Table 3.

Relevant properties of prescription opioids and the overall opioid use prevalence per 1000 patients (‰) between 2009 and 2017

Prescription opioidsa	Physicochemical propertiesb			Pharmacokinetic propertiesc			Pharmacodynamic propertiesd			Prevalence (‰)
	logP	PSA	MW	MDR1	CYP2D6	CYP3A4	DOR	KOR	NMDAR
Agonist
Morphine	1.0	52.9	285.3	+	−	+	+	+	−	342.1
Fentanyl	4.1	23.6	336.5	+	−	+	+	+	−	297.5
Oxycodone	1.0	59.0	315.4	−	+	+	+	+	−	263.3
Hydromorphone	1.7	49.8	285.3	−	−	−	+	+	−	242.1
Hydrocodone	2.1	38.8	299.4	−	+	+	+	−	−	182.4
Meperidine	2.9	29.5	247.3	−	+	+	−	+	+	82.3
Tramadol	2.7	32.7	263.4	+	+	+	+	+	+	55.7
Codeine	1.2	41.9	299.4	−	+	+	+	+	−	43.9
Loperamide	4.4	43.8	477.0	+	+	+	+	+	−	23.1
Diphenoxylate	5.7	53.3	452.6	−	−	−	+	−	−	8.4
Methadone	4.1	20.3	309.4	+	+	+	+	−	+	7.8
Partial agonist
Nalbuphine	2.0	73.2	357.4	−	−	−	+	+	−	45.7
Butorphanol	3.7	43.7	327.5	−	−	−	+	+	−	29.5
Buprenorphine	4.5	62.2	467.6	+	+	+	+	+	−	3.2
Antagonist
Naloxone	1.5	70.0	327.4	−	−	+	+	+	−	157.8

CYP cytochrome P450, DOR delta opioid receptor, KOR kappa opioid receptor, logP lipophilicity, MDR1 multi-drug resistance protein 1, MW molecular weight, NMDAR N-methyl-d-aspartate receptor, PSA polar surface area

^aPrescription opioids are categorized by their action on the mu opioid receptor (MOR), ordered by their overall prevalence

^bRelevant physicochemical properties include logP, PSA, and MW

^cRelevant pharmacokinetic properties include whether the opioid interacts with [+ for interacting, − for not interacting] (1) efflux transporter, MDR1 and (2) metabolic enzymes, CYP2D6 and CYP3A4

^dRelevant pharmacodynamic properties include whether the opioid interacts with [+ for interacting, − for not interacting] (1) other opioid receptors, DOR and KOR and (2) non-opioid receptor in modulating opioid analgesia