CNS N27 Flashcards

1
Q

Major site for drug toxicity

A

CNS

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2
Q

Empirical approach to drugs

A

stumble upon a drug that treats symptoms, leads to research on mechanism of underlying disease

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3
Q

Rational approach to drugs

A

know mechanism of disease, develop drugs to treat disease

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4
Q

Lipophilic drugs for CNS

A

brain is 50% fat, so most drugs are lipophilic

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5
Q

Brain receives _____ of cardiac output

A

high percentage

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6
Q

Blood Brain Barrier

A

tight junctions of endothelial cells + foot pedicels of astrocytes

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7
Q

Blood Brain Barrier inhibits particle diffusion for which 3 characteristics

A

Size (< 1000)
Charge (neutral)
Metabolic susceptibility (not metabolized by MAO and COMT)

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8
Q

Drugs mainly cross the BBB by

A

simple diffusion; they are small (<1000), uncharged, lipid soluble, resistant to metabolic breakdown

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9
Q

2 types of cells found in the brain

A

Glia and Neurons

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10
Q

Glia

A

support neurons + complex role

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11
Q

Neurons

A

processing of information; drugs work by altering neuronal function

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12
Q

Electrical Conduction

A

along cell surface and axon

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13
Q

Transmission

A

across synapses via neurotransmitters

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14
Q

3 types of signal transmission

A
Adenylate Cyclase (cAMP)
Phosphoinositide (IP3)
Alteration of intracellular ion conc. (Na, Ca, K , Cl)
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15
Q

Agonist

A

drugs that mimic the action of a transmitter

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16
Q

Antagonist

A

drugs that block the receptor

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17
Q

Enhancers of reducer drugs

A

enhance or reduce the effects of transmitters

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18
Q

Example of an agonist

A

Beta-agonist that mimics epinephrine to increase the rate or force of contraction

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19
Q

Example of an antagonist

A

Beta-antagonist (propranolol) competitively blocks the epinephrine receptor and prevents actions of epinephrine and other agonists

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20
Q

GABA receptor mechanism

A

GABA binds receptor –> Cl channels open –> influx of Cl –> hyperpolarization –> decreased neuronal firing

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21
Q

Benzodiazepines

A

used in anxiety, as sedative, anticonvulsant, muscle relaxant; bind a distinct receptor on the Cl channel and enhance the effect of GABA

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22
Q

Barbituates

A

may also enhance GABA

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23
Q

Dopamine Mechanism

A

synthesized from tyrosine, AP –> release of DA into cleft–> effect in target cell–> terminated by reuptake

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24
Q

I-DOPA effect Dopamine by

A

effecting the uptake and synthesis (increasing DOPA action)

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25
Q

Amphetamines effect Dopamine by

A

stimulating release

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26
Q

Cocaine effect Dopamine by

A

preventing reuptake

27
Q

Reserpine effect Dopamine by

A

interferes with storage

28
Q

MAO inhibitors effect Dopamine by

A

preventing breakdown of DA

29
Q

Bromocryptine

A

Agonist to the postsynaptic receptor

30
Q

Haloperidol

A

antagonist to the postsynaptic receptor

31
Q

Methylxanthenes (caffeine)

A

many effects on postsynaptic cell (increased cAMP)

32
Q

Neurotransmitter criteria

A

present in presynaptic cell, release upon stimulation, stimulation of nerve has consistent effect, antagonists must block the effects, means of terminating action of agent

33
Q

Neurotransmitter: Catecholamines

A

Norepinephrine, epinephrine, dopamine

34
Q

Neurotransmitter: Indolamines

A

serotonin

35
Q

Neurotransmitter: Amino acids

A

GABA, glycine, aspartic acid, glutamic acid

36
Q

Neurotransmitter: AcH and histamine

A

acetylcholine and histamine

37
Q

Neurotransmitter: Opioid Peptides

A

met enkephalin, leu enkephalin, beta-endorphin, dynorphin

38
Q

Miscellaneous Neurotransmitters

A

Substance P, vasoactive intestinal peptide (VIP), cholecystokinin (CCK)

39
Q

Neuromodulator

A

influences neuronal function but is not considered a neurotransmitter (prostaglandins, peptides)

40
Q

Neurohormones

A

released from neurons and act as endocrine hormones (beta-endorphin)

41
Q

Acetylcholine receptors

A

Nicotinic and muscarinic

42
Q

Acetylcholine locations

A

CNS, preganglionic ANS, postganglionic PSN

43
Q

Dopamine receptors

A

D1-D5

44
Q

Dopamine locations

A

brainstem, coritcal, limbic, extrapyramidal, and endocrine areas

45
Q

Serotonin receptors

A

5-HT1 - 5-HT3

46
Q

Serotonin location

A

pons, midbrain, reticular formation

47
Q

function of Acetylcholine

A

learning, memory, ANS

48
Q

Function of Dopamine

A

complex thought, motor function, regulation, reward mechanism, mood

49
Q

Function of Serotonin

A

Sleep-wake cycle, feeding, sensory processing, mood

50
Q

Chronic use of drugs leads to 2 things

A

drug tolerance and drug dependence

51
Q

Drug tolerance

A

decreased sensitivity to drug

52
Q

Pharmacokinetic (drug dispositional) tolerance

A

induction of enzymes that metabolize the drug

53
Q

Pharmacodynamic tolerance

A

changes in sensitivity to dugs due to change sin the number of receptors or changes in the sensitivity of the receptor-effector mechanism

54
Q

Drug Dependance

A

Physiological changes in the body that occur with drug use, so that when the drug is stopped physical withdrawal signs occur

55
Q

Drug Addiction

A

drug use interferes with life

56
Q

Physical and Psychological dependence

A

Once believed to be separate, but now believed to be interrelated

57
Q

Physical Dependence

A

physiological adaptation to chronic drug exposure (tolerance also occurs (pharmacodynamic and pharmacokinetics))

58
Q

Cross dependence

A

use of a lesser drug to prevent withdrawal symptoms from a more severe drug

59
Q

Cross tolerance

A

tolerance to 1 drug may cause tolerance to another drug to increase

60
Q

Sympathomimetic effects

A

drugs may affect CNS and periphery; stimulation of NE in CNS will also cause STIMULUATION of NE in the SNS

61
Q

Sympatholytic effects

A

drugs that inhibit NE transmission in the CNS may also cause INHIBITION of NE in the SNS

62
Q

Parasympathomimetic effects

A

increased cholinergic transmission in CNS and increased cholinergic transmission of PNS

63
Q

Parasympatholytic effects

A

decreased cholinergic transmission in CNS and decreased cholinergic transmission in PNS