Pharm GI from pharm perspective Flashcards
Role of SNS in GI motility and sphincter tone: Receptors & effects in Walls? Receptors & effects in Sphincters? Secretions? Prevailing control?
Walls: relaxes, alpha1 & 2
Sphincters: contracts, alpha1
Secretions: no
Prevailing control: no
(probably by inhibition of sympathetics)
Role of PNS in GI motility and sphincter tone: Receptors & effects in Walls? Receptors & effects in Sphincters? Secretions? Prevailing control?
Walls: contracts, M3
Sphincters: relaxes, M3
Secretions: increases, M3
Prevailing control: yes
effect of ganglionic blocade in PNS (cholinergic)?
reduced tone/motility. Constipation. Decreased secretions.
Role of serotonin:
Other name
Excess & insufficiency results?
Other name: 5-HT
Excess: motility up = D-IBS
Insufficiency: motility down = C-IBS
Tegaserod
Partial 5HT-4 agonist, selective serotonin agonist
tx of C-IBS
Withdrawn - heart attack, stroke
Treatment of IBS - full agonist/antagonist or partial?
partial, to prevent overtreatment to opposite problem.
etiology of IBS
breach of wall -> dendritic cell uptake of antigens -> presentation to T cells, alpha4beta7 integrin adhesion of T cells, CNS signaling -> symptoms
noninflammatory, no ulcers or damage!
5 classes of drugs for IBS
stool softeners antidiarrheal agents antiplasmotics TCAs SSRIs
Are probiotics useful in IBS?
Yes, but not high success rates
Acupuncture in IBS?
Herbal medicines in IBS?
Psychology in IBS?
Acupuncture in IBS? no
Herbal medicines in IBS? unproven, but promising
Psychology in IBS? not in adults, maybe in adolescents.
IBD:
2 examples
etiology
pivotal signaling agent
2 examples: chron’s and ulcerative colitis
etiology: dysbiosis -> inflammation
pivotal signaling agent: TNFalpha
4 TNFalpha inhibitors
infliximab
adalimumab
golimumab
certolizumab pegol
Treat IBD with TNFalpha inhibs?
Yes, but not front line. 3rd in line. (glucocorticoids, then immunomodulators, then TNFalpha inhibs)
3 opioid receptors and their effects
delta: delayed transit
kappa & mu: delayed transit & visceral antinicociception
Opioid effects on: gallbladder gastroduodenum small bowel colon anorectum
gallbladder: biliary pain, digestion delay
gastroduodenum: anorexia, nausea, emesis
small bowel: constipation, delayed digestion
colon: constipation, bloating, spasms, pain
anorectum: incomplete evacuation, strain
5 types of drug induced diarrhea
osmotic secretory disordered (cholinergic tone) inflammatory (flora disruption) C difficile (acid/base or epithelial homostasis) Fatty
metformin side effect
steatorrhea
octreaotride side effect
paradoxical steatorrhea (treats secretory d)
drugs to avoid in pill-induced esophagitis?
anticholinergics
role of P-gp/MDR1
dramatically increases drug bioavailability
role of cyp3A4 vs P-gp/MDR1?
P-gp/MDR1 may control CYP3A4
4 notorious drugs with gastric interactions
antacids, doxycycline, tetracycline, fluoroquinolones
cimetidine AE WRT PPIs
inhibits tons of cyps
PPIs metabolism
CYP2C19
all but dexlansoprazole inhibit 2C19
dexlansoprazole
doesn’t inhibit CYP2C19