Flexeril Cyclobenzaprine Hcl: Uses, Dosage, Side Effects, Interactions, Warning

Data sources include IBM Watson Micromedex (updated 3 Sep 2023), Cerner Multum™ (updated 28 Aug 2023), ASHP (updated 10 Aug 2023) and others. Cyclobenzaprine reduced or abolished skeletal muscle hyperactivity in several animal models. Animal studies indicate that cyclobenzaprine does not act at the neuromuscular junction or directly on skeletal muscle. Evidence suggests that the net effect picture of flexeril 5 mg of cyclobenzaprine is a reduction of tonic somatic motor activity, influencing both gamma (γ) and alpha (α) motor systems. As management of overdose is complex and changing, it is recommended that the physician contact a poison control center for current information on treatment. In patients with CNS depression, early intubation is advised because of the potential for abrupt deterioration.

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These patients are generally more susceptible to drugs with potentially sedating effects, including cyclobenzaprine. FLEXERIL should be used with caution in subjects with mild hepatic impairment starting with a 5 mg dose and titrating slowly upward. Due to the lack of data in subjects with more severe hepatic insufficiency, the use of FLEXERIL in subjects with moderate to severe impairment is not recommended.

Cyclobenzaprine

One study compared FLEXERIL 5 mg and 10 mg t.i.d. to placebo; and a second study compared FLEXERIL 5 mg and 2.5 mg t.i.d. to placebo. Primary endpoints for both trials were determined by patient-generated data and included global impression of change, medication helpfulness, and relief from starting backache. Each endpoint consisted of a score on a 5-point rating scale (from 0 or worst outcome to 4 or best outcome). The plasma concentration of cyclobenzaprine is increased in patients with hepatic impairment (see CLINICAL PHARMACOLOGY, Pharmacokinetics, Hepatic Impairment).

• The acute oral LD50 of FLEXERIL is approximately 338 and 425 mg/kg in mice and rats, respectively.
• Evidence suggests that the net effect of cyclobenzaprine is a reduction of tonic somatic motor activity, influencing both gamma (γ) and alpha (α) motor systems.
• In both cases, the patients took serotonergic medications (phenelzine and duloxetine) before starting cyclobenzaprine.[21] Clinicians should also monitor for vital signs, as cyclobenzaprine can cause reflex tachycardia.
• There is also evidence that cyclical antidepressants may decrease the seizure threshold by interfering with chloride conductance on the GABA receptor.
• Less frequent dosing should be considered for hepatically impaired or elderly patients (see PRECAUTIONS, Impaired Hepatic Function, and Use in the Elderly).

The incidence of drowsiness, the most frequent adverse reaction, was similar with both drugs. Concomitant use of monoamine oxidase (MAO) inhibitors or within 14 days after their discontinuation. Hyperpyretic crisis seizures, and deaths have occurred in patients receiving cyclobenzaprine (or structurally similar tricyclic antidepressants) concomitantly with MAO inhibitor drugs.

SIDE EFFECTS

Among the most dreaded toxicities linked with cyclical antidepressants, overdoses affect fast-acting sodium channels in the cardiac conduction system. Cyclical antidepressants block the cardiac sodium channel and cause prolongation of cardiac depolarization, which manifests as QRS widening on electrocardiograms. There is also evidence that cyclical antidepressants may decrease the seizure threshold by interfering with chloride conductance on the GABA receptor. It is available in immediate-release tabletsof 5 milligrams, 7.5 milligrams, and 10 milligrams and extended-release capsules of 15 milligrams and 30 milligrams and is usually given three times daily. The extended-release formulation should be administered at the same time each day. The capsule may be swallowed whole, but its contents also may be sprinkled onto a tablespoon of applesauce for immediate consumption without chewing the granules.

Multiple drug ingestion (including alcohol) is common in deliberate cyclobenzaprine overdose. As management of overdose is complex and changing, it is recommended that the physician contact a poison control center for current information on treatment. Signs and symptoms of toxicity may develop rapidly after cyclobenzaprine overdose; therefore, hospital monitoring is required as soon as possible. The acute oral LD50 of FLEXERIL is approximately 338 and 425 mg/kg in mice and rats, respectively. The plasma concentration of cyclobenzaprine is increased in the elderly (see CLINICAL PHARMACOLOGY, Pharmacokinetics, Elderly).

Clinicians should monitor for signs and symptoms of serotonin syndrome if the patient is taking other serotonergic drugs. In two case reports, the authors described patients who quickly developed serotonin syndrome after initiating cyclobenzaprine in the short term. In both cases, the patients took serotonergic medications (phenelzine and duloxetine) before starting cyclobenzaprine.[21] Clinicians should also monitor for vital signs, as cyclobenzaprine can cause reflex tachycardia.

In case of acute cyclobenzaprine overdose, emergency medicine physicians and triage nurses should stabilize the patient. If EKG demonstrates QRS prolongation, the clinician should initiate sodium bicarbonate therapy. In severe overdose, ventricular arrhythmias and seizures may require MICU-level of care under the supervision of a critical care physician. As discussed above, the clinician should consider contacting the poison control center in refractory cases. A psychiatrist consult is required for deliberate poisoning of cyclobenzaprine.

For most patients, the recommended dose of FLEXERIL is 5 mg three times a day. Based on individual patient response, the dose may be increased to 10 mg three times a day. Use of FLEXERIL for periods longer than two or three weeks is not recommended. Drugs.com provides accurate and independent information on more than 24,000 prescription drugs, over-the-counter medicines and natural products. This material is provided for educational purposes only and is not intended for medical advice, diagnosis or treatment.

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Seizures should be controlled with benzodiazepines or, if these are ineffective, other anticonvulsants (e.g. phenobarbital, phenytoin). Physostigmine is not recommended except to treat life-threatening symptoms that have been unresponsive to other therapies, and then only in close consultation with a poison control center. In the higher dose groups this microscopic change was seen after 26 weeks and even earlier in rats which died prior to 26 weeks; at lower doses, the change was not seen until after 26 weeks.