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Pharmacology > Motility, Laxatives, Anti-diarrheals, IBD > Flashcards

Motility, Laxatives, Anti-diarrheals, IBD Flashcards

1
Q

Which classes of drugs stimulate motility?

A
  1. Metocloparamide
  2. Cholinergic or Acetylcholinesterase
  3. Macrolides
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2
Q

Bethanecol, Neostigmine, are in what drug class?

A
  1. Cholinergic or Acetylcholinesterase
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3
Q

What is MOA of bethanecol

A

stimulates muscarinic receptors on muscle cells and my-enteric plexus
*used to tx gastroparesis

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4
Q

What is MOA of neostigmine?

A

blocks AChE to prolong affect of Ach

* enhances gastric and colonic emptying

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5
Q

What are the ADE of cholinergic agents?

A
  • salivation
  • N/V/D
  • bradycardia
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6
Q

What are the clinical uses of cholinergic agents?

A
  • GERD
  • diabetic gastroparesis
  • post surgical disorders that cause delayed emptying ( vagotomy, antrectomy
  • to promote advancement of nasoenetric tubes from stomach to duodenum
  • non-ulcer dyspepsia
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7
Q

What is MOA of metoclopramide?

A

Dopamine receptor antagonist

  • blocks cholinergic smooth muscle stimulation
  • Increases: esophageal peristalsis, gastric emptying, LES pressure
  • has NO effect in small intestine or colon
  • anti-emetic action: blocks chemo receptor zone in medulla
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8
Q

What are ADE of metoclopramide?

A
  • CNS: insomnia, agitation, drowsiness
  • Extra pyramidal effects: Parkinsonism, dystonias, akathisia
  • Tardive dyskinesia
  • elevated prolactin (galactorrhea, gynecomastia, impotence , menstrual disorders
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9
Q

What is MOA of macrolides/ azithromycin?

A

-binds motilin receptors on gastrointestinal smooth muscle and produce onset of migrating motor complex

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10
Q

What is a disadvantage to using macrolides?

A

-rapid tolerance develops

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11
Q

What is the clinical use of macrolides?

A
  • tx for gastroparesis

- used when patient has upper GI bleed and need to promote gastric emptying of blood for endoscopy

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12
Q 
What drug class do the follwoing belong to:
Bulk forming
Stool softeners
osmotic laxatives
stimulant laxatives
chloride channel activator 
Guanylate-cyclase C agonists
Opioid receptor antagonist 
Seratonin 5HT4 receptor agonist
A

Laxatives

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13
Q

Which drug classes can cause constipation?

A
  • Opioids
  • Diuretics
  • Calcium carbonate or or AlOH antacids
  • Iron preparations
  • NSAIDS
  • TCA
  • Anti-cholinergic
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14
Q

How do you prevent constipation?

A
  • high fiber diet
  • adequate fluid intake
  • exercise
  • heeding of nature’s call
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15
Q

How do you treat constipation?

A

-treat the specific diagnosis
or
choose symptomatic therapy
Ex. give opioid antagonist to tx opioid induced constipation

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16
Q

Which agents cause watery evacuation of stool in 1-6 hrs?

A

PEG-4L
Magnesium citrate or Magnesium hydroxide
Bisacodyl -rectal prep
sodium phosphate

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17
Q

Which agents cause semi fluid stools in 6-12 hrs?

A

Bisacodyl- 15mg orally

Senna

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18
Q

Which bulking agents cause fecal softening in 1-3 days?

A

Psyllium
Polycarbophil
Methylcellulose4-6 gm/day

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19
Q

What is MOA of bulk forming laxatives?

A

they are indigestible colloids that attract water creating bulk and dilating the colon ( emollient gel created)=peristaltic waves

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20
Q

What are common preparations of bulk forming agents?

A
  • Natural: psyllium, methylcellulose

synthetic: polycarbophil

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21
Q

What are ADE of laxatives?

A

bloating and flatulence

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22
Q

What is clinical use of bulking laxatives?

A
  • used for prevention of constipation

- don’t use in mega colon or mega rectum

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23
Q

What is MOA of stool softeners?

A

-decrease surface tension of stool allowing water to penetrate and soften the stool main passage easier

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24
Q

Name two stool softeners?

A
  • docusate (rectal or oral administration

- mineral oil ( lubricates fecal material, not tasty but take with juice?

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25
What is the clinical use of stool softeners?
- tx fecal impaction in kids and adults - prevent constipation - reduce straining at defecation
26
What are the disadvantages of stool softeners?
- long term use can cause deficiency in fat soluble ADEK vitamins - aspiration can lead to lipid pneumonitis
27
What is MOA of osmotic laxatives?
-work in the colon by retaining water in the lumen ( create an osmotic pressure) side note: the colon is isotonic and cannot concentrate or dilute
28
Lactulose and Sorbitol -nonabsorbable sugar laxatives | Milk of Mg (MgOH)
ADE of Lactulose/Sorbitol: flatulence | ADE of milk of mg: dont use if pt has renal issues
29
What is clinical use of Sugar/Salt osmotic laxatives?
acute constipation or prevention of chronic constipation
30
Which osmotic laxative is considered a purgative?
Mg citrate or Sodium phosphate | -prompt bowel evacuation in 1-3 hrs
31
What are some concerns with sodium phosphate?
- high phosphate - low calcium - high soidum - low K * all of these can casue heart issues
32
What is the clinical use of PEG?
- clean colon before endoscopy | - prevention tx in chronic constipation
33
What is special about PEG?
-it is safe for everyone to use because it is an isotonic soln that has an inert, non-absorbable , osmotically active sugar (PEG) and is designed so that no shift in electrolyte fluids occur
34
What are ADE of PEG
safe! | does not cause cramps or flatus!
35
What is MOA of stimulant?
-directly stimulate the enteric NS
36
What is clinical use of stimulant?
long term use for bed bound patients | neurologically impaired
37
T/F Nerve damage may be the cause of chronic constipation rather than the use of stimulant laxatives
True
38
Aloe, senna, and cascara are what drug class?
stimulant laxative -athraquinone derivatives | occur naturally in plants
39
What is MOA of stimulant laxative -athraquinone derivatives?
hydrolyzed in the colon and produce bowel movement in 6-12 hrs when oral 2 hrs when given rectally
40
What is special about Aloe, senna, and cascara?
- chronic use can cause brown pigmentation of colon "melanosis coli" - concern that these agents are carcinogenic but epidemiology studies don't support that
41
What is bisacodyl?
stimulant laxative-dimethylphenate derivative class
42
What is clinical use fo bisacodyl?
tx for acute and chronic constipation - oral dose: 6-10 hrs for bowel movement to happen - rectal dose: 30-60 min for passage to occur - used with PEG for colon cleanse before endoscopy
43
What are ADE of bisacodyl?
safe for long term use | minimal systemic absorption: overall safe
44
Naloxegol, Alvimopan, methylnaltrexzone are what drug class?
Opioid receptor antagonist
45
What is MOA of Opioid receptor antagonist?
act peripherally to block opioid receptors and dont affect analgesia in CNS -don't cross blood brain barrier
46
What is clinical use of methylnaltrexozone?Alvimopan?Naloxegol?
- tx for opioid induced constipation in palliative care - tx for post-operative ileus in hospitalized patients who have undergone large bowel resection, no more than 7 days, CVD risk - tx for opioid induced constipation, contraindicated in pts with obstruction
47
Which drugs can cause diarrhea?
- ABx: clindamycin - Methyldopa - Digoxin - PPI - H2 blockers
48
How do you treat acute diarrhea?
<3 days and fever and neg stool sample: abx and < 3 days and fever with + stool sample for ova, parasite: tx disease < 3 days and no fever: give fluids, loperamide, diet modification
49
How do you tx chronic diarrhea?
> 14 days--> get H&P-->infection, IBD, drug induced, motility issue-->dx: stool sample, endoscopy, culture-->TX : depends on cause if no identified casue give fluids, loperamide, adjust diet
50
T/F It is not appropriate to withhold foods in patients with no dehydration and diarrhea
TRue
51
T/F As bowel movements decrease a band diet is begun
True | BRAT diet
52
T/F Anti-diarrhea agents are not used in bloody diarrhea or systemic toxcity
TRUE
53
What is an anti-motility diarrhea drug?
Opioid agonist | -constipating effect
54
What is an adsorbent anti-diarrheal drug?
Kaolin-pectin
55
What is an anti-secretory anti-diarrheal?
Colloidal bismuth Bile salt binding resins Octreotide Bacterial replacement and enzymes
56
What is MOA of opioid agonists?
- inhibit presynaptic cholinergic neurons in myenteric plexus - increased colonic transmit time and fecal wtaer absorption
57
What is lopermaide?Diphenoxylate?
- opioid agonist-OTC - does not cross blood brain barrier - no analgesia - prescription opioid agonist - with higher doses have CNS effects - can lead to opioid dependence
58
What is MOA of Kaolin-pectin?
adsorbs nutrients, toxins and digestive juices onto the surface of the product
59
What is MOA bile acid sequestrants?
-bile acids are not absorbed in ileum can cause diarrhea in certain disorders? BAS act by binding the bile
60
Cholestyramine, Colestipol, Colesevelam are what drug class?
Bile acid sequestrants
61
What are ADE BAS?
- fecal impaction - constipation - bloating - fat malabsorption - bind other drugs and reduce theri absorption (Except colesevelam)
62
What is an anti-secretory anti-diarrheal?
Octreotide
63
What is somatostatin?
- 14 a.a peptide released in GI tract from D cells, paracrine cells, hypothalamus, enteric nerves - inhibits hormone secretion: - reduces intestinal and pancreatic fluid secretion - slows GI motility and gall bladder contraction
64
What is 1/2 life of somatostatin?
3 min when given by IV-limits is usefulness
65
What is the clinical use of octreotide?
blocks the effects of endocrine tumors other uses: stops pancreatic secretion in patients with a panc fistula, tx for acromegaly ( pituitary tumors), decreases splanchinic blood flow ( GI bleed)
66
Which cancers cause secretory diarrhea?
VIPoma | carcinoid
67
What are ADE of octreotide?
- steatorrhea - bradycardia - hypothyroidism - N/V/D, flatulence
68
TX for bacterial agent causing diarrhea
``` C. jejuni: Cipro or Azithro Cholera: Cipro or Azithro, or Doxy C. diff: oral vancoycin or metronidazole Shigella: Cipro, Azithro Giardia: Metronidazole E. hystolitca: Metro, Tinidazole ```
69
What are the three types of IBS?
IBS-D IBS-C IBS-M
70
What is 1st ine tx for IBS-C?
1st: Psyllium 2nd line: PEG 3rd line: Lubiprostone, linaclotide, plecanatide Refractory: tegaserod , prucalopride
71
T/F For IBS-C PEG improves constipation but not abdominal pain?
TRUE
72
What is MOA of Lubiprostone?
- stimulates type II chloride channel in small intestine and draws chloride rich fluid into the lumen - stimulates intestinal motility
73
What is the clinical use of lubiprostone?
used for IBS-C in women >18 y/o | unproven efficacy in men
74
ADE of lupbiprostone?
- reduce the dose in hepatic issues - Nasuea - Pregnancy C category-don't use in women of child bearing age
75
What is MOA of Linaclotide?
Guanylate Cyclase C Agonist - stimulates intestinal fluid secretion and reduces transit time
76
When do you prescribe linaclotide?
used in patients who have constipation despite being on PEG tx -significant improvement in abdominal pain
77
What is ADE of Linaclotide?
Diarrhea
78
What is MOA of Plecanatide?
Guanylate Cyclase -C agonist : increase in cGMP luminal intestinal epithelium which increase bicarbonate and Chloride and increases GI transit time
79
What is the clinical use of Plecanatide?
chronic constipation IBS-C
80
What is black box warning for Plecanatide?
dehydration risk in pediatric patients | -don't use in pregnancy
81
What are ADE of plecanatide?
UTI Sinusitis Increased AST/ALT
82
What is MOA of tegaserod?
5-HT4 receptor agonist | -stimulates peristaltic reflex and intestinal secretion
83
What is the clinical use of tegaserod?
only used in emergency situations for IBS-C or chronic idiopathic constipation in women <55
84
What are ADE of tegaserod?
increased # of cardiovascular deaths
85
What is MOA of Prucalopride?
selective high affinity 5HT4 receptor agonist -promotes cholinergic and non adrenergic neurotransmission by enteric neurons leading to peristaltic reflex , intestinal secretions and GI motility
86
T/F Reduce dose of Prucalopride in patients with renal issues
True
87
What are ADE of prucalopride?
N/V/D | HA
88
What is 1st tx for IBS-D?
1st: loperamide | give 2mg 45 min before each meal, on regularly scheduled doses
89
How does loperamide work?
- inhibits peristalsis, prolongs transit time, | - it does NOT improve bloating or abdominal pain
90
What is Eulaxodine?
-it is mu and kappa receptor agonist and kappa receptor antagonist
91
What is MOA of Eluxadoline?
-acts locally to reduce abdominal pain and diarrhea doe not cause constipating effects!! -A mixed mu-opioid receptor agonist, delta-opioid receptor antagonist and kappa opioid receptor agonist
92
What is the clinical use for Eluxadoline?
IBS-D
93
What is contraindications for use Eluxadoline? (4)
biliary disorders liver failure pancreatitis alcohol use
94
What are ADE of Eluxadoline?
``` nausea constipation pancreatitis CNS depression abuse potential ```
95
What is 2nd line tx for IBS-D?
Bile acid sequestrants Cholestyramine, Colestipol, Colesevelam -50% of patients with IBS-D have bile acid malabsorption
96
What are ADE of bile acid sequestrants?
bloating, flatulence, abdominal pain, constipation
97
What is MOA for Alosetron?
5HT3 receptor antagonist block activation of visceral afferent pain sensation from enteric NS to spinal cord and reduce sensation of nausea, bloating, and pain -blockade at the terminal ends of entric neurons also decreases motility in left colon and increases total colonic time
98
What is the clinical use of Alosetron?
IBS-D in women who have failed all other therapies | efficacy in men not established
99
PK of alosetron?
potent 5HT3 antagonist-long duration of action extensive cytochrome P450 metabolism -rapidly absorbed in GI- 50% bioavailability
100
What is efficacy of alosetron?
- reduces lower abdominal pain, cramps, urgency and diarrhea - reduces # of bowel movements and improves stool consistency
101
What is black box warning for Alosetron?
GI toxictity ADE: constipation, ischemic colitis requires FDA approval No know drug interactions
102
What is additional therapy that can help tx chronic abdominal pain in IBS?
TCA: low dose amitriptyline or desipramine - alters CNS processing of visceral afferent info - reduces stool liquidity and frequency
103
What is the role of antispasmodics in IBS?
- dicylcomine and hyoscyamine - work through anti-cholinergic activities dry mouth, - -higher doses can cause visual disturbances, urinary retention, constipation

Pharmacology (47 decks)

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