Biseptol & Isoniazid
Biseptol & Isoniazid
Biseptol & Isoniazid
G. Domagk
(1895–1964),
bacteriologist and
pathologist discovered
the first sulfonamide in
1935. Nobel prize for
Physiology and Medicine
in 1939.
Mechanism of action
•Unlike man, most bacteria cannot
utilize external folic acid, a nutrient
which is essential for growth, and they have
to synthesize it from para-aminobenzoic
acid (PABA). Sulfonamides are struc-
turally similar to PABA and inhibit the
enzyme dihydrofolate synthetase in the
biosynthetic pathway for folic acid.
•High concentrations of PABA antagonize
the effectiveness of sulfonamides.
PABA Sulfanilamide
DHF synthetase DHF reductase
Lyell
syndrome
after oral
intake of
Co-trimoxazole
Clcr
DRUG PREPARATIONS
t1/2 8–16 h:
- sulfamethoxazolе
- sulfametrolе
t1/2 > 16 h:
- sulfadimethoxinе
- sulfalen
Sulfacetamidе
•collyrium 20% 10 ml
Sulfadicramide
For local
treatment
of bacterial
conjunctivitis
Low GI abssorption (30%)
- Sulfaguanidinе
in GI infections
Sulfasalazinе
(Salazopyrin )®
• colitis ulcerosa
Sulfamethoxazole/Trimethoprim:
Co-trimoxazolе (BAN)
•Biseptol® - tab. 480 mg
•Trimezol® - tab. 480 mg
•960 mg/12 h 7–10 days
Co-trimoxazolе (BAN)
Trimethoprim inhibits dihydrofolate
reductase which converts dihydrofolate
to tetrahydrofolate:
DHF synthetase DHF reductase
PRC B have:
•Azithromycine
•Erythromycine
•Penicillins
•Most
cephalosporines
PRCs LRCs
A: controlled studies L1: safest (Ibuprofen,
show no risk (Vit. B9) Paracetamol)
B: no evidence of risk in L2: safer (Cephalosporins,
humans (Penicillins) Omeprazole)
C: risk cannot be ruled L3: moderately safe
out (Bisoprolol) (Acarbose, Aspirin)
D: positive evidence of L4: possibly hazardous
risk (Diazepam) (Diazepam, Lithium)
X: contraindicated in L5: contraindicated
pregnancy (Estrogens) (ACE inhibitors)
(11) Administer the drug in optimum dose
and frequency
– Inadequate dose may encourage the
development of microbial resistance.
– Intermittent dosing is preffered to
continual infusion.
– Plasma concentration monitoring can be
applied to optimize therapy with aminoglyco-
sides, fluoroquinolones, cephalosporins,
etc. in patients with kidney disease.
(12) Continue therapy until apparent
cure has been achieved.
– Most acute infections are treated for
5 to 10 days. There are many exceptions
to this, such as typhoid fever, tuberculo-
sis, and infective endocarditis, in which
relapse is possible long after apparent
clinical cure and so the drugs are
continued for a long time, determined
by clinical experience.
(13) Test for cure. In some infections, microbio-
logical proof of cure is desirable because
disappearance of symptoms and signs
occurs before the microorganisms are
eradicated, e.g. urinary tract infections
(examinations must be done after
withdrawal of chemotherapy).
(14) Prophylactic chemotherapy for surgical
and dental procedures should be of very limited
duration. It should be started at the time of
surgery to reduce the risk of producing
resistant microorganisms.
(15) Remeber that the most important carriers
of cross infections are your 10 fingers.