PHARM - Drugs of Abuse - Week 9 Flashcards

1
Q

Why does dependence to drugs occur?

A

Progressive pharmacological adaptation to the drug, resulting in tolerance

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2
Q

What happens to homeostasis in response to repeated drug exposure? What is a consequence of this?

A

It is reset. An individual in this state needs continuous drug administration to maintain normal function.

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3
Q

If there is a dependence on drugs, what happens if the drug is abruptly stopped?

A

Withdrawal symptoms occur

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4
Q

Define abstinence.

A

Practice of not doing something or having something that is wanted or enjoyable

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5
Q

Define psychological dependence, including the physiological basis for it, and what normally happens in individuals with no dependence.

A

Also called addiction - administration of substances or certain behaviours activate brain reward circuits.
These motivate normal behaviour which most people enjoy without being compelled to repeat them.

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6
Q

What occurs with reflexice acivation of reward circuits?

A

It becomes involuntary, drawing a person into compulsive repetition and putting focus on the immediate pleasure despite negative consequences.

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7
Q

Where is the primary action of drugs of abuse?

A

In the CNS - the brain reward circuits

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8
Q

What system specifically do addictive drugs activate? What consequence does this result in?

A

The mesolimbic dopamine system, producing a rewarding-reinforcing action.

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9
Q

What effect does alcohol have on the CNS?

A

Depressant

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10
Q

What neurotransmitter does alcohol bind to and increases transmission of what neurotransmitter?

A

Binds to GABA and increases GABA-ergic transmission

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11
Q

What two neurotransmitter receptors are altered by alcohol?

A

NMDA and 5-HT3 (serotonin)

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12
Q

Is alcohol rapidly or slowly absorbed and distributed?

A

Rapid

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13
Q

Describe how alcohol is processed by the body in terms of percentages (5).

A

90% is oxidised in the liver

The rest is eliminated via saliva, sweat, breath, and urine

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14
Q

Can an overdose of alcohol be fatal? Explain why.

A

Yes, due to the effects of being a depressant and acetaldehyde (a metabolite)

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15
Q

After what time period following cessation of heavy drinking does the dependence on alcohol become apparent?

A

6-12 hours

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16
Q

Name 5 withdrawal symptoms of alcohol after 6-12 hours.

A
Hand tremors
Nausea
Excessive sweating
Agitation
Anxiety
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17
Q

Name a withdrawal symptom of alcohol after 12-24 hours (1).

A

In some individuals, visual/tactile/auditory hallucinations may occur

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18
Q

Name a withdrawal symptom of alcohol after 24-48 hours (1).

A

In some individuals, siezures may occur

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19
Q

Name a withdrawal symptom of alcohol after 48-72 hours. What percentage of mortality is it associated with?

A

Delirium - 5-15% mortality

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20
Q

What is the standard first-line treatment for acute alcohol withdrawal symptoms?

A

Benzodiazepines

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21
Q

What is naltrexone and what does it prevent? How long is its action?

A

An opioid receptor antagonist
Prevents euphoria
Long action - 24-72h

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22
Q

How does naltrexone work (2)?

A

Blocks action of the endogenous opioids released by alcohol

Blocks activation of dopamine reward pathways

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23
Q

What overall effect will naltrexone have (2)?

A

Decreases pleasurable effects linked to alcohol consumption

Reduces cravings

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24
Q

Name 4 common adverse effects and one serious but rare adverse effect of naltrexone.

A
Insomnia
Headache
Fatigue
Dizziness
Hepatotoxicity
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25
What must be monitored during naltrexone therapy?
Liver function
26
What does disulphiram promote?
Abstinence in motivated alcoholics after initial detoxification
27
What is disulphiram?
Aldehyde dehydrogenase inhibitor
28
How does disulphiram work (2)?
Blocks degradation of acetaldehyde to acetate | Acetaldehyde accumulates in the body and casues unpleasant symptoms
29
Name 7 symptoms of disulphiram and a reason why if applicable.
``` Intense flushing Headache (throbbing) Sweating The above are caused due to acetaldehyde being a potent vasodilator Nausea Vomiting BP changes Hyperventilation ```
30
When is acamprosate used?
Maintenance of abstinence in alcohol dependence
31
What effect does acamprosate have on the CNS (2)?
Restores normal activity in glutamate and GABA systems.
32
How long does acamprosate therapy last?
Up to a year
33
What should be checked before acamprosate therapy?
Creatinine levels
34
Name 3 side effects of acamprosate.
Rash Diarrhoea Changes in libido
35
What addiction exceeds all others?
Nicotine addiction
36
What does nicotine cause the release of? Give 3 consequences of this. What do these 3 increase the risk of?
Catecholamine release Increases heart rate, vascular resistance, and hypertension Increases risk for coronary artery disease
37
What do catecholamines stimulate the mobilisation of?
Free fatty acids
38
How does nicotine affect LDLs and HDLs?
Increases LDLs and decreases LDLs
39
Mechanistically, how does nicotine act?
Acts as a nAChR agonist, increasing dopamine neuron activity
40
How do nicotine patches work?
Patch impregnated with nicotine, which provides slow absorption into the circulation. Heps reduce cravings.
41
How does bupropion aid nicotine addiction?
Inhibits noradrenaline and dopamine re-uptake
42
Name 6 side effects of bupropion.
``` Insomnia Agitation Anxiety Visual disturbances Impaired concentration Rash ```
43
What are opioids used for typically?
Treatment of pain
44
What do opioids do in addition to reducing the perception of pain?
Produce a state of well-being or euphoria
45
What is the most frequently abused opioid?
Heroid (diacetylmorphine)
46
What kind of drug is heroin (aside from being an opioid)?
Prodrug
47
What is heroin metabolised to?
Morphine
48
Why is heroin more effective than morphine (2)?
Greater lipid solubility - crosses the blood brain barrier more rapidly
49
Why does heroin cause respiratory depression?
It inhibits brainstem respiratory mechanisms
50
Name 6 adverse effects of heroin.
``` Antitussive effect Miosis Bradycardia Nausea Vomiting Constipation ```
51
What are opioids agonists of?
G-protein coupled opioid receptors
52
Which receptor do heroin, morphine, codeine, and oxycodone act on?
μ receptor
53
Do all opioids induce tolerance and dependence upon cessation?
Yesd
54
What kind of drug is used for opioid overdose?
Opioid antagonists
55
Give an example of an opioid antagonist, what kind of overdose it is used to treat, and how quickly it acts.
Naloxone, short acting so used for acute opioid overdose
56
What is the main active constituent in cannabinoids?
THC
57
Name 4 beneficial therapeutic effects of THC (5).
Anti-emetic Muscle relaxing effects Improves seizure control in patients with epilepsy Useful for anorexia linked to weight loss in cancer patients and patients infected with HIV (cachexia)
58
What is the main CNS action of THC? Name 2 effects this can have.
CB1 receptor | Can cause loss of coordination and painful muscle spasms
59
What kind of a drug is cocaine?
Psychostimulant and hallucinogen
60
Name three kinds of psychostimulants.
Cocaine | Ice Speed
61
What three effects do psychostimulants have?
Procudes excitement Euphoria Decreases fatigue
62
Name 4 hallucinogens.
LSD PCP Ecstasy GHB (liquid ecstasy)
63
Are hallucinogens addictive?
No, theyre non-addictive drugs of abuse
64
Where do hallucinogens typically target?
Cortical and thalaic circuits rather than mesolimbic dopamine ones.
65
What do psychostimulants and hallucinogens interfere with?
Multiple neurotransmitter and receptor systems
66
In what three ways can cocaine be administered?
Injected Snorted Smoked
67
Is cocaine rapidly or slowly absorbed?
Rapid
68
Does cocaine cause CNS or PNS effects?
Both
69
What does cocaine block the uptake of (3)?
Neuronal uptake of dopamine, noradrenaline, and serotonin
70
What happens following a dose of cocaine (3)?
Intense euphoria Dysphoria/irritability Craving for more drug
71
Name 5 symptoms of cocaine overdose.
``` Acute fear Psychotic symptoms Hypertension Tachycardia Coronary vasospasm ```
72
Describe the mechanisms of amphetamines (2).
Acts as a competitive inhibitor reducing uptake of noradrenaline and dopamine
73
How do amphetamines enter neurons?
By uptake or diffusion
74
What do amphetamines do once inside the cell (3)?
Interact with VMAT and inhibit uptake of dopamine and noradrenaline into vesicles
75
What is LSD an agonist of and what does it increase transmission of?
Agonist of serotonin, increases glutaminergic transmission
76
What does LSD inhibit and where?
Inhibits 5-HT neurons from firing in raphe nuclei
77
What is PCP? Give its common name.
Phencyclidine - angel dust
78
What is PCP and antagonist to?
Glutamate NMDA-receptor
79
What four effects does PCP have on neurotransmitters?
Inhibits uptake of dopamine, noradrenaline, and serotonin | Stimulates dopamine release
80
What four behavioural effects does PCP have?
Euphoria Excitation Dysphoria Aggression
81
What can chronic use of PCP lead to? Is it reversible or irreversible?
Irreversible schizophrenia-like psychosis
82
What is the common name for MDMA?
Ecstasy
83
What two neurotransmitters does MDMA stimulate the release of?
Dopamine and serotonin
84
What four things does MDMA affect?
Mood, sleep, memory, and apetite
85
What does acute toxicity of MDMA cause?
Hyperthermia
86
What is meant by serotonin syndrome, what drug is it caused by, and is it fatal?
Hyperserotoninergic state caused by MDMA | May be fatal
87
Name 12 symptoms of serotonin syndrome.
``` Abnormal muscle movements Muscle rigidity Sweating Disruption in thermoregulation Confusion Agitation Restlessness Hallucinations Tachycardia Hypertension Loss of control Death ```
88
What is a common date rape drug and why?
GHB - it is an odourless liquid that readily mixes with alcohol Causes euphoria, enhanced safety perceptions, social closeness, amnesia, then sedation/coma