Laxatives, Antidiarrheals, Antiemetics, Prokinetics Flashcards
1
Q
Bulk-forming laxatives
A
- Psyllium, Methylcellulose. wheat dextrin, polycarbophil
- Hydrophilic colloids which absorb water and form emollient gel that distends colon + promotes peristalsis
- Ind: Chronic constipation; pregnancy const
- AE: Bloating/flatulence
- Contra: OIC; HF; PD; intestinal ulceration
2
Q
Docusate Sodium
A
- Stool Softener detergent
- Indications: Hard stool, chronic constipation, Fe supplementation
- AE: Hypomagnesemia
- Contra: >7 days; pain, N/V present; concomitant use w/ mineral oil
3
Q
Mineral Oil
A
- Stool softenre; coats bowel w/ waterproof film
- Ind: Acute or Chronic constipation
- AE: Aspiration Pneumonial DEC nAKED absorption; anal leakage
- Contra: Debillitated patients; docusate use; <6YO; *Pregnancy
4
Q
Salt-laxatives
A
- MagCit, MagOH, MagSO4, NaPO4
- Osmotic retention of water in intestinal lumen
- Ind: Enema for constipation; Bowel prep;
- Contra: Electrolye abnormalites; Rena;/cardiac patients; Nephrotoxicity in NaPO4
5
Q
Salt-free osmotic laxatives
A
- Glycolytely; PEGs - Mirolax
- Indications: Bowel Prep; Miralax for occasional constipation
- AE: CV/Renal Disease; Diuretics; NSAIDS
6
Q
Nondigestable sugars/alcohols
A
- Lactulose
- INC pH -> inhibition of NH3 diffusion -> osmotic retention of fluid in lumen
- Ind: Constipation
- AE: Electrolyte imbalance; dehydration; cramping; distention; diarrhea
7
Q
Bisacodyl
A
- Irritates smooth muscle of intestine
- Ind: Bowel cleaning; constipation
- AE: cramping, electrolyte imbalance
8
Q
Arthraquinone (derivatives)
A
- Senna, Aloe, Cascara
- Stimulate peristasis via nerve plexus
- Ind: Occasional constipation; off-label to empty the bowel
- AE: cramping; electrolye imbalance
9
Q
Linaclotide/Plecanatide
A
- Chloride secretion activators; bind GCC -> INC cGMP -> INC Cl/HCO3 secretion
- Ind: CIC; IBS-C
- AE: Abdominal distention, diarrhea, flatulence, headache; dehydration
- Contra: Mech obstruction; <6YO
10
Q
Lubiprostone
A
- activating chloride channels on the apical membrane of the gastrointestinal tract to increase intestinal fluid secretion and improve fecal transit.
- Ind: CIC, OIC, IBS-C
- AE: Diarrhea, headache, nausea
- Contra: Mechanical Obstruction
11
Q
Diphenoxylate
A
- Opioid Agonist
- Ind: Acute/chronic diarrhea
- AE: CNS effects like sedation; Opioid dependence
- synergistic w/ atroine
12
Q
Difenoxin
A
- Active metabolite of Diphenoxylate
- More powerful; habit-forming
- Used w/ Atropine to prevent misuse
13
Q
Loperamide
A
- Mu Opioid agonist in Myenteric plexus leading to relaxation f smooth muscle w/ NO CNS activity (No BBB)
- Ind: acute/chronic diarrhea; Traveler’s diarrhea; Cancer diarrhea
- AE: Constipation/ileus; Torsades
14
Q
Eluxadoline
A
- Mu/Kappa agonist + delta antagonist
- Ind: IBS-D
- AE: Sphincter of Oddi spasm -> pain, pancreatitis, INC enzymes
- Contra: Biliary obstruction, Sphincter of Oddi dysfunction, pancreatic Dx. Obstruction, hepatic impairment, alcoholism
15
Q
Bismuth Subsalicylate
A
- Antimicrobial + stimulates fluid/electrolyte absorption
- Ind: Traveler’s diarrhea + dyspepsia
- AE: Large dose Neurotoxic; CNS effects; Discoloration of tonuge or fecal matter; Hearing loss + Tinnitus
- Contra: ASllergy, Ulcer, Coagulopathy, Salicylate use, Reye’s Syndrome (viral illness)
16
Q
Octreotide
A
- Analog of endogenous somatostatin -> reduce VIP, serotonin, gastrin, secretin,+ PPT -< INC transit + absoprtion\
- Ind: Severe/watery Diarrhea by carcinoid syndrome; Diarrhea of chemo, HVG, short-gut, and Dumping syndrome
- AE: GI distress, Headaches, gallstones
17
Q
Bile Resins
A
- Binds excess bile acids + bacterial toxins
- Ind: Cholesterolemia, Bile salt-induced diarrhea
- AE: Drug absoprtion
18
Q
Sulfasalazine
A
- Broken down by gut bacteria to 5-ASA, an antiinflammatory + Anti-secretorya gent; DEC PGE, IL-1, TNF-a, + lipoxygenase
- Ind: Ulcerative Colitis S/S
- AE: Folate deficiency; Rash, nausea, anorexia, headache
19
Q
Scopolamine
A
- Competitive M1 antagonist that interferes vestibular neurons
- Ind: Motion sickness; post-op Nausea
- AE: CNS (psychosis exacerbation, etc); Somnolence; Xerostomia
20
Q
Meclizine (Dromamine)
A
- H1 antihistamine in vestibular apparatus
- Ind: N/V; Pregnancy N/V; Motion Sickness
- AE: Drowsiness, dry mouth, dry/blurry vision, tachycardia
21
Q
Dimenhydrinate
A
- 1st gen H1 antagonist
- Ind: Chemotherapy-induced N/V
- AE: Drowsiness, dry mouth, blurry vision, tachycardia
22
Q
Prochlorperazine
A
- Blocks postsynaptic D1/2 + a1 receptors on the vomiting centers
- Indications: Severe N/V; CINV;
- AE: Extrapyramidal effects, Drowsiness, dry mouth, blurred vision, orthostatic hypotension
- Contra: Parkinsons; Dementia; Psychosis
23
Q
Promethazine
A
- Inhibits postsynaptic D1/2 receptors + alpha1 receptors in vomiting centers
- Ind: Post-Op N/V; CINV
- AE: Extrapyramidal effects; drowsiness, dry mouth, blurry vision; orthostatic hypotension
- Contra: Parkinson’s; Children
24
Q
Droperidol
A
- Dopamine receptor antagonist
- Ind: Only PONV
- AE: extrapyramidal effects; QT Prolongation; Torsades
- Contra: Parkinsons; QT prolonged
25
Metoclopramide
- D2 antagonist + ACh enhancer
- Ind: CINV; Diabetic Gastroparesis; GERD; Dyspepsia;
- AE: Tardive Dyskinesia; extrapyramidal; fatigue; somnolesence; headache;
26
Domperidone
- D2 receptor antagonist Only
| - Ind: Prevention induced GI symptoms w/ dopaminergic agonists used in PD; Promotes Motility
27
Ondansetron
- 5-HT3 antagonist
- Ind: CINV; PONV; Acute raiation-induced N/V
- AE: headache, constipation, fatigue
- Contra: Use of Apomorphine
28
Dolasetron
- 5-HT3 Antagonist
- Ind: CINV
- AE: QT Prolongation; Headache, constipation, fatigue
29
Granisetron
- 5HT-3 antagonist
- Ind: CINV
- AE: Constipation, headache, fatigue, ileus, injection sire reaction
30
Palonosetron
- 2nd gen 5HT-3 antagonist
- Longer T1/2; increased efficacy
- Ind: CINV; PONV
- AE: Constipation; headache fatigue ileus, injection site reaction
31
Dronabinol
- CB1 antagonist
- Ind: CINV
- AE: Tachycardia; Orthostatic hypotension; increased appetite; somnolence; euphoria
32
Nabilone
- CB1 receptor antagonist
- Ind: CINV
- AE: Tachycardia, erthostatic hypotensionl inc appetite somnolencel euphoria
33
Benzodiazepine Antiemetics
- Alprazolam; Lorazepam
- Anti GABA-A agonist
- Ind: anxiety; anticipatory N/V
- AE: Dizziness, sedation, appetite changes; memory impairment
34
Aprepitant
- Inhibits Substance P/neurokinin-1 receptor -> INC 5-HT activity
- Ind: CINV; PONV
- AE: dizziness; diarrhea; fatiguel constipation; hiccups
- Contra: CYP3A4 inhibitor -> DEC dexamethosone
35
Fosaprepitant
I.V prodrug of Aprepitant
36
Netupitant
- Substance P/Neurokinin-1 inhibitor -> INC 5-HT activity
- Ind: CINV; PONV
- AE: Dizziness; fatiguel constipationl hiccups
- Contra: CYP3A4 inhibitor -> Reduce Dexamethasone
37
Rolapitant
- Inhibits Substance P/Neurokinin-1 receptor
- CINV/PONV
- NO Dose adjustment for dexamethasone
38
Bethanechol Ind:
- Post-op distention
| - Gastric atony follwing vagotomy
39
Neostigmine indications
- Colonic pseudo-obstruction
40
Motilin + Macrolide
- MAcrolides (erythromyocin, etc) mimic motilin -> Gastric emptying
- Ind: Preo-op for gastroparesis
41
Prucalopride
- 5-HT4 agonist -> peristalsis, secretions, +_ motility
- Ind: CIC; OIC
- AE: distentionl diarrhea; dizziness; headache
42
Tagaserod
- 5-HT4 agonist -> peristalsis, secretions, +_ motility
- Ind: IBS-C in women under 65YO
- AE: distentionl diarrhea; dizziness; headache
43
Dexcamethasone
- Corticosteroid w/ antiemetic properties
- enhances 5-HT3 antagonists;
- Ind: CINV
