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drugs of alcohol and drug abuse Flashcards

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1
Q

drugs for Tx of acute alcohol withdrawal syndrome

A

diazepam
lorazepam
oxazapam
thiamine

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2
Q

drugs for prevention of alcohol abuse

A

acamprosate
disulfiram
naltrexone

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3
Q

drugs for Tx of acute methanol or ethylene glycol poisoning

A

ethanol

fomepizole

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4
Q

alcohol abuse

A

use of alcohol in dangerous situations or use of alcohol in spite of adverse consequences

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5
Q

alcohol dependence

A

all of characteristics of alcohol abuse plus physical dependance

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6
Q

protective genetic factors

A

polymorphisms in alcohol dehydrogenase and aldehyde dehydrogenase are protective against alcohol dependance

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7
Q

susceptible genetic factors

A

D4R, GABAaR, tyrosine hydroxylase

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8
Q

absorption of alcohol

A

peak at 30min
mostly absorbed in small intestines
extensive first pass

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9
Q

meta of alcohol

A

zero order kinetics

7-10g of alcohol/hr

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10
Q

alcohol dehyrogenase (ADH)

A

cytosolic enzyme converts ethanol to acetaldehyde and is located primarily in liver
NAD requires
aspirin inhibits gastric ADH and can increase ethanol bioavailability

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11
Q

Fomepizole

A

inhibits ADH and is used in Tx of acute methanol or ethylene glycol poisoning

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12
Q

aldehyde dehydrogenase (ALDH)

A

mitochondrial enzyme converts aldehyde to acetic acid

NAD required

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13
Q

NAD with alcohol meta

A

2mol of NAD for every mol of ethanol

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14
Q

disulfiram

A 
inhibits ALDH 
used to Tx pts with alcohol dependance b/c build up of acetaladehyde causes lots of adverse effects
not used often d/t poor pt compliance
effects up to 14 days after last dose
hepatotoxic
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15
Q

microsomal ethanol oxidizing system (MEOS)

A

chronic alcohol consumption induces MEOS activity and can result in enhanced activation of toxins, free radicals, and hydrogen peroxide

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16
Q

intoxication level

A

80mg/dl = .08% BAC

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17
Q

BAC 50-100

A

sedation, subjective ‘high’, slower rxn time

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18
Q

100-200

A

impaired motor fnx, slurred speech, ataxia

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19
Q

200-300

A

emesis, stupor

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20
Q

300-400

A

coma

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21
Q

> 500

A

respiratory depression, death

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22
Q

alcohol effects on ion Ch in CNS

A

decreases NMDAR activity

increases GABAR activity

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23
Q

alcohol effects heart

A

decreased contractility when BAC >100

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24
Q

alcohol on smooth mm

A

vasodilation and mm relaxation

severe overdose hypothermia d/t vasodilation can occur

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25
Q

how does alcohol cause damage

A 
increased oxidative stress
depletion of glutathione
damage to mito
growth factor dysregulation
potentiation of cytokine-induced injury
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26
Q

chronic alcohol and esophagus

A 
esophageal dysfnx
esophageal reflux
barrets esophagus
traumatic rupture 
mallory-weiss tears
CA
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27
Q

chronic alcohol and stomach

A

disrupt mucosal barrier -> acute and chronic gastritis

beverages containing >40% alcohol direct toxic effect

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28
Q

chronic alcohol and intestines

A

chronic diarrhea -> malabsorption -> deficiencies
vit Bs
osteoporosis
low magnesium

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29
Q

chronic alcohol and neurotoxicity

A 
peripheral nn parasthesias
ataxia
dementia and demylinating disease
wernicke-korsakoff
blurring vision
30
Q

chronic alcohol and CV

A 
dilated cardiomyopahty w/ventricular hypertrophy and fibrosis
arrhythmia's
HTN
CHD
stoke
31
Q

chronic alcohol and endocrine

A

unbalance of steroids -> gynecomastia and testicular atrophy

32
Q

FAS

A 
intrauterine growth retardation
microcephaly
poor coordination
underdevelopment of midfacial region
minor joint abnormalities 
-fetus has little-no ADH activity
33
Q

alcohol DDIs

A

increased CYP450s
additive CNS depression
other drugs can inhibit ALDH (metronidazole, trimethoprim)

34
Q

management of acute alcohol intoxication

A

prevention of severe respiratory depression and aspiration of voitus
glucose to Tx hypoglycemia and ketosis
thiamine
K if severe vomiting

35
Q

management of alcohol withdrawal

A

electrolyte rebalancing and thiamine therapy

long or short acting benzos

36
Q

long acting benzos

A 
chlordiazepoxide
cloraxepate
diazepam
less frequent dosing and built in tapering effect
bad for ppl w/bad livers
37
Q

short acting benzos

A

lorazepam
oxazepam
can be given to those w/bad livers

38
Q

naltrexone

A

MOA: u opioid R antagonist
use: Tx of alcohol and opioid addiction
CI: acute hepatitis, liver failure
must be opioid free before administration

39
Q

acamprosate

A

MOA: weak NMDAR antagonist and GABAR agonist
reduces short and long term relapse rates when combo w/psychotherapy
caution in renal disease
ADRs:GI and rash
can be combo w/naltrexone and disulfiram

40
Q

off label drugs for alcohol dependance

A

topiramate

odansetron

41
Q

methanol poisoning symptoms and Tx

A

common symptom blurred vision

  • respiratory support
  • suppression of metabolism by ADH (ethanol and fomepizole)
  • hemodialysis
  • alkalinization to counteract acidosis
42
Q

ethylene glycol Tx

A

hemodialysis
ethanol infusion
fomepizole

43
Q

opioid R anatagonisits

A

naloxone

naltrexone

44
Q

synthetic opioid

A

methadone

45
Q

partial u-opioid R agonist

A

buprenorphine

46
Q

nictotinic R partial agonist

A

varenicline

47
Q

NMDA R antagonist

A

acamprosate

48
Q

cannabinoid R agonist

A

rimonabant

not approved in US

49
Q

3 classes of molecular targets for mesolimbic system

A

Gio coupled Rs
ionotropic Rs
monoamine transporters

50
Q

nonaddictive drugs of abuse

A 
LSD
mescaline
psilocybin
PCP
ketamine
51
Q

LSD, mescaline, psilocybin

A

repetitive exposure leads to rapid tolerance (tachyphylaxis)

animals will not self administer hallucinogens -> not addictive

52
Q

long term effects of the nonaddictive drugs

A

PCP- irreversible schizo like psychosis

LSD- flashbacks for years

53
Q

drugs that activate Gio

A

opioids
cannabinoids
CHB (liquid ecstasy or date rape drug)

54
Q

opiods

A

in VTA bind u opioid Rs -> decrease GABA -> disinhibit dopaminergic neurons

55
Q

withdrawal of opioids

A

intense dysphoria, nausea, vomiting, mm aches, lacrimation, rhinorrhea, mydiasis, piloerection, sweating, diarrhea, yawning, fever

56
Q

naloxone

A

MOA: pure opiod antagonist that reverses effects of a dose of opiates w/in min
provokes an acute withdrawal syndrome

57
Q

methadone, buprenorphine

A

long acting opioids used for substiution therapy
tolerance and physical dependence develop slower then others
given w/supervision
abrupt discontinuation -> withdrawal

58
Q

canabinoids

A

retrograde messengers

THC- disinhibiits DA neurons by inhibiting GABA

59
Q

dronabinol

A

FDA approved THC analog used for anorexia and weight loss in AIDs and CA

60
Q

nabilone

A

THC analog used for refractory nausea and vomiting associated w/CA chemo and adjunct in chronic pain

61
Q

GHB

A

activates GABAbR w/low affinity
euphoria, enhances sensory, social closeness, amnesia, sedation, coma
liquid ex, or date rape

62
Q

drugs that mediate via ionotropic Rs

A

nicotine
benzos and barbituates
alcohol
inhalants

63
Q

nicotine

A

MOA: selective agonist of the nAChR on DA neurons in VTA

activation fulfills the DA requirement of addictive drugs

64
Q

Tx for nicotine

A

nicotine
buproprion (antidepressent)
varenicline ( partial nAChR agonist)

65
Q

inhalants

A

most produce euphoria
unknown MOA
overdose is supportive care

66
Q

drugs that bind transporters of biogenic amines

A

bind some combo of DAT, NET, VMAT, SERT
cocaine
amphetamines
ectascy

67
Q

cocaine

A
  • in PNS cocaine inhibits VNaCh and can be used as local anesthetic
  • blocks DAT and increases DA concentrations in nucleus accumbens
  • blocks NET and activated SNS
68
Q

symptoms of cocaine

A 
loss of appetite, hyperactivity, lack of sleep
overdose- hyperthermia, coma, death
withdrawal not as severe as other opiods
reverse tolerance can occur
Tx supportive care
69
Q

amphetamines MOA

A
  • taken up by DAT
  • block VMAT and deplete synaptic vesicles of NT
  • increasing cytoplasmic levels of NT cause release of NT reversing action of biogenic amine transporters
70
Q

withdrawal of amphetamines

A

dysphoria, drowsiness, general irritability

71
Q

ecstasy MOA

A

similar to amphetamines

preferential affinity for SERT and strongly increases the extracellular concentration of serotonin

72
Q

toxic effects of ecstasy

A

hyperthermia
dehydration
serotonin syndrome
seizures

Psych (8 decks)

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