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Difference between hydroquinone and "Cispera", a cream used to treat chloasma overseas

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Difference between hydroquinone and "Cispera", a cream used to treat chloasma overseas

Cyspera R is a cosmetic cream used in cases of 30 melasma patients at the 2013 Annual Meeting of the American Academy of Dermatology Association (AAD).

In Japan, up to 2% of "hydroquinone", which suppresses the enzyme that synthesizes melanin, is allowed in cosmetics, but we will confirm the difference from hydroquinone and the precautions for safe use. ..

Ingredients of cispera

Cysteamine Various ingredients are mixed in cispera, but the one that is attracting attention is "cysteamine".

Cysteamine Injecting cysteamine into a black goldfish was discovered in 1966 by Dr. Chavin's research team to decolorize white. Furthermore, in 1968, a research team of Dr. Pathak and Dr. Bleehen showed that it was more effective than hydroquinone.

In this way, although the effects of cysteamine have been shown in the past, the reason why it has not been commercialized is that it was difficult to commercialize it as an application agent for the skin due to the pungent odor of cysteamine. I will.

However, in 2012, Scientis developed a new technology that stabilizes the ingredients as an external preparation and strongly reduces the odor. As a result, Sispera containing 5% cysteamine was commercialized as a cream.

Cysteamine is a compound found in mammalian cells

Cysteamine is a compound found in mammalian cells Cysteamine is said to be contained in high concentrations in human breast milk among mammals, and acts as an antioxidant.

To explain the function of antioxidants, let's start with "active oxygen".

Reactive oxygen refers to atoms and molecules with an odd number of electrons.

A molecule is the smallest unit that has the properties of a substance and is composed of a combination of atoms. At the center of an atom is a nucleus in which two electrons are paired, but some of them have an odd number of electrons, and active oxygen corresponds to them.

Reactive oxygen species are unstable because they are not paired with electrons, and try to stabilize by robbing (oxidizing) electrons from others.

On the other hand, antioxidants that act as "reduction", which is the opposite of oxidation, neutralize the oxidizing power of active oxygen by giving electrons to active oxygen and prevent oxidation .

Reactive oxygen is generated by the uptake of oxygen into the body and protects the body from harmful substances such as bacteria, but when it is overproduced, it also attacks healthy cells. As a result, aging such as age spots, wrinkles, and sagging will appear.

Therefore, it can be expected to prevent aging by suppressing the action of active oxygen that is excessively generated by the functioning of antioxidants.

Cysteamine odor

Cysteamine is a component that is also used as a component of hair perm solution, and cysteamine-containing cispera has a peculiar odor, as it is sometimes described as "perm solution-like odor".

In hair, a kind of protein "keratin" is bound in various forms such as cystine bond, salt bond, and hydrogen bond, but in perm, the bond is cut with a reducing agent (1st liquid) and an oxidizing agent (2nd liquid). By recombining, it is waved or straightened.

Cysteamine is a component contained in one of the various bonds of keratin that reduces the "cystine bond".

All ingredients of cispera

Water, mineral oil, systemamine hydrochloride, niacinamide, Butyrospermum Parkii (shea butter), lecithin, glyceryl stearate, isopropyl myristate, cetyl alcohol, ascorbyl palmitate, ceteares 20, sodium ascorbyl phosphate, octyldodecanol, phenoxyethanol, Ethylhexyl glycerin, propyl heptyl caprylate, ceteales 12, cetearyl alcohol, cetyl palmitate, fragrance, xanthan gum, dipolyhydroxystearate Peg 30, tocopherol, mitsuro, BHT, EDTA tetrasodium, hexyl cinnamaldehyde, linalol, geraniol

Those who are suitable for cispera

  • Those who are worried about spots and freckles caused by sunburn
  • Those who are concerned about pigmentation such as acne scars
  • Those who are concerned about dullness and pigmentation of the lips
  • Those who want to get rid of pigmentation around the eyes
  • Those who are worried about darkening of the body

Parts where cispera can be used

Cispera can be used on any part of the face, not just the face. / p>

  • Face (around eyes, including lips)
  • neck
  • hand
  • side
  • elbow
  • knee
  • lips
  • Areola
  • Butt
  • Delicate zone

Pigmentation process and action by antioxidants

Pigmentation process

The skin is layered from the outside with the epidermis and dermis, but the epidermis is further divided into four layers. The cells "melanocytes" that make melanin pigments that cause spots and chloasma are located in the "basal layer," which is the lowest layer of the epidermis.

Melanin pigment is contained in granules called "melanosomes" and is passed to skin cells called "keratinocytes" by the action of proteins and the like. And if the skin is healthy, the layered epidermis is pushed up by the metabolism of the skin called turnover. In the process, melanosomes are digested and the melanin pigment is eventually excreted from the body along with old keratin.

However, when melanin pigment is excessively produced and the turnover cycle is disturbed, it becomes difficult for the melanin pigment to be excreted from the body, and it accumulates and appears as pigmentation or spots .

If we take a closer look at the process by which melanin pigments are produced in the basal layer, when melanocytes are activated by stimuli such as ultraviolet rays, melanin pigments are produced as follows.

Melanin pigments are produced by the chemical reaction of tyrosine oxidation and polymerization in melanosomes.

  1. Tyrosine is oxidized by "tyrosinase"
  2. "Dopa" is produced (tyrosine hydroxylase activity)
  3. Action of "tyrosinase" on dopa Oxidation by dopaoxidase to produce "dopaquinone" (dopaoxidase activity)
  4. "Dopaquinone" oxidizes and changes to "Indolol compound"
  5. Become a melanin pigment

Characteristics due to the action of cysteamine

Antioxidants are said to have multiple effects on the melanin production pathway, including:

  • Preventing tyrosine from being oxidized
  • Suppresses the production of dopa
  • Inhibition of changes to indole compounds (inhibition of the first and last stages of melanin synthesis)
  • Inhibition of Fenton reaction * by quenching (quenching) of iron and copper ions
  • Quenching of dopaquinone (removal of dopaquinone from the melanin production pathway)
  • Increased intracellular glutathione (antioxidant effect)
  • Reduces dark melanin in the stratum corneum to a brighter color with antioxidant properties

* When the Fenton reaction occurs, active oxygen is generated.

There are two types of melanin pigments, black melanin (eumelanin) and yellow melanin (pheomelanin). When dopaquinone oxidizes, black melanin is produced, but in the presence of antioxidant cysteine and glutathione, dopaquinone binds to them to produce yellow melanin, which prevents the production of black melanin. I will.

The following nine actions are effective in influencing the process by which melanin pigments are made. There are multiple components that have each effect, but in cispera, cysteamine and niacinamide are said to have five effects.

Mechanism of action component
Tyrosinase inhibitor Cysteamine, hydroquinone, succinic acid, arbutin, azelaic acid, ascorbic acid, ellagic acid, glycolic acid, EFG
Dopa oxidase inhibitor Cysteamine, mulberry extract
Peroxidase Substrate Inhibitor (Protects from Oxidative Stress) Cysteamine
Increased intracellular glutathione Cysteamine
Inhibition of melanosome translocation Niacinamide, soybean extract, ypserene, dorian acid
Anti-hormonal agent Flutamide
Improved stratum corneum turnover Tretinoin, glycolic acid
Blocking the plasmin pathway Tranexamic acid
Cytotoxicity Hydroquinone

Treatment with cispera announced overseas

Explaining abroad, 16 weeks of treatment with cispera has been shown to reduce the melanin index of melasma lesions by 67% and the area of melasma by 58%.

It was shown that the melanin index of chloasma lesions was reduced by 67%.

A 58% reduction in melasma area was shown

In addition, the results have been shown in multiple clinical evaluations other than the cases with AAD introduced at the beginning.

Double bride test results

In 2015, the British Journal of Dermatology (BJD) conducted the first double-blind study in 50 patients with epidermal melasma, confirming its effectiveness. I did. The double-blind test is a commonly used method to check the efficacy and therapeutic effect of a drug. The purpose is to confirm the true effect of the drug, and clinical trials are conducted without knowing which one is the real drug, both on the side of the treatment and on the side of the treatment.

References: Evaluation of the efficacy of cysteamine 5% cream in the treatment of epidermal melasma: a randomized double-blind placebo-controlled trial

Comparison with other treatments to lighten blemishes

"Skin Research & Techonology" has shown clinical results that it is more effective than the Krigman prescription in treating 50 patients with chloasma. Krigman prescription is a treatment with "Krigman ointment" (containing hydroquinone, tretinoin and dexamethasone), a whitening ointment jointly created by Dr. Krigman and Dr. Virus, and it is reported that it has the effect of thinning spots in 6 to 8 weeks. I am.

Sispera can also be used when Krigman ointment is ineffective.

References: Clinical evaluation of efficacy, safety and tolerability of cysteamine 5% cream in comparison with modified Kligman's formula in subjects with epidermal melasma: A randomized, double-blind clinical trial study

In addition, the treatment results show that it has fewer complications and is more effective than "tranexamic acid mesotherapy," in which "tranexamic acid," which is also used as an internal medicine and is used to treat age spots, is injected into the skin with a needle.

References: Clinical evaluation of efficacy and tolerability of cysteamine 5% cream in comparison with tranexamic acid mesotherapy in subjects with melasma: a single-blind, randomized clinical trial study

Difference between Cispera and "Hydroquinone"

We will confirm the difference from the ingredient "hydroquinone" that suppresses the production of melanin pigment due to sunburn.

The use of hydroquinone may have side effects such as redness and rashes. In addition, there is a risk of vitiligo, which causes a part of the skin to become white when used for a long period of time, and care must be taken when using it, such as darkening of spots when exposed to ultraviolet rays.

It is said that there is no risk of using Cispera for a long period of time as the skin gradually gets used to it, even if it may be irritating immediately after the start. In addition, since it does not cause chemical changes due to light such as "darkening of stains" (it is not photosensitive), it can be used at any time of the day, daytime, or night, so it is easier to use than hydroquinone. I can say.

However, it is recommended to take UV protection when going out so that you can feel the effect more while using Sispera.

Precautions for using hydroquinone

May have side effects

Hydroquinone, sometimes called a "skin bleaching agent," is said to have the effect of thinning and preventing blemishes. On the other hand, it is characterized by skin damage such as redness, rashes, itchiness and rough skin, and allergic reactions.

In addition, hydroquinone alone has low penetration into the skin, so it is often used in combination with "tretinoin," which accelerates turnover and removes dead skin cells. Since the use of tretinoin involves downtime such as peeling (exfoliation of old dead skin cells), dryness, and redness , the combination of tretinoin and hydroquinone is a method that some people avoid.

Risk of vitiligo

When used for a long period of time, hydroquinone increases the risk of vitiligo and makes it less effective .

It is also known as a potentially mutagenic and carcinogenic compound and is known to induce ochronosis.

References: Hydroquinone and its analogues in dermatology --a potential health risk

References: Exogenous ochronosis: the failure of depigmenting creams

References: xogenous Ochronosis

Spots may darken

In addition, the area where hydroquinone is applied may have dark spots when exposed to ultraviolet rays. Therefore, you should refrain from using hydroquinone before going out .

Comparison table of cysteamine and hydroquinone

Cysteamine Hydroquinone
Origin of the molecule Human origin Chemical substances
Mechanism of action Inhibition of tyrosinase, inhibition of peroxidase, increase of intracellular glutathione, termination of reaction of dopaquinone (quenching), inhibition of fenton-type reaction to generate active oxygen, decrease of melanin in stratum corneum Tyrosinase inhibition
merit High decolorization effect, no photosensitivity, biocompatibility & degree of oxidation is acceptable High decolorization effect
Side effects Mild irritation (when not used as instructed) Rebound (exacerbation of pigmentation), photosensitivity, ochronosis, black spots, bleaching
safety Non-cytotoxic, anti-mutagenic, anti-carcinogenic, radioprotective -

In addition to hydroquinone, there are several other ingredients that are thought to act on the production of melanin pigments. For example, there are non-hydroquinone topical agents such as tranexamic acid, kojic acid, arbutin, azelaic acid, retinoids, and hydroxy acids, which are said to have no downtime after long-term use, but tend to have mild effects. It is said to be in.

Cispera can be used by people with hydroquinone allergies

Since Cispera does not have the peeling that occurs with hydroquinone, it can also be used by the following people.

  • Those who are allergic to hydroquinone
  • Those who are concerned about downtime of treatment methods that use tretinoin and hydroquinone together

How to use Sispera in two stages

The use of cispera is divided into two stages.

  • Stage 1 (Intensive Care Unit): Once daily for 16 weeks
  • Second stage (maintenance treatment period): 2 days a week, once a day

You can expect to maintain healthy skin by first performing intensive care for 16 weeks and then using Cispera 2 days a week as maintenance treatment.

It can be used in any of the morning, noon, and night hours, but it is said that the effect will be felt sooner when used at night.

Also, while using Sispera, keep your skin moisturized and use a sunscreen with a high SPF value such as SPF50.

How to use once a day

The usage once a day is as follows.

Use after resting the skin

Since cispera has high penetrating power, it is desirable to apply it to the skin where some sebum remains.

If you use it on dry skin after washing your face, it will easily cause irritation such as strong redness and rash, so if you use it after washing your face, wait at least 1 hour before using it. In addition, there is no problem even if you moisturize with lotion etc. after a while. By using Cispera after moisturizing, irritation due to dryness can be suppressed .

Wait 15 minutes after application

Apply the entire amount of Cispera pushed 2-4 times and wait 15 minutes.

Leaving it unrinsed for more than 15 minutes can cause redness and irritation.

Rinse away

After washing with a cleanser, rinse with lukewarm water.

Moisturize

Moisturize well after washing your face.

What you need to know before using Sispera

The irritation after applying Sispera gradually disappears

Side effects may include a tingling sensation, heat, and redness, which can be subsided by rinsing and allowing time. Such a reaction is normal, and although it may continue for several days from the day when the application of Cispera is started, it is said that the irritation is basically eliminated as the skin gradually gets used to it .

However, if you do not see any improvement after a few days and the strong stimulus does not disappear, please consult a medical institution.

Sispera is stored at 15 ° C to 30 ° C

It is recommended to store at room temperature of 15 ℃ to 30 ℃.

In addition, since cispera has the property of oxidizing and turning brown when exposed to air, remove any oxidized cream when using it. The container of Sispera is sealed in a vacuum state. Since the contents are pumped out , the cream inside the container does not come into contact with the air .

About combination with other beauty medicine

It is recommended to refrain from using cispera during downtime after a peeling procedure to remove dead skin cells or other cosmetology.

Those who cannot use cysteamine

  • For sensitive skin
  • Those who use tretinoin or retinol
  • Those who are undergoing peeling treatment
  • Those with peeling or redness
  • Pregnant or lactating people, children under 15 years old (children) because they have not been tested

Retinol is Vitamin A. Tretinoin is a modified retinol structure that has been approved by the FDA (US Food and Drug Administration), the Ministry of Health, Labor and Welfare of Japan, as a drug used to treat skin spots, wrinkles, and acne.

References: Tretinoin

How to purchase Sispera and precautions when purchasing

Sispera can be purchased at medical institutions and sales sites operated by medical institutions, and has a capacity of 50g.

The Ministry of Health, Labor and Welfare has issued a warning regarding the purchase of cream for the purpose of whitening.

"Please be careful about using overseas creams for whitening personally imported via the Internet."

Please check that it is a genuine product without purchasing it easily . Also, if you purchase at a medical institution, you can consult with us if you have any trouble during use, so you can rest assured.

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