❖ Assist B cells in humoral response to form antibodies

2. Suppressor T cells (T8)

IMMUNE SYSTEM FUNCTION ❖ suppress B cell synthesis of antibody production via
feedback mechanism.
⮚ Reacts protectively against foreign antigens or mutations in the
body
1. Defense
2. Homeostasis
3. Surveillance

⮚ Non – specific immunity
★ Do not act on only one or two specific invaders, but rather
provide a more general defense by simply acting against
anything recognized as not self
⮚ Specific immunity
★ Recognize specific threatening agents and respond by
targeting their activity against these agents.
3. Memory T cells
❖ store future immune response to some antigen.
4. Cytotoxic T cells
❖ directly attack antigen thus altering cell wall membrane with
resultant cell lysis; also release chemical mediators known
as lymphokines which can attract and hold macrophages
and lymphocytes to the site of injury.

BODY’S DEFENSES
❖ reaction to tissue injury caused by the release of chemical mediators
❖ Barrier defenses that cause both a vascular response and the migration of fluid and
⮚ Mucous membranes – GI, GU, mucus, respiratory tract cells to the injured site
⮚ Skin – physical barrier, glands, sloughs off, flora
❖ Major histocompatibility complex (MHC) / Human Leukocytes 3 chemical mediators
Antigens (HLA)
⮚ Self and non self ⮚ Histamines
❖ Cellular defenses ⮚ Kinins
⮚ Leukocytes - stem cells in BM ⮚ Prostaglandins
● Lymphocytes – Tcells, Bcells natural killer cells
● Myelocytes – neutrophils, basophils, macrophage Important chemical mediators
⮚ Mast cells – don’t circulate
● Release mediators when stimulated

Mechanisms of Specific Immunity:

⮚ Humoral immunity (B – Lymphocyte)

⮚ Cell – mediated immunity (T – lymphocyte)

● Humoral immunity (B-Lymphocyte)

❖ Involves the formation of antibodies by plasma cells in
response to foreign proteins
❖ TYPES OF IMMUNOGLOBULINS
● IgG
● IgA
● IgM
● IgE Cardinal signs of Inflammation
● IgD ● Redness (rubor)
● Cell-mediated immunity (T-Lymphocyte) ● Edema (tumor)
❖ involves attack of microbes by special killer T cells formed ● Heat (calor)
from lymphocytes ● Pain (dolor)
❖ Influence and regulate the activities of antibody mediated ● Loss of function
immunity and inflammation by producing and releasing of
CYTOKINES ANTI-INFLAMMATORY AGENTS
❖ It functions primarily in delayed hypersensitivity reactions;
rejection of transplants; and viral, fungal, and chronic ❖ also called PROSTAGLANDIN INHIBITORS (inhibit the biosynthesis
infections. of prostaglandin which can affect the inflammatory process)

Several types of T cells:

1. Helper T cells (T4)

1
 ❖ Derived from from SALICYLIC ACID (acetylsalicylic acid)
used with cardiac
disorders : PLATELET AGGREGATION

Pharmacokinetics: well absorbed in GIT: can cause GIT UPSET

Pharmacodynamics: inhbits COX-1 and COX-2

Indication: mild – moderate pain; control of fever; inflammatory

conditions

SALICYLISM – aspirin toxicity

⮚ Tinnitus
⮚ Confusion
⮚ Dizziness

Nursing Considerations

✔ Monitor CBC, PT, PTT, kidney & liver function test

✔ Additive effect on clients on ANTI-COAGULANT!
✔ Stop a week BEFORE SURGERY.
✔ Observe for SIGNS of BLEEDING!
✔ NOT to be administered for flu/viral symptoms in CHILDREN
✔ Monitor SERUM LEVEL: 15 – 30mg/dl

Discharge teaching:

✔ Increase OFI: to prevent SALICYLATE CRYSTALLURIA

✔ Take with FULL stomach.
✔ Report signs of bleeding.
2 forms of Cyclo-Oxygenase ✔ DC if with signs of TOXICITY
✔ No to pregnant….
1. COX 1 – protects the stomach lining and regulates blood ✔ Do not crush enteric coated….
platelets
2. COX 2 – triggers inflamation and pain 2. Para – chlorobenzoic Acid

Additional properties of Anti-inflammatory agents: INDOMETHACIN (Indocin)

✔ Relief of pain (analgesic) ❖ for RA, gouty arthritis & osteoarthritis

✔ Reduction of elevated body temperature (antipyretic) ❖ Causes GIT UPSET
✔ Inhibition of platelet aggregation (anticoagulant) ❖ Causes CORNEAL CLOUDINESS, VISUAL FIELD
CHANGES
CLASSIFICATIONS

1. Non-steroidal Anti-inflammatory Drugs (NSAIDs)

2. Corticosteroids 3. Phenylacetic Acid Derivatives

DICLOFENA SODIUM (Voltaren)

● Inhibit the enzyme COX ❖ has minimal to no antipyretic effect

● Can be: ANALGESIC, ANTIPYRETIC, ❖ A/E similar to other NSAIDS
ANTI-INFLAMMATORY ❖ INJECTABLE NSAID: Ketorolac (Toradol)
● More appropriate in reducing: SWELLING, PAIN, JOINT ● has greater analgesic effect
STIFFNESS ● short term pain management

7 groups of NSAIDs

1. Salicylates (related to aspirin) 4. Propionic Acid Deviratives

❖ Aspirin like but w/ STRONGER effect & LESS GI
1.1 ASPIRIN (ASA) IRRITATION
❖ Well absorbed in the GIT

2
 ❖ Short half –life but highly protein bound - Hyperpigmentation
❖ Metablozied in the liver - Weight gain
❖ May take several days to see anti-inflammatory effect - Hirsutism
● IBUPROFEN (Motrin) - Lowered resistance to infections
⮚ Hypoglycemia – if taken with insulin or - GIT upset
OHD (oral hypoglycemic drug)
⮚ Toxicity - if taken with calcium channel
blockers
● Naproxen (Naprosyn)
● Ketoprofen (Orudis)
● Fenoprofen Calcium (Nalfon) Nursing implications:
● Suprofen (Profenal)
● Flurbiprofen 1. Monitor BP, weight, I & O, Blood glucose & K+
● Oxaprozin 2. Corticosteroid doses are not interchangeable.
3. It should not be abruptly withdrawn (it cause ADRENAL
5. Fenamates INSUFFICIENCY).
- Used for acute and chronic arthritic conditions 4. Oral form should be taken with FULL stomach.
- S/E: TINNITUS, EDEMA, DIZZINESS, PRURITIS
● MECLOFEN-AMATE SODIUM MONOHYDRATE Discharge teaching
(MECLOMEN)
● MEFENAMIC ACID (PONSTAN, DOLFENAL) 1. Taken with full stomach.
6. Oxicams 2. Not to abruptly stop.
- Indicated for long term treatment of arthritic conditions 3. Eat food high in potassium.
- Highly protein bound 4. Avoid crowds and individual w/ infection.
- Cause GIT IRRITATION 5. Restrict sodium, alcohol and caffeine.
● Piroxicam (Feldene) – should not be taken with aspirin 6. For inhaled drugs: rinse mouth after.
or other NSAIDs
Common drugs
7. Selective Cox – 2 Inhibitors
- Less risk of GIT upset
● Prednisone (Pred 10)
- Used among clients needing HIGH DOSES of
● Fludcortisone (Florinef)
anti-inflammatory agents
● Hydrocortisone (Cortisol)
● REFOCOXIB (VIOXX)
● Dexamethasone (Decadron)
● CELECOXIB( CELEBREX)
● Methylprednisolone (Medrol)

✔ Vaccines
✔ Immune stimulants
❖ hormones that regulate protein, carbohydrate, and fat
✔ Immune suppressants
metabolism and affect other body processes such as
inflammation
❖ Suppress anti – inflammatory reactions
❖ (stabilize lysosomal membranes preventing release of
❖ Comes from the Latin word for smallpox, “vaccinia”
proteolytic enzymes)
❖ Immunizations contained weakened or altered protein antigens
❖ Half life is long, thus, given OD (once a day in a large
❖ Can be made from chemically inactivated microorganisms or from
prescribed dose)
live, weakened viruses or bacteria.
❖ Toxoids are vaccines that are made from the toxins produced by
WHAT ELSE DOES IT DO?
the microorganism.
⮚ Immunity
1. Atrophy of thymus gland.
● Innate immunity
2. Decrease number of lymphocytes, plasma cells and eosinophils.
● Acquired immunity
3. Interfere T and B lymphocytes’ role
⮚ Active immunity - occurs when antigens enter the body and the
4. Interfere immune and inflammatory response.
body responds by making specific antibodies against the antigen
Circadian Rhythm ⮚ Passive immunity - occurs when antibodies against a specific
antigen are in a person’s body but the person did not actively
- NATURAL GLUCOCORTECOSTEROIDS generate these antibodies
- peak level = after awakening and early phase of sleep
- IMPLICATION: Therapy given at midnight is more potent Types of Acquired Immunity
rather than at noon

Side Effects:

- Euphoria
- Insomnia
- Increase apppetite
3
 ACTION AND INDICATION:

● Stimulate active immunity in people who are at high risk for

development of a particular disease.
● Vaccines are thought to provide lifelong immunity to the
disease against which the patient is being immunized.

CONTRAINDICATIONS AND CAUTIONS

● Presence of immune deficiency

● During pregnancy because of potential effects on the fetus
and on the success of the pregnancy
● Known allergies to any of the components of the vaccine
● Patients who are receiving immunoglobulin or who have
received blood or blood products within the last 3 months
because a serious immune reaction could occur.

Vaccines ADVERSE EFFECTS

- contain whole microbes (dead or attenuated) that are not X moderate fever, chills
pathogenic but can induce formation of antibodies X rash
X Body malaise
Toxoids X drowsiness
X anorexia, vomiting
- contain detoxified microbe by products which are antigenic X Irritability.
and can induce antibody formation X Pain, redness, swelling, and even nodule formation at the
injection site
LIVE VS. INACTIVATED PRODUCTS
X severe hypersensitivity reactions

Live Attenuated Type

CHOLERA VACCINE

- Route: SC or IM
- Have EPINEPHRINE at bedside

HEMOPHILUS INFLEUENZAE

- Route: IM
- Shake well & store in medical refrigerator.
- May be given at the same time w/ DPT but at different site.
- Have EPINEPHRINE at bedside.
Inactivated (killed) Type

HEPATITIS B

- Route: (Killed) IM
- Store open and unopened vial in the refrigerator

INFLUENZA

Vaccinations in Special Situations - Route: IM

- Given annually
● Premature infants should be vaccinated on the same - No to w/ ALLERGY to EGGS!
chronological age as full term infants and with the same - Refrigerate
recommended dose.
● There is no contraindication to breastfeeding and vaccinations. MEASLES
● Vaccinations during pregnancy depend on weighing the
potential risk of the vaccine against the result of disease - Route: (Live) SC
exposure. - May need to reimmunize if given <15 months
● Contraindications to all vaccines include history of anaphylaxis - No to w/ ALLERGIES to EGG and NEOMYCIN
or the presence of moderate to severe illness with or without
fever. MENIGOCOCCAL MENIGITIS VACCINE

- Route: SC
- One dose only

POLIOMYELITIS VACCINE

4
 - Route: Oral Recombinant DNA Technology

RABBIES VACCINE ● Interferon alfa-2a (Roferon-A)

● Interferon alfa-2b (Intron-A)
- Route: IM ● Interferon alfacon-1 (Infergen)
- Pre-exposure: 2 doses 1 week apart followed by a third dose ● Interferon alfa-n3 (Alferon N)
between 21 and 28 days ● Interferon b-1a (Avonex)
- Post-exposure:
Therapeutic action and indications
RUBBELLA
- Act to prevent virus particles from replicating inside other
- Route: SC cells
- Women must not become pregnant 3 months after - Stimulate receptor sites on non-invaded cells to produce
immunization antiviral proteins
- Inhibit tumor growth and replication
Nursing Management

⮚ Assessment
- Age
- Physical Condition
- History of exposure
- Previous immunization
⮚ Nursing Diagnosis
- Deficient knowledge: vaccine-preventable diseases, risks
KINETICS
and benefits of vaccination
- Ineffective health maintenance
- Well absorbed SC and IM
⮚ Planning
- Excreted primarily through kidneys
- Client will adhere to the immunization
- Teratogenic
- Client will be free of A/E.
⮚ Interventions
Contraindications and Precautions
- Adhere to the storage and ensure potency of the product.
- Administer within time limits. X Known allergies
- Administer in separates and do not mix in one syringe. X Pregnancy and lactation
- Documentation. X Cardiac disease
- Observe for A/E. X Myelosuppression
- Have emergency drug on hand. X CNS dysfunction
- Provide client with record.
⮚ Client teaching Adverse drug reactions
- Discuss manifestations and risks of diseases.
- Inform female of childbearing age to avoid pregnancy 1 X Stimulate immune and inflammatory reactions
month post immunization or depending on the vaccine. X anorexia and nervosa
- Avoid contact with immunocompromised. X Headache, dizziness
- Remind them to bring immunization record and to adhere to X Bone Marrow depression
schedule strictly. X depression and suicidal ideation
⮚ Evaluation X photosensitivity, liver impairment

INTERLEUKINS

- used to energize immune system when exhausted from fighting
prolonged invasion or needs help fighting a specific pathogen or
cancer cells
⮚ Interferons - naturally released from human cells in response
to viral invasion
⮚ Interleukins - synthetic compounds that communicate
between lymphocytes, which stimulate cellular immunity and
inhibit tumor growth
⮚ T&B cell modulators - restore immune function and
stimulates immune system activity levamisole (Ergamisol)
INTERFERONS
- naturally produced and released human cells that have been
invaded by viruses
- released from cells in response to other stimuli
Subclasses:
- chemicals produced by T-cells to communicate between
leukocytes
- stimulates cellular activity by increasing activity of natural
killer cells, platelets, cytokines
- Drugs: Aldesleukin (Proleukin)
Oprelvekin (Neumega)
Therapeutic actions and indications:
- naturally produced by helper T cells to act cell activity and
decreased tumor growth by increasing lymphatic numbers
and activities
- when administered, increased number of natural killer cells
and lymphocytes, cytokine act, circ platelet
⮚ Aldesleukin – special renal carcinomas that are
invest for treatment of AIDS and related D/O
⮚ Oprelvekin – prevents severe thrombocytopenia
(<plts) post myelosuppression or chemo
5
KINETICS ● Bone marrow depression
● Get baseline status
- cleared by kidneys ⮚ Nursing diagnosis
- embryocidal and teratogenic ● Acute pain related to CNS, GI and flu-like effects
- use barrier contraceptives ● Imbalance nutrition: less than body requirements
- no lactation because of potential ADR related to flu – like symptoms
● Anxiety related to diagnosis and drug therapy
C/I AND CAUTIONS ● Deficient knowledge regarding therapy
⮚ Interventions
- allergies to E.coli prod ● Periodic laboratory tests.
- pregnancy and lactation women ● Administer as indicated.
- caution with liver/renal/cardiac ● Monitor for A/E.
● Arrange for supportive care and comfort
Adverse drug reaction measures.
● Instruct female client to use contraceptives.
- Inflammatory Response – lethargy, myalgia, arthralgia, ● Provide thorough teaching.
fatigue, fever ● Offer support and encouragement.
- Respiratory difficulties, CNS changes, cardiac ⮚ Evaluation

T AND B CELL MODULATORS

- Specified drug – Levamisol (Ergamisol) – immune

stimulation and restore suppressed immune function - used in conjunction with corticosteroids
- beneficial with organ transplant and treatment of
Therapeutic actions and INDS autoimmune disorder
- T&B cell suppressor, interleukin receptor antagonist,
monoclonal
- FOCUS ON PATIENT SAFETY!!!

T & B CELL SUPPRESSORS

Specified drugs:

⮚ Cyclosporine (Sandimmune/Neoral)
- suppress rejection with transplantation
- most commonly used immune suppressant
- embryotoxic and breast milk
⮚ Alefacept (Amevive)
- adults with severe chronic psoriasis for systemic therapy =
teratogenic, non- lactation
⮚ Azathioprine (Imuran)
- prevents rejection with renal homo-transplantation
C/I and Cautions
Therapeutic Actions
- Pregnancy
- Lactation - exact mechanism if unknown
- Allergy - block antibody production (B cells)
- inhibit suppressor and helper T cells
Adverse Effects - modify release of interleukins and T cell growth factor

- immune stimulation – flu-like effects (lethargy, myalgia, C/I ANG CAUTIONS

arthralgia, fever)
- taste perversion - pregnancy and lactation
- dizziness headache - renal and hepatic impairment
- known neoplasms
DRUG/DRUG INTERACTION
ADR
- disulfiram type reaction with alcohol
- can increase phenytoin level - infections
- neoplasms,
NURSING CARE MANAGEMENT - hepatotoxicity, renal

⮚ Assessment Drug/Drug Interaction

● Allergies
● Pregnancy or lactation - incomplete toxicity if in combine with other hepatotoxic or
● Hepatic, renal, CNS or cardiac disease nephrotoxic drugs

6
 Effects

⮚ Bactericidal – kills bacteria

⮚ Bacteriostatic – inhibit bacterial growth
INTERLEUKIN – I
MECHANISMS OF ACTION
- elevated in response to inflammation (ex. R.A.)
● Inhibition of bacterial cell wall synthesis
Prototype: ● Alteration in cell membrane function
● Inhibition of protein synthesis
⮚ Anakinra (Kineret) ● Inhibition of nucleic acid metabolism
- Block the effect of interleukin – I receptors ● Interference with Intermediate Cell Metabolism
- Pharmacokinetics:
recommended dose: 100mg/dl (SQ) NATURALLY RESISTANT BACTERIA TO AN ANTIBIOTIC
metabolized in the tissues
Contraindication & Caution - A natural, or inherent, resistance occurs without previous
- Known allergy to E.coli produced products exposure to the antibacterial drug
- pregnancy and lactation, renal, immunosuppression, active - For example, the gram negative (non-gram staining)
infection bacterium Pseudomonas aeruginosa is resistant to Penicillin
- Alcoholic beverages are contraindicated G
- SQ and store in refrigerator ( note the expiration date)

Adverse reaction
- headache, sinusitis, nausea, diarrhea, URTI other infections
- injection site reactions
Drug/Drug interactions
- Etanercept (Enbrel) – monitor closely d/t severe life
threatening reactions to occur
Screen factors that could aggravate conditions
✔ Arrange for lab tests before and periodically during therapy
✔ Protect from infection and maintain strict asepsis esp. with
invasive procedures
✔ Arrange for supportive care and comfort measures
✔ Provide small frequent meals, mouth care
✔ Barrier contraceptives
✔ Provide thorough patient teaching on adverse effects,
problem warning signs, administration
AQUIRED RESISTANT BACTERIA TO AN ANTIBIOTIC
- An acquired resistance is caused by prior exposure to the
antibacterial
- For example: Staphylococcus aureus was once sensitive to
penicillin G; previous exposure have caused this organism to
become resistant to it
GENERAL ADVERSE REACTIONS
⮚ Allergic reactions – rash pruritus, hives, anaphylaxis
⮚ Super impose infection – secondary infection
⮚ Organ toxicity – liver and kidney
NARROW – SPECTRUM ANTIBIOTIC
- Primarily effective against one type of organism
- Example: Penicillin and Erythromycin are used to treat
infections caused by gram-positive bacteria

BROAD – SPECTRUM ANTIBIOTIC

- Antibacterials and antimicrobials are substances that inhibit
the growth of bacteria or kill it and other microorganisms
- Antibiotic refers to chemicals produced by one kind of
microorganism that inhibits the growth of or kills another
Background
- Frequently used to treat infections when the offending
microorganisms has not been identified by C&S
- Certain broad – spectrum antibiotics, such as tetracycline
and the cephalosporins can be effective against both gram –
positive and gram-negative organisms

Bacteria

- Single cell prokaryotes lacking a true nucleus and

nucleus membranes 1. PENICILLINS
- With a rigid cell wall
Background
History
- Became widely used in 1945
1928 – Alexander Fleming - Considered ‘miracle drug”
- Penicillin G is the 1st PCN orally but with poor absorption
1939 – Howard Florey purified PCN (penicillin) to be used
commercially
Derivatives
1945 – PCN was used and marketed

7
 ● Broad spectrum PCN (Aminopenicillins) - bactericidal
● Penicillinase resistant PCN (Antistaphylococcal)
● Extended Spectrum Penicillins (Antipseudomonal) Generations
● Beta – Lactamase Inhibitors
⮚ First Generation
DRUGS IN FOCUS - Effective against gram + bacteria and some gram – bacteria
- Proteus, E.Coli, Klebsiella (PECK)
❖ Drug class - Cephalexin, cefradine
⮚ Amoxicillin: Broad spectrum PCN ⮚ Second Generation
Trade names: Amoxil, Amoclav - Same as 1st
Dosage: Adult - PO 250-500 mg q 8H - H. influenzae, enterobacter Aerogenes, Neisseria
Child - PO 20-40 mg/kg/d in 3 (HENPECK)
divided doses - Cefaclor, cefuroxime
⮚ Dicloxacillin: Penicillinase resistant PCN ⮚ Third Generation
Trade names: Dynapen, Dycill - Same as 1st and 2nd but less effective vs gram + more potent
Dosage: A - PO: 125-500 mg q6H vs gram – bacteria
C - PO: 12.5-25 mg/kg/d q6H - Pseudomonas A., serratia (HENPECKS)
- Cefotaxime, ceftazidime, ceftriaxone
MODE OF ACTION AND INDICATIONS ⮚ Fourth Generation
● Primarily bactericidal - Still in dev’t
● inhibition of the enzyme in cell wall synthesis - Active against gram + and gram – and P. aeroginosa
● Indicated for the treatment of respiratory tract infections, - Cefipime
UTI’s, otitis media, treatment of Staph. Aureus infection
DRUG IN FOCUS
SIDE EFFECTS AND ADVERSE REACTIONS
❖ Drug class
● Hypersensitivity, thrombophlebitis ⮚ Cefazolin: 1st generation Cephalosporin
● Superinfection,electrolyte imbalance Trade names: Ancef
● other common GI disturbances ⮚ Cefaclor: 2nd generation Cephalosporin
Trade names: Ceclor
PRECAUTIONS AND CONTRAINDICATIONS MODE OF ACTIONS AND INDICATIONS
● Inhibits cell wall synthesis
● nursing moms ● Cefazolin – to treat bone and joint infxns, genital infxns and
● with asthma endocarditis
● renal impairment ● Cefaclor – to treat ear infxns, ampi resistant strains
● h/x of hypersensitivity to PCN and cephalosporin ● Both – to treat urinary, respiratory and skin infections

DRUG – LAB – FOOD INTERACTIONS SIDE EFFECTS AND ADVERSE REACTIONS

● broad spectrum penicillins may decrease OC effectiveness ● hypersensitivity and superinfection

● Increase effect with ASA, probenecid ● common GI disturbances
● decrease effects with tetracycline and erythromycin ● alterations in blood clotting with large doses
● may inactivate aminoglycosides ● allergic reactions, electrolyte imb.
● may decrease effect with acidic or fruit juices ● nephrotoxicity with a preexisting renal d/o

NURSING RESPONSIBILITIES PRECAUTIONS AND C/I:

✔ assess for any type of allergy to PCN or cephalosporins
✔ check labs liver fxn test, AST, ALT
✔ Culture and sensitivity testing (C&S)
✔ S/S of superinfection, anal or genital discharge with
long-term therapy
✔ Have epinephrine ready for severe reactions
✔ Admin oral form on empty stomach with a full glass of water
✔ Avoid oral PCNs with milk, fruit juices, soft drinks
✔ If GI disturbances occur, may give small frequent meals to
ensure adequate nutrition
✔ Report other S/S of S/E and ADR
✔ Advise to take full course regardless if feeling better.
2. CEPHALOSPORINS
● pregnancy and lactation
● hepatic or renal impairment
● hypersensitivity to cephalosporins and PCN’s
DRUG – LAB – FOOD INTERACTIONS
● increase effect with probenecid
● increase toxicity with loop diuretics, aminoglycs, colistin,
vancomycin
● dec effect with tetra and eryth
● alcohol may elicit disulfiram like reaction
NURSING RESPONSIBILITIES

Background ● screen for known allergies to drug and components

- fungus named Cephalosporium acremonium ● hx of renal ds and current preg and lactation status
- discovered in seawater at a sewer outlet of the coast of ● C&S at site of infection
Sardinia in 1948 ● note respi status and renal fxn tests
- introduced in 1960’s ● ensure that pt receives full course of antibx tx
8
 ● small frequent meals as tolerated ● give on empty stomach unless with extreme GI disturbances
● monitor for signs of superinfection ● give with full glass water and not fruit juice
● advise to ingest buttermilk or yogurt ● instruct to take full course of therapy and report for S/S of
S/E and ADR’s
CAUTION
4. TETRACYCLINES
PCN <> CEPHALOSPORIN
BACKGROUND
3. MACROLIDES
● 1st broad spectrum antibiotic effective against gram + and –
BACKGROUND bacteria and other organisms (e.g. mycobacteria, rickettsiae,
spirochetes, chlamydiae)
● include Azithromycin ● inhibit bacterial protein synthesis and bacteriostatic also
used for severe acne vulgaris
Clarithromycin
DRUG IN FOCUS
Erythromycin
❖ Drug class
● inhibit protein synthesis by attaching to 50S ribosome ⮚ Doxycline: antibacterial tetracycline
● broad spectrum antibiotics Trade names: Doryx, Adoxa
● used to treat mild to moderate infxns of respi tract, sinuses, Dosage: Systemic Infxns (infections?):
GI, skin and soft tissue, STD’S Adult - PO 100mg q12, IV: 100-200 mg q
24H
DRUG IN FOCUS Child (>8y.o.) - PO: 4.4 mg/kg/d in 1-2 divided
dose
❖ Drug class IV – 4.4 mg/kg/d OD or BID
⮚ Azithromycin: antibacterial macrolide MOA AND INDICATIONS
Trade names: Zithromax ● 1st broad spectrum antibx effective against gram + and –
Dosage: Adult - PO 250-500 mg/d bacteria and other organisms e.g. mycobacteria, rickettsiae,
Child - PO 20-40 mg/kg/d spirochetes, chlamydiae
IV – 500mg /d ● inhibit bacterial protein synthesis and
MOA AND INDICATIONS ● bacteriostatic
● proved to be a good alternative to those allergic to PCN
● inhibit protein synthesis by attaching to the 50S Ribosome S/E AND ADR’S
● to treat gram + and some gram – organisms; respiratory
infxns, gonorrhea, skin infections ● GI disturbances
● fatal hepatotoxicity has been reported
S/E AND ADR’S ● skeletal effects involve damage to teeth and bones
● photosensitivity and rash
● General GI disturbances ● hypersensitivity
● hypersensitivity reactions, tinnitus ● superinfections
● superinfections, hearing loss
● hepatotoxicity PRECAUTIONS AND C/I

PRECAUTIONS AND C/I ● known allergies to drug

● use in young children
● cautious use with liver d/o ● hepatic and renal dysfunction
● pregnancy and lactation ● pregnancy and lactation
● hypersensitive to macrolides
DRUG – LAB – FOOD INTERACTIONS
DRUG – LAB – FOOD INTERACTIONS
● antacids and Fe containing drugs may prevent absorption of
● can ^ serum levels of theophylline, carbamazepine,digoxin tetracyc from GI tract
warfarin ● can reduce effect of PCN’s if taken concurrently
● decreased effect with PCN and clindamycin ● Oral contraceptives effectivity may be reduced
● cycloserine can also increase serum resulting to increased
renal toxicity NURSING RESPONSIBILITIES
● food decreases absorption
● sensitive to gastric contents ● obtain hx of dietary intake and drugs client currently takes
● may give on empty stomach to increase absorption
NURSING RESPONSIBILITIES ● lab values monitored
● monitor V/S and UO
● assess V/S and UO ● instruct to store out of light and extreme heat
● check liver fxn tests ● check expiry date
● C&S before therapy ● may cause teratogenic effect
● monitor V/S periodically ● kids < 8yo not to take tetracyclines
9
5. AMINOGLYCOSIDES Dosage: Adult - PO 250 mg q 12h
● Gentamicin (Garamycin) IV – 200mg q 12h, infused over 60 min.
● Amikacin (Amikin)
● Neomycin (Mycifradin) MOA AND INDICATIONS
● Treatment of respiratory, dermatological, urinary tract, ear,
DRUG IN FOCUS eye, bone, and joint infections; treatment after anthrax
exposure, typhoid fever
❖ Drug class
⮚ Garamycin: antibacterial aminoglycosides ● Interferes with DNA replication in susceptible gram-negative
Trade names: Gentamicin (Garamycin) bacteria, preventing cell reproduction
Dosage:
Adult:
IM; 3 mg/kg/dl in 3-4 divided doses S/E AND ADR’S
IV; 3-5 mg/kg/dl in 3 divided doses
● Nausea and vomiting, diarrhea, abdominal cramps,
MOA AND INDICATIONS flatulence, headache
● Group of powerful antibiotics used to treat serious infections ● Urticaria, Oral candidiasis, crystalluria, hematuria, seizures
caused by gram- negative aerobic bacilli (Pseudomonas
aeruginosa, E. coli, Proteus species, PRECAUTIONS AND C/I:
Klebsiella-Enterobacter-Serratia group, Citrobacter group
and Staphylococcus species) ● known allergies to drug;
● Bactericidal: they inhibit protein synthesis in susceptible ● pregnant or lactating women
strains of gram-negative bacteria, which in turn leads to loss ● renal dysfunction; seizures
of functional integrity of the bacterial cell membrane, causing
cell death DRUG – LAB – FOOD IINTERACTIONS

S/E AND ADR’S ● Increase effect with probenecid, theophylline, caffeine

● Decrease drug absorption with antacids, iron
● Anorexia, N & V, rash, numbness, visual disturbances
● Oliguria, urticaria, palpitation, superinfections NURSING RESPONSIBILITIES

PRECAUTIONS AND C/I: ● Assess vital signs and intake and urine output
● Assess laboratory results to determine renal function
● known allergies to drug ● Obtain a drug and diet history
● hepatic and renal dysfunction ● Administer ciprofloxacin 1h before meals or 2h after meals
before or after antacids and iron products for absorption.
DRUG – LAB – FOOD INTERACTIONS Give with a full glass of water.
● Check for signs and symptoms of superinfection
● Increased risk of ototoxicity with loop diuretics, ● Monitor serum theophylline levels. Check for symptoms of
methoxyflurane central nervous system stimulation: nervousness, insomnia,
● Increased risk of nephrotoxicity with amphotericin B, anxiety and tachycardia
polymyxin, flurosemide, vancomycin
7. SULFONAMIDES
NURSING RESPONSIBILITIES
BACKGROUND
● lab values monitored especially renal and liver functions
● monitor V/S and UO ● One of the oldest antibacterial agents used to combat
● Check for hearing loss infection
● Monitor signs and symptoms of superinfection (stomatitis, ● Drugs that inhibit folic acid synthesis necessary for the
vaginitis and or genital itching) synthesis of purine and pyrimidines, which are precursors of
RNA and DNA
6. FLUOROQUINOLONES

BACKGROUND
● Sulfasalazine (Azulfidine)
● Relatively new class of antibiotics with a broad spectrum of ● Cotrimoxazole (Septra, Bactrim)
activity. These drugs which are all made synthetically are
associated with relatively mild adverse reactions DRUG IN FOCUS
● Ciprofloxacin (Cipro)
● Norfloxacin (Noroxin) ❖ Drug class
⮚ Antibacterial: sulfonamides
DRUG IN FOCUS Trade names: sulfasalazine (Azulfidine)
Dosage:
❖ Drug class Adult - 3-4g/day PO in evenly divided doses,
⮚ Antibacterial: quinolone, fluoroquinolone then 500 mg PO q.i.d
Trade names: Ciprofloxacin (Cipro)

10
 P – 40-60mg/kg/day PO in four equally divided doses PCN’S

MOA AND INDICATIONS ● Take medication exactly as prescribed for duration

● Should take oral doses with water and avoid other
● Treatment of rheumatoid arthritis, arthritis; ulcerative colitis beverages with the drug
● Blocks PABA, an essential component of folic acid synthesis
in susceptible gram-negative and gram-positive bacteria; two CEPHALOSPORINS
thirds of the oral dose passes into the colon, where the
sufapyridine and aminosalicylic acid carrier split, giving a ● Encourage to report diarrhea, seizures, SOB
local anti-inflammatory agent to the colon
MACROLIDES
S/E AND ADR’S
● Should take drug as prescribed and check for interactions
● Nausea and vomiting with other drugs
● diarrhea, ● Client should know proper dosage
● hepatocellular necrosis
● hematuria TETRACYCLINES
● bone marrow suppression
● Steven –Johnson syndrome ● Advise on measures to address photosensitivity
● Rash ● May last a few minutes to several days
● Photophobia
● fever, chills AMINOGLYCOSIDES

PRECAUTIONS AND C/I - Amikacin, gentamicin

● Educate client on drug, purpose, ADR
● known allergies to drug ● Hearing loss may occur even after complete therapy,
● renal dysfunction ototoxicity, CN VIII (EMERGENT)
● pregnancy and lactation ● Force fluids unless contraindicated
● Report tinnitus, high frequency hearing loss, nausea,
DRUG – LAB – FOOD INTERACTIONS vertigo
● Educate on S/S of superinfection
● Increase hypoglycemic effect with an oral hypoglycemic
drug FLUOROQUINOLONES
● When sulfonamides are taken with cyclosporine, the risk of
nephrotoxicity rises - Norfloxacin, ciprofloxacin
● Measures to avoid photosensitivity
NURSING RESPONSBILITIES ● Educate on S/S that need to be reported
● (cns), irregular heartbeat
● Assess the client’s renal function
● Assess whether the client is hypersensitive to sulfonamides SULFONAMIDES
● Administer sulfonamides with a full glass of water. Extra fluid
intake can prevent crystalluria and kidney stone formation. ● Forced fluids and take with food
● Monitor the client’s intake and output ● Severe hypersensitivity reactions
● Monitor vital signs
● Observe the client for hematologic reaction that may lead to
life-threatening anemias
● Check for signs and symptoms of superinfection BACKGROUND

NURSING CONSIDERATIONS ● Tuberculosis (TB) is caused by the acid fast bacillus

● The most common side effects of antibiotics are nausea,
vomiting and diarrhea.
● Antibiotics should always be taken for the length of time
prescribed.
● All oral antibiotics are absorbed better if taken with at least 6
– 8 ounces of water,
● A therapeutic response to antibiotic treatment includes
disappearance of fever, lethargy, drainage, and redness.
● Each class of antibiotics has specific side effects and drugs
that the agents interact with and must be carefully assessed
and monitored.
● Signs and symptoms of superinfections include: fever,
perineal itching, cough, lethargy, or any unusual discharge.
Mycobacterium tuberculosis and frequently called tubercle
bacillus.
● transmitted by droplet nuclei through sneezing and coughing
– inhaled through the air sacs of the lungs
● if immunity compromised, then this spreads to other organs
via blood and lymphatic system. But if with strong immune
system, phagocytes attack them.
● characterized by anorexia, cough and sputum production,
increased fever, night sweats, weight loss and positive AFB
in sputum.
● increased incidence with racial minorities; immigrants; HIV
increased risk factor b/c TB is often the initial manifestation
DRUGS

SPECIFIC PATIENT TEACHING TIPS ● very effective but takes months to complete
● usually done with combination therapy

11
FIRST LINE OF DRUGS ● treatment of all forms of active TB and usually in combination
with other tuberculostatic drugs
P - Pyrazinamide ● prophylaxis for high risk patients

I – Isoniazid (INH) S/E AND ADR’S

R - Rifampin ● drowsiness, dizziness

● psychotic behavior
E - Ethambutol ● peripheral neuropathy
● nausea, vomiting, anorexia
S – Streptomycin ● rashes, jaundice

SECOND LINE OF DRUGS CONTRAINDICATIONS

A - Aminosalicylic acid and salts (P.A.S. Na) ● acute liver/renal disease

● cautious use with convulsive disorders, psychoses
C - Capreomycin ( Capastat) ● hx with allergic reactions
● alcoholics
C - Cycloserine (Seromycin) ● pregnant or lactating women

E - Ethionamide (Trecator-SC)

SIDE EFFECTS DRUG INTERACTIONS

● PAS: GIT disturbances and hepatotoxicity
● Capreomycin: ototoxicity and nephrotoxicity
● Ethambutol: retrobulbar, neuritis and blindness
● Isoniazid: peripheral neuritis and hepatotoxicity
● Rifampicin: hepatitis
● Streptomycin: hepatotoxicity, ototoxicity, nephrotoxicity and
blood dyscrasias
NURSING CONSIDERATIONS
● Patient education should include the importance of strict
compliance to regimen for improvement of condition or cure.
● Patient should not consume alcohol while taking any of these
medications
● Vitamin B6 is needed to combat peripheral neuritis
associated with isoniazid
● Women on oral contraceptive therapy and taking rifampicin
should be counseled on other forms of birth control because
of the ineffectiveness of oral contraception while on
rifampicin
● Patients must be reminded that they are contagious during
the initial period of the illness and its diagnosis, so they
should make every effort to wash their hands and cover their
mouths when coughing or sneezing
DRUG IN FOCUS:
❖ Drug class
Isoniazid (INH, Nydrazid)
Dosage:
Adult - PO/IM: 5mg/kg/d ; max 300mg/d
Child - PO/IM: 10-20 mg/kg/d; max 300mg/d.
Prophylaxis: 10mg/kg/d
● can increase serum levels of phenytoin
● INH and rifampin can increase hepatotoxicity
● LABS
NURSING MANAGEMENT
● determine hx of TB
● assess and record baseline data necessary for detection of
a/r
● check lab tests prior to and during therapy
● evaluate s/s of peripheral neuropathy
● monitor for hepatic d/fxn.
● monitor for signs of hypersensitivity
● monitor for visual disturbances d/t drug s/e
PATIENT TEACHINGS
● 1hr before meals or 2hrs after
● TAKE DRUG AS PRESCRIBED and encourage to keep all
follow up appointments with AP
● NO alcohol and follow up with AP on other drugs client may
be taking
● Participate with sputum testing
● Report s/s of peripheral neuropathy
● Clients with rifampin may turn urine, feces, saliva, sputum,
sweat and tears red orange. Soft contact lenses may be
permanently stained.
● Ethambutol to be taken in single dose
● Educate on preventing spread of infection esp at initial
period and dx
● Educate on need for rest, sleep habits, edeq nutrition
● Keep drugs away from kids
● Encourage to wear medical alert tag or bracelet

MECHANISM OF ACTION

● Bactericidal FUNGI
● resistance develops when used alone.
● can antagonize Vit. B6 - Infection caused by fungus is MYCOSIS

USES ⮚ Yeasts – single celled fungi that reproduce by budding

12
 ⮚ Molds – multicellular and characterized by long branching ● CNS- headache, dizziness, paresthesias
filaments
ANTIFNGAL DRUGS CONTRAINDICATIONS
- Also called ANTIMYCOTICS
- Used to treat 2 types of fungal infections: ● hypersensitivity
⮚ Superficial – skin and MM ● Cautious use in pregnancy and in clients with liver problems
⮚ Systemic – lung or CNS ● Drug alleRgy, liver and renal failure
● Itroconazole – not for clients with severe cardiac problems
● Voriconaxole – fetal harm

1. Polyenes DRUG INTERACTIONS

- Severe systemic infection
- Histoplasmosis, Cryptococcosis, systemic ● increases PT when taken with warfarin
Candidiasis ● Hypoglycemic reactions with oral sulfonyloreas, phenytoin,
haldol, cyclosporine
DRUG IN FOCUS ● Lipid lowering agents
● Corticosteroids
⮚ Amphotericin ● other nephrotoxics
- given IV ● Digoxin
- S/E: flushing, fever, chills, n&V,
hypotension,paresthesias, thombophlebitis NURSING MANAGEMENT
- HIGHLY TOXIC: nephrotoxic, electrolyte imbalance
2. Azoles ● Assess V/S, CBCs, liver and renal function tests
- candidiasis, histoplasmosis, blastomycosis and tinea ● Assess thoroughly for allergies, previous and current
infections medications
- Available forms: vaginal tablet, cream, ointment and solution ● assess client’s health hx
- ketoconazole 1st effective antifungal drug orally absorbed ● during infusion, check V/S q 15-30 mins or as needed
3. Antimetabolites ● Monitor for ADR reactions while on therapy.
- Flucytosine- used in combination with other ● use clear solutions and no precipitates
drugs(Amphotericin B) ● weigh weekly
- well absorbed from the GI tract
4. Antiprotozoal PATIENT TEACHING
- Atovaquone (Mepron) - for mild to moderate Pneumocystis
carinii pneumonia ● Instruct to take drugs as prescribed
5. Echinocandins (Caspofungin) ● Advice to obtain lab testing as indicated
- candida and aspergisollis infection ● Advice to avoid operating hazardous equipment
- Given IV ● Encourage to report S/E
- Phlebitis at the IV site and increased AST and ALT - ● Females on vaginal antifungal infections should refrain from
common adverse effects. intercourse and until actively resolved.
● some antifungals may take a long duration and to continue
DRUG IN FOCUS therapy even if feeling better
● encourage to wear light and cool clothing and to keep
⮚ Nystatin (Mycostatin) affected areas clean and dry.
- Given orally or topically for CANDIDAD INFECTION
- Oral suspension is common
Dosage:
Systemic Candidiasis
Adult - PO/IV: 400mg/d 1 then
200mg/d for 4wks
Child - PO/IV: 3-6mg/kg/d
Vaginal Candidiasis
Adult - PO: 15omg x I1 dose
SIDE EFFECTS
● Nausea, headache
BACKGROUND
● skin rash
● Anorexia
● Protozoa – single celled organisms that are the smallest and
● Vomiting
simplest members of the animal kingdom
● diarrhea in large doses
● Parasite – any organism that feeds on another living
organism in a way that results in varying degrees of harm to
ADVERSE DRUG REACTIONS
the host organism
● parasitic protozoans – harmful protozoa that live on or in
● Cardiac dysrhythmias
human beings or animals and cause disease in the process
● electrolyte imbalance
● Prevalent in tropics
● nephrotoxic and hepatotoxic,
● common malaria/leishmaniasus/amebiasis
● GI disturbances- diarrhea,

13
 ● Assess history
● Special attention and documentation of malaria
manifestations
● Visual acuity, renal fxn tests, GI status, ECG
4 SPECIES ● Monitor U/O; liver fxn tests
● Oral doses given with food
● Plasmodium vivax ● Give exactly as prescribed
● Plasmodium falcifarum
● Plasmodium malariae PATIENT TEACHING
● Plasmodium ovale
- transmitted by bite of infected female anopheles mosquito ● Educate on need for prophylaxis
- S/S Classic Malaria Paroxysm – chills and rigors ● Educate to report any changes in vision
- fevers up to 104C ● AVOID ALCOHOL
- diaphoresis, extreme fatigue ● Take as prescribed for duration
and prolonged sleep ● Avoid operating hazardous equipment
- repeats periodically in 48-72
hour cycle
- headache, nausea and joint pain
⮚ Bithionol (Actamer) - Effective against flukes
⮚ Diethylcarbamazine (Hetrazan) – Treatment for
nematode-filaria
- drug that destroys or prevents the dev’t of the malaria parasite in ⮚ Mebendazole (Vermox) - Treatment for giant roundworm,
human hosts hookworm, pinworm
- these drugs work against the parasite within the human body
- Often given in combination INDICATION AND MOA

SPECIFIC AGENTS ● act on metabolic pathways that are present in the invading
worm but absent or significantly different in the human host.
● chloroquine (Aralen) ● Treatment of infections by certain susceptible worms.
● hydroxychloroquine (Plaquenil)
● mefloquine (Lariam) C/I AND CAUTIONS
● primaquine (generic)
● pyrimethamine (Daraprim) ● Presence of known allergy to the drugs
● quinine (generic) ● Pregnancy and Lactation
● Renal or hepatic disease
THERAPEUTIC ACTIONS AND INDICATIONS ● Severe diarrhea and malnourishment

● Used to kill plasmodium organisms ADVERSE EFFECTS

● Effective in interrupting plasmodial reproduction of protein
synthesis in RBC stage ● Local effect- abdominal discomfort (diarrhea); pain
● Systemic effect- headache and dizziness; fever, shaking,
CONTRAINDICATIONS AND CAUTIONS hills, and malaise, associated with an immune reaction to the
death of the worms; rash; pruritus; and loss of hair. Changes
● Drug allergy in protein synthesis by the liver (Steven-Johnson syndrome);
● Tinnitus renal failure and severe bone marrow depression
● Pregnancy
● Liver disease and Alcoholism NURSING MANAGEMENT
● lactation
● retinal disease or damage ● Obtain a history of foods client has eaten especially meat
and fish, and how the food was prepared
GENERAL ADVERSE EFFECTS ● Note if any other person in the household has been checked
for helminthes (worms)
● CNS and IMMUNE REACTION– headache, dizziness, fever, ● Assess baseline vital signs and collect a stool specimen
shaking, chills, malaise ● Collect a stool specimen in a clean container
● GI – nausea, vomiting, dyspepsia, anorexia ● Administer the prescribed antihelminics after meals
● HEPATIC Dysfunction ● Report for any side effects.
● DERMATOLOGICAL – rash, pruritus, alopecia
● VISUAL CHANGES PATIENT TEACHING
● Cinchonism – n&v, tinnitus, vertigo
● Thorough hand washing
DRUG – DRUG INTERACTIONS ● Laundering of bed linens, pajamas, and underwear
● Disinfection of toilet facilities at least daily and of bathroom
● Valproic acid – decreased serum levels of valproic acid floors periodically
● Beta blockers – cardiac toxicity ● Proper sanitation and hygiene in food preparation and
storage is essential
NURSING MANAGEMENT

14
 - Phosphodiesterase breaks down cAMP, which is
needed to relax smooth muscles
⮚ Antihistamines - Theophylline is the most common, aminophylline is the
- Two types of histamine blockers: Histamine 1 blockers and parenteral form of theophylline
Histamine 2 blockers C. Anticholinergics
- H2 blockers are used in the treatment of gastric acid - Ipratropium bromide (Atrovent) is only agent used for
disorders such as ulcers treatment of COPD
- H1 blockers are the agents most people are referring to - Used for maintenance and not for relief of acute
when they use the term antihistamine. bronschospasms
- H1 blockers prevent the harmful effects of histamine. - Work by blocking the bronchoconstrictive effects of
- Used for treatment of seasonal allergic rhinitis, anaphylaxis, acetylcholine
insect reactions, etc. D. Corticosteroids
- beclomethasone, dexamethasone, flunisolide. And
⮚ Non-sedating antihistamines triamcinolone are examples
- Drugs such as loratadine (Claritin) and fexofenadine - Work by stabilizing the membranes of cells that release
(Allegra) harmful bronchoconstricting substances
- Devoid of most sedating effect that most antihistamines have E. Indirect – acting agents
- Non sedating because they avoid the central nervous system - Cromolyn (Nasalcrom) and nedocromil (Tilade)
and work peripherally - Only used prophylactically; used for management of
⮚ Decongestants chronic pulmonary disease
- Consists of adrenergics and corticosteroids - Work by stabilizing the mast cell wall, thereby
- Most are adrenergic drugs such as pseudoephedrine and preventing potentially harmful vasoconstrictive
phenylephrine substances from being released
- The adrenergics work by stimulating engorged and swollen
blood vessels in the sinuses to constrict, which decreases
pressure and allows mucous membranes to drain
⮚ Antitussives
- Antitussives are used to stop or reduce coughing
- Are either opioid or non-opioid Purpose of cancer treatment
- Opioid agents: codeine and hydrocodone
- Non opioid antitussives: benzonatate and dextromethorphan - Prolong survival time or improve quality of life
⮚ Expectorants
- Drugs that aid in expectoration or removal of mucus Cancer Therapies include:
- Work by reducing the viscosity of seretion by thinning them
down 1. Surgery
- Guaifenesin, and terpin hydrate are two most common 2. Radiation
expectorants 3. Chemotherapy
- Their mechanism of action is related to their ability to irritate 4. Hormonal manipulation
the gastrointestinal tract to cause reflex stimulation or 5. Immunotherapy
irritation of the respiratory tract 6. Gene therapy
⮚ Mucolytics 7. Targeted therapy
- Water is the best
- Most common form comes in acetylcysteine Surgery
- Decreases the viscosity of pulmonary mucus and may be
Rationale for cancer treatment
administered by nebulization.
- Not indicated for routine use in bronchial asthma patients
● first method to cure cancer
with mucus accumulation, because it is frequently irritating
● involves the removal of diseased tissue
and may elicit reflex bronchospasm, further impairing the
patient’s respiratory function
Purposes of Cancer Surgery
- Prompt removal of the liquefied secretions is necessary after
use of mucolytic agent
1. Prophylaxis
⮚ Brochodilators and antiasthma
2. Diagnosis (biopsy)
A. Beta agonists
3. Cure
- Work by stimulating adenylate cyclase, which produces
4. Control (Cytoreductive Surgery)
more cAMP and in turn causes relaxation of the smooth
5. Palliation
muscle that surrounds the airways
6. Determination of therapy
- May stimulate alpha and beta receptors, beta 1 and
- effectiveness (“second look”)
beta 2, or just beta 1
7. Reconstructive or rehabilitative surgery
- Beta 2 stimulants are the most specific for the lungs
and have the fewest side effects
Side effects of surgical therapy
B. Xanthines
- Caffeine, theobromine, and theophylline are examples X loss of a specific body part or its function
of xanthines X reduces function
- Work by inhibiting phosphodiesterase X results in major scarring or disfigurement

15
 X Client may be anxious about the chances of surviving the cancer ❖ Chemotherapy is useful in treating cancer because its effects
and may be grieving about a loss of body image or a change in are systemic, providing the opportunity to kill metastatic cancer
lifestyle cells that may have escaped local treatment.
❖ Chemotherapy used along with surgery or radiation is termed
Nursing care of clients undergoing surgical therapy adjuvant therapy.

1. The physical care needs of the client having surgery for cancer are Mechanism of Action
similar to those related to surgery for other reasons.
2. Consider the client’s ability (and the ability of family and significant 1. Chemotherapy has some selectivity for killing cancer cells
others) to cope with the uncertainty of cancer and its treatment and over normal cells.
with the changes in body image and role. 2. This killing effect on cancer cells is related to the ability of
chemotherapy to damage DNA and interfere with cell
division.
3. Thus the tumors most sensitive to chemotherapy are those
are rapidly growing.
4. Chemotherapy drugs usually are given systemically and
exert their cell-damaging (cytotoxic) effects against healthy
cells as well as cancer cells.
5. The normal cells most affected by chemotherapy are those
that divide rapidly, including skin, hair, intestinal tissues,
spermatocytes, and blood-forming cells.

Actions of Chemotherapeutic Drugs:

1. Cell cycle non-specific (CCNS)

- Drugs that act during any phase of the cell cycle
- More effective against large, slowly growing cells
2. Cell cycle specific (CCS)
- Drugs that exert their influence during a specific phase of the
cell cycle
⮚ Gap 0 (G0) – resting phase - Effective against rapidly growing/dividing cells
⮚ Gap 1 (G1) phase
- post mitotic gap Cell cycle nonspecific (CCNS)
- production of enzyme for DNA synthesis
- lasts for 15 to 18 hours - Alkylating drugs
⮚ Synthesis (S) phase - Antitumor/Cytotoxic Antibiotics
- DNA synthesis / DNA will double - Nitrosureas
- lasts for 10 – 20 hours
Cell cycle specific (CCS)
⮚ Gap 2 (G2) phase
- pre-mitotic gap - Antimetabolites
- RNA synthesis for later mitosis - Mitotic Inhibitors
- the post-synthesis phase in which the cell is prepared - Topoisomerase Inhibitors
for mitosis - Antineoplastic enzymes/ topoisomerase inhbitors
- lasts for approximately 3 hours - Vinca alkaloids
⮚ Mitosis (M) phase
- lasts for approximately 1 hour Factors that affect the cancer cells response to chemotherapeutic
- cell division agents

Chemotherapy 1. Doubling time

- The time it takes for the number of cells in a neoplasm to
❖ the treatment of cancer with chemical agents double, with shorter doubling times implying more rapid
❖ chemotherapy is used to cure and to increase survival time growth
2. Growth fraction
Goal of Chemotherapy - The percentage of cells in mitosis at any given time

1. kill all neoplastic cell and produce a total cure Chemotherapy drugs are classified by the specific types of action they
(not achieved, because most agents are only cytotoxic and exert in the cancer cells
not tumoricidal)
2. to control the growth of cancer cells while maintaining the 1. Antimetabolites
best quality of life, with least possible level of discomforts, 2. Antitumor antibiotics
compromise and treatment of adverse effects 3. Alkylating agents
4. Antimitotic agents / Mitotic inhibitors
Rationale for cancer therapy 5. Topoisomerase inhibitors
6. Miscellaneous chemotherapeutic agents
7. Combination chemotherapy
16
Common combination of chemotherapeutic agents ● estramustine (Emcyt)

1. ABVD Nitrosureas
- doxorubicin hydrochloride (Adriamycin)
- bleomycin sulfate (Blenoxane) ● carmustine
- vinblastine sulfate (Velban) ● lomustine
- dacarbazine (DTIC-Dome) ● streptozocin
2. CHOP
- Cyclosphosphamide (Cytoxan) Probable alkylators
- doxorubicin hydrochloride (Adriamycin)
- vincristine sulfate (Oncovin) ● altretamine
- prednisone ● procarbazine
3. CMF (may be referred to as CMFP when prednisone is ● busulfan
included) ● carboplatin
- cyclosphosphamide (Cytoxan) ● cisplatin
- methotrexate (Mexate) ● dacarbazine
- fluorouracil (5-FU) ● oxaliplatin
4. COPP (may be referred to as A-COPP when doxorubicin ● temozolomide
hydrochloride [Adriamycin] is included)
- cylosphosphamide (Cytoxan) Carboplatin (Paraplatin®)
- vincristine sulfate (Oncovin)
- procarbazine hydrochloride (Matulane) ❖ Myelosuppression: thrombocytopenia
- prednisone ❖ GI: Nausea/vomiting= antiemetics
5. CVP ❖ Renal- special dose calculation = AUC
- cyclosphosphamide (Cytoxan) ❖ Hypersensitivity
- vincristine sulfate (Oncovin)
- prednisone Cisplatin (Platinol®)
6. FAC
❖ Nephrotoxicity = monitor Cr, hydration, I & O’s, weights,
- fluorouracil (5-FU)
diuretics, replace K+, Mg++ prn
- doxorubicin hydrochloride (Adriamycin)
❖ GI: nausea/vomiting = antiemetics
- cyclosphosphamide (Cytoxan)
❖ Myelosuppression
7. MOPP
❖ Neurologic
- mechlorethamine hydrochloride (Nitrogen Mustard,
- Peripheral neuropathies
Mustargen)
- Ototoxicity
- vincristine sulfate (Oncovin)
❖ Vesicant potential
- procarbazine hydrochloride (Matulane)
- Prednisone
How to manage extravasation of vesicant antineoplastic drugs:
8. VAC
- vincristine sulfate (Oncovin)
1. stop the infusion immediately, contact the physician, but leave the IV
- dactinomycin (Cosmegen)
catheter in place
- cyclosphosphamide (Cytoxan)
2, aspiration of residual drug or blood from the catheter

3. consult institutional policy/pharmacist regarding the use of antidote,

warm/cold compress application
A. Alkylating Agents
- cross-link DNA, making the two DNA strand bind tightly 4. document the incident properly
together. This tight binding prevents proper DNA and RNA
Cyclophosphamide (Cytoxan®)
synthesis, inhibiting cell division.
- Cell cycle nonspecific (CCNS)
❖ Hemorrhagic cystitis = hydration, take early in day
- Break DNA helix strand, abnormal base pairing
❖ Given orally or intravenously
- Common side effects:
❖ GI: nausea and vomiting
- myelosuppression, hypersensitivity, renal, GI, cutaneous,
❖ Cutaneous: alopecia
secondary malignancies
❖ Myelosuppression
❖ Secondary malignancies
Examples:

MESNA (2-mercaptoethane sulphonate sodium)

Classic alkylators/ nitrogen mustards

- A cytoprotectant/chemoprotectant
● chlorambucil (Leukeran)
- a drug given with high dose cyclophosphamide to inactivate
● cyclophosphamide (Cytoxan)
urotoxic metabolites in the bladder and minimize damage to
● ifosfamide (Ifex)
the kidney.
● mechlorethamine HCl (Mustargen)
● melphalan (Alkeran)
Ifosfamide (Ifex®)
● thiotepa
17
 ❖ Hemorrhagic cystitis = MESNA, hydration, check UA for - floxuridine (FUDR)
blood - fluorouracil (5-FU)
❖ GI: nausea/ vomiting - gemcitabine
❖ Cutaneous: alopecia
❖ Myelosuppression Capecitabine (Xeloda®)
❖ Neurologic = neuro check
❖ Irritant ❖ Oral drug: take on full stomach with plenty of water
❖ GI toxicities: nausea/vomiting, mucositis, diarrhea,
Oxaliplatin (Eloxatin®) hepatotoxicity
❖ Cutaneous: hand and foot syndrome
❖ Neurologic (acute vs. late) - monitor for redness, tingling, numbness
- Peripheral neuropathies ❖ Myelosuppression: anemia
- Cold-induced dysesthesias = avoid cold! ❖ Potential drug interaction with warfarin
❖ GI: nausea/vomiting = antiemetics ❖ Indicated for the treatment of metastatic breast cancer
❖ Myelosuppression
❖ Irritant Cytarabine (Cytosar-U®)
❖ Vesicant potential = central line
❖ Myelosuppression: leukopenia, thrombocytopenia, anemia
B. Antimetabolites ❖ GI: nausea/vomiting, mucositis, diarrhea, hepatotoxicity
● They closely resemble normal metabolites and are “counterfeit” ❖ Cutaneous: rashes, alopecia
metabolites that fool cancer cells into using them in cellular ❖ Treatment for myelocytic, lymphocytic & meningeal leukemia
reaction. Because antimetabolites cannot function as proper & non-Hodgkin’s lymphoma
metabolites, their presence impairs cell divisions. High dose
● Act in S- phase ❖ Keratitis (inflammation of the cornea) = steroid eye drops
● Cell cycle specific drug (CCS) ❖ Neurological-cerebellar = check handwriting, gait
● Interfere with DNA synthesis ❖ Palmar-plantar rash (painless swelling & erythema to painful
● Common side effects: blistering of the patient’s palms and soles)
- Myelosuppression, GI, Cutaneous

Specifically, they inhibit cellular growth by interfering with the synthesis

or actions 3 classes of compounds critical to cellular reproduction: Fluorouracil (5-FU)

⮚ folic ❖ A pyrimidine antagonist

⮚ acidpurines ❖ Myelosuppression
⮚ pyrimidines ❖ GI: nausea / vomiting, mucositis, diarrhea
❖ Cutaneous: alopecia, rashes, dry skin, hyperpigmentation, nail
Mechanism of action changes, photosensitivity= sunscreen!
❖ Irritant= central line for continuous infusion
❖ It will falsely substitute purines, folic acids, and pyrimidines; ❖ Treatment regimens include: palliative treatment for colon, rectum,
or stomach, breast and pancreatic cancer
❖ It will inhibit the critical enzyme, involved in the synthesis or
function of purine, folic acid and pyrimidines. Gemcitibine (Gemzar®)
❖ Thus, they inhibit the synthesis of DNA, RNA and proteins
necessary for cellular reproduction ❖ Myelosuppression: anemia leukopenia, thrombocytopenia
❖ GI: nausea/ vomiting
Examples: ❖ Cutaneous: rash, edema, alopecia
❖ General: flu-like symptoms, transient febrile episodes
Folate antagonists ❖ Structurally related to cytarabine & believes to have superior
antitumor activity than cytarabine
- methotrrexate (MTX) ❖ First line therapy for locally advanced or metastatic cancer of the
- pemetrexed pancreas and treatment of non-small cell lung cancer

Purine antagonist Methotrexate (MTX)

- cladribine ❖ A folic acid antagonist

- allopurinol ❖ GI: nausea/ vomiting, mucositis, diarrhea, hepatotoxicity
- fludarabine (F-AMP) ❖ Cutaneous: rashes, alopecia, photosensitivity
- rasburicase ❖ Others: hypersensitivity, fever/ chills
- mercaptopurine (6-MP) ❖ Treatment for solid tumors such as breast, head & neck, and lung
- pentostatin CA, management of lymphocytic anemia, non-Hodgkins lymphoma
- thioguanine (6-TG) ethotrexate (MTX)
High dose
Pyrimidine antagonists ❖ Avoid folic acid, NSAIDs, Sulfa…during infusion
❖ Renal = hydration to alkalinize urine (pH>7)
- capecitabine ❖ Monitor MTX serum level (500 mg/m2)
- cytarabine (ara-C)

18
 ❖ High levels: requires an antidote known as Leucovorin calcium 3. if pain, erythema, or swelling persists beyond 48°, discuss with the
to “rescue” phycisian for further treatment (surgical or other options)
❖ Neurotoxicity =neuro
D. Hormonal Therapy

❖ Cell cycle nonspecific

❖ Alters the environment and inhibit tumor growth by blocking the
C. Antitumor / Cytotoxic Antibiotics body’s sex hormone receptor.
❖ damage the cell’s DNA and interrupt DNA or ❖ Rationale: sex hormones acts to accelerate the growth of some
ribonucleic acid (RNA) synthesis (by intercalation (the common types of malignant hormone (breast & prostate)
drug is inserted to between the 2 strands of DNA ❖ Common side effects:
molecule) - GI, gynecomastia, fluid / sodium retention, menstrual
❖ Cell cycle nonspecific (CCNS), more active in the irregularity, libido changes
S-phase
❖ Common side effects: Examples:
- Myelosuppression, GI, cutaneous, and other
organ toxicities Female – specific neoplasms (Breast CA)
anastrazole tamoxifen
Examples megestrol toremifene
aminoglutethimide fluoxymesterone
Anthracyclines fulvestrant testolactone
medroxyprogesterone
daunorubicin idarubicin Male – specific neoplasms (Prostate CA)
bicalutamide flutamide
doxorubicin valrubicin nilutamide leuprolide
goserelin estramustine
epirubicin

D.1. Corticosteroids (glucocorticoids)

Other cytotoxic antibiotics - an anti-inflammatory agent that suppress the inflammatory

process that occurs as a result of tumor growth.
bleomycin mitoxantrone - exact MOA is unknown, but it is believed to block the
steroid-specific receptors on the surface of the cell which
dactinomycin pentostatin slows the growth fraction of the tumor and retards its growth.

motomycin plicamycin D.2. Sex Hormones (Estrogen, Androgens)

Bleomycin (Blenoxane®) A. Estrogen preparation

❖ hypersensitivity - diethylstilbestrol (DES, stilbestrol)

❖ test dose (prior to 1st dose) - ethinyl estradiol (Estynyl)
❖ cutaneous: hyperpigmentation, alopecia, - chlorotrianisene (TACE)
❖ photosensitivity - conjugated estrogens (Premarin)
❖ other organ toxicities: pulmonary
❖ lifetime dose limit: 400 units ❖ A palliative treatment used to decrease the progression of
❖ General: fever and chills – acetaminophen prostatic cancer in men and to slow the growth of hormone-
dependent breast CA in women.
Doxorubicin (Adriamycin ®)
❖ It suppress tumor growth and promotes remission of the
❖ myelosuppression cancer for up to 1 year.
❖ GI: nausea/vomiting, mucositis
❖ Cutaneous: alopecia, photosensitivity, radiation recall B. Progestins
❖ Other: Cardiotoxicity - hydroxyprogesterone caproate (Duralutin)
- lifetime dose 550 mg/m2 - medroxyprogesterone acetate (Depo-Provera)
❖ Vesicant - megestrol acetate (Megace)
❖ Liposomal formulation (Doxil®) with less toxicity
- potential for back pain, fever/chills, and hand-foot syndrome ❖ acts by shrinking the cancer cells
❖ ADR: fluid retention, thrombotic (clot) disorders
Treatment of doxorubicin Extravasation
C. Androgens
1. cool the site to patient tolerance for 24 hours
❖ given to treat advanced breast cancer in premenopausal
2. elevate & rest the extremity for 24-48 hours, then have patient women
resumed normal activity as tolerated ❖ it promotes regression of the tumor

19
 Arsenic trioxide, asparaginase, bortezomib, Erwinia asparaginase,
Hydroxyurea, imatinib mesylate, Mitotane, Pegasparagase,
Procarbazine

D. Antiestrogens A. Proteasome Inhibitors

⮚ Tamoxifen (Nolvadex) ⮚ bortezomib (Velcade)

- Used to treat breast cancer tumors that are
estrogen receptor positive
⮚ Raloxifene (Evista)
- A selective estrogen receptor modulator
(SERM), that acts like an antiestrogen to slow
tumor growth. With lesser S/E than tamoxipen
- prevents the breakdown of certain proteins and
transcription factors and inactivate genes and proteins that
help cancer cells survive antineoplastic therapy, thus causing
cancer cell death.
Side effects

D.3. Gonadotropin – Releasing Hormone Analogues fatigue malaise

nausea vomiting
Luteinizing hormone – releasing hormone agonists (LH-RH) diarrhea anorexia
constipation thrombocytopenia
✔ Leuprolide (Lupron) fever anemia
✔ Goserelin (Zoladex) peripheral neuropathy

❖ Suppress the secretion of FSH and LH from the pituitary gland B. Monoclonal Antibodies (Moabs, mAbs) trastuzumab
❖ Initially, there is an increase in testosterone levels is seen (Herceptin)
❖ However, with continued use, the pituitary becomes insensitive
to this stimulation which leads to the reduction in the production - treatment of breast cancer
of androgens and estrogens - blocks the effects of the growth factor protein human
epidermal growth factor 2 (HER 2), which transmits growth
D.4. Antiandrogens signals to the cancer cells.
- can be used alone or as vehicles to deliver drugs, toxins or
- Flutamide (Eulexin) radioactive material to tumor sites.
- Nilutamide (Nilandron)
- Bicalutamide (Casodex) Side effects which occur during the initiall treatment & will subside
after the 1st treatment:
❖ Useful in treating men with hormone-responsive prostate cancer
that has metastasized X fever
❖ Works by binding to androgen receptors and blocking the effects of X chills
dihydrotestosterone on the prostate cancer cells X pain
X weakness
D.5. Aromatase Inhibitors X nausea
X vomiting
❖ In postmenopausal women, the ovaries no longer produce X diarrhea
estrogen, but androgen is converted to estrogen. X headache
❖ Treatment of choice for hormonally sensitive breast cancer in PM X rashes
women who had their ovaries removed. X difficulty breathing

- anastrozole (Arimidex) Asparaginase (Elspar ®)

- letrozole (Femara)
- exemestane (Aromasin) ❖ check order as multiple formulations!
❖ an enzyme that catalyzes the conversion of the amino acid
❖ blocks the peripheral conversion of androgens to estrogen, thus asparagine to aspartic acid & ammonia.
suppressing the postmenopausal synthesis of estrogen and ❖ Cancer cells then cannot synthesize the asparagine which is
slowing tumor growth necessary for DNA synthesis and proteins needed for cell survival

Side effects and ADR

E. Miscellaneous Agents (Antineoplastic Enzymes) X GI: nausea/ vomiting

Hepatotoxicity
❖ Act in various phases (primarily S) X Fever
❖ Inhibit synthesis X Hyperglycemia – pancreatitis
❖ Common side effects: X Hypersensitivity
- myelosuppression, GI, hepatotoxicity
Bortezomib (Velcade®)
Examples:
❖ Important to have 72 hours between doses
❖ Myelosuppression
❖ GI: nausea/ vomiting, diarrhea
20
❖ Others ❖ Act in pre-mitotic phases (G2 and S)
- hypotension ❖ Induce irreversible blockage of cells and interfere with
- Peripheral neuropathy topoisomerase II enzyme reaction
- Blurred vision
❖ Common side effects:
Imatinib mesylate (Gleevec®) - hypersensitivity, Myelosuppression, GI, Hypotension

❖ Take with food & at least 8 oz of water Examples

❖ Edema and fluid retention = monitor weight
❖ GI: irritation, nausea/ vomiting, hepatotoxicity etoposide, teniposide
❖ Myelosuppression: neutropenia, thrombocytopenia
Etoposide (VP-16)
F. Nitrosureas
❖ Cell cycle nonspecific ❖ Myelosuppression
❖ Break DNA helix and inhibit DNA replication ❖ Hypersensitivity
❖ Cross blood-brain barrier ❖ Hypotension (orthostatic)
❖ Common side effects: ❖ GI: nausea/vomiting, anorexia
- Myelosuppression,
- G1: nausea/ vomiting High dose
- Gonadal toxicity
❖ GI: mucositis, diarrhea
Examples: ❖ Drug instability = watch for precipitation!

carmustine, lomustine, streptozocin G.3. Taxanes

Carmustine (BCNU®) ❖ Act in G2 and M phase

❖ Inhibit cell division
❖ Crosses blood-brain barrier ❖ Common side effects:
❖ Myelosuppression… delayed/ double nadir - hypersensitivity, Myelosuppression, Cutaneous,
❖ GI: nausea/ vomiting Neurologic Toxicities
❖ Pulmonary fibrosis
❖ Irritant = may need to: Examples:
- slow down rate
- put in larger volume of fluid Paclitaxel, Docetaxel

G. Plant Alkaloids/ Mitotic Inhibitors Paclitaxel (Taxol®)

✔ Camptothecins
✔ Epipodophyllotoxins ● Hypersensitivity = premedicate with Dexamethasone, Cimetidine,
✔ Taxanes Diphenhydramine
✔ Vinca alkaloids ● Administer with non-PVC bag/tubing, 0.22 micron filter
● Myelosuppression
G.1. Camptothecins/ Topoisomerase 1 inhibitors ● Cutaneous: alopecia
● Neurologic: peripheral neuropathies
❖ Act in S-phase ● Irritant with vesicant potential
❖ Topoisomerase 1 inhibitors
❖ Cause double strand DNA damage Docetaxel (Taxotere®)
❖ Common side effects:
❖ Myelosuppression, Alopecia, Diarrhea ● Administer with non- PVC bag/tubing,
● Myelosuppression
Examples: ● Cutaneous: alopecia
● Neurologic: peripheral neuropathies
irinotecan, topotecan ● Fluid retention

Irinotecan (Camptosar®) G.4. Vinca Alkaloids

❖ Myelosuppression ❖ Act in G2 and M phases

❖ GI: ❖ Block DNA production
- nausea/ vomiting, ❖ Prevent cell division
- cramping/diarrhea ❖ Common side effects
⮚ acute = Atropine - Myelosuppression, Autonomic and Peripheral
⮚ delayed = immodium 4mg initial dose, followed by Neurotoxicity (decrease in muscular strenght, numbness and
2mg q2 hrs (4mg q4hrs at night), until no diarrhea x 12 tingling of fingers & toes)
hrs.
Examples:
G.2. EPIPODOPHYLLOTOXINS / TOPOISOMERASE 2 INHIBITOR vinblastine, vincristine, vinorelbine

21
Vincristine (Oncovin®) - Myelosuppression,
- injection site erythema
● Autonomic neurotoxicity: constipation, impotence
● Peripheral neurotoxicity: numbness, weakness, myalgias Examples
● General: alopecia
● Vesicant - interferon alfa-2a (Referon A®),
● Increased toxicity with doses > 2mg - interferon alfa-2b (Intron A®)

Interleukins

Biotherapy Action:

- The use of agents derived from biologic sources or agents - Stimulate activation of immune cells (T and B cells, NK cells,
that affect biologic responses. LAK cells, tumor-infiltrating lymphocytes).

Principles of the Immune Surveillance Theory Side Effects:

✔ As multiple genetic mutations occur over years, cells may - fever,

transform from normal to malignant - chills,
✔ Cancers cells express antigens on the cell surface - headache,
(tumor-associated antigens) - N/V,
✔ Immune system recognizes the antigens as “non-self” - Myelosuppression,
✔ Immune response can be mounted in defense - cardiac changes,
- diarrhea,
Methods of Biotherapeutic Action -
- capillary leak syndrome.
✔ Enhancing immune response
✔ Altering body’s responses that allow cancer cells to grow Examples:
✔ Increasing vulnerability of cancer cells
✔ Preventing metastasis - aldesleukin (IL-2 Proleukin®),
✔ Altering pathways of transformation of normal cells into - oprelvekin (IL-11, Neumega®).
malignant ones
✔ Enhancing repair of normal cells Hematopoietic Growth Factors
✔ Changing behavior of cancer cells
Action:
Biotherapy Agents
- Stimulates the differentiation, proliferation, maturation, and
Cytokines functioning of hematopoietic cells.

❖ Cytokines are a broad class of protein cell regulators produced Side Effects:
by the immune system
❖ Most cytokines possess multiple effects - bone pain,
❖ Cytokines include - injection site pain,
- Interferons - N/V,
- Interleukins - Other
- Hematopoietic growth factors
Examples:
Cytokines (Interferons)
- Erythropoietin- epoetin alfa (ProCrit®), darbepoetin
Action (Aranesp®)
- G-CSF- filgrastin (Neupogen®), pegfilgrastin (Neulasta TM)
- Antiviral - GM-CSF- sargramostim (Leukine®)
- Antiproliferative - Oprelvekin- IL-11 (Neumega®)
- immunomodulatory
HER 1/ EGFR (Tyrosine Kinase Inhibitor)
Side effects:
Action:
- fever
- chills Inhibition of EGFR-TK leads to inhibition
- headache, of tumor growth and progression and
- N/V, promotion of cell death.
- Diarrhea
- , fatigue, Side Effects:
- depression,
- anorexia, - GI: diarrhea, (loperamide), nausea and vomiting
- confusion,

22
 - Cutaneous: rash, dry skin, prurits, photosensitivity, - Gemtuzumab ozogamicin (Mylotarg®)
paronychial inflammation
- Pulmonary: (interstitial lung disease) rare RADIOISOTOPE CONJUGATES

Example: erlotinib (Tarceva TM) Ibritumomab tiuxetan (Zevalin®)

Monoclonal Antibodies ● Administered in two separates doses

● Premedicate with antiemetics
- Highly specific proteins derived from a single clone of ● Infusion-related hypersensitivity
antibody-producing cells that recognize and bind to only one ● Myelosuppression
tumor associated antigen ● Secondary malignancies
- Actions of unconjugated monoclonal antibodies ● Observe radiation precautions for beta emitter
⮚ Direct effects in producing apoptosis or
programmed cell death Tositumomab 1-131 (Bexxar®)
⮚ Indirect effects by activating host defense
mechanism to mediate antitumor activity ● Single treatment course consisting of two steps
● Infusion related hypersensitivity
Side effects ● Myelosuppression
● Delayed onset hypothyroidism
X Acute infusion-related hypersensitivity reactions. ● Secondary malignancies
X Symptoms range from mild or moderate (fevers, rigors, N/V, ● Observe radiation safety precautions for gamma emitter
headache) to more severe (urticaria, dyspnea, hypotension,
bronchospasm, anaphylaxis). IMMUNE TOXIN CONJUGATES
X Myelosuppression
X Others, dependant on agent used Gemtuzumab ozogamicin (Mylotarg®)

Examples: ● Infusion-related hypersensitivity

● Pre-medicate
- rituximab (Rituxan®), ● Monitor vital signs
- Trastuzumab (Herceptin®), ● Severe Myelosuppression
- cetuximab (Erbitux®). ● Tumor lysis syndrome
- Alemtuzumab (Campath®), ● Mucositis
- bevacizumab (Avastin®) - see antiangiogenic agents. ● Filter
● Protect from light
Rituximab (Rituxan®)
BIOTHERAPY AGENTS
● Infusion-related hypersensitivity
● Myelosuppression ● Cellular therapies
● Tumor lysis syndrome in high risk patients
● Mucocutaneous reactions - Dendritic cells
● HBV reactivation
- Tumor- infiltrating lymphocytes (TILs)
Trastuzumab (Herceptin®)
● Vaccine
● Infusion-related hypersensitivity ● Gene therapy
● Cardiac toxicity
● Diarrhea

Cetuximab (Erbitux®)

● Infusion-related hypersensitivity ANGIOGENESIS

● Rash
● Interstitial lung disease - The growth of new blood vessels within a tumor.
● Administer through a 0.22 micron filter
ANTIANGIOGENIC AGENTS
Conjugated monoclonal antibodies bound to radioisotopes or other
toxins. Action:

Radioisotope conjugates Target the neovasculature of tumors to halt their growth, prevent
tumor spread.
- Ibritumomab tiuxetan (Zevalin®)
Side Effects:
- Tositumomab 1-131 (Bexxar®)
Dependent on agent used.
Immune toxin conjugates
Examples:

23
 - Bevacizumab (anti-VEGF, Avastin®)

- Thalidomide (Thalomid®)

Bevacizumab (Avastin®)

● Infusion-related hypersensitivity
● GI perforation/wound healing complications
● Hypertension
● Bleeding
● Proteinuria
● Arterial thromboembolic events
● Do not administer or mix with dextrose solutions

Thalidomide (Thalomid®) NERVOUS SYSTEM

● Birth defects ● Central Nervous System

● Drowsiness/sedation o Brain
● Constipation o Spinal Cord
● Peripheral neuropathy o Blood Brain Barrier
● Rash ● Peripheral Nervous System
● Peripheral edema o Somatic Nervous System
● Orthostatic hypotension o Autonomic Nervous System
● Appetite increase and/or weight gain ▪ Sympathetic
● Neutropenia ▪ Parasympathetic

Principles of Radioimmunotherapy (RIT) NEURONS

❖ Use of unsealed radionuclide-labeled monoclonal antibodies ● Also known as nerve

❖ The conjugated monoclonal antibodies recognize the cells: convey electrical
tumor-associated antigen impulses
❖ Radioactivity is delivered to tumor cells ● Cell Body: metabolic
❖ Goal: Destroy or inactivate cancer cells while preserving center of the neuron
normal tissue integrity. ● Projections
– Dendrites: bring
Radioimmunotherapy impulses to cell body
– Axon: carries
❖ Radioactive isotopes emit one or more types of radiation impulses away from
the body.
- Alpha particles

- Beta particles

- Gamma rays
NEUROGLIA
❖ Radioactive biologicals should be handled according to
guidelines for the specific isotope used.
- Ibritumomab tiuxetan (Zevalin®) – Beta emitter
- Tositumomabe 1-131 (Bexxar®) – Gamma emitter
ANATOMY AND PHYSIOLOGY
● Also called Glial Cells
● Cells that support, insulate, and protect neurons
● Cannot transport impulses
● Have to ability to reproduce
● CNS Neuroglia
1. Astrocytes: have numerous projections that anchor cells to
capillaries. It helps form the blood brain barrier.
2. Microglia: spider-like cells that clear dead cells and bacteria
in the CNS.
3. Ependymal cells: ciliated cells lining the brain and spinal
cord which help circulate the CSF.
4. Oligodendrytes: provide myelin sheaths for CNS nerve cells.
● PNS Neuroglia
1. Schwann Cells: myelin sheath around nerve fibers in CNS. It
contains neruolemma which is important in fiber
regeneration. It separates therefore has gaps called nodes
Ranvier which allows impulses to “jump”
2. Satellite Cells: protective, cushioning cells.

24
NERVE IMPULSE TRANSMISSION
● Electrochemical process
o Electrical: within neuron’s membrane
o Chemical: from one neuron to another
● Irritability: the ability to respond to a stimulus and
convert it into a nerve impulse
● Conductivity: the ability to transmit impulse.
IRRITABILITY
● Stimulus: opens sodium gates. It can be light, sound, pressure or
neurotransmitter from another neuron.
● Sodium enters cell via diffusion: DEPOLARIZATION.
● This initiates an ACTION POTENTIAL or NERVE IMPULSE, which
is propagated throughout the entire axon.
● Sodium gates become impermeable. Potassium goes out of the
cell restoring negative charge inside of cell: REPOLARIZATION.
● Sodium-Potassium Pump later returns the Na outside cells and K
inside cell.
● ACTION POTENTIAL
CONDUCTIVITY
● From one neuron to another
● Action Potential reaches axon terminal: vesicles release
RETICULAR ACTIVATING SYSTEM
neurotransmitters
● Neurotransmitters diffuse across synapse and travel to the dendrite
of the receiving neuron.
● Myelin Sheath: allows for faster conduction
● Nodes of Ranvier
NEUROTRANSMITTERS
SPINAL CORD
● Acetylcholine: communicates between nerves and muscles. Also
● is connected to the brain and extends from the foramen magnum to
important in memory and learning.
● Amines
● contains 31 pairs of spinal nerve with each nerve having both a
o Epinephrine
o Norepinephrine: primary neurotransmitter of SNS, affects mood
● primarily sends impulses to and from the brain.
o Serotonin: involved in sleep, moods, emotions
o Dopamine: needed in motor control and fine muscle
BLOOD BRAIN BARRIER
movements. It also affects emotions and moods.
● Gamma-aminobutyric Acid (GABA): inhibitory, reduces
aggression and anxiety, muscle relaxing properties.
BRAIN
● CEREBRUM
o The highest functional area of the brain.
o
Interprets sensation.
o
Seat of intellect, language, and memory
o
Controls consciousness and voluntary motor activities.
o
If depressed: drowsiness, decreased sensation, alertness, and
concentration.
o If stimulated: greater ability to concentrate and receive
sensation.
● CEREBELLUM
o In charge of movement and coordination
o If depressed: causes dizziness
● BRAINSTEM
o Includes the Midbrain, Pons and medulla oblongata
o Midbrain: serves as a major relay center.
o Pons: plays an essential part in respiration
o Medulla Oblongata: center for many vital functions and reflexes.
It controls respirations, vasomotor activities, and cardiac
arteries. Controls vomiting, coughing, and swallowing reflexes.
● THALAMUS
o Located between the two cerebral spheres
o Serves as a major relay center for all sensory information except
sound
o Key area in sensing pain and pain relief.
● HYPOTHALAMUS
o regulates the ANS.
o Controls heart rate, blood pressure, water and electrolyte
balance, appetite, body temperature, intestinal motility, and body
weight.
o Plays a major part in metabolism.
● LIMBIC SYSTEM
o has high levels of epinephrine, norepinephrine, and serotonin.
o is believed to affect our emotions and impulses such as anger,
motivation, stress, pleasure, etc.
o has been a key in controlling mood disorders such as
depression, mania, and anxiety.
o in charge of our sleep-wake cycle.
o contains large amounts of serotonin, the chief neurotransmitter
of sleeping.
o Increased serotonin induces sleep
o decreased serotonin induces wakefulness.
o key area in alleviating sleep disorders.
upper lumbar region of vertebral column.
dorsal root (for sensation) and a ventral root (for motor).
● functioning boundary of the CNS to keep proteins and toxins out.
● serves as challenge as it also keeps many drugs out.
● Mostly because brain has the most impermeable capillaries
● Astrocyte projections contribute to the barrier
● Water, glucose, essential amino acids can pass easily through the
barrier
25
PERIPHERAL NERVOUS SYSTEM
● Somatic Nervous System – in charge of voluntary muscle
movement
● Autonomic Nervous System – in charge of involuntary muscle
movement
AUTONOMIC NERVOUS SYSTEM
● SYMPATHETIC
o Also called as the Adrenergic system
o Thoracolumbar lumbar B (from T1-L2)
o Used to handle stress for short periods of time
o Main neurotransmitter: Norepinephrine
● PARASYMPATHETIC
o also called the Craniosacral division
o originate from CN III, VIII, IX,X and sacral segments S2-S4.
o associated with conservation and restoration or energy stores.
o Main neurotransmitter: Acetylcholine
o 2 Types of Receptors – Muscarinic and Nicotinic
▪ Muscarinic receptors - affect pupil constriction, increased GI
motility and secretions and increased urinary bladder
contraction.
▪ Nicotinic receptors on muscle contraction, autonomic
responses and release of epinephrine and norepinephrine
from the adrenal medulla.
DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM
ADRENERGIC AGONISTS
● Sympathomimetics
● Alpha and Beta Adrenergic
o Act on both alpha and beta receptors of the Adrenergic System.
o Some of these Drugs are preparation of catecholamines.
o Epinephrine- for treatment of shock
o Norepinephrine - for shock and cardiac arrests
o Dopamine – choice for treatment of shock because it increases
blood flow to kidneys
● Alpha 1 Agonist – Phenylephrine
o Vasoconstriction with little or no effect on the heart.
o Used to treat colds and allergies.
o Parentally to treat shock, shock like states
o Topically- to treat allergic rhinitis and relieve symptoms of otitis
media
o Opthalmically – to dilate pupils for examination
● Alpha 2 – Clonidine (Catapres)
o Controls release of Norepinephrine from CNS
o To treat hypertension
o To treat cancer pain with opiates
o Ease withdrawal from opiates
o Associated with bad dreams, sedation, drowsiness
o Caution in patients with extreme hypotension, CHF, and
bradycardia
● Beta 1 – Isoproteronol HCI
o Activates both beta 1 and beta 2
o For asthma
o Aside from bronchodilation it also causes
o tachycardia
o Antagonize effect of beta blockers
● Beta 2 – Albuterol Sulfate
o Bronchodilation without tachycardia
o For asthma
▪ Terbutaline sulfate
– for short term treatment of asthma
– arrest preterm labor
● Contraindication/ Caution for Adrenergics
o Pheochromocytoma – a condition where there is an
overstimulation of the adrenal medulla.
o Tachyarrhythmias and Ventricular fibrillation –increase in HR
and O2 consumption by these drugs can exacerbate the
condition
o Hypovolemia where treatment is fluid replacement
o Halogenated Hydrocarbons (general anesthetics)– because it
sensitizes myocardium to catecholamines
o Caution with any kind of peripheral vascular disease
o (Raynaud’s Ds) - exacerbates systemic vasoconstriction.
● Adverse Effects
o General: Headache, sweating, piloerection
o SNS: arrhythmias, palpitations, angina, dyspnea
o GI: N/V
● Drug Interaction
o Increased effect with MAOIS’s
o Decreased effect with adrenergic blockers
● Nursing Responsibilities
o Monitor V/S especially BP and heart rate
o Report S/E such as tachycardia. Palpitations, increased BP
o Monitor for urinary output and urinary retention
o Monitor IV site. Infiltration of these drugs may cause tissue
necrosis of tissues.
o Monitor blood sugar.
o Antidote: Phentolamine Mesylate (Regitine)
ADRENERGIC ANTAGONISTS
● Adrenergic Blocking Agents
o Blocks effects of adrenergic neurotransmitters by either
▪ Directly, by occupying the alpha or beta receptors or
26
 ▪ Indirectly, by inhibiting release of epinephrine and
norepinephrine
● Non-Selective Alpha Blocker- Phentolamine (Regitine)
o Mechanism of Action
▪ Blocks both alpha 1 and alpha 2 receptors
▪ Blocks alpha 1- vasodilation – lowers BP
▪ Blocks alpha 2 – prevents feedback control of
norepinephrine release which may cause reflex tachycardia
o Therapeutic Effect
▪ Prevent or control hypertensive episodes
▪ Reverses vasoconstrictive effect of Norepinephrine and
Dopamine
o Contraindicated in Allergies, CAD, MI
o Caution in pregnancy, lactation, gastritis, and peptic ulcer
o Adverse Effects
▪ Hypotensive episodes
▪ Nausea
▪ Flushing
▪ Tachycardia
▪ MI
▪ Arrhythmias
o Drug-Drug Interaction
▪ Decreased therapeutic effect if given with
sympathomimetics
▪ Alcohol can further cause vasodilation
o Nursing Responsibilities
▪ Monitor HR and BP
▪ For epinephrine extravasation inject Phentolamine
directly into area of extravasation
● Selective Alpha 1 Blocker – Doxazosin (Cardura)
o Therapeutic Actions and Indications
▪ Causes vasodilation thus decreasing blood pressure –
treatment for hypertension
▪ Also used to treat BPH
o Contraindications and Cautions
▪ Presence of allergies and lactation
▪ Caution in CHF, Renal Failure, Hepatic impairment,
pregnancy
o Adverse Effects
▪ CNS: Weakness, fatigue, drowsiness, depression
▪ GI: N/V, abdominal pain and diarrhea
▪ CV: arrhythmias, hypotension, edema CHF and angina.
▪ General: flushing, rhinitis, reddened eyes, nasal
congestion, priapism.
o Drug-Drug- interaction
▪ Increased hypotensive effects if used with other
antihypertensives
o Nursing Responsibilities
▪ Monitor BP, pulse rhythm, and cardiac output.
▪ Safety precautions for CNS effects and orthostatic
hypotension
▪ Small frequent meals if there is GI upset
▪ Supportive care and comfort measures
● Non-Selective Beta Blocker – Propanolol (Inderal)
o Blocks beta 1 causing the following effects
▪ Decreases heart workload, thus decreasing oxygen
consumption, dysrrhythmias, and heart rate
▪ Blocks beta receptors in the juxtaglomerular apparatus of
nephron, thus decreasing renin release and BP
o Blocks Beta 2 causing the following effects
▪ Causes bronchial tubes to constrict
▪ Uterine contraction
o Indication
▪ chronic angina pectoris, essential hypertension, mild
tachycardia, MI
o Contraindications
▪ Allergy, bradycardia, heart block, asthma, shock, CHF,
bronchospasm, COPD, acute asthma, pregnancy, and
lactation
o Caution in
▪ DM (can block s/sx of hypoglycemia or hyperglycemia)
▪ Thyrotoxicosis
▪ Liver dysfunction
o Adverse Effects
▪ Cardiac arrhythmias, flushing, reflex tachycardia,
bradycardia, dizziness, hypotension, headache
o Drug-Drug- interaction
▪ Paradoxical Hypertension if given with Clonidine
▪ Decreased antihypertensive effect if given with NSAIDS
▪ Ergot Alkaloids- possibility of peripheral ischemia
o Nursing Responsibilities
▪ Don’t’ stop drug abruptly. Taper for 2 weeks
▪ Monitor blood sugar levels
▪ Safety and comfort measures
▪ Instruct client not take any OTC drugs
▪ Monitor for bronchocostriction
▪ Monitor V/S especially heart rate and BP
● Beta 1 Selective Blocker Metoprolol (Lopressor)
o Blocks beta 1 only
o Effects on Beta 2 are least likely to occur
CHOLINERGIC AGENTS
● Also called as Parasympathomimetics.
● 2 Types
o Direct acting – mimics acetylcholine
o Indirect Acting - inhibits acetylcholinesterase, an enzyme that
inhibits breakdown of acetylcholine
● Direct Acting Cholinergic Agonists
o Mechanism of action
▪ Mimics effect of Acetylcholine and parasympathetic
stimulation
o Therapeutic Actions and Indications
▪ Bethanechol – relaxes bladder sphincter to improve bladder
emptying
▪ Cevimeline- to increase secretions in the mouth and GIT;
Sjogrens syndrome
▪ Carbachol and Pilocarpine to induce miosis
o Contraindications and Cautions
▪ Any condition that may have an undesirable effects with
PNS stimulation. Bradycardia, hypotension, CAD,
vasomotor instability, Asthma, GI obstruction
o Adverse Effects
▪ GI: N/V, cramps, diarrhea, increased salivation, involuntary
defecation
▪ CV: bradycardia, heart block, hypotension, cardiac arrest
▪ GU: urinary urgency
▪ General: flushing, increased sweating
o Drug-Drug Interaction
▪ May have increased risk of cholinergic effect if combined
with acetylcholinesterase inhibitors
● Indirect Acting Cholinergic Agonists
o Mechanism of action
▪ Reacts with acetylcholinesterase to prevent breakdown of
acetylcholine
o Therapeutic Actions and Indications
▪ MYASTHENIA GRAVIS – autoimmune disease that make
antibodies against ACh receptors. It is characterized by
muscle weakness and paralysis, including the diaphragm.
27
 ▪ Edrophonium (Tensilon)- used as a diagnostic tool. Very
short action (10-20 min)
▪ Neostigmine (Prostigmine) – doesn’t cross blood brain
barrier but strong at neuromuscular junction. Short action
(2-4 hrs)
▪ Pyridostigmine (Mestinon) – similar to Neostigmine but has
loner action (3-6 hrs)
▪ Ambenonium (Mytelase) – similar to Pyridostigmine but
cannot be taken if patient is unable to swallow. Available
only in oral form
▪ Alzheimer’s Disease – progressive disorder involving
neural degeneration, loss of memory and ability to carry
ADL’s
▪ There is progressive loss of Ach-producing neurons and
their target neurons.
▪ Tacrine (Cognex)
▪ Galantamine (Razadyne)
▪ Rivastigmine (Exelon)
▪ Donepezil (Aricept) – once a day dosing
▪ These drugs cross blood-brain barrier
o Contraindications
▪ Allergy to drugs
▪ Bradycardia
▪ Intestinal or Urinary Obstruction
▪ Pregnancy – can stimulate labor
▪ Lactation
o Caution- asthma, CAD, PUD, Arrhythmias, epilepsy, or
parkinsonism
o Adverse Effects
▪ Associated with stimulation of PNS
o Drug-Drug Interaction
▪ Increased risk of GI bleeding with NSAID’s
▪ Can double the effect of Theophylline
o Nursing Responsibilities
▪ Give slow IVTT
▪ Have Atropine Sulfate on standby
▪ Discontinue drug if excessive salivation, diarrhea,
▪ emesis or frequent urination becomes a problem.
▪ Give with meals
▪ Inform physician in patient has to undergo surgery.
▪ Safety and comfort measures
● Cholinergic Blocking Agent: Atropine Sulfate
o Mechanism of action
▪ Blocks acetylcholine receptors at the Muscarinic cholinergic
receptor sites
o Therapeutic Actions and Indications
▪ To depress salivation and bronchial secretions
▪ Bronchial dilation
▪ Inhibit vagal responses in the heart
▪ Relax GIT and GUT
▪ Inhibit GI secretions
▪ To cause mydriasis
▪ Cycloplegia – inhibition of the ability of lens to accommodate
near vision
o Contraindications
▪ With any condition that can be exacerbated by blocking the
PNS: Glaucoma, stenosing peptic ulcer, intestinal atony,
paralytic ileus, GI obstruction, BPH and bladder atony,
cardiac, arrhythmias, tachycardia, myocardial ischemia,
impaired, kidney, liver function.
o Caution in
▪ lactation, HPN, spasticity and brain damage.
o Adverse Effects
▪ Caused by systemic blockade of cholinergic system
▪ CNS: blurred vision, pupil dilation, photophobia,
cyclolpegia, increased IOP, weakness, dizziness, insomnia,
mental confusion.
▪ GI: dry mouth, nausea, heartburn, constipation, paralytic
ileus
▪ CV: Tachycardia, palpitations
▪ GU: Urinary hesitancy and retention
▪ Integ: decreased sweating
▪ Suppression of lactation
o Drug-Drug Interaction
▪ Anticholinergic effect increases with antihistamines,
antiparkinson drugs, MAOI’s, TCA’s
o Nursing Responsibilities
▪ Ensure adequate hydration and temperature control
▪ Provide comfort measures
▪ Candy for dry mouth, dark room for photosensitivity,
small, frequent meals to alleviate GI discomfort, bowel
program to help constipation, safety precautions
▪ Monitor BP, ECG, urine output, cardiac output
DRUGS AFFECTING THE CENTRAL NERVOUS SYSTEM
ANXIOLYTIC AND HYPNOTIC AGENTS
● CNS Depressants
● Anxiety: feeling of apprehension, tension, nervousness, and fear
● Sedation – loss of awareness or reaction to environmental stimuli
● Hypnosis - drowsiness causing sleep
● Benzodiazepines Diazepam (Valium)
o Advantages:
▪ Lower fatality rates with acute toxicity and overdose
▪ Lower potential for abuse
▪ More favorable side effects and adverse effects profile
▪ Fewer potentially serious drug interactions
o Mechanism of action
▪ Acts in the Limbic system and the RAS to make GABA more
effective
o Indications:
▪ Anxiety disorders,
▪ alcohol withdrawal,
▪ hyperexcitability and agitation,
▪ preoperative relief of anxiety and tension
▪ to aid in balanced anesthesia
28
 ▪ For status epilepticus
o Contraindications
▪ Allergies to benzodiazepines, psychosis, acute, narrow angle
glaucoma, shock, coma, acute alcoholic intoxication,
pregnancy, and lactation.
o Caution in elderly or debilitated clients
o Adverse Effects
▪ CNS: sedation, drowsiness, depression, lethargy, blurred
vision.
▪ GI: dry mouth, constipation, N/V, elevated liver enzymes may
result
▪ CV: hypo/hypertension, arrhythmias, palpitations, respiratory
difficulties
▪ Hema: blood dyscrasias, anemia
▪ GU: urinary retention and hesitancy, loss of libido, changes
in sexual functioning
▪ Phlebitis and thrombosis at injection site
o Drug-Drug- interaction
▪ Alcohol and other CNS depressants should be avoided
▪ Increased effect if given with cimetidine, oral contraceptives
or disulfram
▪ Decreased effect with theophylline or ranitidine
o Nursing Responsibilities
▪ Do not administer intra-arterially because serious
arteriospasm and gangrene may occur. Monitor injection site
▪ Do not mix IV solution with other drugs.
▪ Use oral form as much as possible
▪ If to be given IV, give slow IVTT.
▪ Arrange to reduce dosage of narcotics to decrease potential
effects and sedation.
▪ Maintain bed rest for at least 3 hours after receiving
parenteral dose.
▪ Taper dosage when discontinuing. May cause seizures
▪ Provide comfort measures
o Antidote – Flumazenil
● Barbiturates
o Once drug of choice
o Likelihood of sedation and adverse effects were higher.
o Higher risk for addiction and dependence
o Classifications
▪ Long-acting – to control seizure and epilepsy
– Ex. Phenobarbital
▪ Intermediate Acting – Useful as sleep sustainers for
maintaining long periods of sleep
– Ex. Aminobarbital (Amytal)
▪ Short-acting- used to induce sleep for those having difficulty
sleeping
– Ex. Secobarbital (Seconal)
▪ Ultrashort acting – used as anesthesia
– Ex. Thiopental sodium (Penthotal)
o Mechanism of action
▪ Inhibit neuronal impulse conduction in the ascending RAS,
depress the cerebral cortex, alter cerebellar function and
depress motor output.
o Indications
▪ Indicated for relief of signs and symptoms of anxiety
▪ For sedation, insomnia, and seizures.
▪ Parenteral - for acute manic reactions and seizures.
o Contraindications
▪ Allergies to barbiturates and other hypnotic drugs
▪ Latent or manifest porphyria
▪ Hepatic or renal impairment
▪ Respiratory Distress
▪ Pregnancy (Teratogenic)
o Caution
▪ Patients with acute or chronic pain
▪ Seizure disorders
▪ Chronic hepatic, renal respiratory disorders
▪ Breastfeeding
o Adverse Effects
▪ CNS: drowsiness, somnolence, lethargy, ataxia, vertigo,
▪ paradoxical excitement, anxiety and hallucinations
▪ GI: N/V, constipation, diarrhea, epigastic pain
▪ CV: bradycardia, hypotension, syncope
▪ Respi: respiratory depression, hypoventilation,
▪ laryngospasm
▪ Hypersensitivity: rash, serum sickness, Steven-Johnson
syndrome
o Drug-Drug Interaction
▪ Alcohol and other depressants – increased CNS
depression
▪ MAOIs – increased serum levels
▪ Decreased effectiveness of oral anticoagulants, digoxin,
▪ TCAs, corticosteroids, valproic acid, anticonvulsants,
acetaminophen
o Nursing Responsibilities
▪ Do not administer intra-arterially because serious
arteriospasm and gangrene may occur. Monitor injection site
▪ Do not mix IV solution with other drugs.
▪ Use oral form as much as possible
▪ If to be given IV, give slow IVTT.
▪ Arrange to reduce dosage of narcotics to decrease potential
effects and sedation.
▪ Maintain bed rest for at least 3 hours after receiving
parenteral dose.
▪ Taper dosage when discontinuing. May cause seizures
▪ Provide comfort measures
ANTIPARKINSON DRUGS
● progressive chronic neurological disorder
● Damage of neurons to basal ganglia
● Substantia nigra – dopamine rich area of the brain that
supplies neurotransmitters to the corpus striatum
● Corpus striatum and substantia nigra - maintains muscle
tone, coordination
● Extrapyramidal system – neural network in the brain
involved in the coordination of unconscious muscle
movement
● Substantia nigra inhibits the corpus striatum by supplying it
with dopamine. Corpus striatum inhibits substantia nigra by
supplying it with gamma-aminobutyric acid. They inhibit
each other in a balanced manner.
● Acetylcholine, an excitatory neurotransmitter is secreted in
the area of the corpus striatum to coordinate intentional
movements of the body.
● With the degeneration of the substantia nigra there is not
enough dopamine to counteract acetylcholine, causing the
excitatory cells to dominate.
● Anticholinergics
o to reduce rigidity and tremors
o Have more affinity for CNS than PNS
▪ Benztropine (Cogentin)
▪ Biperidine (Akineton)
▪ Diphenhydramine (Benadryl) – antihistamine with
anticholinergic properties, used for patients who cannot
tolerate more potent drugs and during the early phase of
the disease
29
 ▪ Procyclidine (Kemadrin) ● Also knows as neuroleptics
▪ Trihexyphenidyl (Artane) ● Psychotics: “loss of contact with reality”
o blocks the action of acetylcholine in CNS to help restore – e.g. hallucinations, delusions, paranoia, speech
dopamine-acetylcholine balance. abnormalities and affective problems
o To control EPS and drug induced pseudoparkinsonism ● Schizophrenia – most common type of psychosis
o Decreases rigidity, tremors. Peripheral effect include – Usually occur during adolescence and early adulthood
diminished drooling. ● Excess of the neurotransmitters Dopamine and Serotonin
● Dopaminergics ● 2 Classifications of Symptoms
o Dopamine – cannot cross blood brain barrier o Positive/ Hard Symptoms: delusion, hallucinations, grossly
o Levodopa – precursor of dopamine, can cross the blood disorganized thinking, speech and behavior
brain barrier and eventually converted to dopamine. 99% of o Negative/Soft Symptoms: flat affect, lack of volition, social
Levodopa is converted to dopamine in the periphery by dopa withdrawal
decarboxylase. Only 1% reaches brain. ● Used to control psychotic signs and symptoms
o Carbidopa – given with Levodopa, inhibits the enzyme dopa ● 2 Types of Antipsychotics
decarboxylase o Typical or Traditional Antipyschotics
▪ Diminishes the metabolism of Levodopa in the GIT and ▪ Dopamine antagonists
periphery thus making it more available to cross the – Chlorpromazine (Thorazine)
blood brain barrier – Haloperidol (Haldol)
o Sinemet (Levodopa – Carbidopa combination) – Haloperidol decanoate
o Advantages: – Fluphenizine decanoate (Prolixin) – given via
▪ Lower dosage of Levodopa injection
▪ Single dose per day – every 2-4 weeks, deep IM Z track method
▪ More dopamine reaches basal ganglia ▪ Blocks Dopamine Receptors: D2, D3, D4 – associated with
o Disadvantage – more side effects: N/V, dystonia, psychotic mental illness
behavior ▪ Typical antipsychotics have stronger affinity to D2 which is
o Dopamine Agonists associated with extrapyramidal symptoms.
▪ Amantadine (Symmetrel) – an antiviral drug that ▪ Contraindicated: CNS depression, circulatory collapse,
increases release of dopamine. Effective only as long Parkinson’s Disease, bone marrow suppression, blood
as there is possibility of dopamine release dyscrasias, prolonged QT interval (aggravate dysrhythmias)
▪ Bromocriptine (Parlodel) – more effective than ▪ Caution: Glaucoma, PUD, Urinary/Intestinal Obstruction,
amantadine. seizures (can lower seizure threshold), hyperthyroidism,
▪ Does not depend on cells in the area to biotransform it active alcoholism (risk for further CNS depression)
or release of already produced dopamine ▪ Side Effects
o COMT (Catechol-O-methyltransferase) Inhibitors – Most common: sedation, weakness, tremors
▪ Talcapone (Tasmar) – Anticholinergic: dry mouth, nasal congestion, flushing,
▪ Entacapone (Comtan) constipation, urinary retention, blurred vision
- COMT – inactivates dopamine – Extrapyramidal Symptoms
o Contraindicated a. Pseudoparkinsonism
▪ allergy ❖ similar to S/Sx of Parkinson’s Disease
▪ angle-closure glaucoma ❖ Stooped posture
▪ skin lesions – dopamine may cause melanoma ❖ Masklike face
▪ pregnancy and lactation ❖ Rigidity
o Caution: CV cases, hepatic and renal cases, ❖ Tremors at rest
bronchial asthma, PUD, urinary tract obstruction ❖ Shuffling gait
o Adverse Effects due to stimulation of dopamine ❖ Pill rolling
receptors ❖ bradykinesia
▪ CNS: dizziness, lethargy, headache, malaise, confusion, b. Akathisia
anxiety, nervousness, blurred vision, ataxia ❖ intense need to move about
▪ PNS: N/V, dysphagia, constipation/diarrhea, bone ❖ Restless
marrow depression, cardiac arrhythmias, hypotension. ❖ Trouble standing still
o Clinically important DDI ❖ Feet in constant motion
▪ MAOI’s – increase risk of hypertensive crisis ❖ Rocking back and forth
▪ Vit. B6 or phenytoin – decreased efficacy ❖ Treated with a benzodiazepine
o Nursing Responsibilities (Lorazepam) or a beta blocker
1. Give with meals to alleviate GI irritation. (Propanolol)
2. Safety measures because of blurred vision and dizziness. c. Acute dystonia
3. Ask client to void before giving medication. ❖ muscle spasm of face, tongue, neck, and
4. Bowel program to relieve constipation. back
5. Monitor hepatic, renal and hematologic exams. ❖ Torticollis – twisted head and neck
6. Do not give with foods high in protein and B6. ❖ Opisthotonus – tightness of the entire
7. Assess for improvement of signs and symptoms of body with head backed
Parkinsonism. ❖ and an arched neck
❖ Oculogyric crisis - Abnormal involuntary
ANTIPSYCHOTICS upward movement of eyes
❖ Facial grimacing

30
 ❖ Laryngeal spasm – may cause 10. Do teaching on how to identify signs of EPS.
impairment of airways
❖ Treated with anticholinergic Benztropine ANTIDEPRESSANTS
mesylate (Cogentin) or
Diphenhradramine (Benadryl) ● Biogenic Amine Theory of Depression
d. Tardive Dyskinesia o Theory that believes that depression is caused by
❖ syndrome of permanent, involuntary deficiency of three neurotransmitters: Norepinephrine,
movements characterized by: dopamine and serotonin. These may be due to
⮚ Protrusion and rolling of tongue ▪ Monoamine oxidase may break them down to be
⮚ Sucking, smacking motion of lips recycled and stored in the neurons
⮚ Chewing motion ▪ Rapid fire of neurons causes their depletion
⮚ Involuntary movement of body and ▪ Increased number or sensitivity of postsynaptic
extremities receptors thus causing their depletion.
❖ Later phase of EPS reaction to
antipsychotics ● Tricyclic Antidepressants Imipramine (Tofranil)
❖ Drug should be stopped immediately
e. Neuroleptic Malignant Syndrome
❖ potentially fatal, idiosyncratic reaction to
antipsychotics
❖ Characterized by: rigidity, high fever,
unstable BP, dysrhythmias, respiratory
failure, delirium, pallor, coma and
❖ increase in the enzyme CPK. Client may
be agitated or stuporous.
❖ Dehydration, poor nutrition, medical
condition can increase risk of NMS
❖ Discontinue medication ASAP.
❖ Immediate adequate hydration
❖ Hypothermic blankets and anitpyretics
❖ Administer benzodiazepines and muscle
relaxants (Dantrolene)
o Atypical Antipsychotics
▪ Serotonin/Dopamine Antagonists
– Clozapine (Clozaril)
o Mechanism of action
– Risperodone (Risperdal)
▪ Inhibits presynaptic reuptake of Norepinephrine and
– Olanzapine (Zyprexa)
serotonin and increased stimulation of postsynaptic
▪ Can treat both positive and negative symptoms
receptors. Have anticholinergic affects
▪ Not likely to cause EPS – has more affinity to D4
o Indications:
than D2
▪ Depression
▪ Increase risk for agranulocytosis and weight gain
▪ Enuresis in children older than 6yrs old
▪ Increased risk for hyperlipidemia, DM, cardiac
▪ Clomipramine is used for obsessive compulsive disorders
disorders
o Contraindications and Cautions
▪ Dopamine System Stabilizers
▪ Allergy to any TCA
– Ariprazole (Abilify)
▪ Recent myocardial infarction
– Enhance dopmainergic transmission,
▪ Myelography within the previous 24 hrs or in the next 48
balances dopamine if output is too high
hrs
or too low thus controlling side effects of
▪ Pregnancy and lactation
medications
o Caution
● Nursing Responsibilities
▪ History of seizures
1. Stay with patient until drug is swallowed.
▪ Hepatic of renal impairment
2. Safety. Orthostatic Hypotension, drowsiness and
▪ Preexisting CV disorders,
blurred vision may occur.
▪ Conditions that would be exacerbated by anticholinergics:
3. Administer with food or milk to decrease GI
angle closure glaucoma, urinary retention, prostate
irritation.
hypertrophy, GI or GU surgery
4. Do not chew or crush enteric coated tablets.
▪ Bipolar patients
5. Protect drugs in liquid form from light. Avoid
o Adverse Effects
contact with skin as it may cause contact
▪ CNS: sedation, sleep disturbances, fatigue, hallucinations,
dermatitis.
disorientation, difficulty concentrating, weakness, ataxia
6. For injections, deep IM route using Z-track
tremors
method. DO NOT MASSAGE SITE.
▪ GI: dry mouth, constipation, N/V, anorexia, cramps,
7. Do not stop drug abruptly. Refer to physician for
vomiting
tapering of dosage.
▪ GU: urinary retention and hesitancy, loss of libido,
8. Comfort measures: Ice chips for dry mouth, void
changes in sexual functioning
before taking the drug.
▪ CV: orthostatic hypotension, hypertension, arrhythmias,
9. Monitor CBC, lipid profile, blood glucose, ECG.
▪ MI, angina, palpitations, stroke
31
 o Drug-Drug Interaction ▪ Moderate amounts of Tyramine
▪ Increased TCA effect and adverse reactions with – Meat extracts: consommé and boullion, pasteurized
Cimetidine, Fluoxetine, Ranitidine light and pale beer, avocados
▪ Increases effect of anticoagulants ▪ Low amounts of Tyramine
▪ Increase risk of arrhythmias and hypertension with – Distilled liquors: vodka, gin, scotch, rye
sympathomimetics – Cheese: American, mozzarella, cottage cheese,
▪ Increase risk of hyperpyretic crisis, severe convulsions, cream cheese
▪ hypertensive episodes, death with MAOI’s – Chocolate
o Nursing Responsibilities – Fruits, figs, raisins, grapes, pineapple, oranges
1. Limit access if patient is suicidal. – Sour cream, yogurt
2. Maintain initial dose for 4-8 weeks o Nursing Responsibilities
3. Give major portion at bed time because of drowsiness 1. Limit access of drug to suicidal pts.
and anticholinergic effects 2. Monitor patient for 2-4 wks to ascertain onset of full
4. Taper dosage. therapeutic effect
5. Comfort and safety measures 3. Monitor BP
● Monoamine Oxidase Inhibitors 4. Monitor for adverse effects
o Isocarboxazid (Marplan) 5. Monitor Liver Function
o Phenelzine (Nardil) o Antidote – Phentolamine (Regitine)
o Tranylcypromine (Parnate)
o Mechanism of action ● Selective Serotonin Reuptake Inhibitors
▪ Inhibits breakdown of biogenic amines (NorEpi, Dopa, o Mechanism of action
and serotonin), making them more available at the ▪ Specifically blocks the reuptake of serotonin with little
synaptic cleft and neuronal storage vesicles. effect on NE. It has less side effects and a better choice
o Indication for many patients
▪ For depression o Therapeutic Actions and Indications
o Contraindications ▪ For depression, OCD’s, bulimia, panic disorders,
▪ Pheochromocytoma, CV diseases, abnormal CNS premenstrual dysmorphic disorder.
vessels, or defects, renal and hepatic impairment, o Contraindications and Cautions
myelogrpahy for the past 24 or in the next 48 hrs ▪ Allergy to drugs, pregnancy and lactation
o Caution in Psychiatric Patients, seizure disorders and o Caution in with impaired renal or hepatic function, or
hyperthyroidism diabetes
o Adverse Effects o Adverse Effects
▪ CNS: Dizziness, excitement, nervousness, mania, ▪ CNS: headache, dizziness, insomnia, anxiety, tremors,
hyperreflexia, tremors, confusion, insomnia, agitation, agitation, and seizures.
blurred vision. ▪ GI: N/V, diarrhea, dry mouth anorexia, constipation,
▪ GI: Liver toxicity, N/V, diarrhea or constipation, anorexia, changes in taste
weight gain, dry mouth, abdominal pain. ▪ GU: painful menstruation, cystitis, sexual dysfunction,
▪ GU: Urinary retention, dysuria, incontinence, sexual urgency, and impotence.
dysfunction ▪ Respi: cough, dyspnea, URTI
▪ CV: Orthostatic hypotension, arrhythmias, palpitations, o Drug-Drug- interaction
angina ▪ Not to be taken with other antidepressants or St. John’s
o HYPERTENSIVE CRISIS – occipital headache, palpitations, Wort
stiff neck, nausea, vomiting, sweating, dilated pupils, o Nursing Responsibilities
photophobia, chest pains,. May progress to intracranial 1. Limit access if patient is suicidal.
bleeding. 2. Maintain initial dose for 4-8 weeks
o Drug-Drug- interaction 3. Give major portion at bed time because of drowsiness
▪ Other antidepressants – hypertensive crisis, coma, and anticholinergic effects
convulsions, Serotonin syndrome 4. Taper dosage.
▪ Wait 6 weeks after last antidepressant before 5. Comfort and safety measures
administering MAOI
▪ Tyramine ANTIMANIC DRUGS
– causes release of monoamines
– normally broken down by MAO enzymes ● Mood stabilizers
– may be absorbed in high concentrations with MAOI’s. ● Mania – opposite of depression, overstimulation of neurons
– Can cause hypertensive crisis ● Lithium (Lithane, Lithotabs)
▪ High in Tyramine ● Atypical antipsychotics
– Aged cheese: cheddar, blue cheese, swiss, o Olanzapine (Zyprexa)
Camembert o Aripiprazole (Abilify)
– Aged or fermented meats, fish or poultry: chicken ● Anticonvulsant
pate, beef liver pate, caviar o Carbamezapine (Tegretol)
– Brewer’s yeast o Valproic Acid (Depakene)
– Fava beans o Lamotrigine (Lamictal)
– Red wines: Chianti, burgundy, sherry, vermouth ● LITHIUM
– Smoked or pickled meats, fish or poultry: herring, o Alters sodium transport in nerve and muscle cells. Inhibits
sausage, corned beef, salami, pepperoni, soy sauce release of norepinephrine and dopamine but not serotonin.

32
 o Contraindications: hypersensitivity to lithium, renal or cardiac
problems, pregnancy and lactation, conditions that have
decreased sodium: hyponatremia, dehydration, diuretic use
o Lithium depletes sodium reabsorption. Hyponatremia leads to
Lithium retention and toxicity.
o Therapeutic range: 0.5 to 1.5 mEq/L
o Serum levels should be monitored twice a week when therapy
is initiated then every 2 to 3 months during long term therapy.
o Side Effects
▪ less than 1.5 mEq: CNS depression, lethargy slurred
speech, polyuria (may be due to renal toxicity), N/V, diarrhea
▪ 1.5 to 2 mEq/L: intensification of all of the above with ECG
changes
▪ 2 to 2.5 mEq/L: ataxia, clonic movements, hyperreflexia,
seizures, severe ECG changes, hypotension, decreased
intravascular volume due to increased output of diluted urine
(reflective of renal damage), pulmonary toxicity
▪ Above 2.5 mEq/L: complex multiorgan toxicity
o Drug-Drug Interaction
▪ Haloperidol- can cause encephalopathic syndrome
▪ Carbamazepine – increase CNS toxicity
▪ Iodide salt – increase risk of hypothyroidism
▪ Thiazide – increase risk for Lithium toxicity because of
sodium loss
▪ NSAIDS – may increase serum levels of lithium. Not advised
to be taken together.
o Nursing Responsibilities
1. Give with meals to prevent GI upset. Small frequent meals
are preferred.
2. Instruct client to avoid caffeine.
3. Arrange to decrease dose after acute manic episode.
4. Ensure adequate intake of salt and fluids.
5. Monitor for signs of depression and suicidal tendencies.
6. Monitor for Intake and Output, polyuria and signs of fluid
volume deficit.
7. Monitor for electrolyte imbalances and ECG changes.
8. Safety measures: siderails and assistance during
ambulation.
9. Instruct client that full effect will be seen within 1-2 weeks.
10. Comfort and supportive measures.
CENTRAL NERVOUS SYSTEM STIMULANTS
● ADHD
o short attention span, hyperactivity and impulsivity.
o stimulants tend to decrease distractibility and hyperactivity thus
increasing attention span
● Narcolepsy – condition characterized by excessive drowsiness and
uncontrollable sleep attacks during daytime
● Amphetamine-like Drugs
o Methylphenidate (Ritalin, Concerta) – for ADHD and other
hyperactivity disorders. Also for narcolepsy
o Pemoline (Cylert) – not drug of choice because of hepatic failure
o Dexmethylphenidate (Focalin) – used in lower doses than
methylphenidate. Only for treatment of ADHD in children 6 yrs
and above.
o Modafinil (Provigil) for narcolepsy, improving shift work sleep
disorder and for improving wakefulness in people with
obstructive sleep apneas.
● Mechanism of action
o Act as cortical and RAS stimulants, possible by increasing
release of catecholamines from presynaptic neurons, leading to
stimulation of postsynaptic neurons
o ADHD – this paradoxical effect calms hyperexcitability through
increased stimulation of an immature RAS, leading to the ability
to better select incoming stimuli
o Narcolepsy – stimulates cortex
● Contraindications and Cautions
o Allergies, marked anxiety, agitation, tension, cardiac disease,
severe fatigue, glaucoma, pregnancy, lactation
● Adverse Effects
o CNS: nervousness, insomnia, dizziness, headache, blurred
vision, difficulty with accommodation,
o GI: anorexia, nausea, and weight loss
o CV: hypertension, arrhythmias, angina
o Integ: rashes
o Physical and psychological dependence
● Drug-Drug- interaction
o Increased risk of toxicity and adverse effects with MAOIs
o Increased drug levels with TCAs and Phenytoin
o Caffeine – increases drug action
● Nursing Responsibilities
1. Monitor V/S
2. Arrange to dispense the least amount of drug possible to
3. minimize risk of overdose and abuse.
4. Monitor for tolerance and dependence
5. Monitor for drug abuse
6. Caffeine containing foods should be avoided
7. Monitor for S/E’s, ADRs
8. Monitor height, weight, and growth of child.
9. Give before 6 pm to prevent insomnia
10. Should be given 30-45 minutes before meals because food
affects absorption rate
ANTIEPILEPTIC DRUGS
● Epilepsy
o seizure due to sudden discharge of excessive electrical energy
from nerve cells in brain
o Loss or disturbance of consciousness and usually by a
convulsion (abnormal motor reaction) jerking
● Types of Seizures
o Partial simple (Jacksonian)
▪ occur in a single area of the brain and may involve single
muscle movement or sensory alteration
o Partial complex
▪ involve complex sensory changes such as mental distortion,
hallucination, changes in personality, loss of consciousness.
Motor changes include, involuntary urination, chewing
motions, diarrhea
o Generalized Absence (Petit Mal)
▪ Involve abrupt brief (3-5 sec) periods of loss of
consciousness. Common in children will usually disappear at
puberty.
o Tonic – Clonic (Grand Mal)
▪ Involve dramatic tonic-clonic muscle contractions, loss of
consciousness, and a recovery period characterized by
confusion and exhaustion
● Hydantoins
o Phenytoin – stabilize nerve membranes and limit spread of
excitability from the initiating focus.
▪ Has least toxic effects, small effect on sedation and is
non-addicting.
▪ Has very narrow therapeutic range 10-20 ug/ml.
o Contraindications and Cautions
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 ▪ Allergies, Blood dyscrasias, psychiatric disorders
▪ Pregnancy (can cause teratogenic effect) and Lactation
o Caution in DM, SLE, liver or hepatic impairment
o Adverse Effects
▪ Sever liver toxicity, bone marrow suppression, gingival
hyperplasia, hirsutism
o Toxic signs: sedation, ataxia, nystagmus, diplopia
o Drug-Drug- interaction
▪ CNS depression if taken with alcohol
▪ Evening primrose- can increase risk of seizures
▪ Gingko – can increase side effects
▪ Cimetidine , Sulfonamides – increase action of hydantoins
▪ Anticoagulants, Aspirin – increased activity
▪ Decreased absorption with antacids and antineoplastic drugs
o Nursing Responsibilities
1. Monitor serum drug level
2. Instruct not to drive or perform hazardous activity
3. Do not abruptly stop medication. Rebound seizures may
occur.
4. Use soft toothbrush to prevent irritation and bleeding due to
gingival hyperplasia.
5. Regular dental check –up
6. Take with food or milk at the same time everyday
7. Provide counseling regarding risks of pregnancy for women
of childbearing age
8. IM route not recommended. If to be given IV, do not mix with
Dextrose solution. Flush tubing with NSS before and after
drug administration.
9. Discontinue drug if allergies, liver dysfunction or severe skin
rash occurs.
● Magnesium Sulfate
o Mechanism of action
▪ Blocks peripheral muscular neurotransmission by reducing the
sensitivity of the motor endplate and lowering the excitability
of the motor membrane
o Therapeutic Actions and Indications
▪ Anticonvulsant
▪ Uterine relaxant
▪ Magnesium deficiency
o Contraindications and Cautions
▪ Do not give if allergic to magnesium
▪ Do not administer 2 hours before delivery
o Adverse Effects
▪ Circulatory collapse, myocardial depression, respiratory
paralysis, CNS depression
o Drug-Drug- interaction
▪ Heart block if given with calcium used as treatment for digitalis
toxicity
o Nursing Responsibilities
▪ Monitor for patellar reflexes and respiration rate. Respiratory
paralysis usually occurs after knee-jerk reflex disappears
▪ -Monitor urine output. Output must be more than 100cc in the
last for hours to assure adequate kidney perfusion
o Antidote Calcium Gluconate
NARCOTICS AND ANALGESICS
● Pain perception
● Narcotics- first derived from opium. Acts on CNS. Suppresses not
only respiratory center but also cough reflex.
● Meperidine – no antitussive effect
● Codeine – antitussive 1/120th the potency of morphine
● Opioid receptors
o mu – primarily pain blocking receptors. But also accounts for
respiratory depression, euphoria, decreased GI activity, pupil
constriction and development of physical dependence
o kappa – associated with some anesthesia, pupillary
constriction, sedation, dysphoria
o beta- reacts with enekphalins to modulate pain transmission
o sigma – pupillary dilation and may be responsible for
hallucinations, dysphoria, and psychoses
● Narcotic Agonists (Morphine)
o Mechanism of action
▪ Acts at specific opioid receptor sites in CNS to produce
analgesia.
o Therapeutic Actions and Indications
▪ Relief of severe to acute or chronic pain, preop medication,
analgesia during anesthesia and specific individual
indications.
o Contraindications and Cautions
▪ Contraindicated in allergy to drug pregnancy, labor lactation
o Caution in respiratory dysfunction, recent GI or GU surgery,
acute abdomen or ulcerative colitis
o Adverse Effects
▪ CNS: light headedness, drowsiness, psychoses, anxiety,
fear, hallucination, pupil constriction
▪ Respi: Respiratory depression, apnea, shock
▪ CV: orthostatic hypotension, cardiac arrest
▪ GI: N/V constipation, biliary spasm
▪ GU: ureteral spasm, urinary retention, hesitancy, loss of
libido
o Drug-Drug- interaction
▪ Increased respiratory depression with barbiturate general
anesthetics, MAOIs, phenothiazines
o Nursing Responsibilities
▪ Provide narcotic antagonist (Naloxone) at bedside in case
of overdose or adverse reaction
▪ Monitor for respiratory depression
▪ Monitor for constipation
▪ Never administer to patients with biliary disorders
▪ Monitor timing of analgesic
▪ Monitor injection site for irritation and extravasation
▪ Do not inject in a poorly perfused area
● Narcotic Agonists-Antagonists
o Stimulate certain receptors but block others
o Have less potential for abuse than narcotic agonists
o Have been associated with more psychotic- like reactions
o Buprenorphine (Buprenex) –mild or moderate pain
o Butorphanol (Stadol) – preop med to relieve moderate to
severe pain for migraine headaches
o Nalbuphine (Nubain) moderate to severe pain, as anad junct to
general anesthesia,a nd relieve pain during labor and delivery
o Pentazocine (Talwin) oral form. Highly abused drug
o Contraindications and Cautions
▪ Contraindicated in allergy to drug pregnancy, labor lactation
▪ Same as Morphine. However should not be used to treat
morphine dependence as it can precipitate withdrawal
syndrome
o Adverse Effects
▪ CNS: light headedness, drowsiness, psychoses, anxiety,
fear, hallucination, pupil constriction
▪ Respi: Respiratory depression, apnea, shock
▪ CV: orthostatic hypotension, cardiac arrest
▪ GI: N/V constipation, biliary spasm
▪ GU: ureteral spasm, urinary retention, hesitancy, loss of
libido
▪ Same as morphine but has less tendency for dependence
o Drug-Drug- interaction
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 ▪ Increased respiratory depression with barbiturate general ❖ involves relaxation of skeletal muscles, stabilization of
anesthetics, MAOIs, phenothiazines respiration, loss of eye reflexes. Surgery is performed
o Nursing Responsibilities here.
▪ Provide narcotic antagonist (Naloxone) at bedside in case of
overdose or adverse reaction STAGE 4: MEDULLARY PARALYSIS
▪ Monitor for respiratory depression ❖ very deep CNS depression with loss of respiratory and
▪ Monitor for constipation vasomotor center stimuli. Death can occur rapidly.
▪ Never administer to patients with biliary disorders ▪ Administration of General Anesthetics
▪ Monitor timing of analgesic ❖ Induction – from beginning of anesthesia until Stage 3
▪ Monitor injection site for irritation and extravasation ❖ Maintenance – upon reaching Stage 3 until completion
▪ Do not inject in a poorly perfused area of procedure
● Narcotic Antagonists – Naloxone (Narcan) ❖ Recovery – from discontinuation of anesthetic until
o Mechanism of action patient has regained consciousness, movement and
▪ Binds with opioid receptors but do not activate it ability to communicate.
o Indications – Needs continues monitoring to provide
▪ Used to block unwanted effects of narcotics life support as needed
o Contraindications and Cautions ▪ Types of General Anesthesia
▪ Allergies ❖ Barbiturates
▪ Narcotic addiction –because it can precipitate withdrawal – intravenous anesthetics used to induce rapid
syndrome anesthesia which is then maintained with an inhaled
o Adverse Effects drug
▪ N/V tachycardia, hypertension, tremors, anxiety, CNS – Thiopental Sodium (Penthotal) – is probably the most
excitement, reversal of analgesia widely used of IV anesthetics. Very rapid onset of
action and ultrashort recovery period. No analgesic
ANESTHETIC AGENTS properties.
– Methohexital (Brevital) – cannot come in contact with
● used to cause complete or partial loss of sensation silicone (rubber stoppers and disposable syringes)
● 2 Types ❖ Non-Barbiturates
1) General Anesthetics – Midazolam
▪ CNS depressants that cause loss of pain sensation and – Droperidol (Inapsine)
consciousness – Etomidate (Amidate)
▪ Produces sedation, hypnosis, anesthesia, amnesia and – Ketamine (Ketalar)
unconsciousness – Propofol (Diprivan)
▪ Depresses RAS and cerebral cortex ❖ Anesthetic Gases
▪ Blocks autonomic reflexes. – Nitrous Oxide (blue cylinder) – very potent analgesic,
▪ Carries risk of cardiac, respiratory, GI and immune weakest of the gas anesthetics but least toxic
compromise ⮚ Frequently used in dental surgery
▪ 3 Goals ⮚ Given with oxygen
1. Analgesia – Cyclopropane (orange cylinder) – not a very good
2. Unconsciousness analgesic
3. Amnesia – Ethylene (red cylinder)
▪ Balanced Anesthesia ❖ Volatile Liquids
❖ use of a combination of drugs, each with a specific use – unstable at room temperature and release gases,
to achieve analgesia, muscle relaxation, which are inhaled
unconsciousness and amnesia. – Mostly halogenated carbons
❖ Includes: – May cause malignant hyperthermia. Treated with
✔ Preoperative meds: anticholinergics – decrease Dantrolene
secretions, prevents bradycardia – Halothane (Flouthane) – prototype
✔ Sedative-Hypnotics: benzodiazepines and ⮚ Metabolized in liver into toxic hydrocarbons and
barbiturates- to relax patient, facilitate amnesia, and bromide increasing risk for hepatic toxicity
decrease SNS stimulation ⮚ Has a rare Recovery syndrome characterized by:
✔ Antiemetics: minimize N/V fever, anorexia, N/V, eventual hepatitis
✔ Antihistamine: minimize allergic reaction – Desflourane – can cause respiratory reactions
✔ Narcotics ⮚ Not recommended in people with respiratory
✔ Inhaled Gas problems and pediatric patients
✔ Muscle relaxant – Enflurane – associated with renal toxicity, cardiac
▪ Stages of Anesthesia arrhythmias and respiratory depression
STAGE 1: ANALGESIA ⮚ Not to be given to patients with renal, respiratory
❖ loss of pain and sensation but patient still conscious and or cardiac dysfunction
able to communicate – Isoflurane – does not cause as much respiratory or
STAGE 2: EXCITEMENT OR DELIRIUM cardiac side effects but can cause hypotension,
❖ Excitement or delirium – period of excitement and hypercapnea, muscle soreness and bad taste in the
combative behavior. Increased SNS response mouth
(tachycardia, increased RR and BP changes) – Sevoflurane (Ultane) – latest of the volatile liquids.
STAGE 3: SURGICAL ANESTHESIA Very rapid clearance thus minimizing side effects.

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 ⮚ Contraindications
X Status asthmaticus
X Absence of suitable veins for an IV ❖ Central Nerve block
administration – Caudal Block: injection into the sacral canal below the
⮚ Caution in severe CV problems epidural area
⮚ Associated with the depressive effects of the drug: – Epidural Anesthesia: injection of anesthesia in the
CV depression, shock, respiratory depression, epidural area
laryngospasm, bronchospasm, N/V, increased ⮚ Low dose – can impair sensation without impairing
somnolence, delirium mobility
⮚ Malignant Hyperthermia – extreme muscle rigidity, ⮚ High dose – impairs both sensation and mobility
severe hyperpyrexia, acidosis and in some cases – Spinal Anesthesia: blocks sensation in the lower
death. Treated with dantrolene. abdomen and all the areas below it
⮚ Anaphylactic Reaction ⮚ Medication in injected into spinal fluid
⮚ Nursing Responsibilities – Intravenous Regional Anesthesia (Bier Block)
1. Only trained personnel can administer
anesthesia.
2. Monitor v/s. Check for signs of respiratory or
cardiac
3. depression and malignant hyperthermia. Have
dantrolene on stand by.
4. V/S, ECG and urine output should be monitored
frequently until recovery phase and client is
conscious.
5. Safety measures because of delirium and sedation.
6. Emergency equipment should be on standby.
2) Local Anesthetics
▪ loss of sensation in limited areas of the body
▪ 2 Types
1. Esthers - Benzocaine
2. Amides – Lidocaine
▪ Mechanism of Action
❖ Temporarily interrupts production and conduction of
nerve impulses. Prevents sodium from entering cell
thus no depolarization will happen.
▪ Contraindications
❖ Allergy to any local anesthetic or parabens (esters
used as a preservative in cosmetics) ⮚ drain all blood from an extremity.
❖ Heart block ⮚ A tourniquet is used to prevent the anesthetic agent
❖ Shock from entering the general circulation.
❖ Decreased plasma esterases ⮚ Anesthesia is injected into the vein of the arm or leg.
▪ Modes of Administration Allows surgery in a bloodless field.
❖ Topical ⮚ Drug-Drug Interaction
❖ Infiltration X Increased neuromuscular blockade if given with
❖ Nerve Block succinylcholine
– Peripheral Nerve Block X Epinephrine – given together with lidocaine for
– Central Nerve Block vasoconstriction thus lessening the systemic
❖ Intravenous Regional Anesthesia (Bier Block absorption of drug
❖ Infiltration – injecting anesthesia directly into tissue ⮚ Nursing responsibilities
that is to be treated (sutured, drilled, cut)
❖ Field Block - injecting anesthesia all around the area
surrounding the tissue affected by the operation.
Anesthesia comes in contact with all nerve endings
surrounding the area. Usually for tooth extractions
❖ Nerve Block – blocks pain by injecting anesthesia
along the nerves that supply a region.
– Performed away from the
surgical field
– Peripheral nerve block
⮚ brachial plexus
⮚ intercostals

36
 1. Have emergency equipment on standby in
case of adverse reaction.
2. Have drugs for managing hypotension,
cardiac arrest, allergic reactions, and CNS
alteration on standby
3. Establish safety precautions because of
drowsiness, change in sensorium, loss of
sensation and mobility.
4. For spinal anesthesia make sure patient is
adequately hydrated and advice to stay flat
on bed for 8-12 hours to prevent spinal
headache.
5. Monitor urinary output for 8 hours. Urinary
retention is common in regional anesthesia
that affects lower abdomen.
6. Local anesthetics should never be
absorbed systemically.
MUSCLE RELAXANTS
● Neuromuscular Abnormalities
o Muscle Spasms – injury to
musculoskeletal system.
Flood of sensory impulses
from spinal cord. Impulses
trigger contraction which cuts
off blood supply. This causes
build up of lactic acid,
resulting in pain
o Muscle spasticity - injury to
CNS. A permanent condition.
May be due to increase in
excitatory influences or
decrease in inhibitory
influences.
o Centrally Acting Muscle Relaxant
▪ Also called spasmolytics. Acts on the spinal cord.
▪ Baclofen (Lioresal) – for muscle spasticity associated
with neuromuscular diseases such as multiple
sclerosis, muscle rigidity, spinal cord injuries.
▪ May be in intrathecal forms.
▪ Therapeutic Actions and Indications
❖ Exact mechanism is not known, it is thought to
involve action in upper or spinal interneurons.
▪ Contraindications and Cautions
❖ Known allergy
❖ Muscle spasms resulting from rheumatic disorders.
❖ Should not be used to treat spasticity that
contributes to locomotion, upright position and
increased function.
▪ Cautiously in patients with history of epilepsy, any
condition marked by muscle weakness, hepatic or renal
dysfunction, pregnancy and lactation.
▪ Adverse Effects
❖ CNS depression: drowsiness, fatigue, weakness,
confusion, headache, insomnia.
❖ GI: nausea, dry mouth, anorexia, constipation
❖ Others: hypotension, arrhythmias, urinary frequency
or urgency.
▪ Drug-Drug- interaction
❖ Alcohol and any other CNS depressant – CNS
depression may increase
▪ Nursing Responsibilities
1. Discontinue drug at any sign of
hypersensitivity
2. Instruct client not to drive or do anything that
requires mental alertness
3. Taper drug slowly over 1-2 weeks to prevent
development of psychosis and hallucination
o Direct Acting Muscle Relaxants
▪ Dantrolene (Dantrium)
▪ Mechanism of action
❖ Acts within skeletal muscle fibers, interfering
with the release of calcium from muscle
tubules. This prevents contractions.
▪ Therapeutic Actions and Indications
❖ Controls spasticity from upper motor neuron
disorders, including spinal cord injuries,
myasthenia gravis, muscular dystrophy,
cerebral palsy.
▪ Also prevents malignant hyperthermia- state of
intense muscle contraction and resulting
hyperpyrexia.
▪ May occur as an adverse effect of Succinylcholine
in surgery).
▪ Contraindications and Cautions
❖ Allergy to drug
37
 ❖ If spasticity that contributes to locomotion,
upright position,
❖ or increased function
▪ Caution: in women and patients older than 35 y/o
because of increased risk of potentially fatal
hepatocellular disease
❖ History of liver disease
❖ Respiratory depression
❖ Pregnancy
▪ Adverse Effects
❖ Direct heptocellular damage and
hepatitis
❖ CNS depression: drowsiness, fatigue,
weakness, confusion,
❖ headache, insomnia and visual
disturbances
❖ GI: irritation, diarrhea, constipation,
abdominal cramps.
▪ Drug-Drug- interaction
❖ With estrogen – can increase incidence
of hepatocellular toxicity.
▪ Nursing Responsibilities
1. Discontinue drug at any sign of liver
dysfunction
2. Periodically discontinue drug for 2-4
days to monitor
3. effectiveness of drug.
4. Discontinue drug if diarrhea gets to
severe.

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