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Oral medications commonly used for spasticity

Oral medications commonly used for spasticity
Medication Mechanism Usual dosing Adverse effects
Age group Starting dose Titration Maximum dose
Baclofen Centrally acting, GABA-B agonist Adults 5 mg once daily 5 mg per dose every 3 to 7 days 80 mg per day; some patients may require up to 120 mg per day

Gastrointestinal: constipation, nausea, vomiting.

Genitourinary: urinary retention.

Neurologic: ataxia, confusion, dizziness, hypotonia, paresthesias, sedation, weakness.

A withdrawal syndrome (eg, seizures, hallucinations, rebound spasticity, high fever, hypertension) may occur with abrupt discontinuation.

Adolescents and children ≥8 years 5 mg 2 or 3 times daily 5 mg per dose every 7 days 60 mg per day; higher doses may be administered with close monitoring
Children 2 to <8 years 0.5 mg/kg per day in 2 or 3 divided doses (maximum: 2.5 mg/dose) 0.5 mg/kg per day every 7 days 2 mg/kg per day (40 mg per day; doses up to 60 mg per day have been reported)
Diazepam Centrally acting, GABA-A agonist Adults and adolescents >12 years 2 mg once or twice daily or 5 mg at bedtime May increase in increments of 2 to 5 mg per day every 7 days 40 to 60 mg per day in 3 or 4 divided doses

Neurologic: ataxia, cognitive impairment (eg, memory disturbances), dizziness, sedation.

Neuromuscular: asthenia.

Potential for dependence.

A withdrawal syndrome (eg, agitation, psychosis, seizures) may occur with abrupt discontinuation.

Children ≥6 months to 12 years 0.01 to 0.3 mg/kg in 2 to 4 divided doses (maximum: 2 mg/dose) May increase in increments of 0.1 to 0.3 mg/kg (maximum 10 mg) per day every 7 days 20 to 40 mg per day (not to exceed 10 mg per dose)
Dantrolene Peripherally acting, inhibits calcium release from sarcoplasmic reticulum of the muscle Adults, adolescents, and children (≥5 years) who weigh ≥50 kg 25 mg once daily Every 7 days as follows:
  • 25 mg 3 times daily, then
  • 50 mg 3 times daily, then
  • 100 mg 3 times daily

Some patients may require 100 mg 4 times daily

100 mg 4 times daily

Potentially irreversible hepatotoxicity requires regular monitoring; stop therapy if benefits are not evident within 45 days. Use the lowest dose associated with optimal response.

Gastrointestinal: diarrhea, nausea.

Neurologic: drowsiness, lethargy, paresthesias, weakness.

Adolescents and children (≥5 years) who weigh <50 kg 0.5 mg/kg/dose once or twice daily Every 7 days as follows:
  • 0.5 mg/kg/dose 3 times daily, then
  • 1 mg/kg/dose 3 times daily, then
  • 2 mg/kg/dose 3 times daily

Some patients may require 2 mg/kg/dose 4 times daily

2 mg/kg/dose 4 times daily (not to exceed 100 mg per dose or 400 mg per day)
Tizanidine Centrally acting, alpha-2 adrenergic agonist Adults

2 mg once daily at bedtime

For spasticity associated with certain comorbidities (eg, ALS, stroke), may start with 2 mg 2 to 3 times daily

May increase in increments of 2 to 4 mg per day every 3 to 7 days

36 mg per day in 3 or 4 divided doses

For patients with ALS, doses >24 mg per day may not confer additional benefit

Cardiovascular: hypotension.

Gastrointestinal: vomiting, xerostomia.

Hepatic: reversible elevation of transaminase, liver injury ranging from hepatitis to acute liver failure.

Neurologic: dizziness, drowsiness, fatigue, sedation, weakness.

A withdrawal syndrome (eg, dysthermia, hallucinations, hypertension, nausea, tremor, and tachycardia) may occur with abrupt discontinuation.

Adolescents and children ≥10 years 2 mg once daily at bedtime May increase in increments of 2 to 4 mg per day every 3 to 7 days 24 mg per day in 3 to 4 divided doses
Children 2 to <10 years 1 mg once daily at bedtime May increase in increments of 2 to 4 mg per day every 3 to 7 days 24 mg per day in 3 to 4 divided doses
Dosing in this table is for patients with normal kidney and liver function; for dose adjustments, refer to the drug monographs included with UpToDate. In general, titration stops once an effective dose is reached; not all individuals will require the maximum dose. Titration can be slowed if adverse effects develop. When discontinuing therapy, tapering is advised. Refer to UpToDate topic reviews for additional details on managing spasticity from specific syndromes.
ALS: amyotrophic lateral sclerosis; GABA: gamma-aminobutyric acid.
References:
  1. Oleszek JL, Davidson LT. Spasticity. In: Nelson Textbook of Pediatrics, 21st ed, Kliegman RM, St Geme JW III (Eds), Elsevier Health Sciences 2020. p.3760.
  2. Nair KPS, Marsden J. The management of spasticity in adults. BMJ 2014; 349:g4737.

Prepared with data from: UpToDate Lexidrug. More information available at https://online.lexi.com/.

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