7.23.2017 | Nicholas Babcock
[6 ] It is highly recommended to taper one's dose by gradually lowering the amount taken each day for a prolonged period of time instead of stopping abruptly. [7 ]. It's worth noting that the sudden discontinuation of benzodiazepines can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death.
Because flumazenil is a short-acting drug and the effects of diazepam can last for days, several doses of flumazenil may be necessary. Although not usually fatal when taken alone, a diazepam overdose is considered a medical emergency and generally requires the immediate attention of medical personnel. This drug is only used in cases with severe respiratory depression or cardiovascular complications. Artificial respiration and stabilization of cardiovascular functions may also be necessary. The antidote for an overdose of diazepam (or any other benzodiazepine) is flumazenil (Anexate). [19 ] [20 ] [21 ] [22 ].
Certain combinations may be safe in low doses of each but still increase the potential risk of death. The list below contains some common potentially dangerous combinations, but may not include all of them. Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.
[9 ]. The anticonvulsant properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.
[12 ] [13 ]. These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.
Diazepam presents cross-tolerance with all benzodiazepines, meaning that after its consumption all benzodiazepines will have a reduced effect.
[23 ] After cessation, the tolerance returns to baseline in 7-14 days. Tolerance will develop to the sedative-hypnotic effects within a couple of days of continuous use. 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.
Diazepam is regulated in most countries as a prescription drug.
See responsible use section. WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity.
Advantages of diazepam in comparison to certain other benzodiazepines are a rapid onset of action [5 ] and high efficacy rates, which are important for managing acute seizures and panic attacks.
Diazepam, first marketed as Valium by Hoffmann-La Roche, is a benzodiazepine drug. Diazepam is a core medicine in the World Health Organization's Essential Drugs List, the minimum medical needs for a basic health-care system. It possesses anxiolytic, anticonvulsant, sedative, muscle relaxant, depressant and amnestic properties. [2 ] It is commonly used to treat a wide range of conditions including anxiety, panic attacks, insomnia, seizures, muscle spasms, and restless legs syndrome. [3 ] Diazepam, first synthesized by Leo Sternbach, [4 ] has been one of the most frequently prescribed medications in the world since its launch in 1963. It may also be used in some surgical procedures to induce amnesia.
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. [8 ] As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects ) of diazepam on the nervous system.
It is strongly discouraged to consume moderate to heavy dosages of these substances together.
Likewise, adverse effects become much more likely on higher doses and may include injury or death. The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects.
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 [28 ], however care is primarily supportive in nature.
Diazepam has a low toxicity relative to dose. [16 ] However, it is potentially lethal when mixed with depressants like alcohol or opioids.
[24 ] [25 ] For more information on tapering from benzodiazepines in a controlled manner, please see this guide. 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.
DISCLAIMER : PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
The benzyl ring of the bicyclic core is substituted at R 7 with a chlorine group. Diazepam is a drug of the benzodiazepine class. Diazepam also contains an oxygen group double bonded to R 2 of its diazepine ring to form a ketone. Further, the benzodiazepine ring is bonded at R 5 to an aromatic phenyl ring. At R 1, diazepam is substituted with methyl group. Benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at R 1 and R 4. This oxygen substitution at R 2 is shared with other benzodiazepine drugs with the suffix -azepam.
[1 ]. Death may occur when benzodiazepines are combined with depressants such as opiates, barbiturates, thienodiazepines, alcohol or other GABAergic substances.
Additional experience reports can be found here:. There are currently no anecdotal reports which describe the effects of this compound within our experience index.
[26 ] Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal. There is an increased risk of hypertension, seizures, and death. 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.
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 [27 ]. 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. Benzodiazepine overdose may occur when a benzodiazepine is taken in extremely heavy quantities or concurrently with other depressants. Benzodiazepine overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly and properly.
Diazepam is extremely physically and psychologically addictive.
It is strongly recommended that one use harm reduction practices, such as volumetric dosing, when using this substance to ensure the administration of the intended dose.
The oral LD 50 (lethal dose in 50% of the population) of diazepam is 720 mg/kg in mice and 1240 mg/kg in rats. [17 ] D. [18 ]. Greenblatt and colleagues reported in 1978 on two patients who had taken 500 and 2000 mg of diazepam, went into moderay deep comas, and were discharged within 48 hours without having experienced any important complications in spite of having high concentrations of diazepam and its metabolites esmethyldiazepam, oxazepam, and temazepam (according to samples taken in the hospital and as follow-up). J.Diazepam