Complicated by the great variety of medications available and their differing modes of action

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 22

Anticonvulsants, Antiparkinsonian

Drugs, and Agents for Alzheimer’s

Disease

Introduction

• The following slides discuss various anticonvulsants,

antiparkinsonian drugs, and agents for Alzheimer’s

disease

– Refer to the chapter for specific side effects, precautions

or contraindications, and interactions

Anticonvulsants (1 of 4)

• Seizures are brief abnormal neuronal discharges in the

brain that occur repeatedly and without warning

• Reduces the number and/or severity of seizures in

patients with epilepsy

– Epilepsy: 2 or more unprovoked seizures, characterized

by sudden attacks of altered consciousness, motor

activity, or sensory impairment

• Treatment is based on type, severity, and cause of

seizures

– Treatment failure can result from inappropriate

anticonvulsant selection

Anticonvulsants (2 of 4)

• Two major groups

– Primary generalized seizures

▪ Begin with widespread electrical discharges that involves

both sides of the brain at once

▪ Further classified as convulsive or non-convulsive

– Partial seizures (focal)

▪ Begin with an electrical discharge in one limited area of

the brain

▪ No loss of consciousness (simple partial)

▪ Loss of consciousness (complex partial)

Anticonvulsants (3 of 4)

• Primary Generalized Seizures

– Tonic-clonic: abrupt loss of consciousness; falling, with

tonic extension of trunk and extremities, followed by

alternating contractions and relaxation of the muscles

– Absence epilepsy: absence of convulsions; sudden

onset; brief loss of consciousness with no falling, usually

occurs in children

• Febrile seizures: most common childhood seizure

disorder; single, brief, and generalized

Anticonvulsants (4 of 4)

• Partial seizures

– Caused by a lesion in the temporal lobe of the brain and

limited to one cerebral hemisphere

– Last from 10 seconds to five minutes

– Complex symptoms

– Can be preceded by an aura

• Unilateral seizures

– Affect only one side of the body

– Some patients may have mixed seizure patterns

Drug Therapy for Generalized and Partial

Seizures

• First generation anticonvulsants

– Prophylactic treatment of generalized and partial

seizures should start with a single drug such as

valproate, lamotrigine, levetiracetam, carbamazepine,

oxcarbazepine, or phenytoin

▪ Aim of therapy is to prevent seizures without oversedation

Drug Therapy for Febrile Seizures (1 of 2)

• Routine treatment of febrile seizures

– Involves searching for the cause of the fever and taking

measures to control it

– Most children with febrile seizures do not require

anticonvulsant drugs

▪ Those that do may be treated with rectal diazepam gel if

the seizure lasts longer than five minutes

Drug Therapy for Febrile Seizures (2 of 2)

• Routine treatment of febrile seizures

– American Academy of Pediatrics Subcommittee on

Febrile Seizures does not recommend continuous or

intermittent antiepileptic drug (AED) therapy for children

with one or more simple febrile seizures

Drug Therapy for Absence Seizures (1 of 3)

• Drug of choice for management of absence epilepsy is

Zarontin

– Effective only for this type of epilepsy

– Lacks idiosyncratic hepatotoxicity of valproic acid

• Other drugs in use include Klonopin, Depakene, and

Lamictal

Drug Therapy for Absence Seizures (2 of 3)

• Second-generation anticonvulsants

– Neurontin, Lamictal, Keppra, oxcarbazepine, Topamax,

etc.

▪ For adjuvant treatment of partial (psychomotor) and

generalized seizures

Drug Therapy for Absence Seizures (3 of 3)

• Second-generation anticonvulsants

– Compared to first-generation anticonvulsants

▪ Not yet considered superior in efficacy for seizure control

▪ Fewer adverse effects and drug interactions; does not

require drug level monitoring; daily dosing

• See Table 22-1

Antiparkinsonian Drugs (1 of 6)

• Antiparkinsonian drugs are usually given for

Parkinson’s disease (PD)

– Chronic neurological disorder characterized by fine,

slowly spreading muscle tremors, rigidity, and

generalized slowness of movement

– Most common neurodegenerative disease in adults

– Severe disability in 10-20 years

– Underlying pathology is not completely understood

Antiparkinsonian Drugs (2 of 6)

• Normal dopamine activity as it relates to acetylcholine

is diminished, with resulting relative overactivity of

cholinergic output

• Before interlining treatment, it is important to rule out

drug-induced parkinsonism (DIP)

Antiparkinsonian Drugs (3 of 6)

• Dopamine replacement

– Carbidopa-Levodopa crosses the blood-brain barrier,

where it is converted to dopamine

▪ Enhances effects of levodopa, increasing therapeutic

effect of dopamine in CNS and reducing adverse

reactions

• Dopamine agonists

– Mirapex and Requip are commonly used in conjunction

with levodopa to delay onset of levodopa-caused

motor complications or given alone in early PD

Antiparkinsonian Drugs (4 of 6)

• MAO-B inhibitors

– monoamine oxidase-B is responsible for breaking down

dopamine and tyramine in the brain

▪ In PD, increase levels of dopamine

• Selegiline (Eldepryl) and rasagiline (Azilect)

– Selective MAO type-B inhibitors

– Sometimes prescribed as adjunctive monotherapy for

early PD or after levodopa has been used for several

years

Antiparkinsonian Drugs (5 of 6)

• Rasagiline (Azilect)

– The only MAO-B inhibitor approved as initial

monotherapy for PD

– Also approved as an addition to levodopa later in the

disease

• Anticholinergic agents

– restore the cholinergic-dopaminergic balance in PD

– Include synthetic atropine-like drugs, such as Cogentin

and Artane

Antiparkinsonian Drugs (6 of 6)

• Amantadine

– Alters dopamine release

– Treats extrapyramidal reactions associated with

prolonged use of phenothiazines, carbon monoxide

poisoning, or cerebral arteriosclerosis

• COMT inhibitors

– Blocks the enzyme responsible for metabolizing

peripheral levodopa

– Increase concentration of levodopa and dopamine

• See Table 22-2

Agents for Restless Legs Syndrome (1 of 2)

• Sensorimotor neurologic disorder characterized by a

distressing urge to move the legs, often accompanied

by a marked sense of discomfort in the legs

– Triggered by rest or inactivity and is temporarily relieved

by movement

– Follows a circadian pattern, with symptoms being most

intense in the evening and nighttime

– May be primary or secondary

Agents for Restless Legs Syndrome (2 of 2)

• Primary RLS involves the CNS and dopaminergic

pathway

– Dopamine agonists Mirapex, Requip, and Neupro patch

are FDA-approved treatments

• Second-line agents

– Neurontin, benzodiazepines (such as clonazepam), and

opioids (hydroco-done, oxycodone, tramadol)

Agents for Alzheimer’s Disease (1 of 4)

• Dementia

– Variety of diseases and conditions that develop when

nerve cells in the brain die or no longer function normally

• Alzheimer’s disease

– Devastating, progressive decline in cognitive function,

having a gradual onset, usually beginning between 60

and 90 years of age, followed by increasingly severe

impairment in social and occupational functioning

Agents for Alzheimer’s Disease (2 of 4)

• Cholinesterase inhibitors

– Prevent breakdown of acetylcholine in the synaptic cleft,

thereby increasing acetycholine levels and improving

cognitive function

– Do not treat underlying pathology

– May slow the progression, but do not cure the disease

– Examples: Cognex, Aricept, Razadyne and Exelon

Agents for Alzheimer’s Disease (3 of 4)

• NMDA receptor antagonist

– Namenda is thought to selectively block the excitotoxic

effects with abnormal transmission of the

neurotransmitter glutamate

– Can be used as monotherapy or in combination therapy

with cholinesterase inhibitors

Agents for Alzheimer’s Disease (4 of 4)

• Decision on whether to continue drug therapy in

Alzheimer’s patients

– Based on quality of life, treatment goals, potential

benefits, adverse effects, and costs

▪ If quality of life is poor, stabilizing or slowing further

decline may not be an appropriate goal, and drug therapy

should be discontinued

• See Table 22-3

Essentials of Pharmacology for

Health Professions Eighth Edition

Chapter 23

Endocrine System Drugs

Introduction (1 of 3)

• Endocrine

– Exerts its affects more slowly and over a longer period of

time

– Internal secretion (hormone) produced by a ductless

gland that secretes directly into the bloodstream

• Hormones

– Chemical messengers with specialized functions in

regulating activities of specific cells or organs

Introduction (2 of 3)

• Endocrine system drugs

– Natural hormones secreted by ductless glands or

synthetic substitutes

• Endocrine system drug categories

– Pituitary hormones

– Adrenal corticosteroids

– Thyroid agents

– Antidiabetic agents

Introduction (3 of 3)

• The following slides discuss various endocrine system

drugs

– Refer to the chapter for specific side effects, precautions

or contraindications, and interactions

Pituitary Hormones (1 of 2)

• Pituitary gland: the master gland

– Regulates the function of the other glands

– Secretes several hormones

▪ Somatotropin (human growth hormone):

o Secreted by the anterior pituitary lobe

o Regulates growth

o Insufficient production will result in growth abnormalities

Pituitary Hormones (2 of 2)

– Secrets several hormones (con’t)

▪ Adrenocorticotropic hormone (ACTH): Cortrosyn, a

synthetic peptide of ACTH, is used mainly for diagnosis of

adrenocortical insufficiency

– Treatment of associated disorders is usually reserved for

the corticosteroids

Adrenal Corticosteroids (1 of 3)

• Adrenal glands secrete hormones called

corticosteroids

– Act on the immune system to suppress the body’s

response to infection or trauma

– Relieve inflammation, reduce swelling, and suppress

symptoms in acute conditions

– Two broad categories: replacement therapy and

immunosuppressant agents

– Corticosteroid therapy is not curative, but is used as

supportive therapy with other medications

Adrenal Corticosteroids (2 of 3)

• Some conditions treated with corticosteroids

– Allergic reactions

– Acute flare-ups of rheumatic or collagen disorders

– Acute flare-ups of severe skin conditions

– Acute respiratory disorders

– Long-term prevention of symptoms in severe persistent

asthma or chronic management of COPD

Adrenal Corticosteroids (3 of 3)

• Some conditions treated with corticosteroids (con’t)

– Malignancies

– Cerebral edema

– Organ transplant

– Life-threatening shock

– Acute flare-ups of ulcerative colitis

• Prednisone can be given by alternate-day therapy

• Long term therapy given more than 14 consecutive

days must be tapered

• See Table 23-1

Thyroid Disorders (1 of 3)

• The thyroid is an endocrine gland located in the front

part of the neck

– Responsible for regulating the rate of metabolism

– When thyroid levels are low, the pituitary gland releases

TSH, which promotes the synthesis of T4 (thyroxine)

and T3 (triiodothyronine), the active form of thyroid

hormone

– Thyroxine is later converted in the body to T3

Thyroid Disorders (2 of 3)

• Thyroid agents can be natural (thyroid) or synthetic

(Synthroid)

– Thyroid preparations are used in replacement therapy

for hypothyroidism

– Most common thyroid problem in the U.S.

▪ Diminished or absent thyroid function

▪ Hypothyroidism causes slowed metabolism

Thyroid Disorders (3 of 3)

• Antithyroid agents

– (Tapazole and propylthiouracil or PTU)

▪ Hyperthyroidism can be caused by Graves’ disease

▪ Used to relieve the symptoms of hyperthyroidism in

preparation for surgical or radioactive iodine therapy, or

for those who are not candidates for either procedure

o Methimazole is the treatment of choice

• See Table 23-2

Antidiabetic Agents (1 of 9)

• Diabetes mellitus (DM) is a group of hormonal

diseases

– Characterized by impaired metabolism of carbohydrates,

fats, and proteins that results in elevated levels of blood

glucose

– Classified as insulin-dependent Type 1 (characterized by

destruction of pancreatic beta cells) or Type 2

(characterized by insulin resistance and deficiency)

• See Table 23-3

Antidiabetic Agents (2 of 9)

• Result of long term poorly controlled diabetes is

vascular injury

• Seventh leading cause of death in the U.S.

• Medications are given to lower blood glucose levels

include parenteral inulin and oral and injectable

noninsulin antidiabetic agents

Antidiabetic Agents (3 of 9)

• Insulin

– Required as replacement therapy for Type 1 diabetics

with insufficient production of insulin from the islets of

Langerhans in the pancreas

– Required in patients with Type 2 who have failed to

maintain satisfactory concentrations of blood glucose

with therapy including dietary regulation and oral

antidiabetic agents

– Must be administered parenterally

– Marketed as two types: biosynthetic human or analog

Antidiabetic Agents (4 of 9)

• Insulin preparations (See Table 23-4)

– Differ mainly in their onset, peak, and duration of action

(See Figure 23-3)

– Diabetes therapy with insulin focuses initially on

controlling fasting plasma glucose with the use of a long-

acting insulin analog (Lantus or Levemir)

– There are many different types of insulins available

Antidiabetic Agents: Insulin pump

Antidiabetic Agents (5 of 9)

• Hyperglycemia

– Elevated blood glucose

– Cause, symptoms and treatment: see text

• Hypoglycemia

– Lowered blood glucose

– Cause, symptoms and treatment: see text

• Oral and injectable non-insulin antidiabetic agents

– Patients may sometimes be treated with diet

– Frequently necessary to combine diet and oral

antidiabetic agents

Antidiabetic Agents (6 of 9)

• Biguanides

– Work by decreasing hepatic glucose production and

enhancing insulin update in muscle (e.g., Glucophage)

• Sulfonylureas

– Consist of first-generation agents (e.g., chlorpropamide,

tolbutamide) and second-generation agents (e.g.,

glipizide, glyburide)

– Work by increasing insulin production from the pancreas

and by improving peripheral insulin activity

Antidiabetic Agents (7 of 9)

• Alpha-glucosidase inhibitors

– Precose

– Delay digestion of complex carbohydrates (e.g., starch)

and subsequent absorption of glucose, resulting in a

smaller rise in blood glucose concentrations following

meals

Antidiabetic Agents (8 of 9)

• Incretin therapies

– Agents that mimic actions of incretin hormones may be

beneficial

▪ Examples: Byetta, (a GLP-1), Januvia and Onglyza.

▪ See Table 23-5

• Meglitinides

– Starlix and Prandin stimulate beta cells to produce

insulin

Antidiabetic Agents (9 of 9)

• Thiazolidinediones

– Actos and Avandia lower blood glucose by decreasing

insulin resistance and improving sensitivity to insulin in

muscle, liver, and adipose tissue

• SGLT2Inhibitor Therapy

– Newest class

– Decrease the reabsorption of glucose in the kidney

– Example: Invokana

• See Table 23-5

Essentials of Pharmacology for

Health Professions Eighth Edition

Chapter 24

Reproductive System Drugs

Introduction (1 of 2)

• Hormones that regulate reproductive system functions

include endogenous chemical substances

– Originate within different areas of the body

• Reproductive hormones categories

– Gonadotropic

– Androgens

– Estrogens

– Progestins

Introduction (2 of 2)

• The following slides discuss various reproductive

system drugs

– Refer to the chapter for specific side effects, precautions

or contraindications, and interactions

Gonadotropics (1 of 2)

• Gonadotropic hormones

– Follicle-stimulating hormone (FSH)

▪ Stimulates development of ovarian follicles in the female

and sperm production in testes of the male

– Luteinizing hormone (LH)

▪ Works in conjunction with FSH to induce secretion of

estrogen, ovulation, and development of corpus luteum

Gonadotropics (2 of 2)

• Gonadotropic hormones

– Luteotropic hormone (LTH)

▪ Stimulates secretion of progesterone by the corpus

luteum and secretion of milk by the mammary gland

Androgens (1 of 2)

• Male sex hormones

– Secreted mainly in the interstitial tissue of the testes in

the male and secondarily in the adrenal glands of both

sexes

– Inadequate production in the male may be due to

pituitary malfunction or to atrophy, injury to, or removal

of the testicles, resulting in eunuchism or eunuchoidism

Androgens (2 of 2)

• Uses of androgens include:

– Replacement

– Congenital

– Acquired

– Palliative treatment

– Treatment of endometriosis and fibrocystic disease of

the breast

– Treatment of cachexia

• Dangers of illegal use if anabolic steroids

• See Table 24-1

Erectile Dysfunction Medications

• Inability to achieve or maintain an erection sufficient for

satisfactory performance

– Incidence increases with age

– Nitric oxide: principal mediator in attaining and

maintaining an erection

• Phosphodiesterase (PDE) inhibitors

– Block phosphodiesterase type 5, found in the corpus

cavernosum

▪ Thought to impair the production of nitric oxide

• Examples: Viagra, Cialis, Levitra

Estrogens (1 of 3)

• Female sex hormones

– Produced mainly by the ovary and secondarily by the

adrenal glands

– Responsible for development of female secondary

sexual characteristics

– Produce an environment suitable for fertilization,

implantation, and nutrition of the early embryo

– Affect secretion of hormones FSH and LH from the

anterior pituitary gland

Estrogens (2 of 3)

• Menopause

– Natural life event, or can be artificially induced

– Levels of estrogen and progesterone are reduced,

leading to vasomotor symptoms and atrophic vaginitis

• Estrogen therapy (ET): estrogen alone

– Associated with increased risk of endometrial carcinoma

in women with an intact uterus

▪ Progestin combined with estrogen, reduces the risk of

endometrial cancer substantially

Estrogens (3 of 3)

• Hormone replacement therapy (HT)

– Woman’s Health Initiative (WHI) study

▪ See Chapter text for risks and benefits of HT

• Uses of estrogen therapy:

– Contraception

– Menopausal relief

– Hypogonadism

– Prevention of osteoporosis

– Atrophic vaginitis

Progestins (1 of 2)

• Progesterone

– Hormone secreted by the corpus luteum and adrenal

glands

– Responsible for changes in uterine endometrium in the

second half of the menstrual cycle

▪ Preparation for implantation, development of maternal

placenta after implantation, and development of

mammary glands

– Progestins are synthetic drugs that exert progesterone-

like activity

Progestins (2 of 2)

• Uses of progestin's

– Amenorrhea and abnormal uterine bleeding

– Contraceptive agents

– Postmenopausal

– Adjuvant and palliative therapy for advanced

endometrial and breast cancers

– Management of paraphilia

• See Table 24-3

Contraceptives Agents

• Estrogen-progestin oral contraceptives

– Safe and effective

– Suppress FSH and LH

– Progestin-only contraceptives

▪ Indicated for woman who can’t tolerate estrogen side

effects

▪ Prevent pregnancy and used for the treatment of fibroids,

endometriosis, painful heavy periods, irregular cycles

Choice of Contraceptives (1 of 3)

• Estrogen-progestin oral contraceptives

– Classified according to estrogen content and formulation

▪ Monophasic, biphasic, triphasic, and four-phasic

– Extended- or continuous-cycle oral contraceptives

▪ Decrease or eliminate hormone-free interval

• Progestin-only contraceptives

– Recommended for patients who do not tolerate estrogen

or in whom it is contraindicated

Choice of Contraceptives (2 of 3)

• Progestin-containing intrauterine device (IUD)

– Mirena contains a reservoir of levonorgestrel, a synthetic

progestin

▪ Releases small amounts of progesterone daily, providing

five years of continuous contraception protection

▪ Inhibits sperm migrations, change in the ovum transport

and alteration of the endometrium

Choice of Contraceptives (3 of 3)

• Postcoital contraception (“morning after pill”)

– Combined estrogen-progestin contraceptive pills used in

case of emergency

– Not without risk

– Available option to women who are exposed to an

unintentional risk of pregnancy

– Must be administered within 72 hours of unprotected

intercourse

– Examples: Next Choice and ulipristal acetate

• See Table 24-4

Drugs for Labor and Delivery (1 of 5)

• Oxytocin is a hormone that stimulates the uterus to

contract, thus inducing childbirth

– Also acts on the mammary gland to stimulate the

release of milk

• Synthetic chemicals used to stimulate uterine

contractions are called oxytocics

– Include oxytocin and prostaglandin E1 and E2

• Goal of labor induction

– Facilitate vaginal delivery of a healthy infant

Drugs for Labor and Delivery (2 of 5)

• Oxytocin: Uses

– Induction of labor with at-term or near-term pregnancies

associated with hypertension, diabetes or uterine fetal

death at term

– Prolonged or dysfunctional uterine inertia occurs

Drugs for Labor and Delivery (3 of 5)

• Prostaglandins are released as a natural part of the

cervical ripening process

– Those causing contraction of the myometrial muscle

include dinoprostone or prostaglandin E2 (Prostin E2,

Cervidil, Prepidil), and the oral synthetic prostaglandin

E1 analog, misoprostol (Cytotec), and the prostaglandin

F2-alpha analog carboprost (Hemabate)

Drugs for Labor and Delivery (4 of 5)

• Mifepristone (RU-486)

– Antiprogesterone drug used to terminate an unwanted

pregnancy (in conjunction with misoprostol)

– Only for use very early in pregnancy

– Requires 3 visits to a qualified physician

• Methylergonovine

– Semisynthetic ergot alkaloid used for prevention and

treatment of postpartum and postabortion hemorrhage

Drugs for Labor and Delivery (5 of 5)

• Terbutaline

– Classified as a bronchodilator drug

– Also used with careful monitoring in the management of

preterm labor

• Magnesium sulfate

– For prevention and control of seizures in eclamptic

patients

▪ Preeclampsia is characterized by new-onset

hypertension, edema, and proteinuria

• See Table 24-5

Other Gonadotropic Drugs

• Gonadotropin-releasing hormones (GnRH)

– Act in the pituitary to suppress ovarian and testicular

hormone production and inhibit estrogen and androgen

synthesis

– GnRH analogs that inhibit gonadotropin secretion are

used in the management of endometriosis

– Examples: Lupron and Synarel

Essentials of Pharmacology for

Health Professions Eighth Edition

Chapter 25

Cardiovascular Drugs

Introduction (1 of 2)

• Cardiovascular drugs

– Medications that affect the heart and blood vessels, as

well as anticoagulant and antiplatelet agents that

prevent clotting

▪ Cardiac glycosides, antiarrhythmic agents, antilipemic

agents, antihypertensives, vasodilators, vasoconstrictors,

anticoagulants, platelet inhibitors, thrombolytic and

hematopoietic agents

Introduction (2 of 2)

• The following slides discuss various cardiovascular

drugs

– Refer to the chapter for specific side effects, precautions

and contraindications, and interactions

Cardiac Glycosides (Digoxin)

• Cardiac glycosides

– Occur widely in nature or can be prepared synthetically

– Act directly on the myocardium to increase the force of

myocardial contractions

– Digoxin is the only clinical drug currently used in the

cardiac glycoside family

▪ Used primarily in treatment of heart failure in patients with

symptoms that persist after optimization of treatment with

an ACE inhibitor, a beta-adrenergic blocker, and/or a

diuretic

Antiarrhythmic Agents (1 of 5)

• “Arrhythmia" refers to any change from the normal

sequence of electrical impulses of the heart

• Tachycardia (too fast), bradycardia (too slow),

fibrillation (erratic)

– Antiarrhythmic agents act in different ways to suppress

various types of cardiac arrhythmias

▪ Atrial or ventricular tachycardias, atrial fibrillation or flutter,

and arrhythmias that occur with digoxin toxicity or during

surgery and anesthesia

Antiarrhythmic Agents (2 of 5)

• Adenosine (Adenocard)

– Injectable antiarrhythmic agent

– Multiple electrophysiologic activities

▪ Restores normal sinus rhythm in paroxysmal

supraventricular tachycardia by slowing conduction time

through the atrioventricular (AV) node

▪ Vasodilatory, antiadrenergic, and negative chronotropic

(decrease in rate) properties that act to decrease cardiac

oxygen demand

Antiarrhythmic Agents (3 of 5)

• Amiodarone (Cordarone)

– Oral and injectable antiarrhythmic agent approved for

treatment of refractory life-threatening ventricular

arrhythmias

– Widely used for preventing recurrence of atrial fibrillation

• Beta-adrenergic blockers

– Antiarrhythmics that combat arrhythmias by inhibiting

adrenergic (sympathetic) nerve receptors

– Example: propranolol

Antiarrhythmic Agents (4 of 5)

• Calcium channel blockers

– Verapamil (Calan) and diltiazem (Cardizem)

– Indicated for treatment of atrial fibrillation/flutter and

PSVT

• Lidocaine

– Local anesthetic

– Administered for antiarrhythmic effects and membrane-

stabilizing action

– Second choice for treatment of ventricular arrhythmias

Antiarrhythmic Agents (5 of 5)

• Procainamide

– Quinidine, and disopyramide (Norpace)

– Act by decreasing myocardial excitability, inhibiting

conduction; may depress myocardial contractility

– Possess anticholinergic properties

• Propafenone (Rythmol)

– Treats symptomatic supraventricular arrhythmias or

severe, life-threatening ventricular arrhythmias

• See Table 25-1

Antihypertensives (1 of 5)

• Hypertension

– Systolic blood pressure (SBP) of 140 or greater or

diastolic blood pressure (DBP) of 90 or greater

– Antihypertensives may control hypertension, but they do

not cure it

– Drugs given to lower blood pressure act in various ways

▪ Varies according to stage of hypertension, physical

factors, and effectiveness in individual cases

Antihypertensives (2 of 5)

• Thiazide diuretics

– Most patients meeting the criteria for drug therapy

should be started on thiazide-type diuretics

▪ Either alone or in combination with a drug from one of the

other drug classes

– Appear to be as effective as other antihypertensive

agents and are inexpensive

Antihypertensives (3 of 5)

• Beta-adrenergic blockers

– Suitable for initial therapy in some patients with angina,

postmyocardial infarction, ischemic heart disease, heart

failure, and certain arrhythmias

– Example: Coreg, Toprol

• Calcium channel blockers

– Initial therapy option for hypertensive patients with

diabetes or high coronary disease risk

Antihypertensives (4 of 5)

• Angiotensin-converting enzyme inhibitors (ACE)

– First- or second-line agents in the treatment of

hypertension

– Excellent alone or in combination with other

antihypertensives (e.g., diuretics)

– Example: Lisinopril

• Angiotensin receptor blockers

– Similar to ACE inhibitors (ACEIs)

– Block angiotensin receptor that causes vasoconstriction

when stimulated by angiotensin II

Antihypertensives (5 of 5)

• Angiotensin receptor blockers (ARB)

– Similar to ACEI’s and are used as alternatives.

– They block the angiotensin receptor and block the effect

of angiotensin II

– Does not change the heart rate

– Lower incidence of side effects

Other Antihypertensives

• Antiadrenergic agents

– Clonidine (Catapress) is central-acting and Prazosin

(Minipress) is peripherally acting alpha-adrenergic

blockers

– Other agents in this class are used to treat benign

prostatic hypertrophy (BPH)

• Peripheral vasodilator

– Hydralazine is sometimes used in the treatment of

moderate to severe hypertension with CHF

– See Table 25-2

Coronary Vasodilators

• Treat angina

– Acute pain resulting from insufficient blood supply

(ischemia) to a part of the heart

– Angina pectoris: most common form of angina

▪ Involves chest pain resulting from decreased blood supply

to the heart muscle

▪ Nitrates most commonly used for relief of acute angina

pectoris (nitroglycerin and isosorbide)

• See Table 25-3

Antilipemic Agents (1 of 7)

• Elevated total blood cholesterol levels above 200

mg/dL

– Key risk factor for coronary heart disease

• Cardiovascular disease is the leading killer of men and

women in the United States

• High cholesterol can lead to:

– Arterial blockage, hardening of the arteries, blood clots,

heart attack, or stroke, and may even play a role in

dementia

Antilipemic Agents (2 of 7)

• Lipoproteins transport cholesterol and other fats

through the blood stream

– Low-density lipoproteins (LDLs; “bad cholesterol”)

– Very low-density lipoproteins (VLDLs; triglycerides),

precursor to LDL

– Triglycerides (TG) stored in fat

– High-density lipoproteins (HDLs; “good cholesterol”)

Antilipemic Agents (3 of 7)

• Six categories are used to lower cholesterol levels:

– Statins

▪ HMG-CoA reductase inhibitors, inhibit the enzyme for

cholesterol synthesis

▪ Most potent lipid-lowering medications available for

monotherapy

▪ First choice in managing high cholesterol

▪ Examples: Lipitor, Zocor

Antilipemic Agents (4 of 7)

• Bile acid sequestrants

– Cholestyramine (Questran) and colesevelam (WelChol)

– Bind bile acids in the intestine, interrupting the process

by which bile acids are returned to the liver for reuse

Antilipemic Agents (5 of 7)

• Nicotinic acid (Niacin)

– Reduces hepatic synthesis of triglycerides; inhibits the

mobilization of free fatty acids from the peripheral

tissues

– Lowers serum total, LDL cholesterol, and triglyceride

levels

– Raises HDL cholesterol levels

Antilipemic Agents (6 of 7)

• Fibric acid derivatives (fibrates)

– Fibrates fenofibrate (TriCor) and gemfibrozil (Lopid)

possess minimal LDL-reducing capacity

– Especially effective in patients who have extremely high

triglyceride levels, elevated cholesterol levels, and

combined forms of hyperlipidemia

– Good choice for diabetics

Antilipemic Agents (7 of 7)

• Cholesterol absorption inhibitor

– Ezetimibe (Zetia) moderately reduces LDL by inhibiting

intestinal absorption of both dietary and biliary

cholesterol, blocking its transport in the small intestine

• Omega-3 fatty acids

– Eicosapentaenoic acid (EPA) and docosahexaenoic acid

(DHA)

– Prevent primary and secondary heart disease and

reduce triglycerides

• See Table 25-4

Antithrombotic Agents

• Inappropriate thrombus formation

– Can be caused by vessel-wall injury, circulatory stasis,

increased blood coagulability, immobilization, obesity,

cigarette smoking, medication therapy, and other factors

• Antithrombotic agents interfere with or prevent

thrombosis or blood coagulation

– Anticoagulants, platelet inhibitors, and thrombolytics

Anticoagulants (1 of 2)

• Prevent formation of fibrin clot by interfering with one of

the steps leading to fibrin formation

– Oral and injectable

– Purpose: prevent clot formation existing in such

conditions as venous thrombosis, stroke, PE, and

coronary artery occlusion

• Warfarin (Coumadin) is administered orally

– Alters synthesis of blood coagulation factors in the liver

by interfering with the action of vitamin K

– Monitor therapy with INR

Anticoagulants (2 of 2)

• New oral anticoagulants

– Dabigatran, rivaroxaban, and apixaban

– Rapid onset, lab monitoring not required

• Heparin and low-molecular weight heparins

– Heparin is not absorbed from the GI tract and standard

type (UFH) must be administered intravenously or

subcutaneously

– LMWH (Lovenox) type is usually only administered

subcutaneously but may be given IV

• See Table 25-5

Platelet Inhibitor Therapy (1 of 3)

• Anti-platelet agents

– Inhibit aggregation (clumping) and release of

thromboplastin from the platelets to begin the clotting

process

• Platelet inhibitors utilize a variety of mechanisms to

interfere with activation pathways to prevent platelet

clumping

– Given as prophylactic therapy or as secondary

prevention

Platelet Inhibitor Therapy (2 of 3)

• Dipyridamole (Persantine)

– Non-nitrate coronary vasodilator that inhibits platelet

aggregation

• Aspirin

– Ability to inhibit platelet aggregation clumping

– Used after myocardial infarction or recurrent transient

ischemic attacks to reduce risk of recurrence

– Used to reduce risk of myocardial infarction in patients

with unstable angina

Platelet Inhibitor Therapy (3 of 3)

• Adenine diphosphate receptor antagonists clopidogrel

(Plavix)

– Blocks activation of the platelet’s receptor surface,

thereby inhibiting platelet activation

– Prevent thrombosis of coronary artery stents when used

with ASA

– Newest agent: Brilinta

Thrombolytic Agents

• The body maintains a process to dissolve clots

(fibrinolysis) after they have formed

– Tissue plasminogen activator (t-PA) is a natural peptide

that initiates fibrinolysis

– Thrombolytic agents dissolve and liquefy the fibrin of an

existing clot

– Thrombolytic drugs (e.g., reteplase and alteplase)

potentiate t-PA, resulting in clot dissolution, reperfusion

of organs, and restoration of blood flow to tissues

Hematopoietic Agents (1 of 2)

• Hematopoiesis

– The formation, differentiation, and maturation of blood

cells into specific cell lines

• Erythropoiesis-stimulating agents (ESAs)

– Responsible for regulation of the production and

development of blood cells, normally in the bone marrow

– Example: epoetin alfa (Epogen or Procrit)

Hematopoietic Agents (2 of 2)

• Colony stimulating factors (CSFs)

– A granulocyte colony-stimulating factor (G-CSF),

filgrastim (Neupogen), is involved in the regulation and

production of neutrophils in response to host defense

needs

– Lessens severity of myelosuppression in cancer

patients; has allowed chemotherapy dose intensification

or maintenance of dose intensity

• See Table 25-6

Essentials of Pharmacology for

Health Professions Eighth Edition

Chapter 26

Respiratory System Drugs and

Antihistamines

Introduction (1 of 3)

• Respiratory diseases and disorders

– According to the American Lung Association, lung

disease is the third leading cause of death in the U.S.

– Respiratory diseases range from mild and self-limiting

such as the common cold, to life-threatening such as

bacterial pneumonia, pulmonary embolism, and lung

cancer

Introduction (2 of 3)

• Therapeutic measures for respiratory distress

– Oxygen therapy

– Respiratory stimulants

– Bronchodilators

– Corticosteroids

– Mucolytics and expectorants

– Antitussives

– Smoking cessation

Introduction (3 of 3)

• The following slides discuss various respiratory system

drugs and antihistamines

– Refer to the chapter for specific side effects, precautions

or contraindications, and interactions

Oxygen

• Oxygen treatment

– Used therapeutically for hypoxia (insufficient oxygen

supply to the tissues)

– Decreases the workload of the heart and respiratory

system (especially during distress)

– Treats heart and lung diseases and some central

nervous system (CNS) conditions with respiratory

difficulty or failure

– Administered by endotracheal intubation, nasal cannula,

masks, tents or hoods

Respiratory Stimulants

• Caffeine citrate

– Treats neonatal apnea of prematurity (See Chapter 20)

• Theophylline

– Administered IV and orally to stimulate respiration in

infants (as an alternative to caffeine)

Bronchodilators (1 of 3)

• Act by relaxing smooth muscles of the bronchial tree,

relieving bronchospasm and decreasing the work of

breathing

– For symptomatic treatment of acute asthma and some

forms of COPD

– Can be given orally, parenterally, and by inhalation

▪ Metered dose inhalers (MDIs), dry-powder inhalers

(DPIs), and small volume nebulizers (SVNs)

Bronchodilators (2 of 3)

• Sympathomimetics (adrenergics)

– Potent bronchodilators that increase vital capacity and

decrease airway resistance

– SABA’s and LABA’s

– Examples: albuterol, epinephrine, salmeterol, and others

• Anticholinergics (parasympatholytics)

– Decrease the chemical that promotes bronchospasm

– Example: Atrovent

Bronchodilators (3 of 3)

• Xanthines

– Relaxes the smooth muscle of the bronchial airways and

pulmonary blood vessels

– May possess anti-inflammatory actions

– No longer a first-line treatment

▪ Modest clinical effectiveness (COPD)

▪ Need for serum monitoring

▪ Many adverse effects and drug interactions

• See Table 26-1

Corticosteroids (1 of 2)

• Synthetic corticosteroids

– Relieve inflammation, reduce swelling, decrease

bronchial hyper-responsiveness to triggers, and

suppress symptoms in acute and chronic reactive airway

disease

– Administered systemically for short-term “bursts” during

exacerbations, and occasionally at the beginning of

treatment until symptoms are controlled

Corticosteroids (2 of 2)

• Inhaled corticosteroids (SVN aerosol, DPI, MDI)

– Preferred drug therapy in long-term prophylactic

management of persistent asthma of various severities

• Intranasal corticosteroids

– Increasingly considered first-line therapy for most

noninfectious types of rhinitis

– Reduce congestion, edema, and inflammation

• See Table 26-2

Asthma Prophylaxis (1 of 2)

• Leukotriene inhibitors

– Zafirlukast (Accolate) and montelukast (Singulair)

▪ Oral leukotriene receptor antagonists for asthma

prophylaxis, prevention of exercise-induced

bronchoconstriction, and treatment of chronic asthma

▪ Help control inflammatory process of asthma caused by

leukotriene production, thus helping to prevent asthma

symptoms and acute attacks

Asthma Prophylaxis (2 of 2)

• Mast cell stabilizers

– Rupture or degranulation of mast cells and subsequent

spilling of their chemical mediator contents cause an

inflammatory response that can lead to asthma

– Stabilizing the mast cell membrane has anti-

inflammatory actions that modify the release of

mediators from mast cells and eosinophils

– Example: cromolyn

• See Table 26-3

Mucolytics and Expectorants

• Mucolytics

– Decrease hypersecretion and increase thinning of

pulmonary secretions

– Example: acetylcysteine

• Expectorants

– Increase secretions, reduce viscosity, and help to expel

sputum

– Example: guaifenesin

• See Table 26-4

Antitussives

• Prevent coughing in patients not requiring a productive

cough

– Most produce cough suppression by acting centrally on

the cough center located in the brainstem

– Narcotic antitussive example: codeine

– Nonnarcotic antitussive example: dextromethorphan

– Benzonatate: suppresses cough peripherally

• See Table 26-5

Antihistamines

• Competitively antagonize the histamine1 receptor sites

– Combat the increased capillary permeability and edema,

inflammation, and itch caused by sudden histamine

release

▪ To treat allergy symptoms

– First generation: diphenhydramine (Benadryl)

– Second-generation: fexofenadine (Allegra) and

loratadine (Claritin); selective histamine1 receptor

antagonists, less sedation

Decongestants

• Constrict blood vessels in the respiratory tract

– Results in shrinkage of swollen mucous membranes and

helps to open nasal airway passages

– Frequently combined with antihistamines, analgesics,

caffeine, and/or antitussives

– Examples: phenylephrine (Neo-Synephrine) or

pseudoephedrine (Sudafed)

– Can cause rebound congestion

• See Table 26-6

Safety of Cough/Cold/Allergy Products

• Many cough and cold formulations combine several

drugs

– Use only if the corresponding symptom is present and

each individual component is available in the proper

strength and dosing interval a patient may need

– Caution patients to seek advice from a healthcare

professional familiar with each ingredient

Smoking Cessation Aids (1 of 2)

• Nicotine replacement therapy

– Help lessen withdrawal symptoms by slowly lowering the

level of nicotine in the body

– Examples: Nicorette gum, Commit lozenges, Nicoderm

CQ patch, and Nicotrol inhaler and nasal spray

• Buproprion

– Oral antidepressant drug (Wellbutrin)

– Associated with decreases in cravings and lessening of

nicotine withdrawal

Smoking Cessation Aids (2 of 2)

• Varenicline (Chantix)

– Partial nicotine receptor agonist-antagonist

– Alleviates symptoms of nicotine craving and withdrawal

through agonist activity while inhibiting the effects of

repeated nicotine exposure by its antagonist activity

– Eliminates the pleasurable feelings associated with

smoking

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Josie Eskander

Sandra Coke is vice president for research and development at Great Lakes Foods (GLF), a large snack food company that has approximately 1,000 employees