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Diazepam (Also known as Diastat; Valium; Zetran) is a [[Benzodiazepines|benzodiazepine]] that is commonly used to treat a large range of conditions from anxiety to Meniere’s Disease. It possesses anxiolytic, anticonvulsant, hypnotic, sedative, skeletal muscle relaxant, and amnesic properties. It is also one of the most commonly used drugs to taper off of other [[Benzodiazepines|benzodiazepines]]/[[Alcohol]] withdrawal.


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= History =
<td valign="top" width="50%"><strong>Other Names</strong>


7-chlor-1,3-dihydro-1-methyl-5-phenyl-2H-1,4benzodiazepin-
Diazepam was the second [[Benzodiazepines|benzodiazpine]] (The first of which was Librium) invented by Dr. Leo Sternbach of Hoffmann-La Roche at the company’s Nutley, New Jersey, facility. It was released in 1963 as an improved version of Librium, it became incredibly popular.
Diazepam was the top-selling pharmaceutical in the United States from 1969 to 1982, with peak sales in 1978 of 2.3 billion tablets.


2-on, sleeping pill, tranquilizer,
= Formulations =
It is available in instant release formulations of 2mg, 5mg, and 10mg tablets.


Valium
It is also available in an oral solution of 5mg/5ml (1mg/ml)


Substance type: benzodiazepine


Diazepam, better known as Valium, was originally
= Doses =


synthesized in the laboratory and introduced as a
NOTE: Higher doses have an increased risk of blacking out.


therapeutic drug (psychopharmaca, tranquilizer)
{| class="wikitable"
|+ Oral
| Light || 2.5-5mg


in the 1960s. The substance produces sedative,
|-


euphoric, and especially anxiolytic (anxietyreducing)
| Common || 5-15mg


effects (Henningfield 1988, 17,35*).
|-


During the investigation of diazepam's
|Heavy || 15-30mg+


pharmacology, it was discovered that the human
|}


nervous system has a special receptor for this
= Duration =
Note: Duration can be significantly longer with higher doses.
{| class="wikitable"
|+ Oral
|-
| Onset || 30-90 Minutes
|-
| Total || Up to 24 hours, Main effects are generally felt for roughly 8-12 hours.
|}


molecule, known as the benzodiazepine receptor


or the [3H] -diazepam receptor. Luk et al. (1983)
= Effects =
== Positive ==
*Euphoria
*Relaxation
*Anti-Anxiety effects


found three isoflans in the urine of cattle that may
== Neutral ==
*Drowsiness
*Appetite fluctuation


possibly dock (as neurotransmitters) in the
== Negative ==
*Memory loss
*Blackout potential
*Motor skill impairment
*Dizziness
*Depression
*Irritability, aggression, rage
*Personality changes
*Emotional and social dissociation or de-realization (long term use)


benzodiazepine receptor. It is known that the
= Harm Reduction =
When on high doses of [[Benzodiazepines|benzodiazepines]], users are likely to black out and potentially hurt themselves through a variety of adventures. If you are using it as a sleep aid, it's recommended to continue doing what you're doing until you begin to feel drowsy, then go to bed.
Some users report Diazepam (and [[Benzodiazepines|benzodiazepines]] in general) to lead to compulsive redosing, trying to find a “high” which is where a fair amount of the point above comes from. To avoid this keep doses low and be wary of reduced inhibitions while under the influence of Diazepam.
== Interactions ==
As with other depressants, Diazepam should not be combined with any other CNS depressants (such as [[Alcohol]]), at the risk of respiratory depression, which can lead to death.


kavapyrones (cf. Piper methysticum) bind to the
See the [[Drug combinations]] chart for more information.


[3H] -diazepam receptor. Recently, flavonoids in
= Chemistry and Pharmacology =
Diazepam can be administered orally, intravenously (Has to be diluted, as it is painful and damaging to veins), intramuscularly, or as a suppository.
Peak plasma levels occur between 30 and 90 minutes after oral administration and between 30 and 60 minutes after intramuscular administration; 10-45 minutes for Rectal, and between 1-5 minutes intravenously.
Diazepam is highly protein-bound, with 95-99% of the absorbed drug being protein-bound.
Diazepam is highly lipid-soluble, and is widely distributed throughout the body after administration. It easily crosses the blood-brain-barrier. After absorption, diazepam is redistributed into muscle and adipose tissue. Continual dialy doses of Diazepam quickly build to a high concentration in the body (mainly in adipose tissue)
Diazepam unergoes oxifative metabolism by demethylation (CYP 2C9, 2C19, 2B6, 3A4, and 3A5) hydroxylation (CYP 3A4 and 2C19) and glucuronidation in the liver as part of the cytochrome P450 enzyme system.
The main active metabolite of diazepam is Desmethyldiazepam (Nordiazepam) Other metabolites inclue minor active metolites temazepam and oxazepam. 


the buds of the South American linden tree (Tilia
= Legal Status =
== International ==


tomentosa Moench; Tiliaceae; cf. tila) were found
Diazepam is a schedule IV controlled drug under the Convention on Psychotropic Substances.
== UK ==


to bind to the benzodiazepine receptor. A
Classified as a Class C drug.


substance found in Passiflora caerulea 1. (cf.
[[Category:Chemicals]]


Passiflora spp.), 5,7-dihydroxyflavone, also docks
[[Category:Drugs]]


to the same location (Viola et al. 1994).
[[Category:Depressant]]
 
The benzodiazepine receptor has been shown
 
to be present in all vertebrates, suggesting that it
 
appeared at a very early date in the evolution of
 
the nervous system and has been preserved into
 
the present. This indicates that it plays an
 
important function in the nervous system and that
 
there are endogenous substances that bind to it in
 
order to transmit certain messages (Muller 1988).
 
But what do these substances look like? At first
 
they were thought to be polypeptides, but then
 
traces of diazepam and desmethyldiazepam were
 
discovered in the brains of humans and other
 
animals. Because diazepam and its initial
 
metabolite appear in breast milk and the placenta
 
after the ingestion of Valium (Wessen et al. 1985),
 
it was first believed that the diazepam must have
 
been introduced into the body from outside" But
 
when diazepam was subsequently also found to be
 
present in brains that dated to a time before the
 
discovery of Valium synthesis, it was concluded
 
that diazepam was not a synthetic chemical at all
 
but a naturally occurring neurotransmitter in the
 
nervous system (Muller 1988). Thus it was
 
demonstrated that "Valium, the very symbol of
 
chemical psychopharmaca" (Zehentauer 1992,
 
121 *), is actually a natural substance.
 
Pharmacologists were surprised when subsequent
 
research demonstrated the presence of diazepam
 
and desmethyldiazepam in potatoes (Solanum
 
tuberosum 1.; cf. Solanum spp.) and in such diverse
 
grains as wheat (Triticum aestivum 1.; cf. beer),
 
corn/maize (Zea mays), and rice (Oryza sativa 1.;
 
cf. sake) (Muller 1988). Valium, in other words, is
 
a natural active constituent in plants. However, the
 
concentration in these plants is so low that a
 
person would likely not notice any Valium effects
 
even after consuming a whole sack of potatoes.
 
Valium is one of the most widely used sedative
 
drugs in modern society and is normally prescribed
 
for the treatment of anxiety and sleeping
 
disorders.498 Not surprisingly, Valium also finds
 
use as a recreational drug in some circles, particularly
 
in combination with other substances. Its
 
euphoric properties can be greatly affected by
 
alcohol, which can at times counteract the sedative
 
properties, resulting in powerful stimulating effects.
 
Valium is one of the more commonly used
 
psychopharmaca in the music scene. Several rock
 
bands, including the classic "space rock" band
 
Hawkwind CValium 10," 1978), have dedicated
 
titles to the substance.</td>
<td valign="top" width="53%"><strong>Commercial Forms and Regulations
 
</strong>Valium is available by prescription only. In the
 
United States, it is listed as a Schedule IV drug
 
under the Controlled Substances Act.<strong></strong>
 
Literature
 
Flesch, Peter. 1996. SchlafstOrungen bei iilteren
 
Patienten: Auf Benzodiazepine kann meist
 
verzichtet werden. Jatros Neurologie 12:6-7
 
(interview).
 
Henningsfield, Jack E. 1988. Barbiturates: Sleeping
 
potion or intoxicant. The Encyclopedia of
 
Psychoactive Drugs. London, Toronto, and New
 
York: Burke Publishing Company.
 
Luk, Kin-Chun, Lorraine Stern, Manfred Weigele,
 
Robert A. O'Brien, and Nena Sprit. 1983.
 
Isolation and identification of "diazepam-like"
 
compounds from bovine urine. Journal of
 
Natural Products 46 (6): 852-61.
 
Muller, Walter E. 1988. Sind Benzodiazipine 100%
 
Natur? Deutsche Apotheker Zeitung126 (13): 672-74.
 
Viola, H., C. Wolfman, M. Levi de Stein, C.
 
Wasowski, C. Pena, J. H. Medina, and A. C.
 
Paladini. 1994. Isolation of pharmacologically
 
active benzodiazepine receptor ligands from Tilia
 
tomentosa (Tiliaceae). Journal of
 
Psychopharmacology 44:47-53.
 
Wesson, Donald R, Susan Camber, Martha Harkey,
 
and David E. Smith. 1985. Diazepam and
 
desmethyldiazepam in breast milk. Journal of
 
Psychoactive Drugs 17 (1): 55-56.</td>
</tr>
 
</table>

Latest revision as of 05:36, 26 June 2015

Diazepam (Also known as Diastat; Valium; Zetran) is a benzodiazepine that is commonly used to treat a large range of conditions from anxiety to Meniere’s Disease. It possesses anxiolytic, anticonvulsant, hypnotic, sedative, skeletal muscle relaxant, and amnesic properties. It is also one of the most commonly used drugs to taper off of other benzodiazepines/Alcohol withdrawal.


History

Diazepam was the second benzodiazpine (The first of which was Librium) invented by Dr. Leo Sternbach of Hoffmann-La Roche at the company’s Nutley, New Jersey, facility. It was released in 1963 as an improved version of Librium, it became incredibly popular. Diazepam was the top-selling pharmaceutical in the United States from 1969 to 1982, with peak sales in 1978 of 2.3 billion tablets.

Formulations

It is available in instant release formulations of 2mg, 5mg, and 10mg tablets.

It is also available in an oral solution of 5mg/5ml (1mg/ml)


Doses

NOTE: Higher doses have an increased risk of blacking out.

Oral
Light 2.5-5mg
Common 5-15mg
Heavy 15-30mg+

Duration

Note: Duration can be significantly longer with higher doses.

Oral
Onset 30-90 Minutes
Total Up to 24 hours, Main effects are generally felt for roughly 8-12 hours.


Effects

Positive

  • Euphoria
  • Relaxation
  • Anti-Anxiety effects

Neutral

  • Drowsiness
  • Appetite fluctuation

Negative

  • Memory loss
  • Blackout potential
  • Motor skill impairment
  • Dizziness
  • Depression
  • Irritability, aggression, rage
  • Personality changes
  • Emotional and social dissociation or de-realization (long term use)

Harm Reduction

When on high doses of benzodiazepines, users are likely to black out and potentially hurt themselves through a variety of adventures. If you are using it as a sleep aid, it's recommended to continue doing what you're doing until you begin to feel drowsy, then go to bed. Some users report Diazepam (and benzodiazepines in general) to lead to compulsive redosing, trying to find a “high” which is where a fair amount of the point above comes from. To avoid this keep doses low and be wary of reduced inhibitions while under the influence of Diazepam.

Interactions

As with other depressants, Diazepam should not be combined with any other CNS depressants (such as Alcohol), at the risk of respiratory depression, which can lead to death.

See the Drug combinations chart for more information.

Chemistry and Pharmacology

Diazepam can be administered orally, intravenously (Has to be diluted, as it is painful and damaging to veins), intramuscularly, or as a suppository. Peak plasma levels occur between 30 and 90 minutes after oral administration and between 30 and 60 minutes after intramuscular administration; 10-45 minutes for Rectal, and between 1-5 minutes intravenously. Diazepam is highly protein-bound, with 95-99% of the absorbed drug being protein-bound. Diazepam is highly lipid-soluble, and is widely distributed throughout the body after administration. It easily crosses the blood-brain-barrier. After absorption, diazepam is redistributed into muscle and adipose tissue. Continual dialy doses of Diazepam quickly build to a high concentration in the body (mainly in adipose tissue) Diazepam unergoes oxifative metabolism by demethylation (CYP 2C9, 2C19, 2B6, 3A4, and 3A5) hydroxylation (CYP 3A4 and 2C19) and glucuronidation in the liver as part of the cytochrome P450 enzyme system. The main active metabolite of diazepam is Desmethyldiazepam (Nordiazepam) Other metabolites inclue minor active metolites temazepam and oxazepam.

Legal Status

International

Diazepam is a schedule IV controlled drug under the Convention on Psychotropic Substances.

UK

Classified as a Class C drug.

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