Prescription Required
In stock
Manufacturer
ACTAVIS PHARMA/
SKU
00591565810

cyclobenzaprine 10 mg tablet

Generic
$0.03 / tablet
$1.09 / tablet
$1.06 / tablet
+ -
1,000 tablets Available
Total Price:

Uses

Muscular Conditions

Cyclobenzaprine is used as an adjunct to rest and physical therapy for the relief of muscular spasm associated with acute, painful musculoskeletal conditions. Skeletal muscle relaxants generally appear to be more effective than placebo in providing symptomatic relief of acute low back pain, but are associated with a high incidence of adverse effects. Although comparative studies are limited, available data suggest that various skeletal muscle relaxants generally have similar efficacy for such use. Acute low back pain usually is a benign and self-limiting condition that improves spontaneously over time; if pharmacologic therapy is required, an analgesic agent such as acetaminophen or a nonsteroidal anti-inflammatory agent (NSAIA) generally is recommended as first-line therapy for most patients. Skeletal muscle relaxants (alone or in combination with analgesics) may be used as an option for short-term relief of acute low back pain; however, the possibility of adverse effects, particularly adverse CNS effects, should be considered. In general, skeletal muscle relaxants should be used with caution after weighing the potential risks against the benefits in individual patients.

Efficacy of cyclobenzaprine hydrochloride 10 mg initially was established in 8 controlled clinical studies comparing cyclobenzaprine, diazepam, and placebo for their effect on muscle spasm, local pain and tenderness, limitation of motion, and restriction in activities of daily living. Improvement in patients receiving cyclobenzaprine was substantially greater than in those receiving diazepam in 3 studies and was comparable to diazepam in the remaining 5 studies.

Efficacy of cyclobenzaprine hydrochloride 5 mg was evaluated in 2 controlled clinical studies; in one study patients received cyclobenzaprine hydrochloride 5 or 10 mg or placebo 3 times daily, and in the second study patients received 2.5 or 5 mg of the drug or placebo 3 times daily. In both studies, efficacy of cyclobenzaprine hydrochloride 5 mg was substantially greater than placebo for patient-assessed primary end points (i.e., global impression of change, medication helpfulness, and relief from starting backache) by the seventh day of treatment. In addition, cyclobenzaprine 5 mg was substantially more effective than placebo for a physician-assessed secondary end point (reduction in presence and extent of palpable muscle spasm). In the study comparing cyclobenzaprine 5 or 10 mg 3 times daily with placebo, both dosages of the drug were substantially more effective than placebo by the third or fourth day (48-72 hours after the first dose of medication) of treatment. The only efficacy-related difference between the 2 dosages was in onset of patient-rated relief from starting backache, which occurred after the third or fourth dose in patients receiving 5 mg but after the first 2 doses in patients receiving 10 mg. In the second study, the 2.5 mg dosage of cyclobenzaprine was no more effective than placebo.

Analysis of data from controlled studies indicates that an effective dosage of cyclobenzaprine may produce clinical improvement whether or not sedation occurs. A subanalysis of data from patients in both studies who received either cyclobenzaprine hydrochloride (5 mg 3 times daily) or placebo and did not report somnolence demonstrated a meaningful treatment effect for all primary efficacy variables for the 5-mg dose despite the absence of somnolence in these patients. The manufacturer states that no well-controlled clinical studies have been performed to determine whether cyclobenzaprine will enhance the clinical effects of aspirin or other analgesics or vice versa when such combinations are used to manage acute musculoskeletal conditions.

Some data suggest that cyclobenzaprine may be useful for the treatment of fibrositis. Cyclobenzaprine is ineffective in the treatment of spasticity associated with cerebral or spinal disease or in children with cerebral palsy.

Dosage and Administration

Administration

Cyclobenzaprine hydrochloride is administered orally.

Dosage

Muscular Conditions

The recommended oral dosage of cyclobenzaprine hydrochloride for most adults and adolescents 15 years of age and older is 5 mg 3 times daily. Depending on response, dosage may be increased to 10 mg 3 times daily. The manufacturer states that cyclobenzaprine should be used only for short periods (e.g., up to 2-3 weeks) because adequate evidence of effectiveness for more prolonged use is not available and because muscle spasm associated with acute, painful musculoskeletal conditions generally is of short duration and specific therapy for longer periods seldom is warranted.

Dosage in Hepatic Impairment

The manufacturer states that cyclobenzaprine hydrochloride dosage should be initiated with caution and less frequent dosing should be considered in patients with mild hepatic impairment, beginning with a 5 mg dose and slowly titrating upward. Use of the drug is not recommended in patients with moderate or severe hepatic impairment.

Dosage in Geriatric Patients

The manufacturer states that less frequent dosing should be considered in geriatric patients, initiating cyclobenzaprine hydrochloride with a 5 mg dose and titrating upward slowly.

Cautions

The most common adverse effects reported in patients receiving cyclobenzaprine in clinical studies were drowsiness, dry mouth, dizziness, fatigue, and headache. Cyclobenzaprine is closely related to the tricyclic antidepressants, and the possibility that cyclobenzaprine may cause adverse effects similar to those of the tricyclic antidepressants should be considered.

Nervous System Effects

Drowsiness occurred in 29 or 38% of patients receiving cyclobenzaprine 5 or 10 mg, respectively, compared with 10% of those receiving placebo in controlled studies; drowsiness also was reported in 39 or 16% of patients receiving cyclobenzaprine 10 mg in controlled studies or during postmarketing surveillance, respectively. Dizziness occurred in 1-3% of patients receiving cyclobenzaprine 5 or 10 mg in controlled studies, and in 11 or 3% of patients receiving cyclobenzaprine 10 mg in clinical studies or during postmarketing surveillance, respectively. Fatigue occurred in 6% of patients receiving either 5 or 10 mg of cyclobenzaprine compared with 3% of those receiving placebo in controlled studies; fatigue or tiredness occurred in 1-3% of patients receiving 10 mg of the drug in controlled studies and in postmarketing surveillance.

Headache occurred in 5% of those receiving 5 or 10 mg of cyclobenzaprine and in 8% of those receiving placebo in controlled studies; headache occurred in 1-3% of patients receiving 10 mg of the drug in controlled studies and postmarketing surveillance. Irritability, decreased mental acuity, nervousness, asthenia, and confusion occurred in 1-3% of patients receiving 5 or 10 mg of cyclobenzaprine in controlled studies or during postmarketing surveillance in patients receiving 10 mg of the drug.

Malaise, seizures, ataxia, vertigo, dysarthria, hypertonia, tremors, disorientation, insomnia, depressed mood, abnormal sensations, anxiety, agitation, psychosis, abnormal thinking, abnormal dreaming, hallucinations, excitement, paresthesia, and diplopia were reported during postmarketing surveillance or in less than 1% of patients receiving 10 mg of the drug in controlled studies. Other adverse nervous system effects that have been reported in patients receiving other tricyclic drugs or rarely with cyclobenzaprine but for which a causal relationship with the drug could not be established include decreased or increased libido, abnormal gait, delusions, aggressive behavior, paranoia, peripheral neuropathy, Bell's palsy, alterations in EEG patterns, and extrapyramidal manifestations.

GI Effects

Dry mouth occurred in 21 or 32% of patients receiving 5 or 10 mg, respectively, of cyclobenzaprine and in 7% of those receiving placebo in controlled studies. Dry mouth also occurred in 27 or 7% of patients receiving 10 mg of the drug in clinical studies or during postmarketing surveillance, respectively. Abdominal pain, acid regurgitation, dyspepsia, constipation, diarrhea, nausea, and unpleasant taste occurred in 1-3% of patients receiving 5 or 10 mg of cyclobenzaprine in controlled studies or during postmarketing surveillance in patients receiving 10 mg of the drug. Vomiting, anorexia, GI pain, gastritis, thirst, edema of the tongue, and flatulence were reported during postmarketing surveillance or in less than 1% of patients receiving 10 mg of the drug in controlled studies. Paralytic ileus, tongue discoloration, stomatitis, and parotid swelling were reported in patients receiving other tricyclic drugs or rarely with cyclobenzaprine, but a causal relationship with cyclobenzaprine could not be established.

Respiratory Effects

Upper respiratory infection and pharyngitis occurred in 1-3% of patients receiving cyclobenzaprine 5 or 10 mg in controlled studies. Dyspnea was reported in patients receiving other tricyclic drugs or rarely with cyclobenzaprine, but a causal relationship with cyclobenzaprine could not be established.

Cardiovascular Effects

Syncope, tachycardia, arrhythmia, vasodilation, palpitation, and hypotension were reported during postmarketing experience or in less than 1% of patients receiving cyclobenzaprine 10 mg in clinical studies; hypertension, myocardial infarction, heart block, and stroke have been reported in patients receiving other tricyclic drugs or rarely with cyclobenzaprine, but a causal relationship with cyclobenzaprine could not be established.

Dermatologic and Sensitivity Reactions

Anaphylaxis, angioedema, pruritus, facial edema, urticaria, rash, and sweating occurred during postmarketing experience or in less than 1% of patients receiving cyclobenzaprine 10 mg in clinical studies; photosensitivity, and alopecia have been reported in patients receiving other tricyclic drugs or rarely with cyclobenzaprine, but a causal relationship with cyclobenzaprine could not be established.

Musculoskeletal Effects

Local weakness and muscle twitching were reported during postmarketing experience or in less than 1% of patients receiving cyclobenzaprine 10 mg in clinical studies; myalgia was reported in patients receiving other tricyclic drugs or rarely with cyclobenzaprine, but a causal relationship with cyclobenzaprine could not be established.

Genitourinary Effects

Urinary frequency and/or urinary retention were reported during postmarketing experience or in less than 1% of patients receiving cyclobenzaprine 10 mg in clinical studies; impaired urination, dilatation of the urinary tract, impotence, testicular swelling, gynecomastia, breast enlargement, and galactorrhea have been reported in patients receiving other tricyclic drugs or rarely with cyclobenzaprine, but a causal relationship with cyclobenzaprine could not be established.

Hematologic Effects

Purpura, bone marrow depression, leukopenia, eosinophilia, and thrombocytopenia have been reported in patients receiving other tricyclic drugs or rarely with cyclobenzaprine, but a causal relationship with cyclobenzaprine could not be established.

Hepatic Effects

Abnormal liver function and rarely, hepatitis, jaundice, and cholestasis were reported during postmarketing experience or in less than 1% of patients receiving cyclobenzaprine 10 mg in clinical studies.

Other Adverse Effects

Blurred vision was reported in 1-3% of patients receiving cyclobenzaprine 10 mg in controlled studies or in postmarketing surveillance. Tinnitus and ageusia each have been reported during postmarketing surveillance or in less than 1% of patients receiving cyclobenzaprine 10 mg in controlled studies.

Elevation or reduction of blood glucose, weight gain or loss, syndrome of inappropriate antidiuretic hormone (SIADH), chest pain, and edema have been reported in patients receiving other tricyclic drugs or rarely with cyclobenzaprine, but a causal relationship with cyclobenzaprine could not be established.

Precautions and Contraindications

Cyclobenzaprine shares the toxic and drug interaction potentials of the tricyclic antidepressants, and the usual precautions of tricyclic antidepressant therapy should be observed. and The possibility that cyclobenzaprine may cause other adverse effects similar to those of the tricyclic antidepressants should be kept in mind, especially when the dosage for musculoskeletal conditions is exceeded.

Cyclobenzaprine should be used with caution in patients with mild hepatic impairment, and its use is not recommended in patients with moderate or severe hepatic impairment. Plasma concentrations of cyclobenzaprine are increased in patients with hepatic impairment, and such patients generally are more susceptible to sedation caused by some drugs, including cyclobenzaprine. Therefore, when cyclobenzaprine is used in patients with mild hepatic impairment, dosage should be titrated carefully, usually initiating therapy at the low end of the dosage range.(See Dosage and Administration: Dosage in Hepatic Impairment.)

Because cyclobenzaprine has adverse anticholinergic effects, it should be used with caution in patients with a history of urinary retention, angle-closure glaucoma, or increased intraocular pressure or in patients receiving anticholinergic drugs. Patients should be warned that cyclobenzaprine may impair their ability to perform hazardous activities requiring mental alertness or physical coordination such as operating machinery or driving a motor vehicle, particularly when the drug is used with alcohol or other CNS depressants.

Cyclobenzaprine is contraindicated in patients with hyperthyroidism, congestive heart failure, arrhythmias, heart block or conduction disorders, known hypersensitivity to the drug or any ingredient in the formulation and in the acute recovery phase following myocardial infarction. Cyclobenzaprine also is contraindicated in patients receiving monoamine oxidase inhibitors and should not be used within 14 days following discontinuance of these agents.

Pediatric Precautions

Safety and efficacy of cyclobenzaprine in children and adolescents younger than 15 years of age have not been established.

Geriatric Precautions

Plasma concentrations of cyclobenzaprine and the frequency and severity of adverse effects, with or without other concomitantly used drugs, are increased in the elderly. Geriatric patients receiving cyclobenzaprine may be at increased risk for adverse CNS effects (e.g., hallucinations, confusion, sedation), adverse cardiovascular effects resulting in falls or other sequelae, and interactions with other drugs or diseases. Therefore, cyclobenzaprine should be used in the elderly only if clearly needed. Dosage should be titrated carefully in geriatric patients, initiating therapy at the low end of the dosage range.(See Dosage and Administration: Dosage in Geriatric Patients.)

Pregnancy, Fertility, and Lactation

Pregnancy

Reproduction studies in rats, mice, and rabbits using cyclobenzaprine doses up to 20 times the human dose have not revealed evidence of harm to the fetus. There are no adequate and controlled studies to date using cyclobenzaprine in pregnant women, and the drug should be used during pregnancy only when clearly needed.

Fertility

Reproduction studies in rats, mice, and rabbits receiving cyclobenzaprine have not revealed evidence of impaired fertility.

Lactation

It is not known whether cyclobenzaprine is distributed into milk; however, the drug is distributed into milk in rats. Because some related tricyclic antidepressants are distributed into milk, cyclobenzaprine should be used with caution in nursing women.

Drug Interactions

Cyclobenzaprine is structurally and pharmacologically related to tricyclic antidepressants and shares the drug interaction potentials of these drugs. For additional information on potential drug interactions of tricyclic antidepressants, .

Monoamine Oxidase Inhibitors

Concomitant use of cyclobenzaprine or structurally similar tricyclic antidepressants with monoamine oxidase (MAO) inhibitors has resulted in hyperpyretic crisis, seizures, and death. Cyclobenzaprine is contraindicated in patients receiving MAO inhibitors and should not be used within 14 days following discontinuance of these drugs.

CNS Depressants

Cyclobenzaprine may be additive with or may potentiate the action of other CNS depressants (e.g., alcohol, barbiturates). Cyclobenzaprine, especially when used concomitantly with alcohol or other CNS depressants, may impair the patient's ability to perform activities requiring mental alertness or physical coordination (e.g., operating machinery, driving a motor vehicle).

Tramadol

Cyclobenzaprine and structurally similar tricyclic antidepressants may enhance the risk of seizures in patients receiving tramadol. For additional information about the risk of seizures in patients receiving these drugs, .

Hypotensive Agents

Cyclobenzaprine and structurally similar tricyclic antidepressants may block the hypotensive effects of guanethidine (no longer commercially available in the US) and other similarly acting drugs.

Nonsteroidal Anti-inflammatory Agents

Concomitant use of cyclobenzaprine with diflunisal or naproxen reportedly was well tolerated and did not appear to result in any unexpected adverse effects. However, concomitant use of cyclobenzaprine with naproxen has been associated with an increased incidence of drowsiness. Plasma concentrations of aspirin or cyclobenzaprine were unaffected when the drugs were administered concomitantly. It has not been established whether combined therapy with cyclobenzaprine and aspirin (or other analgesics) will result in enhanced clinical efficacy.

Pharmacokinetics

Absorption

Orally administered cyclobenzaprine is well absorbed. Cyclobenzaprine undergoes enterohepatic circulation, and appears to be metabolized during its first pass through the GI tract and/or liver. Mean oral bioavailability of the drug is estimated to range from 33-55%. Following oral administration of a single 5- or 10-mg dose of cyclobenzaprine hydrochloride, peak plasma concentrations of 4.3 or 8.5 ng/mL, respectively, are attained in about 4 hours. When cyclobenzaprine is administered 3 times daily, steady-state plasma concentrations are attained within 3-4 days that are about fourfold greater than those after a single dose. In healthy individuals receiving the drug 3 times daily, a mean steady-state peak plasma cyclobenzaprine concentration of 14.9 or 25.9 ng/mL was achieved at 4 or 3.9 hours after administration of a 5 or 10 mg dose, respectively.

Values for steady-state mean area under the cyclobenzaprine concentration time curve (AUC) were about 1.7 times greater in male and female individuals 65 years of age and older than in younger adults. Mean AUCs in geriatric males were about 2.4 times greater than in younger males, and those in elderly females were about 1.2 times greater than in younger females.(See Cautions: Geriatric Precautions.)

Peak plasma cyclobenzaprine concentrations and AUCs in 15 patients with mild hepatic impairment (and one with moderate hepatic impairment) were twice those observed in healthy individuals. Insufficient data exist to establish the safety of cyclobenzaprine use in patients with moderate or severe hepatic impairment.(See Cautions: Precautions and Contraindications.)

Distribution

Cyclobenzaprine is widely distributed into body tissues. It is not known if cyclobenzaprine is distributed into milk in humans; however, the drug is distributed into milk in rats. It is not known if cyclobenzaprine crosses the placenta. The drug is extensively (about 93%) bound to plasma protein.

Elimination

Cyclobenzaprine is extensively metabolized by both oxidative and conjugative pathways. Hepatic cytochrome P-450 (CYP) 3A4, 1A2, and (to a lesser extent) 2D6 isoenzymes are responsible for oxidative N-demethylation of the drug. Orally administered cyclobenzaprine is excreted in urine principally as inactive glucuronide metabolites; less than 1% of the drug is excreted renally as unchanged drug. Elimination of the drug is slow; plasma clearance is 700 mL/minute per 1.73 m and the effective elimination half-life is about 18 hours (range: 8-37 hours). Decreased clearance and increased plasma concentrations of the drug occur in the elderly and those with hepatic impairment.(See Cautions: Precautions and Contraindications and see Cautions: Geriatric Precautions.)

Write Your Own Review
You're reviewing:CYCLOBENZAPRINE 10 MG TABLET
Your Rating