Drug Index

GENERIC NAME :
lorazepam

BRAND NAMES :
Ativan (Injection 2 mg/mL, 4 mg/mL), Lorazepam (Tablets 0.5 mg, 1 mg, 2 mg), Lorazepam Intensol Oral Solution, (Concentrated 2 mg/mL), Apo-Lorazepam (Canada), Novo-Lorazem (Canada), Nu-Loraz (Canada),

STREET NAMES :
downers, benzo's, tranq's

BRIEF DESCRIPTION :
Lorazepam is categorized as a central nervous system sedative/hypnotic (tranquilizer). It belongs to a class of drugs known as benzodiazepines, which are the most widely prescribed medications that affect central nervous system function. Lorazepam is considered a short acting benzodiazepine. Peak concentrations in the bloodstream occur one to two hours following oral administration. The mean half-life of unconjugated lorazepam in human plasma is about 12 hours and for its major metabolite, lorazepam glucuronide, about 18 hours. At clinically relevant concentrations, lorazepam is approximately 85% bound to plasma proteins. Lorazepam is rapidly conjugated at its 3-hydroxy group into lorazepam glucuronide which is then excreted in the urine. Lorazepam glucuronide has no demonstrable CNS activity in animals. Lorazepam interacts with the ?-aminobutyric acid (GABA)-benzodiazepine receptor complex in the brain. This interaction is presumed to be responsible for lorazepam's mechanism of action. Lorazepam exhibits relatively high and specific affinity for GABA receptor sites, but does not displace GABA. Attachment to the specific binding site enhances the affinity of GABA for its receptor site on the same receptor complex. The pharmacodynamic consequences of benzodiazepine agonist actions include antianxiety effects, sedation, and reduction of seizure activity. The intensity of action is directly related to the degree of benzodiazepine receptor occupancy.

INDICATIONS FOR USE :
It may be used therapeutically to produce sedation, induce sleep, relieve anxiety, prevent seizures, or interrupt seizures (in status epilepticus). The injectable from of lorazepam is used for treatment of status epilepticus.

ABUSE AND ADDICTIVE POTENTIAL :

Lorazepam has a strong potential for dependence (addiction). In general, short acting potentially addictive drugs (like lorazepam) pose a higher risk for developing addiction than longer acting drugs. This is especially true in individuals with a history of drug addiction or alcoholism. Dependence can occur even after relatively short term therapy in the recommended dosage. In general, benzodiazepines should be prescribed for short periods only (e.g. 2- 4 weeks). Extension of the treatment period should not take place without reevaluation of the need for continued therapy. Abrupt discontinuation of this medication should be avoided. 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 dependent on lorazepam 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. Significantly adverse clinical events, some life-threatening, can be a direct consequence of physical dependence to lorazepam. Rebound (a return of symptoms of anxiety or panic disorder to a level substantially greater in frequency and/or more severe in intensity than before taking lorazepam) are often observed after taking the medication for a few weeks or months. Withdrawal can appear in some individuals following cessation of recommended doses after as little as one week of therapy. Symptoms noted in withdrawal from lorazepam may include:

• heightened sensory perception

• impaired concentration

• dysosmia (problems with smell or taste)

• clouded sensorium (confusion or difficulty thinking)

• paresthesias (tingling, pricking, or numbness of the skin)

• muscle cramps

• muscle twitch

• diarrhea

• blurred vision

• decrease appetite and weight loss

• anxiety

• insomnia (difficulty sleeping)

• seizure (convulsions)

Discontinuation of lorazepam 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:

• slurred speech
• impaired coordination
• diminished reflexes
• coma
• death

• 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 :
Lorazepam has central nervous system depressants affects. Individuals taking lorazepam should be cautioned about engaging in hazardous operations or activities that require complete mental alertness. Lorazepam 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. Hypomania and mania have been reported in association with the use of lorazepam in patients with depression. Precaution should be observed in using this medication in patients who have impaired kidney, liver, or lung function. Changes in the absorption, distribution, metabolism and excretion of benzodiazepines have been reported in disease states including alcoholism, impaired liver function, in impaired kidney function. Also, in geriatric patients the half-life of elimitation of the drug may be extended several hours, requiring careful monitoring and possibly a lower dosage range of prescribing medication. The most frequent adverse reaction to Lorazepam was sedation (15.9%), followed by dizziness (6.9%), weakness (4.2%), and unsteadiness (3.4%). The incidence of sedation and unsteadiness increased with age. Other adverse reactions to benzodiazepines, including lorazepam are fatigue, drowsiness, amnesia, memory impairment, confusion, disorientation, depression, unmasking of depression, disinhibition, euphoria, suicidal ideation/attempt, ataxia (balance impairment), asthenia, extrapyramidal symptoms, convulsions/seizures, tremor, vertigo (dizziness), eye-function/visual disturbance (including diplopia and blurred vision), dysarthria (slurred speech), change in libido (sex drive), impotence, decreased orgasm; headache, coma; respiratory depression, worsening of sleep apnea, worsening of obstructive pulmonary disease; gastrointestinal symptoms including nausea, change in appetite, constipation, jaundice, increase in liver enzymes; hypersensitivity reactions, anaphylactic reactions; skin reactions. Paradoxical (opposite of expected) reactions, including anxiety, excitation, agitation, hostility, aggression, rage, sleep disturbances/insomnia, sexual arousal, and hallucinations may occur in some individuals. A child born of a mother who is taking benzodiazepines maybe at some risk for withdrawal symptoms following birth. Benzodiazepines are also known to be excreted in human milk.

SIDE EFFECTS :
* see cautions

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


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