lMEDICINAL FORMS
There can be variation in the licensing of different medicines
containing the same drug. Forms available from special-order
manufacturers include: oral solution
Solution for injection
▶Neostigmine (Non-proprietary)
Neostigmine metilsulfate 2.5 mg per 1 mlNeostigmine 2. 5 mg/ 1 ml
solution for injection ampoules| 10 ampouleP£ 5. 45 DT = £ 5. 45
Tablet
▶Neostigmine (Non-proprietary)
Neostigmine bromide 15 mgNeostigmine 15 mg tablets|
140 tabletP£ 120. 52 DT = £ 120. 52
eiiiiF 648
Pyridostigmine bromide
lDRUG ACTIONPyridostigmine bromide has weaker
muscarinic action than neostigmine.
lINDICATIONS AND DOSE
Myasthenia gravis
▶INITIALLY BY MOUTH
▶Neonate:Initially 1 – 1. 5 mg/kg, dose repeated
throughout the day, then (by mouth using immediate-
release medicines) increased if necessary up to 10 mg, to
be increased gradually and given 30 - 60 minutes before
feeds.▶Child 1 month–11 years:Initially 1 – 1. 5 mg/kg daily, then
(by mouth using immediate-release medicines)
increased to 7 mg/kg daily in 6 divided doses, to be
increased gradually; (by mouth using immediate-
release medicines) usual dose 30 – 360 mg daily in
divided doses
▶Child 12–17 years: 30 – 120 mg, dose repeated throughout
the day; (by mouth using immediate-release
medicines) usual dose 300 – 600 mg daily in divided
doses, consider immunosuppressant therapy if total
daily dose exceeds^360 mg, down-regulation of
acetylcholine receptors possible if total daily dose
exceeds 450 mglINTERACTIONS→Appendix 1 : pyridostigmine
lRENAL IMPAIRMENT
Dose adjustmentsReduce dose; excreted by kidney.
lMEDICINAL FORMS
There can be variation in the licensing of different medicines
containing the same drug. Forms available from special-order
manufacturers include: oral suspension, oral solution
Tablet
▶Pyridostigmine bromide (Non-proprietary)
Pyridostigmine bromide 60 mgPyridostigmine bromide 60 mg
tablets| 200 tabletP£ 45. 48 DT = £ 44. 02
▶Mestinon(Meda Pharmaceuticals Ltd)
Pyridostigmine bromide 60 mgMestinon 60 mg tablets|
200 tabletP£ 45. 57 DT = £ 44. 02
2.3 Spasticity
Other drugs used for SpasticityDantrolene sodium, p. 821.
Diazepam, p. 220MUSCLE RELAXANTS›CENTRALLY ACTING
Baclofen 21-Nov-2016
lINDICATIONS AND DOSE
Chronic severe spasticity of voluntary muscle
▶BY MOUTH
▶Child 1 month–7 years:Initially 300 micrograms/kg daily
in 4 divided doses, increased gradually at weeklyintervals until satisfactory response; maintenance
0. 75 – 2 mg/kg daily in divided doses, review treatment
if no benefit within 6 weeks of achieving maximum
dose; maximum^40 mg per day
▶Child 8–17 years:Initially 300 micrograms/kg daily in
4 divided doses, increased gradually at weekly intervals
until satisfactory response; maintenance 0. 75 – 2 mg/kg
daily in divided doses, review treatment if no benefit
within 6 weeks of achieving maximum dose; maximum
60 mg per day
Severe chronic spasticity of cerebral or spinal origin
unresponsive to oral antispastic drugs (or oral therapy
not tolerated) (specialist use only)
▶BY INTRATHECAL INJECTION
▶Child 4–17 years:Test dose 25 – 50 micrograms, to be
given over at least 1 minute via catheter or lumbar
puncture, then increased in steps of 25 micrograms
(max. per dose 100 micrograms), not more often than
every 24 hours to determine initial maintenance dose;
maintenance 25 – 200 micrograms daily, adjusted
according to response, dose-titration phase, most
often using infusion pump (implanted into chest wall
or abdominal wall tissues) to establish maintenance
dose retaining some spasticity to avoid sensation of
paralysisIMPORTANT SAFETY INFORMATION
Consult product literature for details on test dose and
titration—important to monitor patients closely in
appropriately equipped and staffed environment during
screening and immediately after pump implantation.
Resuscitation equipment must be available for
immediate use. Treatment with continuous pump-
administered intrathecal baclofen should be initiated
within 3 months of a satisfactory response to intrathecal
baclofen testing.lCONTRA-INDICATIONS
▶With intrathecal useLocal infection.systemic infection
▶With oral useAvoid oral route in active peptic ulceration
lCAUTIONS
GENERAL CAUTIONSDiabetes.epilepsy.history of peptic
ulcer.hypertonic bladder sphincter.psychiatric illness.
respiratory impairment
SPECIFIC CAUTIONS
▶With intrathecal useCoagulation disorders.malnutrition
(increased risk of post-surgical complications).previous
spinal fusion procedure
lINTERACTIONS→Appendix 1 : baclofen
lSIDE-EFFECTS
GENERAL SIDE-EFFECTS
▶Common or very commonAsthenia.confusion.
constipation.depression.diarrhoea.dizziness.
drowsiness.dry mouth.euphoric mood.hallucination.
headache.hyperhidrosis.hypotension.nausea.
paraesthesia.respiratory disorders.sexual dysfunction.
skin reactions.sleep disorders.urinary disorders.vision
disorders.vomiting
▶UncommonBradycardia.hypothermia.taste altered
▶Rare or very rareWithdrawal syndrome
SPECIFIC SIDE-EFFECTS
▶Common or very common
▶With intrathecal useAnxiety.appetite decreased.chills.
dyspnoea.fever.hypersalivation.neuromuscular
dysfunction.oedema.pain.pneumonia.seizure
▶With oral useGastrointestinal disorder.muscle weakness.
myalgiaBNFC 2018 – 2019 Spasticity 649
Musculoskeletal system10