Antibacterial Drugs 1

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antibactERial

dRUgs (V.2023)

Manny L. Mamaril, RN, MAN, LPT, PhD


School of Nursing
PathogEnicity and viRUlEncE
Pathogenicity Virulence Mechanisms
✔ Capability of microbes/organisms to 1. Invasiveness
cause a disease ✔ Ability of the pathogen to grow
✔ Human pathogens: Viruses, bacteria, extremely rapidly and cause
fungi, unicellular organisms direct damage to surrounding
(protozoans), and multicellular animals
(fleas, mites, and worms) tissues by sheer numbers
✔ Example: Streptococcus A group
✔ Enter through broken skin, ingestion, bacteria that cause necrotizing
inhalation, or contact with a mucous fasciitis (flesh-eating disease)
membrane such as the nasal, urinary,
2. Production of toxins
or vaginal mucosa
✔ Example: Clostridium tetani
Virulence which produces tetanospasmin
✔ A pathogen that is able to produce which interfere with motor neuron
activity which causes tetanus
disease when present in small
numbers
BACtERiA
ClAssifiCAtiOn Of bACtERiA
1. GRAft STAIN 3. ABILTY TO USE OXYGEN
✔ Application of dyes on a ✔ AEROBIC – Thrive on oxygen-
bacterial sample to rich environment
✔ ANAEROBIC - Grows best
determine if the bacteria is
gram-positive or gram-
negative without oxygen
2. CELLULAR SHAPE ❖ Importance: It will determine
✔ Rods – bacilli what type of medications will
✔ Spherical shapes – cocci
be used in treating diseases
✔ Spirals – spirilla
GRAM-StAin PROCEDURE
BACtERiAL sHAPEs
OxygEn
REqUiREMEnts
1. Obligate Aerobes – Grow in
the presence of oxygen
2. Obligate Anaerobes – Grow in
the absence of oxygen
3. Facultative Anaerobes –
Show better growth in the
presence oxygen but can live
without oxygen
4. Aerotolerant Anaerobes – Can
grow in the presence of
oxygen but can live without
oxygen
Anti-infECtivE DRUgs Bactericidal Drugs

✔ Any drug that is effective ✔ Drugs that kill


against pathogens such as bacteria
drugs for bacterial, fungal, Bacteriostatic Drugs
viral, or parasitic infections ✔ Slow down growth of bacteria allowing the
✔ Goal: Assist body’s defenses in body’s
eliminating pathogen natural defenses to eliminate the
microorganisms
Antibiotics
Selective Toxicity
✔ Drugs that eliminate bacteria ✔ Characteristic of antibiotics to target
✔ Pharmacologic classes are bacteria due to their cell walls, different
grouped according to their biochemical pathways, and production of
mechanism of action certain enzymes
ACqUiRED REsistAnCE
✔ Drug-resistance/ Drug-insensitivity
of certain bacteria
✔ Spontaneous and random
mutations in the bacterial
chromosome during replication
that result in reproductive
advantages
✔ Ability to survive in harsh
conditions such as in the presence
of antibiotics
✔ Cause: Widespread and
unwarranted use of antibiotics
HOsPitAL-
ACqUiRED
infECtiOns (HAI)/
NOSOCOMIAL
INFECTIONS
WAys tO COMbAt DRUg-REsistAnCE AnD HAi
1. Prevent infections when possible
✔ Immunizations 4. Advise patients to take anti-
infectives for the full length of
2. Use right drug for infection
therapy
✔ Perform culture and sensitivity
tests 5. Prevent transmission of the
pathogen
✔ Apply standard infection
3. Restrict use of antibiotics to those
conditions deemed medically control procedures
necessary ✔ Teach patient proper hygiene
✔ Use antibiotics for bacterial
infections not viral infections
unless warranted (example:
prophylactic therapy)
HOst fACtORs AffECting AntibiOtiC tREAtMEnt
1. Host Defenses 4. Other Patient Variables
✔ Patient’s immune system condition ✔ Age, pregnancy status, and
✔ Patients with compromised or genetics

suppressed immune system will Very young and very old cannot
need stronger drugs metabolize or excrete antibiotics;
2. Local Tissue Conditions doses should be lowered
✔ Conditions at the infection site ✔ Drugs can cross placenta –
✔ CNS infections require stronger Tetracyclines
drugs to cross the blood-brain
barrier ✔ Patients with G6PD cannot receive
sulfonamides, chloramphenicol or
3. Allergy History nalidixic acid because their RBC
✔ Allergy to antibiotics can be fatal may rupture
✔ Always take the drug history
MECHAnisMs
Of ACtiOn Of
AntibACtERiAL
DRUgs
MECHANISMS OF ACTION OF ANTIBIOTICS

1. Cell Wall Synthesis Inhibitors


✔ Interfere with peptidoglycan synthesis

2. Protein Synthesis Inhibitors


3. Use the Biochemical Pathways of the Bacteria
to Form ftetabolites
4. RNA Synthesis Inhibitors
5. DNA Synthesis Inhibitors
PEniCiLLins
PEniCiLLins
✔ First mass-produced antibiotic
✔ Isolated from the fungus, Penicillium
in 1942
✔ MOA: Weakens bacterial cell wall by
binding to penicillin-binding
receptor, which causes water to
enter the cell killing the organism
✔ Gram + bacteria are commonly
affected including the
staphylococci and streptococci
PEniCiLLins
✔ Penicillin G potassium ✔ Adverse Effects: ftinor:
✔ Indications: Pneumonia;
Allergy – rash, pruritus, and
fever; Less common AEs -
meningitis; skin, bone and
Lowered RBC, WBC, or
joint infections; stomach
platelet counts
infections; blood and valve
infections; gas gangrene; ❖ Allergy to one penicillin
tetanus; anthrax; and sickle- increases risk of allergy to
cell anemia in infants other drugs in the same
✔ One of the safest class of
class
antibiotics ❖ Bactericidal
PEniCiLLin-
REsistAnCE
✔ Beta-lactam ring is
responsible for
antibacterial activity
✔ Beta-lactamase or
penicillinase is secreted by
some resistant bacteria,
which splits the ring into
two and inhibits
antibacterial activity
CHEMiCALLy-MODifiED PEniCiLLins vs REsistAnt bACtERiA
3. Extended-Spectrum Penicillins
1. Penicillinase-Resistant Penicillin ✔ Piperacillin
✔ Oxacillin and dicloxacillin ✔ Effective against more microbial
species than aminopenicillins, which
(antistaphylococcal drugs) include Enterobacter, Klebsiella, and
Bacteroides fragilis, and
2. Broad-Spectrum Penicillin Pseudomonas aeruginosa, which is
(Aminopenicillin) responsible for cases HAIs

✔ Amoxicillin and ampicillin 4. Beta-Lactamase Inhibitors


✔ Available as fixed-dosed combinations
✔ Effective against a wide with other penicillins
range of ✔ Clavulanate + amoxicillin = Co-
microorganisms Amoxiclav(Augmentin)

✔ For upper respiratory and
Clavulanate + ticarcillin = Timentin
✔ Sulbactam + ampicillin = Sultamicillin
genitourinary tract infections (Unasyn)
✔ Tazobactam + piperacillin = Zosyn
NURsing PROCEss nOtEs: PEniCiLLins
In-Patient ftanagement Out-Patient ftanagement
✔ Assess for allergy to penicillin or ✔ Educate patient to finish entire
cephalosporins prescription
✔ Liver enzymes: ALP, ALT, and AST ✔ Inform healthcare staff about
✔ Urine output of >30ml/h or >600ml a medications and drug allergies
day ✔ Discontinue drug if there are
✔ ftonitor vital signs particularly signs of allergy and consult the
temperature doctor right away
✔ ftonitor infected area ✔ Keep drugs away from children
✔ Have epinephrine available for ✔ Increase fluid intake

severe allergic reactions
Take medications with food
✔ Evaluate drug side effects
CEPHALOsPORins
CEPHALOsPORins
✔ One of the largest antibiotic class (20 ✔ CI: Patients who have
available) experienced penicillin allergy
✔ Classified by generation
✔ AE: Allergic reactions – skin
✔ Bactericidal rashes, GI complaints; Earlier
✔ MOA: Contain a beta-lactam ring generations can cause kidney
which attach to penicillin-binding toxicity
proteins and inhibit bacterial wall ❖ Safe drugs with similar AEs to
synthesis those of penicillin
✔ Indications: Often used for gram-
negative infections and for patients
who cannot tolerate penicillins
CEPHALOsPORins
1st Generation – Cephalexin, Cefazolin
✔ DOC for Pseudomonas,
✔ ftost effective against gram-positive organisms Klebsiella, Neisseria, Salmonella,
including staphylococci and streptococci Proteus and H. influenza
✔ Beta-lactamase bacteria is 4th and 5th Generation – Cefepime,
resistant 2nd Generation – Cefaclor, Ceftaroline

Cefuroxime Effective against organisms that
✔ ftore potent and more resistant to beta-lactamase developed resistance to earlier
✔ Broader spectrum against gram-negative cephalosporins
organisms 3rd Generation – Cefixime, ✔ 4th Gen – Can enter CSF to treat
Ceftriaxone CNS infections
✔ Broader spectrum than second-generation drugs ✔ 5th Gen – To treat ftRSA infections
✔ Longer duration of action and resistant to beta-
lactamase
NURsing PROCEss nOtEs: CEPHALOsPORins
Out-Patient ftanagement
In-Patient ftanagement
✔ Educate patient to finish entire
✔ Assess for allergy to
prescription
cephalosporins or penicillins
✔ Inform healthcare staff about
✔ Record elevated temperature or
medications and drug allergies
decreased urine output
✔ Discontinue drug if there are signs of
✔ Renal and Liver labs: BUN, serum
allergy and consult the
creatinine, AST, ALT, ALP and
bilirubin doctor right away
✔ Perform culture and sensitivity ✔ Keep drugs away from children
tests ✔ Report superinfections
✔ Ingest buttermilk, yogurt, or
acidophilus supplement to prevent
superinfection of intestinal flora
✔ Drink adequate amounts of fluids
tEtRACyCLinEs
tEtRACyCLinEs
✔ MOA: Bind to bacterial ribosomes and inhibit bacterial protein synthesis
✔ Bacteriostatic – slow down microbial growth
✔ Indications: Rocky fmountain spotted fever, typhus, cholera, Lyme
disease, peptic ulcers cause by H. pylori and chlamydial infections;
Acne vulgaris when used topically or in PO low doses
✔ Contraindications: Patients younger than 8 years old and pregnant
women; Not to be taken with milk or iron supplements; Patients with
pre-existing liver disease
✔ AE: Gastric distress, photosensitivity; Yellow discoloration in
teeth of children; Fetal bone and teeth malformation ; Superinfection in
high doses
TEtRACyCLinEs
✔ Doxycycline and minocycline have longer
duration of action and are more lipid-soluble
which make them enter the CSF
✔ Tigecycline (newest) used for drug-resistant
intra-abdominal infections especially caused by
ftRSA; AE are nausea and vomiting; Available
IV infusion
❖ Certain drugs can be hepatotoxic
❖ Discard when outdated because it can be
NURsing PROCEss nOtEs: TETRACYCLINES
In-Patient ftanagement Out-Patient ftanagement


Educate patient to finish entire prescription
Labs: Renal and Liver function
✔ Inform healthcare staff about medications and drug
(BUN, serum creatinine, AST, ALT, adverse effects
bilirubin) ✔ Store tetracycline away from light and extreme heat
✔ Drug and diet history; Dairy ✔ Check expiration dates
product, antacids, iron, calcium, ✔ Explain teratogenic effects to pregnant patients
magnesium, and digoxin ✔ Explain side effects like yellowing of teeth to

parents with children younger than 8 years old
Culture and sensitivity tests
✔ Use sun block and protective clothing during sun
✔ Administer tetracycline 1 hour exposure
before or 2 hours after meals for ✔ Report signs of superinfection
optimum absorption ✔ Oral hygiene
✔ Avoid milk products, iron, and antacids
MACROLiDEs
MACROLiDEs
Erythromycin, azithromycin, ✔ positive bacteria and many
Effective against gram-

clarithromycin gram-negative species
✔ Isolated from Streptomyces ✔ Drugs are used against
in a soil sample in 1952 bacteria residing INSIDE host
✔ Safe alternatives to penicillin cells (intracellular parasites)
such as Listeria, Chlamydia,
✔ Low doses- bacteriostatic; Neisseria, and Legionella
higher doses in susceptible ✔ Indications: Whooping
organisms – bactericidal cough, Legionnaire’s
✔ MOA: Inhibit protein synthesis disease, and infections by
streptococcus, H. influenza,
by binding to the bacterial and ft. pneumoniae
ribosomes
MACROLiDEs
✔ Clarithromycin – Used to treat
✔ Broad-spectrum peptic ulcer disease due to its
antibiotics activity against H. pylori
✔ Contraindications: ✔ Azithromycin – Newer drug;
Drug allergy Longer half- life and cause
✔ AE: mild GI upset, less gastric irritation;
Administered only for 5 days;
diarrhea, and
Single dose effective against
abdominal pain; gonorrhea
Superinfection
NURsing PROCEss nOtEs: MACROLiDEs
In-Patient Management Out-Patient Management
✔ Vital signs and urine output ✔ Educate patient to finish
✔ Liver enzymes entire prescription

✔ Inform healthcare staff about
Drug history; Antacids affect peak level
of azithromycin
✔ Culture and sensitivity tests
medications and adverse
effects (nausea, vomiting,
✔ Signs of liver damage
diarrhea, abdominal cramps,
✔ Administer oral azithromycin 1 hour
before or 2 hours after meals; Give with
itching)
water, not fruit juice ✔ Report superinfection
✔ Antacids such be given 2 hours (stomatitis or vaginitis)
before or after azithromycin ✔ Report onset of diarrhea
AMinOgLyCOsiDEs
AMinOgLyCOsiDEs
✔ MOA: Act by inhibiting
✔ Streptomycin, gentamicin, bacterial protein synthesis
neomycin, kanamycin,
✔ Indications: Treatment of aerobic
amikacin
gram- negative bacteria,
✔ Streptomycin was discovered mycobacteria, and some
in 1942 and named after protozoans
Streptomyces griseus, a soil
microorganisms ✔ Sometimes administered
concurrently with penicillin,
✔ Bactericidal
cephalosporin, or vancomycin to
✔ Toxic than other antibiotics
treat enterococcal infections
AMinOgLyCOsiDEs

✔ Given parenterally – Poorly ✔ Neomycin – Topical use for


absorbed in GI tract infections of the skin,
✔ If given oral, this is to sterilize eyes, and ears
GI tract prior to bowel surgery✔ Paromomycin – Oral use
✔ CI: Patients with ear and for treatment of parasitic
kidney problems infections
✔ AE: Ototoxicity (hearing ✔ Streptomycin – Restricted
impairment to deafness) and to treatment of
nephrotoxicity but reversible tuberculosis because
(abnormal urinary function emergence of bacterial
tests – elevated BUN) resistance
NURsing PROCEss nOtEs: AMinOgLyCOsiDEs

In-Patient Management Out-Patient


✔ Vital signs and urine output Management
✔ Labs: Renal and liver function ✔ Increase fluid intake unless
tests such as BUN, serum restricted
✔ Report side effects (nausea,
creatinine, ALT, ALP, AST and
bilirubin; Electrolytes vomiting, tremors, tinnitus,
✔ ftedical history related to renal pruritus, and muscle
or hearing disorders cramps)
✔ ftonitor intake and output, ✔ Must wear sunblock and
should be at least 600ml/day protective clothing during sun
✔ Check for hearing loss exposure
✔ Monitor for superinfection
fLUOROqUinOLOnEs
FLUOROqUinOLOnEs (QUINOLONES)
✔ Nalidixic acid, ciprofloxacin, ✔ Indications: Infections of the
respiratory, GI, and genitourinary
moxifloxacin tracts, and some skin and soft-
✔ Bactericidal tissue infections
✔ Effective against gram-negative ✔ Preferred drugs for
treatment of
pathogens; uncomplicated UTI
Newer drugs are more effective
✔ Well-absorbed orally and
against administered either once or twice a
gram-positive microbes such as day
staphylococci, streptococci, and ✔ Taken with food; But not with
enterococci multivitamins, or mineral
supplements because it can reduce
✔ ftOA: Inhibit 2 bacterial enzymes: absorption
DNA gyrase and topoisomerase
IV; Affect DNA synthesis
FLUOROqUinOLOnEs (QUINOLONES)
✔ Ciprofloxacin is used for post-
✔ CI: Age 60 and above and those exposure prophylaxis against
using corticosteroids; Not Bacillus anthracis (anthrax),
approved for children under age Yersinia pestis (plague),
18 because it interferes cartilage Francisella tularensis
development; Pregnancy and (tularemia), and Brucella
lactation melitensis (brucellosis)
✔ AE: Nausea, vomiting, and ✔ Gatifloxacin and
diarrhea; Dysrhythmia
(moxifloxacin) and potential besifloxacin are available in
hepatotoxicity; CNS effects; drops to treat infections of
Cartilage toxicity with risk for the external eye
tendonitis and tendon rupture
(Achilles tendon)
NURsing PROCEss nOtEs: FLUOROqUinOLOnEs
In-Patient Management
Out-Patient Management
✔ Vital signs and urine output
✔ Increase fluid intake (6-8 glasses)
✔ Fluid intake should be 2L a day unless restricted
✔ Labs: BUN and serum creatinine for
✔ Avoid caffeinated drinks
renal function
✔ Avoid operating motor vehicles or
✔ Drug and diet history: Antacids, iron hazardous machinery
preparations, caffeine intake, NSAIDs
✔ Wear sunglasses, sun block, and
✔ Culture and sensitivity tests protective clothing when in the sun
✔ ftonitor intake and output; urine pH
✔ Report side effects
✔ Check for superinfection
✔ Monitor theophylline and blood glucose
levels
SULFONAMIDES
sULfOnAMiDEs
✔ Older drugs / Folic acid ✔ Indications: UTI, Pneumocystis
inhibitors carinii pneumonia, and shigella
✔ Bacteriostatic infections of the small bowel
✔ Broad-spectrum ✔ AE: Crystalluria, hypersensitivity
reactions, nausea and vomiting;
✔ Limited use due to resistant Rare: Aplastic anemia (loss of
bacteria bone marrow function), acute
✔ NOA: Inhibit bacterial growth hemolytic anemia and
agranulocytosis
by inhibiting the synthesis of
folic acid or folate
sULfOnAMiDEs
Sulfamethoxazole-Trimethoprim Silver sulfadiazine
(TMP-SMZ)
✔ Brand: Bactrim ✔ Topical cream used to
✔ Used for UTIs treat infections in
✔ Do culture and sensitivity tests patients with serious
first before administration
burns
✔ Absorbed readily when given
orally and excreted rapidly via
✔ Can cause allergic
kidneys reactions due to sulfur
NURsing PROCEss nOtEs: sULfOnAMiDEs
In-Patient Management Out-Patient Management
✔ Assess renal function by checking urinary ✔ Encourage patient to drink several quarts of
output, BUN, and serum fluids daily to avoid
creatinine crystalluria
✔ Medical history: Contraindicated in liver and ✔ Tell pregnant patients to avoid sulfonamides
renal disease during the last 3 months of pregnancy
✔ Determine if patient is hypersensitive to ✔ No antacids during therapy

sulfonamides Report allergic reactions
✔ Drugs history
✔ Take sulfonamides 1 hour before or 2 hours
✔ Labs: CBC after meals with full glass of water
✔ Administer with full glass of water ✔ Report bruising or bleeding
✔ Record intake and output ✔ CBC
✔ Note temperature
✔ Wear sunglasses, avoid direct sunlight, use
✔ Observe for hematologic reactions – Check sun block and protective clothing to
CBC decrease photosensitive reactions
✔ Check for superinfection
CARBAPENEMS
CARBAPEnEMs
✔ Imipenem,ertapenem, ✔ Disadvantage: Can only
doripenem, meropenem be given parenterally
✔ Bactericidal ✔ AE: Diarrhea,
✔ Broadest antimicrobial spectrum nausea, rashes,
✔ MOA: Contain beta-lactam ring and
and inhibit bacteria by inhibiting thrombophlebitis at
construction of cell wall injection sites
✔ Very resistant to beta-lactamase
CARBAPEnEMs
Imipenem Ertapenem
✔ Broadest antimicrobial ✔ Narrow spectrum but
spectrum longer half-life
✔ Administered fixed-dose ✔ Used for serious
with cilastatin abdominopelvic and skin
Meropenem infections, community-
acquired pneumonia, and
✔ Used for peritonitis
complicated UTI
and bacterial
meningitis
MISCELLANEOUS

ANTIBIOTICS
CLinDAMyCin
✔ Effective against gram-positive and ✔ AE:
gram- negative bacteria (Fusobacterium Pseudomembranous
and Clostridium perfringens)
colitis
✔ DOC for abdominal infections caused
by
Bacteroides
✔ CI: Hypersensitivity, regional enteritis,
or ulcerative colitis
MEtROniDAzOLE
✔ Effective against anaerobes that
are common causes of ✔ Prototype drug for
abscesses, gangrene, diabetic antiprotozoal
skin ulcers and deep wound
infections medications
✔ Also used for H. pylori infections ✔ AE: Oral – Nausea, dry
of the stomach associated with
PUD
mouth, and headache:
✔ Have activity against both
High doses -
bacteria and multicellular neurotoxicity
parasites
VAnCOMyCin
✔ Reserved for severe infections ✔ Other AE: Hypotension,
from gram- positive organisms superinfections,
such as S. aureus and generalized tingling
Streptococcus pneumoniae after IV administration,
✔ Used after bacteria has become chills, fever, skin rash,
resistant to safer antibiotics hives, hearing loss and
✔ Indications: MRSA infections nausea
✔ AE: Ototoxicity and nephrotoxicity:
Red-man syndrome –Occurs
with rapid administration and
histamine is released in the body

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