Lorazepam; Uses, Dosage, Side Effects, Interactions

Lorazepam
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Lorazepam is a benzodiazepine with anxiolytic, anti-anxiety, anticonvulsant, anti-emetic and sedative properties. Lorazepam enhances the effect of the inhibitory neurotransmitter gamma-aminobutyric acid on the GABA receptors by binding to a site that is distinct from the GABA binding site in the central nervous system. This leads to an increase in chloride channel opening events, facilitation of chloride ion conductance, membrane hyperpolarization, and eventually inhibition of the transmission of nerve signals, thereby decreasing nervous excitation.

Lorazepam is an orally available benzodiazepine used widely in the therapy of anxiety and insomnia. As with most benzodiazepines, lorazepam therapy has not been associated with serum aminotransferase or alkaline phosphatase elevations, and clinically apparent liver injury from lorazepam has not been reported and must be very rare if it occurs at all.

Lorazepam is an intermediate-duration psychoactive drug of the benzodiazepine class which produces anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, anti-nausea, depressant and preanesthetic effects.I t affects chemicals in the brain that may be unbalanced in people with anxiety.

Mechanism of Action of Lorazepam 

Lorazepam binds to an allosteric site on GABA-A receptors, which are pentameric ionotropic receptors in the CNS. Binding potentiates the effects of the inhibitory neurotransmitter GABA, which upon binding opens the chloride channel in the receptor, allowing chloride influx and causing hyperpolerization of the neuron.

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Lorazepam is a benzodiazepine with anxiolytic, anti-anxiety, anticonvulsant, anti-emetic and sedative properties. Lorazepam enhances the effect of the inhibitory neurotransmitter gamma-aminobutyric acid on the GABA receptors by binding to a site that is distinct from the GABA binding site in the central nervous system. This leads to an increase in chloride channel opening events, a facilitation of chloride ion conductance, membrane hyperpolarization, and eventually inhibition of the transmission of nerve signals, thereby decreasing nervous excitation.

Indications of Lorazepam 

Contra Indications of Lorazepam 

Dosages of Lorazepam 

Strengths:  0.5 mg;  1 mg; 2 mg; 4 mg/mL; 2 mg/mL; 1 mg/mL

Insomnia

  • 2 to 4 mg orally administered at bedtime

Anxiety

Tablets

  • Initial dose: 2 to 3 mg orally per day administered 2 to 3 times per day
  • Maintenance dose: 1 to 2 mg orally 2 to 3 times a day
  • IV: 2 mg total, or 0.044 mg/kg, whichever is smaller

Light Anesthesia

  • IM: 0.05 mg/kg up to a maximum of 4 mg
  • IV: 2 mg total, or 0.044 mg/kg, whichever is smaller

Status Epilepticus

  • 0.1 mg/kg IV up to 4 mg per dose; may repeat in 5 to 10 minutes
  • Maximum dose: 8 mg

Pediatric Dose for Anxiety

12 years or older

  • Initial dose: 2 to 3 mg orally per day administered 2 to 3 times per day
  • Maintenance dose: 1 to 2 mg orally 2 to 3 times a day.

Pediatric Dose for Insomnia

12 years or older

  • 2 to 4 mg orally administered at bedtime

Side Effects of Lorazepam 

The most common

Common

Serious

Drug Interactions of Lorazepam 

Lorazepam may interact with following drug, supplements & may change the efficacy of drugs

Pregnancy and Lactation of Lorazepam 

FDA pregnancy category D

Pregnancy 

Benzodiazepines should not be used during pregnancy, especially during the first and last trimesters. Benzodiazepines may cause fetal damage when administered to pregnant women. If the drug is prescribed to a woman of childbearing potential, she should be warned to contact her physician about stopping the drug if she intends to become, or suspects that she is, pregnant. There is a possibility that infants born to mothers who take benzodiazepines chronically during the later stages of pregnancy may develop physical dependence.

Lactation

Lorazepam is excreted in small amounts in breast milk. Mothers who are breast-feeding should not take benzodiazepines. Sedation and inability to suckle have occurred in neonates of lactating mothers taking benzodiazepines.

References

Lorazepam

 

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