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;
56 Cards in this Set
- Front
- Back
What are Sulfonamides used for?
|
antibacterial agent
chemotherapeutic agent cures/ prevents systemic infection: tx for: UTI, PCP, sinusitis, bronchitis, otitis, burns and inflammatory bowel dx. |
|
Sulfonamides are derivatives of _______?
|
PABA (in sunscreen)
|
|
What are the 3 classifications of sulfonamides?
|
1. rapidly absorbed sulfonamindes-- short, intermediate and long acting
2.Poorly absorbed-- active in intestinal lumen 3. Special Uses. |
|
1. rapidly absorbed sulfonamides
What are the 2 short acting drugs? |
short acting- 4-8 hrs
sulfi-sox-azole sulfa-dia-zine |
|
1. rapidly absorbed sulfonamides
What is the 1 intermediate acting drugs? |
intermediate-12-18hrs
Sulfa-methox-azole (Gantanol) |
|
1. rapidly absorbed sulfonamides
Long acting |
Long acting- 7 days
Sulfa-doxine |
|
2. Poorly absorbed--
SULFA-SALA-ZINE Where is it active? What is it converted to? What are the adverse effects? What is it used for? |
sulfa-sala-zine --> 5-amino-salicylate and sulfapyridine in intestinal lumen.
AE: reversible infertility Use: inflammatory bowel and rheumatoid arthritis |
|
What are the 4 derivatives of 5-aminosalicylate?
|
1.Pen-tasa
2. A-sa-col 3. Ol-sal-azine 4.Ro-wasa |
|
Pentasa
Identify release and delivery. |
controlled release
delivered to entire GI and small bowels |
|
Asacol
release and delivery |
Delayed release --> terminal ileum and beyond
used to treat Ulcerative Colitis |
|
Ol-sal-azine
|
prodrug
coupled 5-ASA--> split by intestinal bacteria |
|
Rowasa
use? |
rectal enema and suppositories
used for proctosigmoiditis |
|
3. sulfonamides for Special Uses
Name 3 |
1.Sulfa-cet-amine
2.Mafenide 3.Sliver sulfa-diazine |
|
Sulfa-cet-amide
Use? |
tx of opthalamic infections
ie. trachoma Sulfi-sox-azole- used for topical use in eye |
|
Ma-fen-ide
Use? Side effects? How do you stop the AE? |
tx of BURNS
AE: allergy and pain carbonic anhydrase inhibitor (para-carboxy-benzenen-sulfonamide- CAI) Stop Mafenide by infusing Sodium bicarbonate to prevent acidosis. |
|
Silver Sulfa-dia-zine
Use? AE? |
use: prevent infection of burns and ulcers
AE: rash, itch, allergy |
|
What is the mechanism of action of sulfonamides?
|
BACTERIOSTATIC
COMPETATIVE INHIBITOR of dihydropteroate synthase (needed to incorporate PABA > pteridine>DHFA>DHF> folic acid Sulfonamide is chemically similar to PABA-->incorporated -->dysfn. folic folate Final elimination- cellular and humoral |
|
Describe the Pharmacokinetics of sulfonamides.
absorbed? biotransformed? |
absorbed from GI
biotransformed in liver excreted in urine displaces bilirubin from albumin--> CNS convulsions decrease solubility in acidic urine --> precipitation Can enter CNS, placenta and breast milk (avoid 3rd tri.) Inactivated by acetylation biodegradation can be toxic--> renal failure |
|
7 therapeutic uses for Sulfonamides.
Drug used to treat UNCOMPLICATED UTI, cystitis |
Sulfi-sox-azole + Phena-zo-pyridine (pain relief)
ineffective for pseudomonas infection |
|
DOC in Toxoplasmosis
|
Sulfa-DIA-zine + Pyrimeth-amine +folinic acid(to prevent megaloblastic anemia)
|
|
Used to treat nocardia TRACHOMA and LGV
|
short acting sulfas-
sulfa-SOX-azole sulfa-DIA-ZINE |
|
used to treat UTI, RTI and PCP
combination drugs from UTI? |
Sulfa-METHOX-azole + Tri-METHO-prime (SMZ + TMP)
UTI- add phen-azo-pyridine |
|
prophylaxis in malaria
|
Sulfa-DOXINE + Pyri-meth-amine
|
|
Used for burns and infections
|
silver sulfa-diazine
|
|
Identify 5 adverse effects of sulfonamide.
|
1. hypersensitivity
2.crystalluria 3. acute hemolytic anemia 4. kernicterus 5. displacement/ competiton of drugs |
|
hypersensitivity
|
sensitization to sulfonamide
rash Stevens-Johnson syndrome focal necrosis of liver cross reactivity |
|
cystalluria
|
occurs with low soluable and older sulfamides.
ie. Sulfa-diazine (tx for toxoplasmosis +AIDS) |
|
acute hemolytic anemia
|
seen in pts with G-6-PD
rarely agranulocytosis, aplastic anemia caused by myelotoxic effects |
|
kernicterus (convulsions and seizures)
age? |
neonates and premature babies with immature BBB.
Sulfonamides displace bilirubin from binding sites --> BBB--> brain--> seizures |
|
displacement/competition of drugs
|
sulfonamides complete with METHO-TREX-ATE
Tol-but-amide Warfarin Hydantoin for binding sites and increases plasma levels of these drugs. |
|
Identify the drug interactions with sulfonamide.
|
Meth-en-amine
releases formaldehyde in acid mdeia of urine--> form complex with sulfonamide. |
|
Identify the Bacterial RESISTANCE to sulfonamides.
|
1. lowered affinity/ sensitivity to dihydro-pteronate synthase
2. increased production of PABA 3. decreased permiability --> less intracellular accumulation 4. increased inactivation- rapid acetylation |
|
Fill in the blank:
Trimethoprim is structually similar to ______. It is a weak ____, caught in _____ media --> reaching high [ ] in ____ and _______ fluids. |
similar to folic acid
is a weak base in acid media reach high [ ] in prostatic and vaginal fluids |
|
SMZ + TMP have _____ effect.
How? Method of administration? |
synergistic effects by:
sequential blocade of DHFA and THFA synthesis. Inhibit dihydro-pteroate synthase and dihydro-folate reductase. ORAL ADMINISTRATION |
|
mechanism of action Sulfa-methox-azole trimethoprime
SMX + TMP |
sulfamethoxazole--> (-) DHpteroate synthase--?(-) DHFA
Trimethoprime --> (-) DHFreductase--> (-)THFA leads to impaired DNA synthesis |
|
Identify the spectrum of activity of SMZ + TMP
Effective against... back up drug for... Alternative drug for... |
Effective against E.coli, salmonella, PCP & nocardia
back up drug--> strep, staph, diptheria and kelbsiella alternative drug -->brucellosis (DOC= Doxy + streptomycin) alternative drug --> listeriosis (DOC= ampicillin) |
|
What are the adverse effects of TMP +SMZ?
|
megaloblastic anemia
leucopenia thrombocytopenia mnemonic- TMP- treats marrow poorly Jaundice- allergic chol. hepatitis skin rash, fever, SDJohnson |
|
Mnemoniic for TMP/SMX
T-tree M-Mouth Z-GIT SX- syndrome (AIDS) |
T- tree (respiratory tree)- strep, H influenza, sinitism bronchitis
M- mouth- e.coli, salmonella, shigella --> diarrhea P-Pee- UTI, prostatitis, urethritis S- syndrome- AIDS, PCP, Toxoplasmosis |
|
Name the 5 antimicrobial agents used in UTI.
|
1. Flouroquinolones 4 generations
2. meth-en-amine mandelate 3. SMZ +TMP 4. sulfonamides quinolones |
|
Fluoroquinolones (4 generations)
Generation 1: name drugs spectrum use |
nalidixic acid
norfloxacin used for pathogen of urinary tract narrow spectrum |
|
2nd generation antimicrobials used in UTI
|
cipro-floxacin
o-floxacin- good for gram neg, gonococcal, mycobac, mycoplasma pneumonia |
|
3rd generation
|
lome-floxacin
gati-floxacin spar-floxin good against Gram +, MRSA, enterococci |
|
4th generation
|
moxi-floxacin
trova-flocacin broadest spectrum + against anerobes |
|
Quinolones: mechanism of action
|
inhibits gyrase mediated supercoiling of DNA
post antibiotic effect effective against gram neg, pos, anaerobic infection. used on skin, tissue RTI & GI |
|
What drugs are used to tx PROSTATITIS?
|
Nor-floxacin
Cipro-floxacin O-floxacin |
|
Drugs Tx for STD
|
Cipro-floxacin
O-floxacin Fluoroquintalones- gonoccocal and non-(chlamydia) |
|
PID Tx drugs
|
O-floxacin + Clindamycin
Metronidazole (anaerobes) |
|
name all the therapeutic uses of sulfanimides.
|
prostatitis
STD PID Diarrhea RTI Travelers diarrhea anthrax |
|
identify the locations of quinolone distribution
|
urine
kidney lungs prostate stool bile> CSF>bone |
|
antiacids can cause ______.
Elimination via ___________. _________ ---> Obstruction |
antiacids interfere with adsorption
elimination viw tubular secretion Probenecid --> obstruction --> toxic [ ] in plasma |
|
What causes sulfonamide drug resistance?
|
change in porins
change in reflux pumps decreased accumulation change in sensitivity of enzymes point mutation |
|
Identify the adverse effects of sulfonamides.
|
GI irritation
skin rash PHOTOSENSITIVITY H/Dizzy hallucination/ delirium seizurs arthalgia joint swelling (in kids +Fquinolones) tendinitis Sparfloxacin --> prolonged QT wave Trovafloxacin--> hepatotoxic Fluroquinalones--> increase [plasma] of theophyilline |
|
What is methe-namine mandelate used for?
How? AE? |
Urinary antiseptic activity
by liberating formaldehyde (pH <5.5) NO effect at alkaline pH. AE: gastritis, cystitis,hematuria, frew. peeing |
|
Nitrofurantoin
mechanism excretion use? AE? |
mechanism- reactive intermediates --> damage DNA
Excreted in urine Use- UTI e.coli AE: gastritis, photosensitivity, peripheral neuritis. acute pulm. rxn--> pneumonitis, pulm. fibrosis hemolysis (G6PD), hepatocellular damage, brown urine |
|
Phen-azo-pyridine
use? overdose? combination of drugs? |
used with urinary antiseptics
NO antibacterial agents Urinary analgestic effect- relieve pain red and orange pee overdose--> methemoglobinemia Phenazo-pyridine combined with sulfisoxazole or sulfamethoxazole and sulfadiazine |
|
what are the AE ???
what drugs are involved? |
cross rxn with penicillin
INHIBIT VIT K --> HYPOTHROM ce-fa-man-dole ce-fote-tan ce-fo-perazone hemolytic anemia nephrotixicity |