UCSF home page | About UCSF | UCSF Medical Center

Skip to TransPortal content

Enlarge Text
Click to increase the text size. Restore Text
Click to restore original text size. Reduce Text
Click to decrease the text size.


Decrease the text size \| Restore text size \| Increase the text size

Procainamide

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter

Transporter	Synonyms	Km (μM)	Cell System	Reference
SLC47A2	MATE2K	4100	HEK293-MATE2K	Masuda, 2006
SLC47A1	MATE1	1230	HEK293-MATE1	Tanihara, 2007
SLC47A2	MATE2K	1580	HEK293-MATE2K	Tanihara, 2007

In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter

Transporter	Synonyms	Inhibitor	IC50 (μM)	Ki (μM)	Substrate used	Cell System	Reference
SLC47A1	MATE1	Procainamide	24		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE1	Astorga, 2012
SLC47A2	MATE2K	Procainamide	19.1		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE2K	Astorga, 2012
ABCC2	MRP2, cMOAT	Procainamide	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Procainamide	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Procainamide	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A5	OCTN2	Procainamide		1400	L-carnitine	MDCKII-hOCTN2	Diao, 2010
SLC22A3	OCT3	Procainamide		738	N-methylpyridinium	HRPE-OCT3	Wu, 2000
ABCB11	BSEP	Procainamide	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A2	OCT2	Procainamide		50	Tetraethylammonium	OCT2-expressing oocytes	Gorboulev, 1997
SLC22A4	OCTN1	Procainamide	<1000		Tetraethylammonium	HEK293-OCTN1	Yabuuchi, 1999
SLC22A4	OCTN1	Procainamide	1000		Tetraethylammonium	HRPE-rOCTN1	Wu, 2000
SLC22A1	OCT1	Procainamide	14.5		Tetraethylammonium	HeLa-OCT1	Bednarczyk, 2003
SLC47A1	MATE1	Procainamide		217	Tetraethylammonium	HEK293-MATE1	Tsuda, 2009
SLC47A2	MATE2K	Procainamide		178.1	Tetraethylammonium	HEK293-MATE2	Tsuda, 2009
SLC22A1	OCT1	Procainamide	51.3		YM155	HEK293-OCT1	Minematsu, 2010
SLC22A2	OCT2	Procainamide	91.9		YM155	HEK293-OCT2	Minematsu, 2010

Clinical Drug-Drug Interactions

DDI	Implicated Transporter*	Interacting Drug	Affected Drug	AUC	Cmax	CLR	CL/F	t1/2	Effect on PD	Reference	More Details
DDI	Implicated Transporter*	Interacting Drug	Affected Drug	Clinical PK Impact(fold change)					Effect on PD	Reference	More Details
1	OCTs/MATEs	Cimetidine	Procainamide	1.4	NS	0.6	ND	1.3	ND	Somogyi, 1983	DDI 1

PK = pharmacokinetic
The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PD = pharmacodynamic
ND = not determined
NS = not significant
N/A = information not available
Calculation of Fold Change: fold change in the presence of the interacting drug = (value with interacting drug)/(value without interacting drug)
fold change > 1: increase in pharmacokinetic value
fold change < 1: decrease in pharmacokinetic value