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Table 1 Physicochemical properties and pharmacokinetics of immediate-release β-adrenergic antagonists

From: Extracorporeal treatment for poisoning to beta-adrenergic antagonists: systematic review and recommendations from the EXTRIP workgroup

Drug

MW (Da)

Protein binding (%)

VD (L/kg)

F (%)

TMAX (h)

Endogenous T1/2 (h)

Endogenous CL (mL/min)

Renal CL (mL/min), Normal GFR

Therapeutic range (mg/L)

References

Normal GFR

CKD

Normal GFR

ESKD

Normal GFR

ESKD

Acebutolol

336

10–25

1.5–2.5

N/A

35–50

2.0–4.0

4–10&

600–800

N/A

150–300

0.2–2

[19, 68, 69, 80, 138,139,140,141,142,143,144,145,146,147,148]

Alprenolol

249

80–90

2.5–3.5

N/A

5–15

1.0–2.0

2–4

N/A

800–1000

N/A

50

0.03–0.15

[149,150,151,152] [153]

Atenolol

266

0–5

1.0–1.2

50–60

3.0–3.5

5–8

50–100

140–180

20

120–140

0.1–1.5

[11, 20, 73, 78, 79, 85, 90, 105, 118, 124, 148, 154,155,156,157,158,159,160,161,162,163]

Betaxolol

344

50

4.5–6.0

5.0–6.5

75–90

2.5–4.0

14–16

25–35

220–270

100–150

50

0.005–0.05

[86, 148, 164,165,166,167,168]

Bisoprolol

325

30

2.0–3.0

90

1.5–2.5

9–12

25–35

200–250

50

120–150

0.01–0.1

[93, 98, 148, 169,170,171,172,173,174,175]

Bopindolol

381

N/A

1.8–2.0

N/A

70

1.0–2.0

4–6

8

350–400

N/A

N/A

0.001–0.015

[148, 176,177,178,179,180]

Carteolol

292

10–30

4

N/A

85

2.0

5–7

30–35

650

N/A

250

0.01–0.1

[148, 181,182,183]

Carvedilol

405

98

1.5–2.5

N/A

20–30

1.0–3.0

6–7

600

5

0.02–0.2

[96, 148, 184,185,186,187,188,189,190]

Celiprolol

379

25

4–5

N/A

30–70

2.0–4.0

5–7

N/A

900–1000

N/A

180–220

0.05–0.5

[191,192,193]7 [148, 194,195,196,197,198,199,200]

Cetamolol

310

N/A

3.5

2.5

N/A

2.5–3.0

7

10–12

420*

150

100–150

0.01–0.1

[201,202,203]

Esmolol

295

55

2.0–3.5

Not applicable

0.2

10,000–15,000

100–200

0.15–2

[95, 148, 204, 205]

Labetalol

328

50

5.0–9.0

20–30

0.5–1.5

3–10

10–12

1200–2000

20

0.03–0.3

[92, 206,207,208,209,210,211,212] [94, 148, 213]

Medroxalol

372

N/A

10–15

N/A

30–50

2–3

7–15

N/A

1000–1100

N/A

80–100

N/A

[213,214,215]

Mepindolol

262

55

5.7**

N/A

N/A

1.4

3–6

650**

N/A

0**

0.007–0.07

[88, 148, 216, 217]

Metipranolol

309

70

3–4

N/A

40–50

0.5–2.0

2.5–3.0

1100–1300

N/A

120–150

0.02–0.1

[97, 148, 218,219,220,221]

Metoprolol

267

10

3.0–4.0

N/A

40–60

1.5–2.0

3–5

800–1200

100

0.03–0.5

[222,223,224,225] [9, 73, 82, 106, 148, 226,227,228,229,230]

Nadolol

309

15–25

1.5–2.0

N/A

30

2.8

10–15

30–45

120–250

30

80–120

0.01–0.25

[75, 89, 148, 231,232,233,234]

Nebivolol

405

98

9–12

Variable

1–3

10–15

800–1000

30

0.001–0.05

[148, 235,236,237,238,239,240,241]

Oxprenolol

265

80–85

0.8–1.2

0.8

35–50

0.5–1.5

1–2

600–750

550

10

0.05–0.3

[84, 148, 242,243,244,245,246,247,248,249,250,251,252]

Penbutolol

291

90–95

0.5–1.0

N/A

90

1.0–2.0

15–20

30

300–600

N/A

5

0.01–0.3

[253] [148, 254,255,256,257,258,259,260,261,262]

Pindolol

248

40–55

1.3–2.3

1.6–1.8

50–90

0.5–1.5

3–5

450–550

180–240

150–250

0.02–0.15

[148, 263,264,265,266,267,268,269]

Practolol

266

57

1.5

N/A

90–100

2–5

10–13

60–80

135

20

100–120

1.5–5

[65, 67, 148, 270,271,272,273,274]

Prenalterol

225

5

2.5–3.5

N/A

25–35

0.5–2.5

1.5–2.5

N/A

800–1400

N/A

200–800

0.01–0.04

[275,276,277,278,279,280,281,282]

Propranolol

259

85–95

3.0–5.0

20–50

1.5–2.0

3–5

800–1200

5

0.02–0.3

[20, 66, 70, 74, 154, 230, 283,284,285,286,287,288,289,290,291,292,293,294,295,296,297,298,299,300] [73, 87, 131, 148, 301, 302]

Sotalol

272

0

1.3–1.5

90

2.5–3.5

5–9

35–60

120–160

20–25

80–120

0.5–3

[71, 83, 303,304,305,306,307] [13, 15, 115, 148, 303, 306, 308,309,310]

Talinolol

363

60**

3.0–3.5

55

2.5–3.5

10–12

20–25

320–380

150–200

0.04–0.15

[99, 104, 107, 148, 311,312,313]

Timolol

316

10

2.0–2.5

N/A

60

1.3–2.0

3–5

450–580

N/A

100

0.005–0.1

[300, 314,315,316,317] [72, 148, 315]

Tolamolol

316

90

1.2–1.8

N/A

N/A

1–3

2–3

1100

N/A

N/A

N/A

[318,319,320]

  1. MW: Molecular weight, VD: Volume of distribution, F: bioavailability, TMAX: Time to maximum concentration, T1/2: elimination half-life, CL: Clearance, N/A: Not available
  2. *  Not adjusted for bioavailability, ** No reference from primary data (taken from reviews)
  3. & conflicting data, perhaps due to non-sensitive assays which included measurement of metabolites in early reports [68, 69]
  4. Total body clearance and volume of distribution were obtained from intravenous data. If these data were unavailable but reported for oral data (i.e., as V/F or CL/F), then values were adjusted for bioavailability
  5. This systematic review has taken the liberty to review all BAAs for which data exist, even if some are not currently commercially available
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