Page last updated: 2024-10-16

acetaldehyde and Flushing

acetaldehyde has been researched along with Flushing in 42 studies

Acetaldehyde: A colorless, flammable liquid used in the manufacture of acetic acid, perfumes, and flavors. It is also an intermediate in the metabolism of alcohol. It has a general narcotic action and also causes irritation of mucous membranes. Large doses may cause death from respiratory paralysis.
acetaldehyde : The aldehyde formed from acetic acid by reduction of the carboxy group. It is the most abundant carcinogen in tobacco smoke.
aldehyde : A compound RC(=O)H, in which a carbonyl group is bonded to one hydrogen atom and to one R group.
acetyl group : A group, formally derived from acetic acid by dehydroxylation, which is fundamental to the biochemistry of all forms of life. When bound to coenzyme A, it is central to the metabolism of carbohydrates and fats.

Flushing: A transient reddening of the face that may be due to fever, certain drugs, exertion, or stress.

Research Excerpts

ExcerptRelevanceReference
"A cutaneous test has been applied in examination of the flushing response to ethanol and acetaldehyde in 402 Chinese of Han ethnicity."7.68Cutaneous vasomotor sensitivity to ethanol and acetaldehyde: subtypes of alcohol-flushing response among Chinese. ( Dyck, LE; Fang, CY; Yu, PH, 1990)
" We hypothesized that the phenomenon represents acetaldehyde syndrome, not response to increased blood levels of ethanol as might be supposed."7.67Acetaldehyde syndrome after celiac plexus alcohol block. ( Fukunaga, T; Mizoi, Y; Mori, K; Noda, J; Umeda, S, 1986)
" Blood acetaldehyde and blood ethanol analyses were performed together with recordings of blood pressure, pulse rate, and flushing intensity during the hour after ethanol infusion."5.06Diphenhydramine and the calcium carbimide-ethanol reaction: a placebo-controlled clinical study. ( Johnsen, J; Mørland, J; Ripel, A; Stowell, A, 1986)
"The association between alcohol consumption and bladder cancer risk has been insufficiently investigated in East Asian populations, who frequently have the inactive enzyme for metabolizing acetaldehyde."3.85Alcohol consumption and bladder cancer risk with or without the flushing response: The Japan Public Health Center-based Prospective Study. ( Eto, M; Goto, A; Inoue, M; Iwasaki, M; Masaoka, H; Matsuo, K; Sawada, N; Shimazu, T; Tsugane, S; Yamaji, T, 2017)
"We investigated the effect of direct administration of acetaldehyde on behavioral measures of anxiety and on hormonal markers of stress in mice."3.78Anxiogenic and stress-inducing effects of peripherally administered acetaldehyde in mice: similarities with the disulfiram-ethanol reaction. ( Aragon, CM; Correa, M; Escrig, MA; Pardo, M, 2012)
"Peripheral accumulation of acetaldehyde, the first metabolite of ethanol, produces autonomic responses in humans called "flushing"."3.78Anxiogenic and stress-inducing effects of peripherally administered acetaldehyde in mice: similarities with the disulfiram-ethanol reaction. ( Aragon, CM; Correa, M; Escrig, MA; Pardo, M, 2012)
"The correlation among degrees of alcohol intoxication, facial flushing, blood alcohol concentration (BAC) and blood acetaldehyde level was studied in 117 male alcoholic patients who underwent various tests to assess alcohol influence."3.68Degrees of alcohol intoxication in 117 hospitalized cases. ( Adachi, J; Fukunaga, T; Imamichi, H; Mizoi, Y; Ogawa, Y; Ueno, Y, 1991)
"A cutaneous test has been applied in examination of the flushing response to ethanol and acetaldehyde in 402 Chinese of Han ethnicity."3.68Cutaneous vasomotor sensitivity to ethanol and acetaldehyde: subtypes of alcohol-flushing response among Chinese. ( Dyck, LE; Fang, CY; Yu, PH, 1990)
"An ethnic predisposition to ethanol-provoked flushing among diverse Mongoloid populations may be the consequence of a delayed oxidation and accumulation of acetaldehyde."3.67Cutaneous vascular sensitivity to lower aliphatic alcohols and aldehydes in Orientals. ( Fortner, G; Wilkin, JK, 1985)
" We hypothesized that the phenomenon represents acetaldehyde syndrome, not response to increased blood levels of ethanol as might be supposed."3.67Acetaldehyde syndrome after celiac plexus alcohol block. ( Fukunaga, T; Mizoi, Y; Mori, K; Noda, J; Umeda, S, 1986)
"Alcohol-sensitive Japanese subjects with facial flushing and an increase in heart rate during ethanol intoxication exhibited marked individual variation in accumulation of acetaldehyde."3.67Suppression of acetaldehyde accumulation by 4-methylpyrazole in alcohol-hypersensitive Japanese. ( Inoue, K; Kera, Y; Kiriyama, T; Komura, S, 1985)
"Fomepizole 15 mg/kg was given with improvement within 1."1.38Fomepizole for severe disulfiram-ethanol reactions. ( Monte, AA; Sande, M; Thompson, D, 2012)
"Acetaldehyde was ten times more potent than ethanol at inducing corticosterone release."1.38Anxiogenic and stress-inducing effects of peripherally administered acetaldehyde in mice: similarities with the disulfiram-ethanol reaction. ( Aragon, CM; Correa, M; Escrig, MA; Pardo, M, 2012)
"Facial flushing was recognized in 75% of the subjects."1.28Degrees of alcohol intoxication in 117 hospitalized cases. ( Adachi, J; Fukunaga, T; Imamichi, H; Mizoi, Y; Ogawa, Y; Ueno, Y, 1991)

Research

Studies (42)

TimeframeStudies, this research(%)All Research%
pre-199016 (38.10)18.7374
1990's12 (28.57)18.2507
2000's5 (11.90)29.6817
2010's8 (19.05)24.3611
2020's1 (2.38)2.80

Authors

AuthorsStudies
Matsuura, K1
Kushio, S1
Imai, H1
Kudo, H1
Wakuda, H1
Otani, N1
Kuranari, M1
Sekiguchi, A1
Ohyama, T1
Uemura, N1
Masaoka, H1
Matsuo, K1
Sawada, N1
Yamaji, T1
Goto, A1
Shimazu, T1
Iwasaki, M1
Inoue, M1
Eto, M1
Tsugane, S1
Himemiya-Hakucho, A1
Tanaka, T1
Liu, J1
Fujimiya, T1
Brooks, PJ1
Enoch, MA1
Goldman, D1
Li, TK1
Yokoyama, A2
Luo, HR1
Wu, GS1
Pakstis, AJ1
Tong, L1
Oota, H1
Kidd, KK1
Zhang, YP1
Omori, T1
Yokoyama, T1
Sande, M1
Thompson, D1
Monte, AA1
Haberl, B1
Pfab, R1
Berndt, S1
Greifenhagen, C1
Zilker, T1
Sanaei-Zadeh, H1
Escrig, MA1
Pardo, M1
Aragon, CM1
Correa, M1
Bae, KY1
Kim, SW1
Shin, HY1
Kim, JM1
Shin, IS1
Kim, SJ1
Kim, JK1
Yoon, JS1
Kim, JS1
Kim, YJ1
Kim, TY1
Song, JY1
Cho, YH1
Park, YC1
Chung, HW1
Nitzan, Z1
Dan, M1
Karamanakos, PN1
Pappas, P1
Marselos, M1
Johnston, C1
Wiles, PG2
Pyke, DA2
Groop, L1
Eriksson, CJ2
Huupponen, R1
Ylikahri, R1
Pelkonen, R1
Chao, HM1
Ward, RJ1
McPherson, AJ1
Chow, C1
Ealing, J1
Sherman, DI1
Yoshida, A1
Peters, TJ1
Guivernau, M1
Quintanilla, ME1
Tampier, L1
Lao, B1
Czyzyk, A1
Szutowski, M1
Szczepanik, Z1
Tsukamoto, S2
Kanegae, T1
Uchigasaki, S1
Kitazawa, M1
Fujioka, T1
Fujioka, S1
Imamura, Y1
Nagoya, T2
Shimamura, M2
Mieda, Y1
Whitfield, JB1
Martin, NG1
Ijiri, I2
Adachi, J2
Mizoi, Y4
Fukunaga, T4
Ogawa, Y1
Ueno, Y2
Imamichi, H1
Niemelä, O1
Israel, Y1
Yu, PH1
Fang, CY1
Dyck, LE1
Gallant, DM1
Hatake, K1
Taniguchi, T1
Ouchi, H1
Sakaki, N1
Hishida, S1
Fujiwara, S1
Nishimura, A1
Muto, T1
Saito, M1
Tainaka, H1
Wilkin, JK1
Fortner, G1
Chan, AW1
Ho, SB1
DeMaster, EG1
Shafer, RB1
Levine, AS1
Morley, JE1
Go, VL1
Allen, JI1
Jones, AW1
Neiman, J1
Hillbom, M1
Stowell, A1
Johnsen, J1
Ripel, A1
Mørland, J1
Noda, J1
Umeda, S1
Mori, K1
Jerntorp, P2
Ohlin, H2
Sundkvist, G1
Almér, LO2
Sabán, J1
Ordóñez, A1
Navascués, I1
Suárez Terry, R1
Serrano Ríos, M1
Suwaki, H1
Inoue, K1
Kera, Y1
Kiriyama, T1
Komura, S1

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Treatment of Asian Flushing Syndrome With Topical Alpha Agonists[NCT03497442]Early Phase 120 participants (Actual)Interventional2018-07-12Completed
A Phase IIa, Prospective, Randomized, Blinded, Intra-Subject Controlled, Single Dose, Dose Escalation Study of Antizol® for Mitigation of Acetaldehyde Related Toxicity in Human Subjects With Symptoms of Inborn Altered Ethanol Metabolism With Concomitant E[NCT00661141]Phase 232 participants (Actual)Interventional2008-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Pharmacokinetics (PK) of 4-MP: Maximum Plasma Concentration (Cmax)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionng/mL (Mean)
1.0 mg/kg Antizol Followed by Ethanol2386
Ethanol Followed by 1.0 mg/kg Antizol1358
3.0 mg/kg Antizol Followed by Ethanol5605
Ethanol Followed by 3.0 mg/kg Antizol4680
5.0 mg/kg Antizol Followed by Ethanol8623

PK of 4-MP: Apparent Clearance (CL/F)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

InterventionL/hr (Mean)
1.0 mg/kg Antizol Followed by Ethanol6.70
Ethanol Followed by 1.0 mg/kg Antizol8.23
3.0 mg/kg Antizol Followed by Ethanol3.15
Ethanol Followed by 3.0 mg/kg Antizol2.99
5.0 mg/kg Antizol Followed by Ethanol2.35

PK of 4-MP: Apparent Volume of Distribution During Terminal Phase (Vz/F)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

InterventionLiters (Mean)
1.0 mg/kg Antizol Followed by Ethanol26.3
Ethanol Followed by 1.0 mg/kg Antizol24.7
3.0 mg/kg Antizol Followed by Ethanol24.4
Ethanol Followed by 3.0 mg/kg Antizol24.9
5.0 mg/kg Antizol Followed by Ethanol24.7

PK of 4-MP: Area Under the Plasma Concentration-Time Curve (AUC), Calculated to the Last Measured Concentration (AUC[0-t])

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionng*hr/mL (Mean)
1.0 mg/kg Antizol Followed by Ethanol13804
Ethanol Followed by 1.0 mg/kg Antizol7409
3.0 mg/kg Antizol Followed by Ethanol44942
Ethanol Followed by 3.0 mg/kg Antizol34310
5.0 mg/kg Antizol Followed by Ethanol109298

PK of 4-MP: AUC, From Time 0 Extrapolated to Infinite Time (AUC[0-∞])

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionng*hr/mL (Mean)
1.0 mg/kg Antizol Followed by Ethanol11035
Ethanol Followed by 1.0 mg/kg Antizol7627
3.0 mg/kg Antizol Followed by Ethanol55452
Ethanol Followed by 3.0 mg/kg Antizol57028
5.0 mg/kg Antizol Followed by Ethanol136871

PK of 4-MP: DN AUC(0-∞)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Intervention(ng*hr/mL)/mg (Mean)
1.0 mg/kg Antizol Followed by Ethanol149
Ethanol Followed by 1.0 mg/kg Antizol122
3.0 mg/kg Antizol Followed by Ethanol317
Ethanol Followed by 3.0 mg/kg Antizol334
5.0 mg/kg Antizol Followed by Ethanol460

PK of 4-MP: DN AUC(0-t)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Intervention(ng*hr/mL)/mg (Mean)
1.0 mg/kg Antizol Followed by Ethanol223
Ethanol Followed by 1.0 mg/kg Antizol103
3.0 mg/kg Antizol Followed by Ethanol231
Ethanol Followed by 3.0 mg/kg Antizol204
5.0 mg/kg Antizol Followed by Ethanol378

PK of 4-MP: Dose-Normalized (DN) Cmax

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Intervention(ng/mL)/mg (Mean)
1.0 mg/kg Antizol Followed by Ethanol38.3
Ethanol Followed by 1.0 mg/kg Antizol18.9
3.0 mg/kg Antizol Followed by Ethanol27.6
Ethanol Followed by 3.0 mg/kg Antizol28.0
5.0 mg/kg Antizol Followed by Ethanol30.2

PK of 4-MP: Half-Life (T1/2)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionhours (Mean)
1.0 mg/kg Antizol Followed by Ethanol2.72
Ethanol Followed by 1.0 mg/kg Antizol3.11
3.0 mg/kg Antizol Followed by Ethanol5.37
Ethanol Followed by 3.0 mg/kg Antizol5.76
5.0 mg/kg Antizol Followed by Ethanol9.26

PK of 4-MP: Percentage of AUC0-∞ Obtained by Extrapolation (AUC%Extrap)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionpercentage (Mean)
1.0 mg/kg Antizol Followed by Ethanol16.8
Ethanol Followed by 1.0 mg/kg Antizol13.0
3.0 mg/kg Antizol Followed by Ethanol3.31
Ethanol Followed by 3.0 mg/kg Antizol4.37
5.0 mg/kg Antizol Followed by Ethanol13.2

PK of 4-MP: Time to Cmax (Tmax)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionhours (Median)
1.0 mg/kg Antizol Followed by Ethanol1.00
Ethanol Followed by 1.0 mg/kg Antizol2.50
3.0 mg/kg Antizol Followed by Ethanol0.667
Ethanol Followed by 3.0 mg/kg Antizol1.48
5.0 mg/kg Antizol Followed by Ethanol1.00

PK of Acetaldehyde: AUC(0-∞)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

InterventionµM*hr (Mean)
1.0 mg/kg Antizol Followed by Ethanol234
Ethanol Followed by 1.0 mg/kg Antizol154
3.0 mg/kg Antizol Followed by Ethanol297
Ethanol Followed by 3.0 mg/kg Antizol302
5.0 mg/kg Antizol Followed by Ethanol188
Placebo Followed by Ethanol205
Ethanol Followed by Placebo227

PK of Acetaldehyde: AUC(0-t)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

InterventionµM*hr (Mean)
1.0 mg/kg Antizol Followed by Ethanol178
Ethanol Followed by 1.0 mg/kg Antizol118
3.0 mg/kg Antizol Followed by Ethanol155
Ethanol Followed by 3.0 mg/kg Antizol167
5.0 mg/kg Antizol Followed by Ethanol128
Placebo Followed by Ethanol163
Ethanol Followed by Placebo139

PK of Acetaldehyde: AUC%Extrap

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionpercentage (Mean)
1.0 mg/kg Antizol Followed by Ethanol19.0
Ethanol Followed by 1.0 mg/kg Antizol18.8
3.0 mg/kg Antizol Followed by Ethanol13.1
Ethanol Followed by 3.0 mg/kg Antizol9.78
5.0 mg/kg Antizol Followed by Ethanol24.7
Placebo Followed by Ethanol13.7
Ethanol Followed by Placebo14.5

PK of Acetaldehyde: Cmax

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

InterventionµM (Mean)
1.0 mg/kg Antizol Followed by Ethanol59.6
Ethanol Followed by 1.0 mg/kg Antizol37.6
3.0 mg/kg Antizol Followed by Ethanol50.9
Ethanol Followed by 3.0 mg/kg Antizol55.9
5.0 mg/kg Antizol Followed by Ethanol40.0
Placebo Followed by Ethanol60.3
Ethanol Followed by Placebo42.7

PK of Acetaldehyde: DN AUC(0-∞)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

InterventionµM*hr/mg (Mean)
1.0 mg/kg Antizol Followed by Ethanol0.00682
Ethanol Followed by 1.0 mg/kg Antizol0.00432
3.0 mg/kg Antizol Followed by Ethanol0.00929
Ethanol Followed by 3.0 mg/kg Antizol0.0105
5.0 mg/kg Antizol Followed by Ethanol0.00626
Placebo Followed by Ethanol0.00616
Ethanol Followed by Placebo0.00752

PK of Acetaldehyde: DN AUC(0-t)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

InterventionµM*hr/mg (Mean)
1.0 mg/kg Antizol Followed by Ethanol0.00547
Ethanol Followed by 1.0 mg/kg Antizol0.00329
3.0 mg/kg Antizol Followed by Ethanol0.00470
Ethanol Followed by 3.0 mg/kg Antizol0.00597
5.0 mg/kg Antizol Followed by Ethanol0.00439
Placebo Followed by Ethanol0.00521
Ethanol Followed by Placebo0.00455

PK of Acetaldehyde: DN Cmax

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

InterventionµM/mg (Mean)
1.0 mg/kg Antizol Followed by Ethanol0.00181
Ethanol Followed by 1.0 mg/kg Antizol0.00104
3.0 mg/kg Antizol Followed by Ethanol0.00157
Ethanol Followed by 3.0 mg/kg Antizol0.00201
5.0 mg/kg Antizol Followed by Ethanol0.00138
Placebo Followed by Ethanol0.00193
Ethanol Followed by Placebo0.00141

PK of Acetaldehyde: T1/2

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionhours (Mean)
1.0 mg/kg Antizol Followed by Ethanol3.14
Ethanol Followed by 1.0 mg/kg Antizol3.08
3.0 mg/kg Antizol Followed by Ethanol2.48
Ethanol Followed by 3.0 mg/kg Antizol1.72
5.0 mg/kg Antizol Followed by Ethanol3.45
Placebo Followed by Ethanol2.39
Ethanol Followed by Placebo2.09

PK of Acetaldehyde: Tmax

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionhours (Median)
1.0 mg/kg Antizol Followed by Ethanol0.500
Ethanol Followed by 1.0 mg/kg Antizol0.650
3.0 mg/kg Antizol Followed by Ethanol1.00
Ethanol Followed by 3.0 mg/kg Antizol1.33
5.0 mg/kg Antizol Followed by Ethanol0.500
Placebo Followed by Ethanol0.500
Ethanol Followed by Placebo0.925

PK of Ethanol: AUC(0-∞)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionmg*hr/mL (Mean)
1.0 mg/kg Antizol Followed by Ethanol245
Ethanol Followed by 1.0 mg/kg Antizol263
3.0 mg/kg Antizol Followed by Ethanol237
Ethanol Followed by 3.0 mg/kg Antizol215
5.0 mg/kg Antizol Followed by Ethanol271
Placebo Followed by Ethanol214
Ethanol Followed by Placebo198

PK of Ethanol: AUC(0-t)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionmg*hr/dL (Mean)
1.0 mg/kg Antizol Followed by Ethanol209
Ethanol Followed by 1.0 mg/kg Antizol209
3.0 mg/kg Antizol Followed by Ethanol205
Ethanol Followed by 3.0 mg/kg Antizol135
5.0 mg/kg Antizol Followed by Ethanol231
Placebo Followed by Ethanol157
Ethanol Followed by Placebo152

PK of Ethanol: AUC%Extrap

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionpercentage (Mean)
1.0 mg/kg Antizol Followed by Ethanol14.7
Ethanol Followed by 1.0 mg/kg Antizol20.5
3.0 mg/kg Antizol Followed by Ethanol13.2
Ethanol Followed by 3.0 mg/kg Antizol20.0
5.0 mg/kg Antizol Followed by Ethanol12.1
Placebo Followed by Ethanol13.4
Ethanol Followed by Placebo13.9

PK of Ethanol: CL/F

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

InterventiondL/hr (Mean)
1.0 mg/kg Antizol Followed by Ethanol140
Ethanol Followed by 1.0 mg/kg Antizol138
3.0 mg/kg Antizol Followed by Ethanol142
Ethanol Followed by 3.0 mg/kg Antizol131
5.0 mg/kg Antizol Followed by Ethanol112
Placebo Followed by Ethanol159
Ethanol Followed by Placebo167

PK of Ethanol: Cmax

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionmg/dL (Mean)
1.0 mg/kg Antizol Followed by Ethanol62.7
Ethanol Followed by 1.0 mg/kg Antizol70.3
3.0 mg/kg Antizol Followed by Ethanol80.5
Ethanol Followed by 3.0 mg/kg Antizol43.3
5.0 mg/kg Antizol Followed by Ethanol74.9
Placebo Followed by Ethanol59.3
Ethanol Followed by Placebo55.1

PK of Ethanol: DN AUC(0-∞)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Intervention(mg*hr/dL)/mg (Mean)
1.0 mg/kg Antizol Followed by Ethanol0.00760
Ethanol Followed by 1.0 mg/kg Antizol0.00731
3.0 mg/kg Antizol Followed by Ethanol0.00705
Ethanol Followed by 3.0 mg/kg Antizol0.00768
5.0 mg/kg Antizol Followed by Ethanol0.00917
Placebo Followed by Ethanol0.00681
Ethanol Followed by Placebo0.00617

PK of Ethanol: DN AUC(0-t)

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Intervention(mg*hr/dL)/mg (Mean)
1.0 mg/kg Antizol Followed by Ethanol0.00648
Ethanol Followed by 1.0 mg/kg Antizol0.00585
3.0 mg/kg Antizol Followed by Ethanol0.00613
Ethanol Followed by 3.0 mg/kg Antizol0.00483
5.0 mg/kg Antizol Followed by Ethanol0.00791
Placebo Followed by Ethanol0.00508
Ethanol Followed by Placebo0.00476

PK of Ethanol: DN Cmax

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Intervention(mg/dL)/mg (Mean)
1.0 mg/kg Antizol Followed by Ethanol0.00195
Ethanol Followed by 1.0 mg/kg Antizol0.00198
3.0 mg/kg Antizol Followed by Ethanol0.00243
Ethanol Followed by 3.0 mg/kg Antizol0.00155
5.0 mg/kg Antizol Followed by Ethanol0.00261
Placebo Followed by Ethanol0.00193
Ethanol Followed by Placebo0.00175

PK of Ethanol: T1/2

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionhours (Mean)
1.0 mg/kg Antizol Followed by Ethanol1.51
Ethanol Followed by 1.0 mg/kg Antizol1.95
3.0 mg/kg Antizol Followed by Ethanol1.43
Ethanol Followed by 3.0 mg/kg Antizol1.78
5.0 mg/kg Antizol Followed by Ethanol1.67
Placebo Followed by Ethanol1.45
Ethanol Followed by Placebo1.32

PK of Ethanol: Tmax

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

Interventionhours (Median)
1.0 mg/kg Antizol Followed by Ethanol1.50
Ethanol Followed by 1.0 mg/kg Antizol0.833
3.0 mg/kg Antizol Followed by Ethanol0.500
Ethanol Followed by 3.0 mg/kg Antizol1.42
5.0 mg/kg Antizol Followed by Ethanol0.500
Placebo Followed by Ethanol0.500
Ethanol Followed by Placebo1.01

PK of Ethanol: Vz/F

(NCT00661141)
Timeframe: Days 1 and 2: prior to administration of 1st treatment (ethanol or study drug); 10, 20, and 30 min prior to administration of second treatment (study drug or ethanol); 40, 50, 60 min and 2, 3, 4, 5, 6, and 8 hr post administration of 1st treatment

InterventiondL (Mean)
1.0 mg/kg Antizol Followed by Ethanol297
Ethanol Followed by 1.0 mg/kg Antizol387
3.0 mg/kg Antizol Followed by Ethanol295
Ethanol Followed by 3.0 mg/kg Antizol330
5.0 mg/kg Antizol Followed by Ethanol242
Placebo Followed by Ethanol287
Ethanol Followed by Placebo321

Number of Participants With Adverse Events (AEs), Serious AEs, and AEs Leading to Study Discontinuation

AEs were collected to evaluate the safety and tolerability of oral Antizol with concomitant ethanol administration in particitpants with symptoms of acetaldehyde toxicity associated with altered ethanol metabolism. AE: any untoward medical event that occurs following the first administration of study medication until the study participant's last study visit, whether or not the event is considered drug related. SAE: an event that meets any of the following criteria: results in death; is life threatening; requires inpatient hospitalization or prolongation of an existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect in the offspring of an exposed subject; is medically significant or an important medical event as assessed by investigator or sponsor; is, in the opinion of the investigator, an important medical event. (NCT00661141)
Timeframe: Study Day 0 through Study Visit Day 7

,,,,
InterventionParticipants (Count of Participants)
Any AEMild AEModerate AESevere AELife-Threatening/Disabling AEDeathPossibly or Probably Related AEAE Leading to Study DiscontinuationSerious AE
Antizol 1.0 mg/kg131320001300
Antizol 3.0 mg/kg660000600
Antizol 5.0 mg/kg880000500
Overall282870002700
Pooled Placebo211950001800

Reviews

9 reviews available for acetaldehyde and Flushing

ArticleYear
The alcohol flushing response: an unrecognized risk factor for esophageal cancer from alcohol consumption.
    PLoS medicine, 2009, Mar-24, Volume: 6, Issue:3

    Topics: Acetaldehyde; Adult; Alcohol Drinking; Alcoholism; Aldehyde Dehydrogenase; Aldehyde Dehydrogenase, M

2009
Alcohol and aldehyde dehydrogenase polymorphisms and a new strategy for prevention and screening for cancer in the upper aerodigestive tract in East Asians.
    The Keio journal of medicine, 2010, Volume: 59, Issue:4

    Topics: Acetaldehyde; Adult; Alcohol Dehydrogenase; Alcohol Drinking; Alcoholism; Aldehyde Dehydrogenase; Al

2010
Chlorpropamide--alcohol flush: the case in favour.
    Diabetologia, 1984, Volume: 26, Issue:1

    Topics: Acetaldehyde; Alcohol Drinking; Biomechanical Phenomena; Chlorpropamide; Diabetic Angiopathies; Drug

1984
The chlorpropamide alcohol flush.
    Clinical science (London, England : 1979), 1984, Volume: 67, Issue:4

    Topics: Acetaldehyde; Alcohol Drinking; Chlorpropamide; Diabetes Mellitus, Type 2; Dose-Response Relationshi

1984
Alcohol and the mystique of flushing.
    Alcoholism, clinical and experimental research, 1995, Volume: 19, Issue:1

    Topics: Acetaldehyde; Alcohol Drinking; Alcoholism; Aldehyde Dehydrogenase; Alleles; Cross-Cultural Comparis

1995
[Biological actions of acetaldehyde].
    Nihon hoigaku zasshi = The Japanese journal of legal medicine, 1999, Volume: 53, Issue:3

    Topics: Acetaldehyde; Animals; Blood Pressure; Catecholamines; Dogs; Ethanol; Flushing; Humans; Intestinal A

1999
Racial differences in alcohol sensitivity.
    Alcohol and alcoholism (Oxford, Oxfordshire), 1986, Volume: 21, Issue:1

    Topics: Acetaldehyde; Alcohol Dehydrogenase; Alcohol Drinking; Alcohol Oxidoreductases; Alcoholism; Aldehyde

1986
[Flush induced by chlorpropamide-alcohol (CAF): a genetic marker of diabetes mellitus or an undesirable effect of the drug?].
    Revista clinica espanola, 1985, Volume: 176, Issue:3

    Topics: Acetaldehyde; Alcohol Drinking; Chlorpropamide; Diabetes Mellitus, Type 1; Diabetes Mellitus, Type 2

1985
Alcohol and alcohol problems research 2. Japan.
    British journal of addiction, 1985, Volume: 80, Issue:2

    Topics: Acetaldehyde; Alcohol Drinking; Alcoholism; Aldehyde Dehydrogenase; Female; Fetal Alcohol Spectrum D

1985

Trials

6 trials available for acetaldehyde and Flushing

ArticleYear
Association between psychomotor function and ALDH2 genotype after consuming barley shochu: A randomized crossover trial.
    Clinical and translational science, 2023, Volume: 16, Issue:4

    Topics: Acetaldehyde; Alcohol Drinking; Aldehyde Dehydrogenase; Aldehyde Dehydrogenase, Mitochondrial; Cross

2023
The acute effects of ethanol and acetaldehyde on physiological responses after ethanol ingestion in young healthy men with different ALDH2 genotypes.
    Clinical toxicology (Philadelphia, Pa.), 2012, Volume: 50, Issue:4

    Topics: Acetaldehyde; Adult; Aldehyde Dehydrogenase; Aldehyde Dehydrogenase, Mitochondrial; Blood Pressure;

2012
Roles of chlorpropamide, alcohol and acetaldehyde in determining the chlorpropamide-alcohol flush.
    Diabetologia, 1984, Volume: 26, Issue:1

    Topics: Acetaldehyde; Adult; Alcohol Drinking; Chlorpropamide; Diabetes Mellitus, Type 2; Dose-Response Rela

1984
Alcohol tolerance in patients with non-insulin-dependent (type 2) diabetes treated with sulphonylurea derivatives.
    Arzneimittel-Forschung, 1994, Volume: 44, Issue:6

    Topics: Acetaldehyde; Adult; Aged; Blood Gas Analysis; Blood Glucose; Body Temperature Regulation; Diabetes

1994
Elimination kinetics of ethanol and acetaldehyde in healthy men during the calcium carbimide-alcohol flush reaction.
    Alcohol and alcoholism (Oxford, Oxfordshire). Supplement, 1987, Volume: 1

    Topics: Acetaldehyde; Cyanamide; Cyanides; Ethanol; Flushing; Humans; Male

1987
Diphenhydramine and the calcium carbimide-ethanol reaction: a placebo-controlled clinical study.
    Clinical pharmacology and therapeutics, 1986, Volume: 39, Issue:5

    Topics: Acetaldehyde; Administration, Oral; Adult; Blood Pressure; Clinical Trials as Topic; Cyanamide; Cyan

1986

Other Studies

27 other studies available for acetaldehyde and Flushing

ArticleYear
Alcohol consumption and bladder cancer risk with or without the flushing response: The Japan Public Health Center-based Prospective Study.
    International journal of cancer, 2017, 12-15, Volume: 141, Issue:12

    Topics: Acetaldehyde; Adult; Aged; Alcohol Drinking; Female; Flushing; Humans; Japan; Male; Middle Aged; Pro

2017
Effect of Alcohol Sensitivity in Healthy Young Adults on Breath Pharmacokinetics of Acetaldehyde After Mouth Washing with Alcohol.
    Alcoholism, clinical and experimental research, 2018, Volume: 42, Issue:11

    Topics: Acetaldehyde; Adult; Alcohol Drinking; Aldehyde Dehydrogenase, Mitochondrial; Area Under Curve; Brea

2018
Origin and dispersal of atypical aldehyde dehydrogenase ALDH2487Lys.
    Gene, 2009, Apr-15, Volume: 435, Issue:1-2

    Topics: Acetaldehyde; Alcohol Drinking; Aldehyde Dehydrogenase; Aldehyde Dehydrogenase, Mitochondrial; Allel

2009
Fomepizole for severe disulfiram-ethanol reactions.
    The American journal of emergency medicine, 2012, Volume: 30, Issue:1

    Topics: Acetaldehyde; Alcohol Dehydrogenase; Antidotes; Disulfiram; Drug Interactions; Ethanol; Female; Flus

2012
Case series: Alcohol intolerance with Coprine-like syndrome after consumption of the mushroom Lepiota aspera (Pers.:Fr.) Quél., 1886 (Freckled Dapperling).
    Clinical toxicology (Philadelphia, Pa.), 2011, Volume: 49, Issue:2

    Topics: Acetaldehyde; Aged; Alcohol Drinking; Coprinus; Drug Therapy, Combination; Dyspnea; Erythema; Ethano

2011
Treatment of Asian flush with abacavir.
    Medical hypotheses, 2011, Volume: 77, Issue:2

    Topics: Acetaldehyde; Alcohol Dehydrogenase; Aldehyde Dehydrogenase; Aldehyde Dehydrogenase, Mitochondrial;

2011
Anxiogenic and stress-inducing effects of peripherally administered acetaldehyde in mice: similarities with the disulfiram-ethanol reaction.
    Pharmacology, biochemistry, and behavior, 2012, Volume: 100, Issue:3

    Topics: Acetaldehyde; Alcohol Deterrents; Alcohol Drinking; Aldehyde Dehydrogenase; Animals; Anxiety; Behavi

2012
Association of ALDH2 polymorphism with sensitivity to acetaldehyde-induced micronuclei and facial flushing after alcohol intake.
    Toxicology, 2005, Jun-01, Volume: 210, Issue:2-3

    Topics: Acetaldehyde; Adult; Alcohol Drinking; Aldehyde Dehydrogenase; Aldehyde Dehydrogenase, Mitochondrial

2005
Disulfiram-like effect of cyproterone acetate.
    European journal of obstetrics, gynecology, and reproductive biology, 2009, Volume: 146, Issue:2

    Topics: Acetaldehyde; Adult; Contraceptives, Oral, Combined; Cyproterone Acetate; Disulfiram; Ethanol; Ethin

2009
Comment on "Disulfiram-like effect of cyproterone acetate" [Z. Nitzan, M. Dan, Eur. J. Obstet. Gynecol. Reprod. Biol.].
    European journal of obstetrics, gynecology, and reproductive biology, 2009, Volume: 146, Issue:2

    Topics: Acetaldehyde; Aldehyde Dehydrogenase; Animals; Cyproterone Acetate; Disulfiram; Ethanol; Flushing; H

2009
Identification and characterisation of alcohol-induced flushing in Caucasian subjects.
    Alcohol and alcoholism (Oxford, Oxfordshire), 1994, Volume: 29, Issue:4

    Topics: Acetaldehyde; Adolescent; Adult; Alcohol Drinking; Aldehyde Oxidoreductases; Female; Flushing; Human

1994
Investigations on the ethanol-induced flushing reaction: effects of propranolol and dipyridamole on acetaldehyde and prostacyclin metabolism.
    Toxicology, 1994, May-31, Volume: 90, Issue:1-2

    Topics: Acetaldehyde; Aldehyde Dehydrogenase; Animals; Dipyridamole; Epoprostenol; Ethanol; Flushing; Male;

1994
Changes in free and bound alcohol metabolites in the urine during ethanol oxidation.
    Arukoru kenkyu to yakubutsu izon = Japanese journal of alcohol studies & drug dependence, 1993, Volume: 28, Issue:6

    Topics: Acetaldehyde; Acetates; Acetone; Adult; Alcohol Drinking; Ethanol; Flushing; Humans; Male; Methanol;

1993
Aversive reactions and alcohol use in Europeans.
    Alcoholism, clinical and experimental research, 1993, Volume: 17, Issue:1

    Topics: Acetaldehyde; Adult; Alcohol Drinking; Aldehyde Dehydrogenase; Cross-Cultural Comparison; Diseases i

1993
Degrees of alcohol intoxication in 117 hospitalized cases.
    Journal of studies on alcohol, 1991, Volume: 52, Issue:5

    Topics: Acetaldehyde; Adult; Aged; Alcoholic Intoxication; Alcoholism; Ethanol; Flushing; Hospitalization; H

1991
Hemoglobin-acetaldehyde adducts in human volunteers following acute ethanol ingestion.
    Alcoholism, clinical and experimental research, 1990, Volume: 14, Issue:6

    Topics: Acetaldehyde; Adult; Alcoholic Intoxication; Enzyme-Linked Immunosorbent Assay; Female; Flushing; He

1990
Cutaneous vasomotor sensitivity to ethanol and acetaldehyde: subtypes of alcohol-flushing response among Chinese.
    Alcoholism, clinical and experimental research, 1990, Volume: 14, Issue:6

    Topics: Acetaldehyde; Adolescent; Adult; Aged; Alcohol Drinking; Aldehyde Dehydrogenase; China; Ethanol; Fem

1990
Aldehyde dehydrogenases and alcoholism.
    Alcoholism, clinical and experimental research, 1990, Volume: 14, Issue:2

    Topics: Acetaldehyde; Alcoholism; Aldehyde Dehydrogenase; Cross-Cultural Comparison; Flushing; Humans

1990
Possible involvement of kinins in cardiovascular changes after alcohol intake.
    Pharmacology, biochemistry, and behavior, 1990, Volume: 35, Issue:2

    Topics: Acetaldehyde; Adolescent; Adult; Alcohol Drinking; Aldehyde Dehydrogenase; Blood Pressure; Ethanol;

1990
The flushing syndrome after ethanol intake caused by aldehyde dehydrogenase deficiency in Orientals.
    Acta medicinae legalis et socialis, 1989, Volume: 39, Issue:1

    Topics: Acetaldehyde; Adult; Alcohol Drinking; Aldehyde Dehydrogenase; Catecholamines; Flushing; Humans; Jap

1989
Determinations of ethanol, acetaldehyde and acetate in blood and urine during alcohol oxidation in man.
    Alcohol and alcoholism (Oxford, Oxfordshire), 1989, Volume: 24, Issue:2

    Topics: Acetaldehyde; Acetates; Acetic Acid; Adult; Alcohol Drinking; Dose-Response Relationship, Drug; Etha

1989
Cutaneous vascular sensitivity to lower aliphatic alcohols and aldehydes in Orientals.
    Alcoholism, clinical and experimental research, 1985, Volume: 9, Issue:6

    Topics: 1-Propanol; Acetaldehyde; Alcohols; Aldehydes; Asian People; Ethanol; Female; Flushing; Forearm; Hum

1985
Opiate antagonist nalmefene inhibits ethanol-induced flushing in Asians: a preliminary study.
    Alcoholism, clinical and experimental research, 1988, Volume: 12, Issue:5

    Topics: Acetaldehyde; Adult; Alcohol Drinking; Asian; Blood Pressure; Body Temperature Regulation; Endorphin

1988
Acetaldehyde syndrome after celiac plexus alcohol block.
    Anesthesia and analgesia, 1986, Volume: 65, Issue:12

    Topics: Acetaldehyde; Aldehyde Dehydrogenase; Celiac Plexus; Ethanol; Flushing; Humans; Nerve Block; Phenoty

1986
Effects of chlorpropamide and alcohol on aldehyde dehydrogenase activity and blood acetaldehyde concentration.
    Diabetes research (Edinburgh, Scotland), 1986, Volume: 3, Issue:7

    Topics: Acetaldehyde; Adult; Aged; Aldehyde Dehydrogenase; Chlorpropamide; Diabetes Mellitus, Type 1; Diabet

1986
Aldehyde dehydrogenase activity and large vessel disease in diabetes mellitus. A preliminary study.
    Diabetes, 1986, Volume: 35, Issue:3

    Topics: Acetaldehyde; Aged; Aldehyde Dehydrogenase; Chlorpropamide; Diabetes Mellitus, Type 2; Diabetic Angi

1986
Suppression of acetaldehyde accumulation by 4-methylpyrazole in alcohol-hypersensitive Japanese.
    Japanese journal of pharmacology, 1985, Volume: 38, Issue:1

    Topics: Acetaldehyde; Adult; Alcoholic Intoxication; Flushing; Fomepizole; Heart; Heart Rate; Humans; Male;

1985