MODULE 8  Allergy to any component of the drug.

 To prevent
DRUGS ACTING ON THE ENDOCRINE
SYSTEM
Lesson 1: Hypothalamic and Pituitary agents
HYPOTHALMIC AGENTS
 Can inhibit or stimulate the release of hormones from
the anterior pituitary using hormones or factors.
 However, not all these hormones are available for
pharmacological use.
 Stimulating factors (agonists)
- include growth hormone-releasing hormone
(GHRH), thyrotropin-releasing hormone
(TRH), gonadotropin-releasing hormone
(GnRH), corticotropin-releasing hormone
(CRH), and prolactin-releasing hormone
(PRH).
 Factors that inhibit (antagonists)
- include somatostatin (growth hormone-
inhibiting factor) and prolactin-inhibiting
factor.
hypersensitivity reactions.
 Peripheral vascular disorders. Can alter absorption
of drugs.
 Rhinitis. Alters absorption of nafarelin nasal spray.
 Renal or hepatic impairment. Interfere with drug
metabolism and excretion.
 Pregnancy or lactation. Potential adverse effects to
fetus or neonates.
Adverse Effects
 Agonists: increased release of sex hormones,
ovarian overstimulation, flushing, increased
temperature and appetite, fluid retention
 Antagonists: decreased testosterone level, loss of
energy, decreased sperm count and activity,
alterations in secondary sex characteristics (decrease
in female sex hormones, amenorrhea), fluid and
electrolyte changes, insomnia, irritability
PITUITARY DRUGS
Drugs that affect anterior pituitary hormones 
 mimic or antagonize the effects of specific pituitary
hormones. They are used as replacement therapy, for
diagnostic purposes, and for blocking the effects of
anterior pituitary hormones.
 The anterior pituitary hormone that is most commonly
used pharmacologically is growth hormone (GH).

Drugs Affecting Posterior Pituitary Hormones

 The posterior pituitary stores two hormones
produced by the hypothalamus (antidiuretic hormone
Therapeutic Action or vasopressin [ADH] and oxytocin).
 ADH possesses antidiuretic, hemostatic, and
 Not clearly identified as there are only minute
vasopressor properties. It is the hormone affected
quantities found.
in diabetes insipidus, a condition characterized by
 Not all of them are used as pharmacological agents.
production of a large amount of dilute urine containing
Some are used for diagnostic purposes only and
no glucose.
others are primarily used as antineoplastic agents.

Tesamorelin is used to stimulate GH and its lipolytic effects, Anterior Pituitary Hormone Drugs
helping to decrease the excess abdominal fat in HIV-infected
patients with lipodystrophy.

Indications
 Agonists like goserelin, histrelin, leuprolide, and
nafarelin are analogues of GnRH. They decrease
production of sex hormones. They are used as
treatment for precocious puberty, endometriosis, and
advanced prostate cancer.
 Antagonists of GnRH like degarelix and ganirelix are
used as treatment for advanced prostate cancer and
inhibition of premature LH surge in women
undergoing controlled ovarian stimulation for fertility.

Contraindications and Cautions

ANTERIOR PITUITARY HORMONE DRUGS
GROWTH HORMONES AGONISTS
1|Pascual, Airine A.
Growth Hormones Agonists – are responsible for linear
skeletal growth, growth of internal organs, protein synthesis,
and stimulation of processes required for normal growth.
Disease Spotlight: GH Deficiency
 Hypopituitarism
 Dwarfism
 Somatotropin deficiency syndrome (SDS)
Therapeutic Action
 replacing human GH and stimulates skeletal growth,
growth of internal organs, and protein synthesis.
Indications
 long-term treatment of children with growth failure
associated with various deficiencies, girls with
Turner’s syndrome, AIDS wasting and cachexia, GH
deficiency in adults, and treatment of growth failure in
children of small gestational age who do not achieve
catch-up growth by 2 years of age.
 Somatropin (Nutropin, Saizen, Genotropin,
Serostim) and somatropin rDNA origin
(Zorbtive) are used for GH replacement today.
Contraindications and Cautions
 Allergy to any component of the drug. To prevent
hypersensitivity reactions.
 Closed epiphyses and cranial lesions. Risk of
serious complications with somatropin.
 Abdominal surgery and acute illness are
secondary to complications of open-heart
surgery. Potential problems with healing.
 Pregnancy or lactation. Potential adverse effects on
the fetus.
Adverse Effects
 development of antibodies to GH
 inflammation and autoimmune-type reactions
(swelling, joint pain)
 endocrine reactions (hypothyroidism, insulin
resistance).
Nursing Responsibility
 Reconstitute the drug following manufacturer’s
directions because individual products
vary;  administer IM or SQ as ordered for appropriate
drug delivery.
 Monitor response closely to determine the need for
dose adjustment.
 Monitor thyroid function, glucose tolerance, and GH
levels periodically to monitor endocrine changes and
to institute treatment as needed.
 Provide comfort measures to help patients cope with
the drug effects.  hypersensitivity reactions.
 Provide patient education (storage, preparation,
administration techniques) about drug effects and
warning signs to report to enhance patient knowledge
and to promote compliance.    
ANTERIOR PITUITARY HORMONE DRUGS
GROWTH HORMONE ANTAGONISTS
Growth Hormone Antagonists – are used in treating GH
hypersecretion (hyperpituitarism) caused by pituitary tumors.
Disease Spotlight: Hyperpituitarism
 GH hypersecretion is usually caused by pituitary
tumors and can occur at any time in life.
 Gigantism occurs before the epiphyseal plates of the
long bones fuse and cause acceleration in linear
skeletal growth. Individuals with gigantism can reach
7 to 8 feet in height with normal body proportions.
 Acromegaly is a form of hyperpituitarism after
epiphyseal closure (adults). As linear growth is
impossible, hypersecretion of GH causes
enlargement in the peripheral parts of the body such
as hands and feet as well as internal organs (heart).
Therapeutic Action
• acting directly on postsynaptic dopamine receptors in
the brain to inhibit GH secretion
• Octreotide and lanreotide are somatostatin
analogues which are more potent in inhibiting GH
release with less of an inhibitory effect on insulin
release. They are used instead of somatostatin.
Indications
 Treatment of Parkinson’s disease, hyperprolactinemia
associated with pituitary adenomas, female infertility
associated with hyperprolactinemia, and acromegaly,
short-term treatment of amenorrhea or galactorrhea.
 Bromocriptine is a semisynthetic ergot alkaloid and
a dopamine agonist which is frequently used to treat
acromegaly. It may also be used as an adjunct to
irradiation.
Contraindications and Cautions
 Allergy to any component of the drug. To prevent
 Pregnancy or lactation. Potential adverse effects on
the fetus.
2|Pascual, Airine A.
  Diabetes, thyroid dysfunction. May be exacerbated
by blocking GH.
Adverse Effects
 CNS: headache
 CV: sinus bradycardia, arrhythmias
 GI: nausea, vomiting, abdominal cramps,
constipation, diarrhea, acute cholecystitis, cholestatic
jaundice, biliary tract obstruction, pancreatitis
 Others: decreased glucose tolerance, inflammation at
injection sites
Interactions
 Erythromycin. Increased toxicity with bromocriptine
 Phenothiazine. Decreased effectiveness of
bromocriptine
 Opioids. Higher doses of pegvisoman will be required
Nursing Responsibility
 Reconstitute the drug following manufacturer’s
directions because individual products
vary;  administer IM or SQ as ordered for appropriate
drug delivery.
 Inject lanreotide deep into subcutaneous fat in the
superior quadrant of the buttocks and alternate from
right to left to ensure proper drug delivery and prevent
local reactions.  constipation, dry mouth
 Monitor thyroid function, glucose tolerance, and GH
levels periodically to monitor endocrine changes and
to institute treatment as needed.
 Arrange for baseline and periodic ultrasound
evaluation of gallbladder if using octreotide or
lanreotide to detect any gallstone development and to
arrange for appropriate treatment.
 Provide comfort measures to help patients cope with
the drug effects. 
 Provide patient education about drug effects and
warning signs to report to enhance patient knowledge
and to promote compliance.    
POSTERIOR PITUITARY HORMONES DRUGS
The posterior pituitary stores two hormones produced by the
hypothalamus (antidiuretic hormone or vasopressin [ADH] and
oxytocin).
ADH possesses antidiuretic, hemostatic, and vasopressor
properties.
- It is the hormone affected in diabetes insipidus, a condition
characterized by production of a large amount of dilute urine
containing no glucose.
Therapeutic Action
 Pressor and antidiuretic effect by causing the cortical
and medullary parts of the collecting duct to become
permeable to water, thereby increasing water
reabsorption and decreasing urine formation.
 Increasing levels of clotting factor VIII
Indications
 Treatment of neurogenic diabetes insipidus and
hemophilia A
Contraindications and Cautions
 Allergy to any component of the drug. To prevent
hypersensitivity reactions.
 Severe renal dysfunction. Can alter the effects of
the drug
 Any known vascular disease. Can be exacerbated
by the effects of the drug on vascular smooth muscle
 Pregnancy. Risk of premature uterine contractions.
 Lactation. Potential adverse effects to the neonate.
Adverse Effects
 Water intoxication. Drowsiness, light-headedness,
headache, coma, convulsions
 GI: abdominal cramps, flatulence, nausea, vomiting,
 Local reaction at injection site
Interactions
 Carbamazepine, chlorpropamide. Increased
antidiuretic effects if with desmopressin
 Digoxin, ACEI, ARBs, potassium-sparing
diuretics. Risk of hyperkalemia with tolvaptan and
conivaptan
 Telithromycin. Severe tolvaptan toxicity.
Nursing Implementation with Rationale
 Monitor patient fluid volume to watch for signs of
water intoxication and fluid excess or excessive fluid
loss.
 Monitor patients with vascular disease for any sign of
exacerbation to provide immediate treatment.
 Monitor condition of nasal passages if given
intranasally to observe for nasal ulceration, which can
occur and could affect drug absorption.
 Provide comfort measures to help patients cope with
the drug effects. 
 Provide patient education about drug effects and
warning signs to report to enhance patient knowledge
and to promote compliance.    
Lesson 2: Adrenocortical agents
3|Pascual, Airine A.
  drugs used as short-term treatment to suppress
immune system in patients with inflammatory
disorders.
 They are also used for replacement therapy to
maintain hormone levels when adrenal glands are not
functioning adequately.
ADRENOCORTICAL AGENTS
(GLUCOCORTICOIDS)
Glucocorticoids
 Glucocorticoids are agents that stimulate an increase
in glucose levels for energy.
 They also increase the rate of protein breakdown and
decrease the rate of protein formation from amino
acids to preserve energy.
 They are also capable of lipogenesis, or the formation
and storage of fat in the body for energy source.
Therapeutic Action
 bind to cytoplasmic receptors of target cells to form
complex reactions needed to reduce inflammation
and to suppress immune system.
 Other glucocorticoids like hydrocortisone, cortisone,
and prednisone also have mineralocorticoid activity so
they can affect potassium, sodium, and water levels.
They can also limit the activity of lymphocytes to act
within the immune system. Furthermore, they inhibit
the spread of phagocytes to the bloodstream and
injured tissues.
Indications
 short-term treatment of inflammatory disorders by
blocking the actions of arachidonic acid leading to
decrease in formation of prostaglandins and
leukotrienes.
 Local agents are used to treat local inflammation.
 Systemic use is indicated for treatment of some
cancers, hypercalcemia associated with cancer,
hematological disorders, and some neurological
infections.
 When combined with mineralocorticoids, some of
these drugs can be used in replacement therapy for
adrenal insufficiency.
Contraindications and Cautions
 Allergy to any component of the drug. To prevent
hypersensitivity reactions.
 Acute infection. Can be exacerbated by the blocking
effects of the drug on inflammation and immune
system.
 Diabetes. Glucose-elevating effect of the drug can
disrupt glucose control
 Other endocrine disorders. Potential of imbalance.
 Pregnancy. Potential adverse effects on the fetus
Adverse Effects
 increased methylprednisolone toxicity among African
Americans
 growth retardation
 local inflammation and infections
 burning and stinging sensation at injection site.
Interactions
 Erythromycin, ketoconazole, troleandomycin.
Increased toxic effects.
 Salicylates, barbiturates, phenytoin, or rifampin.
Decreased serum level and effectiveness if with.
Implementation with Rationale
 Administer drug daily at 8 to 9 AM to mimic normal
peak diurnal concentration levels and thereby
minimize suppression of the hypothalamic-pituitary
axis (HPA).
 Space multiple doses evenly throughout the day to try
to achieve homeostasis.
 Taper doses when discontinuing give the adrenal
glands a chance to recover and produce
adrenocorticoids.
 Protect patient from unnecessary exposure to
infection and invasive procedures because steroids
suppress the immune system, and the patient is at
increased risk for infection.
 Provide comfort measures to help patients cope with
drug effects.
 Provide patient education about drug effects and
warning signs to report to enhance patient knowledge
and to promote compliance.
ADRENOCORTICAL AGENTS
(MINERALOCORTICOIDS)
Mineralocorticoids
- affect electrolyte levels directly and help maintain
homeostasis.
- The classic mineralocorticoid is aldosterone.
Therapeutic Action
 Aldosterone increases sodium reabsorption in the
renal tubules and increases potassium and hydrogen
excretion, leading to water and sodium retention.
Indications
4|Pascual, Airine A.
  partial replacement therapy in cortical insufficiency
conditions, treatment of salt-losing adrenogenital
syndrome; off-label use: treatment of hypotension.
Contraindications and Cautions
 Allergy to any component of the drug. To prevent
hypersensitivity reactions.
 Severe hypertension, heart failure, or cardiac
disease. Resultant increased blood pressure
 Lactation. Potential adverse effects to the baby.
 Infection. Can alter adrenal response
 High sodium intake. Severe hypernatremia can
occur.
Adverse Effects
 CNS: headache, weakness
 CV: edema, hypertension, heart failure,
 Others: possible hypokalemia, allergic reactions from
skin rash to anaphylaxis.
Interactions
• Salicylates, barbiturates, hydantoins, rifampin, and
anticholinesterase. Decreased effectiveness of these
drugs.
Nursing Responsibility
 Use only in conjunction with appropriate
glucocorticoids to maintain control of electrolyte
balance.
 Increase dose in times of stress to prevent adrenal
insufficiency and to meet increased demands for
corticosteroids under stress.
 Monitor for hypokalemia (weakness, serum
electrolytes) to detect the loss early and treat
appropriately.
 Discontinue if signs of overdose (excessive weight
gain, edema, hypertension) occur to prevent the
development of more severe toxicity.
 Provide comfort measures to help patients cope with
drug effects.
 Provide patient education about drug effects and
warning signs to report to enhance patient knowledge
and to promote compliance.
Lesson 3: Thyroid and Parathyroid agents
Thyroid hormones are made available to replace the low or
absent levels of natural thyroid hormone and suppress the
overproduction of TSH by the pituitary.
These can contain both natural and synthetic thyroid hormone.
Parathyroid agents are drugs used to treat disorders that
affect serum calcium levels. This can be
either antihypocalcemic agent or antihypercalcemic agent.
The parathyroid glands are four very small groups of glandular
tissue located on the back of the thyroid gland. This
produces PTH and calcitonin to maintain body’s calcium
balance. PTH is the most important regulator of serum calcium
levels in the body.
THYROID AGENTS
Therapeutic Action
 This is replacement hormone for hypothyroid states
like myxedema coma, goiters, and thyroid
cancer increases the metabolic rate of body tissues,
increasing oxygen consumption, respiration, heart
rate, growth and maturation, and the metabolism of
fats, carbohydrates, and proteins.  
 Levothyroxine, a synthetic salt of T4, is the most
frequently used replacement hormone because of its
predictable bioavailability and reliability.
Indications
 Replacement hormone for hypothyroid states like
myxedema coma, goiters, and thyroid cancer
 Treatment for thyroid toxicity in conjunction with
antithyroid drugs
 Treatment for thyroid overstimulation during
pregnancy
Contraindications and Cautions
 Allergy to any component of the drug. To prevent
hypersensitivity reactions.
 Acute thyrotoxicosis (unless used in conjunction
with antithyroid drugs). Can be exacerbated by the
drugs
 Myocardial infarction. Can be exacerbated by the
drugs
 Lactation. Drug enters breast milk and can suppress
infant’s thyroid production
 Addison disease. The body will not be able to deal
with drug effects.
 Pregnancy. Potential adverse effects on the fetus
 Liothyronine and liorix have greater incidence of
cardiac side effects.
Adverse Effects
 Skin reactions and loss of hair
 Symptoms of hyperthyroidism
Interactions
 Cholestyramine. Decreased absorption of thyroid
hormones (take two hours apart)
 Anticoagulants. Increased bleeding
 Digitalis glycosides. Decreased effectiveness of
digitalis glycosides.   
5|Pascual, Airine A.
Nursing Responsibility
 Administer a single daily dose before breakfast each
day to ensure consistent therapeutic levels.
 Administer with a full glass of water to prevent
difficulty of swallowing and esophageal atresia.
 Monitor cardiac response to detect cardiac adverse
effects.
 Arrange for periodic blood tests of thyroid function to
monitor the effectiveness of the therapy.
 Provide comfort measures (temperature control, rest
as needed, safety precautions) to help patients cope
with drug effects.
 Provide patient education about drug effects and
warning signs to report to enhance patient knowledge
and to promote compliance.
ANTITHYROID AGENTS
Therapeutic Action
 Thioamides lower thyroid hormones by preventing
the formation of thyroid hormones in the thyroid cells.
They also partially inhibit the conversion of T4 to T3 at
cellular level. Thioamides include propylthiouracil
(PTU) and methimazole.
 Iodine solutions in high doses block thyroid function.
They cause the cells to become oversaturated with
iodine and stop producing hormones.
Indications
 Treatment of hyperthyroidism
 Thyroid blocking in a radiation emergency
Contraindications and Cautions
 Allergy to any component of the drug. To prevent
hypersensitivity reactions.
 Pregnancy. Development of cretinism. PTU is the
drug of choice for pregnant women.
 Lactation. Risk of antithyroid activity in the infant
(neonatal goiter)
 Pulmonary edema or tuberculosis. Contraindicated
with strong iodine products.
Adverse Effects
 Thioamides: drowsiness, lethargy, bradycardia,
nausea, skin rash
 PTU: nausea, vomiting, GI complaints, severe liver
toxicity
 Methimazole: bone marrow suppression
 Iodine solution: hypothyroidism; metallic taste and
burning sensation in the mouth, sore teeth and gums,
diarrhea; staining of teeth, skin rash, and
development of goiter. I131 is only for patients over 30
years old because of adverse effects associated with
radioactivity.
Interactions
 Thioamides: increased bleeding with oral
anticoagulants and PTU
 Iodine solutions: changes in the metabolism and
level of anticoagulants, theophylline, digoxin,
metoprolol, and propranolol
Nursing Responsibility
 Administer PTU three times a day, around the clock to
ensure consistent therapeutic levels.
 Give iodine solution through a straw to decrease
staining of teeth; tables can be crushed.
 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.
PARATHYROID AGENTS
(ANTIHYPOCALCEMIC AGENTS)
Antihypocalcemic Agents
 Antihypocalcemic agents are drugs used to treat
deficient levels of PTH.
Therapeutic Action
 a vitamin D compound that regulates the absorption
of calcium and phosphate from the small intestine,
mineral resorption in bone, and reabsorption of
phosphate from renal tubules, increasing the serum
calcium level.
 Teriparatide stimulates new bone formation leading
to an increase in skeletal mass. It increases serum
calcium and decreases serum phosphorus.
Indications
 Management of hypocalcemia in patients on chronic
renal dialysis
 Management of hypocalcemia associated with
hypoparathyroidism and with sustained systemic
glucocorticoids therapy
Contraindications and Cautions
6|Pascual, Airine A.
  Allergy to any component of the drug. To prevent
hypersensitivity reactions.
 Hypercalcemia or Vitamin D toxicity. Can be
exacerbated by drug effects.
 Pregnancy and lactation. Potential adverse effects
to the fetus. Calcitriol has been associated with
hypercalcemia in babies when used by nursing
mothers.
 Teriparatide is associated with osteosarcoma in
animal studies.
Adverse Effects
 CNS: weakness, headache, somnolence, irritability
 GI: metallic taste, nausea, vomiting, dry mouth,
constipation
Interactions
 Magnesium-containing antacids. Risk for
hypermagnesemia.
 Cholestyramine or mineral oil. Reduced absorption of
antihypocalcemic agents; separate for at least two
hours.
Nursing Responsibility
 Monitor serum calcium concentration before and
periodically during treatment to allow for adjustment of
dose to maintain calcium levels within normal limit.
 Provide supportive measures (e.g., analgesics, small
and frequent meals, help with activities of daily living)
to help patients deal with CNS and GI effects of the
drug.
 Arrange for nutritional consultation if GI effects are
severe to ensure nutritional balance.
 Provide patient education about drug effects and
warning signs to report to enhance patient knowledge
and to promote compliance.
PARATHYROID AGENTS
(ANTIHYPERCALCEMIC AGENT)
Antihypercalcemic Agents
 Antihypercalcemic agents are drugs used to treat
PRH excess or hypercalcemia. These agents
include bisphosphonates and calcitonin salmon.
 These drugs act on the serum levels of calcium and
do not suppress the parathyroid gland or PTH.
Therapeutic Action
 Bisphosphonates slow normal and abnormal bone
resorption without inhibiting bone formation and
mineralization.
 Calcitonin inhibits bone resorption and lowers
elevated serum calcium. It also increases the
excretion of filtered phosphate, calcium, and sodium
by the kidney.
Indications
 Bisphosphonate is used to treat and prevent
osteoporosis in postmenopausal women and in men.
It is also used to treat glucocorticoid-induced
osteoporosis as well as to treat Paget’s disease.
 Calcitonin is used for treatment of Paget’s disease,
postmenopausal osteoporosis, and emergency
treatment of hypercalcemia.
Contraindications and Cautions
 Allergy to any component of the drug. To prevent
hypersensitivity reactions.
 Hypocalcemia. Worsened by calcium-lowering effect
of bisphosphonates
 Pregnancy and lactation. Potential adverse effects
to fetus or neonate
 Renal dysfunction. Can alter drug excretion.
 Upper GI disease. Can be aggravated by
bisphosphonates. A drug should be taken with a full
glass of water and the patient should stay upright for
30 minutes because serious esophageal erosion can
occur.
 Allergy to salmon or fish products. To prevent
hypersensitivity reaction with taking calcitonin
 Pernicious anemia. Can be worsened by calcitonin
Adverse Effects
 Bisphosphonates: headache, nausea, diarrhea
 Calcitonins: flushing of the face and hands, skin
rash, nausea and vomiting, urinary frequency, and
local inflammation at the site of injection
Interactions
 Bisphosphonates. Decreased absorption if with iron,
antacids, or multiple vitamins so separate by at least
30 minutes; GI distress with aspirin.
 There is no clinically important drug-drug interaction
with calcitonin.
Nursing Responsibility
 Ensure adequate hydration with any of these agents
to reduce the risk of renal complications.
 Arrange for concomitant vitamin D, calcium
supplements, and hormone replacement therapy if
used to treat postmenopausal osteoporosis.
 Rotate injection sites and monitor for inflammation if
using calcitonin to prevent tissue breakdown and
irritation.
7|Pascual, Airine A.
  Monitor serum calcium before and periodically during
treatment to allow for dose adjustment.
 Arrange for periodic blood tests of renal function if
using gallium to monitor for renal dysfunction.
 Provide comfort measures to help patients cope with
drug effects.
Lesson 4: Antidiabetic Agents
Antidiabetic agents are group of drugs 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 (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.
Therapeutic Action
 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
 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
The type of Insulin to be use depends on its rate of absorption:
 rapid-acting, such as lispro (Humalog)
 short-acting, such as regular insulin (Humulin R)
 intermediate-acting, such as NPH
 long acting, such as glargine (Lantus) and insulin
detemir (Levemir).
Contraindications and Cautions
 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
 hypoglycemia and ketoacidosis
 local reactions at the injection site (lipodystrophy).
Interactions
 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 Responsibility
 Ensure that patient has dietary and exercise regimen
and uses 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.
 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.
8|Pascual, Airine A.
  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 patients cope with
drug effects.
 Provide patient education about drug effects and
warning signs to report to enhance patient knowledge
and to promote compliance.     agents that act like sulfonylureas to increase insulin
ANTIDIABETIC AGENTS (SULFONYLUREAS)
Therapeutic Action
 Sulfonylureas stimulate insulin release from the beta
cells in pancreas. They improve insulin binding to
insulin receptors and may increase the number of
insulin receptors.
 They are also known to increase the effect of
antidiuretic hormones on renal cells.
Indications
 Sulfonylureas are used as an adjunct to diet and
exercise for the treatment of type 2 diabetes older
than 10 years of age; extended-release form for
patients older than 17 years of age; adjunct treatment
with polycystic ovary syndrome.
Therapeutic Action
 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 decreases 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 the development of lactic acidosis
and GI distress.
 Meglitinides nateglinide and repaglinide are newer
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 post
meal 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
post meal glucose levels. It should not be used when
the 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
 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.
 Bromocriptine, a dopamine agonist used to treat
Parkinson’s disease was approved in 2009 as a CNS
approach to treat type 2 diabetes.
Nursing Responsibility:
 Administer the drug as prescribed in the appropriate
relationship to meals to ensure therapeutic
effectiveness.
 Ensure that patient has dietary and exercise regimen
and uses 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.
 Monitor response carefully; blood glucose monitoring
is the most effective way to evaluate dose. Obtain
9|Pascual, Airine A.
 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 patients cope with
drug effects.
 Provide patient education about drug effects and
warning signs to report to enhance patient knowledge
and to promote compliance.

10 | P a s c u a l , A i r i n e A .
MODULE 9
DRUGS ACTING ON THE
CARDIOVASCULAR SYSTEM
Lesson 1: Anti-Hypertensive Agents
Anti-Hypertensive Agents affect different areas
of blood pressure control so in most cases, these agents are
combined for synergistic effect.
Main action of antihypertensive agents is to alter the body’s
regulating mechanisms (e.g., baroreceptors, renin-angiotensin-
aldosterone system, etc.) responsible for maintaining normal
blood pressure.
ACE INHIBITORS
Angiotensin-converting enzymes inhibitors (ACE
Inhibitors) are antihypertensive agents that act in the lungs to
prevent the conversion of angiotensin I into angiotensin II,
which is a potent vasoconstrictor.
Therapeutic Action
 By preventing the production of angiotensin II which is
a potent vasoconstrictor and a stimulator of
aldosterone release, blood pressure is decreased with
resultant loss of serum sodium and fluid but with
a slight increase in serum potassium.
Indications
 Primarily indicated for hypertension and can be used
alone or in combination with other drugs.
 Aside from its indication in treating hypertension, it is
also combined with diuretics and digoxin in
the treatment of heart failure and left ventricular
dysfunction. The resultant effect is decreased in
peripheral resistance and blood volume leading to
decreased cardiac workload.
 It is also approved for treatment of diabetic
nephropathy, in which the renal artery is being
damaged by diabetes. It is thought that decreased in
stimulation of angiotensin receptors in the kidney will
slow down the damage in the renal artery.
Contraindications and Cautions
 Allergy to ACE inhibitors. Prevent severe
hypersensitivity reactions.
 Renal impairment. Decreased renal blood flow effect
of these drugs can exacerbate renal impairment.
 Heart failure. Changes in hemodynamics caused by
these drugs can exacerbate heart failure.
 Hyponatremia and hypovolemia. Can be
exacerbated by the therapeutic effects of the drug.
 Pregnancy and lactation. Can cause potential
adverse effects to the fetus and can decrease milk
production. Pregnant women are advised to use
barrier type of contraceptives while taking this drug.
Adverse Effects
 GI: irritations, ulcer, constipation, liver injury
 GU: renal insufficiency, renal failure, proteinuria
 CV: reflex tachycardia, chest pain, heart failure,
cardiac arrhythmias
 EENT: rash, alopecia, dermatitis, photosensitivity
 Captopril is associated with sometimes-fatal
pancytopenia, cough, and GI distress.
Interactions
 Allopurinol: increased risk for hypersensitivity
 NSAIDs: increased risk for decreased
antihypertensive effects
Nursing Responsibility
 Educate patients on the importance
of healthy lifestyle choices which include regular
exercise, weight loss, smoking cessation, and low-
sodium diet to maximize the effect of antihypertensive
therapy.
 Administer drug on empty stomach one hour before or
two hours after meal to ensure optimum drug
absorption.
 Monitor renal and hepatic function tests to alert doctor
for possible development of renal and/or hepatic
failure as well as to signal need for reduced drug
dose.
 Monitor for presence of manifestations that signal
decreased in fluid volume (e.g., diarrhea, vomiting,
dehydration) to prevent exacerbation of hypotensive
effect of drug.
 Educate patient and family members about drug’s
effect to the body and manifestations that would need
reporting to enhance patient knowledge on drug
therapy and promote adherence.
ANGIOTENSIN II-RECEPTOR BLOCKERS
ARBs are antihypertensive agents that exert their action by
blocking vasoconstriction and release of aldosterone through
11 | P a s c u a l , A i r i n e A .
selective blocking of angiotensin II receptors in vascular
smooth muscles and adrenal cortex.
Therapeutic Action
 The main action is to block the blood pressure raising
effect of the renin-angiotensin-aldosterone system
(RAAS).
Indications
 Like ACE inhibitors, they can also be used alone for
treatment of hypertension or in combination with other
antihypertensive agents.
 Utilized in treatment of heart failure for patients who
do not respond to ACE inhibitors.
 By blocking the effects of angiotensin receptors in
vascular endothelium, these drugs are able to slow
down the progress of renal disease in patients with
type 2 diabetes and hypertension.
Contraindications and Cautions
 Allergy to ARBs. Prevent severe hypersensitivity
reactions.
 Renal and hepatic impairment. Can alter
metabolism and excretion of drugs which can
increase the risk for toxicity.
 Hypovolemia. Can be exacerbated by the drug’s
action on blocking important life-saving compensatory
mechanisms.
 Pregnancy and lactation. Can cause potential
adverse effects to the fetus and potential termination
of pregnancy between second and third trimester. It is
still not known whether ARBs can enter breast milk,
but it is generally not allowed in lactating women
because of potential adverse effects to the
neonate.
Adverse Effects
 CNS: headache, dizziness, syncope, weakness
 Respiratory: symptoms of upper respiratory tract
infections (URTI), cough
 GI: diarrhea, abdominal pain, nausea, dry mouth,
tooth pain
 EENT: rash, alopecia, dry skin
Interactions
 Phenobarbital, indomethacin, rifamycin: loss of
effectiveness of ARBs
 Ketoconazole, fluconazole, diltiazem: decreased
antihypertensive effects of ARBs
Nursing Responsibility
 Educate patients on the importance of healthy lifestyle
choices which include regular exercise, weight loss,
smoking cessation, and low-sodium diet to maximize
the effect of antihypertensive therapy.
 Administer drug with food to prevent GI distress
associated with drug intake.
 Monitor renal and hepatic function tests to alert doctor
for possible development of renal and/or hepatic
failure as well as to signal need for reduced drug
dose.
 Provide comfort measures (e.g. quiet environment,
relaxation techniques, etc.) to help patients tolerate
drug effects.
 Educate patient and family members about drug’s
effect to the body and manifestations that would need
reporting to enhance patient knowledge on drug
therapy and promote adherence.
CALCIUM-CHANNEL BLOCKERS
Calcium-channel blockers as antihypertensive agents
decrease blood pressure, cardiac workload, and myocardial
consumption of oxygen.
Since these drugs can significantly decrease cardiac workload,
they are effective in treatment of angina.
Therapeutic Action
 These drugs inhibit the movement of calcium ions
across myocardial and arterial muscle cell
membranes. As a result, the action potential of these
cells is altered, and cell contractions are blocked.
 Resultant effects include depressed myocardial
contractility, slow cardiac impulse in conductive
tissues, and arterial dilation and relaxation.
Indications
 Like ACE inhibitors and ARBs, they can also be used
alone for treatment of hypertension or in combination
with other antihypertensive agents.
 Extended-release preparations are usually indicated
for hypertensions in adults.
Contraindications and Cautions
 Allergy to calcium-channel blockers. Prevent
severe hypersensitivity reactions.
 Heart block (sick sinus syndrome). Can be
exacerbated by conduction-slowing effect of the drug.
 Renal and hepatic impairment. Can alter
metabolism and excretion of drugs which can
increase the risk for toxicity.
 Pregnancy and lactation. Can cause potential
adverse effects to the fetus and should not be used
unless the benefit to the mother clearly outweighs the
12 | P a s c u a l , A i r i n e A .
 risk to the fetus. It is not clear whether this drug can
enter breast milk, so another method of feeding is
implemented for lactating mothers who are taking this
drug.
Adverse Effects
 CNS: headache, dizziness, light-headedness, fatigue
 CV: hypotension, bradycardia, peripheral edema,
heart block
 GI: nausea, hepatic injury
 EENT: rash, skin flushing
Interactions
 Increased serum level and toxicity of cyclosporine if
taken with diltiazem.
 Grapefruit juice can increase serum level and toxicity
of calcium-channel blockers.
Nursing Responsibility
 Educate patients on the importance of healthy lifestyle
choices which include regular exercise, weight loss,
smoking cessation, and low-sodium diet to maximize
the effect of antihypertensive therapy.
 Monitor blood pressure and heart rate and rhythm to
detect possible development of adverse effects.
 Provide comfort measures for the patient to tolerate
side effects (e.g. small frequent meals for nausea,
limiting noise and controlling room light and
temperature to prevent aggravation of stress which
can increase demand to the heart, etc.)
 Educate patient and family members about drug’s
effect to the body and manifestations that would need
reporting to enhance patient knowledge on drug
therapy and promote adherence.
 Emphasize to the client the importance of strict
adherence to drug therapy to ensure maximum
therapeutic effects.
Vasodilators
Direct vasodilators are used when the previous drugs
mentioned are not effective.
These antihypertensive agents are reserved for severe
hypertension and hypertensive emergencies.
Therapeutic Action
 These antihypertensive agents exert their effect by
acting directly on smooth muscles. Consequently,
there will be muscle relaxation and vasodilation. Both
of these will cause a drop in blood pressure.
Indications
 As mentioned, these drugs are only used for
hypertension cases that do not respond to other drug
therapies.
 Nitroprusside is used in maintaining controlled
hypotension during surgery.
 Nitroprusside is administered intravenously;
hydralazine is available for oral, intravenous, and
intramuscular use; and minoxidil is available for oral
use only.
Contraindications and Cautions
 Allergy to direct vasodilators. Prevent severe
hypersensitivity reactions.
 Cerebral insufficiency. Can be exacerbated by
drug’s action to cause sudden drop in blood pressure.
 Peripheral vascular disease, CAD, heart failure,
tachycardia. These conditions can be exacerbated
by a sudden drop in blood pressure.
 Pregnancy and lactation. Can cause potential
adverse effects to the fetus and should not be used
unless the benefit to the mother clearly outweighs the
risk to the fetus. The drug can enter breast milk and
can cause potential adverse effects to the neonate. If
needed by lactating mothers, another method of
feeding is instituted.
Adverse Effects
 CNS: headache, dizziness, anxiety
 CV: reflex tachycardia, heart failure, edema, chest
pain
 GI: nausea, vomiting, GI upset
 EENT: rash, lesions (e.g., minoxidil is associated with
abnormal hair growth.)
 Nitroprusside is metabolized into cyanide so it can
cause cyanide toxicity characterized by dyspnea,
ataxia, loss of consciousness, distant heart sounds,
and dilated pupil.
 Nitroprusside suppresses iodine uptake which leads
to development of hypothyroidism.
Nursing Responsibility
 Educate patients on the importance of healthy lifestyle
choices which include regular exercise, weight loss,
smoking cessation, and low-sodium diet to maximize
the effect of antihypertensive therapy.
 Monitor blood pressure and heart rate and rhythm
closely to evaluate for effectiveness and ensure quick
response if blood pressure falls rapidly or too much.
 Provide comfort measures for the patient to tolerate
side effects (e.g., small frequent meals for nausea,
limiting noise and controlling room light and
temperature to prevent aggravation of stress which
can increase demand to the heart, etc.)
 Monitor patients for any manifestations that could
decrease fluid volume inside the body (e.g., vomiting,
diarrhea, excessive sweating, etc.) to detect and treat
excessive hypotension.
13 | P a s c u a l , A i r i n e A .
  Educate patient and family members about drug’s
effect to the body and manifestations that would need
reporting to enhance patient knowledge on drug
therapy and promote adherence.
 Emphasize to the client the importance of strict
adherence to drug therapy to ensure maximum
therapeutic effects.
Lesson 2: Cardiotonic Agents
Cardiotonic Agents are drugs used to increase the contractility
of the heart
CARDIAC GLYCOSIDES
Cardiotonic agents from foxglove or digitalis plants. They exert
their effects on the cardiac muscles by affecting levels of
intracellular calcium. In turn, the contractility of the muscles is
increased.
Therapeutic Action
 Allows more calcium to enter during contraction,
therefore increasing the force of contraction – positive
inotropic effect.
 Consequently, there is increased cardiac output and
renal perfusion. A good blood supply to the kidney
decreases renin release. This downplays the activity
of renin-angiotensin-aldosterone system (RAAS)
which causes more fluid to be excreted in the body
through urine. A decrease in blood volume eases the
workload of the heart.
 Another mechanism of this drug is to decrease the
workload of the heart and slow down relaxation of the
cells. Therefore, this drug can increase the strength of
contractility without increasing the rate of contraction
(negative chronotropic effect).
Indications
 Primarily indicated for decreasing workload of the
heart and relieving HF.
 Digoxin is especially indicated for atrial flutter, atrial
fibrillation, and paroxysmal atrial tachycardia.
Contraindications and Cautions
 Allergy to any component of digitalis preparation.
Prevent severe hypersensitivity reactions.
 Ventricular tachycardia or fibrillation. These are
potentially fatal arrhythmias and should be treated
with another drug.
 Heart block (sick sinus syndrome). Can be
worsened by drug’s effect on slowing conduction
through AV node
 Idiopathic hypertrophic subaortic
stenosis (IHSS). Obstruction of outflow tract to the
aorta can result from increasing the force of
contraction and this can lead to other severe
problems.
 Acute myocardial infarction (MI). Increasing the
force of contraction can damage the heart muscles
more.
 Renal insufficiency. Drug is excreted through urine
and the existing renal insufficiency can contribute to
development of drug toxicity.
 Pregnancy and lactation. Can cause potential
adverse effects to the fetus or neonate.
Adverse Effects
 CNS: headache, weakness, drowsiness, vision
changes (most commonly reported is seeing yellow
halo around objects)
 CV: arrhythmias
 GI: GI upset, anorexia
 NURSING ALERT!  Signs and symptoms of
digitalis toxicity: anorexia, nausea, vomiting,
malaise, depression, irregular heart rhythms (e.g.,
heart block, heart arrhythmias, and ventricular
tachycardia)
Interactions
 Digoxin immune Fab or DigiFab: antidote; these
antibodies bind molecules of digoxin, making them
unavailable at site of action. Used when serum
digoxin is >10 ng/mL and serum potassium is >5
mEq/L.
 Verapamil, amiodarone, quinine, erythromycin,
tetracycline, cyclosporine: increased therapeutic
and toxic effects of digoxin. Combination of digoxin
with any of these drugs would warrant decrease in
dose of digoxin to prevent toxicity.
 Potassium-losing diuretics: increased risk of
cardiac arrhythmias
 Thyroid hormones, metoclopramide,
penicillamine: decreased therapeutic effects of
digoxin. Increasing the dose of digoxin is important.
 Cholestyramine, charcoal, colestipol, antacids,
bleomycin, cyclophosphamide,
methotrexate: decreased absorption of digoxin. In
this case, digoxin must be taken 2-4 hours after taking
any of these drugs.
 St. John’s wort, psyllium: decreased therapeutic
effect of digoxin
 Ginseng, hawthorn, licorice: increased risk of
digoxin toxicity
Nursing Responsibility
 Check drug dose and preparation carefully to avoid
medication errors because drug has narrow safety
margin.
14 | P a s c u a l , A i r i n e A .
  Do not administer drug with food and antacids to
prevent decreased in drug absorption.
 IMPORTANT! Count apical pulse for one full minute
before administering drug to monitor for adverse
effects.
 Drug is withheld if pulse is less than 60 beats per
minute in adults and 90 beats per minute in infants.
 The apical pulse is taken after one hour and if it
remains low, nurse must document it, withhold the
dose, and inform doctor.
 Assess pulse rhythm to detect arrhythmias which are
early signs of drug toxicity.
 Weigh the patient daily to monitor for fluid retention
and HF. Assess dependent areas for presence of
edema and note its degree of pitting to assess
severity of fluid retention.
 Monitor serum digoxin level as ordered (normal: 0.5-2
ng/mL) to evaluate therapeutic dosing and
development of adverse effects.
 Provide comfort measures (e.g. small frequent meals
for GI upset, instituting safety measures for
drowsiness and weaknesses, and providing adequate
room lighting for patients with visual disturbances) to
help patients tolerate drug effects.
 Promote rest periods and relaxation techniques to
balance supply and demand of oxygen.
 Ensure maintenance of emergency drugs and
equipment at bedside (e.g., potassium salts and
lidocaine for arrhythmias, phenytoin for seizures,
atropine in case of clinically significant low heart rate,
and cardiac monitor) to promote prompt treatment in
cases of severe toxicity.
 Educate patients on drug therapy including drug
name, its indication, and adverse effects to watch out
for to enhance patient understanding on drug therapy
and thereby promote adherence to drug regimen.
PHOSPHODIESTERASE INHIBITORS
aid in increasing force of myocardial contractility through their
enzyme-blocking effect. This in turn, increases the flow of
calcium into the myocardial cells.
Therapeutic Action
 By blocking the enzyme phosphodiesterase, cyclic
adenosine monophosphate (cAMP) increases. cAMP
stimulates flow of calcium towards the myocardium
and thereby increases the force of cardiac
contractility.
 Increases intracellular calcium and prolongs the effect
of sympathetic stimulation. This leads to three major
effects: vasodilation, increased oxygen consumption,
and arrhythmias.
Indications
 Only indicated for short-term treatment of patients not
responding to cardiac glycosides, vasodilators, and
diuretics.
 Drug use is only limited to severe situations because
it is associated with fatal ventricular arrhythmias.
Contraindications and Cautions
 Allergy to phosphodiesterase inhibitors and
bisulfites. Prevent severe hypersensitivity reactions.
 Severe aortic or pulmonary valvular
disease. Exacerbated by increased contraction.
 Acute MI. Exacerbated by increased contraction and
oxygen demand.
 Conditions with fluid volume deficit. Exacerbated
by increased renal perfusion which ultimately leads to
increased urine output.
Adverse Effects
 CV: ventricular arrhythmias, ventricular fibrillation,
hypotension, chest pain
 GI: nausea, vomiting, GI upset, abdominal pain
 Hema: thrombocytopenia
 Associated hypersensitivity reactions: vasculitis,
pericarditis, pleuritis, and ascites
 Burning at intravenous injection site
Interactions
 In solution together with furosemide: precipitate
formation
Nursing Responsibility
 Protect drug from light to prevent drug from
degradation.
 Ensure patency of intravenous access to promote
safe administration of drug.
 Weigh patient daily and fluid intake and output to
evaluate resolution of HF.
 Assess skin condition, noting presence of petechiae
and other manifestations of easy bruising and
bleeding to assess presence of thrombocytopenia.
 Monitor intravenous injection site to promote prompt
interventions in cases of burning sensation and/or
irritation.
 Provide comfort measures (e.g., small frequent meals
for GI upset, instituting safety measures for
drowsiness and weaknesses, and providing adequate
room lighting for patients with visual disturbances) to
help patients tolerate drug effects.
 Educate patients on drug therapy including drug
name, its indication, and adverse effects to watch out
for to enhance patient understanding on drug therapy
and thereby promote adherence to drug regimen.
15 | P a s c u a l , A i r i n e A .
Lesson 3: Antidysrhythmic Agents
Antidysrhythmic Agents address arrhythmia by altering cells’
automaticity and conductivity.
All cells in the heart are capable of undergoing spontaneous
contractions (automaticity). Therefore, these cells are capable
of generating excitatory impulses.
Disruptions in the conduction of these impulses affect
contractility of the heart as well as the volume of blood pumped
by the heart each minute (cardiac output).
Arrhythmia is the term applied for disruptions that interfere
with generation of impulses and conduction of these impulses
to the myocardium.
CLASS I ANTIARRHYTHMICS
This class blocks sodium channels in the cell membrane during
action potential. The subgroup under this class is based on
their mechanism in blocking sodium channels.
This class is local anesthetics and membrane-stabilizing
agents because of their ability to bind more quickly to sodium
channels.
Therapeutic Action
 Class I antiarrhythmics stabilize cell membrane by
depressing phase 0 of action potential. They bind to
sodium channels and change the duration of action
potential of the cells.
 Class Ia drugs depress phase 0 and prolong duration
of action potential.
 Class Ib drugs somewhat depress phase 0 and
shorten duration of action potential.
 Class Ic drugs markedly depress phase 0 and
extremely slows conduction but has little effect on the
duration of action potential.
Indications
 Primarily indicated for decreasing workload of the
heart and relieving HF.
 Digoxin is especially indicated for atrial flutter, atrial
fibrillation, and paroxysmal atrial tachycardia.
Contraindications and Cautions
 Allergy to Class I antiarrhythmics. Prevent severe
hypersensitivity reactions.
 Bradycardia, heart block. Unless an artificial
pacemaker is in place, the conduction-altering effect
of drug can lead to total heart block.
 HF, hypotension, shock. Exacerbated by effects of
drug on action potential.
 Electrolyte imbalance. Can alter drug effectiveness
 Renal, hepatic dysfunction. Interfere with drug
bioavailability and excretion
 Pregnancy and lactation. Can cause potential
adverse effects to the fetus or neonate.
Adverse Effects
 CNS: dizziness, drowsiness, fatigue, twitching, mouth
numbness, slurred speech, vision changes, tremors
 CV: arrhythmias, hypotension, vasodilation, potential
for cardiac arrest
 Respiratory: respiratory depression
 Hema: bone marrow depression
 EENT: rash, hypersensitivity reactions, hair loss
Interactions
 Digoxin, beta-blockers: increased risk for developing
arrhythmias
 Quinidine with digoxin: quinidine competes with
digoxin at renal transport sites so it can increase
chances of developing digoxin toxicity
 Cimetidine: increased Class Ia toxicity
 Anticoagulants: increased risk of bleeding
CLASS II ANTIARRHYTHMICS
This class interferes with action potential by blocking beta
receptors in the heart and kidneys. This, in turn, blocks phase
4 of action potential.
Class II antiarrhythmics are beta-adrenergic blockers.
Therapeutic Action
 Class II antiarrhythmics engage in competitive
inhibition of beta receptors specifically found in the
heart and kidneys. For this reason, there is a
decrease in heart rate, excitability, and cardiac output.
Conduction through AV node also slows down. In the
kidneys, the release of renin is decreased.
 These effects decrease blood pressure and stabilize
the highly excitable heart. As a result, the workload of
the heart is lessened.
Indications
16 | P a s c u a l , A i r i n e A .
  This class is specifically indicated for treatment of
supraventricular tachycardia and premature
ventricular contractions (PVCs).
Contraindications and Cautions
 Sinus bradycardia (<45 beats per minute), heart
block. Exacerbated by the therapeutic effects of the
drug.
 HF, cardiogenic shock, asthma, respiratory
depression. Exacerbated by blocking beta receptors.
 Pregnancy and lactation. Can cause potential
adverse effects to the fetus or neonate.
 Diabetes, thyroid dysfunction. Altered by blockade
of beta-receptors
 Renal, hepatic dysfunction. Interfere with
bioavailability and excretion of drugs.
Adverse Effects
 CNS: dizziness, fatigue, dreams, insomnia
 CV: arrhythmias, hypotension, bradycardia, AV
blocks, alteration in peripheral perfusion
 Respiratory: bronchospasm, dyspnea
 GI: anorexia, diarrhea, constipation, nausea, vomiting
 Other: loss of libido, decreased tolerance to exercise,
alterations in blood glucose level
Interactions
 Verapamil: increased adverse drug effects
 Insulin: increased hypoglycemia
CLASS III ANTIARRHYTHMICS
This class prolongs and slows down the outward movement of
potassium during phase 3 of action potential. These drugs act
directly on the heart muscles to prolong repolarization and
refractory period.
All of these drugs are proarrhythmic and have the possibility of
inducing arrhythmias.
Therapeutic Action
 Class III antiarrhythmics’ ability to prolong refractory
period and repolarization increases the threshold for
ventricular fibrillation.
 These are used to treat life-threatening arrhythmias
for which no other drugs have been effective.
 This class can also act on peripheral tissues to
decrease peripheral resistance.
Indications
 Amiodarone is the drug of choice for ventricular
fibrillation and pulseless ventricular tachycardia.
Contraindications and Cautions
 AV Block. Ibutilide and dofetilide exacerbate this
health condition.
 Renal, hepatic dysfunction. Interfere with
bioavailability and excretion of drugs.
 Shock, hypotension, respiratory depression,
prolonged QT interval. Depressed action potentials
can worsen these health problems.
Adverse Effects
 CNS: weakness, dizziness
 CV: arrhythmias, HF
 GI: nausea, vomiting, GI distress
 Amiodarone is associated with liver toxicity, ocular
abnormalities, and very serious cardiac arrhythmias.
Interactions
 Digoxin, quinidine: increased toxic drug effects
 Antihistamines, phenothiazines, tricyclic
antidepressants: increased risk of proarrhythmias
 Dofetilide combined with ketoconazole, verapamil,
cimetidine: increased risk for adverse drug effects
 Sotalol combined with antacids, NSAIDs, and aspirin:
loss of effectiveness of sotalol
CLASS IV ANTIARRHYTHMICS
Include two calcium-channel blockers, namely: diltiazem and
verapamil.
This class blocks the movement of calcium towards the cell
membrane.
Therapeutic Action
 Class IV antiarrhythmics depress action potential
generation and slows down phases 1 and 2 of action
potential. This action slows down both conduction and
automaticity.
Indications
 Other uses of diltiazem and verapamil include
treatment for hypertension and angina.
Contraindications and Cautions
 Allergy to calcium-channel blockers. Prevent
hypersensitivity reactions.
 Heart block (sick sinus syndrome). Unless an
artificial pacemaker is in place, heart blocks can be
exacerbated by the effects of the drug.
 HF, hypotension. Exacerbated by hypotensive effect
of the drug.
 Pregnancy, lactation. Potential adverse effects to
neonate or fetus.
 Renal, hepatic dysfunction. Interfere with
bioavailability and excretion of drugs.
17 | P a s c u a l , A i r i n e A .
Adverse Effects
 CNS: weakness, dizziness, fatigue, depression,
headache
 CV: hypotension, shock, edema, HF, arrhythmia
 GI: nausea, vomiting, GI distress
Interactions
 Verapamil with beta-blockers: increased risk of
cardiac depression
 Digoxin: additive slowing of AV node conduction
 Atracurium, pancuronium, vecuronium: increased
respiratory depression
 Increased risk of cardiac depression if IV preparation
of these drugs were given 48 hours within
administration of IV beta-adrenergic blockers.
 Diltiazem can increase serum level of cyclosporine.
Nursing Responsibility
 Titrate the dose to the smallest amount enough to
manage arrhythmia to decrease the risk of drug
toxicity.
 Monitor cardiac rhythm closely to detect potentially
serious adverse effects and to evaluate drug
effectiveness.
 Provide comfort and safety measures (e.g., raising
side rails, adequate room lighting, noise control) to
help patients tolerate drug effects.
 Ensure maintenance of emergency drugs and
equipment at bedside to promote prompt treatment in
cases of severe toxicity.
 Educate patients on drug therapy including drug
name, its indication, and adverse effects to watch out
for to enhance patient understanding on drug therapy
and thereby promote adherence to drug regimen.
Lesson 4: Antianginal Agents
Antianginal Agents used primarily to restore the balance
between the oxygen supply and demand of the heart. These
drugs dilate the coronary vessels to increase the flow of
oxygen to the ischemic regions. Other than that, they
also decrease the workload of the heart so the organ would
have less demand for oxygen. 
NITRATES
Nitrates are antianginal agents that provide fast action to
directly relax smooth muscles and depress muscle tone
without affecting nerve activity.
Nitrates reduce preload and myocardial muscle tension by
dilating the veins. Also, they reduce afterload by dilating the
arteries. Both of these actions lower oxygen demand by
decreasing the workload of the heart.
Therapeutic Action
 The main effect is a drop in systemic blood pressure.
 It compensates by increasing blood flow to healthy
arteries and veins because affected vessels already
lose their elasticity.
Indications
 Use during pregnancy is not established.
 Sublingual nitroglycerin is most effective for recurrent
variant angina.
 Continuous infusion or transdermal patch for unstable
angina.
Contraindications and Cautions
 Allergy to nitrates – prevent hypersensitivity reactions
 Severe anemia – decreased cardiac output (CO)
caused by nitrates is dangerous for blood with low-
oxygen binding capacity
 Head trauma and cerebral hemorrhage – relaxation of
cerebral vessels can lead to intracranial bleeding
 Pregnancy and lactation – potential harm to fetus
 Hepatic and renal disease – alteration in drug
metabolism and excretion
 Conditions that can limit CO (e.g., hypovolemia,
hypotension, etc.
Adverse Effects
 CNS: throbbing headache, dizziness, weakness
 GI: nausea, vomiting, incontinence
 CV: hypotension, reflex tachycardia, syncope
 EENT: pallor, flushing, sweating
 Large dose leads to methemoglobinemia and
cyanosis.
Interactions
 Ergot derivatives: risk for hypertension; decreased
antianginal effect
 Heparin: decreased therapeutic effect of nitrates
 PDE-5 inhibitors: risk for severe hypotension
Nursing Responsibility
 Instruct patients not to swallow sublingual
preparations to ensure therapeutic effects. Take three
tablets with a 5-minute interval, for a total of three
doses. If the pain does not subside, seek medical
help.
 Ask for presence of burning sensation to ensure drug
potency.
 Protect drug from sunlight to maintain drug potency.
18 | P a s c u a l , A i r i n e A .
  For sustained release forms, take drug with water and
do not crush for these preparations need to reach GIT
intact.
 Rotate injection sites and provide skin care as
appropriate to prevent skin abrasion and breakdown.
 Avoid abrupt stop of long-term therapy. Taper doses
for 4-6 weeks to prevent myocardial infarction.
 Provide comfort measures: small frequent meals,
appropriate room temperature and lights, noise
reduction, ambulation assistance, reorientation, and
skin care.
BETA-ADRENERGIC BLOCKERS
Beta-adrenergic blockers are drugs which block or lyse the
effects of sympathetic stimulation. Hence, they are also
called sympatholytics.
Therapeutic Action
 Main effects include decreased blood pressure,
contractility, and heart rate by blocking the beta-
receptors in the heart and juxtaglomerular apparatus
of the kidneys. These combined effects reduce the
oxygen demand of the heart.
 Usually used in therapy with nitrates because of
reduced adverse effects and increased exercise
tolerance.
 Not indicated for variant angina because therapeutic
effect of drugs can cause vasospasm.
Indications
 Nadolol is used for management of chronic angina. It
is the drug of choice in angina patients with
hypertension.
 Propranolol is the prototype drug of this class. It is
used for the treatment of angina and syncope.
 Nebivolol, the newest adrenergic blocking agent,
does not produce the same adverse effects seen in
propranolol.
Contraindications and Cautions
 Bradycardia, heart block, and cardiogenic shock –
blocking effect of drugs exacerbates these conditions
 Pregnancy and lactation – potentially harmful effects
to the fetus or neonate
 Diabetes, chronic obstructive pulmonary disease
(COPD), thyrotoxicosis, and peripheral vascular
diseases – blocking effect prevents maintaining
homeostatic requirements of these diseases
Adverse Effects
 CNS: emotional depression, dizziness, fatigue, sleep
disturbances
 GI: gastric pain, nausea, vomiting, colitis, diarrhea
 CV: heart failure, reduced cardiac output, arrhythmia
 Respiratory: dyspnea, cough, bronchospasm
Interactions
 Clonidine: increased rebound hypertension
 NSAIDs: decreased antihypertensive effects
 Epinephrine: hypertension followed by bradycardia
 Ergot alkaloids: peripheral ischemia
 Insulin and oral hypoglycemic agents: alteration in
blood glucose levels without the patient experiencing
manifestations of hypo- or hyperglycemia
Nursing Responsibility
 Give drug as ordered following safe and appropriate
administration to ensure therapeutic effects.
 Provide comfort measures: ambulation assistance,
raised siderails, appropriate room light and
temperature, and rest periods
 Monitor cardiopulmonary status closely to detect
possible alterations in vital signs which signal need for
dose adjustment and to prevent related adverse
effects.
 Educate client about the need to not abruptly stop
therapy as this can lead to rebound hypertension and
myocardial infarction.
CALCIUM-CHANNEL BLOCKERS
Calcium-channel blockers are drugs which block heart
contraction by inhibiting movement of calcium ions, thereby
altering arterial and cardiac muscle action potentials.
They basically produce vasodilation and relief of spasm. They
do not increase lipid levels.
Serve as a substitute for classic and variant angina when beta-
blockers and nitrates are contraindicated.
Therapeutic Action
 By blocking contractions, loss of muscle tone and
vasodilation occur, consequently decreasing
peripheral resistance.
19 | P a s c u a l , A i r i n e A .
  Relieves vasospasm in variant angina, thereby
increasing blood flow to the heart.
 Can block atherosclerotic process in endothelial cells
Indications
 Treatment of variant angina, chronic angina and
effort-associated angina
Contraindications and Cautions
 Allergy to drugs
 Heart block and sick sinus syndrome – conduction
problems in this disease may be exacerbated by slow
conduction effect of drugs
 Renal and hepatic dysfunctions – alteration with
metabolism and excretion of drugs
 Heart failure – worsened by decreased cardiac output
effect of the drug.
Adverse Effects
 CNS: dizziness, lightheadedness, fatigue, and
headache
 GI: nausea, hepatotoxicity effect of the drug
 CV: hypotension, bradycardia, peripheral edema
 EENT: flushing, rash
Interactions
 Cyclosporine with diltiazem: increased serum level
and toxicity of cyclosporine
 Cyclosporine with verapamil: heart block and digoxin
toxicity. Verapamil increases level of digoxin.
 Digoxin with verapamil: depressed myocardial
conduction
 General anesthesia with verapamil: serious
respiratory distress
Nursing Responsibility
 Monitor blood pressure and heart rate and rhythm to
detect possible development of adverse effects.
 Provide comfort measures for the patient to tolerate
side effects (e.g. small frequent meals for nausea,
limiting noise and controlling room light and
temperature to prevent aggravation of stress which
can increase demand to the heart, etc.)
 Educate client on measures to avoid angina attacks
(e.g. diet changes, rest periods, etc.)
 Emphasize to the client the importance of strict
adherence to drug therapy to ensure maximum
therapeutic effects.
Lesson 5: Lipid Lowering Agents
Antihyperlipidemic Drugs lower serum levels
of cholesterol and various lipids. They are also called as lipid-
lowering agents; these drugs provide effective treatment for
hyperlipidemia (increased lipid level in the blood).
BILE ACID SEQUESTRANTS
These drugs are used to normalize high serum level of
cholesterol.
Therapeutic Action
 Bile acid sequestrants exert their effect in the
intestines by binding into bile acids which contain
a high level of cholesterol.
 The resultant insoluble complex formed by this
combination is then excreted through feces.
 As this happens, more LDL segments from the
circulation will be absorbed by the intrahepatic
circulation to make more bile acids.
Indications
 Bile Acid Sequestrants are used as the treatment for
primary hypercholesterolemia (high cholesterol and
high LDL) as an adjunct to diet and exercise.
 Cholestyramine is also used to treat pruritus
associated with partial biliary obstruction.
Interactions
 Bile acid sequestrants delay the absorption of thiazide
diuretics, corticosteroids, digoxin, warfarin, and
thyroid hormones. Therefore, if needed, these drugs
are taken 1 hour before or 4-6 hours after a meal.
Contraindications and Cautions
 Allergy to bile acid sequestrants. Prevent severe
hypersensitivity reactions.
 Complete biliary obstruction. Prevent bile from
being secreted into the intestines.
 Abnormal intestinal function. Aggravated by the
presence of bile acid sequestrants.
 Pregnancy and lactation. Potential decrease in
absorption of fat and fat-soluble vitamins can be
detrimental to fetus or neonate.
Adverse Effects
 CNS: headache, anxiety, fatigue, drowsiness
 GI: GI upset, constipation, fecal impaction, nausea,
aggravated hemorrhoids
 Hema: increased bleeding time, decreased
production of clotting factors
 Musculoskeletal: muscle aches, muscle pains
 Other: rash, fat-soluble vitamin deficiencies
Nursing Responsibility
 Administer powdered agents already mixed with
fluids to ensure drug effectiveness.
20 | P a s c u a l , A i r i n e A .
  Instruct client not to chew, crush, and cut
tablets because these drugs are meant to be broken
down in the intestines and premature crushing will
render active ingredients ineffective.
 Administer drug before meals to ensure that drug is
in the GI tract together with food.
 Administer other drugs 1 hour before or 4-6 hours
after bile acid sequestrants to avoid drug
interactions.
 Arrange for a bowel program to effectively address
constipation if it ever occurs.
 Instruct patients to increase oral fluid intake and
dietary fiber intake to prevent constipation.
 Provide comfort measures (e.g., small frequent
meals for GI upset and instituting safety measures for
drowsiness and weaknesses) to help patients tolerate
drug effects.
 Educate patients on drug therapy including drug
name, its indication, and adverse effects to watch out
for to enhance patient understanding of drug therapy
and thereby promote adherence to drug regimen.
HMG-COA REDUCTASE INHIBITORS
HYDROXYMETHYLGLUTARYL – COENZYME A
REDUCTASE INHIBITOR.
This drug group increases the cell absorption of LDL by
blocking the enzyme (HMG-CoA reductase) regulating the
rate-limiting step in the synthesis of cholesterol. With this
alteration in fat metabolism, HDL increases slightly.
Drugs under this classification are chemically modified
compounds from the products of fungi.
Therapeutic Action
 In a sense, HMG-CoA reductase inhibitors block the
completion of cholesterol synthesis in the body.
 These are primarily indicated as adjunct medicine
with diet and exercise for treatment of high cholesterol
and LDL levels in the blood.
Indications
 Pravastatin, lovastatin, and simvastatin are indicated
for patients with documented CAD to slow
progression of the disease.
 Together with these three agents, atorvastatin is used
as prophylaxis for first myocardial infarction attack for
patients with multiple risk factors for CAD.
Contraindications and Cautions
 Allergy to HMG-CoA reductase inhibitors. Prevent
severe hypersensitivity reactions.
 Active liver disease. Exacerbated by the drug’s
therapeutic effect and has potential to lead to severe
liver failure.
 Pregnancy, lactation. Potential for drug adverse
effects to fetus or neonate.
 Impaired endocrine function. Problems can arise
due to alteration in the formation of steroid hormones.
 Renal impairment. Caution is given to patients taking
other statins and close monitoring in instituted.
Atorvastatin is not affected by renal diseases.
Adverse Effects
 CNS: headache, dizziness, insomnia, fatigue, blurred
vision, cataract development
 CV: increased risk for cardiovascular effects with
simvastatin started at 80 mg for new patients
 GI: flatulence, nausea, vomiting, cramps, abdominal
pain, constipation
 Hepatobiliary: increase liver enzymes, acute liver
failure with use of atorvastatin and fluvastatin
Interactions
 Cyclosporine, erythromycin, gemfibrozil, niacin,
antifungal drugs: increased risk for rhabdomyolysis
 Digoxin, warfarin: increased serum levels and
resultant toxicity of HMG-CoA reductase inhibitors
 Oral contraceptives: increased serum estrogen
 Grapefruit juice: increased serum levels and
resultant toxicity
Nursing Responsibility
 Administer drug at bedtime to maximize
effectiveness of the drug because peak of cholesterol
synthesis is from midnight to 5 AM. However,
atorvastatin can be given at any hour of the day.
 Monitor serum cholesterol and LDL levels to
determine effectiveness of drug therapy.
 Monitor results of liver functions tests to
determine possible liver damage.
 Ensure patient has initiated a 3–6-month diet and
exercise program before initiating drug therapy to
ensure need for drug therapy.
 Emphasize the importance of lifestyle changes to
the patient to decrease risk of CAD and promote drug
effectiveness.
 Provide comfort and safety measures to help
patients tolerate drug side effects.
 Educate patients on drug therapy including drug
and adverse effects to
name, its indication,
watch out for to enhance patient
understanding on drug therapy and thereby
promote adherence to drug regimen.
CHOLESTEROL ABSORPTION INHIBITORS
21 | P a s c u a l , A i r i n e A .

Cholesterol absorption inhibitors are one of the new class of
drugs approved (2003) to lower serum cholesterol levels.
Therapeutic Action
 Acting on the brush border of intestines, cholesterol
absorption inhibitors block the absorption of dietary
cholesterol. Consequently, less cholesterol goes to
the liver, and it increases the cholesterol clearance to
make up for the drop.
Indications
 Adjunct to diet and exercise as a monotherapy or in
combination with HMG-CoA inhibitors or bile acid
sequestrants.
 Used in combination with statins to treat homozygous
familial hypercholesterolemia.
Contraindications and Cautions
 Allergy to cholesterol absorption inhibitors.
Prevent severe hypersensitivity reactions.
 Liver disease, pregnancy, lactation: not used if
combined with statins because of the effects of statins
to these health conditions. The effect of this class on
fetuses and neonates is not known.
Adverse Effects
 CNS: headache, dizziness, fatigue
 Respiratory: upper respiratory tract infection (URI)
 GI: mild abdominal pain, diarrhea
 Musculoskeletal: muscle aches and pains, back pain
Interactions
 Cholestyramine, fenofibrate, antacid,
gemfibrozil: elevated serum level of cholesterol
absorption inhibitors
 Cyclosporine: increased toxicity of cholesterol
absorption inhibitors
 Fibrates: increased risk for development of
cholelithiasis
 Warfarin: increased serum warfarin levels
Nursing Responsibility
 Monitor serum cholesterol and LDL levels. To
determine the effectiveness of drug therapy.
 Monitor results of liver functions tests. To
determine possible liver damage.
 Ensure patient has initiated a 3–6-month diet and
exercise program before initiating drug
therapy. To ensure the need for drug therapy.
 Emphasize the importance of lifestyle changes. To
the patient to decrease the risk of CAD and promote
drug effectiveness.
 Provide comfort and safety measures. To help
patients tolerate drug side effects.
 Educate patients on drug therapy.  Include in the
teaching plan the drug name, its indication, and
adverse effects to watch out for to enhance patient
understanding of drug therapy and thereby promote
adherence to the drug regimen.
Lesson 6: Drugs Affecting Blood
Coagulations
These groups of drugs affect clot formation and resolution by
hindering different steps in clotting formation which include
altering the formation of platelet plug (antiplatelet drugs),
interfering the clotting cascade and thrombin formation
(anticoagulant drugs), and stimulating the plasmin system to
break down the formed clot (thrombolytic agents).
ANTIPLATELET AGENTS
This drug class exerts its action by decreasing the
responsiveness of platelets to stimuli that cause it to clump or
aggregate. Through this, formation of platelet plug is
decreased.
Therapeutic Action
 By blocking receptor sites on the platelet membrane,
platelet adhesion and aggregation is inhibited.
 Also, platelet-platelet interaction as well as interaction
of platelets to clotting chemicals are prevented.
Indications
 Primarily indicated for cardiovascular diseases that
have potential for development of vessel occlusion.
 Other indications include maintenance of arterial and
venous grafts, preventing cerebrovascular occlusion,
and including them as an adjunct to thrombolytic
therapy for treatment of myocardial infarction.
 One drug, anagrelide, blocks the production of
platelets in bone marrow.
Contraindications and Cautions
 Allergy to antiplatelet agents. Prevent severe
hypersensitivity reactions.
 Known bleeding disorder. Increased risk of
excessive blood loss
 Recent surgery. Increased risk of bleeding in
unhealed blood vessels
22 | P a s c u a l , A i r i n e A .
  Closed head injuries. Increased risk of bleeding in
injured blood vessels of the brain
 History of thrombocytopenia. Anagrelide decreased
bone marrow production of platelets.
 Pregnancy, lactation. Generally inadvisable because
of potential adverse effects to fetus or neonate
Adverse Effects
 CNS: headache, dizziness, weakness
 GI: GI distress, nausea
 Skin: skin rash
 Hema: bleeding (oftenly occurs while brushing the
teeth)
Interactions
 Increased risk of bleeding if combined with another
drug that affects blood clotting.
Nursing Responsibility
 Administer drug with meals to relieve GI upset.
 Provide comfort measures for headache because
pain due to headache may decrease patient
compliance to treatment regimen.
 Educate patients on ways to promote safety like using
electric razor, soft-bristled toothbrush, and cautious
movement because any injury at this point can
precipitate bleeding.
 Educate patients on drug therapy including drug
name, its indication, and adverse effects to watch out
for to enhance patient understanding on drug therapy
and thereby promote adherence to drug regimen.
Anticoagulants
By interfering with clotting cascade and thrombin
formation, anticoagulants are able to interfere with the normal
clotting process.
Therapeutic Action
 Warfarin, an oral agent in this class, reduces Vitamin
K-dependent clotting factors. As a result, the clotting
process is prolonged.
 Two new oral agents, dabigatran and rivaroxaban,
directly inhibit thrombin (last step in clotting process)
and factor Xa, respectively.
 Heparin and antithrombin block formation of thrombin
from prothrombin.
Indications
 Among the many indications for this drug class
include stroke and systemic emboli risk reduction,
nonvalvular atrial fibrillation, and deep vein
thrombosis.
 Heparin is used for prevention of blood clots in blood
samples, dialysis, and venous tubing. It also does not
enter breastmilk, so it is the anticoagulant of choice
for lactating women.
 Antithrombin is a naturally occurring anticoagulant
and is a natural safety feature in the clotting system.
Contraindications and Cautions
 Allergy to anticoagulants. Prevent severe
hypersensitivity reactions.
 Known bleeding disorder, recent trauma/surgery,
presence of indwelling catheters, threatened
abortion, GI ulcers. These conditions can be
compromised by increased bleeding tendencies.
 Pregnancy, lactation. Warfarin is a contraindication.
Interactions
 Anticoagulants, salicylates, penicillin, cephalosporin:
increased bleeding if combined with heparin
 Nitroglycerin: decreased anticoagulation if combined
with heparin
 Cimetidine, clofibrate, glucagon, erythromycin:
increased bleeding if combined with warfarin
 Vitamin K, phenytoin, rifampin, barbiturates:
decreased anticoagulation if combined with warfarin
 Antifungals, erythromycin, phenytoin, rifampin:
alteration in metabolism of dabigatran and
rivaroxaban
Adverse Effects
 Warfarin is associated with alopecia, dermatitis, bone
marrow depression, and less frequently with
prolonged and painful erections
 Direct drug toxicity is characterized by nausea, GI
upset, diarrhea, and hepatic dysfunction.
Nursing Responsibility
 Assess signs signifying blood loss (e.g. petechiae,
bruises, dark-colored stools, etc.) to determine
therapy effectiveness and promote prompt
intervention for bleeding episodes.
 Establish safety precautions (e.g., raising side rails,
ensuring adequate room lighting, padding sides of
bed, etc.) to protect patient from injury.
 Maintain antidotes on bedside (e.g., protamine sulfate
for heparin, Vitamin K for warfarin) to promptly treat
drug overdose.
 Evaluate effectiveness by monitoring the following
blood tests: prothrombin time (PT) and international
normalized ratio (INR) for warfarin; and whole blood
clotting time (WBCT) and activated partial
thromboplastin time (APTT) for heparin.
 Educate patients on drug therapy including drug
name, its indication, and adverse effects to watch out
for to enhance patient understanding on drug therapy
and thereby promote adherence to drug regimen.
23 | P a s c u a l , A i r i n e A .
 THROMBOLYTIC AGENTS
Thrombolytic agents promote clot resolution, the process of
activating the plasmin system to break down the thrombus or
clot that has been formed.
Therapeutic Action
 The conversion of plasminogen to plasmin is the
body’s natural anticlotting system. Thrombolytic
agents’ action to activate this promotes breakdown of
fibrin threads and dissolution of formed clots.
 It is necessary to prevent vessel occlusion and
therefore, to deliver adequate blood flow to body
systems.
Indications
 For treatment of acute MI, pulmonary embolism, and
acute ischemic stroke.
 Also, for clearing of occluded intravenous catheters
and central venous access devices.
Contraindications and Cautions
 Allergy to thrombolytics. Prevent severe
hypersensitivity reactions.
 Known bleeding disorder, recent trauma/surgery,
acute liver disease, cerebrovascular accident
within 2 months, GI ulcers. These conditions can
affect normal clotting factors and normal plasminogen
production.
 Pregnancy, lactation. Potential adverse effects to
fetus or neonate.
Adverse Effects
 CV: cardiac arrhythmias, hypotension
 Hema: bleeding (most common)
 Hypersensitivity reaction (uncommon) is
characterized by rash, flushing, and bronchospasm.
Interactions
 Anticoagulant, antiplatelet: increased risk of bleeding
Nursing Responsibility
 Assess signs signifying blood loss (e.g., petechiae,
bruises, dark-colored stools, etc.) to determine
therapy effectiveness and promote prompt
intervention for bleeding episodes.
 Establish safety precautions (e.g., raising side rails,
ensuring adequate room lighting, padding sides of
bed, etc.) to protect patient from injury.
 Evaluate effectiveness by monitoring coagulation
studies to adjust drug dose appropriately.
 Educate patients on drug therapy including drug
name, its indication, and adverse effects to watch out
for to enhance patient understanding on drug therapy
and thereby promote adherence to drug regimen.
Lesson 7: Drugs Used to Treat Anemias
ERYTHROPOIESIS-STIMULATING AGENTS
agents are used to activate the bone marrow to produce more
RBCs, it is necessary to ensure that the patient has sufficient
quantities of the components needed to make RBCs, including
sufficient iron.
Therapeutic Action
 promote the development of RBCs in the bone
marrow.
Indications
 prevention of anemia associated with renal failure and
for patients on dialysis; for anemia associated with
AIDS therapy; and for anemia associated with cancer
chemotherapy where the bone marrow is depressed
and the kidneys may be impaired by toxic drugs
(Procrit only).
Contraindications and Cautions
 presence of unregulated hypertension due to the
possibility of more hypertension as RBC numbers rise
and strain inside the vascular system increases.
 with documented hypersensitivity to every part of the
medication to prevent hypersensitivity reactions.
 with lactation due to the potential for allergic-type
neonatal reactions.
Adverse Effects
 CNS: weakness, asthenia and dizziness on the CNS
and the risk for severe seizures
 GI: Nausea, vomiting, and diarrhea
 CV: hypertension, edema, and even chest pain, both
of which may be linked to a rise in RBC numbers that
may alter the equilibrium within the cardiovascular
system.
AGENTS USED FOR IRON DEFICIENCY
ANEMIA
24 | P a s c u a l , A i r i n e A .
 Therapeutic Action
 cell growth and division and for the formation of high
stroma in RBCs

Indications
 replacement medication for food disorders, as a
supplement in high-demand conditions such as
maternity and lactation, and for the treatment of
megaloblastic anemia

Contraindications and Cautions

Therapeutic Action
 allergy to any part of the medication
 improve the concentration of blood iron.  caution in the case of compromised liver or kidney
activity,
Indications
Adverse Effects
 treatment of iron deficient anemia and can also be
used as an adjunctive therapy in patients taking an  cytotoxic and is associated with adverse effects
erythropoietic-stimulating drug associated with the death of cells, especially in cells
that are rapidly turning over.
Contraindications and Cautions
Interactions
 known allergy to any of these formulations because
extreme hyper-sensitivity reactions have been  elevated risk of uric acid levels when this drug is
correlated with the parenteral type of iron. paired with other uricosuric agents

Adverse Effects Agent for Sickle Cell Anemia

 GI: GI pain, including GI discomfort, anorexia, fatigue,
vomiting, diarrhea, dark stools, and constipation

Interaction
Therapeutic Action
 Increased levels of iron occur as iron preparations are
taken with chloramphenicol  increases the amount of fetal hemoglobin formed in
 Decrease Anti-infective reaction with ciprofloxacin, the bone marrow and dilutes the development of
norfloxacin, or ofloxacin taken with iron due to defective hemoglobin S in adults with sickle cell
reduced absorption anemia
 antacids, tetracyclines or cimetidine: Reduce
absorption of Iron Indications
 Acid liquids should increase the absorption of iron
 Iron is not absorbed if taken with antacids, eggs, milk,  Primary indication for Sickle Cell Anemia
coffee, or tea.

Agent for Megaloblastic Anemia

25 | P a s c u a l , A i r i n e A .
MODULE 10
DRUGS ACTING ON THE RENAL SYSTEM
Lesson 1: Thiazide and Thiazide-like Diuretics
Thiazide diuretics belong to a chemical class of drugs
called sulfonamides. Thiazide-like diuretics have different
chemical structure but work in the same mechanism as that of
thiazide diuretics.
This is among the most commonly used classes of diuretics.
Therapeutic Action
 It causes active pumping out of chloride from the cells
lining the ascending limb of Loop of Henle and distal
tubule by blocking the chloride pump. Since sodium
passively moves with chloride to maintain electrical
neutrality, both sodium and chloride are excreted in
the urine.
Indication
 Considered to be a milder form of diuretics compared
to loop diuretics.
 First-line drugs for management of essential
hypertension
Contraindications and Cautions
 Allergy to loop diuretics. Prevent severe
hypersensitivity reactions.
 Fluid and electrolyte imbalances. Can be
potentiated by the changes in fluid and electrolyte
levels caused by diuretics.
 Severe renal failure, anuria. May prevent diuretics
from working; can precipitate crisis stage due to blood
flow changes brought about by diuretics.
 Systemic lupus erythematosus (SLE).  Can
precipitate renal failure because the disease already
causes changes in glomerular filtration.
 Glucose tolerance abnormalities and diabetes
mellitus. Worsened by glucose-elevating effect of
some diuretics
 Gout. Already reflects abnormality in tubular
reabsorption and secretion.
 Liver disease. Could interfere with drug metabolism
and lead to drug toxicity.
 Bipolar disorder. Can be exacerbated by calcium
changes brought about by the use of this drug.
 Pregnancy, lactation. Can cause potential adverse
effects to the fetus and baby. Routine use of this drug
in pregnancy is not appropriate and should be used
only when there is underlying pathological conditions.
For lactating women, an alternative method of feeding
should be instituted.
Adverse Effects
 CNS: weakness
 CV: hypotension, arrhythmias
 GI: GI upset
 GU: hypokalemia (can precipitate hyperglycemia),
hypercalcemia, hyperuremia, slightly alkalinized urine
(can lead to bladder infections)
Interactions
 Cholestyramine or colestipol: decreased absorption of
diuretics; must be taken separated by at least 2
hours.
 Digoxin: increased risk for digoxin toxicity because of
changes in serum potassium levels
 Quinidine: increased risk for quinidine toxicity
 Antidiabetic agents: decreased effectivity of
antidiabetics
 Lithium: increased risk for lithium toxicity
Lesson 2: Loop Diuretics
This type of diuretic exerts its main effect on the loop of Henle.
Hence, so named.
Referred to as high-ceiling diuretics because they are
capable of causing greater degree of diuresis compared to
other types.
Therapeutic Action
 Blocks the action of chloride pump in the ascending
limb of the loop of Henle, where 30% of sodium is
normally reabsorbed. This causes decreased
reabsorption of chloride and sodium.
 Exerts the same effect on the descending limb of loop
of Henle and distal tubule causing sodium-rich urine.
Indication
 Indicated for treatment of acute HF, acute pulmonary
edema, and edema associated with HF or with renal
or liver disease, and hypertension.
 Drug of choice when rapid and extensive diuresis is
needed. It can produce a fluid loss up to 20 pounds
per day.
26 | P a s c u a l , A i r i n e A .
  Proven to be effective even with the presence of acid-
base disturbances, renal failure, electrolyte
imbalances, and nitrogen retention.
 Also used in the treatment of pulmonary edema but its
effect only influences the blood that reaches the
nephrons.
 Ethacrynic acid is used less frequently in the clinical
setting because newer drugs are more potent and
reliable.
Contraindications and Cautions
 Allergy to thiazides and sulfonamides. Prevent severe
hypersensitivity reactions.
 Electrolyte depletion. Can be potentiated by the
changes in fluid and electrolyte levels caused by
diuretics.
 Severe renal failure, anuria. Exacerbated by the
effects of the drug.
 Systemic lupus erythematosus (SLE).  Can precipitate
renal failure because the disease already causes
changes in glomerular filtration.
 Glucose tolerance abnormalities and diabetes
mellitus. Worsened by glucose-elevating effect of
some diuretics
 Gout. Already reflects abnormality in tubular
reabsorption and secretion.
 Hepatic coma. Exacerbated by fluid shifts associated
with drug use.
 Pregnancy, lactation. Can cause potential adverse
effects to the fetus and baby. Routine use of this drug
in pregnancy is not appropriate and should be used
only when there is underlying pathological conditions.
For lactating women, an alternative method of feeding
should be instituted.
Adverse Effects
 CNS: dizziness
 CV: hypotension
 GI: GI upset
 GU: hypokalemia (can precipitate hyperglycemia),
increased bicarbonate excretion (can lead to
alkalosis), hypocalcemia and tetany
 EENT: ototoxicity, reversible loss of hearing
Interactions
 Aminoglycosides or cisplatin: increased ototoxicity
effect of loop diuretics
 Anticoagulants: increased anticoagulation effects
 Indomethacin, ibuprofen, salicylates and other
NSAIDs: decreased antihypertensive effects and loss
of sodium
Lesson 3: Carbonic Anhydrase Inhibitors
Relatively mild diuretics
Therapeutic Action
 Inhibits the action of the enzyme carbonic
anhydrase, the catalyst for the formation of sodium
bicarbonate stored as alkaline reserve in the renal
tubules and is important for the excretion of hydrogen.
 It slows down the movement of hydrogen ions which
leads to greater amounts of sodium and bicarbonate
lost in the urine.
Indication
 Most often used for the treatment of glaucoma.
Inhibition of carbonic anhydrase results in decreased
secretion of aqueous humor of the eyes.
 Also used as adjunct to other diuretics when more
intense diuresis is needed.
Contraindications and Caution
 Allergy to carbonic anhydrase inhibitors,
thiazides, antibacterial sulfonamides. Prevent
severe hypersensitivity reactions.
 Chronic noncongestive angle-closure
glaucoma. Not effectively treated by this drug.
 Fluid and electrolyte imbalance, renal or hepatic
disease, adrenocortical insufficiency, respiratory
acidosis, chronic obstructive pulmonary disease
(COPD). Could be exacerbated by fluid and
electrolyte changes caused by these drugs.
 Pregnancy, lactation. Can cause potential adverse
effects to the fetus and baby. Routine use of this drug
in pregnancy is not appropriate and should be used
only when there is underlying pathological conditions.
For lactating women, an alternative method of feeding
should be instituted.
Adverse Effects
 CNS: paresthesia, confusion, drowsiness
 CV: hypotension
 GU: hypokalemia (can precipitate hyperglycemia),
increased loss of bicarbonate (can lead to metabolic
acidosis)
Interactions
 Salicylate, lithium: increased excretion of these drugs
Lesson 4: Potassium Sparing Diuretics
27 | P a s c u a l , A i r i n e A .
Less powerful than loop diuretics but they retain potassium
instead of wasting it.
Typically used for patients who have high risk for hypokalemia
associated with diuretic use.
Therapeutic Action
 This type of diuretic causes a loss of sodium while
promoting the retention of potassium.
 Spironolactone acts as aldosterone antagonist which
blocks the action of aldosterone in the distal tubule.
On the other hand, amiloride and triamterene block
potassium secretion through the tubule.
Indication
 This is often used as adjuncts with thiazide or loop
diuretics or in patients who are especially at risk if
hypokalemia develops.
 Spironolactone is the drug of choice for
treating hyperaldosteronism typically seen in
patients with liver cirrhosis and nephrotic syndrome.
Contraindications and Cautions
 Allergy to potassium-sparing diuretics. Prevent
severe hypersensitivity reactions.
 Hyperkalemia, renal disease, anuria. Exacerbated
by the effects of the drug.
 Pregnancy, lactation. Can cause potential adverse
effects to the fetus and baby. Routine use of this drug
in pregnancy is not appropriate and should be used
only when there is underlying pathological conditions.
For lactating women, an alternative method of feeding
should be instituted.
Adverse Effects
 CNS: lethargy, confusion, ataxia
 CV: arrhythmias
 Musculoskeletal: muscle cramps
 GU: hyperkalemia, increased loss of bicarbonate (can
lead to metabolic acidosis)
 Associated with various androgen effects such as
hirsutism, gynecomastia, deepening of the voice, and
irregular menses.
Interactions
 Salicylates: decreased diuretic effect
Lesson 5: Osmotic Diuretics
This type of diuretic exerts their therapeutic effect by pulling
water into the renal tubule without loss of sodium.
Only one osmotic diuretic is currently
available, mannitol (Osmitrol).
Therapeutic Action
 Mannitol is a sugar that is not well reabsorbed by the
tubules, and it acts to pull large amounts of fluid into
the urine due to the osmotic pull exerted by large
sugar molecule.
 This also pulls fluid into the vascular system from
extravascular spaces like aqueous humor.
Indication
 Mannitol is usually used in acute situations when it is
necessary to decrease IOP before eye surgery or
during acute attacks of glaucoma.
 Diuretic of choice in cases of increased cranial
pressure or acute renal failure due to shock, drug
overdose, or trauma.
 Also available as an irrigant in transurethral prostatic
resection and other transurethral procedures.
Contraindications and Cautions
 Renal disease, anuria, pulmonary congestion,
intracranial bleeding, dehydration,
HF. Exacerbated by large shifts in fluid related to drug
use.
 Pregnancy, lactation. Can cause potential adverse
effects to the fetus and baby. Routine use of this drug
in pregnancy is not appropriate and should be used
only when there is underlying pathological conditions.
For lactating women, an alternative method of feeding
should be instituted.
Adverse Effects
 CNS: light-headedness, confusion, headache
 CV: hypotension, cardiac decompensation, shock
 GI: nausea, vomiting
 GU: fluid and electrolyte imbalance
 Most common and potentially dangerous adverse
effect related to an osmotic diuretic is the sudden
drop in fluid levels.
Nursing Responsibility: Diuretics
• Administer drug with food or milk if GI upset is a problem to
buffer drug effect on the stomach lining.
• Administer intravenous diuretics slowly to prevent severe
changes in fluid and electrolytes.
• Administer oral form early in the day to prevent increased
urination during sleep hours.
• Monitor patient response to drugs through vital signs, weight,
serum electrolytes and hydration to evaluate effectiveness of
drug therapy.
• Assess skin condition to determine presence of fluid volume
deficit or retention.
• Provide comfort measures (e.g. skin care, nutrition referral,
etc.) to help patient tolerate drug effects.
28 | P a s c u a l , A i r i n e A .
MODULE 11
DRUGS ACTING ON THE RESPIRATORY
SYSTEM
Lesson 1: Introduction to the Respiratory
System
FUNCTIONS OF THE RESPIRATORY SYSTEM
 Oxygen supplier. The job of the respiratory system is
to keep the body constantly supplied with oxygen.
 Elimination. Elimination of carbon dioxide.
 Gas exchange. The respiratory system organs
oversee the gas exchanges that occur between the
blood and the external environment.
 Passageway. Passageways that allow air to reach
the lungs.
 Humidifier. Purify, humidify, and warm incoming air.
Lesson 2: Bronchodilators
Bronchodilators or antiasthmatics are medications used to
facilitate respiration by dilating the airways. They are helpful in
symptomatic relief or prevention of bronchial asthma and for
bronchospasm associated with COPD.
XANTHINES
The xanthines come from a variety of naturally occurring
sources. These drugs were once the main treatment choices
for asthma and bronchospasm. However, because they have a
relatively narrow margin of safety and interact with many other
drugs, they are no longer considered the first-choice
bronchodilators.
Therapeutic actions of Xanthines
 A direct effect on the smooth muscles of the
respiratory tract, both in the bronchi and in the blood
vessels.
 A theory suggests that xanthines work by directly
affecting the mobilization of calcium within the cell.
 They do this by stimulating two prostaglandins,
resulting in smooth muscle relaxation, which
increases the vital capacity that has been impaired by
the bronchospasm or air trapping.
 Xanthines also inhibit the release of slow-reacting
substance of anaphylaxis and histamine, decreasing
the bronchial swelling and narrowing that occurs as a
result of these two chemicals.
Indications
 Relief of symptoms or prevention of bronchial asthma.
 Reversal of bronchospasm associated with COPD.
Contraindications and Cautions
 Co-morbidities. Caution should be taken with any
patient with GI problems, coronary disease,
respiratory dysfunction, renal or hepatic disease,
alcoholism, or hyperthyroidism because these
conditions can be exacerbated by the systemic effects
of xanthines.
 Long-term parenteral use. Xanthines are available
for oral and parenteral use; the parenteral drug should
be switched to oral form as soon as possible because
the systemic effects of the oral form are less acute
and more manageable.
 Pregnancy. Although no studies are available of
xanthine effects on human pregnancy, they have
been associated with fetal abnormalities and
breathing difficulties at birth in animal studies, so use
should be limited to situations in which the benefit to
the mother clearly outweighs the potential risk to the
fetus.
 Lactation. Because the xanthines enter breastmilk
and could affect the baby, another method of feeding
the baby should be selected if these drugs are
needed during lactation.
Adverse Effects
 CNS: Irritability, restlessness, dizziness.
 Cardiovascular: Palpitations, life-threatening
arrhythmias.
 Others: Loss of appetite, fever, flushing.
 GU: Proteinuria.
 Respiratory: Respiratory arrest.
Interactions
 Nicotine. Nicotine increases the metabolism of
xanthines in the liver; xanthine dose must be
increased in patients who continue to smoke while
using xanthines.
SYMPATHOMIMETICS
 Sympathomimetics are drugs that mimic the effects
of the sympathetic nervous system.
29 | P a s c u a l , A i r i n e A .
  One of the actions of the sympathetic nervous system
is dilation of the bronchi with increased rate and depth
of respiration.
 This is the desired effect when selecting a
sympathomimetic as a bronchodilator.
Therapeutic actions
 At therapeutic levels, the action of most
sympathomimetics is specific to the beta-receptors
found in the bronchi.
 Other systemic effects include increased blood
pressure, increased heart rate, vasoconstriction, and
decreased renal and GI blood flow- all actions of the
sympathetic nervous system.
 Epinephrine, the prototype drug, is the drug of choice
for adults and children for the treatment of acute
bronchospasm, including that caused by anaphylaxis;
it is also available for inhalation.
Indications
 Long-acting treatment and prophylaxis of
bronchospasm and prevention of exercise-induced
bronchospasm in patients 2 years and older.
 Long-term maintenance treatment of
bronchoconstriction in COPD.
 Treatment of acute bronchospasm in adults and
children, although epinephrine is the drug of choice.
 Treatment and prophylaxis of acute asthma attacks in
children over 6 years old.
Contraindications and Cautions
 Underlying conditions. These drugs are
contraindicated or should be used with caution,
depending on the severity of the underlying condition,
in conditions that would be aggravated by the
sympathetic stimulation, including cardiac disease,
vascular disease, arrhythmias, diabetes, and
hyperthyroidism.
 Pregnancy and lactation. These drugs should be
used during pregnancy and lactation only if the
benefits to the mother clearly outweigh potential risks
to the fetus or neonate.
Adverse Effects
 CNS: Headache, restlessness.
 Cardiovascular: Palpitation, tachycardia.
 Skin: Pallor, local burning, and stinging.
 GU: Decreased renal formation.
 Respiratory: Rebound congestion with nasal
inhalation.
 Misc: Fear, anxiety.
Interactions
 Special precautions should be taken to avoid the
combination of sympathomimetic bronchodilators with
general anesthetics.
 Cyclopropane and halogenated
hydrocarbons. Because these drugs sensitize the
myocardium to catecholamines, serious cardiac
complications could occur.
ANTICHOLINERGICS
 Patients who cannot tolerate the sympathetic effects
of sympathomimetics might respond to
the anticholinergic drugs ipratropium (Atrovent) and
tiotropium (Spiriva).
 These drugs are not as effective as the
sympathomimetics but can provide some relief to
those patients who cannot tolerate the other drugs.
Therapeutic actions
 Anticholinergics are used as bronchodilators because
of their effect on the vagus nerve, which assist to
block or antagonize the action of the neurotransmitter
acetylcholine at vagal-mediated receptor sites.
 By blocking the vagal effect, relaxation of smooth
muscle in the bronchi occurs, leading to
bronchodilation.
Indications
 Maintenance and treatment of bronchospasm for
adults with COPD.
 Long-term, once-daily maintenance and treatment of
bronchospasm associated with COPD in adults.
Contraindications and Cautions
 Co-morbidities. Caution should be used in any
condition that would be aggravated by the
anticholinergic or atropine-like effects of the drug,
such as narrow-angle glaucoma, bladder neck
obstruction or prostatic hypertrophy, and conditions
aggravated by dry mouth and throat.
 Allergy. The use of ipratropium or tiotropium is
contraindicated in the presence of known allergy to
the drug or to soy products or peanuts to prevent
hypersensitivity reactions,
30 | P a s c u a l , A i r i n e A .
  Pregnancy and lactation. These drugs are not
usually absorbed systematically, but as with all the
drugs, caution should be used in pregnancy and
lactation because of the potential for adverse effects
on the fetus or nursing baby.
Adverse Effects
 CNS: Dizziness, headache.
 GI: Nausea, gastrointestinal distress.
 Cardiovascular: Palpitations.
 Respiratory: Cough.
 Misc: Nervousness.
NURSING RESPONSIBILITY:
BRONCHODILATORS
 Relieve GI upset. Administer oral drug with food or
milk to relieve GI irritation if GI upset is a problem.
 Monitor drug response. Monitor patient response to
the drug (e.g., relief of respiratory difficulty, improved
airflow) to determine the effectiveness of the drug
dose and to adjust dose as needed.
 Provide comfort. Provide comfort measures
including rest periods, quiet environment, dietary
control of caffeine, and headache therapy as needed,
to help the patient cope with the effects of drug
therapy.
 Provide follow-ups. Provide periodic follow-up,
including blood tests, to monitor serum theophylline
levels.
 Individual drug response. Reassure patient that the
drug of choice will vary with each individual; these
sympathomimetics are slightly different chemicals and
are prepared in a variety of delivery systems; a
patient may have to try several different
sympathomimetics before the most effective one is
found.
 Proper administration and dosage. Advise the
patient to use the minimal amount needed for the
shortest period necessary to prevent adverse effects
and accumulation of drug levels.
 Proper use of sympathomimetics. Teach the
patients who use one of these drugs for exercise-
induced asthma to use it 30 to 60 minutes before
exercising to ensure peak therapeutic effects when
they are needed.
 Use of adrenergic blockers. Alert the patient that
long-acting adrenergic blockers are not for use during
acute attacks because they are slower acting and will
not provide the necessary rescue in a state of acute
bronchospasm.
 Increase oral fluid intake. Ensure adequate
hydration and provide environmental controls such as
the use of a humidifier, to make the patient more
comfortable.
 Encourage voiding. Encourage the patient to void
before each dose of medication to avoid urinary
retention related to drug effects.
 Small, frequent meals. Provide small, frequent
meals and sugarless lozenges to relieve dry mouth
and GI upset.
 Use of inhalator. Review the use of inhalator with the
patient; caution the patient not to exceed 12
inhalations in 24 hours to prevent serious adverse
effects.
 Educate the patient. Provide thorough patient
teaching, including the drug name and prescribed
dosage measures to help avoid adverse effects,
warning signs that may indicate problems, and the
need for periodic monitoring and evaluation, to
enhance patient knowledge about drug therapy and to
promote compliance.
 Provide patient support. Offer support and
encouragement to help the patient cope with the
disease and the drug regimen.
Lesson 3: Expectorants
Expectorants are drugs that liquefy the lower respiratory tract
secretions. They are used for the symptomatic relief of
respiratory conditions characterized by a dry, nonproductive
cough.
Therapeutic actions
 Enhances the output of respiratory tract fluids by
reducing the adhesiveness and surface tension of
these fluids, allowing easier movement of the less
viscous secretions.
Indications
 Symptomatic relief of respiratory conditions
characterized by a dry, nonproductive cough.
Contraindications and Cautions
 Allergy. This drug should not be used in patients with
a known allergy to the drug to prevent hypersensitivity
reactions.
 Pregnancy or lactation. This drug should be used
with caution in pregnancy and lactation because of
the potential adverse effects on the fetus or baby.
 Cough. This drug should not be used with persistent
coughs, which could be indicative of an underlying
medical problem.
Adverse Effects
 GI: Nausea, vomiting, anorexia.
 CNS: Headache, dizziness.
 Underlying cough: The most important consideration
in the use of these drugs is discovering the cause of
the underlying cough; prolonged use of the OTC
preparations could result in the masking of important
symptoms of a serious underlying disorder.
 Respiratory: Rhinorrhea, bronchospasm.
31 | P a s c u a l , A i r i n e A .
  Skin: Rash.
Lesson 4: Antitussive
Drugs that suppress the cough reflex. It acts on the cough-
control center in the medulla to suppress the cough reflex; if
the cough is nonproductive and irritating, an antitussive may be
taken.
Therapeutic actions
 Acts directly on the medullary cough center of the
brain to depress the cough reflex.
 Because they are centrally acting, they are not the
drugs of choice for anyone who has a head injury or
could be impaired by central nervous system
depression.
Indications
 Local anesthetic on the respiratory passages, lungs,
and pleurae, blocking the effectiveness of the stretch
receptors that stimulate a cough reflex.
 For relief of moderate to moderately severe pain.
 For the treatment of dry cough, drug withdrawal
syndrome, opioid type drug dependence, and pain.
Adverse Effects
 CNS: Drowsiness and sedation.
 GI: Nausea, constipation, dry mouth, GI upset.
Nursing Responsibility
 Prevent overdosage. Ensure that the drug is not
taken any longer than recommended to prevent
serious adverse effects and severe respiratory tract
problems.
 Assess underlying problems. Arrange for further
medical evaluation for coughs that persist or are
accompanied by high fever, rash, or excessive
secretions; To detect the underlying cause of
coughing, and to arrange for appropriate treatment of
the underlying problem.
 Provide other relief measures from cough. These
nursing interventions may include humidifying the
room, providing fluids, use of lozenges, and cooling
room temperature.
 Educate the patient. Provide thorough patient
teaching, including the drug name and prescribed
dosage, measures to help avoid adverse effects,
warning signs that may indicate problems, and the
need for periodic monitoring and evaluation, to
enhance patient knowledge about drug therapy and
promote compliance.
 Provide emotional support. Offer support and
encouragement to help the patient cope with the
disease and the drug regimen.

Contraindications and Cautions

 Patent airways. Patients who need to cough to
maintain the airways (e.g., postoperative patients and
those who have undergone abdominal or thoracic
surgery) to avoid respiratory distress.
 Asthma and emphysema. Patients with asthma and
emphysema are contraindicated because cough
suppression could lead to accumulation of secretions
and a loss of respiratory reserve.
 Addiction. Patients who are hypersensitive to or
have a history of addiction to narcotics; codeine is a
narcotic and has addiction potential
 Sedation. Patients who need to drive or be alert
should use codeine, hydrocodone, and
dextromethorphan with extreme caution because
these drugs can cause sedation and drowsiness.
 Pregnancy. Patients who are pregnant and lactating,
because of the potential for adverse effects on the
fetus or baby, including sedation and CNS
depression.

Interactions
 Monoamine oxidase inhibitors
(MAOI). Dextromethorphan should not be used with
MAOIs because hypotension, fever, nausea,
myoclonic jerks, and coma could occur.

32 | P a s c u a l , A i r i n e A .
MODULE 12
DRUGS ACTING ON THE
gASTROINTESTINAL SYSTEM
Lesson 1: Introduction to Gastrointestinal
System
FUNCTION OF DIGESTIVE SYSTEM
 Ingestion. Food must be placed into the mouth before
it can be acted on; this is an active, voluntary process
called ingestion.
 Propulsion. If foods are to be processed by more than
one digestive organ, they must be propelled from one
organ to the next; swallowing is one example of food
movement that depends largely on the propulsive
process called peristalsis (involuntary, alternating
waves of contraction and relaxation of the muscles in
the organ wall).
 Food breakdown: mechanical digestion. Mechanical
digestion prepares food for further degradation by
enzymes by physically fragmenting the foods into
smaller pieces, and examples of mechanical digestion
are: mixing of food in the mouth by the tongue,
churning of food in the stomach, and segmentation in
the small intestine.
 Food breakdown: chemical digestion. The
sequence of steps in which the large food molecules
are broken down into their building blocks by
enzymes is called chemical digestion.
 Absorption. Transport of digested end products from
the lumen of the GI tract to the blood or lymph is
absorption, and for absorption to happen, the
digested foods must first enter the mucosal cells by
active or passive transport processes.
 Defecation. Defecation is the elimination of
indigestible residues from the GI tract via the anus in
the form of feces.
Lesson 2: Drugs Affecting Gastointestinal
Secretions
HISTAMINE-2 (H2) RECEPTOR ANTAGONISTS
block the release of acid in response to gastrin or
parasympathetic release.
Therapeutic actions
 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
 Short-term treatment of active duodenal ulcer or
benign gastric ulcer.
 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.
Contraindications and Cautions
 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
 CNS: Dizziness, confusion, headache, somnolence.
 Cardio: Cardiac arrhythmias, cardiac arrest.
 GI: Diarrhea.
 Reproductive: Impotence.
 Skin: Rash.
33 | P a s c u a l , A i r i n e A .
  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. Phenytoin. Beta-adrenergic
blockers. Alcohol. Quinidine. Lidocaine. Theophylline.
Chloroquine. Benzodiazepines. Nifedipine.
Pentoxifylline. TCAs. Procainamide. Carbamazepine.
Nursing Responsibility
 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 arrythmias
 Assess 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.
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
 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.
Indication
 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.
Contraindications and Cautions
 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.
 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
 GI: Gastric rupture.
 Systemic alkalosis: headache, nausea, irritability,
weakness, tetany, confusion.
 Misc: Hypokalemia.
Interactions
34 | P a s c u a l , A i r i n e A .
  Alkalinity. Most drugs are prepared for an acidic
environment, and an alkaline environment can
prevent them from being broken down for absorption
or can neutralized them so that they cannot be
absorbed.
Nursing Responsibility
 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 minimize them, warning signs that may
indicate possible problems and the need to notify the
health care provider immediately.
PROTON PUMP INHIBITORS
Proton pump inhibitors suppress the secretion of
hydrochloric acid into the lumen of the stomach.
Therapeutic actions
 Blocks the final step of acid production, lowering the
acid levels in the stomach
 Inhibits the hydrogen-potassium adenosine
triphosphate enzyme system on the secretory surface
of the gastric parietal cells.
Indication
 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.
Contraindications and Cautions
 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
 CNS: Headache, dizziness, vertigo, insomnia.
 Skin: Rash
 GI: Diarrhea, abdominal pain, nausea, vomiting.
 Respiratory: Upper respiratory infections, cough.
Interactions
 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. Decrease the effectiveness of clopidogrel if
combined with esomeprazole
35 | P a s c u a l , A i r i n e A .
Nursing Responsibility
 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.
GI PROTECTANT
GI protectants surround every wounded region in the stomach
to avoid more acid damage.
Therapeutic actions/Indications
 Sucralfate forms an ulcer-adherent complex at
duodenal ulcer sites, protecting the sites from acid,
pepsin and bile salts prevents the activity of pepsin in
gastric juices, preventing further degradation of
proteins in the stomach, including the membrane of
the intestine
Adverse Effect
 Constipation is the most common adverse reaction
reported. Diarrhea, fatigue, indigestion, abdominal
pain and dry mouth may also occur
Contraindications and Cautions
 should not be given to any person with known drug
allergy or any of its components to avoid
hypersensitivity reactions.
 renal disease or undergoing dialysis as aluminum
build-up can occur when used with aluminum-
containing items.
Interactions
 aluminum salts are mixed with sucralfate, there is a
chance of elevated levels of aluminum and aluminum
toxicity. If this mixture is used, strict caution should be
taken.
 phenytoin, fluoroquinolone antibiotics such as
ciprofloxacin, norfloxacin or penicillamine are mixed
with sucralfate, lower serum levels and drug efficacy
can result.
PROSTAGLANDIN
used to secure the stomach lining
Therapeutic actions/Indications
 prevents gastric acid secretion and enhances the
production of bicarbonate and mucosa in the
stomach, thereby protecting the stomach lining
 used to avoid NSAID-induced gastric ulcers in
patients at high risk of gastric ulcer complications
such as aged or frail patients with a history of ulcers
in the past.
Contraindications and Cautions
 contraindicated with allergies to some portion of the
medication
 contraindicated during breastfeeding because it is an
abortifacient
Adverse Effect
 nausea, diarrhea, stomach pain, flatulence, vomiting,
dyspepsia, and constipation
 Geniturinary symptoms due to the action of
prostaglandins on the fetus include abortion, heavy
bleeding, spotting, cramping, hypermenorrhea,
dysmenorrhea, and other menstrual disorders
Digestive Enzymes
compounds formed in the GI system that break down food into
accessible nutrients
Therapeutic actions/Indications
 serve as a thickening agent in dry mouth
environments.
 Pancreatic enzymes are alternative enzymes that aid
digestion and absorption of fats, proteins and
carbohydrates.
36 | P a s c u a l , A i r i n e A .
Contraindications and Cautions
 contraindicated with allergies to some portion of the
medication
Adverse Effect
 abnormal electrolyte absorption, such as increased
levels of magnesium, sodium, or potassium.
Lesson 3: Drugs Affecting Gastrointestinal
Motility
LAXATIVES: CHEMICAL STIMULANTS
Laxative or cathartic medications are recommended for short-
term relief of constipation, for the avoidance of straining
Therapeutic actions/Indications
 used where a full evacuation of the intestine is
desirable.
Contraindications and Cautions
 contraindicated with allergies to some portion of the
medication
 acute abdominal disorders, including appendicitis,
diverticulitis, and ulcerative colitis, where improved
motility can contribute to rupture or further
exacerbation of the inflammation
Adverse Effect
 diarrhea, stomach cramping, and nausea are the
most common side effects associated with laxatives.
LAXATIVES: BULK STIMULANTS
fast-acting, violent laxatives that induce a significant rise in
fecal matter.
Therapeutic actions/Indications
 increasing the intestinal fluid that enlarges, inhibits
local stretch receptors and activates local behavior.
Contraindications and Cautions
 contraindicated with allergies to some portion of the
medication
 acute abdominal disorders, including appendicitis,
diverticulitis, and ulcerative colitis, where improved
motility can contribute to rupture or further
exacerbation of the inflammation
Adverse Effect
 diarrhea, stomach cramping, and nausea are the
most common side effects associated with laxatives.
GASTROINTESTINAL STIMULANTS
These medications induce parasympathetic activity or improve
the response of the GI tissues to parasympathetic activity
Therapeutic actions/Indications
 inducing parasympathetic activity throughout the GI
tract, these drugs increase GI secretions and motility
at a general level within the tract
Contraindications and Cautions
 contraindicated with allergies to some portion of the
medication
 GI distortion or perforation that could be aggravated
by GI stimulation
Adverse Effect
 nausea, vomiting, diarrhea, bowel spasm, and
cramping
Interaction
 Decreased immunosuppressive impact and elevated
toxicity of cyclosporine with metoclopramide
ANTIDIARRHEALS
block activation of the GI tract for symptomatic relief of
diarrhea
37 | P a s c u a l , A i r i n e A .
Therapeutic actions/Indications
 interrupt the motility of the GI tract by direct action on
the lining of the GI tract to suppress local reflexes

Contraindications and Cautions

 contraindicated with opioid allergy to some portion of
the medication
 GI distortion or perforation that could be aggravated
by GI stimulation

Adverse Effect
 constipation, distention, stomach pain, nausea,
vomiting, dry mouth and even poisonous megacolon

Lesson 4: Antiemetic Agents

38 | P a s c u a l , A i r i n e A .
MODULE 13
ACTING ON THE RENAL SYSTEM
ACTIONS, THERAPEUTIC USES,
PREPARATIONS, DOSAGES, MODES OF
ADMINISTRATION OF SELECTED DRUGS
AND MEDICAL PLANTS
Lesson 1: Methotrexate
an antineoplastic drug that has long been used to treat
psoriasis because it suppresses inflammation and spread of T
lymphocytes. It may have major adverse effects.
Action
 Methotrexate is a folic acid antagonist that inhibits
DNA synthesis. It irreversibly binds to dihydrofolate
reductase, inhibiting the formation of reduced folates,
and thymidylate synthetase, resulting in inhibition of
purine and thymidylic acid synthesis.
Contraindications
Severe renal or hepatic impairment, pre-existing profound
bone marrow suppression in patients with psoriasis or
rheumatoid arthritis, alcoholic liver disease, AIDS, pre-existing
blood dyscrasias, pregnancy (in patients with psoriasis or
rheumatoid arthritis), breast-feeding.
Adverse Reactions
Ulceration of the mouth and GI disturbances (e.g. stomatitis
and diarrhea), bone marrow depression, hepatotoxicity, renal
failure, skin reactions, alopecia, ocular irritation, arachnoiditis
in intrathecal use, megaloblastic anemia, osteoporosis,
precipitation of diabetes, arthralgias, necrosis of soft tissue and
bone, anaphylaxis, impaired fertility.
 Potentially Fatal: Pulmonary reactions (e.g.
interstitial lung disease); neurotoxicity (e.g.
leukoencephalopathy, paresis, demyelination) with
intrathecal use; fetal deaths.
Drug Interactions
Decreased effectiveness with folic acid and its derivatives.
 Potentially Fatal: Increased toxicity with NSAIDs and
salicylates; probenecid; some penicillins;
aminoglycosides neomycin and paromomycin;
sulfonamides such as sulfafurazole and
sulfamethoxazole; co-trimoxazole or trimethoprim;
nephrotoxic agents (e.g. cisplatin); ciclosporin;
etretinate. Synergistic enhancement of effects with
fluorouracil. Increased bioavailability of
mercaptopurine. Reduces serum-valproate
concentrations. Reduced serum concentrations with
colestyramine. Increased serum concentrations with
omeprazole.
Lesson 2: Lithium Carbonate
a mood-stabilizing drug that has been shown to promote
neuronal growth and reduce brain atrophy in people with long-
standing mood disorders
Action
Lithium's exact mechanism is unclear, but it alters
intraneuronal metabolism of catecholamines and sodium
transport in neurons and muscle cells.
Contraindications
Severe renal and cardiac disease; severe dehydration, sodium
depletion, debilitation.
Overdosage
 Symptoms: Sedation, confusion, tremors, joint pain,
visual changes, seizures, coma.
 Management: No specific antidote.
 Acute overdose: Discontinue admin and remove any
unabsorbed drug by gastric lavage.
 Correct fluid and electrolyte imbalances and provide
supportive care. Dialysis (severe cases).
Adverse Reactions
Exacerbation of psoriasis, acne, rash; nausea, diarrhoea,
vertigo, muscle weakness, dazed feeling; loss of concentration;
tremors; hypothyroidism; wt gain, oedema; cardiac
arrhythmias; exophthalmos; restlessness; electrolyte
disturbances.
 Potentially Fatal: Severe neurotoxicity, leucopenia.
Drug Interactions
Reduced serum levels with carbonic anhydrase inhibitors,
chlorpromazine, sodium-containing preparations, theophylline,
urea. Enhanced hypothyroid effects with iodine salts.
Enhanced effects of neuromuscular-blocking agents. Reduced
pressor response to sympathomimetics.
 Potentially Fatal: Increased risk of lithium toxicity
with ACE inhibitors, angiotensin receptor antagonists,
loop diuretics, metronidazole, phenytoin. Increased
39 | P a s c u a l , A i r i n e A .
 risk of neurotoxicity with carbamazepine, calcium-
channel blockers, haloperidol, methyldopa,
phenothiazines, SSRIs, TCAs. Increased serum
levels with COX-2 inhibitors, NSAIDs (except
sulindac, aspirin), tetracyclines, thiazide diuretics.
Increased risk of encephalopathy with haloperidol.
Increased risk of serotonin syndrome with
sibutramine. Fatal malignant hyperpyrexia may occur
when used with MAOIs.
Lesson 3: Lagundi (Vitex negundo)
Lagundi (scientific name: Vitex negundo) is a shrub which
grows in the Philippines.
 It is one of the ten herbal medicines authorized by the
Philippine Ministry of Health as an important herbal
medicine of proven therapeutic value.
 A team of researchers from the University of the
Philippines, with support from PCHRD, formulated
a lagundi-based drug which can effectively ease the
symptoms of respiratory infections specifically cough
and asthma. It is in syrup and tablet forms and is
good for both children and adults.
 The drug is a product of multiple scientific studies and
clinical trials as part of the National Integrated
Research Program on Medicinal Plants (NIRPROMP).
Lagundi formulation was wheezing and effective in
preventing the spread of disease-causing
microorganisms, reducing fever, decreasing the
viscosity of mucus, improving the color of phlegm,
alleviating shortness of breath and wheezing, and
lessening the frequency of cough. “Lagundi” is a
common term for Vitex negundo L., which is
traditionally used to treat insect and snake bites,
ulcers, rheumatism, sore throat, cough, fever, and
clogged sinuses. This plant is common and widely
distributed in the country.
Benefits
transmission of poisons and venom from bites of poisonous
animals. The juice extracted from the flowers of the Lagundi
plant is used as an aid for diseases such as fever, diarrhea,
liver disorders, and even cholera. Although decoction of plant
leaves is suggested to be used by individuals to help improve
the flow and output of milk, as well as to induce menstruation.
Lesson 4: Niyog-Niyogan (Quisqualis Indica
L.)
Niyog-niyogan or Rangoon Creeper is an excellent vine for
outdoor gardens. This ligneous plant, scientifically
called Quisqualis indica L.  It is also known as Burma or
Rangoon Creeper, Liane Vermifuge and Chinese
honeysuckle. 
Benefit and Treatment
Almost all of its components are used individually or combined
with other ingredients as a cure for various diseases. In the
Philippines, they are taken to rid citizens of parasitic worms.
Some may use these to help relieve cough and diarrhea.
Medical experts, urging patients to contact their doctors as
inappropriate dosing can cause hiccups. Niyog-niyogan leaves
are used to treat body pain by inserting them in various trouble
areas of the body. Compound decoctions of niyog-niyogan
leaves are used in India to relieve flatulence.
Preparation and Use
 Niyog-niyogan seeds can be used as an anthelmintic.
They are eaten raw two hours before the patient's last
meal of the day. Adults can take 10 seeds while
children between 4 and 7 years of age can consume
up to four seeds only. Children from 8 to 9 years of
age will take six seeds and children from 10 to 12
years of age will consume seven seeds.
 Decoctions of its roots are often used as a treatment
for rheumatism, although its fruits are used as an
effective way to relieve toothaches.

 Relief with asthma and pharyngitis

 Recommended relief of rheumatism, dyspepsia, boils,
diarrhea
 Management of cough, colds, fever, influenza, and
other bronchopulmonary disorders
 Relieve signs of chicken pox
 Removal of the worms and boils

Preparation and Use

 Boil half a cup of fresh or dried leaves in 2 cups of
water for 10 to 15 minutes. Drink half a cup 3 times a
day.
 For skin diseases or conditions, apply the decoction
of the leaves and roots directly to the skin.
 The root is especially good for the treatment of
dyspepsia, worms, boils, colic, and rheumatism.

The decoction (boiling in water) of the roots and leaves of

Lagundi is applied to wounds and is used as an aromatic bath
for skin diseases. Boiled seeds are consumed to avoid the

40 | P a s c u a l , A i r i n e A .