Anti-diarrhoeals

Question 1

What are 6 groups of drugs used to treat diarrhoea?

Answer 1

1) Opioid agonist
2) Colloidal bismuth compounds
3) Intestinal adsorbents
4) Products of Lactobacillus acidophilus
5) Bile salt-binding resins
6) Somatostatin-like peptides

Question 2

What are the anti-diarrhoeal agents for acute diarrhoea?

Answer 2

1) Opioid agonists
2) Colloid bismuth compounds
3) Intestinal adsorbents
4) Lyophilizate of killed Lactobacillus acidophilus

Question 3

What are the anti-diarrhoeal agent for chronic diarrhoea?

Answer 3

1) Bile salt-binding resins
2) Somatostatin-like peptides

Question 4

What is the 1st line drug for rapid, symptomatic relief of diarrhoea?

Answer 4

Loperamide

Question 5

What are 2 examples of opioid agonists?

Answer 5

1) Loperamide
2) Diphenoxylate (+ atropine)

Question 6

What is the moa of opioid agonists?

Answer 6

Act in enteric NS → ↑colonic transit time

Question 7

What is the main concern of loperamide use?

Answer 7

Overdose → risk of cardiac abnormalities

Question 8

Which of the opioid agonists are at risk of dependence and what is done to prevent it?

Answer 8

Diphenoxylate (@ high dose)
- prep w atropine to discourage overdose and dependence

(Loperamide does not cross BBB)

Question 9

What are 3 AEs of opioid agonists?

Answer 9

1) CNS effects: addiction/dependence/abuse
2) Diphenoxylate + atropine → parasympatholytic effects (eg. xerostomia)
3) Risk of cardiac abnormalities on loperamide overdose

Question 10

What are 2 examples of colloidal bismuth compounds?

Answer 10

1) Bismuth subcitrate
2) Bismuth subsalicylate

Question 11

What is the moa of colloidal bismuth compounds?

Answer 11

1) Antimicrobial effect + binds to enterotoxins
2) Mucosal protective agent

(salicylate inhibits intestinal prostaglandin prod and Cl secretion, ↓ stool frequency and liquidity in acute infectious diarrhea)

Question 12

Which anti-diarrhoeal drug turns tongue and stools black?

Answer 12

Colloid Bismuth Compounds

Question 13

What are 4 AEs of colloidal bismuth compounds?

Answer 13

Usually good safety profile
just cause:
a) Harmless blackening of stool
b) harmless blackening of the tongue

Renal insufficiency → Bismuth toxicity and encephalopathy
1) Ataxia
2) Headaches
3) Confusion
4) Seizures

Question 14

In which px should bismuth compounds be avoided?

Answer 14

Renal insufficiency
(+ dont use LT)

Question 15

What are 2 examples of intestinal adsorbents?

Answer 15

1) Kaolin
2) Diosmectite

Question 16

What is the moa of intestinal adsorbents?

Answer 16

1) Adsorbs bacteria, bacterial toxins, and fluid
2) Decrease stool liquidity and number

Question 17

What is the main AE of intestinal adsorbent?

Answer 17

Constipation

Question 18

Intestinal adsorbents should not be taken with _____________ within _____________.

Answer 18

Any other medication within 2 hrs of other medications

Question 19

What is an example of a lyophilizate of killed Lactobacilius acidophilus?

Answer 19

Lacteol fort

Question 20

What is the moa of Lacteol fort?

Answer 20

Heat-inactivated Lactobacillus acidophilus adheres onto surface of intestinal cells
→ normalise intestinal flora by competitive exclusion
→ prevent overcolonisation by other organisms

Question 21

What is indicated in traveler’s diarrhoea?

Answer 21

Lacteol fort

Question 22

When is lacteol fort (lyophilizate of killed Lactobacilius acidophilus) contraindicated?

Answer 22

px with lactose intolerance (formulation contains lactose monohydrate)

Question 23

What is an example of a bile salt-binding resins used as a anti-diarrhoeal?

Answer 23

1) Cholestyramine
2) Colestipol
3) Colesevelam

Question 24

What is the moa of bile salt-binding resins used as a anti-diarrhoeal?

Answer 24

Resins bind to bile salts in colon → alleviate diarrhoea cause by osmotic laxative-like effect of fecal bile salts

Question 25

What are 6 AEs of bile salt-binding resins used as a anti-diarrhoeal?

Answer 25

1) Bloating
2) Flatulence
3) Constipation
4) Fecal impaction
5) Exacerbated fat malabsorption

Question 26

Bile salt-binding resins should not be taken with _____________ within _____________.

Answer 26

Any other oral drugs within 2 hrs

Question 27

What is used to treat chronic diarrhoea due to Crohn’s disease or surgical resection of ileum?

Answer 27

Bile salt-binding resins (eg. Cholestyramine)

Question 28

What is used to treat chronic secretory diarrhoea due to GI and neuroendocrine tumours (eg. VIPoma and Carcinoid tumours)?

Answer 28

Somatostatin-like peptides (eg. Ocreotide)

Question 29

How is Octreotide administered?

Answer 29

1) Subcut injection
2) Intramuscular depot formations

Question 30

What is the moa of somatostatin-like peptides (eg. Octreotide)?

Answer 30

Mimics somatostatin → wide spread effects:
1) Inhibit release of hormones and transmitters (eg. gastrin, VIP, 5-HT)
2) ↓ intestinal and pancreatic secretions
3) ↓GI motility and ↓inhibits gallbladder contraction

Question 31

What are 5 AEs of Somatostatin-like peptides?

Answer 31

1) Steatorrhoea (↓pancreatic secretion)
2) Nausea, abdo pain, flatulence, diarrhoea
3) Gall stones, gall sludge → acute cholecystitis
4) Bradycardia
5) LT treatment → hypothyroidism

Question 32

When is activated charcoal used?

Answer 32

Emergency treatment of certain types of poinings?

Question 33

What are 4 AEs of charcoal?

Answer 33

1) Nausea, vomiting
2) Aspiration → bronchiolitis obliterans, empyema, ARDS
3) LT → maladsorption of drugs