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111 Cards in this Set

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Telithromycin (Ketolides ) is useful for ______ resistant organisms
macrolide
Streptogramins/Oxazolidinones are ______ inhibitors
Protein synthesis
Dalfopristin + quinupristin
Act synergistically to inhibit ________ function
ribosome
Linezolid (an oxazolidinone)
Inhibit protein synthesis by interfering with _______
translation
Linezolid effective against what?
anerobic gram positive organisms
Linezolid: Approved for ________-resistant infections
vancomycin
Why Linezolid should not be used with what mood drugs?
Also has MAOI activity
Chloramphenicol is good for what bugs?
Broad spectrum antibiotic effective against most anerobic and aerobic organisms except Pseudomonas aeruginosa
When do you use Chloramphenicol?
Reserved for life threatening infections due to serious adverse effects

Orally absorbed
Penetrates CSF
Bad things about Chloramphenicol
Dose related bone marrow depression
Dose related reversible anemia
Idiosyncratic aplastic anemia (usually fatal)
Grey baby syndrome
Grey baby syndrome?
Infants have a decreased ability to conjugate chloramphenicol
High levels of drug accumulate in blood
Symptoms: abdominal distention, vomiting, cyanosis, hypothermia, decreased respiration, vasomotor collapse
Lincosamides (2)
Clindamycin and lincomycin
Lincosamides Activity similar to ____
erythromycin
Lincosamides Effective against ______
anerobes



(Penetrates most tissues including bone)
Bad things about Lincosamides
Pseudomembranous colitis can occur because Clostridium difficile is resistant to clindamycin
Folate Antagonists (8)
Sulfamethoxazole
Trimethoprim
Cotrimoxazole
Sulfacetamide
Sulfadiazine
Sulfapyridine
Sulfasalazine
sulfisoxazole
Bacteria cannot absorb folic acid
Synthesize it from ______
PABA (parabenzoic acid), pteridine, and glutamate
Humans cannot synthesize folic acid- must take in through _____
diet (vitamin)
________ are structurally similar to PABA

Block the incorporation of PABA into dihyropteroic acid
Sulfonamides
________ prevents reduction of dihydrofolate to tetrahydrofolate (inhibits dihydrofolate reductase)
Enzyme is present in humans but drug has lower affinity for human enzyme
Trimethoprim
Sulfamethoxazole is most commonly combined with trimethoprim due to matching ________
half lives
spectrum of TMP-SMX
Broad spectrum
Clinical situations to use Folate antagonists
Used for UTIs, Pneumocystis carinii pneumonitis
Quinolones (11)
Ciprofloxacin
Enoxacin
Levofloxacin
Norfloxacin
Ofloxacin
Sparfloxacin
Trovafloxacin
Gatifloxacin
Gemifloxacin
Lomefloxacin
Moxifloxacin
Interesting side effect of Quinolones
tendon rupture
Quinolones Primarily used to treat ____
UTIs
Quinolones Inhibit NA synthesis by inhibiting __________ which is the bacterial enzyme responsible for unwinding and supercoiling DNA
DNA gyrase
Only class of antimicrobials that inhibits DNA replication
Quinolones
Spectrum of quinolones
Broad spectrum
Newer quinolones are good for what conditions?
UTIs, lower respiratory tract infections, bone and joint infections, prostatitis

Some effective against Pseudomonas aeruginosa
Some orally active
What's this?

Prodrug
In acidic pH, hydrolyzed to ammonia and formaldehyde
Formaldehyde is bactericidal
Methenamine
______ responsible for both tuberculosis and leprosy is slow growing - requires long term therapy
Mycobacteria
Simple comment on slow growing bug therapy
Need combination therapy
Antituberculosis/Antileprosy Drugs
First line agents (5)
Isoniazid
Pyrazinamide
Rifampin
Ethambutol
Streptomycin
Antituberculosis/Antileprosy Drugs
Second line agents (9)
Aminosalicyclic acid
Capreomycin
Cycloserine
Ethionamide
Kanamycin
Quinolones
Rifabutin
Viomycin
Rifapentine
Isonazid Inhibits the synthesis of _______which are constituents of the mycobacterial cell envelope -unique in mycobacteria
mycolic acids
What is the Polymorphism for isoniazid ?
Fast and slow acetylators
Bad things about isoniazid
Hepatic dysfunction
Peripheral neuropathy due to pyridoxine deficiency
How do you overcome Peripheral neuropathy during isoniazid treatment?
coadministration of pyridoxine
Drug of choice for chemoprophylaxis in recent convertors
isoniazid
What is a recent convertor?
Patient has a negative TB test in the past but the test is positive 1 yr later patient is referred to as a recent convertor
What is treatment for recent convertors?
Recommendation that person should be placed on isoniazid for 6-12 months as long as there is no evidence of clinical disease (ie positive chest x-ray)
What drug is this?

Inhibits RNA synthesis
Binds to the ß subunit of DNA-dependent RNA polymerase forming an inactive complex
Rifampin
Riampin
Resistance occurs due to single step mutation that alters the ______
ß subunit
What is Rifampin used to treat?
Effective against tuberculosis and some gram positive and negative pathogens
Bad thing about Rifampin
Deacetylated to an active metabolite
Induces cytochrome P450 enzymes
Increased metabolism of other drugs
Can cause a drug-induced hepatitis
Can color secretions (urine, saliva, feces, sweat, tears)red-orange
Can result in discoloration of contact lenses
analog of rifampin that is active against some strains of resistant mycobacterium tuberculosis
Rifabutin
Pyrazinamide mechanism of action
unknown
Pyrazinamide is used to treat what?
Only effective against Mycobacterium tuberculosis - particularly effective against intracellular organisms
Bad things about pyrazinamide?
Hyperuricemia occurs in all patients but clinical gout is rare
Hepatotoxicity
Ethambutol mechanism of action?
unknown
Bad things about ethambutol
Least potent of first line drugs
Can cause optic neuritis
Loss of central vision
Impaired red-green discrimination
Hyperuricemia that can result in gout
Dapsone is Mainly used in the treatment of _____
leprosy
Dapsone is a Structural analog of _____
PABA


-->Competitive inhibitor of folic acid synthesis
Fungal infections
Many occur ________
in poorly vascularized or avascular tissues (nails, hair, superficial layer of skin)
Fungal drugs Can be classified by activity: what are they (2)?
Systemic (disseminated balstomycosis, coccidiodomycosis)
Superficial (dermatophytes of skin, hair and nails
MOA classifications of Fungal drugs
Azoles
Polyenes
Others
Polyenes (2)
Amphotericin B
Nystatin
MOA of polyenes
MOA: Binds ergosterol (principal fungal membrane sterol) which disrupts membrane and results in loss of electrolytes from cell
polyenes Commonly used to treat disseminated yeast and fungal infections in _____ patients
immunosuppressed
Nystatin used for topical treatment of ______(too toxic for systemic use)
Candida albicans
How do you give ampho B?
Amphotericin B is not absorbed orally - must be given iv or topically
Bad things about polyenes
Nephrotoxicity

With initial dose, fever, chills and tachypnea often occur
WIth polyenes, Need to keep patient well hydrated to reduce _______
nephrotoxicity
Azole Antifungals
Imidazoles
Topical (5)
Butoconazole
Clotrimazole
Econazole
Oxiconazole
Sulconazole
Azole Antifungals
Imidazoles
Topical and systemic (2)
Ketoconazole
Miconazole
Azole Antifungals
Triazoles
Systemic (4)
Fluconazole
Itraconazole
Voriconazole
Terconazole
Main problem with azole antifungals (put it in you head)
drug interactions
Azole Antifungals
Inhibit synthesis of ergosterol by inhibiting ______
14-alpha demethylase
Advantages of triazoles vs imidazoles
Fewer side effects
Better drug distribution
Fewer drug interactions
Other Antifungals (5)
Caspofungin
Flucytosine
Griseofulvin
Terbinafine
Tolnaftate
Caspofungin
IV antifungal agent
Indicated for treatment of invasive _____
aspergillosis and candidiasis
Caspofungin Noncompetitively inhibits the synthesis of ß-(1,3)-D-glucan, a major component of ______
fungal cell walls
Terbinafine Administered orally for treatment of superficial fungal infections
Terbinafine and tolnaftate inhibit squalene epoxidase - squalene accumulates inside the fungal cell
Terbinafine is effective against ______fungi
nail and hair
Griseofulvin Binds to ____- in keratin precursor cells which then become resistant to fungal infections
keratin
Dermatophyte infection can only be cured when infected cells are replaced by keratin containing _________
griseofulvin
Antiprotozoal Drugs (15)
Metronidazole
Dehydroemetine
Eflornithine
Emetine
Iodoquinol
Melarsoprol
Nifurtimox
Pentamidine
Quinacrine
Sodium stibogluconate
Suramin
Atovaquone
Meglumine antimonate
Benznidazole
Nitrazoxamide
One of most effective drugs against anerobic bacteria and protozoans
Penetrates protozoal and bacterial cell walls - cannot enter mammalian cells
Metronidazole
Metronidazole Must be activated in the cell
_____- activates the drug
Nitroreductase
Reduced metronidazole inhibits DNA replication by causing breaks and inhibiting _____
repair
Ferredoxin?
reduces metronidazole
Metronidazole
Effective in the treatment of
what?
Vaginal trichomoniasis
Giardiasis
Amebiasis
Bad things about metronidazole
Nausea, vomiting, diarrhea
Turns urine dark or red-brown
Metallic taste
Disulfiram-like reaction when taken with alcohol
Abdominal cramping, vomiting, flushing, headache
Antimalerial Drugs (7)
Chloroquine
Primaquine
Quinine
Doxycycline
Hydroxychloroquine
Mefloquine
Pyrimethamine
Maleria caused by protozoan (____)
Some strains fo Plasmodia can persist in liver resulting in relapse
plasmodium
_______ is considered drug of choice for Maleria
Chloroquine
________ is effective against liver forms of maleria - often used for prophylaxis or prevention of relapse
Primaquine
________ used for prophylaxis for travelers entering areas where chloroquine sensitive maleria is present
Chloroquine
Bad thing about long term chloroquine use
Can become concentrated in melanin containing structures leading to corneal deposits and blindness
Bad thing about Primaquine
can cause hemolytic anemia in glucose-6-dehydrogenase deficient patients
Bad thing about quinine
Cinchonism:
Sweating, tinnitis, impaired hearing, blurred vision, nausea, vomiting , diarrhea
Types of worms
Cestodes (flatworms, tapeworms)
Trematodes (flukes)
Nematodes (whip, pin, hook)
Cestodes remain in ______ - treatment confined to ______
intestine
Trematodes move through ______ - treatment must be systemic
blood and tissues
Treatment of Cestodes/Trematodes
drug of choice
Praziquantel
what eats pinworm eggs?
roaches
Good choice of drug to treat systemically
Praziquantel is absorbed orally and therefore can have a systemic effect
Treatment of Nematodes
Albendazole
Mebendazole
Pyrantel
Given orally with little systemic absorption for nematode treatment
Albendazole and mebendazole
treatment of nematodes that paralyzes the worms
Pyrantel
Anti-HIV Drugs: Reverse transcriptase inhibitors (13)
Abacavir
Didanosine
Lamvudine
Stavudine
Zalcitabine
Zidovudine
Amprenavir
Delavirdine
Efavirenz
Nevirapine
Emtricitabine
Adefovir
Tenofovir
Anti-HIV Drugs Inhibit formation of viral DNA from RNA by ____
reverse transcriptase
Nucleoside analogs related to thymidine and adenosine - get incorporated into viral DNA and terminate ______
DNA elongation
Reverse transcriptase enzyme mutates rapidly - how do we delay emergence of resistance?
Use of 2 or more reverse transcriptase inhibitors delays emergence of resistance
Interferes with processing of viral protein and prevents formation of new viral products
Protease Inhibitors
Bad things about Protease Inhibitors
Metabolic abnormalities
Changes in fat deposition
Anti-HIV Drugs: Protease inhibitors
Ampenavir
Indinavir
Nelfinavir
Ritonavir
Saquinavir
Atasanavir
Lopinavir
Fosamprenavir
Anti-HIV Drugs: Fusion Inhibitor (1)
Enfivirtide
Anti-Influenza Drugs: Most are ________ inhibitors which block release of virus from infected cells
neuraminidase
Anti-Influenza Drugs:
If used within _____ hrs of onset of illness, duration of illness is shortened by one half
48
Anti-Influenza Drugs (4)
Amantadine
Rimantadine
Oseltamivir
Zanamivir