W13 Pharmacology Flashcards

(52 cards)

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
Indications, contraindications and side effects of loperamide
I: symptomatic relief of acute and chronic diarrhea C: worsening diarrhea while on drug SE: constipation
26
Mechanism of action of bismuth subsalicylate
Antisecretory effects Subsalicylate mediated reduction of - intestinal prostaglandin production —> reduced motility - chloride secretion —> reduced liquidity Antimicrobial effects
27
Drugs used to reduce inflammation in IBD
``` Aminosalicylates Glucocorticoids Immunosuppressants Anti-TNFa therapy Anti-integrin therapy ```
28
Mechanism of action of 5-ASA
Anti-inflammatory: - NSAID like inhibition of prostaglandins ? - interfere with cytokine production ? - reduced leukocyte activity ?
29
Pharmacokinetics of 5-ASA
Acts topically | Up to 80% absorbed in small intestine
30
5 ASA formulations that are absorbed primarily in large intestine
Sulfasalazine, balsalazide, olsalazine Azo conjugation Prevents absorption until bacterial cleavage in large colon
31
5-ASA indications and contraindications
I: UC - induction and maintenance of remission C: children <2 (Reye’s syndrome), aspirin allergies
32
5-ASA side effects
``` Nausea Headaches Impaired folate absorption Hypersensitivity (rare) Kidney inflammation (rare) ```
33
Glucocorticoids examples
Prednisone | Prednisolone
34
Glucocortioids mechanism of action
Anti-inflammation: - inhibition of chemokine/cytokine production - inhibited transcription of several pro-inflammatory mediators
35
Pharmacokinetics of glucocorticoids
Enema and suppository formulations
36
Indications and contraindications of glucocorticoids
I: induction of remission in IBD C: peptic ulcer disease, heart disease or hypertension with HF, osteoporosis
37
Side effects of glucocorticoids
Peptic ulcer disease Adrenal suppression Fewer with budesonide
38
Example of an immunosuppressant
Azathioprine (purine analogue)
39
Mechanism of action of azathioprine
Converted it guanine analogue that halts DNA/RNA synthesis | Somewhat selective for rapidly dividing cells
40
Mechanism of action of methotrexate (immunosuppressant)
Inhibition of a key enzyme required for nucleotide synthesis Inhibition of cell proliferation unlikely at doses used in IBD treatment
41
Indications and contraindications for immunosupressants
Azathioprine - UC, CD —> induction and maintenance of remission - Con: adjust dosing in TPMT deficient individuals Methotrexate -CD —> induction and maintenance of remission
42
side effects of immunosuppressants
Nausea and vomiting Bone marrow suppression Hypersensitivity to azathioprine - fever, pancreatitis, hepatitis, diarrhea
43
What is infliximab
Anti-TNF-a drug
44
Mechanism of action of Anti-TNF-a drugs
Monoclonal antibody against tumour necrosis factor | -major pro-inflammatory cytokine in IBD
45
How is infliximab administered and what is its half life
IV | 8-10 days
46
Indications for infliximab
Induction and maintenance of unresponsive to previous therapies moderate to severe CD and UC
47
Contraindications of Anti-TNF-a
``` Current infecctions Latent infections (TB, Hep B) ```
48
Side effects of anti-tNF-a
Opportunistic infections | Hypersensitivity
49
What is a drug used for anti-integrin therapy ?
Vedolizumab
50
Mechanism of action of anti-integrin therapy
Prevent leukocyte adhesion to endothelium via integrin antagonism
51
Indications for anti-integrin therapy
Moderate to severe UC and CD unresponsive to other therapies - carefully monitored IV at 0,2,6,14 weeks
52
Side effects of vedolizumab
Nasopharyngitis Headache Arthralgia