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. 2021 Jan 19;13(1):124. doi: 10.3390/pharmaceutics13010124

Table 2.

Characteristics of the drugs used in the study. The main enzymatic targets (substrates, inhibitors, and inducers) are specified.

Drug Name and Chemical Structure HAM ATC Class
(Code)
BDDCS Class ALOX5 AMPK BSEP COX CYP GLP-1 HMGCoAR MAO NMDA ABC PLA2G2A SLC UGT References
BCRP MRP Pgp PEPT; OCT; OAT, MATE, OATP
Alprazolam
Inline graphic
Y Benzodiazepine derivatives
(N05BA12)
I - - - - 3A4S↓
3A5S
3A7S
2C9S
2C19S
- - - - - - - - - - [217,218,219]
Atorvastatin
Inline graphic
Y HMG CoA reductase inhibitors
(C10AA05)
II - - S - 3A4S↑
3A5S
3A7S
2B6
2C8S↓
2C9
2C19
2D6
- - - S 1S
2S
4S
5S
S↓ - 21A3S
21A6S↓
21A8S
21A9S
1A1S
1A3S
[218,219,220,221,222]
Clopidogrel
Inline graphic
Y Platelet aggregation inhibitors excl. heparin
(B01AC04)
II - - - - 1A2S
3A4S
3A5S
2B6S↓
2C8
2C9S↓
2C19S
- - - - - S - 21A8S
22A122A2
- [218,219,223,224,225]
Diclofenac
Inline graphic
Y Anti-inflammatory agents, non-steroids
(S01BC03)
II - S 1
2
1A2S
3A4S↓
2B6S
2C8S
2C9S↓
2C18S
2C19S
2E1
- - - - S 1
4
21A6
21A8S
21A14
22A11
22A6
22A8
1A3s
1A9s
2B4s
2B7s
[218,219,226,227]
Memantine
Inline graphic
N Other anti-dementia drugs
(N06DX01)
III - - - - 2B6
2C19
- - - ANT - - - - 15A1
15A2
22A8
22A1
22A2S↓
22A4S
47A1S
- [218,222,228,229,230,231]
Metformin
Inline graphic
Y Biguanides
(A10BA02)
III - - - - - - S - - - 22A1S
22A2S↓
22A3S
47A1S
47A2S
- [218,222,232,233,234,235]
Piracetam
Inline graphic
N Other psychostimulants and nootropics
(N06BX03)
III - - - - - - - - - - - 0 - - - [236]
Propranolol
Inline graphic
Y β-blocking agents, non-selective
(C07AA05)
I - - - - 1A1
1A2S
3A4S
3A5S
3A7S
2C19S
2D6S↓
- - A - - - S - 22A2 - [218,237,238,239,240]
Sertraline
Inline graphic
N Selective serotonin reuptake inhibitors
(N06AB06)
I - - - - 1A2
3A4S
2B6S↓
2C9S↓
2C19S↓
2D6S↓
2E1S
- - AS
BS
- S - S↓ - 6A2
6A3↓S
6A4↓S
36A1
1A3S
1A6S
2B4S
2B7S
[217,218,219,241,242,243]
Tadalafil
Inline graphic
N Drugs used in erectile dysfunction
(G04BE08)
II - - - - 3A4S
3A5S
- - - - - - S - - - [218,219,244]

—target inhibition; —target induction; s—drug is substrate of the target; ANT—drug is a target antagonist; 0—No effect; ()—Not reported; ABC—ATP-binding cassette; ALOX5—Arachidonate 5-lipoxygenase; AMPK—AMP-activated protein kinase; BCRP—Breast cancer resistance protein; BSEP—Bile salt export pump (ABCB11); COX—Cyclooxygenase; CYP—Cytochrome P450; GLP-1—Glucagon-like peptide-1; HMGCoAR—3-hydroxy-3-methyl-glutaril-CoA reductase; MAO—Monoamine Oxidase; MATE—Multi-antimicrobial extrusion protein; MRP—Multidrug resistance-associated protein; NMDA—N-methyl-d-aspartate; OAT—Organic anion transporter; OATP—Organic-anion-transporting polypeptide; OCT—Organic cation transport; P-gP—Glycoprotein P; UGT—Uridine diphosphate-glucuronosyltransferase; PLA2G2A—Phospholipase A2 Group IIA; SLC—Solute Carriers (15A/PEPT; 22A1-3/OCT1-3; 22A4/OCTN1; 22A6,8,11/OAT1,3,4; 47A/MATE; 21A3/OATP1A2; 21A6,8/OATP1B1,3; 21A9/OATP2B1; 21A14/OATP1C1); PEPT—Peptide transporter. HAM—High-Alert Medications [44]; Y—yes; N—No; ATC—Anatomical Therapeutic Chemical [36]; BDDCS—Biopharmaceutics Drug Disposition Classification System [37,38,39,40,41,42,43].