Psycho-Babble Medication Thread 662997

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Re: What's the best Benzo for Social Phobia? » Crazy Horse

Posted by MARTY on July 1, 2006, at 13:45:57

In reply to Re: What's the best Benzo for Social Phobia? » MARTY, posted by Crazy Horse on July 1, 2006, at 9:57:49

SURGEON GENERAL WARNING:
PLEASE TAKE NOTE THAT WE ARE JOKING, we know each other well. ;)

Let's start with psychopharmaceutical babbling:
What's your dosage of Clonazepam ?
When do you take it ?
How are you feeling on it ? do you like it ?

OK.. now let's get serious:

> Marty,
> Please, Please, quit drinking Tequila with your Haldol. I know you well enough to tell by your post that you are extremely intoxicated and my friend with ALL the medication you are on this simply is not prudent.

Wait a minute.. I not sure anymore, is it clonazepam that you are taking or is it CLOWNazepam ? Bozo. ;)


>Combining the large amounts of alcohol you drink with your high-potency antipsychotics and your antidementia meds may cause ECG changes, including prolongation of QT interval, T-wave inversion, and appearance of U waves.

woooooh.. you should definitively stop reading Ed_Uk and SLS stuff: too complicated for your tiny mini little shrunken drunken brain. :P

>And furthermore, will most likely worsen your chronic impotence problem. Please friend try to stop or limit your alcohol consumption...i say this as a concerned friend.

Impotence? My banana is much more potent than your banana! Mine has her active isomer isolated (Left Test*cle) ... so no comparaison with your little generic :D ahah


Hope you're well buddy
Marty

 

Re: What's the best Benzo for Social Phobia? » Crazy Horse

Posted by tepiaca on July 3, 2006, at 1:48:47

In reply to What's the best Benzo for Social Phobia?, posted by Crazy Horse on June 30, 2006, at 17:47:31

> I finally got my pdoc to write me a script for Klonopin..after much begging! I've been on Ativan for over 20 yrs. and just don't feel it works for me anymore. I want something to help w/Social Phobia, along w/my EMSAM. My PDoc insists a benzo is a benzo except for differences in the half life. All opinions are appreciated...is Klonopin generally better for S.P. than the other benzos? And why or why not? Thanks!

you know my case crazy =) . Xanax is the best , forgetting the short high life. Klono male me depressed when ore than 1 mg.
>
The best for you
Tepi

> Monte

 

QUESTION..2 mgs. Ativan is equal to??

Posted by Crazy Horse on July 3, 2006, at 10:23:03

In reply to Re: What's the best Benzo for Social Phobia? » Crazy Horse, posted by tepiaca on July 3, 2006, at 1:48:47

I have been told conflicting stories:

1) .50 Klonopin is equal to 2 mgs. of Ativan

2) .50 Klonopin is equal to 1 mg. of Ativan.

Anybody know which one is the correct answer. Your help is very much apreciated. Thanks!

Monte

 

Re: What's the best Benzo for Social Phobia? » tepiaca

Posted by Crazy Horse on July 3, 2006, at 10:33:29

In reply to Re: What's the best Benzo for Social Phobia? » Crazy Horse, posted by tepiaca on July 3, 2006, at 1:48:47

> > I finally got my pdoc to write me a script for Klonopin..after much begging! I've been on Ativan for over 20 yrs. and just don't feel it works for me anymore. I want something to help w/Social Phobia, along w/my EMSAM. My PDoc insists a benzo is a benzo except for differences in the half life. All opinions are appreciated...is Klonopin generally better for S.P. than the other benzos? And why or why not? Thanks!
>
> you know my case crazy =) . Xanax is the best , forgetting the short high life. Klono male me depressed when ore than 1 mg.
> >
> The best for you
> Tepi
>
>
>
> > Monte
>
>

Hi Tepi,

Thanks for your imput. Sorry i haven't been helpful to you the last couple of months..i have been very sick myself. I still think of you often and always remember you in my prayers. Please Babblemail me and let me know how you are doing.

Your friend,

Monte

 

Re: QUESTION..2 mgs. Ativan is equal to??

Posted by Squiggles on July 3, 2006, at 10:46:24

In reply to QUESTION..2 mgs. Ativan is equal to??, posted by Crazy Horse on July 3, 2006, at 10:23:03

> I have been told conflicting stories:
>
> 1) .50 Klonopin is equal to 2 mgs. of Ativan
>
> 2) .50 Klonopin is equal to 1 mg. of Ativan.
>
> Anybody know which one is the correct answer. Your help is very much apreciated. Thanks!
>
> Monte

From benzo.org.uk:

also known as Lorazepam, the equivalence is

1-2Ativan : 0.5Klonopin

http://benzo.org.uk/ (Equivalence Table).

Squiggles

 

Re: QUESTION..2 mgs. Ativan is equal to?? » Squiggles

Posted by MARTY on July 3, 2006, at 23:12:21

In reply to Re: QUESTION..2 mgs. Ativan is equal to??, posted by Squiggles on July 3, 2006, at 10:46:24

> From benzo.org.uk:
> also known as Lorazepam, the equivalence is
>
> 1-2Ativan : 0.5Klonopin

> http://benzo.org.uk/ (Equivalence Table).
> Squiggles

Nice equivalence table, bad table cell ;)

Take a look again on the table and you'll see that 1 mg (NOT 1 - 2 mg) of Lorazepam (Ativan) is equivalent to 0.5 mg of Clonazepam (Klonopin).

See ya around
Marty

 

Re: QUESTION..2 mgs. Ativan is equal to?? » MARTY

Posted by Squiggles on July 4, 2006, at 7:40:07

In reply to Re: QUESTION..2 mgs. Ativan is equal to?? » Squiggles, posted by MARTY on July 3, 2006, at 23:12:21

> > From benzo.org.uk:
> > also known as Lorazepam, the equivalence is
> >
> > 1-2Ativan : 0.5Klonopin
>
> > http://benzo.org.uk/ (Equivalence Table).
> > Squiggles
>
> Nice equivalence table, bad table cell ;)
>
> Take a look again on the table and you'll see that 1 mg (NOT 1 - 2 mg) of Lorazepam (Ativan) is equivalent to 0.5 mg of Clonazepam (Klonopin).
>
> See ya around
> Marty
>


I see 1-2 with a footnote on
alternative approximations; i'm
not sure how you interpret that as
1;

Squiggles

 

Re: QUESTION..2 mgs. Ativan is equal to?? » Squiggles

Posted by MARTY on July 4, 2006, at 9:43:41

In reply to Re: QUESTION..2 mgs. Ativan is equal to?? » MARTY, posted by Squiggles on July 4, 2006, at 7:40:07

> I see 1-2 with a footnote on
> alternative approximations; i'm
> not sure how you interpret that as
> 1;
>
> Squiggles
>

:P I'm sorry to insist to look again.. there's benzos starting with "LO" and even one by "LOR" maybe you look to fast... I asure you that LORAZEPAM (ATIVAN, TEMESTA) is 1 mg in the table.

Marty

 

Re: QUESTION..2 mgs. Ativan is equal to?? » MARTY

Posted by Squiggles on July 4, 2006, at 9:52:48

In reply to Re: QUESTION..2 mgs. Ativan is equal to?? » Squiggles, posted by MARTY on July 4, 2006, at 9:43:41

> > I see 1-2 with a footnote on
> > alternative approximations; i'm
> > not sure how you interpret that as
> > 1;
> >
> > Squiggles
> >
>
> :P I'm sorry to insist to look again.. there's benzos starting with "LO" and even one by "LOR" maybe you look to fast... I asure you that LORAZEPAM (ATIVAN, TEMESTA) is 1 mg in the table.
>
> Marty

You're right! I'm sorry and glad I was
not prescribing.

Squiggles

 

Re: QUESTION..2 mgs. Ativan is equal to?? » Squiggles

Posted by MARTY on July 4, 2006, at 9:55:42

In reply to Re: QUESTION..2 mgs. Ativan is equal to?? » MARTY, posted by Squiggles on July 4, 2006, at 9:52:48

> > Marty
>
> You're right! I'm sorry and glad I was
> not prescribing.
>
> Squiggles

:P LOL Happens to me all the time :)

Marty

 

Re: QUESTION..2 mgs. Ativan is equal to?? » MARTY

Posted by Crazy Horse on July 4, 2006, at 10:39:23

In reply to Re: QUESTION..2 mgs. Ativan is equal to?? » Squiggles, posted by MARTY on July 4, 2006, at 9:55:42

> > > Marty
> >
> > You're right! I'm sorry and glad I was
> > not prescribing.
> >
> > Squiggles
>
> :P LOL Happens to me all the time :)
>
> Marty

DAMN..I can b a r e l y bring myself to say this.. but (for once) Martin is right...oops almost had to regurgitate..:) But thanks to BOTH of you for careing enough to respond...:) MARTINI..FOR A CAN UH DUH boy, your pretty smart! :)

CRAZY MONTE

 

Re: QUESTION..2 mgs. Ativan is equal to?? » Crazy Horse

Posted by MARTY on July 4, 2006, at 13:35:58

In reply to Re: QUESTION..2 mgs. Ativan is equal to?? » MARTY, posted by Crazy Horse on July 4, 2006, at 10:39:23

> FOR A CAN UH DUH boy, your pretty smart! :)
>

uh, Tell me something I don't know. Look at this, is an excerpt from PubMed:

In a double-blind clinical trial, 29 Canadian and 27 placebo have been challenged to the elevated plus maze. 8% (2.32) of the Canadians succeed in finding the cheese at the middle of the maze. Only 6% (1.62) of the placebo succeed the same test. In light of these isignificant results, we can't conclude anything but that both, Canadians and Placebo, seems to be attracted by cheese. More study should be make in order to determine if is itn't cheese that is attracted to both Canadians and Placebo. Either way, Canadian were barely superior to placebo and so deserve to be called "Intelligent Human Beings". It is of interest to note that one of the Canadian f**ked the cheese and that a new species arise from this act. After a couple of minutes the strange specimen shouted "POUUUTINE!!!!!" and start to sing something remembering Celine Dion, but without all those common disgraful note. More study should be done on that specimen that we decided to call "Quebecer".

Ia. 100-29, University FisherPrice. Marty, Bexton and NGO 2006. (n18, p28 - Journal of United BS)

See ? :)=
Marty

 

Re: QUESTION..2 mgs. Ativan is equal to?? » MARTY

Posted by Squiggles on July 4, 2006, at 13:58:51

In reply to Re: QUESTION..2 mgs. Ativan is equal to?? » Crazy Horse, posted by MARTY on July 4, 2006, at 13:35:58

> > FOR A CAN UH DUH boy, your pretty smart! :)
> >
>
> uh, Tell me something I don't know. Look at this, is an excerpt from PubMed:
>
> In a double-blind clinical trial, 29 Canadian and 27 placebo have been challenged to the elevated plus maze. 8% (2.32) of the Canadians succeed in finding the cheese at the middle of the maze. Only 6% (1.62) of the placebo succeed the same test. In light of these isignificant results, we can't conclude anything but that both, Canadians and Placebo, seems to be attracted by cheese. More study should be make in order to determine if is itn't cheese that is attracted to both Canadians and Placebo. Either way, Canadian were barely superior to placebo and so deserve to be called "Intelligent Human Beings". It is of interest to note that one of the Canadian f**ked the cheese and that a new species arise from this act. After a couple of minutes the strange specimen shouted "POUUUTINE!!!!!" and start to sing something remembering Celine Dion, but without all those common disgraful note. More study should be done on that specimen that we decided to call "Quebecer".
>
> Ia. 100-29, University FisherPrice. Marty, Bexton and NGO 2006. (n18, p28 - Journal of United BS)
>
>
>
> See ? :)=
> Marty

Hee :-)

I was wondering if the Placebo group was defined as a nation; i.e. "distinct" from the rest of Canada, and what kind of cheese was used - was it Stilton or Rocquefort? I saw a neologism in some articles (Dr. Torrey used it) in psychiatric
lingo - anasognosia [?], but that couldn't be it because lack of self-awareness seems such an essential characteristic of those who populate the land of the free and the home of the brave.
When you're no. 1 you don't need self-awareness - you're recognized like a Roman. Must have been a multi-cultural group of rodents - yup maybe
Canuck rodents.

Squiggles

 

Re: QUESTION..2 mgs. Ativan is equal to??

Posted by sdb on July 4, 2006, at 16:51:52

In reply to Re: QUESTION..2 mgs. Ativan is equal to?? » MARTY, posted by Squiggles on July 4, 2006, at 13:58:51

45mg ketazolam or 60mg prazepam could be a very good alternative to clonazepam etc.

Valium (diazepam) is just a dirty drug compared with ketazolam (see some studies, which I can support completely). Unfortunately both substances are not available in pharmacies, but maybe by chemical providers or import in the US.

 

Re: QUESTION..2 mgs. Ativan is equal to?? » MARTY

Posted by Crazy Horse on July 5, 2006, at 9:36:21

In reply to Re: QUESTION..2 mgs. Ativan is equal to?? » Crazy Horse, posted by MARTY on July 4, 2006, at 13:35:58

> > FOR A CAN UH DUH boy, your pretty smart! :)
> >
>
> uh, Tell me something I don't know. Look at this, is an excerpt from PubMed:
>
> In a double-blind clinical trial, 29 Canadian and 27 placebo have been challenged to the elevated plus maze. 8% (2.32) of the Canadians succeed in finding the cheese at the middle of the maze. Only 6% (1.62) of the placebo succeed the same test. In light of these isignificant results, we can't conclude anything but that both, Canadians and Placebo, seems to be attracted by cheese. More study should be make in order to determine if is itn't cheese that is attracted to both Canadians and Placebo. Either way, Canadian were barely superior to placebo and so deserve to be called "Intelligent Human Beings". It is of interest to note that one of the Canadian f**ked the cheese and that a new species arise from this act. After a couple of minutes the strange specimen shouted "POUUUTINE!!!!!" and start to sing something remembering Celine Dion, but without all those common disgraful note. More study should be done on that specimen that we decided to call "Quebecer".
>
> Ia. 100-29, University FisherPrice. Marty, Bexton and NGO 2006. (n18, p28 - Journal of United BS)
>
>
>
> See ? :)=
> Marty

You are freakin' CRAZY Louis!!! You are definitely a "Cheesy CA NAH DEE UN!" And i think the cheese you eat is "dusted" with PCP :)
I most definiely feel a strong cognitive enhancer, perhaps NAMENDA, may help a "man" like you with severe dementia and most definite symptoms of progressive Alzheimer's disease. Memantine may be used in conjunction w/acetylcholinesterase inhibitors to help even a severe case as yours. Unfortunately, cognitive improvement with w/severe dementia cases like yours with Namenda is only modest...which for you would be a HUGE improvement. :)

Your adopted big bro,

CRaZy HOrSe (huma comana letesh)

 

Re: blocked for week » Crazy Horse » MARTY

Posted by Dr. Bob on July 5, 2006, at 21:59:56

In reply to Re: QUESTION..2 mgs. Ativan is equal to?? » Crazy Horse, posted by MARTY on July 4, 2006, at 13:35:58

> FOR A CAN UH DUH boy, your pretty smart! :)
>
> Crazy Horse

> More study should be done on that specimen that we decided to call "Quebecer".
>
> Marty

Please don't post anything that could lead others (such as Canadians or Quebecers) to feel put down.

But please don't take this personally, either, this doesn't mean I don't like you or think you're bad people.

If you or others have questions about this or about posting policies in general, or are interested in alternative ways of expressing yourself, please first see the FAQ:

http://www.dr-bob.org/babble/faq.html#civil
http://www.dr-bob.org/babble/faq.html#enforce

Follow-ups regarding these issues should be redirected to Psycho-Babble Administration. They, as well as replies to the above posts, should of course themselves be civil.

Thanks,

Bob

 

Re: QUESTION..2 mgs. Ativan is equal to??

Posted by sdb on July 7, 2006, at 21:00:33

In reply to Re: QUESTION..2 mgs. Ativan is equal to?? » Squiggles, posted by MARTY on July 3, 2006, at 23:12:21

> > From benzo.org.uk:
> > also known as Lorazepam, the equivalence is
> >
> > 1-2Ativan : 0.5Klonopin
>
> > http://benzo.org.uk/ (Equivalence Table).
> > Squiggles
>
> Nice equivalence table, bad table cell ;)
>
> Take a look again on the table and you'll see that 1 mg (NOT 1 - 2 mg) of Lorazepam (Ativan) is equivalent to 0.5 mg of Clonazepam (Klonopin).
>
> See ya around
> Marty
>


If you want to change the duration of action and the amount (ng/ml) of clonazepam during time you can simply drink some grapefruit juice (clonazepam is mainly substrate of CYP3A4, grapefruit juice is an "OTC" inhibitor of CYP3A4). The effect of grapefruit juice
on clonazepam, diazepam and other drugs can be up to 24h. Hypericum (St. John's wort) does the opposite and it would lead to faster breakdown of clonazepam (inducer of CYP3A4).
Lorazepam is not substrate of CYP3A4, thus you can not change things with simple methods. Be careful doing that because the change on metabolism will depend on several factors eg. age, liver function, different phenotypes of the CYP3A4, other drugs you take and the dosages. I tested this myself with low dosages and the research is more or less consistent with reality.

sdb

 

Re: Rumination-snapper

Posted by Squiggles on July 7, 2006, at 21:16:43

In reply to Re: QUESTION..2 mgs. Ativan is equal to??, posted by sdb on July 7, 2006, at 21:00:33

> > > From benzo.org.uk:
> > > also known as Lorazepam, the equivalence is
> > >
> > > 1-2Ativan : 0.5Klonopin
> >
> > > http://benzo.org.uk/ (Equivalence Table).
> > > Squiggles
> >
> > Nice equivalence table, bad table cell ;)
> >
> > Take a look again on the table and you'll see that 1 mg (NOT 1 - 2 mg) of Lorazepam (Ativan) is equivalent to 0.5 mg of Clonazepam (Klonopin).
> >
> > See ya around
> > Marty
> >
>
>
> If you want to change the duration of action and the amount (ng/ml) of clonazepam during time you can simply drink some grapefruit juice (clonazepam is mainly substrate of CYP3A4, grapefruit juice is an "OTC" inhibitor of CYP3A4). The effect of grapefruit juice
....
> sdb


"duration" but not potency right?

Squiggles

 

Re: Rumination-snapper (nm)

Posted by sdb on July 8, 2006, at 6:09:04

In reply to Re: Rumination-snapper, posted by Squiggles on July 7, 2006, at 21:16:43

> > > > From benzo.org.uk:
> > > > also known as Lorazepam, the equivalence is
> > > >
> > > > 1-2Ativan : 0.5Klonopin
> > >
> > > > http://benzo.org.uk/ (Equivalence Table).
> > > > Squiggles
> > >
> > > Nice equivalence table, bad table cell ;)
> > >
> > > Take a look again on the table and you'll see that 1 mg (NOT 1 - 2 mg) of Lorazepam (Ativan) is equivalent to 0.5 mg of Clonazepam (Klonopin).
> > >
> > > See ya around
> > > Marty
> > >
> >
> >
> > If you want to change the duration of action and the amount (ng/ml) of clonazepam during time you can simply drink some grapefruit juice (clonazepam is mainly substrate of CYP3A4, grapefruit juice is an "OTC" inhibitor of CYP3A4). The effect of grapefruit juice
> ....
> > sdb
>
>
> "duration" but not potency right?
>
> Squiggles
>

Yes.

 

Re: Rumination-snapper }} Squiggles

Posted by sdb on July 8, 2006, at 18:57:54

In reply to Re: Rumination-snapper (nm), posted by sdb on July 8, 2006, at 6:09:04

> > > > > From benzo.org.uk:
> > > > > also known as Lorazepam, the equivalence is
> > > > >
> > > > > 1-2Ativan : 0.5Klonopin
> > > >
> > > > > http://benzo.org.uk/ (Equivalence Table).
> > > > > Squiggles
> > > >
> > > > Nice equivalence table, bad table cell ;)
> > > >
> > > > Take a look again on the table and you'll see that 1 mg (NOT 1 - 2 mg) of Lorazepam (Ativan) is equivalent to 0.5 mg of Clonazepam (Klonopin).
> > > >
> > > > See ya around
> > > > Marty
> > > >
> > >
> > >
> > > If you want to change the duration of action and the amount (ng/ml) of clonazepam during time you can simply drink some grapefruit juice (clonazepam is mainly substrate of CYP3A4, grapefruit juice is an "OTC" inhibitor of CYP3A4). The effect of grapefruit juice
> > ....
> > > sdb
> >
> >
> > "duration" but not potency right?
> >
> > Squiggles
> >
>
> Yes.

Here is a study but diazepam is not only metabolized by CYP3A4:
------------------------------------------------------------------

Eur J Drug Metab Pharmacokinet. 1998 Jan-Mar;23(1):55-9. Related Articles, Links

Interaction between grapefruit juice and diazepam in humans.

Ozdemir M, Aktan Y, Boydag BS, Cingi MI, Musmul A.

Department of Pharmacology, Medical Faculty, University of Osmangazi, Eskisehir, Turkey.

Grapefruit juice has been reported to markedly improve the bioavailability of triazolam, midazolam, terfenadine, cyclosporine and several dihydropyridine calcium channel blockers including felodipine, nifedipine, nitrendipine and nisoldipine. Because these drugs are metabolized by the hepatic cytochrome P450 isozyme (CYP) 3A4, the inhibitory effect of grapefruit juice is thought to results from inhibition of CYP3A4. In this study, our aim was to investigate the effects of grapefruit juice on plasma concentrations of diazepam. Eight healthy male and female subjects participated in this study. Oral (5 mg) diazepam was administered with either 250 ml water and grapefruit juice. Blood samples were collected for a 24 h period, and whole blood concentrations of diazepam were measured enzyme immunoassay. The mean AUC(0-24) of diazepam was increased 3.2-fold (P < 0.001) and Cmax was increased 1.5-fold (P < 0.05) by the grapefruit juice. Grapefruit juice postponed the tmax of diazepam from 1.50 h to 2.06 h (P < 0.01).

 

Re: Rumination-snapper }} Squiggles » sdb

Posted by Squiggles on July 8, 2006, at 19:15:21

In reply to Re: Rumination-snapper }} Squiggles, posted by sdb on July 8, 2006, at 18:57:54


> Here is a study but diazepam is not only metabolized by CYP3A4:
> ------------------------------------------------------------------
>
> Eur J Drug Metab Pharmacokinet. 1998 Jan-Mar;23(1):55-9. Related Articles, Links
>
> Interaction between grapefruit juice and diazepam in humans.
>
> Ozdemir M, Aktan Y, Boydag BS, Cingi MI, Musmul A.
>
> Department of Pharmacology, Medical Faculty, University of Osmangazi, Eskisehir, Turkey.
>
> Grapefruit juice has been reported to markedly improve the bioavailability of triazolam, midazolam, terfenadine, cyclosporine and several dihydropyridine calcium channel blockers including felodipine, nifedipine, nitrendipine and nisoldipine. Because these drugs are metabolized by the hepatic cytochrome P450 isozyme (CYP) 3A4, the inhibitory effect of grapefruit juice is thought to results from inhibition of CYP3A4. In this study, our aim was to investigate the effects of grapefruit juice on plasma concentrations of diazepam. Eight healthy male and female subjects participated in this study. Oral (5 mg) diazepam was administered with either 250 ml water and grapefruit juice. Blood samples were collected for a 24 h period, and whole blood concentrations of diazepam were measured enzyme immunoassay. The mean AUC(0-24) of diazepam was increased 3.2-fold (P < 0.001) and Cmax was increased 1.5-fold (P < 0.05) by the grapefruit juice. Grapefruit juice postponed the tmax of diazepam from 1.50 h to 2.06 h (P < 0.01).
>

Interesting; drug interactions are interesting in
general but to know exactly what effect one
drug has on another, or on an enzyme or hormone
can be very useful. In this case the inhibition of grapefruit juice (not just grapefruit because
of quantity i would imagine) can be used for or
against the potentiation of these drugs. I use
the word potentiation but that may not be quite
correct. What is bioavailability? Does it mean that the blockage of cytochrome P450 isozyme represses the liver metabolism, and therefore the
stuff is voided, much like lithium's kidney voidance is increased by sodium and potassium?

Also, how would you use this cytochrome blockage to the advantage of regulating the benzo dose?
It might take some fine measurement.

Squiggles

 

Re: AUC, grapefruit }} Squiggles

Posted by sdb on July 8, 2006, at 19:47:08

In reply to Re: Rumination-snapper }} Squiggles » sdb, posted by Squiggles on July 8, 2006, at 19:15:21

>
> > Here is a study but diazepam is not only metabolized by CYP3A4:
> > ------------------------------------------------------------------

> >
> > Eur J Drug Metab Pharmacokinet. 1998 Jan-Mar;23(1):55-9. Related Articles, Links
> >
> > Interaction between grapefruit juice and diazepam in humans.
> >
> > Ozdemir M, Aktan Y, Boydag BS, Cingi MI, Musmul A.
> >
> > Department of Pharmacology, Medical Faculty, University of Osmangazi, Eskisehir, Turkey.
> >
> > Grapefruit juice has been reported to markedly improve the bioavailability of triazolam, midazolam, terfenadine, cyclosporine and several dihydropyridine calcium channel blockers including felodipine, nifedipine, nitrendipine and nisoldipine. Because these drugs are metabolized by the hepatic cytochrome P450 isozyme (CYP) 3A4, the inhibitory effect of grapefruit juice is thought to results from inhibition of CYP3A4. In this study, our aim was to investigate the effects of grapefruit juice on plasma concentrations of diazepam. Eight healthy male and female subjects participated in this study. Oral (5 mg) diazepam was administered with either 250 ml water and grapefruit juice. Blood samples were collected for a 24 h period, and whole blood concentrations of diazepam were measured enzyme immunoassay. The mean AUC(0-24) of diazepam was increased 3.2-fold (P < 0.001) and Cmax was increased 1.5-fold (P < 0.05) by the grapefruit juice. Grapefruit juice postponed the tmax of diazepam from 1.50 h to 2.06 h (P < 0.01).
> >
>
> Interesting; drug interactions are interesting in
> general but to know exactly what effect one
> drug has on another, or on an enzyme or hormone
> can be very useful. In this case the inhibition of grapefruit juice (not just grapefruit because
> of quantity i would imagine) can be used for or
> against the potentiation of these drugs. I use
> the word potentiation but that may not be quite
> correct. What is bioavailability? Does it mean that the blockage of cytochrome P450 isozyme represses the liver metabolism, and therefore the
> stuff is voided, much like lithium's kidney voidance is increased by sodium and potassium?
>
> Also, how would you use this cytochrome blockage to the advantage of regulating the benzo dose?
> It might take some fine measurement.
>
> Squiggles

Bioavailability is a measurement of "how much" from the therapeutically active substances reach
the systemic circulation and later the site of action eg. for diazepam: the brain -> if you take grapefruit juice more active diazepam will reach your brain because of a "modified" first pass in the liver. Substances will spread out in to different compartiments. Diazepam should reach the brain to have the drugs clinical response.

If you give something IV the bioavailability is 100%. If you take a drug orally you will not reach
100%, because of poor absorption from the gastrointestinal tract, degradation or metabolism of the drug prior to absorption, hepatic first pass effect, lipid membranes etc.

There is more to tell about but bioavailability (AUC = Area under the curve) means the amount of substance that really reaches for example the receptors of brain GABA-CL channels in the case of diazepam, clonazepam.

sdb

 

Re: AUC, grapefruit }} Squiggles » sdb

Posted by Squiggles on July 8, 2006, at 19:58:01

In reply to Re: AUC, grapefruit }} Squiggles, posted by sdb on July 8, 2006, at 19:47:08


> There is more to tell about but bioavailability (AUC = Area under the curve) means the amount of substance that really reaches for example the receptors of brain GABA-CL channels in the case of diazepam, clonazepam.
>
> sdb

Thank you. Pharmacology is fascinating. I looked
at the Merck manual but that (with the exception of endocrinology and cardiac chapters) is one of the most complex; maybe because it is so mathematical.

Yes, I would imagine that through the vein is the fastest, uninterrupted route to the brain of any drug, as no organ or condition of the body or other drug can interfere in its reaching the brain; unless there is low blood pressure, or some arterial disease or maybe even anemia.

Squiggles

 

Re: AUC, grapefruit II. }} Squiggles

Posted by sdb on July 8, 2006, at 20:00:25

In reply to Re: AUC, grapefruit }} Squiggles, posted by sdb on July 8, 2006, at 19:47:08

>Also, how would you use this cytochrome blockage to >the advantage of regulating the benzo dose?

Take care doing that (if your're an old person, having bad liver, known seizure or respiration problems) but maybe you can have an advantage. It is very, very unlikely to be toxic using a moderate diazepam, clonazepam dosage.

As you can read above you can take less diazepam, clonazepam for the same response and the plasmalevels are more flat. Actually a good thing if you take the drug continuously.

sdb

 

Re: hypericum - St. John's wort INTERACTION

Posted by sdb on July 12, 2006, at 13:21:24

In reply to Re: AUC, grapefruit II. }} Squiggles, posted by sdb on July 8, 2006, at 20:00:25

I did some experiments and it seems that hypericum is a very effective inducer of cyp3a.

Thats means: If you take only five pills during five days (of maybe 450mg) the clonazepam or valium maybe working as a placebo pill.

I am not entirely sure and will do some more experiments. But take care combining the hypericum with occasional use of some benzodiazepines.

It is very well known that hypericum does influence other drugs but it is not so well known that hypericum does influence other drugs in psychiatry e.g. benzodiazepines.

Take care

sdb


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