Laxatives Flashcards

(37 cards)

1
Q

What are 7 groups of drugs used as laxatives?

A

Physical:
1) Bulk-forming
2) Stool surfactant
3) Osmotic

Physiological:
4) Stimulant
5) Cl channel activators
6) Opioid receptor antagonists
7) 5-HT4 receptor antagonists

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2
Q

What are 3 examples of bulk-forming agents?

A

1) Psyllium (fibre)
2) Methylcellulose (semi-synthetic)
3) Polycarbophil (synthetic)

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3
Q

What is the moa of bulk-forming agents?

A

Indigestible, hydrophilic colloids (fibre)
→ absorbs water → form bulk, emollient gel → distend colon
→ promote peristalsis

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4
Q

What are 3 AEs of bulk-forming agents?

A

Bacterial digestion of fibres in colon:
1) Flatus
2) Bloating
3) Abdo pain

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5
Q

What should bulk-forming agents be administered with?

A

Lots of water

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6
Q

When should bulk-forming agents be avoided?

A

1) Suspected obstruction
2) ↓absorption of other oral drugs (do not use within 2 hrs before or after)

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7
Q

What are 2 examples of stool surfactant agents (softeners)?

A

1) Glycerin + NaCl (enema)
2) Mineral Oil (Oral)

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8
Q

What is the moa of stool surfactant agents?

A

↓ surface tension → water and lipids can penetrate stool

  • mineral oil lubricates + slows water reabsorption from stool
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9
Q

What are 2 main AEs of stool surfactant agents?

A

Mineral oil:
1) Aspiration → sever lipid pneumonitis (aspiration pneumonia)

2) LT use → ↓fat-soluble vit ADEK absorption

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10
Q

What are 3 examples of osmotic laxatives?

A

Nonabsorbable sugars
1) Lactulose
2) Sorbitol

Non-absorbable salts:
1) MgOH
2) Na2PO4
3) Magnesium citrate

Macrogol (balanced polyethylene glycol)

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11
Q

What are 2 general AEs of osmotic laxative and 4 for Na2PO4?

A

General: bacterial digestion of sugars
1) Flatus
2) Abdo cramps

Na2PO4:
1) HyperPO4
2) HyperNa
3) HypoCa
4) HypoK
5) Cardiac arrythmia, ARF 2° to nephrocalcinosis)

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11
Q

What should osmotic laxatives be administered with?

A

Lots of water

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11
Q

In which px should sodium phosphate be avoided?

A

1) Frail, elderly
2) Diuretics, cannot adequately hydrate
3) Renal insufficiency
4) Cardiac disease

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12
Q

What is the moa of osmotic laxatives?

A

Osmosis of water into bowel → ↑stool liquidity & volume
→ stimulate peristalsis

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13
Q

Which of the osmotic laxatives are the safest in terms of limited AEs and why?

A

Balanced macrogol
- contains sugar w electrolytes → avoids significant electrolyte shifts
- does not produce significant cramps or flatus

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14
Q

What are 2 examples of stimulant laxatives (cathartics)?

A

1) Senna (anthraquinone derivatives)
2) Bisacodyl (diphenylmethane derivatives)

15
Q

What is the moa of stimulant laxatives?

A

Poorly understood
produce migrating colonic contractions by:
1) direct stimulation of enteric NS
2) Colonic electrolyte and fluid secretion

16
Q

What 2 laxatives are used for colonic cleansing prior to a colonscopy?

A

Bisacodyl (stimulant laxative)
Balanced Macrogol (PEG) (Osmotic laxative)

17
Q

What are 2 AEs of stimulant laxatives?

A

Anthraquinone derivatives (eg. senna):
1) Chronic use → brown pigmentation of colon
2) Possible carcinogenicity

Diphenylmethane derivatives (eg. Bisacodyl)
3) Cardiac toxicity

18
Q

What should px who are taking oral bisacodyl be advised of?

A

No milk product 1hr of taking bisacodyl
(milk product → break down enteric coating → gastric irritation/dyspepsia)

19
Q

What is an example of a chloride channel activator?

20
Q

What is the moa of lubiprostone?

A

1) Stimulate Type 2 Cl channels (ClC-2) in small intestine
2) ↑Cl-rich fluid secretions
3) Stimulates motility → ↓transit time

21
Q

What are 2 AEs of Cl channel activators?

A

1) Return of constipation after discontinuation
2) Nausea due to delayed gastric emptying

22
Q

When should Cl-channel activators be avoided?

A

Pregnant women

23
Which laxatives induce soft stools in 1-3days?
1) Bulk laxatives 2) Osmotic laxatives (lactulose) 3) Stool surfactant agents
24
Which laxative induce soft/semi-fluid stools in 6-8hrs?
Stimulant laxatives (oral)
25
Which laxative induce watery stools in 1-3 hrs?
1) Osmotic laxatives 2) PEG/Balanced macrogol 3) Suppository (Bisacodyl)
26
What is an example of an opioid receptor antagonist?
Methylnaltrexone bromide
27
What is the specific indication of Methylnaltrexone bromide?
Opioid-induced constipation (µ-opioid receptor antagonist) - subcut every 2 days
28
Does Methylnaltrexone bromide block the CNS analgesic effects of opioids?
No, does not readily cross BBB
29
What are 5 AEs of opioid receptor antagonists?
1) Abdo pain 2) Nausea 3) Diarrhoea 4) Flatulence 5) Sweating 6) GI perforation (rare but severe)
30
What are 2 examples of 5-HT4 receptor agonists?
1) Prucalopride 2) Cisapride
31
What is the moa of 5HT4 agonists?
Stimulate 5-HT4 receptors on nerve terminals in the GIT walls → ↑NT release and smooth muscle motor activity →prokinetic/promotes GI motility
32
What are 5 common AEs of 5HT4-receptor agonists?
1) Abdo pain 2) Nausea 3) Dizziness 4) Headache 5) Diarrhoea
33
What is the difference in AEs of Cisapride and Prucalopride?
Cisapride: 5HT4 partial agonist → adverse cardiovascular effects (actions at hERG K+ channels) Prucalopride: high-affinity 5-HT4 agonist (no CVS effects)
34
When are 5-HT4 receptor agonists contraindicated?
During intestinal obstruction
35
What are 2 laxative classes that should not be used in intestinal obstruction?
1) 5-HT4 receptor agonists (eg. prucalopride) 2) Bulk-forming agonists (eg. Psyllium)