Drug Index

GENERIC NAME :
clonazepam
BRAND NAMES :
klonopin tablets (0.5 mg, 1 mg, 2 mg)
STREET NAMES :
downers, benzo's, tranq's
BRIEF DESCRIPTION :
Clonazepam is categorized as a central nervous system sedative/hypnotic (tranqulizer). It belongs to a class of drugs known as benzodiazepines, which are the most widely prescribed medications that affect central nervous system function. It is widely prescribed for treatment of seizure disorder and panic disorder. The precise mechanism by which Clonazepam exerts its antiseizure and antipanic effects is unknown, although it is believed to be related to its ability to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Clonazepam is rapidly and completely absorbed after oral administration. The absolute bioavailability of Clonazepam is about 90%. Maximum plasma concentrations of Clonazepam are reached within 1 to 4 hours after oral administration. Clonazepam is approximately 85% bound to plasma proteins. Clonazepam is highly metabolized, with less than 2% unchanged Clonazepam being excreted in the urine. Biotransformation occurs mainly by reduction of the 7-nitro group to the 4-amino derivative. This derivative can be acetylated, hydroxylated, and glucuronidated. Cytochrome P-450, including CYP3A, may play an important role in Clonazepam reduction and oxidation. The elimination half-life (the time it takes to remove half of the medication from the blood stream) of Clonazepam is typically 30 to 40 hours. Clonazepam pharmacokinetics are dose independent throughout the dosing range. There is no evidence that Clonazepam induces its own metabolism or that of other drugs in humans.
INDICATIONS FOR USE :

Clonazepam tablets are useful alone or as an adjunct (in combination with other medications) in the treatment of the Lennox-Gastaut syndrome (petit mal variant), akinetic and myoclonic seizures. In patients with absence seizures (petit mal) who have failed to respond to succinimides, Clonazepam may be useful. In some studies, up to 30% of patients have shown a loss of anticonvulsant activity, often within 3 months of administration. In some cases, dosage adjustment may reestablish efficacy. Clonazepam Tablets are indicated for the treatment of panic disorder, with or without agoraphobia (abnormal fear of being helpless in a situation from which escape may be difficult or embarrassing that is characterized initially often by panic or anticipatory anxiety and finally by avoidance of open or public places), as defined in DSM-IV. Panic disorder is characterized by the occurrence of unexpected panic attacks and associated concern about having additional attacks, worry about the implications or consequences of the attacks, and/or a significant change in behavior related to the attacks. Panic disorder (DSM-IV) is characterized by recurrent unexpected panic attacks, i.e., a discrete period of intense fear or discomfort in which four (or more) of the following symptoms develop abruptly and reach a peak within 10 minutes:

(1) palpitations, pounding heart or accelerated heart rate;

(2) sweating;

(3) trembling or shaking;

(4) sensations of shortness of breath or smothering;

(5) feeling of choking;

(6) chest pain or discomfort;

(7) nausea or abdominal distress;

(8) feeling dizzy, unsteady, lightheaded or faint;

(9) derealization (feelings of unreality) or depersonalization (being detached from oneself);

(10) fear of losing control;

(11) fear of dying;

(12) paresthesias (numbness or tingling sensations);

(13) chills or hot flushes.
ABUSE AND ADDICTIVE POTENTIAL :
Clonazepam is a benzodiazepine and demonstrates potential for dependence (addiction). This is especially true in individuals with a history of drug addiction or alcoholism. Addiction-prone individuals (such as drug addicts or alcoholics) should be under careful surveillance when receiving clonazepam or other psychotropic agents because of the predisposition of such patients to habituation and dependence. Abrupt discontinuation should be avoided if it has been used for several consecutive weeks or months. Tolerance can occur in some individuals after taking the medication for several weeks or months. This means that dosages prescribed for treatment may need to be increased some over time to achieve the therapeutic response. It also means that individuals who have become addicted to clonazepam will need to progressively increase the dosage to achieve the desired mood state that the addict is seeking. Addicted individuals often take several times the recommended dosage. Clonazepam withdrawal symptoms are similar in character to those noted with barbiturates and alcohol ( e.g., convulsions, psychosis, hallucinations, behavioral disorder, tremor, abdominal and muscle cramps) have occurred following abrupt discontinuance of clonazepam. The more severe withdrawal symptoms have usually been limited to those patients who received high doses over an extended period of time. Generally milder withdrawal symptoms ( e.g., dysphoria and insomnia) have been reported following abrupt discontinuance of benzodiazepines taken continuously at therapeutic levels for several months. Consequently, discontinuation of clonazepam should be done under the supervision of a physician and often involves tapering the medication slowly and/or use of other medications to manage withdrawal symptoms.

OVERDOSAGE :
Manifestations of overdoseage may include:

• somnolence (extreme drowsiness or deep, prolonged sleep)

• confusion

• slurred speech

• impaired coordination

• diminished reflexes

• coma

• death

Emergency medical treatment is advised if overdose is suspected.

CAUTIONS :
Individuals taking clonazepam should be cautioned about engaging in hazardous operations or activities that require complete mental alertness. Ciazepam should not be used simultaneously with alcohol or any other central nervous system depressant drugs. Taken together, these drugs can potentiate the potency and effect of each drug. Precaution should be observed in using this medication in patients who have impaired kidney or liver function. Also, in geriatric patients the half-life of elimination of the drug may be extended several hours, requiring careful monitoring and possibly a lower dosage range of prescribing medication. There have been reports of worsening problems with seizures in some individuals prescribed this medication for the treatment of seizures. For those who have the expected reduction in seizures, abrupt discontinuation of clonazepam may precipitate seizures. The possibility of negative interactions with other medications you are taking exists. Tell your doctor or pharmacist about any other prescription medications you are taking, alcohol use and any “street” drug use. An increased risk of congenital malformations associated with the use of benzodiazepine drugs has been suggested in several studies. There may also be non-teratogenic risks associated with the use of benzodiazepines during pregnancy. There have been reports of neonatal flaccidity, respiratory and feeding difficulties, and hypothermia in children born to mothers who have been receiving benzodiazepines late in pregnancy. In addition, children born to mothers receiving benzodiazepines late in pregnancy may be at some risk of experiencing withdrawal symptoms during the postnatal period. Benzodiazepines are also known to be excreted in human milk.

SIDE EFFECTS :
The adverse experiences for clonazepam are provided separately for patients with seizure disorders and with panic disorder. Seizure Disorders: The most frequently occurring side effects of clonazepam are referable to CNS depression. Experience in treatment of seizures has shown that drowsiness has occurred in approximately 50% of patients and ataxia (an inability to coordinate voluntary muscular movements) in approximately 30%. In some cases, these may diminish with time; behavior problems have been noted in approximately 25% of patients. Others, listed by system, are: Neurologic: Abnormal eye movements, aphonia (loss of voice and of all but whispered speech), choreiform movements (spasmodic movements of the limbs and facial muscles and by incoordination), coma, diplopia (double vision), dysarthria (difficulty in articulating words), “glassy-eyed” appearance, headache, hypotonia (weak muscle tone), nystagmus (involuntary usually rapid movement of the eyeballs), respiratory depression, slurred speech, tremor, vertigo (dizziness). Psychiatric: Confusion, depression, amnesia, hallucinations, hysteria, increased libido (sex drive), insomnia, psychosis, suicidal attempt (the behavior effects are more likely to occur in patients with a history of psychiatric disturbances). The following paradoxical reactions(unexpected opposite reactions) have been observed: excitability, irritability, aggressive behavior, agitation, nervousness, hostility, anxiety, sleep disturbances, nightmares and vivid dreams. *This is not s complete list if side effects and others may occur. Tell your doctor or pharmacist about any unusual or bothersome side effect.

FOR MORE INFORMATION :
*this is a condensed description for clonazepam. For more details check with your physician, pharmacist, or other resources such as The Physicians' Desk Reference (PDR) or http://www.drugs.com


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