NEUROMUSCULAR BLOCKING DRUGS ›

DEPOLARISING

Suxamethonium chloride

(Succinylcholine chloride)

l DRUG ACTION Suxamethonium acts by mimicking

acetylcholine at the neuromuscular junction but

hydrolysis is much slower than for acetylcholine;

depolarisation is therefore prolonged, resulting in

neuromuscular blockade.

l INDICATIONS AND DOSE

Neuromuscular blockade (short duration) during surgery

and intubation

▶ BY INTRAVENOUS INJECTION

▶ Adult: 1–1.5 mg/kg

l UNLICENSED USE Doses of suxamethonium in BNF may

differ from those in product literature.

IMPORTANT SAFETY INFORMATION

Should only be administered by, or under the direct

supervision of, personnel experienced in its use.

l CONTRA-INDICATIONS Duchenne muscular dystrophy . family history of malignant hyperthermia . hyperkalaemia . low plasma-cholinesterase activity (including severe liver

disease). major trauma . neurological disease involving

acute wasting of major muscle . personal or family history

of congenital myotonic disease . prolonged immobilisation

(risk of hyperkalaemia). severe burns

l CAUTIONS Cardiac disease . neuromuscular disease .raised

intra-ocular pressure (avoid in penetrating eye injury). respiratory disease . severe sepsis (risk of hyperkalaemia)

l INTERACTIONS → Appendix 1: suxamethonium

l SIDE-EFFECTS

▶ Common or very common Arrhythmias . bradycardia (may

occur with repeated doses) . flushing . muscle contractions

involuntary . myoglobinaemia . myoglobinuria . post

procedural muscle pain .rash

▶ Rare or very rare Apnoea . cardiac arrest. hypersensitivity . malignant hyperthermia .respiratory disorders .trismus

SIDE-EFFECTS, FURTHER INFORMATION Premedication with

atropine reduces bradycardia associated with

suxamethonium use.

l ALLERGY AND CROSS-SENSITIVITY Allergic cross-reactivity

between neuromuscular blocking drugs has been reported;

caution is advised in cases of hypersensitivity to these

drugs.

l PREGNANCY Mildly prolonged maternal neuromuscular

blockade may occur.

l BREAST FEEDING Unlikely to be present in breast milk in

significant amounts (ionised at physiological pH). Breastfeeding may be resumed once the mother recovered from

neuromuscular block.

l HEPATIC IMPAIRMENT Manufacturer advises caution,

particularly in end stage hepatic failure (increased risk of

prolonged apnoea due to reduced hepatic synthesis of

plasma cholinesterase).

l MEDICINAL FORMS There can be variation in the licensing of

different medicines containing the same drug. Forms available

from special-order manufacturers include: solution for

injection

Solution for injection

▶ Suxamethonium chloride (Non-proprietary)

Suxamethonium chloride 50 mg per 1 ml Suxamethonium chloride

100mg/2ml solution for injection ampoules | 10 ampoule P £28.80–£50.00

▶ Anectine (Aspen Pharma Trading Ltd)

Suxamethonium chloride 50 mg per 1 ml Anectine 100mg/2ml

solution for injection ampoules | 5 ampoule P £3.57

NEUROMUSCULAR BLOCKING DRUGS ›

NON-DEPOLARISING

Non-depolarising f

neuromuscular blocking drugs

IMPORTANT SAFETY INFORMATION

Non-depolarising neuromuscular blocking drugs should

only be administered by, or under direct supervision of,

personnel experienced in their use, with adequate

training in anaesthesia and airway management.

l CAUTIONS Burns (resistance can develop, increased doses

may be required). cardiovascular disease (reduce rate of

administration). electrolyte disturbances (response

unpredictable). fluid disturbances (response

unpredictable). hypothermia (activity prolonged, lower

doses required). myasthenia gravis (activity prolonged,

lower doses required). neuromuscular disorders (response

unpredictable)

l SIDE-EFFECTS

▶ Common or very common Flushing . hypotension

▶ Uncommon Bronchospasm . hypersensitivity . skin

reactions

▶ Rare or very rare Muscle weakness . myopathy (after

prolonged use in intensive care)

l ALLERGY AND CROSS-SENSITIVITY Allergic cross-reactivity

between neuromuscular blocking drugs has been reported;

caution is advised in cases of hypersensitivity to these

drugs.

l PREGNANCY Non-depolarising neuromuscular blocking

drugs are highly ionised at physiological pH and are

therefore unlikely to cross the placenta in significant

amounts.

l BREAST FEEDING Non-depolarising neuromuscular

blocking drugs are ionised at physiological pH and are

unlikely to be present in milk in significant amounts.

Breast-feeding may be resumed once the mother has

recovered from neuromuscular block.

eiii F abovei

Atracurium besilate

(Atracurium besylate)

l INDICATIONS AND DOSE

Neuromuscular blockade (short to intermediate duration)

for surgery and intubation

▶ INITIALLY BY INTRAVENOUS INJECTION

▶ Adult: Initially 300–600 micrograms/kg, then (by

intravenous injection) 100–200 micrograms/kg as

required, alternatively (by intravenous injection)

initially 300–600 micrograms/kg, followed by (by

intravenous infusion) 300–600 micrograms/kg/hour

Neuromuscular blockade during intensive care

▶ INITIALLY BY INTRAVENOUS INJECTION

▶ Adult: Initially 300–600 micrograms/kg, initial dose is

optional, then (by intravenous infusion)

270–1770 micrograms/kg/hour; (by intravenous

infusion) usual dose 650–780 micrograms/kg/hour

DOSES AT EXTREMES OF BODY-WEIGHT

▶ To avoid excessive dosage in obese patients, dose

should be calculated on the basis of ideal body-weight.

l INTERACTIONS → Appendix 1: neuromuscular blocking

drugs, non-depolarising

BNF 78 Neuromuscular blockade 1337

Anaesthesia

15

l SIDE-EFFECTS

▶ Rare or very rare Cardiac arrest. circulatory collapse . shock

▶ Frequency not known Seizure

SIDE-EFFECTS, FURTHER INFORMATION Hypotension, skin

flushing, and bronchospasm is associated with histamine

release. Manufacturer advises minimising effects of

histamine release by administering over 1 minute in

patients with cardiovascular disease or sensitivity to

hypotension.

l DIRECTIONS FOR ADMINISTRATION For intravenous infusion

(Tracrium®; Atracurium besilate injection, Hospira;

Atracurium injection/infusion, Genus), give continuously

in Glucose 5% or Sodium Chloride 0.9%; stability varies

with diluent; dilute requisite dose with infusion fluid to a

concentration of 0.5–5 mg/mL.

l MEDICINAL FORMS There can be variation in the licensing of

different medicines containing the same drug.

Solution for injection

▶ Atracurium besilate (Non-proprietary)

Atracurium besilate 10 mg per 1 ml Atracurium besilate

250mg/25ml solution for injection vials | 1 vial P £16.50 (Hospital

only)

Atracurium besilate 25mg/2.5ml solution for injection ampoules | 5 ampoule P £9.25 (Hospital only) | 5 ampoule P £11.50 | 10 ampoule P £18.50 | 10 ampoule P £16.56 (Hospital only)

Atracurium besilate 50mg/5ml solution for injection ampoules | 5 ampoule P £17.50 (Hospital only) | 5 ampoule P £17.50 | 10 ampoule P £35.00 | 10 ampoule P £30.04 (Hospital only)

▶ Tracrium (Aspen Pharma Trading Ltd)

Atracurium besilate 10 mg per 1 ml Tracrium 250mg/25ml solution

for injection vials | 2 vial P £25.81

Tracrium 25mg/2.5ml solution for injection ampoules | 5 ampoule P £8.28

Tracrium 50mg/5ml solution for injection ampoules | 5 ampoule P £15.02

eiiiF 1337i

Cisatracurium

l INDICATIONS AND DOSE

Neuromuscular blockade (intermediate duration) during

surgery and intubation

▶ INITIALLY BY INTRAVENOUS INJECTION

▶ Adult: Initially 150 micrograms/kg, then (by

intravenous injection) maintenance 30 micrograms/kg

every 20 minutes, alternatively (by intravenous

infusion) initially 180 micrograms/kg/hour, then (by

intravenous infusion) maintenance

60–120 micrograms/kg/hour, maintenance dose

administered after stabilisation

Neuromuscular blockade (intermediate duration) during

intensive care

▶ INITIALLY BY INTRAVENOUS INJECTION

▶ Adult: Initially 150 micrograms/kg, initial dose is

optional, then (by intravenous infusion)

180 micrograms/kg/hour, adjusted according to

response; (by intravenous infusion) usual dose

30–600 micrograms/kg/hour

DOSES AT EXTREMES OF BODY-WEIGHT

▶ To avoid excessive dosage in obese patients, dose

should be calculated on the basis of ideal body-weight.

l INTERACTIONS → Appendix 1: neuromuscular blocking

drugs, non-depolarising

l SIDE-EFFECTS

▶ Common or very common Bradycardia

l DIRECTIONS FOR ADMINISTRATION For intravenous infusion

(Nimbex ®, Nimbex Forte ®), give continuously in Glucose

5% or Sodium Chloride 0.9%; solutions of 2 mg/mL and

5 mg/mL may be infused undiluted; alternatively dilute

with infusion fluid to a concentration of 0.1–2 mg/mL.

l MEDICINAL FORMS There can be variation in the licensing of

different medicines containing the same drug.

Solution for injection

▶ Cisatracurium (Non-proprietary)

Cisatracurium (as Cisatracurium besilate) 2 mg per

1 ml Cisatracurium besilate 20mg/10ml solution for injection

ampoules | 5 ampoule P £37.75 (Hospital only) |

5 ampoule P £32.09–£37.75 | 10 ampoule P £75.50

Cisatracurium besilate 20mg/10ml solution for injection vials | 5 vial P £37.75 (Hospital only) | 5 vial P £35.86

Cisatracurium (as Cisatracurium besilate) 5 mg per

1 ml Cisatracurium besilate 150mg/30ml solution for injection vials | 1 vial P £45.00 (Hospital only) | 1 vial P £26.43–£29.54

▶ Nimbex (Aspen Pharma Trading Ltd)

Cisatracurium (as Cisatracurium besilate) 2 mg per 1 ml Nimbex

20mg/10ml solution for injection ampoules | 5 ampoule P £37.75

Cisatracurium (as Cisatracurium besilate) 5 mg per 1 ml Nimbex

Forte 150mg/30ml solution for injection vials | 1 vial P £31.09

eiiiF 1337i

Mivacurium

l INDICATIONS AND DOSE

Neuromuscular blockade (short duration) during surgery

and intubation

▶ INITIALLY BY INTRAVENOUS INJECTION

▶ Adult: 70–250 micrograms/kg; (by intravenous

injection) maintenance 100 micrograms/kg every

15 minutes, alternatively (by intravenous infusion)

maintenance 8–10 micrograms/kg/minute, (by

intravenous infusion) adjusted in steps of

1 microgram/kg/minute every 3 minutes if required;

(by intravenous infusion) usual dose

6–7 micrograms/kg/minute

DOSES AT EXTREMES OF BODY-WEIGHT

▶ To avoid excessive dosage in obese patients, dose

should be calculated on the basis of ideal body-weight.

l CAUTIONS Burns (low plasma cholinesterase activity; dose

titration required). elderly

l INTERACTIONS → Appendix 1: neuromuscular blocking

drugs, non-depolarising

l SIDE-EFFECTS

▶ Uncommon Tachycardia

l HEPATIC IMPAIRMENT

Dose adjustments Reduce dose in severe impairment.

l RENAL IMPAIRMENT

Dose adjustments Clinical effect prolonged in renal

failure—reduce dose according to response.

l DIRECTIONS FOR ADMINISTRATION For intravenous

infusion, give continuously in Glucose 5% or Sodium

chloride 0.9%. Dilute to a concentration of

500 micrograms/mL; may also be given undiluted. Doses

up to 150 micrograms/kg may be given over 5–15 seconds,

higher doses should be given over 30 seconds. In asthma,

cardiovascular disease or in those sensitive to reduced

arterial blood pressure, give over 60 seconds.

l MEDICINAL FORMS There can be variation in the licensing of

different medicines containing the same drug.

Solution for injection

▶ Mivacron (Aspen Pharma Trading Ltd)

Mivacurium (as Mivacurium chloride) 2 mg per 1 ml Mivacron

10mg/5ml solution for injection ampoules | 5 ampoule P £13.95

Mivacron 20mg/10ml solution for injection ampoules | 5 ampoule P £22.57

1338 Anaesthesia adjuvants BNF 78

Anaesthesia

15

eiiiF 1337i

Pancuronium bromide

l INDICATIONS AND DOSE

Neuromuscular blockade (long duration) during surgery

and intubation

▶ BY INTRAVENOUS INJECTION

▶ Adult: Initially 100 micrograms/kg, then

20 micrograms/kg as required

Neuromuscular blockade (long duration) during intensive

care

▶ BY INTRAVENOUS INJECTION

▶ Adult: Initially 100 micrograms/kg, initial dose is

optional, then 60 micrograms/kg every 60–90 minutes

DOSES AT EXTREMES OF BODY-WEIGHT

▶ To avoid excessive dosage in obese patients, dose

should be calculated on the basis of ideal body-weight.

l INTERACTIONS → Appendix 1: neuromuscular blocking

drugs, non-depolarising

l SIDE-EFFECTS Apnoea . arrhythmia . hypersalivation . increased cardiac output. miosis

SIDE-EFFECTS, FURTHER INFORMATION Pancuronium lacks

histamine-releasing effect, but vagolytic and

sympathomimetic effects can cause tachycardia.

l HEPATIC IMPAIRMENT Possibly slower onset, higher dose

requirement, and prolonged recovery time.

l RENAL IMPAIRMENT Use with caution; prolonged duration

of block.

l MEDICINAL FORMS There can be variation in the licensing of

different medicines containing the same drug.

Solution for injection

▶ Pancuronium bromide (Non-proprietary)

Pancuronium bromide 2 mg per 1 ml Pancuronium bromide

4mg/2ml solution for injection ampoules | 10 ampoule P £50.00

(Hospital only)

eiiiF 1337i

Rocuronium bromide

l INDICATIONS AND DOSE

Neuromuscular blockade (intermediate duration) during

surgery and intubation

▶ INITIALLY BY INTRAVENOUS INJECTION

▶ Adult: Initially 600 micrograms/kg; (by intravenous

injection) maintenance 150 micrograms/kg,

alternatively (by intravenous infusion) maintenance

300–600 micrograms/kg/hour, adjusted according to

response

▶ Elderly: Initially 600 micrograms/kg; (by intravenous

injection) maintenance 75–100 micrograms/kg,

alternatively (by intravenous infusion) maintenance up

to 400 micrograms/kg/hour, adjusted according to

response

Neuromuscular blockade (intermediate duration) during

intensive care

▶ INITIALLY BY INTRAVENOUS INJECTION

▶ Adult: Initially 600 micrograms/kg, initial dose is

optional; (by intravenous infusion) maintenance

300–600 micrograms/kg/hour for first hour, then (by

intravenous infusion), adjusted according to response

DOSES AT EXTREMES OF BODY-WEIGHT

▶ To avoid excessive dosage in obese patients, dose

should be calculated on the basis of ideal body-weight.

l INTERACTIONS → Appendix 1: neuromuscular blocking

drugs, non-depolarising

l SIDE-EFFECTS

▶ Uncommon Procedural complications .tachycardia

▶ Rare or very rare Angioedema . circulatory collapse . face

oedema . malignant hyperthermia . paralysis . shock

l HEPATIC IMPAIRMENT

Dose adjustments Reduce dose.

l RENAL IMPAIRMENT

Dose adjustments Reduce maintenance dose; prolonged

paralysis.

l DIRECTIONS FOR ADMINISTRATION For continuous

intravenous infusion or via drip tubing, may be diluted with

Glucose 5% or Sodium Chloride 0.9%.

l MEDICINAL FORMS There can be variation in the licensing of

different medicines containing the same drug.

Solution for injection

▶ Rocuronium bromide (Non-proprietary)

Rocuronium bromide 10 mg per 1 ml Rocuronium bromide

50mg/5ml solution for injection ampoules | 10 ampoule P £24.00

Rocuronium bromide 50mg/5ml solution for injection vials |

10 vial P £28.00–£36.50 | 10 vial P £28.00 (Hospital only)

Rocuronium bromide 100mg/10ml solution for injection vials | 10 vial P £57.00–£73.00 | 10 vial P £57.00 (Hospital only)

▶ Esmeron (Merck Sharp & Dohme Ltd)

Rocuronium bromide 10 mg per 1 ml Esmeron 50mg/5ml solution

for injection vials | 10 vial P £28.92 (Hospital only)

1.2 Neuromuscular blockade

reversal

Neuromuscular blockade reversal

Neuromuscular blockade reversal

Anticholinesterases

Anticholinesterases reverse the effects of the nondepolarising (competitive) neuromuscular blocking drugs

such as pancuronium bromide but they prolong the action of

the depolarising neuromuscular blocking drug

suxamethonium chloride.

Neostigmine is used specifically for reversal of nondepolarising (competitive) blockade. It acts within one

minute of intravenous injection and its effects last for 20 to

30 minutes; a second dose may then be necessary.

Glycopyrronium bromide p. 1335 or alternatively atropine

sulfate p. 1334, given before or with neostigmine, prevent

bradycardia, excessive salivation, and other muscarinic

effects of neostigmine.

Other drugs for reversal of neuromuscular blockade

Sugammadex p. 1340 is a modified gamma cyclodextrin that

can be used for rapid reversal of neuromuscular blockade

induced by rocuronium bromide or vecuronium bromide. In

practice, sugammadex is used mainly for rapid reversal of

neuromuscular blockade in an emergency.

ANTICHOLINESTERASES

Neostigmine with glycopyrronium

bromide

The properties listed below are those particular to the

combination only. For the properties of the components

please consider, neostigmine p. 1125, glycopyrronium

bromide p. 1335.

l INDICATIONS AND DOSE

Reversal of non-depolarising neuromuscular blockade

▶ BY INTRAVENOUS INJECTION

▶ Adult: 1–2 mL, repeated if necessary, alternatively

0.02 mL/kilogram, repeated if necessary; maximum

2 mL per course

BNF 78 Neuromuscular blockade reversal 1339

Anaesthesia

15

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