SULFONAMIDES

 “sulfa drugs”
 One of the oldest antibacterial agents; when
Penicillin (miracle drug) was initially marketed,
sulfa was not prescribed
 First isolated from a COAL TAR derivative
compound in early 1900; produced for clinical use
against coccal infections in 1935.
 First group of drugs used against bacteria
 Not classified as an antibiotic because they were
not obtained from biologic substances.
 MODE OF ACTION
 Inhibit bacterial synthesis of FOLIC ACID, essential for
bacterial growth, necessary for synthesis of PURINE &
PYRIMIDINES, which are precursors of RNA & DNA
 For cells to grow and reproduce, they require Folic acid;
human cannot synthesize FA but depend on folate from the
diet. Bacteria are impermeable to FA & must synthesize it
inside the cell
 Remain inexpensive & effective against UTI, trachoma, ear
infection, newborn eye prophylaxis
 90% effective against E. coli; useful in treatment of
meningococcal meningitis & against organisms Ch;amydia &
Toxoplasma gondii; not effective against viruses & fungi
 PHARMACOKINETICS
 [A] well absorbed by the GIT;
 [M] liver
 [D] well distributed to body tissues and brain
 [E] urine

 PHARMACODYNAMICS
 Many for ORAL administration
 Also in solution & ointment for ophthalmic use and in
cream form = SILVER SULFADIAZINE (silvadene) and
MAFENIDE ACETATE (Sulfamylon)
 Most – highly protein bound & displaced other drugs by
competing for CHON sites
 2 CLASSIFICATIONS
I. SHORT ACTING:
A. SULFADIAZINE - ORAL AGENT W/ BROAD SPECTRUM USE
- slowly absorbed from GIT, peak 3-6 hr
- poorly soluble in urine, cause crystallization; can damage
kidneys if < H20 intake
B. SULFISOXAZOLE (Gantrisin) – broad spectrum ; recommended
by Centers for Disease Control for treatment of STD
- useful with Sulfadiazine in prophylactic treatment of
streptococcal infection- Rheumatic fever; hypersensitive to Penicillin
- rapidly absorbed from GIT, peak 2 hr
- excreted in urine, t ½ = 4.5 -7.8 hrs
II. INTERMEDIATE
a. SULFAMETHOXAZOLE (Gantanol)
- poorer water solubility than Sulfisoxazole
b. SULFASALAZINE (Azulfidine)
- used to treat ULCERATIVE COLITIS and CROHN’s
disease
- carried by AMINOSALICYLIC ACID (Aspirin)

- rapidly absorbed from GIT, peak levels 2-6 hrs

- Metabolized in the liver
- excreted – urine; t ½ 5-10 hrs
 c. COTRIMOXAZOLE (Septra, Bactrim)
- combination drug of Sulfamethoxazole & trimethoprim
(synergistic effect)
- effective in treating otitis media, bronchitis, UTI and
pneumonitis by Penumocystis Carinii
- DOC : Pneumocystis Carinii Pneumonia (PCP)
- infused over 60-90 minutes; no IM
- [A] rapidly from the GIT; peak 2 hrs
-[M] liver
[E] urine ;t ½ 7-12 hrs

PC :Teratogenic- birth defects - Kernicterus ; distributed into

Breastmilk = diarrhea & rash on infant
 THERAPEUTIC ACTION:
 Competitively block PARA-AMINOBENZOIC ACID(PABA) to prevent
synthesis of Folic acid in susceptible bacteria that synthesize their
own folates for production of DNA & RNA

 ADVERSE EFFECTS/SIDE EFFECTS

 rash, itching
 BLOOD : hemolytic anemia, aplastic anemia, pancytopenia
(prolonged and high dosages)- due to BM depression
 GI : anorexia, N/V {SFF}
 CRYSTALLURIA (crystals in urine); hemturia (sulfonamides are
insoluble in acid urine) {Increase OFI – dilutes the drug}
Adverse effects…
 Photosensitivity {AVOID sunbathing & excess UV
light}
 Cross-sensitivity – with different sulfonamides

 Hepatotoxicity & nephrotoxicity

 Superinfections {frequent oral care, ice chips,

sugarless candy- to relieve discomfort)
 Hypersensitivity reaction = STEVEN’S
JOHNSONS SYNDROME {D/C drug}
 CNS effects : HA, dizziness, vertigo, ataxia,
convulsions, depressions (d/t effect to nerves)
 DRUG INTERACTIONS:
 Increase effects of Warfarin
 Decrease absorption if taken with antacids

 Increase hypoglycemic effect of sulfonylureas

 Decrease effectiveness of contraceptives

 NURSING CARE

 Baseline S. crea, BUN, urine output (should be 1,200 ml/day)

 Increase OFI- 2,000 ml/day or >; administer with full glass of
H20
 Baseline CBC, liver enzymes (AST, ALT, alkaline
phosphatase); monitor for jaundice, icteric sclera
 Monitor VS, check for fever & bleeding
 Observe for hematologic reaction that may lead to life-
threatening anemias; monitor signs of sorethroat, purpura
 Check for signs of superinfections
 Administer 1 hr ac or 2 hrs pc with 1 glass of water
Nursing Care
 Avoid/limit sun exposure, use sunblock
 Use clinistix to monitor urine sugar & ketones in diabetic
patients (not clinitest tab)
 Not to be taken with antacids
 Avoid during last trimester of pregnancy

S unlight sensitivity
U ndesirable effects – RASH, RENAL TOXICITY
L ook for urine output, fever, sore throat &
bleeding
F luids galore
A norexia, anemia
 UNCLASSIFIED ANTIBACTERIAL DRUGS:

 CHLORAMPHENICOL (Chloromycetin)
 Discovered in 1947
 MOA: BACTERIOSTATIC – inhibits bacterial protein
synthesis
 SPECTRUM : BROAD – especially against
ricketssiae, mycoplasma, H. influenzae
 USES: serious infections of SKIN, SOFT TISSUE,
CNS infections – including meningitis, ophthalmic
infections --- when less toxic drugs cannot be used; t
½ = 1.5-4 hrs
 PC : C
 PB – 50-60%
CHLORAMPHENICOL (Chloromycetin)

 SIDE EFFECTS :
 BM depression – blood dyscrasias
 NEURO – confusion, peripheral neuritis, depression

 GRAY SYNDROME – in newborn characterized by :

abdominal distention, vomiting, pallor, cyanosis; NB
may die due to immature liver function.
 NURSING CARE :
 Monitor infection, bleeding
 monitor for anemia, CBC
 monitor LOC
 UNCLASSIFIED ANTIBACTERIAL DRUGS

 SPECTINOMYCIN HYDROCHLORIDE (Trobicin)

 introduced in 1971 against Neisseria gonorrhea (GONORRHEA)
 allergic to PCN, Cephalosporins, Tetracycline
 administered IM single dose – BACTERIOSTATICS
 PC : B; PROTEIN BOUND – 10%; t ½ = 1-3 hrs

 QUINUPRISTIN / DALFOPRISTIN (Synercid)

 Treat VREF – Vancomycin-resistant Enterococcus faecium
bacteremia & skin infected by S. eus & S. pyrogenes
 Disrupts CHON synthesis of the organism
 When administered through peripheral IV line = PAIN, EDEMA &
phlebitis
 SE: N/V, diarrhea, pseudomembranous colitis
Headache, anaphylaxis, elevated AST & ALT
SPECTINOMYCIN HYDROCHLORIDE (Trobicin)
QUINUPRISTIN / DALFOPRISTIN (Synercid)

 NURSING CARE :
 Check for DHN, monitor stools
 Check for patency of IV line; infuse over 1 hr
in D5W
 Check for S/S of anaphylaxis

 Monitor ALT, AST, jaundice, icteric eyes

 Give ice chips, SFF

 PEPTIDES
- derived from cultures of bacillus subtilis
 POLYMYXIN  BACITRACIN
 Interferes with cellular  Inhibits cell wall
membrane synthesis
 Bactiricidal  Bactericidal/
 Affects gram (-) like E. bacteriostatic
coli, P. auruginosa,  Most gram (+), some
klebsiella, shigella gram (-), can treat
 Not absorbed orally meningitis
 IM causes pain  Not absorbed by GIT

 Best given slow IV  Given IM/IV

 SE: dizziness  SE: N/V

 AE: nephrotoxicity/  AE: nephrotoxicity,

neurotoxicity respiratory paralysis,
blood dyscrasia,
anaphylaxis