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Diazepam (Valium)

Group: Depressants
Nicknames: Vallies, Blues, Yellows, V, Valley Girls, MSJ
Last reviewed: October 2026

Pharmacology

Diazepam is a GABA-A receptor positive allosteric modulator. What this means is that diazepam makes GABA – our brain’s main inhibitory neurotransmitter – more effective. GABA activates GABA-A receptors, which turn down the signals between nerve cells, thereby calming the brain and subsequently the mind.

Diazepam has a high oral bioavailability of around 80%, meaning it is efficiently absorbed when swallowed. Following oral administration, diazepam is quickly absorbed and metabolised by the body. Peak concentrations in plasma (proportionate to the dose) occur approximately 30 to 90 minutes after ingestion.

Diazepam has a duration of around 4–8 hours; however, the drug and its metabolites can stick around for between 1 and 10 days. Diazepam is metabolised by a range of CYP liver enzymes, including CYP3A4 – an enzyme blocked by grapefruit, combined contraceptive pill, and several SSRIs, antifungals, and antiretroviral medications. Diazepam’s metabolites are active benzos, which may be responsible for diazepam’s relatively long after-effects which can last between 12 to 36 hours. Additionally, the breakdown of diazepam becomes even slower in older age.

When diazepam is taken long term, the brain’s GABA receptors become desensitised, requiring higher doses for the same effect. It is advised that people taking diazepam 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 diazepam which may lead to dangerous withdrawal symptoms such as seizures. Instead, it is advised to taper gradually with medical supervision. For people dependent on other benzos, they may switch to diazepam as it stays in the blood longer (half life 30–56 hours), making tapering more gradual.

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

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