brief discussion on immunosupresants, helpful for medical students

2. • SELECTIVE INHIBITORS OF CYTOKINE PRODUCTION AND FUNCTION
1. Cyclosporine
2. Sirolimus
3. Tacrolimus
• IMMUNOSUPPRESSIVE ANTIMETABOLITES
1. Azathioprine
2. Mycophenolate mofetil
3. Mycophenolate sodium
• ANTIBODIES
1. Alemtuzumab
2. Antithymocyte globulins
3. Basiliximab
4. Dacilizumab
5. Muromonab-cd3
• ADRENOCORTICOIDS
1. Methylprednisolone
2. Prednisolone
3. Prednisone
CLASSIFICATION

3. • LIPOPHILIC CYCLIC POLYPEPTIDE
• COMPOSED OF 11 AMINO ACIDS
• EXTRACTED FROM SOIL FUNGUS
• USED TO PREVENT REJECTION OF KIDNEY LIVER AND CARDIAC
ALLOGENEIC TRANSPLANTS
• IS AN ALTERNATIVE TO METHOTREXATE FOR THE RA
• ALSO USED FOR PTS WITH RECALCITRANT PSORIASIS THAT DOES
NOT RESPOND TO OTHER THERAPIES
CYCLOSPORINE

4. 
 MANYARE DOSE DEPENDENT( SO BLOOD LEVELS MONITIORING IS IMP)
 NEPROTOXICITY(MOST COMMON &IMPORTANT)-MONITORING KIDNEY
FUNCTION IS CRITICAL
 HEPATOTOXICITY CAN ALSO OCCUR(LIVER FUNCTION SHOULD BE
ASSESSED PERIODICALLY)
 INFECTIONS ARE COMMON AND LIFE THREATENING( VIRAL INFECTIONS
DUE TO HERPES,CYTOMEGALOVIRUS)
 LYMPHOMA MAY OCCUR.
 ANAPHYLACTIC RXNS.
 OTHER TOXICITIES-
(HTN,HYPERLIPIDEMIA,HYPERKALEMIA,TREMOR,HIRSUTISM,GUM
HYPERPLASIA,GLUCOSE INTOLERANCE)
CYCLOSPORINE-ADR

5. 
 MACROLIDE ISOLATED FROM A SOIL FUNGUS.
 IS APPROVED FOR THE PREVENTION OF REJECTION OF LIVER
AND KIDNEY TRANSPLANTS
 AND IS GIVEN WITH CORTICOSTERIODS AND /OR AN
ANTIMETABOLITE.
 THIS IS MORE FAVOURED OVER CsA BECOS OF ITS POTENCY
AND DECRESED EPISODES OF REJECTION
 AN OINTMENT PREPARTION HAS BEEN APPROVRD FOR
MODERATE TO SEVERE ATOPIC DERMATITIS
ADR
 NEPROTOXICITY,
 NEUROTOXICITY(TREMOR,SEIZURE,HALLUCINATIONS)
TACROLIMUS

6.  RECENTLYAPPROVED MACROLIDE
 OBTAINED FROM FERMENTATION OF SOIL MOLD.
 EARLIER NAME WAS RAPAMYCIN.
 APPROVED FOR USE IN RENAL TRANSPLANTATION.
 AVAILABLE ONLYAS ORAL PREPARATION.
 HIGH FAT MEALS CAN DECREASE THE DRUG ABSORPTION.
 LONG HALF LIFE.
 LOADING DOSE IS REQUIRED AT THE TIME OF INITIATION OF THERAPY.
 ADR
 FREQUENT SIDE EFFECT- HYPER LIPIDEMIA
 COMBINATION OF CsAAND SRL IS MORE NEPHROTOXIC.
 IMPAIRED WOUND HEALING HAS BEEN NOTED WITH OBESE PTS
&DIABETIC PPLE
SIROLIMUS

7.  FIRST AGENT TO ACHIEVE WIDE SPREAD USE IN ORGAN
TRANSPLANTATION.
 IT’S A PRODRUG.
 CONVERTED TO 6 MERCAPTOPURINE THEN TO CORRESPONDING
NUCLEOTIDE THIOINOSINIC ACID.
 MAJOR NON IMMUNE TOXICITY IS BONE MAAROW SUPPRESSION.
 CONCOMITTANT USE WITH ACE INHIBITORS OR COTRIMAZOLE IN
RENAL TRANSPLANT PTS LEAD TO EXAGERRATED LEUKOPENIC
RESPONSE.
AZATHIOPRINE

8. 
 REPLACED AZATHIPRINE BECOS OF THE SAFETY AND EFFICACY IN
PROLONGING GRAFT SURVIVAL.
 SUCCESFULLY USED IN HEART KIDENY AND LIVER TRANSPLANTS.
 ADR- - DIARRHEA,NAUSEA,VOMITING,ABDOMINAL
PAIN,LEUKOPENIA,ANEMIA
 HIGHER DOSES ARE ASSOCIATED WITH CYTOMEGALOVIRUS
INFECTION.
 TO MINIMIZE GI EFFECTS ENTERIC COATED FORM WAS DEVELOPED
MYCOPHENOLATE
MOFETIL

9. 
 IT’S A MONOCLONAL ANTIBODY.
 SYNTHESISED BY HYBRIDOMA TECHNOLOGY.
 USED FOR TREATMENT OF ACUTE REJECTION OF RENAQL
ALLOGRAFTS AS WELLAS FOR CORTICOSTERIOD RESISTANT
ACUTE ALLOGRAFT REJECTION IN CARDIAC AND HEPATIC
TRANSPLANT PATIENTS.
 ADR
ANAYPHALACTIC RXNS,SEIZURES,ENCEPHALOPATHY
CEREBRAL OEDEMA,ASEPTIC MENINGITIS
MUROMONAB

10. 
 BASILIXIMAB AND DACLIZUMAB
 BOTH AGENTS HAVE BEEN APPROVED FOR PROPHYLAXIS OF
ACUTE REJECTION IN RENAL TRANSPLANTATION.
 NOT USED FOR THE TREATMENT OF ONGOING REJECTION.
 ADR: GI EFFECTS(MAJOR)
IL-2 RECEPTOR
ANTAGONISTS

11. 
 CURRENTLY APPROVED FOR THE TREATMENT OF REFARCTORY B
CELL CHRONIC LYMPHOCYTIC LEUKEMIA.
 ADR- NEUTROPENIA,ANEMIA,PANCYTOPENIA
ALEMTUZUMAB

12. 
 FIRST PHARMACOLOGICALAGENTS TO BE USED AS
IMMUNOSUPPRESSIVES BOTH IN TRANSPLANTATION AND IN
VARIOUS AUTO IMMUNE DISORDERS.
 ADR-
 DIABETOGENIC,
 HYPERCHOLERSTREMIA,
 CATARACTS,
 OSTEOPOROSIS
 ,HTN ON PROLONGED USE
CORTICOSTEROIDS