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Essentials of Pharmacology for

Health Professions Eighth Edition

Chapter 16

Gastrointestinal Drugs

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

Introduction (2 of 2)

• The following slides discuss various gastrointestinal

drugs

– Refer to the chapter for specific side effects,

contraindications, and interactions

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

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

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

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

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

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

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

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)

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

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

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)

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

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

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

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

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

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

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)

Essentials of Pharmacology for

Health Professions Eighth Edition

Chapter 17

Anti-infective Drugs

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

o Wound, throat, urine or blood

o Usually not available for 24-48 hours

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

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

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

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

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.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Essentials of Pharmacology for

Health Professions Eighth Edition

Chapter 18

Eye and Ear Medications

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Essentials of Pharmacology for

Health Professions Eighth Edition

Chapter 19

Analgesics, Sedatives, and

Hypnotics

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

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

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

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

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.

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)

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

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

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”

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

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

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

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

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

Essentials of Pharmacology for

Health Professions Eighth Edition

Chapter 20

Psychotropic Medications, Alcohol,

and Drug Abuse

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Illegal Drug Abuse (1 of 7)

• Amphetamines

– Examples: methamphetamine (“crystal,” “crank,” “ice,”

“meth,” “speed”) and methylenedioxymethamphetamine

(MDMA, “Ecstasy”)

– Abrupt withdrawal may unmask mental problems

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

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)

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

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”

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

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

Essentials of Pharmacology for

Health Professions Eighth Edition

Chapter 21

Musculoskeletal and Anti-

Inflammatory Drugs

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

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

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

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

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

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

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

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

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

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

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

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

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

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