Pharmacological Effects and Toxicogenetic Impacts of Omeprazole: Genomic Instability and Cancer

Table 4

Gastroprotective effects of OME and mechanisms of action that may lead to protection and/or risk of genomic instability.

Dose/concentration	Study	Test system	Mechanisms of action	Prevention/risk of DNA damage	References
5-40 mg/kg	Clinical	Human ()	H2 receptor antagonists and PPIs	Oxidative stress	[57]
20 and 40 mg/kg	Clinical	—	pH control	Not identified	[58]
20, 40, and 100 mg/kg	Clinical	Human ()	Inhibition of CYP2C19, pharmacokinetics, gastroprotection of microdoses	Oxidative stress	[42, 43]
10 mg/14 days	Clinical	Human ()	Gastroprotection	Not identified	[62]
20 mg/kg	Clinical	Human ()	Histamine blockage	Not identified	[59]
—	Clinical	Human ()	Mechanisms involved in the gastric diseases	Oxidative stress	[63]
20 mg/kg	Clinical	Human ()	Pharmacokinetics-antiulceratives	Not identified	[64]
20 mg	Clinical	Human ()	Better action in patients with CYP 2 C1Q PM phenotype	Not identified	[65]
20 mg+amoxicillin 750 mg	Clinical	Human ()	Antacids, dose-dependent, CYP2C19 polymorphisms	Infection, oxidative stress	[66]
0.7, 1.4, and 4 mg/kg	In vivo	Horses	Pharmacokinetic and pharmacodynamic mechanisms	Not identified	[67]
15, 30, and 60 mg/kg	In vivo	Rats	Reduced necrotic damage, increased mucosal and gastric acid secretion reduction	Not identified	[52]
200 g/ml	In vivo	Rats	Increased prostaglandins synthesis and sulfhydryl compounds	Oxidative stress	[60]
40 mg/kg	In vivo	Rats	Inhibition of caspase 1, AC-YVAD-CMK, silencing of inflammasome NLRP3	Inhibition of apoptosis	[61]
40 mg/kg	In vivo	C57BL1 mice ()	Upregulation of BAX and caspase 3 → increased cell necrosis	Induction of apoptosis and necrosis	[61]
20 mg/kg	In vivo	Rats	Gastric protection, inhibition of H^+/K^+-ATPase system	Not identified	[68]
15 mg/kg	In vivo	Rats	Decreases blood flow, increased glycoproteins, prostaglandins, necrosis factor (TNF-α)	Not identified	[69]
1-100 μM	In vitro	Human hepatocyte cell line	Activation of AhR and induction of CYP1A	Catalytic activities	[41]

PPIs: proton pump inhibitors; TNF-α: tumor necrosis factor-alpha.