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Pharmacology > 27 Psychoactive drugs > Flashcards

27 Psychoactive drugs Flashcards

1
Q

27.01 PSYCHOMOTOR STIMULANTS

Amfetamine, methylenedioxymethamfetamine (MDMA), methylphenidate - actions

A

CNS stimulation: arousal, alertness, concentration
euphoria/excitement
stereotyped behaviour
anxiety
reduced appetite
sympathomimetic actions: tachycardia, pupillary dilation, etc.

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2
Q

27.01 PSYCHOMOTOR STIMULANTS

Amfetamine, methylenedioxymethamfetamine (MDMA), methylphenidate - MOA

A

inhibits neuronal reuptake of MA, inhibits MAO and vesicular MA transporter
raised cytosolic levels of MAs and release from nerve terminals, mainly by reverse operation of the MA transporter
increased MA levels in synapse
sympathomimetic actions due to release of NA in the periphery

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3
Q

27.01 PSYCHOMOTOR STIMULANTS

Amfetamine, methylenedioxymethamfetamine (MDMA), methylphenidate - abs/distrib/elim

A

orally active
amfetamine half-life 10h
renal excretion enhanced by urine acidification
methylphenidate is also administered by patch

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4
Q

27.01 PSYCHOMOTOR STIMULANTS

Amfetamine, methylenedioxymethamfetamine (MDMA), methylphenidate - clinical use

A

attention-deficit hyperactivity disorder (ADHD), narcolepsy

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5
Q

27.01 PSYCHOMOTOR STIMULANTS

Amfetamine, methylenedioxymethamfetamine (MDMA), methylphenidate - adverse effects

A

aggression, restlessness, insomnia, paranoia
anorexia, weight loss
psychotic states/hallucinations
dependence
dehydration/hyper­thermia (MDMA)
hypertension
sudden death in patients with pre-existing cardiac abnormalities

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6
Q

27.02 PSYCHOMOTOR STIMULANTS

Methylxanthines: caffeine, theophylline - actions

A

psychomotor stimulant effects, mild diuresis, stimulation of cardiac muscle, relaxation of smooth muscle (especially bronchial muscle)

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7
Q

27.02 PSYCHOMOTOR STIMULANTS

Methylxanthines: caffeine, theophylline - MOA

A

antagonism of A2 purine receptors and part inhibition of phosphodiesterase
peripheral actions are exerted mainly on the heart, smooth muscle and kidney

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8
Q

27.02 PSYCHOMOTOR STIMULANTS

Methylxanthines: caffeine, theophylline - abs/distrib/elim

A

given orally

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9
Q

27.02 PSYCHOMOTOR STIMULANTS

Methylxanthines: caffeine, theophylline - clinical use

A

caffeine is included with aspirin in some preparations for treating headaches
treatment of apnoea of prematurity
theophylline is mainly used as a bronchodilator in severe asthma

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10
Q

27.02 PSYCHOMOTOR STIMULANTS

Methylxanthines: caffeine, theophylline - adverse effects

A

hyperglycaemia, tachycardia
caffeine withdrawal symptoms include headache and irritability

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11
Q

27.03 PSYCHOMOTOR STIMULANTS

Nicotine - actions

A

CNS stimulant
peripherally, stimulates autonomic ganglia

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12
Q

27.03 PSYCHOMOTOR STIMULANTS

Nicotine - MOA

A

central effects are on nicotinic acetylcholine receptors (nACRs), which are widely expressed in the brain
balance between activation of nACRs, causing neuronal excitation, and desensitisation, causing synaptic block
peripheral effects result from stimulation of autonomic ganglia and peripheral sensory receptors, mainly in the heart and lungs (tachycardia, increased cardiac output and arterial pressure, reduced GI motility, sweating)

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13
Q

27.03 PSYCHOMOTOR STIMULANTS

Nicotine - abs/distrib/elim

A

nicotine is metabolised to cotinine, mainly in the liver, within 1-2h

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14
Q

27.03 PSYCHOMOTOR STIMULANTS

Nicotine - clinical use

A

nicotine replacement therapy improves chances of giving up smoking

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15
Q

27.03 PSYCHOMOTOR STIMULANTS

Nicotine - adverse effects

A

tolerance develops rapidly to the effects of nicotine, giving rise to physical and psychological dependence

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16
Q

27.04 CNS DEPRESSANTS

Ethanol - actions

A

CNS depressant

17
Q

27.04 CNS DEPRESSANTS

Ethanol - MOA

A

enhancement of GABA and glycine action, inhibition of calcium channel opening, activation of potassium channels and inhibition at NMDA-type glutamate receptors, inhibition of adenosine transport

18
Q

27.04 CNS DEPRESSANTS

Ethanol - abs/distrib/elim

A

given orally
rapid absorption, substantial fraction cleared by first-pass metabolism
about 80% metabolised, 5-10% excreted unchanged in expired air and in urine

19
Q

27.04 CNS DEPRESSANTS

Ethanol - clinical use

A

little or no therapeutic value, but widely used in many countries for its psychoactive properties

20
Q

27.04 CNS DEPRESSANTS

Ethanol - adverse effects

A

neurological degeneration occurs with heavy and binge drinking, causing dementia and peripheral neuropathies
long-term ethanol consumption causes liver disease, progressing to cirrhosis and liver failure
physical and psychological dependence
ethanol misuse during pregnancy can result in impaired foetal development and foetal alcohol syndrome

21
Q

27.04 CNS DEPRESSANTS

Ethanol - special notes

A

disulfiram can be used as aversion therapy to discourage ethanol excess
if combined with ethanol, it results in a severe reaction (flushing, tachycardia, hyperventilation and distress) due to excessive acetaldehyde accumulation in the bloodstream

22
Q

27.05 OTHER PSYCHOACTIVE DRUGS

Cocaine

A

sympathomimetic action: inhibits uptake of dopamine, serotonin and noradrenaline transport

23
Q

27.05 OTHER PSYCHOACTIVE DRUGS

Benzodiazepines

A

CNS depressant

24
Q

27.05 OTHER PSYCHOACTIVE DRUGS

Zopiclone and other Z drugs

A

CNS depressant

25
Q

27.05 OTHER PSYCHOACTIVE DRUGS

Gabapentin and pregabalin

A

CNS depressant

26
Q

27.05 OTHER PSYCHOACTIVE DRUGS

Ketamine

A

blocks the NMDA-type glutamate receptor ion channel
misuse associated with ulcerative cystitis, liver damage and bladder pain

27
Q

27.06 MAJOR PSYCHEDELIC DRUGS

Lysergic acid deithylamide (LSD)

A

interacts with 5-HT and dopamine receptors
psychotomimetic action attributed to 5-HT2A receptors enhancing glutamatergic transmission in the cerebral cortex is very potent - causes a long-lasting sense of dissociation and disordered thought

28
Q

27.06 MAJOR PSYCHEDELIC DRUGS

Mescaline

A

agonist at 5-HT2A and other 5-HT receptors
related to amfetamine
derived from Mexican peyote cactus

29
Q

27.06 MAJOR PSYCHEDELIC DRUGS

Psilocybin

A

metabolised to psilocin
related to 5-HT
active substance in magic mushrooms

30
Q

27.06 MAJOR PSYCHEDELIC DRUGS

Salvinorin A

A

opioid receptor agonist
known as ‘herbal ecstasy’
contained in Salvia divinorum

Pharmacology (34 decks)

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