Antibacterial agent PPT

1. Product Brief
Brand Name : Furotil®
Generic Name : Cefuroxime Axetil
Strength : Tablet: 250 mg and 500 mg.
Dosage Form : Tablet
Therapeutic Use : For the treatment of various bacterial infections
Brand slogan : Antibiotic with difference.

2. Pharmacokinetic data
Bioavailability 37% on empty stomach, up to 52% if taken after food
Metabolism axetil moiety is metabolized to acetaldehyde and acetic acid
Half-life 1.2 hour
Excretion Urine 66-100% Unchanged
Semi synthetic, broad-spectrum, bactericidal
2nd generation cephalosporin antibiotic.

3. Mechanism of action
Cefuroxime are bactericidal and have the same mode of action as
other beta-lactam antibiotics (such as penicillins) but is less
susceptible to Beta-lactamase. Cephalosporins disrupt the
synthesis of the peptidoglycan layer of bacterial cell walls. The
peptidoglycan layer is important for cell wall structural integrity.
The final transpeptidation step in the synthesis of the
peptidoglycan is facilitated by transpeptidases known as
penicillin-binding proteins (PBPs).

4. Generation of Cephalosporins
Gen Examples Specturm Pathogens
1st Cephradine
Cefalexin
Cefadroxil
Cefazolin
More:
Gram+Ve
Less:
Gram–Ve
Gram-positive
Streptococci, Staphylococci
Gram- negative
E. coli, K. pneumoniae
2nd Cefoxitin
Cefuroxime
Cefaclor
Less:
Gram+Ve
More:
Gram-Ve
Gram-positive
S. aureus, S. pneumoniae
Streptococci
Gram-negative
E. coli, Klebsiella, H. influenzae, M.
catarrhalis, Neisseria, Proteus,
Anaerobes
Bacteroides fragilis

5. Gen Example Spectrum Pathogens
3rd Ceftriaxone
Cefotaxime
Ceftazidime
Ceftibuten
Cefixime
Less:
Gram+Ve
More:
Gram-ve
Gram-negative aerobes
E. coli, Klebsiella, Proteus,
H. influenzae, M. catarrhalis,
Neisseria sp, Enterobacter sp.,
Acinetobacter, Morganella morganii,
Serratia, Pseudomonas
4th Cefepime
Cefpirome
Extended:
Gram+ve
More:
Gram-ve
As first generation
Same as third generation
Generation of Cephalosporins

6. Absorption and Metabolism
After oral administration, cefuroxime axetil is absorbed
from the gastrointestinal tract and rapidly hydrolyzed by
nonspecific esterases in the intestinal mucosa and blood to
cefuroxime.
Cefuroxime is subsequently distributed throughout the
extracellular fluids. The axetil moiety is metabolized to
acetaldehyde and acetic acid.

7. Dosage & Administration
Population/Infection Dosage Duration (days)
Adolescents and Adults (13 years and older)
Throat and Tonsil
Infections
250 mg; 12 hourly 10 days
Sinus Infection 250 mg; 12 hourly 10 days
Bronchitis 250 or 500 mg; 12 hourly 5 to 10 days
Skin Infections 250 or 500 mg; 12 hourly 10 days
Urinary Tract Infection 250 mg; 12 hourly 7 to 10 days
Gonorrhea The usual Treatment is of 1g Single dose
Early Lyme disease 500 mg; 12 hourly 20 days
Pediatric Patients (Who can swallow tablets whole)
Acute Otitis Media 250 mg; 12 hourly 10 days
Acute Bacterial
Maxillary Sinusitis
250 mg; 12 hourly 10 days
Furotil Tablets

8. Dosage & Administration
Sequential therapy:
Pneumonia: 1.5 g 2-3 times daily for 48-72 hours followed by
500 mg twice daily for 7-10 days
AECB: 750 mg 2-3 times daily for 48-72 hours followed by
500 mg twice daily for 5-10 days

9. Target Doctors
•Gynecologists
•ENT Specialists
• Urologists
• Nephrologists
•Dermatologist
• Pediatricians
• Medicine Specialists
• GPs
• All competitors’ brand prescribers

10. Urinary tract infections (UTIs) are one of the most
common bacterial infections during pregnancy. UTIs are
associated with risks to both the fetus and the mother,
including pyelonephritis, preterm birth, low birth
weight, and increased perinatal mortality. So it is
very important to treat UTI with a safe and effective
Antibiotic as two lives are directly involved here.
UTI in pregnancy
But,
Quinolone i.e. Ciprofloxacin is not safe in pregnancy
Macrolide i.e. Azithromycin is highly resistant to urinary pathogens and only 6% of
the administered drug excreted through urine as unchanged condition
On the other hand,
Safety of Cefuroxime has been established by direct clinical trial on pregnant
woman
95% of the administered drug excreted through urine as unchanged condition

11. Pregnancy category : FDA (United states) : B

12. Cefuroxime is a safe antibiotic in all stages of pregnancy
Safety of Cefuroxime is established through direct clinical trial on pregnant women
No of patients: 78 pregnant women and their 80 infants.
● 13 women in the first trimester
● 19 women in the second trimester
● 46 women in the third trimester
18 months follow up after birth, it is found that – No abnormalities in terms of
physical and mental development were observed to any of the children and their
mothers.

13. Cefuroxime is highly effective in uncomplicated UTI
No of patients: 140 women with uncomplicated UTI
Drug used: Cefuroxime 250 mg twice daily
Results: Cefuroxime axetil may be used safely and
effectively to treat uncomplicated UTI at a dose of 250
mg bid
97%
Clinical success rate

14. Cefuroxime is effective and safe treatment option for acute
pyelonephritis during pregnancy
No of patients: 101 pregnant women with acute pyelonephritis
• 52 women in Cefuroxime group
• 49 women cefradine group
Drug used:
• Cefuroxime 750 mg inj tid for 3 days followed by
250 mg tablet bid for 11 days
• Cefradine 1 gm inj qid for 3 days followed by
500 mg tablet tid for 11 days
Cefuroxime Cefradine
96.2%
89.8%

15. Cefuroxime for the treatment of Community-acquired pneumonia
Total no of patients: 162
Cefuroxime axetil group: cefuroxime axetil 500 mg twice a day (n = 84) for 10 days.
Amoxycillin/clavulanate group: amoxycillin/clavulanate 500 mg/125 mg three times a
day (n = 78) for 10 days.
Result: Cure or improvement were achieved 100% and 96% in case of patients treated
with cefuroxime axetil or amoxycillin/clavulanate, respectively.
Cefuroxime amoxycillin/clavulanate
100%
96%
Clinical
success
rate

16. cefuroxime axetil in treatment of secondary bacterial infections of
Acute Bronchitis
Patients received 5 or 10 days of treatment (n = 177 in each group) with
Cefuroxime axetil at 250 mg twice daily. Patients in the 5 days group received
placebo on days 6 to 10.
Result: A satisfactory clinical outcome was achieved in 82% & 86% of the
clinically evaluated patients treated with 5 days & 10 days group respectively.
5 days
10 days
82% 86%
Clinical
success
rate

17. Cefuroxime for the treatment of Acute Uncomplicated Gonorrhoea
No of patients: 140 (Men:110 & Women: 30)
Drug used: Single oral doses of cefuroxime axetil (1.5
gm) with 1 gm probenecid.
Results: The cure rate was 100%.
100%
Clinical success rate

18. • Cefuroxime injection was
used to treat 28 neonates
with suspected or proved
infection.
• There was significant
clinical improvement in
27 of them after 5 days
treatment and each was
well on discharge from
hospital.
• Dose : 50mg/kg twice a
day for 5 days
Cefuroxime in the treatment of neonates
96%
Clinical success rate

19. Cefuroxime for the treatment of SSTI
A total of 330 patients were enrolled at 10 centers and were randomly assigned to
receive cefuroxime axetil 250 mg (n = 107), cephalexin 500 mg (n = 111) or cefadroxil
500 mg (n = 112), twice daily for 10 days.
Clinical and bacteriological efficacy of three oral cephalosporins were evaluated and it
was found that Cefuroxime was superior to others.
Cefuroxime
Cefadroxil
Cephalexin
Cefuroxime
Cefadroxil
Cephalexin
Clinical cure rate Bacteriological eradication
97%
94%
89%
96%
93%
85%

20. Studies shows that
cefuroxime axetil is as
effective or more
effective than of
cefaclor, amoxicillin
or amoxiclav for
Acute Otitis Media.
Cefuroxime for the treatment of ENT infection (ear infection)
96%
Clinical success rate

21. A 10 days course of
cefuroxime is highly
effective for the
treatment of
pharyngitis and
tonsillitis.
Cefuroxime for the treatment of ENT infection
(Pharyngitis and Tonsillitis)
95%
Clinical success rate

22. Cefuroxime for the treatment of
Enteric fever
98.6%
Clinical
success rate

23. Thank You