cyclobenzaprine

Absorption: Well absorbed from the GI tract.

Distribution: Unknown.

Protein Binding: 93%.

Metabolism/Excretion: Mostly metabolized by the liver.

Half-Life: 1–3 days.

Time/Action Profile ⬆ ⬇

(skeletal muscle relaxation)

ROUTE	ONSET	PEAK‡	DURATION
PO	within 1 hr	3–8 hr	12–24 hr
Extended release	unknown	unknown	24 hr

‡Full effects may not occur for 1–2 wk.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Concurrent use of or use within 14 days of MAO inhibitor therapy;
Immediate period after MI;
Severe or symptomatic cardiovascular disease;
Cardiac conduction disturbances;
Hyperthyroidism.

Use Cautiously in:

Cardiovascular disease;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Children 15 yr (safety and effectiveness not established);
Geri: Appears on Beers list. risk of anticholinergic adverse reactions, sedation, and fractures in older adults. Avoid use in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: arrhythmias

EENT: dry mouth, blurred vision

GI: constipation, dyspepsia, nausea, unpleasant taste

GU: urinary retention

Neuro: dizziness, drowsiness, confusion, fatigue, headache, nervousness

Interactions ⬆ ⬇

Drug-drug:

Additive CNS depression with other CNS depressants, including alcohol, antihistamines, opioid analgesics, and sedative/hypnotics.
Additive anticholinergic effects with drugs possessing anticholinergic properties, including antihistamines, antidepressants, atropine, disopyramide, haloperidol, and phenothiazines.
Avoid use within 14 days of MAO inhibitors (hyperpyretic crisis, seizures, and death may occur).
Drugs that affect serotonergic neurotransmitter systems, including tricyclic antidepressants, SSRIs, SNRIs, fentanyl, buspirone, tramadol, and triptans↑ risk of serotonin syndrome.

Drug-Natural Products:

Concomitant use of kava-kava, valerian, chamomile, or hops can ↑ CNS depression.

Route/Dosage ⬆ ⬇

PO (Adults and Children ≥15 yo): Acute painful musculoskeletal conditions: Immediate-release: 10 mg 3 times daily (range 20–40 mg/day in 2–4 divided doses; not to exceed 60 mg/day); Extended-release: 15–30 mg once daily. Fibromyalgia: 5–40 mg at bedtime (unlabeled).

Availability ⬆ ⬇

(Generic available)

Immediate-release tablets: 5 mg; 7.5 mg; 10 mg
Extended-release capsules (Amrix): 15 mg; 30 mg

Assessment ⬆ ⬇

Assess patient for pain, muscle stiffness, and range of motion before and periodically during therapy.
Geri: Assess geriatric patients for anticholinergic effects (sedation and weakness).
Assess for serotonin syndrome (mental changes [agitation, hallucinations, coma], autonomic instability [tachycardia, labile BP, hyperthermia], neuromuscular aberrations [hyperreflexia, incoordination], and/or GI symptoms [nausea, vomiting, diarrhea]), especially in patients taking other serotonergic drugs (SSRIs, SNRIs, triptans).

Implementation ⬆ ⬇

PO: Administer doses at same time each day. May be administered with meals to minimize gastric irritation.
- DNC: Swallow extended-release capsules whole; do not open, crush, or chew. Capsules may be opened and contents sprinkled onto applesauce; swallow immediately without chewing. Rinse mouth to make sure contents have been swallowed.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed, at the same time each day; do not take more than the prescribed amount. Take missed doses within 1 hr of time ordered; otherwise, return to normal dose schedule. Do not double doses. Do not stop abruptly, may cause nausea, headache, and malaise; discontinue gradually.
Medication may cause drowsiness, dizziness, and blurred vision. Caution patient to avoid driving or other activities requiring alertness until response to drug is known.
Advise patient to avoid concurrent use of alcohol or other CNS depressants with this medication.
If constipation becomes a problem, advise patient that increasing fluid intake and bulk in diet and stool softeners may alleviate this condition.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any other Rx, OTC, or herbal products.
Advise patient to notify health care professional if symptoms of urinary retention (distended abdomen, feeling of fullness, overflow incontinence, voiding small amounts) occur.
Instruct patient to notify health care professional immediately if signs and symptoms of serotonin syndrome, irregular or abnormal heartbeat, fast heartbeat, or allergic reaction (difficulty breathing, hives, swelling of face or tongue, itching) occur.
Inform patient that good oral hygiene, frequent mouth rinses, and sugarless gum or candy may help relieve dry mouth.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇