Cyclosporine

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Cyclosporine Brand Names

Cequa | Gengraf | Neoral | Restasis | Sandimmune | SangCya

What is Cyclosporine

Cyclosporine is an oral and parenteral immunosuppressive agent. It is a cyclic polypeptide consisting of 11 amino acids and is produced by the fungus Beauveria nivea.

Cyclosporine is used to prevent allograft rejection; the drug has revolutionized transplantation by improving transplant survival, reducing hospitalization, and reducing patient morbidity.

Cyclosporine is also effective in various autoimmune conditions such as uveitis, psoriasis, type I diabetes mellitus, rheumatoid arthritis, inflammatory bowel disease, and certain nephropathies.

While many of these uses are still experimental, cyclosporine capsules and oral solution, USP (Modified) are approved by the FDA for the treatment of refractory rheumatoid arthritis and psoriasis.

Adverse reactions of cyclosporine treatment and the relapse of the conditions upon discontinuation of therapy limit the drugs use in autoimmune diseases. Ophthalmic formulations (i.e., solution and emulsion) are approved by the FDA to increase tear production in patients with ocular inflammation associated with keratoconjunctivitis sicca.

In October 2004, Chiron Corporation submitted an NDA to the FDA for Pulminiq (cyclosporine, USP) inhalation solution.

Fewer patients who received compounded cyclosporine by inhalation three times a week for 2 years after lung transplantation died (3 of 28) as compared with patients who received placebo (14 of 30) in addition to standard immunosuppression, but no difference between the groups was found for the main outcome, which was the rate of histologic acute rejection.

Despite an approvable status granted by the FDA, development of Pulminiq is currently arrested as per a decision by the manufacturer.

Indications

  1. aplastic anemia
  2. atopic dermatitis
  3. Crohn’s disease
  4. graft-versus-host disease (GVHD)
  5. graft-versus-host disease (GVHD) prophylaxis
  6. heart transplant rejection prophylaxis
  7. immune thrombocytopenic purpura (ITP)
  8. kidney transplant rejection prophylaxis
  9. liver transplant rejection prophylaxis
  10. lupus nephritis
  11. myasthenia gravis
  12. nephrotic syndrome
  13. psoriasis
  14. psoriatic arthritis
  15. rheumatoid arthritis
  16. ulcerative colitis
  17. xerophthalmia

Side Effects

  1. abdominal pain
  2. acne vulgaris
  3. acute respiratory distress syndrome (ARDS)
  4. alopecia
  5. anaphylactoid reactions
  6. anemia
  7. angioedema
  8. anorexia
  9. anxiety
  10. appetite stimulation
  11. arthralgia
  12. arthropathy
  13. asthenia
  14. ataxia
  15. azotemia
  16. BK virus-associated nephropathy
  17. bleeding
  18. blepharitis
  19. blurred vision
  20. bone fractures
  21. bronchospasm
  22. bullous rash
  23. candidiasis
  24. cataracts
  25. chest pain (unspecified)
  26. cholestasis
  27. confusion
  28. conjunctival hyperemia
  29. conjunctivitis
  30. constipation
  31. cough
  32. depression
  33. diabetes mellitus
  34. diarrhea
  35. dizziness
  36. drowsiness
  37. dysarthria
  38. dysgeusia
  39. dyspepsia
  40. dysphagia
  41. dyspnea
  42. dysuria
  43. eczema vaccinatum
  44. edema
  45. elevated hepatic enzymes
  46. emotional lability
  47. encephalopathy
  48. epiphora
  49. epistaxis
  50. eructation
  51. esophagitis
  52. fatigue
  53. fever
  54. flatulence
  55. flushing
  56. folliculitis
  57. foreign body sensation
  58. gastritis
  59. GI bleeding
  60. gingival hyperplasia
  61. gingivitis
  62. glossitis
  63. goiter
  64. gout
  65. gynecomastia
  66. headache
  67. hearing loss
  68. heart failure
  69. hematuria
  70. hemolytic anemia
  71. hemolytic-uremic syndrome
  72. hepatic failure
  73. hepatitis
  74. hiccups
  75. hirsutism
  76. hot flashes
  77. hyperbilirubinemia
  78. hyperchloremic acidosis
  79. hypercholesterolemia
  80. hyperesthesia
  81. hyperglycemia
  82. hyperkalemia
  83. hyperlipidemia
  84. hyperprolactinemia
  85. hypertension
  86. hypertrichosis
  87. hypertriglyceridemia
  88. hyperuricemia
  89. hypoesthesia
  90. hypoglycemia
  91. hypomagnesemia
  92. immunosuppression
  93. increased urinary frequency
  94. infection
  95. infertility
  96. influenza
  97. insomnia
  98. jaundice
  99. lethargy
  100. leukoencephalopathy
  101. leukopenia
  102. leukorrhea
  103. libido decrease
  104. libido increase
  105. lymphadenopathy
  106. lymphoma
  107. malaise
  108. menstrual irregularity
  109. metabolic acidosis
  110. migraine
  111. muscle cramps
  112. musculoskeletal pain
  113. myalgia
  114. myocardial infarction
  115. nausea
  116. nephrotoxicity
  117. new primary malignancy
  118. night sweats
  119. nocturia
  120. ocular discharge
  121. ocular inflammation
  122. ocular irritation
  123. ocular pain
  124. ocular pruritus
  125. pancreatitis
  126. papilledema
  127. paresthesias
  128. peptic ulcer
  129. peripheral neuropathy
  130. pharyngitis
  131. polyuria
  132. pruritus
  133. psoriasis
  134. pulmonary edema
  135. purpura
  136. rash
  137. renal tubular necrosis
  138. rhinitis
  139. seizures
  140. sinus tachycardia
  141. sinusitis
  142. skin cancer
  143. skin ulcer
  144. spermatogenesis inhibition
  145. stomatitis
  146. thrombocytopenia
  147. thrombosis
  148. tinnitus
  149. tremor
  150. urinary incontinence
  151. urinary urgency
  152. urticaria
  153. vertigo
  154. visual impairment
  155. vomiting
  156. weakness
  157. weight gain
  158. weight loss
  159. wheezing
  160. xerosis
  161. xerostomia

Monitoring Parameters

  • CBC
  • cyclosporine concentrations
  • LFTs
  • serum bilirubin
  • serum creatinine/BUN
  • serum electrolytes
  • serum lipid profile
  • serum uric acid
  • skin cancer screening exam

Contraindications

  • alcoholism
  • biliary tract disease
  • breast-feeding
  • children
  • contact lenses
  • electrolyte imbalance
  • encephalopathy
  • fungal infection
  • geriatric
  • gout
  • hepatic disease
  • herpes infection
  • herpes simplex keratitis (dendritic keratitis)
  • hyperkalemia
  • hypertension
  • hyperuricemia
  • hypomagnesemia
  • immunosuppression
  • infants
  • infection
  • jaundice
  • lymphoma
  • nephrotoxicity
  • new primary malignancy
  • ocular infection
  • polyoxyethylated castor oil hypersensitivity
  • pregnancy
  • radiation therapy
  • renal disease
  • renal failure
  • renal impairment
  • requires a specialized care setting
  • requires an experienced clinician
  • skin cancer
  • sunlight (UV) exposure
  • vaccination
  • varicella
  • viral infection

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  • Vincristine
  • Vincristine Liposomal
  • Vinorelbine
  • Vorapaxar
  • Voriconazole
  • Warfarin
  • Yellow Fever Vaccine, Live
  • Zafirlukast
  • Zanubrutinib
  • Zileuton
  • Zoledronic Acid
  • Zonisamide

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