 Drugs used to treat GERD –PPIs & H2 rec antagonists

 PUD – erosion of lower stomach/duodenum from H. pylori

 Risk factors for PUD – H. pylori, NSAIDs, acid, pepsin, smoking
 These protect against PUD – mucus, bicarbonate, blood flow, prostaglandins
 Antibiotics used to treat PUD – amoxicillin, Biaxin, tetracycline, Flagyl
 Other drugs working to treat or defend against PUD – bismuth salicylate (pepto), misoprostol, sucralfate, PPIs, H2 rec antagonists,
antacids, muscarinic antag (pirenzepine)
 Tx of H. pylori – usually 2-3 antibiotics w/ PPI or H2 rec antag for 10-14 days

Cimetidine
(Tagamet)

Classification H2 receptor antagonist. Others: Ranitidine (Zantac), famotidine (Pepcid), nizatidine

MOA (brief) Competitive blocker of histamine H2 rec sites of parietal cells. Diminish effects of gastrin & Ach. Inhibit gastric acid
secretion.
Dosage/Route PO, IV; PO-onset 30 min, peak 1 hr, duration 4-5 hr
Adverse Effects Diarrhea, constipation, gynecomastia, impotence, dec libido, dec sperm count. CNS – hepatic/renal problems,
confusion, hallucinations, lethargy
Drug Interactions Meperidine, Phenytoin (dilantin), diazepam, theophylline, warfarin, ETOH, digoxin, ketoconazole, antacids
When is it used? PUD, GERD,
Metabolic Effects Hepatic 1st pass effect; metabolized by cytochrome p450 – will inc the ½ life of theophylline
Nursing Best if taken with food to slow absorption & prolong effects. H2 rec antag can be taken to prevent GERD from
considerations certain irritating foods.
Omeprazole
(Prilosec)
Therapeutic Proton pump inhibitor. Others: Esomeprazole (Nexium), Lansoprazole (Prevacid), Pantoprazole, Rabeprazole,
Classification Dexlansoprozole,
MOA Block final step of acid production; nonreversible inhibition of H+/K+ ATPase
Adverse Effects Diarrhea, abdominal pain, n/v, constipation, headache, dizziness, back pain, muscle pain; rare: anemia,
thrombocytopenia, eosinopenia, leukocytosis
Drug Interactions Drugs dependent on gastric pH (iron salts, ampicillin); diazepam, phenytoin, warfarin
When is it used? Hypersecretory disorders, duodenal ulcer, erosive esophagitis (GERD)
Metabolic Effects Rapid absorption in intestine
Nursing Take 30 minutes before morning meal. Taken as maintenance (every day)
considerations

Misoprostol

Therapeutic Antisecretory Drug that enhances mucosal defenses. (analog of prostaglandin E1)
Classification
MOA (brief) Serves as a replacement for endogenous prostaglandins. (NSAIDs cause ulcers by inhibiting pg biosynthesis).
Promotes secretion of bicarbonate and mucus, and maintains submucosal blood flow.
Adverse Effects Diarrhea *, constipation, abdominal pain, n/v, dyspepsia, flatulence, HA. Toxicity: sedation, tremor, convulsions,
dyspnea, fever, palpitations, hypotension, bradycardia
Contraindications Pregnancy category X
Drug Interactions antacids
When is it used? Prevention of gastric ulcers caused by long-term therapy with NSAIDs
Nursing Obtain serum pregnancy test first. Begin on 2nd or 3rd day of period. Give verbal & written instructions of dangers.
considerations Comply with birth control measures.

 Pirenzepine – an anticholinergic drug used to treat PUD. Produces “selective blockade” of muscarinic receptors that regulate gastric acid
secretion. Inhibits gastric acid secretion without pronounced anticholinergic side effects. Most common SE: dry mouth.
Sucralfate

Classification Antiulcer Medication – “Pepto Bismol on steroids”

MOA (brief) Paste-like material adheres to ulcer crater creating a barrier to back-diffusion of pepsin and bile salts.
Dosage/Route PO – suspension; lasts 6 hours; 4-8 week therapy time
Adverse Effects Constipation, (no severe AE)
Contraindications Chronic renal failure, dialysis pts
Drug Interactions By raising gastric pH above 4, antacids may interfere with sucralfate’s effects. Administer these at least 30 min
apart. Impedes absorption of phenytoin, theophylline, digoxin, warfarin, fluoroquinolones. Cimetidine, Ranitidine,
tetracycline.
When is it used? To treat existing duodenal & gastric ulcers.
Nursing Administer 1 hr before meals and at bedtime. Increase fluids and fiber.
considerations

Antacids MOA Adverse Effects Other

Neutralize stomach acid Caution in pts w/ HTN (antacids
w/ high Na+ content)
Aluminum Hydroxide Has low ANC (anti-neutralizing Constipation; dec PO4 Has high Na+ content
capacity absorption.

Magnesium Hydroxide Has high ANC. Rapid acting w/ Diarrhea Do not give to pts w/ renal
Liquid-milk of magnesia long DOA. impairment.

Calcium Carbonate High ANC. Rapid acting. Long Rebound acid, belching, flatus,
DOA constipation

Sodium Bicarbonate Elevates urinary pH & excretes Belching, flatus. Not good for tx Do not give to pts w/ HTN.
acidic drugs. Rapid acting. Short of ulcers, but good for acidosis.
DOA.
  Drugs that cause constipation: analgesics, antacids (Al), anticholinergics*, antidepressants, antidiarrheals, antihistamines*,
antihypertensives (some), antiparkinsonian drugs, barium sulfate, diuretics, iron supplements*, muscle relaxants (some)

Anti-constipation drugs MOA Adverse Effects & uses Dose/Response Time

Bulk Forming Laxatives Softens stool by pulling more H20 Take w/ full glass of water. Soft,
Methylcellulose, psyllium, into sm intest & colon, inc fecal formed stool 1-3 days after tx.
Polycarbophil mass & promotes peristalsis.
Fiber!

Surfactant Laxatives Water penetrates sm intest & Can take for a while. Produces
Docusate sodium, calcium colon. soft stool 24-72h after tx. Take
with full glass of water.

Stimulant Laxatives Stimulates peristalsis; softens High abuse factor. 2 uses: opioid PO – semifluid stool in 6-12h.
Bisacodyl, senna, stool secreting h20 & electrolytes induced constip & tx of slow supp – stool in 15-60 min. not for
castor oil (quick – 2-6h) into intestines intest transit. long-term use.

Osmotic Laxatives Osmosis in sm intest & colon; Uses: surgery, purge ingested Mg & Na - Low dose – 6-12 h;
Mg, sodium phosphate softening feces & promoting fecal poison, evacuate dead parasites Mg & Na -high dose – 2-6 h.
Polyethylene glycol (miralax) swelling & peristalsis PG –prior to colonoscopy PG-4L, 250ml q 10 min for 2-3 hr

Misc. Laxatives
Mineral oil Lubricates & dec h20 absorb (col) Lipid pneumonia (orally) enema for impaction (5-30 min)

Glycerin suppositories Lubric & causes reflex rectal Used to re-establish normal Evacuation in 30 min.
contraction (colon) bowel fcn after termination of lax
abuse.

Lactulose Similar to osmotic laxatives L: Used in liver L: Only use if not responding to
PEG soln dz(ETOH/cirrhosis) to lower bulk forming lax. Soft stool 1-3
blood ammonia; SE: cramps, days after tx.
flatus
 Lubiprostone Opens chloride channels in Not absorbed – no SE Used for idiopathic constipation
intestinal epithelium and IBS in women over 18.
Color key from previous table: Red – immediate response (5-30 min); Green – quick response (2-6hr); Orange – semi-quick response (6-12 hr);
Pink – delayed response (1-3 days)

Drugs that cause diarrhea: Mg, antihypertensives, antimicrobials*, antineoplastics, bile acids, cardiac glycoside, cholinergics, cholinesterase
inhibitors*, osmotic & stimulant laxatives*, quinidine

*Opioids are most effective anti-diarrheal agents.

Diphenoxylate - Opioid Antidiarrheal – schedule C5 controlled substance. Atropine is given to prevent abuse. Given after loose watery stool for
acute diarrhea. AE – CNS depression, euphoria, confusion, sedation, restlessness. Contraindications – acute bowel infections, glaucoma, BPH. DI:
alcohol, barbs, tranquilizers, MAOIs.

Loperamide (Imodium) – Opioid antagonist – OTC -

Antiemetics MOA

5HT3 rec antagonists Chemo, radi, post-op, pregnancy

Ondansetron, etc.

Substance P/neurokinin1 antag Block rec in the brain Prevents acute & delayed emesis Chemo. With or without food.
aprepitant, fosaprepitant

Cannabinoids Unknown. CIII D: THC in pill form (refrigerate) Chemo, sickle cell anemia.
Dronabinol, nabilone Does not produce same high. Caution pts w/ CV dz. AE:
tachycardia, hypotension

Dopamine Antagonists Blocks rec in CTZ Extrapyramidal effects; Chemo, post-op, general.
Phenothiazines: -azines Anticholinergic effects. Can cause Parkinson-like shakes
Butyrophenones: Haloperidol M: causes long-term nerve Promethazine: dry mouth,
Other: Metoclopramide, damage drowsy
Domperidone

Anticholinergics: A: block h1 rec

Antihistamines: - ines
Other: scopolamine S: Transderm patches S -Use: motion sickness
Ondansetron

Classification Antiemetic – most effective drug to combat n/v

Drug Names Zofran
MOA Blocks 5HT3 rec
Pharmacology
Dosage/Route IV, PO
Therapeutic Range
Adverse Effects Constipation, HA, rash. Rare: bronchospasm, tachycardia, chest pain, hypokalemia, ECG changes, tonic clonic seizure
Contraindications Impaired renal/hepatic fcn; caution in pregnancy, lactation.
Precaution pts:
Drug Interactions More effective with dexamethasone (IV for emesis)
When is it used? Emesis: chemo, perioperative; pregnancy
Metabolic Effects P450 drug metabolizing enzymes
Lab considerations Transient elevations in AST, ALT.
Nursing Prevents acute emesis, but not delayed emesis. Monitor bowel fcn & liver enzymes.
considerations