Uncommon Benzodiazepines

BENZODIAZEPINE DERIVATIVES -> Agonise the GABAa receptors which result in sedative, hypnotic, anxiolytic, anticonvulsant, and muscle relaxant properties. They are useful in treating anxiety, insomnia, agitation, seizures, muscle spasms, alcohol withdrawal and as a premedication for medical or dental procedures. However due to these effects they are considered to be major drugs of abuse. If they are used intravenously and are non-water soluble (as the vast majority of benzos are); abscesses, cellulitis, thrombophlebitis, arterial puncture, deep vein thrombosis, and gangrene can occur. In general, benzodiazepines are safe (very high LD50) but can be taken in overdoses and can cause dangerous deep unconsciousness. If mixed with other classes of sedatives, opioids or alcohol (the main cause of fatality when mixed with heavy alcohol use); the potential for toxicity and fatal overdose increases. Very effective in short term use, although cognitive impairments and paradoxical effects such as aggression or behavioral disinhibition can occur. A minority react reverse and contrary to what would normally be expected. Long-term use is controversial due to concerns about adverse psychological and physical effects, increased questioning of effectiveness, and, because benzodiazepines are prone to cause tolerance, physical dependence, and, upon cessation of use after long-term use, a withdrawal syndrome. The elderly are at an increased risk of suffering from both short- and long-term adverse effects,810 including an associated roughly 50% increase in the risk of dementia, especially with Triazolam which can cause death in the elderly.

COMMON

Alprazolam - Short acting anxiolytic. High affinty for AX BZD subunits

Clonazepam - Chlorinated derivative of nitrazepam. Up to 50 hour HL

Diazepam - The gold standard. Used in Alcohol withdrawals and benzodiazepine withdrawals.

Flurazepam - Very long half life (Up to 250 hours) which makes it practically useless as a hypnotic, but... hmm. Interesting.

Lorazepam - 3-OH benzo. Has mild affinity for all subunits.

Lormetazepam - ^^

Midazolam - Water soluble, Is now used other than Pentobarbital in Lethal Injection.

Nitrazepam - Typical benzo. Tolerance raises fast.

Oxazepam - Typical benzo. Moderate affinity for all. Slow onset.

Prazepam - Long half life (up to 224hrs) however fewer side effects than normal benzos.

Temazepam - 3-OH hypnotic. Approved in the US for short term treatment of insomnia. Typical benzo, but is fairly euphoric.

COMMON OVERSEAS

Bentazepam - Only Spain.

Cinolazepam - Pretty much just as a Hypnotic.

Clotiazepam - Thienodiazepine, Stage 2 NREM sleep is significantly increased by this drug. Effective in short term management of anxiety. Used in France/Japan. 95+ BA orally. 6-18 HL.

Cloxazolam - Metabolised into delorazepam. Uh... Increased heart rate for some? No sense. Typical benzo other than that.

Loprazolam - Imidazole deriv. Marketed for short term treatment of insomnia.

Medazepam - Must have someone smarter than me read this as I understand none of it. But yeah... *

Nordazepam - Active metabolite of Diazepam/Chlordiazepoxide/Clorazepate/Prazepam/Pinazepam/Medazepam. Up to 200 hour half life.

Tofisopam - anxiolytic but no anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties. PDE10A inhibitor, so could be useful in schizophrenia

SOUTH-EAST ASIAN

Etizolam - Unscheduled in Western countries, so has become an RC too.

Fludiazepam - Strong Diazepam analogue, 4x binding affinity of Diazepam.

Flutazolam - Japanese benzo

Flutoprazepam - Longer acting and more potent than diazepam. Japanese.

Haloxazolam - Marketed in Japan. Comparing Estazolam and Haloxazolam found that haloxazolam only affects gamma motor neurons, where the other effects both.

Mexazolam - Benzo derivative effective for only one week and losing effectiveness at 3 weeks

Nimetazepam - Sold under "Erimin" and is scripted short term for severe insomnia. 95%+ Oral BA. Hypnotic effects felt within 30 minutes. And hits peak plasma level within an hour, and the mean HL is 14-30 hours. N-Methyl analogue of Nitrazepam, to which it partially metabolises into. Which has a long half life, so, carefulness. (lol being careful)

Rilmazafone - Water soluble japanese benzo

Adinazolam - Triazolobenzodizepine (TBZD) Was apparently made to enhance the antidep effect of alprazolam. Odd drug. Metabolites are A-OH-alprazolam (Nomenclature blows) and estazolam.

Brotizolam - Extremely potent benzo active at 80-100ug.

Camazepam - Benzo with reduced side effects such as impaired cognition. Metabolites into Temazepam.

Clobazepam - selective ω2 agonist on the GABAa receptor. Non-hypnotic. GABA(B)

Flumazenil - GABA(A) ANTAGONIST. I don't understand this at all. It's something.

Flunitrazepam - High potency, causes heavy amnesia (commonly referred to as a date-rape drug). Only prescribed in the worst of cases for insomnia and is only prescribed for short-term use.

Ketazolam - Similar effects to Diazepam. With less sedation.

Pinazepam - Fucking odd wiki page. Something something fetus... But, has a propargyl group for whatever reason. Appears to produce anxiolytic shit in animals. Main metabolites are nor-desmethyldiazepam and oxazepam.

Quazepam - Trifluoroethyl, Selectively targets GABA(A) subtype A1 which is responsible for sleep. Subs completely in animals in Ambien/Lunesta.

Tetrazepam - Weak muscle relaxing anxiolytic

Triazolam - Short activity, heavy sedative, very euphoric. Was a common benzo in the US until it was found that use in the elderly was known to cause deaths, now it is rarely prescribed.

Zolazepam - Used with Tiletamine as a veterinary anaesthetic. Telazol is 1:1 ratio of the compounds. 4x potency of diazepam.

Flubromazepam - Slightly weaker than Diazepam, focuses mainly on anxiolytic effects.

Diclazepam - 2-choloro of Diazepam. Faster onset, less "hangover" the next day.

Estazolam - Superior to Triazolam

Nifoxipam - Metabolite of Flunitrazepam

Phenazepam - Potent soviet benzo, now RC.

Pyrazolam - Water soluble benzo, that is mostly anxiolytic.

1,4-BENZODIAZEPINES

Cyprazepam - Typical benzo.

Delorazepam - Typic benzo. Delorean-azepam!

Doxefazepam - Deriv. of flurazepam, and was 2-4x potent, and also being half as toxic.

Elfazepam - Typical benzo but stimulates appetite like Devazepide.

Flutemazepam - 3-hydroxy analogue of temazepam, looks fucking perfect on paper! COME ON GUYS.

Fosazepam - water soluble analogue of diazepam however low potency. (.6:1)

Gidazepam - Soviet benzo.

Halazepam - Less potential to cause hostility and aggression than diazepam.

Meclonazepam - Showing up on the RC market. Just think legal Clonazepam, and that's probably what we have here. Also has anti-parasitic effects against the parasitic worm "Schistosoma Mansoni"

Menitrazepam - Similar in structure to tetrazepam and nimetazepam. 7-chloro group of tetrazepam replaced with nitro by the looks. Mainly hypnotic, but effects take longer to come up.

QH-II-66 - Highly selective GABAa5 agonist which was created to replicate the effects of alcohol.

Quazepam - 200-hour half-life hypnotic benzo.

Reclazepam - Similar effects to other benzo deriv's. A short duration of action.

Ro5-2904 - High affinity for GABA(A)

Sulazepam - Thioamide deriv. of Diazepam. Metabolised into diazepam/desmethyldiazepam/oxydiazepam. No clue on potency.

Tolufazepam - Nothing on it. Sulphur is in... I dunno anymore.

1, 5-BENZODIAZEPINES

CP-1414S - Related to Clobazam potency nearly similar, but more sedation.

Triflubazam - Related to Clobazam, long half life and duration.

2, 3-BENZODIAZEPINES

Girisopam - selective anxiolytic action with no sedative, anticonvulsant or muscle relaxant effects

Talampanel - Noncompetitive antagonist of the AMPA receptor.

TRIAZOLOBENZODIAZEPINES

Flubromazolam - Related to triazolam and pyrazolam. Maybe a mix in the middle in potency. So .75 ~= 10 Diazepam?

IMIDAZOBENZODIAZEPINES

Bretazenil - Highly potent, partial GABAa agonist with less tolerance than normal. A possible base for a better social drug than alcohol.

Climazolam - Similar in structure to triazolam and is used in veterinary medicine for anaesthetizing animals. Interesting.

FG-8205 - Related to Bretazenil, slight selectivity for a1, little sedation.

Imidazenil - Partial GABAa agonist, blocks sedative effects of other benzos, does not produce tolerance or addiction.

Iomazenil (123I) -

Remimazolam - Similar to Midazolam but faster acting and shorter lasting than <<. Water soluble.

Ro48-6791 - Similar to Midazolam but 4-6x the potency, faster acting and shorter lasting than <<. Water soluble.

SH-053-R-CH3-2′F - Has high selectivity, binding affinity and efficacy at the a5 subtype, also blocks the nootropic effects of an inverse agonist? No shit.

OXAZOLOBENZODIAZEPINES

Oxazolam - Prodrug for desmethyldiazepam.

THIENODIAZEPINES

Ciclotizolam - Partial agonist at GABA(A), similar binding affinity to brotizolam, but a low efficacy... very very interesting.

PYRIDODIAZEPINES

Lopirazepam - Pyridodiazepine analogue of lorazepam. Assume same effects yet less potent, never marketed. Yet scheduled. Thanks america.

Zapizolam - Pyridodiazepine analogue of triazolam. Less in potency I'd assume.

PYRAZOLODIAZEPINES

Ripazepam - Related to Zolazepam.

Zomebazam - Anxiolytic properties, structurally related to Razobazam and Zometapine.

PYRROLODIAZEPINES

Premazepam - Partial GABA(A) agonist. More "derpy" than diazepam itself the first day, but more than one day apparently that switches? Hmm. Odd. 7.5mg ~= 5mg Diazepam. HL = 10-13 hours

TETRAHYDROISOQUINOBENZODIAZEPINES

Clazolam - Fused benzodiazepine and tetrahydroisoquinoline derivative. Anxiolytic and antidepressant properties.

BENZODIAZEPINE PRODRUGS

Avizafone - Water soluable prodrug to Diazepam, can be IM'd. Used mainly as an antidote to poisoning with Organophosphate nerve agents.