Table 2 Comparative analysis of early onset NMBAs at different doses expressed as multiples of ED95 (effective dose 95)
From: Neuromuscular blockers and their reversal: have we finally found the on-off switches?
| Drug (ED95) | Dose | Onset time | Histamine (Savarese et al. 2004; Belmont et al. 2004) | Duration of action (recovery to TOFr ≥ 0.90) reversal/recovery |
|---|---|---|---|---|
| Succinylcholine (Heerdt et al. 2004) (0.3 mg/kg) | 0.45 mg/kg | 65 s | Yes | 5 min (Spont. recovery) |
| 0.6 mg/kg | 55 s | Yes | 6.4 min (Spont. recovery) | |
| 3–4 ED95, 1 mg/kg | 45 s | Yes | 12.5 min, hyperkalemia, bradycardia, masseter muscle spasm, fasciculations, postoperative myalgia, ↑IOP | |
| Mivacurium (Lien 2013; Diefenbach et al. 1995) 0.06–0.08 mg/kg | 2–3 ED95 | 2.5 min | Yes | 10–12 min (withdrawn from the US market 2006), erythema, hypotension, bronchospasm |
| 3 ED95 | NA | Yes | 22 min (Rh) | |
| Rapacuronium (ORG-9487) (Blobner et al. 2000; Sunaga et al. 2010a; Heerdt et al. 2016) 1 mg/kg | 1.5 ED95 | 60–90 s | No | < 20 min, withdrawn from market (2001): fatal bronchospasm |
| 1.5–2.5 ED95 | 50–60 s | Yes | 20 min, tachycardia, hypotension, and bronchospasm | |
| Cisatracurium (Savarese et al. 2018) 0.05 mg/kg | 3–4ED95 | 5–6 min | No |
30–45 min (Hoffman degradation) Not affected by hepatic/renal disease |
| Rocuronium (De May et al 1994; Sunaga et al. 2010b; Chavan et al 2016, Kaullen et al. 2018) 0.3 mg/kg | 1–1.5× ED95 | 60–180 s | No |
18–20 min (Spont) Duration prolonged in liver disease |
| 2× ED95 | 60–90 s | No | 3.75 times SCH; 3.75 × 6 min (Spont) | |
| 3–4× ED95 | 50–60 s | No | 7.5 times SCH; RSI dose; reversible by high dose sugammadex, as early as 3 min post-administration | |
|
Gantacurium (Savarese et al. 2010; Boer and Carlos 2018; Heerdt et al. 2015; Lien et al. 2009) (0.19 mg/kg) Not available for clinical use | 2× ED95 | 70 s | No | 15 min (Spont.) |
| 2.5× ED95 | 60 s | No | 8 min (Spont. recovery identical to Sch) (Lien et al. 2009) | |
|
4–5× ED95 (rhesus) | 60 s | No |
10.4 min (Spont.) 2–3 min(l-cysteine 50 mg/kg 1 min after gantacurium) | |
| 4–5× ED95 | 90 s | Yes | 15 min (Spont) study on human volunteers (Ma et al. 2012a) | |
|
CW002 (Savarese et al. 2010; Boer and Carlos 2018; Ma et al. 2012b) (0.077 mg/kg) Not available for clinical use | 1.8 x ED95 | 90 s | No | 33.8 min (clinical duration of action), 73 min (spont. reversal; TOFr 0.9), minimal cardiopulmonary effects |
| 4–5×ED95 (rhesus) | NA | Yes | 2–3 min with l-cysteine (50 mg/kg) given 60 s after CW002 | |
| CW011 (Savarese et al. 2010; Boer and Carlos 2018) (0.025 mg/kg); not clinically used | 4–5×ED95 (rhesus) | NA | Yes |
20.8 min (clinical duration of action) 2–3 min with l-cysteine(50 mg/kg) reversal |