Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: Topical products for joint and muscular pain, Capsaicin and similar agents, ATC code: M02AB01.
Although the precise mechanism of action of capsaicin is not fully understood, current evidence suggests that capsaicin renders skin insensitive to pain by depleting and preventing re-accumulation of substance P in peripheral sensory neurons.
Substance P is thought to be the principal chemo-mediator of pain impulses from the periphery to the Central Nervous System.

Pharmacokinetic Properties

5.2 Pharmacokinetic properties
Absorption after topical application is unknown. Average consumption of dietary spice from capsicum fruit has been estimated as 2.5 g/person/day in India and 5.0 g/person/day in Thailand. Capsaicin content in capsicum fruit is approximately 1 % therefore daily dietary intake of capsaicin may range from 0.5-1 mg/kg/day for a 50kg person. Application of 3 tubes (90 gram) of a 0.025% cream each week results in a 3.21 mg/day topical exposure. Application of3 tubes (90 gram) of a 0.075% cream each week results in a 9.6 mg/day topical exposure. Assuming 100% absorption in a 50 kg person, daily exposure would be 0.064 mg/kg for the 0.025% cream and 0.192 mg/kg for the 0.075% cream which is approximately one seventh to one eighth of the above mentioned dietary intake for the 0.025% cream and one third to one quarter of the above mentioned dietary intake for the 0.075% cream.