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MD4001 Pharmacology > CNS stimulants > Flashcards

CNS stimulants Flashcards

1
Q

What are the 3 main classes of CNS stimulants?

A
  • Convulsants and respiratory stimulants
  • Psychotomimetic drugs
  • Psychomotor stimulants
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2
Q

What are the 3 main categories of harm of CNS stimulants?

A
  • Physical harm (acute vs chronic risks) (route of administration; primary or secondary risk)
  • Dependance (intensity of pleasure; tolerance, craving, withdrawal), (physical vs psychological dependance)
  • Social harm (e.g drink driving)
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3
Q

What is a primary risk associated with physical harm?

A

Anaphylaxis, overdose

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4
Q

What is a secondary risk associated with physical harm?

A

Infection

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5
Q

What are the 3 classes of drugs in the UK as classified by the UK Misuse of Drugs Act?

A
  • Class A (“most dangerous”, harshest punishment)
  • Class B
  • Class C (“least capacity for harm” - more leniant punishment)
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6
Q

What are examples of convulsants and respiratory stimulants?

A
  • Doxapram

- Strychnine

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7
Q

What are examples of psychomimetic drugs?

A
  • Hallucinogens (LSD, psilocybin, mescaline, MDMA)
  • Dissociative anaesthetics (ketamine, PCP)
  • Cannabis
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8
Q

What are examples of psychomotor stimulants?

A
  • Amphetamines, khat, cocaine, nicotine

- Methylxanthines (caffeine, theophylline)

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9
Q

What is doxapram and what is it used for?

A
  • Short acting respiratory stimulant used in respiratory failure
  • Stimulates chemoreceptors in carotid bodies in carotid chemoreceptors
  • Post-operative respiratory depression, acute respiratiry failure, neonatal apnea
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10
Q

What is a convulsant and respiratory stimulant that can lead to poisining?

A

Strychnine

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11
Q

How does strychnine cause poisining (mechanism of action)?

A
  • Powerful convulsant
  • Violent extensor spasms triggered by minor sensory stimuli
  • Blocks glycine receptors
  • Small doses cause an improvement in visual and auditory acuity (can be performance enhancing)
  • Used as a poison for centuries
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12
Q

What are examples of Psychomimetic drugs?

A

Hallucinogens

  • LSD (D-lysergic acid diethylamine)
  • Psilocybin (magic mushrooms)
  • Mescaline
  • MDMA (ecstasy)
  • DMT
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13
Q

How do psychomimetic drugs work?

A
  • Act on 5-HT receptors and transporters

- Acts on Locus coeruleus (sensory signals) and Raphe nuclei (sleep, wakefulness and mood)

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14
Q

What are the main effects of hallucinogens?

A

Mental processes
- Alter perceptions of sights and sounds
- Hallucinations (visual, auditory, tactile or olfactory)
- Sounds can be perceived as visions
- Thought processes illogical and disconnected
Can cause a ‘bad trip’ (menacing quality, paranoid delusions), flashbacks can be reported weeks or months later

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15
Q

What is the tolerance like for hallucinogens?

A
  • Develops quickly (plus cross-talk between drugs)
  • No physical withdrawal syndrome
  • Psychological effects (“flashbacks”, psychosis)
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16
Q

What are the risks associated with hallucinogen use?

A
  • Risk of injury and accidental death whilst intoxicated
  • Poisoning due to mistaken identity
  • Adrenergic effects with LSD
  • GI effects with psilocybin
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17
Q

What is the meaning of a “dirty drug”?

A

Drugs that may bind to many different molecular targets or receptors in the body, and so tend to have a wide range of effects and possibly adverse drug reactions e.g LSD

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18
Q

What are dissociative anaesthetics?

A
  • Psychomemetic drugs
  • Analgesic
  • Cause stereotyped motor behaviour like amphetamine
  • Can give a ‘bad trip’
  • NMDA receptor antagonists
    (PCP and Ketamine)
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19
Q

What is Phencyclidine (PCP, ‘angel dust’)?

A
  • Psychomemetic drug
  • Dissociative anaesthetic
  • Synthesised as a possible IV general anaesthetic
  • Found to produce disorientation and hallucinations
  • NMDA receptor antagonist
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20
Q

What is ketamine used for clinically?

A

Induction and maintenance of anaesthesia

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21
Q

What are examples of dissociative psychomimetic anaesthetics?

A
  • Phencyclidine (PCP, angel dust)

- Ketamine

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22
Q

What is tolerance and dependance like for dissociative anaesthetics?

A
  • Rapid over regular, repeated doses

- Dependance (physical and psychological) and withdrawal syndromes with PCP

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23
Q

What are the risks associated with dissociative anaesthetics?

A
  • Accidents/loss of control / automatic behaviour
  • PCP: hyperthermia, convulsions
  • Ketamine: overdose with heart attack / respiratory failure (rare)
  • Higher physical risk than classical hallucinagens
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24
Q

What are the main psychoactive metabolites of cannabis?

A

Tetrahydrocannabinol (THC) and 11-hydroxy-THC

25
Q

What type of drug is cannabis?

A

Psychomimetic

26
Q

What are examples of psychomotor stimulants?

A
  • Amphetamine
  • Dextroamphetamine
  • Methylamphetamine (ritalin)
  • Lisdexamfetamine mesylate
  • MDMA (methylphenidate, 3,4-methylenedioxymethamphetamine) (chemically similar but can be considered seperate)
27
Q

What are the main effects of psychomotor stimulants?

A
  • Locomotor stimulation
  • Euphoria and excitement
  • Insomnia
  • Anorexia (diminishes with continued use)
  • Stereotypic behaviour (chronic use)
28
Q

What is th main clinical use of Lisdexamfetamine mesylate?

A

(ADHD) Attention defecit hyperactivity disorder

29
Q

What is Lisdexamfetamine mesylate a prodrug for (metabolised into)?

A

Dextroamphetamine

30
Q

How does MDMA differ from amphetamines?

A

Substitution of aromatic ring and resembles more of the structure of mescalin - gives it a character that makes it somewhere in between psychomimetics and psychomotor stimulants

31
Q

What are the behavioural effects of amphetamines and what are these effects most likely due to?

A

Release of dopamine rather than Noradrenaline

  • Subjects become confident, hyperactive and talkative
  • Sex drive is said to be enhanced
  • Fatigue (both physical and mentl) is reduced
  • Does not enhance mental performance, just ability to concentrate for longer
32
Q

Describe the mode of action of amphetamines?

A
  • Competitive inhibitors of monoamine uptake
  • Displace monoamines (i.e. noradrenaline, dopamine) from vesicles into cytoplasm
  • Inhibit MAO at high concentrations
  • Cause NET to work in reverse causes NA to be pumped out synapse, long and insidous release of dopamine and NA
33
Q

What dies the nigrostriatal dopamine pathway control?

A

Motor

34
Q

What does the mesolimbic and mesocortical dopamine pathway control?

A

Behavioural effects

35
Q

What dies the tuberohypophyseal system / dopamine pathway control?

A

Endocrine

36
Q

What NA pathway in the brain is associated with wakefulness and alertness?

A

Locus coeruleus

37
Q

What NA pathway in the brain is associated with blood pressure regulation?

A

BP regulation

38
Q

What is the tolerance like in amphetamines?

A

Rapid tolerance euphoric and anorexic effects, slowly for other effects

39
Q

What is the dependance like for amphetamines?

A

Moderate dependance due to euphoria it produces

40
Q

What is amphetamine psychosis?

A
  • If taken repeatedly over a few days
  • Almost indistinguishable from an acute schizophrenic attack
  • Stereotypic behaviour
  • After cessation, usually a period of deep sleep (after which the subject may feel lethargic, depressed, anxious and often hungry)
41
Q

What the risks associated with amphetamines?

A
  • Vascular accidents (e.g tachycardias, arrhythmias, increased BP)
  • Cerebral convulsions and coma
  • Excitation syndrome (hypererthermia/tachycardia)
  • Anorexia
  • Cognitive impairment
  • Personality/mood
  • Chronic paranoid psychosis
42
Q

What is “Khat” (Catha edulis)?

A
  • Psychomotor stimulant
  • Contains cathinone, an amphetamine-like stimulant
  • Cause alertness, talkativeness, suppress apetite, alerntess, insomnia
  • Used as a social lubricant (NE Africa)
43
Q

What is nicotine (nicotiana tabacum)?

A
  • Psychomotor stimulant
  • Both stimulant for CNS effects, release of adrenaline via activation of splanchnic nerves of sympathetic nervous system
  • Also depressant effects
44
Q

What class of drug is cocaine (from erythroxylum coca)?

A
  • Psychomotor stimulant
45
Q

What are the effects cocaine?

A
  • Potent inhibitor of catecholamine uptake into nerve terminals (especially dopamine)

Effects resemble that of amphetamine

  • Euphoria (related to decreased dopamine and 5-HT reuptake)
  • Altertness and wakefulness
  • Increased confidence and strength
  • Heightened sexual feelings
  • Indifference to concerns/cares
46
Q

How can cocaine be absorbed?

A

Many routes

  • Nasal administration damages nasal mucosa and septum (constricts blood vessels and can lead to necrosis)
  • Free-base form (crack) can be smoked
47
Q

What is cocaine’s tolerance and dependance like?

A
  • Tolerance occurs rapidly
  • Physical dependance usually mild
  • Strong psychological dependance occurs
48
Q

What are the acute risks associated with cocaine?

A
  • CV (increased BP, HR, ventricular fibrilation, Heart attack, respiratory arrest, stroke)
  • Muscle spasms, tremor
  • Hyperthermia
  • Seizures, headaches, excited delirium
49
Q

What are the chronic risks associated with cocaine?

A
  • Heart attacks due to furring of coronary arteries
  • Malnutrition and weight loss
  • Decresased libido and impotence
  • Personality/mood (e.g anxiety, depression, repetitive behaviours, delusions, psychosis)
  • Toxic syndrome - similar to acute paranoid schizophrenia
50
Q

What are the main two methylxanthines?

A

Caffeine and theophylline

51
Q

What are methylxanthines (caffeine and theophylline) classified as?

A

Psychomotor stimulants

52
Q

What are the effects of methylxanthines, caffiene and theophylline?

A
  • CNS stimulants
  • Diuretics
  • Cardiac muscle stimulants
  • Smooth muscle relaxants (especially bronchial)
53
Q

What are the main psychological effects of methylxanthines?

A

Reduce fatugue and improve mental performance without any euphoria

54
Q

What is the mechanism of action of methylxanthines?

A
  • Inhibit cAMP/cGMP phosphodiesterases
  • Block purine receptors (adenosine receptors of the A1 and A2 subtype
  • Diuresis possibly due to vasodilation of the afferent glomerular arterioles causing increased GFR
  • Tolerance and habituation develop to a small extent
55
Q

What can theophylline be used as clinically?

A

Bronchodilator in severe asthma attacks

56
Q

What drugs are considered class A?

A
  • Cocaine
  • Methamphetamine
  • LSD
  • Ecstacy / MDMA
57
Q

What drugs are considered class B?

A
  • Amphetamines
  • Ketamine
  • Cannabis
  • Mephylphenidate
58
Q

What drug are considered class C?

A

Khat

MD4001 Pharmacology (8 decks)

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