Products
Immunosuppressants are commercially available in numerous dosage forms, for example, as creams, ointments, tablets, capsules, solutions, eye drops, and injectables.
Structure and properties
Within immunosuppressants, several groups can be identified. These include steroids such as the glucocorticoids, substances of microbiological origin such as ciclosporin and mycophenolate mofetil, derivatives of nucleic acids and their components such as azathioprine, small molecules, and biologics such as monoclonal antibodies and false receptors.
Effects
The agents have immunosuppressive properties, meaning that they selectively or nonselectively weaken the immune defenses of humans. The mechanisms of action vary. For example, immunosuppressants can destroy immune cells, suppress their functions, disrupt signaling cascades, or bind and inactivate mediators of the immune system.
Indications
Major indications include (selection):
- Allergic diseases
- Rheumatic diseases such as rheumatoid arthritis
- Skin diseases
- Psoriasis, psoriatic arthritis
- Prevention of graft rejection after transplantation.
- Inflammatory bowel disease
- Bronchial asthma
- Eye diseases such as uveitis
- Multiple sclerosis
- Bechterew’s disease (ankylosing spondylitis)
Many are autoimmune diseases, diseases caused by an overactive immune system.
Dosage
According to the drug label. Immunosuppressants are administered both topically and systemically (orally and parenterally). Significantly fewer adverse effects can be expected with topical use. Good adherence to therapy is critical for the prevention of graft rejection.
Active ingredients (selection)
The following is a selection of immunosuppressive agents: Glucocorticoids, cortisone tablets:
- Betamethasone (Betnesol)
- Dexamethasone (Fortecortin, generic).
- Hydrocortisone (Hydrocortone, generics)
- Methylprednisolone (Medrol)
- Prednisolone (Spiricort, generics)
- Prednisone (generic, Lodotra)
- Triamcinolone (Kenacort)
Cytostatic drugs:
- Azathioprine (Imurek, generic).
- Cyclophosphamide (Endoxan)
- Methotrexate (e.g., Metoject, generic).
- Mitoxantrone (Novantrone)
T-cell blockers, calcineurin inhibitors:
- Ciclosporin (Sandimmune).
- Everolimus (e.g., Afinitor)
- Pimecrolimus (Elidel)
- Sirolimus (Rapamune)
- Tacrolimus (Prograf, Modigraf)
Inosine monophosphate dehydrogenase inhibitor:
- Mycophenolic acid (Mycortic, generic).
- Mycophenolate mofetil (Cellcept, generic).
Sphingosine-1-phosphate receptor modulators:
- Fingolimod (Gilenya)
- Ozanimod (Zeposia)
- Siponimod (Mayzent)
Monoclonal antibodies:
- Alemtuzumab (Lemtrada)
- Natalizumab (Tysabri)
- Ocrelizumab (Ocrevus)
- Ofatumumab (Kesimpta)
- Rituximab (MabThera)
- Sarilumab (Kevzara)
- Tocilizumab (Actemra)
Janus kinase inhibitors:
- Baricitinib (Olumiant)
- Ruxolitinib (Jakavi)
- Tofacitinib (Xeljanz)
- Upadacitinib (Rinvoq)
TNF-alpha inhibitors:
- Adalimumab (Humira)
- Certolizumab pegol (Cimzia)
- Etanercept (Enbrel)
- Golimumab (Simponi)
- Infliximab (Remicade)
Contraindications
Contraindications to immunosuppressants include (examples):
- Hypersensitivity
- Increased risk of opportunistic infections
- Severe active infections or active chronic infections, such as with hepatitis or tuberculosis.
- Active malignant diseases
- Pregnancy, lactation
Full precautions can be found in the drug label.
Interactions
Concurrent therapy with other immunosuppressive agents may further increase the risk for infectious disease. Vaccine efficacy may be limited and administration of live vaccines is not recommended.
Adverse effects
Among the most common potential adverse effects of immunosuppressants are infectious diseases.These can be mild (such as a cold), but also severe and fatal, such as blood poisoning. The risk of severe disease progression is greater, and infections that are harmless in immunocompetents can take a severe course in immunosuppressed individuals. Immunosuppressants can activate latent (dormant) infections, for example, herpes virus infections and hepatitis (liver inflammation). Opportunistic infections are infectious diseases that occur mainly when immune function is reduced. These include, for example, fungal infections such as candidiasis and aspergillosis. Hygiene measures are recommended for the prevention of infections, for example regular hand washing, use of disinfectants and hygiene masks, and avoidance of crowds. Patients have an increased risk of cancer, for example lymphoma. Because this includes skin cancer, good sun protection measures are recommended.
