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MEDI 202 - Genes To Community > Drugs of Abuse > Flashcards

Drugs of Abuse Flashcards

1
Q

What are the factors that limit the therapeutic usefulness of drugs?

A

Tolerance
Physical dependence
Psychological dependence

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2
Q

What are examples of drugs that are commonly abused?

A

CNS stimulants
Hallucinogens
Opioid analgesics
CNS depressants
Sedative-hypnotics
Inhalants

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3
Q

What are examples of CNS stimulants?

A

Cocaine, amphetamines, nicotine

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4
Q

What category do LSD, marijuana, mescaline, and phencyclidine fall under?

A

Hallucinogens

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5
Q

What are examples of opioid analgesics?

A

Morphine and heroin

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6
Q

What kind of drug is ethanol?

A

CNS depressant

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7
Q

What are examples of sedative-hypnotics?

A

Alprazolam and diazepam

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8
Q

What kind of drugs are toluene, nitrous oxide and amyl nitrate?

A

Inhalants

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9
Q

What are CNS stimulants?

A

Drugs that have a chemical structure similar to monoamine neurotransmitters

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10
Q

How do CNS stimulants produce their actions?

A

Stimulating the release and blocking the reuptake of monoamine neurotransmitters

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11
Q

What are the effects of cocaine on CNS?

A

Enhances the activity of dopamine by binding tightly at the dopamine transporter forming a complex that blocks the transporter’s function.

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12
Q

What happens if the transporter’s function is blocked?

A

It can no longer perform its reuptake function thus increasing the amount of dopamine available

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13
Q

What is responsible for the addictive property of cocaine?

A

The stimulation of the pleasure centre of the human brain

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14
Q

What does cocaine do in relation to norepinephrine?

A

Blocks reuptake of norepinephrine and serotonin and pre-synaptic neurons

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15
Q

Why is cocaine also considered a local anaesthetic agent?

A

Produces a direct effect on cell membranes by blocking sodium channel activity, preventing the generation and conduction of nerve impulses.

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16
Q

What is the half-life of cocaine?

A

0.7 to 1.5 hours

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17
Q

How is cocaine metabolised?

A

By cholinesterase enzymes in liver

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18
Q

What is the metabolism process of cocaine?

A

Metabolised to benzoylecgonine and ecgonine methyl ester, both excreted in urine

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19
Q

What happens if cocaine is taken while consuming alcohol?

A

Cocaethylene is formed which is more euphoric and toxic than cocaine itself.

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20
Q

What are the side effects of cocaine intake?

A

Psychiatric complaints, hyperthermia, chest pain, agitation, convulsion.

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21
Q

How is cocaine toxicity treated?

A

Calming and cooling the patient, benzodiazepines could be used to calm an agitated patient.

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22
Q

What is amphetamine?

A

A sympathetic amine that shows neurologic and clinic effects very similar to ccocaine

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23
Q

What is the mechanism of action when it comes to amphetamine?

A

Inhibiting weakly the reuptake transport
Releasing intracellular stores of catecholamines
Inhibiting monoamine oxidase responsible for the catabolism of monoamines

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24
Q

What does the consumption of amphetamine lead to?

A

Elevation of catecholamine neurotransmitters in synaptic spaces induces stimulation of the entire cerebrospinal axis and leads to increased alertness, decreased fatigue, and insomnia.

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25
Q

Where is amphetamine metabolised?

A

In the liver

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26
Q

Where is amphetamine excreted?

A

In the urine

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27
Q

How long does the euphoria of amphetamine last?

A

4 to 6 hours

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28
Q

What are some side effects of amphetamine?

A

Dependence tolerance and drug-seeking behaviour.

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29
Q

What are some additional side-effects of both cocaine and amphetamine?

A

Increased norepinephrine (increased heart rate, blood pressure, mydriasis and hyperactivity)

Increased dopamine (paranoia, hallucinations, and endocrine disturbances)

Increased serotonin (aggressiveness, dyskinesia, decreased appetite)

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30
Q

What is the common name of methylenedioxymethamphetamine?

A

Ecstasy or Molly

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31
Q

What is MDMA?

A

Synthetic substance that does not exist in nature

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32
Q

What is the difference between MDMA and amphetamine?

A

There is a methylenedioxy group attached to the aromatic ring of MDMA.

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33
Q

What is the mechanism of action of MDMA?

A

Interferes with the storage of serotonin, and increases the amount of serotonin available to be released. Acts of serotonin transported and promotes the release of serotonin in synapse.

34
Q

What does MDMA act as?

A

Indirect monoaminergic agonist

35
Q

What does MDMA cause?

A

Significant increase in synaptic serotonin levels

36
Q

What is the relation between MDMA and dopamine?

A

MDMA blocks the dopamine transporter and enhances the release of dopamine noradrenaline

37
Q

Why can’t MDMA be inhaled?

A

Because the methylenedioxy group raises the boiling point.

38
Q

What is the elimination half-life of MDMA?

A

7 hours

39
Q

Where is MDMA absorbed?

A

Really absorbed from the GI tract

40
Q

Where is MDMA metabolised?

A

In the liver

41
Q

What are some side effects of MDMA?

A

Hyperthermia and movement disorders are known as serotonin syndrome.
Dehydration and renal failure.

42
Q

Why are benzodiazepines given to MDMA patients?

A

To calm and cool the patients

42
Q

What drug is given to treat the serotonin syndrome symptoms?

A

Cyproheptadine

42
Q

What is the effect of khat?

A

Increase the release and inhibit the reuptake of catecholamines

43
Q

What other drugs is khat similar to?

A

Cocaine and amphetamine

44
Q

What are the drugs that bind to transporters of biogenic amines?

A

CNS stimulants: cocaine, amphetamine, MDMA, khat

45
Q

What are examples of hallucinogens?

A

LSD, marijuana, synthetic cannabinoids

46
Q

What is LSD?

A

Acts as a partial agonist at serotonin receptors

47
Q

How long do the effects of LSD last?

A

Between 6 and 12 hours

48
Q

Where is the drug eliminated?

A

In the urine: 1% as unchanged and 13% as the major metabolite (O-H-LSD)

49
Q

What are the side effects of LSD?

A

Hallucinations, mood alterations, sleep disturbances, and anxiety, loss of judgment, and impaired reasoning

50
Q

What is the mechanism of action of marijuana?

A

THC is the main active ingredient in marijuana and it binds to and activates specific receptors.

51
Q

What are the receptors the THC binds to called?

A

Cannabinoid receptors.

52
Q

Where are the cannabinoid receptors found?

A

Parts of the brain that control memory, thought and concentration.

53
Q

How does marijuana affect the reward system?

A

By inducing the release of endorphins in the brain
By acting as a dopamine agonist

54
Q

What is the effect of inducing the release of endorphins?

A

Produces the feeling of pleasure and reward

55
Q

What is the effect of marijuana acting as a dopamine agonist?

A

Stimulating reinforcement regions in the mesh-telencephalic dopamine system

56
Q

Why does marijuana accumulate in the milk?

A

Due to its lipophilic qualities

57
Q

What are the two main signs of marijuana use?

A

Increased heart rate and conjunctival reddening, however, decrease in blood pressure and in psychomotor performance can also occur

58
Q

What are synthetic cannabinoids?

A

Synthetic forms of different nolecular structure from cannabinoids found in marijuana plants, they can produce 800 times greater effects

59
Q

What are the most common examples of opioids?

A

Morphine, heroine, codeine, oxycodone

60
Q

What kind of individuals often develop an addiction to opioids?

A

Those who take them for recreational purposes.

61
Q

What are the effects of opioids?

A

Euphoria, analgesia, sedation, cough suppression and constipation

62
Q

What are the toxicity effects of opioids?

A

Respiratory depression, nausea, and vomiting.

63
Q

What are the withdrawal symptoms of opioid use?

A

Lacrimation, yawning, sweating, restlessness, muscle cramping, and diarrhea.

64
Q

What do opioids bind onto?

A

μ-DOR, δ-DOR or κ-DOR

65
Q

What leads to the distinct and sometimes opposing effects of opioids?

A

Distinct signalling and expression of opioid receptors through the brain

66
Q

What does the activation of μ-DOR in the VTA cause and how is that different from the activation of κ-DOR?

A

Activation of μ-DOR causes an inhibition of GABA which leads to a disinhibition of dopamine neurons. While activation of κ-DOR receptors inhibit directly dopamine neurons.

67
Q

What are the drugs that activate G protein-coupled receptors?

A

Hallucinogens, opioids

68
Q

What is the mechanism of action for ethanol?

A

Modulating the activity of inotropic rectors such as GABA, glutamate receptors, MDMA receptors, glycine receptors, and the serotonin receptors.

69
Q

How does alcohol exert its desired and toxic effects?

A
  • Increasing the effects of inhibitory neurotransmitter GABA
  • Releasing endogenous opioids in the reward system
70
Q

What happens if the inhibitory neurotransmitter GABA is increased?

A

Suppression of the activity of the CNS

71
Q

What happens if ethanol is consumed in high doses and why?

A

Coma and respiratory depression, because it is a general CNS depressant.

72
Q

What kind of drug is ethanol?

A

Drug that mediates its effect via inotropic receptors

73
Q

What are the side effects of ethanol consumption?

A

Nausea, vomiting and hypotension

74
Q

What can chronic ethanol abuse cause?

A

Profound hepatic, cardiovascular, pulmonary, hematologic, endocrine, metabolic, and CNS damage

75
Q

What does treatment of ethanol withdrawal rely on ?

A

Benzodiazepines

76
Q

What is used to treat the dependence of ethanol?

A

Naltrexone: white still consuming ethanol
Disulfiram and Acamprosate: once abstinence is achieved

77
Q

What is the function of naltrexone?

A

Blockade of μ-opioid receptors; therefore blocks normal reaction of the part of the brain that produces the feeling of pleasure and reward

78
Q

What is the function of acamprosate?

A

Modulation of the glutamate (excitatory) and GABA (inhibitory) neurotransmission restore imbalance between neuron excitation and inhibition

79
Q

What is the function of disulfiram?

A

Inhibits aldehyde dehydrogenase and prevents the metabolism of acetaldehyde.

80
Q

Why should disulfiram not be taken while consuming ethanol?

A

It causes the accumulation of acetaldehyde in the blood which causes sweating, headache, and flushing.

MEDI 202 - Genes To Community (23 decks)

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