Chloroxylenol

Brand names

Chloroxylenol is marketed under several brand names, including Dettol, Haffkinol, Doctor Woodworth’s Antiseptic Disinfectant Solution, and Pinotol Disinfectant. It is also a common ingredient in numerous products—such as ear drops and other antiseptic formulations—sold under a variety of brand names.

Common brand names include:

• Dettol: A widely recognized antiseptic disinfectant formulated with chloroxylenol, alcohol, and terpineol.

• Haffkinol: An antiseptic product that incorporates chloroxylenol as an active ingredient.

• Doctor Woodworth’s Antiseptic Disinfectant Solution: An antiseptic formulation containing chloroxylenol.

• Pinotol Disinfectant: A disinfectant brand that uses chloroxylenol as its main component.

MECHANISM OF ACTION

As a phenolic antiseptic, chloroxylenol is thought to act by allowing its hydroxyl (-OH) groups to bind to specific proteins on bacterial cell membranes, disrupting their structure and causing the cell contents to leak out. This disruption enables chloroxylenol to penetrate the cell further, where it interacts with additional proteins and enzymes, impairing essential cellular functions. At higher concentrations, chloroxylenol causes the coagulation of proteins and nucleic acids within the bacterial cell, resulting in the rapid death of the microorganism.

PHARMACOKINETICS

Absorption

No chloroxylenol was detected in the blood after topical application of 2 g of p-chloroxylenol in an ethanol/olive oil mixture to human subjects. Following a 5 g dose, only trace amounts were observed. When 8 g was administered, blood levels reached 1 mg% (1 mg/dL) after 3 hours and 4 mg% (4 mg/dL) after 24 hours. With a 20 g dose, concentrations of 4 mg% (4 mg/dL) were detected after 30 minutes, decreasing to 1 mg% (1 mg/dL) after 72 hours.

Distribution

The sole available data on the volume of distribution for chloroxylenol indicate a mean steady-state volume of distribution (Vss) of 22.45 L, determined following a single intravenous dose of 200 mg administered to healthy mongrel dogs.

Metabolism

Animal studies show that chloroxylenol is rapidly absorbed through the skin, reaching peak levels within 1–2 hours, and is almost completely eliminated by the kidneys within 24 hours. Its main urinary metabolites are glucuronides and sulfates, and its pharmacokinetic behavior is similar to that of triclosan, which is also quickly excreted as a glucuronide metabolite.

Excretion

The primary route of excretion is believed to be through urine, with smaller amounts excreted in bile and trace levels detected in exhaled air.

PHARMACODYNAMICS

Chloroxylenol, a substituted phenol, has long been used as an active ingredient in antiseptic and disinfectant products for external application. It is effective at low concentrations, exhibiting bactericidal activity against a broad spectrum of Gram-positive and Gram-negative bacteria.

ADMINISTRATION

Chloroxylenol is intended for topical, external use only and should be diluted before application, avoiding contact with the eyes, nose, or mouth. It is commonly found in products such as antibacterial soaps, disinfectants, and antiseptics. For ear infections, a specialized otic formulation is administered by placing drops directly into the ear. Always follow the specific instructions provided, as the method of use depends on the product and its intended purpose.

DOSAGE AND STRENGTH

Chloroxylenol is available in various products as an active ingredient with strengths typically ranging from 0.3% to 5%. The specific dosage and strength depend on its intended use (e.g., general antiseptic, surgical scrub, or otic solution) and whether the product is used undiluted or diluted before application.

DRUG INTERACTIONS

Currently, chloroxylenol is not known to have significant systemic drug interactions, largely because it is used topically and minimally absorbed into the bloodstream. However, a few considerations are important:

1. Topical Medications: Using multiple topical antiseptics or medicated products on the same area may reduce effectiveness or cause local irritation.

2. Otic (Ear) Formulations: When used in the ear, chloroxylenol should not be combined with other otic medications unless advised by a healthcare professional, as it may alter efficacy or increase irritation.

3. Eye, Nasal, or Oral Products: Accidental contact with mucous membranes should be avoided, as interactions or irritation could occur with other medications used in these areas.

Because systemic absorption is minimal, interactions with oral or systemic drugs are unlikely. The main concern is local compatibility with other topical products.

FOOD INTERACTIONS

No significant food interactions have been reported for topical chloroxylenol products. However, ingestion of chloroxylenol can lead to severe gastrointestinal injury and other toxic effects, and may interact with certain chemicals or medications if taken internally or in large amounts.

CONTRAINDICATIONS

Chloroxylenol is contraindicated in individuals with known hypersensitivity to chloroxylenol or any components of the product. It should also be avoided in the following situations:

• Eczematous skin: Do not apply to areas affected by eczema.

• Severely damaged skin or deep wounds: Not suitable for use on extensively damaged skin or deep puncture wounds.

• Sensitive areas: Avoid contact with the eyes, middle ear, brain meninges, or mucous membranes of the mouth and nose.

• Internal use: Intended for external use only. Ingestion can cause severe systemic toxicity, gastrointestinal corrosion, and in extreme cases, death.

• Perforated eardrum: Ear drops containing chloroxylenol should not be used if the eardrum is perforated, as this may lead to complications in the middle ear.

SIDE EFFECTS

Common/Mild Side Effects

Side effects from normal, topical use may include: 

• Skin irritation (redness, itching, stinging, burning, dryness)

• Contact dermatitis (a type of eczema caused by direct contact with an allergen or irritant)

• Skin discoloration

• Hypersensitivity (allergic reactions, which can be rare but more severe)

OVER DOSE

Chloroxylenol overdose is uncommon due to its primary use as a topical agent, but accidental ingestion or excessive topical application can lead to significant toxicity. Swallowing chloroxylenol may cause gastrointestinal irritation, including nausea, vomiting, abdominal pain, and diarrhea, and in severe cases can result in systemic effects such as central nervous system depression, low blood pressure, metabolic disturbances, and even death. Excessive use on the skin, especially on broken or sensitive areas, can cause local irritation, redness, or chemical burns. There is no specific antidote for chloroxylenol overdose, so treatment is mainly supportive and symptomatic, including gastrointestinal decontamination if ingestion is recent, monitoring of vital signs, and appropriate medical care.

TOXICITY

Chloroxylenol is generally regarded as having low systemic toxicity in humans when used properly in diluted topical applications. However, it is considered harmful if ingested and can cause severe irritation to the eyes and skin. Additionally, it is highly toxic to aquatic organisms and poses a particular danger to cats.