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Drugs that act in the central nervous system (1). Introduction to the pharmacology of CNS drugs. Cortex ( 皮质 ). evolutionally formed last receiving and processing information, control of sight, listening, movement, memory, wake, autonomic function. Limbic system ( 边缘系统 ).
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Cortex(皮质) • evolutionally formed last • receiving and processing information, control of sight, listening, movement, memory, wake, autonomic function
Limbic system(边缘系统) A group of interconnected deep brain structures, common to all mammals, and involved in olfaction, emotion, motivation, behavior, and various autonomic functions.
limbic system边缘系统: hippocampus海马、amygdala杏仁、septal area膈区、basal ganglia基底节
Cerebellum(小脑) responsible for the regulation and coordination of complex voluntary muscular movement as well as the maintenance of posture and balance. The cerebellum has been reported to play a role in psychiatric conditions such as schizophrenia, autism, mood disorders, dementia, and attention deficit hyperactivity disorder(ADHD).
Diencephalon(间脑) The diencephalon is a complex of structures within the brain, whose major divisions are the thalamus and hypothalamus. It functions as a relay system between sensory input neurons and other parts of the brain, as an interactive site for the central nervous and endocrine systems, and works in tandem with the limbic system.
central part of the brain, under the cortex and basal ganglion and above the hypothalamus relay station of senses
hypothalamus下丘脑 :integrative area of autonomic nerve regulation of temperature, water balance, metabolism, blood pressure, circadian rhythm, sex activity, sleeping, etc
tegmentum(被盖),ascending reticular activating system, NTS, area postrema regulation of sleeping, wake, eye movement, vomiting, cardiovascular and respiratory reflex
Spinal cord脊髓: pathways of senses and movement;autonomic reflex
mesolimbic pathway: memory and motivating behaviors mesocortical pathway: thinking and schizophrenia nigrostriatal pathway: motor control tuberoinfundibular pathway: hormones secretion
Cellular organization of the brain 1012 neurons 1014 synapses complex net
Ion channels and receptors 1, voltage-gated channels: fast responses 2, ligand-gated channels (ionotropic receptors 离子型受体) 3,metabotropic receptors(促代谢型受体), G protein related, indirectly modulate the voltage-gated channels: slow, diversity
Pre-synaptic action potential→voltage-sensitive calcium channels → Ca2+ into the terminals → transmitter release → acting at the receptors post-synaptically → EPSP or IPSP
Sites of drug action 1, presynaptic action potential 2, synthesis 3, storage 7, degradation 4, metabolism 8, receptor 5, release 9, ionic conductance 6, reuptake
Cellular organization of the brain 1012 neurons 1014 synapses complex net
neurotransmitters at central synapses Ach: acetylcholine NA: noradrenaline DA: dopamine 5-HT: serotonin; 5-hydroxytrptamine GABA: γ-aminobutyric acid glutamate
Opioid peptides 阿片样肽 Histamine 组胺 Prostaglandins 前列腺素 Tackykinins 速激肽 Glycine 甘氨酸 Adenosine 腺苷
Modulators 调质: to modulate the response of a neuron to a neurotransmitter or hormone Transmitter and modulator, action changeable sometimes
Chapter 11 General anesthetics 全身麻醉药 General anaesthesia全麻: a state characterized by unconsciousness, analgesia, amnesia, skeletal muscle relaxation and loss of reflexes. different from pain relieving
针灸、冷冻 • 公元前五世纪(战国时代):扁鹊,记载中药麻醉,无从考证 • 公元前二世纪,华陀,麻沸散刮骨疗毒;曼陀罗主要成分东莨菪碱,中枢抑制作用 • 十九世纪中叶前,国外放血造成休克昏迷行手术;压迫肢体致发麻、冷冻止痛 • 十九世纪三十年代,国外捆绑或抓住病人进行手术 • 太监,醉酒,或敲头致昏
inhaled anesthetics • enflurane(恩氟烷), isoflurane(异氟烷), desflurane(地氟烷), sevoflurane(七氟烷), nitrous oxide(氧化亚氮) • ether(乙醚), cyclopropane(环丙烷) flammable, no longer used clinically now
O O N N N Nitrous oxide 氧化亚氮 (笑气) Nitric oxide 一氧化氮 (递质)
airway→alveoli →blood →brain • airway←alveoli ←blood ←brain
blood:gas partition coefficient blood/gas partition coefficient is the ratio of the amount dissolved in blood to the amount in the same volume of gas in contact with that blood. The more blood-soluble the agent (high blood-gas partition coefficient), the slower the onset of effect and the slower the patient goes to sleep new inhaled anesthetics have low partition coefficient
MAC(minimum alveolar concentration):the anesthetic concentration that produces immobility in 50% of patients exposed to a noxious stimulus.
mechanism To be demonstrated action: depressing spontaneous and evoked activity of neurons