Temazepam

Temazepam, sold under the brand name Restoril among others, is a medication of the benzodiazepine class which is generally used to treat severe or debilitating insomnia.

[9][7] Prescriptions for hypnotics such as temazepam have seen a dramatic decrease since 2010, while anxiolytics such as alprazolam, clonazepam, and lorazepam have increased or remained stable.

They have largely been replaced by z-drugs (zopiclone, zolpidem) and atypical antidepressants (trazodone, mirtazapine) as first line treatment for insomnia.

[8] Common side effects include drowsiness, motor and cognitive impairment, lethargy, confusion, euphoria, and dizziness.

[18] The American Academy of Sleep Medicine's 2017 clinical practice guidelines recommended the use of temazepam in the treatment of sleep-onset and sleep-maintenance insomnia.

[19] The United States Air Force uses temazepam as one of the hypnotics approved as a "no-go pill" to help aviators and special-duty personnel sleep in support of mission readiness.

[22] Temazepam, similar to other benzodiazepines and nonbenzodiazepine hypnotic drugs, causes impairments in body balance and standing steadiness in individuals who wake up at night or the next morning.

[23] The smallest possible effective dose should be used in elderly or very ill patients, as a risk of apnea and/or cardiac arrest exists.

If temazepam must be prescribed to people in these groups, they should generally be monitored very closely for signs of misuse and development of dependence.

[25] Side effects are typical of hypnotic benzodiazepines, though temazepam has more pronounced CNS depressant effects, and include somnolence, sedation, dizziness, fatigue, ataxia, headache, lethargy, impairment of memory and learning, longer reaction time and impairment of motor functions (including coordination problems),[26] slurred speech, decreased physical performance, numbed emotions, reduced alertness, muscle weakness, blurred vision (especially in higher doses or in those with low tolerance), and inattention.

In medical literature from Australia, Ireland, the UK, Canada, and the United States, temazepam is the only benzodiazepine which has been fatal in overdoses without combination with other CNS depresssants.

[31] Hyperhydrosis, hypotension, burning eyes, increased appetite, changes in libido, hallucinations, faintness, nystagmus, vomiting, pruritus, gastrointestinal disturbances, nightmares, palpitation and paradoxical reactions including restlessness, aggression, violence, overstimulation and agitation have been reported, but are rare (less than 0.5%).

[35] In use longer than one to two weeks, tolerance will rapidly develop towards the ability of temazepam to maintain sleep, resulting in a loss of effectiveness.

Gradual and careful reduction of the dosage, preferably with a long-acting benzodiazepine with long half-life active metabolites, such as chlordiazepoxide or diazepam, are recommended to prevent severe withdrawal syndromes from developing.

[49] Rare cases are reported in the medical literature of psychotic states developing after abrupt withdrawal from benzodiazepines, even from therapeutic doses.

[56] A 1993 British study found temazepam to have the highest number of deaths per million prescriptions among medications commonly prescribed in the 1980s (11.9, versus 5.9 for benzodiazepines overall, taken with or without alcohol).

The authors noted several factors, such as differences in potency, receptor affinity, and rate of absorption between benzodiazepines, could explain this higher toxicity.

[58] The main pharmacological action of temazepam is to increase the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABAA receptor.

N-oxides are prone to undergo the Polonovski rearrangement when treated with acetic anhydride, and this was illustrated by the synthesis of oxazepam.

[30] A 1985 study found that temazepam and triazolam maintained significantly higher rates of self-injection than a variety of other benzodiazepines.

The study tested and compared the abuse liability of temazepam, triazolam, diazepam, lorazepam, oxazepam, flurazepam, alprazolam, chlordiazepoxide, clonazepam, nitrazepam, flunitrazepam, bromazepam, and clorazepate.

All test subjects consistently showed a strong preference for temazepam and triazolam over all the rest of the benzodiazepines included in the study.

[71][72] Benzodiazepines are commonly detected by customs at different ports and airports, arriving by mail, also found occasionally in the baggage of air passengers, mostly small or medium quantities (up to 200–300 tablets) for personal use.

[76] Temazepam use was particularly associated with violent or disorderly behaviours and contact with the police in a 1997 study of young single homeless people in Scotland.

[81] Street terms for temazepam include king kong pills (formerly referred to barbiturates, now more commonly refers to temazepam), jellies, jelly, Edinburgh eccies, tams, terms, mazzies, temazies, tammies, temmies, beans, eggs, green eggs, wobbly eggs, knockouts, hardball, norries, oranges (common term in Australia and New Zealand), rugby balls, ruggers, terminators, red and blue, no-gos, num nums, blackout, green devils, drunk pills, brainwash, mind erasers, neurotrashers, tem-tems (combined with buprenorphine), mommy's big helper, vitamin T, big T, TZ, the mazepam, resties (North America) and others.

The drug is considered to have a high potential for abuse and addiction, but has accepted medical use for the treatment of severe insomnia.

[91] In Slovenia, it is regulated as a Group II (Schedule 2) controlled substance under the Production and Trade in Illicit Drugs Act.

[93] Temazepam is banned in Sweden and possession and distribution of even small amounts is punishable by a prison sentence and a fine.

[97] In the United States, Temazepam is a Schedule IV drug under the international Convention on Psychotropic Substances of 1971 and is only available by prescription.

[98] Temazepam is available in English-speaking countries under the brand names Euhypnos, Normison, Norkotral, Nortem, Remestan, Restoril, Temaze, and Temtabs.

Prepn: [ 64 ] S. C. Bell, U.S. patent 3,197,467 (1965 to Am. Home. Prod.). See also: E. Reeder et al., U.S. patent 3,340,253 and U.S. patent 3,374,225 (1967, 1968, both to Hoffmann-La Roche ).
Apro temazepam