Acrivastine

Biological Activity

In peripheral histamine antagonism as measured by histamine-induced flares and wheals, acrivastine is equipotent to triprolidine and a 4 to 8 mg dose of acrivastine has been shown to be effective in allergic rhinitis. This means that there is considerable separation between the expected therapeutic dose and a dose at which central nervous system impairment might occur.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information

References

Quantitative determination of acrivastine and pseudoephedrine hydrochloride in pharmaceutical formulation by high performance liquid chromatography and derivative spectrophotometry.
Altuntas TG, et al. J Pharm Biomed Anal. 1998 May;17(1):103-9. PMID: 9608432.

Terfenadine alters action potentials in isolated canine Purkinje fibers more than acrivastine.
Lang DG, et al. J Cardiovasc Pharmacol. 1993 Sep;22(3):438-42. PMID: 7504135.