Discussion Main Pharmacy
Topic Option 1: Let’s say John calls into the office and is requesting a refill for his prescription narcotic, Percocet. He just received a 30-day supply of Percocet less than two weeks ago. He becomes irate that it cannot be filled. How should you handle John’s phone call? Should you make the doctor aware he is already out of his Percocet? What schedule drug does Percocet fall into? What are the potential dangers with John’s situation?
DeVore, A. (2015). The electronic health record for the physician’s office. St. Louis, MO: Elsevier.Essentials of Pharmacology for Health Professions
Eighth Edition
Chapter 16
Gastrointestinal Drugs
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1
Introduction (1 of 2)
Gastrointestinal drug categories
Antacids
Drugs for treatment of ulcers and gastroesophageal reflux disease (GERD)
Antispasmodics
Management of inflammatory bowel disease
Antidiarrheal agents
Antiflatulents
Laxatives and cathartics
Antiemetics
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Introduction (2 of 2)
The following slides discuss various gastrointestinal drugs
Refer to the chapter for specific side effects, contraindications, and interactions
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Antacids
Act by partially neutralizing gastric hydrochloric acid
Widely available in many over-the-counter (OTC) preparations for the relief of indigestion, heartburn, and sour stomach
Generally have a short duration of action, requiring frequent administration
May contain aluminum, calcium carbonate or magnesium and sodium
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Agents for Treatment of Ulcers and GERD (1 of 3)
H2-blockers
Reduce gastric acid secretion by acting as histamine2 blockers (Example: Pepcid)
Reduce gastric acid released in response to stimuli
Proton pump inhibitors (PPI)
May be used long-term for severe GERD, to prevent NSAID-induced ulcers, and for hypersecretory conditions
Omeprazole: gastric antisecretory agent
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Agents for Treatment of Ulcers and GERD (2 of 3)
Gastric mucosal agents
Misoprostol (Cytotec)
Synthetic form of prostaglandin E1
Inhibits gastric acid secretion and protects the mucosa from the irritant effect of certain drugs
Sucralfate (Carafate)
Inhibitor of pepsin, given on an empty stomach
Reacts with HCl to form a paste that adheres to the mucosa, protecting the ulcer from irritation
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Agents for Treatment of Ulcers and GERD (3 of 3)
Helicobacter pylori treatment
Bacterial infection
Treated successfully with multiple-drug regimens (over 14 days).
See Chapter 17
See Table 16-1
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Antispasmodics/Anticholinergics
Help to calm the bowel
Work by decreasing motility (smooth muscle tone) in the GI tract
Dicyclomine (Bentyl)
Used for treatment of irritable bowel syndrome and other functional disturbances of GI motility
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Agents for Inflammatory Bowel Disease
Inflammatory bowel disease (IBD)
Chronic condition that causes inflammation in the lining of the GI tract
Includes Crohn’s disease and ulcerative colitis
Salicylates
Designed to reach the ileum and colon, bypassing the stomach and upper intestines
Examples: mesalamine and sulfasalazine used for Crohn’s disease and ulcerative colitis
Glucocorticoids
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Antidiarrheal Drugs (1 of 3)
Act in various ways
Reduce the number of loose stools
Patients experiencing diarrhea are instructed to stay hydrated
Salicylates
Bismuth subsalicylate (e.g., Kaopectate, Pepto-Bismol) has anti-infective and antisecretory properties, a direct mucosal protective effect, and weak antacid and anti-inflammatory effects
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Antidiarrheal Drugs (2 of 3)
Opiate agonists
Act by slowing intestinal motility, allowing for more reabsorption of fluid
Example: Loperamide
Probiotics
Living microorganisms that can alter a patient’s intestinal flora; may provide benefit in numerous GI diseases
Lactobacillus
Saccharomyces boulardii (Florastor)
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Antidiarrheal Drugs (3 of 3)
Clostridium difficile infection
One of the most common causes of infectious diarrhea in the United States
Symptoms include watery diarrhea, nausea, and/or abdominal pain or tenderness
Caused by eradication of native intestinal flora with broad-spectrum antimicrobials and overuse of PPI and H2-blocker therapy
Oral medications include metronidazole (Flagyl) or vancomycin
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Antiflatulents
For the symptomatic treatment of gastric bloating and postoperative gas pains
Help to break up gas bubbles in the GI tract
Simethicone
See Table 16-2
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Laxatives and Cathartics (1 of 4)
Laxatives promote evacuation of the intestine and are used to treat constipation
Included in this category are cathartics, or purgatives
Promote rapid evacuation of the intestine and alteration of stool consistency
Divided into seven categories according to action (see Chapter text for list)
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Laxatives and Cathartics (2 of 4)
Bulk-forming laxatives
Soften the stool by absorbing water and increase fecal mass to facilitate defecation
Stool softeners
Surface-acting agents that moisten stool through a detergent action
Emollients
Promote stool movement through the intestines by softening and coating the stool
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Laxatives and Cathartics (3 of 4)
Saline laxatives
Promote secretion of water into the intestinal lumen
Should be taken infrequently, in single doses
Stimulant laxatives
Cathartic in action; produce strong peristaltic activity; may alter intestinal secretions in several ways
Produce some degree of abdominal discomfort
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Laxatives and Cathartics (4 of 4)
Osmotic laxatives
Exert an action that draws water from the tissues into the feces and reflexively stimulates evacuation
Chloride channel activator
Lubiprostone increases intestinal fluid secretion by activating chloride channels in the epithelium
Mu-opioid receptor agonist
Opioid induced constipation
See Table 16-3
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Antiemetics (1 of 4)
For the prevention or treatment of nausea, vomiting, vertigo, or motion sickness
Many different products are available, varying in their actions, condition treated, and route of administration
See Table 16-4
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Antiemetics (2 of 4)
Anticholinergics
Dimenhydrinate (Dramamine) or scopolamine: for the treatment of motion sickness
Available in a transdermal patch
Meclizine (Antivert): antihistamine for the prevention and treatment of nausea, vomiting, and/or vertigo associated with motion sickness
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Antiemetics (3 of 4)
Antidopaminergics
Dopamine receptor antagonists interfere with the stimulation of chemoreceptor trigger zone (CTZ) in the brain, thereby blocking messages to the GI tract
Most frequently used agents to control nausea and vomiting in this class:
Prochlorperazine (Compazine): no longer marketed, caused extrapyramidal reactions
Phenergan, Reglan
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Antiemetics (4 of 4)
Serotonin receptor antagonists
Preferentially block serotonin receptors found centrally in the CTZ and peripherally in the intestines to control emesis
Serotonin is a major neurotransmitter involved in emesis located in the gut
Ondansetron (Zofran) and dolasetron (Anzemet)
For the prevention and treatment of post-operative (PONV) and chemotherapy-induced nausea and vomiting (CINV)
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Essentials of Pharmacology for Health Professions
Eighth Edition
Chapter 17
Anti-infective Drugs
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22
Introduction
Treatment of infection
Complicated by the great variety of medications available and their differing modes of action
First step: identify the causative organism and specific medication to which it is sensitive
Culture and sensitivity (C&S) tests
Wound, throat, urine or blood
Usually not available for 24-48 hours
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Resistance (1 of 2)
Organisms may build up resistance to drugs and are therefore, no longer effective because of:
Frequent use
Incomplete treatment
Anti-infective resistance is caused by many factors
Complex strategies needed to combat the problem
Seventy percent of bacteria that cause HAI’s are resistant to at least one drug
Example: MRSA
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Resistance (2 of 2)
Selection of anti-infective drugs
Infection site
Status of hepatic and/or renal function
Patient age
Pregnancy or lactation
Likelihood of organisms developing resistance
Known allergy to the anti-infective drug
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Adverse Reactions
Three categories
Allergic hypersensitivity
Over-response of the body to a specific substance (anaphylaxis)
Direct toxicity
Results in tissue damage
Indirect toxicity or superinfection
Manifested as a new infection due to absence of normal flora in the intestines or mucous membranes
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Vaccines/Immunizations
Centers for Disease Control and Prevention (CDC)
Currently recommends routine vaccination
Prevent 17 vaccine-preventable diseases that occur in infants, children, adolescents, or adults
Information regarding vaccines and immunizations changes from time to time and requirements may vary by state, territory, or country
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Antibiotics
Refers to a large spectrum of medicines that are useful for treating and preventing infections by bacteria.
No effect on viruses, fungal or other types of infection
Improper use causes resistance
Side effects, precautions, contraindications and interactions are listed for each drug. Refer to the Chapter text.
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Aminoglycosides
Treats many infections caused by:
Gram-negative bacteria (e.g., Escherichia coli and Pseudomonas)
Gram-positive bacteria (e.g., Staphylococcus aureus)
Effective in short-term treatment of many serious infections
Septicemia (e.g., bacteria in bloodstream causing low blood pressure) when less toxic drugs are ineffective or contraindicated
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Cephalosporins
Semisynthetic beta-lactam antibiotic derivatives produced by a fungus
Related to penicillins
Some patients allergic to penicillin are also allergic to cephalosporins
Classified as first, second, third, or fourth, or fifth generation
According to organisms susceptible to their activity
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Macrolides
Treats many infections of the respiratory tract, skin conditions, or for some sexually transmitted infections
Considered among the least toxic antibiotics
Preferred for treating susceptible organisms under conditions in which more toxic antibiotics might be dangerous
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Penicillins
Beta-lactam antibiotics produced from certain species of a fungus
Treats many streptococcal and some staphylococcal and meningococcal infections
Drug of choice for treatment of syphilis
Used prophylactically to prevent recurrences of rheumatic fever
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Carbapenems
Belong to the beta-lactam class of antibiotics
Have a very broad spectrum of activity against gram-negative and gram-positive organisms
Primary treatments include pneumonia, febrile neutropenia, intra-abdominal infections, diabetic foot infections, and significant polymicrobial infections
See Table 17-1
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Quinolones
For adult treatment of some infections of the urinary tract, sinuses, lower respiratory tract, GI tract, skin, bones, and joints, and in treating gonorrhea
Some organisms are showing increased resistance
Reserve for infections that require therapy with a fluoroquinolone
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Tetracyclines
Broad-spectrum antibiotics
Treats infections caused by Lyme disease, rickettsia, chlamydia, or some uncommon bacteria
Some organisms are showing increasing resistance
Use only when other antibiotics are ineffective or contraindicated
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Antifungals (1 of 3)
Treat specific susceptible fungal disease
Medications are quite different in action and purpose
Amphotericin B
Administered IV for the treatment of severe systemic and potentially fatal infections caused by susceptible fungi, including Candida
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Antifungals (2 of 3)
Fluconazole (Diflucan)
Works against many fungal pathogens, including most Candida, without the serious toxicity of amphotericin B
Micafungin (Mycamine)
Given IV
Provides new treatment options against Candida and Aspergillus species
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Antifungals (3 of 3)
Nystatin
Structurally related to Amphotericin B
Orally treats oral cavity candidiasis
Also used as a fungicide in the topical treatment of skin and mucous membranes
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Antituberculosis Agents
Tuberculosis (TB)
Caused by a bacterium called Mycobacterium tuberculosis, which primarily attacks the lungs
Antituberculosis agents are administered for two purposes
To treat latent or asymptomatic infection (no evidence of clinical disease)
For treatment of active clinical tuberculosis and to prevent relapse
Treatment can be challenging
See Table 17-2
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Miscellaneous Anti-Infectives (1 of 3)
Clindamycin
Treats serious respiratory tract infections, septicemia, osteomyelitis, serious infections of the female pelvis caused by susceptible bacteria, and for Pneumocystis jirovecii pneumonia associated with AIDS
Prophylactic use in dental procedures for penicillin-allergic patients
May be a viable therapeutic option for community-acquired MRSA
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Miscellaneous Anti-Infectives (2 of 3)
Metronidazole (Flagyl)
Synthetic antibacterial and antiprotozoal agent
Effective against protozoa
One of the most effective drugs against anaerobic bacterial infections
Also useful in treating Crohn’s disease, antibiotic-associated diarrhea, rosacea, and H. pylori infection
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Miscellaneous Anti-Infectives (3 of 3)
Vancomycin
Structurally unrelated to other available antibiotics
IV vancomycin is used in the treatment of potentially life-threatening infections caused by susceptible organisms
Drug of choice for MRSA
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Agents for VRE
Linezolid (Zyvox)
Indicated for gram-positive infections
Approved for the treatment of bacterial pneumonia skin, skin structure infections, and MRSA and VRE infections
Effective in treating diabetic foot infections
Administered by IV infusion or orally
See Table 17-3
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Sulfonamides
Among the oldest anti-infectives
Increasing resistance of many bacteria has decreased the clinical usefulness of these agents
Used most effectively in combinations with other drugs
Example: sulfamethoxazole and trimethoprim
Resistance develops more slowly
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Urinary Anti-Infectives
Urinary tract infection (UTI)
Symptomatic inflammatory response from the presence of microorganisms in the urinary tract
One of the most common bacterial infections for which patients seek treatment
First-line urinary anti-infectives for empiric treatment of uncomplicated lower UTI are sulfamethoxazole-trimethoprim and nitrofurantoin
See Table 17-4
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Antivirals
Acyclovir
Primarily treats herpes simplex, herpes zoster (shingles), and varicella zoster (chickenpox) infections
Neuraminidase inhibitors
Indicated for the treatment of uncomplicated acute illness due to influenza types A and B
Ribavirin
Treats infants and young children with respiratory syncytial virus (RSV) infections via nasal and oral inhalation, Lassa fever and Hepatitis C
See Table 17-5
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Treatment of HIV/AIDS Infections (1 of 4)
See Table 17-6
Highly specialized field
Those actively practicing in that field must be updated frequently on the many new medications and frequently changing protocols
Treatment of HIV infection
Consists of using highly active antiretroviral therapy (HAART) combinations of three or more antiretroviral (ARV) agents
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Treatment of HIV/AIDS Infections (2 of 4)
Antiretroviral protease inhibitors (PIs)
Block the activity of the HIV enzyme essential for viral replication late in the virus life cycle
Nucleoside reverse transcriptase inhibitors (NRTIs)
Inhibit an enzyme responsible for viral replication early in the virus life cycle
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Treatment of HIV/AIDS Infections (3 of 4)
Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
Inhibit an enzyme responsible for viral replication early in the viral life cycle
Fusion inhibitors (FIs)
Block entry of HIV into cells, which may keep the virus from reproducing
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Treatment of HIV/AIDS Infections (4 of 4)
CCR5 antagonists
Block a co-receptor required for HIV entry into human cells
Integrase inhibitor
Raltegravir (Isentress): first ARV designed to slow the advancement of HIV infection by blocking the enzyme needed for viral replication
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HIV Information and Resources
Sources of current recommendations for clinical use of antiretrovirals (ARVs)
Department of Health and Human Services
Florida/Caribbean Aids Education and Training Center
AETC National Resource Center Drug Interactions
Johns Hopkins HIV Guide
National HIV Telephone Consultation Service
University of California, San Francisco
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Essentials of Pharmacology for Health Professions
Eighth Edition
Chapter 18
Eye and Ear Medications
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52
Introduction (1 of 2)
Most common eye diseases in Americans 40 years and older
Age-related macular degeneration, glaucoma, cataracts, and diabetic retinopathy
Conjunctivitis: inflammation of the conjunctiva (“pink eye”)
One of the most frequent causes of patient seeking help
Allergens, irritants, abrasion, bacteria and viruses are common causes
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Introduction (2 of 2)
Medications for the eye
Anti-infectives
Anti-inflammatory agents
Antiglaucoma agents
Mydriatics (pupil dilation)
Local anesthetics
The following slides discuss various eye medications
Refer to the chapter for specific side effects, contraindications, and interactions
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Anti-Infectives
Treat superficial eye infections caused by susceptible organisms
Ointments are preferable to drops in children and patients with poor adherence
Drops are preferred in adults
Ointments will cause blurring of vision for 20 minutes after instillation
Determine causative organism when possible
Preparations can be single or in combination
Antivirals
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Anti-Inflammatory Agents (1 of 4)
Relieve eye or conjunctiva inflammation in allergic reactions, burns, postoperatively, or irritation from foreign substances
Corticosteroids
Useful in acute stages of eye injury
Prevent scarring, for severe symptoms, or when condition is unresponsive to other medications
Do not use for extended periods of time
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Anti-Inflammatory Agents (2 of 4)
Nonsteroidal anti-inflammatory drugs (NSAIDs)
Treat postoperative inflammation following cataract surgery
Alternative to corticosteroids if a contraindication exists
Immunologic agents
Increases tear production in patient’s with dry eye
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Anti-Inflammatory Agents (3 of 4)
Antihistamines/decongestants
Block histamine receptors in conjunctiva, relieving ocular pruritis associated allergic conjunctivitis
Cause vasoconstriction of blood vessels, providing relief from minor eye irritation and redness
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Anti-Inflammatory Agents (4 of 4)
Ophthalmic lubricants
Provide a barrier function at the level of the conjunctival mucosa
Help to dilute and flush various allergens and inflammatory mediators that may be present on the ocular surface
See Table 18-1
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Antiglaucoma Agents (1 of 5)
Glaucoma
A group of sight-threatening diseases of the eye in which there is increased intraocular pressure (IOP) due to obstruction of outflow of aqueous humor
Causes deterioration of and damage to the optic nerve resulting in vision loss
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Antiglaucoma Agents (2 of 5)
Glaucoma types
Acute (angle-closure) glaucoma
Characterized by a sudden onset of pain, blurred vision, and a dilated pupil
Considered a medical emergency
Chronic (open-angle) glaucoma
Much more common, often bilateral
Develops slowly over a period of years with few symptoms except a gradual loss of peripheral vision and possibly blurred vision
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Antiglaucoma Agents (3 of 5)
Antiglaucoma drugs given to lower intraocular pressure
Carbonic anhydrase inhibitors: reduce formation of hydrogen and bicarbonate ions
Diuretic effect; reduces production of aqueous humor
Miotics: cause pupil to contract
Reduce IOP by increasing aqueous humor outflow
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Antiglaucoma Agents (4 of 5)
Beta-adrenergic blockers: used topically to lower IOP in open-angle glaucoma
Decreased rate of aqueous humor production
Alpha agonists: decreases formation and increases outflow of aqueous humor
Minimal effects on cardiovascular or pulmonary hemodynamics
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Antiglaucoma Agents (5 of 5)
Prostaglandin analogs: greatest reduction in IOP by increasing outflow of aqueous humor
May be used concomitantly with other topical ophthalmic drugs to lower IOP
See Table 18-2
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Mydriatics
Topically dilates the pupil for ophthalmic examinations
Example: atropine
Also acts as a cycloplegic (paralyzes the muscles of accommodation)
Drug of choice in eye examinations for children
Often used for adults because of fast action and fast recovery time
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Local Anesthetics
Applied topically to the eye for minor surgical and diagnostic procedures, removal of foreign bodies, or painful injury
Example: tetracaine (TetraVisc)
See Table 18-3
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Otic (Ear) Medications (1 of 3)
Made up of three parts: outer, middle and inner
Serve two purposes: hearing and balance
Common ear conditions
Ear infections
Earwax (cerumen) buildup
Otitis media
Bacteria in the middle ear which leads to inflammation
Treatment includes an antibiotic and NSAIDS
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Otic (Ear) Medications (2 of 3)
Topical preparations for ear infections
“swimmers ear” or otitis externa
Cipro, Floxin and Cortisporin are the most common
Prescribed for 7-14 days
Drops that are designed to treat pain and inflammation associated with ear infections
Vosol, Auralgan
Systemic Preparations
Refer to Chapter 17: Amoxicillin and Augmentin
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Otic (Ear) Medications (3 of 3)
Earwax buildup and blockage
Earwax (cerumen) in the canal can inhibit hearing and can cause pain
Most common in older adults
Debrox is an OTC that is used to soften and loosen excessive earwax
See Table 18-4
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Essentials of Pharmacology for Health Professions
Eighth Edition
Chapter 19
Analgesics, Sedatives, and Hypnotics
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Introduction (1 of 2)
Analgesics, sedatives, and hypnotics
Depress central nervous system (CNS) action to varying degrees
Some drugs can be classified into more than one category, depending on the dosage
Analgesics: relieve pain
Sedatives: calm, soothe, or produce sedation
Hypnotics: produce sleep
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Introduction (2 of 2)
The following slides discuss various analgesics, sedatives, and hypnotics
Refer to the chapter for specific side effects, precautions, contraindications, and interactions
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Analgesics (1 of 8)
Pain is the most common reason for patients to seek out medical care
Most common types: back, neck, migraine, and facial or jaw pain
Is subjective: can be experienced or perceived only by the individual subject. Pain scale: 1 to 10
Can be blocked by endorphins
Endogenous analgesics produced within the body as a reaction to severe pain or intense exercise
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Analgesics (2 of 8)
Opioid analgesics
Full or pure agonists, partial agonists, or mixed agonist-antagonists
Each bind to specific receptors with varying degrees of action
Classified as controlled substances
Potential for abuse and psychological dependence
Tolerance and physiological dependence
See Table 19-1
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Analgesics (3 of 8)
Opioid induced constipation (OIC)
Not-self limiting
Occurs because the digestive tract contains similar receptors (mu) that are targeted in pain relief, slowing the transit time
Most of the time, hydration, stool softeners or stimulant are effective
For severe OIC, prescription strength medication is required.
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Analgesics (4 of 8)
Tramadol (Ultram)
Centrally acting synthetic analog of codeine with a dual mechanism of action
Produces analgesia by weak inhibition of norepinephrine and serotonin reuptake; is an opioid receptor agonist
Less potential for abuse or respiratory depression (although both may occur)
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Analgesics (5 of 8)
Nonopioid analgesics
See Table 19-2
Many available without prescription as over-the-counter (OTC) medications
Given for relieving mild to moderate pain, fever, and anti-inflammatory conditions
Used as a coanalgesic in severe acute or chronic pain requiring opioids
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Analgesics (6 of 8)
Salicylates (aspirin) are most commonly used for their analgesic and antipyretic properties, as well as for their anti-inflammatory action
Acetaminophen has analgesic and antipyretic properties, but very little effect on inflammation. (major changes in Tylenol dosing)
Aspirin and acetaminophen are frequently combined with opioids or with other drugs for more effective analgesic action
Nonsteroidal anti-inflammatory drugs (NSAIDS) are discussed in Chapter 21
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Analgesics (7 of 8)
Adjuvant analgesics
May enhance analgesic effect with opioids and nonopioids, produce analgesia alone, or reduce side effects of analgesics
Treatment for nerve pain and fibromylagia
Tricyclic antidepressants
Treats fibromyalgia and nerve pain associated with herpes, arthritis, diabetes, and cancer, migraine or tension headaches, insomnia, and depression
Pain often described as “burning”
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Analgesics (8 of 8)
Anticonvulsants
Examples: Neurontin and Tegretol
Commonly used for management of nerve pain associated with neuralgia, herpes zoster (shingles), and cancer
Implemented when patient describes pain as “sharp,” “shooting,” “shock-like pain,” or “lightning-like”
See Table 19-3
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Local Anesthetic
Lidocaine patch (Lidoderm)
Approved for management of postherpetic neuralgia
Can provide significant analgesia in other forms of neuropathic pain
Diabetic neuropathy and musculoskeletal pain such as osteoarthritis and low back pain
Provides pain relief through a peripheral effect and generally has little, if any, central action
Must be applied to intact skin
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Antimigraine agents
Migraine is the most common neurovascular headache and may include nausea, vomiting, and sensitivity to light and noise.
Simple/opioid analgesics and NSAIDs are effective, especially if taken at initial sign of migraine
Serotonin receptor agonists (SRAs)
Action: serotonin levels decrease, while vasodilation and inflammation of blood vessels in brain increase as migraine symptoms worsen
Effective treatment for nausea and vomiting
See Table 19-4
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Sedatives and Hypnotics (1 of 2)
Medications used to promote sedation in smaller doses, and sleep in larger doses
Insomnia is one of the most prevalent sleep disorders
Antihistamines (Benadryl) and Barbiturates
Benzodiazepines (BZDs) and nonbenzodiazepines
Less abuse potential
Withdrawal effects are observed after long-term use and respiratory depression (when taken with alcohol) can be potentially fatal
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Sedatives and Hypnotics (2 of 2)
Melatonin receptor agonist
Ramelteon (Rozerem): first FDA-approved prescription medication that acts on melatonin receptor
Mimics action of melatonin to trigger sleep onset
Dependence and abuse potential are eliminated
Not classified as a controlled substance
Works quickly, generally inducing sleep in less than one hour
See Table 19-5
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Essentials of Pharmacology for Health Professions
Eighth Edition
Chapter 20
Psychotropic Medications, Alcohol, and Drug Abuse
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85
Introduction (1 of 2)
Psychotropic refers to any substance that acts on the mind
Psychotropic medications are drugs that can exert a therapeutic effect on a person’s mental processes, emotions, or behavior
Classified according to the purpose for administration: CNS stimulants, antidepressants, anxiolytics, antimanic, and antipsychotic medications
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Introduction (2 of 2)
The following slides discuss various psychotropic medications
Refer to the chapter for specific side effects, precautions or contraindications, and interactions
Drug and alcohol abuse is also discussed
Refer to the chapter for specific symptoms and treatment options
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CNS Stimulants (1 of 2)
CNS (central nervous system) stimulant medications
Given to promote CNS functioning
Caffeine
Helps fight fatigue and drowsiness
Examples: NoDoz, Vivarin, and caffeine citrate
Prolonged, high intake of caffeine in any form may produce tolerance, habituation, and psychological dependence
See Table 20-1
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CNS Stimulants (2 of 2)
Amphetamine/methylphenidate preparations
Controlled substances (Schedule II)
Treats attention-deficit hyperactivity disorder (ADHD) in children over age six and for narcolepsy
Examples: Adderall and Ritalin
Wakefulness-promoting agents
Provigil is a psychostimulant approved for narcolepsy, sleep apnea, and shift-work sleep disorder
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Selective Norepinephrine Reuptake Inhibitor (SNRI) for ADHD
Atomoxetine (Strattera)
Selective norepinephrine reuptake inhibitor
First nonstimulant, noncontrolled drug approved for attention-deficit hyperactivity disorder (ADHD)
Structurally related to fluoxetine
Does not have a potential for abuse, has less insomnia, less effect on growth, and has been shown to be safe and effective
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Antidepressants (1 of 5)
Major depressive disorder (MDD)
Caused by a chemical imbalance in the brain
Mental disorder characterized by an all-encompassing low mood accompanied by low self-esteem and loss of interest or pleasure in normally enjoyable activities
Antidepressant medications, sometimes called mood elevators, are used primarily to treat patients with various types of depression
“Black box” warning
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Antidepressants (2 of 5)
Tricyclic antidepressants
Mechanism of action involves potentiation of norepinephrine and serotonin activity by blocking their reuptake
Monamine oxidase inhibitors (MAOIs)
Mechanism of action involves increasing concentrations of serotonin, norepinephrine, and dopamine in the neuronal synapse by inhibiting the MAO enzyme that degrades or breaks down these nuerotransmitters
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Antidepressants (3 of 5)
Selective serotonin reuptake inhibitors (SSRIs)
First-line medications for treatment of depression
Greater safety in the cases of overdose
Selectively block reabsorption of serotonin, helping to restore the brain’s chemical balance
Example: Prozac and Zoloft
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Antidepressants (4 of 5)
Selective norepinephrine reuptake inhibitors (SNRIs)
Inhibit reuptake of serotonin and norepinephrine
Affective in patients with chronic pain
Examples: Cymbalta and Effexor
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Antidepressants (5 of 5)
Heterocyclic antidepressants
Comparable efficacy to first-generation tricyclic antidepressants,
Differing effects on dopamine, norepinephrine, and serotonin
Distinctly different adverse effect profiles
Examples: Wellbutrin and Remeron
See Table 20-2
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Antimanic Agents
Bipolar disorder
Mental illness characterized by severe fluctuations in mood extremes
Patients may experience high (mania) and low (depression) mood swings with a diminished capacity for daily functioning
Lithium
Treatment of mania, lowered the suicide rate
Serum levels are checked to prevent toxicity
See Table 20-3
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Anxiolytics (1 of 2)
Anxiety becomes a disorder when it becomes excessive and difficult to control
Types of anxiety disorders
Social anxiety, post-traumatic stress disorder, panic attacks, and obsessive compulsive behavior
Benzodiazepines (BDZs)
For short-term treatment of anxiety disorders, some psychosomatic disorders and insomnia, and alcohol withdrawal
Examples: Valium, Klonopin, and Versed
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Anxiolytics (2 of 2)
Other anxiolytics
Buspirone (BuSpar)
Indicated for treatment of generalized anxiety disorder, but not other anxiety disorders (or depression)
Hydroxyzine (Vistaril)
Used IM as a pre- and postoperative antiemetic and sedative
See Table 20-4
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Antipsychotic Medications/Major Tranquilizers (1 of 3)
Also called neuroleptics
First and second generation agents
Useful in two major areas
Relieving symptoms of psychoses including delusion, hallucinations, agitation, and combativeness
Relieving nausea and vomiting
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Antipsychotic Medications/Major Tranquilizers (2 of 3)
Modify disturbed behavior and relieve severe anxiety without impairment of consciousness
Work primarily by blocking dopamine receptors
Results in unbalanced cholinergic activity
Causes frequent extrapyramidal side effects to include tardive dyskinesia
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Antipsychotic Medications/Major Tranquilizers (3 of 3)
Atypical antipsychotics
Block both serotonin and transiently block dopamine receptors
Less potential for adverse effects
There is no “ideal” antipsychotic medication
Both conventional and atypical antipsychotic medications are associated with significant adverse drug reactions
See Table 20-5
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Drug Abuse (1 of 2)
Drug abuse
The use of a drug for other than therapeutic purposes
Drug addiction
A combination of tolerance, psychological dependence, physical dependence, and withdrawal syndrome with physiological effects
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Drug Abuse (2 of 2)
Chemical dependency
A condition in which alcohol or drugs have taken control of an individual’s life and affect normal functioning
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Alcohol (1 of 2)
Ethyl alcohol, ethanol)
Classified as a psychotropic drug and a CNS depressant
Number one drug problem in the U.S.
Responsible for more than half of the traffic accidents in the U.S and most commonly abused drug among American teenagers
Fast acing depressant and rapid absorbed from the GI tract
Prolonged use can cause CNS damage
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Alcohol (2 of 2)
Alcohol poisoning
Symptoms include cold, clammy skin; stupor; slow, noisy respirations; and alcoholic breath
Mortality associated with acute alcohol poisoning alone is uncommon, but can be an important factor when mixed with recreational drugs
Treatment: Refer to chapter text for description
Chronic alcoholism
Refer to chapter text for symptoms and treatment options
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Prescription Drug Abuse
Nation’s fastest growing drug problem
Second most-abused category of drugs after marijuana
According to the CDC, death rates from opioid overdoses have more than tripled since 1999
Proper disposal and storage is important for deterring abuse
Most often abused by medical professionals are fentanyl, oxycodone, hydrocodone and BDZ’s
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Illegal Drug Abuse (1 of 7)
Amphetamines
Examples: methamphetamine (“crystal,” “crank,” “ice,” “meth,” “speed”) and methylenedioxymethamphetamine (MDMA, “Ecstasy”)
Abrupt withdrawal may unmask mental problems
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Illegal Drug Abuse (2 of 7)
Marijuana
Active ingredient: tetrahydrocannabinol (THC)
CNS depressant, euphoriant, sedative, and hallucinogen
Marinol is approved for the prevention of chemotherapy-induced nausea and vomiting
Synthetic cannabinoids
“Spice”, “K2”, “skunk”, fake weed: shredded plant material and chemical additives
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Illegal Drug Abuse (3 of 7)
Cocaine
Highly addictive CNS stimulant
Produces euphoria and increased expenditure of energy
Hallucinogens
Produce bizarre mental reactions and distortion of physical senses
Examples: lysergic acid (LSD) and phencyclidine (PCP)
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Illegal Drug Abuse (4 of 7)
Dextromethorphan (DXM)
Semisynthetic morphine derivative
Safe, effective, nonaddictive, OTC cough suppressant when used appropriately
Often abused by teens because of its phencyclidine-like euphoric effect
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Illegal Drug Abuse (5 of 7)
Flunitrazepam (Rohypnol)
Potent benzodiazepine approved for use in Central and South America for ethanol withdrawal
Known on the street as “roofies” and the “date-rape drug”
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Illegal Drug Abuse (6 of 7)
Role of the medical personnel
Have a thorough knowledge of psychotropic drugs, action, and side effects
Be willing to participate in the education of the patient, patient’s family, and others
Give competent care to those under the influence of drugs in a nonjudgmental way
Recognize drug abuse and make appropriate referrals without exception
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Illegal Drug Abuse (7 of 7)
Role of the medical personnel
Keep complete and accurate records of controlled stocks of drugs that could be considered potential drugs of abuse
Report any observed drug abuse to the proper person in authority
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Essentials of Pharmacology for Health Professions
Eighth Edition
Chapter 21
Musculoskeletal and Anti-Inflammatory Drugs
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114
Introduction
Disorders of the musculoskeletal system are rather common
Drugs used to treat such conditions are classified in two broad categories
Skeletal muscle relaxants
Nonsteroidal anti-inflammatory drugs (NSAIDs)
The following slides discuss various musculoskeletal and anti-inflammatory drugs
Refer to the chapter for side effects, precautions or contraindications, and interactions
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Skeletal Muscle Relaxants (1 of 2)
Many disorders associated with pain, spasm, abnormal contraction, or impaired mobility respond to skeletal muscle relaxants
Given only on a short-term basis
Most affect the central nervous system
No direct effect on skeletal muscle
Reduces muscle spasm, causes alterations in the perception of pain, and produces a sedative effect, promoting rest and relaxation
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Skeletal Muscle Relaxants (2 of 2)
Neuromuscular blocking agents (NMBAs)
Cause a direct effect on the muscles including the diaphragm
Used during surgical, endoscopic, or orthopedic procedures
Potentially very dangerous
Can result in respiratory arrest because of the potential to paralyze the diaphragm
See Table 21-1
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Anti-Inflammatory Drugs (1 of 4)
Treat disorders in which the musculoskeletal system is not functioning properly due to inflammation
Examples: arthritis, bursitis, spondylitis, gout, and muscle strains and sprains
Nonsteroidal anti-inflammatory drugs (NSAIDS)
Frequently given for lengthy time periods in maintenance doses as low as possible for effectiveness
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Anti-Inflammatory Drugs (2 of 4)
NSAIDs, such as ibuprofen, inhibit synthesis of prostaglandins
Substances responsible for producing much of the inflammation and pain of rheumatic conditions, sprains, and menstrual cramps
No cure has been found for rheumatic disorders, but many medications are used to alleviate pain
Salicylates (e.g., aspirin) are the oldest drug in this category with analgesic, anti-inflammatory, and antipyretic effects
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Anti-Inflammatory Drugs (3 of 4)
FDA warning regarding over-the-counter (OTC) nonselective NSAIDs
Should be used in strict accordance with label directions
Self-treatment should not exceed ten days, unless directed by a physician
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Anti-Inflammatory Drugs (4 of 4)
COX-2 inhibitor
Celecoxib (Celebrex): NSAID that exhibits anti-inflammatory, analgesic, and antipyretic activities
Selectively inhibits cyclooxygenase-2 (COX-2) prostaglandin synthesis, does not inhibit COX-1
Does not inhibit platelet aggregation (clotting) or inhibit production of mucosal-protective prostaglandins
Increases the risk of a cardiac event
See Table 21-2
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Osteoporosis Therapy (1 of 7)
Osteoporosis
A systemic skeletal disease
Characterized by low bone mass and deterioration of bone tissue, leading to bone fragility and increased susceptibility to fracture, especially of the hip, spine, and wrist
Most commonly affects postmenopausal women
Diagnosis: measure bone mineral density
Therapy includes calcium, vitamin D, and prescription medications
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Osteoporosis Therapy (2 of 7)
Bisphosphonates
Nonhormonal agents
Act directly to inhibit bone reabsorption, increasing bone mineral density at the spine and hip, and decreasing incidence of first and future fracture
Bind strongly to and accumulate in bone, creating a reservoir of drug that is released back into systemic circulation gradually over a period of months or years after treatment is stopped
Examples: Fosamax and Reclast
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Osteoporosis Therapy (3 of 7)
Hormones involved in osteoporosis therapy
Estrogen before menopause helps to maintain a normal bone reabsorption rate in women
Hormone replacement therapy (HRT), estrogen with or without progestin, is recommended for postmenopausal osteoporosis prevention only when unable to take other agents, and when benefits outweigh risks
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Osteoporosis Therapy (4 of 7)
Selective estrogen-receptor modifiers (SERMs)
Raloxifene (Evista) is a selective estrogen receptor modifier with estrogen agonist activity on bone and lipids and estrogen antagonist activity on breast and uterine tissue
Increase bone mineral density, decrease bone reabsorption, and reduce fracture risk without promoting breast or endometrial cancer
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Osteoporosis Therapy (5 of 7)
Calcitonin-salmon
Synthetic form of the hormone calcitonin is available as a nasal spray (Miacalcin) or as a subcutaneous injection
Involves with calcium regulation, increases spinal bone density, and provides an analgesic effect in acute vertebral fractures
Reserved for women who refuse or cannot tolerate HRT or in whom HRT is contraindicated
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Osteoporosis Therapy (6 of 7)
Parathyroid hormone
Teriparatide (Forteo) is an injectable form of parathyroid hormone approved for postmenopausal women and men with osteoporosis at a high risk for having a fracture
Increases GI calcium absorption and renal tubular reabsorption of calcium, increasing bone mineral density, bone mass, and strength
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Osteoporosis Therapy (7 of 7)
Monoclonal antibodies
Prolia: inhibits osteoclast activity
Reserved for patients with a higher risk of fracture
Subcutaneous injection given bi-annually
See Table 21-3
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