Seagers Diarrhea/Constipation Flashcards

1
Q

Loperamide

A

Chemically-related to opioids but does not exhibit analgesic/opiate-like effects, or appear to produce physical dependence

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2
Q

Loperamide: MOA

A

MOA of Loperamide: Interferes with peristalsis (slows transit time)

Direct action on circular and longitudinal muscles of intestinal wall, slowing motility

Also may directly inhibit fluid and electrolyte secretion and/or increase water absorption

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3
Q

Loperamide: Side effects

A

dizziness, drowsiness & urinary retention (anticholinergic)

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4
Q

Diphenoxylate (Lomotil): what it is

A

synthetic opiate agonist (chemically-similar to meperidine) [C-V]

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5
Q

Diphenoxylate (Lomotil): how it works

A

Opioid-effects only seen at very high doses (constipation)

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6
Q

Diphenoxylate (Lomotil): why it was starred by seagers

A

Small quantity of atropine added to discourage deliberate abuse/over-dosage

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7
Q

MOA of Diphenoxylate:

A

Believed to exert effect locally & centrally on GI smooth muscle cells; inhibits GI motility and slows excess GI propulsion

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8
Q

Eluxadoline (Viberzi) (C-IV): MOA of Eluxadoline

A

Agonist at opioid mu & kappa receptors in GI
tract (slows peristalsis/delays digestion)

Antagonist at delta opioid receptors in GI
stomach, pancreas & biliary tract secretions decreased

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9
Q

Eluxadoline (Viberzi) (C-IV): Indication:

A

Indication:

Irritable Bowel Syndrome, Diarrhea- predominant subtype (IBS-D)

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10
Q

Eluxadoline (Viberzi) (C-IV): Side effects:

A

Hepatic/Pancreatic toxicity (increased enzymes)

Pancreatitis hi-risk in pts. w/o a gallbladder – Deaths have occurred

CNS-related (dizziness/fatigue/sedation/euphoria/impaired cognition)

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11
Q

Eluxadoline (Viberzi) (C-IV): Contraindications

A

biliary duct obstruction
sphincter of Oddi dysfunction
alcoholism history of pancreatitis
severe hepatic impairment

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12
Q

Alosetron: MOA

A

Selectively blocks GI-based 5HT3 recepto

Antagonism in GI modulate regulation of visceral pain, colonic transit & GI secretions

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13
Q

Alosetron: indication

A

Chronic, severe IBS-D not responsive to other conventional therapies (women)

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14
Q

Alosetron: SE

A

Constipation+Ischemic Colitis

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15
Q

Ischemic Colitis

A

side effect of alosetron

No refills without a follow-up exam by the prescriber

Physicians must enroll in prescribing program

Patients and physicians must sign a risk-benefit statement and agree to adhere to therapy plans

Additional self-training and testing by physicians to learn to appropriately diagnose IBS required

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16
Q

Cl- Channel Inhibitors-Diarrhea

A

Crofelemer (Mytesi), derived from dark red sap of Croton lechleri tree (botanical pharmaceutical).

17
Q

Crofelemer (Mytesi): MOA

A

Cl- Channel Inhibitors-Diarrhea

Inhibits chloride ion secretion by blocking cAMP-stimulated CFTR (cystic fibrosis transmembrane regulator) & calcium-activated (CaCC) chloride channels

channels regulate fluid secretion by intestinal epithelial cells

18
Q

Crofelemer (Mytesi): indication

A

Non-infectious diarrhea in HIV/AIDS

pts. on anti-retroviral therapy

19
Q

Crofelemer (Mytesi): SEs

A

GI-related
Abdominal distention, elevated AST/ALT/Bilirubin
Upper-Respiratory Infections

20
Q

Antimuscarinics: abdominal pain drugs

A

Hyoscyamine Dicyclomine Clidinium/Chlordiazepoxide

21
Q

Antimuscarinics: MOA

A

Competitively-inhibit autonomic, post-ganglionic cholinergic receptors (multiple sites)

22
Q

Antimuscarinics (for Abd. Pain/Spasms): Results, indications

A

decreased GI motility and spasms (pain), Abdominal pain/spasms, esp. when associated with IBS

23
Q

Laxative & Cathartic Agents

A

Opioid Antagonists: Methylnaltrexone, Naloxegol

Guanylate Cyclase-C Agonists: Linaclotide

Selective Chloride (C2) Channel Activators: Lubiprostone

24
Q

Constipation Type Drug

A

Linaclotide

25
Q

Linaclotide: MOA

A

Binds to GC-C on luminal surface of intestinal epithelium.

Increases intracellular/extracellular concentrations of cGMP

Stimulates secretion of chloride/bicarbonate into intestinal lumen via activation of cystic fibrosis transmembrane conductance regulator (CFTR) ion channel

Results in increased intestinal fluid and accelerated transit

26
Q

Linaclotide: indications

A
Irritable Bowel Syndrome-Constipation
predominant subtype (IBS-C)

Chronic Idiopathic Constipation (CIC)

27
Q

Linaclotide: SE

A

GI-Related: GERD/Dyspepsia/N/V

28
Q

Lubiprostone MOA:

A

a bicyclic fatty acid, prostaglandin E1 (PGE-1) derivative

increases intestinal fluid secretion by activating GI specific chloride channels (ClC-2) in luminal cells of intestinal epithelium

29
Q

Lubiprostone: indications

A
Irritable Bowel Syndrome-Constipation
predominant subtype (IBS-C) (women)

Chronic Idiopathic Constipation (CIC)

Opioid-Induced Constipation (OIC) (non-cancer adults)

30
Q

Lubiprostone: SE

A

Nausea, dyspepsia, dizziness

31
Q

Methylnaltrexone & Naloxegol: MOA

A

peripheral mu-opioid receptor antagonists

No common, significant CNS penetrations/actions or induction of withdrawal/pain symptoms

32
Q

Methylnaltrexone & Naloxegol: indications

A

Opioid-Induced Constipation (OIC)

33
Q

Stimulants

A
Bisacodyl 
Castor Oil 
Glycerin 
Senna 
Na+ Picosulfate
34
Q

Osmotics

A

Lactulose
Mag citrate
Polyethylene glycol (PEG)
Sorbitol (Glycerin)

35
Q

Salines

A

Mag. hydroxide

Na+ phosphate

36
Q

Bulk Forming

A
Dietary (Fiber/Bran)
Fruits/Grains/Cereal)
Psyllium
Methylcellulose/
Carboxymethylcellulose
Calcium polycarbophil
37
Q

Stool Softeners

A

Docusate, Mineral Oil

38
Q

Bulk-forming/Hydrophilic Colloidal Agents

A

Dietary Fiber/Bran, Psyllium, Metamucil, Genfiber, others…