Immunosuppressive Drug Therapy
Immunosuppressive Drug Therapy
DRUG THERAPY
BY
Abhishek S. Sharma
Immune Response
Immune response is a highly sophisticated
defense mechanism of the body which is
composed of Cell mediated and Humoral
immunity (Nossel 1987) . Both of these
response have a high level of specificity
directed to antigenic epitopes expressed
on molecular components of infectious
agents , foreign (Grafts) or transformed
(Malignants) , or even autologous cells
(autoimmunity).
Cells participating in the immune
response
General principles of
Immunosuppression
Immunosuppression:-Immunosuppression is a process of
inhibiting the immune response at different steps .
Eg:-Prednisolone,Hydrocortisone, etc.
Description:-
Was discovered in 1972
Isolated from fungi
Available as I.V , Caps , Tabs
, Sol.
Mechanism Of Action:-
1. Binds with cyclophilin of T-
lymphocytes.
2. Inhibits calcineurin which
induces the transcription of
IL-2.
Adverse drug reactions:-
High blood pressure
Unusual hair growth
Nephrotoxicity
Drug-drug interactions:-
Enzyme inducers:
Carbamazepine,Phenobarbitone.
Enzyme inhibitor:
Acyclovir,antifungals.
Drug-food interactions: Grape fruit juices should
be avoided,vaccination should not be done.
Tacrolimus
Description:-
• Odourless and tasteless
white crystalline powder.
• Isolated from cultures of
Streptomyces
tsukubaensis, strain no.
9993
MOA:-
• Inhibits T – lymphocyte
activation by forming
complex with an
intracellular protein FKBP -
12
• The complex formed
inhibits calcineurin.
ADR:-
Hyperglycaemia
Myocardial Hypertrophy
Hypomagnesia , Hyperkalemia
Drug-Drug interaction:-
Enzyme inducers: Anticonvulsants,Rifabutin ,
Rifampin
Enzyme Inhibitors:-
Anti fungals , Macrolides
Azathioprine
Description:-
Immunosuppressive
metabolite
MOA:-
Non enzymatically
cleaved in
mercaptopurine which
acts as a purine
analogue and inhibitor
of DNA synthesis
Azathioprine
ADR:-
Hematological and gastrointestinal problems
Drug-Drug interactions:-
Usual dosage of azathioprine should be reduced
when used in conjunction with allopurinol.
Use with other leukocyte enhancer like
cotrimoxazole may increase leukopenia in kidney
transplant patients
Use with ACE inhibitor may lead to leukopenia
Mycophenolate Mofetil
Description:-
Newer variety of
immunosuppressant
derieved from penicillium
culture.
MOA:-
Mycophenolic acid inhibits
lymphocyte purine
synthesis by non
competitive inhibition of
enzyme Inosine
Monophosphate
Dehydrogenase.
ADR:-
Diarrhoea , nausea , vomiting , infections ,
anemia.
Drug-Drug Interactions:-
Enzyme Inducer:-
Antacids with Mg and Al hydroxides
Cholestyramine
Enzyme Inhibitor:-
Acyclovir
Renal Transplant Operation
Drug Regime Post Kidney
Transplant
Immunosuppressants
DPCO(Drug Price Control) 1985 act for life saving drugs of this
class should be taken into deep consideration.
BIBLIOGRAPHY
( Ref : - Goodman & Gilman’s The pharmacological basis of theraputics , 9th edition , by
Hardman Joel . G , Limbird Lee E , published by McGraw Hill, int edition 1996 , pg no. 1291 –
1296)
http://en.wikipedia.org/wiki/Immunosuppressant#immunosuppressive
http://www.answers.com/topic/cyclosporine-1
http://www.emcure.co.in/html/vingraf.htm
http://www.rxlist.com/cgi/generic/azathioprine_ad.htm
6)http://gsm.about.com/compact/showmono.asp?monotype=&cpnum=419&r=6078&match=F
Reference:- Smith’s general urology, 13th edition , year of publication :-1992, b
Tanagho Emil .A MD (University of California. San Francisco) McAninch Jack W MD
(University of California….San Francisco)Pg no. 556-562 Book provided by Dr. Sunil Agrawal MS
, Sanjeevani Hospital, Malad(E)
http://www.aakp.org/aakp-library/Transplant-Drugs/
http://www.vesalius.com
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&dopt=AbstractPlus&list
_uids=15846602&query_hl=2&itool=pubmed_docsum
http://ndt.oxfordjournals.org/cgi/content/abstract/13/10/2601?maxtoshow=&HITS=10
&hits=10&RESULTFORMAT=&fulltext=immuno+suppressants&searchid=1&FIRSTIN
DEX=30&resourcetype=HWCIT
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&dopt=AbstractPlus&list
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http://www.springerlink.com/content/rvg24my1hw80t9fx/