Castelanis
Castelanis Uses, Dosage, Side Effects, Food Interaction and all others data.
Boric acid, also known as hydrogen borate, is a weak monobasic Lewis acid of boron with the chemical formula H3BO3. Boric acid is typically utilized in industrial processing and manufacturing, but is also used as an additive in pharmaceutical products, cosmetics, lotions, soaps, mouthwash, toothpaste, astringents, and eyewashes . It is known to exhibit some antibacterial activity against infections such as bacterial vaginosis and candidiasis .
Boric acid exhibits minimal bacteriostatic and antifungal activities . Boric acid is likely to mediate antifungal actions at high concentrations over prolonged exposures .
Phenol is an antiseptic and disinfectant. It is active against a wide range of micro-organisms including some fungi and viruses, but is only slowly effective against spores. Phenol has been used to disinfect skin and to relieve itching. Phenol is also used as an oral analgesic or anesthetic in products such as Chloraseptic to treat pharyngitis. Additionally, phenol and its related compounds are used in surgical ingrown toenail treatment, a process termed phenolization. Research indicates that parental exposure to phenol and its related compounds are positively associated with spontaneous abortion. During the second world war, phenol injections were used as a means of execution by the Nazis. Phenol is a toxic compound whose vapours are corrosive to the skin, eyes, and respiratory tract.
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 .
| Trade Name | Castelanis |
| Generic | Basic Fuchsine + Phenol + Boric Acid + Resorcinol + Acetone + Phenye Mercuric Nitrate + Alcohol |
| Weight | 1%w/v |
| Type | Paint |
| Therapeutic Class | |
| Manufacturer | Pasteur Laboratories Pvt Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
No FDA- or EMA-approved therapeutic indications on its own.
Phenol is an antiseptic and disinfectant used in a variety of settings.
Phenol is primarily indicated for minor sore throat pain, sore mouth, minor mouth irritation, and pain associated with canker sores. Additionally, phenol is indicated in the treatment of focal spasticity.
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 .
Castelanis is also used to associated treatment for these conditions: Acne, Asthenopia, Ocular Irritation, Skin Mycoses, Eye discomfort, Skin disinfection, Irrigation of the ocular surface therapyDermatitis, Dermatitis, Eczematous, Irritation lips, Pruritis of the skin, Psoriasis, Ringworm, Sore Throat, Throat irritation, Moderate, stable PsoriasisAcne Vulgaris
How Castelanis works
Information regarding the mechanism of action of boric acid in mediating its antibacterial or antifungal actions is limited. Boric acid inhibits biofilm formation and hyphal transformation of Candida albicans, which are critical virulence factors . In addition, arrest of fungal growth was observed with the treatment of boric acid .
Phenol is a potent proteolytic agent. Concentrations in the 5% to 7% range dissolve tissue on contact via proteolysis. In high concentrations when injected next to a nerve, phenol produces a chemical neurolysis which is nonselective across nerve fiber size and most prominent on its outer aspect. Local anesthetic effects occur within 5-10 minutes.
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 .
Toxicity
Acute oral LD50 is 2660 mg/kg in rat . Individuals are likely to be exposed to boric acid from industrial manufacturing or processing. Local tissue injury from boric acid exposure is likely due to caustic effects. Systemic effects from boric acid poisoning usually occur from multiple exposures over a period of days and involve gastrointestinal, dermal, CNS, and renal manifestations. Gastrointestinal toxicity include persistent nausea, vomiting, diarrhea, epigastric pain, hematemesis, and blue-green discoloration of the feces and vomit . Following the onset of GI symptoms, a characteristic intense generalized erythroderma follows . Management of mild to moderate toxicity should be supportive. In case of severe toxicity, dialysis may be required in addition to supportive treatment.
Mouse, Subcutaneous, LD50: 0.3-0.35 g/kg. (Duplay and Cazin, 1891; Tollens, 1905). Rat, Subcutaneous, LD50: 0.45. (Deichmann and Witherup, 1944). Rat, Oral, LD50: 0.53. (Deichmann and Witherup, 1944). Rat, Oral, LD50: 0.65. (Flickinger, 1976). Rat, Cutaneous, LD50: 0.67. (Conning and Hayes, 1970).
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 .
Volume of Distribution
Volume of distribution ranges from 0.17 to 0.5 L/kg in humans, where large amounts of boric acid are localized in brain, liver, and kidney .
At I5 min after exposure, the liver contained the highest level of phenol, consisting mainly of free phenol. After 82 minutes post administration, phenol is uniformly distributed in the liver, blood, kidneys, lungs, along with the heart, testes, thymus and the spleen. With the passage of time, the proportion of free to conjugated phenol changed. By 360 minutes most phenol appears in conjugated forms.
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 .
Elimination Route
Boric acid is well absorbed from the gastrointestinal tract, open wounds, and serous cavities but displays limited absorption in intact skin . Following intraperitoneal injection in mice, the peak concentration was reached in about 1.0-1.5 hr in the brain whereas the value was 0.5 hr in other tissues .
Phenol is rapidly absorbed through the skin and into the lungs.
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
According to human cases of poisoning, the elimination half-life of boric acid ranges from 13 to 24 hours .
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
A case report of acute boric acid poisoning following oral ingestion of 21 g of boric acid presents the total body clearance of 0.99 L/h before hemodialysis .
In rabbits, 72% is excreted in the urine, 1% in the feces, 4% in the carcass following sacrifice, and trace amounts were exhaled.
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
Regardless the route of administration, boric acid predominantly undergoes rapid renal excretion of >90% of total administered dose as unchanged form. Small amounts are also excreted into sweat, saliva, and feces. Following administration as ointment, urinary excretion of boric acid accounted for only 1% of the administered dose .
The kidney is the primary route of elimination of phenol.
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 .
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