PHA 4107 Study Guide - Final Guide: Leukotriene, Oseltamivir, Ace Inhibitor
29 May 2018
School
Department
Course
Professor
Lecture 12/13
Drug
Clinical effect
Side Effects
Notes
Aminoglycosides
Acts on the 30S and 50S subunit
Treat gram negative bacteria
Ototoxicity (dizziness,
impaired vision, vertigo
etc), Renal Failure, Toxicity
due to concentration and
duration, delayed
symptoms from
administration
Protein Synthesis Inhibitor
Ototoxicity due to
accumulation of AG in the
labyrinth and cochlea
Tetracyclines
Broad spectrum Bacteriostatic for
rocky mountain spotted fever, lyme
disease and MRSA
Discoloration of teeth used
in pregnancy and <8yrs
Slowly degrades into
nephrotoxic materials
Photosensitivity
Protein Synthesis Inhibitor
Resistance develops through
bacterial conjugation,
modified porins (drug efflux,
ribosomal binding, enzyme
inactivation)
Linezolid
Blocks addition of methionine by
blocking tRNA
Protein Synthesis Inhibitor
Does not exhibit cross-
resistance
Mupircoin
Competes with isoleucine in protein
synthesis
Protein Synthesis Inhibitor
Does not exhibit cross-
resistance
Antifolate
Treats bacterial infections, protozoal
infection and cancer
Competes with PABA
-Humans do not produce folic
acid (no production of
dihydrofolate) therefore host
cells are not affected
Sulfonamides
Affects Dihydropteorate synthase
which stops the creation of
sulfonamides
Used for UTI, burns, ocular infection
Mild to life threatening
rashes (stevens-johnson
syndrome)
Hemolytic anemia,
Kernicterus (excess of
bilirubin)
Fluoroquinolones
Bind to DNA gyrase/topoisomerase
Broad spectrum bacterioside
Resistance:
Efflux pumps, in porins
(uptake), inactivation of
bacterial enzymes, target
enzyme alteration
Nitrofurantoin
Treat lower UTIS
Antibacterial drugs
Rapidly excreted in urine
Polymyxin B
Used in creams and ointments
Antibacterial drugs
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Drug
Clinical effect
Side Effects
Notes
Interacts with cell membrane and
stuff leaks out
Daptomycin
Aggregation will form new channels
for membrane depolarization due to
K efflux
Antibacterial drugs
Tail inserts into cell
membrane.
Rifamixin
Used fo taele’s diahea
Antibacterial drugs
Antimycobacteral
drugs
Treats TB, leprosy, mycobacterium
avium-intracellulare infections
TB drugs
Kills bacilli rapidly, eliminate
dormant/sequestered bacilli
Isolation of patient
Multidrug therapy, direct
observation of drug
administration
Intermittent drugs: less cost
and supervision
2nd line – to treat resistant
infections and HIV
coinfections
Isoniazid
Inhibits synthesis of colic acid
1st line of treatment of TB
Resistance prevelant due to
kata gene mutation, whose
product activates INH
Used for HIV+ people, non-
progressive disease, recently
infected, predisposed
conditions, neonates, latent
cases
Ethambutol
Inhibits arabinosyl transferase and
synthesis of arabinogalactan for cell
wall
Increases permeability of cell wall
1st line of treatment of TB
Gene mutation of arabinosyl
transferase causes resistance
Pyrazinamide
Reduces treatment duration
1st line of treatment of TB
Very rapid bactericidal action
Rifampin
Binds b subunit of RNA polymerase
Inhibits DNA transcription and RNA
synthesis
1st line of treatment of TB
Resistance from decreased
affinity of RNA polymerase to
drug
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Drug
Clinical effect
Side Effects
Notes
Bedaquiline
Blocks proton pump for ATP
synthase in TB
Fata heart rhytms and
sudden death
Streptomycin
Inhibits protein synthesis by
targeting the 30S ribosomal subunit
Macrolides
Target 23S ribosomal RNA, inhibiting
peptidyl transferase
Sulfones
Similar mechanism to sulfonamides
-inhibits pteridioate synthase
Clofazimine
Antiinflammatory antimycobacterial
Rifampin
Most actericidal activity
Thalidomide
-Used for TB and leprosy
-originally banned because a
teratogen
Lecture 14
Drug
Clinical effect
Side Effects
Notes
Allylamine
drugs, azole
derivatives
Inhibits synthesis of ergosterol
Amphotericin B
and polyene
antibiotics
Binds to ergosterol in cell membrane
to increase permeability
For severe fungal infection
VERY toxic, liver failure,
arrhythmias, anemia
Flucytosine
Inhibits protein synthesis
Accumulated by fungal cells
Converted to 5fluorouracil
which incorporates into fungal
RNA
Echinocandins
Prevents fungal cell wall synthesis by
inhibiting b-1,3-glucan synthase and
synthesis of b-1,3 glucan
Ciclopirox
Increase membrane permeability
Griseofulvin
Interferes with microtubule fn,
blocks
Tolnaftate
Appears to inhibit squalene
epoxidase like the allylamines
Nucleoside
Analogs
Must be activated by viral and host
cell kinases before they can inhibit
viral DNA polymerase
First converted to
monophosphate derivative by
kinase
Monophosphate converted to
active triphosphate
metabolite to competitively
inhibit DNA polymerase
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Document Summary
Affects dihydropteorate synthase which stops the creation of sulfonamides. Efflux pumps, in porins ( uptake), inactivation of bacterial enzymes, target enzyme alteration. Interacts with cell membrane and stuff leaks out. Aggregation will form new channels for membrane depolarization due to. Inhibits arabinosyl transferase and synthesis of arabinogalactan for cell wall. 2nd line to treat resistant infections and hiv coinfections. Resistance prevelant due to kata gene mutation, whose product activates inh. Used for hiv+ people, non- progressive disease, recently infected, predisposed conditions, neonates, latent cases. Resistance from decreased affinity of rna polymerase to drug. Fata heart rhytms and synthase in tb sudden death. Binds to ergosterol in cell membrane to increase permeability. Prevents fungal cell wall synthesis by inhibiting b-1,3-glucan synthase and synthesis of b-1,3 glucan. Appears to inhibit squalene epoxidase like the allylamines. Must be activated by viral and host cell kinases before they can inhibit viral dna polymerase. Monophosphate converted to active triphosphate metabolite to competitively inhibit dna polymerase.
