Macrolides

The macrolides are a group of drugs that are generally derived from natural products.  They include a number of antibiotics such as Azithromycin, Clarithromycin, Dirithromycin, Erythromycin and so on.  But within the group are also a number of non-antibiotics - tacrolimus, ciclosporin and pimecrolimus, which are used as immunosuppressants or immunomodulators.

The mode of action is extremely complex, but all affect T-cells and inhibit their action.  In T-cells, activation of the T-cell receptor normally increases intracellular calcium, which acts via calmodulin to activate calcineurin. The drugs inhibit calcineurin thus inhibiting both T-lymphocyte signal transduction and IL-2 transcription [interleukin-2].  They may also inhibit lymphokine production and interleukin release and, therefore, lead to a reduced function of effector T-cells.

A 2008 British Medical Journal article highlights that the combination of macrolides and statins (used for lowering cholesterol)  can lead to debilitating myopathy - a muscular disease in which the muscle fibers do not function for any one of many reasons.

Observations

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• Ciclosporin and Sandimmune
• Complex visual hallucinations and cyclosporine
• Cyclosporine neurotoxicity in heart transplantation
• Neurologic complications of pancreas transplants
• Reversible tacrolimus-induced neurotoxicity isolated to the brain stem
• Tacrolimus