Changa707
Bluelighter
- Joined
- Nov 25, 2014
- Messages
- 162
Seems like all the "old-school" first generation antihistamines out there have a great number of off-label indications...and as an opioid user, I find some of them to be great potentiators...adding an aspect to the high that is very meditative and surreal (especially with the anticholinergics like atropine and benztropine).
I have self-experimented with Equanil, Orphenadrine citrate, Diphenhydramine, Scopolamine, and Benztropine. Keep in mind, I am taking threshold doses of benztropine and scopolamine (250 micrograms)...which still leaves me with visual disturbances, but adds a very unique dissociation to the codeine and temazepam which I combine alongside my antihistamines/anticholinergics.
Orphenadrine seems to pack quite a punch at 100 mg, but I prefer the 0.25 mg benztropine because it causes less mouth dryness and has more prominent CNS depressing effects. Both of these substances seem to induce very mild "Shadow people" sensations...but it's minor.
So lets get into the pharmacology a little bit...since this is the neuroscience/pharmacology thread. I'm not trained in medical school or anything, but I consider myself well-read to some extent...I'm just curious about the potential off-label uses of these drugs I have been talking about. Particularly Orphenadrine and Benztropine. They are both closely related to diphenydramine, orphenadrine moreso. But I feel much less hangover and depressive side effects with orphenadrine than I do with diphenhydramine. I have found that orphenadrine has a sleuth of positive effects for me...it increases mood, produces a sublte sense of calm...yet allows me to be productive and even provides anxiety relief. Interestingly enough, I find orphenadrine to cause insomnia is some instances...it does not really make me sleepy, but gives me energy (kinda like the oxycodone of antihistamines). Same this with Benztropine, which I find to have simutaneously sedating and stimulating effects which add to the floaty feeling I get when nodding on opioids.
Only downside with Bentropine at only 0.25 mg is that the antihistamine effects are mediocre at best, but better than nothing at all. I'd say the benztropine is more like a weak cocaine high with nastier side effects (though I haven't even ventured into higher doses yet, but I know that benztropine is related to tropane alkaloids...so it must share some similarities.
Going off topic here sorry, i'm a bit high...restoril is kicking in alongside the 90 mg codeine. Go back 1.5 hours, I dosed 0.25 mg benztropine and 300 mg gabapentin. The synergy is taking place, and I feel that the benztropine is adding a new dimension of dissociation to the experience, that I quite enjoy (but I could imagine that taking a high dose of this substance on it's own would be unpleasant to say the least).
Hey, but in the end...it's really hard to tell what drug is giving what effect when you are on 4 substances at once (Temazepam, Codeine, Tylenol, Benztropine, & Gabapentin). I can say that the temazepam is the most noticeable, but I can also notice the dissociative effects of the Benztropine quite well. The opiate w/d from smoked heroin are 100% at bay, and I feel great (this is at T+48 hours since last toke).
Anyhow, as bad as Benztropine can be at high doses (not that I have taken high doses, but heard bad experiences)...it can have great benefits in low doses, 0.25 seems to do the trick...next time i'll try 0.5 mg.
So for all you pharmacologists and neuroscientists out there...do you think we will see more off-label uses for first-generation antihistamines and anticholinergics in the future? These drugs seem to be very effective, yet can prove to have undesirable effects even at clinical dosages (especially the anticholinergics). What is it about this H1 receptor that makes it have such a high affinity for binding and having strong CNS depressing effects?
Why do these antihistamines and anticholingeric have such dose-dependent effects, and unpredictability? I have heard of people hallucinating from scopolamine, atropine and others at medicinal dosages.
I know I'm asking a lot here, and am rather disorganized in my presentation...mind me for being under the influence. But I am genuinely curious about this peculiar class of drugs that are H1-receptor antagonists. Maybe there just is this nostalgia surrounding the old school muscle relaxers and antihistamines...i'm talking good old' Promethazine, Carisoprodol, Meprobamate, Orphenadrine, Diphenhydramines....they all seem to work well combined with opioids, though i'm not sure Carisoprodol or Meprobamate has antihistamine effects. But what they do all share in common is that they were developed between 1950s and 1960's. These drugs were very popular when they came out, and still are extremely popular today (except Miltown, which is quite a memorable tradename)!
So big question here....what is the future of H1-receptor antagonists in today's medicine? What don't we yet fully understand about the action of H1-receptor antagonists (pharmacologically speaking)?
I have self-experimented with Equanil, Orphenadrine citrate, Diphenhydramine, Scopolamine, and Benztropine. Keep in mind, I am taking threshold doses of benztropine and scopolamine (250 micrograms)...which still leaves me with visual disturbances, but adds a very unique dissociation to the codeine and temazepam which I combine alongside my antihistamines/anticholinergics.
Orphenadrine seems to pack quite a punch at 100 mg, but I prefer the 0.25 mg benztropine because it causes less mouth dryness and has more prominent CNS depressing effects. Both of these substances seem to induce very mild "Shadow people" sensations...but it's minor.
So lets get into the pharmacology a little bit...since this is the neuroscience/pharmacology thread. I'm not trained in medical school or anything, but I consider myself well-read to some extent...I'm just curious about the potential off-label uses of these drugs I have been talking about. Particularly Orphenadrine and Benztropine. They are both closely related to diphenydramine, orphenadrine moreso. But I feel much less hangover and depressive side effects with orphenadrine than I do with diphenhydramine. I have found that orphenadrine has a sleuth of positive effects for me...it increases mood, produces a sublte sense of calm...yet allows me to be productive and even provides anxiety relief. Interestingly enough, I find orphenadrine to cause insomnia is some instances...it does not really make me sleepy, but gives me energy (kinda like the oxycodone of antihistamines). Same this with Benztropine, which I find to have simutaneously sedating and stimulating effects which add to the floaty feeling I get when nodding on opioids.
Only downside with Bentropine at only 0.25 mg is that the antihistamine effects are mediocre at best, but better than nothing at all. I'd say the benztropine is more like a weak cocaine high with nastier side effects (though I haven't even ventured into higher doses yet, but I know that benztropine is related to tropane alkaloids...so it must share some similarities.
Going off topic here sorry, i'm a bit high...restoril is kicking in alongside the 90 mg codeine. Go back 1.5 hours, I dosed 0.25 mg benztropine and 300 mg gabapentin. The synergy is taking place, and I feel that the benztropine is adding a new dimension of dissociation to the experience, that I quite enjoy (but I could imagine that taking a high dose of this substance on it's own would be unpleasant to say the least).
Hey, but in the end...it's really hard to tell what drug is giving what effect when you are on 4 substances at once (Temazepam, Codeine, Tylenol, Benztropine, & Gabapentin). I can say that the temazepam is the most noticeable, but I can also notice the dissociative effects of the Benztropine quite well. The opiate w/d from smoked heroin are 100% at bay, and I feel great (this is at T+48 hours since last toke).
Anyhow, as bad as Benztropine can be at high doses (not that I have taken high doses, but heard bad experiences)...it can have great benefits in low doses, 0.25 seems to do the trick...next time i'll try 0.5 mg.
So for all you pharmacologists and neuroscientists out there...do you think we will see more off-label uses for first-generation antihistamines and anticholinergics in the future? These drugs seem to be very effective, yet can prove to have undesirable effects even at clinical dosages (especially the anticholinergics). What is it about this H1 receptor that makes it have such a high affinity for binding and having strong CNS depressing effects?
Why do these antihistamines and anticholingeric have such dose-dependent effects, and unpredictability? I have heard of people hallucinating from scopolamine, atropine and others at medicinal dosages.
I know I'm asking a lot here, and am rather disorganized in my presentation...mind me for being under the influence. But I am genuinely curious about this peculiar class of drugs that are H1-receptor antagonists. Maybe there just is this nostalgia surrounding the old school muscle relaxers and antihistamines...i'm talking good old' Promethazine, Carisoprodol, Meprobamate, Orphenadrine, Diphenhydramines....they all seem to work well combined with opioids, though i'm not sure Carisoprodol or Meprobamate has antihistamine effects. But what they do all share in common is that they were developed between 1950s and 1960's. These drugs were very popular when they came out, and still are extremely popular today (except Miltown, which is quite a memorable tradename)!
So big question here....what is the future of H1-receptor antagonists in today's medicine? What don't we yet fully understand about the action of H1-receptor antagonists (pharmacologically speaking)?
Last edited: