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411 > W13 Pharmacology > Flashcards

W13 Pharmacology Flashcards

1
Q

Examples of bulk laxatives

A

Bran, apples, broccoli

Methylcellulose (citrucel), psyllium husk (Metamucil)

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2
Q

Mechanism of action of bulk laxatives

A

Indigestible water absorbing molecules

Intestinal distension leading to ENS stimulation of peristalsis

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3
Q

What are osmotic laxatives

A

Poorly absorbed molecules

  • salts
  • sugars
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4
Q

Mechanism of action of osmotic laxatives

A

Poorly absorbed salts
Retain/ draw water back into colon by osmosis
Increased stimulation of peristalsis
Some soften stools

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5
Q

Examples of stimulant/contact laxatives

A 
Sennosides (Ex-Lax)
Diphenylmethane derivatives (bisacodyl)
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6
Q

Mechanism of action of stimulant/contact laxatives

A

Direct stimulation of myenteric plexuses in ENS

Increased smooth muscle motility and evacuation of contents

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7
Q

What type of laxative is acid sensitive ?

A

Stimulant

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8
Q

What type of laxative is indicated for bowel evacuation?

A

Osmotic

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9
Q

When are laxatives contraindicated?

A

Known/suspected GI blockage

Pregnancy (stimulant (castor oil))

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10
Q

Side effects of bulk laxatives

A

Bloating

Flatulence

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11
Q

Side effects of osmotic laxatives

A

Bloating, flatulence
Cramping, diarrhea
Electrolyte imbalance

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12
Q

Side effects of stimulant laxatives

A

Cramping, diarrhea

Colon pigmentation

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13
Q

Examples of stool softeners (emollients)

A

Glycerin

Docusate

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14
Q

Mechanism of action of stool softeners

A

Lower surface tension —> increase lubrication

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15
Q

Contraindications and side effects of stool softeners

A

Known or suspected GI blockage

Rectal irritation

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16
Q

What is methylnaltrexone?

A

An opioid receptor antagonist

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17
Q

Mechanism of action of opioid receptor antagonists

A

Relieve opioid-mediated inhibition of GI tract —> stimulatory effect on GI motility

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18
Q

Pharmacokinetics of opioid receptor antagnists

A

Subcutaneous administration

Doesn’t readily cross BBB —> peripherally selective effect

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19
Q

Treatment of opioid induced constipation

A
  1. Laxatives and stool softeners
  2. PAMORAs (mu-opioid receptor antagonists )
  3. Chloride channel activators (lubiprostone)
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20
Q

Indications and contraindications of opioid receptor antagonists

A

I: opioid induced constipation
C: known or suspected GI blockage

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21
Q

Side effects of opioid receptor antagonists

A

Abdominal pain and/or cramping
Diarrhea and/or flatulence
Nausea

22
Q

Example of an antimotility agent

A

Loperamide

- selective mu opioid receptor agonist

23
Q

Mechanism of action of loperamide

A

Inhibition of neural activity of the GI tract —>

Increased colonic transport time and water absorption

24
Q

Pharmacokinetics of loperamide

A

Doesn’t readily cross BBB

Doesn’t appear to produce tolerance with chronic use

25
Q

Indications, contraindications and side effects of loperamide

A

I: symptomatic relief of acute and chronic diarrhea
C: worsening diarrhea while on drug
SE: constipation

26
Q

Mechanism of action of bismuth subsalicylate

A

Antisecretory effects
Subsalicylate mediated reduction of
- intestinal prostaglandin production —> reduced motility
- chloride secretion —> reduced liquidity
Antimicrobial effects

27
Q

Drugs used to reduce inflammation in IBD

A 
Aminosalicylates 
Glucocorticoids 
Immunosuppressants 
Anti-TNFa therapy 
Anti-integrin therapy
28
Q

Mechanism of action of 5-ASA

A

Anti-inflammatory:

  • NSAID like inhibition of prostaglandins ?
  • interfere with cytokine production ?
  • reduced leukocyte activity ?
29
Q

Pharmacokinetics of 5-ASA

A

Acts topically

Up to 80% absorbed in small intestine

30
Q

5 ASA formulations that are absorbed primarily in large intestine

A

Sulfasalazine, balsalazide, olsalazine
Azo conjugation
Prevents absorption until bacterial cleavage in large colon

31
Q

5-ASA indications and contraindications

A

I: UC - induction and maintenance of remission
C: children <2 (Reye’s syndrome), aspirin allergies

32
Q

5-ASA side effects

A 
Nausea
Headaches 
Impaired folate absorption 
Hypersensitivity (rare) 
Kidney inflammation (rare)
33
Q

Glucocorticoids examples

A

Prednisone

Prednisolone

34
Q

Glucocortioids mechanism of action

A

Anti-inflammation:

  • inhibition of chemokine/cytokine production
  • inhibited transcription of several pro-inflammatory mediators
35
Q

Pharmacokinetics of glucocorticoids

A

Enema and suppository formulations

36
Q

Indications and contraindications of glucocorticoids

A

I: induction of remission in IBD
C: peptic ulcer disease, heart disease or hypertension with HF, osteoporosis

37
Q

Side effects of glucocorticoids

A

Peptic ulcer disease
Adrenal suppression
Fewer with budesonide

38
Q

Example of an immunosuppressant

A

Azathioprine (purine analogue)

39
Q

Mechanism of action of azathioprine

A

Converted it guanine analogue that halts DNA/RNA synthesis

Somewhat selective for rapidly dividing cells

40
Q

Mechanism of action of methotrexate (immunosuppressant)

A

Inhibition of a key enzyme required for nucleotide synthesis
Inhibition of cell proliferation unlikely at doses used in IBD treatment

41
Q

Indications and contraindications for immunosupressants

A

Azathioprine
- UC, CD —> induction and maintenance of remission
- Con: adjust dosing in TPMT deficient individuals
Methotrexate
-CD —> induction and maintenance of remission

42
Q

side effects of immunosuppressants

A

Nausea and vomiting
Bone marrow suppression
Hypersensitivity to azathioprine
- fever, pancreatitis, hepatitis, diarrhea

43
Q

What is infliximab

A

Anti-TNF-a drug

44
Q

Mechanism of action of Anti-TNF-a drugs

A

Monoclonal antibody against tumour necrosis factor

-major pro-inflammatory cytokine in IBD

45
Q

How is infliximab administered and what is its half life

A

IV

8-10 days

46
Q

Indications for infliximab

A

Induction and maintenance of unresponsive to previous therapies moderate to severe CD and UC

47
Q

Contraindications of Anti-TNF-a

A 
Current infecctions
Latent infections (TB, Hep B)
48
Q

Side effects of anti-tNF-a

A

Opportunistic infections

Hypersensitivity

49
Q

What is a drug used for anti-integrin therapy ?

A

Vedolizumab

50
Q

Mechanism of action of anti-integrin therapy

A

Prevent leukocyte adhesion to endothelium via integrin antagonism

51
Q

Indications for anti-integrin therapy

A

Moderate to severe UC and CD unresponsive to other therapies
- carefully monitored IV at 0,2,6,14 weeks

52
Q

Side effects of vedolizumab

A

Nasopharyngitis
Headache
Arthralgia

411 (16 decks)

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