Antibiotics Flashcards by Hunter Garrett

Name the DNA topoisomerases (class & names)

Fluoroquinolones => “-oxacin”

Quinolone => nalidixic acid

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Name ABx that damages DNA

metronidazole

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name ABx that disrupts bacterial mRNA synthesis (RNA polymerase)

rifampin

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Which ABx bind to protein synthesis 50S subunit? class & name

Chloramphenicol
Clindamycin
Linezolid

Macrolides=> Azithromycin, Clarithromycin, Erythromycin

Streptogramins=> Quinupristin, Dalfopristin

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Which ABx bind to protein synthesis 30S subunit? class & name

Aminoglycosides=> gentamicin, neomycin, amikacin, tobramycin, streptomycin

Tetracyclines=> tetracycline, doxycycline, minocycline

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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

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What are the two types of cell wall synthesis inhibitors?

Peptidoglycan synthesis

Peptidoglycan cross-linking

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What are the cell wall peptidoglycan synthesis inhibitors?

Glycopeptides=> vancomycin, bacitracin

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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

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Name one individual drug from each class of cephalosporins

1=> cephazolin, cephalexin

2=> Cefoxitin, cefaclor, cefuroxime

3=> ceftriaxone, cefotaxime, ceftazidime

4=> Cefipime

5=> Ceftaroline

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What treats anaerobes above the diaphragm? what treats anaerobes below the diaphragm?

Clindamycin above

Metronidazole below

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What does Metronidazole treat?

GET GAP on the Metro!
Giardia, Entamoeba, Trichomonas
Gardnerella vaginalis, Anaerobes (Bacteroides, C. dif), H. Pylori

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What is the “Triple therapy” against H. pylori?

PPI, metronidazole, clarithromycin

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If M. tuberculosis is suspected in the area of the patient, what can be used for prophylaxis?

Isoniazid

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What is the Tx for M. tuberculosis?

RIPE

Rifampin, Isoniazid, Pyrazinamide, Ethambutol

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What is the prophylaxis of M. avium-intracellulare?

Azithromycine, rifabutin

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What is the Treatment for M. leprae?

Long term treatment w/ dapsone & rifampin for tuberculoid form

Add clofazimine for lepromatous form

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What is a meningococcal prophylaxis agent?

rifamycin=> rifampin, rifabutin

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What can be used as chemoprophylaxis in contacts of children w/ H. flu type B?

Rifamycin=> rifampin, rifabutin

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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

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Why is rifabutin favored over rifampin in HIV patients?

Rifampin ramps up p-450 but rifabutin does not

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Antimicrobial prophylaxis for Endocarditis w/ surgical or dental procedures

penicillins

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Antimicrobial prophylaxis for Gonorrhea

Ceftriaxone

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Antimicrobial prophylaxis for Hx of recurrent UTIs

TMP-SMX

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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"