How Do Calcineurin Inhibitors Work?

Calcineurin inhibitors are a class of drugs usedinthechronicmanagement of patients with allografts (transplantof anorganortissuefrom one individual to another of the same species with a differentgenotype) and inflammatory conditions such asatopic dermatitis,rheumatoid arthritis, andpostoperativeimmunosuppression. Calcineurin inhibitors are “immunosuppressants” as they work by inhibiting calcineurin, anenzymethat activates T-cells of theimmune system. T-cell, also called Tlymphocyte, is a type of leukocyte (whitebloodcell)essentialfor cell-mediatedimmunity.

Calcineurin inhibitors areprescription只有米edicines and are administered via口服,intravenous,topical, andophthalmicroutes.

Calcineurin inhibitors work in the following ways:

• They inhibit the action of calcineurin, an enzyme that plays a key role in cell-mediated immunity.
• They bind to theproteinsin the cells called "immunophilins."
• This reduces the release of thecytokine白介素2from T-cells and T-cell proliferation.
• This leads to inhibition of a key signaling phosphatase “calcineurin”; thus, they are known as “calcineurin inhibitors.”
• In addition, they suppress theimmunesystem so that the body can accept the new organ, thus preventing therejectionreaction.
• They work by weakening theskin’s defense system, thereby decreasing theallergic reactionand relieving the skin irritation andinflammation.
• They increase eyes’ natural ability to produce tears, which reduces swelling of the eyes.

Calcineurin inhibitors are used for the prevention and treatment of conditions such as:

• Organ transplant rejectionprophylaxisin:
  • Heart transplant
  • Liver transplant
  • Kidney transplant
  • Cornealgraft(replaces diseased or scarred corneal tissue withhealthytissue from an organdonor)
• Ophthalmic conditions such as:
  • Keratoconjunctivitis(a group of inflammatoryeyeconditions involving thecorneaand theconjunctiva)
  • Keratoconjunctivitis sicca(also known asdry eyesyndrome, aconditioncharacterized by the inability of the eye to produce sufficient tears to keep it moist)
  • Vernal keratoconjunctivitis (an allergic eyediseasethat especially affects young males)
  • Corneal melting (a devastatingcomplicationofend stagecorneal disease)
• Inflammatory conditions such as:
  • Rheumatoidarthritis(achronic diseasemarked by symptoms of inflammation andpainin the joints)
  • Lupusnephritis(inflammation of thekidneythat is caused bysystemic红斑狼疮erythematous)
• Skin conditions such as:
  • Atopicdermatitis(a chronic skin condition characterized by dry, itchy skin)
  • Psoriasis(a skin disease that causes red, itchy scaly patches, most commonly on the knees, elbows, trunk, and scalp)
  • Eczema(an allergic-type condition that causes red, irritated, and itchy skin)
  • Graft versushostdisease (a syndrome characterized by inflammation in different organs which occurs after anallogeneictransplant)
  • Postoperative immunosuppression

Common side effects include:

Tremors (aninvoluntary, rhythmic shaking movement in one or more parts of body)

• Headache
• Diarrhea
• Nausea
• Vomiting
• Stinging/burning/soreness/itching受影响的皮肤
• Stomachupset
• Acne
• Muscleorback pain
• Eye redness/pain
• Watery eyes

Other rare side effects include:

• Folliculitis(a common skin condition in which hair follicles become inflamed)
• Trouble sleeping
• Hypertension(high blood pressure)
• Blurred vision
• Anemia(low number of红细胞)
• Hypophosphatemia(abnormally low level ofphosphatein the blood)
• Asthenia(abnormalphysical weakness or lack of energy)
• Foreign bodysensationin the eyes
• Upperrespiratorytractinfection
• Nephrotoxicity (rapid deterioration in the kidney function because of the toxic effect of medications and chemicals)
• Conjunctivalhyperemia (dilationand redness of conjunctival vessels that can be asymptomof variousoculardisorders)
• Cough

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with yourdoctororpharmacistto make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking yourmedicationand never change your dose or frequency without consulting your doctor.

Genericand brand names of calcineurin inhibitors include:

• Astagraf XL
• Cequa
• Cyclosporine
• Cyclosporine ophthalmic
• Elidel
• EnvarsusXR
• Gengraf
• Hecoria
• Lupkynis
• Neoral
• Pimecrolimus
• Prograf
• Protopic
• Restasis
• Sandimmune
• Tacrolimus
• Tacrolimusointment
• Voclosporin