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Pre final studying > Drugs for Lower GI > Flashcards

Drugs for Lower GI Flashcards

1
Q

What are the 3 groups of treatment for Constipation?

A

Laxatives
opioid receptor antagonists
stool softeners

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2
Q

What are the three types laxatives

A

Bulk
osmotic
stimulant

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3
Q

What are bulk laxatives MOA?

A

MOA:
introduce indigestiable . water absorbing molecules
Intestinal distention leads to ENS stimulation of Peristalsis

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4
Q

What are the three types of bulk laxatives?

A

Dietary fiber- apples

Supplemental intake-
methykcellulose Citucel
Psyllium husk metamucil

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5
Q

What is the MOA of Osmotic laxatives

A

Poorly abosorbed moleucles like salts (MgO2) and sugars (lactulose polyethylene glycol 3350) retain and draw water into colon via osmosis , increase stimulation of peristalsis
may also help as stool softener

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6
Q

What are the Stimulant /contact laxatives? (2)

A

1) Sennosides (Senna spp. Derivatives Ex-lax)
2) Diphenylmethane derivatives

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7
Q

What is MOA of Stimulant/contact laxatives

A

Direct stimulation of myenteric plexuses in the ENS
Increase smooth muscle motility and evacuation of contents

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8
Q

Pharmacokinetics of bulk, osmotic laxatives

A

Minimal systemic absorptions
subject to GI transit rates

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9
Q

Pharmacokinetics of stimulant laxatives?

A

Minimal systemic absorptions
subject to GI transit rates
Need acid sensitive coating

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10
Q

Which type of laxative is used for bowel execution pre-surgery

A

osmotic

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11
Q

CI for bulk and osmotic laxatives

A

Known/suspected GI blockage

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12
Q

CI for Stimulant laxatives

A

Castor oil- Pregnancy- uterine contractions

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13
Q

Side effects for bulk laxatives

A

Bloating and flatulence

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14
Q

Side effect for Osmotic laxatives

A

Bloating and flatulence
cramping and diarrhea
electrolyte imbalances- salts.sugars

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15
Q

Side effect for stimulant laxatives

A

bloating and flatulence
cramping and diarrhea
Colon pigmentation (melanosis coli)

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16
Q

What are the two Stool softeners?

A

Glycerin
Docusate

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17
Q

MOA of stool softeners

A

Lowers surafce tnesion and increases lubrication of feces
reduces effort of excertion

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18
Q

Pharmacokinetics

A

Oral and rectal formaulations

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19
Q

CI of stool softeners

A

Known or suspected GI blockage

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20
Q

Side effects Stool softeners

A

rectal irritation

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21
Q

Name of Opioid receptor antagonists

A

methylnatrexone

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22
Q

MOA of Opioid receptor antagonists

A

selective competitive block of mu (u)-opiod receptors

Relieve opiod mediated inhibition of GI tract
Net stimularoty effect of GI motility

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23
Q

Pharmacokinetics of Opioid RAs

A

Subcutaneous administration
does not cross BBB-> preipherally selective effect
minimal effect on opioid induced analgesia

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24
Q

Opiod constipation treatment

A
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25
Q

Indication for opioid receptor antagonists

A

Opioid induced constipation

pain

palliative-care patients non-responsive to other treatment

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26
Q

Contraindication for Opioid receptor antagonists

A

Known or suspected GI blockage

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27
Q

Side effects of Opioid receptor antagonists

A
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28
Q

What are the two treatments for diarrhea pharm?

A

Opioid receptor agonists- loperamide

and

bismuth subsalicylate

also absorbants and anti-infectives

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29
Q
A
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30
Q

What is MOA of loperamide?

A

selective mu-opioid receptor agonist

inhibition of neural activity in GI tract leading to increase colonic transport time and water absorption

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31
Q

Pharmacokinetics of Loperamide

A

Does not easily cross BBB-> peripherally selective effect

does not appear to produce tolerance with chronic use

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32
Q

Contraindications of loperamide

A

worsening diarrhea while on drug

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33
Q

Side of effects of loperamide

A

Constipation

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34
Q

What ios MOA of bismuth subsalicylate

A

Antisecretory effect

1) reduces intestinal prostaglandin production->educed motility (reduced smooth muscle stim)
2) reduces chloride secretion
3) Antimicrobial effect

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35
Q

What are the 5 drug classes to reduce the inflammatory activity of IBD?

A

Aminosalicylates

Glucocorticoids

immunosuppresants

anti-TNF alpha therapy

Anti-integrin therapy

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36
Q

Name of the one Aminosalicytes that we know :) and the other 4 random ones

A

5-aminosalicylate

(5-ASA)

Azo-conjugated

sulfasalazine

balsalazide

olsalazine(dipendum)

the granule release- Mesalamine

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37
Q

What is the MoA of 5-ASA

A

Anti-inflammatory

Nsaid like inhibition of production

interfere with cytokine production

reduced leukocyte activity

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38
Q

Pharmacokinetics of 5-ASA

A

Acts topically at the site of diseased mucosa within the ileum and or large intestine

don’t need or want systemic absorption and distribution not required

up to 80% absorbed in small intestine

formulation designed to increase drug exposure to the distal small and large intestinal tissue

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39
Q
A
40
Q

indications for 5-ASA

A

UC induction and maintenance of remission

is used in Crohns but unproven use but still 1st line

41
Q

Contraindication for 5-ASA

A

Due to similarity to asprin

Children under 2 (risk of Reye’s syndrome)

Aspirin allergies

42
Q

Side effects of 5-ASA

A

Nausea and or GI upset

Headaches

impaired folate absorption-> supplement recommended

Rare

Hypersensitivity

inflammation of kidney rare- do functional tests 6 wks, 6 months, and the anually

43
Q

Names of the Glucocorticoids we know

A

Prednisone

prednisolone

budesonide

44
Q

MOA of Glucocorticoids

A

Anti-inflammation through

inhibition of chemokine/cytokine production

inhibition transcription of several pro-inflammatory mediators

45
Q

Glucocorticoids pharmacokinetics

A

Low oral bioavailability (1st pass metabolism)

controlled release formulations for increased delivery to distal ileum and colon

46
Q

Indications for use of Glucocorticoids

A

Induction of remission in inflammatory bowel disease

47
Q

CI for Glucocorticoids

A

PUD

Heart disease

Hypertension with heart failure

Osteoporosis

48
Q

Side effects of Glucocorticoids

A

PUD

Adrenal suppression

Fewer side effects with budesonide

49
Q

Name of the 2 immunosuppressants we know

A

Azathioprine

Methotrexate

50
Q

MOA of Azathioprine?

A

Converted to guanine analogue that halts DNA/RNA synthesis

Somewhat selective for cells dividing rapidly such as immune cells

51
Q

MOA methotrexate?

A

Inhibition of a key enzyme required for nucleotide synthesis

inhibition of cell proliferation unlikely at does use in IBD treatment

52
Q

Indications for Azathioprine

A

UC and Crohns disease

induction and maintenance of remission

53
Q

Indications for methotrexate

Crohn’s disease

induction and maintenance of remission

uncertain efficacy in UC

A
54
Q

Contraindications of immunosuppressants

A

Adjusted azathioprine dosing in TPMT deficient individuals

thiopurine metabolism

55
Q

Side effects of immunosupressents

A

Nausea and vomiting

Bone marrow suppression-> anemia, leukopenia

Azathioprine-> hypersensitivity

fever pancreatitis hepatitis diarrhea

56
Q

What is the name of the anti-TNF alpha therapy we know

A

Infliximab

57
Q

MOA of Anti-TNF alpha therapy

A

Mab against tumor necrosis factor

tumor necrosis factor is a major pro-inflammatory cytokine particularly in IBD

58
Q

Pharmacokinetics of Anti-TNF-alpha therpay

A

IV administration

8-10 days half life

59
Q

Indications for Anti-TNF alpha therapy

A

Induction and mainenance of unresponsive to pervious therapies

moderate to severe Crohn’s disease

Moderate to severe UC

60
Q

CI for Anti-TNF-alpha

A

current infections

latent infections TB hep B

Reactivation risk may be able to proactive reat

61
Q

Side effects of anti-TNF-alpha therapy

A

Opportunistic infections

hypersensitivity

62
Q

Anti-integrin therapy name of drug we know

A

vedolizumab

63
Q

MOA of anti-integrin therapy

A

Prevent leukocyte adhesion to endothelium via integrin antagonism

sorta selective for gut endothelial cell adhesion molecules

64
Q

Indications for Anti integrin therapy

A

Moderate to sever UC and Crohns unrepsponsive to other therapies

Carefully monitored IV at 0 ,2 6, 14 weeks ,discontinues if no benefit

65
Q

Side effects

of anti-integrin therapy

A

Nasopharyngitis,headache and or arthralgia in 10%

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Pre final studying (8 decks)

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