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Pharmacology > Drugs of Abuse > Flashcards

Drugs of Abuse Flashcards

1
Q

Substance Abuse Disorder

What are the 3 critical components?

A

Abuse

Craving

Legal problems

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2
Q

What are the criteria of Substance Abuse Disorder?

A
  • Tolerance
  • Withdrawal
  • Using larger amounts than intended
  • Persistent desire and inability to control use
  • Excess time spent
  • Normal activities reduced or given up
  • Unable to cut back

Mild 2-3
Moderate 4-5
Severe >5

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3
Q

What is tolerance?

A

Decreased effect with repeated use of the drug

Need to use more drug to have the same effect

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4
Q

What is withdrawal?

A

Signs and symptoms that emerge when use of drug is stopped

Symptoms subside when drug is administered again

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5
Q

What is the major neuronal circuit involved in drug abuse? Where does it project to?

A

Mesolimbic dopamine system in the VTA, projecting to the nucleus accumbens, amygdala, and prefrontal cortex

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6
Q

What are two mechanisms (generally) by which you can produce withdrawal syndrome?

A

Stop taking the drug

Give an antagonist to the drug

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7
Q

Cocaine

MOA

A

Inhibits dopamine transporter on the presynaptic membrane, preventing reuptake of dopamine

Levels of dopamine in the synaptic cleft increase, mostly in nucleus accumbens

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8
Q

Amphetamines

MOA

A

Inhibits VMAT2, preventing dopamine from being packaged into vesicles in the axon terminal

Dopamine levels increase in the cytoplasm and eventually the dopamine reuptake transporter will reverse its transport of DA from inside –> outside cell into the synapse

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9
Q

What are the acute effects of Psychostimulants (Cocaine, Amphetamines)?

A 
Rush
High confidence
Decreased fatigue and boredom
Decreased appetite
Increased HR, BP, temp
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10
Q

Cocaine

Half life

A

40-80 minutes

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11
Q

Cocaine

Metabolism

A

Metabolized in liver into an inactive compound, which can be detected in urine, saliva, hair, and milk for 8 days after use

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12
Q

What happens if you take cocaine with alcohol?

A

Cocaine will be transesterified, leading to cocaethylene

Cocaethylene causes more euphoria, but a higher cardiotoxic risk

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13
Q

Long Term Consequences of Cocaine/Amphetamine use

A

Sensitization or Tolerance

Impaired neurocognitive functions

Increased risk of autoimmune diseases

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14
Q

Signs of Cocaine Overdose

A 
Hyperactivity
Sweating
Dilated pupils
Agitation
Tremor
Tachycardia
Chest pain
Cardiac arrhythmia (deadly)
HTN
Seizures/coma
Paranoia
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15
Q

Signs of Cocaine Withdrawal

A 
Anxiety and agitation
Insomnia or Hypersomnia
Fatigue
Sweating
Muscle cramp
Hunger
ED
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16
Q

How should Acute Cocaine Withdrawal be treated?

A

Bromocriptine (dopamine agonist)

Benzodiazepines

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17
Q

How should long term addiction to cocaine be treated?

A

Cognitive Behavioral Therapy

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18
Q

List the Opioid Drugs of abuse

A

Morphine
Codeine
Heroin
Oxycodone

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19
Q

Opioids

MOA

A

Inhibit GABAergic neurons by blocking mew receptors

Since GABA normally inhibits release of dopamine, opioids increase the release of dopamine in the nucleus accumbens

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20
Q

Signs of Opioid Overdose

A 
Unconsciousness
Miosis
Hypotension
Bradycardia
Respiratory Depression
Pulmonary edema
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21
Q

Describe the metabolism of heroin

A

Heroin is a prodrug that is converted to 6-monoacetylmorphine by esterases, which is then metabolized to morphine, which contributes to heroin’s duration of effect

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22
Q

Opioid Withdrawal Symptoms

A 
Lacrimation
Rhinorrhea
Yawning
Piloerecetion/gooseflesh
Involuntary movement
Anxiety
Craving
Sleep disturbance
Nausea, vomit, diarrhea
Sweat
Mydriasis
Cramps
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23
Q

What is the primary treatment for opioid overdose?

A

Naloxone

24
Q

Naloxone

MOA

A

Mew opioid competitive antagonist with a high affinity for mew receptors

Fast acting, Short half life

25
Q

What is the primary treatment for opioid dependence?

A

Naltrexone

26
Q

Naltrexone

MOA

A

Mew opioid antagonist with long half life

27
Q

What are two drugs used in withdrawal syndrome and maintenance from opioid addiction?

A

Methadone

Buprenorphine

28
Q

Methadone

MOA

A

Mew-opioid receptor agonist with long half life

Prevents withdrawal symptoms, but does not cause addiction due to its long half life

29
Q

Buprenorphine

MOA

A

Partial mew-opioid receptor agonist

30
Q

How is buprenorphine misused by patients?

A

On its own, could be crushed and injected to cause a high.

It is often combined with naloxone in pills, so patients crush and dissolve it, then inject it IV to get a high. This causes withdrawal symptoms due to presence of Naloxone.

31
Q

Cannabinoids

What is the active compound in marijuana?

A

THC (Delta-9-tetrahydrocannabinol)

32
Q

Cannabinoids

What is the MOA?

A

THC inhibits GABAergic interneurons, causing disinhibition of the mesolimbic DA system

Increases dopamine in nucleus accumbens

33
Q

Acute Effects of Marijuana

A 
Sedation, relaxation
Mood alteration, sense of wellbeing
Altered perception
Impaired judgment, memory, concentration
Increased HR, dry mouth
Increased appetite
Red eyes
34
Q

Adverse Effects of Marijuana

A 
Panic, delirium
Amotivational syndrome
Tolerance
Personality changes
Cognitive deficits (loss of ST memory)
Gateway to other drugs
35
Q

Treatment of Marijuana Abuse

A

Symptomatic

Anxiolytics for anxiety and panic

Antipsychotics for delirium and paranoia

Cognitive behavioral therapy

36
Q

Alcohol

Type A Alcohol Dependence (Onset, Progression, etc)

A
  • Late onset (over 25yo)
  • Few familial EtOH dependency
  • Slower progression
  • Lower criminality
  • Important environmental influence
37
Q

Alcohol

Type B Alcohol Dependence (Onset, Progression, etc)

A

-Early onset (

38
Q

Diseases caused by Chronic Alcohol Use

A 
Alcohol poisoning
Cardiomyopathy
Gastritis
Liver cirrhosis
Polyneuropathy
Psychosis
cancer
Diabetes
HTN
Stroke
Pancreatitis
39
Q

Alcohol

How does it affect GABA and glutamate?

A

Increases effects of GABA

Inhibits effects of Glutamate

Leads to upregulation of NMDA receptors in brain

40
Q

Alcohol withdrawal after chronic intake may result in sudden death. How?

A

NMDA receptor upregulation in the brain from excess alcohol intake –> stop drinking –> more glutamate present –> NMDA overactivation

41
Q

Treatment Stages of Alcohol Dependence (1-4)

A
  1. Identification
  2. Detox/Withdrawal
  3. Rehab
  4. Aftercare
42
Q

What drug class is given to prevent alcohol withdrawal symptoms?

A

Benzodiazepines with long 1/2 life, like diazepam and Iorazepam

43
Q

Symptoms of Alcohol Withdrawal

A

Anxiety, sweating, palpitations, GI upset, insomnia, nausea

Seizures (within first 3 days)

Hallucinations

Delirium tremens (tremor, confusion, fever, tachycardia, HTN, diaphoresis)

44
Q

What drug is used in Alcohol Aversion Therapy?

A

Disulfram

45
Q

Disulfram MOA

A

Inhibits acetaldehyde dehydrogenase, leading to increased levels of acetaldehyde when drinking.

Acetaldehyde makes pt feel sick, so they will hopefully become more averse to drinking.

46
Q

What drug may be used to decrease alcohol cravings?

A

Naltrexone

47
Q

Naltrexone

MOA

A

Antagonist of opioid receptors

Blocks release of DA from nucleus accumbens

48
Q

Why should Naltrexone and Disulfram not be used together?

A

Both are potential hepatotoxins

49
Q

What drug can restore the balance between neuronal excitation and inhibition in alcoholics?

A

Acamprosate

50
Q

Acamprosate

Contraindications and Adverse Effects

A

AEs: diarrhea

Contraind: severe renal disease

51
Q

Benzodiazepines

MOA

A

Indirect agonists of GABA A receptors

52
Q

Benzodiazepine Withdrawal symptoms and management

A

Symptoms: Anxiety, agitation, photo and phonosensitivity, muscle cramps, sleep disturbance, dizzy

Withdrawal Mgmt: Diazepam

53
Q

Nicotine

MOA

A

Nicotinic Ach receptor antagonists

Stimulates neurons in the VTA and increases dopamine in the nucleus accumbens

54
Q

Best Treatment for Nicotine Addiction

A

Varenicline (Chantix)

-partial nicotinic agonist that decreases cravings and nicotine withdrawal syndrome

55
Q

Hallucinogens (LSD, mescaline)

MOA and Symptoms

A

Activate 5HT 2A receptors in cortex

Changes in sensation, illusions, hallucinations

Do NOT induce dependence or addiction

Pharmacology (67 decks)

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