiting when applied to back of mouth via the 9th cranial nerve.
  • dont let it get aspirated-irritating to lungs
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12
Q

Syrup of Ipecac

A
  • emetine (toxic alkaloid) is active ingredient
  • producing vomiting by being stomach irritant
  • causes more problems then it helps. NOT RECOMMENDED!
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13
Q

antiemetic drugs

A
  • used to control vomiting
  • continued vomiting leads to dehydration, acid-base imbalances and electrolyte disturbances and aspiration pneumonia
  • metoclopramide, phenothiazine tranquilizers, anticholinergic drugs, serotonin antagonists, butorphanol, maropitant
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14
Q

phenothiazine tranquilizers as anti emetic drugs

A
  • alpha 2 adrenergic antagonists
  • antagonize CNS stimulatory effects of dopamine
  • decrease vomiting from a variety of causes, incl. motion sickness in the cat.
  • also antihistaminic (dogs) and weak anticholinergic (cats) action
  • includes chlorpromazine, prochlorperazine and acetylpromazine
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15
Q

anticholinergic drugs as anti emetic drugs

A
  • block cholinergic afferent pathways from the GI and the vestibular system to the vomiting centre
  • less effective then other emetics alone
  • more efficacious in motion sickness in cats than dogs(M1 muscarinic receptors found in the vestibular apparatus of the cat)
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16
Q

Antihistaminic drugs as anti emetic drugs

A
  • can block both cholinergic and histaminic nerve transmission responsible for transmission of the vestibular stimulus to the vomiting center in dogs (histamine not involved in cats)
  • H1 blocking drugs used are diphenhydramine, dimenhydrinate, promethazine, cyclizine and meclizine.
  • mild sedation
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17
Q

Metoclopramide

A

Anti emetic!
Reglan
3 anti emetic mechanisms:
1. @low doses inhibits dopaminergic transmission in CNS (dopamine antagonist)
2. peripheral pro kinetic effect increasing gastric and upper duodenal emptying
3. @high doses, inhibits serotonin receptors (via antagonism) in the CRTZ
-less effective in cats than dogs!

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18
Q

Serotonin antagonist as anti emetic drug

A
  • serotonin antagonist for receptors located peripherally on vagal nerve terminals and centrally in the area postrema in the brain.
  • not effective for motion sickness emesis
  • good for emesis caused by cytotoxic drugs/radiation damage to GI mucosa–>serotonin release–>CRTZ.
  • adverse cardiac effects
  • include ondansetron, dolasetron and granisetron.
  • good for radiation and chemotherapy patients
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19
Q

butorphanol

A

Torbutrol

  • effective antiemetic for dogs receiving chemo
  • exerts antiemetic effects directly on vomiting center
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20
Q

Maropitant

A

Cerenia

  • NK1 receptor antagonist used to treat and prevent emesis in dogs
  • safe and effective in cats
  • blocks the binding of substance P in the emetic centre
  • broad spectrum of action against various emetic stimuli (acute vomiting/low dose and motion sickness/high dose)
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21
Q

Antacids

A
  • most common are aluminum hydroxide, magnesium oxide/hydroxide or calcium carbonate
  • neutralize stomach acid to form neutral salt and water
  • not absorbed systemically
  • also decrease pepsin activity, binding to bile acids in the stomach and stimulating local PGE1 production (cell turn over and healing)
  • oxamin powder, MgOH boluses (carmilax), mild of magnesia (MgOH), Neigh-Lox
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22
Q

H2 receptor antagonists used for gastric ulcers

A

-Cimetidine, ranitidine and famotidine

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23
Q

Sucralfate

A

Sulcrate

  • anti ulcer drug that has a cytoprotective effect on the GI mucosa
  • disassociates in acid enviro of stomach to sucrose octasulfate (coats ulcer) and AlOH (neutralizes acid)
  • not absorbed –>no side effects (exception in renal patients)
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24
Q

Proton pump inhibitors

A
  • Mostly benzimidazole derivatives
  • irreversibly block the H+/K+ ATPase proton pump of the gastric parietal cell
  • most effective at shutting down gastric acid production
  • includes omeprazole
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25
Omeprazole
Gastroguard, ulcerguard - proton pump inhibitor approved for use in horses - human form Prilosec used in dogs - inhibits H+/K+ proton pump at the luminal surface of the parietal cell that secretes hydrogen ions into the gastric lumen - ulcers tend to come back after therapy
26
Misoprostol
Cytotec - synthetic prostaglandin E1 analogue that inhibits gastric acid secretion by direct action on the parietal cells (inhibits activation of histamine sensitive adenylate cyclase thus inhibiting GA secretion) - mainly used as preventative - during NSAID therapy for ex.
27
Metoclopramide (motility)
-causes increase motility in upper GI by increasing sensitivity of Ach receptors and increasing amt of Ach release in upper GI and antagonizing dopamine (which inhibits GI motility) -works from esophagus to small intestine -readily crosses BBB- giving dopamine antagonism at CRTZ --> anti emetic BUT get extrapyramidal signs too (bad)
28
Domperidone
Motilium - peripheral dopamine receptor antagonist (dopamine inhibits GI motility) - esophageal, gastric and SI effects - No CNS rxns! (effects of metoclopramide without
29
Cisapride
Propulsid - chemically related to metoclopramide (w/o crossing BBB or having anti dope effects) - it enhances the release of Ach from postganglionic nerve endings of myenteric plexus and antagonized inhibitory actions of serotonin on myenteric plexus ---->increased GI motility and increase HR - most pro kinetic and broader activity than metoclopramide (does colon motility too)
30
Prucalopride
Resotran - potent partial benzamide agonist at 5-HT4 receptors - increases colonic motility - and gastric, pyloric and duodenal motility - increased freq of defecation in dogs and cats (not diarrhea)
31
Motilin receptor agonists
- macrolide antibiotics are motilin receptor agonists (incl. erythromycin and clarithromycin) - also stimulate cholinergic and noncholinergic neural pathways to stimulate motility
32
Acetylcholinesterase inhbitors for motility
- acetylcholinesterase inhbition causes prokinetic action (mostly proximal GI tract) - Ranitidine and nizatidine are two H2 receptor antagonists that inhibit gastric secretion (via H2 antagonism) but are prokinetic due to Achesterase inhibition.
33
Lidocaine (in motility)
- suppression of inhibitory GI reflexes by reduction of postoperative peritoneal irritation is mech of action - also suppresses primary afferent neurons from firing and anti-inflam properties and direct stimulatory effects on sm. muscle.
34
Alpha 2 adrenergic receptor antagonists (motility)
- role in regulating gastric tone and Ach release through presynaptic mech in enteric NS. - adrenergic antagonists prevent the effects of NE on intrinsic neurons and stimulate sm. muscle - treatment for ileus
35
Castor oil
- stimulant (irritant) laxative - potent stimulator of bowel. - hydrolysed to ricinoleic acid in bowel ---> increase h20 secretion in SI
36
Raw Linseed oil
- stimulant (irritant) laxative - similar action to castor oil --> increase h20 secretion in SI - feed daily in horses to supply FAs and mild laxative effect
37
Senna
- stimulant (irritant) laxative - increases gastric fluid secretion and bowel motility---> laxative action - Secokot and Exlax (OTC)
38
Bisacodyl (Dulcolax)
- stimulates enteric nerves to cause colonic mass mvmts. | - also increases fluid and NaCl secretion
39
Hyperosmotic cathartics
- laxative - draw fluid into the bowel by osmosis-->increased fluid content of feces -->intestinal distension --> promotes peristalsis. - ex. Mg salts (epsom salts, milk of magnesia, citro-mag), Na bisphosphate/phosphate (fleet enema)(Don't use in cats), lactulose (Lactulax), polyethylene glycol
40
Lactulose (Lactulax)
- hyperosmotic cathartic laxative - organic acids produced from lactulose fermentation stimulate colonic fluid secretion and propulsive motility. - can alter bowel flora = farts and bloating
41
Polyethylene glycol
- hyperosmotic cathartic - large MW, water soluble polymer used as bulking and softening agent from tx of constipation - not metabolized and minimally absorbed in the intestines - forms Hbonds with water-->high osmotic pressure in bowel lumen-->prevents absorption of h20 out of lumen (powder or soln form0
42
Hydrophilic colloids
- "bulk laxatives" - composed of non absorbed PSC cellulose derivatives - drugs absorb h20 and increase mass of non digestible material in the bowel ex. methylcellulose, pysillium (metamucil), prunes, wheat bran and canned pumpkin. - FIBER
43
Lubricant laxatives
- act by coating the surface of the stool with h20 immiscible film and increase h20 content of feces - also lubricant action - usually contain mineral oil or white petroleum - min oil in horses and cattle, Kat-Lax in cats (hairball passage)
44
Stool softeners (surfactants)
- decrease surface tension and allow h20 to accumulate in the feces - occasionally in horses (nasogastric tube) - ex. dioctyl sodium, sulfosuccinate (DSS), dioctyl calcium sulfosuccinate(surfak, doxidan)
45
Kaolin-Pectin formulations
-acts as a demulcent (substance forming soothing, protective film over mm) and adsorbent in tx of diarrhea. -action like bacterial toxins binding to GI (not Kaopectate anymore which now = bismuth subsalicylate)
46
Activated Charcoal
- derived from wood, peat, coconut or pecan shells - very effective for adsorbing bacterial enterotoxins that cause some types of diarrhea. Also adsorb many drugs and toxins and prevent GI absorption
47
Bismuth Subsalicylate
PeptoBismol, Kaopectate, Corrective Mixture - tx of choice for acute diarrhea (proven efficacy) - Bismuth part may adsorb bacterial enterotoxins and produce gastric/intestinal protective effect - Salicylate part is anti inflammatory action - get black feces - can get toxicity, esp in cats
48
Anticholingeric drugs for anti diarrhea
- they signif decrease intestinal motility and secretions - decrease segmental and propulsive intestinal sm muscle contractions - decrease urgency with diarrhea in small animals, decrease fluid secreted in bowel and decrease abdominal cramps seen with hyper motility. - can only be used in hyper motile forms of diarrhea tho or could make worse (stove pipe effect)(limited use in vet med)
49
Atropine
- anticholergic drug | - not usually used for tx diarrhea because of systemic effects
50
hyoscine butylbromide (buscopan)
- antispasmodic and anticholingeric drug that relaxes the smooth muscle of GI tract - tx of uncomplicated colic - decreases gut sounds - beneficial in choke cases
51
Opioids for diarrhea tx
- can have anti-secretory and anti-motility actions ( mu and delta receptors of the GI tract) - decrease propulsive intestinal contractions and increase segmentation--> constipating effect - increase tone if GI sphincters - opiates also stimulate absorption of fluid, electrolytes and glucose (inhibition of Ca influx and decrease calmodulin activity) - mostly used in dogs (less cats) - dont use in infectious diarrhea (may increase absorption of bacterial toxins when slow GI transit time)
52
Diphenoxylate (Lomotil)
- synthetic opiate that has specific action on GI tract (no system effects) - used to tx diarrhea - used in small animals and large neonates - controlled substance
53
Loperamide
Imodium (OTC) - synthetic opiate with specific action on the GI tract (no systemic effects) - used for diarrhea tx in small animals and neonate large animals - dont use in "ivermectin sensitive" breeds (ABCB1 gene deletion dogs)
54
Paregoric
- tincture of opium found in many antidiarrheal products | - controlled substance (corresponds to morphine)
55
NSAIDS for diarrhea tx
- may be beneficial for diarrhea tx, and very impt in tx of septicaemia/ endotoxemia - action may be anti inflam effect - Anti-PG drugs may directly inhibit fluid and electrolyte hypersecretion by intestinal cells (increased cAMP) - meloxicam calve diarrhea over a week old - ketoprofen reduces fecal output in enterotoxigenic E. coli diarrhea - use with caution
56
Anti-endotoxin serum
- tx of equine and canine endotoxemia - diarrhea tx? - available for parvovirus enteritis in horses and clostridial diseases in ruminants
57
Sulfasalazine (salasopyrin, Alzulfidine)
- 5-aminosalicylic acid product - treatment of chronic colitis - salicylic acid component is active in the GI- causes anti inflammatory effect - anti-lipoxygenase activity, decreased IL-1, decreased PG synthesis and oxygen radical scavenging activity. - commonly used in SAs for ulcer therapy or idiopathic colitis or plasmacytic/lymphocytic colitis after dietary causes ruled out
58
Tylosin (Tylan)
- antimicrobial used for colitis - often given on chronic basis as alternative to sulfasalazine therapy - may have activity against mycoplasma, spirochetes and chlamydia - powdered form for swine given in food
59
Metronidazole (Flagyl)
- fair efficacy against Giardia - given to dogs, cats and horses with IBD - also good some other diarrhea cases due to activity against anaerobes prob. - may be immunosuppressive on GI mucosa too - has neuro effects tho - ANTIDOTE = diazepam
60
Glucocorticoids for chronic colitis
- tx colitis because anti inflam and immunosuppressive effects (colitis due to autoantibodies and T-cells directed against colonic epithelial cells or colitis due to lymphocytic/plasmacytic colitis) - dogs, cats and horses - prednisone or oral dexamethasone - budesonide (Entocort-crohns disease)-dogs with IBD possibly. (HPA suppression tho)
61
N-3 Fatty acids for colitis
- addn of N 3 FA to the diet makes fewer n-6 FA available for AA cascade (reduce inflame?) - derm caps for SA and raw linseed for horses
62
Azathioprine (Imuran)
- immunosuppressive drug used for colitis - metabolized to 6-mercaptopurine which causes immunosuppression by interfering with nucleic acid synthesis and impairing lymphocyte proliferation - monitor cats closely for SEs
63
Ursodiol (Actigall)
- for hepatitis therapy - naturally occurring hydrophilic bile acid that displaces the more hydrophobic bile acid pool in cholestatic liver disease - suppresses hepatic synthesis and secretion of CHO and decreases intestinal absorption of CHO (allows solubilization of CHO containing gallstones) - also increases bile flow and reduces hepatotoxic effect of bile salts by decreasing their detergent action - uses: tx of CHO containing gallstones, idiopathic hepatic lipidosis and chronic active hepatitis.
64
S-adenosylmethionine (SAMe) (Denosyl SD4)
- used for hepatitis therapy - increases levels of hepatic glutathione which is a potent antioxidant that protects hepatic cells from toxins and death. - used in compromised patients to maintain and protect liver fxn - also used in other cdns of tissue oxidant injury and of RBC fragility caused by toxins or drugs (ones related to low glutathione levels)
65
Colchicine
- used in hepatitis therapy (chronic with fibrosis, biliary cirrhosis) - anti-fibroic properties (inhibits microtubular mediated transcellular mvmt of pro collagen into the ECM) and increases collegenase activity (increasing collagen degradation) - anti inflam activity too
66
Penicillamine
- hepatitis therapy - frequent copper chelator used in dogs - vomiting SE
67
Trientine
- hepatitis therapy - copper chelating agent - less adverse effects than penicillamine
68
Prednisone (hepatitis therapy)
-anti inflammatory effects beneficial in tx of chronic hepatitis in Bedlington terriers and west highland white terriers
69
Zinc (hepatitis tx)
- essential cofactor for reducing hepatic copper []s - Zinc leads to intestinal metallothionein (MT) production --> MT induction prevents serosal transfer of copper into blood - zinc good follow up therapy after chelator therapy - zinc shows reduced hepatic copper []s, decrease hepatic enz activity and improved hepatic histologic features after long term therapy - SEs : nausea, vomiting and anorexia
70
Antioxidants (Hepatitis tx)
- free radicals may play a role in initiating and perpetuating damage to liver in chronic active hepatitis - therapy with vit E reduces oxidant damage to hepatic tissue - NOT VIT C
71
Milk thistle (Marin)
-natural remedy for hepatitis therapy used for diseases of the liver and biliary tract -Silymarin is active extract and contain flavonignans (antioxidants) which scavenge free radicals and inhibit lipid per oxidation (APPARENTLY)