Week 5 - CNS Drugs Introduction Flashcards by Christine Parascandola

CNS acting drugs have a major ______/____ and ____ (psychological) importance

therapeutic/clinical, mental

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CNS acting drugs can produce diverse pharmacological & psychological effects. List some examples

 Relief of Pain
 Induction to Anesthesia
 Prevention of Epileptic Seizures
 Treatment of Depression
 Reduction of Anxiety
 Special importance (humans): recreational uses addiction/overdose
(alcohol, tea and coffee, nicotine, cannabis, ecstasy, opioids, cocaine, amphetamines)

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CNS agents are medicines that affect the ___

CNS

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CNS drugs affect the brain’s ____ and _____ of neurotransmitters (NT)

use, output

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Drugs speed up the production of ____

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Drugs slow down _______ of NTs

production

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Drugs mimic ____

NTs

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CNS Drugs: Types

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The Nervous System (NS

divided into CNS and PNS

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The Organization of Nervous System (NS

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Autonomic Nervous System (ANS)

PSNS = rest and digest
Sympathetic = fight or flight

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The BRAIN

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A Nerve is formed of _______ tissue (______ plus blood _______)

nervous, neurons, vessels

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Efferent nerve: nerves that conduct signals _____ the CNS along _____ neurons to their _______ muscles and glands

from, motor, target

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Afferent nerve: carries nerve impulses _____ sensory receptors or sense organs ______ the CNS

from, toward

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Mixed nerve: nerves that contain both _______ and _______ axons, and thus conduct both _______ sensory information and ______ muscle commands in the _____ bundle

afferent, efferent, incoming, outgoing, same

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Spinal nerve: _____ nerve that carries ______, _______, and _____ signals between the spinal cord and the body

mixed, motor, sensory, autonomic

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The building blocks of the CNS are two types of cells: ?

Neurons and Glial cells

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Neurons are specialized nerve cells that can _______ and ____ chemical and electrical signals

receive, transmit

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Glial cells or neuroglia: (support functions)?

 Astrocytes
 Oligodendrocytes (provide myelin for many axons)
 Microglial cells
 Ependymal cells

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The structure of a neuron

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Communication within neurons

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How do Neurons Communicate?

The process is occurring via orchestrated chemical
(release of neurotransmitters) and electrical (alteration of
neuronal membrane potential) actions

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Action potentials are ______ signals carried along neurons

electrical

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Neurotransmitters: the chemical messengers released from ________ neurons so they can “talk” to neighboring cells

presynaptic

The Receptor on the _______ cell is for “hearing” the message

neighboring

Synapses are ______ that allow signals to ____.

junctions, pass

Chemical synapse: * Ionotropic receptors (Ligand-gated ion proteins)

Metabotropic receptors (G-protein coupled proteins) Electrical synapse: * Gap junction proteins

Action potential (AP) (nerve impulse): the change in _____ potential associated with the passage of an ____ ____ the membrane of a neuron

electrical, impulse, along

APs are ?

all-or-nothing (on-off switches)

APs are ____-directional (from the ____ to ____ _____)

one, body, axon terminal

Electrical signal happens when ?

the polarity across their plasma membrane changes

Membrane potential: the differences between ____ and _____ of the cell

inside, outside

Describe a resting potential

Describe an action potential

Voltage-gated ion channels

Changes in polarization occur when ?

ion channels in the membrane open or close, altering the ability of particular types of ions to enter or exit the neuron

Positive potential is defined as?

Depolarization – the opening of channels that let Na+ rush into a neuron The neuron sends electrical signal

Negative potential is defined as?

Hyperpolarization – the opening of channels that let negative ions flow in Prevents the neuron from receiving another stimulus

Electrical and chemical synapses

How Do Neurons Communicate?

Neurotransmitters: Chemical Molecules in the CNS

Small Molecule Transmitters

The neuropeptides are made up of ?

three or more amino acids (larger in size)?

Substance P (__ aa): carries ____ signals and stimulates ____ (high in __)

11, pain, vomiting, VC

Neuropeptide Y: stimulates ___

eating

Endorphins & enkephalins?

inhibit pain

Steroids:

?androgens and estrogens

Dopamine: important in ?

addiction and pleasure-seeking; over-eating, movements, attention and learning, low in Parkinson’s disease

Serotonin: (5-hydroxytryptamine, 5HT). Important for ? Linked with?

sleep, appetite, temperature regulation, mood, anxiety, pain, memory, aggression, and perception. Linked with depression

Acetylcholine: ____ and ___ contractions; blockage causes ____, low in ______

muscle, heart, paralysis, Alzheimer’s

Norepinephrine: involved in body’s ?

emergency response and behavioral processes. Released in (Noradrenalin) stress, excitement. Helps brain work faster, lift our mood, makes us feel alert and focused?

GABA are _____ that keeps neural ______ under control. If disrupted: _____, ______. ____ and ____ boost the action of GABA, make you ____.

inhibitors, communication, seizure, epilepsy, Alcohol, valium, calm

Glycine are ______ that keeps neural communication under control. If disrupted: seizure, epilepsy. Alcohol and valium boost the action of GABA, make you calm

inhibitors

Glutamate: major ______ NT in the CNS, ____ brain functioning, linked to many other pathways, ____ and _____?

excitatory, normal, learning, memory, Anxiety, PTS, OCD, mania, depression, psychosis, schizophrenia

Histamine: ( ______ and ), ?

brain, spinal cord, arousal, attention, feeding behavior, and memory

Substance P: implicated in ?

reproduction, social behaviors, appetite, arousal, pain, reward, and learning and memory

Orexin: (like glutamate): _____ homeostasis. Animals lacking orexin system have ?

energy, narcolepsy and disrupted sleep-wake pattern

The NT-receptor complex may directly regulate the membrane potential by ?

altering permeability of the cell membrane through opening or closing specific ion channels

The NT-receptor complex may initiate a sequence of chemical reactions that ?

alter ion transport across the membrane. Specific intracellular signal molecules are called second messengers

Receptors are the site of ?

action for exogenous DRUGS (usually G protein-coupled receptors, GPCRs

What is the function of the second messenger system?

sustains and amplifies the cellular response to DRUG-RECEPTOR binding?

Neutrotransmitter: Receptor Functions

Functions: * Excitatory PostSynaptic Potentials (EPSP, depolarization leading to action potential) * Inhibitory PostSynaptic Potentials (IPSP, hyperpolarization leading to the “rest” potential)

Examples of neurotransmitters

Glutamate is the main excitatory transmitter in the CNS * GABA is the main inhibitory NT in the adult vertebrate brain * Glycine is the main inhibitory NT in the spinal cord

Whether the effect of a certain NT is excitatory or inhibitory at a given synapse depends on ?

which of its receptor(s) are present on the postsynaptic (target) cell.?

Excitatory?

* Glutamate * Aspartate

Inhibitory

* GABA * Glycine

Mixed?

* Acetylcholine (Ach) * Norepinephrine (NE) * Epinephrine (EP) * Dopamine (D) * Serotonin (5-HT)

Neurotransmitter - Receptor Functions Glutamate, GABA, Acetylcholine, Dopamine, Serotonin

Acetylcholine - Excitatory

Acetylcholine - Inhibitory

CPCRs are?

main targets of existing drugs (30-50-% drugs bind to them)

GPCRs detect molecules ____ the cells and ____ cellular responses

outside, activate

GPCRs regulate ?

sensory (taste, light, smell) and non-sensory (neurological and endocrine) signals

______ comprise the largest family of transmembrane receptors (~ 1000 in humans)

GPCRs

GPCRs are ?

7 transmembrane helixes (7-transmembrane receptors, 7TM- R)

Describe the structure of GPCRs:

7 transmembrane alpha helixes receptors interact (coupled) with trimetic signal-transducing G-proteins G-proteins consist of α, β, and γ subunits 1) Each receptor binds to its ligand, 2) conformational changes 3) α separates from β and γ, 4) they interact with other proteins 5) 2nd messengers (cAMP) act on heart, muscle, vessels