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Drugs for Lower GI Flashcards

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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
Indication for opioid receptor antagonists
Opioid induced constipation pain palliative-care patients non-responsive to other treatment
26
Contraindication for Opioid receptor antagonists
Known or suspected GI blockage
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Side effects of Opioid receptor antagonists
28
What are the two treatments for diarrhea pharm?
Opioid receptor agonists- loperamide and bismuth subsalicylate also absorbants and anti-infectives
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What is MOA of loperamide?
selective mu-opioid receptor agonist inhibition of neural activity in GI tract leading to increase colonic transport time and water absorption
31
Pharmacokinetics of Loperamide
Does not easily cross BBB-\> peripherally selective effect does not appear to produce tolerance with chronic use
32
Contraindications of loperamide
worsening diarrhea while on drug
33
Side of effects of loperamide
Constipation
34
What ios MOA of bismuth subsalicylate
Antisecretory effect 1) reduces intestinal prostaglandin production-\>educed motility (reduced smooth muscle stim) 2) reduces chloride secretion 3) Antimicrobial effect
35
What are the 5 drug classes to reduce the inflammatory activity of IBD?
Aminosalicylates Glucocorticoids immunosuppresants anti-TNF alpha therapy Anti-integrin therapy
36
Name of the one Aminosalicytes that we know :) and the other 4 random ones
5-aminosalicylate (5-ASA) Azo-conjugated sulfasalazine balsalazide olsalazine(dipendum) the granule release- Mesalamine
37
What is the MoA of 5-ASA
**Anti-inflammatory** Nsaid like inhibition of production interfere with cytokine production reduced leukocyte activity
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Pharmacokinetics of 5-ASA
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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indications for 5-ASA
UC induction and maintenance of remission is used in Crohns but unproven use but still 1st line
41
Contraindication for 5-ASA
Due to similarity to asprin Children under 2 (risk of Reye's syndrome) Aspirin allergies
42
Side effects of 5-ASA
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
Names of the Glucocorticoids we know
Prednisone prednisolone budesonide
44
MOA of Glucocorticoids
Anti-inflammation through inhibition of chemokine/cytokine production inhibition transcription of several pro-inflammatory mediators
45
Glucocorticoids pharmacokinetics
Low oral bioavailability (1st pass metabolism) controlled release formulations for increased delivery to distal ileum and colon
46
Indications for use of Glucocorticoids
Induction of remission in inflammatory bowel disease
47
CI for Glucocorticoids
PUD Heart disease Hypertension with heart failure Osteoporosis
48
Side effects of Glucocorticoids
PUD Adrenal suppression Fewer side effects with budesonide
49
Name of the 2 immunosuppressants we know
Azathioprine Methotrexate
50
MOA of Azathioprine?
Converted to guanine analogue that halts DNA/RNA synthesis Somewhat selective for cells dividing rapidly such as immune cells
51
MOA methotrexate?
Inhibition of a key enzyme required for nucleotide synthesis inhibition of cell proliferation unlikely at does use in IBD treatment
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Indications for Azathioprine
UC and Crohns disease induction and maintenance of remission
53
Indications for methotrexate Crohn's disease induction and maintenance of remission uncertain efficacy in UC
54
Contraindications of immunosuppressants
Adjusted azathioprine dosing in TPMT deficient individuals thiopurine metabolism
55
Side effects of immunosupressents
Nausea and vomiting Bone marrow suppression-\> anemia, leukopenia Azathioprine-\> hypersensitivity fever pancreatitis hepatitis diarrhea
56
What is the name of the anti-TNF alpha therapy we know
Infliximab
57
MOA of Anti-TNF alpha therapy
Mab against tumor necrosis factor tumor necrosis factor is a major pro-inflammatory cytokine particularly in IBD
58
Pharmacokinetics of Anti-TNF-alpha therpay
IV administration 8-10 days half life
59
Indications for Anti-TNF alpha therapy
Induction and mainenance of unresponsive to pervious therapies moderate to severe Crohn's disease Moderate to severe UC
60
CI for Anti-TNF-alpha
current infections latent infections TB hep B Reactivation risk may be able to proactive reat
61
Side effects of anti-TNF-alpha therapy
Opportunistic infections hypersensitivity
62
Anti-integrin therapy name of drug we know
vedolizumab
63
MOA of anti-integrin therapy
Prevent leukocyte adhesion to endothelium via integrin antagonism sorta selective for gut endothelial cell adhesion molecules
64
Indications for Anti integrin therapy
Moderate to sever UC and Crohns unrepsponsive to other therapies Carefully monitored IV at 0 ,2 6, 14 weeks ,discontinues if no benefit
65
Side effects of anti-integrin therapy
Nasopharyngitis,headache and or arthralgia in 10%
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