Cyclosporin A NEW

Pharmacological action: 

Cyclosporin A can selectively and reversibly change the function of T lymphocytes, prevent the transcription of lymphoactivin gene, interfere with the transmission of original information, inhibit the release of interleukin-2, interferon and other immune factors, affect humoral and cellular immunity, and inhibit the killing activity of NK cells. Inhibit lymphocyte differentiation and proliferation under the stimulation of antigen or mitogen. However, it has no activity on bone marrow, little effect on B cells, and no significant inhibitory effect on granulocyte survival at therapeutic doses. Oral digestion and absorption were slow and incomplete, only 4% ~ 60%, with an average of 30% of the dose; The relative bioavailability is 20% ~ 50%. The peak value was 2 ~ 8h after oral administration, with an average of 3.5h. There are significant individual differences, such as relative bioavailability of 5% to 89% in kidney transplant patients and 8% to 60% in liver transplant patients. This product is a fat soluble drug, eating and eating fat food can increase absorption. Bile deficiency, stagnation, slow gastric emptying, increased gastrointestinal peristalsis, pancreatic dysfunction and steatorrhea all affect the absorption of this product.

Drug interaction

1. Except glucocorticoids, this product should be avoided in combination with any other immunosuppressant. 

2, this product is mainly metabolized and inactivated in the liver, and any drugs that affect the activity of liver enzymes will affect the metabolism of this product, such as erythromycin, doxycycline, ketoconazole, H2 receptor antagonists, calcium antagonists, androgens, oral contraceptives, all affect the activity of cytochrome P-450 enzyme in the liver cells, which may increase the risk of toxicity of this product. 

3, carbamazepine, phenytoin sodium, phenobarbital, isoniazid, rifamequal can reduce the blood concentration of this product. 

4. Aminoglycoside antibiotics, co-trimoxazole, TMP, amphotericin B, cephalosporins, nitrogen mustards, non-steroidal anti-inflammatory drugs, mannitol, furosemide, etc. can increase the renal toxicity of cyclosporin. 

5, when using this product, calcium and calcium supplements are prohibited, and vaccines are not allowed. 

6, long-term use with glucocorticoid can induce diabetes, hypertension, ulcer disease and osteoporosis, and can increase the toxicity of this product. 

7, in the use of cyclosporine before the use of other immunosuppressants, patients have more overall immunity decline and prone to infection.

Application:

1 New immunosuppressant. A cyclic polypeptide consisting of eleven amino acids. It inhibits the immune function of bodily fluids and cell delivery, without inhibiting bone marrow and without reducing white blood cell count. Prevents rejection of transplanted tissue or organs. It is clinically used for kidney transplantation, liver, lung transplantation and heart transplantation. In addition, it has certain curative effect on autoimmune diseases, schistosomiasis, malaria, diabetes, AIDS, and anti-inflammation properties.

2 It is used to treat leukemia, cancer, kidney transplantation, tuberculosis and so on.

3 Inhibition of T cell receptor signaling pathways for molecular biology research.