Drugs Inhibiting Nucleic Acid Synthesis - 1

An time 1- abilities substances which inhibit

: cell
growth
•

by competing with ,
or
substituting for ,
a

natural substrate in an
enzymatic process .

As :
Sulfonamides ,
trimethoprim .
pyrimetha mine

Sulfon amides
•
These
drugs bacteriostatic
are
agents and act
by
inhibiting folate synthase competitively .

• Selective
toxicity to bacteria as mammalian cells do
not
synthesize folic acid .
 •

Solubility of sulfonamides decrease in acidic urine

,

which
may
result in
precipitation of drug
causing crystal
luria .

Risk is minimum with soluble

drugs like Sulfisoxazole .

Classification :

Clinical Uses :

Sulfonamides alone are limited in use because of

multiple resistance .

Sulfa salazine vis

prodrug used in ulcerative colitis
•
a

and rheumatoid arthritis .

 Pharmacokinetics :

Sulfonamides are
hepatic ally acetylated
•

Renally excreted metabolites cause

crystal luria
•

High protein binding

•
Kern icterus in Neonates ( Avoid in 3rd trimester )

side Effects :

skin rash due ( most

cis to
hypersensitivity common )

ciii
Hemolysis in GGPD deficiency .

Hematuria
ciii )
Crystal luria &

in Photo
toxicity
( v) Kern icterus in New born .

C
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