Pharmaceutical Chemistry Revision

4th Year Pharmacy 2010-2011

Opioids

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1) Answer the following questions:

1A B

Generic: Action:

Why does each drug act like this?

Mention the use of drug (B).

2A B

Generic: Action:

Opioids Used as Antitussives

What are the common str. similarities for both to act as antitussives?

What are the proposed MOA for both?

Mention the proposed metabolism of one of them.

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3A B

Generic: Action:

Which one of them has better affinity for the receptor? Why?

Which of them is stronger? Why?

4A B

Generic: Action:

Which of them is stronger? Why?

Mention the specific use for both drugs.

Enumerate a better alternative for drug (A).

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5A B

Generic: Action:

Which of them is stronger?

Mention the stereochemistry aspects of both indicating their uses.

6A B

Generic: Action:

Why does drug (A) co-administrated with Atropine?

Which is stronger, Drug (B) or Codeine?

Mention the metabolism of drug (A) indicating its activity.

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2) Complete the following statements:

1- "Opiate" is ........ 2- "Opioids" are substances that have ....effects and this effect is blocked by.. 3- .. are opioid peptides isolated from mammalian tissues. 4- Opioids agonist binding sites are ..&.....&.....&.. 5- Opioids that interact ..with the receptor are antagonists. Opioids that interact ..with the receptor are agonists. 6- Morphine is selective for.. receptors and naturally occurring as rotatory. 7- The ..&.....&..... are the most important structure features found in opioids. 8- For mild inflammatory pain we use ..+.. 9- Strong parentral opioids (e.g Fentanyl) are used in case of .... 10- .. is used in obstetrics, due to ..... 11- Buprenorphine blocks the effect of high doses of ..

12- .. used to reverse coma and respiratory depression of opioid overdoses. 13- ..&.. used in opioid addict treatment programs. 14- When opioids are released onto cholinergic neurons .. Ach release, and .. peristalsis. 15- Diphenoxylate HCl is metabolized by ..to 16- Atropine is combined with Diphenoxylate HCl to 17- Codeine Phosphate used as antituusive as it & 18- N-oxides and N-methyl quaternary salts of Morphine are 19- If an opioid contains N-methyl substituent (3-5 carbons), it acts as 20- If an opioid contains N-methyl substitution, it acts as
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21- sterically forces the substituent to remain equatorial. 22- Codeine is agonist and undergoes metabolic to Morphine. 23- Heroin is metabolized towhich cause 24- Removal of epoxide bridge give group. 25- The oxygen bridge is for activity. 26- Methadone is useful due to his activity and duration of action. 27- are flexible molecules have aromatic ring and basic nitrogen essential for activity and is not essential.

28- is the prototype of 4-Phenylpepridines, and has onset and duration of action so used in .. 29- Fentanyl is Morphine potency. 30- & have higher potency and higher safety margin than Fentanyl.

3) Modify the following structures as required:

Strusture 1Modify to Full Antagonist Write your answer here

2-

Its metabolite

3-

Antitussive

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