Lorazepam

Description

Lorazepam is a benzodiazepine drug used in the treatment of anxiety, epilepsy and convulsions (fits) as well as for sedation and as a premedication for people about to undergo minor surgical operations.

Lorazepam has all six of the intrinsic benzodiazepine effects (anxiolysis, anterograde amnesia, sedation/hypnosis, anticonvulsion, antiemesis and muscle relaxation), but is specifically useful for combatting the short term symptoms of anxiety and aggression.

Pharmacology

Like all benzodiazepines, lorazepam works primarily as a gamma-aminobutyric acid type A (GABA-A) receptor positive allosteric modulator. What this means is that lorazepam increases the effects of GABA, our brain’s main inhibitory neurotransmitter which turns down nerve signals, thereby calming the brain and subsequently the mind. Its actions are similar to those of diazepam (Valium) but it is considerably more potent (1 mg lorazepam is equivalent to 10 mg diazepam).

Lorazepam has a high oral bioavailability of around 85%, meaning it is efficiently absorbed when taken by mouth. Following oral administration, lorazepam is slowly absorbed by the body. Peak concentrations in plasma (proportionate to the dose) occur approximately 2 hours after ingestion. Lorazepam has an average duration of approximately 12 hours.

UGT enzymes rapidly convert lorazepam into its inactive metabolite lorazepam-glucuronide, which is then excreted in urine. Differences in the rate of conversion depend on a range of individual factors including weight and cigarette smoking.

When lorazepam is taken long term, the brain’s GABA receptors become desensitised, requiring higher doses for the same effect. It is advised that people taking lorazepam long term do not stop suddenly (cold-turkey). Desensitised GABA receptors take a while to get back to baseline, meaning they will be unable to keep nerve signals in check without lorazepam which may lead to dangerous withdrawal symptoms such as seizures. Instead, it is advised to taper gradually with medical supervision.

As lorazepam turns down brain signals, combining the drug with other depressant drugs increases the risk of overdose. Drinking alcohol alongside lorazepam can cause severe sedation, intoxication and blackouts. In combination with opioids, lorazepam can slow down breathing to dangerous levels.

Harm Reduction

• Start low, go slow: Take a small amount and wait until you can feel the effects before taking more/anything else
• Try not to use alone: If something goes wrong, someone is there to get help
• Be careful mixing: Mixing lorazepam with other depressants increases overdose risk – avoid if you can, otherwise take less of each, as they can increase the effects and risks
• Carry naloxone: Some counterfeit benzos in the UK have been found to contain strong opioids
• Test your stuff: Many lorazepam pills tested in the UK didn’t contain lorazepam, and you can’t see this by eye. Find out how to send a sample to WEDINOS for testing here: https://www.wedinos.wales or pick up some test strips at our Harm Reduction Hub
• If you’ve been prescribed lorazepam and you notice a tolerance starting to develop (you need to keep taking more to get the same effect) speak to your doctor – don’t just start increasing your dose yourself.
• Don’t suddenly stop taking them, or you may start to experience symptoms of withdrawal: these can range from a return of your original symptoms (possibly even worse than before) to totally new symptoms.
• If you have become physically dependent on lorazepam, the symptoms of abruptly stopping are likely to be even worse. It’s important to get proper medical advice on how to reduce your intake slowly.
• It’s also possible to become psychologically dependent on the drug (feeling like you need it all the time). If you think this is happening, see your doctor as soon as possible, but don’t suddenly stop taking it.

History

Lorazepam is one of the ‘classic’ benzodiazepines (with clonazepam, diazepam, flurazepam, etc.). It was first synthesised in the 1970s by Wyeth Pharmaceuticals, now part of Pfizer, and marketed under the brand name ‘Ativan’.

As with many of the other benzodiazepines, lorazepam has a history of non-prescribed (‘recreational’) use, dating back to at least the 1980s. Individuals mostly take it for its relaxant, ‘chill-out’ effects. Due to its powerful and fast-acting nature (including amnesia and sedation-hypnosis as potential reactions), there is also some reported use of lorazepam as a ‘date rape’ drug, with people having had their drinks spiked. However, this has not been confirmed and it may be that lorazepam has been wrongly blamed when other substances (such as flunitrazepam, or rohypnol) are responsible.

Law

• Class C
• Schedule 4 (1)

Possible offences

• Possession
  • Maximum sentence – 2 years/fine/both
• Possession With Intent To Supply
  • Maximum sentence – 14 years/fine/both
• Supply (including being concerned in supply, conspiracy to supply, aggravated supply and offer to supply)
  • Maximum sentence – 14 years/fine/both
• Production
  • Maximum sentence – 14 years/fine/both

In practice maximum sentences are rarely used, for more detailed and accurate information go to our sentencing page.