Pharmacology - Flurazepam (Dalmane)

[Jatelka]

As part of an exciting new project being undertaken by Psych0naut and myself, all the benzos that don't yet have a dedicated thread will be getting one!

Here's some basic info on Flurazepam. Please feel free to add more!

Flurazepam is 7-chloro-1-[2-(diethylamino)ethyl]-5-( o -fluorophenyl)-1,3-dihydro-2 H -1,4-benzodiazepin-2-one dihydrochloride.

It is a pale yellow, crystalline compound, freely soluble in alcohol and very soluble in water. It has a molecular weight of 460.826. Click on the attachment to see it's structure.

Pharmacokinetics

Flurazepam is rapidly absorbed and rapidly metabolized. It is excreted primarily in the urine. Following a single oral dose, peak plasma levels occur at 30 to 60 minutes. The mean half-life is 2.3 hours.The major metabolite is N1-desalkyl-flurazepam, which reaches steady-state after 7 to 10 days of dosing. The half life of elimination of N1-des-alkyl- flurazepam ranges from 47 to 100 hours. The major urinary metabolite is conjugated N1-hydroxyethyl- flurazepam which accounts for 22 to 55 percent of the dose. Less than 1% of the dose is excreted in the urine as N1-desalkyl-flurazepam.

Flurazepam is increasingly effective on the second or third night of consecutive use and that for one or two nights after the drug is discontinued both sleep latency and total wake time may still be decreased, this is due to the effects of the active metabolites.

Flurazepam is indicated for the treatment of insomnia characterized by difficulty in failing asleep, frequent nocturnal awakenings, and/or early morning awakening.

The usual therapeutic dose is 30mg

Adverse Effects:

Common: Dizziness, drowsiness, light-headedness and ataxia

Also reported: Headache, GI symptoms, apprehension, irritability, palpitations and chest pain, myalgia and arthralgia.

There have also been rare occurrences of leukopaenia, sweating, flushes, blurred vision, hypotension, shortness of breath, itching and skin rash, excessive salivation,depression, slurred speech, confusion, restlessness, hallucinations and deranged liver function tests.

Paradoxical reactions, e.g., excitement, stimulation and hyperactivity, have also been reported in rare instances.

As with all benzodiazepines, tolerance and physical dependance can occur with as little as 14 days of continued use. Flurazepam should not be discontinued suddenly

Cautions

Additive efffect with other CNS depressants, including alcohol. Should be used with caution in renal and hepatic failure.
Overdose

Manifestations of flurazepam hydrochloride overdosage include somnolence, confusion, coma and hypotension

Contraindications

Flurazepam is contraindicated in patients with known hypersensitivity to the drug, and in pregnancy.

[Abrad]

SWIM was once prescribed this for sleep but found it left an extremely nasty taste in his mouth for the whole of the next day.