Temazepam

Also known as

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Classification

Depressant, hypnotic

Overview

Temazepam is a benzodiazepine hypnotic agent that is commonly prescribed for the short-term (typically maximum of four weeks) treatment of sleep disorders such as insomnia. It is also occasionally used as a premedication prior to minor surgical procedures.

As a recreational drug, temazepam is sometimes taken as a 'chill out' substance after a night of partying, or just as a relaxant to calm the user down. Some users suggest that at higher doses it can produce a feeling similar to being drunk .

What does it look like?

Small, white or off-white tablets, usually 10mg or 20mg when prescribed, although larger sizes found at street level; various coloured capsules (green being the most common), 7.5mg - 30mg+; 'Restoril' are colour-coded: 7.5mg- blue and pink, 15mg- red and pink, 22.5mg- blue and 30mg- red and blue; also available as an oral solution, typically 10mg/5ml .

Source

Diverted from manufacturers, pharmacies and GPs prescriptions .

Why take it?

Sought after effects

• sedative,
• relaxant ,
• reduced anxiety,
• euphoria .

Undesired effects

• headaches,
• dizziness,
• memory problems (particularly if sleep is interrupted),
• tremors,
• shakiness ,
• drowsiness,
• light-headedness,
• loss of balance,
• loss of coordination,
• confusion,
• low blood pressure,
• hallucinations,
• agitation,
• nightmares .

How long do its effects last?

Onset of effects

• all ROA's - 20 - 90 minutes , .

Duration of effects

• all ROA's - 6 - 10 hours , .

After-effects

• all ROA's - 6 - 12 hours , .

Pharmacology

Temazepam is a drug of the benzodiazepine class .

Temazepam is a minor metabolite of diazepam (valium). It has no notable active metabolites of its own. Like other benzodiazepines, it acts on the GABA receptors in the brain, enhancing their neurotransmissions. GABA acts as a 'nerve calming' agent that reduces anxiety and relaxes the muscles, hence the popularity of temazepam to aid sleep.

Temazepam is relatively long acting (6 - 24 hours), metabolises well, and can lead to a quick build-up of tolerance and addiction. As a result, when prescribed to combat insomnia, it is only used for short periods of time (1 - 2 weeks on average) and at the lowest functional dose for the patient (from 5mg upwards) .

Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter GABA by acting on its receptors . As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of temazepam on the nervous system. When temazepam binds to the GABAA receptor, it causes the Cl- ion pore to open more frequently.

The anticonvulsant properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors , .

Pharmacodynamics

Temazepam is a benzodiazepine used as a hypnotic agent in the management of insomnia. Temazepam produces CNS depression at limbic, thalamic, and hypothalamic levels of the CNS. Temazepam increases the affinity of the neurotransmitter GABA for GABA receptors by binding to benzodiazepine receptors. Results are sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and anxiolytic action .

Absorption

Well absorbed, minimal first-pass metabolism .

Bioavailability

Oral 96% .

Metabolism

Hepatic. Temazepam is completely metabolized through conjugation prior to excretion. The major metabolite is the O-conjugate of temazepam (90%) .

Half-life

Between 8 and 15 hours . 10 - 20 hours .

Elimination

80% is excreted in the urine in the form of its inactive glucuronide conjugate together with small amounts of the demethylated derivative, Oxazepam, also in conjugated form. Only approximately 12% appears in the faeces .

Temazepam was completely metabolised through conjugation prior to excretion; 80% to 90% of the dose appeared in the urine .

Lethal dosage

The oral LD50 of Restoril was 1963 mg/kg in mice, 1833 mg/kg in rats, and > 2400 mg/kg in rabbits.

Tolerance

Tolerance will develop to the sedative-hypnotic effects within a couple of days of continuous use . After cessation, the tolerance returns to baseline in 7 - 14 days. However, in certain cases this may take significantly longer in a manner which is proportional to the duration and intensity of one's long-term usage.

Temazepam presents cross-tolerance with all benzodiazepines, meaning that after its consumption all benzodiazepines will have a reduced effect. Temazepam also has cross-tolerance with all barbiturates, meaning that after consumption, all barbiturates will have a diminished effect .

Mechanism of action

Benzodiazepines bind nonspecifically to benzodiazepine receptors, which affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell .

Mode of use

Orally (swallowed as a tablet/capsule, drunk as an oral solution)

The tablets are sometimes crushed and taken nasally (snorted) and the gelcaps are known to have been used intravenously (injected into the limbs, groin or neck) .

Tablets and oral solution will be swallowed. Users have been known to inject temazepam - it causes extreme irritation and tissue damage if intravenously injected along with the other risks associated with using drugs in this way .

Effects

Common

• diarrhoea,
• dry mouth,
• feeling of constant movement of self or surroundings,
• headache,
• nausea,
• sensation of spinning,
• unusual dullness,
• feeling of sluggishness ,
• drowsiness and tiredness that may persist into the next day,
• nervousness,
• dizziness,
• feeling hungover-like the next day .

Infrequent

• false or unusual sense of well-being,
• fear,
• nervousness,
• mood or mental changes,
• difficult or laboured breathing,
• fast, irregular, pounding, or racing heartbeat or pulse,
• loss of appetite,
• loss of memory,
• nightmares,
• problems with memory,
• hallucinations,
• shakiness and unsteady walk,
• shortness of breath,
• tightness in the chest,
• trouble sleeping,
• uncontrolled eye movements,
• unsteadiness, trembling, or other problems with muscle control or coordination,
• unusual excitement, nervousness, restlessness, or irritability,
• weight loss,
• wheezing .

Allergic reaction

• blurred vision,
• change in consciousness,
• confusion,
• decreased or absent reflexes,
• difficult or troubled breathing,
• postural hypotension,
• irregular, fast, slow, or shallow breathing,
• loss of consciousness,
• cyanosis,
• shortness of breath,
• sleepiness,
• unusual drowsiness,
• unusual tiredness or weakness .

Physical effects

• muscle relaxation,
• physical euphoria,
• perception of increased weight,
• motor control loss,
• respiratory depression,
• sedation,
• seizure suppression,
• decreased heart rate,
• dizziness .

Cognitive effects

• cognitive euphoria,
• compulsive redosing,
• delusions,
• dream potentiation,
• amnesia,
• analysis suppression,
• anxiety suppression,
• confusion,
• disinhibition,
• emotion suppression,
• information processing suppression,
• language suppression,
• memory suppression,
• motivation suppression,
• thought deceleration .

Positive

• anti-anxiety,
• sedative,
• muscle relaxant.

Negative

• high addiction potential,
• withdrawals can be fatal,
• risk of blackout,
• inability to drink,
• inability to drive,
• loss of balance,
• memory loss,
• procrastination,
• "hangover",
• long term effects .

Overdose

• severe thought deceleration,
• slurred speech,
• confusion,
• delusions,
• respiratory depression,
• coma,
• death .

Risks

Short-term

• overdose especially if mixed with alcohol or other depressant substances,
• respiratory depression,
• coma,
• death .

Long-term

• physical dependence,
• tolerance .

Addiction

Temazepam is extremely physically and psychologically addictive. Temazepam is considered to be significantly more addictive than other benzodiazepines .

Dangerous interactions

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Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption .

• Depressants (1,4-Butanediol, 2-methyl-2-butanol, alcohol, barbiturates, GHB/GBL, methaqualone, opioids) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Stimulants - It is dangerous to combine benzodiazepines with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of benzodiazepines, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of benzodiazepines will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only dosing a certain amount of benzodiazepines per hour. This combination can also potentially result in severe dehydration if hydration is not monitored .

Dangerous

• Alcohol - Ethanol ingestion may potentiate the CNS effects of many benzodiazepines. The two substances potentiate each other strongly and unpredictably, very rapidly leading to unconsciousness. While unconscious, vomit aspiration is a risk if not placed in the recovery position. Blacking out and memory loss is almost certain.
• GBL / GHB - The two substances potentiate each other strongly and unpredictably, very rapidly leading to unconsciousness. While unconscious, vomit aspiration is a risk if not placed in the recovery position.
• Opioids - Central nervous system and/or respiratory-depressant effects may be additively or synergistically present. The two substances potentiate each other strongly and unpredictably, very rapidly leading to unconsciousness. While unconscious, vomit aspiration is a risk if not placed in the recovery position Blackouts/memory loss likely
• Tramadol - Central nervous system- and/or respiratory-depressant effects may be additively or synergistically present. Vomit aspiration a risk when passed out, lay down in recovery position if ingested .

Unsafe

• PCP - Both substances potentiate the ataxia and sedation caused by the other and can lead to unexpected loss of consciousness at high doses. While unconscious, vomit aspiration is a risk if not placed in the recovery position. Memory blackouts are likely .

Overdose

Benzodiazepine overdose may occur when a benzodiazepine is taken in extremely heavy quantities or concurrently with other depressants. This is particularly dangerous with other GABAergic depressants such as barbiturates and alcohol since they work in a similar fashion, but bind to distinct allosteric sites on the GABAA receptor, thus their effects potentiate one another. Benzodiazepines increase the frequency in which the chlorine ion pore opens on the GABAA receptor while barbiturates increase the duration in which they are open, meaning when both are consumed, the ion pore will open more frequently and stay open longer . Benzodiazepine overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly and properly.

Benzodiazepine overdoses may be treated effectively in a hospital environment, with generally favourable outcomes. Benzodiazepine overdoses are sometimes treated with flumazenil, a GABAA antagonist , however care is primarily supportive in nature .

Withdrawal

Withdrawal symptoms or rebound symptoms may occur after ceasing usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction .

• seizures,
• memory loss,
• agoraphobia,
• anxiety,
• panic attacks .

Drug testing

How long temazepam is detectable in the body depends on many variables, including which kind drug test is being used and the amount of the drug that you have taken. Temazepam - also known as benzodiazepine - can be detected for a shorter time with some tests, but can be 'visible' for up to three months in other tests.

The timetable for detecting temazepam in the system is also dependent upon each individual's metabolism, body mass, age, hydration level, physical activity, health conditions and other factors, making it almost impossible to determine an exact time temazepam will show up on a drug test .

The following is an estimated range of times, or detection windows, during which temazepam and other drugs in this category of benzodiazepines can be detected by various testing methods -

How long will temazepam show up in a urine test?

Temazepam can be detected in a urine sample for 1 - 6 weeks .

How long does temazepam stay in the blood?

A blood test for Temazepam will detect the drug from 6 to 48 hours .

How long is temazepam detectable in saliva?

A saliva test for Temazepam will detect the drug for 1 - 10 days .

How long does temazepam stay in the hair?

Temazepam, like many other drugs, can be detected with a hair follicle drug test for up to 90 days .

Harm reduction advice

Temazepam can interact with a number of other medications, such as barbiturates, certain anti-depressants and other benzodiazepines, so it's essential that your doctor knows what you're taking (prescription and non-prescription) before giving it to you.

Alcohol and other recreational substances also have interactions with temazepam. Alcohol in particular will enhance its sedative properties, so you'll feel even sleepier and will sleep longer than just with the drug on its own. If you're taking temazepam it's best to avoid alcohol if possible.

Largely due to the problems caused by users injecting, the gelcaps have not been available on the NHS since 1996. As a result, there is now very little use of temazepam intravenously .

• temazepam is very dose sensitive and can quickly become addictive. If you've been prescribed it, stick to the dose stated and don't be tempted to self-dose,
• even small increases can have significant effects. If you overdose, get medical help immediately,
• don't suddenly stop taking it, even if the problem it was prescribed for seems to have cleared up; the shock to your system can be painful and possibly dangerous. Talk to your doctor about slowly reducing the dose,
• if you've bought temazepam on the street, try to make sure you know what size dose it contains; the tablets are most often 10mg or 20mg, but the capsules can contain quite a lot more. Sometimes this will be imprinted on the tablet/capsule itself, but not always. The difference in effect between the different sizes can be big, so be careful,
• the effects can come on quicker than you might be expecting, so make sure you're somewhere safe (preferably at home) and don't drive or operate machinery, etc. when you've taken a dose,
• on the other hand, you may not feel the effects for some time. If you don't feel an immediate effect, DO NOT re-dose; just wait to see what happens. If you've bought from a dealer you can't be sure of exactly what you've got, so it may be impure or not temazepam at all. If in doubt, or you don't get the effect you were looking for, just write it off .

Paraphernalia

If injected, needles, syringes and water .

History

Temazepam was first synthesised in the mid-1960's, but its potential use for treating sleep disorders was not fully appreciated until the early 1970's.

In the 1980's, temazepam became one of the most widely used prescription drugs in the UK for recreational purposes. Following a series of deaths linked to the substance (though probably actually due to its interactions with other substances commonly used alongside it, such as alcohol and heroin) the recreational use of temazepam was considered a serious and growing problem.

Prescribed temazepam is currently available through the NHS in a generic (unbranded) form. However, different manufacturers may use their own initials/logos on the products, and some illicit manufacturers may attempt to mimic these in order to make their product appear 'legitimate'. In the US, temazepam is best known under the brand name 'Restoril', and some capsules bearing this name have been found on the streets in the UK .

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