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Why don't triazolo benzos produce a rush when IV'd?

Well Midazolam is used a lot IV in hospitals due to its High polarity (+therefore solubility in solution) prior to injection but its rapid conversion into a lipophillic molecule in the blood. (As far as I understood it)

my guess would be triazolams don't share the same instant polar - nonpolar conversion and are triazolams more polar than for example diazepam, temazepam? if so that might explain why they are used IV (because they dissolve in solution more) but produce less of a rush.

...anyway if your thinking of self injecting benzo's be warned its highly dangerous and very stupid. Minimal someone else should be there but that sort of thing is really only suitable for clinical settings with people looking after you.
 
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Reminisant B said:
Well Midazolam is used a lot IV in hospitals due to its High polarity (+therefore solubility in solution) prior to injection but its rapid conversion into a lipophillic molecule in the blood. (As far as I understood it)

my guess would be triazolams don't share the same instant polar - nonpolar conversion and are triazolams more polar than for example diazepam, temazepam? if so that might explain why they are used IV (because they dissolve in solution more) but produce less of a rush.
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Triazolo benzos are one's that end in -pam e.g nitrazepam, temazepam, clonazepam etc, many are almost completely insoluble in water. Many of the -lam benzos such as midazolam and triazolam produce a big rush
 
omen_owen mk2 said:
Triazolo benzos are one's that end in -pam e.g nitrazepam, temazepam, clonazepam etc, many are almost completely insoluble in water.
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I don't intend to be pedantic, but this isn't true. There are benzos whose names end in -pam that aren't triazolo, like diazepam, and none of the benzos you just listed are triazolo benzos. The triazolo refers to a heterocylic ring containing three nitrogens. Alprazolam is a good case in point.
 
hussness said:
I don't intend to be pedantic, but this isn't true. There are benzos whose names end in -pam that aren't triazolo, like diazepam, and none of the benzos you just listed are triazolo benzos. The triazolo refers to a heterocylic ring containing three nitrogens. Alprazolam is a good case in point.
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Nothing wrong with pedantism! When it comes to the chemistry of benzos I'm still learning, and used this thread as a source of information:

http://www.bluelight.ru/vb/showthread.php?t=323525&highlight=iv+benzos

I misinterpereted what was being said. Cheers for putting me straight.
 
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hussness said:
I agree that injecting pills isn't smart, but benzos do have a pretty large therapeutic ratio.
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Oral benzodiazepines have a faily large therapeutic index when used alone.

However Intravenous benzodiazepines may have a large therapeutic index when used in a hospital setting BUT self injection is the COMPLETE OPPOSITE.

In most people they cause sudden amnesia when injected (which is why midazolam is used for minor operations or unpleasant procedures) - this is the dangerous part - especially if a person has a large enough quantity to hand. Its very possible the amnesia / drowsiness makes that person inject more and more.

Oral benzos come on slowly but when your injecting them the speed of onset is what can cause such varying degrees of amnesia. All the bad reactions that some people have to them can come on suddenly with no warning.
 
Hussness is right, the triazolo benzos are the ones that end in "lam," or "zolam," (not sure all the "lams" are "zolam") such as alprazolam, triazolam, and midazolam. Note that these are all 1,4 disubstituted.
And if I'm not mistaken, the "pam" benzodiazepines are the non-triazolo 1,4 disubstituted type.

Sorry this is OT and nitpicky.
 
Yeah, it's just pharmacokinetics, poorly water soluble drugs bind heavily to plasma proteins or other membranes, rather than diffusing directly to the brain.

You can just think of it like a stomach that drugs have to pass through. I.e. Water soluble drugs go (when IVed) Blood->Brain; high protein binding ones have to go Blood->Protein->Brain.
 
From my experience,
[1,4]benzodiazepines (ending in -pam) don't produce a rush when IVed.
[1,5]benzodiazepines (ending in -zam) don't produce a rush either.

Benzos ending in -lam all produce a rush in my experience. (triazolo and imidazo ones).
 
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