And thus it begins: Xyzal

The money being wasted on pointless research, that is. Xyzal (levocetirizine), is beginning to have some money spent on research proving that it’s a good drug. I have no doubt it’s a good drug. They’ve isolated the active isomer and decided to market it since the patent on Zyrtec (cetirizine) is running out.

Let’s review, SAT-style:


Expect Zyrtec to go OTC as a means of ensuring continued profitability through marketing. (More people buy brand name Tylenol than the generic — same story for Claritin.)

Here’s the bottom line: everything that Zyrtec works for, Xyzal will work for, and vice versa. Same side effects, too. And because this is so, you will never see a head-to-head study comparing Xyzal with Zyrtec, because the results will prove that it’s just a waste of money. Like Clarinex. Oh sure, there will be a few isolated cases where Xyzal is 0.5% better for 0.1% of the study population, and these studies will be trumpeted, but remember that they’re actually meaningless. You’ll also see studies that show Xyzal is effective for some obscure condition that Zyrtec was never studied for. Just remember that this is done to make Xyzal seem like something more than a me-too drug, and that if someone bothered to spend the money, Zyrtec would work just as well.

So if you like to waste your time doing PAs or you feel an insane need to throw your patients’ money away, prescribe Xyzal. Otherwise keep on using Zyrtec.

30 thoughts on “And thus it begins: Xyzal

  1. Yeah, for the polarization of the light, I suppose you are technically correct. I meant the pointlessness of the drug, though. :)

  2. OK, not that I trust UCB as far as I can throw them…..

    But if someone was on a particularly potent p450 CYP 3A4 inhibitor, like ritonavir, would it be worth using the active metabolite rather than the pro-drug? AUC for cetirizine increases 42% in the presence of therapeutic ritonavir levels, and while that’s similar to the elevation found in the elderly or in mild renal impairment, that strikes me as clinically significant to some degree….

    Eric, NOT a fan of me-too patent extensions.

  3. Whoops, I’m sorry. I mentally jumped a track.

    I thought Xyzal::Zyrtec as Zyrtec::Atarax. My bad.

    Ignore that.


  4. No worries. Actually, in the prescribing information of Xyzal, they are actually using the information for plain ol’ Zyrtec (cetirizine) as it relates to plasma [] in the presence of a potent 34A inhibitor, which I find rather amusing. It’s almost as if they’re acknowledging that the drugs are, for all intents and (clinical) purposes, the same.

    In vitro data indicate that levocetirizine is unlikely to produce pharmacokinetic interactions through inhibition or induction of liver drugmetabolizing enzymes. No in vivo drug-drug interaction studies have been performed with levocetirizine. Drug interaction studies have been performed with racemic cetirizine.

  5. “Expect Zyrtec to go OTC as a means of ensuring continued profitability”

    I thought you knew.. Zyrtec IS going OTC in December.
    I got the notice from Cardinal last month to prebook.
    All strenghts, all forms, will be OTC by the end of the year.

    No reason why this could not have happened years ago.
    Zyrtec has been available in Canada OTC under the name Reactine since the drug was released up there. So is Claritin and Allegra… not sure about about Clarinex, but most likely yes!

  6. Ah. I heard rumors, and it was the next logical move, just like Claritin did.

    Ironic because the price will fall through the floor whereas it’s one of the most expensive antihistamines at the moment.

    This pricing crap is Lame with a capital L.

  7. Actually, Reactine was Rx in Canada for at least a couple of years of life – certainly in the period before it was approved at all in the US – I was a lab rat for a Phase III and wanted to stay on it after (better relief than the other non-sedatings), so I made a trip up there…which must have been about 1993ish.

    UCB ended up with a partnership with Sanofi for Xyzal specifically due to the OTC switch – Pfizer had some restrictions with the sale of the consumer business, I believe.


  8. Actually – no. Atarax/Zyrtec is like Claritin/Clarinex – they are metabolites the body will make one into another. Zyrtec/Xyzal is an isomer like Celexa/Lexapro. Totally different.

  9. Actually – no. Atarax/Zyrtec is like Claritin/Clarinex – they are metabolites the body will make one into another. Zyrtec/Xyzal is an isomer like Celexa/Lexapro. Totally different.


    Claritin: loratidine
    Clarinex: desloratadine

    Zyrtec: cetirizine
    Xyzal: levocetirizine

    Celexa: citalopram
    Lexapro: escitalopram

    The comparison works for all three drugs. Regardless of how it gets there, one is the racemic mixture, and the other is the racemic mixture.

  10. First a few points:

    Clarinex is the active metabolite of clarion. Clinical data between the two has been scarce and not much to report in terms of superiority either way.

    Levocitirizine has been shown in several clinical studies (ie pollen chamber, receptor affinity models, and radiolabeled BBB analysis) to be both more potent and less sedating than zyrtec. The two drugs are similar and may not be worth giving them xyzal if they can get better on clariton or generic fex, but an alergist or ENT who knows the drug will be doing the potential paperwork to get thier patient on Levo.

  11. For those of us with chronic ideopathic urticaria, an isomer might just do the trick. I will gladly pay extra to get the relief I need rather than having to overdose on a combination of benedryl and zyrtec. The mirror image of the medicine might fit better into my H1-receptors – it’s worth a shot!

  12. For years and I mean many years I’ve been trying anything that seemed the least be credible to rid myself of mucus causing me to clear my throat to the point I had do do so before every sentence. I’ve been to Stanford Medical Clinic, UC Davis and several doctors who have tried all types of pill, shots and treatments. I had given up. About a two months ago I saw an ad in the local paper asking the question “Lost you voice? Let us help.” I said “oh sure” and moved on.

    The ad, week after week, kept catching my eye so I decided to give it a try only to learn that it was for a medical group I’d all ready seen a couple of times about my problem with no noticable benefits.

    I set an appointment anyway and up seeing the same doctor I said this visit is pointless and explained why. He did the routine investigation sticking a device up my nose and down to the vocal cord area and informed me things looked perfectly normal.

    After much discussion he said well try this pill and gave me some free samples. It’s new so who knows? The pill is Xyzal. I’ve taken it for two days now and my problem is 95 to a 100% resolved. I can’t believe it. Will it last? I don’t know. I certainly hope it will. I’ve done so many pills I’m near certain at one time Zyrtec was prescribed. I know Claritin and the spin offs do nothing at all for me. For now, from my perspective, Xyzal is a Godsend.

  13. The person who wrote this article is a moron. I have been getting chronic hives for over 4 months and I was taking Zyrtec twice a day in combination with Prednisone and let me tell you ZYRTEC IS GARBAGE. It did nothing to prevent me from getting hives and nothing for my everyday allergies. The very first day I took XYZAL there was a huge noticeable difference in my hives. The hives used to get in my throat and cover my body, now i might get a couple on my arms or stomach, but they are small. And the steroids that are so horrible got cut from 60mg a day to 5mg a day. Now if ZYRTEC AND XYZAL are the same, how come ZYRTEC didn’t do the trick?

  14. The same reason Nexium and Prilosec work differently for a tiny percentage of the population: nobody knows. The human body is fickle, but I never said they were the same, because they’re not.

  15. I’ve just started taking Xyzal prescribed by an allergist. 1st pill last night. I’ve had CIU (hives) for a year now, since I had surgery to remove part of my thyroid. Have been to several Doctors, Endos, and no one even told me of this medicine. I’ve been on 20 mg Zyrtec daily, 300 mg Zantac daily (for H2 blocker), Claritin, Prednisone – you name it, but they’ve continued to strike along with angiodema, been to the hospital with blocked airway twice and now carry epipen wherever I go… I don’t care if this drug is trumped up – desperate people will try anything to cure this damned condition! I’m hopeful that this will work… I also have chronic Gerd and am taking Prevacid along with Synthroid for my thyroid – 44 years old and falling apart at the seams. Anyone heard of thyroid problems causing hives?

  16. Yes, thyroid problems can cause hives and are associated with them. Anytime our body is sick, in any way, our immune system will try and attack the illness but sometimes it overworks and will produce too much histamine thus causing hives. The best advice I have for you, is remember it could be much worse. I have hives and cervical cancer. I have been getting hives for 5 months now every single day, and the only thing that treats them is steroids and Xyzal, and let me tell you I have mood swings, gained 50 pounds, my bones hurt like you cant believe and my chest constantly feels like it’s being hit with a baseball bat. Oh yeah and I have chronic GERD as well. Drink milk for that and avoid greasy food as much as possible. I get the same thing you do with the angiodema, and the blocking of the airways. I have been in the ER 4 times for it and i have thousands of dollars in bills to pay for all the blood testing my allergist had to do that my insurance wont cover because its hives. I’m only 20 years old, and I feel like I’m falling apart too. Strict diet and lots of cardio will make you feel a lot better if your willing to do that. Our bodies go back to the way they are supposed to be when we remove the bad food and exercise, because when you do exercise you heal yourself. x

  17. I am normally sceptical of “the new, latest, greatest” drug but this time it’s different. For years I’ve used Zyrtec, and its generic,plus Singulair at night. I only made the switch to Xyzal last week when my doc gave me some samples, warning me that the ragweed pollen was especially bad this year. Apart from the benefit of fewer sneezes and improved breathing, I was delighted to find that my eyes are no longer painful. Two different eye-doctors gave me RXs for expensive drops and creams without mentioning that allergies might be the root of the problem. This morning was the first time in many months that I have needed NO eyedrops. I’m so glad I tried something new. Now I’m going to try a new inhalant, Xopenex.

  18. I have been fighting hives for 3yrs now. I was hospitolized once. I notice everytime I catch a cold here they come. I was on prednisone for a year and a half. Been through many test and they cant find a thing wrong with me. I have been on all of them. Atarax, cetrizine, loratine, doxipin, benadryl, Zantac and now Xyzal. Xyzal works. It works faster than zyrtec. I never want to be back on prednisone… ever. I also take supplements like bee pollen (not allegic to bees). It is suppose to be a natural anti-histamine. GNC is the chapest place to get it. I have lost hope. Doxipin works but it makes it hard to get out of bed. One comment on prednisone. Mood swings occur just because its a steroid. I had them bad too. Almost caused me my marrige.

  19. Xyzal works. I’m allergic to any tree you can name and all types of grass. I was on Claritin back when it wasn’t OTC, then I was on Singulair and then I was on Zyrtec. And I’ve always been on a nasal spray. My allergist put me on Xyzal about five weeks ago and I CAN BREATH!! I can walk through a park with tons of grass growing everywhere and I don’t sneeze! It’s truly amazing. I don’t think I’ll ever stop taking Xyzal. It has finally provided me with the relief I have been searching for.

    Xyzal. Works.

  20. OK, so is there anything about Zyrtec being much more sedative than Xyzal? My allergy doc prescribed Xyzal with Singular and gave me samples to try for a couple weeks to make sure they worked. Everything worked great, except my insurance required me to use Zyrtec before they would cover Xyzal, so I switched. They both seem to handle my allergies the same, except I’ve noticed a huge increase in drowsiness and sleeplessness with Zyrtec. (I’m one of those people that drowsiness actually keeps me up instead of helping me sleep) Is this common? There was drowsiness with Xyzal, but nothing close to this extreme. So far I’m thinking I’d rather fork over the extra cash if it means I don’t have to wake up in the middle of the night and not be able to go back to sleep for an hour or more every night.

  21. I have had Chronic Hives for a few years. No amount of anti-histamines would help. I took zyrtec during the day and atarax at night with no relief. I do have thyroid antibodies with normal TSH. After finding an article regarding thyroid antibodies and Chronic Hives, I convinced a Dr. to try synthroid treatment to get rid of the hives. This resulted in me being hive free for 9 months – I was even able to tolerate the things I was found to be ever so slightly allergic to – that before synthroid caused Horrible reactions that would rusult in horrible hives that lasted for days and inability to breathe.

    The hives recently returned and my synthroid was increased which has resulted in alleviation of the hives once again and my TSH is still within safe range.

    I really don’t know why everyone with chronic hives isn’t tested for thyroid antibodies and subsequently treated with supression therapy if they test positive for thryoid antibodies.

    Xyzal once released did reduce the severity of hives while zyrtec did nothing.

  22. I’m trying to get PA for Xyzal which worked way better for me than Zyrtec. I also take celexa because my insurance wouldn’t pay for lexapro and understand the mirror image thing. Celexa works just as well for me. But with the antihistamine I have a hypothesis and I’d like feedback. I’ve got lots of allergies and have taken every antihistamine and after awhile they stop working – some kind of tolerance I suppose. So could it be possible that the new drug somehow works when the nearly identical drug has stopped working?

  23. If anyone here is suffering from CHRONIC HIVES

    You need to take Doxepin

    Ask your doctor about it. It will help you.

  24. Worked wonders for my itching. Nothing OTC worked long enough including zyrtec. Just remember to take at bed time. Doctor said if the problem is related to histamine, this works great. Text XYZAL to 62900 to receive a text coupon. I paid just $25 for my prescription.

  25. I have taken them both. I have found a significant difference, for me at least. Zyrtec does not control my skin conditions at all, however Xyzal does. However, I do know of allergy suffers in my family that do better on Zyrtec. I don't think its a all-in-all type of situation. Depending on your condition, one might work better for you than the other does.

  26. Xyzal works much better than Zyrtec did for me, with out the drowsiness. Xyzal is the active isomer of Zyrtec, hence the desired antihistamine effect with half the sleepiness. I ran through a 4-way stop sign at high speed on my morning commute while on Zyrtec and decided to never take it in the morning again.

  27. Xyzal is OTC now in 2017. Thankful for that. Subtly, but solidly handles my allergies. Initially, some can feel –slight– sedation but this goes away after a few days–nothing a zap of coffee or tea won’t fix. The mostly non-sedating Xyzal works really well for me.

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