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Chapter 9
Pharmacology
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Overview
• Clinical pharmacology is the study of the
biologic effects of a drug on a patient when it
is used as a medical treatment
• Drug effects on different systems of the body
will be summarized in this chapter
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Pharmacology and the
Central Nervous System
• Drug classifications affecting the central
nervous system (CNS) include:
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Sedatives
Antianxiety drugs
Antiparkinson drugs
Antipsychotics
Anesthetics
− Hypnotics
− Anticonvulsants
− Antidepressants
− Narcotic analgesics
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Sedatives, Hypnotics,
and Antianxiety Drugs
• Sedatives and hypnotic drugs are used to treat
anxiety and sleep disorders
• Sedation is characterized by decreased
anxiety, motor activity, and mental acuity
• Hypnosis is defined by an increased tendency
to sleep
• Anxiety is a persistent, irrational fear of a
specific object, activity, or situation
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Anticonvulsants
• Seizure is a term for events caused by epilepsy
• Convulsion refers to abnormal motor
movements
• Anticonvulsants prevent or stop convulsive
seizures
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Antiparkinson Drugs
• Parkinson’s disease is characterized by:
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Resting tremor
Resistance to passive movement
Akinesia (inability to initiate movements)
Loss of postural reflexes
Behavioral manifestations
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Antidepressants
• Depression is one of the most common
psychiatric disorders in the United States
• It is characterized by feelings of:
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Intense sadness
Worthlessness
Inability to experience pleasure in activities
Sudden weight gain or loss
Helplessness
(continues)
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Antidepressants
• Depression is characterized by feelings of:
– Impaired functioning
– Loss of energy
– Changes in sleep habits
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Examples of Antidepressants
• Tricyclic antidepressants:
– amitriptyline (Elavil) and nortriptyline (Aventyl)
• Second-generation cyclic antidepressants
– bupropion (Wellbutrin)
• Monoamine oxidase inhibitors
– phenelzine (Nardil)
• Selective serotonin reuptake inhibitors
– citalopram (Celexa) and fluoxetine (Prozac)
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Antipsychotics
• Psychosis is a mental disorder in which a
person’s capacity to recognize reality is
distorted by hallucinations and delusions
• Antipsychotics can be classified as
conventional and atypical agents
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Narcotic Analgesics
• Narcotic analgesics are also referred to as
opioids
• They reduce pain and induce tolerance and
physical dependence
• Drugs made from opium are referred to as
opiates
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Examples of
Narcotic Analgesics
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hydrocodone (Hycodan)
hydromorphone (Dilaudid)
meperidine (Demerol)
methadone (Dolophine)
pentazocine (Talwin)
propoxyphene (Darvon-N)
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Anesthetics
• Anesthesia is the unique condition of
reversible unconsciousness or loss of sensation
• It is characterized by 4 actions:
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Unconsciousness
Analgesia
Immobility
Amnesia
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Examples of
General Anesthetics
• diazepam (Valium)
• propofol (Diprivan)
• thiopental (Pentothal)
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Pharmacology and the Endocrine
System
• The endocrine system consists of specialized
cell clusters, glands, hormones, and target
tissues
• Endocrine drugs are used to treat deficiencies
or excesses of specific hormones or nonendocrine diseases
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Selected Drugs for
Thyroid Gland Conditions
• Diseases of the thyroid gland include:
– Hypothyroidism
– Hyperthyroidism
– Overproduction of thyroid hormone
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Selected Drugs for
Diabetes Mellitus
• The two general classifications for diabetes
mellitus include:
– Type I – insulin-dependent diabetes mellitus (IDDM) must
be treated with insulin
– Type II – non-insulin-dependent diabetes mellitus
(NIDDM) may require SC or IV insulin
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Examples of Insulins
• Rapid-Acting
– Lispro (Aspart)
• Short-Acting
– Regular
• Intermediate-Acting
– NPH and Lente
• Long-Acting
– Ultralente and Glargine
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Examples of
Oral Hypoglycemic Drugs
• Sulfonylureas:
– chlorpropamide (Diabinese) and glipizide (Glucotrol)
• Meglitinides (secretogogues):
– nateglinide (Starlix) and repaglinide (Prandin)
• Biguanides:
– metformin (Glucophage)
(continues)
–
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Examples of
Oral Hypoglycemic Drugs
• Thiazolidinediones (glitazones):
– pioglitazone (Actos) and rosiglitazone (Avandia)
• Alpha-glucosidase inhibitors:
– miglitol (Glyset)
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Oral Contraceptives
• Manipulating estrogen and progesterone levels
can prevent pregnancy
• Oral contraceptives include:
– Estrogen and progestin combinations
– Progestin-only preparations
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Pharmacology and the
Cardiovascular System
• Cardiovascular disorders are among the most
common causes of death in the United States
• These disorders include:
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Angina pectoris
Hypertension
Myocardial infarction
Hyperlipidemia
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Antianginal Drugs
• Angina pectoris often causes a sharp pain that
is usually felt in the chest or arm
• There are three groups of medications for
angina pectoris:
– Nitrates
– Beta-adrenergic blockers
– Calcium channel blockers
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Examples of Antianginal Drugs
• Nitrates:
– isosorbide (Imdur) and nitroglycerin (Nitrolingual)
• Beta-Adrenergic Blockers:
– atenolol (Tenormin) and propranolol (Inderal)
• Calcium Channel Blockers:
– diltiazem (Cardizem) and verapamil (Calan)
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Antihypertensive Drugs
• Hypertension is an abnormal increase in
arterial blood pressure
• Drugs used to treat hypertension include:
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Diuretics
Beta-blockers
Angiotensin-converting enzyme (ACE) inhibitors
Angiotensin II receptor blockers (ARB)
Calcium channel blockers
Alpha-blockers
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Examples of Diuretics
• Thiazide diuretics:
– chlorthalidone (Hylidone and Hygroton)
• Loop Diuretics:
– ethacrynic acid (Edecrin) and furosemide (Lasix)
• Potassium-sparing diuretics:
– Spironolactone (Aldactone) and triamterene (Dyrenium)
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Examples of other
Antihypertensive Drugs
• Beta-blockers:
– atenolol (Tenormin) and bisoprolol (Zebeta)
• ACE Inhibitors:
– enalapril (Vasotec) and lisinopril (Zestril)
• Angiotensin II receptor blockers (ARBs):
– irbesartan (Avapro) and valsartan (Diovan)
• Calcium channel blockers:
– amlodipine (Norvasc) and nifedipine (Procardia)
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Antiarrhythmics
• Arrhythmias are derivations from the normal
pattern of the heartbeat
• Common arrhythmias include:
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Atrial fibrillation
Atrial flutter
Premature ventricular contractions
Ventricular tachycardia
Ventricular fibrillation
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Drug Therapy for Heart Failure
• Heart failure is the inability of the heart muscle
to contract with enough force to properly
circulate blood
• Drugs used for heart failure include:
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Cardiac glycosides
Diuretics
ACE inhibitors
Beta-blockers
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Antihyperlipidemic Drugs
• Diseases associated with plasma lipids can
manifest as an:
– Elevation in triglyceride levels (hyperlipidemia)
– Elevation in the cholesterol level
• Antihyperlipidemic drugs are used only if diet
and exercise programs fail
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Examples of
Lipid-Lowering Drugs
• Bile acid sequestrants:
– colesevelam (Welchol) and colestipol (Colestid)
• Fibric acid derivatives:
– clofibrate (Atromid-S) and gemfibrozil (Lopid)
• Niacin (nicotinic acid):
– immediate release (Niacor) and sustained-release (Niaspan)
• Statins:
– atorvastatin (Lipitor) and simvastatin (Zocor)
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Anticoagulant Drugs
• Without clotting, it is possible to bleed to death
• When clot formation is not desired, however,
anticoagulants prevent formation of blood
clots (thrombi)
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Examples of Anticoagulants
• heparin sodium (Hep-Lock)
• warfarin sodium (Coumadin)
• Low Molecular-weight Heparin:
– dalteparin sodium (Fragmin)
– tinzaparin sodium (Innohep)
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Pharmacology and the
Musculoskeletal System
• Musculoskeletal pain and inflammation in
muscles or joints is common
• Skeletal muscle relaxants are neuromuscular
blocking agents that block somatic motor
nerve impulses
• Another type, used for painful muscle
contractions, are centrally acting skeletal
muscle relaxants
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Analgesics, Antipyretics, and
Anti-inflammatory Drugs
• Some pain is relieved with opioid analgesics
and other types of pain are relieved with
nonopioid analgesics
• Many nonopioid analgesics affect pain, fever,
and inflammation
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Examples of Nonsalicylate AntiInflammatory and Analgesic Agents
(NSAIDs)
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diclofenac (Voltaren)
ibuprofen (Advil, Motrin)
indomethacin (Indocin)
meclofenamate (Meclofen)
meloxicam (Mobic)
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Antimicrobial Agents
• Pathogenic microorganisms produce infections
• Invading microorganisms include:
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Viruses
Bacteria
Fungi
Protozoa
Parasites
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Antibacterial Agents
• Antibacterial agents are classified as either
bactericidal or bacteriostatic
• Bactericidal refers to an agent capable of
killing bacteria
• Bacteriostatic means an agent inhibits, but
does not necessarily kill, bacteria
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Beta-Lactam Antibiotics
• An antibiotic is derived from a natural source
rather than a synthetic source
• Beta-lactam antibiotics include:
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Penicillins
Cephalosporins
Carbapenems
Monobactams
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Penicillins
• Penicillins were the first antibiotics developed
• They are classified as:
– Natural penicillins
– Antistaphylococcal penicillins
– Extended-spectrum penicillins
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Cephalosporins, Macrolides, and
Sulfonamides
• Cephalosporins are semisynthetic antibiotics
related to penicillins
• Macrolides are especially useful against
respiratory infections
• Sulfonamides were the first drugs to prevent
and cure human bacterial infections
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Examples of Cephalosporins
• First Generation:
– cefazolin (Ancef) and cephalexin (Keflex)
• Second Generation:
– cefaclor (Ceclor) and cefotetan (Cefotan)
• Third Generation:
– cefdinir (Omnicef) and cefprozil (Cefzil)
• Fourth Generation:
– cefepime (Maxipime)
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Examples of
Common Macrolides
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azithromycin (Zithromax)
clarithromycin (Biaxin)
erythromycin (Erythrocin)
erythromycin ethylsuccinate (EryPed)
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Examples of Sulfonamides
• Short-acting sulfonamides:
– sulfisoxazole (Gantrisin)
• Intermediate-acting sulfonamides:
– sulfadiazine (Microsulfon) and Sulfamethoxazole
(Sulfamethoxazole)
• Long-acting sulfonamides:
– Sulfasalazine (Azulfidine)
• Combination sulfonamides:
– Trimethoprim/sulfamethoxazole (Bactrim) and
sulfathiazole/sulfacetamide/sulfabenzamide (Sultrin)
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Tetracyclines and Aminoglycosides
• Tetracyclines are effective against certain
bacterial strains that are resistant to other
antibiotics
• Aminoglycosides are used primarily for
infections caused by gram-negative
enterobacteria, but they have high toxicity
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Examples of Aminoglycosides
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amikacin (Amikin)
gentamicin (Garamycin)
kanamycin (Kantrex)
neomycin (Mycifradin)
streptomycin (Streptomycin)
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Fluoroquinolones and
Miscellaneous Agents
• Fluoroquinolones may be useful in penicillinallergic patients
• Miscellaneous antibacterials include:
– Chloramphenicol
– Clindamycin
– Metronidazole
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Examples of Fluoroquinolones
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cinoxacin (Cinobac)
ciprofloxacin (Cipro)
gatifloxacin (Tequin)
nalidixic acid (NegGram)
nitrofurantoin (Furadantin)
norfloxacin (Noroxin)
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Antiviral Agents
• Antivirals are used to treat viral infections
• They act by influencing viral replication, either
of the DNA or RNA type
• Antiretroviral agents effective against HIV
include:
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Nucleoside reverse transcriptase inhibitors (NRTIs)
Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
Protease inhibitors (PIs)
Fusion inhibitors (FIs)
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Examples of
HIV Antiviral Agents
• NRTIs:
– lamivudine (Epivir) and zidovudine (Retrovir)
• NNRTIs:
– delavirdine (Rescriptor) and efavirenz (Sustiva)
• PIs:
– indinavir (Crixivan) and nelfinavir (Viracept)
• FIs:
– enfuvirtide (Fuzeon)
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Highly Active Antiretroviral
Therapy (HAART)
• Antiviral agents are being used either alone or
in combination to treat HIV
• HAART involves the combination of three to
four drugs effective against HIV, especially:
– Nucleoside analogs, and
– Protease inhibitors
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Antifungal Agents
• Antifungals are often used for:
– Systemic
– Local fungal, and
– Topical fungal infections
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Pharmacology and the Respiratory
System
• Upper respiratory tract infections are more
common than lower respiratory tract infections
• They may be caused by viruses, bacteria, or
fungi
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Antihistamines
• Drugs that counteract the action of histamine
are called antihistamines
• The conventional type, used for allergies,
blocks H1 histamine receptors
• The second type, used for peptic ulcers and
gastritis, blocks H2 histamine receptors
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Antitussives
• Agents that relieve or prevent coughing are
called antitussives
• They are classified into two major groups:
– Opioid
– Nonopioid
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Corticosteroids
• Corticosteroids are the most potent and
effective anti-inflammatory agents available
• Administration with a metered dose inhaler
(MDI) is often accomplished with one or two
puffs from a handheld pressurized device
• A dry powder inhaler (DPI) delivers
medication in the form of micronized powder
into the lungs
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Examples of Corticosteroids for
Treating Asthma
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beclomethasone (Beclovent)
budesonide (Pulmicort)
dexamethasone (Decadron)
fluticasone (Flovent)
prednisolone (Prelone)
prednisone (Deltasone)
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Bronchodilators
• Bronchodilators are agents that widen the
diameter of the bronchial tubes
• Bronchodilators include:
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Beta-adrenergic agonists
Theophylline
Anticholinergic drugs
Xanthine derivatives
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Examples of Bronchodilators Used
for Treating Asthma
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albuterol (Proventil)
metaproterenol (Alupent)
salmeterol (Serevent)
Xanthenes:
– aminophylline (Truphylline)
– theophylline (Elixophyllin)
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Antitubercular Agents
• Tuberculosis is more prevalent in:
– Patients with AIDS
– Drug abusers
– Homeless shelter and nursing home residents
(continues)
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Antitubercular Agents
• Primary antitubercular drugs include:
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Isoniazid
Ethambutol
Rifampin
Pyrazinamide
Streptomycin
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Pharmacology and the
Digestive System
• The digestive tract is the organ system
primarily responsible for food absorption and
elimination of solid waste
• This chapter focuses on treatment of:
– Peptic ulcer
– Diarrhea
– Constipation
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Antacids
• The various types of antacids differ in:
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Cation content
Neutralizing capacity
Duration of actions
Side effects
Cost
• Antacids are over-the-counter (OTC) drugs
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Histamine Receptor Antagonists
• There are three types of histamine receptors
• One type mediates acid secretion by gastric
parietal cells and is preferred to other antiulcer
agents because of:
– Convenience of use
– Lack of effect on GI motility
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Examples of Histamine (H2)
Receptor Antagonists
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cimetidine (Tagamet)
famotidine (Pepcid)
nizatidine (Axid)
ranitidine (Zantac)
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Proton Pump Inhibitors
• The final common pathway in gastric acid
secretion is the “proton pump”
• It is an enzyme that exchanges hydrogen ions
for potassium ions
• Proton pump inhibitors should be taken before
meals, preferably in the morning
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Examples of
Proton Pump Inhibitors
• lansoprazole (Prevacid)
• omeprazole (Prilosec)
• rabeprazole (AcipHex)
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Antidiarrheal Agents
• Diarrhea is the manifestation of many illnesses
• The most commonly used antidiarrheals are:
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Anticholinergics
Opioid narcotics
Meperidine congeners
Loperamide
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Laxatives and Stool Softeners
• Constipation is difficult or infrequent passage
of stool
• Constipation is a symptom rather than a
disease
• Laxatives either accelerate fecal passage or
decrease fecal consistency
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