Cap. 4 phar 4 tech ed 4

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© Paradigm Publishing, Inc.

Chapter 4

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Chapter 4 Topics

• _{Fighting Bacterial Infections}

• Major Classes of Antibiotic Drugs

• Storage of Liquid Antibiotics

• _{Ophthalmic Antibiotics}

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© Paradigm Publishing, Inc. 3

Learning Objectives

• _{Identify the}_{major types of antibiotics}_by

drug class.

• Know which auxiliary labels to use when

dispensing major types of antibiotics.

• Define therapeutic effects side effects, and

administration routes of major antibiotics.

• Use antibiotic and general drug

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Fighting Bacterial Infections

• _Bacteria

– _{Single-celled organisms occurring in}

most environments

• Infection

– _{Condition in which bacteria grow in body}

tissues and cause tissue damage by

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Types of Bacteria

• _Aerobic

– _{Needs oxygen to survive}

• Anaerobic

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Bacteria Shapes

(a) Round cocci (b) Rod-like bacilli

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Gram Stain

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Gram Stain Results and

Related Diseases

Shape Gram Stain Bacteria Related Disease

rods

gram-positive Corynebacteria endocarditis

rods

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Gram Stain Results and

Related Diseases

Shape Gram Stain Bacteria Related Disease

cocci gram-positive

Staphylococcus toxic shock syndrome

cocci

gram-negative

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Gram Stain Results and

Related Diseases

Shape Gram Stain Bacteria Related Disease curved or spiral rods gram-negative Campylobacter septicemia spirochetes

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How Antibiotics Work

• _{Prevent folic acid synthesis}

– _Sulfonamides

• _{Inhibit cell wall formation}

– _Penicillins

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How Antibiotics Work

• _{Prevent folic acid synthesis} • _{Inhibit cell wall formation}

• Block protein formation

– _Macrolides

– _{Tetracyclines}

– Aminoglycosides

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How Antibiotics Work

• _{Prevent folic acid synthesis} • _{Inhibit cell wall formation} • _{Block protein formation}

• _{Interfere with DNA formation} • _{Disrupt cell membranes}

– _{Cyclic lipopeptides}

• _{Disrupt DNA structure}

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Dispensing Issues of

Antibiotics

• _{Mix exactly as directed by manufacturer}

• _{Swab counting tray with alcohol}

between drugs to prevent cross-contamination

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Side Effects of Antibiotics

• _{Most antibiotics taken on an empty}

stomach to attain faster absorption

• _Exceptions

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Antimicrobial Resistance

• _{Developing largely because of} – Overuse

– Misuse

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Antimicrobial Resistance

• _{Pharmacy technician—place a label}

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Terms to Remember

bacteria

infection aerobic

anaerobic

(19)

Terms to Remember

bactericidal agent

(20)

Discussion

How might the widespread use of

antibacterial soaps affect the

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Major Classes of Antibiotic

Drugs

• _Sulfonamides

• _Pencillins

• _{Cephalosporins}

• Tetracyclines and Tigecycline

• Macrolides • _Ketolides

• _Quinolones

• _{Streptogramins}

• Aminoglycosides

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Sulfonamides

• _{AKA “sulfa drugs”}

• _{Effective against a broad range of}

microorganisms

• _{Block specific step in biosynthetic}

pathway of folic acid

• _{Interfere with PABA}_{(para-aminobenzoic acid)}

(23)

Drug List

Sulfonamides

– _{sulfamethoxazole-trimethoprim}

(Bactrim, Bactrim DS, Cotrim, Cotrim DS, Septra, Septra DS)

– _{sulfasalazine (Azulfidine)} – _{sulfisoxazole (Gantrisin)}

– Related drug: nitrofurantoin

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Allergy to Sulfonamides

• _{If patient is allergic to sulfa, then}

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Therapeutic Uses of

Sulfonamides

• _{Urinary tract infections (UTIs)} • _{Otitis media}

• Ulcerative colitis

• _{Lower respiratory infections}

• Prophylaxis in Pneumocystis carinii

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Side Effects of Sulfonamides

• _Rash

• Nausea

• Drug fever

• Vomiting

• _Jaundice_(coloracion

amarillenta por niveles altos de bilirubina)

• _{Kidney damage}

• Blood

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Dispensing Issues of

Sulfonamides

• _{Avoid sun}

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Penicillins

• _{Low toxicity}

• _{Derivatives created by manipulating basic} molecular structure of drug

• _{Kills bacteria by preventing them from} forming rigid cell wall

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Drug List

Penicillin Drugs

– _{amoxicillin (Amoxil)} –_{ampicillin (Principen)}

–_{penicillin G (various brand names,}

also different salts, i.e. potassium, sodium)

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Drug List

Resistant Penicillins

Penicillinase-Resistant Penicillins

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Drug List

Extended-Spectrum Penicillins

– carbenicillin (Geocillin)

(32)

Drug List

Penicillin Combinations

– amoxicillin-clavulanate

(Augmentin)

– ampicillin-sulbactam (Unasyn) – piperacillin-tazobactam (Zosyn)

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Therapeutic Uses of

Penicillins

• _Abscesses

• _{Beta-hemolytic streptococcus}

• _Meningitis

• Otitis media

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Therapeutic Uses of

Penicillins

• _{Respiratory infections} • Strep throat

• Tooth and gum infections

• _{Sexually transmitted diseases (STDs;}

syphilis and gonorrhea)

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Side Effects of Penicillins

• _Diarrhea

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Dispensing Issues of

Penicillins

• _{Take on an empty stomach}

– Food slows absorption

– _{Acids in fruit juices or colas could}

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Resistance to Penicillins

• Penicillinase-resistant penicillins work

against gram-positive aerobes

• Extended-spectrum penicillins are

more resistant to gram-negative bacteria

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Cephalosporins

• _{Mechanism of action similar to}

penicillins

• _{Person allergic to penicillin has about}

(39)

Drug List

First-Generation Cephalosporins

(40)

Drug List

Second-Generation Cephalosporins

– _{cefaclor (Ceclor)} – _{cefprozil (Cefzil)}

(41)

Drug List

Third-Generation Cephalosporins

– _{cefdinir (Omnicef)}

– _{cefditoren (Spectracef)} – _{cefixime (Suprax)}

(42)

Drug List

Third-Generation Cephalosporins

(43)

Drug List

Fourth-Generation Cephalosporins

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Dispensing Issues of

Cephalosporins

• Alert pharmacist if patient who is allergic to penicillin is receiving a cephalosporin Rx

• _{If patient wants cephalosporin dispensed,} document communication in case of cross-reaction

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First-Generation

Cephalosporins

• _{Similar to penicillinase-resistant}

penicillins but have greater gram-negative coverage

• Used for

(46)

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Second-Generation

Cephalosporins

• _{Increased activity, especially against}

Haemophilus influenzae

• _{Used for}

– _{Otitis media in children} – _{Respiratory infections}

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Third-Generation

Cephalosporins

• _{Active against wide spectrum of}

gram-negative organisms

• _{Long half-life, so once-a-day dosing}

for some

• Used for

– _{Ambulatory patients}

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Fourth-Generation

Cephalosporins

• _{Broad-spectrum coverage, such as}

cefepime (Maxipime)

• _{Used for}

– _Pneumonia – _UTIs

– _Sepsis

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Side Effects of

Cephalosporins

• _{Share side effects of penicillin} • A few may initiate unique toxic

reactions

• _{Lower frequency of toxicity than}

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Dispensing Issues of

Cephalosporins

• _{All cephalosporins look alike when}

written in the generic form

• Watch dosing and indications for use

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Drugs Related to Penicillins

and Cephalosporins

• _{New beta-lactam drugs differ slightly}

in structure

• Carabpenems, carbacephems, and

monobactam

(52)

Drug List

Carbapenems

– _{ertapenem (Invanz)}

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Drug List

Carbacephem

– _{doripenem (Doribax)} – _{loracarbef (Lorabid)}

Monobactam

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© Paradigm Publishing, Inc. 54 From Wikipedia, the free encyclopedia

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Tetracyclines

• _{Broad-spectrum bacteriostatic}

antibiotics

• _{Inhibit protein synthesis in bacteria by}

binding to ribosomes

• Suppress infection, but require

(56)

Drug List

Tetracyclines

– _{demeclocycline (Declomycin)}

– _{doxycycline (Vibramycin, Oracea,}

Adoxa)

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Therapeutic Uses of

Tetracyclines

• _Acne • Anthrax

• Chronic bronchitis • Lyme disease

• _Mycoplasma _pneumoniae_infection • Rickettsia infection

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Side Effects of Tetracyclines

• _{Gastrointestinal upset with nausea}

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Dispensing Issues of

Tetracyclines

• _{Avoid antacids to avoid chelation with}

minerals

• _{Photosensitization}

• _{Pregnant women and children up to}

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Dispensing Issues of

Tetracyclines

• _{Expired drugs can be toxic, can}

cause fatal renal syndrome

• Pharmacy technician always watch

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Dispensing Issues of

Tetracyclines

• _{Government agencies stockpiling}

tetracyclines due to concern over terrorist attack

• _{Due to toxicity: must be rotated;}

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Tigecycline

• _{New drug class:}_{glycylcycline} • Similar to tetracyclines

• Used for

– _{Skin infections}

(63)

Drug List

Tigecycline

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Macrolides

• _{Inhibit protein synthesis by combining}

with ribosomes

• _{Used primarily to treat pulmonary}

(65)

Drug List

Macrolides

– _{azithromycin (Zithromax, Z Pak,}

Zmax)

– _{clarithromycin (Biaxin)} – _{dirithromycin (Dynabac)}

(66)

Drug List

Macrolides

– _{erythromycin ethylsuccinate (E.E.S.,}

EryPed)

– _{erythromycin lactobionate}

(Erythrocin)

– _{erythromycin stearate (Erythrocin)} – _{erythromycin-sulfisoxazole}

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Therapeutic Uses of

Macrolides

Drugs of choice for

– _Chlamydia

– _{Group A beta-hemolytic streptococcus} – _{H. influenzae}

– _{Legionnaires’ disease} – _{M. pneumoniae}

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Dispensing Issues of

Macrolides

• _{Most antibiotics taken on empty}

stomach

• _{Some forms of erythromycin can}

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Dispensing Issues of

Macrolides

• _{Can be misread}

– _erythromycin – _azithromycin

• _{Dosing should help identify drug}

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Ketolides

• _{Bind to ribosomal subunits and block} protein synthesis

• May inhibit newly forming ribosomes • Bacteria resistant to macrolides,

lincomycin derivatives, and streptogramins is also resistant to ketolides

(71)

Drug List

Ketolides

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Quinolones

• _{Strong, rapid bactericidal action}

against

– _{Most gram-negative bacteria} – _{Many gram-positive bacteria}

• Antagonize enzyme responsible for

(73)

Drug List

Quinolones

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Therapeutic Uses of

Quinolones

• _{Bone and joint infections caused by} gram-negative organisms

• _{Infectious diarrhea}

• _{Ophthalmic infections}

• _{Some sexually transmitted diseases} • _{Upper respiratory infections}

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Side Effects of Quinolones

• _{Primarily gastrointestinal, with nausea and} vomiting

• _{Some joint swelling, dizziness, and} unpleasant taste

• _{Can cause joint problems and} malformations

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Dispensing Issues of

Quinolones

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Streptogramins

• _{Inhibit protein synthesis within the}

bacterial ribosomes

• _{Alternative to vancomycin}

• _{Side effects similar to quinolones:}

(78)

Drug List

Streptogramins

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Aminoglycosides

• _{Used to treat serious infections}

• Inhibits bacterial protein synthesis by

binding to ribosomal subunits

• _{After first dose, dosage adjusted}

(80)

Drug List

Aminoglycosides

– _{amikacin (Amikin)}

– _{gentamicin (Garamycin)} – _{kanamycin (Kantrex)}

– _{neomycin (Mycifradin, Neo-Fradin,}

Neo Rx)

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Side Effects of

Aminoglycosides

• _{Nephrotoxicity (destructive to kidney)} • Ototoxicity (damage organs of

hearing)

– _{Equilibrium problems} – _Tinnitus

– _{Permanent deafness}

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Dosing of Aminoglycosides

• _{Dosed 1x/daily instead of 2 to 3x/daily}

• Less frequent dosing may reduce toxicity

– _{Less drug accumulates in kidneys and ears}

– _{Simplifies drug monitoring}

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Cyclic Lipopetides

• _{Bind bacterial membranes causing}

cell membrane to depolarize

• _{Leads to}

(84)

Drug List

Cyclic Lipopetides

– _{daptomycin (Cubicin)}

• _{Do not take with statins}

(85)

Terms to Remember

sulfonamides

penicillin

cephalosporin

community-acquired NS

(86)

Terms to Remember

tetracycline

chelation macrolide ketolide quinolone

(87)

Terms to Remember

aminoglycoside

sepsis

nephrotoxicity ototoxicity

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Other Antibiotics

• _{Five important antibiotics are}

structurally distinct from

(89)

Drug List

Antibiotics Independent of Class

– _{clindamycin (Cleocin)} – _{linezolid (Zyvox)}

– metronidazole (Flagyl)

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vancomycin (Vancocin)

• _{Bacterial resistance increasing due to}

overuse

• _{Strict CDC guidelines for handling}

(91)

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clindamycin (Cleocin)

• _{Broad-spectrum antibiotic used for}

– _Acne

– _{Penicillin alternative in dental}

prophylaxis

– _{Anaerobic pneumonia}

– _{Bone and bowel infections}

– Female genital and intra-abdominal

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clindamycin (Cleocin)

• _{If patient develops diarrhea, drug}

(93)

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linezolid (Zyvox)

• _{First oxazolidinone approved by FDA} • Inhibits bacterial protein synthesis

(94)

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metronidazole (Flagyl)

• _{Pharmacy technician—place}

_No

(95)

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pentamidine (NebuPent,

Pentam)

• _{Second-line agent for}_Pneumocystis

carinii

• _{Mechanism of action unknown} • _{Patient may develop sudden}

(96)

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Storage of Liquid Antibiotics

• _{After lyophilized (powdered)}

antibiotics are mixed

– _{Some need refrigeration}

– _{Others stored at room temperature}

• Pharmacy technician may tell storage

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Ophthalmic Antibiotics

• _{Some antibiotics have ophthalmic}

(eye) dosage forms

• _{Very few antibiotics have otic forms}

– _{Very painful in the eye}

– _{Otic medicines have different pH than}

(98)

Drug List

Ophthalmic Dosage Forms

– _{azithromycin (AzaSite)} – _{bacitracin (AKtracin)}

– ciprofloxacin (Occuflox, Ciprodex) – erthromycin (Ilotycin)

(99)

Drug List

Ophthalmic Dosage Forms

– _{gentamicin (Gentak, Genoptic)} – _{moxifloxacin (Vigamox)}

– oxfloxacin (Ocuflox)

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Dispensing Issues of

Ophthalmic Antibiotics

• _{Newer eye drops very expensive,}

often rejected by insurance companies

• Pharmacy technician will need to let

prescriber know

– _{What eye drops are available}

(101)

Terms to Remember

ophthalmic

to be used in the eye

otic

to be used in the ear

pH

(102)

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Treating Complications of

Infections

• _{drotrecogin alfa (Xigris)}

– _{Not an antibiotic}

– _{Used in treating some complications of}

sepsis (life-threatening result of serious infections)

(103)

Drug List

Adjunct in Treating Sepsis

(104)

Discussion

• _{Why is resistance developing to}

antibiotics? Is this a problem?

• _{What role can the pharmacy}

(105)

Assignments

• _{Complete Chapter Review activities} • _{Answer questions in Study Notes}

document

• _{Study Partner}