Introduction To Morphine Flashcards
Side-effects of Morphine: 5
Nausea Constipation Tolerance Dependence Pupil constriction
Name 4 binding sites (groups) of morphine:
Phenol
Ether
Alcohol
Amine
When the R group is a H then the drug is called…
When the R group is a CH3 then the drug is called…
Morphine
Codeine
Codeine is an example of a — and has –% the activity of morphine.
prodrug
20
Codeine is metabolised in the – to produce –
Codeine is used for –/– and –.
It is a weaker —, but also has weaker –/–.
Liver Morphine Mild pain Coughs analgesic side-effects
When the OH on the – group is masked and replaced with a – group to make codeine, this – activity.
phenol
methyl
reduces
When R=Ac, the name of the drug is…
This has a – affinity for the – receptor, which – activity.
It is a – potent metabolite of –
The Acetyl group masks the — phenol group.
This compound crosses the blood/brain barrier slower/quicker?
The acetyl group is – in the brain to form –
3-Acetylmorphine low u-opioid decreases less heroin polar quicker hydrolysed morphine
The drug heterocodeine is made when a – group replaces the – group.
It is a direct – of the – receptor.
Methyl
6-Alcohol
Agonist
u-opioid
The 6-OH group is not important for –
When the 6-OH is removed, the – increases, due to the decreased –
The compound crosses the –/– barrier more –
binding activity polarity blood brain easilt
The drug 6-acetylmorphine is made when the – group is replaced with an – group.
This groups masks the – alcohol group making it – to cross the blood/brain barrier.
The – group is free so binding can happen –
dependance is high/low?
6-alcohol acetyl polar easier phenol immediately high
Heroin:
This is where which (2) reactive groups of morphine are replaced with which (1) group?
Heroin has increased/decreased lipid solubility?
Crosses BBB more slowly/quickly?
The — groups are hydrolysed in the — to generate –
The euphoric effects have – onset
Phenol 6-alcohol Acetyl increased quickly acetyl brain morphine rapid
Dihydromorphine:
This is when the – group is removed
This leads to a –% increase/decrease in activity
Alkene
20
increase
When the – group is removed there is – activity.
This means the – is essential for –
Nitrogen
zero
nitrogen
binding
Normorphine:
When NR=N(?)
Reduces activity by –%
Normorphine is more/less polar and therefore crosses the BBB slower/quicker?
Ionised molecules cant cross the –/–/– and are –
Ionised structures are only active if – directly into the –
H 25 more slower BBB inactive injected brain
What is a pharmacophore?
An abstract description of molecular features which are necessary for molecular recognition of a ligand by a biological macromolecule.
