Derobin

Derobin 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 .

Coal tar has antipruritic, keratoplastic and keratolytic properties. It slows down excessive epidermal cell turnover and is often used topically either alone or in combination with other drugs (e.g. salicyclic acid, sulfur) in conditions such as dandruff, seborrheic dermatitis or psoriasis.

Decrease bacterial growth.

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.

Trade Name Derobin
Generic Anthralin + Salicylic Acid + Coal Tar
Weight 1.15%
Type Ointment
Therapeutic Class
Manufacturer Usv Pvt Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Derobin
Derobin

Uses

Dithranol is used for subacute and chronic psoriasis.

Coal Tar Cream is used for psoriasis. Soritar Cream has a keratoplastic and antipruritic effect in psoriasis.

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).

Derobin is also used to associated treatment for these conditions: Psoriasis Chronic, Quiescent PsoriasisDandruff, Psoriasis, Seborrheic Dermatitis, Seborrhoeic Dermatitis of the ScalpAcne, 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 Derobin 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 .

Coal tar ointment is a keratolytic. It works by slowing bacterial growth and loosening and softening scales and crust.

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

Derobin 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%.

Adults and children over 12 years of age: Ensure that the lesions are clean. Apply a thin layer of Coal Tar Cream two or three times a day on to the affected areas massage in gently and leave to dry.

For young children under 12 years of age and the elderly: The emulsion may be diluted by mixing it with a few drops of cooled freshly boiled in the palm of the hand.

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.

Skin and subcutaneous tissue disorders: Skin irritation, photosensitivity of the skin, Coal Tar Cream may cause acne-like eruptions of the skin. There is an increased risk of skin cancer in psoriatic patients treated with a combination of Coal Tar Cream and UVB radiation has been reported. However epidemiological studies of patients treated with Coal Tar Cream on its own are inconclusive. The risk of toxicity should be taken into account when considering the prescribing this product for the patient.

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 .

LD50: Not available.

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

Intended for local use only, no systemic absorption.

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 .

Intended for local use only, no systemic absorption.

Half Life

Intended for local use only, no systemic absorption.

Clearance

Intended for local use only, no systemic absorption.

Elimination Route

Intended for local use only, no systemic absorption.

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.

There is no direct evidence of the safety in pregnant and lactating mother. Coal tar preparations have been in use for many years without apparent ill-consequence. No harmful effects on the health of the child is anticipated with the proper use of coal tar. However it is recommended that the use of coal tar in pregnancy and lactation is restricted to intermittent use in low concentrations on a small percentage of body’s surface, use during the first trimester be avoided.

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.

Coal Tar should not be used when a patient has known sensitivity to Coal Tar or any of the other ingredients. If you have folliculitis and acne vulgaris. Coal Tar Cream should not be used on patients who have disease characterised by photosensitivity such as lupus erythematosus or allergy to sunlight. Coal Tar Cream should not be applied to inflamed or broken skin. Warnings and precautions: For topical administration only. Coal Tar Cream may cause skin irritation, should this occur the treatment should be reviewed and if necessary discontinued. Coal Tar enhances photosensitivity of the skin after applying Coal Tar Cream exposure to direct sunlight should be avoided. Use with care near the eyes and mucous membranes. If any emulsion should accidentally enter the eye, flush with normal saline solution or water. Do not apply to genital and rectal areas. Apply with caution to the face do not get in the eyes. Hydrogenated polyoxyl castor oil may cause skin reactions. Methyl and propyl hydroxybenzoates may cause allergic reactions that might be cause a delayed reaction.

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.

There is no evidence that an overdose of topical Coal Tar Cream would be harmful other than a hypersensitivity to coal tar. Ingestion of Coal Tar Cream may require gastric lavage depending on the quantity taken and should be treated symptomatically.

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.

Storage Condition

Store between 15-30°C. Protect from excessive heat.

Store in a cool and dry place, protected from light.

Store at a temperature below 25° C.

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