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Dichlorobenzyl alcohol | CAS No: 1777-82-8 | GMP-certified suppliers
A medication that provides symptomatic relief of acute and postoperative sore throat through antiseptic and local anesthetic effects, commonly used in over-the-counter throat preparations.
Therapeutic categories
AlcoholsAnti-Infective Agents, LocalBenzene DerivativesBenzyl CompoundsDrugs that are Mainly Renally ExcretedThroat Preparations
Generic name
Dichlorobenzyl alcohol
Molecule type
small molecule
CAS number
1777-82-8
DrugBank ID
DB13269
Approval status
Approved drug
ATC code
R02AA03
Primary indications
- Dichlorobenzyl alcohol in combination with [DB13908] is available in over-the-counter products used for symptomatic relief of acute sore throat and postoperative sore throat
Product Snapshot
- Dichlorobenzyl alcohol is available in multiple oral formulations including tablets, lozenges, mouthwash, and sprays
- It is primarily used for symptomatic relief of acute and postoperative sore throat
- The compound is approved for use in the Canadian market
Clinical Overview
Dichlorobenzyl alcohol (CAS Number 1777-82-8) is an organic compound classified within the dichlorobenzenes, characterized by a benzene ring substituted with two chlorine atoms. It functions primarily as a mild antiseptic agent and local anesthetic, commonly employed in the symptomatic management of acute and postoperative sore throat.
Clinically, dichlorobenzyl alcohol is utilized in over-the-counter formulations, frequently in combination with amylmetacresol, for relief from throat pain, soreness, and difficulty in swallowing. These products are approved and marketed under various regulatory jurisdictions, with Health Canada recognizing the compound as an active anatomical therapeutic ingredient, while the U.S. FDA typically categorizes it as an inactive ingredient in approved drug products.
Pharmacodynamically, in vitro studies demonstrate that the combination of dichlorobenzyl alcohol and amylmetacresol exhibits virucidal activity against multiple viruses implicated in the common cold, evidenced by reductions in viral load. Clinical trials indicate that lozenges containing dichlorobenzyl alcohol provide noticeable pain relief starting approximately five minutes post-administration, with effects persisting up to two hours and reaching steady-state relief around 45 minutes after use.
The mechanism of action encompasses antibacterial, antiviral, and local anesthetic effects. The local anesthetic property is attributed to a blockade of sodium channels, resulting in diminished nerve excitability. The antiseptic effect is hypothesized to involve denaturation and structural alteration of external microbial proteins, although the precise molecular interactions remain incompletely defined.
Regarding pharmacokinetics, dichlorobenzyl alcohol is primarily renally excreted. Safety profiles indicate it is generally well-tolerated when used topically within recommended doses, with minimal systemic toxicity. However, comprehensive toxicological data are limited.
In pharmaceutical sourcing, quality considerations include ensuring high purity and conforming to pharmaceutical-grade standards aligned with pharmacopeial specifications. Reliable suppliers must provide certificates of analysis and maintain rigorous quality control to support consistent efficacy and safety in finished products.
Clinically, dichlorobenzyl alcohol is utilized in over-the-counter formulations, frequently in combination with amylmetacresol, for relief from throat pain, soreness, and difficulty in swallowing. These products are approved and marketed under various regulatory jurisdictions, with Health Canada recognizing the compound as an active anatomical therapeutic ingredient, while the U.S. FDA typically categorizes it as an inactive ingredient in approved drug products.
Pharmacodynamically, in vitro studies demonstrate that the combination of dichlorobenzyl alcohol and amylmetacresol exhibits virucidal activity against multiple viruses implicated in the common cold, evidenced by reductions in viral load. Clinical trials indicate that lozenges containing dichlorobenzyl alcohol provide noticeable pain relief starting approximately five minutes post-administration, with effects persisting up to two hours and reaching steady-state relief around 45 minutes after use.
The mechanism of action encompasses antibacterial, antiviral, and local anesthetic effects. The local anesthetic property is attributed to a blockade of sodium channels, resulting in diminished nerve excitability. The antiseptic effect is hypothesized to involve denaturation and structural alteration of external microbial proteins, although the precise molecular interactions remain incompletely defined.
Regarding pharmacokinetics, dichlorobenzyl alcohol is primarily renally excreted. Safety profiles indicate it is generally well-tolerated when used topically within recommended doses, with minimal systemic toxicity. However, comprehensive toxicological data are limited.
In pharmaceutical sourcing, quality considerations include ensuring high purity and conforming to pharmaceutical-grade standards aligned with pharmacopeial specifications. Reliable suppliers must provide certificates of analysis and maintain rigorous quality control to support consistent efficacy and safety in finished products.
Identification & chemistry
| Generic name | Dichlorobenzyl alcohol |
|---|---|
| Molecule type | Small molecule |
| CAS | 1777-82-8 |
| UNII | 1NKX3648J9 |
| DrugBank ID | DB13269 |
Pharmacology
| Summary | Dichlorobenzyl alcohol exhibits antibacterial, antiviral, and local anesthetic effects primarily through modulation of sodium channel activity and disruption of protein structures. Its antiseptic action is associated with denaturation and tertiary structural changes of external proteins, while its local anesthetic effect involves sodium channel blockade. Therapeutically, it is used in combination formulations targeting viral and bacterial pathogens to provide symptomatic relief of acute and postoperative sore throat. |
|---|---|
| Mechanism of action | The use of dichlorobenzyl alcohol has been related to its antibacterial, antiviral and local anesthetic properties. The local anesthetic action of dichlorobenzyl alcohol is thought to be due to a reduced sodium channel blockade. The antiseptic mechanism of action of dichlorobenzyl alcohol is not fully understood but it is thought to be related to a denaturation of external proteins and rearrangement of the tertiary structure proteins. |
| Pharmacodynamics | In vitro studies with the combination of dichlorobenzyl alcohol and amylmetacresol have shown a virucidal against a number of viruses associated with the common cold which is observed by a reduction in the viral load. In clinical trials, administration of dichlorobenzyl alcohol lozenges has been shown to generate a reduced throat soreness and to provide pain relief and relief from difficulty in swallowing 5 minutes after administration. This effect can last for even 2 hours. The relief effect was shown to reach a steady-state after 45 minutes. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Sodium channel protein | Humans | antagonist |
ADME / PK
| Absorption | Dichlorobenzyl alcohol is released almost immediately from its formulation and reaches peak concentration after 3-4 minutes. The concentration in saliva after 120 minutes represents about 50% of the administered dose. |
|---|---|
| Half-life | This pharmacokinetic property has not been fully studied. |
| Protein binding | This pharmacokinetic property has not been fully studied. |
| Metabolism | Dichlorobenzyl alcohol is metabolized in the liver to form hippuric acid. |
| Route of elimination | In preclinical trials, dermal administration of dichlorobenzyl alcohol results in renal elimination of 90% of the administered dose. After metabolism, dichlorobenzyl alcohol is excreted in the urine. |
| Volume of distribution | This pharmacokinetic property has not been fully studied. |
| Clearance | This pharmacokinetic property has not been fully studied. |
Formulation & handling
- Dichlorobenzyl alcohol is a small molecule suitable for oral and transmucosal formulations such as lozenges, tablets, and sprays.
- The compound exhibits moderate lipophilicity (LogP 2.41) and limited water solubility, which should guide excipient selection to optimize bioavailability.
- No specific peptide or biologic-related stability concerns exist, but standard solid-state handling and storage conditions apply.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is currently marketed in Canada with patent protection recently expired, allowing for increased availability of generic formulations. The market is proceeding toward maturity with established prescribing patterns and competitive pricing. |
|---|
| Markets | Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for dichlorobenzyl alcohol in the Canadian market includes several originator companies producing branded antibacterial throat lozenges, with products such as Benylin and Cepacol available. The presence of multiple branded formulations indicates established market players with a focus on consumer health products. There is no specific information on patent status, suggesting that generic competition may either be established or imminent based on typical product lifecycle patterns. |
|---|
Safety
| Toxicity | Fertility and mutagenicity studies do not indicate any effect driven by dichlorobenzyl alcohol. Overdose studies indicate that in systemic overdose there might be a presence of a CNS transitory stimulation followed by CNS and cardiovascular. Chronic administration is not recommended as it might alter the normal microbial balance of the throat. depression In rats, the reported LD50 is of about 2.7 g/kg when administered orally. |
|---|
High Level Warnings:
- Acute systemic overdose may induce transient central nervous system stimulation followed by CNS depression and cardiovascular effects
- Chronic exposure could disrupt normal microbial flora of the throat
- Oral LD50 in rats is approximately 2
Dichlorobenzyl alcohol is a type of Anti-infective Agents
Anti-infective agents are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of various infectious diseases. These agents play a crucial role in combating bacterial, viral, fungal, and parasitic infections. The demand for effective anti-infective APIs has grown significantly due to the increasing prevalence of drug-resistant microorganisms.
Anti-infective APIs encompass a wide range of substances, including antibiotics, antivirals, antifungals, and antiparasitics. Antibiotics are particularly important in fighting bacterial infections and are further categorized into different classes based on their mode of action and target bacteria. Antivirals are designed to inhibit viral replication and are essential in the treatment of viral infections such as influenza and HIV. Antifungals combat fungal infections, while antiparasitics are used to eliminate parasites that cause diseases like malaria and helminthiasis.
The development and production of high-quality anti-infective APIs require stringent manufacturing processes and adherence to regulatory standards. Pharmaceutical companies invest heavily in research and development to discover new and more effective anti-infective agents. Additionally, ensuring the safety, efficacy, and stability of these APIs is of utmost importance.
The global market for anti-infective APIs is driven by factors such as the rising incidence of infectious diseases, the emergence of new and drug-resistant pathogens, and the growing demand for improved healthcare infrastructure. Continuous advancements in pharmaceutical technology and the development of innovative drug delivery systems further contribute to the expansion of this market.
In conclusion, anti-infective agents are a critical category of pharmaceutical APIs that play a pivotal role in treating infectious diseases. Their effectiveness in combating various types of infections makes them essential components in the arsenal of modern medicine.
