GI Pharmacology 2 Flashcards
drug classes for inflammatory bowel disease
*aminosalicylates
*immune modulators:
-glucocorticoids
-purine analogs
-tofacitinib
*monoclonal antibodies
aminosalicylates (5-ASA) - MOA
*local anti-inflammatory effects
*act topically (not systemically) in the intestine
aminosalicylates (5-ASA) - specific drugs
*sulfasalazine
*olsalazine
*pentasa
*asacol
*apriso
*lialda
aminosalicylates - uses
*Crohn’s disease
*ulcerative colitis
aminosalicylates - ADEs
ADEs of sulfasalazine:
-GI upset
-headaches
-arthralgias
-bone marrow suppression
-allergic reactions
*impairment of folate absorption (supplement recommended)
aminosalicylates - unique facts
*if using sulfasalazine, supplement folate
glucocorticoids for IBD - MOA
*suppress production of inflammatory mediators (cytokines & chemokines)
glucocorticoids - specific drugs
*prednisone
*methyl prednisolone
*budesonide
*hydrocortisone rectal products
glucocorticoids - GI uses
*Crohn’s disease
*ulcerative colitis
budesonide
*a glucocorticoid
*high first-pass hepatic metabolism (decreased systemic absorption)
*pH controlled delayed release
*watch out for drug interactions (CYP3A4)
*used to tx moderate to severe active disease in UC and Crohn’s
purine anti-metabolites - MOA
*alters purine nucleotide synthesis which affects DNA synthesis & function
*helps in Crohn’s and UC
azothioprine - drug class & MOA
*purine antimetabolite
*immunosuppressive (suppresses T-cells and has anti-inflammatory properties)
purine anti-metabolites - specific drugs
*azothioprine
*6-mercaptopurine
purine anti-metabolites (azothioprine) - GI uses
*Crohn’s disease
*ulcerative colitis
*autoimmune hepatitis
purine anti-metabolites - ADEs
*leukopenia
*pancreatitis
tofacitinib - drug class
JAK inhibitor
tofacitinib - MOA
*inhibits JAK-STAT pathway -> decreased synthesis of inflammatory cytokines
tofacitinib - uses
*treatment and maintenance of ulcerative colitis
*some rheumatology diseases
tofacitinib - ADEs
*increased risk of infections
*reactivation of infections (TB, shingles)
tofacitinib - unique facts
*some CYP3A4 drug interactions
anti-TNF monoclonal antibodies - specific drug
*infliximab
infliximab - target
TNF receptor (anti-TNF monoclonal antibody)
anti-TNF monoclonal antibodies (infliximab) - MOA
*blocks pro-inflammatory actions of TNF (tumor necrosis factor)
anti-TNF monoclonal antibodies (infliximab) - uses
*Crohn’s disease
*ulcerative colitis
*some rheum diseases
anti-TNF monoclonal antibodies (infliximab) - ADEs
*increased risk of acquiring or reactivating infections
*increased risk of skin cancers & lymphoma
anti-integrin monoclonal antibodies - specific drug
vedolizumab
vedolizumab - target
anti-integrin monoclonal antibody (inhibits mucosal WBC adhesion & migration)
anti-integrin monoclonal antibodies (vedolizumab) - MOA
*inhibits mucosal WBC adhesion & migration
anti-integrin monoclonal antibodies (vedolizumab) - uses
*2nd line drug for Crohn’s disease & ulcerative colitis
anti-integrin monoclonal antibodies (vedolizumab) - ADEs
*infection
*arthralgia
anti-integrin monoclonal antibodies (vedolizumab) - unique facts
less risk of PML than natalizumab
anti-IL12/23 monoclonal antibodies - specific drug
ustekinumab
ustekinumab - target
*anti IL12 and IL-23 antibody (inhibits cell-mediated inflammation by blocking cell signaling, cytokine production, and gene activation)
anti-IL12/23 monoclonal antibodies (ustekinumab) - MOA
inhibits cell-mediated inflammation by blocking cell signaling, cytokine production, and gene activation
anti-IL12/23 monoclonal antibodies (ustekinumab) - uses
*Crohn’s
*ulcerative colitis
anti-IL12/23 monoclonal antibodies (ustekinumab) - ADEs
*allergic reactions
*increased infections
*headache
bulk-forming laxatives - MOA
*indigestible, hydrophilic colloid
*distends colon & promotes peristalsis
bulk-forming laxatives - specific drugs
*psyllium
*methyl cellulose
*polycarbophil
bulk-forming laxatives - ADEs
*bloating
*flatus
bulk-forming laxatives - uses
constipation
osmotic laxatives - MOA
non-absorbable compounds that increase fecal fluid
osmotic laxatives - specific drugs
*polyethylene glycol (most commonly used)
*Mg salts
*Mg citrate & sulfate
*sorbitol
*lactulose
osmotic laxatives - uses
*constipation
*bowel prep
osmotic laxatives - ADEs
*diarrhea
*bloating
*cramps
stimulant laxatives - MOA
directly stimulates enteric nervous system
stimulant laxatives - specific drugs
*senna
*bisacodyl
stimulant laxatives - uses
*constipation
*bowel prep
stimulant laxatives - ADEs
*diarrhea
*bloating
*cramps
*nausea
lubiprostone - drug class
chloride secretion activator
lubiprostone - MOA
stimulates type-2 chloride channel in small intestine (increases Cl in intestine, leading to increased intestinal motility to tx constipation)
lubiprostone - uses
*chronic constipation
*IBS-C
lubiprostone - ADEs
nausea
linaclotide - drug class
chloride secretion activators
linaclotide - MOA
activates guanylate cyclase-C on luminal surface of intestine
linaclotide - uses
*chronic constipation
*IBS-C
linaclotide - ADEs
*diarrhea
*nausea
*dizziness
dicyclomine - drug class
anticholinergic (for IBS-D)
dicyclomine - MOA
*M1 cholinergic receptor antagonist (block M1 Ach receptors)
*decreases smooth muscle contractility & GI motility (to tx IBS-D)
dicyclomine - GI uses
*IBS-D
*GI antispasmodic
dicyclomine - ADEs
dry mouth, constipation, dry eyes, other anticholinergic side effects
alosetron - drug class
5-HT3 antagonist
alosetron - MOA
decreases afferent signaling from GI tract (by inhibiting GI 5-HT3 receptors)
alosetron - uses
*severe IBS-D in women who have not responded to other therapies
alosetron - ADEs
*severe constipation
*ischemic colitis
note - much worse ADEs than other 5-HT3 antagonists
peppermint oil for GI uses
*drug class = menthol
*MOA = kappa-opioid & 5-HT3 antagonist
*uses = IBS-D
*ADEs = GERD, nausea
loperamide - drug class
*opioid agonist (alternative = diphenoxylate)
note - the STANDARD anti-diarrheal drug
loperamide - MOA
*mu-opiod agonist in GI tract
note - the STANDARD anti-diarrheal drug
loperamide - uses
*IBS-D
*OTC treatment of diarrhea
note - the STANDARD anti-diarrheal drug
loperamide - ADEs
*constipation
*nausea
*somnolence
*abuse of high doses?
amitriptyline - drug class
tricyclic antidepressant
amitriptyline - MOA
*acts on 5-HT, NE, H1, & Ach in CNS & enteric nervous system (inhibiting 5-HT and NE reuptake like SNRIs)
*decreases visceral pain perception & GI motility
amitriptyline - GI uses
*IBS-D
*diabetic neuropathy
*pain disorders
amitriptyline - ADEs
lots (sedation, anticholinergic, sedation, weight gain, cardiac, serotonin-related)
SSRIs for GI uses
*sertraline, citalopram, escitalopram
*MOA = blocks 5-HT reuptake
*GI uses = IBS-D
*ADEs = sexual dysfunction, headache, weight gain
albendazole & mebendazole
*drug class: anti-helminth
*uses: tapeworm, cysticercosis, roundworm, pinworm, hookworm
*ADEs: abdominal pain, nausea, vomiting
thiabendazole
*drug class: anti-helminth
*uses: cutaneous larva migrans, strongyloides, trichinosis
*ADEs: nausea, vomiting, dizziness
ivermectin
*drug class: anti-helminth
*uses: strongyloides!!
*ADEs: dizziness, rash/pruritus, peripheral edema, tachycardia
nitazoxanide
*drug class: anti-protozoan
*uses: cryptosporidiosis, giardiasis
*ADEs: abdominal pain, nausea, headache
trimethoprim-sulfamethoxazole (TMP/SMX)
*drug class: antibiotic anti-protozoan
*MOA: INTERRUPT FOLIC ACID SYNTEHSIS
*uses: protozoa (Cystoisospora belli & Cyclospora); lots of bacterial infections
*ADEs: hypersensitivity, bone marrow suppression, hyperkalemia