Bulk forming laxatives:
Psyllium
Methylcellulose
Polycorbophil
Indigestible colloids absorb water to form a gel in the GI tract, to distend it and induce peristalsis
Use in constipation refractory to dietary changes
Can lead to bloating and farts
Stool softeners:
Docusate
Glycerin suppository
Mineral oil
Absorbs water and lipids into stool, lubricate and soften
Docusate in-patient; mineral oil in kids and debilitated pts
Long term ADEK def.
Osmotic laxatives: Magnesium hydroxide Magnesium citrate Sorbitol Lactulose Sodium phosphate Polyethylene glycol
Soluble, but non-absorbable, alter water in colon, increases fecal fluid
Uses: acute constipation, prevent chronic constipation
MgCitrate and NaPhosphate are purgatives
Polyethylene glycol for colonoscopy prep
AE: No Mg(OH)2 in renal disease, sorbitol and lactulose digested by bacteria to bloating and farts, maintain adequate water intake
Risk of electrolyte changes with NaPhos
NaPhos is out in renal and heart dz
Stimulant laxatives: Bisacodyl Aloe vera Senna Cascara sagrada
Stimulates ENS and colonic secretions In neuro pts, or bed bound Biscodyl for normal constipation Biscodyl with polyethylene glycol in 'scope prep May cause cramping
H2-R antagonists: Cimetidine Ranitidine Famotidine Nizatidine
Competitive/ selective inhibitors of parietal cell H2-R
suppress basal and meal-stim. acid in a linear dose-dep.
Most pronounced on nocturnal acid
Cimetidine is weakest, famotidine strongest
2nd line for GERD/PUD
As effective for NSAID-induced PUD
Non-ulcer dyspepsia, prophylaxis
AE: diarrhea, HA, fatigue, myalgia, constipation
NO in pregnancy, caution in nursing
Cimetidine is a CYP inhibitor BEWARE
PPIs:
-prazole
Irreversible inhibitor of H/K ATPase on lumenal surface of parietal cells, prodrug needs protonation in stomach
Marked suppression of basal and meal-acid
1hr pre-meal
1st line in GERD/PUD, part of HpI triple therapy
AE: diarrhea, HA, abdpain, enteric infection, dementia
Antacids:
CaCO3
Mg(OH)2 + Al(OH)3, Mg(OH)2 + Al(OH)3
Weak bases react in stomach to form salts and water, reduce gastric acid and pepsin activity
Intermittent HB
AE: constipation, cramps, diarrhea
Sucralfate
Binds and coats necrotic ulcers (needs acid), may stimulate PG synthesis
Prevent and heal duodenal ulcers
AE: Constipation, do not give with acid-reducing agents
Bismuth subsalicylate
Bismuth subcitrate potassium
Bi binds and coats necrotic tissue, barrier and anti-toxin in HpI
Salicylate inhibits PG and chloride in the intestines, reduce stool frequency and liquidity
Use: HpI with normal, etc.
AE: harmless stool darkening, no in renal dz
Misoprostol
PGE1 analog
Enhances mucosal protection, reduces cAMP to down H+
For NSAID-ulcers
AE: diarrhea, no in women of childbearing potential
Metoclopramine
D2 antagonist hastens esophageal clearance, raises LES tone, speeds gastic emptying, antiemetic
Post surgery or DM gastric motor failure relief
CNS: EPS, anx, dep, drowsiness
Lubiprostone
FA from PGE1, activates T2Cl-channel produces chloride rich secretion to soften stools, increase motility
Use: chronic idiopathic const. IBS-C, Opioids
AE: diarrhea, nausea, HA, pain, no in kids
Linaclotide
Peptide agonist of guanylate cyclase 2C to activate CFTR, moves bowels reduces pain
USE: CIC, IBS
AE: diarrhea, no in kids
mu-opioid-R agonists: diphenoxylate, loperamide
increase fecal transit time, no analgesia
USE: non-spec. diarrhea
Loperamide can cause mild cramping
Diphenoxylate can cause CNS tox, dependence, contains atropine
Eluxadoline
agonist at mu and kappa, antagonist at delta
Decrease abd pain and reduce diarrhea
USE in IBS-D
AE: constipation, nausea, Oddi spasm to pancreatitis
NO in cholecystectomy, gallstones, pancreatitis, liver dz
Octreotide
SST analog, inhibits secretion of hormones and NTs (gastrin, secretin, VIP, H), reduces intestinal secretion, slows GI motility and inhibits GB
Tx: Carcinoid or VIPoma, diarrhea in vagotomy, dumping syndrome and short bowel syndrome
AE: nausea, pain, farts, fat and ADEK loss, gallstones and hypothyroidism
Amitriptyline and Desipramine
TCAs with SNRI and antiCh, alter central processing, reduce stool frequency and liquidity
AE: antiCh
Alosteron
Antagonist to 5-HT3-R
Women with IBS-D who are refractory
AE: common: constipation
AE: rare: ischemic colitis
Mesalamine, sulfasalazine, olsalazine, balsalazine
Inhibit inflammatory mediators from COX and lipoxygenase
Works topically
1st line for UC
AE: Nausea, HA, arthralgias, myalgias, BM supp, malaise
GCs
Anti-inflammatory effect, prednisone/prednisolone is PO, hydrocortisone is PR
USE: IBD, PR is preferred, budesonide for CD
SYYMPTOM treatment
Azathioprine, 6-MP, MTX
Inhibits purine biosynth, immunosuppression of lymphoid cell prolif.
AZT/6-MT induces and maintains remission of UC/CD
MTX- only CD
AE: n/v BM supp, mucositis, hepatotox (AZT, 6MP)
Infliximab, adalimumab, golimumab, certrolizumab
anti-TNF, prevent inflamm cytokine binding
Suppress TH1, suppresses cytokine release
CD: Infliximab, adalimumab, certrolizumab
UC: Infliximab, adalimumab, golimumab
AE: Opportunists, reactions
Natalizumab, vedolizumab
N: anti-alpha4 integrin; V: anti alpha4beta7 integrin
Prevents leukocyte adhesion
V>N CD or UC
AE: N: PML from polyoma v.
Antiemetics:
Ondasetron, Granisetron, Dolasetron, Palonosetron
Antagonist at 5-HT3-R
Block on vagus afferents, and postrema, antiemesis from vagal or Chtx (not motion sickeness)
USE: acute Chtx emesis, post-op emesis, give w/ GC and NK1-R antagonist
AE: HA, dizzy, constipation
