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Pharmacology Test #6 > Substance Abuse > Flashcards

Substance Abuse Flashcards

1
Q

Physical dependence

A

withdrawal signs occur upon discontinuation; can be physically dependent but not addicted

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2
Q

Psychological dependence

A

Addiction; compulsive drug use; drug seeking, craving, despite negative consequences

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3
Q

Tolerance

A

higher doses are required to elicit the same effect, functional changes in receptors or drug metabolism; reflects adaptive changes the body has made to compensate for the drug’s presence

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4
Q

Withdrawal

A

signs of symptoms occurring as a result of drug discontinuation

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5
Q

All abused drugs active which dopamine pathway?

A

all abused drugs activate the mesolimbic DA pathway, causing release of DA in forebrain structures such as the NAc and PFC

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6
Q

How is dopamine usually used in the brain?

A

dopamine is normally used as a learning signal in the brain (signaling the difference between expected and actual reward)

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7
Q

Addiction to drugs is what type of learning?

A

maladaptive learning, often stronger than “natural rewards”

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8
Q

Precipitated withdrawal

A

pharmacologically-induced onset of withdrawal; often worse than normal withdrawal because some or all the receptors are blocked at once

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9
Q

Example of precipitated withdrawal

A

buprenorphine can induced precipitated withdrawal to opioids such as heroin

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10
Q

Conditioned withdrawal

A

withdrawal (and possible drug seeking) brought on or exacerbated by environmental cues

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11
Q

What did the controlled substance ace of 1970 establish?

A

established schedules for controlled substances

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12
Q

Alcohol used recreationally for

A

anxiolytic and euphoria

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13
Q

Other uses of alcohol besides recreationally

A

disinfectant, analgesic, organic solvents

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14
Q

How do you define alcoholism?

A

If it interferes with daily life, if you continue to do it even though it negatively impacts your life

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15
Q

Differences in distribution of alcohol between men and women

A

Men have 58% body water whereas women have 48% , so men can dilute it more and therefore drink more

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16
Q

What type of kinetics is alcohol eliminated by?

A

eliminated with zero order kinetics (constant rate)

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17
Q

Acute tolerance of alcohol

A

intoxication greater when BAC is ascending versus descending

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18
Q

Chronic tolerance of alcohol

A

greater concentrations needed to achieve desired effect

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19
Q

Fomepizol inhibits

A

Alcohol dehydrogenase (ADH)

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20
Q

Disulfiram inhibits

A

Aldehyde dehydrogenase (ALDH)

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21
Q

Fomepizol is used to treat

A

methanol, ethylene glycol poisoning

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22
Q

Disulfiram is used for

A

used for motivated drinkers; sensitizes a person to ethanol; disuades ethanol use during abstinence

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23
Q

Describe alcohol metabolism

A
  1. Ethanol is metabolized to acetaldehyde by alcohol dehydrogenase
  2. Acetaldehyde is metabolized to acetate by aldehyde dehydrogenase
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24
Q

CNS targets of alcohol

A
  1. GABA(A) receptor potentiator (hyperpolarizes neuronal membrane, inhibits firing)
  2. NMDA receptor antagonist (inhibits excitatory aa receptor)
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25
Q

What contributes to the CNS depression, cognitive deficits and memory impairment seen with alcohol?

A

NMDA receptor antagonism

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26
Q

Effects of the CNS targets of alcohol

A
  1. Mild CNS stimulation (disinhibition)
  2. CNS depression
  3. Cognitive impairment
  4. Motor impairment
  5. Coma, death
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27
Q

Acute organ toxicity from alcohol

A
  1. CNS: sedation, ataxia, intoxication

2. Cardiovascular: vasodilation, CV depression

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28
Q

Chronic organ toxicity from alcohol

A
  1. CNS: tolerance, physical dependence, nerve injury
  2. CV: prevent coronary disease, cardiomyopathy, arrhythmias, hypertension
  3. Liver/GI: liver disease (cirrhosis)
  4. Cancer: mouth, pharynx, larynx, esophagus, liver
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29
Q

Drug interactions with alcohol

A
  1. Synergy with CNS depressants
  2. Inhibits metabolism of phenothiazines, TCAs, sedative-hypnotics
  3. Disulfiram
  4. Acetaminophen (promotes liver damage by NAPQI)
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30
Q

Contraindications for alcohol use

A
  1. Liver disease
  2. Peptic ulcers: ethanol is a secretagogue
  3. Epilepsy: ethanol changes neuronal excitability
31
Q

Treatment of ethanol intoxication

A

support respiration, prevent aspiration when at 300-500 mg/dl

32
Q

Treatment of Methanol and ethylene glycol toxicity

A

fomepizole or ethanol, hemodialysis

33
Q

General treatment of alcoholism

A
  1. Detoxification (ethanol abstinence syndrome)

2. Psycho-social and drug therapy

34
Q

Treatment of ethanol abstinence syndrome

A
  1. prevent seizures, delirium, arrhythmias
  2. maintain potassium, magnesium, phosphate balance
  3. Thiamine to prevent Wernicke-Korsakoff syndrome
  4. Substitute benzodiazepine for alcohol initially, then taper
  5. Antidepressants for mood
35
Q

Naltrexone

A

mu, kappa opioid antagonist; attenuates alcohol’s action

36
Q

Acamprosate

A

GABA system activator; NMDA antagonist; substitutes for some of alcohol’s actions

37
Q

Ondansetron

A

5HT3 antagonism for emesis

38
Q

Topiramate

A

anticonvulsant

39
Q

Vaclofen

A

GABA(b) antagonism

40
Q

Varenicline

A

nAChR partial agonist

41
Q

Endogenous cannabinoids

A

2-arachidonyl glycerol (2-AG) and anandamide

42
Q

Endogenous cannabinoids involved with which processes in the body?

A

memory, appetite, synaptic transmission

43
Q

How does marijuana cause euphoria?

A

perhaps via disinhibition of the DA system and other NT systems

44
Q

MOA of THC

A

Activates CB1 receptors on VTA GABA neurons; these receptors are coupled to K+ channels, and activation of CB1 receptors increases potassium conductance in these VTA GABA neurons (inhibits GABAergic neurons)

45
Q

What does THC inhibition of GABAergic neurons do?

A

because these cells normally provide tonic inhibition to neighboring DA cells, reducing their activity causes activation of DA neurons via a disinhibition mechanism

46
Q

Nabilone

A

THC analog for chronic pain

47
Q

Rimonabant

A

CB1 inverse agonist, appetite suppressant (withdrawn)

48
Q

Dronabinol

A

synthetic THC analog, chemotherapy nausea/vomiting, weight control in AIDS

49
Q

Perceptual hallucinations

A

shape, color

50
Q

Psychotic episodes

A

depersonalization, hallucinations, distorted time perception

51
Q

Somatic symptoms of hallucinogens

A

dizziness, nausea, paresthesias, blurred vision

52
Q

What are hallucinogens?

A

a group of drugs that produce perceptual disturbances that can span the range from slightly odd to highly dangerous (psychotic)

53
Q

Are hallucinogens addictive?

A

No; tolerance develops but they are typically not addictive

54
Q

Paresthesias

A

tickling, tingling, burning, prickling, or numbness of a person’s skin with no apparent long term physical effect

55
Q

Lysergic acid diethylamide

A

LSD; 5HT2a partial agonist; psychosis possible, enhanced Glu transmission

56
Q

MDMA

A

ectasy; 5HT, NE, DA releaser, 5HT syndrome possible

57
Q

Mescaline

A

5HT2A partial agonist

58
Q

Psilocybin mushrooms

A

5HT2A agonist; mimics 5HT

59
Q

Phencylidine

A

PCP; NMDA, nAChR antagonist, D2 partial agonist

60
Q

Ketamine

A

dissociative anesthetic (separation of mind and body); NMDA antagonist

61
Q

Hallucinogen pharmacology centers on the effects of which system?

A

serotonin system - with a few having actions at glutamate systems as well

62
Q

Which hallucinogens target the glutamate system

A

PCP and ketamine

63
Q

MOA for opioid dependence

A
  1. MOR activation inhibits VGCCs, reducing GABA release onto DA neurons
  2. MOR activation activates GIRK channels, hyperpolarizing GABa neurons, reducing AP firing
  3. disinhibition of DA transmission
64
Q

Opioids

A
  1. Heroin
  2. Morphine
  3. Oxycodone
  4. Methadone
  5. Buprenorphine
  6. Naltrexone
65
Q

Methadone

A

MOR full agonist; NMDA antagonist; chronic pain, opiate cessation

66
Q

Buprenorphine

A

potent MOR partial agonist; KOR/DOR antagonist; chronic pain, opiate cessation

67
Q

Naltrexone

A

MOR, KOR antagonist, alcohol and opiate cessation

68
Q

Morphine

A

MOR agonist, analgesia

69
Q

Oxycodone

A

MOR and KOR agent, analgesia, chronic pain

70
Q

Heroin

A

schedule I illicit drug

71
Q

Physical symptoms of opioid withdrawal

A

tremors, chills, perspiration, tachycardia, flu-like symptoms, vomiting, diarrhea

72
Q

Psychological symptoms of opioid withdrawal

A

dysphoria, anxiety, insomnia, depression, cravings

73
Q

Treatment of opioid withdrawal

A
  1. Substitute long-acting, high-affinity/potency often partial agonist (buprenorphine)
  2. Detoxification

Pharmacology Test #6 (12 decks)

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