engleski

BASIC PHARMACOOLOGICAL ASPECTS OF PAIN ACTING DRUGS

At the peripheral level, C or A delta fibres are excited by noxious stimuli. Involved molecules are released from cellular lysis, the inflamed surrounding tissues and C or A delta fibres themselves. Recently, molecular biology and genomics have led to the development of new target-selective entities for use in pain relief. A number of receptors and ion channels present in sensory neurons such as tetrodotoxin insensitive Na+ channel, capsaicin-gated i.e. vanilloid receptor 1(VR1), proton-gated or acid-sensing ion channel (ASIC) channels etc. are now under investigation as new potential analgesic drug targets.During pain transmission at the end of the peripheral nerves in the dorsal horn of the spinal cord, the first synapses are modulated by glutamate and many peptides. A lot of supraspinal sites are activated: the brain stem, the pontomesencephalic regions, the thalamic sites and the cortex. Descending inhibitory controls triggered by noxious stimuli probably play an important role too. Currently it is also believed that neuroplasticity plays a crucial role in the onset and maintenance of chronic pain symptoms - including the upregulation of sensory neuron-specific sodium channels and vanilloid receptors, phenotypic switching of large myelinated axons, sprouting within the dorsal horn, and loss of inhibitory neurons due to apoptotic cell death.

pain; antinociception; analgetic drugs

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