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PYB260 > Week 5 - Amphetamines and Cocaine > Flashcards

Week 5 - Amphetamines and Cocaine Flashcards

1
Q

What are stimulants?

A
  • Mimic sympathetic nervous system and work on neurotransmitters
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2
Q

What do the drugs stimulate the transmission of?

A
  • Epinephrine (E)
  • Norepinephrine (NE)
  • Dopamine (DA)
  • Serotonin (5-HT)
  • “Sympathomimetic” - serotonin as indolamine
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3
Q

What type of amines are these neurotransmiters

A

Monoamines (MAs) or biogenic amines

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4
Q

What are E, NE and DA

A

Catecholamines - very similar chemical structures

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5
Q

What is the natural amphetamine?

A

Ephedrine - used by Chinese cultures

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6
Q

What are the synthetic amphetamines and what are they used for?

A
  • D-amphetamine = ADHD
  • L-amphetamine = mirror image as D but more potent
    DI-amphetamine - ADHD and narcolepsy
  • Methamphetamine (speed) - ADHD and obesity
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7
Q

What are the amphetamine-like stimulants (synthetic)

A
  • Methylphenidate (MPH/Ritaline)

- Pipradrol

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8
Q

What is cocaine?

A
  • Extracted from leaf of coca plant native to Sth America = Cathionone (khat)
  • Extracted from African shrub

Synthetic = methcathionone (bupropion)

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9
Q

Are amphetamines an acid or a base, and what is the pKa?

A
  • Weak base - pKa = 9-10
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10
Q

What are the methods of administration?

A
  • Oral

- Injection and inhalation

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11
Q

What are the advantages of oral administration of amphetamines?

A
  • Ionized in digestive system (slower rate of absorption)
  • Blood levels can be kept constant
  • Medical uses
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12
Q

What is the pKa of cocaine and what are it’s main routes of administration?

A

pKa = 8.7

- Usually injected or inhaled

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13
Q

What is the oral administration of cocaine?

A
  • Sucking coca leaves
  • Mix leaves with lime (stone) (wood ashes) to decrease ionization (increase absorption) - makes more basic/lining of digestive tract more basic to increase absorption
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14
Q

What is tooting of cocaine?

A

inhaling vapor from heated powder

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15
Q

What is freebasing of cocaine?

A

Separates cocaine from HCl

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16
Q

What is crack cocaine?

A

Cocaine HCl + sodium bicarbonate

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17
Q

What is snorted

A
  • powdered salt (cocaine HCl)
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18
Q

What is the absorption of amphetamines for oral administration?

A
  • Determined by food in stomach and physical activity

- Peak blood levels within 30 min - 4 hrs

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19
Q

What is the absorption of amphetamines for inhalation

A

approx 2.5 hrs

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20
Q

What ist he absorption of amphetamines for IV

A

5 minutes

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21
Q

What is the absorption time for inhalation of cocaine?

A

10-20 mins

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22
Q

What is the distribution of amphetamines and cocaine?

A

Cross BBB and concentrate in brain, spleen and kidneys

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23
Q

What is the excretion of amphetamines?

A
  • Depends on pH of urine: more basic = more reabsorption
  • 50% excreted unchanged/ 50% metabolized by liver
  • ½ life = 7-14 hours if acidic urine & 16-34 hours if basic
  • Also excreted through sweat & saliva
  • Metabolites can also be active with long half lives
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24
Q

What is the absorption of cocaine?

A
  • ½ life = 45-75 minutes, also dependent on urine pH
  • Metabolites may be present in urine 24-36 hours after admin.
  • Metabolites also deposit in hair
25
Q

What synapses do amphetamines effect?

A

5HT, E, NE and DA (esp)

26
Q

What are the three effects of amphetamines at the synapse?

A
  1. Cause NT to leave into synaptic cleft
  2. Increase NT released due to AP
  3. Block reuptake (& inhibit MAO activity)
27
Q

What is the effect of cocaine at the synapse

A
  1. Reuptake blocker
28
Q

What is the effect on the PNS

A

stimulate epinephrine synapses - fight or flight

29
Q

What is the effect on the CNS?

A

Multiple:

  1. Increased DA in nucleus accumbens (reinf & motivation)
  2. Increased DA in nigrostriatal system (motor activity)
  3. Cocaine blocks APs (via Na+ ion channel blocking) - local anesthetic (Procaine)
30
Q

What are the effects of stimulants on the body?

A
  • Increase HR and BP
  • Vasodilation
  • Bronchodilation
31
Q

What are the side effects of stimulants on the body?

A
  • Headaches
  • Dry mouth
  • Upset stomach
  • -> Methamphetamines has fewer PNS effects
32
Q

What are the effects on stimulants on sleep?

A
  • Prevents sleep
  • Insomnia
  • Suppression of REM sleep
33
Q

What are the effects of stimulants on mood?

A
  • Improve mood (3-6hrs)
  • ↓ fatigue/ ↑ energy
  • Rush
  • Followed by depression/crash
  • Acute tolerance to pleasurable effects
  • Cocaine has shorter-acting effects (<10-20mins ‘pleasurable’)
34
Q

What are the effects of stimulants on behaviour?

A
  • Stereotyped behavior – repetitive acts that are meaningless (e.g. pacing)
  • Punding at high doses – repetitive meaningless acts that last for a long time (e.g. moving things back and forth)
35
Q

What are the mental disturbances associated with stimulants?

A
  • Amphetamine psychosis or ‘monoamine psychosis’
  • Hallucinations, delusions, hostility/violence, paranoia
  • Disappears in a few days with no lasting effects
  • At high doses cocaine can also induce psychosis
  • Formication – feeling of bugs crawling on skin (cocaine bugs, or “crank” bugs with amphetamine use)
36
Q

What are the sensory effects of stimulants?

A
  • ↑ visual acuity (CFF) & auditory acuity

* Time underestimated (seems longer than usual)

37
Q

What are the effects of stimulants on performance?

A
  • ↑ endurance
  • Fatigue effects = ↓ (improve) RT & ↑ coordination (especially complex tasks)
  • ↑ vigilance & attention
  • Most effects seen on simple or learned performance vs. novel performance tasks; narrowing or “tunneling” of attentional focus
38
Q

What are the effects of stimulants on athletic performance?

A

1 % improvement on swimming and track performance

–> Banned substance

39
Q

What are the effects of stimulants on appetite?

A

• Anorectic effects; mechanisms unclear
↑ ‘other’ (motoric) behavior
Stimulation of areas of the hypothalamus (e.g., Yu et al., 2017)
↓ DA midbrain activation to (sweet) rewards (Melrose et al., 2016)
• ↑ metabolism & ↓ food intake = weight loss
• Evidence about thalamus being dulled, also maybe that the dopamine pathway of food is suppressed

40
Q

What is the unconditioned behaviour in animals?

A 
•	↑ SMA (Low and intermediate doses)
•	Stereotyped behaviours
•	Auto-mutilation (Higher doses)
•	↓ food &amp; water
Conditioned Behavior
41
Q

What is the conditioned behaviour in animals?

A
  • Rate dependency effect (↑low-rate behaviours, ↓high-rate behaviours); doesn’t apply to punished behavior
  • Operant effects of cocaine not as significant as amphetamines
42
Q

Can amphetamines and cocaine be discriminated?

A
  • Amphetamines create dissociation (e.g. drug state discrimination)
  • Amphetamines & cocaine discriminate from saline but not as well as barbiturates or benzodiazepines
43
Q

Do amphetamines generalise?

A
  • Amphetamine generalizes to cocaine, MPH, & some MAO inhibitors
  • Amphetamines do not really generalize to caffeine, nicotine, barbiturates, hallucinogens
44
Q

What is the self administration of amphetamines in humans?

A
  • Sporadic (run-abstinence cycle)
  • Depends on reason for taking the drug
  • ‘speed freaks’
45
Q

What is the self-administration of cocaine in humans?

A

• Sporadic (run-abstinence cycle)
• Usually mixed with other drugs
o Speedball (+heroin) or mixed with depressants

46
Q

What is the self-administration in animals?

A
  • Cocaine administration by rats
  • More reinforcing than any other drug (monkeys)
  • Erratic pattern of administration
  • Monkeys will self-administer lethal dose
47
Q

What is the self-administration in animals increased by?

A

o Stress
o Prior experience
o Caffeine, heroine and alcohol

48
Q

What is the acute tolerance of stimulants?

A
  • Cocaine – disappears rapidly (<24 hrs)

* To subjective effects but not BP and HR

49
Q

What the the chronic tolerance?

A
  • Appetite suppression – 2 weeks
  • HR and BP
  • Lethal effects
  • No tolerance to effects on sleep
50
Q

What are the withdrawal effects?

A
  • Depression – within ½ hr for cocaine and hrs for amphetamines
  • Dose dependent severity
  • REM rebound, frequent awakenings
  • LT cocaine use can cause on-going depression; may be treated with anti-depressants
  • LT, amphetamine use can lead to suicidal thinking/attempts; may present as if clinically depressed, with changed (often increased) sleep and appetite
51
Q

What are the clinical uses of amphetamines?

A

• ADHD (Ritalin, Dexedrine, Adderall, Cylert)
o Paradoxical effect
o Suggests ADHD due to deficiency in NE & DA
• Obesity (Dexatrim, Tenuate, Sanorex)
o Tolerance to effects in 2 weeks – continue to increase dose
• Narcolepsy (Provigil – nedaphonil)
o Few side effects
o No tolerance to sleep effects
• Some cold and flu preparations

52
Q

What are the clinical uses of cocaine?

A

• Local anesthetic
o In nose, mouth etc. to ease discomfort of tubes
o Dental work

53
Q

What are the harmful effects of amphetamine?

A

• Restlessness, confusion, dizziness
• Punding, stereotyped behaviour
• Paranoid psychosis
• Internal bleeding & strokes from ↑ BP
• Cessation may → suicidal depression, & sleep disturbance (REM rebound)
• Brain damage from ruptured blood vessels in the brain; DA neuron damage (see Thompson et al., 2004)
• Lifestyle effects
HIV/AIDS, hepatitis (IV users)
Immune functioning (nutritional deficiencies, sleep disturbance)

54
Q

What are the harmful effects of cocaine?

A
  • Jaundice / liver disease
  • Inflammation & ulcers in the nose (& damage to septum)
  • Cocaine runs (financial problems)
  • Paranoia, hallucinations, cravings, antisocial behaviour, attention & concentration probs, blurred vision, weight loss
55
Q

What are the harmful effects of cocaine and amphetamine on reproduction?

A 
•	↑ sexual activity
	low doses: prolong erection, delay ejaculation; enhance female libido
•	Continuous high doses of cocaine: disinterest
•	Birth abnormalities
•	‘crack babies’
	Retardation of growth
	Premature
	Abruptio placentae
	Behavioral problems
56
Q

What happens in cocaine overdose?

A
  • Muscle weakness
  • Respiratory depression
  • Cardiovascular effects – sudden-death
57
Q

What are the phases of cocaine overdose?

A

2 phases (‘caine reaction’):

  1. Excitement followed by headache, nausea, vomiting, convulsions
  2. Lose consciousness, respiratory depression, cardiac failure, death (hypoxic brain damage risk)
58
Q

What is the treatment of overdose?

A

• OD treatment: diazepam (control seizures), artificial respiration (control breathing), chlorpromazine (antipsychotic) antagonist to toxic effects of cocaine

59
Q

What is the treatment for stimulant addiction?

A

• Detoxification
• Strong probability of relapse due to intense craving
• Pharmacotherapies: (used with mixed success)
Antidepressants (e.g., bupropion/Zyban)
Modafinil
Oral d-amphetamine
Naltrexone
• Behavioral Therapies
Contingency management, community reinforcement

PYB260 (9 decks)

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