GASTROINTESTINAL MEDICATIONS

ANTIULCERS ANTIEMETICS ANTIDIARRHEALS

USES
Peptic Ulcer Disease
Gastric & duodenal ulcers

Gastroesophageal Reflux Gastric Hyperacidity

Stress ulcers

ANTIULCER DRUGS
Reduce gastric acidity and promote healing

ANTACIDS
HISTAMINE-2 RECEPTOR ANTAGONISTS (H2ANTAGONISTS) PROTON PUMP INHIBITORS MICELLANEOUS PRODUCTS

ANTACIDS
ACTION: NEUTRALIZE gastric acid (HCL) and Ph thus pepsin production (a proteolytic enzyme that can digest the stomach wall in an acidic environment)

 Commonly used antacids are: -Aluminum compounds -Magnesium compounds -Calcium compounds Antacids differ in the amounts needed to neutralize gastric acid, in onset of action and in adverse side effects. Antacids work locally to correct gastric hyperactivity Liquid suspensions usually work faster than chewable tabs. Tabs must be chewed thoroughly.

ALUMINUM BASED ANTACIDS

Low neutralizing capacity (large amounts are required) Slow onset of action Major Side Effect: Constipation Example: Amphogel

MAGNESIUM BASED ANTACIDS

High neutralizing capacity Rapid onset of action Side effect: Diarrhea, Hypermagnesemia Example: MOM, Mag-Ox Contraindicated in patients with renal failure

CALCIUM BASES ANTACIDS

Rapid onset of action May cause hypersecretion of gastric acid= Acid Rebound Side Effects: constipation, kidney stones Example: Tums

Combination Antacids
Combination of aluminum hydroxide and magnesium hydroxide **Combined to minimize constipation and diarrhea, combining fast-acting and slow-acting antacids can prolong gastric acid neutralization May contain simethicone (an antiflatulent). Reportedly s gas bubbles thus ing GI distention and abdominal discomfort Examples: Maalox, Mylanta, Gelusil

HISTAMINE (H-2) RECEPTOR ANTAGONISTS (H-2RAS)

Histamine is a substance found in almost every body tissue and released in response to certain stimuli. In the GI tract, histamine causes strong stimulation of gastric acid secretion. The histamine acts on receptors located on the parietal cells in the stomach to increase production of hydrochloric acid. These receptors are called H-2 receptors.

H-2 RAs ACTION

H-2RAs inhibit secretion of gastric acid stimulated by histamine They decrease the amount, acidity, and pepsin content of gastric juices. H-2RAs are rapidly absorbed and reach peak effectiveness in approx. 1-1.5 hours.

CLINICAL INDICATIONS
Prevention and treatment of peptic ulcer disease Esophagitis resulting from gastroesophageal reflux GI bleeding due to acute stress ulcers Zollinger-Ellison syndrome

H-2RAs (contd)
A. cimetidine (Tagamet) Was the first of the H-2RAs Has the most side effects including confusion and agitation High risk of drug-drug interactions Increases risk of toxicity and adverse effects with such drugs as: warfarin(anticoagulant),theophylline(bronchodiator), some antiarrhythmics and anticonvulsants. Serum digoxin levels may decrease if administered concurrently with cimetidine

Newer H-2RAs (cond.)

B. famotidine (Pepcid)
C. nizatidine (Axid) D. ranitidine (Zantac)
More potent than cimetidine Longer duration of action Smaller doses can be given less frequently Few drug-drug interactions Few S.E.: dizziness, H/As, transient diarrhea

H-2RAs (contd)
Use cautiously in patients with renal impairment elderly, children and pregnant woman Usually administered with meals and HS Low doses can be purchased OTC Can mask S&S of GI problems; may delay treatment After treatment of acute ulcer (usually 6-8 weeks), H-2RAs may be administered daily @ HS for maintenance therapy(suppresses nocturnal secretion of gastric acid) Antacids and H-2RAs usually prescribed concurrently. Do not give at the same time, administer antacid 1 hr before or after H-2RAs

PROTON PUMP INHIBITORS (PPIS)

Strongest gastric acid suppressants available ACTION: Binds to the gastric proton pump inhibiting the activity of the enzyme H+K+-ATPase, to prevent pumping or release of gastric acid into the stomach lumen and blocks the final step of acid production.

INDICATIONS FOR USE

Short term treatment of: -peptic ulcer disease -GERD -erosive esophagitis that did not respond/heal with conventional courses of H-2RAs. PPIs are the treatment of choice with Zollinger-Ellison syndrome.

PPIS (contd)
A. B. C. D. Omeprazole (Prilosec) Lansoprazole (Prevacid) Pantoprazole (Protonix) Rabeprazole (Aciphex)

PPIs (contd)
Administered orally, before meals Swallow whole; do not chew or crush Adverse effects: -usually well tolerated -nausea, diarrhea, headache may be reported PPIs & H-2RAs should NOT be administered concurrently. Drug interactions: PPIs (primarily prilosec) may serum[ ] of specific meds ex. Anticoagulants, Valium and Dilantin

OTHER/MISCELLANEOUS ANTIULCER DRUGS

1. Sulcralfate (Carafate) -ACTION: when an ulcer is present, sucralfate combines with the ulcer exudate, adheres to the ulcer site and forms a protective barrier over the ulcer. Sucralfate requires an acid Ph for activation thus should NOT be given with an antacid, H-2RAs or PPIs.

sucralfate (Carafate) contd

INDICATIONS FOR USE -effective in healing duodenal ulcers and in maintenance therapy to prevent ulcer recurrence Side effects -because sucralfate is not absorbed systemically, few SE are observed. Most common SE: constipation

sucralfate (Carafate) contd

Take sucralfate on an empty stomach at least one hour ac & HS
(7a-11a-4p-9p)

Do NOT take an antacid for approx. 1 hr before or after taking sucralfate. Sucralfate may absorption of other drugs -ex: certain antiinfectives, digoxin,
coumadin, dilantin

This can avoided or minimized by giving the affected drug 2 hrs before sucralfate.

Other Antiulcers contd

2. Misoprostol (Cytotec) ACTION: synthetic form of prostaglandin E. Naturally occurring prostaglandin E is produced in the mucosal cells of the stomach and duodenum and inhibits gastric acid secretion, s mucous and bicarbonate secretion and may protect gastric mucosa.

Cytotec contd
Indication for Use -Prevention of NSAID-induced ulcerations and bleeding. -take concurrently when on high doses of NSAIDS such as patients with arthritis taking ibuprofen Side Effects: diarrhea most common -contraindicated in pregnant women Administer orally, with food

ANTIDIARRHEALS
Used to treat diarrhea, a symptom of numerous conditions that increase GI motility or irritation of the GI tract that results in rapid loss of bowel contents. Consequently, absorption fluids and electrolytes is limited.

Antidiarrheals contd
ACTION: reduce the fluid content of the stool and decrease peristalsis and motility of the intestinal tract. Choice of antidiarrheal agent depends largely on the cause. Three common groups of antidiarrheals 1. Opioids 2. Intestinal Flora Modifiers 3. Absorbents

Antidiarrheals contd
1. Opioids- most effective for symptomatic relief of
diarrhea

a. Diphenoxylate with atropine sulfate (Lomotil) b. loperamide (Imodium) also available OTC Derivative of meperidine (Demerol) Decreases GI motility The effective antidiarrheal dose is lower than that which can cause euphoria or analgesia

Antidiarrheals contd
2. Intestinal Flora Modifiers -lactobacillus acidophilus (Lactinex) Used to treat diarrhea caused by antibiotics; reestablishes normal intestinal flora and may be used prophylactically in patients with a history of antibiotic-induced diarrhea Packet of lactinex granules must be kept in refrigerator

Antidiarrheals contd
3. Absorbent Antidiarrheal agents -absorb bacteria & toxins, thus remove the cause of diarrhea; provides relief of abdominal cramping. a. Bismuth salts (Pepto-Bismol) -commonly used OTC med -contains salicylates (aspirin) which may provide an anti-inflammatory effect -assess for aspirin sensitivity -avoid use in infants & children--risk of producing Reyes syndrome

Antidiarrheals contd Absorbents

b. Kaolin and Pectin (Kaopectate) -widely used OTC medication to self-treat diarrhea. -clinical effectiveness in decreasing diarrhea has not been established.

Antidiarrheals contd Nursing Implications

Assess: duration, frequency, amount, consistency of diarrhea Try to determine cause -concurrent use of medications -travel history -spicy &/or contaminated foods -GI history -use of laxatives

Nursing Implications contd

Monitor labs; check results of stool specimens Assess for S&S of F&E imbalance Interventions:
F&E replacement I/O Dietary modifications; clear liquids, avoid irritating foods Frequent handwashing Inspect rectal area for irritation Teach pt to take meds only as directed Stop antidiarrheals when diarrhea controlled to avoid adverse SE such as constipation

ANTIEMETICS
Used to prevent or treat nausea and vomiting (N/V) N/V are common symptoms associated with a variety of causes, e.g.:
Systemic illness or infection Post-operative status motion sickness Pain Drug therapy ex: anticancer agents Impaired GI motility Overeating or ingestion of foods or fluids that irritate GI mucosa

Antiemetics contd
Most antiemetics prevent or relieve N/V by acting on N/V centers in the brain:
Vomiting center Chemoreceptor trigger zone (CTZ) Cerebral cortex Vestibular apparatus (as with motion sickness) Or a combination of the above

Antiemetics contd
Most antiemetics have
Anticholinergic Antidopaminergic Antihistaminic or Antiserotonergic effects

Antiemetics contd
A. Phenothiazines
- prochlorperazine (Compazine) - promethzine (Phenegran) - chorpromazine (Thorazine) -po, IV, IM, supp -CNS depressants -blocks dopamine from receptor sites in the brain and act on the CTZ -not all phenothiazines are effective antiemetics -may turn urine pink to reddish brown -Thorazine IM can be given to treat severe hiccups as sometimes seen after abdominal surgery due to irritation of the phrenic nerve

Antiemetics contd
B. Anticholinergics e.g. 1. Scopolamine transdermal patch -effective in relieving N/V associated with motion sickness blocks acetylcholine, a neurotransmitter in the CNS -releases medication over a 3-day interval; produces fewer adverse anticholinergic effects than oral forms

Antiemetics contd
2. trimethobenzamide (Tigan) -Blocks CTZ -Must give deep IM because it is highly irritating to tissues -has been linked to the development of Reyes syndrome in children

Antiemetics contd
C. Antihistamines e.g. hydroxyzine (Vistaril) meclizine (Antivert) dimenhydrinate (Dramamine) -blocks histamine-1 and acetylcholine (as with anticholinergics)

Antiemetics contd
D. Serotonin Receptor Antagonists e.g. ondansetron (Zofran)** granisetron (Kytril) -blocks serotonin receptors in the CTZ -drug of choice for chemo-induced nausea** -can be administered 1 hour before chemo -Zofran also effective in controlling post-operative vomiting**

Misc. Antiemetics
E. Prokinetic Agents e.g. metoclopramide (Reglan) -ac and HS -s GI motility and the rate of gastric emptying; also blocks dopamine -indications for use include GERD, diabetic gastroparesis -can be given with other antiemetics

Misc. Antiemetics contd

F. dronabinol (Marinol) -is a cannabinoid (derivative of marijuana) - route: po -can be used in the management of N/V associated with anticancer drugs when other antiemetics are not effective -may be use to stimulate appetite in patients with anorexia e.g. HIV+ patients

Nursing Implication for Antiemetics

Identify causes of N/V Assess for FVD related to vomiting Replace fluid & electrolytes Administer antiemetics 30-60 mins before nausea-producing event; e.g. travel, cancer chemotherapy, radiation, may even be admin pre-operatively in some cases Because pain may cause N/V, admin before painful diagnostic test or dressing change

 oral is preferred for prophylactic use Rectal and parenteral forms preferred for therapeutic use Assess for adverse effects: excessive sedation and drowsiness and other anticholinergic SE.