Clonazepam


Description

A benzodiazepine used to treat various seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop [FDA Label] [

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Pharmacology

Indication

Clonazepam is indicated as monotherapy or as an adjunct in the treatment of Lennox-Gastaut syndrome... Read more

Pharmacodynamic

The pharmacodynamic properties of clonazepam are common among benzodiazepines and include anticonvul... Read more

Mechanismofaction

Gamma-Aminobutyric acid (GABA) is considered the principal inhibitory neurotransmitter in the human... Read more

Absorption

Clonazepam is rapidly and almost entirely absorbed after oral administration as tablets [FDA Label]... Read more

Proteinbinding

The recorded plasma protein binding of clonazepam ranges between 82–86% [ Read more

Volumeofdistribution

Clonazepam distributes very rapidly to various organs and body tissues with preferential uptake by b... Read more

Clearance

The documented clearance for clonazepam is approximately 55 ml/min regardless of gender [ Read more

Halflife

The mean elimination half-life determined for clonazepam is independent of the dose given and has be... Read more

Routeofelimination

Approximately 50-70% of a clonazepam dose is excreted in the urine and 10-30% is excreted in the fec... Read more

Toxicity

Benzodiazepines like clonazepam commonly cause drowsiness, ataxia, dysarthria, and nystagmus. Overdo... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Somnolence US
  • Kind: experimental
    • Percent: 26-50%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Drowsiness US
  • Kind: experimental
    • Percent: 50%
  • Clinical Trial
    Ataxia US
  • Kind: experimental
    • Percent: 30%
  • Clinical Trial
    Behavior Problems US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 5-12%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Upper Respiratory Tract Infection US
  • Kind: experimental
    • Percent: 6-10%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 6-9%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Coordination abnormal US
  • Kind: experimental
    • Percent: 1-9%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: 6-8%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Ataxia US
  • Kind: experimental
    • Percent: 1-8%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Sinusitis US
  • Kind: experimental
    • Percent: 2-8%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Dysmenorrhea US
  • Kind: experimental
    • Percent: 0-6%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 0-5%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Influenza US
  • Kind: experimental
    • Percent: 2-5%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Memory disturbance US
  • Kind: experimental
    • Percent: 2-5%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Allergic Reaction US
  • Kind: experimental
    • Percent: 1-4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 0-4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Colpitis US
  • Kind: experimental
    • Percent: 0-4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Intellectual ability reduced US
  • Kind: experimental
    • Percent: 0-4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 1-4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Dysarthria US
  • Kind: experimental
    • Percent: 0-4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Coughing US
  • Kind: experimental
    • Percent: 0-4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 2-4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Appetite decreased US
  • Kind: experimental
    • Percent: 0-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 0-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Impotence US
  • Kind: experimental
    • Percent: 0-3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Libido decreased US
  • Kind: experimental
    • Percent: 0-3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Bronchitis US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Urinary Tract Infection US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Micturition frequency US
  • Kind: experimental
    • Percent: 1-2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Ejaculation delayed US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Emotional Lability US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Accident US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Weight increase US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Wound US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Weight decrease US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Edema foot US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Ankle Edema US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Injury US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Edema periorbital US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Fever US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Edema US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Abrasions US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Shivering US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Vertigo US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Otitis US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Earache US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial

    Contraindications

    • Hypersensitivity:
      • benzodiazepines
    • Regions: US
    • Regions: US
    • Patient Conditions:
        • Name: Acute narrow angle glaucoma
        • Drugbank Id: DBCOND0107878
        • Modification Of:
          • Base:
            • Name: Narrow angle glaucoma
            • Drugbank Id: DBCOND0104923
          • Severity:
            • Includes:
              • acute
    • Regions: US
    • Patient Conditions:
        • Name: Significant liver disease
        • Drugbank Id: DBCOND0107858

    Food Interactions

    • Avoid alcohol.
    • Avoid excessive quantities of coffee or tea (Caffeine).
    • Take without regard to meals.

    Interactions

    Type in a drug name to check for interaction with Clonazepam

    The metabolism of (R)-warfarin can be decreased when combined with Clonazepam.
    The metabolism of (S)-Warfarin can be decreased when combined with Clonazepam.
    The risk or severity of adverse effects can be increased when Clonazepam is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The therapeutic efficacy of Clonazepam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Clonazepam.
    The risk or severity of adverse effects can be increased when Clonazepam is combined with 4-Bromo-2,5-dimethoxyamphetamine.
    The risk or severity of adverse effects can be increased when Clonazepam is combined with 4-Bromo-2,5-dimethoxyphenethylamine.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Clonazepam.
    The risk or severity of adverse effects can be increased when Clonazepam is combined with 4-Methoxyamphetamine.
    The metabolism of 5-androstenedione can be decreased when combined with Clonazepam.
    The risk or severity of adverse effects can be increased when Clonazepam is combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of Clonazepam can be decreased when combined with 6-Deoxyerythronolide B.
    The therapeutic efficacy of Clonazepam can be decreased when used in combination with 6-O-benzylguanine.
    The therapeutic efficacy of Clonazepam can be decreased when used in combination with 7-Deazaguanine.
    The metabolism of Clonazepam can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The risk or severity of adverse effects can be increased when Clonazepam is combined with 7-Nitroindazole.
    The risk or severity of adverse effects can be increased when Clonazepam is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
    The therapeutic efficacy of Clonazepam can be decreased when used in combination with 7,9-Dimethylguanine.
    The therapeutic efficacy of Clonazepam can be decreased when used in combination with 8-azaguanine.
    The therapeutic efficacy of Clonazepam can be decreased when used in combination with 8-chlorotheophylline.

    References

    • 1 . Dreifuss FE, Penry JK, Rose SW, Kupferberg HJ, Dyken P, Sato S: Serum clonazepam concentrations in children with absence seizures. Neurology. 1975 Mar;25(3):255-8. [PubMed: 1089913]
    • 2 . Robertson MD, Drummer OH: Postmortem drug metabolism by bacteria. J Forensic Sci. 1995 May;40(3):382-6. [PubMed: 7782744]
    • 3 . Rosen GM, Turner MJ 3rd: Synthesis of spin traps specific for hydroxyl radical. J Med Chem. 1988 Feb;31(2):428-32. [PubMed: 2828624]
    • 4 . Rosen GM, Demos HA, Rauckman EJ: Not all aromatic nitro compounds form free radicals. Toxicol Lett. 1984 Aug;22(2):145-52. [PubMed: 6089382]
    • 5 . Earley JV, Fryer RI, Ning RY: Quinazolines and 1,4-benzodiazepines. LXXXIX: Haptens useful in benzodiazepine immunoassay development. J Pharm Sci. 1979 Jul;68(7):845-50. [PubMed: 458601]
    • 6 . DeVane CL, Ware MR, Lydiard RB: Pharmacokinetics, pharmacodynamics, and treatment issues of benzodiazepines: alprazolam, adinazolam, and clonazepam. Psychopharmacol Bull. 1991;27(4):463-73. [PubMed: 1687613]
    • 7 . Nardi AE, Machado S, Almada LF, Paes F, Silva AC, Marques RJ, Amrein R, Freire RC, Martin-Santos R, Cosci F, Hallak JE, Crippa JA, Arias-Carrion O: Clonazepam for the treatment of panic disorder. Curr Drug Targets. 2013 Mar;14(3):353-64. [PubMed: 23256724]
    • 8 . Jenner P, Pratt JA, Marsden CD: Mechanism of action of clonazepam in myoclonus in relation to effects on GABA and 5-HT. Adv Neurol. 1986;43:629-43. [PubMed: 2418652]
    • 9 . Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons.
    • 10 . Shorter, Edward (2005). A Historical Dictionary of Psychiatry. Oxford University Press.
    • 11 . Electronic Medicines Compendium: Clonazepam Rosemont 2mg/5ml Oral Solution [Link]
    • 12 . Rivotril (Clonazepam) 0.5 mg and 2 mg Tablets Canadian Product Monograph [File]
    • 13 . Clonazepam Fact Sheet from http://cdn.neiglobal.com/content/pg/live/clonazepam.pdf [File]
    • 14 . Rivotril (Clonazepam) Australian Product Information [File]

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