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antimicrobials, antimicrobal therapy, antifungal/parasito therapy,…
antimicrobials
antimicrobal therapy
cephalosporin
β-lactam, inhibit wall synthesis, less susceptible to penicillinase
Listeria, Atypical(chlamydia, mycoplasma), MRSA, Enterococci are not covered
1st-generation(cefazolin, cephalexin): gram+ cocci, Proteus mirabilis, E.coli, Klebsiella pneumoniae
2nd-generation(cefaclor, cefoxitin, cefuroxime, cefotetan): gram+ cocci, H.influenzae, E.aerogenes, Neisseria spp., Serratia, E.coli, Klebsiella
3rd-generation(ceftriaxone, ceftaxine, cefpodoxime, ceftazidime): gram- resistant to other β-lactam
4th generation(cefepime): gram-
5th generation(ceftaroline): broad, cover Listeria, MRSA, Enterococcus faecalis
adverse: hypersensitivity, AIHA
resistance: inactivated by caphalosporinase, structual change
protein synthesis inhibitors
basic
30S: aminoglycoside, tetracycline
50S: chloramphenicol, clindamycin, erythromycin, linezolid
target ribosome(70S, made of 30S and 50S)
aminoglycoside
gentamicin, neomycin, amikacin, tobramycin, streptomycin
binding 30s of ribosome, require O₂ (ineffective against anaerobic)
severe gram - rod
adverse: nephrotoxicity, neuromuscler blockade, ototoxicity, teratogen
tetracycline
bind to 30S, prevent attachment of aminoacyl-tRNA
tetracycline, doxycycline, minocycline
do not take with milk, antacid, iron-containing preparation
M.pneumoniae, Rickettsia, Chlamydia, MRSA(dexycycline), acne
discoloration of teeth and inhibitation of bone growth in children, contraindicated in pregnancy, doxycycline has no nephrotoxicity
glycylcycline
tigecycline
bind to 30S
macrolide
bind to 23S rRNA of 50S ribosomal subunit
atypical pneumonia, STIs, gram+ cocci
adverse: gastrointestinal motility issues, arrhythmia, acute colestatic hepatitis, rash, eosinophilia
azithromycin, clarithromycin, erythromycin
chloramphenicol
block peptide transfer to 50S
used to treat meningitis, rickettsial disease, toxicity
adverse: anemia, aplastic anemia, gray baby syndrome
clindamycin
block peptide transfer to 50S
oxazolidinone
linezolid
binding to 50S
gram+ including MRSA and VRE
adverse: bone marrow suppression, peripheral neuropathy, serotonin syndrome
polymyxin
multi-drag resistant gram- bacteria
nephrotoxity, neurotoxity, respiratory failure
bind to phospholipid, disrupt cell membrane→leakage of cellular component→cell death
colistin, polymyxinB
Penicilin G,V
prototype β-lactam antibody
bind penicillin-binding protein, block transpeptidase cross-linking of peptidoglycan in cell wall
G: IV or IM; V: oral
used for gram+ organism(S.pneumoniae, S.pyogenes, Actinomyces), gram- cocci(N.meningitis) and spirochetes
β-lactamase sensitive
adverse: coombs+ hemolytic anemia, interstitial nephritis
resistance: β-lactamase, mutation in penicillin-binding protein
核酸合成阻害
PABA+ Pteridine
dihydropteroic acid
dihydrofolic acid
tetrahydrofolic acid
thymidine
DNA
methionine
protein
purines
DNA, RNA
trimethoprim
inhibit dihydrofolate reductase
combination with sulfonamides(TMP-SMX) used for UTIs
adverse: megaloblastic anemia, leukopenia, granulocytopenia
fluoroquinolones(ニューキノロン)
ciprofloxacin, enoxacin, norfloxacin, pfloxacin; respiratory: gemifloxacin, levofloxacin, moxifloxacin
inhibit topoisomerase2, 4
must not be taken with antacids
gram - rod of urinary and GI tract, some gram+, otitis externa
adverse: GI upset, superinfection, skin rash, headache, dizziness, contraindicated in pregnant women, nurshing(授乳中) mothers, and children (damage to cartilage), tendonitis, tendon rupture
dapsone(ジアフェニルスルフォン)
similar to sulfonamide
leprosy, pneumocystis jirovecii prophylaxis
methemoglobinemia
daptomycin
disrupt cell membrane
S.aureus skin infection, bacteremia, endocarditis, VRE
adverse: myopathy, rhabdomyolysis(横紋筋融解症)
sulfonamides
inhibit dihydropteroate synthase; thus inhibit folate synthesis
gram+, -, Nocardia, TMP-SMX for simple UTI
sulfamethoxazole(SMX), sulfisoxazole, sulfadiazine
adverse: hypersensitivity reaction, nephrotoxicity, kernicterus in infant
hemolysis in G&PD deficiency
metronidazole
form toxic free radical metabolite
giardia, entamoeba, trichomonas, gardnerella vaginalis, anaerobe
can be used in place of amoxicillin in H.pylori in case of penicillin allergy
adverse: disulfiram-like reaction(アルデヒド蓄積により悪酔い)
penicillinase-sensitive penicillins
amoxicillin, ampicillin
similar to penicillin, wider spectrum, with clavulanic acid to protect against β-lactamase
H.influenzae, H.pylori, E.coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, Shigella
adverse: hypersensitivity, rash, pseudomembranous colitis
resistance: penicillinase
penicillinase resistant penicillin
dicloxacillin, nafcillin, oxacillin
similar to penicillin, narrow spectrum
S.aureus
adverse: hypersensitive reaction, intestinal nephritis
MRSA has altered penicillin-binding protein site
monobactam
aztreonam
less susceptible to β-lactamase
prevent cell wall synthesis by binding protein 3
gram - only, for penicillin-allergic patient, those wtih renal insufficiency
adverse: nontoxic, GI upset
carbapenem
doripenem, imipenem, meropenem, ertapenem
wide apectrum and significant side effect
limit use to life-threatening
adverse: GI distress, rash, CNS toxicity
vancomycin(グリコペプチド系)
inhibit cell wall synthesis by binding D-Ala-D-Ala portion of cell wall precursors, not susceptible to β-lactamase
gram+, serious, multidrug-resistant drug
adverse: nephrotoxicity, ototoxicity, thrombophlebitis(血栓静脈炎), redman syndrome(diffuse flushing), DRESS syndrome(eosinophilia, systemic symptom)
β-lactamase inhibitor
clavulanic acid, avibactam, sulbactam, tazobactam
antipseudomonal penicillins
antifungal/parasito therapy
antithelminthic therapy
pyrantel pamoate, ivermectin, mebendazole, praziquantel, diethylcarbamazine
antiprotozoal therapy
pyrimethamine (toxoplasmosis); suramin and melarsoprol(trypanosoma brucei); nifurtimox (T. cruzi); sodium stibogluconate (leishmaniasis)
anti-mite/louse therapy
permethrin, malathion, lindane
terbinafine
inhibit fungal enzyme squalene epoxidase
for dermatophytoses(皮膚糸状菌症)
adverse: GI upset, headache, hepatotoxicity, taste disturbance
chloroquine
block detoxication of heme into hemozoin
plasmodial species other than P.falciparum
treat P.falciparum with artemether/lumefantrine and atovaquone/proguanil, if life-threatening, use quinidine
adverse: retinopathy, pruritus
griseofulvin
interfere with microtubule function; disrupt mitosis
oral, inhibit growth of dermatophytes
adverse: teratogenic, carcinogenic, etc
amphotericinB
adverse: fever, hypotension, nephrotoxicity, arrhythmias, anemia, IV plhebitis(静脈炎)
supplement K⁺ and Mg⁺
cryptococcus, blastomyces, coccidioides, candida, mucor
bind ergosterol and form membrane pore
flucytosine
inhibit RNA and DNA synthesis
in combination with amphotericinB
echinocandins
anidulafungin, caspofungin, micafungin
inhibit cell wall synthesis by inhibiting synthesis of β-glucan
for invasive aspergillosis, candida
adverse: GI upset, flushing
azoles
clotrimazole, fluconazole, isaconazole, ketoconazole, miconazole, vericonazole
inhibit fungal sterol synthesis by inhibiting cytochrom P-450
fluconazole to cryptococcal meningitis in AIDS and candidal infection; itraconazole to blastomyces, coccidioides, histoplasma; voriconazole for aspergillus and some candida; isavuconazole for serious aspergillus and mucor
adverse: testosterone synthesis inhibition, liver dysfunction
nystatin
same as amphotericinB, too toxic
oral candida, diaper rash or vaginal candidiasis
prophylaxis
for HIV patient
CD4<100: TMP-SMX: pneumocystis pneumonia and toxoplasmosis
CD4<50: azithromycin, clarithromycin: mycobacterium avium complex
CD4<200: TMP-SMX: pneumocystis pneumonia
pregnant woman carrying group B strep: penicillin G or ampicillin
syphilis: benzathine penicillin G
postsurgical infection of S.aureus: cefazolin
high risk for endocarditis, undergoing surgical or dental procedure: amoxicillin
UTIs: TMP-SMX
gonococcal conjunctivitis: erythromycin
meningococcal infection: ceftriaxone, ciprofloxacin, rifampin
gonorrhea: ceftriaxone
strep pharyngitis(連鎖球菌咽頭炎) in child with prior rheumatic fever: benzathine penicillinG or oral penicillin V
antiviral therapy
avoid in pregnancy
clarithromycin: embryotoxic
tetracycline: discolored teeth, inhibition of bone growth
fluoroquinolones: cartilage damage
ribavirin: teratogenic
amynoglycosides: ototoxicity
griseofulvin: teratogenic
sulfonamides: kernicterus(核黄疸)
chloramphenicol: gray baby syndrome
HIV therapy
3 drugs; 2 NRTIs and an integrase inhibitor
NRTIs
inhibit nucleotid binding to reverse transcriptase
zidovudine is used during pregnancy
adverse: bone marrow suppression, lactic acidosis, anemia, pancreatitis
abacavir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir, zidovudine
highly active antiretoroviral therapy(HAART)
NNRTIs
delavirdine, efavirenz, nevirapine
inhibit reverse transcriptase
rash, hepatotoxicity
protease inhibitor
atazanavir, darunavir, fosamprenavir, indinavir, lopinavir, ritonavir, saquinavir
HIV-1 protease (cleave polypeptide into functional part) inhibitor
hyperglycemia, GI intolerance, lipodystrophy(脂肪異栄養症), nephropathy, hematuria, thrombocytopenia
integrase inhibitor
dolutegravir, elviteravir, raltegravir
inhibit integration
fusion inhibitor
enfuvirtide: bind at gp41, inhibiting entry
bind CCR5 on Tcell or monocyte, inhibiting interaction with gp120
acyclovir/ famciclovir/ valacyclovir
guanosine analog, monophosphorylated by HSV/VZV thymidine kinase→few adverse effect, inhibit DNA polymerase
HSV, VZV, weak activity against EBV
valacyclovir is a prodrug of acyclovir, have better oral bioavailability
adverse: renal failure, neuropathy
ganciclovir
guanosine analog, 5'-monophosphate formed by CMV viral kinase, inhibit viral DNA polymerase
CMV
valganciclovir is a prodrug
adverse: bone marrow supression, renal toxicity
foscarnet
viral DNA/RNA polymerase inhibitor and HIV reverse transcriptase inhibitor
for CMV retinitis (when ganciclovir fails), acyclovir-resistant HSV
adverse: nephrotoxicity, electrocyte abnormalities, seizure
cidofovir
inhibit viral DNA polymerase
CMV, HSV
adverse: nephrotoxicity
oseltamivir/ zanamivir
inhibit influenza neuraminidase→↓release of progeny virus
both influenza A and B
interferon
adverse: flu-like, depression, neutropenia, mopathy
chronic HBV and HCV, Kaposi sarcoma, hairly cell leukemia, condyloma acuminatum, renal cell carcinoma, melanoma, multiple sclerosis, CGD
disinfection and sterilization(殺菌)
autoclave, alcohol, chlorhexidine, chlorine, hydrogen peroxide, iodine and iodophors, quaternary amine
hepatitis C therapy
combination of drugs; ledipasvir(phosphoprotein inhibitor), ribavirin(inhibit synthesis og guanine nucleotide), simeprevir(HCV protease), sofosbuvir(inhibit HCV RNA-dependent RNA polymerase)
antimycobacterial drug
use
M avium-intracellulare(非結核性抗酸菌): azithromycin, rifabutin (prophylaxis); azithromycin or clarithromycin + ethambutol (treatment)
M.leprae: dapsone and rifampin (treatment)
M.tuberculosis: isoniazid (prophylaxis); rifampin, isoniazid, pyrazinamide, ethambutol (treatment)
ethambutol
↓carbohydrate polymerization of cell wall
mycobacterium tuberculosis
adverse: optic neuropathy
streptomycin
inhibit 30S ribosome
mycobacterium tuberculosis(second line)
tinnitus, vertigo(回転性めまい), ataxia, nephrotoxicity
rifamycin
rifampin, rifabutin
inhibit DNA-dependent RNA polymerase
mycobacterium tuberclosis, leprosy
adverse: hepatotoxicity, red orange body fluid
rifabutin favored in HIV infection (less cytochrome P-450 stimulation)
isoniazid
mycobacterium tuberculosis
hepatotoxicity, P-450 inhibition, SLE, acidosis, vitB6 deficiency
↓synthesis of mycolic acid (cell wall element)
pyrazinamide
mycobacterium tuberculosis
to highly resistant bacteria
MRSA: vancomycin, daptomycin, linezolid, tigecycline, ceftaroline, doxycycline
VRE: linezolid, streptogramins(quinupristin, dalfopristin)
multidrug-resistant P aeruginosa, Acinetobacter baumannii: polymyxin B, E