Lorazepam

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Merlit, Temesta; Belgium: Docloraze, Lauracalm, Lorazemed, Lorazepam, Lorazetop, Loridem, Optisedine, Temesta; Cyprus: Lorans, Lorivan, Tavor; Denmark: Temesta; Finland: Lorazepam, Temesta; France: Lorazepam, Temesta; Germany: Ativan, Lorazepam, Somagerol, Tavor, Temesta, Tolid; Greece: Ativan, Cecil, Dorm, Modium, Novhepar, Tavor, Titus, Trankilium; Ireland: Ativan; Italy: Control, Lorans, Loralin, Lorazepam, Tavor, Zeloran; Latvia: Lorafen; Lithuania: Lorafen; Luxembourg: Lauracalm, Lorazepam, Loridem, Temesta, Vigiten; Malta: Ativan, Lorans, Lorazepam, Lorivan; Netherlands: Lorazepam, Temesta; Poland: Lorafen; Portugal: Ansilor, Lorazepam, Lorenin, Lorsedal, Rialam; Romania: Anxiar; Slovenia: Loram, Lorsilan; Spain: Donix, Idalprem, Lorazepam, Orfidal, Placinoral; Sweden: Temesta; UK: Ativan.

North America

Canada: Ativan, Loraz, Lorazepam; USA: Ativan, Lorazepam.

Latin America

Argentina: Aplacasse, Calmatron, Emotival, Kalmalin, Lorazepam, Lorezan, Lyovial, Microzepam, Nervistop, Sidenar, Trapax; Brazil: Ansirax, Lorapan, Lorax, Lorazefast, Lorazepam, Max-Pax, Mesmerin; Mexico: Ativan, Lorazepam, Sinestron.

Asia

Japan: Azrogen, Rocosgen, U Pan, Wypax.

Drug combinations

Chemistry

Lorazepam: C~15~H~10~Cl~2~N~2~O~2~. Mw: 321.16. (1) 2H-1,4-Benzodiazepin-2-one, 7-chloro-5-(2-chlorophenyl)-1,3-dihydro-3-hydroxy-, (±)-; (2)(±)-7-Chloro-5-(o-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one. CAS-846-49-1 (1969).

Pharmacologic Category

Anticonvulsants; Benzodiazepines. Anxiolytics, Sedatives, and Hypnotics; Benzodiazepines. (ATC-Code: N05BA06).

Mechanism of action

Binds to stereospecific benzodiazepine receptors on postsynaptic GABA neuron at several sites within CNS, including limbic system, reticular formation. Enhancement of inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization.

Therapeutic use

Management of anxiety disorders or short-term (≤4 months) relief of symptoms of anxiety or anxiety associated with depressive symptoms. Status epilepticus, preanesthesia for desired amnesia.

Pregnancy and lactiation implications

Teratogenic effects observed in some animal studies. Lorazepam crosses human placenta. Respiratory depression, withdrawal symptoms, or hypotonia might occur if administered late in pregnancy or near time of delivery. Sedation and impaired nursing may occur in infants exposed to lorazepam from breast milk.

Unlabeled use

Ethanol detoxification. Insomnia. Psychogenic catatonia. Partial complex seizures. Agitation (I.V.). Antiemetic adjunct.

Contraindications

Hypersensitivity to lorazepam or any component of the formulation (cross-sensitivity with other benzodiazepines may exist). Acute narrow-angle glaucoma. Sleep apnea (parenteral). Intra-arterial injection of parenteral formulation. Severe respiratory insufficiency (except during mechanical ventilation).

Warnings and precautions

Benzodiazepines associated with anterograde amnesia. Might cause CNS depression. Paradoxical reactions, including hyperactive or aggressive behavior, reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use. Use with caution in hepatic impairment. Might worsen hepatic encephalopathy. Use with caution in impaired gag reflux. Use caution in depression, particularly if suicidal risk may be present. Not recommended for use in primary depressive or psychotic disorders. Use with caution in renal impairment. Use with caution in respiratory disease, including COPD or sleep apnea. Benzodiazepines may cause significant respiratory depression. Effects with other sedative drugs or ethanol might be potentiated. Use with caution in debilitated patients. Benzodiazepines associated with falls and traumatic injury. Some products may contain benzyl alcohol («gasping syndrome» in neonates). Parenteral formulation contains polyethylene glycol. Does not have analgesic, antidepressant, or antipsychotic properties. Rebound or withdrawal symptoms might occur following abrupt discontinuation or large decreases in dose. Flumazenil may cause acute withdrawal in patients receiving long-term benzodiazepine therapy.

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