Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
59 Cards in this Set
- Front
- Back
|
Sulfonamides - history
|
azide dyes found to be antibiotic
split to active sulfanilamide and toxic metabolite (para-di and tri amines) |
|
|
Sulfonamides - static or cidal
|
static (competitive inhibitors)
|
|
|
Sulfonamides - target/MOA
|
competitive inhibitor of folate synthetase
may also be incorporated structural analog of PABA (substrate) |
|
|
Sulfonamides - selectivity
|
humans do not make folate
|
|
|
Sulfonamides - SAR - N4
|
must be free amine or amine with an easily removed group
mimics PABA |
|
|
Sulfonamides - SAR - N1
|
can only be monosubstituted to act as Bronsted acid
- pKa of 6.0-7.4 - ionized form mimics PABA - unionized penetrates membranes R group is an aromatic heterocycle |
|
|
Sulfonamides - SAR - SO2-NH
|
essential
mimics COOH on PABA |
|
|
Sulfonamides - spectrum
|
G+ and G- bacteria
|
|
|
Sulfonamides - absorption
|
well absorbed from stomach and SI
|
|
|
Sulfonamides - elimination
|
renal
|
|
|
Sulfonamides - drugs
|
Sulfisoxazole
Sulfamethoxazole Iclaprim Sulfasalazine Olsalazine Topical - sulfacetamide - silver sulfadiazine |
|
|
Sulfonamides - side effects
|
hypersensitivity
- rash most common - Stevens-Johnson syndrome (rare) - anaphylaxis hematological - G6PD deficiency, often in AA's - hemolytic anemia - 65% change of recurring (CI) kernicterus renal damage - crystallization - drink lots of water |
|
|
Sulfonamides - mechanisms of resistance
|
resistance is common
test for susceptibility before using as monotherapy change target (alter folate synthetase) (most common) enzymatic inactivation (acetylation) circumvent block (folate and nucleic acids from outside, puss) overcome block (more PABA) |
|
|
Sulfisoxazole - drug products
|
Sulfisoxazole - DC'd
Sulfisoxazole Acetyl - pediatric, still used Pediazole = Acetylsulf + erythromycin - for otitis media |
|
|
Sulfamethoxazole v. Sulfisoxazole
|
slower abs/excretion
more N acetylation leads to more crystallization |
|
|
Trimethoprim - target/MOA
|
inhibitor of dihydrofolate reductase
|
|
|
Trimethoprim - spectrum
|
G+ and G- aerobes
not MRSA or Pseudomonas |
|
|
Trimethoprim - side effects
|
well-tolerated
GI (NVD) Hematologic (same as sulfa drugs) |
|
|
Cotrimoxazole - drugs
|
trimethoprim
sulfamethoxazole Bactrim |
|
|
Cotrimoxazole - spectrum
|
G+ aerobes
- includes MRSA G- aerobes Chlamydia Nocardia PCP B. cepacia (DOC) S. maltophilia (DOC) |
|
|
Cotrimoxazole - absorption
|
well-absorbed
not influenced by food |
|
|
Cotrimoxazole - penetration
|
large Vd
penetrates into CSF (meningitis) |
|
|
Cotrimoxazole - elimination
|
renally excreted
adjust dosage for dysfunction |
|
|
Cotrimoxazole - uses
|
primary uses
- skin and soft-tissue - PCP UTI and prostititis URTI and LRTI (G- resistance issues) Secondary uses - GI infections - meningitis - osteomyelitis - nocardia infections - bacteremia |
|
|
Cotrimoxazole - side effects
|
GI (mild)
hyper sensitivity - skin reactions like sulfa - mucher higher in HIV hematologic (most serious) renal (crystallization) drug fever |
|
|
Cotrimoxazole - dosing
|
BASED ON TRIMETHOPRIM COMPONENT
UTI - 5 mg/kg/day of TMP - 1 DS bid Systemic - 8-10 mg/kg/day - 2 DS bid PCP - 12-20 mg/kg/day - 2 DS qid to tid half for CrCl 15-30 ml/min |
|
|
Nitrofurantoin - drug names
|
Macrobid
Macrodantin |
|
|
Nitrofurantoin - uses
|
only for UTIs
can be used in pregnancy |
|
|
Nitrofurantoin - spectrum
|
E. coli
Entercoccus S. saprophyticus NOT ACTIVE AGAINST: - Kleb - Pseudo - Acineto |
|
|
Nitrofurantoin - absorption/distribution
|
well-absorbed
large Vd does not distribute to tissues well |
|
|
Nitrofurantoin - elimination
|
renally excreted
|
|
|
Nitrofurantoin - side effects
|
GI (take with food to limit)
Hypersensitivity CNS - HA - dizziness - confusion Peripheral neuritis Pulmonary toxicity - acute is reversible - chronic is irreversible (very rare) Hematologic - hemolytic anemia in G6PD pts |
|
|
Fosfomycin - static or cidal
|
cidal
|
|
|
Fosfomycin - spectrum
|
Enterobacteriaceae
P. aeruginosa Staphylococci Entercoccus including VRE (broader than Nitrofurantoin) |
|
|
Fosfomycin - absorption
|
food impairs absorption
|
|
|
Fosfomycin - elimination
|
excreted unchanged in urine
|
|
|
Fosfomycin - adverse events
|
GI (diarrhea, nausea)
HA dizziness vaginitis dyspepsia |
|
|
Fosfomycin - uses/dosing
|
UTIs only (broader spectrum than nitrofurantoin)
3 g X 1 dose |
|
|
Isoniazid - static or cidal
|
cidal against growing organisms
static against nonreplicating organisms |
|
|
Isoniazid - spectrum
|
Mycobacterium tuberculosis
Mycobacterium kansasii |
|
|
Isoniazid - resistance
|
develops rapidly
use in combination |
|
|
Isoniazid - absorption/distribution
|
well absorbed
food decreases absorption well distributed penetrates CSF |
|
|
Isoniazid - elimination
|
metabolized (rapid and slow aceylation)
|
|
|
Isoniazid - side effects
|
Neurotoxicity
- peripheral neuropathy (reversible) - give 10 mg pyridoxine for every 100 mg of INH Hepatotoxicity - age related (>35 yo) - results in hepatitis - chronic EtOH intake - pre-existing disease - taking other hepatotoxic drugs |
|
|
Pyrazinamide - spectrum/use
|
M. tuberculosis
|
|
|
Pyrazinamide - resistance
|
happens rapidly if monotherapy
|
|
|
Pyrazinamide - dosing
|
20-35 mg/kg/day
(500 mg tablets) |
|
|
Pyrazinamide - absorption/distribution
|
well absorbed
widely distributed crosses BBB |
|
|
Pyrazinamide - side effects
|
GI (most common)
hepatotoxicity interstitial nephritis |
|
|
Ethambutol - static or cidal
|
static
|
|
|
Ethambutol - spectrum
|
M. tuberculosis
|
|
|
Ethambutol - absorption/distribution
|
well absorbed
well distributed crosses BBB |
|
|
Ethambutol - elimination
|
renally excreted
|
|
|
Ethambutol - dosing
|
15-25 mg/kg/day
(100 and 400 mg tablets) |
|
|
Ethambutol - side effects
|
neuropathy (most common)
- red-green vision defect - dose related - visual acuity and color perception testing at 4-6 weeks |
|
|
Iclaprim - Dr. Davis
|
serious G+ infections
- MRSA - VRSA - macrolide/quinolone/TMP-resistant Skin and soft tissue infections |
|
|
Olsalazine and sulfasalazine - Dr. Davis
|
used for ulcerative colitis
cleaved at -N=N- becomes 5-aminosalacylic acid (antiinflammatory) |
|
|
Sulfacetamide - Dr. Davis
|
N-acetyl group removed in vivo
opthalmics |
|
|
Silver sulfadiazine - Dr. Davis
|
antibacterial and antifungal
burns (prophylaxis) |
