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UNIT-II
Drugs Used to Treat and Prevent
Infections
Presenter:
Nursing Lecturer:
Imtiaz ahmed
(Generic BSN)
6/25/2023
1
OBJECTIVES
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By the end of the session learners will be able to:
Define and review common terms and concepts related to
antimicrobial therapy.
List general principles and considerations related to antimicrobial
therapy.
Discuss mechanism of action and indication of using antimicrobial
therapy.
State appropriate nursing implications for a client receiving
antimicrobial
drugs.
Why antibiotics only destroy bacterial cells and not human cells?
•Because, the antibiotics are synthesized from the bacterialDNA
itself and designed to target the bacterial cell only.
Thick peptidoglycan
layer in their cell
membranes
Thin single layer of
peptidoglycan and
an additional outer
lipid membrane
with small holes
through which only
small drug
molecules can pass
Gram Positive Gram Negative
antimicrobial drugs
REVIEW
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1. Antimicrobialagent:
Are the drugs that inhibit the growth of, or kill the bacteria and other
microorganisms (e.g. virus, protozoa, fungi)
Extended Spectrum Antibiotics
Term applied that are modified to be effective against (Gram +ve and Gram –ve)
Exp: Ampicillin
Broad spectrum antimicrobial agents
Drugs that are effective against several groups of organisms.
(Gram positive and Gram negative)
and also alter the nature of the normal bacterial flora and precipitate a
superinfection.
Exp: Tetracycline andsome Cephalosporin
Narrow spectrum antimicrobial agents
Drugs that are effective against one group of organisms or few specific
organisms. E.g. Penicillin (Gram +ve)
DEFINITIONS:
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organisms through
3. BactericidalAction
To kill the organisms through antimicrobial drugs
4. BacteriostaticAction
To stop the growth and reproduction of the
antimicrobial drugs
5. Antibiotic Resistance:
Antibiotic resistance is the ability of bacteria or other microbes to resist
the effects of an antibiotic. Antibiotic resistance occurs when bacteria
change in some way that reduces or eliminates the effectiveness of drugs.
Bacteria may bring about antibiotic resistance by: Changing their
receptor’s structures, occupying receptors with some other molecules,
destroying the antibiotics (in some cases)
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Indication
Treatment (curative use) and prevention of infection
(prophylactic use)
Major Side effects
Allergic or hypersensitivity reactions, organ toxicity and resistance
to
certain micro organisms
Dose
Individualized; depends on causative agent, chosen drug, and
patient’s
condition
Route of administration
Oral, intravenous, intramuscular, topical.
Duration of therapy
Depends on specific drug, average duration is approximately 7 –
14 days
•Before beginning therapy, Assess drug allergies; hepatic, renal and
cardiac function and other lab studies.
•Obtain thorough patient health history, e.g. Immune status especially
in case of
recurrent infections
•Assess for contraindications to antibiotic use and potential drug
interactions.
•It is ESSENTIAL to obtain cultures (Blood, Spinal Fluid, Pleural
Fluid, Synovial Fluid, Peritoneal and Urine) BEFOREbeginning
antibiotic therapy.
•Instruct patient to take antibiotics exactly as prescribed for the
specified lengthof time.
•For safety reasons, check the name of the medication carefully since
there are many agents that sound alike or have similar spellings.
Antibiotics: Nursing Intervention
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Mechanism OfAction:
By inhibiting bacterial cell wall
synthesis
Alteration in membrane
permeability
By inhibiting bacterial protein
synthesis
By inhibiting DNA andRNA
synthesis
Interference with cellular
metabolism
Antimicrobials
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Classifications:
Antibacterial
Antifungal
Antiviral
Antiparasitic
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Antimicrobial Classification
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Empiric Therapy: Treatment of an infection before specific organism
has been reported through culture sensitivity test; empiric therapy is
with broad spectrum antibiotics.
Definitive Therapy: The treatment plan for a disease or disorder that
has been chosen as the best one for a patient after all other choices have
been considered.
Prophylactic therapy: Treatment with antibiotics to prevent an
infection, as in intra- abdominal surgery, after pacemaker implantation.
Classifications of antibacterial agents:
1. Beta-lactam antibacterial (Penicillin, Cephalosporin)
2. Macrolides
3. Aminoglycosides
4. Fluorquinolones
5. Tetracycline
6. Sulfonamides
Anti-Bacterial
12
Mechanism of action: Bactericidal
Inhibit the synthesis of the Peptidoglycan layer of bacterial
cell wall Leakage of intracellular contents
microorganisms’destruction.
1. It inhibits transpeptidase which carries out cross linking
between various layers of cell membrane.
2. It activates autolysin enzyme by binding with penicillin
binding proteins and lysis of bacteria occurs results in
Bacterial cell death.
Example: Penicillin, Cephalosporin, Carbapenem
- These are known as Beta Lactam antibiotics due to the
presence of beta lactam ring in their molecular structure.
- Resistance may develop due to beta lactamase enzyme
produced
by some bacteria that destroy the beta lactam ring in their
molecular structure.
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1. Beta-LactamAntibacterial
antimicrobial drugs 13
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 Some of the initial Penicillins were narrow spectrum (gram positive);
however some recent derivatives are broad spectrum, effective, and
widely used antibacterial agent.
Examples: Classification
1.Natural Penicillins: ( Penicillin-G, Penicillin-V) Obtained from fungus.
Penicillin G (Benzylpenicillin) has a activity against (Gram +ve, -ve and
Spirochetes). More than 90% of Streptococcus aureus are producing
pencillinase hence resistant to Penicillin-G.
(Penicillin remains the drug if choice for the treatment of Gas Gangrene
(Clostridium Perfringens) and Syphilis (Trponema Palidium).
Penicillin V Only available in Oral formulation has a spectrum similar to that
of Penicillin G but NOT used for the severe infections because of its limited
oral absorption.
2. Semi-Synthetic Penicillins: (Ampicillin, Amoxicillin) also known as
aminopenicillins or extended spectrum Penicillins.
Beta-Lactam Antibacterial
A. Penicillin
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13
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Penicillin
 Ampicillin and Amoxicillin are effective against Gram –ve
(H.Influenzae, E.Coli, Proteus mirabilis). Ampicillin with or
without addition of Gentamycin is the drug of choice for Gram +ve
Bacillus Listeria monocytogens. Widely used in the treatment of
Respiratory infections.
 3. Antistaphylococcal Penicillins: (Dicloxacillin, Methicillin,
Naficillin, Oxacillin)
 Are Beta-Lactamase (pencillinase-resistant penicillins), that’s why
their use is restricted against the infections caused by pencillinase-
producing staphylococci including MSSA (Methicillin Sensitive
Staphylococci aureus).
 Methicillin is not used because of its toxicity (interstitial nephritis)
only used to identify the resistant strains of MRSA is currently a
source of serious community and (Hospital acquired infections.
Beta-Lactum Antibacterial
A. Penicillin
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 Antipseudomonal Penicillin: (Pipperacillin) is also known as
antipseudomonal penicillin because of its activity against Pseudomonas
aeruginosa.
 RESISTANCE:
 1. Beta Lactamase Production
 2. Decreased Permeability to the Drug
 3. Altered Penicillin Binding Protiens
 Pharmkinetics
 Routes of Drug Administration:
 Ampicillin + Sulbactum , Pipperacillin + Tazobactum
 Naficillin, Oxacillin (IV or IM)
 Penicillin V, Amoxicillin and Dicloxacillin (Oral)
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 Depot Forms: Penicillin G (Slowly absorb in the
circulation and persist at low level for a log time)
 Absorption: Take Dicloxacillin by Empty stomach
because it will be destroyed by Stomach acid. While
amoxicillin is gastric stable.
 Distribution: Distributed throughout the body
Can Cross Placental Barrier No any Teratogenic effects
Can not cross BBB only cross in case of meningitis.
 Metabolism: Metabolized in the Liver
 Excretion: Excreted From Kidney via (Tubular
Secretory System and Glomerular Filtration)
 Adverse Reactions:
Hypersensitivity, Diarrhea, Nephritis, Neurotoxicity,
Hematologic Toxicities (Thrombocytopenia)
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Beta-Lactam Antibiotics
2. Cephalosporins
 Cephalosporins closely related to penicillin by
functionally and structurally.
 Cephalosporins have the same mode of action as
penicillins, as they are affected by the same resistance
mechanism.
 Cephalosporins are classified as;
 1st Generation, 2nd Generation, 3rd Generation, 4th
Generation on the basis of (Bacterial susceptibility
patterns and resistance to beta-lactamases.
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First generation
Cephalosporin's
Second
generation
Cephalosporins
Third generation
Cephalosporins
Fourth generation
Cephalosporins
Modest activity
against: (Proteus
mirabilis, E.Coli,
K. Pneumonia)
Oral caity
aenarobes are also
sensitive.
Gram negative
and activity
against Gram
positive is weaker
Broad spectrum
(Highly active against
Gram negative)
-Third Generation
antibiotics has great
therapeutic levels in
(CSF)
Broadest spectrum
(Highly active against
Gram negative)
Exp:
Parenteral:
Cefazolin (Kefzol)
Oral:
Cephalexin
(keflex),
Cephradine
(Velosef)
Exp:
Parenteral:
Cefuroxime
(Zinacef)
-It crosses
the Blood
Brain
Barrier
(BBB)
Exp:
Parenteral:
Cefotaxime (Clafron)
Ceftriaxone (Rocephin)
Has the longest Half
Life (6-8 hours)
Oral:
Cefixime (Cefspan)
Example: Cefepime
(Maxipime)
Effective against
Pharyngitis
Pneumonia, otitis,
sinusitis, RTIs
Meningitis , gonorrhea,
influenza, typhoid
Septicemia, Hospital
acquired pneumonia
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Pharmacokinetics
 Administration: Many Cephalosporins must be
administered IV or IM. Because of their poor oral
absorption.
 Distribution: Distributed very well into body fluids.
Adequate therapeutic levels in CSF regardless of
inflammation (Meningitis).
 Elimination: Eliminated via Tubular secretion and
glomerular filtration. Therefore doses must be adjusted in
case of renal dysfunction.
 One exception: Ceftriaxone (3rd Gen) is excreted via Liver
into feces. Therefore ceftriaxone is frequently
administered in patient with renal insufficiency.
Adverse Reaction:
 Anaphylactic Response, Stevens-Jhonson syndrome, or
toxic epidermal necrolysis to penicillins should be avoided
or used with caution in individual with penicillin allergy .
-Broadest spectrum (mixed infections)
-Bactericidal
Example: Imipenem, Meropenem, Doripenum
These drugs are used as empiric therapy because of their activity
against Beta Lactamase producing Gram +ve and Gram –ve organisms,
anaerobes, P. Aeroginosa.
Pharmacokinetics:
-Administration: IV
-Distribution: Penetrate well into body tissues and fluids, including
CSF when meninges are inflamed.
Excretion: Excreted by glomerular filtration. Therefore dose must be
adjusted in patients with renal insufficiency.
Adverse Effects: Nausea, Vomiting, Diarrhea (NVD), Eosinophilia and
Neutropenia are less common. High levels of Imipenem may provoke
Seizures. Patient with Penicillin allergy can use Carbapenems.
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Beta-Lactam Antibiotics: 3. Carbapenem
• Assess and monitor for Penicillin allergy.
• Cautiously administer Penicillin, as those patients who have taken
Penicillin without any problem in past, still have a chance of subsequent
reaction with future doses.
• Monitor renal and liver function tests and I/O.
• Give oral Penicillins on empty stomach with full glass of water. (because
it is sensitive to HCL).
• While administering penicillins, IV site should be changed
q48hrs to minimize blood vessel irritation.
• Give I/M injections into large muscles and rotate sites, as it causes pain.
• Look for and report signs of resistance.
• Monitor patients receiving Imipenem for seizures especially elderly and
patients with renal impairment.
• If nausea appears with Imipenem administration, slow I/V rate.
Beta-Lactam Antibiotics (Nursing Care)
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Vancomycin (Glycopeptide)
 Vancomycin is a tricyclic glycopeptide active
against Aerobic and anaerobic gram positive bacteria,
including MRSA, MRSE.
 MOA: It binds to the precursors, disrupting
polymerization and cross linking required for maintenance
of cell wall integrity. This results in bactericidal activity.
 Indications: Used against MRSA, Skin and soft tissue
infections, infective endocarditis and nosocomial
pneumonia.
 Frequency of administration dependent on renal function.
Therefore, monitoring of creatinine clearance is required
to optimize exposure and minimize toxicity . Therapeutic
Range of Creatinine is maintained between 10-20mcg/ml.
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Vancomycin
 Side Effects:
 Ototoxicity, Nephrotoxicity, Thrombophlebitis, Red
man syndrome, hypotension from rapid infusion (it
releases histamine with rapid infusion causing
vasodilation.
 Nursing Care:
 Monitor I/O and V/S.
 Obtain and monitor renal and auditory functions tests.
 Administer IV slowly.
 Look for serum Creatinine and BUN
 Have its serum level checked periodically.
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Macrolides
 Macrolides are group of antibiotic with a macrocyclic
lactone structure to which one or more deoxy ribose
sugars are attached.
 Choice of Drug alternative to penicillin in individuals
with an allergy to Beta-Lactam antibiotics.
 Names of Macrolides:
 Erythromycin, Clarithromycin, Azithromycin,
Telithromycin.
 Mechanism of Action (MOA)
 Macrolides binds irreversibly to a site on the 50S
subunit of the bacterial ribosome, thus inhibiting
translocation steps of Protein synthesis.
 Generally it is Bacteriostatic, they may be Bactericidal
on high doses.
Macrolides
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 Indication:
 URTI, Skin Infections, Pertussis, Syphilis, Diphtheria,
Intestinal Infections, Alternative use of Penicillin.
 Pharmacokinetics:
 1.Absorption: Erythromycin is destroyed by gastric acid
hence given in enteric coated form. Clarithromycin,
Azithromycin and Telithromycin are stomach stable.
Erythromycin and Azithromycin are available in IV form.
 2. Distribution: Widely distributes well to the body and
tissues fluids can reach to the prostatic fluid except CSF.
All fours drugs are widely distributed in the Liver.
 3. Elimination: Undergo hepatic metabolism.
 4. Excretion: Metabolites are excreted in the bile.
• Erythromycin must be used cautiously in patients with
history of hepatic impairment
• I/V Erythromycin should be diluted sufficiently
and administered slowly.
• Monitor hepatic function periodically.
• Administer with full glass of water / with meal
• Oral suspension should be refrigerated and shaken well
before use.
Macrolides (Nursing Care)
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Aminoglycosides
 Aminoglycosides are used for the treatment of serious
infections due to aerobic gram-negative bacilli; however the
clinical use is limited due to serious toxicities.
 Mechanism of Action (MOA):
 Inside the cell aminoglycosides bind the 30s ribosomal sub-
unit, where they interfere with assembly of the functional
ribosomal apparatus and cause the 30s subunit of the
completed ribosome to misread the genetic code.
 Bactericidal
 Drugs: Amikacin, Gentamicin, Tobramycin, Streptomycin,
Neomycin.
 Antibacterial Spectrum: Effective against aerobic gram
–ve, Aminoglycoside + Beta lactam drug to produce
synergistic effect.
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Aminoglycosides (Pharmacokinetics)
 Absorption: All drugs are given parenterally except:
Neomycin
 Distribution: Drug is hydrophobic so distribution to
body fluid is variable.
 Can penetrate placental barrier and may accumulate in
fetal plasma.
 Elimination: 90% of parenteral aminoglycoside are
excreted unchanged in the urine except Neomycin which is
excreted in feces.
 Adverse Effects:
 Ototoxicity (Deafness may be irreversible), Vertigo,
Nephrotoxicity, Neuromuscular paralysis, Allergic
Reaction (Contact dermatitis is common reaction to
topically applied neomycin).
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Aminoglycosides (Nursing Care)
• Monitor hearing and balance.
• Monitor renal function tests and I/O specially
serum Cr and BUN.
• Adequate hydration is vital.
• Administer Gentamycin cautiously in clients with
impaired renal function, reduced hearing,
dehydration, and neuromuscular disorders.
• Monitor for dizziness and ringing in ears.
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Tetracyclines
 Tetracycline is bacteriostatic drug consist of four fused
rings with a system of conjugated double bonds.
 Mechanism of Action (MOA):
 Tetracyclines concentrate intracullarly in susceptible
organism. The drug bind irreversibly to 30s subunit of
bacterial ribosome. This action prevents binding of
tRNA to mRNA-ribosome complex.
 Antibacterial Spectrum: Effective against gram
+ve, gram –ve bacteria, protozoa, spirochetes,
mycobacteria and Chlamydia infections.
 Drugs: Demeclocycline, Doxycycline, Minocycline,
Tetracycline.
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Tetracyclines (Pharmacokinetics)
 Absorption: Absorbed after oral ingestion.
Administration with dairy products or substances like;
(Divalent and Trivalent cations Example: Mg, Ca, Al).
Present in both forms IV and Oral.
 Distribution: Tetracyclines are well concentrate in the
Bile, Liver, Kidney, Gingival fluid, Skin, Teeth and Bones.
Minocycline and doxycycline achieve therapeutic levels in
th CSF. All Tetracycline cross placental barrier.
 Elimination: Minocycline undergoes hepatic
metabolism and is eliminated lesser extent via kidney.
Doxycycline is preferred in patients with renal dysfunction
it is excreted via bile and feces.
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Adverse Effects:
 Gastric discomfort: (Due to irritation of gastric mucosa),
Should be taken on empty stomach.
 Effects on calcified tissues: (Discoloration or
hypoplasia of teeth, temporary stunting of growth).
Contraindicated in Children and Infants.
 Hepatotoxicity:
 Phototoxicity: (Severe sunburn may occur in patients
receiving tetracycline) who are exposed to sun.
 Vestibular dysfunction: Dizziness, Vertigo, Tinnitus.
 Psuedotumor cerebri: Benign intracranial hypertension
characterized by headache and blurred vision. (Rare)
 Contraindications: Not Used in pregnant and
breastfeeding women. Not used in children age less then 8-
years.
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Tetracyclines (Nursing care)
• Administer with food.
• While giving I/M injections, rotate sites.
• Avoid taking with dairy foods, antacids, iron
preparations.
• Adequate hydration.
• Advise for protective clothing and sunscreen to
prevent from photo-toxicity.
• Monitor liver and renal function
• Take complete history for pregnancy and lactation
• Assess for vestibular toxicity
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Chloramphenicol
 Broad Spectrum Antibiotic (Bacteriostatic)
 US market removed drug from the market due to its toxicity.
 MOA:
 Chloramphenicol binds to the bacterial 50s ribosomal
subunit and inhibits protein synthesis at the peptidyl
transferase reaction.
 Antibacterial Spectrum:
 Active against (Chlamydiae, Rickettsiae, Spirochetes and
anaerobes).
 Pharmacokinetics:
 Administered in IV form widely distributed in the body.
Crosses BBB, undergoes hepatic metabolism. Elimination is
via Urine. Drug is also secreted into Breast Milk.
Adverse Effects
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 Anemias
 Gray Baby Syndrome (Neonates have a low capacity to
glucouronidate the antibiotic, and they have
underdeveloped renal function, which decreased their
ability to excrete the drug. This leads to drug accumulation
to concentrations that interfere with the function of
mitochondrial ribosomes, causing poor feeding, depressed
breathing, cardiovascular collapse, cyanosis (hence the
term “Gray Baby” and death.
 Drug Interactions:
 Inhibits some of the hepatic mixed function oxidases.
Preventing Metabolism of Warfarin and Phenytoin.
Chloramphenicol (Nursing Care)
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-Use cautiously in infants, children and patients with
history or family history of bone marrow suppression.
-Take oral drug with full glass of water on empty
stomach.
-Monitor Chloramphenicol blood levels.
-Check CBC before, during and after therapy
Fluorquinolones
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 Broad Spectrum (most effective for gram -ve)
 Bactericidal activity
 MOA:
 Fluorquinolones enters the cell through porin channels,
bind to the topoisomerases and DNA gyrase and interfere
with DNA ligation. This interference increases the number
of permanent chromosomal breaks, trigering cell lysis.
 Antibacterial Spectrum:
 1st Generation (Nalidixic acid) Narrow Spectrum
 2nd Generation (Ciprofloxacin) Broadened Coverage
 3rd Generation (Levofloxacin) Broad Spectrum
 4th Generation (Moxifloxacin, Gemifloxacin, Delafloxacin)
enhanced the gram +ve activity.
Pharmacokinetics:
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 Absorption: Well absorbed orally. Levofloxacin and
Moxifloxacin having a bioavailability that exceeds 90%.
 Distribution: Binding to plasma proteins ranges from
20% to 84%. Distributed well into all tissues and body
fluids. Penetration into cerebrospinal fluid is good.
 Elimination: Excretion via renal. Therefore dose
adjustment needed in case of renal failure.
 Adverse Reactions:
 Diarrhea, Nausea, Headache, Dizziness, Tendon rupture,
Arrythemia, Seizure, Peripheral Neuropathy,
Phototoxicity.
Clinical Uses
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 1. Ciprofloxacin: is used to treatment of Traveler’s
diarrhea, typhoid fever and anthrax.
 2. Levofloxacin: Similar activity to ciprofloxacin. But 1st
Line therapy for the Community Acquired Pneumonia
(CAP).
 3. Moxifloxacin: Patient has a history of exposure to
Quinolones three months back then this drug will be used
as 2nd line agent for management of drug susceptible
tuberculosis.
 4. Gemifloxacin: Used in management for community
acquired respiratory infections.
 5. Delafloxacin: Used against MRSA and skin infections
(Fluorquinolones) Nursing Care
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 I/V Ciprofloxacin, and Ofloxacin should be infused
slowly into a large vein over 60 minutes to minimize
discomfort and venous irritation.
 Administer cautiously in patients with CNS
disorders.
 Avoid taking within 2 hours of antacid
administration which reduces absorption.
 Avoid exposure to sun (reduced potency).
 Administer drug with the full glass of water.
 Monitor strictly for bleeding if administered with
anti coagulant (increases plasma concentration
of Warfarin).
 Monitor QT interval on ECG and report.
Sulfonamides (Folate Antagonists)
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 Folic Acid is a co-enzyme essential in the synthesis of
RNA, DNA and Amino Acids.
 Sulfa drugs are family of antibiotics that inhibit
synthesis of folate.
 Drugs of Sulfonamides: Mafenide, Silver
Sulfadiazine, Sulfasalazine
 Antibacterial Spectrum: Active against Gram +ve
and Gram –ve. Sulfadiazine in combination with the
pyrimethamine is preferred treatment of toxoplasmosis.
 Pharmacokinetics:
 Absorption: Well absorbed via oral. IV and ointments
 Distribution: Bind to serum albumin well distributed
in body tissues, can cross BBB and Placental barrier to
enter fetal tissues.
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Pharmacokinetics (Cont..
 Metabolism: Metabolized via Liver. Their precipitate
(Crystalluria “Stone Formation”).
 Excretion: Unchanged Sulfa drug and metabolites
eliminated via Glomerular filtration. Dose adjustment is
needed in case of Renal Failure.
 Adverse Effects:
 Crystalluria
 Hypersensitivity (Rashes, Angioedema, Stevens-Jhonson
Syndrome)
 Hematopoietic Disturbance (Hemolytic Anemia)
 Kernicterus: Bilirubin associated brain damage.
 Contraindications:
 Avoided in Pregnancy Newborn and infants less than 2
months.
MOA (Sulfonamides)
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Nursing Care
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 Assess for allergy with Sulfa drugs
 Monitor strict I/O, changes might indicate effect on renal
function. Visually examine urine for crystals.
 Monitor CBC periodically.
 Instruct and reinforce adequate hydration.
 Instruct client to avoid foods such as those containing Vit
C that produce acidic urine.
 Administer on empty stomach with full glass of water.
However, if GI irritation occurs, can administer with food.
Reference
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 Lippincott Illustrated Reviews: Pharmacology
(Lippincott Illustrated Reviews Series) 7th Edition

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Anti-Microbials.pptx

  • 1. UNIT-II Drugs Used to Treat and Prevent Infections Presenter: Nursing Lecturer: Imtiaz ahmed (Generic BSN) 6/25/2023 1
  • 2. OBJECTIVES 6/25/2023 2 By the end of the session learners will be able to: Define and review common terms and concepts related to antimicrobial therapy. List general principles and considerations related to antimicrobial therapy. Discuss mechanism of action and indication of using antimicrobial therapy. State appropriate nursing implications for a client receiving antimicrobial drugs.
  • 3. Why antibiotics only destroy bacterial cells and not human cells? •Because, the antibiotics are synthesized from the bacterialDNA itself and designed to target the bacterial cell only. Thick peptidoglycan layer in their cell membranes Thin single layer of peptidoglycan and an additional outer lipid membrane with small holes through which only small drug molecules can pass Gram Positive Gram Negative antimicrobial drugs REVIEW 6/25/2023 3
  • 4. 1. Antimicrobialagent: Are the drugs that inhibit the growth of, or kill the bacteria and other microorganisms (e.g. virus, protozoa, fungi) Extended Spectrum Antibiotics Term applied that are modified to be effective against (Gram +ve and Gram –ve) Exp: Ampicillin Broad spectrum antimicrobial agents Drugs that are effective against several groups of organisms. (Gram positive and Gram negative) and also alter the nature of the normal bacterial flora and precipitate a superinfection. Exp: Tetracycline andsome Cephalosporin Narrow spectrum antimicrobial agents Drugs that are effective against one group of organisms or few specific organisms. E.g. Penicillin (Gram +ve) DEFINITIONS: 6/25/2023 4
  • 5. organisms through 3. BactericidalAction To kill the organisms through antimicrobial drugs 4. BacteriostaticAction To stop the growth and reproduction of the antimicrobial drugs 5. Antibiotic Resistance: Antibiotic resistance is the ability of bacteria or other microbes to resist the effects of an antibiotic. Antibiotic resistance occurs when bacteria change in some way that reduces or eliminates the effectiveness of drugs. Bacteria may bring about antibiotic resistance by: Changing their receptor’s structures, occupying receptors with some other molecules, destroying the antibiotics (in some cases) 6/25/2023 5
  • 6. 6/25/2023 6 Indication Treatment (curative use) and prevention of infection (prophylactic use) Major Side effects Allergic or hypersensitivity reactions, organ toxicity and resistance to certain micro organisms Dose Individualized; depends on causative agent, chosen drug, and patient’s condition Route of administration Oral, intravenous, intramuscular, topical. Duration of therapy Depends on specific drug, average duration is approximately 7 – 14 days
  • 7. •Before beginning therapy, Assess drug allergies; hepatic, renal and cardiac function and other lab studies. •Obtain thorough patient health history, e.g. Immune status especially in case of recurrent infections •Assess for contraindications to antibiotic use and potential drug interactions. •It is ESSENTIAL to obtain cultures (Blood, Spinal Fluid, Pleural Fluid, Synovial Fluid, Peritoneal and Urine) BEFOREbeginning antibiotic therapy. •Instruct patient to take antibiotics exactly as prescribed for the specified lengthof time. •For safety reasons, check the name of the medication carefully since there are many agents that sound alike or have similar spellings. Antibiotics: Nursing Intervention 6/25/2023 7
  • 8. Mechanism OfAction: By inhibiting bacterial cell wall synthesis Alteration in membrane permeability By inhibiting bacterial protein synthesis By inhibiting DNA andRNA synthesis Interference with cellular metabolism Antimicrobials 6/25/2023 8
  • 10. 6/25/2023 10 Empiric Therapy: Treatment of an infection before specific organism has been reported through culture sensitivity test; empiric therapy is with broad spectrum antibiotics. Definitive Therapy: The treatment plan for a disease or disorder that has been chosen as the best one for a patient after all other choices have been considered. Prophylactic therapy: Treatment with antibiotics to prevent an infection, as in intra- abdominal surgery, after pacemaker implantation. Classifications of antibacterial agents: 1. Beta-lactam antibacterial (Penicillin, Cephalosporin) 2. Macrolides 3. Aminoglycosides 4. Fluorquinolones 5. Tetracycline 6. Sulfonamides Anti-Bacterial
  • 11. 12 Mechanism of action: Bactericidal Inhibit the synthesis of the Peptidoglycan layer of bacterial cell wall Leakage of intracellular contents microorganisms’destruction. 1. It inhibits transpeptidase which carries out cross linking between various layers of cell membrane. 2. It activates autolysin enzyme by binding with penicillin binding proteins and lysis of bacteria occurs results in Bacterial cell death. Example: Penicillin, Cephalosporin, Carbapenem - These are known as Beta Lactam antibiotics due to the presence of beta lactam ring in their molecular structure. - Resistance may develop due to beta lactamase enzyme produced by some bacteria that destroy the beta lactam ring in their molecular structure. 6/25/2023 11 1. Beta-LactamAntibacterial
  • 13.  Some of the initial Penicillins were narrow spectrum (gram positive); however some recent derivatives are broad spectrum, effective, and widely used antibacterial agent. Examples: Classification 1.Natural Penicillins: ( Penicillin-G, Penicillin-V) Obtained from fungus. Penicillin G (Benzylpenicillin) has a activity against (Gram +ve, -ve and Spirochetes). More than 90% of Streptococcus aureus are producing pencillinase hence resistant to Penicillin-G. (Penicillin remains the drug if choice for the treatment of Gas Gangrene (Clostridium Perfringens) and Syphilis (Trponema Palidium). Penicillin V Only available in Oral formulation has a spectrum similar to that of Penicillin G but NOT used for the severe infections because of its limited oral absorption. 2. Semi-Synthetic Penicillins: (Ampicillin, Amoxicillin) also known as aminopenicillins or extended spectrum Penicillins. Beta-Lactam Antibacterial A. Penicillin 6/25/20 23 13
  • 14. 6/25/2023 14 Penicillin  Ampicillin and Amoxicillin are effective against Gram –ve (H.Influenzae, E.Coli, Proteus mirabilis). Ampicillin with or without addition of Gentamycin is the drug of choice for Gram +ve Bacillus Listeria monocytogens. Widely used in the treatment of Respiratory infections.  3. Antistaphylococcal Penicillins: (Dicloxacillin, Methicillin, Naficillin, Oxacillin)  Are Beta-Lactamase (pencillinase-resistant penicillins), that’s why their use is restricted against the infections caused by pencillinase- producing staphylococci including MSSA (Methicillin Sensitive Staphylococci aureus).  Methicillin is not used because of its toxicity (interstitial nephritis) only used to identify the resistant strains of MRSA is currently a source of serious community and (Hospital acquired infections.
  • 15. Beta-Lactum Antibacterial A. Penicillin 6/25/2023 15  Antipseudomonal Penicillin: (Pipperacillin) is also known as antipseudomonal penicillin because of its activity against Pseudomonas aeruginosa.  RESISTANCE:  1. Beta Lactamase Production  2. Decreased Permeability to the Drug  3. Altered Penicillin Binding Protiens  Pharmkinetics  Routes of Drug Administration:  Ampicillin + Sulbactum , Pipperacillin + Tazobactum  Naficillin, Oxacillin (IV or IM)  Penicillin V, Amoxicillin and Dicloxacillin (Oral)
  • 16. 6/25/2023 16  Depot Forms: Penicillin G (Slowly absorb in the circulation and persist at low level for a log time)  Absorption: Take Dicloxacillin by Empty stomach because it will be destroyed by Stomach acid. While amoxicillin is gastric stable.  Distribution: Distributed throughout the body Can Cross Placental Barrier No any Teratogenic effects Can not cross BBB only cross in case of meningitis.  Metabolism: Metabolized in the Liver  Excretion: Excreted From Kidney via (Tubular Secretory System and Glomerular Filtration)  Adverse Reactions: Hypersensitivity, Diarrhea, Nephritis, Neurotoxicity, Hematologic Toxicities (Thrombocytopenia)
  • 17. 6/25/2023 17 Beta-Lactam Antibiotics 2. Cephalosporins  Cephalosporins closely related to penicillin by functionally and structurally.  Cephalosporins have the same mode of action as penicillins, as they are affected by the same resistance mechanism.  Cephalosporins are classified as;  1st Generation, 2nd Generation, 3rd Generation, 4th Generation on the basis of (Bacterial susceptibility patterns and resistance to beta-lactamases.
  • 18. 2/18/2015 16 First generation Cephalosporin's Second generation Cephalosporins Third generation Cephalosporins Fourth generation Cephalosporins Modest activity against: (Proteus mirabilis, E.Coli, K. Pneumonia) Oral caity aenarobes are also sensitive. Gram negative and activity against Gram positive is weaker Broad spectrum (Highly active against Gram negative) -Third Generation antibiotics has great therapeutic levels in (CSF) Broadest spectrum (Highly active against Gram negative) Exp: Parenteral: Cefazolin (Kefzol) Oral: Cephalexin (keflex), Cephradine (Velosef) Exp: Parenteral: Cefuroxime (Zinacef) -It crosses the Blood Brain Barrier (BBB) Exp: Parenteral: Cefotaxime (Clafron) Ceftriaxone (Rocephin) Has the longest Half Life (6-8 hours) Oral: Cefixime (Cefspan) Example: Cefepime (Maxipime) Effective against Pharyngitis Pneumonia, otitis, sinusitis, RTIs Meningitis , gonorrhea, influenza, typhoid Septicemia, Hospital acquired pneumonia 6/25/2023 18
  • 19. 6/25/2023 19 Pharmacokinetics  Administration: Many Cephalosporins must be administered IV or IM. Because of their poor oral absorption.  Distribution: Distributed very well into body fluids. Adequate therapeutic levels in CSF regardless of inflammation (Meningitis).  Elimination: Eliminated via Tubular secretion and glomerular filtration. Therefore doses must be adjusted in case of renal dysfunction.  One exception: Ceftriaxone (3rd Gen) is excreted via Liver into feces. Therefore ceftriaxone is frequently administered in patient with renal insufficiency. Adverse Reaction:  Anaphylactic Response, Stevens-Jhonson syndrome, or toxic epidermal necrolysis to penicillins should be avoided or used with caution in individual with penicillin allergy .
  • 20. -Broadest spectrum (mixed infections) -Bactericidal Example: Imipenem, Meropenem, Doripenum These drugs are used as empiric therapy because of their activity against Beta Lactamase producing Gram +ve and Gram –ve organisms, anaerobes, P. Aeroginosa. Pharmacokinetics: -Administration: IV -Distribution: Penetrate well into body tissues and fluids, including CSF when meninges are inflamed. Excretion: Excreted by glomerular filtration. Therefore dose must be adjusted in patients with renal insufficiency. Adverse Effects: Nausea, Vomiting, Diarrhea (NVD), Eosinophilia and Neutropenia are less common. High levels of Imipenem may provoke Seizures. Patient with Penicillin allergy can use Carbapenems. 6/25/2023 20 Beta-Lactam Antibiotics: 3. Carbapenem
  • 21. • Assess and monitor for Penicillin allergy. • Cautiously administer Penicillin, as those patients who have taken Penicillin without any problem in past, still have a chance of subsequent reaction with future doses. • Monitor renal and liver function tests and I/O. • Give oral Penicillins on empty stomach with full glass of water. (because it is sensitive to HCL). • While administering penicillins, IV site should be changed q48hrs to minimize blood vessel irritation. • Give I/M injections into large muscles and rotate sites, as it causes pain. • Look for and report signs of resistance. • Monitor patients receiving Imipenem for seizures especially elderly and patients with renal impairment. • If nausea appears with Imipenem administration, slow I/V rate. Beta-Lactam Antibiotics (Nursing Care) 6/25/2023 21
  • 22. 6/25/2023 22 Vancomycin (Glycopeptide)  Vancomycin is a tricyclic glycopeptide active against Aerobic and anaerobic gram positive bacteria, including MRSA, MRSE.  MOA: It binds to the precursors, disrupting polymerization and cross linking required for maintenance of cell wall integrity. This results in bactericidal activity.  Indications: Used against MRSA, Skin and soft tissue infections, infective endocarditis and nosocomial pneumonia.  Frequency of administration dependent on renal function. Therefore, monitoring of creatinine clearance is required to optimize exposure and minimize toxicity . Therapeutic Range of Creatinine is maintained between 10-20mcg/ml.
  • 23. 6/25/2023 23 Vancomycin  Side Effects:  Ototoxicity, Nephrotoxicity, Thrombophlebitis, Red man syndrome, hypotension from rapid infusion (it releases histamine with rapid infusion causing vasodilation.  Nursing Care:  Monitor I/O and V/S.  Obtain and monitor renal and auditory functions tests.  Administer IV slowly.  Look for serum Creatinine and BUN  Have its serum level checked periodically.
  • 24. 6/25/2023 24 Macrolides  Macrolides are group of antibiotic with a macrocyclic lactone structure to which one or more deoxy ribose sugars are attached.  Choice of Drug alternative to penicillin in individuals with an allergy to Beta-Lactam antibiotics.  Names of Macrolides:  Erythromycin, Clarithromycin, Azithromycin, Telithromycin.  Mechanism of Action (MOA)  Macrolides binds irreversibly to a site on the 50S subunit of the bacterial ribosome, thus inhibiting translocation steps of Protein synthesis.  Generally it is Bacteriostatic, they may be Bactericidal on high doses.
  • 25. Macrolides 6/25/2023 25  Indication:  URTI, Skin Infections, Pertussis, Syphilis, Diphtheria, Intestinal Infections, Alternative use of Penicillin.  Pharmacokinetics:  1.Absorption: Erythromycin is destroyed by gastric acid hence given in enteric coated form. Clarithromycin, Azithromycin and Telithromycin are stomach stable. Erythromycin and Azithromycin are available in IV form.  2. Distribution: Widely distributes well to the body and tissues fluids can reach to the prostatic fluid except CSF. All fours drugs are widely distributed in the Liver.  3. Elimination: Undergo hepatic metabolism.  4. Excretion: Metabolites are excreted in the bile.
  • 26. • Erythromycin must be used cautiously in patients with history of hepatic impairment • I/V Erythromycin should be diluted sufficiently and administered slowly. • Monitor hepatic function periodically. • Administer with full glass of water / with meal • Oral suspension should be refrigerated and shaken well before use. Macrolides (Nursing Care) 6/25/2023 26
  • 27. 6/25/2023 27 Aminoglycosides  Aminoglycosides are used for the treatment of serious infections due to aerobic gram-negative bacilli; however the clinical use is limited due to serious toxicities.  Mechanism of Action (MOA):  Inside the cell aminoglycosides bind the 30s ribosomal sub- unit, where they interfere with assembly of the functional ribosomal apparatus and cause the 30s subunit of the completed ribosome to misread the genetic code.  Bactericidal  Drugs: Amikacin, Gentamicin, Tobramycin, Streptomycin, Neomycin.  Antibacterial Spectrum: Effective against aerobic gram –ve, Aminoglycoside + Beta lactam drug to produce synergistic effect.
  • 28. 6/25/2023 28 Aminoglycosides (Pharmacokinetics)  Absorption: All drugs are given parenterally except: Neomycin  Distribution: Drug is hydrophobic so distribution to body fluid is variable.  Can penetrate placental barrier and may accumulate in fetal plasma.  Elimination: 90% of parenteral aminoglycoside are excreted unchanged in the urine except Neomycin which is excreted in feces.  Adverse Effects:  Ototoxicity (Deafness may be irreversible), Vertigo, Nephrotoxicity, Neuromuscular paralysis, Allergic Reaction (Contact dermatitis is common reaction to topically applied neomycin).
  • 29. 6/25/2023 29 Aminoglycosides (Nursing Care) • Monitor hearing and balance. • Monitor renal function tests and I/O specially serum Cr and BUN. • Adequate hydration is vital. • Administer Gentamycin cautiously in clients with impaired renal function, reduced hearing, dehydration, and neuromuscular disorders. • Monitor for dizziness and ringing in ears.
  • 30. 6/25/2023 30 Tetracyclines  Tetracycline is bacteriostatic drug consist of four fused rings with a system of conjugated double bonds.  Mechanism of Action (MOA):  Tetracyclines concentrate intracullarly in susceptible organism. The drug bind irreversibly to 30s subunit of bacterial ribosome. This action prevents binding of tRNA to mRNA-ribosome complex.  Antibacterial Spectrum: Effective against gram +ve, gram –ve bacteria, protozoa, spirochetes, mycobacteria and Chlamydia infections.  Drugs: Demeclocycline, Doxycycline, Minocycline, Tetracycline.
  • 31. 6/25/2023 31 Tetracyclines (Pharmacokinetics)  Absorption: Absorbed after oral ingestion. Administration with dairy products or substances like; (Divalent and Trivalent cations Example: Mg, Ca, Al). Present in both forms IV and Oral.  Distribution: Tetracyclines are well concentrate in the Bile, Liver, Kidney, Gingival fluid, Skin, Teeth and Bones. Minocycline and doxycycline achieve therapeutic levels in th CSF. All Tetracycline cross placental barrier.  Elimination: Minocycline undergoes hepatic metabolism and is eliminated lesser extent via kidney. Doxycycline is preferred in patients with renal dysfunction it is excreted via bile and feces.
  • 32. 6/25/2023 32 Adverse Effects:  Gastric discomfort: (Due to irritation of gastric mucosa), Should be taken on empty stomach.  Effects on calcified tissues: (Discoloration or hypoplasia of teeth, temporary stunting of growth). Contraindicated in Children and Infants.  Hepatotoxicity:  Phototoxicity: (Severe sunburn may occur in patients receiving tetracycline) who are exposed to sun.  Vestibular dysfunction: Dizziness, Vertigo, Tinnitus.  Psuedotumor cerebri: Benign intracranial hypertension characterized by headache and blurred vision. (Rare)  Contraindications: Not Used in pregnant and breastfeeding women. Not used in children age less then 8- years.
  • 33. 6/25/2023 33 Tetracyclines (Nursing care) • Administer with food. • While giving I/M injections, rotate sites. • Avoid taking with dairy foods, antacids, iron preparations. • Adequate hydration. • Advise for protective clothing and sunscreen to prevent from photo-toxicity. • Monitor liver and renal function • Take complete history for pregnancy and lactation • Assess for vestibular toxicity
  • 34. 6/25/2023 34 Chloramphenicol  Broad Spectrum Antibiotic (Bacteriostatic)  US market removed drug from the market due to its toxicity.  MOA:  Chloramphenicol binds to the bacterial 50s ribosomal subunit and inhibits protein synthesis at the peptidyl transferase reaction.  Antibacterial Spectrum:  Active against (Chlamydiae, Rickettsiae, Spirochetes and anaerobes).  Pharmacokinetics:  Administered in IV form widely distributed in the body. Crosses BBB, undergoes hepatic metabolism. Elimination is via Urine. Drug is also secreted into Breast Milk.
  • 35. Adverse Effects 6/25/2023 35  Anemias  Gray Baby Syndrome (Neonates have a low capacity to glucouronidate the antibiotic, and they have underdeveloped renal function, which decreased their ability to excrete the drug. This leads to drug accumulation to concentrations that interfere with the function of mitochondrial ribosomes, causing poor feeding, depressed breathing, cardiovascular collapse, cyanosis (hence the term “Gray Baby” and death.  Drug Interactions:  Inhibits some of the hepatic mixed function oxidases. Preventing Metabolism of Warfarin and Phenytoin.
  • 36. Chloramphenicol (Nursing Care) 6/25/2023 36 -Use cautiously in infants, children and patients with history or family history of bone marrow suppression. -Take oral drug with full glass of water on empty stomach. -Monitor Chloramphenicol blood levels. -Check CBC before, during and after therapy
  • 37. Fluorquinolones 6/25/2023 37  Broad Spectrum (most effective for gram -ve)  Bactericidal activity  MOA:  Fluorquinolones enters the cell through porin channels, bind to the topoisomerases and DNA gyrase and interfere with DNA ligation. This interference increases the number of permanent chromosomal breaks, trigering cell lysis.  Antibacterial Spectrum:  1st Generation (Nalidixic acid) Narrow Spectrum  2nd Generation (Ciprofloxacin) Broadened Coverage  3rd Generation (Levofloxacin) Broad Spectrum  4th Generation (Moxifloxacin, Gemifloxacin, Delafloxacin) enhanced the gram +ve activity.
  • 38. Pharmacokinetics: 6/25/2023 38  Absorption: Well absorbed orally. Levofloxacin and Moxifloxacin having a bioavailability that exceeds 90%.  Distribution: Binding to plasma proteins ranges from 20% to 84%. Distributed well into all tissues and body fluids. Penetration into cerebrospinal fluid is good.  Elimination: Excretion via renal. Therefore dose adjustment needed in case of renal failure.  Adverse Reactions:  Diarrhea, Nausea, Headache, Dizziness, Tendon rupture, Arrythemia, Seizure, Peripheral Neuropathy, Phototoxicity.
  • 39. Clinical Uses 6/25/2023 39  1. Ciprofloxacin: is used to treatment of Traveler’s diarrhea, typhoid fever and anthrax.  2. Levofloxacin: Similar activity to ciprofloxacin. But 1st Line therapy for the Community Acquired Pneumonia (CAP).  3. Moxifloxacin: Patient has a history of exposure to Quinolones three months back then this drug will be used as 2nd line agent for management of drug susceptible tuberculosis.  4. Gemifloxacin: Used in management for community acquired respiratory infections.  5. Delafloxacin: Used against MRSA and skin infections
  • 40. (Fluorquinolones) Nursing Care 6/25/2023 40  I/V Ciprofloxacin, and Ofloxacin should be infused slowly into a large vein over 60 minutes to minimize discomfort and venous irritation.  Administer cautiously in patients with CNS disorders.  Avoid taking within 2 hours of antacid administration which reduces absorption.  Avoid exposure to sun (reduced potency).  Administer drug with the full glass of water.  Monitor strictly for bleeding if administered with anti coagulant (increases plasma concentration of Warfarin).  Monitor QT interval on ECG and report.
  • 41. Sulfonamides (Folate Antagonists) 6/25/2023 41  Folic Acid is a co-enzyme essential in the synthesis of RNA, DNA and Amino Acids.  Sulfa drugs are family of antibiotics that inhibit synthesis of folate.  Drugs of Sulfonamides: Mafenide, Silver Sulfadiazine, Sulfasalazine  Antibacterial Spectrum: Active against Gram +ve and Gram –ve. Sulfadiazine in combination with the pyrimethamine is preferred treatment of toxoplasmosis.  Pharmacokinetics:  Absorption: Well absorbed via oral. IV and ointments  Distribution: Bind to serum albumin well distributed in body tissues, can cross BBB and Placental barrier to enter fetal tissues.
  • 42. 6/25/2023 42 Pharmacokinetics (Cont..  Metabolism: Metabolized via Liver. Their precipitate (Crystalluria “Stone Formation”).  Excretion: Unchanged Sulfa drug and metabolites eliminated via Glomerular filtration. Dose adjustment is needed in case of Renal Failure.  Adverse Effects:  Crystalluria  Hypersensitivity (Rashes, Angioedema, Stevens-Jhonson Syndrome)  Hematopoietic Disturbance (Hemolytic Anemia)  Kernicterus: Bilirubin associated brain damage.  Contraindications:  Avoided in Pregnancy Newborn and infants less than 2 months.
  • 44. Nursing Care 6/25/2023 44  Assess for allergy with Sulfa drugs  Monitor strict I/O, changes might indicate effect on renal function. Visually examine urine for crystals.  Monitor CBC periodically.  Instruct and reinforce adequate hydration.  Instruct client to avoid foods such as those containing Vit C that produce acidic urine.  Administer on empty stomach with full glass of water. However, if GI irritation occurs, can administer with food.
  • 45. Reference 6/25/2023 45  Lippincott Illustrated Reviews: Pharmacology (Lippincott Illustrated Reviews Series) 7th Edition