GI and Renal Pharm
Terms
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- Increase gastric pH to above 4 so that pepsin is inactivated
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ANTACIDS
calcium-containing s/e - hypercalcemia w/ renal impairment
Aluminum - constipation, hypophosphatemia
Magnesium - hypermagnesemia, diarrhea
Sodium - instigate CHF -
Inhibit histamine at H2 Receptor --> reduced basal and food stimulated gastric acid secretion and volume
Associated w/ hypersensitivity, confusion in elderly, gynecomastia and infertility in males -
Cimetidine (tagamet)
also increases levels of drugs P450 system - Omeprazole
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Proton-pump inhibitor - irreversibly inhibits the H+/K+ ATPase pump of the parietal cell
Well tolerated - Effective for GUs and DUs, esophagitis, healing of ulcers assoc with NSAIDs, Zollinger-Ellison Syndrome, used in combination with antibiotics for H. pylori
- Proton Pump Inhibitors
- Sucralfate (carafate)
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Surface protective agent
forms ulcer adherent complex
inhibits pepsin activity, absorbs bile salts, may stimulate PG secretion
-short term treatement of DU
- requires acidic envt - Bismuth Salts
- binding to ulcers, may stimulate PG synthesis, increase mucous production, inhibit pepsin
- Used in combination with antibiotics to decrease H pylori
- Bismuth salts
- analog of PGE1- used for NSAID induced ulceration
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Misprostol
CONTRAINDICATED IN PREGNANCY
causes abdominal pain and diarrhea -
Increases GI motility
Mimics cholinergic action but is a dopamine antagonist -
Metoclopramide
(can cause somnolence, nervousness, dystonia, parkinsonism, tardive dyskinesia) -
Antiemetic with cholinergic and serotenergic activity
can cause fatal arrythmias -
Cisapride
(off the market) - Block Dopamine receptors in chemoreceptor trigger zone
- Phenothiazines
- Serotonin receptor antagonist used to treat nausea associated with cancer therapy
- Onsdansetron
- Dronabinon
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marijuana derivative
antiemetic -
Opioid derivative used in treatment of diarrhea
usually used with atropine -
Diphenoxylate
(metabolized to active product)
contraindicated in ulcerative colitis b/c of toxic megacolon - Loperamide
- inhibits Ach release through presynaptic opioid receptors in gut
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First line therapy for IBD
antiinflammatory agent - inhibits cyclooxygenase and lipoxygenase -
sulfasalazine
side effects:(20%)malaise, nausea, abdominal discomfort anorexia, folate malabsorption, hypersensitivity, many others - Tolerated by 80-90% of those who cant tolerate 5-ASA
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Olsalazine (dipentum)
contains 2 molecules of 5-ASA and is broken down in colon to release 5-ASA - Resin coated 5-ASA - released in a pH dependent manner in distal ileum and colon
- Mesalamine (Asacol)
- Ethycellulose coated 5-ASA - time dependent release from jejenum to colon
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Mesalamine (Pentasa)
best formulation for small bowel disease - immunomodulator that inhibits purine metabolism.
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6-MP (purinethol)
steroid sparing
slow onset - 3 months
bone marrow suppression, pancreatitis - Inhibits IL-2 - used as a temporary measure in severe colitis
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Cyclosporine
onset 1-2 weeks
side effects: HTN, Seizures, Parasthesias, tremor, cholestasis, others - Folic acid antagonist most effective in crohn's disease.
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Methotrexate
steroid sparing - chimeric antibody against TNF-alpha. Used for moderate, severe or fistulizing crohn's disease
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Infliximab
s/e: increased risk of infection, infusion reaction, tachyphylaxis, nausea, serum sickness -
Non-selective B-blocker
decreases renin, CO, and peripheral resistance -
proponolol
can cause bronchial constriction - Most popular selective B-blocker
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Metoprolol
(atenolol - similar but longer acting) - alpha1 and Beta blocker
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Labetalol
(carvedilol is another drug with combined a/B effects) -
Peripheral A1 blocker - causes vasodilation without reflex cardiac stimulation
Used in HTN with benign prostatic hypertrophy -
Prasozin
Doxazosin
S/E: Orthostasis - first dose effect - helped by taking at night - Central A2 agonist - decreases peripheral autonomic tone
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Clonidine
S/E - sedation, rebound HTN, dry mouth - Arterial vasodilator that works directly on smooth muscle
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Hydralazine
S/E: reflex tachycardia, Na retention and edema
always use with B-blockers and furosemide - Potent arterial vasodilator that opens K channels- relaxation of smooth muscle cells but not used except for as a topical treatment for BALDNESS
- Minoxidil