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24 Cards in this Set

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Aminoglycosides pharmacokinetics (admin, distrib, elim, protein binding)
Admin - Not absorbed well, IV/IM
Distrib - No CNS penetration
Elim - via kidney unchanged
Protein - Very little binding
Aminoglycosides Mech
Cidal. Bind to 30s ribosomal subunit preventing protein synth. Also cause misreading of mRNA leading to translation of a mutant protein which becomes a pore which disrupts the cell membrane and can cause death.
Aminoglycoside Spectrum
Used for aerobic G- bacilli, staph, and certain mycobacteria. (only aerobic b/c entrance into cell is an active process requireing O2)
Aminoglycoside Resistance
1) Modification of enzymes that inactivate aminoglycosides (major mech). Adenyltransferase, acetyltransferase, phosphotransferase.
2) Altered ribosomal binding site
3) Altered aminoglycoside uptake
Aminoglycosides Side effects
Nephrotoxicity - Major one. accumulation leads to proximal tubular damage of kidneys. Will see dark brown casts in urine.
Ototoxicity - Vestibular and auditory. Irreversible, risk factors include length of therapy, repeated exposre, loop diuretics, increased age, renal probs.
NM blockade, inhibit presynaptic release of Ach and decreased post syn sensitivity.
Streptomycin (class, spectrum, side effects)
Class: Aminoglycoside
Spectrum: Used alone for TB, used with penicillin for strep, enterococci, tularemia, plague, brucellosis
SE: Hypersensitivity, Ototoxicity, less nephrotox than other aminos
Gentamicin (class, spectrum, side effects)
Class: Aminoglycoside, is the workhorse
Spectrum: Aerobic G-, pseudomonas, kelbsiela, Serratia. Strep and pneumococci are resistant.
SE: Ototox is worst. Is also the most nephrotoxic amino,
Tobramycin (class, spectrum, side effects)
Similar to gentamicin but costs more and is better against pseudomonas. Also less toxic.
Kanamycin (class, spectrum, side effects)
Class: Aminoglycoside
Spectrum: No longer used in U.S. Used topically. Used against some G- and pre-surgery.
SE: Oto and nephro, and cause super infection if used to sterilize bowel pre surgery.
Amikacin (class, spectrum, side effects)
Class: aminoglycoside
Spectrum: Broadest spectrum, useful in hospitals, has a resistance to many enzymes which break it down, therefore saved for reserve for real bad cases. Works on pseudomonas.
SE: Oto and nephro with emphasis on auditory.
Neomycin (class, spectrum, side effects)
Class: Aminoglycoside
Spectrum: Broad, good for + and - but to toxic for systemic use; only topical. Used to sterilize bowel pre surgery and for burns, wounds, and ulcers.
SE: Hypersensitivity when topical, severe oto and nephro when taken systemically, superinfection if taken to sterilize bowel.
Tetracycline pharmacokinetics (Admin, Distrib, Elim, protein bound)
Admin: Well absorbed in SI, can be given orally. Absorb impaired by food, divalent cations, dairy, and antacid. Doxo and minocyclin are unaffected.
Distrib: Well, crosses placenta, enters CNS.
Elim: Most are metabolized and excreted by kidneys. Doxycycline almost all feces. Impaired liver function is a contraindication (kidney is fine).
Protein: Is bound to protein.
Tetracycline mech
Static. Binds to 30s subunit inhibiting protein synth. Never given in combo with penicillin b/c is staitc.
Tetracycline Resistance
Plasmid encodes for proteins which interfere with its active uptake and pumps which pump out the antibiotic. Resistance to one is usually resistance to all.
Tetracyclenes Side effects
Never give to children before they have their permanent teeth (or pregnant women) or they will be brown and discolored.
Some have photox.
Hypersensitivity - Can cause pruritis and vaginitis in addition to usual.
GI
Liver
2 main types of tetracyclene super infections
Staph entercolitis and pseudomembranous colitis caused by C. difficile
Tetracyclene Spectrum
Static. Better at treating G-. Can treat G+ cocci First choice for:
Rickettsia
Mycoplasma
Chlamydia
Brucellosis
Cholera
Plague
Lyme disease.
Alternative for:
Clostridium, Leptospira, Actinomyces, resp infections, acne.
Tetracyclenes examples and key side effects
Demecocycline and Minocycline cause phototoxcicity in addition to general SEs. All tetracyclenes end in -cyclene.
Chloramphenicol pharmakokinetics (admin, distrib, elim, protein)
Admin: Can be given orally
Distrib: Enters CNS as well as placenta and breast milk
Elim: Inactivated by glucuronidation and p450 in liver. Counterindicated if hepatic failure. Metabolism can be induced or inhibited.
Protein: Yes, 50% is bound.
Chloramphenicol Mech
Static but cidal to H. influenzae. Binds to 50s subunit preventing protein synth.
Chloramphenicol resistance
Occurs via induction of acetyltransferase which acetylate and inactivates the Ab.
Chloramphenicol Side Effects
Irreversible aplastic anemia - Most important SE. While rare, leads to bone marrow depression and is up to100% fatal (why its not commonly used)
Reversible decreased iron and hemaglobin content
Hypersensitivity
In neonates, can cause gray baby syndrome - grey color, vomiting, feeding probs, rapid resp., cyanosis.
Chloramphenicol Spectrum
Broad bu only usually used if there is a resistance to tetracyclenes:
Meningitis
Typhoid fever
Abscesses
Rocky Mountain
Brucellosis
Chloramphenicol drug interactions
Can inhibit microsomal enzymes which biotransform other drugs. Can also increase the half-life and [] of drugs bound to albumin like warfarin.