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190 Cards in this Set
- Front
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DOC for lyme disease
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Doxy and amoxicillin
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toxicity of tetracycline
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quantity> length of administration
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MOA of tetracycline
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1. inhibit attachment of amino acid-tRNA to A site
2. inhibit attachment of N-formyl met-tRNA to 30S 3. block initiation complex accumulate in prokaryotes |
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SE of tetra
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GI irritation
photosensitivity onycholysis (nail pigmentation) renal toxicity (aggravate uremia) Fanconi syndrome stain teeth deformity/growth of bone dizziness and vertigo vestibular reactions |
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major contraindication
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PREGNANT
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DOC tetracycline
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chollera
rickettsia coviella granuloma inguinale relapsing fever chlamydia nonspecific urethritis |
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Tetra + drug interation?
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oral contraceptive (decrease absorption)
Fe3+, Al3+, Ca2+, Mg2+, Zn2+ |
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tigecycline derived from
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minocycline
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MOA of tigecycline
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binds 30S subunit
blocks amino acyl-RNAs binding |
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tigecycline not used for
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pseudomonas or proeus
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TX place
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complicated skin/skin-structure infections
complicated intra-abdominal infections not useful bc of resistant bacteria CI in kids |
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Tigecycline SE
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photosensitivity
serum amylase hyperbilirubinemia elevated BUN |
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USED FOR TYPHOID FEVER
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chloramphenicol
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main SE of chloramphenicol
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**nausea, vomiting diarrhea
unpleasant taste GRAY BABY transient bone marrow suppression aplastic anemia |
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MOA of chloramphenicol
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bind 50S
inhibit peptidyl transferase prevents mRNA from binding 50S |
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TX place
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complicated skin/skin-structure infections
complicated intra-abdominal infections not useful bc of resistant bacteria CI in kids |
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chloramphenicol is inactived by
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acetylation (carried on plasma)
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Tigecycline SE
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photosensitivity
serum amylase hyperbilirubinemia elevated BUN |
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mech of toxicities
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decrease mitochondrial protein synthesis
prevents polysomes --> single ribosome increased decrease peptifyl transferase decrease cytochrome C oxidase decrease ATPases |
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USED FOR TYPHOID FEVER
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chloramphenicol
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main SE of chloramphenicol
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**nausea, vomiting diarrhea
unpleasant taste GRAY BABY transient bone marrow suppression aplastic anemia |
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chloramphenicol + erthromycin
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compete for 50s
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chloramphenicol + penicillin
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BS + BC
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MOA of chloramphenicol
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bind 50S
inhibit peptidyl transferase prevents mRNA from binding 50S |
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chloramphenicol is inactived by
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acetylation (carried on plasma)
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AG - dont use with these drugs bc of renal toxicity
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Vanocymycin
Amp B Cephalosporins Polymyxin B |
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mech of toxicities
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decrease mitochondrial protein synthesis
prevents polysomes --> single ribosome increased decrease peptifyl transferase decrease cytochrome C oxidase decrease ATPases |
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chloramphenicol + erthromycin
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compete for 50s
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chloramphenicol + penicillin
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BS + BC
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AG - dont use with these drugs bc of renal toxicity
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Vanocymycin
Amp B Cephalosporins Polymyxin B |
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Gentamicin + carbenicillin
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chemic interaction
loss of activity of both |
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gentamicin with what two antibiotics will cause nephrotoxicity?
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polymixin B and cephalothin
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MOA of gentamicin
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binds 30S subunit
penetrate bacterial wall: oxygen-dependent passive diffusion through OM active transport through cell membrane into cytoplasm *oxygen-dependent block further translation and premature termination incorporate incorrect amino acid block initiation of protein synthesis by inhibiting met-amino tRNA binding to ribosomes to form initiation complex |
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resistance to AG
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change 30S structure
decrease entry in bacteria *30S structures convey resistance: R factor (plasmid): acetylation adenylation phosphorylation inactive products |
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what drug is 100% excreted by kidney? High TI
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AG
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toxicities of AG
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8th cranial nerve
renal damage>5 days NMJ junctional blockade OTOXICITY: auditory and vestibular damage RENAL TOXICITY |
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gentamicin + ethacrynic acid
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ototoxic
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spectinomycin DOC For
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gonorrhea
acute gonococcal urethritis, proctitis, cervicitis LESS TOXIC than AG |
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neomycin is used to tx what bacteria
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gram positive cocci
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how is neomycin used?
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nor oral or parenteral
Sterilize bowel disturb normal bacterial flora |
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toxicity of neomycin
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hypersensitivity reactions
contact dermatitis** bladder irrigation (+polymyxin B) curare-like effect |
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3 sugars joined together
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gentamicin
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gentamicin is the DOC for
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klebsiella
proteus P aeriginosa often combined w/ penicillin + cephalosporin |
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uses of aminoglycosides
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enteric bacteria gram (-)
synergism w/ beta-lactams 1 MASSIVE DOSE CONCENTRATION Dependent kill time-dependent toxicity |
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streptogramins A and B =
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quinupristin
dalfopristin |
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streptogramins bind
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50S ribosomal subunit
close to each other synergistic effect |
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uses for quinupristin+dalfopristin
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Vancomycin resistant enterococcus faeicium
KILLS except faecium kill slowly bacteremia/respiratory tract reserved for serious infections |
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Oxazoladinones
Linozelolid (gram+) |
inhibit protein synthesis
vancomycin-resistant R. faecium multiple resistant organnisms 80% excreted in uring |
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how is Oxazoladinones
Linozelolid (gram+) administered? |
orally
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toxicity of Oxazoladinones
Linozelolid (gram+) |
gi headache rash thrombocytopenia weak inhibitor of monoamine very expensive
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uses of quinolones
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UTI
prostatitis STDs GI and abdominal infections respiratory tract infections Bone, joint, soft tissue infections ANTHRAX |
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toxicities of quinolones
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GI
crystalluria cartilage and joint swelling tendonitis --> tendon rupture |
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what ab makes ROS?
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nitrofuantoin
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CI of nitrofuantoin
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do not use in severe renal insufficiency
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isoniazid pro drug is activated by
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catalase-peroxidase
inhibit carbohydrate metabolism --> accumulate phosphorylated hexoses --> inhibition of glycolysis inhibit synthesis of mycolic acid, component of cell wall increases hydrogen peroxide --> death |
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isoniazid is selective how?
*RESISTANCE DEV RAPIDLY |
1. catalase-peroxidase mut
2-mycolic acid biosynthesis is altered 3-INH Uptake is reduced |
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isoniazid is inactivated by metabolism how?
where? |
acetylation
liver, kidney, bowel mucosa |
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toxicites of isoniazid
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slow-acetylators: pyridoxine deficiency
hepatic toxicity (increased by alcohol) peripheral neuropathy peripheral neuritis |
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therapeutic place of isoniazid
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most important drug in tx of tuberculosis
9 mo prophylatically at least 2 drug to avoid resistance |
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drug regimen for pregnant
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INH
Rifampin Ethambutol |
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clinical significance of slow acetylators
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pyrodoxine deficiency
intermittent tx diphenyhydantoin (toxicity) |
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INH can cause hepatic necrosis especially in kids w/
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rifampin
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MOA of INH
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activated by catalase-peroxidase --> inhibit carbohydrate metabolism
accumulate phosphorylated hexoses --> inhibit glycolysis inhibit synthesis of mycolic acid component of cell wall --> increase hydrogen peroxide --> death |
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MOA of Ethambutol
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not well known
may interfere w/ synthesis of RNA and/or synthesis of mycolic acid |
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uses of ethambutol
|
M. tuberculosis
M. bovis |
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SE of ethambutol
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retrobulbar neuritis
visual function before administration CI in young kids MUST CHECK EYES for blurred vision and color blidness |
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Rifampin
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NOT synthesized
MUST BE ISOLATED Cancer chemotherapy? |
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MOA of rifampin
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inhibit DNA-dependent RNA synthesis by interfering w/ RNA polymerase
mutant beta subunit in resistant cells |
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ethambutol is proven very effective in management of tx failures such as
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atypical mycobacteria
extrapulmonary infections |
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rifampin can possibly be used to tx
|
cancer
active TB meningococcal carrier state TB meningitis inhibit mult of certain viruses: vaccinia, adeno, cowpox, trachoma |
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Pyrazinamide
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convey resistance in 6-8 weeks
no need for hospitalization LIVER DAMAGE - toxicity tolerable for slow duration |
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RIfampin SE
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Flulike symptoms
potent inducer of P450 |
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SE of streptomycin
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ototoxicity
nephrotoxicity |
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SE Of cycloserine
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peripheral neuropathy
**GRAND MAL/PETIT mal seizures depression psychosis headache tremor vertigo confusion visual disturbances |
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what to anti-TB drugs do you give B6 to help with peripheral neuropathy side effect
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isoniazid
cycloserine |
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ethionamide SE
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GI probs
mental depression neurological |
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Aminosalicylic acid (PAS) -rarely used but cannot use in conjunction
SE of |
Rifampin
GI problems, hypersensitivity, compliance INHIBIT COUPLING ENZYMES actetylated to inactivate |
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Dapsone used for
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leprosy
SULFA DRUGS inhibits folic acid synthesis compete w/ PABA |
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combination therapy
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Dapson
Rifampin Clofazimine |
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what drug causes phocomelia?
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thalidomide
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thalidomide is used for
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erythema nodosum lepropsum
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what is the combination therapy for leprosy?
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rifampin decreases infectivity
clofazimine skin discoloration dapsone 2 year long treatment |
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mycobacterium avium complex can be treated w/
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rifabutin
macrolides flouroquinolines amikacin Clofazimine clarythromycin/azithromycin ethambutol rifabutin/clofazimine flouroquinolone ethionamide |
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thalidomide is used for
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erythema nodosum lepropsum
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what is the combination therapy for leprosy?
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rifampin decreases infectivity
clofazimine skin discoloration dapsone 2 year long treatment |
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mycobacterium avium complex can be treated w/
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rifabutin
macrolides flouroquinolines amikacin Clofazimine clarythromycin/azithromycin ethambutol rifabutin/clofazimine flouroquinolone ethionamide |
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isoniazid + rifampin
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hepatotoxicity
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rifampin + oral contraceptives
|
decreases elimination half-life and reduce bioavailability (induce P450)
excreted estrogen progesterone as glucuronide conjugates in bile kill gut flora and prevent steroid reabsoption |
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SE of dapsone
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GI probs
blood dycriasis |
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gammaglobulin MOA
|
unknown
block penetration into cell? may cause anaphylactoid shock (rare) tx: polio, hepA and B rabies measles |
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MOA of Oseltamivir, Zanamivir
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inhibit neuramidinase
causes viral aggregation at cell surface no release of virus |
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Oseltamivir, Zanamivir tx
|
Influenza A and B
|
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tertian malaria
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P. vivax
most common, mild every 2 days |
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malignant malaria
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P. falciparum
severe irregular hypoglycemia, hemolysis, shock --> death |
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quartan malaria
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P. malariae
least common, intermediate paroxysm every 3 days |
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dormant hepatic stage
relapses exoerythrocytic |
P. vivax
P. ovale |
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one cycle of liver invasion
liver infection < 4 weeks only in erythrocytes |
P. malariae
P. falciparum |
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MOA of chloroquine
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blood schizonticide
inhibit DNA synthesis (intercalates) buildup of free heme NOT EFFECTIVE AGAINST LIVER STAGES |
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CI of chloroquine
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Retinal/visual abnormalities
alcoholism neurologic disorders pregnancy? may be safe |
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Toxicities of chloroquine
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cardiac: hypotension arrythmias arrest
G6PDH --> RBC hemolysis ocular: excreted in tears |
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uses of chloroquine
|
suppressive prophylactice
acute attack and cures against falciparum and malariae acute attack but NOT cure for vivax and ovale (both in liver and erythrocyte) |
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aminoquinolone MOA
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inhibit DNA synthesis
buildup of free heme |
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amodiaquine -similar to chloroquine
low cost can replace chloroquine |
serious toxicity is rare
not used chemoprophylaxis serious toxicity is rare used in combo w/ artemisinins agranulocytosis aplastic anemia, hepatic |
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artemisinin
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not used in US
excellent teratogenic in animals |
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mefloquine is given
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orally
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contraindications of mefloquine
|
epilepsy
psychiatric disorders cardiac conditions pregnancy in 1st trimester |
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prophylaxis drug combo
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Mefloquine + chloroquine
|
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what is blackwater fever?
|
intravascular hemolysis
renal failure G6PDH deficiency NADPH decreases |
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what causes blackwater fever?
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quinine = cinchona alkaloid
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what SE of cinchona alkaloid?
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curare-like effects
hypoglycemia ototoxicity mutagenic and teratogenic? ototoxic GI toxicity visual toxicity |
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what is cinchonism?
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ototoxic
GI toxicity visual toxicity |
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Cinchona alkaloid is used esp for
|
severe P.falciparum marlaria
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what drug is the only exo-erythrocytic?
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8-aminoquinolines
PRIMAQUINE |
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wathare the side effects of primaquine?
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hemolytic anemia
methemoglobinemia |
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what is the MOA of primaquine?
|
tissue schizonticide
OXIDANT ETS of parasite binds to DNA terminal prophylaxis after leaving a endemic area |
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what is the radical cure for vivax and ovale?
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primaquine + chloroquine
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what drug causes megaloblastic anemia?
|
primaquine
|
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prodrug chloroguanide -->
|
dihydrotriazine metabolite (active form of drug)
|
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what are the slow acting drugs that can be used for malaria?
|
Sulfones and sulfonamides
inhibit coupling enzyme inhibit dihydropteroate synthetase |
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metronidazole
is a prodrug that must |
accept an electron to form a reactive nitro radical disrupts replication and transcription of DNA
|
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indirect luminal amebicides
|
tetracycline
erythromycin paromomycin |
|
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what is the MOA of indirect luminal amebicides?
|
affect the bacterial flora that support amoeba
|
|
|
direct acting luminal amebicides
|
pamomycine
diiofohydrozyquine (iodoquinol) paromomycin |
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what is the MOA of direct acting luminal amebicides?
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inhibit protein synthesis
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what are tissue amebicides?
|
emetine/dehydroemetine: inhibit protein synthesis
*cardiac toxicity: major prob metronidazole replacing chloroquine: accumulate in liver, toxicities in GI upset, ocular, cardiac, decrease G6PDH psychosis |
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what drugs can be use for trypanosomes?
|
suramin
pentamidine melarsoprol Nifurtimox (Chaga's) |
|
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what is used to tx leishmaniasis?
|
pentamidine
sodium stibugluconate |
|
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what is used to giardiasis?
|
metronidazole
nitaxoxanide |
|
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what does piperazine citrate tx?
SE? |
ascaris and pinworms
SE: seizures |
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what is thiabendazole is used for?
|
TRICHINELLA
strongyloides larva migrans pseudo hookworms |
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what is the DOC Of trichinella?
|
thiabendazole
|
|
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what is albendazole/mebendazole used for?
MOA? |
pinworms, ascaris, hookworm, trichuris, trichinosis
IMPAIRS GLUCOSE UPTAKE |
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what is the MOA of pyrantel pamoate?
|
inhibits NMJ transmission
pinworms ascaris hookworms |
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what is the MOA praziquantel?
|
increase permeability of cell membrane
increase influx of calcium paralysis of helminth |
|
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what drug is used for all 4 species of schistosomiasis?
|
ocular cysticercosis (kill tapeworm larva in eye) --> ocular lesion
GI prob CNS probs |
|
|
pentamidine can be used for
|
P. jiroveci
Leishmaniasis Trypanosomes |
|
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babesiosis
|
quinine + clindamycin
|
|
|
Babesia is a
|
tickborne disease
rare, severe fatal 108 wks elderly immunocompromised |
|
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what are the anti-cestodes?
|
niclosamide: kill scolex
praziquantel: increases cell membrane permeability--> paralysis albendazole - impairs glucose uptake quinacrine - relaxes scolex paromomycin - inhibit protein synthesis |
|
|
what drug kills the scolex
|
niclosamide
|
|
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what drug paralyzes the scolex?
|
quinacrine
|
|
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what is trichomoniasis tx with?
|
metronidazole
|
|
|
ascaris and hookworm infection
use what drug? |
pyrantel pamoate
eggs in fecal material--> ingest--> larvae in intestine --> enter portal blood --> lung-respiratory tract--> reswallowed mature in intestine |
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what do you use to tx toxoplasmosis
|
sulfa
pyrimethamine |
|
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what drugs have to pick 3Ps
|
Idoxuridine
Vidarabine Lamivudine Acyclovir valacyclovir (ester prodrug) ganciclovir ribavirin Viroptic |
|
|
ascaris and hookworm infection
use what drug? |
pyrantel pamoate
eggs in fecal material--> ingest--> larvae in intestine --> enter portal blood --> lung-respiratory tract--> reswallowed mature in intestine |
|
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what is the MOA of idoxuridine?
|
incorporate into viral DNA to inhibit DNA precursors
only used topically |
|
|
what do you use to tx toxoplasmosis
|
sulfa
pyrimethamine |
|
|
what drug causes disulfirm like reaction and metal taste?
|
metronidazole
|
|
|
what drugs have to pick 3Ps
|
Idoxuridine
Vidarabine Lamivudine Acyclovir valacyclovir (ester prodrug) ganciclovir ribavirin Viroptic |
|
|
what are the SE of idoxuridine?
|
local allergic reaction
irritation inflammation itching edema of eyelids photophobia lacrimal duct occlusion prob with healing process VIRUS target RAPID SYNTHESIS OF DNA |
|
|
what is the MOA of idoxuridine?
|
incorporate into viral DNA to inhibit DNA precursors
only used topically |
|
|
why is idoxuridine not used systemically?
|
stomatitis
leukocytopenia thrombocytopenia hepatotoxic carcinogenic teratogenic |
|
|
what drug causes disulfirm like reaction and metal taste?
|
metronidazole
|
|
|
virarabine = adenine arabinoside
|
at low concentrations inhibit virus DNA synthesis
high concentration inhibit host DNA synthesis |
|
|
what are the SE of idoxuridine?
|
local allergic reaction
irritation inflammation itching edema of eyelids photophobia lacrimal duct occlusion prob with healing process VIRUS target RAPID SYNTHESIS OF DNA |
|
|
how does virarabine = arabinoside lose activity?
|
deaminated to hypoxanthine arabinoside
|
|
|
why is idoxuridine not used systemically?
|
stomatitis
leukocytopenia thrombocytopenia hepatotoxic carcinogenic teratogenic |
|
|
how virarabine used?
|
Topically, burning, photophobia, lacrimation may be problems
not used systemically bc neurotox and teratogenic |
|
|
virarabine = adenine arabinoside
|
at low concentrations inhibit virus DNA synthesis
high concentration inhibit host DNA synthesis |
|
|
how does virarabine = arabinoside lose activity?
|
deaminated to hypoxanthine arabinoside
|
|
|
how virarabine used?
|
Topically, burning, photophobia, lacrimation may be problems
not used systemically bc neurotox and teratogenic |
|
|
DNA viruses - what drugs?
|
Acyclovir
Vidarabine Idoxuridine |
|
|
what drug induces > 20 proteins
inhibit virus protein synthesis (translation) inhibits penetration and uncoating, translation, assembly |
intereferon alpha 2a and 2b
|
|
|
what drug do you use for chronic hep B virus?
|
Interferon
Lamivudine |
|
|
what drug do you use for genital warts?
|
Interferons
|
|
|
what are the main uses of interferon?
|
Hep B, C, genital warts
rhinovirus |
|
|
what are the SEs of interferon?
|
influenza-like syndrome
neurotoxic bone-marrow suppression depression/suicide |
|
|
what is the MOA of lamivudine
|
cytidine derivative
decrease HIV RT decrease hep B virus DNA polymerase** |
|
|
MOA of acyclovir
|
inhibit DNA polymerase
cause chain termination when incorporated into viral DNA systemic administration--> phelbitiss, renal dysfunction, CNS agitation, confusion tremors probably not teratogenic |
|
|
what drugs can you use for herpes simplex keratitis
|
acyclovir
viroptic |
|
|
what drugs can you use for genital herpes?
|
acyclovir
valacyclovir |
|
|
what are the uses of acyclovir?
|
herpes simplex keratitis type I
genital herpes oral: decrease new lesions herpes simplex encephalitis for immunocompromised with varicella and herpes zoster |
|
|
what is the moA of ganciclovir?
|
inhibits DNA synthesis
by inhibiting preferentially DNA polymerase |
|
|
what is the SE of ganciclovir?
|
inhibits DNA synthesis
inhibit viral>cell DNA polymerases |
|
|
what is the main use of ganciclovir?
|
CMV retinitis in AIDS PTS
|
|
|
what antiviral gets stuck in the ventilators?
|
ribavirin
*used for severe respiratory infections in kids but also diminishes pulmonary function |
|
|
what is the tx for Hep C?
|
interferon + ribavirin
|
|
|
what is a contraindication of ribavirin?
|
pregnancy
should not conceive for 6 months |
|
|
RIbavirin can be used for what viruses?
|
DNA and RNA
|
|
|
what is the MOA of cidofovir
|
inhibits viral DNA polymerase
|
|
|
what is the SE of cidofovir
|
nephrotoxic
|
|
|
what is the MOA of viroptic?
|
flourinated pyramidine
monophosphate inhibits thymidylated synthetase blocking dUMP-->TUMP incorporated triphosphate into viral DNA |
|
|
what are the drugs that inhibit RNA polymerase?
|
Foscarnet
Ribavirin |
|
|
what is the MOA of foscarnet?
|
binds calcium
inhibits RNA polymerase, RT |
|
|
what is the SE of foscarnet?
|
hypocalcemia, nephrotoxicity
seizures cardiac dysrythmias |
|
|
what is the MOA of viroptic?
|
flourinated pyramidine
monophosphate inhibits thymidylated synthetase blocking dUMP-->TUMP incorporated triphosphate into viral DNA |
|
|
what are the drugs that inhibit RNA polymerase?
|
Foscarnet
Ribavirin |
|
|
what is the MOA of foscarnet?
|
binds calcium
inhibits RNA polymerase, RT |
|
|
what is the SE of foscarnet?
|
hypocalcemia, nephrotoxicity
seizures cardiac dysrythmias |
