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

4Qpharm3-test1 > CNS intro, Alcohol,Sed/Hyp, GABA (barbituates, benzos) > Flashcards

Flashcards in CNS intro, Alcohol,Sed/Hyp, GABA (barbituates, benzos) Deck (50):
1

CNS Acetylcholine: involved in (8)

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

2

Acetylcholine degenerates in which dz?

Alzheimer's

3

Norepinepherine/noradrenaline:
a. involved in:
b. acts on:

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

4

Dopamine involved in (4 basic processes)

reward
reinforcement
motivation
addiction

5

Dopamine involved in which 2 diseases

Parkinson's
Schizophrenia

6

Dopamine receptor

G-protein coupled receptor

7

Dopamine receptors: stimulatory, inhibitory

D1=stimulatory
D2=inhibitory

8

D2 receptor is (stim or inhib?)

inhibitory

9

D1 receptor is (stim or inhib?)

stimulatory

10

Serotonin-5HT: involved in (6)

mood
promotes sleep
anxiety
OCD
hunger
appetite

11

Serotonin receptor type

G protein coupled receptors

12

CNS Monoamines (3)

Norepinepherine/noradrenaline
dopamine
serotonin

13

GABA function

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

14

Glutamate function

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

15

Glutamate receptor type(s)

a. Ionotropic receptors: NMDA, AMPA
b. Metabotropic receptors- post=excitatory, pre=inhibitory

16

Neuropeptides & their functions (4)

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

17

Alcohol pharmokinetics

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

18

Blood alcohol content determinants

based on sex, age, body fat
peaks 30-90 mins after last drink

19

Alcohol metabolism

-ZERO ORDER kinetics
-broken down by alcohol dehydrogenase to acetaldehyde & then by aldehyde dehydrogenase to acetate
-oxidation requires NAD+

20

Disulfiram action

inhibits aldehyde dehydrogenase (necessary for metabolism of alcohol)

21

Alcohol MOA (4)

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

Alcohol CNS effects (LOW DOSES) [6]

disinhibition
decreased anxiety
mild euphoria
increased confidence
mood swings
decreased concentration

23

Alcohol CNS effects (HIGH DOSES)

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

24

Alcohol smooth muscle effects

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