SansRosa's Shortcomings - Not the Treatment we Hoped for... - Rosacea Knowledge Forum by Geoffrey Nase PhD

Dr. Geoffrey Nase · #1 (**permalink**) 19th May 2011, 11:13 PM

At three different strengths SansRosa still induces significant rebound redness or stops working in under a month. These are well-documented in the clinical literature and confirmed by rosacea testers on the various forums.

SansRosa utilizes a constrictor that is receptor-dependent and that is the core reason for its shortcomings. Chronic activation of these selective receptors causes them to over-react or to internalize and become non-responsive.

SansRosa has a place as a three to five day treatment for facial redness, but after this time frame, rebound dilation or non-responsiveness will take over.

The key to finding the proper constrictor is to find selective G-protein activated ingredients or vascular-specific ingredients that work directly on the intracellular calcium levels inside the vascular smooth muscle of rosacea blood vessels (e.g. Sarcoplasmic Reticulum and voltage-gated channels).

You can induce mild-to-moderate constriction indefinitely if you target G-proteins or intracellular calcium stores. The primary problem is that we still have skin specialists working on complex-vascular oriented events.... that is akin to asking a foot doctor to perform a cadiac bypass. Each medical profession has their specialty training and they rarely ever wander out of their comfort zone. This also explains why rosacea, a core vascular disorder, has been so poorly researched and treated for decades by skin specialists (Dermatologists). We fall through the cracks of medical specialties.

__

Katie - Moderator · #2 (**permalink**) 19th May 2011, 11:42 PM

Quote:

Originally Posted by Dr. Geoffrey Nase

At three different strengths SansRosa still induces significant rebound redness or stops working in under a month. These are well-documented in the clinical literature and confirmed by rosacea testers on the various forums.

SansRosa utilizes a constrictor that is receptor-dependent and that is the core reason for its shortcomings. Chronic activation of these selective receptors causes them to over-react or to internalize and become non-responsive.

SansRosa has a place as a three to five day treatment for facial redness, but after this time frame, rebound dilation or non-responsiveness will take over.

The key to finding the proper constrictor is to find selective G-protein activated ingredients or vascular-specific ingredients that work directly on the intracellular calcium levels inside the vascular smooth muscle of rosacea blood vessels (e.g. Sarcoplasmic Reticulum and voltage-gated channels).

You can induce mild-to-moderate constriction indefinitely if you target G-proteins or intracellular calcium stores. The primary problem is that we still have skin specialists working on complex-vascular oriented events.... that is akin to asking a foot doctor to perform a cadiac bypass. Each medical profession has their specialty training and they rarely ever wander out of their comfort zone. This also explains why rosacea, a core vascular disorder, has been so poorly researched and treated for decades by skin specialists (Dermatologists). We fall through the cracks of medical specialties.

__

This is certainly consistent with the reports coming in. What a dissapointment!!!

-Katie

Aaron1980 · #3 (**permalink**) 24th May 2011, 02:25 AM

Quote:

Originally Posted by Dr. Geoffrey Nase

At three different strengths SansRosa still induces significant rebound redness or stops working in under a month. These are well-documented in the clinical literature and confirmed by rosacea testers on the various forums.

SansRosa utilizes a constrictor that is receptor-dependent and that is the core reason for its shortcomings. Chronic activation of these selective receptors causes them to over-react or to internalize and become non-responsive.

SansRosa has a place as a three to five day treatment for facial redness, but after this time frame, rebound dilation or non-responsiveness will take over.

The key to finding the proper constrictor is to find selective G-protein activated ingredients or vascular-specific ingredients that work directly on the intracellular calcium levels inside the vascular smooth muscle of rosacea blood vessels (e.g. Sarcoplasmic Reticulum and voltage-gated channels).

You can induce mild-to-moderate constriction indefinitely if you target G-proteins or intracellular calcium stores. The primary problem is that we still have skin specialists working on complex-vascular oriented events.... that is akin to asking a foot doctor to perform a cadiac bypass. Each medical profession has their specialty training and they rarely ever wander out of their comfort zone. This also explains why rosacea, a core vascular disorder, has been so poorly researched and treated for decades by skin specialists (Dermatologists). We fall through the cracks of medical specialties.

__

Sadly I have to agree. There are over a dozen SansRosa testers on the other forums that I'm in contact with and the results are less than inspiring.

Dr. Nase - can't you develop a succesful topical anti-redness product as it seems to be out of the Derms field of knowledge and right in your vascular breakbasket.

- Aaron

jaydee · #4 (**permalink**) 26th May 2011, 04:17 AM

Quote:

Originally Posted by Dr. Geoffrey Nase

At three different strengths SansRosa still induces significant rebound redness or stops working in under a month. These are well-documented in the clinical literature and confirmed by rosacea testers on the various forums.

SansRosa utilizes a constrictor that is receptor-dependent and that is the core reason for its shortcomings. Chronic activation of these selective receptors causes them to over-react or to internalize and become non-responsive.

SansRosa has a place as a three to five day treatment for facial redness, but after this time frame, rebound dilation or non-responsiveness will take over.

The key to finding the proper constrictor is to find selective G-protein activated ingredients or vascular-specific ingredients that work directly on the intracellular calcium levels inside the vascular smooth muscle of rosacea blood vessels (e.g. Sarcoplasmic Reticulum and voltage-gated channels).

You can induce mild-to-moderate constriction indefinitely if you target G-proteins or intracellular calcium stores. The primary problem is that we still have skin specialists working on complex-vascular oriented events.... that is akin to asking a foot doctor to perform a cadiac bypass. Each medical profession has their specialty training and they rarely ever wander out of their comfort zone. This also explains why rosacea, a core vascular disorder, has been so poorly researched and treated for decades by skin specialists (Dermatologists). We fall through the cracks of medical specialties.

__

is that 3-5 days per week?
if one uses brimonidine/sansRosa say 1-2 times a week with good effects, then in your opinion would this reduce any chance of rebound dilation or non-responsiveness to the medication?

thanks

Dr. Geoffrey Nase · #5 (**permalink**) 28th May 2011, 01:04 AM

Quote:

Originally Posted by jaydee

is that 3-5 days per week?
if one uses brimonidine/sansRosa say 1-2 times a week with good effects, then in your opinion would this reduce any chance of rebound dilation or non-responsiveness to the medication?

thanks

Jaydee,

Excellent question. There is a very good reason why every single constrictor eye drop on the market has a three day warning... do not exceed three straight days and then stop the medication completely for at least a week or your eyes will become dilated and blood shot.

SansRosa will be extremely expensive (prohibitively for many), may still fail testing as it has for 9.5 years thus far, and if it does pass and goes to market -- human nature will take over and rosacea sufferers will use it for more than a few days and they will encounter rebound dilation analagous to topical steroid rebound (but without the skin thinning). That is a near-guarantee.

Galderma is using the wrong constrictor. You cannot use a selective alpha adrenergic receptor agonist. In fact Brominidine is so selective that it acts only on alpha-2A adrenoceptors. After a few days of a constrictor acting on a specific receptor subtype the receptor becomes hyper-responsive via G-protein mediated mechanisms (causing potent constriction) or the receptors internalize into the cell's cytoplasm and you lose all responsiveness for several weeks.

If Galderma Dermatologists collaborated with specialists outside of the skin area (remember these are the same dermatologists that are still using mineral oil, propylene glycol, lanolin, high concentration parabens and petroletum in many of their new products

) they would have developed a very good product years ago for vascular rosacea.

You need to add a dual alpha adrenergic constrictor in able to reduce the chances for rebound dilation. You need to target Cyclic AMP with a dual receptor activator (agonist).

To explain, the blood vessels in the facial skin have three types of adrenergic constrictors (alpha-1, alpha-2 and alpha-3). To complicate matters, each alpha adrenoceptor has several subtypes:

-- alpha-1A
-- alpha-1B
-- alpha-1C

-- alpha-2A
-- alpha-2B
-- alpha-2C

-- alpha-3A
-- alpha-3B
-- alpha-3C (still being studied)

Not only does Bromidine act only on alpha-2 receptors which is bad, but it acts selectively on alpha-2B receptor subtypes, which is doubly-bad. No matter what concentration, these receptors will power-up or power-down quickly. You probably have 2 to 5 days at most to use this product to reduce redness and then you will need to put it away for a week or two.

So, if you want to use it every Friday and Saturday to have a good weekend, this may be the product for you... as long as you can pay for it (Galderma's curative ORACEA (40 mgs doxycyline)

costs $457 per month at CVS Pharmacy... and most insurance companies don't cover the cost. This should be illegal because it costs $6 to purchase 50 mg generic doxcycline for a 30 day supply). Galderma seems to have missed Ethics 101 during their college years for running Pharmaceutical and Non-Profit Companies and they presumably missed Chemistry 101 and BioChemistry 101 as they are using ingredients that were disbanded in the 1940's because they made excellent land fill material.

Seriously, all they need to do is to develop a dual alpha-1 / alpha-2 receptor activator that constricts blood vessels no more than 20% (which equates to a 50% reduction in blood flow based on blood hemodynamics) and you've got yourself a GREAT topical that reduces redness, blotchiness, telangiectasia AND reduces the intensity & duration of flushing.

You can add two active ingredients to achieve this effect or you can use one of the dozen ingredients already available. I used dual alpha adrenoceptor agonists from 1994 through 2007 in my Bio-Medical Laboratory... you can get them from Sigma Chemicals (Research Grade) if you work at a medical laboratory. One of the best active ingredients that I tested on myself over several months was $25 for 10 grams of nanoparticle powder from Sigma chemicals... at a base concentration of 2% to 4% active ingredient, 10 grams (10,000 milligrams) lasts approximately 30 years and can be compounded into almost any lotion base as long as you use DMI to carry the active ingredient and buffer the pH: Dimethyl Isosorbide (DMI) is a high purity solvent and carrier which offers a safe, effective delivery enhancement mechanism for active ingredients in personal care products.

I will now remove myself from thy soapbox

__

Chris D · #6 (**permalink**) 4th June 2011, 11:52 PM

Quote:

Originally Posted by Dr. Geoffrey Nase

Jaydee,

Excellent question. There is a very good reason why every single constrictor eye drop on the market has a three day warning... do not exceed three straight days and then stop the medication completely for at least a week or your eyes will become dilated and blood shot.

SansRosa will be extremely expensive (prohibitively for many), may still fail testing as it has for 9.5 years thus far, and if it does pass and goes to market -- human nature will take over and rosacea sufferers will use it for more than a few days and they will encounter rebound dilation analagous to topical steroid rebound (but without the skin thinning). That is a near-guarantee.

Galderma is using the wrong constrictor. You cannot use a selective alpha adrenergic receptor agonist. In fact Brominidine is so selective that it acts only on alpha-2A adrenoceptors. After a few days of a constrictor acting on a specific receptor subtype the receptor becomes hyper-responsive via G-protein mediated mechanisms (causing potent constriction) or the receptors internalize into the cell's cytoplasm and you lose all responsiveness for several weeks.

If Galderma Dermatologists collaborated with specialists outside of the skin area (remember these are the same dermatologists that are still using mineral oil, propylene glycol, lanolin, high concentration parabens and petroletum in many of their new products

) they would have developed a very good product years ago for vascular rosacea.

You need to add a dual alpha adrenergic constrictor in able to reduce the chances for rebound dilation. You need to target Cyclic AMP with a dual receptor activator (agonist).

To explain, the blood vessels in the facial skin have three types of adrenergic constrictors (alpha-1, alpha-2 and alpha-3). To complicate matters, each alpha adrenoceptor has several subtypes:

-- alpha-1A
-- alpha-1B
-- alpha-1C

-- alpha-2A
-- alpha-2B
-- alpha-2C

-- alpha-3A
-- alpha-3B
-- alpha-3C (still being studied)

Not only does Bromidine act only on alpha-2 receptors which is bad, but it acts selectively on alpha-2B receptor subtypes, which is doubly-bad. No matter what concentration, these receptors will power-up or power-down quickly. You probably have 2 to 5 days at most to use this product to reduce redness and then you will need to put it away for a week or two.

So, if you want to use it every Friday and Saturday to have a good weekend, this may be the product for you... as long as you can pay for it (Galderma's curative ORACEA (40 mgs doxycyline)

costs $457 per month at CVS Pharmacy... and most insurance companies don't cover the cost. This should be illegal because it costs $6 to purchase 50 mg generic doxcycline for a 30 day supply). Galderma seems to have missed Ethics 101 during their college years for running Pharmaceutical and Non-Profit Companies and they presumably missed Chemistry 101 and BioChemistry 101 as they are using ingredients that were disbanded in the 1940's because they made excellent land fill material.

Seriously, all they need to do is to develop a dual alpha-1 / alpha-2 receptor activator that constricts blood vessels no more than 20% (which equates to a 50% reduction in blood flow based on blood hemodynamics) and you've got yourself a GREAT topical that reduces redness, blotchiness, telangiectasia AND reduces the intensity & duration of flushing.

You can add two active ingredients to achieve this effect or you can use one of the dozen ingredients already available. I used dual alpha adrenoceptor agonists from 1994 through 2007 in my Bio-Medical Laboratory... you can get them from Sigma Chemicals (Research Grade) if you work at a medical laboratory. One of the best active ingredients that I tested on myself over several months was $25 for 10 grams of nanoparticle powder from Sigma chemicals... at a base concentration of 2% to 4% active ingredient, 10 grams (10,000 milligrams) lasts approximately 30 years and can be compounded into almost any lotion base as long as you use DMI to carry the active ingredient and buffer the pH: Dimethyl Isosorbide (DMI) is a high purity solvent and carrier which offers a safe, effective delivery enhancement mechanism for active ingredients in personal care products.

I will now remove myself from thy soapbox

__

Dr. Nase,

This explains why its been undergoing testing for nearly 10 years. Your description tells the story and helps us understand what some physicians can do and what they can't . Dermatologists do not focus on the vascular form of rosacea because they were not trained in that area.

I guess they're throwing up a hail mary with SansRosa.

Chris

Katie - Moderator · #7 (**permalink**) 6th June 2011, 06:21 AM

Quote:

Originally Posted by Dr. Geoffrey Nase

Jaydee,

Excellent question. There is a very good reason why every single constrictor eye drop on the market has a three day warning... do not exceed three straight days and then stop the medication completely for at least a week or your eyes will become dilated and blood shot.

SansRosa will be extremely expensive (prohibitively for many), may still fail testing as it has for 9.5 years thus far, and if it does pass and goes to market -- human nature will take over and rosacea sufferers will use it for more than a few days and they will encounter rebound dilation analagous to topical steroid rebound (but without the skin thinning). That is a near-guarantee.

Galderma is using the wrong constrictor. You cannot use a selective alpha adrenergic receptor agonist. In fact Brominidine is so selective that it acts only on alpha-2A adrenoceptors. After a few days of a constrictor acting on a specific receptor subtype the receptor becomes hyper-responsive via G-protein mediated mechanisms (causing potent constriction) or the receptors internalize into the cell's cytoplasm and you lose all responsiveness for several weeks.

If Galderma Dermatologists collaborated with specialists outside of the skin area (remember these are the same dermatologists that are still using mineral oil, propylene glycol, lanolin, high concentration parabens and petroletum in many of their new products

) they would have developed a very good product years ago for vascular rosacea.

You need to add a dual alpha adrenergic constrictor in able to reduce the chances for rebound dilation. You need to target Cyclic AMP with a dual receptor activator (agonist).

To explain, the blood vessels in the facial skin have three types of adrenergic constrictors (alpha-1, alpha-2 and alpha-3). To complicate matters, each alpha adrenoceptor has several subtypes:

-- alpha-1A
-- alpha-1B
-- alpha-1C

-- alpha-2A
-- alpha-2B
-- alpha-2C

-- alpha-3A
-- alpha-3B
-- alpha-3C (still being studied)

Not only does Bromidine act only on alpha-2 receptors which is bad, but it acts selectively on alpha-2B receptor subtypes, which is doubly-bad. No matter what concentration, these receptors will power-up or power-down quickly. You probably have 2 to 5 days at most to use this product to reduce redness and then you will need to put it away for a week or two.

So, if you want to use it every Friday and Saturday to have a good weekend, this may be the product for you... as long as you can pay for it (Galderma's curative ORACEA (40 mgs doxycyline)

costs $457 per month at CVS Pharmacy... and most insurance companies don't cover the cost. This should be illegal because it costs $6 to purchase 50 mg generic doxcycline for a 30 day supply). Galderma seems to have missed Ethics 101 during their college years for running Pharmaceutical and Non-Profit Companies and they presumably missed Chemistry 101 and BioChemistry 101 as they are using ingredients that were disbanded in the 1940's because they made excellent land fill material.

Seriously, all they need to do is to develop a dual alpha-1 / alpha-2 receptor activator that constricts blood vessels no more than 20% (which equates to a 50% reduction in blood flow based on blood hemodynamics) and you've got yourself a GREAT topical that reduces redness, blotchiness, telangiectasia AND reduces the intensity & duration of flushing.

You can add two active ingredients to achieve this effect or you can use one of the dozen ingredients already available. I used dual alpha adrenoceptor agonists from 1994 through 2007 in my Bio-Medical Laboratory... you can get them from Sigma Chemicals (Research Grade) if you work at a medical laboratory. One of the best active ingredients that I tested on myself over several months was $25 for 10 grams of nanoparticle powder from Sigma chemicals... at a base concentration of 2% to 4% active ingredient, 10 grams (10,000 milligrams) lasts approximately 30 years and can be compounded into almost any lotion base as long as you use DMI to carry the active ingredient and buffer the pH: Dimethyl Isosorbide (DMI) is a high purity solvent and carrier which offers a safe, effective delivery enhancement mechanism for active ingredients in personal care products.

I will now remove myself from thy soapbox

__

Wow. You took the words right out of my mouth Dr. Nase.

It's like the blind leading the blind. I wonder if Dr. Dahl is involved in this study? I would think he's heading it up after his wonderful publication that reached every Derm's desktop titled, "Metronidazole Remains Remission in Rosacea". What a pile of junk. And he's one of our foremost rosacea derms that works at the Mayo Clinic.

Freakin unbelievable.

- Katie

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