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80 Cards in this Set
- Front
- Back
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What are the actions of the class Penicillins?
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Pen G and V (oral)
bind to PBP and inhibit their function (Transpeptidase) cross linking of peptidoglycan |
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What are the uses of the Penincillin G/Vs?
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Bacteriacidal
Gram + organism N. Meningitidis (gram - cocci) , T. Pallidum (spirochetes) |
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What are the Toxicities? Resistance?
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Hypersensitivity rxns, Hemolytic Anemia (IgM, cold Abs)
Penicillinases (beta lactamase) cleaves the beta lactam ring |
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What are the wide spectrum penicillin's?
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Ampicillin and Amoxicillin (better oral bio)
Still penicillinase sensitive combine with clavulanic acid to protect against beta lactamase |
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What is the clinical use of the Extended spectrum Ampicillin and Amoxicillin?
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HELPSS kills enterococci
Haemophilis influenza, E. coli, Listeria, Proteus, Slamonella, Shigella, enterococci |
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Unique toxicity of Ampicillin?
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Pseudomembrane colitis
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What are the Penicillinase-resistant penicillins?
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Oxacillin, Nafcillin, dicloxacillin (DON)
Narrow spectrum due to bulky R group |
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What is the use of the DON penicillins?
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S. Aureus (not MRSA)
use naf for staph |
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What is a unique toxicity of the DON, narrow spectrum, Penicillinase?
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Interstitial nephritis
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What are the Extended spectrum Penicillins? What are they used for?
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Ticarcillin and Piperacillin
treat PSEUDOMONAS + gram - rods use with penicillinase because sensitive |
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What are the Beta lactamase inhibitors?
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Claculanic acid, Sulbactam, Tazobactam
CAST |
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What are the Cephalosporins?
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B lactams, less susceptible to penincillinases
organism not covered are LAME: Listeria, Atypicals (Chlamydia/Mycoplasma), MRSA, Enterococci Ceftaroline covers MRSA |
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What are the first gen Cephalosporins? what do they cover
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Cefazolin and cephalexin
PEcK gram + cocci Proteus E. coli Klebsiella |
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What are the second gen Cephalosporins? what do they cover
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Cefoxitin, cefaclor, cefuroxime
HEN PEcKS Gram + cocci Haemophilus Enterobacter Neisseria Proteus E.coli Klebsiella Serratia |
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What are the third gen Cephalosporins? what do they cover
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Ceftriaxone, cefotaxime, ceftazidime
serious gram - Ceftriaxone-meningitis and gonorrhea (three axes for big balls and bad headache) Ceftazidime- Pseudomonas (dime for mona) |
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What are the fourth gen Cephalosporins? what do they cover
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Cefepime
Better against pseudomonas and gram + |
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What are the 5th gen Cephalosporins? what do they cover
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Ceftaroline
Broad gram + and Gram - MRSA (not pseudomona) |
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What drugs cover Pseudomona so Far?
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Ticarcillin, Piperacillin
Ceftazidime, Cefepime (Pime, Dime for Mona) |
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What are the Toxicities of the Cephalosporins?
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Hypersensitivity
Vit K deficiency- wipe out K producing bacteria Increase the Nephro and Oto toxicity of amingoglycosides |
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What is Aztreonam? what can it be used for?
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Mono bactam, resistant to beta-lactamase (binds PBP3)
Synergistic with amingoglycosides Gram negative aerobic rods only! (like amino glycosides) nontoxic (GI upset) |
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What are the Carbapenems?
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Imipenem, meropenem, ertapenem, doripenem (-enems)
Broad spectrum, lactamase resistant CILASTATIN (inhibitor of renal dehydropeptidase I) to decrease the inactivation of the drug in the renal tubules The kill is LAstin and ciLASTATIN |
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What are the clinical uses of Carbapenems?
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Gram + cocci (Staph, Strep)
Gram - rods Anaerobes ( Anaeobes Cant Breath Air) Meropenum has dec. risk of seizures and is stable against dehydropeptidase I (no need for cilastatin) |
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What are the toxicities Carbapenems?
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limit their use to bad drugs
Skin Rash CNS- cause Seizures GI distress |
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What is Vancomycin?
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Inhibits peptidoglycan by binding to d-ala-d-ala portion cell wall
Gram + only! (serious dudes: MRSA, enterococci, C. diff) |
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What are the toxicities? Resistance?
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NOT trouble free
Nephrotoxic Ototoxic Thrombophlebitis RED MAN SYNDROM (antihistamine and slow infusion rate) Resistance: mod d-ala-d-ala to D-ala-D-LAC |
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What is the mnemonic for the protein synth inhibitors?
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Buy AT 30, CCEL at 50
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Which protein synth. inhibitor is cidal?
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Aminoglycocides (cides for cidal)
Linezolid is variable |
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Where do they all bind?
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Linezolid formation ribosome
Aminoglycocides inhibit initiation complex (A initiates the alphabet) Chloramphenicol inhibits Peptidyl transferase Macrolides/Clindamycin inhibit translocation (macroSLIDES and cleaning mice sweep back and forth) Tetracyclines inhbit tRNA binding (T for T binding) |
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What are the aminoglycocides?
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Mean GNATS caNNOT kill anaerobes
inhibit initiation complex, cause misreadings Require O2 for uptake (thus only aerobes) uses: Gram - rods and are synergistic with Beta lactams Neomycin for bowel surgery |
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What are the toxicities of the aminoglycocides? Resistance
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caNNOT
Nephrotoxic (esp with cephalosporins) Neuromusclar blockade Ototoxic (esp. with loop diuretics) Teratogenic Resistance: acetylation, phosphorylated, adenylated |
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What are the Tetracyclines?
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Tetra, Xocy, mino cycline
static precent attachment of aminoacyl-tRNA limited CNS penetration Doxycycline is fecally eliminated so can be used in renal failure DO NOT take with milk, anacides, or iron containing preps because divalent cations will inhibit absorption (don't add di, and tris together!) |
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What is the use of the Tetracyclines?
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Borrelia burdorferia (Lyme disease)
M. Pneumoniae (mycoplasma) Can accumulate intracellular so good for Chlamydia and Rickettsia Also used to treat Acne |
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What is the Toxicity and Resistance of the cyclines?
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4 T's
Teeth, Tiny Bones, Tan, Teratogenic GI distree Discoloration of the teeth Inhibits bone growth in children (binds to di cations) Photosensitive Teratogenic- CI in pregnancy Resistance: decrease uptake and increased efflux by plasmid encoded transport pumps |
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What are the Macrolides?
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ACE (-omycines)
Azythromycin, Clarithromycin, Erythromycin Static Inhibit translocation (bind to 50s) |
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What are the uses of the Macrolides?
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Atypical Pneumonias (Mycoplasma, Chlamydia, Legionella)
STDs (chlamydia) Gram postive cocci (strep/staph) if allergic to penicillin |
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What are the Toxicities of the MACROlides? Resistance?
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MACRO
GI MOTILITY issues (slows down) Arrythmias (prolongs QT interval) acute Cholestatic hepatitis Rash eOsinophilia increases with serum concentration of Theophyllins and oral anticoagulants Inhibit P450 (A cute gentleman CIPped Iced Grapfruit juice QUIckly And KEpt Munching on a Soft Cinammon Roll) Resistance: Methylate 23s rRNA to prevent binding |
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What is Chloramphenicol?
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Blocks peptidyltransferase at 50s rRNA
static Meningitis (HiB, Neisseria, Strep pneumo), Rocky mountain fever (rickettsia) not really used anymore |
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What is the Toxicity and resistance of Chloramphenicol?
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Anemia
Aplastic Anemia Grey Baby syndrome(lack UDP glucuronyl transferase) Cant Make New Blood Cells Properly REsistance: plasmid encoded acetyl transferase inactivates drug |
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What is Clindamycin?
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Blocks translocation (peptide transfer) at 50s
static Anaerobic infections (bacteriodes, clostridium) in Aspiration pneumonia Lung Abscess and Oral infections also for invasive GAS Treats anaerobes above diaphragm vs. metronidazole below |
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What is the toxicity of CLindamycin?
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Pseudomembrane colitis
Fever Diarrhea |
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How do the Sulfonamides work? What are they used for? Toxicity?
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Inhibit folate synth- para aminobenzoic acid (PABA) antimetabolites inhibit dihydropteroate synthase
CU: gram +/-, Nocardia, Chlamydia UTIS Toxicity: Hypersensitivity Hemolysis in G6PD Nephrotoxic (tubulintersitial nephritis) Photosensitive Kernicterus in infants displace drugs from albumin (increase warfarin effect)q |
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What is Trimethoprim? how is it used? Toxicity?
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Inhibits bacterial DHFR
static TMP-SMX for UTIs Shigella Salmonella PCP propho TOXO propho (TMP: treats marrow poorly) Toxicity: Megaloblastic anemia Leukopenia Granulocytopenia Give supplemental folinic acid |
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What are the fluroquinolones? Use? Toxicity?
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-Floxacins
inhibit DNA gyrase (topoisomerase) cidal don't give with antacids CU: Gram negative rods urinary and GI tracts (pseudomonas), Neisseria, and some gram + Toxicity: the Lones hurt your Bones GI Superinfections Skin Rashes Headache Dizziness Tendonitis, tendon rupture, leg cramps, myalgias Don't give to pregnant women- Damage Cartilage Prolong QT interval |
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What is Metronidazole?
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Free radicals damage DNA
Cidal and antriprotozal GET GAP on the METRO Giardia Entamoeba Trichomonas Gardnerella vaginalis Anaerobes (Bacteroides, c.diff) used with PPI and clarithromycin for H.Pylori Toxicity: Disulfriam like(flushing, tachycardia, hypotension) with alcohol, headache, metal taste |
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How do you treat TB?
MAC? M. Leprae? |
TB: Rifampin, Isonizide, pyrazinamide, Ethambutol (RIPE)
MAC: clarithromycin, ethambutal ML: Dapsone, rifampin, clofazimine |
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What is Isoniazide and what is it used for?
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Dec. the synthesis of mycolic acid (found in TB) but relies on bacterial Catalase-peroxidase for activation (KatG)
CU: TB,only agent used in solo propholaxis too Diff. Half lives depending on slow/fast acetylation by liver |
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What are the toxicities of Isoniazide?
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INH- injures Neurons and Hepatocytes
Dec. the uptake of vitamin B6, pyridoxine (which subsequently can dec. vit. B3) Neurotoxic and hepatotoxic give Pyridoxine to prevent neuro toxicity (B6 involved in the synth of myelin) Can cause a siderblastic anemia too |
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what are the rifamycins? What are their uses?
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Rifampin and Rifabutin
Inhibit DNA-dependent RNA polymerase CU: TB, also in Leprosy and dec. resistance to Dapsone used in propho for neisseria meningitis and HiB |
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What are the toxicities of the rifamycins?
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Hepatotoxic
Increases P450 Red body fluids Rifabutin doesn't increase P450 |
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What are the R's of rifamycin?
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RNA polymerase inhibitor
Ramps up P450 Red/orange fluids Rapid resistance if used alone Rifampin ramps up P450, but rifabutin doesnt |
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What is Pyrazinamide?
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Acidifies intracellular compartments vie conversion to an acid- good for TB which is in the phagolysosome (macros)
CU: TB Toxicity: Hyperuricemia, hepatoxic The Pirate for The Boat, Acid and Gout |
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What is Ethambutol?
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Dec. Carbohydrate polymerization of TB, blocks arabinosyltransferase
CU:TB Toxicity: Optic neuropathy (red/green blind) Bethlaham is in the desert, arabia, and hard to see in the desert |
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How can you treat MRSA?
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Vancomycin, Daptomycin (depolymerizes membrane but can cause myopathy, and inc. CPK, inactivated by plum surfactant), Ceftaroline, linezolid
VRE: Linezolid and streptogramins (quinupristin/dafopristin) |
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What does amphotericin B do?
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Binds to ergosterol (cholesterol found in fungi) and forms pores
CU: serious systemic mycoses Cryptococcus, blasto, histo, coccidoidio, Candida, mucor Intrathecally for fungal meningitis Supplement K and Mg2+ due to altered renal tubular permeability |
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What are the toxicities of Ampho B?
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Fever chills (shake and bake)- infusion run
Hypotension Nephrotoxic- hydration helps, dec. GFR Arrythmias Anemia- dec. epo synth IV phlebitis Ampho the Terrible for kidneys DEc. GFR, dec. Mg/K+, dec. EPO production |
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What is nystastin?
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Similar action to ampho
Swish and swallow for candidiasis or topical for diaper or vaginal |
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What are the Azoles?
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Inhibit ergotEROL (the fungal sterol) by inhibiting the P450 enzyme that converts Lanosterol to ergosterol
CU: local and less serious systemic mycoses Fluconazol for cryptococcal meningitis in AIDS Itrazonazol for Blasto, coccidoides, Histo |
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What are the toxicities?
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Testosterone inhibitors (es. Ketoconazole, used to decrease Test, may cause gynecomastia)
Liver dysfunction (inhibits P450) |
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What is Flucytosine?
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Inhibits DNA and RNA synthesis by converting to 5-FU by cytosine deaminase
CU: systemic fungi (esp. meningitis by cryptococcus) with ampho B Toxicity: Bone marrow supression (inhibits DNA synth..duh) |
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What are the echinocandins?
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the -Fungins
Inhibit cell wall synthesis by inhibiting beta-glucan CU: invasive aspergillosis, Candida Toxicity: Flushing (antihistamine), GI upset |
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What does Terbinafine do?
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Inhibits fungal enzyme squalene epoxidase (nafine for squalene- sound similar)
CU: dermatophytoses (onychomycosis- finger and toes) Toxicity: Hepatotoxic, GI upset, Taste disturbances, Headaches |
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What is Griseofulvin?
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Interferes with microtubule functions, thus inhibiting mitosis (deposits in keratin containing tissues i.e nails)
CU: oral for superficial dermatophytes (tinea, ringworm) Toxicity: Teratogenic (inhibits mitosis), carcinogenic (disrupts DNA synth), increases P-450 and warfarin metabolism, confusion and headaches |
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What are the anti protozoan therapies?
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Pyrimethamine (toxo) suramin and melarsoprol (trypanosoma brucei), nirutimox (T. cruzi), sodium stigloconate (Leishmaniasis)
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What is Chloroquine?
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blocks detox of heme, thus it builds up is is toxic to plasmodia
CU: tx plasmodia except falciparum (pump that dec. [conc], artemether/lumafantrine or atovaquone/proquanil) Lifethreatening use quinidine or quinine |
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What the the toxicities of Chloroquine?
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Retinopathy
Pruritus |
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What are the Antihelminthic drugs?
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Mebendazole, pyrante pamoate, ivermectin, diethylcarbamazine, praziquantel,
immobilize the worms Praqiquantel against flukes (schistosoma) |
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What are Zanamivir and Oseltamivir used for?How do they work?
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-amivir's (amindase viral inhibitors)
Inhibit influenza neuroamindase-> dec. release progeny CU: Flu A/B |
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What is Ribavirin?
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Inhibits synth. quanine nucleotides by comp. inhibiting inosine monophosphate dehydrogenase
CU: RSV, HCV Toxicity: Teratogen!, Hemolytic Anemia quan running in with one ribbon |
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What are Acyclovir, Famciclovir, Valacyclovir used for? how do they act?
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-Clovir (nucleoSides)
Phosphorylated by HSV/VZV thyimidine kinase (need cells to be infected to work, thus few SE) Guanosine analoges Inhibit viral DNA polymerase and chain terminate CU: HSV/VZV, weak against EBV, none against CMV used to genital lesions and encephalitis (daily) Toxicity: Obstructive Crystalline nephropathy and acute renal failure if not hydrated |
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What is Ganciclovir?
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5'monophosphate formed by CMV viral kinase
Guanosine analog Triphosphate formed by cellular kinase and inhibits DNA polymerase CU: CMV Toxicity: Pancytopenia (Leukopenia, neutropenia, Thrombocytopenia) Renal Toxicity more toxic to the host than the other -clovirs (BM) |
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What is Foscarnet?
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ViralDNA polymerase inhibitor
Binds to pyrophosphate-binding of enzyme (does not need activation) Foscarnet (pyroFOSphate) CU: CMV retinitis (when ganciclovir fails) or acyclovir Rest HSV Toxicity: Nephrotoxic, chelates Mg and Ca leading to dec. reabsorption (Low Ca, PTH also inhibited by low Mg levels) |
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What is Cidofovir?
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inhibits viral DNA polymerase, no activation needed
CU: CMV retinitis long T1/2 Toxicity: Nephrotoxic (adm probenecid and IV saline to reduce) |
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HIV therapy, what does HAART mean?
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Highly active retroviral therapy
2 nucleoside reverse transcriptase inhibitors (NRTI) + 1 non-NRTI or protease inhibitor or 1 intregrase inibitor |
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What are the Protease inhibitors?
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-Navir (never tease with a protease inhibitor)
assembly of visions depends on HIV-1 protease (pol gene) to cleave polypeptide HIV mRNA -Prevent the maturation of new viruses Toxicities: Ritonavir (retains no P450) boost other drug concentrations by inhibiting P450 General Tox: Hyperglycemia, GI intolerance (Nausea and diarrhea) Lipodystrophy (cortisol like redistribution) Nephropathy and Hematuria (indinavir) Hyperglycemia Lipodystrophy Nephropathy Hematuria |
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What are the NRTIs?
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Competitively inhibit nucleotide binding to reverse transcriptase and terminate DNA chain (lack 3'-OH)
Tenofovir is a nucleoTide, others are nucleosides (need P before active) ZDV (zidovudine) for propho and pregnant (have you dined (vudine) with my nuclear (nucleoside) family) |
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What are the toxicities of the NRTIs?
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Bone marrow suppression -Reveres with G-CSF and EPO
Peripheral Neuropathy Lactic Acidosis (nuecleosides) Rash (Tenofovir) Anemia (ZDV) Pancreatitis (didanosine) |
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What are the NNRTIs?
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-VIR- DEN
DelaVIRdine EfaVIRenz NeVIRapine Bind to reverse transcriptase at a different site than the NRTIs- do not require phosphorylation to be active |
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What are the Toxicities of the NNRTIs?
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Rash
Hepatotoxic Vivid dreams and CNS symptoms with Efavirenz Delaviridine and efavirenz CI in pregnancy |
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What are the Integrase inhibitors?
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RalTEGRAvir (inTEGRAse)
Inhibits HIV genome integration into host cell by inhibiting HIV integrase Toxicity: Hypercholesterolemia |
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What are the Fusion Inhibitors?
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Enfuvirtide (ENtry/FUshion) binds to gp41 and inhibts viral entry
Maraviroc- binds CCR-5 on T/mono cells, inhibiting interaction with gp120 Toxicity: skin reactions at injection site |
