t5drugs Flashcards
antibacterial, antidepressants
Penicilloic acid
one of the breakdown products of penicillin that can cause an hypersensitivity rxn
how to tx pseudomonas
1. anti-pseudomonas penicillins: ticracillin and piperacillin
3rd gen cepholosonin(zone and dime),
4th gen cepholosporin
Carbapenems(except Etrapenem)
Monobactam/ Aztronam
amino glycoside
tx febrile neutropenia
anti-pseudomonas penicillins: ticracillin and piperacillin
Cefipime - 4th gen cepholosporins
Chloramphenicol
anything broad spectrum will work
MRSA tx
5th gen - ceftraroline
Vancomycin(DOC)
Daptomycin
tetracyclines
clindamycin
linezolid
mupirocin
rifampin
can be given by inhalation to CF patiences
aztronam for pseudomonas
binds D-ala D-ala
vancomycin
becomes resistant is D-ala changes to D-lactate
empiric
treatment of infective endocarditis
what if the person has a valve replacement
what is there is resistance to the first line
Vanco and gent
if there is a valve replacement add rifampin
if there is resistance to vanco try daptomycin / linezolid
tx c.diff
Vanco (oral!)
Fidaxomicin
Metronidazole
what is daptomycin off limits for (2)
pneumonia
also do not give with statins bc both elevate creatine phosphokinase/ causes muscle pain.
Binds to cell membrane via calcium-dependent insertion
of lipid tail, results in
daptomycin
Results in depolarization of cell membrane with K+ efflux
→ cell death
Bind reversibly to 30S subunit of ribosome, preventing….
tetracyclines
preventing attachment of aminoacyl tRNA
drug that can target intracellular orgs
what else does this drug cover
list then
tetracycline
and covers atypical
listeria, Rocky Mountain, chlamydia/neisseria, mycoplasma
intracellular orgs
10
listeria, Neisseria, herpes, toxplasmosis, chlamydia, mycoplasma tuberculosis, rickettsia, leishmania, brucella-parasite
common tetracycline resistnace
increased efflux pump
inference with binding of ribosomes.
severe acne & rosacea
tetracycline
emperic therapy of outpatient community acquired pneumonia
outpatient with comorbidities
doxycycline
or
macrolide
if comorbidities: rest fluoroquinolone or macrolide plus beta lactam
treating atypical pneumonia
examples?
tetracyclines
macrolides(DOC)
Mycoplasma,
Chlamydia, Legionella
syphillus tx if allergic to peniclinnin
tetracycline
tetracyclin
Drugs of choice for:
Used in combination for:
* H.pylori eradication
* Malaria prophylaxis and treatment
* Treatment of plague, tularemia, brucellosis
- *Chlamydia
- *Mycoplasma pneumoniae
- Lyme disease
- Cholera
- Anthrax prophylaxis
- Rickettsia (Rocky Mountain Spotted Fever,
dont take with calcium
tetracycline
floroquinolones
tetracyclines AE
discoloration of teeth, growth stunt(dont give in pregnancy and under 8yo)
fatal hepatotoxicity
accumulation in many organs including skin causing photosensitivity
concentration dependent killing
aminoglycosides
one dose a day is more efficious
all the other drugs are time dependent killing
30S ribosomal subunit prior to
ribosome formation leading to irreversible inhibition of
initiation complex :
* misreading of mRNA, &
* blockade of translocation
amino glycoside
aminoglycoside resistance
synthesis of enzymes that
modify and inactivate drug by acetylation,
phosphorylation and adenylation
issue with 30s
Empiric therapy of serious infections eg, septicemia,
nocosomial respiratory tract infections, complicated
UTI’s, endocarditis etc
aminoglycosides
Neomycin for
bowel surgery prep and hepatic
encephalopathy, as well as topically
gonorhea
first line
2nd line
if resistant
- ceftriaxone
- aztronam
Gentamicin + azithromycin
high levels of amino glycoside in
renal coretx and inner ear
amino glycoside AE
time and concentration dependent(can accumulate in blood)
ototoxicity, nephrotoxicity, NM blockade, contraindicated in pregnancy bc can cause tubular necrosis
hepatic encephalopathy
neomycin, lactulose, oral vanco, oral metro, rafiximin
reduce
plasma ammonia concentrations
laculose
also acts as a factitive
Reversibly bind to the 23S rRNA of the 50S subunit
blocking…
macrolides
blocking translocation
Binding site is identical or close to that for clindamycin & chloramphenicol
-chloramphenicol blocks peptidyltransferase
-clindamycin blocks translocation
streptogramins also bind here
macrolides resistance
Production of esterase that hydrolyze drugs
modification of ribosomal binding site
emperic therapy of inpatient community acquired pneumonia
macrolide + beta lactam
3/4th gen floroquinolone
(can mix up all three)
DOC for whooping cough (B.pertussis)
erythromycin
CYP P450 inhibition
macrolides: E and C
macrolides AE
hepatic
QT prolongation
GI upset(give fluids)
which antibiotics have contraindications with statins
macrolides (bc inhibits CYP 450)
daptomycin(both elevate CPK)
babesiosis tx
macrolides
life threatening with no alternatives
chloramphenicol
glycyclin
cifipem
streptogratins(G+)
Can inhibit protein synthesis in mitochondrial ribosomes
result?
chloramphenicol
bone marrow toxicity- irreversible aplastic anemia
Inhibits hepatic oxidases (3A4 & 2C9)
chloramphenicol
chloramphenicol AE
bone marrow toxicity
grey baby syndrome
ricketsia
chloramphenicol
causes C diff
clindamycin
amp/amoxicillin
cepholosporins
fluoroquinolone
PCP tx
co-trimethoprim
or
clindamycin + primaquine
toxoplasmosis tx
cotrimoxazole + pyrimethamine
or
clindamycin + pyrimethamine
Binds to unique site on 23S ribosomal RNA of 50S
subunit causing…
linezolid
causing inhibition of 70s complex formation
linezolid ae
long term
bone marrow suppression/ thrombocytopenia
optic neuropathy
peripheral neuropathy
serotonin syndrom if also taking MAO I
Block protein synth by binding RNA polymerase
providing coverage against…
fidaxomicin
covers G+ aerobes and anaerobes
Fidaxomicin AE
GI
approved for all bactrove 6 mo
Only topical/intranasal agent with activity against
MRSA
mupirocin
only treats staph and strep
Binds to bacterial isoleucyl transfer-RNA synthetase
resulting in the inhibition of protein synthesis
mupirocin
meningitis prophylaxis
Cefriaxone
Rifampin
Ciprofloxacin
tx travelers diahrea
first choice and alt
ciprofloxacin
or
amoxicillin
levofloxacin can tx
community acquired pneumonia / walking pneumonia
STDs(not syphillus)
URTI
TB
emperic tx for pylonephritis
floroquinolone
fluoroquinolone ae
CT snapping
peripheral neuropathy
QT prolongation
superinfections
not for children less than 18
Structural analogs of p-aminobenzoic acid (PABA) which will….
sulfonamides
which will inhibit the production of folic acid bc it is a competitive inhibitor to dihydrohopterate synthase
sulfonamides uses
topically for ocular or burns ir orally for UTI
coveras G- and G+
sulfonamides AE
nephrotoxicity - crystaluria
in pts with G6PD causes haemapoetic disturbances
kernicterus
takes other drugs off albumin, so will fuck up warfarin/ phenytoin
Structurally similar to folic acid which will inhibit….
trimethoprime
which will inhibit dihydrofolate reductase
*antifolate products are contraindicated in pregnancy
trimethoprime uses
UTI
prostatitis
vagninitis
reaches high concentrations in the urine and prostatic fluids
cotrimoxazole uses
DOC UTI
DOC PCP
DOC norcardia
toxo, UTRI
cotrimoxazole AE
pancytopenia/hemolytic anemia
renal tubular acidosis in babies
contraindicated in pregnancy for kernicterus, albumin problem and other sulfa AE
cyp450 inhibitor
Undergoes reductive bioactivation of its nitro group by
ferredoxin. Forms cytotoxic products that interfere with nucleic acid
synthesis
metronidazole
Blocks transcription by binding to b subunit of bacterial
DNA-dependent RNA polymerase leading to…
inhibition of RNA synthasis
rifampin
rifampin uses
mycobacteria…TB!
MRSA
G+ and G-(Hib prophylacis)
prophylaxis meningitis
rifampin resistance
rpoB mutation in RNA polymerase
Hib prophylaxis
rifampin
cyp 450 inducers
rifampin
rifampin AE
organe fluids
light chain proteinuria
SAFE IN PREG
hepatotoxic
PolymyxinB coverage
polymyxin B
only used as topical for G- but if systemic extremely nephrotoxic
via cationic detergent
Reduction of drug by bacteria in the urine leads
to formation of reactive intermediates that subsequently
damage bacterial DNA
nitrofurantoin
prophylaxis for infective endocarditis
if allergic mild/severe
if cant take oral pills
amoxicillin
if mild allergic: cepholexin
if severe allergic: clindamycin, macrolide,
if cant take oral meds: ampicillin/clinda
(not just dental procedure but any invasive respiratory tract procedure)
nitrofusomide contraindications
renal insufficiency
at term of pregnancy
infants have risk of hemolytic anemia
gun shot anitbiotics
if allergic
carbapenem
if allergic
vancomycin + gentimycin
sx and tx:
-klebsiella pneum
-legionella pneumo
-mycoplasma pneu
-maxorella
-aspirational pneum
-chlamydia pneumo
Klebsiella-“jelly sputum” and causes lobar pneumo G-: 1.ceftriaxone, 2.fluoro
Legionella-MSI inc GI and confusion, need iron and cysteine for culture: 1. fluoro/macrolide 2. tetracycline
mycoplasma- dry cough and low fever 1. macrolide, tetracycline 3. fluoro
maxorella: like most UTRI, amoxicillin, co-trimoxizole, cepholosprins
aspirational/anaerobic = clindamycin
chlamydia-obligate intracellular =1.doxycycline 2. macrolide/ fluoro
emperic STD tx
ceftriaxone and doxycycline
chlamydia tx
first line
if resistantr
what is a confirmatory test
doxycycline
azithromycin OR levofloxacin
diagnosed with NAAT
infective endocarditis caused by alpha hemolytic strep viridian
3
penicillin/ampicillin
vancomycin
ceftriaxone
for some reason they suggest option to add gentimycin
staph aureus infective endocarditis tx
anti-staph beta lactams
if mild allergy: cefazolin
if severe: vancomycin
for some reason they suggest the option to add gentimycin
GAS pharyngitis but allergic to penicillins
macrolide
clindamycin
cotrimoxazole
goes for most URTI
tularemia tx
first line and back up
streptomycin
chloramphenicol
giardia presentation and tx
tx: metronidazole
GI protozoa
UTI tx first line and other options
what if pregnant
co-trimoxazole
nitrofuscion
cipro
amoxicillin
if pregnant:
penicillins, cepholosporins, nitrofucion/sulfonamides but not if past 38 weeks/end of term
prostatits tx
fluoroquinolone
co-trimoxazole
doxy
emperic meningitis
vancomycin + ceftriaxone
MAC treatment and prophylaxis
macrolide, ethanbutol, rifabutin
prophylaxis is macrolide
virus life cycle
blocked with:
neuramidase inhibitors, endonuclease inhibitors, guanosine analogue, nucleoside/tide analogue, NS inhibitors, purine/pyrimidine analogue
binding, uncoating, gene replication, iron assembly, maturation, release
Neuramidase inhibitors block release
endonuclease inhibiors, guanosine analogue, ATP analogue, neucleoside/tide analogue, NS inhibitors, and purine/ pyrimidine analogue(only on actively replicating) block gene replication
for HIV it is binding, fusion/entry, unceasing, reverse transcriptase, integration, transcript, assembly, maturation, release
neuramidase binds
sailiac acid R
so cant be cleaved from host
Prophylaxis and treatment of Influenza A and B
acute uncomplicated
Neuramidase Inhibitors
1. Oseltamivir(oral)
Permavir (parenteral)
Zanamavir(nasal)
endonuclease inhibitor- if 12 or older
both have to be less than 48 hrs
Neuramidase Inhibitor AE
Oselatamivir: Gi upset, eat with food.
Zanamavir: airway irritation avoid in asthma and CPOD
Pernavir:itchy, peeling skin
Endonuclease inihbitor AE
diahreah and bronchitis
polymerase acidic
(PA) protein
required for coral gene replication and blocked by endonuclease inhibitor
Inhibits RNA-dependent RNA polymerase
guanosine analogue:
ribavirin
(another guanosine analogue is abacavir)
-inhibits by inhibiting guanosine triphosphate formation so can do mRNA capping
ATP analogue: Remdesivir
-evades proofreading by viral exoribonuclease EXoN
Both cause dec in viral RNA production
NS5B: Sofobuvir.
prevents viral mRNA capping
ribaviran
Influenza A & B, Parainfluenza, RSV, HCV,
ribaviran
ribaviran AE
prolonged distribution into RBCs and can cause hemolytic anemia causing JAUNDICE
and is pregnany X
COIVD 19 tx
remdesivir
remdesivir AE
Respiratory failure*, hypokalemia, hypoalbuminemia,
neutropenia, jaundice
indirectly inhibit RNA & DNA synthesis by inducing protein expression that inhibit virus infection
(PKR)
interferons
what are the different interferons used for
alpha: for CHRONIC Hep b + entecavit and for Hep C+ ribaviran, condyloma acuminata(HPV-NE dsDNA), hairy cell leukemia, Kaposi sarcoma(HHV8), melanoma
beta: multiple sclerosis
gamma:l chronic granulomatous disease
interferon AE
flu sx, neutropenia esp when with zidovudine(HIV)/ myelosupression
can cause liver failure if given in acute HBV
Usually pegylated to improve PK profile
interferon alpha
suppressive for Hep B
interferon alpha and nucleotide/side inhibitors
Triphosphate form (active) needs to be phosphorylated
Lamivudine, Adefovir, Tenofovir, Entecavir (nucleoside/tide analouges)
-which will supress HBV and HIV reverse transcriptase
all drugs with cycle/ciclo
-to be activated by viral thymidine kinase and host kinases…cidofovir and trifluridine only need to be phosphorylated by the host kinases
NRTIs [hosphorlated by host
Hepatitis B and HIV
Lamivudine. If you want to treat HBV give a low dose less frequent. can also prevent the vertical transmission if given in the last 4 weeks
Entecavir for lamivudine resistant HBV/HIV and just preferred for acute and chronic
-previr
N3/N4a inhibitor for Hep C
Bind reversibly to nonstructural serine protease
and inhibit replication of HCV / distruction
sim glec tela
previr
use if INFa + ribavirin did not work or also if never treated
if treating chronic HCV + Ledipasvir
N3/4a AE
severe itching, rash, photosensitivity, Stevens-Johnson
syndrome (rare)
Inhibits viral phosphoprotein, which is necessary for viral
replication, assembly, and secretion of HCV
NS5a, LEDIPASVIR
LEDIPASVIR AE
headache, diahrea
DNA polymerase inhibitor and DNA chain terminator
acyclovir/v
ganciclovir/v
cidofovir
penciclovir
HSV types 1 and 2, VZV & some Epstein-Barr (HSV4)
acyclovir
NOT CMV bc that bug doesn’t code thymidine kinase
*DOC for HSV encephalitis
-temporal leison
acyclovir
IC herpes prophylaxis and treatment for normal general herpes
acyclovir
RESISTANCE is due to:
* Altered or deficient thymidine kinases
*Altered viral DNA polymerase with decreased affinity for
acyclovir
acyclovir
why give vancyclovir less often
prodrug of acyclovir so have greater oral bioavailability. will partially metabolize causing accumulation in kidneys (even if giving acyclovir IV)
obstructive crystalline nephropathy
how to prevetn
IV acyclovir
hydrate the pt and infuse slowly
CMV infection (retinitis, esophagitis, colitis etc.) & CMV
prophylaxis in immunocompromised
Gancyclovir/valgalcyclovir
RESISTANCE is due to:
* Reduced intracellular phosphorylation
* UL97 or viral DNA polymerase mutations
ganciclovir
Gancyclovir AE
myelosupression and neutropenia
Ganciclovir resistant HSV
cidofovir
also for Used for CMV retinitis in HIV-AIDS patients
- NOT phosphorylated by viral kinases
- Requires activation by host cell kinases
cidofovir
cidofovir AE
nephrotoxicity , needs to be paired with probenecid(blocks tubular secretion of the drug)
Active against HSV-1, HSV-2 and VZV
- Used for topical treatment of HSV (cold sores): poor oral
absorption
pencyclovir
DOC for HSV keratoconjunctivitis and recurrent epithelial keratitis
Active against HSV-1, HSV-2 and vaccinia virus
TRIFLURIDINE
given as ophthalmic ointment only
Selectively inhibits the pyrophosphate binding site on viral DNA polymerases
foscarnet
doesn’t require phosphorylation
Binds specifically and selectively to CCR5 which blocks
blocks fusion and entry
MARAVIROC
Structurally similar to gp41
enfuvirtide
will inhibit fusion
Lack of 3’OH terminates DNA elongation
NRTIs
HIV
NRTIs AE
lactic acidosis
peripheral neuropat (bc inhibiton of DNA poly)
Zidovudine and stavudine = dyslipidemia
thymidine anlouge
stavudine
Zidovudine
Strong inhibitor of beta and gamma DNA polymerases (high affinity for mitochondrial DNA
polymerase, which can lead to toxicity)
stavudine, didamosine
s++peripheral neuropahty, lactic acidosis, hyperlipidemia, weakness, pancreatitis
d++pancreatitis, peripheral neuropath, hepatic dysfunction DO NOT GIVE
adenosine analouge
tenofovir
the only nucleotide
didanosine
tenofovir AE
can cause GI upset in lactose intolerant ppl
must monitor creatine levels
tenofovir + didenoaine / +atazanavir
inc concentrations didanosine
dec concentration of atazanavir and will need to add ritonavir
one of the recommended ARVs for pregnancy, labor,
postpartum and post-exposure prophylaxis of infants. used for LOW risk infants(mom was taking her meds)
*Significant reduction in vertical transmission of HIV
zidovudine
zidovudine AE
MACROCYTIC anemia
neutropenia
dont give with stavudine
cytosine analoude
lamivudine
emtricitabine
DOES NOT affect mitochondrial DNA synthesis or bone marrow
precursor cells
LAMIVUDINE
High level resistance occurs with single amino acid substitutions
LAMIVUDINE
Hyperpigmentation of palms and soles
emtricitabine
Contraindicated if patient has HLA-B*5701 mutation.
abacaivir
can cause type 4 delay hypersensitivity rxn
Noncompetitive inhibitors of
REVERSE
TRANSCRIPTASE
RILPIVIRINE
EFAVIRENZ
NEVIRAPINE
inhibition of RNA & DNA-dependent DNA polymerase
NNRTIs
*Used for HIV-1 ONLY
NNRTIs
better because there is less likely to have attack on blood tissues
NNRTI AE
skin irritation SJS
=tissue necrosis
they fuck with CYP
One of the NNRTIs recommended for use in pregnancy
Rilpivirine
Rilpivirine AE
QT prolongation, elevated LFT, elevated creatine
HIV drug High rate (50%) of CNS toxicities (dizziness, drowsiness, insomnia,
nightmares, vivid dreams, headaches)
Psychiatric disturbances (depression, mania, psychosis)
possible association with suicidality
efavirenz
also teratogenic
and need to monitory lipid levels
Nevidapine AE
severe hepatotoxicity and should not be used in women with +250 or in men +400
Its only current use is for post-exposure prophylaxis of high-
risk infants born to HIV-infected mothers
Nevidapine
-tegravir
integrase inhibitors
GI upset, rash, elevated CPK,
rhabdomyolysis
Raltegravir and Dolutegravir
-navir
protease inhibitors
reversible inhibition of HIV aspartyl proteases
protease inhibitors
which will block maturation so the viron that is released is non infectious
Resistance is due to
accumulation of stepwise
mutations
protease inhibitors
which protease inhibitors are particularly affected by high fat meals
inc availability in nelfavir
dec availability in indinavir
- Disturbances in lipid metabolism (hypertriglyceridemia,
hypercholesterolemia & diabetes)
protease inhibitors
get Cushing type
except atazanavir
which protease inhibitor can not be boosted by ritonovir
nelfinavir
PK enhancers block
CYP 3A4
*Used commonly in combination
with the INSTI elvitegravir
*Also found in combination with
darunavir and atazanavir
COBICISTAT
*Used in combination with
most protease inhibitors but
not nelfinavir
ritonavir
HIV prophylaxis
EMTRICITABINE
+
TENOFOVIR
HIV post exposure prophylaxis
EMTRICITABINE
+
TENOFOVIR
+
Dolutegravir/Raltegravir
give for 28 days
HIV treatment naive reginem
tenofovir + emtricitabine +Dolutegravir/ Raltegravir/ Bictegravir
abacavir + lamivudine + Dolutegravir
cold agglutination tests for what orgs
mycoplasma pneumo
EBV
CMV
Legionella
daptomycin AE
muscle pain, interstitial fibrosis
amoxicillin resistance reason vs amoxicillin-clav resistance
- increased enzymatic destruction of antibiotic
- modification of PBPs
monitoring for herpes drugs
acyclovir need CBC, renal, and liver
gancyclovir: CBC, renal
cidofovir : renal
forscanet: renal. electrolytes
Physical examination shows a somnolent
man with conjunctival icterus, ascites, and 2+ edema of the lower extremities.
Cranial nerves are intact. Muscle strength is 4/5 throughout. When he is awake,
there is a postural and action tremor of the forearms and hands that is
accompanied by a sudden, brief loss of muscle strength. His speech is normal,
and he can follow simple commands
hepatic encephalitus
condylomata lata, a maculopapular rash involving the palms and soles, and patchy alopecia
secondary ssyphillus
bactracin
topical use
antibiotic works as cell wall inhibitor
inhibited by antacids
tetracycline
antifungals
intracellular orgs
bacteria: ricketsia, chlamydia, neissera, listeria, mycoplasma
parasite: brucella, toxo, leishmania
virus: herpes
-pristin
streptogramin
