Gai less

Gai less Uses, Dosage, Side Effects, Food Interaction and all others data.

Gai less, 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 . Gai less acts on sigma-1 receptors, as well as kappa and mu-opioid receptors.

Gai less 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 .

Gai less
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Dosage
Side Effect
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Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
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Trade Name	Gai less
Generic	Pentoxyverine
Pentoxyverine Other Names	Carbetapentane, Pentoxyverine
Type
Formula	C₂₀H₃₁NO₃
Weight	Average: 333.472 Monoisotopic: 333.230393862
Protein binding	No pharmacokinetic data available.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	Japan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Gai less is a medication used to suppress a cough in the common cold, flu, bronchitis, and sinusitis.

Indicated as a cough suppressant to relieve cough caused by the common cold, flu, bronchitis, and sinusitis .

Gai less is also used to associated treatment for these conditions: Bronchial irritation, Cough, Throat irritation

How Gai less works

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 . Gai less 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 .