Anti-inflammatory Agents

Salicylates ✓ have anti-inflammatory, antipyretic, and analgesic properties

✓ some of the oldest anti-inflammatory drugs used
✓ generally available without prescription and are relatively nontoxic when used
as directed
✓ aspirin is one of the most widely used drugs for treating inflammatory
conditions
✓ other synthetic salicylates include balsalazide, choline magnesium
trisalicylate, diflunisal, mesalamine, olsalazine, and salsalate

Actions and Indications

• inhibit the synthesis of prostaglandin
• the antipyretic effect may be related to blocking of a prostaglandin mediator
of pyrogens at the thermoregulatory center of hypothalamus
• at low level, aspirin affects platelet aggregation by inhibiting the synthesis of
thromboxane A2
• at higher levels, aspirin inhibits the synthesis of prostacyclin
• indicated for the treatment of mild to moderate pain, fever, and numerous
inflammatory conditions including rheumatoid arthritis and osteoarthritis

Pharmacokinetics
• readily absorbed directly from the stomach reaching peak levels within 5 to 30
minutes
• metabolized in the liver and excreted in the urine, with a half life of 15
minutes to 12 hours
• cross the placenta and enter the breast milk

Contraindications and Cautions

• presence of known allergy to salicylates, other NSAIDs, or tartrazine
• bleeding abnormalities
• impaired renal function
• chicken pox or influenza
• surgery or other invasive procedures scheduled within 1 week
• pregnancy and lactation

Adverse Effects
• result of direct drug effects on the stomach and on clotting systems
• salicylism can occur with high levels of aspirin
• signs of salicylate toxicity: hyperpnea, tachypnea, hemorrhage, excitement,
confusion, pulmonary edema, convulsions, tetany, metabolic acidosis, fever,
coma, and cardiovascular, renal and respiratory collapse
NSAIDs ✓ provide strong anti-inflammatory and analgesic effects without the adverse
effects associated with the corticosteroids
✓ include propionic acids, acetic acids, fenamates, oxicam derivatives, and
cyclooxygenase-2 (COX-2) inhibitors
Propionic Acids
• fenoprofen
• flurbiprofen
• ibuprofen
• ketoprofen
• naproxen
• oxaprozin
Acetic Acids
• diclofenac
• etodolac
• indomethacin
• ketorolac
• nabumetone
• sulindac
• tolmetin
Fenamates
• meclofenamate
• mefenamic acid
Oxicam Derivatives
• meloxicam
• piroxicam
Cyclooxygenase-2 Inhibitor
• celecoxib

Therapeutic Actions and Indications

• the anti-inflammatory, analgesic and antipyretic effects are largely related to
inhibition of prostaglandin synthesis
• block two enzymes, COX-1 and COX-2
• indicated for the relief of signs and symptoms of rheumatoid arthritis and
osteoarthritis, for the relief of mild to moderate pain, for treatment of primary
dysmenorrhea, and for fever reduction

Pharmacokinetics
• rapidly absorbed from the GIT, reaching peak levels in 1- 3 hours
• metabolized in the liver and excreted in the urine
• cross the placenta and into the breast milk

Contraindications and Cautions

• NSAIDs are contraindicated in the presence of allergy to NSAID or salicylate
• celecoxib is also contraindicated in the presence of allergy to sulfonamides
• CV dysfunction or hypertension
• peptic ulcer or known GI bleeding
• pregnancy or lactation
• renal or hepatic dysfunction
 Adverse Effects
• nausea, GI pain, dyspepsia, constipation, diarrhea, or flatulence caused by
direct GI effects of the drug
• headache, dizziness, somnolence, and fatigue also occur frequently
• bleeding, platelet inhibition, hypertension and bone marrow depression have
been reported with chronic use
• rash and mouth sores may occur
• anaphylactic reactions ranging up to fatal anaphylactic shock

Drug Interactions
• decreased diuretic effect when taken with loop diuretics
• potential for decreased antihypertensive effect of beta blockers if these drugs
are combined
• lithium toxicity, especially when combined with ibuprofen

Analgesics

✓ drugs that help to alleviate pain without loss of consciousness

✓ opioid analgesics were originally obtained from the opium plant
✓ 3 groups of opioid analgesics that interact with opioid receptors to bring
pain relief

• opioid agonists
• opioid agonists-antagonists
• opioid antagonists
Opioid Agonists Morphine, Alfentanil, Codeine, Fentanyl, Hydrocodone, Hydromorphone,
Levomethadyl, Levorphanol, Meperidine, Methadone, Oxycodone, Oxymorphone,
Propoxyphene, Remifentanil, Sufentanil

Action
- stimulate Mu, Kappa, Epsilon and possibly Delta receptor sites to bring about pain
relief, euphoria, and sedation

Uses
- relief of moderate to severe pain, adjunct to general anesthesia, relief of chronic
pain, antitussive, postoperative medications
Opioid Pentazocine, Buprenorphine, Butorphanol, Dezocine, Nalbuphine
Agonists-
Antagonists Action
- block and stimulate different opioid receptors to produce pain relief, sedation, and
euphoria; can cause psychotic type reactions and withdrawal in clients who have
taken opioids for extended periods of time

Uses
- pain relief during labor and delivery, relief of moderate to severe pain, adjunct to
general anesthesia
 Opioid Naloxone, Nalmefene, Naltrexone
Antagonists
Action
- attach to opioid receptors without stimulating them and reverse effects of opioids

Uses
- narcotic overdose, reversal of respiratory depression from narcotics

Adverse Effects
- tremors, drowsiness, hypertension, tachycardia, sweating, nausea, vomiting,
elevated partial thromboplastin time, hyperventilation, reversal of analgesia
Acetaminophen ✓ used to treat mild to moderate pain and fever and often is used in place of
NSAIDs or salicylates
✓ most frequently used drug for managing pain and fever in children
✓ widely available OTC and is found in many combination products
✓ causes liver toxicity than can lead to death when taken in high doses

Action and Indications

• acts directly on the thermoregulatory cells in the hypothalamus to cause
sweating and vasodilation
• indicated for the treatment of pain and fever associated with a variety of
conditions; for the prophylaxis of children receiving DPT immunizations and
for the relief of musculoskeletal pain associated with arthritis

Pharmacokinetics
• rapidly absorbed from the GIT, reaching peak levels in 0.5 to 2 hours
• extensively metabolized by the liver and excreted in the urine, with a half
life of about 2 hours
• caution should be used in patients with hepatic or renal impairment
• crosses the placenta and enters breast milk

Contraindications
• presence of allergy to acetaminophen
• used cautiously in pregnancy and lactation
• hepatic dysfunction or chronic alcoholism

Adverse Effects
• headache, hemolytic anemia, renal dysfunction, skin rash, and fever
• hepatotoxicity

Immunosuppressants

Corticosteroids ✓ suppress immune responses and reduce inflammation

✓ natural or synthetic
✓ natural corticosteroids are hormones produced by the adrenal cortex
✓ most corticosteroids drugs are in synthetic forms
 ✓ classified according to their biological activities:

• glucocorticoids
- cortisone acetate and dexamethasone
- affect carbohydrate and protein metabolism
• mineralocorticoids
- aldosterone and fludrocortisone acetate
- regulate electrolyte and water balance
Glucocorticoids ✓ stimulate an increase in glucose levels, increase the rate of protein
breakdown and decrease the rate of protein formation from amino acids
and cause lipogenesis
✓ most are synthetic analogues of hormones secreted by the adrenal
cortex
✓ exert anti-inflammatory, metabolic, and immunosuppressant effects
✓ include beclomethasone, betamethasone, budesonide, flunisolide,
cortisone, hydrocortisone, dexamethasone, hydrocortisone,
methylprednisolone, prednisolone, prednisone, triamcinolone

Pharmacokinetics
• absorbed well from many sites, metabolized by natural systems mostly
within the liver, and excreted in the urine
• known to cross placenta and enter the breast milk
• beclomethasone and flunisolide: available in the form of respiratory
inhalant and nasal spray
• betamethasone - parenteral use in acute situations, oral and topical
• budesonide - intranasal use
• cortisone - oral and parenteral
• dexamethasone and triamcinolone - multiple forms for dermatological,
ophthalmological, intra-articular, parenteral, and inhalational uses
• hydrocortisone - preferred for use as topical or ophthalmic agent
• methylprednisolone - oral, parenteral, intra-articular, and retention
enema preparations
• prednisolone - intralesional and intra-articular injection; oral and topical
forms
• prednisone – oral

Pharmacodynamics
✓ enter target cells and bind to cytoplasmic receptors, initiating many
complex reactions that are responsible for anti-inflammatory and
immunosuppressive effects
✓ glucocorticoids inhibit immune responses by:

• suppressing or preventing cell-mediated immune reactions

• reducing levels of leukocytes, monocytes and eosinophils
• decreasing the binding of immunoglobulins to cell surface receptors
• inhibiting interleukin synthesis
 Pharmacotherapeutics
• indicated for the short-term treatment of many inflammatory disorders,
to relieve discomfort, and to give the body a chance to heal from the
effects of inflammation
• used to treat local inflammation as topical agents, intranasal or inhaled
agents, intra-articular injections, and ophthalmic agents
• systemic use is indicated for the treatment of some cancers,
hypercalcemia associated with cancer, hematological disorders, and
some neurological infections
• some can be used in replacement therapy for adrenal insufficiency when
combined with mineralocorticoids

Adverse reactions
Endocrine System:
• DM
• Hyperlipidemia
• adrenal atrophy
• hypothalamic-pituitary-adrenal axis suppression
• cushingoid signs and symptoms (buffalo-hump, moon face and elevated
blood glucose levels)
Mineralocorticoids ✓ affect electrolyte and water balance
✓ the classic mineralocorticoid is aldosterone
✓ mineralocorticoids that are available include fludrocortisone acetate and
hydrocortisone

Pharmacokinetics
• fludrocortisone acetate is absorbed well and distributed to all parts of
the body
• metabolized in the liver to inactive metabolites
• excreted by the kidneys primarily as inactive metabolites
• known to cross placenta and to enter the breastmilk; should be avoided
during pregnancy and lactation

Pharmacodynamics
• fludrocortisone acetate affects fluid and electrolyte balance by acting on
the distal renal tubule to increase sodium reabsorption and potassium
and hydrogen secretion

Pharmacotherapeutics
• increase sodium reabsorption in renal tubules leading to sodium and
water retention, and increase potassium excretion
• replacement therapy for patients with adrenocortical insufficiency
• may be used to treat salt-losing congenital adrenogenital syndrome after
the patient’s electrolyte balance has been restored
 Adverse Effects
• common AE are related to the increased fluid volume seen with sodium
and water retention* and possible hypokalemia
• allergic reactions ranging from skin rash to anaphylaxis

Immunosuppressant Agents

✓ interfere with the immune response

✓ used to prevent organ rejection in organ transplantation and in the
treatment of autoimmune diseases
✓ include T and B cell suppressors and monoclonal antibodies
✓ protect skin with sunscreen and clothing when out in the sun
✓ notify physician before taking any drugs when taking
immunosuppressants
✓ do not become pregnant while on drug therapy
✓ patient is at high risk for infection
✓ all side effects need to be reported immediately to the physician
T and B cell • cyclosporine, alefacept, azathioprine, glatiramer acetate, methotrexate,
suppressors mycophenolate, pimecrolimus, sirolimus, tacrolimus

Pharmacodynamics
• interfere with the release of T-cell growth factor and interleukins, hamper
the activity of helper and suppressor T cells, and prevent antibody
production by B cells

Pharmacotherapeutics
• prevention of rejection in kidney, heart and liver transplants
• rheumatoid arthritis
• decrease relapse in multiple sclerosis

Adverse and Side Effects

• tremor, headache, seizures, depression, confusion, hallucinations, high
blood pressure, hirsutism, acne, oily skin, tinnitus, hearing loss, elevated
blood glucose, gynecomastia, decreased serum bicarbonate, elevated
potassium and magnesium, nausea, vomiting, diarrhea, gingival
hyperplasia, anorexia, nephrotoxicity, anemia, leukopenia,
thrombocytopenia, sinusitis, sore throat, lymphoma, leg cramps, fever,
chills, edema, weight loss

Contraindications
• lactation
• pregnancy
• allergy to these drugs
• liver or kidney disease
 Client Education
• can take with food
• do not breast-feed
• excess hair will go away when you stop taking the drug
• drugs should be taken on same schedule each day to maintain drug levels

Monoclonal • muromonab CD3, adalimubab, alemtuzmab, basiliximab, bevacizumab,

Antibodies cetuximab, daclizumab, efalizumab, erlotinib, gemtuzumab,
ibritumomab, infliximab, natalizumab, omalizumab, palivizumab,
pegaptanib, rituximab, trastuzumab

Pharmacodynamics
• block specific receptor sites in the immune system
• muromonab-CD3 acts as an antibody to T cells and inactivates them, thus
suppressing the immune system

Pharmacotherapeutics
• prevention of rejection in kidney, heart and liver transplants
• respiratory syncitial virus (RSV), Chron’s disease, relapsed follicular B cell
non-Hodgkin’s lymphoma, breast cancer tumors that over-express human
epidermal growth factor receptor 2 protein, B cell chronic lymphocytic
leukemia, colorectal cancer, plaque psoriasis, relapsing forms of multiple
sclerosis, asthma, and neurovascular age-related macular degeneration

Adverse and Side Effects

• tremor, elevated heart rate, diarrhea, nausea, vomiting, wheezing,
difficulty of breathing, chest pain, pulmonary edema, chills, fever, risk of
Pneumocystis carinii, Legionella, Crytococcus, Serratia, Cytomegalovirus,
Herpes simplex

Contraindications
• overload of fluid
• allergy to these drugs

Client Education
• do not become pregnant while on drug therapy or for 3 months after
ending the therapy
• notify physician of fever, infection, nausea, vomiting, wheezing or chest
pain
• eat small, frequent meals to keep weight stable

Vaccines

✓ immunizations containing weakened or altered protein antigens that

stimulate the formation of antibodies against a specific disease
✓ used to promote active immunity
 ✓ can be made from chemically inactivated microorganisms or from live or
weakened viruses or bacteria

Therapeutic Actions and Indications

• stimulate active immunity in people who are at high risk for development
of a particular disease
• the vaccine needed for a patient depends on the exposure the person will
have to the pathogen

Contraindications and Cautions

• contraindicated in the presence of immune deficiency, during pregnancy,
with known allergy to any components of the vaccine, or in patients who
are receiving immune globulin or who have received blood or blood
products within the last 3 months
• caution should be used any time a vaccine is given to a child with a
history of febrile convulsions or cerebral injury, or in any condition in
which a potential fever would be dangerous and in the presence of any
acute infection

Adverse Effects
• associated with the immune or inflammatory reaction that is being
stimulated: moderate fever, rash, malaise, chills, fretfulness, drowsiness,
anorexia, vomiting, and irritability
• pain, redness, swelling and even nodule formation at the injection site
• hypersensitivity reactions in rare instances

Drug Interactions
• should not be given with any immunosuppressant drugs, including
corticosteroids
Bacilli Calmette- prevention of tuberculosis with high risk of exposure
Guerin (BCG)
Haemophilus immunization of children against H. influenzae type b and hepatitis B infections
Influenzae B
conjugate vaccine
and Hepatitis B
Surface Antigen
Pneumococcal immunization against pneumococcal infections
Vaccine
Diphtheria and immunization of adults and children against diphtheria and tetanus
Tetanus Toxoids
Human prevention of diseases caused by oncogenic HPV types 16 and 18 in female ages
Papillomavirus 10-25 y.o.
(HPV)
recombinant
vaccine, bivalent
types 16 and 18
 Varicella Virus immunization against chicken pox infections in adults and children more than or
Vaccine equal to 12 months of age.

Immune Sera

✓ passive immunity can be achieved by providing preformed antibodies to a

specific antigen; these antibodies are found in immune sera, which may
contain antibodies to toxins, venins, bacteria, viruses, or even red blood
cell antigen factors
✓ sera that contain antibodies to specific bacteria or viruses

Therapeutic Actions and Indications

• used to provide passive immunity to a specific antigen
• may be used as prophylaxis against specific diseases after exposure in
patients who are immunosuppressed
• used to lessen the severity of a disease after known or suspected
exposure

Contraindications and Cautions

• history of severe reaction to any immune sera or to products similar to
the components of the sera
• should be used with caution during pregnancy, in patients with
coagulation defects, or thrombocytopenia, or in patients with a known
history of previous exposure to the immune sera

Adverse Effects
• attributed either to the effect of immune sera on the immune system
(rash, nausea, vomiting, chills, fever) or to allergic reactions (chest
tightness, falling blood pressure, difficulty breathing)
• local reactions such as swelling, tenderness, pain, or muscle stiffness at
the injection site, are very common
Antithymocyte treatment of renal transplant acute rejection in conjunction with
immune globulin immunosuppression
Cytomegalovirus attenuation of primary cytomegalovirus disease after renal transplantation
immune globulin
Hepatitis B postexposure prophylaxis against hepatitis B
immune globulin
Lymphocyte management of allograft, rejection in renal transplantation; treatment of aplastic
immune globulin anemia
Rabies immune protection against rabies in nonimmunized patients exposed to rabies
globulin