Uncommon Benzodiazepines: Difference between revisions
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Revision as of 15:04, 13 January 2015
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.
Alprazolam - Short acting anxiolytic. High affinty for AX BZD subunits
Clonazepam - Chlorinated derivative of nitrazepam. Up to 50 hour HL
Diazepam - The gold mother fucking 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 soluable, shit burns snorted. wat. 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 less side effects than normal benzos.
Temazepam - 3-OH hypnotic. Approved in the US (ofc) for short term treatment of insomnia. Typical benzo, but is fairly euphoric.
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 God damn. 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
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. Metabolises 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 - Strongest hypnotic benzo available, 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 nordesmethyldiazepam and oxazepam (wat?)
Quazepam - Trifluoroethyl (Make it a methyl god dammit) Selectivly targets GABA(A) subtype A1 which is responsible for sleep. Subs completely in animals in Ambien/Lunesta (PLEASE GET ME THIS)
Tetrazepam - Weak muscle relaxing anxiolytic
Triazolam - Short activity, heavy sedative, very euphoric. Was a common benzo in the US until it wa found that use in the elderly was known to cause deaths, now it is rarely prescribed.
Zolazepam - Used with Tiletamine as a ventinary 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 soluable benzo, that is mostly anxiolytic.
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 selevctive 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. 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.
CP-1414S - Related to Clobazam potency nearly similar, but more sedation.
Triflubazam - Related to Clobazam, long half life and duration.
Girisopam - selective anxiolytic action with no sedative, anticonvulsant or muscle relaxant effects
Talampanel - Noncompetitive antagonist of the AMPA receptor.
Flubromazolam - Related to triazolam and pyrazolam. Maybe a mix in the middle in potency. So .75 ~= 10 Diazepam?
Bretazenil - Highly potent, partial GABAa agonist with less tolerance than normal. Possible base for better social drug than alcohol.
Climazolam - Similar in structure to triazolam and is used in veterinary medicine for anesthetizing 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.
Oxazolam - Prodrug for desmethyldiazepam.
Ciclotizolam - Partial agonist at GABA(A), similar binding affinity to brotizolam, but a low efficacy... very very interesting.
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.
Ripazepam - Related to Zolazepam.
Zomebazam - Anxiolytic properties, strucutally related to Razobazam and Zometapine.
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
Clazolam - Fused benzodiazepine and tetrahydroisoquinoline derivative. Anxiolytic and antidepressant properties.
Avizafone - Water soluable prodrug to Diazepam, can be IM'd. Used mainly as an antidote to poisoning with Organophophate nerve agents.