SULPHONAMIDES AND QUINOLONES

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SULPHONAMIDES AND QUINOLONES

Drugs Dosa ge MOA ADR USES
Sulphonamides Sulfonamides, being structural analogues of PABA inhibit bacterial folate synthase

  • FA is not formed and a number of essential metabolic reactions suffer
  • Nausea, vomiting and epigastric pain
  • Crystalluria
  • Hypersensitivity , Steven Johnson syndrome
  • Hepatitis
  • Topical use- contact sensitization- so not allowed
  • Hemolysis in person with G6PD deficient individuals
  • Kernicterus precipitated in newborns
  • Systemic use of sulfonamides alone is rare now
  • Suppressive therapy of

chronic UTI

  • Streptococcal pharyngitis
  • As cotrimoxazole– P. jiroveci and nocardiosis
  • Along with pyrimethamine- used for Malaria and Toxoplasmosis
  • Ocular sulfacatamide- used in trachoma
  • Topical sulfadiazine- in Burn
Cotrimoxazole (Fixed dose combination of trimethoprim and sulfamethoxazole) 1:20 SULPHONAMIDES AND QUINOLONES
  • All adverse effects seen with sulfonamides
  • Nausea, vomiting, stomatitis, headache and rashes
  • Folate deficiency- megaloblastic anemia
  • Blood dyscarias
  • Cotrimoxazole shouldn’t be given in pregnancy- neonatal haemolysis and methemoglobenemia
  • Patient with renal disease- Uremia
  • AIDS patient with P. jiroveci infection- Fever rash and BM supression
  • BM toxicity in elderely
  • UTI
  • Respiratory tract infection- both URTI and LRTI, otitis media
  • Bacterial diarrhea and dysentery- E.coli, Shigella, Salmonella, and Y. enterocolitica
  • Pneumocystis jiroveci
  • Chancroid
  • Typhoid
Drugs Dosa ge MOA ADR USES
Quinolones (Nalidixic acid)
  • Active against gram negative bacteria- E. coli, Proteus, Klebsiella, Shigella but not Pseudomonas
  • Inhibiting bacterial DNA gyrase and is bactericidal
  • GI upset, rashes
  • Neurological- headache, drowsiness, vertigo, visual disturbances, seizures
  • Photoxicity
  • G6PD deficiency- Hemolysis
  • Urinary antiseptic
  • Diarrhea- caused by Proteus, E.coli, Shigella or Salmonella
Fluoroquinolones (See above for the names)

Prototype- Ciprofloxacin

  • 1st gen– More for gram negative
  • 2nd gen– also gram positive
  • Inhibit enzyme bacterial DNA gyrase (primarily active in gram negative bacteria), which nicks double stranded DNA, introduces negative supercoils and the reseals the nicked ends
  • Gram positive- target of FQ is Topoisomerase IV
  • Good safety record
  • GI– N, V, bad taste, anorexia, Diarrhea is rare
  • CNS– dizziness, headache, restlessness, anxiety, insomnia, impairment of concentration
  • Skin/hypersensitivity– rash, pruritus, photosensitivity, swelling of lips
  • Tendinitis and tendon rupture
  • UTI
  • Gonorrhea
  • Chancroid
  • Bacterial enteritis
  • Typhoid
  • Bone, soft tissue, gynaecological and wound infections
  • Respiratory infection
  • TB– 2nd line drug
  • Gram negative septicaemia
  • Meningitis– Gram negative
  • Prophylaxis in neutropenic cancer
  • Conjunctivitis
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