Protar K

Uses

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

Treatment of superficial and deep mycoses:

• Infections of the skin, hair and nails by dermatophytes and/or yeasts (dermatomycosis, onychomycosis, perionyxis, pityriasis versicolor, chronic mucocutaneous candidiasis etc.) especially when topical treatment is difficult or not very effective, owing to involvement of large skin surfaces or to lesions affecting deeper dermal layers, nails and hairs
• Yeast infection of the mouth (oral thrush, perleche) and the gastrointestinal tract
• Vaginal candidiasis, especially chronic recurrent cases or cases responding poorly to topcial treatment
• Systemic mycotic infections such as systemic candidiasis, paracoccidioidomycosis, histoplasmosis, coccidioidomycosis etc.

Maintenance treatment to prevent recurrence in systemic mycotic infections and in chronic mucocutaneous candidiasis.Prophylactic treatment to prevent mycotic infection in patients with reduced host defenses, e.g., patients with cancer, organ transplant and burns.

Protar K is also used to associated treatment for these conditions: Dandruff, Psoriasis, Seborrheic Dermatitis, Seborrhoeic Dermatitis of the ScalpBacterial Vaginosis (BV), Blastomycosis, Candidiasis, Systemic, Chromomycosis, Chronic Mucocutaneous Candidiasis (CMC), Coccidioidomycosis, Dandruff, Endogenous Cushing's Syndrome, Histoplasmosis, Infections, Fungal, Paracoccidioidomycosis, Seborrheic Dermatitis, Tinea Corporis caused by Epidermophyton floccosumin, Tinea Corporis caused by Trichophyton mentagrophytes, Tinea Corporis caused by Trichophyton rubrum, Tinea Cruris caused by Epidermophyton floccosumin, Tinea Cruris caused by Trichophyton mentagrophytes, Tinea Cruris caused by Trichophyton rubrum, Tinea Pedis caused by Epidermophyton floccosumin, Tinea Pedis caused by Trichophyton mentagrophytes, Tinea Pedis caused by Trichophyton rubrum, Vaginal Candidiasis, Vulvovaginal Candidiasis, Cutaneous candidiasis, Recalcitrant Dermatophytosis, Tinea versicolor caused by Malassezia infection

How Protar K works

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

Ketoconazole interacts with 14-α-sterol demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This results in inhibition of ergosterol synthesis and increased fungal cellular permeability due to reduced amounts of ergosterol present in the fungal cell membrane. This metabolic inhibition also results in accumulation of 14α-methyl-3,6-diol, a toxic metabolite. The increase in membrane fluidity is also thought to produce impairment of membrane-bound enzyme systems as components become less closely packed.

Dosage

Protar K dosage

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.

Oral-

Fungal infections:

• Adult: 200 mg once daily; may increase to 400 mg once daily if clinical response is insufficient. Continue treatment until symptoms have cleared and cultures have become negative.
• Child: ≥2 yr 3.3-6.6 mg/kg once daily. Treatment duration: 1-2 wk for candidiasis; at least 4 wk in recalcitrant dermatophyte infections and up to 6 mth for other systemic mycoses.
• Elderly: No dosage adjustment needed.

Topical (Adult)-

Pityriasis versicolor, Skin fungal infections:

• As 2% cream: Apply 1-2 times daily to cover affected and surrounding area until at least a few days after disappearance of symptoms.
• As 2% shampoo: Apply on scalp once daily for up to 5 days. For prophylaxis: As 2% shampoo, use once daily for a max of 3 days before exposure to sunlight.

Seborrhoeic dermatitis:

• As 2% foam: Apply to the affected area bid for 4 wk.
• As 1 or 2% shampoo: Apply on the scalp twice wkly for 2-4 wk. For prophylaxis: As 2% shampoo, use once every 1-2 wk.

Duration of Treatment

• Pityriasis versicolor: 1 to 6 weeks
• Dermatomycoses: 2 to 8 weeks
• Onychomycoses: 1 to 12 months
• Mycoses of hair and scalp: 1 to 2 months
• Chronic mucocutaneous candidiasis : 1 to 12 months
• Oral mycoses: 5 to 10 days
• Systemic candidiasis: 1 to 2 months
• Paracoccidioidomycosis,histoplasmosis
• and other systemic mycosis: 1 month to 2 years

Side Effects

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.

Ketoconazole is very well tolerated. Nausea and itching may occasionally occur. In some patients, an idosyncratic liver reaction may occur (incidence 1 : 10,000).

Toxicity

LD50: Not available.

Symptoms of overdose include acute liver injury, which may include both hepatocellular and cholestatic injury, accompanied by anorexia, fatigue, nausea, and jaundice. In case of overdose, gastric lavage with activated charcoal may be used if within one hour of ketoconazole ingestion otherwise provide supportive care. If the patient shows signs of adrenal insufficiency, administer 100 mg hydrocortisone once together with saline and glucose infusion and monitor the patient closely. Blood pressure and fluid and electrolyte balance should be monitored over the next few days.

Precaution

Predisposition to adrenocortical insufficiency. Admin with acidic drink in patients with achlorhydria. Pregnancy and lactation.

Interaction

Reduced absorption with antimuscarinics, antacids, H2-blockers, PPIs and sucralfate. Reduced plasma concentrations with rifampicin, isoniazid, efavirenz, nevirapine, phenytoin. May also reduce concentrations of isoniazid and rifampicin. May reduce efficacy of oral contraceptives. May increase serum levels of CYP3A4 substrates e.g. digoxin, oral anticoagulants, sildenafil, tacrolimus.

Volume of Distribution

Intended for local use only, no systemic absorption.

Ketoconazole has an estimated volume of distribution of 25.41 L or 0.36 L/kg. It distributes widely among the tissues, reaching effective concentrations in the skin, tendons, tears, and saliva. Distribution to vaginal tissue produces concentrations 2.4 times lower than plasma. Penetration into the CNS, bone, and seminal fluid are minimal. Ketoconazole has been found to enter the breast milk and cross the placenta in animal studies.

Elimination Route

Intended for local use only, no systemic absorption.

Ketoconazole requires an acidic environment to become soluble in water. At pH values above 3 it becomes increasingly insoluble with about 10% entering solution in 1 h. At pH less than 3 dissolution is 85% complete in 5 min and entirely complete within 30 min. A single 200 mg oral dose produces a Cmax of 2.5-3 mcg/mL with a Tmax of 1-4 h. Administering ketoconazole with food consistently increases Cmax and delays Tmax but literature is contradictory regarding the effect on AUC, which may experience a small decrease. A bioavailablity of 76% has been reported for ketoconazole.

Half Life

Intended for local use only, no systemic absorption.

Ketoconazole experiences biphasic elimination with the first phase having a half-life of 2 hours and a terminal half life of 8 hours.

Clearance

Intended for local use only, no systemic absorption.

Ketoconazole has an estimated clearance of 8.66 L/h.

Elimination Route

Intended for local use only, no systemic absorption.

Only 2-4% of the ketoconazole dose is eliminated unchanged in the urine. Over 95% is eliminated through hepatic metabolism.

Pregnancy & Breastfeeding use

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.

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.

Contraindication

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.

Hypersensitivity; preexisting liver disease. Concurrent use with CYP3A4 substrates e.g. HMG-CoA reductase inhibitors (e.g. lovastatin, simvastatin), midazolam, triazolam, cisapride, dofetilide, eplerenone, nisoldipine, pimozide, quinidine, terfenadine, astemizole, ergot alkaloids (e.g. ergotamine, dihydroergotamine).

Special Warning

Renal Impairment: Oral: No dosage adjustment needed.

Hepatic Impairment: Oral: Contraindicated.

Acute Overdose

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.

Storage Condition

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

Store between 15-25° C. Protect from moisture and light.

Innovators Monograph

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