Imipenem Cilastatin

Imipenem Cilastatin Brand Name– Primaxin

What is Imipenem Cilastatin

Imipenem is a beta-lactam antibiotic derived from thienamycin and is the first drug to be classified as a carbapenem antibiotic.

Cilastatin is added as an inhibitor of dehydropeptidase-1, an enzyme found in the renal tubule border that metabolizes imipenem. Without cilastatin, imipenem is rapidly metabolized and causes toxicity to the proximal tubule.

Cilastatin itself has no antibacterial activity.

Imipenem possesses several traits that make it an effective antibiotic including: a) more efficient penetration through the bacterial cell wall, b) resistance to bacterial enzymes, and c) affinity for all bacterial PBPs.

Imipenem has a broader spectrum of activity than do many other beta-lactam antibiotics.

Clinically, the combination of imipenem-cilastatin is used to treat severe or resistant infections, especially those that are nosocomial in origin.

The FDA approved imipenem-cilastatin in November 1985.

Indications

  1. Acinetobacter calcoaceticus
  2. Acinetobacter sp.
  3. Aeromonas hydrophila
  4. Alcaligenes sp.
  5. anthrax
  6. appendicitis
  7. Bacillus sp.
  8. Bacteroides fragilis
  9. Bacteroides intermedius
  10. Bacteroides sp.
  11. Bacteroides thetaiotaomicron
  12. Bifidobacterium sp.
  13. bone and joint infections
  14. Capnocytophaga sp.
  15. cellulitis
  16. Citrobacter sp.
  17. Clostridium perfringens
  18. Clostridium sp.
  19. community-acquired pneumonia
  20. cystic fibrosis
  21. diabetic foot ulcer
  22. endocarditis
  23. Enterobacter cloacae
  24. Enterobacter sp.
  25. Enterococcus faecalis
  26. Escherichia coli
  27. Eubacterium sp.
  28. febrile neutropenia
  29. Fusobacterium sp.
  30. Gardnerella vaginalis
  31. gynecologic infections
  32. Haemophilus ducreyi
  33. Haemophilus influenzae (beta-lactamase negative)
  34. Haemophilus influenzae (beta-lactamase positive)
  35. Haemophilus parainfluenzae
  36. intraabdominal infections
  37. Klebsiella oxytoca
  38. Klebsiella pneumoniae
  39. Klebsiella sp.
  40. Listeria monocytogenes
  41. lower respiratory tract infections
  42. melioidosis
  43. Morganella morganii
  44. Neisseria gonorrhoeae
  45. Nocardia sp.
  46. nosocomial pneumonia
  47. Pantoea agglomerans
  48. Parabacteroides distasonis
  49. Pasteurella sp.
  50. Peptococcus sp.
  51. Peptostreptococcus sp.
  52. peritonitis
  53. pneumonia
  54. Prevotella bivia
  55. Prevotella disiens
  56. Prevotella melaninogenica
  57. Propionibacterium sp.
  58. Proteus mirabilis
  59. Proteus vulgaris
  60. Providencia rettgeri
  61. Providencia stuartii
  62. Pseudomonas aeruginosa
  63. sepsis
  64. Serratia marcescens
  65. Serratia sp.
  66. skin and skin structure infections
  67. Staphylococcus aureus (MSSA)
  68. Staphylococcus epidermidis
  69. Staphylococcus saprophyticus
  70. Streptococcus agalactiae (group B streptococci)
  71. Streptococcus pneumoniae
  72. Streptococcus pyogenes (group A beta-hemolytic streptococci)
  73. Streptococcus sp. (Group C)
  74. Streptococcus sp. (Group G)
  75. urinary tract infection (UTI)
  76. Veillonella sp.
  77. Viridans streptococci

Side Effects

  1. abdominal pain
  2. acute generalized exanthematous pustulosis (AGEP)
  3. agitation
  4. agranulocytosis
  5. anaphylactoid reactions
  6. angioedema
  7. anuria
  8. arthralgia
  9. asthenia
  10. azotemia
  11. candidiasis
  12. chest pain (unspecified)
  13. colitis
  14. confusion
  15. cyanosis
  16. diarrhea
  17. dizziness
  18. drowsiness
  19. dysgeusia
  20. dyskinesia
  21. dyspnea
  22. elevated hepatic enzymes
  23. encephalopathy
  24. eosinophilia
  25. erythema
  26. erythema multiforme
  27. fever
  28. flushing
  29. glossitis
  30. hallucinations
  31. headache
  32. hearing loss
  33. hemolytic anemia
  34. hepatic failure
  35. hepatitis
  36. hyperbilirubinemia
  37. hyperchloremia
  38. hyperhidrosis
  39. hyperkalemia
  40. hypersalivation
  41. hyperventilation
  42. hyponatremia
  43. hypotension
  44. infection
  45. injection site reaction
  46. jaundice
  47. leukopenia
  48. myoclonia
  49. nausea
  50. neutropenia
  51. oliguria
  52. palpitations
  53. pancytopenia
  54. paresthesias
  55. phlebitis
  56. polyuria
  57. proteinuria
  58. pruritus
  59. pseudomembranous colitis
  60. pyrosis (heartburn)
  61. rash
  62. renal failure (unspecified)
  63. seizures
  64. sinus tachycardia
  65. Stevens-Johnson syndrome
  66. superinfection
  67. thrombocytopenia
  68. thrombocytosis
  69. tinnitus
  70. tongue discoloration
  71. tooth discoloration
  72. toxic epidermal necrolysis
  73. tremor
  74. urine discoloration
  75. urticaria
  76. vertigo
  77. vomiting
  78. weakness

Monitoring Parameters

  • CBC
  • LFTs
  • serum creatinine/BUN

Contraindications

  • breast-feeding
  • carbapenem hypersensitivity
  • cephalosporin hypersensitivity
  • colitis
  • dialysis
  • diarrhea
  • geriatric
  • GI disease
  • head trauma
  • inflammatory bowel disease
  • laboratory test interference
  • neurological disease
  • penicillin hypersensitivity
  • pregnancy
  • pseudomembranous colitis
  • renal failure
  • renal impairment
  • seizure disorder
  • seizures
  • ulcerative colitis

Interactions

  • Colchicine; Probenecid
  • Disulfiram
  • Ganciclovir
  • Oral Contraceptives
  • Probenecid
  • Sodium picosulfate; Magnesium oxide; Anhydrous citric acid
  • Theophylline, Aminophylline
  • Valganciclovir
  • Valproic Acid, Divalproex Sodium
  • Warfarin