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Diethyltoluamide API Manufacturers & Suppliers

General Description:

Diethyltoluamide, identified by CAS number 134-62-3, is a notable compound with significant therapeutic applications. Diethyltoluamide (DEET) is the common active ingredient in many insect repellent products. It is widely used to repel biting pests such as mosquitoes and ticks. Every year, DEET formulations are used to protect populations from mosquito-borne illnesses like West Nile Virus, the Zika virus, malaria, and/or tick-borne illnesses like Lyme disease and Rocky Mountain spotted fever. And, despite concerns over excessive exposure to the chemical, appropriate usage of the chemical at the recommended dosages and routes of administration have generally proven to be safe - even when most DEET products are largely designed to be applied directly to human skin, where the exact mechanisms of actions in which DEET is capable of repelling insects and causing toxicity to humans is still not fully elucidated.

Indications:

This drug is primarily indicated for: Diethyltoluamide, or DEET, is an active ingredient that is predominantly indicated for as an insect repellant used to repel biting pests like mosquitoes and ticks . Products containing DEET currently are available to the public in a variety of liquids, lotions, sprays, and impregnated materials like towelettes or roll-ons . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Diethyltoluamide undergoes metabolic processing primarily in: Diethyltoluamide (DEET) is metabolized in humans by cytochrome P450 enzymes into the primary metabolites N,N-diethyl-m-hydroxymethylbenzamide (BALC) and Nethyl-m-toluamide (ET) . Although several P450 isoenzymes have elicited activity in DEET metabolism, it appears that the CYP2B6 and CYP2C19 enzymes are the principal P450s responsible for the transformation of DEET to BALC and ET, respectively . Most of the body load is metabolized by such hepatic P450 enzymes, with only 10%–14% recovered unchanged in the urine . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Diethyltoluamide are crucial for its therapeutic efficacy: Most diethyltoluamide (DEET) formulations employ the agent as a liquid to be applied onto human skin in an effort to repel mosquitoes from feeding on the skin. Topical application and absorption is consequently the most common route of absorption. When used appropriately, DEET formulations are generally not indicated for too many other routes of absorption or administration, like parenterally or orally. DEET is absorbed quickly through intact skin; 48% of the applied dose is totally absorbed within 6 hours . Topical absorption is the usual route of entry as DEET is normally applied to the skin as a mosquito repellent . DEET applied to the skin has also been shown to accumulate in the dermis . DEET is rapidly absorbed after oral ingestion . Additionally, animal experiments demonstrate that DEET can cross the placenta . DEET is efficiently absorbed across the skin and by the gut . Blood concentrations of about 3 mg/L have been reported several hours after dermal application in the prescribed fashion . Between 9% and 56% of dermally applied DEET is absorbed through the skin with peak blood levels being attained within 1 hour . Absorption through the skin varies according to the site exposed to the DEET . In animal model surfaces corresponding to the human palmar surface (an area that is typically heavily exposed during the application of liquid DEET), 68% of administered topical DEET was absorbed . As a consequence, small children are at increased risk of excessive absorption of DEET applied to the skin because of their relatively higher surface to volume ratio compared to adults . The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Diethyltoluamide is an important consideration for its dosing schedule: The elimination half-life of diethyltoluamide (DEET) is observed to be about 2.5 hours . This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Diethyltoluamide exhibits a strong affinity for binding with plasma proteins: Readily accessible data regarding the protein binding of diethyltoluamide (DEET) is not available. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Diethyltoluamide from the body primarily occurs through: Diethyltoluamide (DEET) is principally excreted via the kidneys, where the initial phase is initially rapid but not more than 50% of the absorbed dose is excreted during the first 5 days . In a study with a human volunteer weighing 65.8 kg and having been treated with 15 g of 95% DEET, urinary levels of DEET and a metabolite were measurable 4 hours after the initial exposure and persisted 48 hours later . Maximum urinary levels of DEET observed were 207 mg/L at 8 hours . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Diethyltoluamide is distributed throughout the body with a volume of distribution of: After dermal application, about 17% of the absorbed diethyltoluamide (DEET) dose enters the bloodstream . DEET accumulates in the skin, contributing to local irritation and possibly even bullous dermatitis . Accumulation within the body, however, has not been reported and experimentally there have been no cumulative effects of subtoxic doses of DEET; but various case reports of toxicity in man suggests that accumulation of the repellent could occur, and with deleterious effects . This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Diethyltoluamide is a critical factor in determining its safe and effective dosage: Readily accessible data regarding the clearance of diethyltoluamide (DEET) is not available. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Diethyltoluamide exerts its therapeutic effects through: When used appropriately, diethyltoluamide (DEET) containing products are designed to be applied directly to people's skin as a means to elicit a repelling action to keep insects from targeting human skin . At the amounts and doses recommended for use on human children and adults, noticeable absorption or systemic exposure is not expected . Owing to the proportional difference in size between humans and insects, however, the exposure of insects to the applied DEET (whether topically or via inhalation of DEET) is expected to be enough to interfere with the insects' sensory attraction to human skin . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Diethyltoluamide functions by: The exact mechanism(s) of action by which both (a) insects are repelled by diethyltoluamide (DEET), and (b) humans can be affected deleteriously by exposure to toxic amounts of DEET have not yet been formally elucidated . Research is ongoing regarding the exact mechanism of action by which DEET is capable of repelling insects. However, the most longstanding mechanism proposes that the DEET chemical blocks the olfactory receptors of insects for the volatile 1-octen-3-ol compound that is an element in human sweat and breath . As a consequence, this proposed mechanism suggests that the blockade of insects' senses for this 1-octen-3-ol blinds and prevents the triggering of their biting and/or feeding instinct on humans and other animals that produce that compound . Nevertheless, this theory has not yet been fully elucidated. Furthermore, recent studies have demonstrated that DEET binds to certain molecular targets like the Anopheles gambiae odorant binding protein 1 (AgamOBP1) with high shape complementarity and the antennae-specific odorant receptor CquiOR136 of the southern house mosquito, Culex quinquefasciatus . In southern house mosquitos with reduced CquiOR136 transcript levels, behavioral tests demonstrated that this phenotype showed demonstrably lower responses/repulsion to DEET . Again, however, such findings require continued research and do not formally elucidate the mechanism of action by which DEET can repel insects. And finally, the mechanism of toxicity in which DEET is capable of eliciting effects of neurotoxicity in humans who have been exposed to toxic levels of the agent is also poorly understood . A recent study proposes that DEET is capable of blocking Na+ and K+ channels in the rat animal model . This ion channel blocking activity of DEET in neurons may subsequently contribute to the kind of neuro-sensory adverse effects like numbness experienced after inadvertent application to the lips or mouth of humans . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Diethyltoluamide belongs to the class of organic compounds known as n,n-dialkyl-m-toluamides. These are aromatic that contain a m-toluamide, where the carboxamide group is N- substituted with two alkyl chains, classified under the direct parent group N,N-dialkyl-m-toluamides. This compound is a part of the Organic compounds, falling under the Benzenoids superclass, and categorized within the Benzene and substituted derivatives class, specifically within the Toluenes subclass.

Categories:

Diethyltoluamide is categorized under the following therapeutic classes: Acids, Carbocyclic, Agrochemicals, Amides, Antiparasitic Products, Insecticides and Repellents, Benzamides and benzamide derivatives, Benzene Derivatives, Benzoates, Compounds used in a research, industrial, or household setting, Ectoparasiticides, Incl. Scabicides, Insecticides and Repellents, Insect Repellents, Insecticides and Repellents, Pesticides, Protective Agents, Toxic Actions. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.