MODULE 3 - Drugs Affecting The Body System

Topic A

Topic Title: Drugs Acting on Reproductive System

The female reproductive system works in a cyclical fashion and altering the components of this cycle can
have a variety of effects to the body. Hormones and hormonal-like agents are primarily drugs that affect the
female reproductive system.

Generic and Brand Names

Table of commonly encountered female reproductive system drugs, their generic names, and brand names:

Classifications Generic Name Brand Name

Sex Hormones
estradiol Estrace
estrogens, conjugated C.E.S, Premarin
Estrogens
estrogens, esterified Menest
estropipate Ortho-Est, Ogen
desogestrel Kariva, Cyclessa
drospirenone Yasmin, YAZ
etonogestrel Implanon
levonorgestrel Mirena, Plan B
Progestins medroxyprogesterone Provera
norethindrone acetate Aygestin
norgestrel Ovrette
progesterone (generic)
Ulipristal Ella
R5 Estrogen Receptor Raloxifene Evista
Modulators toremifene Fareston
Fertility Drugs Cetrorelix Cetrotide
chorionic gonadotropin Chorex, Profasi, Pregnyl
Clomiphene Clomid
follitropin alfa Gonal-F
follitropin beta Follistim
 ganirelix Antagon
lutropin alfa Luveris
Menotropins Pergonal, Repronex
Uterine Motility Drugs
Ergonovine Ergotrate
Oxytocics methylergonovine Methergine
Oxytocin Pitocin, Syntocinon
Carboprost
Abortifacients Dinoprostone Hemabate
mifepristone Cervidil, Prepidil Gel, Prostin E2

Female Sex Hormones

Female sex hormones both can be used to replace missing hormones or to decrease the release of
endogenous hormones. The female sex hormones include estrogen and progesterone.

Therapeutic Action

The desired and beneficial actions of female sex hormones are as follows:

Estrogens
 The most potent endogenous female sex hormone responsible for estrogen effects on the body.
 Affect the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH).
 Responsible for the proliferation of the endometrial lining and are known to compete
with androgens for receptor sites.
 The loss of estrogen is responsible for the signs and symptoms of menopause in the uterus,
vagina, breasts, and cervix.

Progestins
 Transform the proliferative endometrium into a secretory endometrium. They also inhibit the
secretion of FSH and LH.
 Prevent follicle maturation and ovulation as well as uterine contraction.
 Exact mechanism of action in its function as a contraceptive is not known but it thought that
circulating progestins and estrogens “trick” the hypothalamus and pituitary and prevent the release
of gonadotropin-releasing hormone (GnRH), FSH, and LH. Therefore, follicle development and
ovulation are prevented.

Indications

Female sex hormones are indicated for the following medical conditions:
Estrogens
 Used for hormone replacement therapy (HRT) in small doses when ovarian activity is blocked or
absent.
 Used as palliation for the discomforts of menopause in the first few years of menopause, when
many of the beneficial effects of estrogen are lost.
 Treat female hypogonadism and ovarian failure; to prevent postpartum breast engorgement.
 To slow bone loss in osteoporosis.
 Palliation of cancers that have known receptor sensitivity.

Progestins
 Transform the proliferative endometrium into a secretory endometrium. They also inhibit the
secretion of FSH and LH.
 Prevent follicle maturation and ovulation as well as uterine contraction.
 Exact mechanism of action in its function as a contraceptive is not known but it it thought that
circulating progestins and estrogens “trick” the hypothalamus and pituitary and prevent the release
of gonadotropin-releasing hormone (GnRH), FSH, and LH. Therefore, follicle development and
ovulation are prevented.

Here are some important aspects to remember for indication of female sex hormones in different age
groups:

Children
 Have undergone little testing in children. They can cause premature closure of epiphysis so caution
is important in growing children.
 Smallest dose possible is used for prescribed oral contraceptives in teenage girls.

Adults
 Women receiving any of these drugs should receive an annual medical examination, including
breast examination and Pap smear, to monitor for adverse effects and underlying medical
conditions.
 Women taking estrogen should be advised not to smoke because of the increased risk of
thrombotic events.
 Women who are receiving these drugs for fertility programs should receive a great deal of
psychological support and comfort measures to cope with the many adverse effects associated
with these drugs. The risk of multiple births should be explained.
 Drugs are used in treatment of specific cancers in males and they should be advised about the
possibility of estrogenic effects.
 Not indicated during pregnancy or lactation because of potential for adverse effects on the fetus or
neonate.

Older adults

 HRT is no longer commonly used by postmenopausal women.

Contraindications and Cautions

Estrogens

The following are contraindications and cautions for the use of estrogens and progestins:
 Allergy to estrogens. Prevent hypersensitivity reactions.
 Idiopathic vaginal bleeding, breast cancer, estrogen-dependent cancer. Can be exacerbated by
drug.
 History of thromboembolic disorders, cerebrovascular accident, heavy smokers. Increased risk
of thrombus and embolus development
 Hepatic dysfunction. Estrogen have effects on liver function.
 Pregnancy. Estrogen are linked to serious fetal defects
 Lactating women. Possible effects to the neonate
 Metabolic bone disease. Estrogen has bone-conserving effect and could exacerbate the disease.
 Renal insufficiency. Can interfere with the renal excretion of the drug and increase the risk for
potential adverse effects on fluid and electrolyte balance
 Hepatic impairment. Can alter the metabolism of the drug and increase the risk for the adverse
effects, including those on the liver and GI tract.

Progestins
 Pelvic inflammatory disease (PID), sexually transmitted diseases, endometriosis,
pelvic surgery. Progestins have effects on the vasculature of the uterus.
 Drosperinone is contraindicated in patients who are at risk for hyperkalemia due to its
antimineralocorticoid effects and the risk of hyperkalemia.
 Epilepsy, migraine headaches, asthma, cardiac or renal dysfunction. Potential exacerbation of
these conditions.

Adverse Effects

Use of female sex hormones may result to these adverse effects:

Estrogen
 GI: nausea, vomiting, abdominal cramp, bloating, colitis, acute pancreatitis, cholestatic jaundice,
hepatic adenoma
 GU: breakthrough bleeding, menstrual irregularities, dysmenorrhea, amenorrhea, changes in libido
 Systemic effects: fluid retention, electrolyte disturbances, headache, dizziness, mental changes,
weight changes, edema

Progestins

 Systemic effects are similar to estrogen.

 Dermal patch contraceptives are associated with same systemic effects, as well as local skin
irritation.
 Vaginal gel use is associated with headache, nervousness, constipation, breast enlargement, and
perineal pain.
 Intrauterine systems are associated with abdominal pain, endometriosis, abortionPID, and
expulsion of the intrauterine device.
 Vaginal use is associated with local irritation and swelling.
Interactions

The following are interactions involved in the use of female sex hormones:

Estrogen
 Barbiturates, rifampin, tetracyclines, phenytoin: decreased serum estrogen levels
 Corticosteroids: increased therapeutic and toxic effects of corticosteroids.
 Nicotine: Increased risk of thrombi and emboli
 Grapefruit juice: inhibition of metabolism of estradiols
 St. John’s wort: can affect metabolism of estrogens and can make estrogen-containing
contraceptives less effective.

Progestins
 Barbiturates, carbamazepine, phenytoin, griseofulvin, penicillin, tetracyclines, rifampin: reduced
effectiveness of progestins
 St. John’s wort: can affect the metabolism of progestins and can make progestin-containing
contraceptives less effective.

Estrogen Receptor Modulators

Estrogen receptor modulators are agents that either stimulate or block specific estrogen receptor sites.

Therapeutic Action

The desired and beneficial actions of depolarizing estrogen receptor modulator are:
 To produce some of the positive effects of estrogen replacement while limiting the adverse effects.
 To increase bone mineral density without stimulating the endometrium.

Indications

Estrogen receptor modulators are indicated for:

 Prevention and treatment of osteoporosis in postmenopausal women.

Some important aspects to remember for indication of estrogen receptor modulators in different age
groups:

Children

Have undergone little testing in children. They can cause premature closure of epiphysis so caution is
important in growing children.

Adults

Women receiving any of these drugs should receive an annual medical examination, including breast
examination and Pap smear, to monitor for adverse effects and underlying medical conditions.
Not indicated during pregnancy or lactation because of potential for adverse effects on the fetus or
neonate.
Older adults

HRT is no longer commonly used by postmenopausal women.

Contraindications and Cautions

Contraindications and cautions for the use of estrogen receptor modulators are the following:
 Allergy to estrogen receptor modulators. Prevent hypersensitivity reactions.
 Pregnancy, lactation. Potential effects on the fetus or neonate.
 History of venous thrombosis or smoking. Increased risk of blood clot formation if smoking and
estrogen are combined.

Adverse Effects

Use of estrogen receptor modulators may result to these adverse effects:

 Raloxifene has been associated with GI upset, nausea, and vomiting.
 Changes in fluid balance may cause headache, dizziness, visual changes, and mental changes.
 Specific estrogen receptor stimulation may cause hot flashes, skin rash, edema, and
vaginal bleeding.

Interactions

The following are drug-drug interactions involved in the use of estrogen receptor modulators:
 Cholestyramine: reduced raloxifene absorption
 Highly protein-bound drugs (e.g. diazepam, ibuprofen, indomethacin, naproxen): interference on
binding sites
 Warfarin: decreased prothrombin time if taken with raloxifene

Nursing Considerations

Important nursing considerations when administering female sex hormones and estrogen receptor
modulators:

Nursing Assessment

Important things the nurse should include in conducting assessment, history taking, and examination:
 Assess for the mentioned cautions and contraindications (e.g. drug allergies, cardiovascular
diseases, metabolic bone disease, history of thromboembolism, etc.) to prevent any untoward
complications.
 Perform a thorough physical assessment (e.g. bowel sounds, skin assessment, vital signs, mental
status, etc.) to establish baseline data before drug therapy begins, to determine effectiveness of
therapy, and to evaluate for occurrence of any adverse effects associated with drug therapy.
  Assist with pelvic and breast examinations. Ensure specimen collection for Pap smear and obtain a
history of patient’s menstrual cycle to provide baseline data and to monitor for any adverse effects
that could occur.
 Arrange for ophthalmic examination especially for patients who are wearing contact lenses
because hormonal changes can alter the fluid in the eye and curvature of the cornea, which can
change the fit of contact lenses and alter visual acuity.
 Monitor laboratory test results (e.g. urinalysis, renal and hepatic function tests, etc.) to determine
possible need for a reduction in dose and evaluate for toxicity.

Nursing Diagnoses

Some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
 Ineffective tissue perfusion related to changes in the blood vessels brought about by drug therapy
and risk of thromboemboli
 Excess fluid volume related to fluid retention
 Acute pain related to systemic side effects of gastrointestinal (GI) pain and headache

Implementation with Rationale

Vital nursing interventions done in patients who are taking female sex hormones and estrogen receptor
modulators:
 Administer drug with food to prevent GI upset.
 Provide analgesic for relief of headache as appropriate.
 Provide small, frequent meals to assist with nausea and vomiting.
 Monitor for swelling and changes in vision or fit of contact lenses to monitor for fluid retention and
fluid changes.
 Provide comfort measures to help patient tolerate drug effects.
 Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
 Educate client on drug therapy to promote understanding and compliance.

Evaluation

Some aspects of care that should be evaluated to determine effectiveness of drug therapy:
 Monitor patient response to therapy (palliation of signs and symptoms of menopause, prevention of
pregnancy, decreased risk factors for coronary artery disease, and palliation of certain cancers).
 Monitor for adverse effects (e.g. GI upset, edema, changes in secondary sex characteristics,
headaches, thromboembolic episodes, and breakthrough bleeding).
 Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
 Monitor patient compliance to drug therapy.

Fertility Drugs

Fertility drugs are agents that stimulate the female reproductive system.

Therapeutic Action
The desired and beneficial actions of fertility drugs are as follows:
 Can be used by women without primary ovarian failure who cannot get pregnant after 1 year of
unprotected sexual intercourse.
 Work either directly stimulate follicles and ovulation or stimulate the hypothalamus to increase FSH
and LH levels, leading to ovarian follicular development and maturation of ova.

Indications

Fertility drugs are indicated for the following medical conditions:

 Treatment of infertility in women with functioning ovaries whose partners are fertile.
 Used to stimulate multiple follicle development for harvesting of ova for in vitro fertilization.
 Menotropins are used to stimulate spermatogenesis in men with low sperm counts and otherwise
normally functioning testes.
 Cetrorelix inhibits premature LH surges in women undergoing controlled overain stimulation by
acting as a GnRH antagonist.
 Follitropin alfa and follitropin beta are FSH molecules injected to stimulate follicular development in
the treatment of infertility and for harvesting of ova in vitro fertilization.

Contraindications and Cautions

The following are contraindications and cautions for the use of fertility drugs:
 Allergy to fertility drug. Prevent hypersensitivity reactions
 Primary ovarian failure. These drugs only work to stimulate functioning ovaries
 Thyroid or adrenal dysfunction. Drugs have effects on the hypothalamic-pituitary acxis
 Ovarian cysts. Can be stimulated by the drugs and can become larger
 Pregnancy. Due to the potential for serious fetal effects
 Idiopathic uterine bleeding. Can represent an underlying problem that could be exacerbated by the
stimulatory effects of these drugs.
 Lactation. Risk of adverse effects on the baby
 Thromboembolic disease. Increased risk of thrombus formation
 Women with respiratory diseases. Alterations in fluid volume and blood flow can overtax
the respiratory system.
Adverse Effects

Use of fertility drugs may result to these adverse effects:

 Greatly increased risk of multiple births and birth defects
 Ovarian overstimulation: abdominal plain, distention, ascites, pleural effusion
 Others: headache, fluid retention, nausea, bloating, uterine bleeding, ovarian enlargement,
gynecomastia, and febrile reactions possibly due to stimulation of progesterone release.

Nursing Considerations

Nursing Assessment

Important things the nurse should include in conducting assessment, history taking, and examination:
  Assess for the mentioned cautions and contraindications (e.g. drug allergies, primary ovarian
failure, thyroid or adrenal dysfunction, ovarian cysts, idiopathic uterine bleeding, thromboembolic
diseases, etc.) to prevent any untoward complications.
 Perform a thorough physical assessment (e.g. skin condition, vital signs, neurological status, etc.)
to establish baseline data before drug therapy begins, to determine effectiveness of therapy, and to
evaluate for occurrence of any adverse effects associated with drug therapy.
 Assist with pelvic and breast examinations. Ensure specimen collection for Pap smear and obtain a
history of patient’s menstrual cycle to provide baseline data and to monitor for any adverse effects
that could occur.
 Monitor laboratory test results (e.g. hormonal levels, renal and hepatic function tests, etc.) to
determine possible need for a reduction in dose and evaluate for ovarian hyperstimulation.

Nursing Diagnoses

Some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
 Acute pain related to headache, fluid retention, or GI upset
 Sexual dysfunction related to alterations in normal hormone control
 Disturbed body image related to drug treatment and diagnosis

Implementation with Rationale

These are vital nursing interventions done in patients who are taking fertility drugs:
 Assess the cause of dysfunction before beginning therapy to ensure appropriate use of the drug.
 Complete a pelvic examination before each use of the drug to rule out ovarian enlargement,
pregnancy, or uterine problems.
 Check urine estrogen and estradiol levels before beginning therapy to verify ovarian function.
 Administer with an appropriate dose of human chorionic gonadotropin as indicated to ensure
beneficial effects.
 Discontinue the drug at any sign of ovarian overstimulation and arrange for hospitalization to
monitor and support the patient if this occurs.
 Provide women with a calendar of treatment days, explanations of adverse effects to anticipate,
and instructions on when intercourse should occur to increase the therapeutic effectiveness of the
drug.
 Provide warnings about the risk and hazards of multiple births so the patient can make informed
decisions about drug therapy.
 Offer support and encouragement to deal with low self-esteem issues associated with infertility.
 Provide comfort measures to help patient tolerate drug effects.
 Educate client on drug therapy to promote understanding and compliance.

Evaluation

Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:
 Monitor patient response to therapy (ovulation).
 Monitor for adverse effects (e.g. abdominal bloating, weight gain, ovarian overstimulation, multiple
births).
  Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
 Monitor patient compliance to drug therapy.

Uterine Motility Drugs: Oxytocics

 Uterine motility drugs stimulate uterine contractions to assist labor (oxytocics) or

induce abortion (abortifacients).

Therapeutic Action

The desired and beneficial actions of oxytocics are the following:

 To stimulate uterine contractions like the action of the hypothalamic hormone oxytocin stored in the
posterior pituitary.
 They directly affect neuroreceptor sites to stimulate uterine contraction and are especially effective
in the gravid uterus.
 Oxytocin, a synthetic form of the hypothalamic hormone, also stimulates the lacteal glands in the
breast to contract, promoting milk ejection in lactating women.

Indications

Oxytocics are indicated for:

 Prevention and treatment of uterine atony after delivery, thus reducing the risk of postpartum
hemorrhage.

Contraindications and Cautions

The following are contraindications and cautions for the use of oxytocics:
 Allergy to oxytocics. Prevent hypersensitivity reactions.
 Cephalopelvic disproportion, unfavorable fetal position, complete uterine atony, early
pregnancy. Can be compromised by uterine stimulation.
 Coronary disease, hypertension. Due to effect of causing arterial contraction which could raise
blood pressure or compromise coronary blood flow.

Adverse Effects
Use of oxytocics may result to these adverse effects:
 Excessive effects: uterine hypertonicity and spasm, uterine rupture, postpartum hemorrhage,
decreased fetal heart rate
 Common effects: GI upset, nausea, headache, dizziness
 Ergotism caused by ergonovine and methylergonovine: nausea, blood pressure changes, weak
pulse, dyspnea, chest pain, numbness and coldness in extremities, confusion,
excitement, delirium, convulsions, coma
 Oxytocin has caused severe water intoxication with coma and even maternal death when used for
a prolonged period.

Nursing Considerations
Important nursing considerations when administering oxytocics:

Nursing Assessment
Important things the nurse should include in conducting assessment, history taking, and examination:
 Assess for the mentioned cautions and contraindications (e.g. drug allergies, current status of
lactation, uterine atony, hypertension, etc.) to prevent any untoward complications.
 Perform a thorough physical assessment (e.g. neurological status, vital signs, labor pattern, uterine
tone, etc.) to establish baseline data before drug therapy begins, to determine effectiveness of
therapy, and to evaluate for occurrence of any adverse effects associated with drug therapy.
 Monitor laboratory test results (e.g. coagulation studies, complete blood count, etc.) to evaluate
hematological studies.

Nursing Diagnoses

Some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
 Acute pain related to increased frequency and intensity of uterine contractions or headache
 Excess fluid volume related to ergotism or water intoxication

Implementation with Rationale

These are vital nursing interventions done in patients who are taking oxytocics:
 Ensure fetal position (if appropriate) and cephalopelvic proportions to prevent serious
complications of delivery.
 Regulate oxytocin delivery using an infusion pump between contractions if it is being given to
stimulate labor to regulate dose appropriately.
 Monitor blood pressure and fetal heart rate frequently during and after administration to monitor for
adverse effects.
 Monitor uterine tone and involution and amount of bleeding to ensure safe and therapeutic drug
use.
 Provide comfort measures to help patient tolerate drug effects.
 Educate client on drug therapy to promote understanding and compliance.

Evaluation
 Aspects of care that should be evaluated to determine effectiveness of drug therapy:
 Monitor patient response to therapy (uterine contraction, prevention of hemorrhage, milk “let
down”).
 Monitor for adverse effects (e.g. blood pressure changes, uterine hypertonicity, water intoxication,
ergotism).
 Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
 Monitor patient compliance to drug therapy.

Abortifacients

Therapeutic Action

The desired and beneficial action of abortifacient is:

  To stimulate uterine activity, dislodging any implanted trophoblasts and preventing implantation of
any fertilized egg.

Indications

Abortifacients are indicated for:

 Evacuation of uterine contents via intense uterine contractions
 Approved for use to terminate pregnancy at 12-20 weeks from the date of the last menstrual
period.

Contraindications and Cautions

The following are contraindications and cautions for the use of abortifacients:
 Allergy to abortifacients and prostaglandins. Prevent hypersensitivity reactions
 After 20 weeks from the last menstrual period. Too late into the pregnancy for an abortion
 Active PID, CV, hepatic, renal, pulmonary disease. Can be exacerbated by the effects of the drug.
 Lactation. Potential for serious effects on the neonate.
 Asthma, hypertension, adrenal disease. Can be exacerbated by drug effects
 Acute vaginitis, scarred uterus. Can be aggravated by uterine contractions

Adverse Effects
Use of abortifacients may result to these adverse effects:
 Due to exaggeration of desired effects: abdominal cramping, heavy uterine bleeding, perforated
uterus, uterine rupture
 Others: headache, nausea, vomiting, diarrhea, diaphoresis, backache, rash

Nursing Considerations
Important nursing considerations when administering abortifacients:

Nursing Assessment
Important things the nurse should include in conducting assessment, history taking, and examination:
 Assess for the mentioned cautions and contraindications (e.g. drug allergies, active PID, CV
diseases, etc.) to prevent any untoward complications.
 Perform a thorough physical assessment (e.g. neurological status, vital signs, skin condition, etc.)
to establish baseline data before drug therapy begins, to determine effectiveness of therapy, and to
evaluate for occurrence of any adverse effects associated with drug therapy.
 Monitor laboratory test results (e.g. leukocyte count, hemoglobin and hematocrit, complete blood
count, etc.) to monitor for excess bleeding.

Nursing Diagnoses
Some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
 Acute pain related to uterine contractions or headache
 Ineffective coping related to abortion or fetal death

Implementation with Rationale

Some vital nursing interventions done in patients who are taking abortifacients:
 Administer via route indicated, following the manufacturer’s directions for storage and preparation,
to ensure safe and therapeutic use of the drug.
 Confirm the age of pregnancy before administering the drug to ensure appropriate use of the drug.
 Confirm that abortion or uterine evacuation is complete by assessing vaginal bleeding and passing
of tissue in the vaginal blood to avoid potential bleeding problems.
 Monitor blood pressure frequently during and after administration to assess for adverse effects.
 Monitor uterine tone and involution and the amount of bleeding during and for several days after
use of the drug to ensure appropriate response to and recovery from the drug.
 Provide comfort measures to help patient tolerate drug effects.
 Educate client on drug therapy to promote understanding and compliance.

Evaluation

Some aspects of care that should be evaluated to determine effectiveness of drug therapy:
 Monitor patient response to therapy (evacuation of uterus).
 Monitor for adverse effects (e.g. GI upset, blood pressure changes, nausea, hemorrhage, etc.).
 Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
 Monitor patient compliance to drug therapy

Drugs affecting the male reproductive system 

- Include androgens (male steroid hormones), anabolic steroids, and drugs that improve penile
dysfunction.

Table of Common Drugs and Generic Names

Table of commonly encountered drugs affecting the male reproductive system, their generic names, and
brand names:

Classifications Generic Name Brand Name

Danazol Danocrine
fluoxymesterone Androxyl
Androgens Androderm, Depo-testosterone, Striant, Androgel,
Testosterone
Fortesta
methyltestosterone Testred, Virilon
Oxandrolone Oxandrin
Anabolic Steroids
oxymetholone Anadrol-50
Alprostadil Caverject, Muse

Penile Erectile Dysfunction Sildenafil Viagra, Revatio

Drugs Tadalafil Cialis, Adcirca
Vardenafil Levitra, Staxyn
Androgens
- Androgens are male sex hormones, which include testosterone (produced in the testes) and
androgens (produced in the adrenal glands).
- Testosterone (Duratest, Testoderm) is the primary natural androgen and is the classic androgen
used today. It is used for treatment of certain breast cancers and hypogonadism, a condition where
there is undeveloped testis. All testosterones are class III controlled substances.

Therapeutic Action
The desired and beneficial actions of androgens are as follows:
 Growth and development of male sex organs and the maintenance of secondary male sex
characteristics.
 Increase the retention of nitrogen, sodium, potassium, and phosphorus and decrease the urinary
excretion of calcium.
 Increase protein anabolism and decrease protein catabolism.
 Increase the production of red blood cells.
Indications
 Androgens are indicated for the following medical conditions:
 Danazol is used for treatment of endometriosis, fibrocystic breast disease, and hereditary
angioedema. It does this by inhibiting the hypothalamic-pituitary-adrenal (HPA) and gonadotropin-
releasing hormones (GnRH), leading to a drop in follicle-stimulating hormone (FSH) and luteinizing
hormone (LH).

Contraindications and Cautions

The following are contraindications and cautions for the use of androgens:
 Allergy to androgens or other ingredients in the drug. Prevent hypersensitivity reactions.
 Pregnancy, lactation. Potential adverse effects on the neonate. It is not clear whether androgens
enter breast milk.
 Presence of prostate or breast cancer in men. Aggravated by the testosterone effects of the drug.
 Liver dysfunction, Cardiovascular disease. Can be exacerbated by the effects of the hormones.
 Topical forms of testosterone have a Black Box Warning alerting user to the risk of virilization in
children who come in contact with the drug from touching the clothes and skin of the man using the
drug.
 Danazol has Black Box warning regarding the risk of thromboembolic events, fetal
abnormalities, hepatitis, and intracranial hypertension.
Adverse Effects
Use of androgens may result to these adverse effects:
 Androgenic effects: acne, edema, hirsutism (increased hair distribution), deepening of the voice,
oily skin and hair, weight gain, decrease in breast size, and testicular atrophy.
 Anti-estrogen effects: flushing, sweating, vaginitis, nervousness, and emotional stability.
 Common effects: headache (possibly related to fluid and electrolyte changes),
dizziness, sleep disorders and fatigue, rash, and altered serum electrolytes.
 A potentially life-threatening effect that has been documented is hepatocellular cancer.

Interactions
The following are drug-laboratory interactions involved in the use of androgens:
  Decreased thyroid function
 Increased creatinine and creatinine clearance (results that are not associated with disease states)
 These effects can last up to 2 weeks after therapy has been discontinued.

Nursing Considerations
Important nursing considerations when administering this drug:

Nursing Assessment
Important things the nurse should include in conducting assessment, history taking, and examination:
 Assess for the mentioned cautions and contraindications (e.g. drug allergy, hepatic dysfunction, CV
diseases, breast/prostate cancer in men, etc.) to prevent any untoward complications.
 Perform a thorough physical assessment (e.g. skin assessment, mental status, abdominal
examination, etc.) to establish baseline data before drug therapy begins, to determine
effectiveness of therapy, and to evaluate for occurrence of any adverse effects associated with
drug therapy.
 Arrange for radiographs of the long bones in children to assess for testosterone effects on growth.

Nursing Diagnoses
Some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
 Disturbed body image related to androgenic effects
 Sexual dysfunction related to androgenic effects

Implementation with Rationale

Some vital nursing interventions done in patients who are taking androgens:
 Monitor responses carefully when beginning therapy so that the dose can be adjusted accordingly.
 Remove an old dermal system before applying a new system to clean, dry, and intact skin to
ensure accurate administration and decrease risk of toxicity.
 Monitor liver function periodically with long-term therapy and arrange to discontinue the drug at any
sign of hepatic dysfunction.
 Provide thorough patient teaching (e.g. measures to avoid adverse effects, warning signs, need for
regular evaluation, especially blood pressure, etc.) to enhance patient knowledge about drug
therapy and to promote compliance with the drug regimen.
 Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.

Evaluation
Some aspects of care that should be evaluated to determine effectiveness of drug therapy:
 Monitor patient response to therapy (e.g. onset of puberty, maintenance of male sexual
characteristics, palliation of breast cancer, etc.).
 Monitor for adverse effects (e.g. androgenic effects, hypoestrogen effects, serum electrolyte
imbalance, headache, etc).
 Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
 Monitor patient compliance to drug therapy.

.
Anabolic Steroids
- Anabolic steroids are testosterone analogues that have been developed to produce the tissue-
building effects of testosterone with less androgenic effect.

Therapeutic Action

The desired and beneficial actions of anabolic steroids are as follows:

 Promote body tissue-building processes.
 Reverse catabolic or tissue-destroying processes
 Increase hemoglobin and red blood cell mass.

Indications

Anabolic steroids are indicated for the following medical conditions:

 Anemias, certain cancers, and angioedema
 Promote weight gain and tissue repair in debilitated patients and protein anabolism in patients who
are receiving long-term corticosteroid therapy.
 Also known to be used illegally for the enhancement of athletic performance by promoting
increased muscle mass, hematocrit, strength, and endurance.

Contraindications and Cautions

The following are contraindications and cautions for the use of anabolic steroids:
 Allergy to androgens or other ingredients in the drug. Prevent hypersensitivity reactions.
 Pregnancy, lactation. Potential masculinization in neonates.
 Liver dysfunction. Drug is metabolized in the liver and are known to cause hepatic toxicity.
 Coronary disease. Potentional increase in cholesterol level through the effect of the drug on the
liver.
 Prostate/breast cancer in males. Exacerbated by the effects of these drugs.

Adverse Effects

Use of anabolic steroids may result to these adverse effects:

 In prepubertal males: virilization (e.g. phallic enlargement, hirsutism, increased skin pigmentation).
 In postpubertal males: inhibition of testicular function, gynecomastia, testicular atrophy, priapism
(painful and continual erection of the penis), baldness, and change in libido.
 In women: hirsutism, hoarseness, deepening of the voice, clitoral enlargement, baldness,
menstrual irregularities.

Interactions
The following are drug-drug interactions involved in the use of anabolic steroids:
 Potential interaction with oral anticoagulants
 Potentially decreased need for antidiabetic agents
 Altered lipid metabolism and lack of effectiveness for lipid-lowering agents

Nursing Considerations
Some important nursing considerations when administering this drug:
Nursing Assessment
These are the important things the nurse should include in conducting assessment, history taking, and
examination:
 Assess for the mentioned cautions and contraindications (e.g. drug allergy, pregnancy and
lactation, CV diseases, etc.) to prevent any untoward complications.
 Perform a thorough physical assessment (e.g. skin assessment, mental status, abdominal
examination, etc.) to establish baseline data before drug therapy begins, to determine
effectiveness of therapy, and to evaluate for occurrence of any adverse effects associated with
drug therapy.
 Arrange for radiographs of the long bones in children to assess for testosterone effects on growth.

Nursing Diagnoses
Some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
 Disturbed body image related to systemic effects
 Acute pain related to GI or CNS effects

Implementation with Rationale

Some vital nursing interventions done in patients who are taking androgens:

 Administer with food if GI effects are severe to relieve GI distress.

 Monitor endocrine and hepatic functions, serum electrolytes before and periodically during therapy
so that dose can be adjusted appropriately and severe adverse effects can be avoided.
 Provide thorough patient teaching (e.g. measures to avoid adverse effects, warning signs, need for
regular evaluation, especially blood pressure, etc.) to enhance patient knowledge about drug
therapy and to promote compliance with the drug regimen.

Evaluation
Some aspects of care that should be evaluated to determine effectiveness of drug therapy:
 Monitor patient response to therapy (e.g. increase in haematocrit, protein anabolism, etc.).
 Monitor for adverse effects (e.g. androgenic effects, serum electrolyte disturbances, epiphyseal
closure, hepatic dysfunction, etc).
 Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
 Monitor patient compliance to drug therapy.

Drugs For Treating Penile Erectile Dysfunction

- Penile erectile dysfunction is a condition in which the corpus cavernosum does not fill with blood to
allow for penile erection.
- Approved drugs for treatment of penile erectile dysfunction include prostaglandinalprostadil
and phosphodiesterase type 5 (PDE5) receptor inhibitor sildenafil.

Therapeutic Action
The desired and beneficial actions of drugs for treatment of penile erectile dysfunction are as follows:
 - Alprostadil acts locally to relax the vascular smooth muscle and allow filling of the corpus
cavernosum, causing penile erection.
- PDE5 receptor inhibitors act to increase nitrous oxide levels in the corpus cavernosum. Nitrous
oxide activates the enzyme cyclic guanosine monophosphate (cGMP) to cause smooth
muscle relaxation and increased flow of blood.

Indications
Prostaglandin and PDE5 receptor inhibitors are indicated for the following medical conditions:
- Treatment of penile erectile dysfunction.

Contraindications and Cautions

The following are contraindications and cautions for the use of these drugs:
- Presence of any anatomical obstruction or condition that might predispose to priapism. The risk
could be exacerbated by these drugs.
- Penile implants.
- Bleeding disorders, CV diseases, optic neuropathy, severe hepatic and renal disorders. 

Adverse Effects
Use of these drugs may result to these adverse effects:
 Local effects associated with alprostadil: pain at injection site, infection, priapism, fibrosis, rash.
 Effects associated with PDE5 inhibitors: headache, flushing, dyspepsia, urinary tract
infection, diarrhea, dizziness, possible eight cranial nerve toxicity and loss of hearing.
 A potentially life-threatening effect that has been documented is hepatocellular cancer.

Interactions
The following are drug-drug interactions involved in the use of these drugs:
 Organic nitrates, alpha-adrenergic blockers. Serious CV effects, including death, have occurred.
 Ketoconazole, itraconazole, erythromycin. Increased sildenafil levels.

Nursing Considerations
Some important nursing considerations when administering this drug:

Nursing Assessment
These are the important things the nurse should include in conducting assessment, history taking, and
examination:
 Assess for the mentioned cautions and contraindications (e.g. drug allergy, penile
implants, bleeding disorders, etc.) to prevent any untoward complications.
 Perform a thorough physical assessment (e.g. skin assessment, mental status, vital signs, etc.) to
establish baseline data before drug therapy begins, to determine effectiveness of therapy, and to
evaluate for occurrence of any adverse effects associated with drug therapy.
 Evaluate laboratory tests for bleeding time and liver function to monitor potential adverse effects on
the liver.

Nursing Diagnoses
Some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
 Disturbed body image related to drug effects
 Sexual dysfunction related to drug effects
Implementation with Rationale
Some vital nursing interventions done in patients who are taking these drugs:
 Assess the cause of dysfunction before beginning therapy to ensure appropriate use of these
drugs.
 Monitor patients with vascular disease for any sign of exacerbation so that the drug can be
discontinued before severe adverse effects occur.
 Monitor responses carefully when beginning therapy so that the dose can be adjusted accordingly.
 Provide thorough patient teaching (e.g. measures to avoid adverse effects, warning signs, need for
regular evaluation, especially blood pressure, etc.) to enhance patient knowledge about drug
therapy and to promote compliance with the drug regimen.

Evaluation
Some aspects of care that should be evaluated to determine effectiveness of drug therapy:
 Monitor patient response to therapy (improvement of penile erection).
 Monitor for adverse effects (e.g. dizziness, flushing, local inflammation or infection,
fibrosis, diarrhea, etc.).
 Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
 Monitor patient compliance to drug therapy.

TOPIC B: CARDIOVASCULAR DRUGS

Antianginal drugs 

- 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.
- They also decrease the workload of the heart so the organ would have less demand for oxygen. 
- Antianginal drugs are nitrates, beta-blockers, and calcium channel blockers

Antianginal Drugs: Generic and Brand Names

Classification Generic Name Brand Name

amyl nitrate Vaporole
Isosorbide mononitrate Imdur, Monoket
Nitrates and Nitrites
Isosorbide dinitrate Isordil, Sorbitrate
Nitroglycerin Nitro-Bid, Nitrostat
Beta-adrenergic blockers acebutolol Sectral
esmolol Brevibloc
 Classification Generic Name Brand Name
metoprolol Toprol, Toprol XL
Nadolol Corgard
propranolol Inderal, Lopressor
Timolol Blocadren
amlodipine Norvasc
diltiazem Diltiazem, Diltiazem SR
Calcium-channel blockers nicardipine Cardene
nifedipine Adalat, Procardia
verapamil Calan, Isoptin
Others:
Piperazineacetamides ranolazine Ranexa
Nonnitrate coronary vasodilators dipyridamole Persantine

Disease spotlight: Coronary Artery Disease

Coronary Artery Disease (CAD)

-  The narrowing of blood vessels supplying oxygen and nutrients to the heart, primarily due to the
development of fatty tumors (atheromas) in the lumen of blood vessels in a process called
atherosclerosis.
- This pathologic process attracts platelets and clotting factors to the area, causing a much larger
obstruction to the vessels. The vessels also lose their natural ability to be elastic, resulting to
inability to dilate and constrict. The heart stimulates the blood vessels to deliver more blood but
blood delivery is limited by narrow vessel diameter, resulting to low oxygen supply of the heart.
- As a consequence of hypoxia, pain (angina) is felt.

There are two types of angina:

1. Classic angina (of exercise), which occurs due to diminished coronary blood flow to the heart; and
2. Vasospastic/Prinzmetal’s/variant angina, which is caused by reversible vasospasm even at rest.

*Both types decrease oxygen supply of the heart.

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 drop in systemic blood pressure.
- It compensates by increasing blood flow to healthy arteries and veins because affected vessels
already lose their elasticity.

Indications
- Children: 
o May be used only for congenital heart defects and cardiac surgery because they can
cause potentially dangerous changes in blood pressure.
- Adults: 
o Should be educated on drug’s various forms and their proper administration, storage,
effectiveness, and manifestations that would warrant prompt medical help.
o Lifestyle modifications such as smoking cessation, low-fat diet, and weight loss should be
encouraged to promote effectiveness of Antianginal therapy.
- Older adults: 
o Safety measures should be instituted as they are prone to adverse effects like arrhythmias
and hypotension.
o They should receive initial low dose because of probably hepatic and renal impairments
which can interfere with metabolism and excretion of drugs.
- Use during pregnancy is not established.
- Sublingual nitroglycerin is most effective for recurrent variant angina.
- Continuous infusion or transdermal patch for unstable angina.

Pharmacokinetics

Route Onset Duration

IV 1-2 min 3-5 min
Sublingual tablet 1-3 min 30-60 min
Translingual spray 2 min 30-60 min
Transmucosal tablet 1-2 min 3-5 min
Oral SR tablet 20-45 min 8-12 h
Topical Ointment 30-60 min 4-8 h
Transdermal 30-60 min 24 h
T1/2: 1-4 min
Metabolism: liver
Excretion: kidney (urine)
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 Management

Nursing Assessment
Presence of mentioned contraindications and cautions
 Skin color and integrity, especially for transdermal or topical forms of nitrates
 Pain and activity level
 Neurological status (level of consciousness, affect, reflexes, etc.)
 Cardiopulmonary status (BP; take heart rate in full minute)
 Electrocardiogram as ordered
 Laboratory tests (e.g. CBC, liver and kidney function tests, etc.)

Nursing Diagnoses
 Decreased cardiac output related to vasodilation and hypotensive effects of the drug
 Risk for Injury related to adverse effects on neurological and cardiovascular status
 Ineffective Tissue Perfusion related to low oxygen supply to myocardial cells
Implementation with Rationale
 Instruct patient 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.
 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.

Evaluation
 Monitor patient response to therapy (pain assessment).
 Monitor for presence of mentioned adverse effects.
 Monitor for effectiveness of comfort measures.
 Monitor for compliance to drug therapy regimen.
 Monitor laboratory tests.

Beta-Adrenergic Blockers

- Beta-adrenergic blockers are drugs which block or lyse the effects of sympathetic stimulation.
- They are also called as 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
1. Nadolol is used for management of chronic angina. It is the drug of choice in angina patients
with hypertension.
2. Propranolol is the prototype drug of this class. It is used for treatment of angina and syncope.
3. Nebivolol, the newest adrenergic blocking agent does not produce the same adverse effects seen
in propranolol.

Pharmacokinetics

Route Onset Peak Duration

Oral 15 min 90 min 15-19 h
IV Immediate 60-90 min 15-19 h
T1/2: 3-4 h
Metabolism: liver
Excretion: kidney (urine)

Food increases bioavailability of propranolol.

Propranolol is the only drug under this class that can cross the blood-brain barrier.

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
 Re spiratory: 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 Considerations

Nursing Assessment

 Assess for presence of mentioned contraindications and cautions.

 Assess neurological status to determine presence of neurological adverse effects. Focus on level
of orientation and sensory function.
 Monitor blood pressure and heart rate accurately. Be sure to count the heart rate in one full minute.
 Auscultate lungs to determine presence of possible respiratory adverse effects.
 Check color and sensation of extremities. Measure capillary refill. This is to evaluate presence of
insufficiencies in the peripheral vascular system.
 Monitor laboratory test results (e.g. electrolyte levels and renal function tests) to ascertain risk for
arrhythmia and discern whether dose adjustment is needed.

Nursing Diagnosis
 Decreased Cardiac Output related to decreased heart rate, blood pressure, and contractile
properties of the heart
 Ineffective Tissue Perfusion related to decreased blood flow to the heart
 Risk for Injury related to possible alterations in CNS while on drug therapy

Implementation with Rationale

  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.

Evaluation
 Monitor patient response to therapy.
 Monitor for presence of mentioned adverse effects.
 Monitor for effectiveness of comfort measures.
 Monitor for compliance to drug therapy regimen.
 Monitor laboratory tests.

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.
- 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

Pharmacokinetics

Route Onset Peak Duration

Oral 30-60 min 2-3 h 2-4 h
SR, ER 30-60 min 6-11 h Varies
IV Immediate 2-3 min Varies
T1/2: SR (3.5-6h); ER (6-7h)
Metabolism: liver
Excretion: kidney (urine)
Contraindications and Cautions
 Allergy to drugs
 Heart block and sick sinus syndrome – conduction problems in these 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, light-headedness, 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 Considerations

Nursing Assessment
 Assess for presence of mentioned contraindications and cautions.
 Inspect skin color and integrity to determine presence of adverse effects on skin.
 Assess the patient’s complaint of pain and the activity level prior to and after the onset of pain to
aid in identifying possible contributing factors to the pain and its progression.
 Monitor cardiopulmonary status closely as the drug can cause severe effects on these two body
systems.

Nursing Diagnosis
 Decreased Cardiac Output related to hypotension and vasodilating effect of the drugs
 Risk for Injury related to cardiovascular and CNS adverse drug effects

Implementation with Rationale

 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.

Evaluation
 Monitor patient response to therapy.
  Monitor for presence of mentioned adverse effects.
 Monitor for effectiveness of comfort measures.
 Monitor for compliance to drug therapy regimen.
 Monitor laboratory tests.

Antiarrhythmics

-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.

Antiarrhythmic: Generic and Brand Names

A table of commonly encountered antiarrhythmic drugs, their generic names, and brand names:

Classifications Generic Name Brand Name

Class I antiarrhythmics
disopyramide Norpace
Class IA procainamide Pronestyl
quinidine Quinaglute, Quinidex
lidocaine Xylocaine
Class IB
mexiletine Mexilitil
flecainide Tambocor
Class IC
Propafenone Rythmol
acebutolol Sectral
Class II Antiarrhythmics esmolol Brevibloc
propranolol Inderal
ibutilide Corvert
Class III Antiarrhythmics
sotalol Betapace
Class IV Antiarrhythmics verapamil Calan, Covera-HS
adenosine Adenocard
Other Antiarrhythmics digoxin Lanoxin
Dronedarone Multaq

Disease Spotlight: Arrhythmias

Arrhythmias (also called dysrhythmias) involve changes in the automaticity and conductivity of the heart
cells.

To better understand this condition, there are two concepts vital to be mastered: conductivity and
automaticity.
Conductivity:
- is the property of the heart cells to transmit spontaneous impulses starting from the sinoatrial (SA)
node, activating all parts of the heart muscle almost spontaneously. Conductivity is the basis of
cardiac contraction and relaxation, allowing the heart to beat. Different areas of the specialized
conductive system include:
- SA node – impulse generation of 60-100 impulses per minute
- AV node – 40-50 impulses per minute
- Ventricular muscle cells – 10-20 impulses per minute

Automaticity:

- is the property of the heart cells to undergo spontaneous depolarization during relaxation. This is
because at this point, potassium flows out of the cell while sodium moves inside: the condition
necessary to produce an action potential. Here are the five phases of action potential:

- Phase 0 – depolarization phase;

o stage in which cell reaches point of stimulation. This phase is characterized by open
sodium gates and sodium ions rushing towards the cell leading to action potential. There is
absence of charge difference between the outside and the inside of the membrane.
- Phase 1 –
o a very short period wherein concentration of sodium equalizes inside and outside of the
cell
- Phase 2 – plateau phase;
o stage in which cell is trying to go back to its resting stage (repolarization). The cell
becomes less permeable to sodium, potassium begins to leave the cell, and calcium starts
to enter the cell.
- Phase 3 – rapid repolarization phase;
o stage in which the sodium gates are closed and potassium flows out of the cell.
- Phase 4 – resting phase;
o stage in which sodium-potassium pump restores the cell’s resting membrane potential in
preparation for the next action potential.

Types of arrhythmias

Depending on factors causing them, here are different types of arrhythmias:

- Changes in rate: tachycardia, bradycardia
- Stimulation from ectopic focus: premature atrial contractions (PACs), premature ventricular
contractions (PVCs), atrial flutter and/or fibrillation (AF), ventricular fibrillation
- Alterations in conduction through the muscle: heart blocks, bundle branch block
 - It can be triggered by the following: electrolyte disturbances, decreased oxygen supply to the cells,
structural damage of the conduction system, drug effects, acidosis, and lactic acid accumulation.

Class I antiarrhythmics

- This class blocks sodium channels in the cell membrane during action potential. Subgroup under
this class is based on their mechanism in blocking sodium channels.
- These class are 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.
 Children
o Antiarrhythmics are not often used for this age group
 Adults
o Usually indicated for emergency cases.
 Evaluation of drug regimen should be done carefully and regularly to ensure effectiveness and
patient safety.
 Drug safety for pregnant women not established.
 This drug can enter breast milk and has been associated with various side-effects.
 Antiarrhythmics I, III, and IV are strictly prohibited to lactating women.
 Older adults
 They are more susceptible to drug toxicity because of underlying conditions that would interfere
with metabolism and excretion of drug.
 Renal and hepatic function should always be monitored.

Pharmacokinetics

Route Onset Peak Duration

IM 5-10 min 5-15 min 2h
IV Immediate Immediate 10-20 min
T1/2: 10 min, then 1.5-3 h
Metabolism: liver
 Excretion: urine

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. That would result to decreased in heart rate, excitability, and cardiac output .

Conduction through AV node also slows down. In the kidneys, release of renin is decreased. These effects
decrease blood pressure and the stabilize the highly-excitable heart. As a result, workload of the heart is
lessened.
Indications

This class is specifically indicated for treatment of supraventricular tachycardia and premature ventricular
contractions (PVCs).

Children: antiarrhythmics are not often used for this age group

Adults: usually indicated for emergency cases. Evaluation of drug regimen should be done carefully and
regularly to ensure effectiveness and patient safety. Drug safety for pregnant women not established. This
drug can enter breast milk and has been associated with various side-effects. Antiarrhythmics I, III, and IV
are strictly prohibited to lactating women.

Older adults: are more susceptible to drug toxicity because of underlying conditions that would interfere
with metabolism and excretion of drug. Renal and hepatic function should always be monitored.

Pharmacokinetics

Route Onset Peak Duration

Oral 20-30 min 60-90 min 6-12 h
IV Immediate 1 min 4-6 h
T1/2: 3-5 h
Metabolism: liver
Excretion: urine

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.

Children: antiarrhythmics are not often used for this age group

Adults: usually indicated for emergency cases. Evaluation of drug regimen should be done carefully and
regularly to ensure effectiveness and patient safety. Drug safety for pregnant women not established. This
drug can enter breast milk and has been associated with various side-effects. Antiarrhythmics I, III, and IV
are strictly prohibited to lactating women.

Older adults: are more susceptible to drug toxicity because of underlying conditions that would interfere
with metabolism and excretion of drug. Renal and hepatic function should always be monitored.

Pharmacokinetics

Route Onset Peak Duration

Oral 2-3 d 3-7 h 6-8 h
IV Immediate 20 min Infusion
T1/2: 10 d
Metabolism: liver
Excretion: urine

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.

Children: antiarrhythmics are not often used for this age group

Adults: usually indicated for emergency cases. Evaluation of drug regimen should be done carefully and
regularly to ensure effectiveness and patient safety. Drug safety for pregnant women not established. This
drug can enter breast milk and has been associated with various side-effects. Antiarrhythmics I, III, and IV
are strictly prohibited to lactating women.

Older adults: are more susceptible to drug toxicity because of underlying conditions that would interfere
with metabolism and excretion of drug. Renal and hepatic function should always be monitored.

Pharmacokinetics

Route Onset Peak Duration

Oral 30-60 min 2-3 h 6-8 h
IV Immediate 2-3 min Unknown
T1/2: 3.5-6 h
Metabolism: liver
Excretion: urine

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.

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 Considerations for Antiarrhythmics

Some important nursing considerations when administering antiarrhythmics.

Nursing Assessment

Some important things the nurse should include in conducting assessment, history taking, and
examination:
 Assess for the mentioned contraindications to this drug (e.g. renal dysfunction, heart blocks,
hypersensitivity, etc.) to prevent potential adverse effects.
 Conduct thorough physical assessment before beginning drug therapy to establish baseline status,
determine effectively of therapy, and evaluate potential adverse effects.
 Assess patient’s neurological status to determine potential CNS drug effects.
 Assess cardiac status closely (e.g. blood pressure, heart rate and rhythm, heart sounds, ec.) to
determine whether change in drug dose is imperative.
 Monitor respiratory rate, rhythm, and depth to assess for respiratory depression and detect
changes associated with development of HF.
 Monitor laboratory test results including complete blood count, renal and liver function tests to
determine the need for possible change in dose and identify toxic effects.

Nursing Diagnoses

Some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
 Decreased cardiac output related to cardiac effects of the drug
 Ineffective tissue perfusion related to decreased blood flow to different parts of the body
 Altered sensory perception related to CNS drug effects
  Risk for injury related to weakness and dizziness

Implementation with Rationale

Vital nursing interventions done in patients who are taking antiarrhythmics:

 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 patient tolerate drug effects.
 Ensure maintenance of emergency drugs and equipment at bedside to promote prompt treatment
in cases of severe toxicity.
 Educate patient 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.

Evaluation

Some aspects of care that should be evaluated to determine effectiveness of drug therapy:
 Monitor patient response to therapy through assessment of cardiac output and rhythm.
 Monitor for adverse effects (e.g. sedation, respiratory depression, CNS effects).
 Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
 Monitor patient compliance to drug therapy.