copyright © 2012, 2007, 2004 by saunders, an imprint of elsevier inc. all rights reserved. 1...

Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 1

Chapter 26Chapter 26

Antiinflammatories and AntihistaminesAntiinflammatories and Antihistamines


ObjectivesObjectives

List both generic and trade drug names List both generic and trade drug names covered in this chapter.covered in this chapter.

Describe the symptoms of inflammation.Describe the symptoms of inflammation. Differentiate between steroidal and Differentiate between steroidal and

nonsteroidal antiinflammatories.nonsteroidal antiinflammatories. List the major side effects of the agents List the major side effects of the agents

discussed.discussed.


Objectives Objectives (cont’d)(cont’d)

List the major cells that are activated List the major cells that are activated from the immune system to repair from the immune system to repair damaged cells.damaged cells.

List the major inflammatory List the major inflammatory conditions.conditions.

List the drug action of pain receptors.List the drug action of pain receptors.


Objectives Objectives (cont’d(cont’d))

List the major medications used in the List the major medications used in the treatment of arthritis, rheumatoid treatment of arthritis, rheumatoid arthritis, osteoarthritis, and other major arthritis, osteoarthritis, and other major conditions.conditions.


The Inflammatory The Inflammatory ResponseResponse

InInflammation can be caused by flammation can be caused by infection, allergic reactions, or injury. infection, allergic reactions, or injury.

Inflammation is a necessary response Inflammation is a necessary response for healingfor healing

Inflammation and pain run hand in handInflammation and pain run hand in hand

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AspirinAspirin England, 1800s—bark from willow tree England, 1800s—bark from willow tree

effective for pain, fever, inflammation.effective for pain, fever, inflammation. Aspirin is Aspirin is acetylsalicylic acid-ASAacetylsalicylic acid-ASA.. The first company to market Aspirin was The first company to market Aspirin was

Bayer Company in 1899.Bayer Company in 1899. Still popular due to Still popular due to effectiveness and low effectiveness and low

costcost


Aspirin Aspirin (cont’d)(cont’d)

Used to treat Used to treat pain, fever, inflammation, anpain, fever, inflammation, and d goutgout

Aspirin should Aspirin should not be given to childrennot be given to children.. Aspirin causes Aspirin causes Reye’s syndromeReye’s syndrome: vomiting, : vomiting,

lethargy, encephalopathy (leads to coma lethargy, encephalopathy (leads to coma and death).and death).

Side effect can be upset stomach.Side effect can be upset stomach. If taken with anticoagulants, increased If taken with anticoagulants, increased

bleeding.bleeding.


Aspirin Aspirin (cont’d)(cont’d)

Most common uses: prevention of strokes Most common uses: prevention of strokes or heart attacks.or heart attacks.

Aspirin decreases platelet aggregation Aspirin decreases platelet aggregation (clotting). (clotting).

Dose to decrease blood clotting isDose to decrease blood clotting is8181 to to 325 mg/day325 mg/day..


NSAIDsNSAIDs NSAIDs (NSAIDs (NoNonsteroidal Antiinflammatory nsteroidal Antiinflammatory

DrugsDrugs) ) have have analgesic, antipyretic, analgesic, antipyretic, antiinflammatoryantiinflammatory properties. properties.

Are available in prescription and OTC Are available in prescription and OTC forms.forms.

Are used for mild or moderate pain.Are used for mild or moderate pain.


Common OTC NSAIDsCommon OTC NSAIDs

Motrin/ibuprofenMotrin/ibuprofen Aleve/naproxenAleve/naproxen


NSAIDsNSAIDs (cont’d)(cont’d)

NSAIDs used to treat muscle pain, NSAIDs used to treat muscle pain, rheumatoid arthritis, bone pain, PMS.rheumatoid arthritis, bone pain, PMS.

Overuse can worsen stomach problems Overuse can worsen stomach problems (GERD).(GERD).

Take with food.Take with food. Do not take with anticoagulants.Do not take with anticoagulants.


Cyclooxygenase (COX)Cyclooxygenase (COX)

Responsible for synthesizing Responsible for synthesizing prostaglandins which are responsible for prostaglandins which are responsible for pain and inflammationpain and inflammation

COX-1COX-1 (protects gastric mucosa (protects gastric mucosa and and promotes platelet aggregation)promotes platelet aggregation)

COX-2 COX-2 (found at sites of tissue injury and (found at sites of tissue injury and in the brain)in the brain)


Cyclooxygenase-2 Cyclooxygenase-2 InhibitorsInhibitors

First-generation NSAIDsFirst-generation NSAIDs Inhibit CInhibit COX-1OX-1 and and COX-2COX-2——decrease in decrease in

inflammation, pain, feverinflammation, pain, fever Negative effect of inhibiting COX-1—gastric Negative effect of inhibiting COX-1—gastric

erosion, ulceration, bleeding, renal damageerosion, ulceration, bleeding, renal damage

Second-generation NSAIDs—COX-2 Second-generation NSAIDs—COX-2 selectiveselective Reduce inflammation, pain, fever without side Reduce inflammation, pain, fever without side

effects of COX-1 inhibitorseffects of COX-1 inhibitors


COX inhibitorsCOX inhibitors

COX-1 inhibitors taken off the market-too COX-1 inhibitors taken off the market-too dangerousdangerous

Most common COX-2 inhibitor- Most common COX-2 inhibitor- Celebrex/celecoxibCelebrex/celecoxib

Auxiliary labels- Auxiliary labels- ““May Cause Dizziness or drowsiness”;May Cause Dizziness or drowsiness”;““Take with food or milk”; Take with food or milk”; ““Do not crush or chew capsules”Do not crush or chew capsules”


Steroids Steroids Steroids are produced naturally by the Steroids are produced naturally by the

bodybody Main gland-adrenal glandMain gland-adrenal gland Used to Used to decrease inflammationdecrease inflammation in in

conditions like RA, OA, asthma, cancerconditions like RA, OA, asthma, cancer High dosesHigh doses can cause decreased can cause decreased

immune response, increased appetite, immune response, increased appetite, bruising, insomnia, restlessness, anxiety, bruising, insomnia, restlessness, anxiety, hypotension, headachehypotension, headache


Serious side effects—if taken over long Serious side effects—if taken over long period of time, taken inappropriately, or period of time, taken inappropriately, or stopped abruptly. stopped abruptly.

Discontinuing a steroid must be done Discontinuing a steroid must be done slowly.slowly.


Steroids (cont’d)Steroids (cont’d)

To treat asthma-steroids (corticosteroids) To treat asthma-steroids (corticosteroids) available in inhalant or parenteral formsavailable in inhalant or parenteral forms

Cause bronchodilationCause bronchodilation Auxiliary label: Shake Well on InhalersAuxiliary label: Shake Well on Inhalers


Common SteroidsCommon Steroids

prednisoneprednisone hydrocortisonehydrocortisone methylprednisolonemethylprednisolone


Controlled AnalgesicsControlled Analgesics

Opiods: to treat paOpiods: to treat painin

Oxycodone, Duragesic (fentanyl), Oxycodone, Duragesic (fentanyl), Vicodin, Percocet, Vicodin, Percocet, Tylenol w/ CodeineTylenol w/ Codeine

May be combined with NSAIDs to May be combined with NSAIDs to intensify their effectsintensify their effects


AntihistaminesAntihistamines

Histamine causes allergic responses Histamine causes allergic responses when antigen is found in the bodywhen antigen is found in the body

Allergic response can become Allergic response can become anaphylactic shock=deathanaphylactic shock=death

Antihistamines block histamine receptorsAntihistamines block histamine receptors


HistamineHistamine11

HH1 1 receptors are found in the lower resp. receptors are found in the lower resp.

tract and skin-tract and skin- When histamine binds with HWhen histamine binds with H11 receptors= receptors=

coughing, sneezing, wheezing, urticaria coughing, sneezing, wheezing, urticaria (rash), bronchiolar constriction(rash), bronchiolar constriction


Histamine2Histamine2

H2 receptors are located in GI tract-H2 receptors are located in GI tract- When histamine binds with H2 When histamine binds with H2

receptors= nausea, vomiting, diarrhea, receptors= nausea, vomiting, diarrhea, crampscramps


Allergic Conditions and Allergic Conditions and Their TreatmentTheir Treatment

OTC drugs used for short-term relief.OTC drugs used for short-term relief. First-generation antihistamines:First-generation antihistamines:

Nonspecific—bind both HNonspecific—bind both H11 and H and H22

Cause sedation (affect CNS)Cause sedation (affect CNS) Decrease nausea, vomiting, motion sickness.Decrease nausea, vomiting, motion sickness.

EX: Benadryl/diphenhydramineEX: Benadryl/diphenhydramine


Allergic Conditions and Allergic Conditions and Their Their Treatment Treatment (cont’d)(cont’d)

Second-generation antihistaminesSecond-generation antihistamines Affect HAffect H11 only only

Cromolyn (inhaled), Allegra/fexofenadine, Cromolyn (inhaled), Allegra/fexofenadine, Zyrtec/cetirizine taken to Zyrtec/cetirizine taken to preventprevent allergic allergic responses.responses.


Antihistamine and Antihistamine and Combination DrugsCombination Drugs

Used to decrease inflammation and Used to decrease inflammation and irritation from allergens.irritation from allergens. Some antihistamines are combined with Some antihistamines are combined with

decongestants.decongestants.

Work best when taken before an allergic Work best when taken before an allergic reaction. reaction.

There are OTC nasal sprays and drops. There are OTC nasal sprays and drops. Steroids used.Steroids used.


Drug InteractionsDrug Interactions

Do not consume alcohol with antihistaminesDo not consume alcohol with antihistamines—will increase—will increase drowsiness.drowsiness.

Antibiotics—macrolidesAntibiotics—macrolides (Erythromycin) (Erythromycin), , ketoconazole, itraconazole—intensify ketoconazole, itraconazole—intensify effects of second-generationeffects of second-generation antihistamines.antihistamines.

Only non-drowsy OTC is Claritin.Only non-drowsy OTC is Claritin.


AnaphylaxisAnaphylaxis

Most severe reactions cause swelling of Most severe reactions cause swelling of airways.airways.

Epinephrine given by inhalation, injection Epinephrine given by inhalation, injection to open airways.to open airways.

copyright © 2012, 2007, 2004 by saunders, an imprint of elsevier inc. all rights reserved. 1...

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