Clonazepam

There is a high incidence of death due to respiratory depression when benzodiazepines are combined with depressants such as opiates, alcohol or other GABAergic substances.

Clonazepam
Molecular structure of Clonazepam
Chemical Nomenclature
Common names	Clonazepam, Klonopin, K-Pins
Systematic name	5-(2-Chlorophenyl)-7-nitro-2,3-dihydro-1,4-benzodiazepin-2-one
Class Membership
Psychoactive class	Depressant
Chemical class	Benzodiazepine
Routes of Administration
Oral Dosage WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. Light 0.25 - 0.5 mg Common 0.5 - 1 mg Strong 1 - 2 mg + Heavy 3 mg + Duration Total 8 - 12 hours Onset 20 - 60 minutes Afterglow 8 - 48 hours

Summary sheet: Clonazepam

Klonopin 0.5 mg.

Klonopin 1 mg

Clonazepam (trade name Klonopin) is a long-acting psychoactive drug of the benzodiazepine class which produces anxiolytic, anticonvulsant, muscle relaxant, amnesic, sedative, and hypnotic effects. Clonazepam, like other benzodiazepines, binds to specific sites on the GABAA gamma-amino-butyric acid receptor. It is commonly used and FDA approved for the medical treatment of panic disorder, generalized anxiety disorder (GAD), and social anxiety disorder (SAD). Clonazepam has an elimination half-life of 18–50 hours to 19–60 hours, and is generally considered to be a long-acting benzodiazepine. Clonazepam has an intermediate onset of action, with a peak blood level occurring one to four hours after oral administration.

Chemistry

Clonazepam is a drug of the benzodiazepine class. Benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at R₁ and R₄. The benzyl ring of clonazepam is substituted at R₈ with a nitro group, NO₂-. Further, the diazepine ring is bonded at R₅ to a 2-chlorinated phenyl ring. Clonazepam also contains an oxygen group double bonded to R₂ of its diazepine ring to form a ketone. This oxygen substitution at R₂ is shared with other benzodiazepine drugs with the suffix -azepam.

Pharmacology

Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors. As this site is the most prolific inhibitory receptor within the brain, its modulation results in the sedating (or calming effects) of clonazepam on the nervous system.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Physical effects

The physical effects of clonazepam can be broken down into several components which progressively intensify proportional to dosage.

These are listed below and generally include:

• Sedation - In terms of energy level alterations, this drug has the potential to be extremely sedating and often results in an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.
• Dizziness
• Muscle relaxation
• Motor control loss
• Respiratory depression
• Seizure suppression

Cognitive effects

The cognitive effects of clonazepam can be broken down into several components which progressively intensify proportional to dosage. The general head space of clonazepam is described by many as one of intense relaxation, anxiety suppression and decreased inhibition. It contains a large number of typical depressant cognitive effects.

The most prominent of these cognitive effects generally include:

• Amnesia
• Anxiety suppression
• Thought deceleration
• Disinhibition
• Information processing suppression
• Compulsive redosing
• Delusions of sobriety - This is the false belief that one is perfectly sober despite obvious evidence to the contrary such as severe cognitive impairment and an inability to fully communicate with others.

Paradoxical effects

Paradoxical reactions to benzodiazepines such as increased seizures (in epileptics), aggression, increased anxiety, violent behavior, loss of impulse control, irritability and suicidal behavior sometimes occur (although they are rare in the general population, with an incidence rate below 1%).

These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.

Toxicity and harm potential

Lethal dosage

The lethal dosage of clonazepam has not been established; however, (like many benzodiazepines) it has a large therapeutic index and margin of safety. Complications may arise when administered in excess. Intentional overdoses have been reported.

As with all GABAergic drugs, overdose can be lethal when mixed with other depressants including alcohol or opioids.

Tolerance and addiction potential

Tolerance will develop to the sedative-hypnotic effects within a couple of days of repeated administration. Abrupt discontinuation of clonazepam following regular dosing over several days can result in a withdrawal phase which includes rebound symptoms such as increased anxiety and insomnia. It is possible to gradually reduce the dose over the course of several days, which will lengthen the duration of the withdrawal period but reduce the perceived intensity.

Benzodiazepine discontinuation is notoriously difficult; it is potentially life-threatening for individuals using regularly to discontinue use without tapering their dose over a period of weeks. There is an increased risk of seizure following discontinuation. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

• Depressants (1,4-Butanediol, 2-methyl-2-butanol, alcohol, barbiturates, GHB/GBL, methaqualone, opioids) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances also potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Stimulants - It is dangerous to combine benzodiazepines with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of benzodiazepines, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of benzodiazepines will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only dosing a certain amount of benzodiazepines per hour. This combination can also potentially result in severe dehydration if hydration is not monitored.

Legal issues

• Australia: Clonazepam is prescription only.
• Canada: Clonazepam is a Schedule IV drug.
• U.K.: It is a Class C drug.
• U.S.: Clonazepam is a Schedule IV substance.
• India: The drug is Schedule H in India.

Preparation methods

Preparation methods for this compound within our preparation index include:

• Volumetric liquid dosing

See also

• Responsible use
• Psychoactive substance index
• Entactogens
• Alcohol
• Benzodiazepines
• Depressants