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PHAR > applying PD/PK theory to examplar drugs-Psychoactive drugs; depressants > Flashcards

applying PD/PK theory to examplar drugs-Psychoactive drugs; depressants Flashcards

1
Q

what are depressants

A

drugs that typically suppress or slow the activity of nerves within the central nervous

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2
Q

what is the most potent cannabinoid?

A

delta9-tetrahydrocannabinoid (delat9-THC)

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3
Q

how is the lipid solubility of a drug determined?

A

octane/water partition coefficient

octane–>liphopilic

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4
Q

how can ethanol cross lipid membrane while being water soluble?

A

lipid membrane are slightly permeable to small uncharged molecules like ethanol so it can diffuse across lipid membranes and access tissues

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5
Q

how to calculate the units of alcohol?

A

alchohol by volumexvolume(mL)/1000

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6
Q

how to calculate the amount of absolute alcohol?

A

alcohol by volumex0.78xvolume per 100mL

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7
Q

what is the local driving limit in the UK?

A

80mg of alcohol/100mL

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8
Q

what tissue membrane is more important for alcohol to reach?

A

small intestine/ileum

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9
Q

what tissue membrane is more important for cannabis to reach?

A

alveoli/alveolus

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10
Q

what is the major obstacle of the oral route of administration?

A

stomach

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11
Q

what factors influence drug distribution?

A

regional blood flow
capillary permeability
tissue localisation
plasma protein binding

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12
Q

does capillary permeability have a big impact on the ability of alcohol and cannabis to access tissues? why?

A

no
because
ethanol –> really small
cannabis –> lipid soluble

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13
Q

why would alcohol be metabolised much faster than cannabis?

A

because most delta9-THC are very highly bound to plasma proteins in the blood and alcohol does not bind to plasma proteins very effectively.
only free drug can be metabolised and eliminated

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14
Q

what tissue and organ have the most water content?

A

blood plasma>liver>brain»>adipose tissue

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15
Q

what tissue/organ have the most fat content?

A

adipose tissue»>liver>brain>blood plasma

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16
Q

2 enzymes are responsible for the majority of alcohol metabolism. what are they?

A

alcohol dehydrogenase -> responsible for 75% of the hepatic metabolism of ethanol to acetaldehyde
aldehyde dehydrogenase –> converts acetaldehyde to acetic acid

17
Q

where can we find these 2 enzymes?

A

in the stomach

18
Q

do females have more or less alcohol dehydrogenase?

A

less

19
Q

another enzyme is used for alcohol metabolism. what enzyme is it? when is it unregulated?

A

cytochrome p450

after chronic alcohol used –> alcohol tolerance

20
Q

do ethanol and delta9-THC have active metabolites?

A

acetaldehyde –> largely responsible for side effects associated with alcohol
11OH-THC–>very lipid soluble which also have the same known effects of cannabis

21
Q

what is the drug target of cannabis?

A

cannabinoid receptor

22
Q

what does the activation of the cannabinoid receptor do?

A

it decreases the activity of adenalyte cyclase which means that it decreases the activity of the cell and therefore have a depressant effect

23
Q

what is andamide?

A

endogenous agonist of the cannabinoid receptor

24
Q

does alcohol have a specific target?

A

no

it can induce weak effects on a number of different targets

25
Q

to what receptor can alcohol bind?

A

opioid receptors that have a number of binding sites

26
Q

how can alcohol have a depressant effect?

A

it needs to inhibit an excitatory effect or increase an inhibitory factor

27
Q

what are 2 common shared effects of alcohol and cannabis?

A

inducing memory loss

impairing psychomotor performance

28
Q

what parts of the brain are vital for formation of memory?

A

dentate gyrus within hippocampus

29
Q

what does the activation of cannabinoid receptors on mitochondria within the dentate gyrus do?

A

leads to impaired memory formation

30
Q

what parts of the brain are important for psychomotor performance? are cannabinoid present in these areas?

A

basal ganglia
cerebral cortex
cerebellum
yes

31
Q

what is the most dangerous toxic effect of alcohol?

A

respiratory depression

in extreme cases: breathing rate could drop so severely –>suffocate

32
Q

can cannabis affect respiration?

A

a little bit since very little cannabinoid receptors in medulla which provides the impulse to breath

33
Q

what is the major toxic effect associated with cannabis?

A

psychosis: inability to display appropriate behiavour within a given context

34
Q

will opioid receptor affect GABA?

A

yes. opioid–> depressant receptor

35
Q

will the bioavailability be affected by the rate of metabolism?

A

no it will be affected by the stomach (whether it is empty or not)

PHAR (5 decks)

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