GIT pharmacology Flashcards

1
Q

List some GIT pathophysiologies that may need pharmacological treatment

A

Antiulcer

Vomiting

Constipation

Diarrhoea

Motility issues

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2
Q

List some neurotransmitters that are involved in GIT function

A

Acetylcholine

Noradrenaline

Histamine (H1, H2)

Opioids

Dopaminergic

Serotonin (5HT3)

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3
Q

List some hormones that are involved in GIT function

A

Gastrin (stomach)

Secretion (duodenum)

Cholecystokinin (regulates fat)

Ghrelin

Motilin

Vasoactive intestinal peptide

Gastric inhibitory peptide

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4
Q

List some causes of gastric ulceration

A

NSAID use

Uraemia

Liver disease

Stress

Increased production of HCl (e.g. mast cell tumor)

Hypotension

Helicobacter

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5
Q

List some normal protective mechanisms of the GIT

A

Mucous layer with high levels of bicarbonates

High cell turnover

Tight junctions

Highly vascularised

Prostaglandins (mucous secretion, blood flow, acid inhibition)

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6
Q

List some classes of antiulcer drugs and gastroprotectants

A

Proton pump inhibitors

Antihistamines

Gastroprotectants

Non-systemic antacids

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7
Q

List a proton pump inhibitor

A

Omeprazole

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8
Q

What is the mechanism of action of omeprazole?

A

Proton pump inhibitors (antiulcer/gastroprotectant)

Irreversible inhibition of H+/K+ ATPase proton pump on parietal cells: weak bases accumulate in acidic environment around proton pump to selectively inhibit active cells

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9
Q

List some antihistamines that may be useful as an antiulcer/gastroprotectant drug

A

Ranitidine

Cimetidine

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10
Q

What is the mechanism of action of ranitidine?

A

Antihistamine

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11
Q

What is the mechanism of action of Cimetidine?

A

Antihistamine

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12
Q

List two gastroprotectants

A

Misoprostal

Sucralfate

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13
Q

Which class of drugs does misoprostal belong to?

A

Gastroprotectants

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14
Q

What class of drugs does sucralfate belong to?

A

Gastroprotectants

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15
Q
A
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16
Q

What are the effects of omeprazole?

A

Inhibits the final step of acid secretion, increasing both basal and food-stimulated gastic acid secretions

(more effective than antacids and H2-antagonists)

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17
Q

What are the preparations of omeprazole

A

Enteric coated tablets/capsules to aid absorption

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18
Q

What are the adverse effects/drug interactions of omeprazole?

A

Well tolerated

Some inhibition of cytochrome P450

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19
Q

What are the mechanisms of action of antihistamine as antiulcer/gastroprotectant drugs?

A

H2 receptor antagonist

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20
Q

What are the effects of antihistamines as GIT drugs?

A

Decrease 90% basal and 60% food-stimulated acid secretion

More effective than antacids, but not as effective as PPIs

Lasts 12-24 hours

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21
Q

What are the adverse effects of cimetidine, ranitidine?

A

Cutaneous eruptions (cats)

gynaecomastia and sexual dysfunction (humans)

Cimetidine inhibits cytochrome p450 - many potential drug interactions

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22
Q

What is the mechanism of action of misoprostal?

A

Prostaglandin E1 analogue

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23
Q

What are the effects of misoprostal?

A

Protects GI mucosa by increasing mucous secrtion and bicarbonate and decreasing secretion of gastric acid (useful for NSAID induced ulcers)

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24
Q

What are the adverse effects of misoprostal

A

Induces parturition, diarrhoea, vomiting

(CAUTION pregnant vets)

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25
What is the mechanism of sucralfate?
Sucrose octasulfate and aluminium hydroxide dissociate in stomach Acid polymerises sucrose octasulfate (sticky coating covers ulcers)
26
What is the indication for sucralfate
symptomatic treatment of gastric ulceration
27
What are the adverse effects of sucralfate
Minor; constipation?
28
What are some of the preparations of non-systemic antacids
Aluminum hydroxide, calcium carbonate or magnesium compounds
29
What are the adverse effects of non-systemic antacids
May result in rebound acid secretion if not continually administered
30
Define vomiting
An active process involving forceful, reflexive ejection of contents from stomach and/or small intestine
31
Define regurgitation
Passive process (gravity or passive changes in thoracic/abdominal pressures) resulting in retrograde expulsion of material from the oesophagus/pharynx/oral cavity/nasal cavity
32
List some classes of antiemetic drugs
Dopamine antagonists Metochlopramide Serotonin antagonists NK1 antagonists Antihistamines Anticholinergics Phenothiazines
33
What is the mechanism of action of domperidone?
Dopamine antagonist in chemosensory trigger zone and GIT + adrenergic antagonist in stomach
34
List an antiemetic dopamine antagonist
Domperidone
35
What is the mechanism of metoclopramide?
Dopamine and serotonin antagonist centrally Peripheral cholinergic effect
36
What are the indications for metoclopramide?
Promotes gastric emptying (prokinetic) Indicated for use in reflux, chemotherapy, decreased gastric emptying, emesis
37
What are the precautions when using metoclopramide?
Caution with GI haemorrhage, obstruction, perforation
38
List a serotonin antagonist anti-emetic
Ondansetron
39
What is the mechanism of action of ondansetron?
Antagnosies 5HT3 receptors in the chemosensory trigger zone and visceral afferent nerves
40
What are the indications for ondansetron
Severe vomiting (potent but expensive, not registered in animals)
41
List an NK1 receptor antagonist antiemetic
Maropitant
42
What is the mechanism of action of maropitant
Blocks the action of substance P on NK1 receptors
43
What are the indications of use for maropitant ?
General emesis and motion sickness in dogs For vomiting following pain or anticancer drugs Not registered in cats
44
List two antihistamines that may be used as an antiemetic
Diphenhydramine Dimenhydrinate
45
What is the mechanism of action of diphenhydramine, dimenhydrinate?
Block histamine receptors in the chemosensory trigger zone of dogs (not cats) Acts in reticular formation to promote sedation
46
What are the indications of diphenhydramine, dimenhydrinate?
Motion sickness in dogs
47
What are some anticholinergics that may be useful as antiemetics?
Hyoscine, atropine, propantheline
48
What is the mechanism of action of hyoscine?
Antiemetic action through antagonism of central muscarinic receptors
49
What are the adverse effects of anticholinergics as antiemetics?
Usually inappropriate due to side effects e.g. GIT ileus, delayed gastric emptying; not routinely used
50
List two phenothiazines that may be useful as antiemetics
Prochlorperazine Chlorpromazine
51
What is the mechanism of action of phenothiazines (prochlorperazine, chlorpromazine)?
Antagonise adrenergic, dopaminergic, histaminergic and muscarinic receptors
52
What are the indications of phenothiazines (prochlorperazine, chlorpromazine)?
Motion sicknes, thunderstorms
53
What are the adverse effects of phenothiazines (prochlorperazine, chlorpromazine)?
Hypotension Sedation Lower seizure threshold
54
Name two centrally acting emetic agents
Apomorphine (dogs) Xylazine (cats)
55
What is the mechanism of action of apomorphine?
Dopamine agonist (emetic)
56
List three peripheral emetics
Hydrogen peroxide 3% (not cats) Syrup of ipecac (less useful in dogs) Washing crystals (sodium carbonate)
57
What are some considerations before inducing emesis?
Why do you want the animal to vomit? (toxins) Can the animal vomit? (Species: not horses; Obstructions) Will the vomiting cause more harm (caustic/conscious?)
58
What are some drug classes that may be useful in treating constipation?
Bulk laxatives Emollient laxatives Hyperosmotic laxatives Stimulant laxatives
59
What are some drug classes that may be useful in treating diarrhoea?
Motility modifying (opioids, anticholinergics) Absorbants Protectancts Sulfasalazine
60
Define constipation
Bowel movements that are infrequent or hard to pass
61
Define obstipation
Failure to pass faeces or gas
62
List four causes of constipation
Anal/rectal pain Decreased/absent motility in colon and rectum Physical obstruction (e.g prostate enlargement, tumour) Dietary indiscretion
63
What is an important consideration in treating constipation
Diagnose any underlying cause (history, PE, radiograph, colonoscopy) or will reoccur Laxatives vs enema
64
List two bulk laxatives
Psyllium, bran
65
What is the mechanism of action of psyllium, bran?
Bulk up faces (added fibre draws water into gut) but requires adequate hydration
66
List an emollient laxative
docusate sodium
67
What is the mechanism of action of emollient laxatives?
Stool softners
68
What are the indications of emollient laxatives?
Anionic detergents contained in enema preparations Also given per os but not registered in dogs/cats
69
List a lubricant laxative
Mineral oil e.g. paraffin
70
What are the indications of lubricant laxatives?
Limited use Not to be used with stool softners
71
List a hyper-osmotic laxative
Polyethylene glycol
72
What are the indications for polyethylene glycol
Requires oro-gastric intubation, primarily for use prior to colonoscopy
73
List two stimulant laxatives
Parasympathomimetics (Bethanecol), Bisacodyl (Dulcolax)
74
What are the limitations of stimulant laxatives
Should not be given with other oral medication Ducolax has potential do damage neurons in GIT if chronic administration
75
What are the four main classes and an example cause of diarrhoea?
Secretory (e.g. E.coli infection) Osmotic (e.g. poor diet) Protein losing enteropathy (e.g. intestinal worms) Inflammatory (e.g IBS)
76
What are the goals of diarrhoea treatment?
Treat fluid and electrolyte loss Modify diet Treat cause Drugs not always required, may be symptomatic relief
77
Why is it important to treat diarrhoea?
Dehydration Loss of electrolytes Acidosis Villous atrophy Malabsorption of nutrients
78
What are the risks of diarrhoea treatment?
Diarrhoea usually protective mechanism Treatment can mask progression of disease Stasis can lead to toxic megacolon Constipation
79
List two opioid derivatives that may be useful in treatment of diarrhoea
Lomotil (Diphenoxylate + atropine) Loperamide
80
What are the effects of lomotil or loperamide?
Increase segmental contractions and delay GIT emptyuing Increase ileocolic valve tone and anal sphincter tone May increase absorption of water
81
Name four absorbents/protectants that may have use in the treatment of diarrhoea
Kaolin, pectin Bismuth subsalicylate Activated charcoal
82
What is the mechanism of action of kaolin, pectin
Suggested to bind toxins and bacteria and sooth GIT (clinical efficacy unproven)
83
What are the indications for bismuth subsalicylate?
Enterotoxigenic or acute diarrhoea
84
What are the uses of activated charcoal
Absorbs toxic substances (not absorbed from GIT)
85
What are the potential adverse effects of activated charcoal?
Emesis if given quickly Diarrhoea, constipation, black faeces
86
What are the indications for sulfasalazine?
Inflammatory bowel disease in dogs and cats | (anecdotal evidence)
87
What are the limitations of using sulfasalazine in IBD?
Needs colonic bacteria to cleave it May cause side effects (e.g. keratoconjunctivitis sicca) Numerous drug interactions
88
Define ileus
Lack of peristalsis
89
List some drugs that may be useful in the treatment of ileus
(+fluids) Metoclopramide Domperidone (Motilium) Cisapride 5HT4 agonists Lidocane (post-op) Maropitant (if pain)
90
What is the mechanism of action of metoclopramide in the treatment of ileus?
5HT4 agonist, 5HT3 and D antagonist
91
What is the mechanism of action of domperidone?
D2 antagonist (does not cross BBB)
92
What is the mechanism of action of cisapride
5HT4 agonist -\> release of Ach from myenteric nerves
93
List 2 novel GIT motility enhancers
motilin and ghrelin agonists E.g. erythromycin, azithromycin = motilin agonists
94
List five possible appetite stimulants
Cyproheptadine Diazepam IV for cats Vitamin supplements Glucocorticoids (DO NOT USE - SE) Mirtrazapine
95
Describe the mechanism of action of cyproheptadine
histamine and serotonin antagonist (useful for appetite stimulation in cats)
96
List the mechanism of action of mirtazapine
alpha2 antagonist increases NE = tricyclic antidepressant + appetite stimulant serotonin antagonist = antiemetic peripheral alpha1 antagonist (sedation, hypotension)
97
What are the indications for parenteral nutrition?
anorexia (actual/expected) \> 3-5 days Poor nutritional status (BCS \< 3/5; wt loss \> 5-10%) Feline patients with hepatic lipidosis
98
List four routes of assisted nutritional supplementation
Naso-oesophageal Oesophageal Gastrostomy Jejunostomy