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FLUOROQUINOLONES-
CIPROFLOXACIN
Dr.Sumeet Dumbre
INTRODUCTION:-
ā€¢ Ciprofloxacin is a fluoroquinolone antibiotic used to treat a number of
bacterial infections.
ā€¢ It is the most potent first generation FQ active against a broad range of
bacteria, the most susceptible ones are the aerobic gram-negative
bacilli, especially the Enterobacteriaceae and Neisseria.
ā€¢ The MIC of ciprofloxacin against these bacteria is usually < 0.1 Ī¼g/ml,
while grampositive bacteria are inhibited at relatively higher
concentrations.
ā€¢ Organisms which have shown
low/variable susceptibility are:
Strep. pyogenes, Strep.faecalis,
Strep. pneumoniae, Mycoplasma,
Chlamydia, Mycobact. kansasii,
Mycobact.avium.
ā€¢ Notable resistant bacteria are:
Bacteroides fragilis, Clostridia,
anaerobic cocci.
PHARMACOKINETICS :-
ā€¢ Ciprofloxacin is rapidly absorbed orally, but food delays
absorption, and first pass metabolism occurs.
ā€¢ Ciprofloxacin (and other FQs) have good tissue penetrability:
concentration in lung, sputum,muscle, prostate and phagocytes
exceeds that in plasma, but CSF and aqueous levels are lower.
ā€¢ It is excreted primarily in urine, both by glomerular filtration and
tubular secretion.
ā€¢ Urinary and biliary concentrations are 10ā€“50 fold higher than
plasma.
CONTRAINDICATIONS:-
ā€¢ Taking tizanidine at the same time.
ā€¢ Use by those who are hypersensitive to any member of the
quinolone class of antimicrobial agents.
ā€¢ Use by those who are diagnosed with myasthenia graves, as
muscle weakness may be exacerbated.
ā€¢ Ciprofloxacin is also considered to be contraindicated in
children, in pregnancy, to nursing mothers, and in people with
epilepsy or other seizure disorders.
ā€¢ Caution may be required in people with Marfan syndrome or
Ehlers-Danlos syndrome.
INDICATIONS:-
ā€¢ Ciprofloxacin is effective in a broad range of infections.
ā€¢ Because of wide-spectrum bactericidal activity, oral efficacy
and good tolerability, it is being extensively employed for
empirical therapy of any infection, but should not be used for
minor cases or where grampositive organisms and/or
anaerobes are primarily causative.
ā€¢ In severe infections, therapy may be initiated by i.v. infusion
and then switched over to oral route.
1.Urinary tract infections
2.Gonorrhoea
3.Chancroid
4.Bacterial gastroenteritis
5.Typhoid
6.Bone, soft tissue and gynaecological and wound infections
7.Respiratory infections
8.Tuberculosis
9.Gram negative septicemia
10.Meningitis
11.Conjunctivitis
INTERACTIONS:-
ā€¢ Plasma concentration of theophylline,caffeine and warfarin is
increased by ciprofloxacin (also by norfloxacin and pefloxacin)
due to inhibition of metabolism: CNS toxicity can occur by
concurrent use of theophylline and a FQ.
ā€¢ NSAIDs may enhance the CNS toxicity of FQs; seizures are
reported.
ā€¢ Antacids, sucralfate and iron salts given concurrently reduce
absorption of FQs.
ADVERSE EFFECTS:-
ā€¢ Ciprofloxacin has good safety record: side effects occur in
~10% patients, but are generally mild; withdrawal isneeded only
in 1.5%.
ā€¢ Gastrointestinal: nausea, vomiting, bad taste,anorexia. Because
gut anaerobes are not affectedā€”diarrhoea is infrequent.
ā€¢ CNS: dizziness, headache, restlessness, anxiety, insomnia,
impairment of concentration and dexterity (caution while
driving). Tremor and seizures are rare, occur only at high doses
or when predisposing factors arepresent: possibly reflect GABA
antagonisticaction of FQs.
ā€¢ Skin/hypersensitivity: rash, pruritus, photosensitivity,
urticaria, swelling of lips, etc. Serious cutaneous reactions
are rare.
ā€¢ Tendinitis and tendon rupture: a few cases have occurred.
Risk of tendon damage is higher in patients above 60 years
of age and in those receiving corticosteroids. The FQ
should be stopped at the first sign of tendinitis.
FLUOROQUINOLONES.pptx
FLUOROQUINOLONES.pptx
FLUOROQUINOLONES.pptx

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FLUOROQUINOLONES.pptx

  • 2. INTRODUCTION:- ā€¢ Ciprofloxacin is a fluoroquinolone antibiotic used to treat a number of bacterial infections. ā€¢ It is the most potent first generation FQ active against a broad range of bacteria, the most susceptible ones are the aerobic gram-negative bacilli, especially the Enterobacteriaceae and Neisseria. ā€¢ The MIC of ciprofloxacin against these bacteria is usually < 0.1 Ī¼g/ml, while grampositive bacteria are inhibited at relatively higher concentrations.
  • 3. ā€¢ Organisms which have shown low/variable susceptibility are: Strep. pyogenes, Strep.faecalis, Strep. pneumoniae, Mycoplasma, Chlamydia, Mycobact. kansasii, Mycobact.avium. ā€¢ Notable resistant bacteria are: Bacteroides fragilis, Clostridia, anaerobic cocci.
  • 4. PHARMACOKINETICS :- ā€¢ Ciprofloxacin is rapidly absorbed orally, but food delays absorption, and first pass metabolism occurs. ā€¢ Ciprofloxacin (and other FQs) have good tissue penetrability: concentration in lung, sputum,muscle, prostate and phagocytes exceeds that in plasma, but CSF and aqueous levels are lower. ā€¢ It is excreted primarily in urine, both by glomerular filtration and tubular secretion. ā€¢ Urinary and biliary concentrations are 10ā€“50 fold higher than plasma.
  • 5.
  • 6. CONTRAINDICATIONS:- ā€¢ Taking tizanidine at the same time. ā€¢ Use by those who are hypersensitive to any member of the quinolone class of antimicrobial agents. ā€¢ Use by those who are diagnosed with myasthenia graves, as muscle weakness may be exacerbated. ā€¢ Ciprofloxacin is also considered to be contraindicated in children, in pregnancy, to nursing mothers, and in people with epilepsy or other seizure disorders. ā€¢ Caution may be required in people with Marfan syndrome or Ehlers-Danlos syndrome.
  • 7. INDICATIONS:- ā€¢ Ciprofloxacin is effective in a broad range of infections. ā€¢ Because of wide-spectrum bactericidal activity, oral efficacy and good tolerability, it is being extensively employed for empirical therapy of any infection, but should not be used for minor cases or where grampositive organisms and/or anaerobes are primarily causative. ā€¢ In severe infections, therapy may be initiated by i.v. infusion and then switched over to oral route.
  • 8. 1.Urinary tract infections 2.Gonorrhoea 3.Chancroid 4.Bacterial gastroenteritis 5.Typhoid 6.Bone, soft tissue and gynaecological and wound infections 7.Respiratory infections 8.Tuberculosis 9.Gram negative septicemia 10.Meningitis 11.Conjunctivitis
  • 9. INTERACTIONS:- ā€¢ Plasma concentration of theophylline,caffeine and warfarin is increased by ciprofloxacin (also by norfloxacin and pefloxacin) due to inhibition of metabolism: CNS toxicity can occur by concurrent use of theophylline and a FQ. ā€¢ NSAIDs may enhance the CNS toxicity of FQs; seizures are reported. ā€¢ Antacids, sucralfate and iron salts given concurrently reduce absorption of FQs.
  • 10. ADVERSE EFFECTS:- ā€¢ Ciprofloxacin has good safety record: side effects occur in ~10% patients, but are generally mild; withdrawal isneeded only in 1.5%. ā€¢ Gastrointestinal: nausea, vomiting, bad taste,anorexia. Because gut anaerobes are not affectedā€”diarrhoea is infrequent. ā€¢ CNS: dizziness, headache, restlessness, anxiety, insomnia, impairment of concentration and dexterity (caution while driving). Tremor and seizures are rare, occur only at high doses or when predisposing factors arepresent: possibly reflect GABA antagonisticaction of FQs.
  • 11. ā€¢ Skin/hypersensitivity: rash, pruritus, photosensitivity, urticaria, swelling of lips, etc. Serious cutaneous reactions are rare. ā€¢ Tendinitis and tendon rupture: a few cases have occurred. Risk of tendon damage is higher in patients above 60 years of age and in those receiving corticosteroids. The FQ should be stopped at the first sign of tendinitis.