19. PHARMACOLOGY OF IMMUNOSUPPRESSANTS AND STIMULANTS

The immune system protects the body from infections and foreign substances. Sometimes, however, it may become overactive (as in autoimmune diseases) or needs to be intentionally suppressed (such as after an organ transplant). In other cases, patients may need medicines to boost the immune response, especially when immunity is weak. Drugs that decrease immune activity are called immunosuppressants, and drugs that increase immunity are known as immunostimulants.


IMMUNOSUPPRESSANTS

These drugs are used to prevent the body from rejecting transplanted organs and to control autoimmune diseases. They work by reducing the activity of immune cells, especially T-cells.

Main Uses

  • Organ transplant (kidney, liver, heart)
  • Autoimmune diseases (rheumatoid arthritis, psoriasis)
  • Inflammatory bowel disease (Crohn’s disease, ulcerative colitis)

Major Classes of Immunosuppressants

1. Calcineurin Inhibitors

These are the most widely used transplant drugs. They block T-cell activation by inhibiting an enzyme called calcineurin.

a. Cyclosporine

One of the first major immunosuppressants used in transplant therapy.

  • Uses: Organ transplantation, rheumatoid arthritis, psoriasis
  • Side effects: Kidney toxicity, gum overgrowth, high blood pressure

b. Tacrolimus

More potent than cyclosporine.

  • Uses: Organ transplant prevention of rejection
  • Side effects: Kidney toxicity, tremors, increased blood sugar

2. Antimetabolites

These drugs interfere with DNA synthesis in immune cells and suppress their multiplication.

a. Azathioprine

  • Uses: Transplantation, autoimmune disorders
  • Side effects: Bone marrow suppression, liver problems

b. Mycophenolate mofetil (MMF)

  • Uses: Often combined with calcineurin inhibitors
  • Side effects: Diarrhoea, low blood counts

3. mTOR Inhibitors

These block a key enzyme (mTOR) needed for T-cell growth.

a. Sirolimus (Rapamycin)

  • Uses: Kidney transplant
  • Side effects: High cholesterol, delayed wound healing

4. Glucocorticoids (Steroids)

These drugs suppress inflammation and immune activity.

  • Prednisolone
  • Dexamethasone

Side Effects

  • Weight gain
  • High blood sugar
  • Weak bones
  • Increased infection risk

5. Biological Agents (Monoclonal Antibodies)

These are targeted therapies that block specific immune pathways.

  • Infliximab – blocks TNF-alpha
  • Rituximab – targets B-cells
  • Basiliximab – prevents transplant rejection

Side Effects of Immunosuppressants (General)

  • Increased risk of infections
  • Higher risk of cancer (due to reduced immune surveillance)
  • Kidney and liver damage (drug-specific)
  • High blood pressure
  • Gastrointestinal upset

IMMUNOSTIMULANTS

These are drugs or biological substances that boost immunity. They are used when the immune system is weak or when enhanced defence is needed.

Main Uses

  • Certain viral infections
  • Cancers
  • Immunodeficiency conditions
  • As vaccines or vaccine adjuvants

Major Classes of Immunostimulants

1. Interferons

Natural proteins that boost antiviral and immune responses.

  • Uses: Hepatitis B & C, some cancers, viral infections
  • Side effects: Flu-like symptoms, fatigue

2. Interleukins

Help activate immune cells like T-cells and natural killer cells.

  • IL-2: used in kidney cancer and melanoma

3. Thymic Hormones

Support T-cell development.

  • Thymosin

4. Colony-Stimulating Factors (CSFs)

These medicines increase blood cell production, especially after chemotherapy.

  • G-CSF (Filgrastim)
  • GM-CSF

Uses

  • Boost white blood cells
  • Prevent infections in cancer patients

Vaccines as Immunostimulants

Vaccines are one of the most effective immunostimulants. They train the immune system to recognize and fight infections.


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