Cyclobenzaprine


Description

Cyclobenzaprine is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine acts on the locus coeruleus where it results in increased norepinephrine release, potentially through the gamma fibers which innervate and in...

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Pharmacology

Indication

For use as an adjunct to rest and physical therapy for relief of muscle spasm associated with acute,... Read more

Pharmacodynamic

Cyclobenzaprine, closely related to the antidepressant amitriptyline, is used as a skeletal muscle r... Read more

Mechanismofaction

Like other tricyclic antidepressants, cyclobenzaprine exhibits anticholinergic activity, potentiatio... Read more

Absorption

Slowly but well absorbed after oral administration

Proteinbinding

Very high (93%)

Volumeofdistribution

Information currently not available.

Clearance

0.7 L/min

Halflife

18 hours (range 8-37 hours)

Routeofelimination

Cyclobenzaprine is extensively metabolized, and is excreted primarily as glucuronides via the kidney... Read more

Toxicity

Oral mouse and rat LD50 are 338 mg/kg and 425 mg/kg respectively. Signs of overdose inclu... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Drowsiness US
  • Kind: experimental
    • Percent: 16-39%
  • Varying Reports
    Drowsiness US
  • Kind: experimental
    • Percent: 29-38%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 21-32%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 7-27%
  • Varying Reports
    Dizziness US
  • Kind: experimental
    • Percent: 3-11%
  • Varying Reports
    Headache US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Upper Respiratory Infection US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Mental acuity decreased US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Irritability US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Acid Regurgitation US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 1-3%
  • Varying Reports
    Nervousness US
  • Kind: experimental
    • Percent: 1-3%
  • Varying Reports
    Confusion US
  • Kind: experimental
    • Percent: 1-3%
  • Varying Reports
    Unpleasant taste US
  • Kind: experimental
    • Percent: 1-3%
  • Varying Reports
    Blurred vision US
  • Kind: experimental
    • Percent: 1-3%
  • Varying Reports
    Nausea US
  • Kind: experimental
    • Percent: 1-3%
  • Varying Reports
    Constipation US
  • Kind: experimental
    • Percent: 1-3%
  • Varying Reports
    Dyspepsia US
  • Kind: experimental
    • Percent: 1-3%
  • Varying Reports
    Fatigue/tiredness US
  • Kind: experimental
    • Percent: 1-3%
  • Varying Reports
    Asthenia US
  • Kind: experimental
    • Percent: 1-3%
  • Varying Reports
    Muscle twitching US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Convulsions US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Hypertonia US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Tremors US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Dysarthria US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Vertigo US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Ataxia US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Seizures US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Local weakness US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Urticaria US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Facial edema US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Anaphylaxis US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Angioedema US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Jaundice and cholestasis US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Abnormal liver function and rare reports of hepatitis US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Edema of the Tongue US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Thirst US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Gastritis US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: <1%
  • Post Marketing Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Arrhythmias
        • Drugbank Id: DBCOND0031410
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Acute recovery phase of myocardial infarction
        • Drugbank Id: DBCOND0107607
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Conduction Disturbances
        • Drugbank Id: DBCOND0071211
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Heart Block
        • Drugbank Id: DBCOND0032425
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Hyperthyroidism
        • Drugbank Id: DBCOND0009048
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Congestive Heart Failure
        • Drugbank Id: DBCOND0029751
    • Route:
      • Topical
    • Regions: US
    • Patient Conditions:
        • Name: Nursing
        • Drugbank Id: DBCOND0040121
    • Route:
      • Oral
    • Regions: US
    • With Categories Coadmin:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996

    Food Interactions

    • Avoid alcohol.
    • Take with food to reduce irritation.

    Interactions

    Type in a drug name to check for interaction with Cyclobenzaprine

    The metabolism of Cyclobenzaprine can be decreased when combined with (R)-warfarin.
    The metabolism of Cyclobenzaprine can be decreased when combined with (S)-Warfarin.
    The risk or severity of hypertension can be increased when Cyclobenzaprine is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
    The risk or severity of hypertension can be increased when Cyclobenzaprine is combined with 1-benzylimidazole.
    Cyclobenzaprine may decrease the hypoglycemic activities of 2,4-thiazolidinedione.
    The therapeutic efficacy of Cyclobenzaprine can be increased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
    The therapeutic efficacy of Cyclobenzaprine can be increased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The metabolism of Cyclobenzaprine can be decreased when combined with 3,5-diiodothyropropionic acid.
    The risk or severity of Cardiac Arrhythmia and CNS stimulation can be increased when 3,5-Diiodotyrosine is combined with Cyclobenzaprine.
    The therapeutic efficacy of Cyclobenzaprine can be increased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
    Cyclobenzaprine may increase the vasopressor activities of 4-Bromo-2,5-dimethoxyphenethylamine.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Cyclobenzaprine.
    The metabolism of Cyclobenzaprine can be decreased when combined with 4-Methoxyamphetamine.
    The metabolism of Cyclobenzaprine can be decreased when combined with 5-androstenedione.
    The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of Cyclobenzaprine can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of Cyclobenzaprine can be decreased when combined with 6-O-benzylguanine.
    The metabolism of Cyclobenzaprine can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with 7-Nitroindazole.
    Cyclobenzaprine may increase the serotonergic activities of 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.

    References

      Information currently not available.

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