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DRUGS USED PRIMARILY FOR GASTROINTESTINAL CONDITIONS

SUBCLASS MECHANISM OF ACTION EFFECTS CLINICAL APPLICATIONS PHARMACOKINETICS, TOXICITIES, INTERACTIONS DRUGS USED IN ACID-PEPTIC DISEASES PROTON PUMP INHIBITORS IRREVERSIBLE BLOCKADE OF + + (PPIS), EG, OMEPRAZOLE, H ,K -ATPASE PUMP IN LANSOPRAZOLE ACTIVE PARIETAL CELLS OF STOMACH

HALF-LIVES MUCH SHORTER THAN DURATION OF ACTION LOW TOXICITY REDUCTION OF STOMACH ACID MAY REDUCE ABSORPTION OF SOME DRUGS AND INCREASE THAT OF OTHERS H2-RECEPTOR BLOCKERS, EG, CIMETIDINE: EFFECTIVE REDUCTION OF NOCTURNAL ACID BUT LESS EFFECTIVE AGAINST STIMULATED SECRETION; VERY SAFE, AVAILABLE OVER THE COUNTER (OTC). CIMETIDINE, BUT NOT OTHER H2 BLOCKERS, IS A WEAK ANTIANDROGENIC AGENT AND A POTENT CYP ENZYME INHIBITOR SUCRALFATE: POLYMERIZES AT SITE OF TISSUE DAMAGE (ULCER BED) AND PROTECTS AGAINST FURTHER DAMAGE; VERY INSOLUBLE WITH NO SYSTEMIC EFFECTS; MUST BE GIVEN FOUR TIMES DAILY ANTACIDS: POPULAR OTC MEDICATION FOR SYMPTOMATIC RELIEF OF HEARTBURN; NOT AS USEFUL AS PPI AND H 2 BLOCKERS IN PEPTIC DISEASES DRUGS STIMULATING MOTILITY METOCLOPRAMIDE D2-RECEPTOR BLOCKER INCREASES GASTRIC GASTRIC PARESIS (EG, IN DIABETES) PARKINSONIAN SYMPTOMS DUE TO BLOCK REMOVES INHIBITION OF EMPTYING AND INTESTINAL ANTIEMETIC (SEE BELOW) OF CENTRAL NERVOUS SYSTEM (CNS) D2 ACETYLCHOLINE NEURONS IN MOTILITY RECEPTORS ENTERIC NERVOUS SYSTEM DOMPERIDONE: LIKE METOCLOPRAMIDE, BUT LESS CNS EFFECT; NOT AVAILABLE IN USA CHOLINOMIMETICS: NEOSTIGMINE OFTEN USED FOR COLONIC PSEUDO-OBSTRUCTION IN HOSPITALIZED PATIENTS MACROLIDES: ERYTHROMYCIN USEFUL IN DIABETIC GASTROPARESIS BUT TOLERANCE DEVELOPS LAXATIVES MAGNESIUM HYDROXIDE, OSMOTIC AGENTS INCREASE USUALLY CAUSES SIMPLE CONSTIPATION; BOWEL MAGNESIUM MAY BE ABSORBED AND OTHER NONABSORBABLE WATER CONTENT OF STOOL EVACUATION WITHIN 4–6 H, PREP FOR ENDOSCOPY (ESPECIALLY CAUSE TOXICITY IN RENAL IMPAIRMENT SALTS AND SUGARS SOONER IN LARGE DOSES PEG SOLUTIONS) BULK-FORMING LAXATIVES: METHYLCELLULOSE, PSYLLIUM, ETC: INCREASE VOLUME OF COLON, STIMULATE EVACUATION STIMULANTS: SENNA, CASCARA; STIMULATE ACTIVITY; MAY CAUSE CRAMPING STOOL SURFACTANTS: DOCUSATE, MINERAL OIL; LUBRICATE STOOL, EASE PASSAGE CHLORIDE CHANNEL ACTIVATOR: LUBIPROSTONE, PROSTANOIC ACID DERIVATIVE, STIMULATES CHLORIDE SECRETION INTO INTESTINE, INCREASING FLUID CONTENT OPIOID RECEPTOR ANTAGONISTS: ALVIMOPAN, METHYLNALTREXONE; BLOCK INTESTINAL U-OPIOID RECEPTORS BUT DO NOT ENTER CNS, SO ANALGESIA IS MAINTAINED 5-HT 4 AGONISTS: TEGASEROD; ACTIVATES ENTERIC 5-HT4 RECEPTORS AND INCREASES INTESTINAL MOTILITY ANTIDIARRHEAL DRUGS LOPERAMIDE ACTIVATES U-OPIOID SLOWS MOTILITY IN GUT WITH NONSPECIFIC, NONINFECTIOUS MILD CRAMPING BUT LITTLE OR NO CNS RECEPTORS IN ENTERIC NEGLIGIBLE CNS EFFECTS DIARRHEA TOXICITY NERVOUS SYSTEM DIPHENOXYLATE: SIMILAR TO LOPERAMIDE, BUT HIGH DOSES CAN CAUSE CNS OPIOID EFFECTS AND TOXICITY COLLOIDAL BISMUTH COMPOUNDS: SUBSALICYLATE AND CITRATE SALTS AVAILABLE. OTC PREPARATIONS POPULAR AND HAVE SOME VALUE IN TRAVELERS' DIARRHEA DUE TO ADSORPTION OF TOXINS KAOLIN + PECTIN: ADSORBENT COMPOUNDS AVAILABLE OTC DRUGS FOR IRRITABLE BOWEL SYNDROME (IBS) ALOSETRON 5-HT3 ANTAGONIST OF HIGH REDUCES SMOOTH MUSCLE APPROVED FOR SEVERE DIARRHEARARE BUT SERIOUS CONSTIPATION POTENCY AND DURATION OF ACTIVITY IN GUT PREDOMINANT IBS IN WOMEN ISCHEMIC COLITIS INFARCTION BINDING

LONG-LASTING REDUCTION OF STIMULATED AND NOCTURNAL ACID SECRETION

PEPTIC ULCER, GASTROESOPHAGEAL REFLUX DISEASE, EROSIVE GASTRITIS

ANTICHOLINERGICS: NONSELECTIVE ACTION ON GUT ACTIVITY, USUALLY ASSOCIATED WITH TYPICAL ANTIMUSCARINIC TOXICITY CHLORIDE CHANNEL ACTIVATOR: LUBIPROSTONE (SEE ABOVE); USEFUL IN CONSTIPATION-PREDOMINANT IBS IN WOMEN ANTIEMETIC DRUGS ONDANSETRON, OTHER 55-HT3 BLOCKADE IN GUT AND EXTREMELY EFFECTIVE IN FIRST-LINE AGENTS IN CANCER USUALLY GIVEN IV BUT ORALLY ACTIVE IN HT3 ANTAGONISTS CNS WITH SHORTER PREVENTING CHEMOTHERAPY; ALSO USEFUL FOR PROPHYLAXIS. 4–9 H DURATION OF ACTION DURATION OF BINDING CHEMOTHERAPY-INDUCED POSTOP EMESIS VERY LOW TOXICITY BUT MAY SLOW THAN ALOSETRON AND POSTOPERATIVE NAUSEA COLONIC TRANSIT AND VOMITING APREPITANT NK1-RECEPTOR BLOCKER IN INTERFERES WITH VOMITING EFFECTIVE IN REDUCING BOTH GIVEN ORALLY IV FOSAPREPITANT CNS REFLEX NO EFFECT ON 5-HT, EARLY AND DELAYED EMESIS IN AVAILABLE FATIGUE, DIZZINESS, DIARRHEA DOPAMINE, OR STEROID CANCER CHEMOTHERAPY CYP INTERACTIONS RECEPTORS CORTICOSTEROIDS: MECHANISM NOT KNOWN BUT USEFUL IN ANTIEMETIC IV COCKTAILS ANTIMUSCARINICS (SCOPOLAMINE): EFFECTIVE IN EMESIS DUE TO MOTION SICKNESS; NOT OTHER TYPES ANTIHISTAMINICS: MODERATE EFFICACY IN MOTION SICKNESS AND CHEMOTHERAPY-INDUCED EMESIS PHENOTHIAZINES: ACT PRIMARILY THROUGH BLOCK OF D 2 AND MUSCARINIC RECEPTORS CANNABINOIDS: DRONABINOL IS AVAILABLE FOR USE IN CHEMOTHERAPY-INDUCED NAUSEA AND VOMITING, BUT IS ASSOCIATED WITH CNS MARIJUANA EFFECTS DRUGS USED IN INFLAMMATORY BOWEL DISEASE (IBD) 5-AMINOSALICYLATES, EG, MECHANISM UNCERTAIN TOPICAL THERAPEUTIC MILD TO MODERATELY SEVERE SULFASALAZINE CAUSES SULFONAMIDE MESALAMINE IN MANY MAY BE INHIBITION OF ACTION SYSTEMIC CROHN'S DISEASE AND ULCERATIVE TOXICITY AND MAY CAUSE GI UPSET, FORMULATIONS EICOSANOID ABSORPTION MAY CAUSE COLITIS MYALGIAS, ARTHRALGIAS, INFLAMMATORY MEDIATORS TOXICITY MYELOSUPPRESSION OTHER SULFASALAZINE AMINOSALICYLATES MUCH LESS TOXIC PURINE ANALOGS AND MECHANISM UNCERTAIN GENERALIZED SUPPRESSION MODERATELY SEVERE TO SEVERE GI UPSET, MUCOSITIS MYELOSUPPRESSION ANTIMETABOLITES, EG, 6MAY PROMOTE APOPTOSIS OF IMMUNE PROCESSES CROHN'S DISEASE AND ULCERATIVE PURINE ANALOGS MAY CAUSE MERCAPTOPURINE, OF IMMUNE CELLS COLITIS HEPATOTOXICITY, BUT RARE WITH METHOTREXATE METHOTREXATE AT THE LOW DOSES USED METHOTREXATE BLOCKS DIHYDROFOLATE REDUCTASE ANTI-TNF ANTIBODIES, EG, BIND TUMOR NECROSIS SUPPRESSION OF SEVERAL INFLIXIMAB: MODERATELY SEVERE INFUSION REACTIONS REACTIVATION OF INFLIXIMAB, OTHERS FACTOR AND PREVENT IT ASPECTS OF IMMUNE TO SEVERE CROHN'S DISEASE AND LATENT TUBERCULOSIS INCREASED RISK OF FROM BINDING TO ITS FUNCTION, ESPECIALLY TH1 ULCERATIVE COLITIS OTHERS DANGEROUS SYSTEMIC FUNGAL AND RECEPTORS LYMPHOCYTES APPROVED IN CROHN'S DISEASE BACTERIAL INFECTIONS CORTICOSTEROIDS: GENERALIZED ANTI-INFLAMMATORY EFFECT; SEE CHAPTER 39 PANCREATIC SUPPLEMENTS PANCRELIPASE REPLACEMENT ENZYMES IMPROVES DIGESTION OF PANCREATIC INSUFFICIENCY DUE TO TAKEN WITH EVERY MEAL MAY INCREASE FROM ANIMAL PANCREATIC DIETARY FAT, PROTEIN, AND CYSTIC FIBROSIS, PANCREATITIS, INCIDENCE OF GOUT EXTRACTS CARBOHYDRATE PANCREATECTOMY PANCREATIN: SIMILAR PANCREATIC EXTRACTS BUT MUCH LOWER POTENCY; RARELY USED BILE ACID THERAPY FOR GALLSTONES URSODIOL REDUCES CHOLESTEROL DISSOLVES GALLSTONES GALLSTONES IN PATIENTS REFUSING MAY CAUSE DIARRHEA SECRETION INTO BILE OR NOT ELIGIBLE FOR SURGERY DRUGS USED TO TREAT VARICEAL HEMORRHAGE OCTREOTIDE SOMATOSTATIN ANALOG MAY ALTER PORTAL BLOOD PATIENTS WITH BLEEDING VARICES REDUCED ENDOCRINE AND EXOCRINE MECHANISM NOT CERTAIN FLOW AND VARICEAL OR AT HIGH RISK OF REPEAT PANCREATIC ACTIVITY OTHER ENDOCRINE PRESSURES BLEEDING ABNORMALITIES GI UPSET

Β-BLOCKERS: REDUCE CARDIAC OUTPUT AND SPLANCHNIC VASCULAR RESISTANCE; SEE CHAPTER 10