Cyclosporine

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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