Drugs Affectinf CNS Flashcards
What are the two groups of opium
What is the natural substrate for opioid receptors
Endorphins
On which receptor does the morphine mostly act
What is not a natural substrate
Morphine
List the effects of Mu-2 activation
Analgesia
Respiratory depression
Euphoria
Decrease GI motility
Physical dependence
Explain opioids and stereoselectivity
What are the opioid therapeutic challenges
What is the difference between OH at position 3 and 6 in morphine
What are the essential pharmacophoric elements of morphine
Explain codeine
Explain metabolism of codeine
Metabolized by o demethylation to give morphine
Explain codeine taken with grapefruit juice
Explain heroin
What are the 3 problems associated with analgesic narcotics
Tolerance
Dependence
Withdrawal symptoms
What are the morphine derivatives antagonists
Naloxone and naltrexone
Explain the activity of naltrexone
Naloxone and naltrexone are used for what
To treat overdose of morphine and heroin
What is one of the signs of morphine poisoning
Acute miosis ( pinpoint pupils)
Explain the binding mode for N-phenethylmorphine
Explain the binding modes for N-allylmorphine
What is the influence of 14-OH group
How to convert morphine to antagonist
Add allyl group
Add OH group
What happens when there is modification to the phenolic OH group in morphine
Decreases activity and addiction
(Codeine used as antitussive)
What happens when there is modification to the alcoholic OH group
Increases activity and addiction because decreased polarity
so more active because less polarity meaning it can penetrate the BBB more
Why is heterocodein less active in vitro
Because of the methods group which is a bulky group so prevent binding
Explain hydrocodone
