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Pharmacology · Topic 66 of 110

Muscle Relaxants (Baclofen, Cyclobenzaprine, Dantrolene)

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Pharmacology · muscle relaxants

Muscle Relaxants (Baclofen, Cyclobenzaprine, Dantrolene)

(Cyclobenzaprine, methocarbamol, carisoprodol, baclofen, tizanidine, dantrolene) Relieve acute muscle spasm or control chronic spasticity. The dangers are sedation, baclofen withdrawal and dantrolene liver toxicity.

01 · Never do thisNever stop baclofen abruptly: taper the dose
02 · Boxed warningOral dantrolene: liver toxicity, check LFTs
03 · All of themSedation, dizziness: no alcohol, fall precautions
01

Used for · don't give

Used for

Acute spasm, short term: cyclobenzaprine, methocarbamol, carisoprodol
Chronic spasticity (MS, spinal cord injury): baclofen, tizanidine, dantrolene
Malignant hyperthermia: IV dantrolene is the antidote

Don't give

Cyclobenzaprine: acute recovery after MI, dysrhythmias, heart block
Cyclobenzaprine: heart failure, hyperthyroidism
Cyclobenzaprine: with an MAOI or within 14 days of one
Tizanidine: with ciprofloxacin or fluvoxamine

Oral dantrolene is contraindicated in active liver disease such as hepatitis or cirrhosis. Ciprofloxacin and fluvoxamine are CYP1A2 inhibitors: they raise tizanidine levels and cause severe hypotension and sedation.

02

How it works

Two jobs: short-term relief of acute spasm, or control of chronic spasticity

Cyclobenzaprine is closely related to tricyclic antidepressants
Tizanidine is an alpha-2 agonist, so it can cause hypotension
Dantrolene acts directly on skeletal muscle, unlike the centrally acting drugs
Baclofen is cleared by the kidneys
03

Side effects

Every muscle relaxant causes sedation and dizziness

Sedation, dizziness — all muscle relaxants
Cyclobenzaprine: dry mouth, urinary retention (anticholinergic effects)
Tizanidine: hypotension
Dantrolene: muscle weakness, drowsiness
Liver toxicity: oral dantrolene (boxed warning), tizanidine
Serotonin syndrome risk: cyclobenzaprine with SSRIs, SNRIs, tricyclics, tramadol
Misuse and dependence: carisoprodol (Schedule IV)
04

Labs & monitoring

Oral dantrolene: expect baseline and ongoing liver function tests
Tizanidine: expect aminotransferase monitoring
Tizanidine: monitor blood pressure
Baclofen in kidney disease: caution, possible dose reduction
Older adults: generally avoid carisoprodol, cyclobenzaprine, methocarbamol

The Beers list names those three because of sedation, anticholinergic effects and fracture risk.

05

Red flags

Baclofen stopped abruptly: hallucinations, seizures, high fever report now
Intrathecal baclofen lost: high fever, altered mental status, rigidity hospital now
Jaundice or dark urine on dantrolene report now
Signs of liver injury on tizanidine report now
Tizanidine ordered with ciprofloxacin or fluvoxamine contraindicated
Cyclobenzaprine ordered with an MAOI or within 14 days contraindicated
06

Giving it

Taper baclofen always, tizanidine after long-term or high-dose use

Baclofentaper the dose
baclofen

Taper it; never stop abruptly. Withdrawal also brings altered mental status and rebound spasticity.

Pumpnever miss a refill
intrathecal baclofen

Never miss a refill. Sudden loss is an emergency requiring immediate hospital evaluation.

Tizanidinetaper after long use
tizanidine

Taper after long-term or high-dose use. An abrupt stop can cause rebound hypertension, tachycardia and hypertonia.

Cyclobenzaprineshort term
cyclobenzaprine

Short term, with rest and physical therapy. Screen for an MAOI and for cardiac contraindications first.

Carisoprodolmisuse risk
carisoprodol

Schedule IV. Abrupt withdrawal after prolonged use can cause insomnia, vomiting, tremor, anxiety and hallucinations.

IV dantrolenethe antidote
dantrolene

The antidote for malignant hyperthermia. It is highly alkaline, so check the IV site often.

More detail
Short-term limitcyclobenzaprine and carisoprodol up to 2 or 3 weeks; older adults start cyclobenzaprine at a lower dose
IV dantrolene extravasationcan cause tissue necrosis; check the IV site for pain, redness and swelling
Dantrolene liver riskgreater at higher doses, in women, in clients over 35, and with other medications
Oral dantrolene, no benefitstopped if no benefit appears within 45 days, which limits unnecessary liver risk
Dantrolene and sunmay cause photosensitivity; teach the client to limit sun exposure
Early intrathecal baclofen withdrawalcan begin with returning spasticity, pruritus, hypotension and paresthesias
Intrathecal baclofen overdosedrowsiness, lightheadedness, respiratory depression, seizures, progression to coma
Baclofen and epilepsycan worsen seizure control
Baclofen in older adults2023 Beers: with eGFR under 60 mL/min, avoid because of encephalopathy risk
Tizanidine consistencyalways with or always without food; do not switch between tablets and capsules
07

Nursing priorities

Never stop baclofen abruptly: the dose is tapered
Intrathecal baclofen pump: never miss a refill; sudden loss is an emergency
Oral dantrolene: baseline and ongoing LFTs; report jaundice or dark urine
Every muscle relaxant: fall precautions and no CNS depressants
Check interactions: cyclobenzaprine with MAOIs, tizanidine with ciprofloxacin
08

Acute spasm or chronic spasticity?

Acute spasmChronic spasticity
DrugsCyclobenzaprine, methocarbamol, carisoprodolBaclofen, tizanidine, dantrolene
Used forShort term, with rest and physical therapySpasticity, as in MS or spinal cord injury
Signature ruleOlder adults generally avoid these (Beers list)Never stop baclofen abruptly
Stopping itCarisoprodol: withdrawal after prolonged useTaper baclofen; taper tizanidine after long-term or high-dose use
09

Teach your patient

No alcohol or other CNS depressants
No driving until you know how the drug affects you
Use fall precautions
Baclofen: never stop it abruptly; the dose is tapered
Baclofen pump: never miss a refill; high fever or altered mental status: hospital now
Dantrolene: report jaundice or dark urine
Tizanidine: rise slowly
Pearl

Never stop baclofen abruptly, and never let an intrathecal pump miss a refill — sudden loss with high fever, altered mental status and rigidity is an emergency.

Sources · Baclofen oral suspension label (DailyMed) · Gablofen, intrathecal baclofen label (DailyMed) · Cyclobenzaprine tablets label (DailyMed) · Tizanidine tablets label (DailyMed) · Carisoprodol tablets label (DailyMed) · Dantrium, dantrolene capsules label (DailyMed) · Dantrolene for injection label (DailyMed) · 2023 AGS Beers Criteria (J Am Geriatr Soc) · Cyclobenzaprine (StatPearls) · Methocarbamol (StatPearls) · Dantrolene (LiverTox) · Dantrolene (StatPearls) · Follow your facility's protocol for muscle relaxant administration.

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