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PHARM 2 > Ecstacy > Flashcards

Ecstacy Flashcards

1
Q

What category does ecstasy belong to?

A

ecstacy is an amphetamine even though it is often classified as a hallucinogen

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2
Q

what is the chemical name for ecstasy?

A

MDMA (3,4- methylenedioxymethamphetamine

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3
Q

how does the structure of ecstasy differ from that of amphetamines?

A

the presence of a methyelenedioxy ring

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4
Q

What happens if you modify the aromatic ring in MDMA?

A

modification of the ring produces reduction in stimulant effects and produces more seotonergic effects

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5
Q

what is the precursor to MDMA?

A

Sassafras trees are aromatic trees that grow across USA and east asia

safrole is an aromatic oil that is obtained from the distillation of the root bark of sassafras trees

SAFAROLE is the precursor to MDMA

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6
Q

how is ecstasy administered?

A

almost always taken in pill form

  • stacking: taking multiple doses simultaneously (not good for naive users)
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7
Q

how much MDMA content in a tablet?

A

depends on the source but most MDMA content ranges from 10mg to 150 mg

effects felt between 75-125mg of MDMA

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8
Q

what is the usage rate of MDMA?

A

small % (less than 10%) will use once per week, may having trouble reducing use but seems to be more psychologically dependant than physiological because not a big withdrawal

often taken with alcohol, cannabis, and amphetamines

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9
Q

what are the psychological effects of MDMA?

A
  • high lasts 2-3 hours
  • positive mood change
  • drop in defence mechanism and increase in empathy for others (entactogens) ..
  • increase self esteem
  • overall stimulant effect
  • used in PTSD sometimes
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10
Q

what are some physiological effects of MDMA?

A
  • rise in BP
  • rise in HR
  • hyperactivity
  • hyperthermia
  • jaw clenching/ bruxism (teeth grinding) due to excess serotonin release from facial nerves
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11
Q

in what ways is the mechanism of MDMA different than amphetamine?

A

ecstasy works the same except its effects are predominately mediated through serotonergic nerve terminals

this is due to that methylenedioxy ring

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12
Q

What is the mechanism of action for MDMA?

A
  • blocks and reverses primarily of serotonin transporters
    but also a bit of dopamine and noradrenaline
  • the potency is 5HT>NA>DA
  • the affinity for MDMA for 5HT transporter is 10 times higher than for the noradrenaline
  • high serotonin levels may lead to release of oxytocin –> a hormone that is related to feelings of empathy and bonding
  • also seems to bind to TAAR receptors similar to amphetamines to reverse the role of transporters
  • serotonin leaks from vesicles into the nerve ending cytoplasm
  • partial inhibition of monoamine oxidase.. not a full one
  • usually classified as a hallucinogen because of its agonistic actions at the serotonin (5HT) 2A receptor due to the methylenedioxy ring
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13
Q

what effect does ecstasy have on dopamine and serotonin levels?

A

in the NA of rats, theres a moderate increase in dopamine (200-300%) which is smaller compared to cocaine and amphetamines
- with MDMA theres 1400% serotonin level increase, which is present in the prefrontal cortex and other parts of the reward pathway

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14
Q

how reinforcing is MDMA?

A
  • its not as reinforcing of a drug though and you do not see a lot of addiction. Animals will self administer but with breaking points that are lower than drugs like cocaine
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15
Q

what other receptors (3) does MDMA bind to?

A
  1. adrenergic receptors –> might be responsible for some cardiovascular effects and hyperthermia
  2. histamine type 1 receptors –> acH release when MDMA BINDS
  3. nicotinic acH receptor alpha-7 receptor –> acts as partial agonist to this and may lead to increased calcium levels in neurons as seen in amphetamines (can lead to excitotoxicity)
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16
Q

How is MDMA metabolized in the liver?

A

metabolized by the same enzyme that metabolizes amphetamines –> CYP2D6… 80% is metabolized and 20% is excreted unchanged

complex metabolism

forms as many as 9 metabolites of MDMA which have been found to produce apoptosis in neurons (toxic)

17
Q

How does tolerance occur after use of MDMA?

A

ecstasy results in reduce transporter activity like AMPH
primarily on the serotonin transporter, but dopamine and noradrenaline also

also results in loss of transporters at the neuronal membrane

18
Q

what are some of the negative effects of MDMA?

A

following injection can include: depression, anxiety, hallucinations and paranoia

withdrawal and or rebound can be severe

“suicide Tuesdays” following a week of clubbing

lethargy, irritability, memory loss and panic

the supply of neurotransmitters like serotonin and dopamine is exhausted and these are all dose dependant

19
Q

What is serotonin syndrome?

A
  • from abnormally high levels of serotonin
  • rapid onset of serotonin causes increase HR, BP, muscle rigidity (esp. in lower limbs), severe perspiration, delirium, diarrhea, hyperthermia, rhabdomyolysis (muscle breakdown)
  • can lead to kidney failure, convulsions, shock, and death

ecstacy is very dangerous if taking psychiatric drugs that work by increasing serotonin levels like prozac (SSRI) because it can cause a serotonin OD.

20
Q

What three factors play a role in MDMA hyperthermia?

A
  • this is the leading cause of death by MDMA
  • experiments in animals and humans show a single dose can significantly increase body temp as much as 43 degrees C, in humans which is Fatal and its made worse because of all the physical exertion and warm environments that MDMA is taken in

Serotonin, noradrenaline and dopamine all three play a role in the hyperthermia

21
Q

How does serotonin cause hyperthermia in MDMA use?

A

serotonin cause CNS dysregulation of the body temperature which leads to hyperthermia

22
Q

how does noradrenaline cause hyperthermia in MDMA use?

A

noradrenaline has adrenergic alpha-1 receptors which cause vasoconstriction and retention of heat since heat can’t escape from BV onto skin as sweat and that causes hyperthermia

another thing is the adrenergic beta-3 receptor which causes mitochondrial uncoupling that generates heat (happens to animals during hibernation) and causes hyperthermia

23
Q

how does dopamine cause hyperthermia in MDMA use?

A

dopamine receptors seem to play a part but we don’t know

24
Q

what does long term body temperature dysregulation lead to?

A

the CNS effects of MDMA on thermoregulation may persist long after drug has left the body

when rats were exposed to single dose of MDMA and multiple doses over 3-4 days

4-6 weeks later, exposed to high ambient temperature displayed impaired ability to thermoregulate

small window of dosing produces long-lasting effects possible at CNS level but not seen in humans yet

25
Q

What is hypoatremia? how does it occur with relation to MDMA usage?

A
  • state of low sodium in the blood
  • excessive thirst is triggered by hyperthermia
  • water intoxication: huge water intake in short period leads to dilution of sodium in blood (water rushes into neurons and cells)
  • also MDMA can trigger excessive release of ADH (antidiuretic hormone) which leads to water retention
  • this can lead to cerebral deem which is brain swelling from cells absorbing too much water, vomitting, coma and respiratory arrest from edema pushing on the brain stem
26
Q

what are some evidence pointing to neuronal death by MDMA use in animal studies?

A

animals studies showed that serotonergic neurons tend to die when exposed to MDMA
- Hatzidimitriou et al (1999) showed neuronal loss in squirrel monkeys after MDMA twice a day for four days

  • 7- years years it caused some regeneration but not all
  • still controversial in humans and could be due to the alternates in the pills like PMA that could be causing this
27
Q

What are some evidence of neuronal death in humans?

A

compared the brain of recreational users to non-users

used on average 96 times over three years

used a radioactive drug that binds to serotonin transporter to see levels in the brain

there was shown to be marked deficits in several brain areas some as high as 50%
- there are fewer 5HT transporters in people who do ecstasy

28
Q

what is the possible mechanism of toxicity caused by MDMA?

A

when 5-HT is being metabolized by MAO’s, hydrogen peroxide is generated

this can form hydroxyl radicals which can damage lipids and proteins

5-HIAL is a reactive and can also damage proteins and lipids and is produced when 5-HT is being metabolized….

5-HIAL is broken down by aldehyde dehydrogenase into 5-HIAA which means if a person is drinking this enzyme will be less involved in 5-HIAL breakdown and more in alcohol therefore, 5-HIAL builds up and becomes dangerous

damage to mitochondria results in damage to the nerve terminals and eventual cell death

metabolism of MDMA alone can produce quinones and semiquinones that produce a large amount of ROS

29
Q

What are deaths associated with MDMA?

A

sudden illness and death can occur even after small doses and sometimes even first time and theres no clear relationship between dose and death

rare combinations of variability in genes for metabolic enzymes may lead to increase production of toxic metabolites (i.e. they might over metabolize 5-HT or produce a lot of metabolites in short amount of time) which might explain why small doses are Fatal for a small number of users compared to total number

87 ecstasy related deaths reported:
8 from heart/circulation
4 from liver damage
9 cerebral edema
30 hyperthermia
14 suicide/accidents
22 unknown

PHARM 2 (14 decks)

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