Agents For Diarrhea And Constipation - Dr. Segars

Question 1

4 agents for D

Answer 1

1. Prostaglandin Inhibitors
2. Opioid Agonists
3. Serotonin Antagonist
4. Chloride Channel Inhibitors

Question 2

5 drugs for Constipation

Answer 2

1. Laxatives and Cathartic agents
2. Peripheral Opioid antagonist
3. Guanylate Cyclase - C agonist
4. Selective Chloride (C2) Channel activators
5. Serotonin type-4 Partial Agonist

Question 3

PGR inhibitors

1

Answer 3

Bismuth

Question 4

Opioid agonist

3

Answer 4

1. Loperamide
2. Diphenoxylate
3. Eluxadoline

Question 5

1 Serotonin antagonist

Answer 5

Alosetron

Question 6

Cl channel inhibitor

1

Answer 6

Crofelemer

Question 7

Peripheral opioid antagonist

3

Answer 7

1. Methylnaltrexone
2. Naloxegol
3. Alvimopan

Question 8

Guanylate Cyclase-C agonist

1

Answer 8

1. Linaclotide

Question 9

Selective Cl (C2) channel activator 
1

Answer 9

Lubiprostone

Question 10

Serotonin Type-4 Partial Agonist

1

Answer 10

Tegaserod

Question 11

Loperamide
For what
How it works

Answer 11

Anti-diarrhea (DONT GIVE IF INFECTION RELATED**)

Chemically like opioid only not effects like it = can cause overdose causing cardiac toxicity, death

Question 12

Loperamide MOA + side effects

Answer 12

1. Slows down the transit time in peristalsis : action on longitudinal and circular muscles, increase fluid and electrolyte reabsorption, inhibit secretion
2. Anticholinergic

Question 13

Diphenoxylate works how and for what

Answer 13

1. = acts like an opioid and effects like it if taking a lot
   = small amount of atropine (strong anti-cholinergic) added to limit abuse, + prescription only
2. Antidiarrheal (not for infections)

Question 14

Diphenoxylate
MOA
Side effects

Answer 14

Inhibit GI motility and propulsion on SM in GI

Anticholinergic (from atropine)

Question 15

Eluxadoline MOA and for what

Answer 15

1. Agonist at mu + kappa GI opioid receptors (slowing), antagonist at delta opioid R (decrease secretions)**
2. IBS- D

Question 16

Eluxadoline
Side effects
Contraindications

Answer 16

1. Hepatic / pancreatic toxicity (increased enzymes)

2. Alcoholism, Hx pancreatitis, no gallbladder*,

Question 17

Alosetron MOA

Answer 17

Blocks GI 5HT receptors (blocking secretion and pain)

Question 18

Alosetron

used for what and when

Answer 18

IBS-D, when other drugs have not worked, and more severe
(Only tested in females)
** I need to go through training and monitor patient to give this**

Question 19

Alosetron side effects

Answer 19

Ischemic Colitis * (black box)

= you have to be trained and monitor patient

Question 20

Alosetron contraindications

Answer 20

Hx ischemic colitis, GI obstruction, perforation,…. Other GI or liver problems
(Bloody D, severe ABD pain, severe constipation =discontinue immediately)

Question 21

Crofelemer MOA

Answer 21

Drug comes from a tree, blocks Cl- secretion by ——I cAMP stimulated CFTR + CaCC in GI
= decrease secretions

Question 22

Crofelemer is used for what and side effects

Answer 22

1. HIV/ AIDS non-infectious D

2. infections, abd distention, elevated Bilirubin

Question 23

Peripheral Opioid Antagonist is for what and MOA

Answer 23

1. Constipation for chronic pain or cancer pt (they are on opioids)
   (Alvimopan = for accelerating time of recovery and preventing postoperative ileus)**
2. Peripherally acting on mu-opioid receptors and block them

Question 24

Peripheral Opioid Antagonist Side effects of alvimopan

Answer 24

= MI more often then not

Can only used in hospitals, and need training to give this, can only give 15 pills

Question 25

Linaclotide MOA and used for what

Answer 25

Guanylate cyclase C (GC-C) agonist , to increase CFTR secretions = IBS-C + CIC (Chronic idiopathic, unknown 1 BM/week, constipation)

Question 26

Lubiproston MOA and used for what

Answer 26

1. PGE-1 derivative : increasing Cl channel 2 secretion of Cl- 2. IBS-C + CIC, OIC (opioid-induced C) = use for opioid pts

Question 27

Tegaserod MOA and used for what

Answer 27

1. increase type 4 5HT receptor in GI (stimulate peristalsis and secretions) 2. IBS-C in women below 65yo)

Question 28

Tegaserod side effects

Answer 28

MI, TIA, CVA , renal disease, liver, disease, GI adhesions and problems (more likely in women over 65yo)

Question 29

Laxatives + Catherartics are used for what

Answer 29

** soften stool** that’s it

Question 30

5 Laxatives + Catherartics

Answer 30

1. Stimulants -> inflammation inducing and irritating 2. Salines -> salts function like osmotics 3. Stool softeners —> just soften 4. Bulk forming —> extent GI to increase P and more feeling to needing to go (need to drink more water) 5. Osmotics —> pull fluid out

Question 31

Laxatives + Catherartics do what to soften and when to NEVER use

Answer 31

Increase inflammation and irritation on GI (Not used for long) = never on ileus

Question 32

Stimulants

Answer 32

1. Bisacodyl 2. Glycerin 3. Senna 4. Na Picosulfate

Question 33

Saline’s

Answer 33

1. Mg salt 2. K salt 3. Na salt

Question 34

Stool softeners

Answer 34

Docusate | Mineral oil

Question 35

Osmotics

Answer 35

``` Lactulose Lactitol Polyethylene glycol Sorbitol (Glycerin) ```

Question 36

Bulk flow

Answer 36

``` Dietary (fibers, brans, fruit, grains) Psyllium Methylcellullose Carboxymethylcellulose Ca Polycarbophil ```

Question 37

Bulk flow works how fast and contraindications

Answer 37

2-4 days | Obstruction and bloating

Question 38

Stool softener has what in it, how fast and contraindications

Answer 38

Surfactants 1-3 days None

Question 39

Stimulants needs to do what before, MOA, contraindications, how long

Answer 39

Pre-colonoscopy prep for Na Picosulfate = increase peristalsis an irritate cells, , increase PGEs = abd cramping, senna (yellow pee), obstruction, ileus = 12hr-36hrs

Question 40

Saline’s how long, needs what, contraindication,

Answer 40

More given the faster = pre-colonoscopy prep = HTN, CHF, Renal disease (electrolyte disturbance), Diuretics

Question 41

Osmotic time, used for what, contraindications, needs what

Answer 41

1-2 days = Hyperammonemia (severe liver disease) + Constipation = same as saline (renal, heart problem patients) = Pre-colonoscopy for Polyethylene glycol (PEG-3350)