FINALS –PHARMA

GASTROINTESTINAL SYSTEM DRUGS

Antacids

- Antacids are used to chemically react with and neutralize the acid in the stomach. They can
provide rapid relief from increased acid levels. They are known to cause GI alterations such as
diarrhea or constipation and can alter the absorption of many drugs.

Antacids: Generic and Brand Names

A list of the most commonly encountered antacids and their brand names.

Classification Generic name Brand name

aluminum salts AlternaGEL

calcium salts Oystercal, Tums

magaldrate Losopan, Riopan

Antacids
Milk of Magnesia,
magnesium salts
others

sodium
Bell-ans
bicarbonate

Disease Spotlight: Ulcer Disease

Erosions in the lining of the stomach and adjacent areas of the GI tract are
called peptic ulcer.

1
  Ulcer patients present with a predictable description of gnawing,
burning pain often occurring a few hours after meals.
 Many of the drugs that are used to affect GI secretions are designed to
prevent, treat, or aid in the healing of these ulcers.
 Further research led many to believe that, because acid production
was often normal in ulcer patients, ulcers were caused by a defect in
the mucous lining that coats the inner lumen of the stomach to
protect it from acid and digestive enzymes.
 Treatment was aimed at improving the balance between the acid
produced and the mucous layer that protects the stomach lining.

What are antacids?

Antacids are a group of inorganic chemicals that neutralize stomach acid.

 Antacids are available OTC, and many patients use them to self-treat a
variety of GI symptoms.
 The choice of an antacid depends on adverse effects and absorption
factors.

Therapeutic actions
The desired actions of antacids include the following:

 Neutralize stomach acid by direct chemical reaction.

 Symptomatic relief of an upset stomach associated with hyperacidity,
as well as the hyperacidity associated with peptic ulcer, gastritis,
peptic esophagitis, gastric hyperacidity, and hiatal hernia.

2
Indication
Antacids are indicated for the following:

 Symptomatic relief of GI hyperacidity, treatment of

hyperphosphatemia, prevention of formation of phosphate urinary
stones.
 Treatment of calcium deficiency, prevention of hypocalcemia.
 Prophylaxis of stress ulcers, relief of constipation.

Pharmacokinetics
Many of these antacids are available in combination forms to take advantage
of the acid-neutralizing effect and block adverse effects.

Route Onset Peak Duration

Oral Rapid 30 min 1-3h

IV Immediate Rapid Unknown

Excretion: Unchanged in urine

Contraindications and Cautions

The following are contraindications and cautions when using antacids:

 Allergy. The antacids are contraindicated in the presence of any

known allergy to antacid products or any component of the drug to
prevent hypersensitivity reactions.

3
  Co-morbidities. Caution should be used in the following instances: any
condition that can be exacerbated by electrolyte or acid-based
imbalance to prevent exacerbations and serious adverse effects;
any electrolyte imbalance, which could be exacerbated by the
electrolyte-changing effects of these drugs; GI obstruction which
could cause systemic absorption of the drugs and increase adverse
effects; renal dysfunction, which could lead to electrolyte disturbance
if any absorbed antacid is neutralized properly.
 Pregnancy and lactation. Antacids are contraindicated for pregnant
and lactating women because of the potential for adverse effects on
the fetus or neonate.

Adverse effects
Adverse effects when using antacids include:

 GI: Gastric rupture.
 Systemic alkalosis: headache, nausea, irritability, weakness,
tetany, confusion.
 Misc: Hypokalemia.

Interactions
Antacids can greatly affect the absorption of drugs from the GI tract.

 Alkalinity. Most drugs are prepared for an acidic environment, and an

alkaline environment can prevent them from being broken down for
absorption or can actually neutralize them so that they cannot be
absorbed.

4
Nursing considerations
Nursing considerations for a patient using antacids include the following:

Nursing Assessment
History taking and physical exam in a patient using antacids include:

 Assess for possible contraindications and cautions: any history of

allergy to antacids to prevent hypersensitivity reactions; renal
dysfunction, which might interfere with the drug’s excretion;
electrolyte disturbances, which could be exacerbated by effects of the
drug; and current status of pregnancy or lactation due to possible
effects on the fetus or newborn.
 Perform a physical examination to establish baseline data before
beginning therapy, determine the effectiveness of the therapy, and
evaluate for any potential adverse effects associated with the drug.
 Inspect the abdomen; auscultate bowel sounds to ensure GI motility.
 Assess mucous membrane status to evaluate potential problems with
absorption and hydration.
 Monitor laboratory test results, including serum electrolyte levels and
renal function tests, to monitor for adverse effects of the drug and
potential alterations in excretion that may necessitate dose
adjustment.

Nursing Diagnosis and Care Planning

Nursing diagnoses related to drug therapy might include the following:

 Diarrhea related to GI effects.
 Risk for constipation related to GI effects.

5
  Imbalanced nutrition: less than body requirementsrelated to GI
effects.
 Risk for imbalanced fluid volume related to systemic effects.
 Deficient knowledge regarding drug therapy.

Nursing Implementation with Rationale

The nursing interventions for patients using antacids are:

 Adequate drug absorption. Administer the drug apart from any other
oral medications approximately 1 hour before or 2 hours after to
ensure adequate absorption of the other medications.
 Ensure therapeutic levels. Have the patient chew tablets thoroughly
and follow with water to ensure that therapeutic levels reach the
stomach to decrease acidity.
 Perform diagnostic testing. Obtain specimens for periodic monitoring
of serum electrolytes to evaluate drug effects.
 Prevent imbalances. Assess the patient for any signs of acid-base or
electrolyte imbalance to ensure early detection and prompt
interventions.
 Institute a bowel program. Monitor the patient for diarrhea or
constipation to institute a bowel program before severe effects occur.
 Ensure adequate nutritional status. Monitor the patient’s nutritional
status if diarrhea is severe or constipation leads to decreased food
intake to ensure adequate fluid and nutritional intake to promote
healing and GI stability.
 Provide patient support. Offer support and encouragement to help
the patient cope with the disease and the drug regimen.
 Educate the patient. Provide thorough patient teaching, including the
drug name and prescribed dose, schedule for administration, signs
and symptoms of adverse effects and measures to prevent or

6
 minimize them, warning signs that may indicate possible problems
and the need to notify the health care provider immediately.

Evaluation
Evaluation of a patient using antacids include:

 Monitor patient response to the drug (relief of GI symptoms caused

by hyperacidity).
 Monitor for adverse effects (GI effects, imbalances in serum
electrolyte, and acid-base status).
 Evaluate the effectiveness of the teaching plan (patient can name the
drug and dosage, as well as describe the adverse effects to watch for,
specific measures to avoid them, and measures to take to increase the
effectiveness of the drug).
 Monitor the effectiveness of comfort measures and compliance with
the regimen.

Histamine-2 Antagonists
Histamine-2 (H2) receptor antagonists block the release of acid in response to
gastrin or parasympathetic release

Histamine-2 Antagonist: Generic and Brand Names

 A table of the most commonly used H2 antagonists.

7
 Classification Generic name Brand name

cimetidine Tagamet

ranitidine Zantac
Histamine-2 antagonists
famotidine Pepcid

nizatidine Axid

Histamine-2 antagonists block the release of hydrochloric acid in response to

gastrin.

 These drugs include cimetidine (Tagamet), ranitidine (Zantac),

famotidine (Pepcid), and nizatidine (Axid).

Therapeutic actions
The desired actions of H2 antagonists include the following:

 Selectively block H2 receptors located on the parietal cells.

 Prevents the release of gastrin, a hormone that causes local release of
histamine (due to stimulation of histamine receptors), ultimately
blocking the production of hydrochloric acid.
 Decreases pepsin production by the chief cells.

Indication
Histamine-2 antagonists are indicated for the following:

 Short-term treatment of active duodenal ulcer or benign gastric ulcer.

8
  Treatment of pathological hypersecretory conditions such as
Zollinger-Ellison syndrome (blocking the overproduction of
hydrochloric acid that is associated with these conditions).
 Prophylaxis of stress-induced ulcers and acute upper GI bleeding in
critical patients (blocking the production of acid protects
the stomach lining, which is at risk because of decreased mucus
production associated with extreme stress).
 Treatment of erosive gastroesophageal reflux (decreasing the acid being
regurgitated into the esophagus will promote healing and decrease
pain).
 Relief of symptoms of heartburn, acid indigestion, and sour stomach.

Pharmacokinetics
Cimetidine, ranitidine, and famotidine are available in oral and parenteral forms

Route Onset Peak Duration

Oral Varies 1-1.5 h 4-5 h

IM, IV Rapid 1-1.5 h 4-5 h

T 1/2: 2 hours

Metabolization: Liver

Excretion: Urine

Contraindications and Cautions

The contraindications and cautions when using H2 antagonists include:

9
  Allergy. The H2 antagonists should not be used with known allergy to any
drugs of this class to prevent hypersensitivity reactions.
 Pregnancy or lactation. Caution should be used during pregnancy or
lactation because of the potential for adverse effects on the fetus or
nursing baby.
 Hepatic or renal dysfunction. Caution should be used in patients with
hepatic or renal dysfunction, which could interfere with drug
metabolism and excretion.
 Prolonged or continual use. Care should also be taken if prolonged or
continual use of these drugs is necessary because they may be
masking serious underlying conditions.

Adverse effects
The adverse effects associated with H2 antagonists are:

 CNS: Dizziness, confusion, headache, somnolence.

 Cardio: Cardiac arrhythmias, cardiac arrest.
 GI: Diarrhea.
 Reproductive: Impotence.
 Skin: Rash.
 Misc: Gynecomastia.

Interactions
Cimetidine, famotidine, and ranitidine can slow down the metabolism of the
following drugs, leading to increased serum levels and possible toxic reactions:

 Warfarin.

 Anti-coagulants.

10
  Phenytoin.

 Beta-adrenergic blockers.
 Alcohol.
 Quinidine.
 Lidocaine.

 Theophylline.
 Chloroquine.

 Benzodiazepines.
 Nifedipine.

 Pentoxifylline.
 TCAs.
 Procainamide.
 Carbamazepine.

Nursing Considerations
Nursing considerations for a patient using H2 antagonists include the following:

Nursing Assessment
Nursing assessment for a patient using H2 antagonists include:

 Assess for possible contraindications and cautions: history of allergy

to any H2 antagonists to prevent potential allergic reactions; impaired
renal or hepatic function, which could affect the metabolism and
excretion of the drug; a detailed description of the GI problem,
including length of time of the disorder and medical evaluation to
evaluate the appropriate use of the drug and possibility of underlying
medical problems; and current status of pregnancy and lactation
because of the potential for adverse effects on the fetus or newborn.

11
  Perform a physical examination to establish baseline data before
beginning therapy, determine effectiveness of the therapy, and
evaluate for any adverse effects associated with drug therapy.
 Inspect the skin for evidence of lesions or rash to monitor for adverse
reactions.
 Evaluate neurological status, including orientation and affect, to
assess CNS effects of the drug and to plan for protective measures.
 Assess cardiopulmonary status, including pulse, blood pressure, and
electrocardiogram (if IV use is needed), to evaluate the cardiac effects
of the drug.
 Perform abdominal examination, including assessment of the liver, to
establish a baseline and rule out underlying medical problem.
 Monitor the results of laboratory tests, including liver and renal
function tests, to predict changes in metabolism or excretion of the
drug that might require dose adjustment.

Nursing Diagnosis and Care Planning

Nursing diagnosis related to the drug therapy might include the following:

 Acute pain related to CNS and GI effects.

 Disturbed sensory perception (kinesthetic, auditory) related to CNS

effects.
 Decreased cardiac output related to cardiac arrhythmias.

 Risk for injury related to CNS effects.

 Deficient knowledge regarding drug therapy.

Nursing Implementation with Rationale

Nursing interventions for patients using H2 antagonists include:

12
  Ensure therapeutic levels. Administer drug with or before meals and at
bedtime (exact timing varies with product) to ensure therapeutic
levels when the drug is most needed.
 Prevent serious toxicity. Arrange for decreased dose in cases of
hepatic or renal dysfunction to prevent serious toxicity.
 Monitor IV doses carefully. Monitor the patient continually if giving IV
doses to allow early detection of potentially serious adverse effects,
including cardiac arrhythmias
 Assess for potential drug-drug interactions. Assess the patient
carefully for any potential drug-drug interactions if given in
combination with other drugs because of the drug’s effects on liver
enzyme systems.
 Provide patient’s comfort. Provide comfort, including analgesics, ready to
access bathroom facilities, and assistance with ambulation, to
minimize possible adverse effects.
 Reorient patient thoroughly. Periodically reorient the patient and
institute safety measures if CNS effects occur to ensure patient safety
and improve and improve patient tolerance of the drug and drug
effects.
 Attend regular follow-ups. Arrange for regular follow-up to evaluate
drug effects and the underlying problems.
 Provide support. Offer support and encouragement to help patients
cope with the disease and the drug regimen.
 Educate the client. Provide patient teaching regarding drug name,
dosage, and schedule for administration; importance of spacing
administration appropriately as ordered; need for readily available
access to bathroom; signs and symptoms of adverse effects and
measures to minimize or prevent them.

Evaluation
Evaluation of a patient using H2 antagonists include:

13
  Monitor patient response to the drug (relief of GI symptoms, ulcer
healing, prevention of progression of ulcer).
 Monitor for adverse effects (dizziness, confusion, hallucinations, GI
alterations, cardiac arrhythmias, hypotension, gynecomastia).
 Evaluate the effectiveness of the teaching plan (patient can name
drug, dosage, adverse effects to watch for, and specific measures to
avoid them).
 Monitor the effectiveness of comfort measures and compliance with
the regimen.

Proton Pump Inhibitors

The gastric acid pump or proton pump inhibitorssuppress gastric acid
secretion by specifically inhibiting the hydrogen-potassium adenosine
triphosphate enzyme system on the secretory surface of the gastric parietal
cells.

Proton Pump Inhibitors: Generic and Brand Names

Atable of the most commonly encountered proton pump inhibitor:

Classification Generic name Brand name

Proton pump dexlansoprazole Kapidex

inhibitors
esomeprazole Nexium

lansoprazole Prevacid

omeprazole Prilosec

14
 pantoprazole Protonix

rabeprazole Aciphex

Disease spotlight: Gastroesophageal Reflux

Gastroesophageal reflux disease (GERD) occurs when stomach acid frequently
flows back into the tube connecting the mouth and the stomach (esophagus).

 GERD is a mild acid reflux that occurs at least twice a week, or

moderate to severe acid reflux that occurs at least once a week.
 Common signs and symptoms of GERD include a burning sensation in
the chest (heartburn), usually after eating, which might be worse at
night; chest pain; difficulty swallowing; regurgitation of food or sour
liquid; and a sensation of a lump in your throat.

What are Proton Pump Inhibitors?

Proton pump inhibitors suppress the secretion of hydrochloric acid into the
lumen of the stomach.

Therapeutic actions
The desired actions of antacids include the following:

 Blocks the final step of acid production, lowering the acid levels in the
stomach.

15
  Inhibits the hydrogen-potassium adenosine triphosphate enzyme
system on the secretory surface of the gastric parietal cells.

Indication
Antacids are indicated for the following:

 Treatment and maintenance of erosive esophagitis, treatment of

heartburn associated with GERD.
 Treatment of GERD, severe erosive esophagitis, duodenal ulcers, and
pathological hypersecretory condition.
 Treatment of gastric ulcer.
 Maintenance therapy for healing duodenal ulcers and esophagitis.
 In combination therapy for eradicating Helicobacter pylori infection.
 Approved for use in children for treatment of GERD, peptic ulcer, and
Zollinger-Ellison syndrome.

Pharmacokinetics
Esomeprazole, lansoprazole, and pantoprazole are available in delayed-release
oral forms and as IV preparations; rabeprazole, dexlansoprazole, and
omeprazole are available only in delayed-release oral forms.

Route Onset Peak Duration

Oral Varies 0.5-3.5h Varies

T 1/2: 30 to 60 mins

Metabolization: Liver

16
Excretion: Urine and bile

Contraindications and Cautions

The following are contraindications and cautions when using proton pump
inhibitors:

 Allergy. These drugs are contraindicated in the presence of a

known allergy to either the drug or the drug components to prevent
hypersensitivity reactions.
 Pregnant or lactating women. Caution should be used in pregnant or
lactating women because of the potential for adverse effects on the
fetus or neonate.
 Patients 18 years old and below. The safety and efficacy of these drugs
have not been established for patients younger than 18 years of age,
except for lansoprazole, which is the proton pump inhibitor of choice
if one is needed for a child.

Adverse effects
Adverse effects when using proton pump inhibitors include:

 CNS: Headache, dizziness, vertigo, insomnia.

 Skin: Rash.
 GI: Diarrhea, abdominal pain, nausea, vomiting.
 Respiratory: Upper respiratory infections, cough.

17
Interactions
Clinically important drug to drug interactions for proton pump inhibitors
include the following drugs:

 Benzodiazepines, phenytoin, warfarin: There is a risk of increased

serum levels and increased toxicity of benzodiazepines, warfarin, and
phenytoin if these are combined with these drugs; patients should be
monitored closely.
 Ketoconazole and theophylline. Decreased levels of ketoconazole and
theophylline have been reported when combined with these drugs,
leading to loss of effectiveness.
 Sucralfate. Sucralfate is not absorbed well in the presence of these
drugs, and doses should be spaced at least 30 minutes apart if this
combination is used.
 Clopidogrel. There is an increased risk of cardiovascular events if
proton pump inhibitors are combined with clopidogrel; this
combination should be avoided.

Nursing considerations
Nursing considerations when using proton pump inhibitors include the
following:

Nursing Assessment
History taking and physical examination of a patient using proton pump
inhibitors include:

 Assess for possible contraindications and cautions: history of allergy

to a proton pump inhibitor to reduce the risk of hypersensitivity
reaction and current status of pregnancyor lactation because of the
potential for adverse effects on the fetus or nursing baby.
18
  Perform a physical examination to establish baseline data before
beginning therapy to determine the effectiveness of the therapy and
to evaluate for the occurrence of any adverse effects associated with
drug therapy.
 Inspect the skin for lesions, rash, pruritus, and dryness to identify
possible adverse effects.
 Assess neurological status, including level of orientation, affect and
reflexes to evaluate for CNS effects of the drug.
 Inspect and palpate the abdomen to determine potential underlying
medical conditions; assess for changes in bowel elimination and GI
upset to identify possible adverse effects.
 Assess respiratory status, including respiratory rate and rhythm; note
evidence of cough, hoarseness, and epistaxis, to monitor for potential
adverse effects of the drugs.

Nursing Diagnosis and Care Planning

Nursing diagnoses related to drug therapy might include the following:

 Diarrhea related to GI effects.
 Risk for constipation related to GI effects.
 Imbalanced nutrition: less than body requirementsrelated to GI
effects.
 Disturbed sensory perception (kinesthetic, auditory) related to CNS
effects.
 Risk for injury related to CNS effects.
 Deficient knowledge regarding drug therapy.

Nursing Implementation with Rationale

Nursing interventions for patients using proton pump inhibitors include the
following:
19
  Proper administration. Administer drug before meals to ensure that
the patient does not open, chew, or crush capsules; they should be
swallowed whole to ensure the therapeutic effectiveness of the drug.
 Safety and comfort measures. Provide appropriate safety and
comfort measures if CNS effects occur to prevent patient injury.
 Institute a bowel program. Monitor the patient for diarrhea or
constipation in order to institute an appropriate bowel program as
needed.
 Monitor nutritional status. Monitor the patient’s nutritional status;
use of small frequent meals may be helpful if GI upset is a problem.
 Ensure follow-up. Arrange for medical follow-up if symptoms are not
resolved after 4 to 8 weeks of therapy because serious underlying
conditions could be causing the symptoms.
 Provide patient support. Offer support and encouragement to help
the patient cope with the disease and the drug regimen.
 Educate the patient and folks. Provide thorough patient teaching,
including the drug name and prescribed dosage; the importance of
taking the drug whole without opening, chewing, or crushing it; signs
and symptoms of possible adverse effects and measures to minimize
or prevent them.

Evaluation
Evaluation of a patient using proton pump inhibitors include the following:

 Monitor patient response to the drug (relief of GI symptoms caused

by hyperacidity, healing of erosive GI lesions).
 Monitor for adverse effects (GI effects, CNS changes, dermatological
effects, respiratory effects).
 Monitor the effectiveness of comfort and safety measures and
compliance with the regimen.

20
  Evaluate the effectiveness of the teaching plan (patient can name the
drug and dosage and describe adverse effects to watch for, specific
measures to avoid them, and measures to take to increase the
effectiveness of the drug).
Endocrine System Drugs

Antidiabetic Agents
Antidiabetic drugs are a group of drug structurally unrelated
to sulfonylureas and are effective when used in combination with insulin or
sulfonylureas. These drugs include alpha-glucosidase inhibitors, biguanides,
dipeptidyl peptidase-4 (DPP-4) inhibitors, human amylin, incretin mimetics,
meglitinides, and thiazolidinediones.

Antidiabetic Agents: Generic and Brand Names

A table of commonly encountered other antidiabetic agents, their generic
names, and brand names:

Classifications Generic Name Brand Name

acarbose Precose,
Alpha-glucosidase miglitol Glyset
inhibitors
miglitol Glyset

Biguanide metformin Glucophage

Dipeptidyl peptidase-4- linagliptin Tradjenta

inhibitors
saxagliptin Onglyza

21
 sitagliptin Januvia

pramlintide
Human amylin Symlin
acetate

exenatide Baraclude
Incretin mimetics
liraglutide Victoza

nateglinide Starlix
Meglitinides
repaglinide Prandin

pioglitazone Actos
Thiazolidinediones
rosiglitazone Avandia

Therapeutic Action
The desired and beneficial action of other antidiabetic agents:

 Alpha-glucosidase inhibitors acarbose and miglitol inhibit alpha-

glucosidase, an enzyme that breaks down glucose for absorption.
Therefore, they delay the absorption of glucose. They have only a mild
effect on glucose levels and do not enhance insulin secretion. They are
associated with severe hepatic toxicity and GI distress.
 Biguanide metformin decrease the production and increases the
uptake of glucose. It is effective in lowering blood glucose and does
not cause hypoglycemia as the sulfonylureas do. It has been
associated with development of lactic acidosis and GI distress.

22
  Meglitinides nateglinide and repaglinide are newer agents that act like
sulfonylureas to increase insulin release.
 Synthetic human amylin pramlintide works to modulate gastric
emptying after a meal to cause a feeling of fullness or satiety. It also
prevents the postmeal rise in glucagon that usually elevates glucose
levels. Human amylin is a hormone produced by beta cells in
the pancreas that is important in regulating postmeal glucose levels. It
should not be used when patient is unable to eat.
 Incretin mimetics exenatide and liraglutide mimic the effects of GLP-1:
enhancement of glucose-dependent insulin secretion by the beta cells
in the pancreas, depression of elevated glucagon secretion, and
slowed gastric emptying to help moderate and lower blood glucose
levels.
 DPP-4 inhibitors lina-, saxa-, and sitagliptin slow the breakdown of
GLP-1 to prolong the effects of increased insulin secretion, decreased
glucagon secretion, and slowed GI emptying.
 Thiazolidinediones pioglitazone and rosiglitazone decrease insulin
resistance.

Indications
Other antidiabetic agents are indicated for the following medical conditions:

 Biguanide metformin is approved for use in children 10 years of age

and older. It is also being used in the treatment of women with
polycystic ovarian syndrome (PCOS).
 Meglitinides nateglinide and repaglinide are used to lower
postprandial glucose levels because they are rapid-acting and with a
very short half-life. They are taken just before meals.
 Thiazolidinediones pioglitazone and rosiglitazone are used in
combination with insulin, metformin, and sulfonylureas in patients
with insulin resistance.

23
  Bromocriptine, a dopamine agonist used to treat Parkinson’s disease
was approved in 2009 as a CNS approach to treat type 2 diabetes.

Pharmacokinetics
Here are the characteristic interactions of other antidiabetic agents and the
body in terms of absorption, distribution, metabolism, and excretion:

Route Onset Peak Duration

Oral Slow 2-2.5 h 10-16 h

T1/2: 6.2 h and then 17 h

Metabolism: liver
Excretion: urine

Contraindications and Cautions

The following are contraindications and cautions for the use of agents to
control blood glucose level:

 Allergy to sulfonylureas and other antidiabetic agents. Avoid

hypersensitivity reactions
 Type 1 diabetes. These patients do not have functioning beta cells and
would have no benefit from the drug.
 Pregnancy and lactation. Potential adverse effect on the fetus or
neonate.

Adverse Effects
Use of other antidiabetic agents may result to these adverse effects:
24
  Common adverse effects include hypoglycemia, lactic acidosis, GI
upset, nausea, anorexia, diarrhea, heartburn, and allergic skin
reaction.
 Pioglitazone is strongly linked with an increased risk
of bladder cancer if it is used for over 1 year.
 Rosiglitazone is linked with increased risk of cardiovascular problems.

Interactions
The following are drug-drug interactions involved in the use of other
antidiabetic agents:

 decreased excretion with drugs that acidify urine

Glucose-Elevating Agents
Glucose-elevating agents raise blood level of glucose when severe
hypoglycemia occurs at <40 mg/dL. Two agents are used to elevate glucose:
diazoxide and glucagon.

Glucose-Elevating Agents: Generic and Brand

Names
A table of commonly encountered glucose-elevating agents, their generic
names, and brand names:

Classification Generic Name Brand Name

Glucose-elevating diazoxide Proglycem,

agents Hyperstat

25
 glucagon GlucaGen

Therapeutic Action
The desired and beneficial action of glucose-elevating agents:

 Increasing blood glucose by decreasing insulin release and

accelerating the breakdown of glycogen in the liver to release glucose.

Indications
Glucose-elevating agents are indicated for the following medical conditions:

 Diazoxide is an oral management of hypoglycemia; intravenous use

for management of severe hypertension.
 Glucagon is used to counteract severe hypoglycemic reactions.

Pharmacokinetics
Here are the characteristic interactions of glucose-elevating agents and the
body in terms of absorption, distribution, metabolism, and excretion:

Route Onset Peak Duration

IV 1 min 15 min 9-20 min

T1/2: 3-10 min

Metabolism: liver
Excretion: bile, urine

26
Contraindications and Cautions
The following are contraindications and cautions for the use of glucose-
elevating agents:

 Diazoxide is contraindicated with known allergies to sulfonamides or

thiazides.
 Pregnancy and lactation. Associated with adverse effects to fetus and
baby.
 There are no adequate studies on glucagon and pregnancy, so use
should be reserved for those situations in which the benefits to the
mother outweigh any potential risks to the fetus.
 Caution should be used in patients with renal or hepatic dysfunction or
cardiovascular disease.

Adverse Effects
Use of glucose-elevating agents may result to these adverse effects:

 Glucagon is associated with GI upset, nausea, and vomiting.

 Diazoxide is associated with vascular effects, including hypotension,
headache, cerebral ischemia, weakness, heart failure, and arrhythmias.
This is because diazoxide has the ability to relax arteriolar
smooth muscle.

Interactions
The following are drug-drug interactions involved in the use of glucose-
elevating agents:

27
  Diazoxide with thiazide diuretics can increase risk of toxicity because
these two are structurally the same.
 Glucagon with oral anticoagulants will increase anticoagulation effects.

Nursing Considerations
Here are important nursing considerations when administering glucose-
elevating agents:

Nursing Assessment
These are the important things the nurse should include in conducting
assessment, history taking, and examination:

 Assess for contraindications and cautions: history of allergy, renal and

hepatic dysfunction, pregnancy to avoid adverse effects.
 Perform a complete physical assessment to establish a baseline before
beginning therapy, monitor effectiveness of therapy, and evaluate for
any potential adverse effects during therapy.
 Assess orientation and reflexes and baseline pulse, blood pressure, and
adventitious sounds to monitor the effects of altered glucose levels,
and abdominal sounds and function, which could be altered by these
drugs.
 Monitor blood glucose levels as ordered to assess the effectiveness of
the drug and patient response to treatment.
 Monitor the results of laboratory tests, including urinalysis, to
evaluate for glucosuria, serum glucose to evaluate response to
therapy, and renal and liver function tests to determine the need for
possible dose adjustment or identify possible toxic effects.

28
Nursing Diagnoses and Care Planning
Here are some of the nursing diagnoses that can be formulated in the use of this
drug for therapy:

 Risk for unstable blood glucose related to ineffective dosing of the

drug
 Imbalanced nutrition: more than body requirements related to metabolic
effects

Nursing Implementation with Rationale

These are vital nursing interventions done in patients who are taking glucose-
elevating agents:

 Monitor blood glucose levels to evaluate the effectiveness of the

drug.
 Have insulin on standby during emergency use to treat
severe hyperglycemia if it occurs as a result of overdose.
 Monitor nutritional status to provide nutritional consultation as
needed.
 Monitor patients receiving diazoxide for potential cardiovascular
effects, including blood pressure, heart rhythm and output, and
weight changes, to avert serious adverse reactions.
 Provide comfort measures to help patient cope with drug effects.
 Provide patient education about drug effects and warning signs to
report to enhance patient knowledge and to promote compliance.

Evaluation
Here are aspects of care that should be evaluated to determine effectiveness
of drug therapy:

29
  Monitor patient response to therapy (stabilization of blood glucose
levels).
 Monitor for adverse effects (hyperglycemia and GI distress).
 Evaluate patient understanding on drug therapy by asking patient to
name the drug, its indication, and adverse effects to watch for.
 Monitor patient compliance to drug therapy.

Insulin
Insulin is a drug that is used to control glucose in patients with diabetes
mellitus. It is the only parenteral antidiabetic agent available for exogenous
replacement of low levels of insulin.

Insulin is the hormone produced by the pancreatic beta cells of the islets of
Langerhans. It is released into circulation when the levels of glucose around
the cells arise. Insulin circulates through the body and reacts with specific
insulin receptor sites to stimulate the transport of glucose into cells to be used
for energy (facilitated diffusion).

Originally prepared from pork and beef pancreas , virtually all insulin is

prepared by recombinant DNA technology now. This is a purer form of insulin
and is not associated with sensitivity problems that many patients developed
with the animal products.

Disease Spotlight: Diabetes Mellitus

 Diabetes Mellitus (literally, “honey urine”) is a condition wherein
there is a complex disturbance in the metabolism of carbohydrates,
proteins, and fats. This alteration results in thickening of the layer
below the endothelial lining of the blood vessels. This, in turn, causes

30
 narrowing, vessel remodeling, and decreased blood flow through
vessels.
 Most frequent clinical signs include hyperglycemia (fasting blood
sugar of >106 mg/dL) and the presence of sugar in the urine
(glycosuria).
 Diabetes is classified into two: type 1 and type 2. Type 1 diabetes is
common in younger people and is connected with cases of viral
destruction of beta cells of the pancreas. On the other hand, type 2 is
adult-onset and is associated with not enough insulin to maintain
glucose control.
 Hyperglycemia (high blood sugar) results when there is an increase in
glucose in the blood. Clinical signs and symptoms include fatigue,
lethargy, irritation, glycosuria, polyphagia, polydipsia, and itchy skin
(from the accumulation of wastes that liver cannot clear).
 Hypoglycemia is a blood glucose concentration lower than 40 mg/dL
and can occur in many clinical situations like starvation and
overtreatment of hyperglycemia. Manifestations include headache,
paresthesias, hunger, and diaphoresis.

Therapeutic Action
The desired and beneficial action of insulin is:

 Insulin replaces endogenous insulin. It is the only parenteral

antidiabetic agent available for exogenous replacement of low levels
of insulin. It reacts with the receptors of the cells to facilitate
transport of various metabolites and ions across cell membranes and
stimulates the synthesis of glycogen from glucose, of fats from lipids,
and of proteins from amino acids.

Indications
Insulin is indicated for the following medical conditions:

31
  Treatment of type 1 diabetes
 Treatment of type 2 diabetes when other agents have failed
 Short-term treatment of type 2 diabetes during periods of stress
 Management of diabetic ketoacidosis, hyperkalemia, and marked
insulin resistance

Pharmacokinetics
Here are the characteristic interactions of insulin and the body in terms of
absorption, distribution, metabolism, and excretion:

Route Onset Peak Duration

Regular 30-60 min 2-4 h 6-12 h

NPH
1-1.5 h 4-12 h 24 h
(Humulin N)

Ultralente
(Humulin 4-8 h 10-30 h 20-36 h
Ultralente)

Lispro
<15 min 30-90 min 2-5 h
(Humalog)

Aspart
10-20 min 1-3 h 3-5 h
(Novolog)

Glargine
60-70 min None 24 h
(Lantus)

32
 Glulisine
2-5 min 30-90 min 2h
(Apidra)

Detemir
1-2 h 3-6 h 5.7-23.3 h
(Levemir)

T1/2: varies with each preparation

Metabolism: cellular level
Excretion: –

Contraindications and Cautions

The following are contraindications and cautions for the use of insulin:

 No contraindications as it is a replacement hormone. However, close

monitoring is needed among pregnant and lactating women to adjust
the dose accordingly. It is the drug of choice for management of
diabetes during pregnancy.
 Insulin does enter breast milk but it is destroyed in the GI tract and
does not affect the nursing infant.
 Insulin-dependent mothers may have inhibited milk production
because of insulin’s effects on fat and protein metabolism.

Adverse Effects
Use of insulin may result in these adverse effects:

 hypoglycemia and ketoacidosis

 local reactions at the injection site (lipodystrophy).

33
Interactions
The following are drug-drug interactions involved in the use of insulin:

 MAOIs, beta blockers, salicylates, alcohol. Increased glucose

reduction
 Beta blockers. Blocking the SNS also blocks many of the signs and
symptoms of hypoglycemia, hindering the patient’s ability to
recognize problems.
 Various herbal therapies (juniper berries, ginseng, garlic, fenugreek,
coriander, dandelion root, celery). Increased risk of developing
hypoglycemia.  

Nursing Considerations
Here are important nursing considerations when administering insulin:

Nursing Assessment
These are the important things the nurse should include in conducting
assessment, history taking, and examination:

 Assess for contraindications or cautions (e.g. history of allergy,

pregnancy, etc.)  so that appropriate monitoring and dose adjustments
can be completed.
 Perform a physical assessment to establish a baseline before beginning
therapy.
 Assess skin lesions; orientation and reflexes; blood pressure, pulse,
respiration and adventitious breath sounds  which could indicate a
response to high or low glucose levels and potential risk factors in giving
insulin.

34
  Inspect skin areas that will be used for injection; note any areas that
are bruised, thickened, or scarred, which could interfere with insulin
absorption and alter anticipated response to insulin therapy.
 Obtain blood glucose levels as ordered to monitor response to insulin.
 Assess activity level, including amount and degree of exercise which
can alter serum glucose levels and need for these drugs.
 Monitor the results of laboratory tests, including urinalysis, for
evidence of glucosuria.

Nursing Diagnoses and Care Planning

Here are some of the nursing diagnoses that can be formulated in the use of
this drug for therapy:

 Risk for unstable blood glucose related to ineffective dosing of

antidiabetic agents
 Imbalanced nutrition: less than body requirements related to the use
of insulin and underlying disease process
 Risk for infection related to glucose levels

Nursing Implementation with Rationale

These are vital nursing interventions done in patients who are taking insulin:

 Ensure that patient has dietary and exercise regimen and using good
hygiene practices to improve the effectiveness of the insulin and
decrease adverse effects of the disease.
 Monitor nutritional status to provide nutritional consultation as
needed.
 Gently rotate the vial containing the agent and avoid vigorous
shaking to ensure uniform suspension of insulin.

35
  Rotate injection sites to avoid damage to muscles and to prevent
subcutaneous atrophy.
 Monitor response carefully to avoid adverse effects.
 Always verify the name of the insulin being given because each insulin
has a different peak and duration, and the names can be confused.
 Use caution when mixing types of insulin; administer mixtures of
regular and NPH insulins within 15 minutes after combining them to
ensure appropriate suspension and therapeutic effect.
 Store insulin in a cool place away from direct sunlight to ensure
effectiveness.  Predrawn syringes are stable for 1 week if refrigerated.
 Monitor patient’s food intake and exercise and activities to ensure
therapeutic effect and avoid hypoglycemia.
 Monitor patient’s sensory losses to incorporate his or her needs into
safety issues, as well as potential problems in drawing up and
administering insulin.
 Provide good skin care and foot care, to prevent the development of
serious infections and changes in therapeutic insulin doses.
 Provide comfort measures to help patient cope with drug effects.
 Provide patient education about drug effects and warning signs to
report to enhance patient knowledge and to promote compliance.    

Evaluation
Here are aspects of care that should be evaluated to determine the
effectiveness of drug therapy:

 Monitor patient response to therapy (stabilization of blood glucose

levels).
 Monitor for adverse effects (hypoglycemia, ketoacidosis, injection-site
irritation).

36
  Evaluate patient understanding on drug therapy by asking the patient
to name the drug, its indication, and adverse effects to watch for.
 Monitor patient compliance to drug therapy.

Sulfonylureas
Sulfonylureas are another group of agent used to control blood glucose level.
These drugs are only effective in patients who have functioning beta cells. They
are not effective for all diabetics and may lose their effectiveness over time
with others.

Sulfonylureas are further classified as first-generation or second-generation

sulfonylureas.

Use of first-generation sulfonylureas is declining as more effective drugs have

become available. Also, they are now thought to possibly cause an increase in
cardiovascular death.

Use of second-generation sulfonylureas have several advantages over first-

generation, including: safer for patients with renal dysfunction as they are
excreted in urine and bile, absence of interaction to many protein-bound drugs,
and longer duration of action.

All of sulfonylureas can cause hypoglycemia.

Sulfonylureas: Generic and Brand Names

Here is a table of commonly encountered sulfonylureas, their generic names,
and brand names:

37
 Classification Generic Name Brand Name

chlorpropamide Diabinese

First-generation tolazamide Tolinase

tolbutamide Orinase

glimepiride Amaryl

Second- glipizide Glucotrol

generation
DiaBeta,
glyburide
Micronase

Therapeutic Action
The desired and beneficial action of sulfonylureas:

 Sulfonylureas stimulate insulin release from the beta cells in pancreas.

They improve insulin binding to insulin receptors and may actually
increase the number of insulin receptors.
 They are also known to increase the effect of antidiuretic hormone on
renal cells.

Indications
Sulfonylureas are indicated for the following medical conditions:

 Sulfonylureas are used as adjunct to diet and exercise for the

treatment of type 2 diabetes older than 10 years of age; extended

38
 release form for patients older than 17 years of age; adjunct treatment
with polycystic ovary syndrome.

Pharmacokinetics
Here are the characteristic interactions of sulfonylureas and the body in terms
of absorption, distribution, metabolism, and excretion:

Route Onset Peak Duration

Oral Slow 2-2.5 h 10-16 h

T1/2: 6.2-17 h
Metabolism: liver
Excretion: urine

Contraindications and Cautions

The following are contraindications and cautions for the use of sulfonylureas:

 Allergy to sulfonylureas. Avoid hypersensitivity reactions

 Type 1 diabetes. These patients do not have functioning beta cells and

would have no benefit from the drug.
 Pregnancy and lactation. Potential adverse effect on the fetus or
neonate.

Adverse Effects
Use of sulfonylureas may result to these adverse effects:

 Hypoglycemia (most common)

39
  GI distress (nausea, vomiting, epigastric discomfort)
 Allergic skin reactions

Interactions
The following are drug-drug interactions involved in the use of sulfonylureas:

 Decreased excretion with drugs that acidify urine

Nursing Considerations
Here are important nursing considerations when administering agents to
control blood glucose level:

Nursing Assessment
These are the important things the nurse should include in conducting
assessment, history taking, and examination:

 Assess for contraindications or cautions (e.g. history of allergy to the

drugs, pregnancy and lactation status, severe renal or hepatic
dysfunction, etc.) which are contraindications in the use of these
agents.
 Perform a complete physical assessment to establish baseline status
before beginning therapy and to evaluate effectiveness and any
potential adverse effects during therapy.
 Assess orientation and reflexes; baseline pulse and blood pressure;
adventitious breath sounds; abdominal sounds and function, to
monitor effects of altered glucose levels.
 Assess body systems for changes suggesting possible complications
associated with poor blood glucose control.

40
  Investigate nutritional intake, noting any problems with intake and
adherence to prescribed diet, to help prevent adverse reactions to
drug therapy.
 Assess activity level, including amount and degree of exercise, which
can alter serum glucose levels and dosage needs for these drugs.
 Monitor blood glucose levels as ordered to evaluate effectiveness of
drug and glycemic control.
 Monitor results of laboratory tests, including urinalysis, for evidence
of glycosuria, and renal and liver function tests, to determine the need
for possible dose adjustment and evaluate for signs of toxicity.

Nursing Diagnoses and Care Planning

Here are some of the nursing diagnoses that can be formulated in the use of this
drug for therapy:

 Risk for unstable blood glucose related to ineffective dosing

of antidiabetic agents
 Imbalanced nutrition: less than body requirements related to metabolic
effects
 Disturbed sensory perception: kinesthetic, visual, auditory, and tactile
related to glucose levels

Implementation with Rationale

These are vital nursing interventions done in patients who are taking
sulfonylureas:

 Administer the drug as prescribed in the appropriate relationship to

meals to ensure therapeutic effectiveness.
 Ensure that patient has dietary and exercise regimen and using good
hygiene practices to improve the effectiveness of the insulin and
decrease adverse effects of the disease.
41
  Monitor nutritional status to provide nutritional consultation as
needed.
 Monitor response carefully; blood glucose monitoring is the most
effective way to evaluate dose. Obtain blood glucose levels as ordered
to monitor drug effectiveness.
 Monitor patients during times of trauma, pregnancy, or severe stress,
and arrange to switch to insulin coverage as needed.
 Provide comfort measures to help patient cope with drug effects.
 Provide patient education about drug effects and warning signs to
report to enhance patient knowledge and to promote compliance.

Evaluation
Here are aspects of care that should be evaluated to determine effectiveness
of drug therapy:

 Monitor patient response to therapy (stabilization of blood glucose

levels).
 Monitor for adverse effects (hypoglycemia and gastrointestinal
distress).
 Evaluate patient understanding on drug therapy by asking patient to
name the drug, its indication, and adverse effects to watch for.
 Monitor patient compliance to drug therapy.

42