depressants Flashcards

1
Q

major inhibitory NT in CNS

A

GABA

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2
Q

Barbiturates absorption

A

small intestine

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3
Q

Barbiturates distribution

A

highly lipid soluble

fast rate of entry into CNS

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4
Q

Barbiturates metabolism

A

slow

induce hepatic drug-metabolizing enzymes (Rx interactions)

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5
Q

Barbiturates MOA

A

bind GABA-A receptor
increases duration of channel opening

high conc: directly activate
hella high conc: decrease release of other NTs

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6
Q

Barbiturates effects

A
CNS depression
low therapeutic index
hypotension
anticonvulsant activity
not analgesic
reduce REM sleep
induce own metabolism
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7
Q

Barbiturates dependence

A

psychological
physical

status epilepticus

abrupt withdrawal is life-threatening

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8
Q

Methohexital

A

ultra-short acting BARB

anesthesia
short procedures

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9
Q

Secobarbital

Pentobarbital

A

short/intermediate acting BARB

sedation
insomnia

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10
Q

Phenobarbital

A

long acting BARB

epilepsy

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11
Q

Barbiturates SE

A

CNS depressant
OD: death
contraindicated in acute intermittent porphyria

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12
Q

Barbiturates Rx interactions

A

additive effects w/CNS depressants
cross-tolerance w/CNS depressants
induction of P450

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13
Q

Ethanol absoprtion

A

GI tract

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14
Q

Ethanol distribution

A

cross BBB

cross placenta

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15
Q

Ethanol metabolism

A

liver
unchanged in urine
sweat

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16
Q

alcohol dehydrogenase

A

oxidizes ethanol to acetaldehyde

17
Q

acetaldehyde dehydrogenase

A

oxidizes acetaldehyde to acetate

18
Q

Ethanol MOA

A

dissolves in neuronal embranes
enhances GABA inhibition
inhibits NMDA Glu-ergic

19
Q

Ethanol effects

A
CNS depression
heat loss (hypothermia)
vasodilation
depress myocardial contractility
stimulates gastric secretions
decreases testosterone
inhibits ADH secretion
20
Q

Ethanol dependence

A

psychological
physical

withdrawal: early awakening, anxiety, tremor, can be life-threatening

21
Q

delirium tremens

A

full-blown alcohol withdrawal syndrome

tremors, motor agitation, anxiety, hyperexcitability, hyperactivity, hyperthermia, hallucinations, toxic psychosis, seizures, death

15% chronic users

Tx: diazepam/clonazepam

22
Q

Ethanol SE

A
blackouts
death by hypothermia
peripheral nerve damage
cerebellar cortical degeneration
macrocytic anemia
iron deficiency
GI bleeding
nutritional deficiencies
pancreatitis
fatty liver
cirrhosis 15%
slow metabolism of other drugs
23
Q

Wernicke-Korsakoff syndrome

A

alcoholic encephalopathy
thiamine deficiency

confusion, abnormal ocular motility, ataxia, polyneuropathy, learning/memory problems

24
Q

fetal alcohol syndrome

A

deformities of face/head (midline), hydrocephaly, holoprosencephaly, prenatal growth deficiency, postnatal growth deficiency

25
Q

Ethanol Rx interactions

A

additive effect

acute: inhibit metabolism of other drugs
chronic: increase rate of drug metabolism

26
Q

Ethanol Tx

A

1) detoxification

2) abstinence

27
Q

Disulfiram

A

inhibits acetaldehyde dehydrogenase

28
Q

Methanol

A

acidosis, optic nerve damage, blindness

Tx: sodium bicarbonate, ethanol

29
Q

alcohol dehydrogenase

A

0th order kinetics