Diphenhydramine (1-300 渭M, 30 s) can block NMDA-activated membrane currents. This property can be responsible for or add to its sedative, analgesic and memory related effects[2].
Diphenhydramine (0-10 mg/kg, i.v. and p.o.) has better oral bioavailability when used in combination with Dimenhydrinate sup>[3].
Diphenhydramine (20 mg/kg, i.p.) can improve the kidney injury induced by Cisplatin (CDDP) in mice, and does not affect the anti-tumor efficacy of Cisplatin[4].
Pharmacokinetic parameters for diphenhydramine after single oral or intravenous administration of diphenhydramine HCl (5 mg/kg) to six healthy dogs by using a noncompartmental model with first-order elimination[3]
| Route | Dose (mg/kg) | AUClast (ng路h/mL) | C0 (ng/Ml) | CL (Ml/h/kg) | T1/2 (h) | Kel (1/h) | MRT (h) | Vss_obs (mL/kg) | Cmax (ng/mL) | Tmax (h) | Vz (mL/kg) | F (%) |
| i.v. | 5 | 391.20 | 266.10 | 2833.04 | 1.89 | 0.45 | 2.47 | 6582.36 | / | / | / | / |
| p.o. | 5 | 153.80 | / | / | 4.98 | 0.59 | 6.97 | / | 35.80 | 1.30 | 180157.36 | 7.75 |
[1]. Jason P Berninger, et al. Effects of the antihistamine diphenhydramine on selected aquatic organisms. Environ Toxicol Chem. 2011 Sep;30(9):2065-72.
[2]. F枚hr KJ, et al. Open channel block of NMDA receptors by diphenhydramine. Neuropharmacology. 2015 Dec;99:459-70.
[3]. Ehling S, et al. Diphenhydramine pharmacokinetics after oral and intravenous administration of diphenhydramine and oral administration of dimenhydrinate to healthy dogs, and pharmacodynamic effect on histamine-induced wheal formation: a pilot study. Vet Dermatol. 2019 Apr;30(2):91-e24.
[4]. Hamano H, et al. Diphenhydramine may be a preventive medicine against cisplatin-induced kidney toxicity. Kidney Int. 2021 Apr;99(4):885-899.