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Increasing bioavailability of benzo's
#41
Yes, thanks RM!

I'm going to look in to this Cimetidine that keeps coming up.
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#42
RM - Thought you might find this interesting:


Quote:Abstract

Cimetidine has been shown to inhibit the liver microsomal metabolism of the benzodiazepines diazepam and chlordiazepoxide, resulting in an increase in half-life and decrease in the clearance of these two drugs. Patients receiving the combination of diazepam and cimetidine have been noted to be more sedated than when given an equal dose of diazepam alone. Many benzodiazepines undergo N-dealkylation and hydroxylation via the cytochrome P450 oxidase system. Cimetidine is thought to bind to cytochrome P450 oxidase and to interfere with many drugs using this path way. Oxazepam and lorazepam are two benzodiazepines not oxidatively metabolized by cytochrome P450, but are glucuronidated by glucuronyl transferase and are, therefore, not subject to metabolic inhibition by cimetidine. Thus, when clinically indicated, oxazepam and lorazepam may be the benzodiazepines of choice to use in combination with cimetidine to eliminate the clinically significant drug interaction seen with diazepam and chlordiazepoxide.

Link: xxxxx://www.ncbi.nlm.nih.gov/pubmed/6116285 (replace xxxxx with https, of course.
A tree is known by its fruit; a man by his deeds. A good deed is never lost; he who sows courtesy reaps friendship, and he who plants kindness gathers love.

-- Saint Basil








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#43
(02-07-2018, 03:56 PM)OldBoy Wrote: RM - Thought you might find this interesting:


Quote:Abstract

Cimetidine has been shown to inhibit the liver microsomal metabolism of the benzodiazepines diazepam and chlordiazepoxide, resulting in an increase in half-life and decrease in the clearance of these two drugs. Patients receiving the combination of diazepam and cimetidine have been noted to be more sedated than when given an equal dose of diazepam alone. Many benzodiazepines undergo N-dealkylation and hydroxylation via the cytochrome P450 oxidase system. Cimetidine is thought to bind to cytochrome P450 oxidase and to interfere with many drugs using this path way. Oxazepam and lorazepam are two benzodiazepines not oxidatively metabolized by cytochrome P450, but are glucuronidated by glucuronyl transferase and are, therefore, not subject to metabolic inhibition by cimetidine. Thus, when clinically indicated, oxazepam and lorazepam may be the benzodiazepines of choice to use in combination with cimetidine to eliminate the clinically significant drug interaction seen with diazepam and chlordiazepoxide.

Link: xxxxx://www.ncbi.nlm.nih.gov/pubmed/6116285 (replace xxxxx with https, of course.
Thanks for this, O. I have seen studies like these. In fact, about 10 years ago I was really psyched by the idea that Tagamet might indeed revolutionize my experience with benzo's (and opioids). I have been in the market for a true potentiator of both for decades. I know that grapefruit juice is a legit potentiator, but I cannot have that because I take the medication Digoxin. So I began trying Tagamet. I must say that I did not notice a different but that's just me. Everyone else seems to note a difference. I have a weird make up. For instance, I noticed that 400mg's of magnesium, taken an hour before a dose of oxy or hydro, definitely improves the experience somewhat. No one else seems to think that. Are you going to try the Tagamet? You are making me feel like giving it another run. Walgreen's used to have a trial size. Not sure if they still do. Otherwise, Amazon is probably your best bet. Let me know. I'll probably do it with you.  RM
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#44
(02-09-2018, 01:38 AM)Rafterman Wrote:
(02-07-2018, 03:56 PM)OldBoy Wrote: RM - Thought you might find this interesting:


Quote:Abstract

Cimetidine has been shown to inhibit the liver microsomal metabolism of the benzodiazepines diazepam and chlordiazepoxide, resulting in an increase in half-life and decrease in the clearance of these two drugs. Patients receiving the combination of diazepam and cimetidine have been noted to be more sedated than when given an equal dose of diazepam alone. Many benzodiazepines undergo N-dealkylation and hydroxylation via the cytochrome P450 oxidase system. Cimetidine is thought to bind to cytochrome P450 oxidase and to interfere with many drugs using this path way. Oxazepam and lorazepam are two benzodiazepines not oxidatively metabolized by cytochrome P450, but are glucuronidated by glucuronyl transferase and are, therefore, not subject to metabolic inhibition by cimetidine. Thus, when clinically indicated, oxazepam and lorazepam may be the benzodiazepines of choice to use in combination with cimetidine to eliminate the clinically significant drug interaction seen with diazepam and chlordiazepoxide.

Link: xxxxx://www.ncbi.nlm.nih.gov/pubmed/6116285 (replace xxxxx with https, of course.
Thanks for this, O. I have seen studies like these. In fact, about 10 years ago I was really psyched by the idea that Tagamet might indeed revolutionize my experience with benzo's (and opioids). I have been in the market for a true potentiator of both for decades. I know that grapefruit juice is a legit potentiator, but I cannot have that because I take the medication Digoxin. So I began trying Tagamet. I must say that I did not notice a different but that's just me. Everyone else seems to note a difference. I have a weird make up. For instance, I noticed that 400mg's of magnesium, taken an hour before a dose of oxy or hydro, definitely improves the experience somewhat. No one else seems to think that. Are you going to try the Tagamet? You are making me feel like giving it another run. Walgreen's used to have a trial size. Not sure if they still do. Otherwise, Amazon is probably your best bet. Let me know. I'll probably do it with you.  RM

Hi RM,

I'm a bit ahead of you - Received 4 bottles of generic (Equate) brand Cimetidine from Amazon on Monday, and tried the following:

1. Cimetidine after a meal, then di@z
2. Cimetidine on an empty stomach, then di@z
3. Cimetidine on an empty stomach, followed by a 15-minute wait, then di@z

Of the three, the third method has a definite effect as a potentiatior - In terms of how quickly the di@z kicks in, it's perceived strength, and the duration of effect.  It seems to increase the properties of the di@z by about 1/3, which is fantastic.


Of course, now to see if the effect is consistent, or if I need to take a break from the Cimetidine every now and then ;-)

Have a great weekend!
A tree is known by its fruit; a man by his deeds. A good deed is never lost; he who sows courtesy reaps friendship, and he who plants kindness gathers love.

-- Saint Basil








Reply
#45
(02-09-2018, 03:16 PM)OldBoy Wrote:
(02-09-2018, 01:38 AM)Rafterman Wrote:
(02-07-2018, 03:56 PM)OldBoy Wrote: RM - Thought you might find this interesting:


Quote:Abstract

Cimetidine has been shown to inhibit the liver microsomal metabolism of the benzodiazepines diazepam and chlordiazepoxide, resulting in an increase in half-life and decrease in the clearance of these two drugs. Patients receiving the combination of diazepam and cimetidine have been noted to be more sedated than when given an equal dose of diazepam alone. Many benzodiazepines undergo N-dealkylation and hydroxylation via the cytochrome P450 oxidase system. Cimetidine is thought to bind to cytochrome P450 oxidase and to interfere with many drugs using this path way. Oxazepam and lorazepam are two benzodiazepines not oxidatively metabolized by cytochrome P450, but are glucuronidated by glucuronyl transferase and are, therefore, not subject to metabolic inhibition by cimetidine. Thus, when clinically indicated, oxazepam and lorazepam may be the benzodiazepines of choice to use in combination with cimetidine to eliminate the clinically significant drug interaction seen with diazepam and chlordiazepoxide.

Link: xxxxx://www.ncbi.nlm.nih.gov/pubmed/6116285 (replace xxxxx with https, of course.
Thanks for this, O. I have seen studies like these. In fact, about 10 years ago I was really psyched by the idea that Tagamet might indeed revolutionize my experience with benzo's (and opioids). I have been in the market for a true potentiator of both for decades. I know that grapefruit juice is a legit potentiator, but I cannot have that because I take the medication Digoxin. So I began trying Tagamet. I must say that I did not notice a different but that's just me. Everyone else seems to note a difference. I have a weird make up. For instance, I noticed that 400mg's of magnesium, taken an hour before a dose of oxy or hydro, definitely improves the experience somewhat. No one else seems to think that. Are you going to try the Tagamet? You are making me feel like giving it another run. Walgreen's used to have a trial size. Not sure if they still do. Otherwise, Amazon is probably your best bet. Let me know. I'll probably do it with you.  RM

Hi RM,

I'm a bit ahead of you - Received 4 bottles of generic (Equate) brand Cimetidine from Amazon on Monday, and tried the following:

1. Cimetidine after a meal, then di@z
2. Cimetidine on an empty stomach, then di@z
3. Cimetidine on an empty stomach, followed by a 15-minute wait, then di@z

Of the three, the third method has a definite effect as a potentiatior - In terms of how quickly the di@z kicks in, it's perceived strength, and the duration of effect.  It seems to increase the properties of the di@z by about 1/3, which is fantastic.


Of course, now to see if the effect is consistent, or if I need to take a break from the Cimetidine every now and then ;-)

Have a great weekend!

Wow! That is phenomenal, O. Now I am certain that I will dive back in and give it another try. I can't say for certain that I used your Method #3, which makes having another go at it even more exciting. Are you thinking of going even further in your studies of this? Say, like waiting an hour after taking the Cimeditine? Or increasing the dose of the Cimeditine? BTW, please tell me again the dose of the C that you were using. Thanks. I am going to grab a trial size at the local Walgreens. Might be a couple of days from now, as I am under the weather. I will definitely let you know what happens. Thanks for all the great info. I hope that you are enjoying your weekend!  RM
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