Pharmacology Review Sheets: GI Drugs, p.

1
Stimulants of GI secretion
Drug

Class
Mechs of Action
Pharmacokinetics/Adverse Effects/Other Comments
Caffeine
Inhibits phosphodiesterase cAMP acid production

Found in coffee, cola, several OTC drugs (ask about this)

Nicotine
Ganglionic stimulation of vagus acid, pepsin
Alcohol
gastrin gastrin release; mucus production and dilutes mucus
(higher concs)
Corticosteroids Anti-inflammatory
Inhibits prostaglandin synthesis
Salicylates (aspirin) Anti-inflammatory
Direct keratolytic effect on epithelium
Old aspirin can clump together, the damage done
NSAIDs
Anti-inflammatory
Inhibits cyclooxygenase (COX) and thus prostaglandin synthesis
Treatment of peptic ulcers
Class

Drugs in that Class Mechs of Action

Pharmacokinetics/Adverse Effects/Other Comments
Tranquilizers
cephalic phase stimuli (used mostly for stress)
Sedatives
Anticholinergics Atropine
Muscarinic ACh blocker
class isnt that important b/c of side effects
Pirenzipine
Specific M1-Muscarinic ACh blocker
H-2 blockers
Cimetidine
H2-histamine receptor blocker
Ranitidine

This

Famotidine
Prostaglandin Misoprostol (PGE1 analog) Inhibits adenyl cyclase, cAMP
analogs
Proton pump
Omeprazole (Prilosec)
Highly specific and irreversible inhibitor of H+-K+-ATPase (
gastric acid secretion)
inhibitors
Specialized to work in acid environments ONLY (i.e. the stomach)
(PPIs)
Lansoprazole
(Same as omeprazole)
action: Longer-acting than omeprazole

Duration of
Adverse effects: Fewer than

omeprazole
Mucosal
protectants

Bismuth subsalicylate Coats lining of stomach

(Pepto-Bismol)
Suppresses H. pylori

Sucrulfate
Binds necrotic tissue (once theres damage) to prevent further erosion
Antacids
Sodium bicarbonate Neutralizes acid
Adverse
effects: If pH is raised to > 4,
(systemic)
- Pepsin activity
- Release of CO2 (perforation
risk)
- Metabolic alkalosis
Otherwise, nice b/c its really
really really cheap!
Antacids
Laxative: Mg oxide
Neutralizes acid

Adverse effects:
(nonsystemic)
Mg hydroxide
- Laxative, for the
entire drug class

Mg trisilicate
to slight absorption
Constip.: Al3+ salts

- Central depressants due

Neutralizes acid

Adverse

effects:
Al hydroxide gel
other antibiotics (bad for patient

- Binds tetracycline,
(being treated for H. pylori)
- Al3+ poisoning

Calcium salts Neutralizes acid

Adverse
effect: Possible urinary calculi (stones)
Note: Current treatment: COMBO therapy
Present CDC recommendation: Lansoprazole, Amoxicillin initially, then follow up with H2-blockers and
proton pump inhibitors for 6 months
FDA recommendation (12/95): Clarithromycin, omeprazole and ranitidine, bismuth citrate initially, then
follow up with H2-blockers and proton pump inhibitors for 6 months
NIH recommendation (2/94): Amoxicillin or tetracycline, metronidazole, bismuth subsalicylate initially,
then follow up with H2-blockers and proton pump inhibitors for 6 months
Pharmacology Review Sheets: GI Drugs, p.2
Antidiarrheal agents
Class

Drugs in that Class

Mechs of Action
Pharmacokinetics/Adverse Effects/Other Comments
Absorbents
Kaopectate: Kaolin (hydrated silicate clay)
available; inexpensive

Widely

combined with pectin (from fruit)

Adverse effects:
Relatively safe, but may interfere with absorption
Bismuth subsalicylate (Pepto-Bismol)
Binds intestinal toxins
Radioopaque: stop using before GI series
Coats internal lining of stomach
Adverse effect:
Innocuous tarry (black) discoloration of stools
Opiates
Diphenoxylate (Lomotil w/atropine)
Powerful, reliable inhibitor of GI motility
Contraindication: Children < 2 years of age
- GI tone, but peristalsis
Often used for travelers diarrhea
Loperamide (Immodium)
Inhibits peristaltic reflux
Structure:
Chemically similar to haloperidol and meripidine
PG-mediated contraction
Duration of action:
Longer than diphenoxylate
Side effect: Abdominal pain
Best anti-diarrheal agent currently
Codeine
GI tone
Adverse effect:
Addictive
Paregoric (camphorated opium tincture)
Peristalsis
Laxatives
Indications: Hemorrhoids, stool softeners (before an X-ray), elimination of poisons, combo with
antihelminthics (to finish the job), for a better stool sample. NOT to get a daily bowel movement!

Class

Drugs in that Class

Mechs of Action
Pharmacokinetics/Adverse Effects/Other Comments
Osmotics
Saline cathartics: Mg citrate, Mg oxide
Retain water in lumen
Hydrophilic colloids: Agar, methyl cellulose, bran,
prunes
Irritants
Esmodin
Adverse effects:
Eventual dependence for bowel movement
(Largest group;
Castor oil
usually too potent) Phenolphthalein (Ex-Lax)
Admin/duration of action: Oral

Bisacodyl:
(6 hrs), rectal (15-60 min)

Adverse effects: Lacks significant

side-effects
Lubricants

Can be used in any patient!!

Adverse effects:
- Dangerous foreign-body reaction in

Mineral oil

some people
- Inhibits absorption of essential fatsoluble vitamins (A, D, E, K)
- Leaks through the anal sphincter
(cant be used for a long time)
Docusate

Emetics

Stool softener

Duration of action: Slow

Adverse effects: Safe

Indications

Contraindications

Ridding the stomach of noxious substances

Lacerations, rupture of stomach/esophagus
First aid treatment of poisoning (Ipecac used here)
Fluid and electrolyte imbalance
Used w/certain anti-helminthic treatments
Interference w/successful outcomes of surgery
Ingestion of strong acids/alkalis, b/c youll do more damage as it comes back up.
Treat by neutralizing acid or base.
Ingestion of kerosene, petroleum distillates b/c it has an anaesthetic effect in the
lungs, and sensitizes cardiac activity to catecholamines.
Can result in foreign body reaction with lymph. Note that insecticides/pesticides
may be packaged w/kerosene and petroleum distillates
Strychinine (rat poison) poisoning b/c you may set off convulsions w/excitation of
the vomiting center. Put them in room w/low light levels, stimuli, then treat
Unconscious patient (b/c of possible lung damage)
Drug

Pharmacokinetics/Actions/Mechs of Action
Adverse
Effects
Syrup of ipecac Admin/Dose: Oral; 15 mL ( oz.)repeated at 20-30 mins if necessary; stop if it doesnt work
after 3 administrations
Dont give w/activated charcoal b/c its a good absorber
Mechanism of action: Acts by irritating stomach, possibly by releasing serotonin (5-HT)
Doesnt always work!!
Apomorphine Administration/Dose: Subcutaneous; 2 mg should induce vomiting in 5-10 minutes
No amnesia, drowsiness
Mechanism of action: Stimulates chemoreceptor trigger zone (CTZ)
Almost always works
Pharmacology Review Sheets: GI Drugs, p.3

Anti-Emetics
Class

Drugs
Pharmacokinetics/Actions/Mechs of Action
Uses
Adverse Effects
Anticholinergics Scopolamine
Admin: Subcutaneous patch, poss. given w/dextramphetamine or ephedrine
Motion sickness
Can, but shouldnt be used in pregnancy
Duration of action: SHORT

Anticholinergic side-effects
Antihistamines Buclizine
Teratogenic
potential: phocomelia (short/absent limbs)
Cyclizine
- Seen w/ buclizine,
cyclizine, meclazine, hydroxyzine
Meclizine
Drowsiness
Hydroxyzine
Anti-cholinergic sideeffects
Dimenhydrinate OTC
Can, but shouldnt be
used in pregnancy
Benadryl
OTC
Anti-dopaminergics Chlorpromazines
Action: Works at chemoreceptor trigger zone (CTZ)
Rx of vomiting and nausea
Parkinson-like side effects
Prochlorperazine
assoc. w/toxins, radiation
Drowsiness
Perphenazine
sickness, cytotoxic drugs Orthostatic
hypotension
Triethylperazine
Anti-cholinergic sideeffects (xerostomia, etc.)
Cholestatic jaundice

 Granulocytopenia, leukopenia,
thrombocytopenia RARE
Metoclopromide Admin: Give ALONE (NOT w/anticholinergics, antihistamines)

incidence of GI reflux Drug Interactions: ergotamine, sedatives, analgesics

Actions: Works at CTZ; stimulates GI LES pressure
(used in migraines)
Sedation, Parkinson-like
effects
5-HT3 antagonists
Granisetron
Used in cancer
Odansetron
chemotherapy
Miscellaneous Promethazine Mechanisms of action: Weakly anti-dopaminergic, weakly
Parkinson-like side effects from antidopaminergic properties
anti-histaminic, weakly anti-cholinergic. Can act at CTZ
Benzquinamide Admin: Administer slowly
Used for post-op nausea
Avoid in patients with hypertension, severe CV disease
Effects: Anticholinergic, antihistaminic, antidopaminergic, mild sedative
Dont use in pregnancy
Duration of action: Short (t = 40 min)
Diphenidol
Effects: Central anticholinergic; acts on vestibular apparatus and CTZ
Toxin-assoc. nausea/vomiting
Visual/auditory hallucinations, disorientation, confusion
Radiation sickness
Anticholinergic
side-effects
Postoperative
Pregnancy concerns
Following general anesthesia
Trimethobenzamide Effects: Not as effective as antidopaminergics
incidence of adverse reactions (drowsiness, Parkinson-like

syndrome, orthostatic
hypotension
Dont give to children w/acute
febrile illness, gastroenteritis,
encephalitis, electrolyte
imbalances (b/c of Reyes synd. risk)
Dronabinol
Schedule II Drug: Limit it to a necessary amount

Used to treat nausea

in pts.
(9-tetrahydro-

Absorption: Poor (10-20%)

in chemotherapy, or in

which
cannabinol) Metabolism: Extensive 1st pass metabolism
other antiemetics
have failed
Elimination: Biphasic elimination (fast for 4 hrs, slow for 25-36 hrs)
Nabilone
Schedule II Drug: Limit it to a necessary amount
Same as dronabinol
Admin/Action: Oral; peak in 2 hrs
Emetrol
Admin: Oral soln of dextrose, levulose, phosphoric acid, lemon/mint flavor
Dont use in people with fructose intolerance
Effect: Acts on wall of GI tract to smooth muscle contraction, for
relief of upset stomach
Bi subsalicylate Effect: Coats stomach to irritation
Has
salicylate; dont use in people w/aspirin intolerance
(Pepto-Bismol)