Roxithromycin for Acne and Rosacea - Rosacea Knowledge Forum by Geoffrey Nase PhD

Dr. Geoffrey Nase · #1 (**permalink**) 11th April 2010, 08:56 PM

Question: "I have moderate acne and rosacea. What is the best oral treatment for this combination?" - Amy

Amy,

Low dose accutane is a favorite of mine. Roaccutane at 2.5 mgs, 5.0 mgs or 10 mgs per day is an excellent treatment.

Roxithromycin, one of the newer macrolide antibiotics is probably the best antibiotic choice for acne and rosacea. The "macrolides" have significantly more anti-inflammatory effects on rosacea skin when compared to tetracyclines, doxycycline, minocycline, oracea, etc. For the most part, rosacea sufferers should put away the old tetracylines. Clinical studies comparing macrolide antibiotics to the older tetracyclines shows much better efficacy in almost every case.

The other benefit of Roxithromycin is that it decreases damaging neutrophils in and around the acne lesions and reduces acne produced lipase (a substance that causes redness and inflammation... exacerbating rosacea blood vessels and overzealous immune cells). Thus, Roxithromycin has distinct advantages over Clarithromycin and Azithromycin for rosacea with coexsiting acne.

Recommended dose for mild to moderate acne is 150 mgs twice daily
Recommended dose for severe acne is 300 mgs twice daily

Dermatology. 2002;204(4):277-80.

Effects of Roxithromycin on the production of lipase and neutrophil chemotactic factor by Propionibacterium acnes.

Akamatsu H, Tomita T, Horio T.

Abstract

BACKGROUND: The macrolide antibiotic roxithromycin is effective against acne associated with inflammation, but the mechanism by which this is achieved has not been clarified.

OBJECTIVE: We studied the effects of roxithromycin on the production of lipase and neutrophil chemotactic factor by Propionibacterium acnes in vitro.

RESULTS: Roxithromycin significantly inhibited the production of lipase and neutrophil chemotactic factor by P. acnes at a concentration one eighth of the MIC, at which the growth curve of P. acnes is not affected.

CONCLUSION: One mechanism of the effectiveness of roxithromycin in acne therapy is thought to be the inhibition of bacterial lipase and neutrophil chemotactic factor production by P. acnes.

Dr. Geoffrey Nase · #2 (**permalink**) 11th April 2010, 10:12 PM

Roxithromycin Outperforms Azithromycin and Clarithromycin

Very interesting findings below:

Roxithromycin treats key rosacea-induced inflammatory pathways:

(1) Migration of neutrophils
(2) Oxidative burst of phagocytes
(3) Production of inflammatory cytokines

J Antimicrob Chemother. 1998 Mar;41 Suppl B:47-50.

Comparative anti-inflammatory effects of roxithromycin, azithromycin and clarithromycin.

Scaglione F, Rossoni G.

Abstract

There are many published reports on the anti-inflammatory effects of macrolides, some dating back to the introduction of erythromycin. Macrolides have been shown to affect a number of the processes involved in inflammation, including the migration of neutrophils, the oxidative burst in phagocytes and the production of various cytokines, although the precise mechanisms are not clear. These effects have been linked to the ability of macrolides to accumulate in mammalian cells. Roxithromycin, a macrolide with better plasma concentrations and higher tissue concentrations than erythromycin, has been tested in a standard animal model used for evaluating anti-inflammatory drugs. When rats were given a prophylactic dose (20 mg/kg), roxithromycin suppressed the oedema produced by injecting carrageenin into the paw with effects almost equal to that seen with the non-steroidal anti-inflammatory drug nimesulide. Azithromycin and clarithromycin, macrolides with better pharmacokinetics than erythromycin, only showed slight anti-inflammatory effects. These results confirm that roxithromycin has anti-inflammatory properties in vivo and encourage the investigation of its mode of action.

Dr. Geoffrey Nase · #3 (**permalink**) 14th April 2010, 01:49 AM

Rosacea is considered a disorder of overactive neutrophils - our immune system in our facial skin thinks its under attack and sends inflammatory neutrophils that destroy everything in site... including blood vessels and skin cells.

Several rosacea specialists have even published medical journal articles indicating that "Rosacea is primarily a Neutrophilic Disorder".

Thus, any medication or treatment that "calms" down the immune response and reduces neutrophil chemotaxis (migration of neutrophils to inflamed tissue) are of tremendous help. That is where Roxithromycin excels:

Modulatory effect of roxithromycin on human neutrophil function

Journal Research in Experimental Medicine
Publisher Springer Berlin / Heidelberg
ISSN 0300-9130 (Print) 1433-8580 (Online)
Issue Volume 196, Number 1 / December, 1996

Abstract

Neutrophils are thought to play a key role in tissue injury. We investigated the effect of roxithromycin, a 14-membered ring macrolide, on human neutrophil functions. The drug inhibitedN-formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide (O 2 − ) production and Ca2+ influx of human neutrophils. The inhibition was overcome by adding an inhibitor of cyclic AMP-dependent protein kinase (PKA), H-89. These results suggest that the drug affects O 2 − production and intracellular Ca2+ concentration of neutrophils via the action of PKA. Moreover, roxithromycin ameliorated endothelial cell injury induced by neutrophils, which may be, in part, due to the effect of the drug on neutrophils. Thus, roxithromycin may contribute to the treatment of diseases worsened by the excessive action of neutrophils.

Dr. Geoffrey Nase · #4 (**permalink**) 14th April 2010, 02:08 AM

IMPORTANT:

A Unifying Theory of Rosacea Pathophysiology

The Role of Neutrophils. The intimate relationship between the vasculature and the immune system, as well as the success of anti-inflammatory agents in the treatment of rosacea, suggests that inflammatory cells such as neutrophils, and other inflammatory mediators, are key pathophysiologic factors in the development of rosacea[21] (Figure 6). The stigmata of rosacea may be manifestations of an inflammatory process: neutrophilic dermatosis.[21] Therefore, pharmacologic modulation of neutrophilic function is critical to the resolution of rosacea.[22]

Excellent Link: http://www.medscape.com/viewarticle/448505_5

Grateful1 · #5 (**permalink**) 30th April 2010, 12:39 AM

Dr. Nase,

Thank you so much for being a guiding light for so many of us.

I have been on and off tetracycline twice in the past 2 years and I am getting on Roxithromycin (rulide). I think I may have developed some 'super-bacteria' as a result...

Do you think starting with a higher dose and then 'leveling-off' may be more helpful with Roxithromycin?

Any strategies or insight that might help this work faster, or more effectively?

I found a study that showed about equal results with using this antibiotic every-other day:

Clinical evaluation of roxithromycin in acne vulgaris: comparison of daily versus alternate day regimen
J Pak Assoc Derma Jan - Mar 2005;15(1):32-6.
Bahawal-Victoria Hospital, Bahawalpur

Roxithromycin, one of the newer macrolides, has been shown to be effective in acne in some clinical trials. These trials have been done with once or twice daily dosage schedules. As another closely related macrolide, azithromycin, has been shown to be effective when used on alternate days, we conducted this trial to see whether an alternate day regimen of roxithromycin gives comparable results with those of daily regimen or not. One hundred and forty patients were included in the study and were randomly divided in two groups. Patients in Group-I used 300 mg of roxithromycin orally once daily for eight weeks. Those in Group- II used 300 mg of roxithromycin orally on alternate days for eight weeks. Results could be evaluated in 125 patients, with 15 patients lost to follow up. Out of 60 patients in Group-I, 32% showed good(>50%) improvement, 57% moderate (25-50%) and 10% slight (<25%) improvement. Of the 65 evaluable patients in Group-II, 28% showed good, 55% moderate and 14% slight improvement. Using chi-square tests the difference between the results of the two groups was found to be insignificant (p>0.5). Side effects noted were transient and were nausea, slight gastric upset and diarrhea in 10% patients in Group-I and 4.6% patients in Group-II. In conclusion, alternate day dosage regimen is found to be almost equally effective but safer and more economical than daily dosage regimen.

Sleera · #6 (**permalink**) 29th January 2011, 11:54 AM

In my experience, this is one of the best anti-inflammatories for rosacea.

Dr. Geoffrey Nase · #7 (**permalink**) 6th February 2011, 11:18 AM

Quote:

Originally Posted by Grateful1

Dr. Nase,

Thank you so much for being a guiding light for so many of us.

I have been on and off tetracycline twice in the past 2 years and I am getting on Roxithromycin (rulide). I think I may have developed some 'super-bacteria' as a result...

Do you think starting with a higher dose and then 'leveling-off' may be more helpful with Roxithromycin?

Any strategies or insight that might help this work faster, or more effectively?

I found a study that showed about equal results with using this antibiotic every-other day:

Clinical evaluation of roxithromycin in acne vulgaris: comparison of daily versus alternate day regimen
J Pak Assoc Derma Jan - Mar 2005;15(1):32-6.
Bahawal-Victoria Hospital, Bahawalpur

Roxithromycin, one of the newer macrolides, has been shown to be effective in acne in some clinical trials. These trials have been done with once or twice daily dosage schedules. As another closely related macrolide, azithromycin, has been shown to be effective when used on alternate days, we conducted this trial to see whether an alternate day regimen of roxithromycin gives comparable results with those of daily regimen or not. One hundred and forty patients were included in the study and were randomly divided in two groups. Patients in Group-I used 300 mg of roxithromycin orally once daily for eight weeks. Those in Group- II used 300 mg of roxithromycin orally on alternate days for eight weeks. Results could be evaluated in 125 patients, with 15 patients lost to follow up. Out of 60 patients in Group-I, 32% showed good(>50%) improvement, 57% moderate (25-50%) and 10% slight (<25%) improvement. Of the 65 evaluable patients in Group-II, 28% showed good, 55% moderate and 14% slight improvement. Using chi-square tests the difference between the results of the two groups was found to be insignificant (p>0.5). Side effects noted were transient and were nausea, slight gastric upset and diarrhea in 10% patients in Group-I and 4.6% patients in Group-II. In conclusion, alternate day dosage regimen is found to be almost equally effective but safer and more economical than daily dosage regimen.

Hello,

I definitely think the tetracyclines should be tucked into a nice deep cupboard as they help very few rosacea sufferers. The problem is that they are inexpensive and are still listed in 2011 Medical Textbooks as the best treatment for rosacea along with Metrogel

.... just look at your doctor's handbooks and PDR's and you will think you've been transported back to the 1800's.

It is highly unlikely that you've built up a resistance or a super bug as these are actually quite rare..... almost non-existant in the real medical world. Rosacea sufferers and mothers with children are told about these superbugs so that they don't ask for antibiotics for a simple cold (as this medication will not help colds anyway). It's definitely overkill.

I think the best way to attack rosacea is via multiple avenues and hard! Safe, but hard because you must break years (even decades) of deep inflammation and you can't do it on one or two medications at standard doses.

Talk to your physician about 500 mgs twice daily for the first three to six months. It sounds like a lot but there is a lot to reverse. Then, when you've beaten back rosacea to the point you can stand, reduce to a maintenance dose (e.g. pulse dosing every Saturday) and see if that keeps you clear.

Keep us posted Grateful!

_

Grateful1 · #8 (**permalink**) 19th April 2011, 05:13 PM

Dr. Nase,

Thanks for the info.

Been on roxi for almost a year now (hard to believe). I would recommend it to anyone who is at a loss.
I get it from sundrugstore and have never been ripped off. good prices. Although shipping takes longer than it should. The pharmacy is in Mumbai, so hopefully it is good quality (?)

At first I was taking a total of 300mgs a day...150mg morning and night, with about a 30% decrease in inflammation after about 4-5 months on it, which takes the edge off.

After 4-5 months of this, it seemed that 300mg a day was too much.

I would get a clear increase in inflammation from taking this dosage

So now I usually take one 150mg every other day, and it works good (30% decrease). It seems like if I take the pills randomly, instead of on a schedule, they work better.

MY QUESTION:
As a general rule of thumb, should taking more roxi provide more anti-inflammatory effects?
Or is it dependent on personal chemistry/inflammatory cycles - ?

Thank you very much for your commitment and hard work.

Grateful1 · #9 (**permalink**) 19th April 2011, 05:22 PM

Dr. Nase,

Do you recommend milk thistle for the liver with the long-term usage of roxithromycin?

Will a good yogurt everyday be enough to counteract side effects?

Thanks again!

Dr. Geoffrey Nase · #10 (**permalink**) 23rd November 2011, 04:15 AM

Quote:

Originally Posted by Grateful1

Dr. Nase,

Do you recommend milk thistle for the liver with the long-term usage of roxithromycin?

Will a good yogurt everyday be enough to counteract side effects?

Thanks again!

Dear Grateful1,

You can't go wrong with milk thistle for your liver. I would just make sure that it is the form that is bound to phospholipids so that the active ingredients can traverse across the liver cells and into the cytosol.

After quite a bit of feedback it looks like Roxithormycin might be better than Clarithromycin and Azithromycin against rosacea papules and pustules. Definitely worth trying... especially for those flare ups.

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