Characteristics of Immunosuppressive Drugs

Classification of drugs
Broadly the immunosuppressive drugs are classified based on their action:

1. Calcineurin inhibitors: They are small molecule drugs and immunophilin – binding drugs. They act as specific T cell inhibitors. E.g., cyclosporine, tacrolimus.

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2. M – TOR inhibitors: these are macrolide antibodies. They target rapamycin inhibitor. E.g., sirolimus.

3. Antiproliferative drugs: they act as cytotoxic drugs. E.g., azathioprine, methotrexate.

4. Glucocorticoids: they act as both immunosuppressant and anti-inflammatory drugs. E.g., prednisolone

5. Biological agents: they are recombinantly produced protein-mediated drugs.

TNFα inhibitors- e.g., infliximab, adalimumab

IL 1 receptor antagonist – e.g., anakinra

IL 2 receptor antagonist – e.g., daclizumab

Anti-CD 3 antibody – muromonab CD- 3

6. Protein drugs

Antibody depleting drugs

Nondepleting antibody drugs

Intravenous immune globulin

Mechanism of action
Immunosuppressive drugs act on either cell-mediated immunity or humoral mediated immunity. A certain group of drugs acts on both types of the immune system. The immune system involves the T lymphocytes, B lymphocytes, mast cells, and macrophages in response to an antigen-specific reaction. The small molecule drugs act by binding to immunophilins and inhibit the nucleotide synthesis. They also act as antimetabolites, and by sphingosine – 1- phosphate receptor antagonist. The immune-suppressive drugs which are administered can interface and act in any step of the immune response.

Glucocorticoids- They act by inhibiting the activity of the monocytes and T helper cells. They also inhibit lymphokines production.

Cyclosporin- It acts by inhibiting the activity of the interleukin- 2 and T lymphocytes.

Azathioprine and methotrexate – The proliferation of the responses is inhibited by these drugs.

Chloroquine- Inhibits the interleukin – 2 production.

Uses and side effects
There is a list of drugs that are prescribed for autoimmune disorders. The autoimmune disorders are conditions where the immune system considers its own cells to be foreign antigens. They are used in autoimmune conditions like rheumatoid arthritis, lupus, myasthenia gravis, and skin conditions like psoriasis, Crohn’s disease, and multiple sclerosis. They are also recommended in the case of organ transplants where they are used as antirejection drugs during both induction and in maintenance. They are used in all types of organ transplants like liver, kidney, lungs, etc. They are administered in case of an anaphylactic reaction and chronic asthmatic conditions. The administration of these drugs results in a series of side effects as they suppress the immune system of the individual. Short term usage leads to nausea, vomiting, diarrhea, and increase their higher susceptibility to infection. They are more prone to community-acquired infections and opportunistic organisms. It causes osteoporosis, where the density of the bone is decreased. It also increases the risk of developing patient malignancy (mostly cutaneous and hematological), cardiovascular disorders due to chronic inflammatory conditions, hyperglycemia, hyperlipidemia, and bone marrow suppressions.

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