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Pentoxyverine API Manufacturers & Suppliers

General Description:

Pentoxyverine, identified by CAS number 77-23-6, is a notable compound with significant therapeutic applications. Pentoxyverine, also referred to as carbetapentane, is a non-opioid central acting antitussive with antimuscarinic, anticonvulsant , and local anesthetic properties. It is an active ingredient in over-the-counter cough suppressants in combination with guaifenesin and H1-receptor antagonists . Pentoxyverine acts on sigma-1 receptors, as well as kappa and mu-opioid receptors. The FDA withdrew the use of all oral gel drug products containing pentoxyverine citrate. Other forms of pentoxyverine citrate continue to be marketed.

Indications:

This drug is primarily indicated for: Indicated as a cough suppressant to relieve cough caused by the common cold, flu, bronchitis, and sinusitis . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Pentoxyverine undergoes metabolic processing primarily in: No pharmacokinetic data available. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Pentoxyverine are crucial for its therapeutic efficacy: In humans, maximum plasma concentrations are achieved 1.2 hours after oral dosing . The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Pentoxyverine is an important consideration for its dosing schedule: The half-life is 2.3 hours following oral dosing . This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Pentoxyverine exhibits a strong affinity for binding with plasma proteins: No pharmacokinetic data available. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Pentoxyverine from the body primarily occurs through: No pharmacokinetic data available. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Pentoxyverine is distributed throughout the body with a volume of distribution of: No pharmacokinetic data available. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Pentoxyverine is a critical factor in determining its safe and effective dosage: No pharmacokinetic data available. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Pentoxyverine exerts its therapeutic effects through: Pentoxyverine induces an antitussive action. In animal studies, intraperitoneal administration of pentoxyverine inhibited citric-acid-induced cough in guinea-pigs _in vivo_ . Some mice and rat studies suggest that pentoxyverine may also exert anticonvulsant activities without inducing a protective effect from NMDA-induced lethality . Protective effects against maximal electroshock-induced seizures in a dose-related fashion was also observed following either intraperitoneal or oral administration . In hERG-transfected cells, pentoxyverine inhibited the outward current of the hERG ion channel with half-maximal inhibition concentrations (IC50) of 3.0 µM . In rats receiving intrathecal administration, pentoxyverine exhibited dose-dependent spinal blockade with a more sensory-selective action over motor blockade . It induced a spinal blockade with a more sensory/nociceptive-selective action over motor blockade compared to lidocaine . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Pentoxyverine functions by: While the mechanism of antitussive action of pentoxyverine is not fully understood, it is thought to be mediated via sigma-1 receptors expressed in the central nervous system . Pentoxyverine acts as an agonist at sigma receptors with the Ki of 75±28 nM, as demonstrated in a competitive binding assay . The function of sigma receptors on cough suppressant activities is unclear, however these receptors are highly expressed in the nucleus tractus solitarius (NTS) of the brainstem where the afferent fibres first synapse . NTS is located very close to the cough centre in the brainstem thus may function as a ‘gate' for the cough reflex and allow sigma-1 receptor agonists to modulate afferent activity prior to reaching the cough center . It is suggested that highly lipophilic sigma-1 agonists may penetrate the CNS following systemic administration. When administered as aerosols, sigma-1 receptor agonists may temporarily act in the periphery to modulate cough by acting activate sigma receptors expressed in the lungs . However there is limited evidence of peripheral localization of the sigma agonists following aerosol administration and the ruling out of systemic exposure . The local anesthesia action of pentoxyverine may occur through inhibition of voltage-gated Na(+) currents . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Pentoxyverine belongs to the class of organic compounds known as benzene and substituted derivatives. These are aromatic compounds containing one monocyclic ring system consisting of benzene, classified under the direct parent group Benzene and substituted derivatives. 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 None subclass.

Categories:

Pentoxyverine is categorized under the following therapeutic classes: Antitussive Agents, Central Nervous System Agents, Cough and Cold Preparations, Cycloparaffins, Respiratory System Agents. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Pentoxyverine include:

• Water Solubility: 1 g/10 ml
• Melting Point: 90-95