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1
Q

What are examples of classes of drugs used as antiemetics?

A

Antihistamines
Antimuscarinics
Cannabinoids
Dopamine antagonists
Glucocorticoids
5HT3 antagonists
Neurokinin-1 antagonists

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2
Q

What are examples of antihistamines used as antiemetics?

A

Cinnarizine
Cyclizine
Promethazine hydrochloride
Promethazine theoclate

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3
Q

What are examples of antimuscarinics used as antiemetics?

A

Hyoscine

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4
Q

What are examples of cannabinoids used as antiemetics?

A

Nabilone

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5
Q

What are examples of dopamine antagonists used as antiemetics?

A

Phenothiazines - prochlorphenazine, perphenazine, trifluorphenazine, chlorpromazine
Droperidol and haloperidol
Metoclopramide
Domperidone

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6
Q

What are examples of glucocorticoids used as antiemetics?

A

Dexamethasone

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7
Q

What are examples of 5-HT3 antagonists used as antiemetics?

A

Granisteron
Ondansetron
Palonosetron

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8
Q

What are examples of neurokinin-1 antagonists used as antiemetics?

A

Aprepitant
Fosaprepitant

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9
Q

Where do 5-HT3 receptor antagonists antiemetics act?

A

Central serotonin receptors in the vomiting centre as well as peripheral serotonin receptors in vagus nerve (GIT)

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10
Q

What are the main uses of 5-HT3 receptor antagonists as antiemetics?

A

Vomiting caused by acute gastroenteritis
Postoperative nausea and vomiting
Cytotoxic drug-induced vomiting

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11
Q

Where do phenothiazines act as antiemetics?

A

D2 receptors in the CTZ

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12
Q

Where do droperidol and haloperidol act as antiemetics?

A

D2 receptors in CTZ

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13
Q

Where does metoclopramide act as antiemetics?

A

D2 antagonist at CTZ and gastric smooth muscle stimulating gastric emptying

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14
Q

Where does domperidone act as antiemetics?

A

D2 receptors in CTZ

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15
Q

What are the indications for phenothiazines as antiemetics?

A

Cytotoxic drug-induced N+V
Postoperative N+V
Radiation sickness

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16
Q

What are the indications for haloperidol as antiemetics?

A

Cytotoxic drug-induced N+V
Postoperative N+V
Radiation sickness

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17
Q

What are the indications for metoclopramide as antiemetics?

A

Postoperative NV
Cytotoxic drug-induced NV

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18
Q

What are the indications for domperidone as antiemetics?

A

Cytotoxic drug-induced NV

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19
Q

which antiemetics are best for motion sickness?

A

Hyoscine hydrobromide
Antihistamine drugs

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20
Q

Which group of antiemetics are typically used in the management of NV in to recieving cytotoxics?

A

5HT3 receptor antagonists

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21
Q

What are the neurogenic 1-receptor antagonists usually given for?

A

prevent nausea and vomiting associated with chemotherapy.

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22
Q

What are the indications for nabilone?

A

It can be considered as an add-on treatment for chemotherapy-induced nausea and vomiting unresponsive to optimised conventional antiemetics.

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23
Q

Which antiemetic is typically given for morning sickness?

A

chlorpromazine hydrochloride
cyclizine
doxylamine with pyridoxine
metoclopramide hydrochloride
prochlorperazine
promethazine hydrochloride/promethazine teoclate
ondansetron

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24
Q

Which antiemetics are best for managing Ménière’s disease?

A

Antihistamines
Phenothiazines

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25
Which antiemetic share typically given for vomiting induced by vestibular disturbances e.g. vertigo or motion?
H1 antihistamines Antimuscarinics
26
Whats the issue with serotonin receptor antagonist use for post operative nausea and vomiting?
Dose-dependant but can cause QT prolongation
27
Why are neurokinin receptor antagonists not used more frequently?
They are really expensive
28
Whats the moa of metoclopramide
Antiemetic action- antagonist activity at D2 receptors in the CTZ Gastroprokinetic activity - mediated by muscarinic activity, D2 receptor antagonist activity, and 5-HT4 receptor agonist activity. The gastroprokinetic effect itself may also contribute to the antiemetic effect Metoclopramide also increases the tone of the lower esophageal sphincter
29
What is the main issue with using metoclopramide as an antiemetic?
It can cause extrapyramidal sympotms thta generally manifest as acute dystonia - particularly in people <30 ans females (should not give to anyone under 20)
30
How do you treat acute dystonia acutely?
Procyclidine hydrochloride
31
Whats the moa of procyclidine?
The mechanism of action is unknown. It is thought that Procyclidine acts by blocking central cholinergic receptors, and thus balancing cholinergic and dopaminergic activity in the basal ganglia. Many of its effects are due to its pharmacologic similarities with atropine.
32
What are side efefcts of antihistamines?
Drowsiness, reduces coordination reaction times and judgement Dry mouth, blurred vision, difficulty peeing Headache
33
Why is prochlorperazine such a useful antiemetic for those with persistent vomiting ?
It is available as a buccal tablet
34
Whats the advanatage of domperidone over metoclopramide and the phenothiazine’s?
Less likely to cause central effects e.g. sedation and dystonia reactions because it does not readily cross the bloo brain barrier
35
What are examples of the less sedating antihistamines?
Cinnarizine and cyclizine
36
What are examples of the more sedating antihistamines?
Promethazine
37
What are examples of bulk forming laxatives?
Bran Ispaghula husk (fybogel) Methyl cellulose Sterculia
38
Whats the indication for bulk-forming laxatives?
adults with small hard stools if fibre cannot be increased in the diet
39
Whats the onset of action of bulk-forming laxatives?
Up to 72 hours
40
What should you inform a pt about to take bulk forming laxatives?
Side effects include nausea, vomiting, flatulance, bloating and diarrhoea Adequate fluid intake must be maintained to avoid intestinal obstruction.
41
How do bulk forming laxatives work?
They draw water in the stool to form a soft, bulky mass which stimulates intestinal peristalsis
42
What are examples of stimulant laxatives?
Bisacodyl Sodium picosulfate Senna Co-danthramer and co-danthrusate
43
What are contraindications of all laxatives?
Intestinal obstruction Severe abdominal pain Symptoms of appendicitis, diverticulitis or UC
44
What are side efefcts of stimulant laxatives?
Abdominal cramp Nausea, vomiting Diarrhoea Weakness Fluid and electrolyte imbalance (Senna also causes reddish/brown urine and Melanosis coli)
45
Why is the use of co-danthramer and co-danthrusate is limited to constipation in terminally ill patients?
because of potential carcinogenicity (based on animal studies) and evidence of genotoxicity.
46
Whats the moa of docusate sodium?
Acts as both a stimulant laxatives and as a faecal softener It acts as a surfactant (lowers surface tension) that allows water to penetrate the stool and make it softer
47
Whats the moa of stimulant laxatives?
They irritate nerve endings in intestinal walls, stimulating smooth muscle contraction and intestinal peristalsis
48
What are contraindications for all laxatives?
Intestinal obstruction Severe abdo pain Symptoms of appendicitis, diverticulitis or UC
49
What are examples of faecal softeners?
Docusate sodium Glycerol suppositories Enter as containing arachis oil Liquid paraffin
50
How do faecal softeners work?
It acts as a surfactant (lowers surface tension) that allows water to penetrate the stool and make it softer
51
What are side effects of faecal softeners?
Nausea, vomiting Abdominal cramping Diarrhoea
52
Why should liquid paraffin be used with caution as a faecal softener?
because of its adverse effects, which include anal seepage and the risks of granulomatous disease of the gastro-intestinal tract or of lipoid pneumonia on aspiration.
53
Whats the moa of osmotic laxatives?
increase the amount of water in the large bowel, either by drawing fluid from the body into the bowel or by retaining the fluid they were administered with.
54
What are examples of osmotic laxatives?
Lactulose Macrogol (brand names include movicol, molative etc) Polyethylene glycol
55
Why is lactulose also useful in the treatment of hepatic encephalopathy?
lactulose is thought to work by promoting the excretion of ammonia and increasing the metabolism of ammonia by gut bacteria
56
What are macrogols?
Inert polymers of ethylene glycol which sequester fluid in the bowel
57
What are the contraindications specific for osmotic saline laxatives?
Renal, hepatic impairment and cardiac conditions
58
What are the contraindications specific for lactulose?
Galactosaemia; gastro-intestinal obstruction; gastro-intestinal perforation; risk of gastro-intestinal perforation Caution with lactose intolerance
59
What is linaclotide? Whats it used for treating? How does it work?
a guanylate cyclase-C receptor agonist Licensed for the treatment of moderate-severe IBS associated with constipation. It increases intestinal fluid secretion and transit, and decreases visceral pain.
60
What is prucalopride? Whats it used for treating?
a selective serotonin 5HT4-receptor agonist with prokinetic properties. It is licensed for the treatment of chronic constipation in adults, when other laxatives have failed to provide an adequate response.
61
What are options for bowel cleansing preparations?
Macrogol 3350 with anhydrous sodium sulfate Potassium chloride Sodium bicarbonate and sodium chloride Citric acid with magnesium carbonate Magnesium citrate with sodium picosulphate Sodium acid phosphate with sodium phosphate
62
How do you manage short-duration constipation?
If dietary measures are ineffective… 1. Bulk-forming laxative If stools remain hard… Add or switch to osmotic laxative If stools are soft but diffiuclt to pass or there is tenesmus -> add stimulant laxative
63
How should you manage opioid-induced constipation?
1. Osmotic laxative and stimulant laxative 2. If inadequate response use naloxegol 3. If inadequate response use methylnaltrexone bromide (avoid bulk-forming laxative altogether)
64
How should you manage faecal impaction of hard stools?
High dose of an oral macrogol (If not response consider rectal glycerol or rectal glycerol and bisacodyl) If still inadequate response -> May consider arachis oil overnight before giving an enema
65
How should you manage faecal impaction of soft stools?
Oral stimulant laxative (Ir response is inadequate consider rectal bisacodyl) If response is still inadequate an enema may be used
66
How should you manage chronic constipation?
1. Bulk-forming laxative 2. Add or change to osmotic laxative (if not effective use lactulose) 3. Stimulant laxative can be added
67
Whats the priority aim of treating diarrhoea?
the prevention or reversal of fluid and electrolyte depletion and the management of dehydration when it is present. This is particularly important in infants, frail and elderly patients, when excessive water and electrolyte loss and dehydration can be life-threatening.
68
How can we prevent or correct diarrhoea dehydration?
Oral rehydration therapy (If severe or unable to drink then urgent admission to hospital and urgent replacement therapy with IV rehydration fluid)
69
What are examples of oral rehydration therapy?
Disodium hydrogen citrate with glucose Potassium chloride and sodium chloride Potassium chloride with rice powder Sodium chloride and sodium citrate
70
How can you treat diarrhoea?
1. Loperamide hydrochloride No other sufficient evidence for any drugs
71
Whats the moa of loperamide?
Loperamide acts on the mu-opioid receptor on the circular and longitudinal intestinal muscle -> inhibit enteric nerve activity -> inhibits the release of acetylcholine and prostaglandins -> reducing propulsive peristalsis and increasing intestinal transit time Loperamide stimulates the intestinal absorption of water and electrolytes by inhibiting calmodulin. Loperamide can bind to and hyperpolarize submucosal secretomotor neurons, promoting dry, hard stools
72
What ate the indications of loperamide?
Symptomatic treatment of acute diarrhoea Chronic diarrhoea Facial incontinence Pain of bowel colic in palliative care
73
What are contraindications of loperamide?
Active ulcerative colitis; antibiotic-associated colitis; bacterial enterocolitis; conditions where abdominal distension develops; conditions where inhibition of peristalsis should be avoided Children under 12
74
What are common side efefcts of loperamide?
GI disturbance Headache
75
What are some antimotility drugs?
Loperamide (imodium) Codeine phosphate Co-phenotrope Kaolin Morphine mixture
76
Whats the moa of dicyclomine?
M1, M2 and M3 receptor antagonist as well as a non-competitive inhibitor ad histamine and bradykinin
77
What is dicyclomine used to treat?
Functional bowel disorder and IBS
78
Whats the moa of mebeverine?
Anticholinergic - works on smooth muscle in GIT It’s an antispasmodic
79
Whats mebeverine used to treat?
IBS
80
Why should lactulose not be used in IBS?
As it can cause bloating
81
What can be used as a second-line option for abdominal pain in IBS in patients who have not responded to antispasmodics, anti-motility drugs, or laxatives?
Low dose TCA (or SSRI if they don’t respond)
82
How does peppermint oil help in IBS?
Peppermint oil has been shown to reduce gastric motility8 by directly acting on gut calcium channels to relax gastrointestinal smooth muscle
83
What are important side efefcts of mesalazine?
GI upset, headache, agranulocytosis, pancreatitis (7x more likely), interstitial nephritis
84
What are important side efefcts of sulphasalazine?
rashes, oligospermia, headache, Heinz body anaemia, megaloblastic anaemia, lung fibrosis As well as all other side effects common to 5ASA drugs

GI AND SURGERY (31 decks)

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