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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
What type of drug is cannabis?
Psychomimetic
26
What are examples of psychomotor stimulants?
- Amphetamine - Dextroamphetamine - Methylamphetamine (ritalin) - Lisdexamfetamine mesylate - MDMA (methylphenidate, 3,4-methylenedioxymethamphetamine) (chemically similar but can be considered seperate)
27
What are the main effects of psychomotor stimulants?
- Locomotor stimulation - Euphoria and excitement - Insomnia - Anorexia (diminishes with continued use) - Stereotypic behaviour (chronic use)
28
What is th main clinical use of Lisdexamfetamine mesylate?
(ADHD) Attention defecit hyperactivity disorder
29
What is Lisdexamfetamine mesylate a prodrug for (metabolised into)?
Dextroamphetamine
30
How does MDMA differ from amphetamines?
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
What are the behavioural effects of amphetamines and what are these effects most likely due to?
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
Describe the mode of action of amphetamines?
- 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
What dies the nigrostriatal dopamine pathway control?
Motor
34
What does the mesolimbic and mesocortical dopamine pathway control?
Behavioural effects
35
What dies the tuberohypophyseal system / dopamine pathway control?
Endocrine
36
What NA pathway in the brain is associated with wakefulness and alertness?
Locus coeruleus
37
What NA pathway in the brain is associated with blood pressure regulation?
BP regulation
38
What is the tolerance like in amphetamines?
Rapid tolerance euphoric and anorexic effects, slowly for other effects
39
What is the dependance like for amphetamines?
Moderate dependance due to euphoria it produces
40
What is amphetamine psychosis?
- 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
What the risks associated with amphetamines?
- 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
What is "Khat" (Catha edulis)?
- Psychomotor stimulant - Contains cathinone, an amphetamine-like stimulant - Cause alertness, talkativeness, suppress apetite, alerntess, insomnia - Used as a social lubricant (NE Africa)
43
What is nicotine (nicotiana tabacum)?
- Psychomotor stimulant - Both stimulant for CNS effects, release of adrenaline via activation of splanchnic nerves of sympathetic nervous system - Also depressant effects
44
What class of drug is cocaine (from erythroxylum coca)?
- Psychomotor stimulant
45
What are the effects cocaine?
- 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
How can cocaine be absorbed?
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
What is cocaine's tolerance and dependance like?
- Tolerance occurs rapidly - Physical dependance usually mild - Strong psychological dependance occurs
48
What are the acute risks associated with cocaine?
- CV (increased BP, HR, ventricular fibrilation, Heart attack, respiratory arrest, stroke) - Muscle spasms, tremor - Hyperthermia - Seizures, headaches, excited delirium
49
What are the chronic risks associated with cocaine?
- 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
What are the main two methylxanthines?
Caffeine and theophylline
51
What are methylxanthines (caffeine and theophylline) classified as?
Psychomotor stimulants
52
What are the effects of methylxanthines, caffiene and theophylline?
- CNS stimulants - Diuretics - Cardiac muscle stimulants - Smooth muscle relaxants (especially bronchial)
53
What are the main psychological effects of methylxanthines?
Reduce fatugue and improve mental performance without any euphoria
54
What is the mechanism of action of methylxanthines?
- 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
What can theophylline be used as clinically?
Bronchodilator in severe asthma attacks
56
What drugs are considered class A?
- Cocaine - Methamphetamine - LSD - Ecstacy / MDMA
57
What drugs are considered class B?
- Amphetamines - Ketamine - Cannabis - Mephylphenidate
58
What drug are considered class C?
Khat

MD4001 Pharmacology (8 decks)

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