Flexeril: Targeted Muscle Spasm Relief for Enhanced Mobility
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Flexeril (cyclobenzaprine hydrochloride) is a centrally acting skeletal muscle relaxant indicated as an adjunct to rest and physical therapy for the relief of muscle spasm associated with acute, painful musculoskeletal conditions. It works by acting primarily within the central nervous system at the brainstem to reduce tonic somatic motor activity, influencing both gamma and alpha motor neurons. While it does not directly relax skeletal muscles, its therapeutic effect is believed to result from its sedative properties and its ability to reduce the intensity of muscle spasms of local origin without interfering with muscle function. Clinical efficacy is typically observed within the first few days of therapy, providing patients with meaningful relief that supports rehabilitation efforts.
Features
- Active ingredient: Cyclobenzaprine hydrochloride
- Available in 5 mg and 7.5 mg oral tablets
- Bioavailability: Approximately 55%
- Half-life: 18 hours (range 8–37 hours) for immediate-release formulation
- Metabolism: Primarily hepatic via CYP3A4 and CYP1A2 isoenzymes
- Excretion: Primarily renal (60%) and fecal (30%)
- Onset of action: Typically within 1 hour
- Peak plasma concentration: 3–8 hours post-administration
Benefits
- Rapid relief from acute muscle spasms, allowing for improved range of motion
- Reduction of local pain and tenderness associated with musculoskeletal conditions
- Facilitation of physical therapy and rehabilitation through decreased muscle hypertonicity
- Short-term adjunctive therapy that complements rest and other conservative measures
- Demonstrated efficacy in clinical trials for conditions involving skeletal muscle spasm
- Minimal interference with neuromuscular transmission at therapeutic doses
Common use
Flexeril is primarily prescribed for the short-term management of muscle spasm associated with acute, painful musculoskeletal conditions. This includes but is not limited to muscle strains, sprains, and injuries resulting from trauma or overexertion. It is commonly used in cases of acute low back pain with muscle spasm, whiplash injuries, and post-surgical muscle guarding. The medication is typically employed as part of a comprehensive treatment plan that includes rest, physical therapy, and other analgesics as needed. It is important to note that Flexeril is not indicated for the treatment of spasticity associated with cerebral or spinal cord diseases, or in children.
Dosage and direction
The recommended dosage of Flexeril for most adults is 5 mg three times daily. Based on individual patient response and tolerance, the dosage may be increased to 7.5 mg or 10 mg three times daily. The maximum recommended dose is 30 mg per day (10 mg three times daily) for no more than two or three weeks. Tablets should be swallowed whole with water and may be taken with or without food. Administration with food may help minimize potential gastrointestinal upset. The medication should be used for the shortest duration consistent with individual patient treatment goals, generally not exceeding three weeks due to insufficient evidence of effectiveness for longer periods and because muscle spasm associated with acute musculoskeletal conditions is generally transient.
Precautions
Patients should be cautioned about engaging in activities requiring mental alertness, such as operating machinery or driving, as Flexeril may cause drowsiness. Concurrent use with alcohol or other CNS depressants should be avoided due to additive sedative effects. Use with caution in patients with mild hepatic impairment; contraindicated in moderate to severe hepatic impairment. Elderly patients may be more sensitive to the effects of cyclobenzaprine and may require lower dosing. Flexeril may enhance the effects of other anticholinergic drugs. Abrupt discontinuation after prolonged use may produce withdrawal symptoms including nausea, headache, and malaise, though this is uncommon with short-term use.
Contraindications
Flexeril is contraindicated in patients hypersensitive to cyclobenzaprine hydrochloride or any component of the formulation. Concurrent use with monoamine oxidase inhibitors (MAOIs) or within 14 days of their discontinuation due to risk of hypertensive crisis, hyperpyrexia, and seizures. Contraindicated in patients with hyperthyroidism, recent myocardial infarction, cardiac arrhythmias including heart block, congestive heart failure, or other significant cardiac disease. Not recommended in patients with moderate to severe hepatic impairment. Should not be used in recovery phase of myocardial infarction. Contraindicated in patients with urinary retention, angle-closure glaucoma, or increased intraocular pressure.
Possible side effect
Common adverse reactions (≥3%) include drowsiness (29–39%), dry mouth (21–32%), dizziness (6–11%), and fatigue (6%). Less frequent side effects may include headache, nervousness, confusion, nausea, constipation, dyspepsia, unpleasant taste, blurred vision, and tachycardia. Rare but serious adverse effects may include allergic reactions, hepatitis, seizures, and serotonin syndrome (especially when used with other serotonergic drugs). Elderly patients may experience hallucinations, confusion, and sedation more frequently. Most side effects are dose-related and may diminish with continued therapy or dose reduction.
Drug interaction
Flexeril has significant interactions with several medication classes. Concomitant use with MAO inhibitors is absolutely contraindicated. Enhanced sedative effects occur with alcohol, benzodiazepines, opioids, and other CNS depressants. May potentiate anticholinergic effects when used with other anticholinergic medications. Cyclobenzaprine may interact with tramadol, increasing seizure risk. Serotonergic drugs (SSRIs, SNRIs, triptans) may increase risk of serotonin syndrome. CYP3A4 inhibitors (ketoconazole, clarithromycin) may increase cyclobenzaprine levels, while inducers (rifampin, carbamazepine) may decrease efficacy. Use with guanethidine may reduce its antihypertensive effect.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next scheduled dose. In that case, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed one. Patients should be advised to maintain a consistent dosing schedule to ensure optimal therapeutic effect while minimizing side effects. If multiple doses are missed, consultation with a healthcare provider is recommended before resuming therapy.
Overdose
Cyclobenzaprine overdose may manifest as severe drowsiness, tachycardia, tremor, agitation, confusion, hallucinations, and cardiac arrhythmias. Severe overdose may lead to coma, cardiac arrest, and death. Management involves immediate medical attention with supportive care including gastric lavage if presented early, activated charcoal, and careful monitoring of cardiac and respiratory function. Treatment is symptomatic and supportive with particular attention to maintaining adequate airway and cardiovascular function. There is no specific antidote for cyclobenzaprine overdose. Dialysis is unlikely to be beneficial due to high protein binding and extensive tissue distribution.
Storage
Store Flexeril tablets at controlled room temperature 20°–25°C (68°–77°F) with excursions permitted between 15°–30°C (59°–86°F). Keep in the original container with the lid tightly closed to protect from moisture and light. Keep out of reach of children and pets. Do not store in bathroom cabinets where moisture levels may fluctuate. Properly discard any medication that is outdated or no longer needed through medication take-back programs or according to FDA guidelines.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Flexeril is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Individual response to medication may vary, and only a healthcare provider can determine the appropriate treatment based on a patient’s specific medical condition, history, and current medications. Patients should not discontinue or change their dosage without consulting their physician. Report any adverse effects to a healthcare provider promptly.
Reviews
Clinical studies demonstrate that Flexeril provides significant relief from muscle spasm within the first few days of treatment. In double-blind studies involving over 1400 patients, cyclobenzaprine showed superior efficacy to placebo in relieving muscle spasm and associated local pain and tenderness. Many patients report improved sleep quality due to reduced pain and muscle discomfort. However, the sedative effects are noted by some patients as limiting daytime functionality. Most clinical trials support the use of cyclobenzaprine for short-term management of acute musculoskeletal conditions, with optimal results achieved when combined with rest and physical therapy. Patient satisfaction is generally high when used appropriately for indicated conditions.