Temazepam

Temazepam is a drug of the benzodiazepine class. Benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at R₁ and R₄. The benzyl ring of temazepam is substituted at R₈ with a chlorine group. Further, the diazepine ring is bonded at R₅ to a phenyl ring. Temazepam also has a hydroxyl group bonded to the 3-position of the diazepine ring.

Temazepam is a white, crystalline substance, very slightly soluble in water, and sparingly soluble in alcohol.

Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors.^[5] 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 GABA_A 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.^[6]

Its main pharmacological action is to increase the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABA_A receptor. This causes sedation, motor impairment, ataxia, anxiolysis, an anticonvulsant effect, muscle relaxation, and a reinforcing effect. As a medication before surgery, temazepam decreased cortisol in elderly patients. In rats, it triggered the release of vasopressin into paraventricular nucleus of the hypothalamus and decreased the release of ACTH under stress.^[7]

In a single- and multiple-dose absorption, distribution, metabolism, and excretion (ADME) study, using tritium-labelled drug, temazepam was well absorbed and found to have minimal (8%) first-pass drug metabolism. No active metabolites were formed and the only significant metabolite present in blood was the O-conjugate. The unchanged drug was 96% bound to plasma proteins. The blood-level decline of the parent drug was biphasic, with the short half-life ranging from 0.4-0.6 hours and the terminal half-life from 3.5–18.4 hours (mean 8.8 hours), depending on the study population and method of determination.^[8]

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), a research literature based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be regarded with a healthy degree of skepticism. It is worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become much more likely with higher doses and may include addiction, serious injury, or death.

Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

• Erowid Experience Vaults: Temazepam

Temazepam has a low toxicity relative to dose.^[14] However, it is potentially lethal when mixed with depressants like alcohol or opioids.

It is strongly recommended that one use harm reduction practices when using this substances. These include volumetric liquid dosing.

Dependence and abuse potential

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

Tolerance will develop to the sedative-hypnotic effects within a couple of days of continuous use.^[15] 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.

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.^[16][17] For more information on tapering from benzodiazepines in a controlled manner, please see this guide.

Benzodiazepine discontinuation is notoriously difficult; it is potentially life-threatening for individuals using regularly to discontinue use without tapering their dose over a period of weeks. There is an increased risk of hypertension, seizures, and death.^[18] Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

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.

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 GABA_A receptor, thus their effects potentiate one another. Benzodiazepines increase the frequency in which the chlorine ion pore opens on the GABA_A 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^[19]. Benzodiazepine overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly and properly.

Symptoms of a benzodiazepine overdose may include severe thought deceleration, slurred speech, confusion, delusions, respiratory depression, coma or death. Benzodiazepine overdoses may be treated effectively in a hospital environment, with generally favorable outcomes. Benzodiazepine overdoses are sometimes treated with flumazenil, a GABA_A antagonist^[20], however care is primarily supportive in nature.

Dangerous interactions

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.

Internationally, Temazepam is included under the United Nations Convention on Psychotropic Substances as a Schedule IV substance.^[21]

• Australia: Temazepam is listed in Schedule 4, making it a prescription only medicine.^{[citation needed]}
• Austria: Temazepam is legal for medical use under the AMG (Arzneimittelgesetz Österreich) and illegal when sold or possessed without a prescription under the SMG (Suchtmittelgesetz Österreich).^{[citation needed]}
• Canada: Temazepam is listed on the CSDA in Schedule IV.^[22] It requires a prescription.
• Germany: Temazepam is controlled under Anlage III BtMG (Narcotics Act, Schedule III)^[23] as of August 1, 1986.^[24] It can only be prescribed on a narcotic prescription form, except preparations which contain up to 20 mg temazepam in each dosage form.^[23]
• Hong Kong: Temazepam is listed in Schedule 1.^{[citation needed]}
• Ireland: Temazepam is listed in Schedule 3 of the Misuse of Drugs Act 1977 as of November 22, 1993.^[25]
• The Netherlands: In the Netherlands, temazepam is a List 2 substance of the Opium Law and is available with a prescription.^{[citation needed]}
• Portugal: Temazepam is a Schedule IV controlled substance.^[26]
• Russia: Temazepam is a Schedule III controlled substance since 2013.^[27]
• South Africa: Temazepam is a Schedule 5 controlled substance.^{[citation needed]}
• Sweden: Temazepam is a prescription drug in List IV (Schedule 4) under the Narcotics Drugs Act (1968).^[28]
• Switzerland: Temazepam is a controlled substance specifically named under Verzeichnis B. Medicinal use is permitted.^[29]
• Thailand: Temazepam is listed in Schedule II of the Psychotropic Substances Act.^{[citation needed]}
• United Kingdom: Temazepam is a Class C controlled substance under the Misuse of Drugs Act 1971.^[30]. Medical professions must follow specific instructions for the prescribing and disposal of temazepam.
• United States: Temazepam is a prescription medication assigned to Schedule IV of the Controlled Substances Act by the DEA.^[31] Many states in the United States require that individuals have specially encoded prescriptions for temazepam.

• Responsible use
• Psychoactive substance index
• Entactogens
• Alcohol
• Benzodiazepines
• Depressants

• Temazepam (Wikipedia)
• Temazepam (Erowid Vault)
• Temazepam (Isomer Design)