Drug info - Cetirizine/Zyrtec

[Exc_quetz]

Recently Cetirizine went from being prescription-only to OTC in the United States. SWIM knows nothing about the drug other than it's an anti-histamine used to treat allergic reactions just like diphenhydramine or loratadine. What SWIM would like to know is if this new(to the public) drug has any recreational value? SWIM thinks most if not all anti-histamines aren't very good for recreation, but doesn't want to miss out on the next dxm just because he didn't ask.

[Paracelsus]

Cetirizine is one of the newer antihistamines, which, like loratadine and unlike diphenhydramine or promethazine, do not cross the blood-brain barrier. Overdose is certainly not recommended, since at least one case of cardiac arrhythmia was reported and related antihistamines (astemizole & terfenadine) were pulled off the market for this reason.

[kalininin]

Originally Posted by Paracelsus

Cetirizine is one of the newer antihistamines, which, like loratadine and unlike diphenhydramine or promethazine, do not cross the blood-brain barrier. Overdose is certainly not recommended, since at least one case of cardiac arrhythmia was reported and related antihistamines (astemizole & terfenadine) were pulled off the market for this reason.

u-h-u-m, overdose not recommended oc, but howbout just dose ?
blood-brainbarrier-stuff means no-high somehow ? how's that then ?

[Exc_quetz]

Damn, owell.

[Paracelsus]

If "dose" would be psychoactive, cetirizine would not be approved in that dose. And yes, if it can't cross the blood-brain barrier, it can not enter the brain, where psychoactive drugs generally act (obviously).

[kalininin]

yep got it thxx

[jok3r]

Zyrtec [Generic Name: ceterizine] is a otc antihistamine almost just like diphenhydramine / benadryl. swim actually takes one everyday before going to class since swims allergies are bad, and unlike diphen. instead of getting very tired and very heavy, swim just has stuff moving off in the corners of his eyes, just like taking a very low recreational dose of diphen. Swim was wondering if one could use zyrtec recreationally, what the doses would be, and what to expect, if even possible.

[sarbanes]

Cetirizine is to hydroxyzine as acetic acid is to methanol. The only difference between the two is a carboxylic in cetirizine, whereas hydroxyzine has an alcohol there. Cetirizine is the primary active metabolite of hydroxyzine, and hydroxyzine itself has little or no anti-histamine activity (and very little central effect). Most of the extremely sedating qualities from hydroxyzine (Atarax/Visteral), come from the cetirizine metabolite. You may ask, how is this possible, as cetirizine is marketed as a new, non drowsiness anti-histamine? Well, when you take hydroxyzine, some of it is metabolized in the brain (as this molecule freely passes the BBB), where it is free to have its central effects. The rest of the molecule (occurring throughout the body), has its beneficial antihistamine effect. The small amount of cetirizine (formed in vivo there), is essentially trapped, and slowly *leaks* out of the brain system, and is finally dealt with by the liver. To the extent that cetirizine (formed from in vivo hydroxyzine), leaches out through the blood brain barrier (i.e. how long the sedating qualities of hydroxyzine dose last), one could correlate the magnitude of central effects due to taking higher dose cetirizine alone. It is not cardio toxic like the old, prototype non-central antihistamine (Hisminal), which, chemically is astemizole, and was voluntarily recalled by Janssen over a decade ago. Unfortunately, hydroxyzine passes the BBB quite easily, while cetirizine doesn't. Hopefully this clears up some misconception regarding the nature of this antihistamine.
Isn’t -COOH easily turned into -OH?

[Omalley]

one of SWIM's friends says this stuff makes him trip, SWIM just doesn't know what he is talking about, he said he took 3 of em and started acting goofy

[nibble]

Originally Posted by Omalley

one of SWIM's friends says this stuff makes him trip, SWIM just doesn't know what he is talking about, he said he took 3 of em and started acting goofy

Are you sure you aren't refering to cyclizine? That's an older gen antihistamine that is psychoactive. It exerts its psychoactive effects through its action as an anticholinergic, that type of drug may produce effects like those described. It definately wasn't cetirizine that caused that anyway, its simply not psychoactive.