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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
how does alcohol cause damage
``` increased oxidative stress depletion of glutathione damage to mito growth factor dysregulation potentiation of cytokine-induced injury ```
26
chronic alcohol and esophagus
``` esophageal dysfnx esophageal reflux barrets esophagus traumatic rupture mallory-weiss tears CA ```
27
chronic alcohol and stomach
disrupt mucosal barrier -> acute and chronic gastritis | beverages containing >40% alcohol direct toxic effect
28
chronic alcohol and intestines
chronic diarrhea -> malabsorption -> deficiencies vit Bs osteoporosis low magnesium
29
chronic alcohol and neurotoxicity
``` peripheral nn parasthesias ataxia dementia and demylinating disease wernicke-korsakoff blurring vision ```
30
chronic alcohol and CV
``` dilated cardiomyopahty w/ventricular hypertrophy and fibrosis arrhythmia's HTN CHD stoke ```
31
chronic alcohol and endocrine
unbalance of steroids -> gynecomastia and testicular atrophy
32
FAS
``` intrauterine growth retardation microcephaly poor coordination underdevelopment of midfacial region minor joint abnormalities -fetus has little-no ADH activity ```
33
alcohol DDIs
increased CYP450s additive CNS depression other drugs can inhibit ALDH (metronidazole, trimethoprim)
34
management of acute alcohol intoxication
prevention of severe respiratory depression and aspiration of voitus glucose to Tx hypoglycemia and ketosis thiamine K if severe vomiting
35
management of alcohol withdrawal
electrolyte rebalancing and thiamine therapy | long or short acting benzos
36
long acting benzos
``` chlordiazepoxide cloraxepate diazepam less frequent dosing and built in tapering effect bad for ppl w/bad livers ```
37
short acting benzos
lorazepam oxazepam can be given to those w/bad livers
38
naltrexone
MOA: u opioid R antagonist use: Tx of alcohol and opioid addiction CI: acute hepatitis, liver failure must be opioid free before administration
39
acamprosate
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
off label drugs for alcohol dependance
topiramate | odansetron
41
methanol poisoning symptoms and Tx
common symptom blurred vision - respiratory support - suppression of metabolism by ADH (ethanol and fomepizole) - hemodialysis - alkalinization to counteract acidosis
42
ethylene glycol Tx
hemodialysis ethanol infusion fomepizole
43
opioid R anatagonisits
naloxone | naltrexone
44
synthetic opioid
methadone
45
partial u-opioid R agonist
buprenorphine
46
nictotinic R partial agonist
varenicline
47
NMDA R antagonist
acamprosate
48
cannabinoid R agonist
rimonabant | not approved in US
49
3 classes of molecular targets for mesolimbic system
Gio coupled Rs ionotropic Rs monoamine transporters
50
nonaddictive drugs of abuse
``` LSD mescaline psilocybin PCP ketamine ```
51
LSD, mescaline, psilocybin
repetitive exposure leads to rapid tolerance (tachyphylaxis) | animals will not self administer hallucinogens -> not addictive
52
long term effects of the nonaddictive drugs
PCP- irreversible schizo like psychosis | LSD- flashbacks for years
53
drugs that activate Gio
opioids cannabinoids CHB (liquid ecstasy or date rape drug)
54
opiods
in VTA bind u opioid Rs -> decrease GABA -> disinhibit dopaminergic neurons
55
withdrawal of opioids
intense dysphoria, nausea, vomiting, mm aches, lacrimation, rhinorrhea, mydiasis, piloerection, sweating, diarrhea, yawning, fever
56
naloxone
MOA: pure opiod antagonist that reverses effects of a dose of opiates w/in min provokes an acute withdrawal syndrome
57
methadone, buprenorphine
long acting opioids used for substiution therapy tolerance and physical dependence develop slower then others given w/supervision abrupt discontinuation -> withdrawal
58
canabinoids
retrograde messengers | THC- disinhibiits DA neurons by inhibiting GABA
59
dronabinol
FDA approved THC analog used for anorexia and weight loss in AIDs and CA
60
nabilone
THC analog used for refractory nausea and vomiting associated w/CA chemo and adjunct in chronic pain
61
GHB
activates GABAbR w/low affinity euphoria, enhances sensory, social closeness, amnesia, sedation, coma liquid ex, or date rape
62
drugs that mediate via ionotropic Rs
nicotine benzos and barbituates alcohol inhalants
63
nicotine
MOA: selective agonist of the nAChR on DA neurons in VTA | activation fulfills the DA requirement of addictive drugs
64
Tx for nicotine
nicotine buproprion (antidepressent) varenicline ( partial nAChR agonist)
65
inhalants
most produce euphoria unknown MOA overdose is supportive care
66
drugs that bind transporters of biogenic amines
bind some combo of DAT, NET, VMAT, SERT cocaine amphetamines ectascy
67
cocaine
- 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
symptoms of cocaine
``` 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
amphetamines MOA
- 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
withdrawal of amphetamines
dysphoria, drowsiness, general irritability
71
ecstasy MOA
similar to amphetamines | preferential affinity for SERT and strongly increases the extracellular concentration of serotonin
72
toxic effects of ecstasy
hyperthermia dehydration serotonin syndrome seizures

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