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Clonazepam: Difference between revisions

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Tier 2 taxonomy consolidation: remove retired Category:Anxiolytics & Sedative-Hypnotics
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{{MedTemplate
{{MedTemplate
| generic           = Clonazepam
| generic           = Clonazepam
| brand             = Klonopin
| brand             = Klonopin
| structure         =  
| structure         =
| classes           = Benzodiazepine, Anticonvulsant, Anxiolytic
| classes           = [[:Category:Benzodiazepines|Benzodiazepine]], [[:Category:Anxiolytics|Anxiolytic]], [[:Category:Anticonvulsants|Anticonvulsant]], [[:Category:Schedule IV controlled substances|Schedule IV controlled substance]]
| mechanism          = GABAA positive allosteric modulator
| uses             = <vote slug="panic-disorder-use">Panic disorder (FDA)</vote>, <vote slug="lennox-gastaut-use">Lennox-Gastaut syndrome (FDA)</vote>, <vote slug="myoclonic-seizures-use">Akinetic and myoclonic seizures (FDA)</vote>, <vote slug="social-anxiety-disorder-use">Social anxiety disorder (off-label)</vote>, <vote slug="rem-sleep-behavior-disorder-use">REM sleep behavior disorder (off-label, evidence-supported)</vote>, <vote slug="restless-legs-syndrome-use">Restless legs syndrome (off-label, second-line)</vote>, <vote slug="acute-mania-adjunct-use">Acute mania adjunct (off-label)</vote>
| uses               =  
| starting_dose     = Anxiety: 0.25 mg PO BID, titrate by 0.125-0.25 mg every 3 days to target 1-4 mg/day divided. Seizures: 1.5 mg/day divided TID, titrate by 0.5-1 mg every 3 days
| starting_dose     =  
| preparations     = Tablets 0.5, 1, 2 mg; orally disintegrating tablets 0.125, 0.25, 0.5, 1, 2 mg
| preparations       =  
| fda_max           = 20 mg/day (seizures); commonly limited to 4 mg/day for anxiety in current practice
| fda_max          =  
| pill_id           =
| routes             =  
| routes           = Oral
| onset             =  
| onset             = 20-60 minutes
| duration           =  
| duration         = 6-12 hours (long-acting among benzodiazepines)
| halflife           =
| halflife          = 30-40 hours (long; accumulates with chronic dosing)<ref name="klonopin-label">FDA Prescribing Information, Klonopin (clonazepam), Genentech/Roche, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/017533s055lbl.pdf</ref>
| bioavailability    =
| bioavailability   = ~90% (oral)<ref name="klonopin-label" />
| pregnancy         =  
| pregnancy        = Limited human data; some signal for cleft palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.{{citation needed}}
| legal              =  
| legal             = [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the benzodiazepine class '''Boxed Warning''' for risk of fatal respiratory depression, coma, and death when combined with opioids<ref name="klonopin-label" />
| intro              =
| mechanism         = <vote slug="clonazepam-mech-claim">Positive allosteric modulator of the GABA-A receptor at the benzodiazepine binding site (α-γ subunit interface), enhancing chloride ion conductance and consequent neuronal inhibition. The long elimination half-life is the clinical signature: smoother symptom coverage than short-acting alternatives but greater accumulation, longer next-day sedation, and longer protracted withdrawal.</vote> Strong CYP3A4 substrate; CYP3A4 inhibitors (ketoconazole, clarithromycin, ritonavir, grapefruit juice) substantially raise plasma exposure. Tolerance to anxiolytic effect, dependence, and significant withdrawal syndrome on abrupt discontinuation; slow taper essential after extended use<ref name="klonopin-label" />.
| pharmacokinetics   =  
| pharmacodynamics  =  
| indications        =  
| dosing             =  
| effects            =
| interactions      = <pharmaInteractions/>
| pregnancy_details  =
| monitoring         =  
| counseling        =  
| anecdotes          =
| seealso            =
| references        =  
}}
}}
== References ==
<references />


[[Category:Benzodiazepines]]
[[Category:Benzodiazepines]]
[[Category:Anxiolytics]]
[[Category:Anxiolytics]]
[[Category:GABAA Positive Allosteric Modulators (General)]]
[[Category:GABAergics]]
[[Category:Anticonvulsants]]
[[Category:Anticonvulsants]]
[[Category:Schedule IV controlled substances]]

Latest revision as of 06:43, 23 May 2026

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Problems

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Titration strategies

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Pharmacy
Starting dose
Anxiety: 0.25 mg PO BID, titrate by 0.125-0.25 mg every 3 days to target 1-4 mg/day divided. Seizures: 1.5 mg/day divided TID, titrate by 0.5-1 mg every 3 days
Preparations
Tablets 0.5, 1, 2 mg; orally disintegrating tablets 0.125, 0.25, 0.5, 1, 2 mg
US FDA Max
20 mg/day (seizures); commonly limited to 4 mg/day for anxiety in current practice
Pharmacology
Routes
Oral
Onset
20-60 minutes
Duration
6-12 hours (long-acting among benzodiazepines)
Half-life
30-40 hours (long; accumulates with chronic dosing)[1]
Bioavailability
~90% (oral)[1]
Pregnancy
Limited human data; some signal for cleft palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.[citation needed]
Legal status
Schedule IV controlled substance in US. Carries the benzodiazepine class Boxed Warning for risk of fatal respiratory depression, coma, and death when combined with opioids[1]
Purported mechanism
Positive allosteric modulator of the GABA-A receptor at the benzodiazepine binding site (α-γ subunit interface), enhancing chloride ion conductance and consequent neuronal inhibition. The long elimination half-life is the clinical signature: smoother symptom coverage than short-acting alternatives but greater accumulation, longer next-day sedation, and longer protracted withdrawal.0 Strong CYP3A4 substrate; CYP3A4 inhibitors (ketoconazole, clarithromycin, ritonavir, grapefruit juice) substantially raise plasma exposure. Tolerance to anxiolytic effect, dependence, and significant withdrawal syndrome on abrupt discontinuation; slow taper essential after extended use[1].

References

  1. 1.0 1.1 1.2 1.3 FDA Prescribing Information, Klonopin (clonazepam), Genentech/Roche, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/017533s055lbl.pdf