Anti-diarrhoeals Flashcards
What are 6 groups of drugs used to treat diarrhoea?
1) Opioid agonist
2) Colloidal bismuth compounds
3) Intestinal adsorbents
4) Products of Lactobacillus acidophilus
5) Bile salt-binding resins
6) Somatostatin-like peptides
What are the anti-diarrhoeal agents for acute diarrhoea?
1) Opioid agonists
2) Colloid bismuth compounds
3) Intestinal adsorbents
4) Lyophilizate of killed Lactobacillus acidophilus
What are the anti-diarrhoeal agent for chronic diarrhoea?
1) Bile salt-binding resins
2) Somatostatin-like peptides
What is the 1st line drug for rapid, symptomatic relief of diarrhoea?
Loperamide
What are 2 examples of opioid agonists?
1) Loperamide
2) Diphenoxylate (+ atropine)
What is the moa of opioid agonists?
Act in enteric NS → ↑colonic transit time
What is the main concern of loperamide use?
Overdose → risk of cardiac abnormalities
Which of the opioid agonists are at risk of dependence and what is done to prevent it?
Diphenoxylate (@ high dose)
- prep w atropine to discourage overdose and dependence
(Loperamide does not cross BBB)
What are 3 AEs of opioid agonists?
1) CNS effects: addiction/dependence/abuse
2) Diphenoxylate + atropine → parasympatholytic effects (eg. xerostomia)
3) Risk of cardiac abnormalities on loperamide overdose
What are 2 examples of colloidal bismuth compounds?
1) Bismuth subcitrate
2) Bismuth subsalicylate
What is the moa of colloidal bismuth compounds?
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)
Which anti-diarrhoeal drug turns tongue and stools black?
Colloid Bismuth Compounds
What are 4 AEs of colloidal bismuth compounds?
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
In which px should bismuth compounds be avoided?
Renal insufficiency
(+ dont use LT)
What are 2 examples of intestinal adsorbents?
1) Kaolin
2) Diosmectite
What is the moa of intestinal adsorbents?
1) Adsorbs bacteria, bacterial toxins, and fluid
2) Decrease stool liquidity and number
What is the main AE of intestinal adsorbent?
Constipation
Intestinal adsorbents should not be taken with _____________ within _____________.
Any other medication within 2 hrs of other medications
What is an example of a lyophilizate of killed Lactobacilius acidophilus?
Lacteol fort
What is the moa of Lacteol fort?
Heat-inactivated Lactobacillus acidophilus adheres onto surface of intestinal cells
→ normalise intestinal flora by competitive exclusion
→ prevent overcolonisation by other organisms
What is indicated in traveler’s diarrhoea?
Lacteol fort
When is lacteol fort (lyophilizate of killed Lactobacilius acidophilus) contraindicated?
px with lactose intolerance (formulation contains lactose monohydrate)
What is an example of a bile salt-binding resins used as a anti-diarrhoeal?
1) Cholestyramine
2) Colestipol
3) Colesevelam
What is the moa of bile salt-binding resins used as a anti-diarrhoeal?
Resins bind to bile salts in colon → alleviate diarrhoea cause by osmotic laxative-like effect of fecal bile salts
What are 6 AEs of bile salt-binding resins used as a anti-diarrhoeal?
1) Bloating
2) Flatulence
3) Constipation
4) Fecal impaction
5) Exacerbated fat malabsorption
Bile salt-binding resins should not be taken with _____________ within _____________.
Any other oral drugs within 2 hrs
What is used to treat chronic diarrhoea due to Crohn’s disease or surgical resection of ileum?
Bile salt-binding resins (eg. Cholestyramine)
What is used to treat chronic secretory diarrhoea due to GI and neuroendocrine tumours (eg. VIPoma and Carcinoid tumours)?
Somatostatin-like peptides (eg. Ocreotide)
How is Octreotide administered?
1) Subcut injection
2) Intramuscular depot formations
What is the moa of somatostatin-like peptides (eg. Octreotide)?
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
What are 5 AEs of Somatostatin-like peptides?
1) Steatorrhoea (↓pancreatic secretion)
2) Nausea, abdo pain, flatulence, diarrhoea
3) Gall stones, gall sludge → acute cholecystitis
4) Bradycardia
5) LT treatment → hypothyroidism
When is activated charcoal used?
Emergency treatment of certain types of poinings?
What are 4 AEs of charcoal?
1) Nausea, vomiting
2) Aspiration → bronchiolitis obliterans, empyema, ARDS
3) LT → maladsorption of drugs