Friday, January 20, 2006
Alphagan P (0.15% brimonidine) and SansRosa
[UPDATE Added, 16th March 2006: I am not a doctor, but to spell out just some of the possible risks as I understand them, of using alpagan p contrary to its prescribed usage (remember, this is a prescription eye-drop for glaucoma!):
fatigue
dangerously low blood pressure
dangerously high blood pressure rebound
coronary problems
long-lasting rebound redness
increased flushing
damage to facial blood vessels
increased blood flow the face (reactive hyperemia)
skin irritation
psychosis...
I could go on. In my opinion anyone using this medicine off-limits, as I say below, is not only foolish but reckless and potentially putting their health, and rosacea, at serious risk.
---
This blog wondered alound a couple of months ago:
"... one of the SansRosa's founders, and his wife happened to be rosacea sufferers. She had put something on her face for an unrelated medical condition and noticed a lightening of her skin" (my note: I wonder what this was!)
Maybe the answer is in the SansRosa patent.
I was recently re-reading the SansRosa patents in a little more detail.
Particularly this one. The amount of detail in the patent is fascinating. It is worth reading in full... Particularly the section where they describe the results of their experimentations with various topical blood vessel constrictors. SanRosa's "secret sauce" is putting such a blood vessel contrictor in a topical, rosacea-friendly formultion whereby systemic absorbtion is not a problem. Why? Because systemic absorbtion of something that causes blood vessel constriction is probably a Very Bad Thing.
Quote:
"1.7. 9 Example 9 Alphagan P (0.15% brimonidine tartrate in isotonic saline and citrate buffer having a pH of 6.3 to 6.5) was supplied by Allergan, Inc. having the composition disclosed in Example 2 above. A study was conducted with four otherwise healthy persons who were independently diagnosed with phase II rosacea (characterized by transitory erythema of the mid-facial areas and early telangiectasis). All subjects followed a morning protocol of cleansing their face with soap and water. After a gentle towel drying and air drying, Alphagan-P was administered by gently rubbing onto areas of facial redness. The application area was again allowed to air dry without any dressing.
Subject 1 is a 59 year old woman with a ten year history of rosacea displaying symptoms of periodic redness flare-ups across her cheeks that usually runs a course of three to four weeks before subsiding under customary dermatological treatment. The subject showed an immediate improvement after the first morning application of Alphagan-P. All redness disappeared within 10 minutes and her face remained symptom free for the entire first day. "
[case histories]
...
"These trials demonstrate that 0. 15% brimonidine tartrate, when used in a daily morning protocol, dramatically eliminates or reduces redness due to rosacea. It is shown to be an effective treatment to greatly accelerate the arrest of a rosacea flare-up. It is further shown to be an effective daily treatment for chronic rosacea redness. "
Alphagan P is a prescription topical eye-drop for use by Glaucoma patients. It contains the active ingredient brimonidine tartrate. Two things of interest.
1. The patent claims that in an experiment, topical application of Alphagan P "dramatically eliminates or reduces redness due to rosacea" and gives case histories.
(Note: I would assume that this is NOT safe to do, in case anyone gets the foolish idea of trying it on themselves - Alphagan P is a serious eye-drop that must be prescribed by a Doctor for glaucoma!).
Even when used properly for glaucoma the eye-drops come with a long list of side-effects and cautions. Certainly when reading about this medication and application as prescribed for glaucoma, there are potentially serious side-effects from systemic absorbtion (see more below).
2. It makes me suspect that brimonidine tartrate or a modified version of it, will be the active ingredient in SansRosa. I guess that the challenge for SansRosa and Collagenex is ensuring that any systemic absorbtion from their topical is either non-existant or within safe limits.
Again, from the patent, talking about systemic effects from these kinds of medications:
"These systemic effects include, cardiopulmonary effects of (3-blockers like timolol; dryness of mouth, flush, fever, tachy cardia, urinary retention, convulsion and irritability with atropine; hypertension with phenylephine; increased salivation, nausea, vomiting, diarrhea, stomach cramps, bronchial secretions, brionchial constriction, asthma, bradycardia, paresthesia with miotics; hypotension with clonidine; and dry mouth, fatigue and drowsiness with apraclonidine and brimonidine. "
Whereas the SansRosa invention... (emphasis mine)
"Summary Of The Invention The present invention provides methods, compounds, and topical skin formulations for treatment of rosacea and its symptoms. Compounds of the invention are a2 adrenoceptor agonists that act on the peripheral vasculature to cause vasoconstriction and thereby ameliorate the symptoms of rosacea. The compounds are delivered in a topical skin composition that insures that the compounds are effective in the skin of a patient but do not penetrate the skin in sufficient amounts to induce serious systemic side effects. "
Previous related posts:
Our first post on SansRosa
Transcript of interview with founder
Windhover SansRosa report snippets
SansRosa patent details
Collagenex purchases SansRosa
fatigue
dangerously low blood pressure
dangerously high blood pressure rebound
coronary problems
long-lasting rebound redness
increased flushing
damage to facial blood vessels
increased blood flow the face (reactive hyperemia)
skin irritation
psychosis...
I could go on. In my opinion anyone using this medicine off-limits, as I say below, is not only foolish but reckless and potentially putting their health, and rosacea, at serious risk.
---
This blog wondered alound a couple of months ago:
"... one of the SansRosa's founders, and his wife happened to be rosacea sufferers. She had put something on her face for an unrelated medical condition and noticed a lightening of her skin" (my note: I wonder what this was!)
Maybe the answer is in the SansRosa patent.
I was recently re-reading the SansRosa patents in a little more detail.
Particularly this one. The amount of detail in the patent is fascinating. It is worth reading in full... Particularly the section where they describe the results of their experimentations with various topical blood vessel constrictors. SanRosa's "secret sauce" is putting such a blood vessel contrictor in a topical, rosacea-friendly formultion whereby systemic absorbtion is not a problem. Why? Because systemic absorbtion of something that causes blood vessel constriction is probably a Very Bad Thing.
Quote:
"1.7. 9 Example 9 Alphagan P (0.15% brimonidine tartrate in isotonic saline and citrate buffer having a pH of 6.3 to 6.5) was supplied by Allergan, Inc. having the composition disclosed in Example 2 above. A study was conducted with four otherwise healthy persons who were independently diagnosed with phase II rosacea (characterized by transitory erythema of the mid-facial areas and early telangiectasis). All subjects followed a morning protocol of cleansing their face with soap and water. After a gentle towel drying and air drying, Alphagan-P was administered by gently rubbing onto areas of facial redness. The application area was again allowed to air dry without any dressing.
Subject 1 is a 59 year old woman with a ten year history of rosacea displaying symptoms of periodic redness flare-ups across her cheeks that usually runs a course of three to four weeks before subsiding under customary dermatological treatment. The subject showed an immediate improvement after the first morning application of Alphagan-P. All redness disappeared within 10 minutes and her face remained symptom free for the entire first day. "
[case histories]
...
"These trials demonstrate that 0. 15% brimonidine tartrate, when used in a daily morning protocol, dramatically eliminates or reduces redness due to rosacea. It is shown to be an effective treatment to greatly accelerate the arrest of a rosacea flare-up. It is further shown to be an effective daily treatment for chronic rosacea redness. "
Alphagan P is a prescription topical eye-drop for use by Glaucoma patients. It contains the active ingredient brimonidine tartrate. Two things of interest.
1. The patent claims that in an experiment, topical application of Alphagan P "dramatically eliminates or reduces redness due to rosacea" and gives case histories.
(Note: I would assume that this is NOT safe to do, in case anyone gets the foolish idea of trying it on themselves - Alphagan P is a serious eye-drop that must be prescribed by a Doctor for glaucoma!).
Even when used properly for glaucoma the eye-drops come with a long list of side-effects and cautions. Certainly when reading about this medication and application as prescribed for glaucoma, there are potentially serious side-effects from systemic absorbtion (see more below).
2. It makes me suspect that brimonidine tartrate or a modified version of it, will be the active ingredient in SansRosa. I guess that the challenge for SansRosa and Collagenex is ensuring that any systemic absorbtion from their topical is either non-existant or within safe limits.
Again, from the patent, talking about systemic effects from these kinds of medications:
"These systemic effects include, cardiopulmonary effects of (3-blockers like timolol; dryness of mouth, flush, fever, tachy cardia, urinary retention, convulsion and irritability with atropine; hypertension with phenylephine; increased salivation, nausea, vomiting, diarrhea, stomach cramps, bronchial secretions, brionchial constriction, asthma, bradycardia, paresthesia with miotics; hypotension with clonidine; and dry mouth, fatigue and drowsiness with apraclonidine and brimonidine. "
Whereas the SansRosa invention... (emphasis mine)
"Summary Of The Invention The present invention provides methods, compounds, and topical skin formulations for treatment of rosacea and its symptoms. Compounds of the invention are a2 adrenoceptor agonists that act on the peripheral vasculature to cause vasoconstriction and thereby ameliorate the symptoms of rosacea. The compounds are delivered in a topical skin composition that insures that the compounds are effective in the skin of a patient but do not penetrate the skin in sufficient amounts to induce serious systemic side effects. "
Previous related posts:
Wednesday, January 18, 2006
What is rosacea?
I added a new page to the site, an introduction for new visitors:
What is rosacea?
It includes some thoughts on current treatments.
What is rosacea?
It includes some thoughts on current treatments.
Saturday, January 07, 2006
Facial flushing in birds
You read it right - avian flushing!
A fascinating little study, may be of interest to some.
It is interesting to contemplate WHY we flush on our faces (and primarily cheeks and nose), and indeed part of the answer to blocking this flushing may be in answering that question.
Some theories being
Function and occurrence of facial flushing in birds, on PubMed
Quote:
"The bare facial skin of both the caracara and the hooded vulture contains a highly vascularised tissue under the epidermis that may be filled with blood and would thus produce red skin colours. In contrast, feathered areas of the head show very few vessels immersed in connective tissue and have no potential for colour changes. Species with flushing colours are few but phylogenetically diverse, as they belong to 12 different avian orders and at least 20 families. The majority are dark-coloured, large-sized species living in hot environments that may have originally evolved highly vascularised skin patches for thermoregulation. Bird behaviour as well as sex and age differences within species suggest that a signalling system for condition or status based on haemoglobin may have been super-imposed to the physiological process of heat dissipation."
A fascinating little study, may be of interest to some.
It is interesting to contemplate WHY we flush on our faces (and primarily cheeks and nose), and indeed part of the answer to blocking this flushing may be in answering that question.
Some theories being
- thermoregulation
- flushing / blushing as a social signal
Function and occurrence of facial flushing in birds, on PubMed
Quote:
"The bare facial skin of both the caracara and the hooded vulture contains a highly vascularised tissue under the epidermis that may be filled with blood and would thus produce red skin colours. In contrast, feathered areas of the head show very few vessels immersed in connective tissue and have no potential for colour changes. Species with flushing colours are few but phylogenetically diverse, as they belong to 12 different avian orders and at least 20 families. The majority are dark-coloured, large-sized species living in hot environments that may have originally evolved highly vascularised skin patches for thermoregulation. Bird behaviour as well as sex and age differences within species suggest that a signalling system for condition or status based on haemoglobin may have been super-imposed to the physiological process of heat dissipation."
Friday, January 06, 2006
Aczone Phase II Clinical Trials Now Recruiting
According to Clinicaltrials.gov, there is a Phase II, Randomized Study of ACZONE™ (Dapsone) Gel 5% for Papulopustular Rosacea recruiting. This is taking place in quite a few states, so if you're interested head on over to the site for information regarding eligibility and the nearest testing locations.
Link to the site:
http://www.clinicaltrials.gov/ct/show/NCT00249782?order=1
Link to the site:
http://www.clinicaltrials.gov/ct/show/NCT00249782?order=1
