We’ll discuss the following:
Introduction.
History of Cyclosporine.
Scientific Classification.
Structure of Cyclosporine.
Uses of cyclosporine.
Plaque Psoriasis Patients.
How Does Cyclosporine Work?
Negative Effects of Cyclosporine.
Forms of Cyclosporine.
Introduction
is animmunosuppressantdrugwidely used inorgan
transplantationto preventrejection.
It reduces the activity of theimmune systemby interfering
with the activity and growth ofT cells.
It was initially isolated from the fungusTolypocladium
inflatum(Beauverianivea), found in a soil sample.
Most peptides are synthesized by ribosomes, but
ciclosporinis a cyclic nonribosomalpeptide of
11 amino acids and contains a single D-amino acid,
which are rarely encountered in nature.
History of Cyclosporine
Comes from the fungus Tolypocladiuminflatumwhich was
discovered in 1970.
Tolypocladiuminflatumwas isolated from Norwegian soil samples.
Found to be immunosuppressant--cyclosporine in 1976 by J. F. Borel
Cyclosporine was approved for use in 1983 to prevent graft
rejection in transplants.
Approved for the treatment of severe psoriasis in 1997.
Structure of Cyclosporine
It was shown to have 11 amino acids
and was determined to play a
significant role in organ transplants.
Cyclic polypeptide .
Ciclosporinis synthesized by anon-
ribosomal peptidesynthetase,
ciclosporinsynthetase.
Uses of cyclosporine
Is an immunosuppressant which suppress or reduce the strength of the
immune system
Cyclosporine is used to prevent transplant rejection in people who have
undergone kidney, heart and liver transplants.
It is approved in the US for the treatment ofrheumatoid arthritis,
severepsoriasisand as anophthalmic emulsionfor the treatment ofdry eyes
(Restasis).
Also used in severeatopic dermatitis ,Kimura's disease,pyoderma
gangrenosum, chronic autoimmuneurticaria
Plaque Psoriasis Patients
Plaque psoriasis is a chronic inflammatory skin condition that is partially due to an
overactive immune system. It causes the body to grow skin cells at a rapid rate
causing these skin cells to pile on top of each other forming red patches---plaque.
In 1997, the Federal Drug administration approved Neoral(cyclosporine) for the
treatment of patients with severe psoriasis.
Usage of cyclosporine suppresses the growth of skin cells
Only used for SEVERE plaque psoriasis if prior methotrexate use is insufficient.
Cyclosporine is highly effective in clearing psoriasis and can prevent relapse.
Not recommended for people who have a weak immune system since cyclosporine
is an immunosuppresant.
Side effects
Kidney problems
High BP
Skin cancer
How Does Cyclosporine Work?
As cyclosporine enters the body, it suppresses T-cell
function.
Reducing T-cell function will enable successful
transplantation since T cells purpose of function is to kill
off objects viewed as foreign.
Cyclosporine reduces the T cell function without
affecting B cell function and the production of
antibodies. Therefore, suppressing T-cell function allows
for the transplanted organ to be accepted without a
problem.
Not all organ transplants will be rejected by the body.
However, cyclosporine is used as precautionary
measures.
Negative Effects of Cyclosporine
Because cyclosporine is an immunosuppressant, it may cause patients to
be vulnerable to OTHER health problems. IT IS VERY TOXIC!!!
Usage of cyclosporine may cause high BP, kidney problems. It also
encourages cancerous tumor growth.
Side effects: headache, vomiting, nausea, diarrhea, upset stomach,
cramps, increased hair growth, tremor, swollen/red/painful gums,
dizziness.
Serious side effects: dark urine, persistent nausea/vomiting, severe
stomach/abdominal pain, yellowing of the skin/eyes, vomit that looks like
coffee grounds, change in the appearance or size of skin moles/lesions,
changes in skin color, loss of consciousness, mental/mood changes,
vision changes, swollen glands, unusual lumps,night sweats
Forms of Cyclosporine
This medicine is usually given 4 to 12 hours before organ
transplantation via needle placed in a vein
Comes in the form of oral capsule and solution (liquid)
Solution must be mixed with a liquid such as orange juice or milk.
NO GRAPE FRUIT OR GRAPEFRUIT JUICE!!!
Comes in the brand name Gengraf, Neoral, SandimmuneCapsules,
SandimmuneOral solution