pharmacology

1. Sulphonamides

2. Sulphonamides:
INTRODUCTION:
The sulfonamides are broad spectrum anti microbial agents that inhabit the growth
of gram positive and gram negative bacteria.
Widely used due to high efficacy and low cast
Synthetic
Derived from sulfanilamide by substituting amino group in their structure
Pharmacokinetics
Sodium salt
IV
Metabolized by liver
Excreted by kidneys
Good CSF penetration
Alone bacteriostatic
Combination bactericidal

3. CLASSIFICATION OF
SULPHONAMIDES

4. Septran: Sulfamethoxazole + Trimethoprim
5 : 1

5. Mechanism of action:
PABA + Pteridine
residue
Protein
biosynthesis
Folinic
acid
RNA
tRNA
rRNA
mRNA
DNA
Bases
DNA
F.A
Cell division
D H F A
R
Trimethopri
m
Synthetas
e
T H F A
R
Sulphamethoxaz
ole
Bacteriost
atic
No Life
Bactericidal

6. SPECTRUM
H.I (Heamophilus Influenza)
Cholera
Brucella
Corynebacterium diphtheria
E.coli
Porteous
Shigella
Certain aerobes
Protozoa like PCP_ (pneumocystis
carnnii pneumonia)
Chloroquine resistant plasmodium
falciparum

7. INDICATIONS
1st line treatment
RTIs Upper and Lower
UTIs
Cystitis
Chronic UTIs
Recurrent UTIs
Skin and soft tissue infections
2nd line treatment
Genital Infections like
Acute gonococcal uretritis
Oropherengeal gonorrhoea
Malaria
 Meningitis

8. ADVERSE EFFECTS
GIT
Diarrhea
Abdominal discomfort
CNS
Headache
Depression
Ataxia(difficulty in balance and
speech)
Nightmares
Fatigue
Vertigo
Renal
Heamochorea (bleeding in urine)
Renal irritation
Liver
Jaundice
Hyper sensitivity
CVS
Methemoglobinemia
Sulphaemoglobinemia
Steven Johnson’s syndrome
kernictyrus