Advanced Pharmacology

Introducing
Classification of Antibiotics
• Cell wall biosynthesis inhibitors (CBIs) have historically been one of the most
effective classes of antibiotics. They are the most extensively used class of
antibiotics and their importance is exemplified by the β-lactams and glycopeptide
antibiotics.
• Penicillin is a medication used to manage and treat a wide range of infections. It is
in the beta-lactam antibiotic class of drugs. This activity describes penicillin's
indications, action, and contraindications as a valuable agent in treating infection.
• Pharmacokinetics: All of the penicillins are readily and actively secreted by the
renal tubules and most are eliminated, almost completely unchanged, in the urine.
The majority are excreted in small quantities in the bile, but this is a major route
for elimination of nafcillin from the body.
• Pharmacodynamics: The penicillin molecule binds to a bacterial enzyme (DD-
transpeptidase) that creates “cross-links” in the bacterial cell wall, preventing the
cross-linking action. Thus penicillin prevents bacteria from creating strong cell
walls, in effect killing the bacteria.
• Nursing Consideration: Monitor signs of allergic reactions and anaphylaxis,
including pulmonary symptoms (tightness in the throat and chest, wheezing, cough
dyspnea) or skin reactions (rash, prurits, urticaria). Notify physician or nursing staff
immediately if these reactions occur.
• Cephalosporins: are beta-lactam antimicrobials used to manage a wide range of
infections from gram-positive and gram-negative bacteria. The five generations of
cephalosporins are useful against skin infection, resistant bacteria, meningitis, and
other infections.
• Pharmacokinetics:  Cephalosporins are typically bactericidal and are similar to
penicillin in their action within the cell wall. Cephalosporins are sometimes
grouped into “generations” by their antimicrobial properties. The 1st-generation
drugs are effective mainly against gram-positive organisms. Higher generations
generally have expanded spectra against aerobic gram-negative bacilli. The 5th-
generation cephalosporins are active against methicillin-resistant Staphylococcus
aureus (MRSA) or other complicated infections. [1]
• Pharmacodynamics: Patients who consume cephalosporins while drinking
alcoholic beverages may experience disulfiram-like reactions including severe
headache, flushing, nausea, vomiting, etc.[2] Additionally, like penicillins,
cephalosporins may interfere with coagulability and increase a patient’s risk of
bleeding. Cephalosporin dosing may require adjustment for patients experiencing
renal impairment. Blood urea nitrogen (BUN) and creatinine should be monitored
carefully to identify signs of nephrotoxicity.
Nursing Consideration: It is also important to note that
cephalosporin can enter breastmilk and may alter bowel
flora of the infant. Thus, use during breastfeeding is often
discouraged. Patients who are allergic to pencillins may also
be allergic to cephalosporins.
Patients who are prescribed cephalosporins should be
specifically cautioned about a disulfiram reaction, which can
occur when alcohol is ingested while taking the medication. 
Additionally, individuals should be instructed to monitor for
rash and signs of superinfection (such as black, furry
overgrowth on tongue; vaginal itching or discharge; loose or
foul-smelling stool) and report to the prescribing provider.
IMEPENEM IS INDICATED FOR THE TREATMENT OF SEVERE OR COMPLICATED SKIN,
TISSUE, JOINT, RESPIRATORY TRACT, INTRAABDOMINAL, URINARY TRACT AND
UROGENITAL INFECTIONS AS WELL AS MENINGITIS, ENDOCARDITIS AND SEPSIS
DUE TO SUSCEPTIBLE ORGANISMS.

PHARMACOKINETICS ITS DISTRIBUTES PARTLY INTO CEREBROSPINAL FLUID. THE

DRUG IS ELIMINATED BOTH BY METABOLISM AND EXCRETION. IN NORMAL
VOLUNTEERS, UP TO 70% IS RECOVERED IN URINE, AND THE REMAINDER IS
ACCOUNTED FOR BY A BETA-LACTAM RING-OPENED FORM OF THE COMPOUND.

PHARMACODYNAMICS: BINDING TO PENICILLIN-BINDING PROTEINS (PBPS) IN THE

BACTERIAL CELL WALL AND INHIBITING PEPTIDOGLYCAN CROSS-LINKING
ASSOCIATED WITH CELL WALL SYNTHESIS, WHICH ULTIMATELY LEADS TO CELL
DEATH.

NURSING CONSIDERATION: WATCH OUT FOR SEIZURES; NOTIFY PHYSICIAN

IMMEDIATELY IF PATIENT DEVELOPS OR INCREASES SEIZURE ACTIVITY. MONITOR
SIGNS OF PSEUDOMEMBRANOUS COLITIS, INCLUDING DIARRHEA, ABDOMINAL
PAIN, FEVER, PUS OR MUCUS IN STOOLS, AND OTHER SEVERE OR PROLONGED GI
PROBLEMS (NAUSEA, VOMITING, HEARTBURN).
VANCOMYCIN: IS A TRICYCLIC GLYCOPEPTIDE ANTIBIOTIC ORIGINALLY DERIVED
FROM THE ORGANISM STREPTOCOCCUS ORIENTALIS. VANCOMYCIN IS USED TO
TREAT AND PREVENT VARIOUS BACTERIAL INFECTIONS CAUSED BY GRAM-POSITIVE
BACTERIA, INCLUDING METHICILLIN-RESISTANT STAPHYLOCOCCUS AUREUS (MRSA).

PHARMACOKINETICS HAVE BEEN WELL DEFINED IN A NUMBER OF RECENT STUDIES

IN MAN. SINCE THE DRUG IS EXCRETED PRIMARILY VIA THE KIDNEYS, DOSAGE
MODIFICATION IS IMPERATIVE IN PATIENTS WITH IMPAIRED RENAL FUNCTION. WITH
THE POSSIBLE EXCEPTION OF AQUEOUS HUMOUR AND CEREBROSPINAL FLUID,
VANCOMYCIN PENETRATES WELL INTO MOST BODY FLUIDS.

PHARMACODYNAMICS WHEN IT REACHES THE CELL WALL OF AN ACTIVELY DIVIDING

SUSCEPTIBLE GRAM-POSITIVE BACTERIUM, VANCOMYCIN BINDS TO THE ACYL-D-
ALA-D-ALA PORTION OF THE GROWING CELL WALL. AFTER BINDING, IT PREVENTS
THE CELL WALL FROM FORMING THE CROSS-LINKING NECESSARY TO KEEP IT
STRONG.
 
Nursing Consideration: Monitor signs of hypersensitivity reactions and
anaphylaxis, including pulmonary symptoms (tightness in the throat
and chest, wheezing, cough dyspnea) or skin reactions (rash, pruritus,
urticaria). Notify physician or nursing staff immediately if these
reactions occur.
Caspofungin is a drug in the echinocandins class of medications used to manage and treat
several medical conditions. These conditions include febrile neutropenia, candida
infections, invasive candidiasis, esophageal candidiasis, and invasive aspergillosis

Pharmacokinetics This homopolysaccharide is a major component of the cell wall of many

pathogenic fungi and yet is absent in mammalian cells. It provides osmotic stability and is
important for cell growth and cell division. In vitro, caspofungin has broad-spectrum
antifungal activity against Candida and Aspergillus 
 
Pharmacodynamics Caspofungin is an antifungal drug, and belongs to a new class termed
the echinocandins. It is used to treat Aspergillus and Candida infection, and works by
inhibiting cell wall synthesis. Antifungals in the echinocandin class inhibit the synthesis of
glucan in the cell wall, probably via the enzyme 1,3-beta glucan synthase.
 
Nursing Consideration Ensure patient is adequately hydrated before and during therapy.
Observe for adverse effects during the first 30 minutes of administration - especially for
cardiotoxicity. Monitor and document vital signs including blood pressure and fluid balance
 
 
Drugs that disrupt the cell membrane: Disrupting the plasma membrane causes rapid
depolarization, resulting in a loss of membrane potential leading to inhibition of protein, DNA
and RNA synthesis, which leads to bacterial cell death.

Amphotericin B is an antifungal medication used for serious fungal infections and

leishmaniasis. The fungal infections it is used to treat include mucormycosis, aspergillosis,
blastomycosis, candidiasis, coccidioidomycosis, and cryptococcosis. For certain infections it is
given with flucytosine.
Pharmacokinetics binds to ergosterol in the fungal cell membrane, which leads to the
formation of pores, ion leakage and ultimately fungal cell death.

Pharmacodynamics exerts its antifungal effect by disruption of fungal cell wall synthesis
because of its ability to bind to sterols, primarily ergosterol, which leads to the formation of
pores that allow leakage of cellular components. This affinity may also account for its toxic
effects against select mammalian cells.

Nursing Consideration Monitor patient response to therapy (resolution of fungal infections).

Monitor for adverse effects (e.g. rash, local irritation, burning, etc). Evaluate patient
understanding on drug therapy by asking patient to name the drug, its indication, and adverse
effects to watch for. Monitor patient compliance to drug therapy.
Daptomycin is a cyclic lipopeptide antibiotic derived from the organism Streptomyces
roseosporus. Daptomycin is used to treat various bacterial infections caused by Gram-
positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and
vancomycin-resistant Enterococci (VRE).

Pharmacokinetics daptomycin (DAP) complexes with calcium to form small micelles, and
subsequent membrane insertion is dependent on both the presence of calcium and
phosphatidylglycerol (PG). Once inserted, DAP oligomerizes and transitions to the inner
membrane leaflet.

Pharmacodynamics Antimicrobial pharmacodynamics is the relationship between the

concentration of an antibiotic and its ability to inhibit the growth of micro-organisms. The
principle pharmacodynamic parameter is the MIC of the target organisms for a drug.
The antibiotic concentration at the site of the infection must exceed the MIC for the target
bacteria in order to obtain an antimicrobial effect. Interestingly, some antibiotics have
prolonged persistent effects (post-antibiotic effect) in which the antibacterial action
continues for a period of time after the antibiotic level falls below its MIC. 11 The ability of
an antibiotic to induce a PAE is an attractive property, as antibiotic concentrations can fall
below the MIC for the bacterium yet retain effectiveness in suppressing microbial growth.
 
NURSING CONSIDERATION MONITOR SIGNS
OF ANEMIA, INCLUDING UNUSUAL FATIGUE,
SHORTNESS OF BREATH WITH EXERTION,
AND BRUISING. NOTIFY PHYSICIAN
IMMEDIATELY IF THESE SIGNS OCCUR.
ASSESS ANY BREATHING PROBLEMS, AND
REPORT SIGNS OF DIFFICULT OF LABORED
BREATHING.
Itraconazole is a medication used in the management and treatment of fungal
infections. It is in the antifungal class of drugs. Many of these fungal infections
are rare; however, they can be detrimental to the immunocompromised.

Pharmacokinetics are characterized by a good oral absorption, an extensive

tissue distribution with tissue concentrations many times higher than in
plasma, a relatively long elimination half-life of about one day and a
biotransformation into a large number of metabolites.
Pharmacodynamics it inhibits the fungal-mediated synthesis of ergosterol, via
inhibition of lanosterol 14α-demethylase.

Nursing Consideration Give capsules with a full meal. Give oral solution
without food. Liquid should be vigorously swished for several seconds and
swallowed. Watch out for side effects such as constipation, upset stomach,
headache, sore or bleeding gums, depression, nervousness, sweating and
muscle pain have been noted.
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