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Pharm > GI therapy > Flashcards

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
Q

Omeprazole

A

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
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26
Q

Misoprostol

A

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.
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27
Q

Metoclopramide (motility)

A

-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)

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28
Q

Domperidone

A

Motilium

  • peripheral dopamine receptor antagonist (dopamine inhibits GI motility)
  • esophageal, gastric and SI effects
  • No CNS rxns! (effects of metoclopramide without
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29
Q

Cisapride

A

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
Q

Prucalopride

A

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
Q

Motilin receptor agonists

A
  • macrolide antibiotics are motilin receptor agonists (incl. erythromycin and clarithromycin)
  • also stimulate cholinergic and noncholinergic neural pathways to stimulate motility
32
Q

Acetylcholinesterase inhbitors for motility

A
  • 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
Q

Lidocaine (in motility)

A
  • 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
Q

Alpha 2 adrenergic receptor antagonists (motility)

A
  • 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
Q

Castor oil

A
  • stimulant (irritant) laxative
  • potent stimulator of bowel.
  • hydrolysed to ricinoleic acid in bowel —> increase h20 secretion in SI
36
Q

Raw Linseed oil

A
  • 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
Q

Senna

A
  • stimulant (irritant) laxative
  • increases gastric fluid secretion and bowel motility—> laxative action
  • Secokot and Exlax (OTC)
38
Q

Bisacodyl (Dulcolax)

A
  • stimulates enteric nerves to cause colonic mass mvmts.

- also increases fluid and NaCl secretion

39
Q

Hyperosmotic cathartics

A
  • 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
Q

Lactulose (Lactulax)

A
  • hyperosmotic cathartic laxative
  • organic acids produced from lactulose fermentation stimulate colonic fluid secretion and propulsive motility.
  • can alter bowel flora = farts and bloating
41
Q

Polyethylene glycol

A
  • 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
Q

Hydrophilic colloids

A
  • “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
Q

Lubricant laxatives

A
  • 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
Q

Stool softeners (surfactants)

A
  • 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
Q

Kaolin-Pectin formulations

A

-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
Q

Activated Charcoal

A
  • 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
Q

Bismuth Subsalicylate

A

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
Q

Anticholingeric drugs for anti diarrhea

A
  • 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
Q

Atropine

A
  • anticholergic drug

- not usually used for tx diarrhea because of systemic effects

50
Q

hyoscine butylbromide (buscopan)

A
  • antispasmodic and anticholingeric drug that relaxes the smooth muscle of GI tract
  • tx of uncomplicated colic
  • decreases gut sounds
  • beneficial in choke cases
51
Q

Opioids for diarrhea tx

A
  • 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
Q

Diphenoxylate (Lomotil)

A
  • 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
Q

Loperamide

A

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
Q

Paregoric

A
  • tincture of opium found in many antidiarrheal products

- controlled substance (corresponds to morphine)

55
Q

NSAIDS for diarrhea tx

A
  • 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
Q

Anti-endotoxin serum

A
  • tx of equine and canine endotoxemia
  • diarrhea tx?
  • available for parvovirus enteritis in horses and clostridial diseases in ruminants
57
Q

Sulfasalazine (salasopyrin, Alzulfidine)

A
  • 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
Q

Tylosin (Tylan)

A
  • 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
Q

Metronidazole (Flagyl)

A
  • 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
Q

Glucocorticoids for chronic colitis

A
  • 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
Q

N-3 Fatty acids for colitis

A
  • 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
Q

Azathioprine (Imuran)

A
  • 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
Q

Ursodiol (Actigall)

A
  • 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
Q

S-adenosylmethionine (SAMe) (Denosyl SD4)

A
  • 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
Q

Colchicine

A
  • 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
Q

Penicillamine

A
  • hepatitis therapy
  • frequent copper chelator used in dogs
  • vomiting SE
67
Q

Trientine

A
  • hepatitis therapy
  • copper chelating agent
  • less adverse effects than penicillamine
68
Q

Prednisone (hepatitis therapy)

A

-anti inflammatory effects beneficial in tx of chronic hepatitis in Bedlington terriers and west highland white terriers

69
Q

Zinc (hepatitis tx)

A
  • 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
Q

Antioxidants (Hepatitis tx)

A
  • 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
Q

Milk thistle (Marin)

A

-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)

Pharm (6 decks)

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