Reversal agent
Sugammadex (Bridion)
Also called Bridion
Indications
- Reversal of rocuronium or vecuronium block after surgery, from moderate (second twitch back) to deep (1–2 post-tetanic counts)
- Immediate reversal about 3 min after an RSI dose of rocuronium when intubation and ventilation fail; it does not relieve upper airway obstruction
- Children from birth (approved 2024); immediate reversal has not been studied in children
- Reversal of rocuronium or vecuronium in the ICU for extubation or a neurologic examination (off-label)
- Rocuronium anaphylaxis unresponsive to epinephrine, as an adjunct (off-label; anecdotal evidence)
Dosing
| Where | Dose |
|---|---|
| Reversal and antidotes | Sugammadex: 2–4 mg/kg routine; 16 mg/kg right after rocuronium |
On the quick cards
Mechanism of action
Sugammadex is a modified γ-cyclodextrin: a ring of eight glucose units with a lipophilic cavity and a hydrophilic outside, whose eight negatively charged carboxyethyl-thio side chains deepen the cavity and attract the blocker's positively charged nitrogen. It encapsulates the steroid nucleus of rocuronium or vecuronium in a tight 1:1 complex held by van der Waals forces, hydrogen bonds and hydrophobic interactions. Free blocker in plasma falls almost to zero, so blocker leaves the receptors and the junction down its concentration gradient and is captured in turn. It does not act on acetylcholinesterase or receptors, so no anticholinergic is needed.
Pharmacology
- Neuromuscular: median time to train-of-four 0.9 is 2.2 min from moderate rocuronium block and 2.7 min (vecuronium 3.3) from deep block; affinity rocuronium > vecuronium >> pancuronium
- Cardiovascular: marked bradycardia, sometimes progressing to cardiac arrest, within minutes of a dose; otherwise no muscarinic effects
- Hematologic: aPTT and PT/INR rise up to 25% for up to 1 h
- Endocrine: binds progestogens, lowering hormonal contraceptive exposure
- Other: signs of light anesthesia (movement, coughing, grimacing) as the paralysis lifts
Pharmacokinetics
| Onset | Reversal within about 2–3 min; after 16 mg/kg given 3 min after rocuronium 1.2 mg/kg, the first twitch recovered to 10% at 4.4 min from the rocuronium dose, vs 7.1 min for spontaneous recovery from succinylcholine 1 mg/kg |
|---|---|
| Duration | The complex stays intact until excreted; recurrence is rare unless the dose was too small or another drug displaces the blocker |
| Half-life | About 2 h; 4, 6 and 19 h in mild, moderate and severe kidney impairment |
| Distribution | Vd 11–14 L (extracellular fluid) |
| Protein binding | None, for the drug or the complex |
| Metabolism | None detected |
| Clearance | About 88 mL/min |
| Elimination | Unchanged in urine with the captured blocker: over 90% within 24 h, 96% in total |
| Kidney failure | Not recommended at CrCl under 30 mL/min; high-flux hemodialysis removes about 70% over 3–6 h, low-flux does not |
| Re-paralysis | After up to 4 mg/kg, wait 5 min before rocuronium 1.2 mg/kg and 4 h before rocuronium 0.6 or vecuronium 0.1 mg/kg (24 h with mild or moderate kidney impairment); after 16 mg/kg wait 24 h, or use a nonsteroidal blocker |
Chemistry
- Octakis-S-(2-carboxyethyl)-octathio-γ-cyclodextrin, octasodium salt (molecular weight 2,178): eight D-glucopyranose units, each carrying a carboxyethyl-thio arm on carbon 6; one defined molecule, so stereoisomers do not arise
- Highly water soluble; the cavity is lipophilic and the rim negatively charged, which fits the quaternary nitrogen of aminosteroids
- Binds rocuronium about three times more tightly than vecuronium; forms no complex with succinylcholine or benzylisoquinoliniums; toremifene can displace the blocker
- 100 mg/mL clear solution, pH 7–8, osmolality 300–500 mOsm/kg, in 2 mL and 5 mL single-dose vials; store at room temperature protected from light (use within 5 days if not)
Adverse effects and cautions
In the one-pagers
- Myasthenic Crisis and Guillain-Barré SyndromeNIV or intubation: MG: resists succinylcholine; deep, long block with rocuronium, so less drug, train-of-four, sugammadex
- Airway and RSIRSI drugs: Sugammadex reverses rocuronium or vecuronium; 16 mg/kg reverses rocuronium immediately. Watch for anaphylaxis, bradycardia; backup contraception for 7 days.
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Sources
- FDA label: Bridion (2026)
- Nag 2013 (sugammadex review)
- PubChem: sugammadex
For education and exam preparation only. Follow your institution’s protocols. Typical adult values for study. Follow the order, the label and your institution's protocols.