CNS intro, Alcohol,Sed/Hyp, GABA (barbituates, benzos) Flashcards

1
Q

CNS Acetylcholine: involved in (8)

A

learning, memory, cognition, attention, wakefulness, arousal, NMJ, nicotinic/muscarinic receptrs

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2
Q

Acetylcholine degenerates in which dz?

A

Alzheimer’s

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3
Q

Norepinepherine/noradrenaline:

a. involved in:
b. acts on:

A

a. mood, attention, arousal, pain regulation, learning, memory
b. acts on G-protein coupled receptors

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4
Q

Dopamine involved in (4 basic processes)

A

reward
reinforcement
motivation
addiction

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5
Q

Dopamine involved in which 2 diseases

A

Parkinson’s

Schizophrenia

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6
Q

Dopamine receptor

A

G-protein coupled receptor

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7
Q

Dopamine receptors: stimulatory, inhibitory

A

D1=stimulatory

D2=inhibitory

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8
Q

D2 receptor is (stim or inhib?)

A

inhibitory

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9
Q

D1 receptor is (stim or inhib?)

A

stimulatory

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10
Q

Serotonin-5HT: involved in (6)

A
mood
promotes sleep
anxiety
OCD
hunger
appetite
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11
Q

Serotonin receptor type

A

G protein coupled receptors

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12
Q

CNS Monoamines (3)

A

Norepinepherine/noradrenaline
dopamine
serotonin

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13
Q

GABA function

A

(Amino Acid)
major INHIBITORY transmitter in the CNS
relieves anxiety & promotes sedation
ACTIVATION OF GABA RECEPTORS ALLOWS CL INTO THE CELL

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14
Q

Glutamate function

A

(Amino Acid)
major EXCITATORY transmitter in the CNS
involved in memory & learning

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15
Q

Glutamate receptor type(s)

A

a. Ionotropic receptors: NMDA, AMPA

b. Metabotropic receptors- post=excitatory, pre=inhibitory

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16
Q

Neuropeptides & their functions (4)

A
  1. Endogenous opioids (endorphins): ↓pain, ↑pleasure-Mu, kappa, delta
  2. Substance P:excitatory-mediates pain transmssn
  3. Neuropeptide Y: regulates food intake & fat storage
  4. Cannabinoids: memory, cognition, pain perception
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17
Q

Alcohol pharmokinetics

A
  1. absorbed in stomach & small intestine
  2. readily crosses BBB & placental barrier
  3. induces CYP450s
    a. ↑acetaminophen toxicity
    b. inhibits breakdown of benzos, barbituates, TCAs, etc
  4. microsomal ethanol oxidizing system induced w/chronic use
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18
Q

Blood alcohol content determinants

A

based on sex, age, body fat

peaks 30-90 mins after last drink

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19
Q

Alcohol metabolism

A
  • ZERO ORDER kinetics
  • broken down by alcohol dehydrogenase to acetaldehyde & then by aldehyde dehydrogenase to acetate
  • oxidation requires NAD+
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20
Q

Disulfiram action

A

inhibits aldehyde dehydrogenase (necessary for metabolism of alcohol)

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21
Q

Alcohol MOA (4)

A
  1. CNS depressant
  2. binds GABA receptor-↑ Cl influx-enhances GABA transmission
  3. long term=downregulation of GABA receptor (tolerance forms)
  4. inhibits glutamate on NMDA receptors=up regulation of NMDA with chronic use
22
Q

Alcohol CNS effects (LOW DOSES) [6]

A
disinhibition
decreased anxiety
mild euphoria
increased confidence
mood swings
decreased concentration
23
Q

Alcohol CNS effects (HIGH DOSES)

A

motor & judgment impairment
slurred speech
ataxia-sedative properties become apparent

24
Q

Alcohol smooth muscle effects

A

vasodilator

hypothermia

25
Alcohol kidney effects
decreased ADH=diuresis
26
Alcohol ABUSE definition
interference in social life for at least 1 month
27
Alcoholism definition
tolerance AND dependence due to prolonged use CONTINUOUS OR PERIODIC LAC OF CONTROL OVER DRINKING, PREOCCUPATION WITH ALCOHOL, USE DESPITE CONSEQUENCES< DISTORTION OF THINKING (DENIAL)
28
Alcohol kinetics & dynamics
Kinetics: ethanol induces CYP2E1-chronic use increases ethanol metabolism Dynamics: ↓GABA receptors and ↑NMDA receptors – withdrawal due to dynamic tolerance – takes time to reset the receptors
29
Alcohol toxicity symptoms (5)
emesis, stupor, coma, respiratory distress, death
30
Tx of alcohol toxicity
thiamine, manage symptoms, correct electrolyte disturbances, correct hypothermia
31
What is the cause of alcohol hangovers?
buildup of metabolites & dehydration
32
How should you tx a seizure due to alcohol?
control w/benzos
33
Effects of chronic alcohol abuse (8 main categories and their manifestions)
Malnutrition – folate and thiamine deficiency Gastritis and pancreatitis Cardiovascular – arrhythmia, cardiac depression, cardiomyopathy, HTN, stroke Teratogenicity – fetal alcohol syndrome Carcinogenicity – increases carcinogenic effects of tobacco Sexual dysfunction – testicular atrophy, impotence, gynecomastia CNS – Korsakoffs & Wernicke’s – peripheral neuropathy Skeletal muscle atrophy
34
What is the most common dz in alcohol abuse and how does it come about
Liver dz due to oxidative stress, tissue damage, lipid peroxidation by acetaldehyde hepatotoxicity may manifest as: fatty liver, fibrosis, cirrhosis, alcoholic hepatitis, liver cancer
35
TTx of alcohol abuse/dependence should consist of which main elements
psychological AND pharmacologic
36
Naltrexone: MOA, used to tx
blocks opioid receptor-blocks ability of alcohol to stimulate reward pathyways [used in tx of alcoholism]
37
Acamprosate: MOA, used to tx
analogue of GABA, restores GABA glutamate balance | [used in tx of alcoholism]
38
Disulfiram: MOA, how do SEs com about/what are SEs
inhibits acetaldehyde dehydrogenase ACETALDEHYDE builds up=flushing, HA, nausea, confusion can have severe effects
39
What other pharm med might you use in the tx of alcohol use disorders?
antidepressants
40
Alcohol withdrawal manifestation (mild, severe)
CAN BE LIFE THREATENING mild=anxiety, irritability, insomnia, nausea, tachycardia severe=hallucinations, DTs, seizures, arrhythmia, hypotension
41
Alcohol withdrawal treatment aims to prevent
seizures, DTs & arrhythmia
42
Anxiety disorders: description
pervasive feeling of tension or apprehension ANXIETY THAT BECOME CHRONIC AND INTERFERES WITH NORMAL FUNCTION SHOULD BE TREATED!! sxs: palpitations, tremor, perspiration, GI effects, dizziness, headache
43
IDEAL ANXIOLYTIC would do what?
calm without daytime sedation and drowsiness & would not cause physical or psychological dependence
44
Anxiety: benzos?
relieve anxiety without sedation
45
Transient insomnia is due to what & tx how
due to situational stress | most effective tx=sedatives/hypnotics
46
Long term insomnia is due to what & tx how
psychiatric dz, chronic drug abuse | most effective tx=TLC
47
hypersomnia, narcolepsy tx
stimulants
48
enuresis tx
TCAs
49
sleep apnea tx
CPAP, TLC
50
IDEAL SEDATIVE/HYPNOTIC should
allow the person to fall aspeep quickly, stay asleep, without a drug hanglover and has a high margin of safety without effect on the REM sleep