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KLEINERkIFFER'S BRILLIANTLY UNBOWLDERIZED BENZODIAZEPINE BALLAD THE BENZODIAZEPINE INFODATADOSEMEGATABLE |
Disclaimer:Nobody here is licensed to even drive, do not use this as medical advice
What are benzos?
Benzodiazepines, often shortened simply as "benzos", are a class of GABAergic psychoactive drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. The first such drug, chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955, and made available in 1960 by Hoffmann LaRoche.
They are used most commonly to treat anxiety but are also used in the treatment of: insomnia (only short term, as tolerance to the hypnotic properties of benzos builds rapidly), seizures, muscle spasm and alcohol withdrawal.
How do they work?
Benzos are positive allosteric modulators of the GABA-A receptor. Unlike other positive allosteric modulators that increase ligand binding, benzodiazepine binding acts as a positive allosteric modulator by increasing the total conduction of chloride ions across the neuronal cell membrane when GABA is already bound to its receptor. So they work by increasing the efficiency of a natural brain chemical, GABA, to decrease the excitability of neurons. This reduces the communication between neurons and, therefore, has a calming effect on many of the functions of the brain.
The GABA-A receptor consist of different subtypes, the predominant subtypes in the brain being those that contain alpha1-, alpha2-, alpha3-, and alpha5-subunits. Studies show, that 2,3GABA-A receptors are important for mediating the anxiolytic effects of benzodiazepines, while motor effects might involve action primarily at ?1GABA-A receptors. The alpha1-containing???2 receptors seem to mediate sedative, anterograde amnesic, and antimyoclonic actions. Muscle relaxant activity of BZDs is mediated partially by alpha1-, alpha2-, alpha3-, and alpha5-containing ???2receptors.
Hypnotic effects by alpha1 subreceptor sites, anxiolytic, and muscle relaxant effects via alpha2 and alpha3 subsites, anticonvulsant properties via alpha5 subsite
So different benzos have different affinities for the subtypes making every benzo unique in its effects.
Dangerous combinations
Benzodiazepines are CNS depressants and thus can increase the action of other CNS depressants and can increase sedation, provoke a black out, impaired motor coordination, suppressed breathing and other adverse effects that can be lethal. In the most extreme cases, especially when benzos are combined with opioids, death can result, so it is no joke to combine benzos with opioids.
If you don't have a extremely high tolerance to both CNS depressants don't combine them, it is not worth the potentially fatal risk.
Even a normal dose of a benzo and a few beers can result in a black out.
If you insist on doing it, have someone around to have an eye on you! And some naloxone if opioids are involved.
Withdrawal
Benzodiazepine withdrawal is no joke and can be lethal in the worst case, as GABA is the most important inhibiting neurotransmitter and going off cold turkey can result in seizures and has the potential to kill you.
A taper is advised, lookup the Ashton manual, the golden standard for a benzo taper, benzo equivalency, and other benzo information.
Approximately Equivalent Oral dosage means equivalent to 10mg diazepam

Source: benzo.org.uk aka the Ashton Manual ( a small addition by morpheuspapaverus)
Alprazolam
Onset of action: Peak concentrations in the plasma occur in 1 to 2 hours following administration (slightly longer sublingual)
Onset: 15-30 min
Half life: IR around 12 hours (6-12 h),ER 10-16 hours
Duration of action: For immediate release round 4-5 hours
Bioavailability of different ROAs: 80-90% orally
Approximately Equivalent Oral dosage: 0.5 - 1mg
Water solubility: 0.04 mg/ml
Good to know: Metabolism by CYP3A4 ->using WGJ (contains bergamottin) will inhibit the metabolism ->longer duration
Bromazepam
Onset of action: Peak concentrations in the plasma occur in 0.5 - 4 hours following administration
Half life: 10-20 hours
Duration of action:
Bioavailability of different ROAs: 60-84% orally
Approximately Equivalent Oral dosage: 3-6mg
Water solubility: 0.0399 mg/mL
Good to know:Most likely metabolised by an enzyme belonging to the CYP family, could be CYP1A2
Chlordiazepoxide
Onset of action: 15-30min
Half life: 5-30 hours; metabolite around 36-200 hours
Duration of action:
Bioavailability of different ROAs:
Approximately Equivalent Oral dosage:25mg
Water solubility: 2 mg/mL
Good to know:
Clonazepam
Onset of action: 0.5 ?€“ 1 hours
Half life: 18-50 hours (mean 30-40)
Duration of action: 6-12 hours
Bioavailability of different ROAs:Around 90% orally
Approximately Equivalent Oral dosage:0.25-2mg
Water solubility: < 0.1 mg/mL
Good to know: Metabolised by CYP3A4 & N-acetyl transferase 2 (3A4 is more abundant in the body, and so it is the de facto enzyme for metabolism). Also, Clonazepam has serotonergic effects unique to benzodiazepines.
Chlorazepate
Onset of action: intermediate acting, peaks within < 2 hours
Half life: 18-50 hours and up to 200hours for the main metabolite desmethyldiazepam
Duration of action: 4-12hrs
Bioavailability of different ROAs: 91%orally
Approximately Equivalent Oral dosage:15mg
Water solubility:0.0248 mg/mL
Good to know: prodrug for Nordazepam
Note: Clorazepate is COMPLETELY converted to Nordazepam prior reaching the liver; so, the two drugs are effectively identical, so taking 10mg Chlorazepate (Tranxene) is basically like taking 9 or 10 mg pure nordazepam PO
Brand name Tranxene, and commonly used to taper in gabaergic wd
Diazepam
Onset of action: Within 15 min (Peaks 1-2hrs)
Half life: 20-100 hours and up to 200hours for the main metabolite desmethyldiazepam
Duration of action: 1-6 hours
Bioavailability of different ROAs: 93-100% orally; 90% rectal
Approximately Equivalent Oral dosage:10mg
Water solubility: 0.05 mg/mL
Good to know: Metabolized by variousCYPs
Flunitrazepam
Onset of action: 15-30 min
Half life: 18-26 h
Duration of action: 4-8 h
Bioavailability of different ROAs: 64-77% oral, 50% suppository
Approximately Equivalent Oral dosage: 1mg
Water solubility: 0.00858 mg/ml, 166mg/L, 0.0086 g/L
Good to know:
Flurazolam
Onset of action:
Half life: 18-26 h
Duration of action:
Bioavailability of different ROAs: 64-77% orally
Approximately Equivalent Oral dosage: 1mg or less
Water solubility:
Good to know: Metabolised mainly viaCYP3A4
Loprazolam
Onset of action: 2 h for peak serum concentration, but might induce sleep within 30 min
Half life: 6-12 h
Duration of action:
Bioavailability of different ROAs:
Approximately Equivalent Oral dosage: 1-2 mg
Water solubility: 10mg/ml
Good to know: 50 % is metabolised into active metabolite (half life and potency equivalent to loprazolam) rest is excreted unchanged
Lorazepam
Onset of action: 15-30min / delayed onset, peak 2-3 hours
Half life: 10-20 h
Duration of action: 6-12 h
Bioavailability of different ROAs: 85-99% orally; up to 94% sublingually
Approximately Equivalent Oral dosage: 1-2mg
Water solubility: 0.08 mg/mL
Good to know: This is a drug that seems to subjectively differ a lot between individual experiences. Some find it "does nothing" while others feel it is a lot stronger. If you feel no effect, don't just keep redosing.
Midazolam
Onset of action: 15-30 min
Half life: 1.5 - 4 h
Duration of action: 1-6 h
Bioavailability of different ROAs: 31-72% orally
Approximately Equivalent Oral dosage: 2-6mg
Water solubility: 0.024 mg/mL
Good to know:
Nitrazepam
Onset of action: peak plasma concentration in around 2 h
Half life: 15-38 h
Duration of action:
Bioavailability of different ROAs:53-94% oral
Approximately Equivalent Oral dosage: 10 mg
Water solubility: 0.0299 mg/mL, 0.03g/L
Good to know: 10mg seems to be a high dose even though it's the same potency as diazepam on paper. Subjectively, nitrazepam feels a lot stronger despite this, and 5mg is strong for most people.
Nordazepam
Onset of action:
Half life:
Duration of action:
Bioavailability of different ROAs:
Approximately Equivalent Oral dosage:
Water solubility: 57 mg/L
Good to know:
Oxazepam
Onset of action: 30-120 min
Half life: 4-21 h
Duration of action:
Bioavailability of different ROAs:95-96% orally
Approximately Equivalent Oral dosage:20-30mg
Water solubility: 0.179 mg/ml
Good to know: Can suppress cortisol levels [https://www.ncbi.nlm.nih.gov/pubmed/1349754],
Metabolised by glucuronidation
Temazepam
Onset of action: 30-60min
Half life: 8-22 h
Duration of action:
Bioavailability of different ROAs: 96% orally
Approximately Equivalent Oral dosage:20mg
Water solubility:0.164 mg/mL
Good to know: No active metabolites
Triazolam
Onset of action: 15-30 min
Half life: 1-6 h
Duration of action: 1-2 hours
Bioavailability of different ROAs: 44% orally; 53% sublingually
Approximately Equivalent Oral dosage: 0.5mg
Water solubility: 0.00453 mg/mL
Good to know:
Z-Drugs (group of so-called "nonbenzodiazepine" drugs with very different chemistry but effects similar to benzodiazepines)
Zolpidem
Onset of action: 15 min
Half life: 2-3 h
Duration of action: 3 h
Bioavailability: 70% oral
Dosage: 5-30 mg
MoA/Affinities: Zolpidem has about10-fold lower affinity for the alpha2- and alpha3- subunits than for alpha1, and no appreciable affinity for alpha5 subunit-containing receptors.
Good to know: belongs to theimidazopyridine class, may cause sleepwalking, can cause hallucinations in high doses. The Ambien Effect aka "Ambien Walrus."
Zopiclone
Onset of action: peak plasma concentration in 1-2 h
Half life: 3-7 h
Duration of action: 3-9 h
Dosage: 2-7.5 mg
Bioavailability: 75-80% oral
MoA/Affinities: it is regarded as being unselective in its binding to alpha1, alpha2, alpha3, and alpha5
Good to know: belongs to thecyclopyrrolone class, In the United States, zopiclone is not commercially available, although its active stereoisomer, eszopiclone, is sold under the name Lunesta. It is however the most common z-drug prescribed in the UK. Often leaves a metal taste in your mouth next day.
Zaleplon
Onset of action: full concentration inaround 1h
Half life: 1-1.5 h
Duration of action: 1h
Dosage: 5-20 mg
Bioavailability: 30% oral
MoA/Affinities: selectively binds withhigh efficacy to the benzodiazepine site (omega1) on theaplha1-containing GABA-A receptors
Good to know: belongs to thepyrazolopyrimidine class, zaleplon appears to induce sleep withoutdisrupting the natural sleep architecture, may cause hallucinationsin high doses
Antagonist:
Flumazenil
Flumazenil competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex. Because the body does not produce endogenous benzodiazepines, flumazenil only creates behavioural effects when administered concurrently with a benzodiazepine receptor agonist or inverse agonist. It can lower the seizure treshold and can cause agitation and anxiety thus should onlybe administered by a trained medical professional in a clinical setting.
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