Sugammadex (Bridion) is the first relaxant-binding agent. It is used to reverse the neuromuscular blockade caused by rocuronium and vecuronium.

Sugammadex Uses:

• Reversal of rocuronium or vecuronium:

  • Reversal of rocuronium or vecuronium-induced neuromuscular inhibition in adults after surgery

Sugammadex dose in Adults

Note:

• Dosing based on actual body weight.
• Doses and timing of administration are based on monitoring for twitch responses and the severity of spontaneous recovery that has occurred.

Sugammadex dose in the routine reversal of rocuronium- or vecuronium-induced blockade: IV:

• Deep block (at least 1 to 2 post-tetanic counts but prior to the appearance of T ):
  • 4 mg/kg as a single dose
• Moderate block (after the appearance of T ):
  • 2 mg/kg as a single dose

  • Re-administration of rocuronium or vecuronium:

    • Waiting durations for re-administration of rocuronium or vecuronium after sugammadex usage for routine reversal vary substantially, ranging from 5 minutes to 24 hours depending on the agent, dosage, and renal function (consult product labeling);
    • if an immediate neuromuscular blockade is needed, a nonsteroidal neuromuscular blocking agent may be required.

• Immediate reversal of rocuronium-induced blockade:

  • IV: at 16 mg/kg as a single dose administered soon (~3 minutes) after administration of a single dose of rocuronium at 1.2 mg/kg.
  • Note: This dose of sugammadex has not been tested and evaluated following the administration of vecuronium.

  • Re-administration of rocuronium or administration of vecuronium:

    • Following sugammadex use for an immediate reversal of rocuronium, wait 24 hours before re-administering rocuronium or administering vecuronium.
    • If more immediate neuromuscular blockade is needed, a nonsteroidal neuromuscular-blocking agent may be required.

Sugammadex dose in Children

Sugammdex Routine reversal of rocuronium-induced moderate blockade:

• Infants, Children, and Adolescents:

  • For ages less than 2 years, the data is very limited:
    • IV: 2 mg/kg as a single dose

Pregnancy Risk Category: B2

• In some studies on animal reproduction, adverse events were observed.
• There is limited information available about sugammadex's use to reverse rocuronium-induced neural blockade following cesarean section.
• Sugammadex administration may reduce the effects of hormonal contraception.
• For women who use oral or non-oral hormonal contraception, an additional nonhormonal contraceptive (eg condom, spermicide), should be used for seven days following a dose sugammadex.

Use Sugammadex while breastfeeding

• Sugammadex may or may not be absorbed into breast milk.
• According to the manufacturer of the breast-feeding device, the decision about whether to continue or stop breastfeeding during therapy should consider the risks to infants, the benefits to the mother, and the benefits to the mother.

Dose in Kidney Disease:

• CrCl 30 to 40 mL/minute

  • There is no need to adjust the dosage.
  • If necessary, you may re-administer sugammadex at a dose of 4 mg/kg after 24 hours.
  • Rocuronium 1.2 mg/kg can be given if a neuromuscular blocker agent must be re-administered sooner. (No dosing is recommended for vecuronium).

• CrCl 30 mL/minute

  • It is not advised.

• Dialysis

  • It is not advised.

Dose in Liver disease:

• The drug manufacturer's labeling does not contain any dosage adjustments (hasn't been studied).
• Use with caution, especially if you have severe edema or coagulopathy.

Common Side Effects of Sugammadex:

• Cardiovascular:

  • Hypotension

• Central nervous system:

  • Headache

• Gastrointestinal:

  • Nausea
  • Vomiting

• Local:

  • Pain at injection site

Less Common Side Effects of Sugammadex:

• Cardiovascular:

  • Hypertension
  • Prolonged QT Interval On ECG
  • Bradycardia
  • Tachycardia

• Central Nervous System:

  • Anesthesia Complication
  • Chills
  • Incisional Pain
  • Dizziness
  • Insomnia
  • Hypoesthesia
  • Anxiety
  • Restlessness
  • Depression

• Dermatologic:

  • Pruritus
  • Erythema

• Endocrine & Metabolic:

  • Hypocalcemia

• Gastrointestinal:

  • Abdominal Pain
  • Flatulence
  • Xerostomia

• Hematologic & Oncologic:

  • Wound Hemorrhage
  • Decreased Red Blood Cells

• Neuromuscular & Skeletal:

  • Limb Pain
  • Musculoskeletal Pain
  • Myalgia
  • Increased Creatine Phosphokinase
  • Neuromuscular Blockade

• Respiratory:

  • Cough

• Miscellaneous:

  • Fever
  • Procedural Complications
  • Hysterectomy

Contraindications to Sugammadex:

• Hypersensitivity to sugammadex and any component of the formulation

Warnings and precautions

• Bradycardia

  • Bradycardia marked and bradycardia without cardiac arrest have been reported. Usually, these cases were discovered within minutes of administration.
  • Pay attention to hemodynamic changes after and during neuromuscular blockade reversal.
  • If bradycardia is severe, you should seek appropriate pharmacologic treatment (e.g. atropine).

• Hypersensitivity

  • Uncommonly, severe hypersensitivity reactions including anaphylaxis or anaphylactic shock have been reported.
  • Patients may experience this even if they have not been exposed to sugammadex before.

• Recurrences of neuromuscular blockade

  • In controlled trials, recurrences of neuromuscular blockade have been reported. Usually, these were associated with suboptimal dosing.
  • After sugammadex has been reversed, it is important to continue monitoring your respiratory system and to ensure that adequate ventilator support is available after extubation.
  • For the possibility of recurrence, it is also important to consider the potential for neuromuscular blockade being induced by any other post-operative drugs.

• Cardiovascular disease

  • Patients with heart disease should exercise caution.

• Hepatic impairment

  • Patients with severe edema or coagulopathy should be treated with caution.

• Hemostasis impaired:

  • Patients with impaired hemostasis or at-risk (eg, coagulopathies or severe liver impairment) should be cautious.
  • We have observed dose-dependent transient increases of activated partial thromboplastin times (aPTT), and normalized prosthrombin times (PT [INR]).
  • Clinical trials did not show significant bleeding effects with low-dose sugammadex or when combined with therapeutic anticoagulation. Patients at high risk and those who received high-dose sugammadex were not properly studied.
  • It is important to monitor hemostatic and coagulation levels carefully.

• Renal impairment

  • Dialysis patients and those with severe renal impairment (CrCl 30 mL/min) are not advised to use this medicine.

Sugammadex: Drug Interaction

Monitoring parameters:

• Neuromuscular stimulation (eg post-tetanic count [PTC] or train-of-4 [TOF]).
• ECG monitoring during and after administration (for bradycardia).
• During recovery, respiratory function is important
• Monitor for anaphylaxis at least five minutes following administration.
• Select patients may have hemostatic or coagulation parameters that are not reported in clinically significant bleeding.

How to administer Sugammadex?

• IV: Give a rapid IV push for 10 seconds, according to the manufacturer.
• However, experts recommend slow IV push to decrease the chance of serious adverse events, such as bradycardia and asystole.
• If sugammadex is administered in the same IV as other products, flush it with saline immediately before and after administering it.

Mechanism of action of Sugammadex:

• Sugammadex, a modified Gamma Cyclodextrin that acts as a select relaxant binding agent, is known.
• It joins forces with rocuronium and vecuronium, two neuromuscular blockers, to generate a complex in the plasma that reduces the number of neuromuscular blockers that can bind to the nicotinic receptors at the neuromuscular junction.
• This has the opposite effect of rocuronium's and vecuronium's neuromuscular inhibition.

Onset:

• <3 minutes

Protein binding:

• Negligible

Metabolism:

• Not metabolized

Half-life elimination:

• Effective: ~2 hours; Prolonged in renal impairment:
• Mild renal impairment: 4 hours;
• Moderate renal impairment: 6 hours;
• Severe renal impairment: 19 hours

Excretion:

• Urine (95% as unchanged drug)

International Brands of Sugammadex:

• Bridion
• Inspiromadex

Sugammadex Brand Names in Pakistan:

No Brands Available in Pakistan.