Transcript Chapter 2 Law and Ethics of Pharmacy Teresa Hopper

Chapter 24
Antiinfectives
Copyright © 2004 by Elsevier Inc. All rights reserved.
Introduction
• Immune system:
– Body built-in defense system
– Identifies and kills foreign bodies
• Antibiotics–help when invading
organism gets out of hand
• Antibiotic–against life
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Introduction
• Antibiotic–natural or synthetic
substance that inhibits or destroys
microorganisms
• Antimicrobial–substances produced
by scientists used against human
infections
• Normal flora–bacteria residing in
human body (mutually beneficial)
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Introduction
• Normal flora–intestines, mouth, throat
• Antibiotics–bacteriostatic, bactericidal
• Bacteriostatic–arrest development or
stop growth of microbes
• Bactericidal–kill microorganisms
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History of Antibiotics
• 1930s–first antibiotic, sulfa
(sulfanilamide) discovered
• Cure staphylococcus infections–
bacteriostatic
• Mass production–WWII
• Used often without regard for
possibility of resistance
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History of Antibiotics
• Patients take drug–feel better–stop
taking drug
• Remaining microbes–build immunity
to drug–infection reappears–bacteria
more resistant to antibiotic
• Microbes–can alter genetic makeup
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History of Antibiotics
• Overuse and misuse of antibiotics–
new strains of bacteria make
antibiotic ineffective
• 1960s–sulfa obsolete
• Limited use today–UTIs, respiratory
infections
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The Discovery of Penicillin
• Alexander Fleming–discovered
penicillin by accident–he inadvertently
contaminated an agar plate with mold
called Penicillium notatum
• Zone of clearance (chemicals from
mold kill off surrounding
microorganisms on plate)
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A petri dish is prepared with nutrient-rich agar. This nutrient feeds
the bacteria which are placed on the plate. The penicillium colony
can be seen with an area of clearance where the bacteria cannot
grow. This occurs because the penicillium inhibits the bacterial
growth.
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History of Antibiotics
• Penicillin agents–around since 1940s–
very effective; bactericidal effect
toward gram-positive bacteria
• 100 individual drugs–available to
combat range of infections
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Gram Stain
• Hans Christian Gram–developed
Gram stain procedure in 1883
• Determine morphology (shape and
appearance) of bacteria
• Gram-positive–bacteria have thick
outer membrane made of
peptidoglycan links
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Gram Stain
• Penicillin–enters links, breaks them,
kills them
• Gram-negative–different type of cell
wall; harder to kill
• Newer antibiotics–kill gram-negative
microorganisms
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Modern Antibiotics
• Penicillinase-producing microbes–
made penicillin ineffective
• Amoxicillin + clavulanate–Augmentin
(strengthens penicillin)
• Ampicillin + sulbactam–Unasyn
• Agents–inhibit the penicillinase
enzymes from breaking down the
antibiotic
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Types of Infections
and Their Treatments
• Common infections–can appear
anywhere on or within the body
• Cause–exposure to environment,
foods we eat, contact with others
• Types of microorganisms include
bacteria, fungi, protozoa, viruses (not
technically an organism), and
multicellular microscopic parasites
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Types of Infections
and Their Treatments
• Internal body–normally a sterile
environment (does not include parts
open to the environment or those that
contain outside substances)
• Body–subject to bacterial, viral,
parasitic infections
• Common areas to be infected–male and
female genital systems; GI tract; upper
and lower respiratory system; skin;
nose and mouth; eyes and ears
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Sexually Transmitted Diseases
(STDs)
• Caused by various bacteria, protozoal
organisms, and viruses
• Can do permanent damage to internal
organs
• Must be treated with correct antibiotic
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Gastrointestinal (GI) Infections
• Stomach–highly acidic environment
usually destroys any bacteria
• Stomach lining injured, juices not
strong enough to kill microbes–
infections occur
• Helicobacter pylori–major infection
of stomach
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GI Infections
• H. pylori–triple drug therapy used
to eradicate: tetracycline, Septra,
metronidazole (bactericidal effect
on bacilli)
• Other areas susceptible to infection–
mouth, throat, trachea
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GI infections
• Anaerobic microbes–do not live in air
• Aerobic microbes–live in air
• Facultative anaerobes–tolerate
oxygen to a certain degree
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Respiratory Infections
• Small particles, microorganisms–
inhaled on dust (bacteria, fungus,
viruses)
• Settle in airways and cause infection
• Common symptoms–wheezing,
coughing, shortness of breath
• Pneumonia–most serious respiratory
infection
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Respiratory Infections
• Pneumonia:
– Infection of the lungs
– Caused by bacteria, viruses, fungi,
parasites, chemicals
– Nosocomial–acquired in hospitals
or nursing homes
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Respiratory Infections
• Elderly and bedridden patients–high
risk of acquiring pneumonia
• Patients with chronic conditions high
risk also–emphysema, bronchitis,
asthma, immunosuppressive disorders
• TB–highly contagious, caused by
Mycobacterium tuberculosis
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Respiratory Infections
• TB–causes inflammation, abscesses,
necrosis, fibrosis of respiratory
system (can spread to other parts
of the body)
• HIV and AIDS–contributes to rise in TB
• Symptoms–chronic coughing, fever,
sweating, weight loss
• Diagnosed by TB skin test and sputum
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Respiratory Infections
• Fungal infections–more prone to
infect patients with:
– Other major illnesses, such as
cystic fibrosis
– Compromised immune systems
(AIDS, cancer patients on
chemotherapy, patients on multiple
antibiotics)
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Respiratory Infections
• Two most common fungal infections–
Candida albicans, Aspergillus
fumigatus
• Bacterial infections–secondary to
chemical exposure–toxins that are
inhaled in fumes
• Asbestos–if inhaled, causes scarring
of lungs; decreases the capacity of
lungs to take in oxygen
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Nosocomial Infections
• Infections acquired in hospitals and
nursing homes
• Hand sanitization and handwashing
major steps to prevention of
nosocomial infections
• Can be deadly
• Can be bacterial, fungal, viral
• Hard to fight
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Infections of the Skin
• Children–skin abrasions, cuts, scrapes
• Keep clean and free from bacteria
• Diabetics–high risk of infections of
skin; lack of blood flow to extremities,
cause septic infections, gangrene
• Hospitalization, strong antibiotics
necessary
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Infections of the Skin
• Fungal infections–common on skin
surface
• Fungus–needs high concentration of
oxygen to live
• Common fungal infection–Tinea pedis
(athlete’s foot)
• OTC medications available
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Infections of Nose and Mouth
• Nose and mouth–constant contact
with air-borne microbes
• Minor colds, flulike symptoms–OTC
products bring relief
• Colds, flu–viral; antibiotics useless
against them
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Infections of Eyes and Eyes
• Eyes, ears–susceptible to infections
because of exposure to environment
• Conjunctivitis–most common eye
infection; inflammation of lining of
eyelids and cornea (conjunctiva)
• Styes–appear on eyelids–discharge
of pus
• Seasonal allergies–cause
conjunctivitis
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Infections of Eyes and Ears
• Otitis media–common ear infection
in babies and children
• Two types–acute and chronic
• Acute–bacterial infection begins as
upper respiratory infection then
proceeds to infect ear
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Infections of Eyes and Mouth
• Chronic form–repeated infections;
cause inflammation of tympanic
membrane; very painful
• Chronic otitis media–may also result
from rupture of tympanic membrane
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Antibiotic Treatments
• Antibiotics–referred to as widespectrum or narrow-spectrum agents
• Narrow-spectrum–covers mostly
gram-positive microbes
• Wide-spectrum–covers gram-positive
and gram-negative microbes
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Penicillin
• Taken from two different molds–
Penicillium notatum and Penicillium
chryogenum
• Grown in laboratories and synthetically
altered to fight off microorganisms
• Drug action–bactericidal against
currently reproducing bacteria
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Penicillin
• Disrupt formation of cell wall so that
bacteria cannot keep a constant
osmotic gradient and lyses (breaks
open)
• Penicillin-type agents–cover mostly
gram-positive organisms
• Susceptible to stomach acid
degradation–take 1 to 2 hours
after meals
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Penicillin
• Infections of GI system–more potent
antibiotics required
• Broader spectrum “cillins”–ampicillin
and carbenicillin–kill both grampositive and gram-negative organisms
• Allergy–nausea, vomiting, diarrhea,
headache, sore mouth, rashes, pain,
fever
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Cephalosporin
• Less affected by stomach acids
• Can be taken with meals
• 10% chance of allergic reaction for
those with penicillin allergies
• Cephalosporin drug listing
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Mycobacterium and
Mycobacterial Treatment
• Two main infections in humans
caused by mycobacterium–TB,
Leprosy
• Both infections–chronic
• Leprosy (Hansen’s disease)–caused by
Mycobacterium leprae
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Leprosy (Hansen’s Disease)
• Caused by Mycobacterium leprae
• Skin lesions appear, ulceration of
feet, loss of hand function, corneal
abrasions, blindness
• Can be treated with dapsone
(bacteriostatic) and clofazimine
(bactericidal)
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TB
• Wasting disease–robs person of
breath and strength
• Many people quit taking medicine
once they felt better–microbe able to
withstand low doses of antibiotics
until became resistant
• 2/3 prisoners have TB–no medication
available to combat disease
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TB
• Few antituberculin-type medications
• Must be taken for full course of
treatment (6 months or years
depending on test results)
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Antituberculin Agents
Generic
Trade
Dosing
Regimen
Isoniazid
Abbreviation: INH
300 mg qd
6-24 months
Rifampin
Rifadin
600 mg qd
Months
to years
Ethambutol
Myambutol
800 mg to
1.6 gm qd
Months
to years
Pyrazinamide
Pyrazinamide
1-2 gm qd
Months
to years
Cycloserine
Seromycin
750 mg to
1 gm qd
Bacteriostatic:
used for
retreatment
Kanamycin
Kantrex
500 mg to
1 gm qd
Bactericidal:
used for
retreatment
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Length
of Time
Aminoglycosides
• Strongest agents in use today
• Bactericidal for many gram-negative
microorganisms
• Drug action–(parenteral) ability to
bind to ribosomes of microorganism
stopping protein synthesis, causing
death
• Narrow range between therapeutic
and toxic levels
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Aminoglycosides
• Calculations needed to determine
appropriate dosage
• Patient’s blood levels of antibiotic
at peak and trough levels drawn for
evaluation
• Patients with renal disease and older
adults–more susceptible to toxic levels
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Additional Antibiotics
• Drug action, indications
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Antibiotic Reference Table 3
Class
Generic
Trade
Indication
Drug action
Tetracyclines*
doxycycline
tetracycline
minocycline
Vibramycin
Achromycin
Minocin
Severe infections
such as respiratory,
GI, and skin
IPS*
Fluoroquinolones†
ciprofloxacin
levofloxacin
ofloxacin
norfloxacin
Cipro
Levaquin
Floxin
Noroxin
TB, Respiratory,
and UTIs
IBDNAS*
Macrolides
azithromycin
clarithromycin
erythromycin
erythro
ethylsuccinate
erythromycin
state
Zithromax
Biaxin
Emycin, Ery-Tab
EES
Respiratory, genital,
GI, and skin
infections
IPS*
Erythrocin
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Antibiotic Reference Table 3
(continued)
Class
Generic
Trade
Indication
Drug action
Carbapenems
imipenem/
cilastin
Primaxin
Serious infections
IBCWS*
Monobactam
aztreonam
Azactam
Wide-spectrum
gram-negative
aerobic
organisms
IBCWS*
Vancomycin
vancomycin
Vancocin
Serious/severe
infections
IBCWS*
GI, gastrointestinal; IBCWS, inhibits bacterial cell wall synthesis; IBDNAS, interferes with bacterial DNA
synthesis; IPS, inhibits protein synthesis; TB, tuberculosis; UTI, urinary tract infection.
*Auxiliary labels: Take on an empty stomach. Take with plenty of water. Avoid dairy products. Avoid
antacids.
Avoid direct sunlight.
†Auxiliary labels: Do not take antacids. Avoid iron/zinc supplements 4 hours before or 2 hours after taking
domestication.
This medication may be either bacteriostatic or bactericidal depending on strength of dosage
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Antifungals
• Fungi–plantlike organisms–grow on
cloth, food, showers, people, warm
moist environment
• Absorb nutrients from environment
or hosts (animals, humans)
• Affect outside of body, not life
threatening, great annoyance;
systemic infection more serious
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Candida Infections
• Candida albicans–resides inside
human body; gets out of control in
weakened immune system
• Candida–different species;
responsible for infections in mouth,
vagina, under finger/toe nails
• Dermatophytic infections–on skin
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Candida Infections
• Agents applied directly to skin
• Infection in bloodstream–parenterals
used
• Topical agents–lotions, creams,
ointment, powders, sprays
• Available OTC (fungicidal, fungistatic)
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Tinea Infections
• Dermatophytosis–caused by
Trichophyton, microsporum, or
Epidermophyton fungus
• Tinea pedis (Athlete’s foot)
• Tinea capitis or ringworm–in scalp
• Babies in groin area–cruris or
diaper rash
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Parasites
• Benefit at the expense of another
• Host–organism being used by parasite
• Kingdom Protista–Phylum Sporozoa
• Morphology–multicellular or
unicellular and how transmitted
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Parasitic Organisms
And Their Description
Cilia
Hairlike structures that work
like oars moving the organism
along
Flagella
A whiplike tail that propels
the organism along
Pseudopodia Footlike protrusions that move
the organism slowly along
Stationary
A cyst form that waits for an
opportunistic environment
before regenerating
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Protozoal Infections and Their
Treatments
Species
Disease name
Transmission
Treatment
Toxoplasma gondii
Toxoplasmosis
Contaminated food,
water, feces of a
bug or cat. Sand
flies, tsetse flies also
carry the disease
Pyrimethaminesulfdiazine Trimethoprim/
sulfamethoxazole
Pentamidine (IV)
Azithromycin
Plasmodium vivax
Malaria
Female mosquitoes
Chloroquine
Quinine
Mefloquine
Primaquine
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Parasitic Conditions–Protozoa
• Human parasites–many protozoa
• Amebiasis–caused by Entamoeba
histolytica
• Cyst form–transmitted via fecal-oral
routes
• Symptoms–abdominal pain, nausea,
flatulence, fatigue
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Parasitic Conditions–Protozoa
• Treatment–Iodoquinol–rids body of
infestation
• Toxoplasmosis–most dangerous
to humans
• Toxoplasma gondii–transferred via
uncooked meat or cysts present in
cat feces; deadly to both infants and
unborn fetus
• Treatment–pyrimethamine,
sulfadiazine
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Parasitic Conditions–Protozoa
• Trichomoniasis–caused by
Trichomonas vaginalis–affects
vaginal area
• Protozoa–affects male and female
urethra
• Metronidazole–drug of choice–must
be used by both sexual partners
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Helminths (Worms)
• Parasitic worms; multicellular
• Two major worms:
– Roundworms (nematodes)
– Flatworms (platyhelminthes)
• Roundworms–50 species that affect
humans (transferred in undercooked
meat)
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Helminths (Worms)
• Some species lodge in the intestines
or lymph nodes, causing harm to host
• Hookworms (type of roundworm)–
transferred via feces through skin
contact
• Flatworms–tapeworms and flukes
• Live by feeding off dead matter or
small organisms (not harmful to
humans)
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Helminths (Worms)
• Tapeworms–reside in intestines
where they absorb food from host
• Eating undercooked meat transfers
them to humans
• Flukes–acquired from water drunk
from feces-contaminated water
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Helminths (Worms)
• Many infections occur:
– In people who live in areas where
sanitation is nonexistent
– Where people are not aware
of problem
– Eating raw meat
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Antihelminthes
and Their Treatments
Species or
Disease Name
Symptoms
Treatment
Roundworms
Trichinosis
Inflammation
Diethylcarbamazine,
ivermectin
Hookworms
Ankylostoma
duodenale,
americanus
Anemia,
weakness,
fatigue
Mebendazole,
albendazole, pyrantel
Pinworms
Enterobius
vermicularis
Anal itching
Mebendazole,
albendazole, pyrantel
Bladder worm
Cysticercus
Forms a cyst
Praziquantel
that can be as
large as an
orange:
symptoms vary
depending on
area infected
Phylum Nematoda
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Antihelminthes
and Their Treatments (continued)
Species or
Disease Name
Symptoms
Treatment
Phylum
Platyhelminthes
Tapeworms
Taenia saginata,
Taenia solium
Diarrhea, weight
loss, perforation
of intestine
Praziquantel,
niclosamide
Flukes
Schistosomiasis
Loss of blood
in feces
Praziquantel
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Parasitic Treatments
• Few ways to deal with parasites:
– Kill them and wash them away
– Rid them from body alive or dead
– Surgically remove them
– Agents–all oral dosage forms
• Main goal–remove from body
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Parasitic Treatments
• Dosage regimen–short term; done in
few oral doses
• All parasites–cause damage to
tissues or organs invaded
• Weaken but do not kill host
(food and shelter cut off)
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Antihelminthic Agents Action of
Drug and Common Dosage
Generic
Trade
Drug Action
Common Dosage
Diethylcarbamazine Hetrazan
Cidal: increases the
loss of filariae,
decreases ability to
produce more
2-3mg/kg po tid
Mebendazole
Vermox
Vermicidal: stops
glucose uptake in
worm
100mg po bid x 3 days
Niclosamide
Niclocide
Cidal: affects
mitochondria
decreases metabolism
8gm x 1 dose or 2gm
po qd x 1 week
(depends on type
of worm infestation)
Oxamniquine
Vansil
Cidal: causes worms
to move to liver
where they are killed
12-15mg/kg po x 1
(dose may vary
depending on type
of worm infestation)
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Antihelminthic Agents Action of
Drug and Common Dosage (continued)
Generic
Trade
Drug Action
Common Dosage
Praziquantel
Biltricide
Paralysis: causes
loss of calcium and
eventual paralysis
of worm which is
then flushed out
25mg/kg pd
tid x 1 day
Pyrantel
Antiminth
Paralysis: causes
depolarization and
eventual paralysis
of worm which is
then flushed out
11mg/kg po x 1 dose
May be repeated
in 2-3 weeks if
necessary
Thiabendazole
Mintezol
Vermicidal: inhibits
essential enzymes
causing death
25mg/kg po
bid x 2 days
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Malaria
• Sporozoan infection
• Symptoms–fever, chills, sweating,
headache, nausea
• Plasmodium–four species responsible
for malaria
• Falciparum–cause death
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Malaria
• Human body–site of sporozoan
reproduction (reservoir)
• Transmission–infected mosquito
• Sporozoa–can be transmitted by
infected needles or syringes, blood
transfusion
• Incubation period–1 week to 1 month
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Malaria
• Prevention and control–control
mosquitoes by insect repellants, fill
in water holes, insecticides
• Diagnosis–blood smears
• Treatment–Chloroquine phosphate
• Resistant strain–mefloquine,
doxycycline, primaquine
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Antivirals
• Viruses–cannot live outside of hosts
• Classification–nucleic acid makeup,
size, host it infects, enveloped or
naked
• Viruses–need host’s DNA to replicate
• Kill host’s cell on leaving or bud off
allowing further reinfections
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Antivirals
• Viruses–do not have ability to
reproduce themselves in same way
as other organisms do
• Makeup closely related to human DNA
• Agents used to destroy virus also
destroy human cells
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Antivirals
• Viral diseases–chicken pox, colds,
influenza, polio, rabies, warts, HIV,
AIDS, cancer
• Five steps in invasion of virions
• Antivirals drug action
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Colds/Flu
• No cure; caused by viruses
• Viruses–mutate very well; change
every year
• Influenzas–can cause death in older
adults and immunocompromised
persons
• Vaccines–given each year to higher
risk persons
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HIV/AIDS
• Bloodborne, sexually transmitted
virus
• No cure
• Virion–does not cause death; renders
host too weak to fight off infections
• HIV virus–attacks immune system of
humans
• Transmitted by body fluids containing
virus
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HIV/AIDS
• Practice safe sex
• Medical settings–protective wear
decreases risk of contamination
• Beginning stages of HIV–body
weakens, T4 lymphocytes decrease
• T-cell count below 200–AIDS
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HIV/AIDS
• Treatments–for both HIV and AIDS
• Aimed at controlling progression of
disease but cannot cure it
• Only way to avoid disease–prevent
contracting it
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Miscellaneous Viral Conditions
• Papillomavirus–causes common
warts
• OTC medications available–Wart-Off
• Herpes viruses–three main types
• Herpes simplex type 1 and type 2
• Herpes zoster
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Miscellaneous Viral Conditions
• Herpes type 1–causes blisters on
surface of skin; can cause blindness
if left untreated
• Herpes type 2–causes infection in
both adults and neonates (contracts
it during birth)
• Herpes zoster–affects nerve endings;
severe pain (shingles)
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Miscellaneous Viral Conditions
• Herpes zoster–cyclical reinfections
• Also causes chicken pox
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Immunity
• Two types:
– Active or passive
• Active–occurs if immunity is from
antibodies produced by the body
(natural or artificial)
• Passive–natural or artificial
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