Naslov
Antagonisti nikotinskih receptora
(Antagonists of the nicotinic cholinergic receptors)

Autori
Zorc, Branka ; Šoronda, Sanja

Izvornik
Farmaceutski glasnik (0014-8202) 55 (1999), 9; 319-327

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, stručni

Ključne riječi
antagonisti; nikotinski receptor; acetilkolin; miorelaksansi; ganglioblokatori
(antagonists; nicotinic receptor; acetylcholine; muscle relaxants; ganglionic blockers)

Sažetak
Nicotinic receptors are present in nerve synapses at ganglia, as well as at the neuromuscular synapses. Drugs are able to show a level of selectivity between two sites. Antagonists of ganglionic nicotinic receptor sites (ganglionic blockers) inhibit the signal transfer in the synapses of the sympathetic and parasympathetic ganglia. Specific blockade of only one type of ganglia is not possible so ganglionic blockers are not therapeutically useful. Antagonists of the neuromuscular junction are useful drugs and are known as muscle relaxants or neuromuscular blocking agents. There are three groups of muscle relaxants: stabilizing, depolarizing and muscle relaxants with dual action. Stabilizing muscle relaxants block acetylcholine receptors in the postsynaptic membrane by competitive inhibition of acetylchloride. The prototype of these compounds is tubocurarine and the other important drugs are pancuronium bromide, vecuronium bromide and atracurium besilate. Depolarizing muscle relaxants depolarize the end-plate just like acetylcholine but prevent repolarization since their elimination is slow. The only therapeutically useful drug in this class is suxamethonium chloride. Some compounds such as decamethonium bromide and hexacarbacholine bromide have both depolarizing and stabilizing activity. Dantrolene is the only muscle relaxant that decreases muscle tone by partial blockade of calcium ion release from the longitudinal system. Centrally-acting muscle relaxants or myotonolytic drugs such as baclofen do not affect neuromuscular transmission at the motor end-plate, but inhibit polysynaptic reflexes.

Izvorni jezik
Hrvatski

Znanstvena područja
Kemija

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