Tylenol 3

[MountainPharmD]

I actually agree with priapism on this one...

50 posts on T#3...

Its better than the 5 miliion replies to the Cycloketocaine... (NCAA Football rambling thread) which has nothing to do with pharmacy.....

---

Members don't see this ad.

 

[DoctorRx1986]

Its better than the 5 miliion replies to the Cycloketocaine... (NCAA Football rambling thread) which has nothing to do with pharmacy.....

Well, you are right on that one. I am the creator of this thread, but like you say, it is actually relevant to pharmacy and not something about your first big purchase, which has far more replies than this one.

 

[cycloketocaine]

Well, you are right on that one. I am the creator of this thread, but like you say, it is actually relevant to pharmacy and not something about your first big purchase, which has far more replies than this one.

No trashing my thread. Not everyone thinks about pharmacy 24/7.

 

[sleazye]

Why do slight differences in functional groups on the otherwise similar looking molecule have such a dramatic effect in drug potency? For example, I've read that diacetylmorphine, which is heroin, and contains a similar structure to codeine and morphine, is far more potent than codeine. I obviously knew this, but why does the presence of those two acetyl groups, CH3CO, have any difference in potency? What do those acetyl groups do to make heroin more potent?


Heroin can cross the blood brain barrier (nonpolar), morphine can not (polar). Heroin is metabolized to morphine and can not diffuse out across the BBB again; therefore, longer, more intense DOA of heroin.

 

[firefighter9015]

Why do slight differences in functional groups on the otherwise similar looking molecule have such a dramatic effect in drug potency? For example, I've read that diacetylmorphine, which is heroin, and contains a similar structure to codeine and morphine, is far more potent than codeine. I obviously knew this, but why does the presence of those two acetyl groups, CH3CO, have any difference in potency? What do those acetyl groups do to make heroin more potent?


Heroin can cross the blood brain barrier (nonpolar), morphine can not (polar). Heroin is metabolized to morphine and can not diffuse out across the BBB again; therefore, longer, more intense DOA of heroin.

Changes in functional groups change the lipophilicity of the drug, therefore chaning its potency and ability to cross the BBB.

 

[Priapism321]

Heroin can cross the blood brain barrier (nonpolar), morphine can not (polar). Heroin is metabolized to morphine and can not diffuse out across the BBB again; therefore, longer, more intense DOA of heroin.

Morphine can not cross the blood brain barrier? I mean, pharmacology changes rapidly, but this sounds like a major break through. How does it cause analgesia if it can't penetrate into the CNS? I am ready to be intrigued. Does this mean morphine does not cause respiratory depression?

 

[DoctorRx1986]

Morphine can not cross the blood brain barrier? I mean, pharmacology changes rapidly, but this sounds like a major break through. How does it cause analgesia if it can't penetrate into the CNS? I am ready to be intrigued. Does this mean morphine does not cause respiratory depression?

I'm not a pharmacy student just yet, so correct me if i'm mistaken, but I do believe morphine causes respiratory depression because like other opiates, it binds to opioid receptors such as the mu, kappa, and delta in the CNS. Some of these receptor variations and receptor subunits do give rise to RD upon activation by the drug molecule. Also, codeine, which is a prodrug of morphine, is said to cause RD. Therefore, morphine should cause RD. I'm also wondering the same thing about the analgesic effects of morphine if it can't penetrate the CNS. How does it bind to opioid receptors that are mostly located in the brain and spinal cord if it can't cross the BBB?

 

[RxWildcat]

I'm not a pharmacy student just yet, so correct me if i'm mistaken, but I do believe morphine causes respiratory depression because like other opiates, it binds to opioid receptors such as the mu, kappa, and delta in the CNS. Some of these receptor variations and receptor subunits do give rise to RD upon activation by the drug molecule. Also, codeine, which is a prodrug of morphine, is said to cause RD. Therefore, morphine should cause RD. I'm also wondering the same thing about the analgesic effects of morphine if it can't penetrate the CNS. How does it bind to opioid receptors that are mostly located in the brain and spinal cord if it can't cross the BBB?

there was a truckload of sarcasm that you missed in his post.

 

[firefighter9015]

Morphine can not cross the blood brain barrier? I mean, pharmacology changes rapidly, but this sounds like a major break through. How does it cause analgesia if it can't penetrate into the CNS? I am ready to be intrigued. Does this mean morphine does not cause respiratory depression?

A more correct way to put that is that morphine does not cross the BBB as rapidly as heroin does.

 

[Priapism321]

Apparently no one on this board senses sarcasm. I guess I will have to revert back to the good old days and resort to personal attacks on less than intelligent posts.

 

[Requiem]

Apparently no one on this board senses sarcasm. I guess I will have to revert back to the good old days and resort to personal attacks on less than intelligent posts.

hahahahah I love it. You need to post more. What are you planning to do post residency?

 

[sleazye]

Morphine can not cross the blood brain barrier? I mean, pharmacology changes rapidly, but this sounds like a major break through. How does it cause analgesia if it can't penetrate into the CNS? I am ready to be intrigued. Does this mean morphine does not cause respiratory depression?

Haha, yeah sorry, my bad. Morphine does not cross the BBB as readily as heroin but does cross.

 

[DrugDealer]

For example, I've read that diacetylmorphine, which is heroin, and contains a similar structure to codeine and morphine, is far more potent than codeine. I obviously knew this, but why does the presence of those two acetyl groups, CH3CO, have any difference in potency? What do those acetyl groups do to make heroin more potent?

Just what everyone else says -- those 2 acetyl groups make heroin more lipophilic, more fat-soluble. It can cross the BBB much more rapidly than morphine, whose polar groups encounter more resistance when they stumble upon the BBB.

Beause it almost instantly enters the BBB, heroin is much more addicting. You know that when you take it, you will get instant gratification. Humans are, in general, quite impatient and do not want to wait for the morphine or codeine to kick in. Thus, these drugs are less likely to be abused than heroin.

 

[Priapism321]

hahahahah I love it. You need to post more. What are you planning to do post residency?

I will be doing what all young Pharmacists who just can't get enough of the 65 hour work weeks and low salary do post residency: another residency.

 

[MountainPharmD]

Apparently no one on this board senses sarcasm. I guess I will have to revert back to the good old days and resort to personal attacks on less than intelligent posts.

Good plan....you should never get away from what works the best....

 

[Requiem]

I will be doing what all young Pharmacists who just can't get enough of the 65 hour work weeks and low salary do post residency: another residency.

Excellent, what field?

 

[Priapism321]

Excellent, what field?

Hematology/Oncology/Stem Cell Transplantation

 

[Knipps]

sarcasm on the internet is hard to interpret.. most of it is followed by some sort of smiley

 

[Requiem]

sarcasm on the internet is hard to interpret.. most of it is followed by some sort of smiley

Nah. The same type of people who miss sarcasm in real life miss it on the internet. Those who grasp it can tell immediately. Or I might just be being sarcastic right now, but those in the know, know.