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Table 1 Studies and reports evaluating the effects of activated charcoal on selected drugs

From: Gastrointestinal decontamination in the acutely poisoned patient

Type report

Subjects

Variables

Drug (oral unless noted)

Conclusion/reference

R, NB, CCS

HV

C, AC, VT

Acetaminophen

AC at 15, 30 and 120 min reduced acetaminophen urinary recovery by 48, 44, and 33% [127]

NR, OB, NB

HPP

AC + NAC, NAC

Acetaminophen

↓ In serum transaminases and prothrombin times with AC + NAC compared to NAC alone [128]

NR, OB, NB

HPP

AC + NAC, NAC

Acetaminophen

↓ In serum transaminase, major adverse effects and death with AC and NAC [129]

R, CCS, NB

HV

C, AC-after 1 h, AC-after 2 h, CL + AC-after 1 h

Acetaminophen

All significantly reduced acetaminophen AUC. The AUC was significantly more reduced when AC given at 1 h compared to 2 h, and GL did not add to AC alone [130]

R, NB

HPP

GL, AC, Ip, C

Acetaminophen

Greatest ↓ in acetaminophen level with AC, then Ip, then GL compared to C. No clinical differences reported [31]

NR, Retro, Ob, NB

HPP

GL + AC, AC, C

Acetaminophen

AC reduced risk for toxic acetaminophen concentrations, GL did not further reduce risk [131]

R, CCS, NB

HV

NAC, AC + NAC

NAC

No significant differences in peak NAC levels with AC [132]

NR, NB, CCS

HV

NAC, AC + NAC

NAC

A 3% reduction in NAC AUC and a 29% reduction in peak NAC levels with AC [133]

[

HV

AC, C

Acetaminophen

The acetaminophen AUC was 58.9% with AC compared to C

(P = 0.01) [134]

Ob, NB

HPP

NAC, NAC + AC

Acetaminophen

The addition of AC significantly (P < 0.05) reduced the T 1/2 and increased the body clearance of acetaminophen [135]

B, R, CCS

HV

C, AC1, AC2 (variable types of AC)

Acetaminophen

Both types of AC reduced AUC for acetaminophen and peak levels of acetaminophen [136]

R, CCS, NB

HV

C, AC, AC+ IM atropine

Acetaminophen

AC significantly reduced AUC for acetaminophen by 20% alone and by 47% in the presence of atropine [137]

CCS, R, NB

Pigs

C, MDAC (variable times)

IV-acetaminophen, digoxin, theophylline, valproic acid

Significantly enhanced elimination (P < 0.01) for acetaminophen, theophylline and digoxin with MDAC, but no increased elimination with valproic acid [138]

R, CSS, NB

HV

C, AC (variable time after ingestion)

Acetaminophen + oxycodone

Compared to control, acetaminophen AUC reduced by 43% 1 h (P < 0.0001), 22% 2 h (P = 0.02) and 15% 3 h (P = 0.26) with AC [139]

R, CCS, NB

HV

C, AC (variable time after ingestion)

Acetaminophen

Compared to control, acetaminophen AUC reduced by 56% 1 h (P < 0.002), 22% 2 h (P < 0.03) and 8% 4 h (NS) with AC [140]

R, CSS, NB

HV

C, AC

Sodium amino-salicylic acid

(1 and 2 g - C,

1 and 2 g - AC,

10 and 20 g - AC

AC was given immediately after salicylic acid. Increasing the dose of salicylic acid reduced the antidotal efficacy of AC and lead to increasing salicylic acid AUC. The salicylic acid AUC increased by more than 4 fold when salicylic acid 10 g dose went to 20 g dose with AC dose held constant [141]

R, CSS, NB

HV

AC (3 variable doses)

Acetaminophen

A 59% increase (P < 0.001) acetaminophen AUC was seen between 50 g AC and 5 g AC both given 1 h after drug [99]

R, CCS, NB

HV

C, Ip, GL, AC after 1 h

Aspirin

Equal reduction in absorption of aspirin as measured by recovered urine salicylate [142]

R, CCS, NB

HV

C, AC, MDAC (1, 2 or 3 doses separated by 4 h)

Aspirin

All 3 AC doses associated with significant (P ≤ 0.01) reduction in urinary salicylate recovery. 3 doses of AC resulted in significantly (P < 0.01) greater recovery of salicylate than 1 or 2 AC doses [143]

R, CCS, NB

HV

C, AC

Aspirin

MDAC associated with a significant (P ≤ 0.01) 9% reduction in serum salicylate AUC and a significant (P ≤ 0.05) 18% reduction in urinary excretion. Considered "clinically modest" effect of "questionable valve" [144]

R, CCS, NB

HV

C, Ip, AC, Ip + AC

Aspirin

Urinary salicylate recovery was 96.3 ± 7.5% in control, 70.2 ± 12.1% Ip, 56.5 ± 12.5% AC, 72.7 ± 14.1%, Ip + AC. There was a significantly greater (P < 0.05) reduction with AC compared to Ip [18]

R, CCS, NB

HV

C, AC (1 h after ingestion)

Aspirin, digoxin, phenytoin

AC reduced the AUC of digoxin (98%), phenytoin (90%) and aspirin (70) [145]

CCS, NB

Canines

C, MDAC

IV-theophylline at 2 different doses

Nasogastric tube in duodenum, AC resulted in 22-47% decrease in theophylline AUC [146]

R, NB

Rats

C, AC, MDAC

IV-theophylline and phenobarbital

MDAC significantly decreased theophylline and phenobarbital serum T 1/2 and AUC while AC had only slight decrease. Thought to be "adsorption" of exsorbed theophylline and phenobarbital [147]

R, CCS, NB

HV

C, MDAC various doses, variable intervals for total dose 150 g AC

IV-theophylline

The AUC of theophylline significantly (P < 0.05) reduced near equally by three schedules of MDAC [148]

R, NB

Rats

C, MDAC

IV-theophylline multiple doses tested

The theophylline AUC and T 1/2 was reduced by 50% and 52% respectively by MDAC [149]

NB

HPP

MDAC

Phenytoin/phenobarbital

Apparent decreased T 1/2 for phenytoin and phenobarbital only after MDAC started [150]

NB

HPP

MDAC

Phenobarbital

Apparent decreased T 1/2 for phenobarbital with MDAC [151]

R, NB

HPP

MDAC, AC

Phenobarbital

In the 5 patients treated with MDAC, the T 1/2 was 36 ± 13 h for phenobarbital, significantly shorter than T 1/2

after single dose AC in 5 patients. No difference in length of time on mechanical ventilation or time in hospital [100]

NB

HPP

MDAC

Phenobarbital

Apparent decrease in T 1/2 phenobarbital with MDAC [152]

R, CSS, NB

HV

C, MDAC, 24 h of urinary alkalinization

IV-phenobarbital

The T 1/2 of phenobarbital was 148 h, 47 h and 19 h during the control, alkalinization and MDAC phases, respectively. All statistically significantly different from each other [153]

R, CSS, NB

HV

C, MDAC

IV-phenobarbital

MDAC deceased phenobarbital T 1/2 from 110 ± 8 to 45 ± 6 h

(P < 0.01) [154]

NB

HPP

MDAC

Phenytoin

Apparent decrease in T 1/2 phenytoin with MDAC [155]

NB

HPP

MDAC

Phenytoin

Apparent decrease in T 1/2 phenytoin with MDAC [156]

R, CSS, NB

HV

C, MDAC

IV-phenytoin

MDAC decreased T 1/2 phenytoin from 44.5 to 72.3 h [157]

R, NB

HPP

AC, MDAC

Carbamazepine

MDAC associated with reduced T 1/2 carbamazepine 12.56 ± 3.5 vs. 27.88 ± 7.36 h (P = 0.0004) compared to single dose AC. MDAC also associated with statistically significant reduced coma, mechanical ventilation and length of hospital stay [101]

NB

HPP

MDAC

Carbamazepine

Apparent decrease in T 1/2 carbamazepine with MDAC [158]

NB

HPP

MDAC, WBI

Carbamazepine

Rebound in carbamazepine serum levels despite MDAC [45]

NB

HPP

MDAC

Valproic acid

Apparent decrease in T 1/2 valproic acid with MDAC [159]

R, NB

HPP

C, AC, MDAC

Pesticides, yellow oleander, medicines or unknown

No difference in rates of mortality between C (6.8%), AC (7.1%) and MDAC (6.3%). Odds ratio 0.96 (95% (F 0.70-1.33) between C and MDAC [104]

R, NB

HPP

C, MDAC

Yellow oleander

MDAC significantly (P = 0.025) reduced mortality from 8% (control) to 2.5% (MDAC). Significant reduction in ICU, digoxin FAB fragments treatment, cardiac pacing, life-threatening arrhythmias, doses of atropine and time in hospital with more [103]

R, CSS, NB

HV

C, AC

Isoniazid

AC reduced isoniazid absorption [160]

R, NB

Rabbits

C, AC

Isoniazid

AC reduced T 1/2 of isoniazid [161]

R, CSS, NB

HV

C, AC

Isoniazid

AC 1 h after isoniazid reduced the isoniazid AUC [162]

  1. ↑ = increased; ↓ = decreased; AC = activated charcoal; AUC = area under serum curve; B = blinded; C = control; CCS = crossover controlled study; GL = gastric lavage; HPP = human poisoned patients; HV = human volunteers; IM = intramuscular; Ip = ipecac; IV = intravenous; LiCl = lithium chloride; MC = multiple center; MDAC = multiple dose AC; NAC = n-acetylcysteine; NB = non-blinded; NC = no change; NR = non-randomized; ob = observational study; R = randomized; Retro = retrospective; SPS = sodium polystyrene sulfonate; SR = sustained release; T 1/2 = serum half-life; VT = variable time