Drug metabolism Flashcards

1
Q

what are the 4 stages of a drugs journey through the body

A

absorption
distribution
metabolism
excretion

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2
Q

absorption

A

drugs are absorbed from administration site to the body’s circulation

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3
Q

give 5 examples to administer drugs

A
oral
intramuscular
subcutaneous
intravenous
transdermal
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4
Q

what is oral administration of drugs

A

swallowing

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5
Q

what is intramuscular administration of drugs

A

flu jab in arm muscle

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6
Q

what is subcutaneous administration of drugs

A

injecting insulin just under the skin

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7
Q

what is intravenous administration of drugs

A

chemotherapy through vein

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8
Q

what is transdermal administration of drugs

A

wearing skin patch

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9
Q

distribution

A

main vehicle - bloodstream

undesired effects = side effects, toxicity

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10
Q

what is the purpose of metabolism

A

deactivate the medicine (sometimes activate the drug)

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11
Q

metabolism

A

process to break down medicine via enzymatic process

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12
Q

what is the main site of metabolism

A

liver

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13
Q

what are the products of metabolism called

A

metabolites

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14
Q

excretion

A

removal of compounds via urine or faeces

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15
Q

name 4 things monitoring metabolism will provide

A

what drug has been used

how effective the person processes the drug

how long the drug stays in the body

what happens to the drug

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16
Q

what is drug metabolism also known as

A

biotransformation

17
Q

what two phases is drug metabolism divided into

A

phase 1 = functionalisation phase

phase 2= conjugation phase

18
Q

which metabolism phase is studied the most

A

phase 1

19
Q

phase 1 common drug metabolism routes

A

oxidation, reduction, hydrolysis

20
Q

phase 2 common drug metabolism routes

A

conjugation and condensation

21
Q

purpose of phase 1

IMPORTANT

A

to expose or add polar function group to the original molecule

22
Q

purpose of phase 2

IMPORTANT

A

to add a very polar molecule to the metabolite or the original molecule to make the molecule water soluble and read for excretion

23
Q

oxidation

A

adding OH group - replacing H in the molecule

adding O such as alcohol - aldehyde

losing hydrogen - carbon carbon single bond to double bond

24
Q

reduction

A

losing or reducing some form of O

carboxylic acid to alcohol

25
Q

hydrolysis

A

Breaking up a molecule by water

Ester to alcohol and carboxylic acid

26
Q

what are two oxidation reactions involving cytochrome P450

A

aromatic hydroxylation

de-alyklation

27
Q

what is aromatic hydroxylation

A

using OH group to replace aromatic ring hydrogens

oxidation reaction

28
Q

what is de-alkylation reaction

A

removes alkyl groups such as methyl and ethyl

depending on type of atom the alkyl group is attached to is often referred to as N- or O- dealkylations

29
Q

what are 3 oxidation reactions not catalyses by cytochrome P450

A

alcohol dehydrogenase

aldehydge dehydrogenase

hydrolysis

30
Q

summary of phase 1 metabolism

A

Virtually every possible chemical reaction a compound can undergo in the lab can also be catalysed by enzyme systems

The products normally end up containing chemically reactive functional groups such as, OH, NH2, COOH

Many drugs can undergo more than one of the phase 1 reactions

31
Q

phase 2 metabolism

A

the phase 2 (conjugation) generally leads to a water-soluble product can be excreted in faeces or urine

the most commonly used sugar for this purpose is glucuronic acid which can conjugate with alcohol, phenol, amine and COOH

phase 2 metabolites are more water-soluble

preparing the drug or the metabolite for excretion by one pathway or another

32
Q

genetic factors affecting drug metabolism

A

body weight
race
sex

33
Q

physiologic factors affecting drug metabolism

A
age
diet
diseases/conditions
kidney function
liver function
34
Q

morphine as an opioid analgesic

A

μ-Opioid receptor (MOR) in the central nervous system

Morphine is an agonist of this receptor

μ-Opioid receptor activation causes analgesia and sedation

Opioid addiction also related to μ-opioid receptor

Class A

35
Q

codeine

A

Codeine does crossed BBB but can’t bind effectively to the opioid receptor

Only 15% of codeine is O-demethylated to morphine

The principal pathways for metabolism of codeine occur in the liver

Less strong biological effect

Class B

36
Q

heroin

A

Heroin is totally metabolised into morphine when taken orally

If injected it will rapid crossing BBB into the brain (a lipophilic molecule)

Then rapidly metabolised into morphine

So you have a high concentration of morphine in the brain to bind to the opioid receptor

Class A