Antiulcer Drugs

Definition
'Antiulcer drugs are a class of drugs, exclusive of the antibacterial agents, used to treat ulcers in the stomach and the
upper part of the small intestine.

Antiulcer Drugs
Brand Name
Possible Common Side Effects Include:
(Generic Name)
Axid (nitzatidine) Diarrhea, headache, nausea and vomiting, sore
throat
Carafate (sucralfate) Constipation, insomnia, hives, upset stomach,
vomiting
Cytotec (misoprostol) Cramps, diarrhea, nausea, gas, headache,
menstrual disorders (including heavy bleeding
and severe cramping)
Pepcid (famotidine) Constipation or diarrhea, dizziness, fatigue,
fever
Prilosec (omeprazole) Nausea and vomiting, headache, diarrhea,
abdominal pain
Tagamet (cimetidine) Headache, breast development in men, depres-
sion and disorientation
Zantac (ranitidine Headache, constipation or diarrhea, joint pain
hydrochloride)
Purpose
Recurrent gastric and duodenal ulcers are caused by Helicobacter pyloriinfections, and are treated with combination
treatments that incorporate antibiotic therapy with gastric acid suppression. Additionally, bismuth compounds have been
used. The primary class of drugs used for gastric acid suppression are the proton pump inhibitors, omeprazole,
lansoprazole, pantoprazole and rabeprazole. The H-2 receptor blocking agents, cimetidine, famotidine, nizatidine, and
ranitidine have been used for this purpose, but are now more widely used for maintenance therapy after treatment with
the proton pump inhibitors. Sucralfate, which acts by forming a protective coating over the ulcerate lesion, is also used in
ulcer treatment and may be appropriate for patients in whom other classes of drugs are not indicated, or those whose
gastric ulcers are caused by non-steroidal anti-inflammatory drugs (NSAIDs) rather than H. pylori infections.

Description
The proton pump inhibitors block the secretion of gastric acid by the gastric parietal cells. The extent of inhibition of acid
secretion is dose related. In some cases, gastric acid secretion is completely blocked for over 24 hours on a single dose.
In addition to their role in treatment of gastric ulcers, the proton pump inhibitors are used to treat syndromes of excessive
acid secretion (Zollinger-Ellison Syndrome) and gastroesophageal reflux disease (GERD).

Histamine H-2 receptor blockers stop the action of histamine on the gastric parietal cells, inhibiting the secretion of gastric
acid. These drugs are less effective than the proton pump inhibitors, but may achieve a 75-79% reduction in acid
secretion. Higher rates of acid inhibition may be achieved when the drug is administered by the intravenous route. The H-
2 receptor blockers may also be used to treat heartburn and hypersecretory syndromes. When given before surgery, the
H-2 receptor blockers are useful in prevention of aspirationpneumonia.

Sucralfate (Carafate), a substituted sugar molecule with no nutritional value, does not inhibit gastric acid, but rather,
reacts with existing stomach acid to form a thick coating that covers the surface of an ulcer, protecting the open area from
further damage. A secondary effect is to act as an inhibitor of the digestive enzyme pepsin. Sucralfate does not bind to the
normal stomach lining. The drug has been used for prevention of stress ulcers, the type seen in patients exposed to
physical stress such as burns and surgery. It has no systemic effects.

Recommended dosage
The doses of the proton pump inhibitors and H-2 receptor blockers vary depending on the drug and condition being
treated. Consult individual references.

The dose of sucralfate for acute ulcer therapy is 1 gram four times a day. After the ulcer has healed, maintenance
treatment may continue at 1 gram two times daily.

Precautions
The proton pump inhibitors are generally well tolerated, and the most common adverse effects are diarrhea, itching, skin
rash, dizziness and headache. Muscle aches and a higher than normal rate of respiratory infections are among the other
adverse reactions reported. Omeprazole has an increased rate of fetal deaths in animal studies. It is not known if these
drugs are excreted in human milk, but because of reported adverse effects to infants in animal studies, it is recommended
that proton pump inhibitors not be used by nursing mothers.

The H-2 receptor blockers vary widely in their adverse effects. Although they are generally well tolerated, cimetidine may
cause confusion in elderly patients, and has an antiandrogenic effect that may cause sexual dysfunction in males.
Famotidine has been reported to cause headache in 4.7% of patients. It is advisable that mothers not take H-2 receptor
blockers while nursing.

Sucralfate is well tolerated. It is poorly absorbed, and its most common side effect is constipation in 2% of patients.
Diarrhea, nausea, vomiting, gastric discomfort, indigestion, flatulence, dry mouth, rash, pruritus (itching),
backpain, headache, dizziness, sleepiness, and vertigo have been reported, as well as rare allergic responses. Because
sucralfate releases small amounts of aluminum into the system, it should be used with caution in patients with renal
insufficiency. There is no information available about sucralfate's safety in breastfeeding.

Interactions
Proton pump inhibitors may increase the pH of the stomach. This will inactivate some antifungal drugs that require an acid
medium for effectiveness, notable itraconazole and ketoconazole.

H-2 receptor blocking agents have a large number of drug interactions. Consult individualized references.

1.
Cardiac glycosides
a. action: makes heart beat slower but stronger
i.improves pumping ability of heart
ii. increases force of heart's contraction
iii. decreases rate of contraction
iv. increases cardiac output
b. examples
i. digitoxin (Crystodigin)
ii. digoxin (Lanoxin)
use
i. congestive heart failure
ii. atrial flutter
iii. atrial fibrillation
d. contraindications
i. ventricular tachycardia
ii. ventricular fibrillation
iii. second and third degree heart block
e. adverse side effects
i. gastrointestinal effects such as nausea and vomiting, diarrhea, and anorexia
ii. bradycardia
iii. xanthopsia
iv. muscle weakness
v. dysrhythmia
f. nursing interventions
i. before giving glycoside, check apical pulse and heart rhythm. Report if < 60 bpm
ii. establish baseline data such as vital signs, electrolytes, clinical symptoms, creatinine clearance test
iii. monitor for drug toxicity
• in children - cardiac arrhythmias
• in adults - visual disturbances, nausea and vomiting,
anorexia
• older clients more prone to toxicity
iv. monitor drug levels
• therapeutic range 0.8 to 2.0 ng/ml
• toxic range > two ng/ml
• diuretics may increase chance of toxicity
g. monitor intake and output
h. client teaching
i. take medication as prescribed
ii. teach client how to take and record pulse daily
iii. identify and report signs of toxicity
• for atrial fibrillation: take pulse and report if below 60 or above 100 or changes in rhythm

• daily weights: report two pound increase

2. Antihypertensives
a.action: dilates peripheral blood vessels
b.examples
i. hydralazine HCL (Apresoline)
ii. enalapril maleate (Vasotec)
iii. reserpine (Serpasil)
iv. prazosin HCL (Minipress)
v. methyldopa (Aldomet)

vi. clonidine (Catapres)

c. use: hypertension
d. contraindications
i. heart block
ii. children
e. adverse side effects
i. orthostatic hypotension
ii. dizziness
iii. bradycardia
iv. tachycardia
v. sexual dysfunction
vi. deterioration in renal function
vii. agranulosis
f. nursing interventions
i. monitor vital signs and blood pressure, sitting and standing
ii. monitor for hearing changes, renal functioning
iii. if hypotension, closely monitor client
iv. encourage intake of foods high in vitamin B
v. teach client
• low sodium diet
• change positions slowly
• take medication as instructed
• avoid hazardous activities
• protect medication from heat and light
GENERIC NAME FOR IMURAN
Azathioprine 50mg; scored tabs.
LEGAL CLASSIFICATION:
Rx
PHARMACOLOGICAL CLASS FOR IMURAN
Immunosuppressant.
MANUFACTURER OF IMURAN
Prometheus Labs, Inc.
INDICATIONS FOR IMURAN
Severe, active, erosive rheumatoid arthritis unresponsive to rest, NSAIDs or gold.

ADULT DOSE FOR IMURAN

1mg/kg per day in 1–2 divided doses. After 6–8 weeks, if needed, increase by 0.5mg/kg per day increments every 4
weeks; max 2.5mg/kg per day. Maintenance: use lowest effective dose.

CHILDREN'S DOSING FOR IMURAN

Not recommended.

CONTRAINDICATIONS FOR IMURAN

Pregnancy (Cat.D).

WARNINGS/PRECAUTIONS FOR IMURAN

Be fully familiar with this product's toxicity before use. Impaired renal function. Monitor blood. Discontinue if ineffective
after 12 weeks. Nursing mothers: not recommended.

INTERACTIONS FOR IMURAN

Avoid concomitant gold, antimalarials or penicillamine. Reduce dose to ⅓ or ¼ with allopurinol. Prior treatment with
alkylating agents increases cancer risk. Anemia, leukopenia with ACE inhibitors. May antagonize warfarin.

ADVERSE REACTIONS FOR IMURAN

Severe leukopenia and/or thrombocytopenia, secondary infections, mutagenic and carcinogenic potential, nausea,
pancreatitis, hepatotoxicity, rash, alopecia.

HOW IS IMURAN SUPPLIED?

Tabs—100

IMURAN (azathioprine), an immunosuppressive antimetabolite, is available in tablet form for oral administration and 100-
mg vials for intravenous injection. Each scored tablet contains 50 mg azathioprine and the inactive ingredients lactose,
magnesium stearate, potato starch, povidone, and stearic acid. Each 100-mg vial contains azathioprine, as the sodium
salt, equivalent to 100 mg azathioprine sterile lyophilized material and sodium hydroxide to adjust pH.

Azathioprine is chemically 6-[(1-methyl-4-nitro-1H-imidazol-5-yl)thio]-1H-purine. The structural formula of azathioprine is:

It is an imidazolyl derivative of 6-mercaptopurine and many of its biological effects are similar to those of the parent
compound.

Azathioprine is insoluble in water, but may be dissolved with addition of one molar equivalent of alkali. The sodium salt of
azathioprine is sufficiently soluble to make a 10mg/mL water solution which is stable for 24 hours at 59° to 77°F (15° to
25°C). Azathioprine is stable in solution at neutral or acid pH but hydrolysis to mercaptopurine occurs in excess sodium
hydroxide (0.1N), especially on warming. Conversion to mercaptopurine also occurs in the presence of sulfhydryl
compounds such as cysteine, glutathione, and hydrogen sulfide.

What is azathioprine (Imuran)?

Azathioprine lowers your body's immune system. The immune system helps your body fight infections. The immune
system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats
the new organ as an invader.

Azathioprine is used to prevent your body from rejecting a transplanted kidney. It is also used to treat symptoms of
rheumatoid arthritis.

Azathioprine may also be used for other purposes not listed in this medication guide.

Azathioprine 50 mg-GG

What are the possible side effects of azathioprine (Imuran)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of
your face, lips, tongue, or throat.

Call your doctor at once if you have a serious side effect such as:

• pale skin, easy bruising or bleeding, unusual weakness;

• fever, chills, sore throat, body aches, weakness, muscle pain, flu symptoms;
• severe nausea, vomiting, or diarrhea;
• severe pain in your upper stomach spreading to your back, fast heart rate;
• pain or burning with urination;
• stomach pain, loss of appetite, dark urine, clay-colored stools, and jaundice (yellowing of the skin or eyes); or
• white patches or sores inside your mouth or on your lips.

Less serious side effects may include:

• mild upset stomach, nausea, diarrhea, loss of appetite;

• hair loss; or
• skin rash.

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side
effect. You may report side effects to FDA at 1-800-FDA-1088.

What is the most important information I should know about azathioprine (Imuran)?
Do not use this medication without telling your doctor if you are pregnant. It could cause harm to the unborn baby. Use an
effective form of birth control, and tell your doctor if you become pregnant during treatment.

Taking azathioprine may increase your risk of developing cancer. Talk with your doctor about your specific risk.

Azathioprine can lower the blood cells that help your body fight infections. This can make it easier for you to bleed from an
injury or get sick from being around others who are ill. To be sure your blood cells do not get too low, your blood will need
to be tested on a regular basis. Your kidney function may also to need to be tested. Do not miss any scheduled visits to
your doctor.

Call your doctor at once if you have a fever, chills, sore throat, body aches, weakness, muscle pain, easy bruising or
bleeding, mouth sores, pale stools, darkened urine, or severe nausea, vomiting, and diarrhea.

If you need to have any type of surgery, tell the surgeon ahead of time that you are using azathioprine. You may need to
stop using the medicine for a short time.

This medication can affect fertility (your ability to have children), whether you are a man or a woman. Talk with your doctor
if you have concerns about this.

Do not receive a "live" vaccine while you are being treated with azathioprine and avoid coming into contact with anyone
who has recently received a live vaccine. There is a chance that the virus could be passed on to you.