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92 Cards in this Set

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Cephalexin (Keflex)
Indications: alt to PCN; Gram + cocci; resistant to staph penicillinase
MOA: inhibits cross-linkage of cell wall peptidoglycans
Adverse effects: Cross-sensitivity; hypersensitivity; broader spectrum can lead to opportunistic infections (candidiasis)
Class: 1st gen cephalosporin
Antibiotics
Substances produced by the natural metabolic processes of some bugs that can inhibit or destroy other bugs.
Semisynthetic
Drugs which are chemically modified in the lab after being isolated from natural sources.
Synthetic
The use of chemical rxns to synthesize antimicrobial compounds in the laboratory
Narrow spectrum
Effective against a limited number of bugs
Broad spectrum
Effective against a wide variety of bugs
What are the steps involved in choosing the right drug?
1. ID bug/its sensitivity
2. Be aware of drug interactions/combinations
3. ID site of infection
4. Know the toxicity of the drug
5. Know pt factors
6. Cost
What is imipenem/cilastatin?
A broad spectrum abx
What is MIC?
Minimum inhibitory concentration. This is the lowest concentration that inhibits growth in broth.
What are the pharmacokinetics of the BBB?
Tight junctions prevent passage so drugs often must be administered intrathecally.
What are the pharmacokinetics of the prostate?
It has an acidic environment that favors bases
What do abx do to kidney fxn?
Most abx are excreted by the kidneys; this may allow amino glycosides to reach toxic levels
When is chloramphenicol used?
For life threatening illness because it is very toxic
What are the mechanisms of resistance?
1. DNA mutations or DNA transfer
2. Modification of target
3. Decreased permeability/increased efflux
4. Inactivation of the drug
What are the ways bugs can transfer DNA to one another?
1. Conjugation
2. Transformation
3. Transduction
What are the sites of action of abxs?
1. Cell wall synthesis
2. Metabolism
3. Protein synthesis
4. Nucleic acid synthesis and fxn
Which abxs are inhibitors of cell wall synthesis?
1. B-lactams
2. Vancomycin
Which abxs are inhibitors of protein synthesis?
1. Tetracyclines
2. Aminoglycosides
3. Macrolides
4. Clindamycin
5. Chloramphenicol
Which abxs are inhibitors of metabolism?
1. Sulfas
2. Trimethoprim
Which abxs are inhibitors of nucleic acid synthesis and fxn?
1. Fluoroquinolones
2. Rifampin
PCN
Indications: inf due to: Gram + cocci, Gram + bacilli, Gram - cocci, anaerobes which are B-lactamase negative, spirochetes
MOA: inhibits cross-linkage of cell wall peptidoglycans
Adverse effects: occasional hypersensitivity
Resistance: B-lactamase
Amoxicillin
Indications: sim to PCN but more Gram - organisms; w/clavulanante, extends spectrum to S. aureus; UTI, sinusitis, otitis, lower resp tract infections
MOA: same as PCN
Adverse effects: same as PCN
Resistance: sim to PCN; reduced uptake, altered PBP
Cephalexin (Keflex)
Indications: Alt to PCN; resists staph penicillinase
MOA: same as PCN
Adverse effects: cross-sensitivity w/ PCN, hypersensitivity; opportunistic infections
Class: 1st gen cephalosporin
Cefaclor (Ceclor)
Indications: More Gram -, less Gram +; H. flu
MOA: PCN
Adverse effects: hypersensetivity rxns, renal tox
Info: po, excreted by kidney, inhib aldehyde dehydrogenase
Class: 2nd gen cephalosporin
Cefotaxime (Claforan)
Indications: More Gram +, less Gram -; specific for meningitis
MOA: PCN
SE: hypersensetivity rxns, renal tox
Info: IM, IV, penetrates CNS, inhib aldehyde hydrogenase
Class: 3rd gen cephalosporin
Cefepime (Maxipime)
Indications: meningitis, P. aeruginosa
MOA: PCN; very broad
Adverse effects: inc risk of superinfection; renal toxicity; inhibition of aldehyde dehydrogenase
Class: 4th gen cephalosporin
Carbapenems
Indications: broadest B-lactam; staph (not MRSA), strep, neisseria, klebsiella, haemophilius, proteus, pseudomonas, bacteroides, anaerobes (except c diff)
MOA: imipenem inhibits cell wall synthesis; cilastatin inhibits renal dihydropeptidase I, which prevents imipenem metabolism
Adverse effects: PCN allergy cross reactivity; sz noted w/imipenem
Aztreonam
Indications: aerobic Gram - rods (H. flu, N. gonorrhea, E. coli, Klebseilla, Proteus, Pseudomonas)
MOA: inhibits cell wall synthesis
Adverse effects: low cross allergenicity; Gram + superinfections
Vancomycin
Indications: MRSA
MOA: inhibition of peptidoglycan synthesis
Adverse effects: fever, chills, redman, shock
Resistance: reduced targets
What type of inhibition is bacteriostatic?
Reversible
What type of inhibition is bacteriocidal?
Irreversible
Tetracycline
Indications: broad; effective against intracellular organisms; Mycoplasma pneumonae, Chlamidae, Rickettsiae
MOA: binds to 30s ribosomal subunit, blocking tRNA access, therefore protein synthesis
Adverse Effects: GI, bones, teeth, kidney, liver, photosensitivity
Resistance: Decreased influx, increased efflux, decreased binding to 30s subunit, enzymatic inactivation of drug
Class: tetracycline
Erythromycin
Indications: diptheria, chlamydial inf, CAP
MOA: binds 50s subunit
Adverse Effects: GI, liver
Resistance: reduce uptake, increased efflux, enzymatic hydrolysis of drug, altered 50s subunit
Class: macrolide
Streptomycin
Indications: Gram - enteric bacteria; used w/B-lactams; plague, tularemia; 2nd line for TB
MOA: inhibits protein synthesis
CI: pregnancy
SE: oto & nephrotox, vertigo
Info: IV, IM, doesn't enter CNS, eye or cells, cleared by kidney, used in combo w/β-lactam ab
Resistance: dec influx, inactivation, altered target
Class: aminoglycoside
Ciproflaxcin (Cipro)
Indications: Prostatitis, MRSA, P. aeruginosa, UTI, bacterial diarrhea; Gram - aerobic bacteria, Gram +
MOA: inhibitions of DNA gyrase (inhibits nucleic acid synthesis/fxn)
Adverse Effects: GI, dizziness, HA, insomnia, hepatitis
Resistance: point mutations in DNA gyrase
Class: fluoroquinolone
Rifampin
Indications: TB, meningitis, h. flu; Mycobacteria, Gram+/Gram-
MOA: inhibits DNA dependent RNA polymerase of some Gram +/- TB and N. meningitidis
Adverse Effects: free of toxicity; orange poop; stigmata
Resistance: dec affinity of the polymerase; develops rapidly-use in combination w/ other drugs
Class: semisynthetic macrocyclic
Sulfisoxazole
Indications: UTIs, pneumocystis carinii
MOA: inhibits folate metabolism; PO
Adverse Effects: hypersensitivity, SJS, precipitates in pee
Resistance: utilization of exogenous folate, overproduction of PABA, loss of target affinity
Class: sulfas
How is TB spread?
By airborne droplets from 1-5 microns in size
Why is TB hard to kill w/abx?
-Slow growing
-Possess a fortified cell wall
-Grows within cell
-Very good at developing resistance to single agents
What is the standard combination therapy for TB?
RIPE
1. Rifampin
2. Isoniazid
3. Pyrazinamide
4. Ethambutol
Isoniazid
Indications: TB
MOA: prevents synthesis of mycolic acids; bactericidal for growing cells and bacteriostatic for resting cells
Adverse Effects: allergic rxns, hepatitis, peripheral neruopathy, jaundice, peripheral neuritis
Resistance: aletred mycolic acid synthesis proteins
Class: antimycobacterial
Rifampicin
Indications: TB; prophylaxis against meningcoccus, staph inf
MOA: inhibits DNA dependent RNA polymerase
Adverse Effects:
Resistance: target alteration
Class: rifamycins
Ethambutol
Indications: TB
MOA: inhibits arabinosyl transferases-cell wall synthesis
Adverse Effects: dose dependent diminished visual acuity
Pyrazinamide
Indications: TB
MOA: inhibits FA synthase I gene
Adverse effects: hepatotoxicity, hyperuricemia, gout
-Bactericidal at weak pH, where TB is found in macrophages
What are the considerations for treating fungal diseases?
1. Fungi/human cells have the same size large ribosomal subunit while bacteria have a smaller one
2. Fungi are slower growing and larger than bacteria
3. Locations of infection
4. Toxicity associated w/long term therapy
5. Fungi have a chitinous cell wall w/B-glucans
6. Fungi use ergosterol instead of cholesterol
7. Antimetabolites
What are the types of fungal infections?
Superficial/Subcutaneous
Systemic
What subtypes are associated with systemic infections?
-Exogenous
-Opportunistic
Caspofungin
Indications: oropharyngeal/esophageal candidiasis; invasive aspergillosis
MOA: inhibits B-(1,3)-glucan synthase-inhibits cell wall synthesis
Adverse Effects: HA, fever, phebitis at site; IV only
Amphotericin B
Indications: systemic fungal infections
MOA: binds to ergosterol; increases permeability of cell membrane
Adverse Effects: hypokalemia, acidosis, glomerular damage, renal tubule degeneration, fevers, HA, NVD, anemia, thrombophlebitis
Resistance: occurs w/altered sterols
Nystatin
Indications: tx of candida
MOA: binds to cell membrane sterols
Info: cream, ointment & powder → mucocutaneous, lozenges → oral candidiasis, PO tabs & suspensions → intestinal candidiasis
Clotrimazole (Lotrimin)
Indications: oral, skin, vaginal infxns; topical: dermatophytes, candidiasis, cryptococcus, tinea (not scalp or nails)
MOA: alters cell membrane permeability
Adverse Effects: induction of liver enzymes
Miconazole (Monistat)
Indications: vulvovaginitis
MOA: disrupts cell membrane
Adverse Effects: itching, burning, cramps, HA
Ketoconazole
Indications: dermatophytes, mucosal infections, seborrbeic dermatitis; systemic infections
MOA: disrupts cell membranes
Adverse Effects: N/V
Resistance:
Class:
Fluconazole
Indications: thrush, esophageal/systemic candidiasis, cryptococcal meningitis
MOA: disrupts cell membrane
Adverse Effects: elevated liver enzymes
Resistance: increased efflux through altered demethylase
Class:
Itraconazole
Indications: blastomycosis, histoplasmosis, onychomycosis
MOA: disrupts cell membrane
Voriconazole
Indications: invasive aspergillosis, invasive nonalbicans candidiasis
MOA: disrupts cell membrane
SE: visual disturbances, altered perception of light, chromatopsia, phytophobia, may ↑ hepatic enzymes (transitory but death possible)
Info: po availability 96% vs IV
5-Fluorocytosine
Indications: Candida, Aspergillus, Cryptococcus; prophylaxis w/ AIDS (w/amphotecerine B)
MOA: inhibits DNA/RNA synthesis
Adverse Effects: neutropenia, BMD
Resistance: transport, cytosine deaminase, anabolism
Info: PO, CSF, low protein binding, no metabolism, renal filtration, neutropenia, BMD, combo w/AZT
Griseofulvin
Indications: dermatophytes
MOA: inhibits microtubules; fungicidal/fungistatic
Adverse effects: CYT3A4 induction-reduces wafarin, BCPs
Amantadine
Indications: tx/prevent flu A; parkinson's
MOA: inhibits viral uncoating
Oseltamivir
Indications: flu A/B
MOA: neurominidase
SE:
Acyclovir
Indications: HSV 1/2; chickenpox
MOA: inhibits DNA synthesis
SE: GI and HA, rare nephrotox w/IV; alteration of VTK causes resistance
Ganciclovir
Indications: CMV
MOA: inhibts DNA synthesis
SE: myelosuppresion; MOA same as acyclovir
Zidovudine
Indications: HAART
MOA: NRTI
SE: myelosuppresion
Nevirapine
Indications: HAART; can be prophylactic for delivery
MOA: NNRTI, binds and inhibits HIV-1rtase
SE: SJS (7%)
Ritonavir
Indications: HAART
MOA: protease-inhibitors; inhibits proteolytic cleavage of GAG-POL polyprotein
SE: induces lipodystrophy
Protease Inhibitors
Indications:
MOA: HAART
SE: induces lipodystrophy
Interferons
Indications: HepB, HepC
MOA: suppresses cell proliferation & inhibits viral replication
SE: severe depression, SI/SA, flu-like s/sx
Ribavirin
Indications: RSV, flu, HepC
MOA: selective viral RNA & DNA synthesis
PIs
Indications: HIV
MOA: protease inhibitor; inhibits proteolytic cleavage of gag-pol polyprotein
SE: Induces lipodystrophy; resistance to monotherapy
Choloroquine
Indications: clinical cure (all forms), prophylaxis for sensitive organisms, radical cure (P. falciparum & P. malariae)
SE: rash, puritis, lupus-like syndromes, retinal/corneal toxicity, ototoxicity w/high doses
CI: porphyria, poriasis
Quinine/Quinidine
Indications: malaria-RBC forms; DOC for chloroquine-resistant plasmodia
SE: may increase uterine contractions, hemolysis/hemoglobinuria, skeletal muscle relaxation from mild NM blockade; PO/IV
Mefloquine
Indications: prophylaxis against all chloroquine-resistant P. vivax (RBC forms)
SE: GI upset, myocardium depression, sz, possible teratogen; PO; sleep/behavior disturbances, elicit latent psych issues
Pyrimethamine/Sulfadoxine
Indications: malaria; presumptive tx; mainly RBC form, some effect on sporozites/pre-RBCs, some effect on 2nd tissue forms
SE: sulfa drug
Primiquine
Indications: malaria; exoerythrocyte and gametocytes; radical cure of p.vivax and p. ovale; won't suppress dz once developed; only drug available for tissue/late stage tx
SE: GI upset, HA, dizziness,
Metronidazole
Indications: E. histolytica, G. lamblia, T. vaginalis; anaerobic bacteria: Bacteroides fragilis & Clostridum difficile
SE: GI irritation, metallic taste, reddish urine, disulfiram-like effect (avoid -OH), carcinogenic in animals, rarely: HA, ataxia, seizures, neuropathies, neutropenia, pregnancy- avoid 1st trimester Info:distributes widely (inc CSF), kills amoeba in GI lumen (mixed amebicide), po & parenteral
Paromomycin
Indications: luminal trophozoites & cysts of E. histolytica, T. vaginalis, tapeworm; combo w/metronidazole for ambebiasis or w/o for asymptomatic amebiasis
SE: SE: GI upset- potential for oto and nephrotox w/paren (aminoglycoside AB) Info: poorly abs from GI tract
Sulfatrim
Indications: pneumocytosis, useful for toxicoplasmosis, porphylaxis
SE: rash, pruritis, cytopenias & transaminase elevation
Mebendazole
Indications: roundworm, whipworm, hookworm, pinworm, trichinosis (w/corticosteriod), may work for some tapeworms
MOA: binds to tubulin, interferes w/protein fxn
SE: GI discomfort & diarrhea Info: 10% abs from GI (↓ system tox), caution in preg- may be teratogenic
Pyrantel pamoate
Indications: roundworm, pinworm, hookworm; 2nd DOC for mebendazole
MOA: cholinesterase inhibitor; depolarizing NM blockage in worm
SE: dizziness, HA, drowsiness
Ivermectin
Indications: DoC for filaria infestation & onchocerciasis (O. volvulus -> river blindness), also for threadworm, roundworm & cutaneous larva migrans
MOA: alters Cl- permeability/paralyzes parasite
SE: puritis, tender lymph nodes, fever; CI w/BBB compromise, don't use w/ drugs that act on the GABA receptor
Thiabendazole
Indications: strongyloidiasis (threadworm), useful for larva migrans and effective in trichinosis and visceral larva migrans
MOA: interferes w/microtubule aggregation
SE: anorexia, N/V, diarrhea, pruritus, HA, dizz, visual & neuropsychiatric disturbances, potential for allergic rxns Info: has anti-inflamm properties
Niclosamide
Indications: most tapeworms
MOA: inhbibits anaerobic oxidative phosphorylation
SE: HA, skin rashes, pruritis (antigenic material from worms), loose stools abdominal discomfort Info: single dose = cure, not abs not effective against cysticercosis (use laxatives for T. solium)
Praziquantel
Indications: shistosomes, many cestodes, trematodes, cysticercosis
MOA: increases Ca2+ permeability, causes contractions then paralysis
SE: low tox, N/V, abdominal discomfort from release of dead worm protein Info: well absorbed, good for systemic infections, little effect on human muscle
What causes Pneumocystosis
Pneumocystis carinii (Pneumocystis jiroveci)
What causes Toxoplasmosis
Toxoplasma gondii
What causes Trichomoniasis
Trichomonas vaginalis
What treats E. histolytica?
Flagyl, paromomycin (cysts)
What causes amebiasis?
E. histolytica
What treats toxicoplasmosis?
Sulfatrim, pryimethamine+sulfadiazine (DOC)
What treats giardiasis?
Flagyl
What treats triachomonoasis?
Flagyl
What treats pneumocystosis?
Sulfa-trim (DOC)