1

Antibiotics
Biological Target / Route of
Class Drug Disease Side Effects Contraindications Drug Resistance
Mechanism Admin.
G (+) cocci
G (-) cocci (meningococci)

G (+) rods (Anthrax,

Diphtheria)

G (-) rods (Bacteriodes)

Syphilis (prophylaxis IV
(acid labile) procaine
& treatment) Treponema syndrome, if
pallidum ( spirochete) w/in 24hrs
given IV instead
Prophylax recurrent oral for
of IM
inactivated by
Penicillin G rheumatic fever newborns & -lactamases
(from group A -hemolytic elderly (reduced porin permeability)

Penicillins Streptococcal pharyngitis)

convulsions
H. flu absorbed in
small intestine,
with massive MRSA:
Inhibits bacterial cell
Probenecid blocks
tubular transport, enterococcal endocarditis wall synthesis inhib. by food doses mutation of
penicillin-
elevates plasma levels
of penicillin
Leptospirosis (bactericidal)
binding protein
Very safe direct toxicity drugs DO2 C for B. fragilis
ND
inhib transpepdidation
(use 1.vancomycin or 2.
imipenem for MRSA)
(DOC: metronidazole,
-lactam ring structure. R-side
clindamycin, cefoxitin, of peptidoglycan sugars allergy &
chain important for
antibacterial activity. imipenem) that results in cross- hypersensitivity Pen G is 100%
Vancomycin & Bacitracin linking of cell wall; Staph resistant,
dont have -lactam ring. Prophylactic after dental, tonsillectomy
oral (acid Most US staphs are
Gram POS - NO outer cell- Penicillin V [same as Pen G] activates autolytic penicillin resistant
wall membrane penicillins stable)
ealily penetrate, very effective enzymes cell lysis (use Nafcillin)
Amoxicillin
Hemophilus (bactericidal) eg autolysin oral (acid
Gram NEG HAVE outer cell
(+ clavulanic acid = N/V/D
Gonorrhea
wall memb pens DONT
stable)
penetrate easily, not effective augmentin)
Gram (+) rods N/V/D
(Listeria monocytogenes) oral (acid
Ampicillin
Gram (-) rods stable) skin rashes
amp up blood flow to the skin
(H. pylori)
Ticarcillin
Synergistic w/aminoglycosides
Gram (-) rods, esp. no oral
a Thai car is a pseudo car pseudomonas absorpion
Staph (lac prod, IV (acid
Nafcillin penicillinase-resistant
penicillin G/V resistant) labile)
Oxacillin Staph (lac prod, oral/parenteral moderate bile excretion penicillinase-resistant
penicillin G/V resistant)

Cloxacillin/Dicloxacillin Staph (lac prod, oral penicillinase-resistant

penicillin G/V resistant)
w/amoxicillin = augmentin
-lactamase Clavulanic Acid w/ticarcillin = timentin
Inhibitors Sulbactam, Tazobactam
 2
Antibiotics cont.

Biological Target / Route of

Class Drug Diseases Side Effects Contraindications Drug Resistance
Mechanism Admin.
form of
BACKS GASP dihydropteroate
inhibits folate with low affinity
UTIs (crystalluria unlikely) synthesis for sulfonamides
treat uncomplicated UTI in non-prego pts THF inhibs purines/pyrimidines
oral route
Toxicity:
Pregnancy
Nocardia infections preferred Bone marrow increased PABA
competes w/PABA production to
(sulfa + minocycline)
(TH4 precursor) for
depression
Increases
Sulfamethoxazole
Drug-resistant malaria & enzyme dihydropteroate slow IV Crystalluria anticoagulant
overcome sulfa
drugs
toxoplasmosis synthetase, blocks folate preferable
Treatment is a SNap (sulfa + pyrimethamine) synthesis to IM
Agranulocytosis effect of oral
anticoagulants alternate
& aplastic
Prevent recurrence of structural analogue of PABA,
(irritates
anemia in high-
(displaces them pathways for
rheumatic fever if Pen G essential for folic acid synthesis muscle from albumin) nucleic acid
risk pts. (rare) synthesis
tissue)
Sulfonamides cannot be given in bacteria
Kernicterus in Synergistic with
and (after meningococcal infection)
acetylation (at N4) crystalluria,
& oxidation in liver (formation of neonates
Sulfonyl urea increased
Trimethoprim crystals, czs irritation & pain) hypoglycemia capacity to
(displaces bilirubin from
destroy or
Stevens-Johnson G6DP-deficient
plasma albumin)
Bacteriostatic, Class II
inactivate drug
Cheap drug to use pts: causes acute
syndrome bacteriostatic
inhibits folate hemolytic anemia
Inhibit folate synthesis or (conjunctival and corneal agents negated by
reduction (inhibits (reduction of RBCs)
acute UTI (E. coli?)
reduction disrupt nucleic scarring, blistered face/gen)
acid and protein synthesis - pus, which
(FAH4) tetrahydrofolic acid
Trimethoprim
DHFR) DHFR: FAH2 FAH4 oral route Elim via kidney contains
for prego use 1 cephalosporin
st
Has a much lower IC50 in bacteria
preferred (impaired renal function)
thymidine &
Local application limited to d/t risk of kernicterus in neonates than humans, ie bacterial DHFR is
ocular infection, prophylaxis in more sensitive than human DHFR purines, so no
burns (czs drug sensitization) (cofactor in thymidylate synthesis)
Some non-key drugs used for need for folate
eye infections and burn victims Combination
Pneumocystic carinii (AIDS) reduces individual
synergistic effect,
Shigella & Salmonella inhibitor of folate
side effects
(Quinolones are DOC)
Co-Trimoxazole synthesis and In AIDS pts:
(Sulfamethoxazole UTI reduction
Fever
+ Trimethoprim) Otitis media in children sequential blocking Rash
pregnancy
Respiratory tract infection effective at 1/10 conc; Leukoplakia
due to H. flu or strep much lower chance of crystalluria

Gonococcal urethritis Folate

deficiency
Oralpharyngeal gonorrhea Hepatitis
 3
Antibiotics cont.

Route of
Class Drug Diseases Biological Target / Mechanism Side Effects Drug Resistance
Admin.
Gram (+) cocci
st
1 gen Cefalexin oral (lexi)
Presurgery
prophylaxis Gram (+) cocci
Skin / soft tissue
Cefazolin
E. coli IV
infection from
S aureus, S pyogenes Klebsiella
Shortest duration Proteus mirabillis
Gram (-) extensive
Have basement membrane and extra R-group that penicillins dont have, making them resistant to -lactamases
Inactive against enterococci and MRSA. Active against Gram neg and Klebsiella. Used in prophylaxis

Cefuroxime H flu
nd penetrates CNS Comm-acquired resp
2 gen
infections (otitis media,
penetrates CNS Furry men sinusitis, pneumonia)
Meningitis
inactive against oral
Pseudomonas
aeruginosa
- Gram (-) extensive
Inhibits bacterial cell
Cefotetan - Mixed aero-anaerobic wall synthesis
Cephalosporins

furry fox likes tea infections (DM lower

Fragile teats limb, intra-abdominal) inhibits transpepdidation that same as penicillin, inactivated by -
results in cross-linking (same as allergy and lactamases (same
- B. fragilis (cefoxitin?) penicillins) hypersensitivity as penicillins)
Huge Gram (-) coverage
Ceftriaxone
tx penicillinase-producing Meningitis
inactive against MRSA &
3rd gen
strains of gonorrhea Haemophilus (prod lac)
enterococci (Strep Group D)
Neisseria (prod lac)
longest duration, Cefotaxime
Tri your taxes, go shop at HNM IV
pens CSF / CNS

tri the tazidime taxi

Ceftazidime Huge Gram (-) coverage
Drink your tazo in the Meningitis
PM
PseudoMonas
P. aeruginosa
Cefepime
Enterobacteria active

4th gen S. aureus

more resistant to
HS PENS
S. pneumoniae
-lactamases than 3rd
gen Haemophilus highly active

Neisseria
 4
Antibiotics cont.

Route
Biological Target / Drug
Class Drug Diseases of Side Effects Contraindications
Mechanism Resistance
Admin.
Substitute for amino-
glycosides Inhibits bacterial cell
wall synthesis NO renal toxicity
DO2ndC: (unlike nephrotoxic Penicillin allergic
IM / resistant to -
Aztreonam
(a mono lactam)
G (-) rods aerobic binds to PBP & inhibits cell
IV
aminoglycosides)
Pts w/renal insufficiency can use
pts. CAN tolerate
lactamases
wall synthesis;
Klebsiella this drug
synergistic with
P. aeruginosa aminoglycosides
renal excretion

Penems &
Serratia
DOC:
Monobactams N/V/D
Enterobacter Skin rash resistant to
Imipenem Penicillin allergy most -
Imipenem-Cilastatin
DO2ndC:
Toxicity: lactamases but
(a carbpenem)
Staph infection (non lac prod) Inactivated by DHPs in renal
not metallo- -
B. fragilis (internal abscess)
Seizures in pts. with tubules low urinary conc
lactamases
renal failure (girl from
P. aeruginosa (burn infection) Ipanema has seizures)
NOT an antibiotic;
Cilastatin use with imipenem inhibits renal dihydropeptidase I and
(not an abx)
thus prevents penem degredation

DOC: Very Toxic:

Rickettsia
Inhibits bacterial
protein synthesis Retard bone growth in Resistant
children (damage teeth orgs contain
Chlamydia binds to 30S subunit - blocks bone nails <8yo) pregnancy active efflux
system
Vibrio cholera binding of tRNA to A site on Suprainfection (bone deformity,
growth inhibition TCs cannot
oral
Tetracycline Plague ribosome; bacteriostatic
(not
(C difficile diarrhea, tx of fetus) enter cells
w/oral vancomycin or
Tetracyclines, Toxic Tetracyclines
Lyme disease (B burgdorferi) bacteria have TC uptake with metronidazole) plasmid-
food)
Chloramphenicol Protozoa (amoeba w/iodoquinol) system concentrate TCs vs.
Hepatic dysfunction Excreted in urine &
mediated
resistance
mammalian cells have TC
4

and bile, adjust dose for

DO2ndC: (preggers) MDR: TC, AMG, CAP
Aminoglycosides uptake & efflux cannot renal impairment linked together
Mycoplasma pneumonia concentrate TCs Renal toxicity resistance is
Prophylax meningococcal meningitis
VCM your BR with a tetracyclone
competition with tRNA for A site on ribosome;
inhibits addn of new aas to peptide chain
Yellow teeth wide-spread
chelates Al, Ca, Mg

prophylaxis for travelers diarrhea photosensitivity not to be taken with

antacids or oral iron

Doxycycline prostate infections Inhibits bacterial GI disturbances Excreted in feces (also

protein synthesis
prophylaxis malaria in Vaginitis minocycline), no
accum in blood, no
Chloroquine-resistant areas dose adjustment
 5
Antibiotics cont.

Biological Target / Route of

Class Drug Diseases Side Effects Contraindications Drug Resistance
Mechanism Admin.
Severe infections only
AmiNOglycosides
STiNG mice 1st line drug for TB
Inhibits bacterial
Enterococcal protein synthesis Nephrotoxic
Streptomycin endocarditis (Creatanine too high)
Deletion of
Viridans strep and
[aerobic Gram (-) bacteria only]
causes misreading of mRNA
(protein synthesis inhibitor) 1) binds to P12 P12 gene
receptor protein on Neuromuscular (chromosomal
staph endocarditis usually IM,
30S subunit blockade resistance)
Severe infections only rarely oral
AmiNOglycosides

Neomycin
Most toxic (hearing
Gram (-) enteric 2) blocks formation of
[mRNA+formyl
or IV (no Serious Plasmid-
adverse
loss), topical use In combo with - methionine+tRNA] effects with
Ototoxicity:
Myasthenia Gravis dependent
only; curare-like
NM block lactams (penicillin, complex oral, but Hearing loss (paralysis d/t NM blockade) production of
Tetracyclines, cephalosporin) to fetus / destructive
Chloramphenicol 3) mRNA is misread only affect enzymes
synergistic, expands GI newborn
and 4) wrong aa inserted
spectrum to Gram (+)
Aminoglycosides Gentamicin
microbes) Vertigo Mutant porins
cont Pseudomonas aeruginosa Progressive
Gentlemen fly
Pseudomonas air
(antipseudomonal penicillin) entry thru porins then O-
loss- vestibular
Mutant 30S
Chronic UTI dep active transport mech
organ
ribosome

E. coli or Klebsiella bacteriocidal

Protein Synthesis Inhibitors Tobramycin pneumo (w/ampicillin,
cephalosporin)

Very Toxic:
Pancytopenia
Rare, deficiency of all cell
elements of blood (aplastic
DO2ndC: anemia), hospital use only

Meningitis (pen resis pts) Inhibits bacterial

TC diseases
protein synthesis bone marrow G6PD-defic. pts (AA)
chloramphenicol
Chloramphenicol disturbances (hemolytic anemia),
Oral acetyl transferase
Typhoid (Salmonella) binds to 50S ribosome
GI Tract Gray Baby low RBC count,
(from a plasmid gene)
and inhibits same as sulfa drugs
pour chlorine into a pan
of bone marrow; gray Brain abscess transpeptidation syndrome
Premies/newborns are ash
inactivates drug
babies climb out of the (caused by anaerobes)
(inhibits peptidyl transferase) gray color; sxs: vomiting,
pool of chlorine Eye infections poor feeding, vasomotor
collapse, irreg resp, death;
cz by defic of hepatic
conjugating enzyme
glucoronlyl transferase

death
 6
Antibiotics cont.

Biological Target / Route of Contra- Drug

Class Drug Diseases Side Effects
Mechanism Admin. indications Resistance
Serious G (+) MDR orgs Inhibits bacterial cell
wall synthesis
Nephrotoxicity
Vancomycin
Glycopeptide (tricyclic) antibiotics Meningitis caused by Staph Ototoxicity
IV requires
(not a lactam)
MRSA prevents peptidoglycan hospitilization Thrombophlebitis
DONT take Vancomycin construction (inhibits
outside hospital C difficile suprainfection cell wall mucopeptide Diffuse flushing (red
Penicillin resistant strep formation), bactericidal man syndrome)
Inhibits bacterial cell
wall synthesis
topical use
Bacitracin Gram (+) cocci interferes with only
Misc. Polypeptide antibiotics
Eye & skin infection regeneration of lipid
carrier in peptidoglycan
synthesis by blocking its
dephosphorylation
Spectinomycin
Related to aminoglycosides
Urogenital gonorrhea for Inhibits protein synthesis
speculum to see urogenital gonorrhea penicillin-allergic pts
UTIs czd by MDR bacteria
Anthrax (prophylaxis up to 60 days)
Ciprofloxacin
Pseudomonas
Shigella
Fluoroquinolones

Salonella infectious diarrheas

E. coli G (-) enterobacteria

Inhibits DNA gyrase; also GI disturbances
Helicobacter induces cleavage of DNA
Suprainfection with
Quinolones

DNA topoisomerase II-

Norfloxacin
Infections of soft tissue, uncoils DNA; inhibits DNA
Oral (excellent
streptococci &
candida
pts <18 yrs
bones, joints (NOT routine) transcription and replication
tissue penetration)
(cartilage
Intraabdominal & NOC NOC its a flox of quinolones Cause seizures damage)
Ofloxacin respiratory tract infections gyrating their hips, orally vomiting w/theophylline
with superinfection from partying;
(NOT routine) keep them away from kids!

Gonococcal infections
Chlamydia
Eradicate meningococci
from carriers
Prophylax traveler diarrhea,
neutropenic pt infections
 7
Antibiotics cont.

Biological Target / Route of

Class Drug Diseases Side Effects Drug Resistance
Mechanism Admin
Use in penicillin-allergic pts.
(same spectrum as penicillin)
Spectinomycin for urogen gonorrhea in p/c allergic pt

Mycoplasma pneumonia (DOC)

(G-) community acquired
Erythromycin Enteric-
Lactone/deoxy sugar Chlamydia (G-) during
pregnancy coated or
esterified
(alternative to tetracyclines) Inhibits protein synthesis
ACE-ith the forms
MaCroLiDes Legionella (destroyed plasmid-mediated
binds to 50S ribosome; by somach
Cornybacterium diphtheriae inhibits aminoacyl acid) gene encodes
a macrolide alternate protein
microplatter of corn, Helicobacter translocation
Macrolides

QID on 50S ribosome

clams, and legumes
Listeria causes inhibition of translocation (protein

Neisseria
synthesis inhibitor) Increases
Bacteriostatic
motility of
Misc.
cont. Bordetella pertussis GI tract

Protein Synthesis
Treponema (if penicillin allergy)
Inhibitors: Campylobacter
Gram (+)
Azithromycin
Chlamydia trochamatis SID
Piece of cake you
must eat (oral) H. flu
Clindamycin
Chloramphenicol Clarithromycin H. pylori (combo w/amox + PPI) BID
Erythromycin
Tetracyclines
AminoGlycosides
Amino acid derivs w/sugar
H. flu
Suprainfection by C. diff
Clindamycin B. fragilis (anaerobic) Inhibits protein synthesis oral (pseudomonas colitis)
Hepatotoxicity
Metronidazole
Dont drink on the metrobus, youll get
GI/CNS problems
Bacteriodes (fragilis) oral, IV Metallic bitter taste
Think anaerobic: Clostridia (difficile) Inhibits DNA synthesis;
available Minor GI, CNS symptoms
-protozoa:
E histolytica (amebic dysentery),
Giardia,
Pseudomembranous colitis bactericidal
rapid complete
absorption,
rapid distro thru
Interferes with alcohol
(clostridial infection related to abx therapy)
Trichomonas A van and a metrobus running over C difficile tissue hi metabolism; avoid alcohol
conc in CSF (disulfiram like effect inhibits aldehyde
UTI
-bacteria:
Bacteroides, dehydrogenase; aldehyde toxicity)
C difficile
binds to phosphotidyl
Polymyxins
Basic peptides, cationic detergent
Topical for eye & ear (with ethanolamine, disrupts
transport; detergent-like action
bacitracin or neomycin) makes pores, compromises
integrity of membranes
 8
Anti-Virals

Biological Target / Route of

Disease Drug Clinical Uses Side Effects Drug Resistance
Mechanism Admin.
IV &
reduces incidence of oral Anemia
opportunistic infections
analogue of pyrimidine, glucoronidase Neutropenia (agranulocytosis/long
RNA RV
Zidovudine stabilizes weight thymidine
in liver term administration)
point mutation in reverse
GI disturbances
replication: causes
1.virion (azido- reduces HIV-associated inactivation
transcriptase leads to
contains RT
2.viralDNA
thymidine: dementia inhibits reverse transcriptase agents that
undergo Skin rash reduced drug sensitivity
integrates in
host as a
AZT)
delays onset of AIDS in phosphorylated by cellular enzymes to
glucoronidati
on may alter Paresthesia response wanes with long-
provirus
HIV+ pts (does NOT effect survival time) the triphosphate derivative Zidovudine term use
3.viralDNA
Thymidine analogue metabolism
Fever, headache
transcribed
to genomic
AZT makes me LAN Reduces risk
(by 66%) of
mammalian -DNA polymerase not
effected, but mitochondrial -DNA is
Probenecid
Abnormalities of Liver increasing viral load due to
immunosuppression
inhibits
RNA and transplacental transmission effected hepatic
mRNA function
4.translation
of viral
Prophylaxis after exposure inactivation /
renal
excretion Myopathy
(with Lamivudine and protease inhibitor)
proteins
5.virus
released by
budding
NRTI dose-related neuropathy
6.virus repl
w/o kill host
Zalcitabine
inhibits reverse transcriptase
GI disturbances
7.someRNA
RVs turn
Purine and
pyrimidine
(dideoxy-
cystidine:
Headache
normal cells
to malignant
nucleoside
RT inhibitors ddC) used in combination with AZT activated in T cells by oral Mouth ulcers
different phosphorylation
Become
pathway than AZT Nail changes
AIDS active after Synthetic cytosine
conversion to
a triphosphate
nucleoside analogue
Edema of lower limbs
HIV virus
interacts
derivative
General malaise
w/CD4 and Triphosphate
chemokine derivatives
a dideoxynucleoside
receptors bind to the
substrate resistance to AZT develops
binding site Lamivudine terminates synthesis of
AIDS drugs used in combination with AZT oral pancreatitis in peds more slowly when given in
are given in (3TC) proviral DNA chain
combo:
Nucleotide
analogs are
combo with Lamivudine
converted to
1) 2 NRTIs nucleotide inhibits reverse transcriptase
+ Protease analogs by
Inhibitor, the body. peripheral neuropathy
2) 2 NRTIs
They are Didanosine chain terminator pancreatitis (dose-related)
prodrugs
+ NNRTI, (dideoxy- oral headache
resistance with long-term
3) NTRI + inosine: ddI) switching to ddI after AZT inhibits reverse transcriptase GI disturbances
NNRTI + PI use, but less so than with
therapy shown to be beneficial Rapidly Skin rash
absorbed, even AZT
Purine
dideoxynucleotide
phosphorylated in the host better w/antacids Bone marrow depression
analogue to a triphosphate Insomnia
Alteration of liver func
 9
Anti-Virals cont.
Biological Target /
Disease Drug Clinical Uses Side Effects Drug Resistance
Mechanism
NtRTI used in combo w/ does not require Renal failure (side effects due to drug accum in proximal tubule)
other antiretrovirals phosphorylation or other
Do NOT require
phosphorylation TenoFoviR -increases didanosine modification for activation Faconi syndrome (impairs proximal tubular kidney function)

or modification
for activation
conc toxicity
-decreases Atazanavir
(not a prodrug) Proteinuria
(less toxicity?)
conc (protease inhibitor) inhibit reverse transcriptase Tubular necrosis
Treatment of do not require
AIDS & related phosphorylation for rash
(on trunk, face, and extremities)

Nevirapine
symptoms activation fever, headache rapid resistance if given alone;
prevention of bind to lipophilic pocket of fatigue decreased when combined
NNRTI transplacental with NRTI
Do not require transmission
reverse transcriptase nausea
phosphorylation (better, cheaper than AZT) distinct from substrate
binding site (allosterically distorts the
rash (not as severe as nevirapine)
to become active
Delavirdine polymerase active site)
Bind to lipophilic
pocket distinct
from substrate
inhibit P-450 system, so
CNS effects: dizziness, drowsiness, insomnia,
binding site headache, confusion, amnesia, agitation,
Efavirenz decrease metabolism of
N N end depression, nightmares
protease inhibitors (except
Efa sips (on nevirapine) Teratogenic in monkeys
her lips) 3ZA4,
AIDS not P450
act synergistically with
Induces metabolic enzyme, CYP3ZA4, which
cont. reduces plasma methodone and serum levels of
NRTIs other antivirals including protease inhibitors
crystallization of drug in urine leads to rapid resistance at sub-optimal
dose must administer at
Indinavir increase bilirubin without hepatic abnormalities highest tolerable dose & in
nephrolithiasis combo with RTIs
inhibition of HIV-1 diarrhea
Protease Nelfinavir
protease (cleaves precursor
protein gag-pol 160kDA to
asthenia
INhibitoRS generate viral proteins headache
one navir
essential for final stage of moderate hypertension
viral formation)
LIRNS the
protease
Ritonavir
GI - N/V/D
INhibitoRS yields immature, noninfectious virions.
Elevated hepatic aminotransferase & Cross resistance to indinavir and ritonavir can
occur but needs 3-11 aa changes
combo of RTIs and protease inhibitors is
Rita does NOT sip
additive or synergistic
triglyceride levels inhibit CYP3A4, leading to
decreased metabolism of other drugs
HIV-1 protease is an aspartyl class protease
Mild diarrhea, abdominal discomfort, nausea
resistance after ~1 yr due to
Saquinavir Low bioavailability & metabolized by P-450, single amino acid mutation
and combo with rifamycin or cabamazepine (48 or 90)
further decreases concentration
 10
Anti-Virals cont.
Route of
Disease Drug Clinical Uses Biological Target / Mechanism Side Effects Drug Resistance
Admin.
Lopinavir sub-therapeutic dose of inhibition of HIV-1 protease
Protease
100 / ritonavir inhibits CYP3A- (cleaves precursor protein to combination results
Inhibitors
Ritonavir mediated metabolism, thus generate viral proteins essential in low resistance
cont.
400 increasing lopinavir concs in final stage of viral formation)
mimics HR2 region of gp41
pts. with persistant HIV-1 resistance does
Fusion Enfuvirtide viral glycoprotein and binds to
replication despite tx with occur, but no cross-
Inhibitors (T-20) gp41, blocking entry of virus
other anti-viral drugs resistance found
into cell (36aa peptide)
AIDS Used in combo with other
cont. CCR5-blocking entry inhibitor;
HIV drugs, incl protease Not approved for pts w/drug
binds CCR5 (protein on
Entry inhibitor ritonavir and sensitive HIV strains (eg
Selzentry membrane of CD4+ cells),
Inhibitors NNRTI delaviridine; for pts starting therapy for the first
preventing HIV from attaching
w/HIV strains resistant to time)
to the cell
multiple antiretroviral drugs
Targets integrase (HIV enzyme
Only for pts whose HIV is that integrates viral genetic material
Integrase
Raltegravir resistant to other into human chromosomes for
Inhibitors
antiretroviral drugs transcription of viral genome for new
viral genomic RNA and proteins)
prodrug converted 1st to a
Shingles (Varicella-Zoster)
Herpes Simplex - Oral if immunocompetent, IV if not monophosphate by viral
thymidine kinase, then to a
Local inflammation at IV mutations in viral
Virus genes for
Chicken pox (Varicella) triphosphate by mammalian
site
thymidine kinase
HSV-1 & HSV-2 Acyclovir - in immunocompromised hosts
kinase: acyclovir-triphosphate
oral or IV Renal dysfunction if given or DNA
DNA virus
Humans are only host
Herpes simplex too rapidly IV polymerase lead to
- Genital, mucocutaneous,herpes encephalitis inhibits viral DNA polymerase
Nausea & headache
STD not seen before puberty
500K cases/yr a) prophylactic tx in immunocompromised resistance
b) prophylactic tx in pt w/recurring genital (30x more selective at herpes virus enzymes than at
HSV-1: infection host enzymes)
Oral involvement in sensory
neurons causes recurrent cold
[same as acyclovir] an L-valyl ester of acyclovir
sores or fever blisters similar to acyclovir
Valacyclovir almost completely metabolized oral
Infects cornea; immune response
leads to scarring clouding and to acyclovir, but higher generally well tolerated
blindness; antibody-dependent
complement-mediated lysis of
bioavailability
infected cells of cornea
Herpes simplex in neonates GI N/V/D
Herpes-assoc. encephalitis
HSV-2:
Genital herpes: both 1 and 2 but
primarily HSV-2
phosphorylated to triphosphate
slow IV or
Neurotoxicity late in therapy
Vidarabine
Maternal-fetal transmission (adenine arabinoside) Varicella-zoster in AIDS pt (by cellular kinase) , which
topical
with high doses (reversible)
results in encephalitis and
disseminated herpes infections. 2nd line drug after acyclovir
inhibits DNA polymerase
Bone marrow disturbances
6% infected, 60% of infected
newborns will die due to
immature immune system
(Foscarnate also used and more effective and
less toxic) Can be carcinogenic
Idoxuridine topically Irritation/ contact dermatitis
All prodrugs (thymidine analogue) Herpes simplex & phosphorylated by cellular
dissolved (due to DMSO)
varicella-zoster infections kinases and incorporated into
VIVA le Herpes! Idox in your in dimethy- Topical only- mutagen too
of the eye both viral and host DNA
both eyes sulfoxide toxic for systemic use
 11
Anti-Virals cont.
Route of Drug
Disease Drug Clinical Uses Biological Target / Mechanism Side Effecs
Admin. Resistance
Cytomegalo guanosine analogue; phosphorylated 1st by Bone marrow suppression
virus Life- or sight- viral protein kinase, then by host kinase to
Ubiq DNA virus
Ganciclovir threatening CMV form triphosphate, which competes with Severe myelosuppression if given
guanosine triphosphate for incorporation into IV with AZT (both cause
Recurrence in
immunosuppressed to
(Guanosine analogue)
Prophylaxis in viral DNA granulocytopenia) in AIDS pts
interstitial pneumonia
transplant pts.
(CMV infect of lung)
AIDS: chorioretinitis,
not broken down rapidly, persists in cell for 18-20hrs Potentially carcinogenic or teratogenic
gastroenteritis, neuro
2 nd
line for CMV pyrophosphate analogue; some
my GF has CMV
Foscarnet
(non-nucleoside inorganic eye infection binds to pyrophosphate binding site and IV Serious nephrotoxicity (reversible resistance
Polly has herpes pyrophosphate analogue)
inhibits viral DNA polymerase with dialysis) foscarnephros on fire reported
and CMV

Early stages of
Lassa Fever Teratogenic
IV for Lassa
Lassa Fever
Respiratory adenosine/guanosine analogue; fever; Embryotoxic
Ribavirin
W African arenovirus (adenosine/guanine
Syncytial Virus
Oral, aerosol Oncogenic
hemorrhagic fever analogue)
Works on many alters viral DNA and mRNA synthesis for RSV & Anemia (dose-related & reversible)
viruses; only tx for flu
viral hemorrhagic I went to ATE-Os and got Lassa fever
fevers
Hep B & C Common:
Translation: dont
Hep B: interfere w/HEP, Fever, headache
Acute: fatigue,nausea
Incr liver involvemnt
Jaundice, dark urine
harry, or kaposi
HBV Lassitude (fatigue)
interferon 2b
Chronic hepatitis
Liver failure
Kaposi sarcoma Myalgia
Hep C:
IFNs are inducible
proteins synthesized by
mammalian cells; involved
Hairy cell induce host enzymes that
Other:
Mild sx at onset
in cell growth, regulation, leukoplakia inhibit translation of viral mRNA
Bone marrow suppression
Longterm infection
Chronic liver dz and modulation of the
Most common reason immune response
IFN receptors (gangliosides) inhibit viral
for liver transplant
replication CV changes
Hep C risk factors:
-Illicit drug injection Rashes & alopecia
Altered thyroid & renal function
-Sex partner w/HCV
-Prison / Juvie interferon 2b
-Body piercing/tattoo HCV
& Ribavirin
-Health care worker
exposed to blood Exacerbate autoimmune dz (thyroiditis)
-Newborn of HCV
mom Acute, reversible hearing loss / tinnitus
Oseltamivir inhibition of viral neuraminidase assoc w/
Tx. and prevention changes in
Ethyl ester prodrug
reqs ester hydrolysis in of flu (type A & B) alteration of virus particle aggregation and oral Renal impairment aa sequence
liver for active form - release of N1 & N2
oseltamivir carboxylate
Influenza
Tx flu A, institutional Blocks viral membrane channel M2, fusion oral
Amantadine;
Rimantadine
outbreak / hi risk pt, of viral and endosomal membrane, releases (sometimes Not serious, infrequent
prophylaxis new virions from infected cell aerosol)
Zanamivir
 12

Anti-Fungals
Route of Drug
Drug Disease Biological Target / Mechanism Side Effects Contraindications
Admin. Resistance
VERY TOXIC
subcutaneous & systemic
Amphotericin B
intrathecal 80% - dose dependent
*fungal meningitis* impaired renal function
MCKNG - superficial injection
blastomyces Forms channels through membrane
coccidioides
for fungal Renal hypokalemia
meningitis causes kaluresis
histoplasma binds to fungal membrane
candida ergosterol, and alters selective
IV, topical
fever, chills, headache
prermeability;
cryptococcus neoformans
aspergillis
nausea, vomiting,
mucor
Give w/steroids, abdominal pain
bacteriocidal heparin, and
antihistamine to
minimize adverse anorexia
thrombocytopenia,
Broad spectrum, potent, serious side reaction
effects, used for systemic fungal
infections, used w/flucytosine (synergy)
leukopenia, anemia

systemic & superficial: Phenobarbital decreases resistance

levels of GF by interfering
ringworm (primarily) Oral GI distress with absorption
via decrease
in drug
Interferes w/Spindle Formation
which dont respond to topical therapy
replaced by: clomitrazole, miconazole, Distro: Hepatotoxicity Anticoagulants diminishes transport
and ketoconazole binds to fungal microtubules; deposits in Rashes activity of coumarins by (uptake by energy
dependent mech)

GriSeoFulvin microsporum interferes with spindle keratinizing

cells (likely (hypersensitivity) increasing metabolism rate
trichophyton formation and prevents cell
division; bacteriostatic
reason not Leukopenia Pregnancy: teratogenic Bacteria,
Actinomyces,
effective
epidermophyton topically) Albuminuria Lupus relapse Nocardia, and
deep fungi
no activity against Candida rashes (hypersensitivity), leukopenia
(hematologic), albuminuria (genitourinary)
resistant

Nystatin Superficial (new yorkers) binds to fungal membrane

oral,
ergosterol, and alters selective
Swish and swallow nasty
Nystatin Candida (intestinal) prermeability; bacteriocidal
topical
Epigastric
distress
metabolized to 5-flurouracil,
Flucytosine subcutaneous & systemic which inhibits thymidylate Hematologic problems
Candida synthetase, which (reduced by admin. of uracil)
AmpB will inhibits DNA & RNA synthesis oral Bone marrow depression
FFuCC
Cryptococcus Stevens-Johnson syndrome in
AIDS pts (usu fatal, blisters
flucytosine An anticancer agent
never used alone: use with on skin, mouth, eyes, genitals)
Amphotericin B for synergism
Side effects due to metabolite 5 flurouroacil
Flucanazole subcutaneous & systemic fungal meningitis use
Itraconzole (DOC) (for systemic FungI) intrathecal Amphotericin B
Fungal infections are called mycoses (superficial and systemic) and are chronic and difficult to treat. Caused by use of broad spectrum antibiotics (eg tetracyclines)
and AIDS. Most fungi are resistant to antibiotics, and bacteria are resistant to anti-fungals. Most anti-fungals have toxic side effects. Development of resistance is rare.
 13
Anti-Fungals cont.

Route of
Drug Diseases Biological Target / Mechanism Side Effects
Admin.
Ketoconazole subcutaneous & systemic AND superficial

azoles synthetic
Candida vaginitis oral
antimycotic agents Cutaneous Dermatophyte infection alternative inhibits synthesis of ergosterol;
superficial increases permeability of membrane; Topical
Clotrimazole
Topical treatment of dermatophytic tinea and bacteriostatic (intravaginal
use for vaginal
clt for your clit
Candida skin infections (eg vaginal candidiasis) candidiasis)
subcutaneous & systemic AND superficial
Miconazole topical severe GI disturbances (oral only)
athletes foot (OTC)
Tolnaftate athletes foot (OTC), tinea cruris unknown topical

Anti-Mycobacterial
Route of
Disease Drug Biological Target / Mechanism Side Effects Contraindications Drug Resistance
Admin.
Leprosy Hemolysis of RBCs
-acid fast (no anemia)
Methemoglobinemia
-footpad of irrad thym
mice, armadillo Dapsone resistance increasing,
-in vivo growth slow inhibition of folate synthesis oral so combination
(incubate yrs/decades)
-not highly contagious the rapzone of dapsone
(structural relative of sulfonamide) GI: Anorexia, N/V therapy used
except young kids
-transmit when exudate
of mucus membranes
Allergic dermatitis
& ulcers reach skin
-rare in US, mainly
Fever
Asia & Africa
-only experts can dx it Rifampin [see TB] [Tuberculoid leprosy = dapsone + rifampin ; Leprotamous leprosy = dapsone + rifampin + clofazimine]
-2 types of infections:

Skin discoloration
1)Tuberculoid T cells
prod -interferon
let macrophages kill
intracellular microbes;
Lepromatous leprosy only (red-brown to black)
paucibacillary (few)
2) Lepromatous Clofazimine Binds DNA, may interfere with DNA oral GI intolerance Expensive!
immune response replication
dominated by IL-4
(blocks -interferon);
multibacillary (many)
Alternative to dapsone, expensive! Clofa the expensive leprosy clown climbing a
DNA ladder in his red/black clown suit

Rifampin, M. avium-intracellulare sxs:

M. avium-
Ethambutol,
Clofazimine, Common systemic bacterial infection in Weight loss, intermittent fever,
Ciprofloxacin, AIDS pts, develop concurrently with chills, night sweats, diarrhea;
intracellulare
Azithromycin, decrease in CD4+ cells (<60) prognosis grave; chemo
Amikacin intervention is marginal

Anti-Mycobacterial cont.
 14

Route of
Disease Drug Biological Target / Mechanism Side Effects Contraindications Drug Resistance
Admin.
Drug-induced hepatitis decreased penetration
Bacteriostatic against resting bacteria Allergic skin eruptions into infected cell
Isoniazid Bacteriocidal against dividing bacteria oral or Fever Decreases mutations leading to
Effective on intracellular bacteria parental
Hepatotoxicity
metabolism of overexpression of
I saw a red (orange) antiepileptic inhA or ahpC
Mycobacterium:
-slim rod shaped
pyre burning the liver Pro-drug activated by catalase- injection
Arthritic symptoms drugs acyl carrier protein reductase, or
-resis. to alanine stains peroxidase enzyme; inhibits mycolic acid oxidative stress protecting gene
-acid fast
-aerobic growth (unique to TB) Pyroxidine deficiency vit. mutation in KatG
-slow growing B6 deficiency catalase-peroxidase enzyme
-nonpathogenic species
widely distributed
-pathogenic species: Bacteriocidal Orange saliva, tears, sweat* Pts. on warfarin,
Rifampin
1)develop slowly
2)chronic course
3)high infectivity
inhibits DNA-dependent RNA Fever glucocorticoids, mutation in DNA-
4)low virulence in Rifampin polymerase in prokaryotic cells
oral GI disturbances narcotic dependent RNA
healthy humans
5)do not prod endo or
Red
RNA (inhibs DNA Effective on intracellular, Gram (+), and Skin eruption analgesics, or polymerase reduced
affinity of drug binding
Exotoxins dependent RNA
Gram (-) bacteria estrogen (oral
Induces hepatic enzymes
6)immune response is polymerase)
contraceptives*)
Good penetration in tissue, macrophages
T-cell mediated
(delayed hypersens) Cytochrome P450 (metabolizes drugs, decr their effect)

Tuberculosis Optic neuritis, if renal function

RIPES with TB decreased: resistance occurs
Ethambutol
Tuberculosis: Red-green color blindness rapidly if given alone
-epidemic 18/19th cent inhibits synthesis of arabinogalactin (cell
Etham the arab Decreased visual acuity
-white plague or
wall component) inhibits bacterial oral
mutations leading to
consumption
-poor hygiene, crowded
-50% world infected
is alone; ethane
torching your
growth GI upset overexpression of emb
-leading cz of death by
infectious dz ww
eye Malaise gene
-global emergency
-US hi-risk populations
incl immigrants, home
Fever
less, IV drug users,
AIDS pts pHyrazinamide active at acid pH only hepatotoxicity
-Factors increasing TB:
multidrug resis strains effective against intracellular bacteria in oral or nausea, vomiting rapidly developed
injection
fever
in prisons, shelters, &
IV drug users; poor For life-threatening macrophages
and resistant TB
structural relative of nicotinamide
drug tx or poor in US;
lack of tx in 3rd world
-combo therapy to hyperuricemia
decrease resistance
aminoglycoside antibiotic RAPID, 3 mechanisms:
irreversibly binds to 30S ribosome, Enzymatic deactivation
inhibits protein synthesis
vertigo & hearing loss of aminoglycoside by
extracellular bacteria only (poor adenylation,acetylation,phosphorylation
Streptomycin
penetration)
IV
8th nerve toxicity in permeability of wall
disequilibrium & deafness prevents abx transport
used for life-threatening TB with
meningitis, in combo w/2+ other drugs Mutation of 30S ribosome
reduces drug binding
causes a misreading of mRNA (protein synthesis inhibitor)
 Anti-Protozoals 15

Drug
Disease Drug Clinical Uses Biological Target / Mechanism Side Effects Contrainidcations
Resistance

prevention Doxycycline prophylax in photosensitivity not to be taken

Chloroquine- inhibits protein synthesis with antacids or
only a tetracycline
resistant areas GI disturbances, Vaginitis oral iron
Malaria
From female
prophylax travel to inhibits parasite hydrolysis of GI upset normal
Caused by:
anopheles
mosquito w/
N. Africa,
Carribean,
hemoglobin, leading to
accumulation of toxic heme
Visual disturbances doses Increased
Chloroquine
Plasmodium
falciparum temperate S. by-products and lysis of cell Headache safe drug efflux
CV changes Decreased
Take 1wk before entering
Stages: area, weekly during trip, America, most of membrane
binds to DNA
-mosquito bite weekly for 4wks after leaving
Central America,
sporozoites
-pre-erythrocytic
part of Middle East Ototoxicity toxicity uptake
Increased
Does not tx latent tissue forms
fragments parasite RNA
sporozoites in
liver develop
into tissue
shizonts (0 sx) tx. of erythrocytic Retinopathy at high
metabolism
-erythrocytic
Tissue rupture,
rls merozoites, prevention
stage alters base-pairing properties of template;
concentrated in acidic food vacuoles (raises pH) Skin eruptions doses
invade RBCs,
asexual devel. OR DOC for prevention Hx of epilepsy -Thailand/Kenya
trophozoite
mat shizont treatment MeFloquine tx of Chloroquine- GI N/V/D or psych dx -Quinine cross-
Dysphoria, dizziness
burst, rls
resistant strains resistance; Take
merozoites
chills, fever
similar to Chloroquine Hypersensitivity in combo
-gametocyto-
genesis (m/f)
but not develop
Mother Fuckin epileptics
and psychiatrics may be taken by CNS signs Prego (teratogen),
ataxia, HA, motor function -Parasitic efflux
prego and kids of drug = resis.
Visual & auditory disturbance kids < 2yrs
in human host
Same as chloroquine
-mosquito bite
gametocytes
(<30lb) when travel -Due to long t1/2
ingested in unavoidable advise no travel
mosq & devel
in gut oocyte to
salivary gland

Symptoms:
Atovaquone and Active against Atovaquone selective inhib of
parasite mitochondrial e- xport; Headaches
erythrocytic AND
-Flu-like -
fever, chills,
proguanil (A&P)
exoerythrocytic
Proguanil metabolizes to a
dihydrofolate reductase inhibitor,
GI disturbances
m. ache, V/D,
cough
enhanced efficacy in combo
stages disrupts deoxythymidylate synth. Mouth ulcers
-Severe P falc
malaria -
liver/kidney Primaquine
The queen is always latent
prevent relapse generation of active oxidation
G6PD-deficient
fail, coma, pts: causes
convulsion
Destroys latent tissue forms
tx. of hepatic stages products
hemolytic anemia
Protection: (vovax, ovale; not P. falciparum)
-anti-mosq
Pyrimethamine inhib folate pathway & DNA
measures,
Slow acting schizontocide synth, produce folate precursors Skin rash
Tx. of erythrocytic
prophylactic
drugs, avoid
mosq bites w/ treatment
Pyrimethamine- stage
2 drugs inhibit different steps in Megaloblastic anemia (hi dose)
wide-spread
DEET, net only folate pathway synergistic
w/permethrin,
long sleeves
Sulfadoxine
inhibition of DNA synthesis Severe-fatal cutaneous rxn. d/t overuse
-Vit B and
ultrasound do
NOT prevent
mind your Ps
and Qs Cinchonism: ear ringing, deaf, HA, Naus
mosquito bites
Quinine only for Chloroquine- Disturbed vision
resistant and similar to Chloroquine, but Rare Thailand,
Jesuit missionary, chicona tree
multidrug-resistant P. more toxic & less effective Dysrhythmias (mvmt, speech) Hypersensitivity East Africa
Hypotension
Poor compliance due to
cinchonism - major drawback! falciparum
Hypoglycemia
Anti-Protozoals cont.

Drug
Melarsopol
Pentamidine
isethionate
Trypanosomiasis: African
sleeping sickness
- transmitted by tsetse flies
- parasite in blood, lymph, CSF
- T. brucei gambiense: slowly
developing CNS involvement
- T. brucei rhodesiense:
Progressive & usu fatal, early
CNS involvement and
terminal cardiac failure
Toxicity in 50% of patients at
therapeutic doses
P on a PLaTe
Suramin
The S&P 500 requires
no CNS involvement
Nifurtimox
American Trypanosomiasis:
- Chagas dz (T. cruzi)
-xmit by bloodsuck triatomid
-Socal to Argentina
-congenital, blood transfusion
-acute fever (kids), chronic GI
& heart problems (adults)
Benznidazole
16
Route of
Parasite / Disease Biological Target / Mechanism Side Effects
Admin
VERY TOXIC!
Late stage African Local reactions
meningoencephalitic arsenic compound
Trypanosomiasis, binds to sulfhydryl groups on proteins, Fever, encephalopathy
with CNS involvement inactivating enzymes HTN & myocardial damage
Vomiting & abdominal colic
IV, d/t rapid decrease in BP (histamine release):
Breathlessness
African Tachycardia
Trypanosomiasis, Dizziness
without CNS Headache
involvement (combo. inhibition of adenosine uptake
Vomiting
w/ suramin for T. IM or IV
brucei gambiense) IM (less rxns but sterile abscesses at injection site):
DNA binding and topoisomerase inhibition
Life threatening hypo- or hyperglycemia & IDD
2nd line for Leishmania Skin rashes
P. carinii pneumo (PCP) Nephrotoxicity (reversible)
Thrombocytopenia, anemia, thrombophlebitis, neutropenia
Elevated liver enzymes
Immediate
Nausea, vomiting
African Shock
Trypanosomiasis,
without CNS Loss of consciousness
involvement inhibits parasite energy production Delayed (O sir ASH!) Very toxic, esp. in
Optic atrophy malnourished patients
usu. used in combo Adrenal insufficiency
with pentamidine
Skin rash
Hemolytic anemia
Acute T. cruzi drug converted to free radicals damage
Hypersensitivity reactions
infections (Chagas dz) membranes, enzymes & DNA GI N/V & weight loss
Nifurtimox & Benznidazole reduce
I went on a T cruzi in my ni Benz b/c Im a radical
Peripheral neuropathy & CNS excitability
Suppression of cell-mediated immune rxns
severity of acute dz, but not effective in
chronic infections
2nd line for T. cruzi free radical formation, like metronidazole similar to metronidazole
 17
Anti-Protozoals cont.

Drug Parasite / Disease Biological Target / Mechanism Side Effects Contraindications

Diloxanide Amebiasis (with luminal amebicide active only against intestinal
well tolerated pregnancy
furoate metronidazole) form of amoeba, not abs from GI tract, given orally

Metronidazole Amebiasis Mixed amebicide active against amebas in both GI headache

\

Amebiasis: Trichomonas vaginalis lumen and systemic tissues Concomitant CNS dz

-Entomoeba histolytica Tx sex partners, tinidazole elsewhere nausea Safe at therapeutic doses in
transmitted fecal-oral
E. histolytica selective toxicity for anaerobic and Microaerophilic
dry mouth and Metallic taste
-humans only host
-poor hygienic conditions
microorgs, and anoxic/hypoxic cells pregnancy (mutagenic,
-trophozoite form of parasite
live as commensals in large
intestine, prod cysts that dont
Giardia (DOC) accepts electrons from flavoproteins, creating free disulfirum-like rxns (interferes
carcinogenic at high doses)

harm host
-may invade intestinal mucosa
[see also antibiotics] radicals damage DNA, proteins, membranes with ethanol metabolism) Im a radical metrosexual, GET out
colitis (amebic dysentery)
-also systemic dz, liver abscess Guinea worms (dracu) use w/diox luminal b/c absorbed before L intestine CNS & peripheral effects of my way, but dont drink and drive

Broad spectrum anntiprotozoal/microbial

luminal amebicide (oral admin); not abs from GI tract,
GI upset & diarrhea
Paromomycin Amebiasis an aminoglycoside; binds 30S ribosome & inhibits
protein synthesis Otherwise well tolerated
Iodoquinol Amebiasis
Giardia Headache, dizziness
Quinacrine Giardia lamblia, flagellated protozoan,
Vomiting
Exacerbates psoriasis
from drinking from contaminated
GQ guy has flavor streams/lakes, human-human intercalates into DNA; flavoenzyme inhibition
Was used to tx malaria
tranmission in day care centers,
institutions, and M homosexuals.
Yellow skin, black & blue nails
Ingested cysts transfor into motile
trophozoites in upper GI tract. Toxic psychosis at high doses
[aerosol form of
Nebupent
Pentamidine isethionate]
Pyrimethamine- Toxoplasmosis, from:
sulfadoxine
- undercooked meat w/cysts
- veggies w/oocyst contaminated soil
Skin rash
- oral contact w/cat feces
- congenital from acutely infected moms
Megaloblastic anemia (hi dose)
PS ive got malaria and
toxoplasmosis
Toxoplasmic encephalitis AIDS deaths
Severe-fatal cutaneous rxn.
[see also malaria]
P. carinii
- most common opp infection in AIDS pts broad-spectrum antibiotic; Hi dose therapy in AIDS pts
Trimethoprim- - trophozoites attach to lung epithelial
cells and form cysts
yields adverse side effects (rash,
Sulfamethoxazole - sporozoites develop and are released to works synergistically to inhibit sequential steps in fever, leucopenia, folate defic.,
reinitiate the trophozoite stage
- fever, SOB, nonproductive cough folate synthesis pathway in bacteria/parasites hepatitis) use lower dose
[see antibiotics]
 18
Anti-Helminthic
Route of
Class Drug Helminth Biological Target / Mechanism Side Effects Contraindications
Admin.
Ascaris
Meendazole Intestinal
capillariasis
Bend for the oral
roundworms ; the Enterobiasis
bends bind to -
tubulin Trichuria bind selectively to worm -tubulin and
inhibit microtubule polymerization
Hookworms uncouple oxidative phosphorylation
GI nematodes, esp.
Albendazole
Ascaris Pregnancy teratogenic &
Roundworms al bend for a
pregnancy HAT
Trichuria embryotoxic in animals
(Nematodes) Hookworms
MOA for helminthes: Ascaris selectively active against GI parasites
-Narcosis/paralysis
GI upset
expulsion Pyrantel Enteribiasis activates nicotinic receptors and inhibits
oral
-damaging the cuticle
Pamoate (lethal if Headache, fever
partial digestion or
Ancylostoma cholinesterases
Rash
rejection by immune
system
given
-interfering with Broad specturm N. americanus depolarizing neuromuscular blocker parenteral)
metabolism
dizziness
Trichostongylus parasite spasm and paralysis
Piperazine 2nd line for Paralysis of parasite skeletal muscle;
2nd line pipes are roundworms & parasites expelled alive lethal at high doses
cheap pinworms (cheap)
Ivermectin Onchocerciasis usually well tolerated
(river blindness) induces tonic paralysis of musculature fever, headache Children <5 yrs.
ver means to
see in Spanish
Nematodes activates invertebrate GABA or glutamate- rash Pregnancy
Broad specturm
-Strongyloidiasis
-Ascariasis
-Trichuriasis
gated Cl- channels
muscle, joint pain Meningitis pts.
-Enterobiasis

Niclosamide Minimal GI absorption

Flatworms
(Cestodes)
Ill give you a nickel Tapeworms Inhibition of oxidative phosphorylation mild
for tapeworms, not (tenia solia/saginata)
enough for ATP
Stim of ATPase leads to depletion of ATP
Praziquantel Schistosomiasis causes increased muscular activity Children <4 yrs.
Flukes followed by contraction & spastic paralysis GI upset
(Trematodes)
Prazi like crazy you
get rid of your flat
Liver flukes by increasing Ca2+ permeability Headache Pregnancy
(also a flatworm) tree flukes Other cestodes & high doses cause tegumental damage which Muscle, joint pain Ocular cysticercosis
flukes activates host immune system (tapeworm)
 19

Others
Drug Parasite / Disease Biological Target / Mechanism Side Effects Contraindications
Structural analogue of D-alanine, prevents
addition of two terminal alanines to the initial
Cycloserine tripeptide on N-acetylmuramic acid
(peptidoglycan inhibitor);
Blocks alanine racemase
Causes a premature termination of the peptide
Puromycin
chain (protein synthesis inhibitor)
DNA intercalating
agents Proflavine Alter base-pairing properties of the template
and Acriflavine
Actinomycin D Inhibition of RNA polymerase
Cinoxapin,
Inhibition of DNA topoisomerase II (cancer)
Doxorubicin
Nitrogen mustards
Covalent modification of DNA (cancer)
and nitrosoureas
Antifungal agent ionophore causes fungal cell
Nystatin
leakage disrupts membrane
Anticancer agent that causes fragmentation of
Bleomycin
DNA
Colchicine,
Cancer chemotherapeutic agents that disrupt
Vinblastine, and
microtubule formation
Vincristine
Carbenicillin (a Toxicity: hypokalemic &
penicillin) transaminase elevation in serum
Fluoroquinolones (others)
Quinolones

Oflaxacin,
Levofloxacin,
Anti-pneumococcal activity
Lomefloxacin,
Moxifloxacin