Anti-infective

agents Nursing

Pharmacology

Anti-infective agents
• drugs that are designed to act selectively on
foreign organisms that have invaded and
 infected the body of a human host.
• Antibiotics - used to treat bacterial infections •
Antivirals, antifungals, antiprotozoals - treat
infections caused by specific protozoa, including
malaria
• Antihelmintics - treat infections caused by worms
• Antineoplastics - treat cancers, diseases caused
by abnormal cells
Mechanisms of Action
• Some anti-infectives interefere with the
biosynthesis of bacterial cell wall. Penicillins work
in this way.
• Some prevent cells of invading organisms from
using substances essential to their growth and
development, leading to inability to divide and
eventually to cell death.
• Many interfere with the steps involved in protein
synthesis, a necessary function to maintain the
cell and allow for cell division. Aminoglycosides,
macrolides and chloramphenicol work in this way.
Mechanisms of Action
• Some interfere with DNA synthesis in the
cell, leading to inability to divide and cell
death. Fluoroquinolones work in this way. •
 Others alter the permeability of cell
membrane to allow essential cell
components to leak out, causing cell death.
Some antiobiotics, antifungals, and
antiprotozoal drugs work in this way. Anti-
infective activity
• Anti-infectives used today vary in their
effectiveness against invading organisms; that is
the spectrum of activity varies.
• Meaning, some are selctive in their action against
 only a few microorganisms > said to have narrow
spectrum of activity.
• Others interfere with biochemical reactions in
many different microorganisms making them
useful for treatment of wide variety of infections >
said to have broad spectrum of activity.
Anti-infective activity
• Bacteriostatic drugs - interfere with the ability of
cells to reproduce or divide.
• Bactericidal - they cause the death of the cells
that affect.
Human immune response - if a client is
 immunocompromised (malnutrition, age. AIDS)
difficult to treat for 2 reasons:
1. cannot totally eliminate the pathogen without
causing severe toxicity in the host
2. these clients do not have immune response in
place to deal with even a few invading organisms.
Resistance
• Because anti-infectives act on specific enzymes
or biological processes, many microorganisms
that do not use that system or process are not
affected by a specific anti-infective drug. These
organisms are said to have natural or intrinsic
 resistance to that drug.
Acquiring resistance (ways):
1. Producing an enzyme that deactivates the
antimicrobial drug.
2. Changing cell permeability to prevent drug from
entering the cell or altering transport systems to
excule drug from active transport into the cell.
Resistance
3. Altering binding sites on membranes or ribosomes. 4.
Producing a chemical that acts as antagonist to the
drug. Preventing resistance:
> Drug dosage is important , should be high enough and
duration of drug therapy should be long enough to
 eradicate or destroy even slightly resistant
microorganisms.
> Health care providers should know the causative
organism.
Identification of the Pathogen - done by culture of
a tissue sample from infected area
Sensitivity of the Pathogen - experience influences
selection of the drug, based on presenting signs
and symptoms thus, in many cases, necessary to
perform sensitivity testing on cultured microbes.
Combination therapy used for several reasons: 1.
may allow doctors to use a smaller dose of each
drug
2. some drugs are synergistic, meaning more
powerful when given in combination.
3. Many microbial infections are caused by
more than one organism.
4. Sometimes, the combined effects of
different drugs delay the emergence of
resistant strains. This is important in TB
and malaria treatment, including some
bacterial infections.
Adverse reactions to anti-infective
therapy
1. Kidney damage - example is use of aminoglycosides ;
pts. should be well hydrated throughout the course of
drug therapy.
2. Gastrointestinal toxicity - causing nausea, vomiting,
stomach upset or diarrhea. Some are toxic to the liver
which can cuase hepatitis or liver failure like many of
cephalosporins.
3. Neurotoxicity - example are aminoglycosides collect in
the 8th cranial nerve can cause dizziness, vertigo and
loss of hearing.
Chloroquine - used to treat malaria can accumulate in
retina and cause blindness. Others can cause
drowsiness, lethargy, reflex changes and even
hallucinations.
Adverse reactions to anti
 infective therapy
4. Hypersensitivity reactions - examples a re
penicillins and cephalosporins have shown
sensitivity or allergic reactions.
5. Superinfections - especially broad-spectrum can
destroy normal flora. When normal flora is
destroyed, opportunistic pathogens can ivade
tissues and cause infections thus called
superinfections. Common superinfections are
vaginal or GI yeast infections and infections
caused by Proteus and Pseudomonas.
6. Prophylaxis - prevent infections before they
occur.
 Antibiotics
Aminoglycosides - used to treat serious
infections caused by gram-negative
aerobic bacilli.
1. amikacin (Amikin) short-term IM or IV and
can cause nephrotoxicity and ototoxicity. 2.
gentamicin (Garamycin) - ophthalmic,
topical, IV
3. streptomycin - very toxic to the 8th cranial
nerve and kidney. Used for TB treatment.
 Antibiotics
Cephalosporins - similar to penicillins in
structure and activity.
1. First-generation - effective against same
gram-positive bacteria that are affected by
penicillin G and and gram-negative
bacteria like E.coli and Klebsiella
pneumoniae.
Examples: cefazolin and cephalexin 2.
Second-generation - effective against
Haemophilus influenzae and Neisseria
species. They are less effective against gram
positive bacteria.
Examples: cefaclor, cefoxitin, cefuroxime
3. Third-generation - more potent against
gram-negative bacilli.
Examples: cefotaxime,ceftazidime,
ceftriaxone
Fluoroquinolones - have broad spectrum of
activity
Example: ciprofloxacin - effective against a wide
spectrum of gram-negative bacteria. Available in
 injectable, oral and topical forms.
Macrolides - interfere with protein
synthesis Examples:
1. erythromycin - good susbstitute for those
allergic to penicllins
2. azithromycin - used for treating mild to moderate
respiratory infections and treating otitis media,
pharyngitis and tonsilitis in children
3. clarithromycin - expensive oral agent for
respiratory, skin and sinus infections and
mycobacteria.
Penicillins - discovered by Alexander Flemming;
bactericidal and used for treatment of streptococcal
infections including pharyngitis, tonsilitis, endocarditis,
 pneumococcal, staph, meningococcal meningitis.
Examples: penicillin G, amoxicillin, ampicillin
Anti-TB drugs (6 months to 2 years)
1. First-line antiTB drugs -
A. isoniazid - affects mycolic acid of bacterium B.
rifampin - alters DNS and RNA bacterium activity 2.
Second-line
A. ethambutol - inhibits cell metabolism
B. pyrazinamide - both bactericidal and bacteriostatic