Antibiotics Flashcards
Name the DNA topoisomerases (class & names)
Fluoroquinolones => “-oxacin”
Quinolone => nalidixic acid
Name ABx that damages DNA
metronidazole
name ABx that disrupts bacterial mRNA synthesis (RNA polymerase)
rifampin
Which ABx bind to protein synthesis 50S subunit? class & name
Chloramphenicol
Clindamycin
Linezolid
Macrolides=> Azithromycin, Clarithromycin, Erythromycin
Streptogramins=> Quinupristin, Dalfopristin
Which ABx bind to protein synthesis 30S subunit? class & name
Aminoglycosides=> gentamicin, neomycin, amikacin, tobramycin, streptomycin
Tetracyclines=> tetracycline, doxycycline, minocycline
What are the Folic acid synthesis (DNA methylation) inhibitors? What is the difference in them?
Sulfonamides (block PABA to DHF) => Sulfamethoxazole, sulfisoxazole, sulfadiazine
Trimethoprim blocks DHF to THF
What are the two types of cell wall synthesis inhibitors?
Peptidoglycan synthesis
Peptidoglycan cross-linking
What are the cell wall peptidoglycan synthesis inhibitors?
Glycopeptides=> vancomycin, bacitracin
What are the cell wall peptidoglycan cross linking inhibitors?
Penicillinase sensitive penicillins => Pen G, V; Ampicillin, Amoxicillin
Penicillinase-resistant penicillins => oxacillin, nafcillin, dicloxacillin
Antipseudomonals=> ticarcillin, piperacillin
Cephalosporins
Carbapenems=> Imipenem, meropenem, ertrapenem, doripenem
Monobactams => aztreonam
Name one individual drug from each class of cephalosporins
1=> cephazolin, cephalexin
2=> Cefoxitin, cefaclor, cefuroxime
3=> ceftriaxone, cefotaxime, ceftazidime
4=> Cefipime
5=> Ceftaroline
What treats anaerobes above the diaphragm? what treats anaerobes below the diaphragm?
Clindamycin above
Metronidazole below
What does Metronidazole treat?
GET GAP on the Metro!
Giardia, Entamoeba, Trichomonas
Gardnerella vaginalis, Anaerobes (Bacteroides, C. dif), H. Pylori
What is the “Triple therapy” against H. pylori?
PPI, metronidazole, clarithromycin
If M. tuberculosis is suspected in the area of the patient, what can be used for prophylaxis?
Isoniazid
What is the Tx for M. tuberculosis?
RIPE
Rifampin, Isoniazid, Pyrazinamide, Ethambutol
What is the prophylaxis of M. avium-intracellulare?
Azithromycine, rifabutin
What is the Treatment for M. leprae?
Long term treatment w/ dapsone & rifampin for tuberculoid form
Add clofazimine for lepromatous form
What is a meningococcal prophylaxis agent?
rifamycin=> rifampin, rifabutin
What can be used as chemoprophylaxis in contacts of children w/ H. flu type B?
Rifamycin=> rifampin, rifabutin
What are the 4 Rs of Rifampin?
RNA polymerase inhibitor
Ramps up microsomal cytochrome P-450
Red/orange body fluids
Rapid resistance if used alone
Why is rifabutin favored over rifampin in HIV patients?
Rifampin ramps up p-450 but rifabutin does not
Antimicrobial prophylaxis for Endocarditis w/ surgical or dental procedures
penicillins
Antimicrobial prophylaxis for Gonorrhea
Ceftriaxone
Antimicrobial prophylaxis for Hx of recurrent UTIs
TMP-SMX
Antimicrobial prophylaxis for Meningococcal infection
ciprofloxacin (DOC), rifampin for children
Antimicrobial prophylaxis for Pregnant women carrying GBS
Ampicillin
Antimicrobial prophylaxis for prevention of gonococcal or chlamydial conjunctivitis in newborn
erythromycin ointment
Antimicrobial prophylaxis for prevention of post-surg infection due to S. aureus
Cefazolin
Antimicrobial prophylaxis for prophylaxis of strep pharyngitis in child w/ prior rheumatic fever
oral penicillin
Antimicrobial prophylaxis for Syphilis
Benzathine penicillin G
HIV patient with CD4 < 200 cells/mm3 - what is the necessary prophylaxis & what infection is it given for?
TMP-SMX for Pneumocystis pneumonia
HIV patient with CD4 < 100 cells/mm3 - what is the necessary prophylaxis & what infection is it given for?
TMP-SMX for Pneumocystis pneumonia & toxoplasmosis
HIV patient with CD4 < 50 cells/mm3 - what is the necessary prophylaxis & what infection is it given for?
Azithromycin for Mycobacterium avium complex
HIV patients who cannot tolerate TMP-SMX may be given what? what is the risk assoc?
Aerosolized pentamidine but does not prevent toxoplasmosis
What is the Tx for MRSA?
vancomycin, daptomycin, linezolid (can cause serotonin syndrome), tigecycline, ceftaroline
What is Tx for VRE?
linezolid and streptogramins (quinupristin/dalfopristin)
Name the anti fungal that inhibits lanosterol synthesis. Name the enzyme that is blocked
Squalene epoxidase is blocked by
terbinafine
Name the anti fungal that inhibits cell wall synthesis
Echinocandins => caspofungin, micafungin, anidulafungin
Name the anti fungal that forms membrane pores
Polyenes => amphotericin B, nystatin
Name the anti fungal that inhibits nucleic acid synthesis
5-flucytosine
Name the anti fungal that inhibits ergosterol synthesis. Name the enzyme that is blocked
14-alpha-demethylase blocked by
Azoles=> fluconazole, ketoconazole, clotrimazole, miconazole, itraconazole, voriconazole
Tx for toxoplasmosis
pyrimethamine
Tx for Trypanosoma brucei
suramin & melaroprol
Tx for T. cruzi
nifurtimox
Tx for leishmaniasis
sodium stibogluconate
MOA for chloroquine
blocks detoxification of heme into hemozoin so heme accumulates & toxic to plasmodia
Why should chloroquine not be used for P. falciparum?
resistance is too high due to membrane pump that decreases intracellular concentration of drug
Tx for P. falciparum
artemether/lumefantrine or atovaquone/proguanil
For life threatening malaria, what Rx should be used?
quinidine (quinine) in US or artesunate
Toxicity of chloroquine
retinopathy;
pruritis (esp in dark skinned individuals)
What is the mechanism of action for Rx in the Tx of helminths? name the treatments
immobilize
Mebendazole, pyrantel pamoate, ivermectin, diethylcarbamazine, praziquantel
What Rx is for flukes (trematodes) such as Schistosoma?
Praziquantel
For HIV antiviral therapy, what are the primary locations of attack of Rx?
fusion; reverse transcriptase; integrase inhibitors; protease inhibitors (proteolytic processing)
Name the protease inhibitors for HIV retroviral therapy
Lopinavir; Atazanavir; darunavir; fosamprenavir; saquinavir; ritonavir; indinavir
Name the integrase inhibitors for HIV retroviral therapy
raltegravir
Name the fusion inhibitors for HIV retroviral therapy
attachment=> maraviroc
penetration=> enfuvirtide
Name the reverse transcriptase inhibitors for HIV retroviral therapy
NRTI=> Tenofovir, Emtricitabine, abacavir, lamivudine, zidovudine, didanosine, stavudine
NNRTI=> nevirapine, efavirenz, delaviridine
Other than HIV therapy, what are the targets of other antiviral therapy?
Protein synthesis;
Uncoating;
nucleic acid synthesis;
release of progeny virus
Name the Rx responsible for inhibiting protein synthesis via preventing binding of virus. Also name what disease it is used in
Interferon-alpha => HBV, HCV
Name the Rx responsible for blocking uncoating of the virus once inside the cell
Amantadine & Rimantadine => no longer used for influenza due to resistance
Amantadine used in Parkinson’s
Name the Rx responsible for blocking the release of viral progeny & disease assoc
Neuraminidase inhibitors => zanamivir & oseltamivir for Influenza A & B
Name the Rx & enzyme that is blocked to prevent nucleic acid synthesis from occurring. Also name disease
Guanine nucleotide synthesis => ribavirin => RSV, HCV
viral DNA polymerase inhibitors => foscarnet & cidofovir for CMV & HSV (if HSV is acyclovir resistant)
Guanosine analogs => acyclovir for HSV, VZV; ganciclovir for CMV
When should HAART begin?
when patients have AIDS defining illness;
low CD4 cell counts (< 500 cells/mm3);
or high viral load
What makes up the HAART regimen?
Regimen consists of 3 drugs to prevent resistance:
[2 nucleoside reverse transcriptase inhibitors (NRTIs)] +
[1 non-nucleoside reverse transcriptase inhibitor (NNRTI) OR 1 protease inhibitor OR 1
integrase inhibitor]
How are protease inhibitors recognized?
ALL protease inhibitors end in -navir
Which protease inhibitor is assoc with DDI?
Ritonavir
How do protease inhibitors in HIV work?
Block the HIV-1 protease (pol gene) which is responsible for assembly thus preventing maturation of new viruses
What are the toxicities assoc w/ HIV protease inhibitors?
hyperglycemia, GI distress;
lipodystrophy; nephropathy;
Hematuria (indinavir)
What is the MOA for NRTIs?
competitively inhibit nucleotide binding to reverse transcriptase & terminate DNA chain which lacks an OH group
What is the structure of the NRTIs?
All are nucleosides while Tenofovir is a nucleoTide
What is used for general prophylaxis & during pregnancy to decrease risk of fetal transmission? What ADE is specifically assoc w/ this Rx?
zidovudine (ZDV, formerly AZT)
anemia
NRTIs are associated w/ bone marrow suppression. How can this be treated?
reversed w/ G-CSF & erythropoietin
ADE of tenofovir
rash
Common ADE w/ all NRTIs
bone marrow suppression & peripheral neuropathy
Lactic acidosis is an ADE of what NRTIs?
nucleosides
What NRTI is assoc w/ pancreatitis?
didanosine
MOA for NNRTIs & name the Rx
Efavirenz, nevirapine, delaviridine
Bind to reverse transcriptase at different site from NRTIs & do NOT require phosphorylation to be active or compete w/ nucleotides
What ADEs are assoc w/ all NNRTIs?
rash & hepatotoxicity
ADE of efavirenz
vivid dreams & CNS symptoms are common
Which NNRTIs are contraindicated in pregnancy?
Delaviridine & efavirenz
Name the Rx & MOA for integrate inhibitors. What is the assoc ADE?
Raltegravir => inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrate
ADE=> hypercholesterolemia
Name the Rx & MOA for the fusion inhibitors. ADE assoc
Enfuvirtide bind gp41 to inhibit viral entry => skin run at injxn
Maraviroc binds CCR-5 on surface of T cells & monocytes
Name the specific type of interferon used for each of its disease associations
IFN-alpha=> chronic HBV, HCV, Kaposi sarcoma, hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma
IFN-Beta=> MS
IFN-gamma=> chronic granulomatous disease
result of giving sulfonamides in pregnancy
kernicterus
result of giving aminoglycosides in pregnancy
ototoxicity
result of giving fluoroquinolones in pregnancy
cartilage damage
result of giving clarithromycin in pregnancy
embryotoxic
result of giving tetracyclines in pregnancy
discolored teeth, inhibition of bone growth
result of giving ribavirin (antiviral) in pregnancy
teratogenic
result of giving griseofulvin (antifungal) in pregnancy
teratogenic
result of giving chloramphenicol in pregnancy
“gray baby”