Pharmacology Exam IIAntimicrobials

Cell Wall Synthesis Inhibitors (Bactericidal)

Drug Name
Mechanism
Spectrum
Inhibits peptidoglycan
Narrow-limited to
Vancomycin

Bacitracin
Penicillin -lactam
Penicillin G

Clinical Uses

Adverse Eff.
Nephrotoxicity
Hearing Loss

Not well
absorbed in GI or
CSF

Nephrotoxicity

Not well
absorbed in GI

formation

G+

Route: IV or IM
Multi-drug
resistant Staph

Inhibits peptidoglycan
carrier

Narrow-some G+

Route: Topical

Inhibits peptidoglycan
cross-linkage (via
transpepdidase)

Broad:G- esp.
spirochetes

Route: IM
Group A Strep

Absorption

Termination
Renal Excretion

Resistance

Notes

Yes

Quinopristin/Dalfopristin
& Linozolid is used if
microbe is vanco
resistant more later

Not well
absorbed in GI
Poor stability in
acid

-lactamasepenicillinase
sensitive

Coadministration with
Procaine or Benzathine
prolongs blood level

Good Stability
in Acid

Penicillinase
sensitive

Route: Oral
Gonorrhea &
Syphilis

Penicillin V
Penicillin H
Phenoxymethyl
Penicillin
Amoxicillin +
Clavulanic Acid
(Augmentin)
Pipercillin +
Tazobactam

Broad

Route: Oral

Broad-G- bacilli

Route: IM

Not well
absorbed in GI

Route: IV or IM

Not well
absorbed in GI

Ticarcillin
Cephalosporins -lactam
1st-Cephalexin Inhibits peptidoglycan
(via
1st-Cephazolin cross-linkage
transpepdidase)
nd
2 -Cefaclor
3rd-Cefotaxim
3rd-Cefixime
4th-Cefepime
Carbapenem -lactam
Imipenem + Inhibits peptidoglycan
(via
Cilastatin cross-linkage
transpepdidase
Meropenem
Ertapenem
Monobactams -lactam
Aztreonam Inhibits peptidoglycan
cross-linkage (via
transpepdidase

More broad than

penicillin:
1st generation is
narrow for G-, broad
for G+
4th generation is
most broad for G- &
narrow for G+

Route: Oral
Route: IM or IV
Route: Oral
Route: IM
Route: Oral
Route: IV or IM

More broad than

both penicillins &
cephalosporins

Route: IV or IM

Broad vs. Pen G:Gbacilli

Route: IV or IM

Nephrotoxicity ( if
combined w/
aminoglycoside)
GI upset
Nausea
Anemia
(reversible)
Allergy (5%)

Clavulanic
Acid:Irreversibl
e inhibition of
penicillinase
Tazobactam:
Irreversible
inhibition of
penicillinase

Augmentin XR is higher
dose that is effective
against amoxicillin
resistant microbes

Renal Excretion

Resistant to
Penicillinases
Distribute to
CSF

Cilastatin inhibits
hepatic peptidases

Not well
absorbed in GI

Broad lactamase
resistance

Cell Membrane Drugs (Antifungal & Bactericidal)

Drug Name
Mechanism
Spectrum
Fungicidal
Broad:GPolymyxin

Clinical Uses

Adverse Eff.

Route: IV or IM

Nephrotoxic

Route: Topical

Nephrotoxic

Route: IV or IM
Deep fungal
infect.
Only in hospitals
where renal fn
can be monitored

Nephrotoxic
(decreases fn
70-80%)
Headache

Detergent effect

Nystatin
Amphotericin B

Azole Group
Imidazole
Triazole
Itraconazole

Fungicidal polyene
Disrupts sterol site in
membrane
Fungicidal polyene
Disrupts sterol site in
membrane

Fungicidal
Inhibits synthesis of
sterols in membrane
Route: IV or IM
(can be oral)

Fluconazole

Fungal menigitis

Clotrimazole

Route: Topical

Terbinafine

Absorption
Not well
absorbed in GI

Fungicidal
Binds to skin hair
and nails

RNA Synthesis

Nitrofurantoin

Alters DNA so that it

cannot act as
template for
replication

Not well
absorbed in GI
Distributes to
CSF

Resistance

Notes
Doesnt require active
replication
Can be given w/
Bacteristatic drug

Slow

Cannot be combined
with polyenes

Fast
Liver
metabolism

Inhibits metabolism of
other drugs

Renal excretion
Useful topicallycommon in antifungal
creams

Route: Topical

Nucleic Acid Synthesis Inhibitors (Bactericidal)

Drug Name
Mechanism
Spectrum
Fluroquinolones
Broad:G+ & GCiprofloxacin Inhibit
bacilli, some
Levofloxacin topoisomerase
(prokaryotic enzyme)
mycobacteria
Rifampin

Mild GI upset &

hepatotoxicity
(reversible)
Mild GI upset &
hepatotoxicity
(reversible)

Termination
Renal Excretion

Narrow:G+, few G(like Pen G except

no spirochetes)

Clinical Uses
Route: Oral

Route: Oral

UTI

Adverse Eff.

Absorption

Dizziness,
seizures
Mild GI upset
cartilage
formation (kids)
Mild GI upset
Orange
secretions

Well absorbed in
GI

Mild GI upset
Headache
Pulmonary
Fibrosis (rare)

Well absorbed in
GI
Distributed in
TBW
Well absorbed in
GI

Termination
Metabolized by
liver
Renal excretion

Metabolized &
activated by
bacteria
Rapid renal exc.

Resistance

Notes

Protein Synthesis Inhibitors (Bacteriostatic)

Drug Name
Mechanism
Spectrum
Aminoglycosides
Broad:G- bacilli
Gentamycin Binds to receptor on
Amikacin
Tobramycin

Minocycline

Macrolides
Erythromycin

Renal Excretion

Extremely Broad:
G+, G-,
actinomycetes,
Rickettsia,
Chlamydia, E.
Histolytica, esp.
Mycoplasma (TB)

Route: Oral, IV, IM

Route: Oral, IV, IM
For young children
Route: Oral only
E. Histolytica
Route: Oral only
E. Histolytica

Mild GI upset
Or @ site of
injection

Renal Excretion
Renal Excretion

Binds 50S subunit &

inhibits peptide bond
form.

Broad: G+, G-,

Rickettsia

Route: Oral

Allergy 5%
Brown color on
teeth
Phototoxicity
Opportunistic
inf.ections: Broad
spec. destroys
normal flora
Allergy
Toxic Bone
Marrow
Suppression vs.
Aplastic anemia
Mild GI upset
Newborn cardiac
toxicity

Well absorbed in
GI
Distributed in
CSF

Liver metabolism
(binds to
glucuronic acid)
Renal excretion

Binds 50S subunit &

inhibits peptide bond
form.

Broad: G+, some

G-, esp.
Mycoplasma (TB)
(like Pen G)
Slightly Broader G+,
GSlightly Broader for
GMainly G+, few G-

Route: Oral

Mild
hepatotoxicity

Well absorbed in
GI

Biliary excretion
Fecal Excretion
Renal 3-5%

Route: Oral

Allergy (5%)
Colitis-type GI
upset
Mild Bone
Marrow
suppression

Mild GI upset (520%)

Liver Metabolism

Broad: Limited to G+
(staph, strep,
enterococcus)

Route: IV

Not well
absorbed in GI

Liver Metabolism
Biliary excretion
Fecal excretion

Slightly Broader:
Limited to G+
(staph, strep,
enterococcus)

Route: Oral

Pain & Inflam. @

site of
administration
Joint & Muscle
Pain
GI upset
Monitor bone
marrow for
thrombocytopeni

Well absorbed in
GI

Liver Metabolism
Renal excretion

Binds to receptor on
30S Subunit
Blocks amino-acyltransfer RNA

Azithromycin
Binds 50S subunit &
inhibits peptide bond
form.

Vancomycin resistant Drugs

Quinupristin/ Binds 50S subunit &
peptide bond
Dalfopristin inhibits
form.
Linezolid

Termination

Not well
absorbed in GI

Clarithromycin

Clindamycin

Absorption

Irreversible
effect on
vestibular fn

(main) + TB
Broader
Broader except
w/TB
Broadest (last
resort)

Doxycycline
Chloramphenicol

Adverse Eff.

Route: IV or IM

30S Subunit
(bacteriostatic)
Causes misread
(bactericidal)

Netilmycin
Tetracyclines
Tetracycline
Oxytetracycline

Clinical Uses

Binds 50S subunit &

Blocks formation of
70S unit

Fecal Excretion
Fecal Excretion

Resistance
Rapid and
common

Notes
Old drug w/ much
resistance

Anti-Metabolite Drugs (Reversible Competitive Antagonists)

Drug Name
Mechanism
Spectrum
Clinical Uses
Sulfonamides (Sulfa Drugs)
Narrow: G+, some
Route: Oral
Sulfisoxazole PABA Anologs
Acetylsulfisoxazole
Succinylsulfathiazole
TrimethoprimSulfamethoxazole
Flucocytosine

folic acid

G-

Used more often

Route: liquid Oral
for children

Decrease GI Flora
prior to surgery
Inhibits DHFR &
PABA

Broader

Fungicidal

Anti-Viral Drugs (non-retroviral)

Drug Name
Mechanism
Anti-Herpes Drugs (non-retroviral)
Acyclovir Guanosine

Clinical Uses

Bone Marrow
suppression
Mild GI upset

Adverse Eff.

Absorption
Well absorbed in
GI
Distributes in
TBW & CSF

Well absorbed in
GI
Distributed in
TBW

Metabolized by
5-fluoro-uracil of
fungus
Renal excretion

Absorption

Termination

Well absorbed in
GI
Distributes in
CSF

Route: Oral
Used for
Cytomegalovirus
(CMV)

Idoxuridine

Thymidine analog
DNA synthesis

Route: Topical in
conjunctiva

Bone Marrowanemia
CNS-dizziness,
headaches
Teratogenic
Too potent for
mammalian cells

Vidarabine

Adenosine analog

Well absorbed in
GI
Distributes to
CSF (not as well
as Acyclovir
Metabolized by
kinases to
triphosphate
level
Metabolized by
kinases to
triphosphate level
Predrug is
metabolized by
GI flora to
activate

Anti-Influenza Drugs (non-retroviral)

Amantadine Blocks viral

Narrow

Route: Oral
Lamivudine
resistant Hep B

Mild GI upset &

Nephrotoxicity

Route: Oral

Mild GI upset

Route: Oral
Prophylactic &
therapeutic
Route: Inhalation
of fine powder

Mild GI upset

uncoating

Oseltamir

Blocks new virion

release

Zanamivir

Blocks new virion

release

Distributes to
CSF if inflame.
meninges
Little distributed
to CSF
Not well
absorbed in GI
Well tolerated

Notes
Soluble in urine
GI Flora will activate by
removing Acetyl group

Renal Excretion

Mild GI upset
Mild
Nephrotoxicity

Inhibits viral DNA

polymerase

Resistance

Renal excretion

Distributes to
CSF

Route: Topically

Adefovir/Dipivoxil

Termination

GI Flora will activate by

removing Succinyl

nucleotide analog
DNA synthesis or
alters structure & fn
Predrug to Acyclovir
Guanosine
nucleotide analog
DNA synthesis or
alters structure & fn

Valacyclovir
Ganciclovor

Narrow

Allergy
Bone Marrow
suppression
CNS toxicity in
newborns
(bilirubin)

Route: Oral
Recurrent UTIs
Route: Oral

Spectrum

Adverse Eff.

Renal Excretion

Renal Excretion
Renal excretion

Resistance

Notes

Anti-Viral Drugs (non-retroviral) Continued

Drug Name
Mechanism
Spectrum
-Interferon
Inhibits viral DNA
Lamivudine
polymerase

Anti-Viral Drugs (retroviral)

Drug Name
Mechanism
Spectrum
Nucleoside reverse transcriptase inhibitors
*Zidovudine (AZT) Thymadine analog is Viral specific (not

*Didanosine

substrate for viral

reverse
transcriptase
Purine analog is
substrate for viral
reverse transcriptase

Fusion Inhibitors
Enfuvirtide

Adverse Eff.

Absorption

Termination

Resistance

DNA Viruses &

Hep B virus

Clinical Uses

Notes
Non-nucleoside antiviral

Adverse Eff.

Route: Oral

GI upset
Anemia

Route: Oral

GI upset
Anemia

mammalian-specific)

Non-Nucleoside reverse transcriptase inhibitors

*Nevirapine
*Efavirenz
Protease Inhibitors
Indinavir Inhibits viral
protease

Clinical Uses
Hep B & C

*Use all three for

Tx

Absorption

Termination

Resistance
High rate of
mutation in
reverse
transcriptase

Notes
-OH group stops
transcription

Selective for viral RT

GI upset
Nephotoxicity
Hyperglycemia
Diabetes
Fat
redistribution
Hyperlipidemia

Inhibits fusion of
HIV to CD4+ cells

Very expensive$20,000/yr