ANTIBACTERIAL AGENTS  Creatinine level

 Direct monitoring of serum level of

 Human cells do not synthesize folic acid
some antibiotics
 Only plants, bacteria, fungi have a cell wall
c. Hepatic function
BODY DEFENSES  Erythromycin and tetracycline
contraindicated in treating patient with
 Barrier defenses liver disease
 Cellular defenses d. Poor perfusion (diabetic, cardiac
 Inflammatory response problems, necrotic tissue)
 Immune response  Ex: lower limbs of patient with dm –
difficult to treat
GRAM NEGATIVE
e. Pregnancy
GRAM POSITIVE  All antibiotic cross the placenta
 Tetracycline and aminoglycosides
BACTERICIDAL
 Antihelmintics – embryotoxic and
 Subs -> death of bacteria (interfere stability of teratogenic
cell membrane, chon, enzymes) f. Lactation
 Preferred to treat: serious life-threatening g. Age
infection and non-functioning immune system  Immature liver and kindey in newborn
-> vulnerable to toxic effect
BACTERIOSTATIC  Chloramphenicol – gray baby
 Prevents/ halts replication of bacteria/ inhibits syndrome
the growth of microorganism  Tetracycline – inhibition of bone
 It is possible for an antibiotic to be bacteriostatic growth
 Slides  Fluoroquinolones – interfere with
cartilage growth
ANTI-INFECTIVES h. Immune compromised (too many
invading microorganism
 Characteristics of ideal anti-infectives
4. Safety of the agent
1. Selective toxicity
a. Pcn least toxic – interferes with a sit
2. Ability to penetrate high affinity for site of
uniwue to the frowth of microorganism
action – mic/ bic
b. Other microbials (chloramphenicol) –
3. Resistant to inactivation by microbial enzyme
less specifc and reserved for life
4. Orally active
threatening disease
5. Long elimination half life
5. Cost of therapy
6. Devoid of adverse drug-drug interaction
7. Absence of developmental/ behavioural toxic EMPIRIC THERAPY
effects
 Selection of antimicrobial agents requires:  Treatment of an infection before specific vulture
1. Organisms identity and it’s sensitivity to information had been reported or obtained
a particular agents  Patient may be too sick to wait for the result of
a. Culture and sensitivity testing the culture and sensitivity testing
2. Site of infection  Indication for immediate empiric therapy:
a. Difficult sites to penetrate 1. Acutely ill patient with infection of unknown
 Cns – blood brain barrier origin
 Intraocular tissue 2. Neutropenic patient
 Prostate 3. Symptoms of meningitis
4. Site of infection
 Necrotic tissue
5. Patient history
3. Patient factors
 Hospital or community acquired
a. Immune compromise
 Immunocompromised
b. Renal function
 Travel record
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  Age
PROPHYLAXIS
 Treatment with antibiotics to prevent an infection
before it occurs
RESISTANCE
 Ability of bacteria over time to adapt to an
antibiotic and produce cells that are no longer
affected by the drug
 Resistance may result from:
 Natural or inherent – innate resistance of the
microorganism (it has its own specific
enzyme system)
 Pseudomonas aeroginosa – resistant to
pcn g
 Acquired – caused by prior exposure
antibacterial
 Staphylococcus aureus – was once
sensitive to pcn g, previous exposure
have caused this organism to become
resistant to it – tend to be resistant to
every drug, except vancomycin.
 Microorganisms develop resistance in many
ways:
 Producing an enzyme that deactivates
antimicrobial drugs
 Changing the permeability of the cell –
intracellular
 Altering the binding site
 Producing a chemical to antagonize the
drug
 Resistant strains/ superbugs:
 Mrsa – methicillin-resistant staphylococcus
aureus
 Orsa – oxacillin-resistant staphylococcus
aureus
 Prs – penicillin-resistant streptococci
 Vre – vancomycin-resistant entercoccis
 Linezolid is effective for these resistant
 Extended-spectrum beta-lactamase (esbl)
 Producing microorganism -> resistance to
most beta-lactam antibiotics (pcn,
cephalosporins and monobactams)
 Very poor outcome
 Pseudomonas – can be killed by pcn
betal-lactams, aminoglycosides,
carbapanems and flouroquinolones
with aminoglycoside
 Preventing the development of resistance
 Identify bacteria
 Correct drug choice
 Full course of therapy
 Avoid inappropriate use
 Combination therapy
NARROW SPECTRUM
 Are used to either gram (+) or gram (-)
 Used for specific infection when causative
organism is known
EXTENDED SPECTRUM
 Effective against gram (+) and some gram (-)
 Also called anti-pseudomonal pcn – effective in
gram (-) and some gram (+)
BROAD SPECTRUM
 Wide coverage of microbial specia
 Both gram (+) and gram (-)
 May cause superinfection
o Clostridium difficile
o Yeast infection – cheesy like, watery
SUPERINFECTION
 An infection caused by a secondary pathogen
that occur during prolonged antibiotic therapy
 Use of broad spectrum anti-infectives
 Destruction of normal flora
 Common superinfection
o Vaginal and gi yeast infections (sore
patches in the mouth, diarrhea and vaginal
itching)
 Clostridium difficile – associated with diarrhea
o Antibiotic associated psedomembtanois
colitis)
 Bloody diarrhea
 Foul odor
COMBINATION THERAPY
 Microbial infections are caused bu more than 1
organism and reacts to different anti-infective
agent
 Reason:
o Smaller dose of combined drug leads to
fewer adverse effects
o Only used when offending pathogen is
known
o It delays the emergence of resistant strains
 Tx for tb, malaria, hiv
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 o More powerful when combined (synergistic a. Fluoroquinolones
effect) b. Rifampin
5. Alter the permeability of the cell membrane
CROSS RESISTANCE
to allow essential cellular components to
 Resistance between antibacterial drugs that leak out
have similar actions a. Antifungals
 Adverse reaction to anti-infective therapy b. Antiprotozoans
o Kidney damage PENICILLINS
o Gi toxicity
o Neurotoxicity (anti tb drugs)  First introduced in the 1940s
o Hypersensitivity reactions (steven johnson’s)  Bactericidal: inhibit cell wall synthesis
o Superinfections  Also called “beta-lactams”
 Pharmacokinetic and pharmacodynamics:  Effective against gram (+) bacteria
o It must not only penetrate the bacterial cell o Streptococcus, enterococcus,
wall in sufficient concentration but must staphylococcus species
have an affinity to the binding sites on the
bacterial cell. ANTIOBIOTICS
o The time that the drug remains at the binding  Natural penicillins
site increases the effect of the antibacterial o Piperacillin
action. (longer half-life) o Ticarcillin
 Type of pathogen o Carbenicillin
 Site of action o Mezlocillin
 Immunocompromised host  Penicillinase-resistant penicillins
1. Interfere w/ biosynthesis of the bacterial cell o cloxacillin
wall  death. o Dicloxacillin
a. ẞ-lactams: o Methicillin
i. Penicillins o Nafcillin
ii. Cephalosporins o Oxacillin
iii. Carbapenems  Extended-specturm penicillins. Amnipenicillins
iv. Monobactams o Amoxicillin
b. Other antibiotics: o Ampicillin
i. Polypeptides o Bacampicillin
ii. Vancomycin
 Antipseudomonal penicillins
iii. Bacitracin
o Penicillin g
iv. Teicoplanin
o Penicillin v
2. As antimetabolites (inhibitors of
 Chemicals have been developed to inhibit these
metabolism) (bacteriostatic / bactericidal)
enzymes:
prevent the microorganism from using subst.
o Clavulanic acid
Essential for their growth & devt.
o Tazobactam
a. Sulfonamide
o Sulbactam
b. Trimethoprim
 These chemicals bind with beta-lactamase and
3. Inhibits chon synthesis (bacteriostatic) ►
prevent the enzyme from breaking down the
prevents normal growth & reproduction
penicillin
a. Tetracyclines
b. Chloramphenicol  Penicillin-beta-lactamase inhibitor or the
c. Aminoglycosides “betalactams”(combination drugs):
d. Clindamycin o Ampicillin + sulbactam = unasyn (ampi-
e. Macrolides sulbactam)
f. Streptogramins o Amoxicillin + clavulanic acid = augmentin
4. Interfere w/ dna & rna synthesis in the cell o Ticarcillin + clavulanic acid = timentin
leading to inability to divide o Piperacillin + tazobactam = zosyn (piptazo)
 Common side effects:
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 o Diarrhea o Ceftazidime – against pseudomonas a. &
o N&v excellent gram (-) coverage
o Abdominal pain o Cefotaxime – good penetration to csf
 Adverse reaction: o Ceftriaxone (rocephin) – iv & im longest half-
o hypersensitivity life (6 – 8 hours) of any cephalospor.
 Most potent group against gram (-)
CEPHALOSPORINS  Less active against gram (+)
 Bactericidal and bacteriostatic  Only drugs that can penetrate blood
 Largest antibiotic class brain barrier to treat cns infections
 Numerous sensitive bacteria  Fourth generations
 Gi effects including pseudomembranous o Cefepime – broader spectrum (both gram (-
colitis ) and gram (+))
o Due to clostridium difficile  Fifth generations
 Watery diarrhea o Ceftaroline
 Mucous & blood in stool o Ceftobiprole – mrsa (methicillin-resistant
 Fever staphylococcus aureus)
 Leukocytosis  Extended spectrum
 Fluid and electrolyte loss NURSING CONSIDERATIONS:
 Shock & even death
 Toxigenic spore-forming (seeding) gram  Gi upset – given with food
(+) bacillus o Can cause false (+) coomb’s test (which
 Enteric organism endemic in community complicates cross matching procedure) (test
and hospitals for antibodies b4 bt)
o Can cause false (+) glucose result for
ANTIBIOTICS: CEPHALOSPORINS clinitest & benedict’s reagent (test for
 Semisynthetic derivatives from a fungus glucose in urine)
 Structurally and pharmacologically related to o Cefamandole, ceftriaxone, cefuroxime if
penicillins taken with alcohol may cause disulfiram
(antabuse)-like reaction
 Divided into groups:
 Intolerance to ingested alcohol
 First generation
 N & v, flushing, dizziness, throbbing
o Cefazolin (ancef) – iv
headache, blurred vision, chest and
o Cephalexin (keflex) - oral
abdominal discomfort & general
 Narrow spectrum
hangover-like
 Streptococci & staphylococcus
 Good gram (+) coverage CARBEPENEMS
 Poor gram (-) coverage
 Used for surgical prophylaxis, uris,  Bactericidal
 Otitis media  Broad spectrum against gram (-) and gram (+)
 Second generation bacteria, anaerobes & pseudomonas aeruginosa
o Cefaclor, cefoxitin  Impt. Last line of defense used when other
o Cefuroxime - oral antibiotics fail
o Cefamandole – can cause  S/e: n & v, diarrhea
hypoprothrombinemia, bleeding & o Imipenem / cilastatin
disulfiram effect (intolerance to ingested o Meropenem
alcohol) o Ertapenem
 Good gram (+) coverage
MONOBACTAM
 Better gram (-) coverage
 Third generation  Aztreonam (azactam) - only one available
o Cefixime – only oral 3rd generation, against  Narrow spectrum
gram (-)  Effective only on gram (-) bacteria such as :
neisseria & pseudomonas
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GLYCOPEPTIDE  Bacteriostatic
 Prevents synthesis of folic acid
 Vancomycin
 Effective against gram (-) & gram(+) bacteria
 Bacitracin – restricted to topical application due
 Many resistant strains due wide range use over
to potential nephrotoxicity
decade
VANCOMYCIN  Effective in treating:
o Variety of systemic infections
 Interferes with cell wall synthesis o Acute uncomplicated uti
 Drug of choice for: reserved for severe infection o Bronchitis
due to: mrsa, septicemia, bone, skin lower rti that o Traveler’s diarrhea
does not respond to other antibiotics o Acute otitis media in children -
 Quinupristin-dalfopristin  Trimethoprim-sulfamethoxazole (tmp-smz)
o Drug combination use to treat vancomycin- o A combination of 2 drugs
resistant enterococcus (vre) infection o Trimethoprim – prevents bacterial
 Highly toxic: resistance to sulfamethoxazole
o Renal failure  Co-trimoxazole (bactrim)
o Superinfections  Drug interaction:
o Ototoxicity o It ↑ coumadin action ► bleeding
o Red man syndrome – redness of the neck o With sulfonylurea (oral hypoglycemic)
and back sudden and sever hypotension, it ↑ hypoglycemic response ► ▼ blood
fever, chills paresthesia due to fast infusion glucose
 S/E: o Decrease effectiveness of oral
o Chills contraceptives
o Dizziness  Adverse effects:
o Fever o Crystalluria - nephrotoxic = ▲ fluid
o Rashes intake & alkalinization of urine
o N&v o Kernicterus - brain damage in newborn due
o Thrombophlebitis at injection site to ▲ bilirubin + avoided in newborn & infants
 Administer over at least 1 hour < 2 mos. Old & pregnant at term
 Rotate iv site o Hypersensitivity reactions:
 Assess for cloudy or pink urine  Rashes
 Immediately report tinnitus (ringing in the ears)  Angioedema
 Stevens-johnson syndrome
TEICOPLANIN
o Cross allergenicity with diuretics
 Bactericidal (furosemide, thiazides, acetazolamide &
 Similar to vancomycin bumetanide)
 Serious gram (+) infection o Photosensitivity = avoid sunlight & use sun
 Longer elimination half-life (40-70hrs) with slow screen
release from tissue Protein synthesis inhibitors
 Less adverse effect than vancomycin
 Tetracyclines
 Chloramphenicol
ANTIMETABOLITES/ INIHIBITORS OF  Aminoglycosides
METABOLISM  Clindamycin
 Macrolides
SULFONAMIDES
 Streptogramins
Sulfadiazine
ANTIBIOTICS: TETRACYCLINES
1. Sulfamethoxazole
 Tetracycline
2. Sulfamethizole
 Doxycycline (doryx, doxy-caps, vibramycin)
3. Sulfisoxazole
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 Generally bacteriostatic INHIBITORS OF DNA & RNA SYNTHESIS
 Inhibit chon synthesis
FLUOROQUINOLONES
 Effective against gram (-) & gram (+) bacteria
 Broadest spectrums of any class of antibiotics 1. Ciprofloxacin (Cipro)
 Also for chlamydia, rocky mountain spotted 2. Norfloxacin (Noroxin)
fever, cholera, lyme dis., helicobacter pylori 3. Ofloxacin (Floxin)
 It binds to ca, mg, and al ions to form insoluble  Interrupts DNA synthesis
complexes  All fluoroquinolones are Bactericidal
 Thus, dairy products, antacids, and iron salts  Effective against gram (-) bacilli &
reduce absorption of tetracyclines enterobacteraceae
 Adverse effect:  Better alternative to more toxic drug such as
o Strong affinity for calcium ► permanent aminoglycosides
discoloration of enamel of teeth (fetus & 8 y/o)  Can act synergistically with ẞ-lactams
– not given at third trimester  First oral antibiotics effective against gram (-)
o Retard fetal skeletal development bacteria
o Superinfection :  Only oral agent effective against pseudomonas
 Diarrhea  Absorption reduced by:
 Pseudomembranous colitis o Antacids, iron , calcium, zinc or
Doxycycline (vibramycin) magnesium supplements
 Adverse effects:
 Has been prescribed for antrax o Crystalluria due to excessive amt. ►
 Often associated with “sunburn” reaction – nephrotoxic
appears upon direct sunlight or sunlamps o Severe phototoxicity (avoidance of
exposure sunlight & sunscreen will not protect, should
be discontinued at the 1st sign)
AMINOGLYCOSIDES
URINARY TRACT ANTISEPTIC
1. Amikacin (amikin)
2. Gentamicin (garamycin) NITROFURANTOIN
3. Tobramycin
 Narrow spectrum & toxicity ► less commonly
4. Streptomycin
used
5. Kanamycin
6. Neomycin  It damages the DNA of cocci
7. Netilmicin  Concentrated only in urine & microorg. at the site
 Bactericidal can be effectively eradicated (from e. coli )
 Very potent antibiotics with serious toxicities  Does not achieve antibacterial levels in the
circulation
 Mainstay treatment of serious infections due to
aerobic gram (-) bacilli (pseudomonas, e. Coli, ANTIMYCOBACTERIAL/ ANTITUBERCULAR
proteus, klebsiella, serratia) DRUGS
 No oral form ► poor absorption
 Serious adverse effects:  Mycobacteria – can cause Tuberculosis &
 Nephrotoxicity (renal failure) Leprosy (Hansen’s Disease)
 Ototoxicity (8th cranial nerve)  It has the ability to hold the stain even in the
 Neuromuscular paralysis presence of “destaining” agent such as an acid -
- “acid-fast” bacteria
 Monitor drug trough level
 Mycolic acid, its outer coat which protects them
MACROLIDES from many disinfectants and allows them to
survive for long period in the environment.
LINCOSAMIDES
 Acts as tuberculostatic or tuberculocidal (combi.)
CHLORAMPHENICOL (CHLOROMYCETIN)  Interferes with mycolic acid – essential
metabolite for mycobacterium tuberculosis
STREPTOGRAMINS  Complete course of treatment
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 Take on empty stomach  Yeast infection of the mouth (thrush) and vagina
 Weigh weekly
MYCOSIS
 Avoid alcohol
 Disease caused by a fungus
ISONIAZID (INH)
 Nystatin (Mycostatin)
 1st choice prescribed for family diagnosed with o Frequently administered as an aoral
tuberculosis suspension for candida infection in the
 Peripheral neuritis - to counteract neurits give mouth
pyridoxine / vit. B6 o Client instruction
 Optic neuritis  SSS – swish, swash and swallow
 Hepatotoxicity (inflam & necrosis occurs, usually  Swish the liquid within the mouth,
in 1st 6 months of treatment) = monitor liver swallow or expel the suspension
enzyme
 Hyperglycemia may occur = check capillary
blood glucose (CBG) SYSTEMIC ANTIFUNGALS
 INH & rifampin cause oral contraceptives to
 Selective toxic to fungal cell membrane
become ineffective.
 Culture fungus
ETHAMBUTOL  Check for drug-drug interactions (CP450
enzyme system)
 Optic neuritis
 Commonly used drugs:
 Blindness o Amphotericin B
RIFAMPIN (RIFAMPICIN) o Fluconazole
o FLucytosine
 Rash & fever o Itraconazole
 Orange discoloration of body fluids (normal) o Ketoconazole – firs effective antifungal
 Remove contact lens drug, orally absorbed, for the treatment of
fungal infection such as candidiasis,
PYRAZINAMIDE (PZA)
histoplasmosis, can produce cardiac
 Inhibits renal excretion of uric acid ► dysrhythmias
asymptomatic hyperuricemia ► gout attack o Miconazole
 Check uric acid and liver function o Nystatin
 Laboratory tests:
o Liver enzymes
TOPICAL FUNGAL INFECTIONS o Electrolytes
o BUN and creatinine
 Topical antifungal agents can cause serious  “shake and bake” – acetaminophen,
local irritation diphenhydramine, glucocorticoids prior to
 Fungus – a cellular organism with a hard cell wall infusion
that contains chitin and many polysaccharides  Rapid infusion – cardiovascular symptoms,
as well as a cell membrane that contains seizures and anaphylaxis, renal dysfunction is
ergosterols common
 Ergosterol – steroid type protein found in the cell
membrane of fungi; similar in configuration to
adrenal hormones and testosterone PROTOZOAN DISEASES
TINEA  Malaria
o Antimalarial - Timing around exposure is
 Athlete’s foot (tinea pedis)
important; Prophylaxis or treatment
 Jock itch (tinea cruris)
 Quinine sulphate - First antimalarial
CANDIDA drug in the 19th century
© MARY ANDREA G. AGORILLA, UST-CON BATCH 2021 | 7
  Monitor for chinchonism (nausea,
vomiting, tinnitus, vertigo)
 Trypanosmiasis – african sleeping sickness,
chagas’ disease
 Leishmaniasis – skin, mucous membrane
 Amebiases
 Giardiasis – intestinal
 Trichomoniasis – vaginal infections
 Pneymocystisis carinii Pneumonia (PCP) -
lungs-AIDS
 Trichinosis – disease that results from ingestion
of encysted roundworm larvae in undercooked
pork; larvae migrate throughout the body to
invade muscle, nervous tissue, etc; can cause
pneumonia, heart failure, and encephalitis

ANTIHELMINTICS

 Albendazole
 Ivermectin
 Mebendazole
 Oxamniquine
 Praziquantel
 Pyrantel
 Thiabendazole
NURSING INTERVENTIONS

 Metronidazole (Flagyl)
o Active against anaerobic organisms such as
clostridium difficile, H. pylori, amebiasis,
trichomoniasis and gram negative bacillus
(in combination with aminoglycosides)
o It inhibits metabolism of anticoagulants
o Avoid alcohol during therapy and at least 48
hours after treatment is complete
o It has antabuse-like effect
o Warn that this medication will produce a
metallic taste and discolored urine
 Antihelmintic drug
o Treat everyone who is in close contact with
a patient
o Monitor CBC – anemia

© MARY ANDREA G. AGORILLA, UST-CON BATCH 2021 | 8