Table 3.

Plasma/serum/tissue concentrations of amantadine in humans

Dose (mg)	Use	Body fluids, µM	Brain–CSF, µM	Brain homog, µM	References
200, p.o. > 8 days 300, p.o	Antiparkinsonian	5.0 (s) 13.5 (s)	4.0 9.5	159 281	Kornhuber et al. (1995)a
300, p.o. 3 weeks	Antidepressive	3.6–5.4 (p)			Rizzo et al. (1973)
200, i.v. 600, p.o. 1–24 weeks	Antiparkinsonian	3–5 (s) 8–11 (s)	1.3		Brenner et al. (1989)
200, p.o. 2 weeks	Antagonism of drug-induced Parkinsonism	2.1–4.5 (p)			Pacifici et al. (1976)
ca. 280–350, p.o	Pharmacokinetics	2.7–3.2 (b)			Bleidner et al. (1965)
274, p.o. ER	Pharmacokinetics extended release for 8 weeks in PD patients	ca. 7.5 (p)			Hauser et al. (2019)
129, p.o. ER 193, p.o. ER 259, p.o. ER 129, p.o. IR (BID)	Pharmacokinetics extended release vs. immediate release	1.74 (p) 2.45 (p) 3.35 (p) 2.15 (p)			deVries et al. (2019)
50–300, p.o.	78 Parkinsonian patients	5.3 (average p)			Nishikawa et al. (2009)
200, p.o. 300, p.o.	Side effects in comparison to rimantadine. Values after 9 doses	4.8 (p) 9.3 (p)			Hayden et al. (1983)
100, p.o.	Efficacy and PK in tardive dyskinesia	2.9 (p)			Greenblatt et al. (1977)
100, p.o. BID	Pharmacokinetics, interaction with oseltamivir, treatment for 5 days	3.39 (p)			Morrison et al. (2007)
350, p.o. (average)	Antidyskinetic activity	4–23 µM			Verhagen Metman et al. (1998)
50, p.o. 200, p.o. 300, p.o. 15 days steady state	Influenza A	0.59 (p) 1.62 (p) 3.06 (p)			Aoki and Sitar (1988) and Aoki et al. (1979)

s serum, p plasma, b blood, BID twice daily, CSF cerebrospinal fluid, IS interstitial fluid, homog. homogenates

^aThe values given for brain homogenates are not derived from the same group of patients as serum and CSF levels

^bCSF levels specified as 1.3 times higher than serum