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Pharm- lecture 11
antibiotics pt 1
33
Pharmacology
Graduate
11/07/2012

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Cards

Term
selective toxicity
Definition

drug's ability to injure target without injuring neighboring cells

Term
disruption of bacterial cell wall
Definition

rigid; high osmotic pressure (action of penicillins, cephalosporin)

Term
bacterial enzyme-inhibition
Definition

PABA of folic acid (action of sulfonamides)

folic acid required by all cells; bacterial synthesis vs. dietary intake

Term
bacterial ribosomal disruption
Definition

protein synthesis function disrupted based on difference in structure (vs mammalian)

Term
bacteriostatic
Definition

inhibits growth of bacteria

Term
bactericidal
Definition

causes death of bacteria

Term
classification of antibiotics
Definition

major classes:

antibacterial, antifungal, antiviral

Term
empiric therapy
Definition

initiation of tx prior to culture results

based on clinical evaluation & knowledge of organism

Term

factors affecting drug chioce, administration or dose

Definition

host defenses

site of infection

age

previous allergic reaction

genetic factors

Term
prophylactic use of antibiotics
Definition

surgery - 1 hr prior & 24 hrs after

bacterial endocarditis (congenital or valvular heart disease; prosthetic valves

neutropenia (high risk for infection

UTI (frequent in women)

influenza - antiviral

Term

penicillin G, V or VK

disrupts cell wall in gram-positive bacteria

Definition

Effects: bactericidal

AE: allergic reactions (0.4-0.7%) reaction, from rash to anaphylaxis; pain at IM site; neurotoxicity in high doses; cross-sensitivity

DD: Pen G & aminoglycoside; given together for synergisitic effect but not in same IV solution - inactivates aminoglycosides

adjust dose for renal impairment

Term

oxacillin (Bactocill)

"penicillinase-resistant penicillins"

cell wall disruption

Definition

altered structure renders drug resistant to inactivation by beta lactamase

Effect: bactericide

AE: minimal (N,D)

Term

amoxicillin (Moxatag)

"broad-spectrum penicillins"

broad-spectrum; cell wall disruption

Definition

ineffective against S. aureus

Effect: bactericide

AE: rash; diarrhea

Term

piperacillin/tazobactam (Zosyn)

"extended-spectrum penicllin"

cell wall distruption

Definition

Use: primarily P. aeruginosa (w/ aminoglycoside) ineffective against S. aureus

Effect: bactericide

AE: ticarcillin (Ticar) - large doses often required: Na overload - edema (CHF); decreased platelet function (promotes bleeding)

Term
penicillins + beta-lactamase inhibitors
Definition

extend spectrum of penicillins

ampicillin + sulbactan (Unasyn)

amoxicillin + clavulanate acid (Augmentin)

ticarcillin + clavulanate acid (Timentin)

piperacillin + tazobactum (Zosyn)

Term
cephalosporins
Definition

weaken bacterial wall

most widely used group of antibiotics

often resistant to beta-lacamases

low toxicity

cross sensitivy to penicillin allergy (1%)

Term

cefazolin (Ancef), cephalexin (Keflex)

"first generation cephalosporin"

cell wall disruption

Definition

Effect: bactericide

AE: allergic reations; thrombophlebitis, disulfram like reaction (N, V w/ ETOH)

Term

cefoxitin (Mefoxin), cefuroxime (Zinacef)

"second generation cephalosporins"

↑ activity against gram-negative bacteria - cell wall disruption; ↑ resistance to beta-lactamases

Definition

Use: ineffective against P. aeruginosa

Effect: bactericide

AE: allergic reations; thrombophlebitis, disulfram like reaction (N, V w/ ETOH)

Term

ceftriaxone (Rocephin)

"third generation cephalosporins"

cell wall disruption

Definition

Use: reach CSF tx meningitis - in adults & children; ineffective against P. aeruginosa

Effect: bactericide

AE: allergic reaction; thrombophlebitis; disulfram like reaction (N, V w. ETOH)

Term

cefepime (Maxipime)

"fourth generation cephalosporins"

cell wall disruption; CSF penetration

Definition

Use: good CNS penetration, P. aeruginosa

Effect: bactericide

AE: allergic reations; thrombophlebitis, disulfram like reaction (N, V w/ ETOH)

Term

imipenem (Primaxin)

"carbapenems"

broadest spectrum; cell wall disruption

Definition

Effect: bactericide

AE: GI (N, V, D); hypersensitivity rash pruritis (itching)' rare - sz; suprainfection (infection on top of infection)(4%)

DD: ↓ valproic acid levels ( ↑ sz threshold)


Term

vancomycin (Vancocin)

disrupts cell wall in gram-positive bacteria

Definition

Route: IV, PO (poor absorption), PR

Use: serious infections only; MRSA & C. Diff; can be used in pts w/ allergy to penicillin

Effect: bactericide

AE: ototoxicity (hearing loss - can be reversed); thrombophelbitis (irritation of vein @ site of IV); red-man syndrome (red skin, itching, hives, tachycardia, hypotension), renal failure

Trough: ~15-20 mcg/mL, less serious infections 10 mcg/mL

Used as last resort; serious infections

blood levels monitored


Term

telavancin (Vibativ)

inhibits cell wall synthesis and binds to cell wall disrupting membrane function

Definition

Use: complicated skin & skin structure infections (MRSA)

AE: taste disturbance, N, V, foamy urine, red-man syndrome, kidney damage (3%), prolong QT interval

DD: others causing renal damage or QT prolongation

Term

fosfomycin (Monural)

cell wall disruption

Definition

Route: PO, single-dose therapy

Use: UTI from e. coli or enterococcus faecalis

Effect: bacteriocide

AE: D, HA

Term

tetracycline (Sumycin), doxycycline (Vibramycin)

broad-spectrum; inhibits protein synthesis in RNA

"bacteriostatic protein synthesis inhibitor (BPSI)"

Definition

Use: rickettsia; Lyme disease

Effect: bacteriostatic

AE: GI; tooth discoloration (avoid in children < 8); suprainfection (C. diff), candida (overgrowth of drug resistant organism); hepatotoxicity; renal toxicity; photosensitivity

DD: give 1 hr before or 2 hr after chelating metal ions (Ca, Fe, Al, Zn, Mg)

↑ bacterial resistance r/t extensive use; avoid in renal pts; D s/s of suprainfection

Term

erythromycin (Ery-tab)

broad spectrum; inhibits protein synthesis in most gram-positive & some gram-negative bacteria

"BPSI"

Definition

Effect: bactreriostatic

AE: GI; QT prolongation & sudden cardiac death, suprainfection, thrombophelbitis, ototoxicity @ high doses

DD: elevates Theo-24, carbamazepine (Tegretol) & warfarin (Coumadin) levels

Term
clarithromycin (Blaxin)
Definition

less N, take w/out regard to meals except extended release (ER) tabs - take w/ meal)

PO, BID dosing

Term
azithromycin (Zithromax)
Definition

take w/ out regard to meals

IV & PO, once daily doing

Term

clindamycin (Cleocin)

inhibits protein synthesis

"BPSI"

Definition

Effect: bacteriostatic

AE: CDAD=C. diff associated diarrhea (bowel suprainfection w/ C. diff - profuse, watery D (mucus & blood)), abd pain, fever, leukocystosis

Term

linezolid (Zyvox)

unlike any other antibiotic

"BPSI"

Definition

Use: "VRE"; nosocomial pneumonia caused by S. Aureus including MRSA

Effect: bacteriostatic

AE: GI - N, D; HA, myelosuppression (suppression of blood cell production in the bone marrow [reversible]); neuropathy (eye(reversible) & peripheral (< 5 months - reversible))

DD: inhibitor of MAOI (risk for severe HTN), SSRI (risk for seratonin syndrome)

Term

gentamycin

narrow-spectrum; alters protein synthesis; bacteriocidal from abnormal proteins

"aminoglycoside"

Definition

Route: IM, IV (do not mix w/ other PCNs in IV solution)

Use: P. aeruginosa

Effect: bactericide

AE: ototoxicity; nephrotoxicity

Dosing: once daily (except in pregnant women & burn pts - need divided doses)

monitoring peak & trough (blood work)

DD: other ototoxic drugs

Term

tobramycin

"aminoglycoside"

Definition

Use: P. aeruginosa

Effect: bactericidal

AE: ototoxic; nephrotoxic, ↑ risk for CDAD

Term

amikacin (Amikin)

broader spectrum against gram-negative bacilli

"aminoglycoside"

Definition

Effect: bactericidal

AE: ototoxic; nephrotoxic

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