PHAR 100 Lecture Notes - Lecture 3: Muscle Relaxant, Generalized Anxiety Disorder, Central Nervous System Depression

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To depress brain activity, decrease glutamate-induced nerve ring. Increase in gaba neuronal ring results in decreased glutamate nerve ring. Gaba = primary inhibitory neurotransmitter in cns. Binds to and selectively opens cl- channels = hyper polarization of postsynaptic membrane. Harder for postsynaptic neuron to transmit incoming messages to other neurons = depress cns neuronal signalling. Sedative hypnotics: modulate ion channel in brain and spinal cord, but bind to di erent site on cl channel. Result is increase in synaptic inhibition = dampening of neuronal responses (enhance inhibitory e ect of gaba) Mechanism of action: activation of the benzodiazepine receptor increases frequency of opening of cl channel. Motor coordination: impairment of motor coordination, response exaggerated with higher dose. Long term use e ects: vary between individuals. Some can take large amount without evidence of intoxication. Secreted into milk, can result in sedation/death of nursing infant. Low, weaker than barbiturates, alcohol, opioids, and stimulants.

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