Anaxeryl

Anaxeryl Uses, Dosage, Side Effects, Food Interaction and all others data.

Dithranol reduces the mitotic rate and proliferation of epidermal cells in psoriasis by inhibiting DNA replication, cellular respiration and key cellular enzymes.

Anthralin is a natural anthraquinone derivative, anti-psoriatic and anti-inflammatory agent. It controls skin growth by reducing the synthesis of DNA and the mitotic activity in the hyperplastic epidermis, normalizing the rate of cell proliferation and keratinization .

Ichthammol is also referred to as ammonium bituminosulfonate or ammonium bituminosulphonate. It is an ammonium salt of dark sulfonated shale oil (bituminous schists) produced via distillation of the oil followed by sulfonation and neutralization. It is available in OTC products as an active ingredient for the treatment of skin disorders such as eczema, psoriasis and boils as it is thought to exhibit anti-inflammatory, antibacterial and antimycotic properties .

Resorcinol is a 1,3-isomer (or meta-isomer) of benzenediol with the formula C6H4(OH)2. It is used as an antiseptic and disinfectant in topical pharmaceutical products in the treatment of skin disorders and infections such as acne, seborrheic dermatitis, eczema, psoriasis, corns, calluses, and warts. It exerts a keratolytic activity. Resorcinol works by helping to remove hard, scaly, or roughened skin.

Although it is primarily indicated for use as a topical application, resorcinol also possesses a well-documented anti-thyroidal activity that is generally not relied upon for any kind of formal therapeutic indication.

In vitro and in vivo studies have demonstrated that resorcinol can inhibit peroxidases in the thyroid and subsequently block the synthesis of thyroid hormones and cause goiter . Resorcinol interferes with the iodination of tyrosine and the oxidation of iodide . In an in vitro study involving lactoperoxidase (LPO) and thyroid peroxidase (TPO), it was shown that the mechanism of these two enzymes can become irreversibly inhibited by way of a suicide inactivation by resorcinol .

Salicylic acid has a potent keratolytic action and a slight antiseptic action when applied topically. It softens and destroys the stratum corneum by increasing endogenous hydration which causes the horny layer of the skin to swell, soften, and then desquamate. At high concentrations, salicylic acid has a caustic effect. It also possesses weak antifungal and antibacterial activity.

Salicylic acid treats acne by causing skin cells to slough off more readily, preventing pores from clogging up. This effect on skin cells also makes salicylic acid an active ingredient in several shampoos meant to treat dandruff. Use of straight salicylic solution may cause hyperpigmentation on unpretreated skin for those with darker skin types (Fitzpatrick phototypes IV, V, VI), as well as with the lack of use of a broad spectrum sunblock. Subsalicylate in combination with bismuth form the popular stomach relief aid known commonly as Pepto-Bismol. When combined the two key ingredients help control diarrhea, nausea, heartburn, and even gas. It is also very mildly anti-biotic.

Anaxeryl
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Anaxeryl
Generic	Anthralin + Ichthammol + Resorcinol + Salicylic Acid
Weight	0.35%w/w, 0.85%w/w, 0.2%w/w, 0.3%w/w
Type	Ointment
Therapeutic Class
Manufacturer	Seignior Pharma
Available Country	Pakistan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Dithranol is used for subacute and chronic psoriasis.

Contemporary therapeutic uses for resorcinol primarily revolve around the use of the phenol derivative as an active ingredient in topical antiseptics or as topical antibacterial skin treatment products for conditions like acne, seborrheic dermatitis, eczema, and others .

6% Salicylic Acid: This topical preparations treat the following common scaly conditions:

Chronic atopic dermatitis
Lichen simplex
Psoriasis
Seborrhoeic dermatitis
Ichthiosis

12% Salicylic Acid: This topical preparations treat the following common scaly conditions:

Warts (small excessive growths of skin caused by a type of virus. Warts often occur on the fingers or on the back of the hands).
Verruca (occurs only on the sole of the feet and can be painful. It often looks like a small white ring of skin with a black dot in the centre).
Corns and Calluses (are hard, thick pads of skin caused by pressure and friction. They usually occur on the feet due to poorly fitting shoes and can occur on the hands).

Anaxeryl is also used to associated treatment for these conditions: Psoriasis Chronic, Quiescent PsoriasisAnal Fissures, Dermatitis, Eczematous, Dry Skin, Hemorrhoids, Internal, Keratinized Tissue, Pruritus Ani, Pyoderma, Skin Irritation, SplinterAcne VulgarisAcne, Actinic Keratosis (AK), Alopecia Areata (AA), Atopic Dermatitis (AD), Blackheads, Chronic Eczema, Chronic cutaneous lupus erythematosus, Corns, Dandruff, Dermatitis, Contact, Dermatitis, Eczematous, Dermatitis, Eczematous of the scalp, Discoid Lupus Erythematosus (DLE), Foot Callus, Fungal skin infection, Furuncle, Hand Eczema, Hyperkeratosis, Hyperkeratosis follicularis et parafollicularis, Infections, Fungal, Infections, Fungal of the Skin Folds, Infections, Fungal of the face, Infections, Fungal of the feet, Infections, Fungal of the hand, Keratosis Palmaris et Plantaris, Lichen, Lichen Plano-Pilaris, Lichen Planus (LP), Lichen simplex chronicus, Molluscum Contagiosum, Musculoskeletal Pain, Neurodermatitis, Palmo-Plantar Pustulosis, Plantar Warts, Pruritus, Psoriasis, Psoriasis Vulgaris (Plaque Psoriasis), Psoriasis of the scalp, Rash, Ringworm of the Skin, Ringworm of the scalp, Seborrheic Dermatitis, Seborrhoeic Dermatitis of the Scalp, Skin Infections, Bacterial, Verrucous Psoriasis, Warts, Calluses, Corticosteroid-responsive dermatoses, Keratinization disorders, Scaling, Scaling of skin, Scalp seborrhea, Superficial Fungal skin infection, Keratolysis

How Anaxeryl works

Anthralin inhibits the proliferation of keratinocytes (epidermal skin cells), prevents the action of T-cells, and promotes cell differentiation, likely through mitochondrial dysfunction. In addition, the production of free radicals may contribute to its anti-psoriatic effect . In vitro studies demonstrate that anthralin prolongs the prophase component of mitosis for keratinocytes and leukocytes . Prophase is the first step of mitosis, the process separating the duplicated genetic material carried in the nucleus of a parent cell into two identical daughter cells . In vivo studies demonstrate that anthralin blocks DNA synthesis and can increase the release of reactive oxygen species .

Anthralin is believed to normalize the rate of epidermal cell proliferation and keratinization by reducing the mitotic activity of the epidermal hyperplasia in psoriasis .

Anti-proliferative and anti-inflammatory effects of anthralin have been demonstrated on both psoriatic and healthy skin. The anti-proliferative effects of anthralin are thought to be due to a combination of inhibition of DNA synthesis and its strong reducing properties. The effectiveness of anthralin as an anti-psoriatic agent is partly owed to its ability to promote lipid peroxidation and reduce the concentration of endothelial adhesion molecules, which are found to be elevated in psoriatic patients , .

Recent studies suggest that its ability to prevent T-lymphocyte activation and normalize keratinocyte differentiation may occur by a direct effect on mitochondria .

Data regarding the specific mechanisms of action of resorcinol does not appear to be readily accessible in the literature. Nevertheless, the effectiveness of the agent in treating various topical, dermatological conditions by eliciting antibacterial and keratolytic actions appears to stem from resorcinol's propensity for protein precipitation . In particular, it appears that resorcinol indicated for treating acne, dermatitis, or eczema in various skin care topical applications and peels revolves around the compound's ability to precipitate cutaneous proteins from the treated skin .

Salicylic acid directly irreversibly inhibits COX-1 and COX-2 to decrease conversion of arachidonic acid to precursors of prostaglandins and thromboxanes. Salicylate's use in rheumatic diseases is due to it's analgesic and anti-inflammatory activity. Salicylic acid is a key ingredient in many skin-care products for the treatment of acne, psoriasis, calluses, corns, keratosis pilaris, and warts. Salicylic acid allows cells of the epidermis to more readily slough off. Because of its effect on skin cells, salicylic acid is used in several shampoos used to treat dandruff. Salicylic acid is also used as an active ingredient in gels which remove verrucas (plantar warts). Salicylic acid competitively inhibits oxidation of uridine-5-diphosphoglucose (UDPG) with nicotinamide adenosine dinucleotide (NAD) and noncompetitively with UDPG. It also competitively inhibits the transferring of the glucuronyl group of uridine-5-phosphoglucuronic acid (UDPGA) to a phenolic acceptor. Inhibition of mucopoly saccharide synthesis is likely responsible for the slowing of wound healing with salicylates.

Dosage

Anaxeryl dosage

Short-contact therapy: As cream: Apply into lesions for up to 60 min/day before washing off. May increase strength gradually from 0.1-2%.

Topical/Cutaneous (Adult)-

Hyperkeratotic and scaling skin conditions: As 1.8-3% preparation: Apply to affected area of the skin and/or scalp 1-4 times daily.

Acne: As 0.5-2% preparation: Apply thinly to affected area 1-3 times daily, reduce to once daily or every other day if dryness or peeling occur.

Warts and calluses:

As 12-40% plaster: Fit over the wart/callus for 48 hr, repeat process 48 hrly as needed until wart/callus is removed (up to 12 wk for warts or up to 14 days for calluses).
As 5-17% preparation in collodion-like vehicle: Apply a small amount to sufficiently cover wart/callus and allow to dry. Repeat 1-2 times daily until wart/callus is removed (up to 12 wk for warts or up to 14 days for calluses).
As 15% preparation in karaya gum-glycol plaster vehicle: Smoothen warts with emery board and place a drop of warm water prior to application. Apply the plaster in the evening and leave in place for at least 8 hr to be removed in the morning. Repeat process 24 hrly, if necessary up to 12 wk.

Side Effects

Burning sensation esp on perilesional skin, temporary staining of skin and hair; skin irritation and/or warmth feeling on application site.

An allergic reaction (shortness of breath, closing of the throat, swelling of the lips, face or tongue or hives) or severe skin irritation.

Toxicity

Some mild adverse effects include alterations in nail coloring, hair coloring, increase in photosensitivity, and skin irritation .

The most common side effects of anthralin are skin irritation and staining of nearby skin, nails, clothing, and other objects that come in contact with the treated patient. The incidence of irritation of psoriatic/surrounding healthy skin is higher in patients who leave anthralin on the skin without rinsing than in those who use short-contact therapy of 2 hours or less, followed by rinsing .

If the psoriatic plaques are well circumscribed, the surrounding normal skin may be protected by the use of a coating agent such as zinc oxide ointment. Anthralin should be applied cautiously to the face and intertriginous areas due to the risk of severe skin irritation .

There is no current evidence of any long-term anthralin toxicity related either to skin exposure or to systemic issues . Some long-term studies in mice have demonstrated anthralin to be tumorigenic in mouse skin. This carcinogenic potential has not been thoroughly evaluated. Tumorigenic and carcinogenic effects of anthralin have not been observed in humans at this time . Anthralin is classified as FDA pregnancy risk category C drug . It is not known if anthralin can cause fetal harm when administered during gestation. Because of the lack of evidential human data, anthralin should be used during pregnancy only when clearly required .

Effects in man include CNS effects, mainly in persons who have used creams containing high levels of resorcinol, effects on the erythrocytes (especially methaemoglobinaemia, mainly in babies and infants) and, after prolonged exposure, effects on the thyroid gland (like goiter or especially chronic myxoedema) . In addition, exogenous ochronosis is associated with prolonged exposure to resorcinol . In persons suffering from resorcinol poisoning, the symptoms included anemia, spleen siderosis, and fatty degeneration of the liver and kidneys .

Oral rat LD50: 891 mg/kg. Inhalation rat LC50: > 900 mg/m3/1hr. Irritation: skin rabbit: 500 mg/24H mild. Eye rabbit: 100 mg severe. Investigated a mutagen and reproductive effector.

Precaution

Patient with fair skin. Children. Pregnancy and lactation.

For external use only. Avoid contact with eyes and other mucous membranes.

Interaction

May enhance the effect of photosensitising drugs. Propylene glycol-containing drugs may oxidise or inactivate dithranol. Withdrawal of long term steroids in psoriasis may cause rebound phenomenon.

Do not use other topical preparations on the treated area unless otherwise directed by your healthcare provider. They may interfere with treatment or increase skin irritation.

Volume of Distribution

Specific data regarding the volume of distribution of resorcinol is not readily available, although it is believed that the compound's volume of distribution is considered large, owing to resorcinol's profile as a lipid-soluble compound .

The volume of distribution is about 170 mL/kg of body weight.

Elimination Route

Anthralin penetrates damaged skin and psoriatic lesions faster and to a greater extent than normal skin, likely due to increased vascularity of psoriatic lesions .

The dermal absorption of resorcinol seems to be low (< 1%) when applied on healthy and intact skin . The agent absorbed very slightly under normal conditions & the absorption was lower when applied to the scalp than to clean shaven skin due to a strong fixation by the hair .

Half Life

Specific data regarding the half-life of resorcinol is not readily available, although, in one case of dermal exposure, an adult male with a 90% phenol exposure had an elimination half-life of about 14 hours .

Clearance

Specific data regarding the clearance of resorcinol is not readily available, although it is generally believed that the relatively low topical absorption or resorcinol does not result in an extensive systemic presence and clearance .

Elimination Route

Specific data regarding the route of elimination of resorcinol is not readily available, although the major metabolite of resorcinol found in the urine was its glucuronide .

About 10% is excreted unchanged in the urine.

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Pregnancy Category C. If used by nursing mothers, it should not be used on the chest area to avoid accidental contamination of the child.

Contraindication

Acute pustular psoriasis or inflamed skin.

It should not be used in any patient known to be sensitive to Salicylic Acid or any other listed ingredients.

Special Warning

Salicylic Acid is used in children over 2 years.

Acute Overdose

Symptoms: Burning and deep staining of the skin.

Management: Rinse first with water only and then wash at a temp not exceeding 30° C.

An overdose of Salicylic Acid topical is unlikely to occur. If you do suspect an overdose or if the medication has been ingested, call a poison control center or emergency room for advice.