Papaverine Hydrochloride

[Ale]

Has anyone tried Papaverine Hydrochloride..alone or combined with any other opiate?
For those who wonder what I'm talking about..Papaverine is an opium alkaloid used mainly in the treatment of visceral spasms.While it is found in the opium poppy, papaverine differs in both structure and pharmacological action from the other opium alkaloids (the so called opiates).

[samuraigecko]

Papaverine was considered to be an "inactive" alkaloid because it did not hold any analgesic properties. However, since around the mid 80's different branches of pharmeceutical companies have been working on different synergies of opiate alkaloids using obscure and not often used alkaloids as a starting point molecule for synthesizing analgesic opiate / opioids.

Much earlier than this the trend was first started with thebaine, which made an awesome starting point for semi synthetic opiates and models for fully synthetic opioids. Some of the most notable being Oxy / Hydro Codones.

Papaverine is supposed to have a very small sedative property from what SWIM remembers of it (although he would have to do some reading on this) and the alkaloid primarily acts in GABA receptors also (if he remembers correctly, if someone has more knowledge on this please feel free to jump on in and correct SWIM).

Oripavine has also been cosidered for a number of synergies which unfortunately never worked out to ones knowledge.

However, if papaverine turns out to be a viable source of a sedative or even a semi-opioid sedative then SWIM is all for it. The price of it would be rather cheap because it is not only the somniferum species of poppy that produces papaverine. It is found in Iceland poppy, California poppy, prickly poppy etc etc and in fairly good quantities too.

Great find by the way, this has real potential for hypothetical situations and great debate.

[Ale]

Many other semi-synthetic opioids are synthesized from Thebaine..such as..oxymorphone, nalbuphine, naloxone, naltrexone, buprenorphine and etorphine among the others.
Swim thought that Hydrocodone was mainly derived from codeine, but I guess it IS derived from Thebaine too..not so sure about this though.
Btw..yeah SWIM thoguht it could be an interesting topic to discuss..unfortunately he doesn't think there's a lot of people who have experiences to share with this obscure alkaloid..actually I'm surprised this thred already got two replies..lol.

[Orchid_Suspiria]

It hurts swim to even hear that trash naloxone called an "opiate".

[samuraigecko]

Originally Posted by Ale

Many other semi-synthetic opioids are synthesized from Thebaine..such as..oxymorphone, nalbuphine, naloxone, naltrexone, buprenorphine and etorphine among the others.
Swim thought that Hydrocodone was mainly derived from codeine, but I guess it IS derived from Thebaine too..not so sure about this though.
Btw..yeah SWIM thoguht it could be an interesting topic to discuss..unfortunately he doesn't think there's a lot of people who have experiences to share with this obscure alkaloid..actually I'm surprised this thred already got two replies..lol.

Hydrocodone has two current methods of synthesis, both of which end up with the same compound.
The first is a combination synthesis of codeine and thebaine and the second is totally synthesized from thebaine alone.
SWIM thinks the latter may be because of cost effectiveness in some companies as thebaine is cheaper and produced in larger quantities.

SWIM also found this which also supports his first theory that it may well also be used as a sedative / hypnotic >

Papaverine hydrochloride is the hydrochloride of an alkaloid obtained from opium or prepared synthetically. It belongs to the benzylisoquinoline group of alkaloids. It does not contain a phenanthrene group as do morphine and codeine. Papaverine hydrochloride is 6,7-dimethoxy-1-veratrylisoquinoline hydrochloride and contains, on the dried basis, not less than 98.5% of C20H21NO4HCI. The molecular weight is 375.85.

Papaverine hydrochloride occurs as white crystals or white crystalline powder. One gram dissolves in about 30 mL of water and in 120 mL of alcohol. It is soluble in chloroform and practically insoluble in ether.

Papaverine Hydrochloride Injection is a clear, colorless to pale-yellow solution.

Papaverine hydrochloride, for parenteral administration, is a smooth-muscle relaxant that is available in vials containing 30 mg/mL papaverine hydrochloride. Each vial also contains edetate disodium, 0.005%. Sodium hydroxide may have been added during manufacture to adjust the pH

smooth muscle relaxant rather than a deep tissue muscle / intra skeletal muscle relaxant like benzo class drugs which means it would be more effective in relaxing smooth tissue rather than hard tissue. These tissues would include the heart, lungs, liver, kidneys, etc. It would probably stop one from being able to get a boner also (LOL). It seems as though this medication has great potential for alleviating the pain and / or discomfort of certain ailments caused by an abnormality in smooth tissue systems.

Hope this has been of help SWIM thinks this thread has potential . . . an opiate which has the potential to be actually classed as a sedative / hypnotic? mmm . . . One wonders if this opiate it as addictive as all other opiates . . . but thats probably a rather dumb question. LOL. However, since it does not contain the phenanthrene group (responsible for mu-opioid affinity and analgesia) as with other opiate alkaloids perhaps the potential for abuse and / or addiction are more minimal? One would love to learn more of this.

[Ale]

Originally Posted by Orchid_Suspiria

It hurts swim to even hear that trash naloxone called an "opiate".

Yeah..in this case we say opioid(not opiate anyway) to refer to any kinda compound with opiate-receptor antagonist properties.

[samuraigecko]

Originally Posted by Ale

Yeah..in this case we say opioid(not opiate anyway) to refer to any kinda compound with opiate-receptor antagonist properties.

well actually this has been of large debate also and opiates ARE opiate receptor agonists as are opioids, the true meanings of both opiate and opioid are described HERE >>> what makes an opiate

So in effect it would be technically an opiate and not an opioid because an opiate is something that is derived from the opium poppy either natural or semi-synthetic. Opioids are generally classed as "fully synthetic" although the opioid base meaning is to classify ALL mu-opioid receptor agonists as a generalist overview.

One thinks that the poster was actually being sarcastic in an amusing way, since naloxone is used to bring one down from their high rather than bring one up to their high. This is not to detract from its much needed place in the scheme of things though, it is no secret that naloxone has saved many lives.

SWIM wonders if this helps on his "not knowing anything" factor found elsewhere LOL . . .

Hope this has been of help

[Ale]

Originally Posted by samuraigecko

well actually this has been of large debate also and opiates ARE opiate receptor agonists as are opioids, the true meanings of both opiate and opioid are described HERE >>> what makes an opiate

So in effect it would be technically an opiate and not an opioid because an opiate is something that is derived from the opium poppy either natural or semi-synthetic. Opioids are generally classed as "fully synthetic" although the opioid base meaning is to classify ALL mu-opioid receptor agonists as a generalist overview.[..]

Actually the link you posted (from Wikipedia) doesn't mention any partial/full antagonist opioid/opiate so I assume the basic rule applies to either agonists, partial agonist(agonists/antagonists) or full antagonists.

[Paracelsus]

Please continue discussion about the definition of opiate/opioid and what substances are in this class in the thread samuraigecko linked to.

Papaverine is a spasmolytic. This alone doesn't make it a sedative/hypnotic. And of course it has no mu-opioid activity, which means it is not an opioid, but simply a "poppy alkaloid."

This may be of interest: Papaverine and other spasmolytics to ease opiate withdrawal symptoms?

[samuraigecko]

Originally Posted by Paracelsus

Please continue discussion about the definition of opiate/opioid and what substances are in this class in the thread samuraigecko linked to.

Papaverine is a spasmolytic. This alone doesn't make it a sedative/hypnotic. And of course it has no mu-opioid activity, which means it is not an opioid, but simply a "poppy alkaloid."

This may be of interest: Papaverine and other spasmolytics to ease opiate withdrawal symptoms?

Agreed, however one showed in his original statement that it had "no phenanthrene group (responsible for mu-opioid affinity and analgesia)" already - but that it did have sedative properties and relaxant properties for smooth muscle tissue (unlike benzo class drugs which also have a sedative effect but act on skeletal muscle tissues).

Since it has no mu-opioid activity one would most certainly have to agree that it is not an opiate or opioid but merely an alkaloid for which they have found a significant medicinal use.

However using papaverine as a base model a stronger sedative with mu-opioid affinity is possible which is what tweaked SWIMs interest in the first place.