Competitive paralyzants

Therefore, the competitive paralyzants normally foimd to combine with the nicotinic receptors and occupy them strategically without causing any activation. Furthermore, ACH cannot activate the already preoccupied receptors, consequently the motor nerve impulses are unable to evoke contractions, and, hence, paralysis takes place. A few of them, however, take shelter in the receptor-operated ionophore which subsequently minimise the prevailing activation of the postsynaptic membrane. 

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Substances that block the serine residue in the active center of acetylcholinesterase [2j—e.g., the neurotoxin E605 and other organophosphates—prevent ACh degradation and thus cause prolonged stimulation of the postsynaptic cell. This impairs nerve conduction and muscle contraction. Curare, a paralyzing arrow-poison used by South American Indians, competitively inhibits binding of ACh to its receptor. 

C. Atropine will not directly paralyze the respiratory muscles. However, it can prevent the detection of early signs of an overdose of neostigmine, which can quickly progress to a depolarizing block of skeletal muscle and paralysis of the respiratory muscles. Dry mouth, ocular disturbances, and tachycardia are common side effects of atropine given alone, but these effects are less likely to occur with competition between atropine and the increase in the synaptic ACh produced by inhibition of AChE by neostigmine. 

Actions Not all muscles are equally sensitive to blockade by competitive blockers. Small, rapidly contracting muscles of the face and eye are most susceptible and are paralyzed first, followed by the fingers. Thereafter the limbs, neck, and trunk muscles are paralyzed, then the intercostal muscles are affected, and lastly, the diaphragm muscles are paralyzed. 

SEQUENCE AND CHARACTERISTICS OF PARALYSIS Following intravenous administration of an appropriate dose of a competitive antagonist, motor weakness progresses to a total flaccid paralysis. Small, rapidly moving muscles e.g., those of the eyes, jaw, and larynx) relax before those of the limbs and trunk. Ultimately, intercostal muscles and finally the diaphragm are paralyzed, and respiration then ceases. Recovery of muscles usually occurs in the reverse order to that of their paralysis, and thus the diaphragm ordinarily is the first muscle to regain function. 

However, this specific category of drugs may be further sub-divided into two heads, namely (/) Competitive (or stabilizing) paralyzants, and ii) Depolarizing paralyzants. 

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