Transcript Chapter 2 Law and Ethics of Pharmacy Teresa Hopper

Chapter 25
Antiinflammatories
and Antihistamines
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
1
Introduction



Many medications available OTC
for inflammation
Muscle pain—leading cause of pain from
inflammation
OTC—NSAIDs and analgesics
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
2
Objectives




List both generic and trade drug names
covered in this chapter.
Describe the symptoms of inflammation.
Differentiate between steroidal and
nonsteroidal antiinflammatories.
List the major side effects of the agents
discussed.
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
3
Objectives (Continued)



List the major cells that are activated from
the immune system to repair damaged
cells.
List the major inflammatory conditions.
List the drug action of pain receptors.
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
4
Objectives (Continued)



List the major medications used in the
treatment of arthritis, rheumatoid arthritis,
osteoarthritis, and other major conditions.
Describe the symptoms of asthma and the
classifications of drugs used to treat
asthma.
Explain the use of inhalers as opposed to
nebulizers and when they are used.
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
5
Inflammation




Caused by infection, allergic reactions,
injury
Necessary for body to heal itself
Roman symptoms: redness, swelling, heat,
pain, loss of function
Body self-repair: blood, cells, natural
chemicals
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
6
Inflammation (Continued)



Chemicals cause vasodilation: blood
rushes in, and the area becomes warmer
Edema occurs in damaged areas that
cannot accommodate influx of blood
For immune system responses to injury,
see Table 25-1
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
7
Inflammation (Continued)




Cyclooxygenase: enzyme that produces
prostaglandin
Prostaglandins responsible for
inflammation, pain, increased temperature
Aspirin inhibits cyclooxygenase;
stops production of prostaglandin
Inflammation occurs only in living tissue
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
8
Inflammation (Continued)

Two types:
 Acute—lasts
a few days
 Chronic—can arise from an acute case
or an injury; causes damage to affected
sites or internal organs

Body heals—scar tissue forms (can alter
normal workings of the body system)
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
9
Glucocorticoids (Steroids)

Steroids:

Secreted from endocrine glands
 Chemical messengers of the body
 Main gland: adrenal gland
 Adrenal cortex produces glucocorticoids,
mineralocorticoids
 Corticotropin—anterior pituitary gland
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
10
Glucocorticoids (Steroids) (Continued)

Two effects on body:
 Physiological (low doses)
 Pharmacological (high doses)
Decrease inflammation, asthma, cancer,
suppress immune system of cancer patients
 Serious side effects—if taken over long
period of time, taken inappropriately,
stopped abruptly

Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
11
Glucocorticoids (Steroids) (Continued)

Drug action of high-dose steroids:

Glucocorticoid therapy affects protein, fat,
glucose metabolism
 Overall effect: reduces muscle mass, bone
density, thinning of skin; fat redistribution
leads to “moon face”
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
12
Glucocorticoids (Steroids) (Continued)



Adverse effects if secretion prolonged
Stressful events, surgery, high doses
cause suppression of lymphocytes, lower
resistance to infections
Other side effects: increased appetite,
increased bruising, insomnia,
restlessness, anxiety, hypotension,
headache
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
13
Osteoarthritis (Degenerative Joint Disease)




Common type of arthritis; painful
Degradation of cartilage, overgrowth
of bones
Wear and tear on bone: extreme pain
Treatment: medication, synovectomy,
arthroplasty
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
14
Rheumatoid Arthritis





Painful and bone-deforming
Affects more women than men
Also affects young adults (20 to 30 yrs)
Possibly viral
Cause within the immune system
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
15
Rheumatoid Arthritis (Continued)


Treatment: physical therapy, medications
(antiinflammatories or analgesics), diet
Removal of excess synovial fluid relieves
pain and joint damage
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
16
Pain




Most pain lasts only a short time
Chronic pain—persistent; lasts for 3 months
or longer
Severity: scale 1 to 10
Acute pain lasts few weeks (muscle and
tendon)
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
17
Asthma




Chronic inflammatory disorder of airways
Can occur in childhood or adulthood
Causes: smoking, cold or flu, animal dander,
environmental contaminants, stress
Airway exposed to irritant: mast cells,
T lymphocytes, neutrophils, epithelial altered
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
18
Asthma



(Continued)
Inflammation of lining—constriction of
bronchioles—can cause death if not
treated
Acute attack—anaphylaxis
No cure
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
19
Allergic Mechanism



Body contact with antigen produces
immunoglobulin E (IgE) antibodies
attached to mast cells (first exposure)
Histamine-1 receptors found in respiratory
tract and skin
Histamine-2 receptors—GI tract
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
20
Allergic Mechanism (Continued)


Second exposure—antigen binds to
IgE antibodies on mast cells—histamine
released—allergic response
Coughing, sneezing, wheezing, rash,
decreased BP, migraine headache,
bronchiolar constriction, increased
heart rhythm, anaphylactic shock
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
21
Antihistamine Reactions



Bind to histamine receptor sites
Antihistamine drugs block histamine-1
receptors
Found in cold and cough preparations (dry
secretions)
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
22
Antihistamine Reactions (Continued)


Histamine-2—GI tract
Histamine-2 blockers—H2 antagonists,
block receptors sites in GI tract
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
23
Antihistamine Reactions (Continued)

First-generation antihistamines
 Nonspecific—bind
both H1 and H2
 Cause sedation (affect CNS)
 Decrease
sickness

nausea, vomiting, motion
Second-generation antihistamines
 Affect
H1 only
 Cromolyn, fexofenadine, cetirizine taken to
prevent allergic responses
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
24
Antihistamine Agents
Trade
Generic
Dosage Form
Uses
Benadryl*
Diphenhydramine
Chlor-Trimeton*
Chlorpheniramine
Allergies,
sedation
Allergies
Tavist 1.25* 2.68†
Phenergan†
Clemastine
Promethazine
suppositories,
Cap, tab, soln(s),
injection
Tab, syrup,
injection
Tab, syrup
Tab, syrup,
sedation,
injection
motion
Atarax, Vistaril†
Hydroxyzine
injection
antiemetic (IV)
Second-Generation Drugs
Claritin*
Loratadine
Zyrtec†
Cetirizine
Tab, cap, syrup,
sedation (PO),
Tab, syrup
Tab, syrup
Allergies
Allergies,
antiemetic,
sickness
Allergies,
Allergies
Allergies
Cap, Capsule; tab, tablet. *OTC †Rx
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
25
The History of Aspirin




England, 1800s—bark from willow tree
effective for pain, fever, inflammation
Active ingredients isolated
Henri Leroux discovered bitter glycoside
(salicin) responsible for medicinal
properties
Aspirin—acetylsalicylic acid
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
26
The History of Aspirin (Continued)




Salicin inhibits prostaglandins
Prostaglandins: hormone-like chemicals;
cause inflammation, pain, elevated
temperature with injury
Salicin used for gout, inflammation from
injury, pain, high fever
In 1899 Bayer Company began to market
aspirin
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
27
What Is Aspirin Used for?


Aspirin should not be given to children
Causes Reye’s syndrome: vomiting,
lethargy, encephalopathy (leads to coma
and death)

Side effect: upset stomach

If taken with anticoagulants—increased
bleeding
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
28
What Is Aspirin Used for? (Continued)





Most common uses: prevention of strokes
or heart attacks
Aspirin decreases platelet aggregation
(clotting)
Clot in brain: stroke
Clot in vessels of heart: heart attack
Clot in lungs: pulmonary embolism
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
29
What Is Aspirin Used for? (Continued)


Dose to decrease blood clotting:
81−325 mg/day
Anticoagulation medications called “blood
thinners”
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
30
NSAIDs

Analgesic, antipyretic, antiinflammatory
properties

Available in prescription and OTC forms

Used for mild or moderate pain

Positive effects

Drug action: inhibition of cyclooxygenase;
act on hypothalamus for antipyretic effect
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
31
NSAIDs




(Continued)
Used to treat muscle pain, rheumatoid
arthritis, bone pain, PMS
Overuse—worsen stomach problems
(GERD)
Take with food
Do not take with anticoagulants
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
32
Drug Action of Cyclooxygenase

Cyclooxygenase:
 Enzyme
that synthesizes prostaglandins
 Found in all tissues
 Two forms of COX: COX-1, COX-2
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
33
Drug Action of Cyclooxygenase (Continued)

COX-1 manages normal functions
 Protects
gastric mucosa
 Promotes

platelet aggregation
COX-2 manages pain and discomfort
 At
tissue injury sites: sensitizes receptors to
pain, mediates inflammation
 In
brain: affects fever and pain perception
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
34
Drug Action of Cyclooxygenase (Continued)

First-generation NSAIDs
 Inhibit
both COX-1 and COX-2—decrease
in inflammation, pain, fever
 Negative effect of inhibiting COX-1—gastric
erosion, ulceration, bleeding, renal damage

Second-generation NSAIDs—COX-2
selective
 Reduce
inflammation, pain, fever without
side effects of COX-1 inhibitors
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
35
Adrenal Effects of Steroid Agents



Glucocorticoids—essential to wellness of
body
Problem of long-term use—decreased
ability of body to produce own
glucocorticoids; may stop all together
Discontinuation—taper dose over a month
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
36
Prednisone Taper Prescription
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
37
Adrenal Effects of Steroid Agents (Continued)




Several routes of administration—oral,
parenteral (IV), intramuscular (IM),
subcutaneous (SC), topical inhalation
Prescriptions—written for smallest effective
dose and least amount of time necessary
Side effects—oral dosages—GI upset
Take with food
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
38
Agents Used to Treat Pain


Pain from inflammation: variety of
medications, NSAIDS
CII, CIII
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
39
Agents Used to Treat Asthma






Most common: beta-adrenergic agonists
Used with bronchodilators (corticosteroids)
Effects: dilation of bronchial artery
Short- and long-acting agents
Dosage forms: inhalant, parenteral
Other agents: anticholinergics
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
40
Agents Used to Treat Asthma (Continued)


Most common route: inhalation
Two methods of inhalation:
 Nebulizer
 Metered-dose

inhalant
Sympathomimetics reduce inflammation of
bronchi; relieve spasm within smooth
muscle of airway
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
41
Agents Used to Treat Asthma (Continued)




Affect alpha-receptors
(smooth muscle of lungs)
Beta-receptors—heart
Treat bronchitis, emphysema, asthma
Side effects: lightheadedness, increased
heart rate
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
42
Xanthine Agents



Works on smooth muscle of bronchioles
Aminophylline, theophylline—oral and
parenteral forms
Indications—symptomatic relief for
prevention of bronchial asthma and other
disorders
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
43
Leukotrienes



Cause smooth muscle of bronchi to
contract, causing labored breathing
Zafirlukast, montelukast, zileuton decrease
bronchoconstriction of airways
Prevent asthma attacks caused by pollen,
dander, cold air, other antigens
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
44
Corticosteriods




Not to be used over a long period of time
Short-term treatment of asthma
Special dosing requirements
All metered-dose inhalers—need “shake
well” auxiliary label
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
45
Cromolyn Sodium




Only antiasthmatic and antiallergic agent
Prevents mast cells from releasing
histamine
Inhaled via metered-dose inhaler, ebulizer,
or nasal inhaler
Prevents allergic reactions if taken before
contact with allergen
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
46
Nebulizers



Treatment given by respiratory therapist in
hospital or at home with proper training
Metaproterenol, albuterol—unit dose
containers—deliver only one dose
Drug inhaled via nose and mouth mask
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
47
Prevention of Anaphylaxis


Most severe reactions cause swelling of
airways
Epinephrine given by inhalation, injection
to open airways
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
48
Allergy Agents (Antihistamines)


Used to decrease inflammation and
irritation from allergens
Allergens also known as antigens- capable
of stimulating an immune response
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
49
Types of Antigens
Manmade
Chemicals
Detergents, cleaners
Topical agents such
as soaps, lotions,
creams
Drugs
Natural Occurring
Chemicals
Venom from snake
bites or bee stings
Heavy molecular weight
compounds such
as blood or Dextran
Pollen
Miscellaneous
Dust
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
Large
lacerations
Animal dander
50
Drug Interactions


Do not consume alcohol with
antihistamines—will increase drowsiness
Antibiotics—macrolides, ketoconazole,
itraconazole—intensify effects of secondgeneration antihistamines
Copyright © 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved.
51