Benzos Rectal administration of Diazapam(Valium) - A guide and an experience report!

[floopysnow]

An experiment into rectal administration of diazapam
I have included my own trip report, but for the adventurous you may consider the following as a guide on how to do it yourself, although please adjust the dose to fit your tolerance/experience.

I have wanted to try both volumetric dosing and rectal administration of diazapam for quite some time as I have heard through various sources that despite diazapam already has a good bioavailibility, it does in fact have a higher rectal bioavailibility, as well as a much faster onset of action, and decided to conduct an experiment of my own, as there seems to limited information on the use of rectal diazapam. The few of posts I found on bluelight and /r/drugs were not particularly informative.
For volumetric dosing where you intend on using the oral route of administration, I must recommend using propylene glycol, as diazapam's solubility is almost three times than with vodka. I have not done any tests on rectal administration of propylene glycol/diazapam, but I plan to experiment with this further in the future.

15ml ethanol dissolves 1000mg of diazapam (Source: HSDB)
Vodka is typically 37.5-40% ethanol
1ml of vodka contains 0.375-0.400ml
1ml of vodka can dissolve 23.8-26.7mg of diazapam

I planned to take 80mg rectally - I wanna say now that I have naturally high tolerance, and I've been taking about 20-30mg each day for the last week or two, so I do not recommend this as a normal test dose to anyone. I wanted the effects of the test dose to be strong enough so that I could notice and document each effect as they manifested. Sources are at the bottom of the report. If anyone else is considering attempting what is written here, please adjust the dosage to fit your tolerance and be careful - better safe than sorry. To a first timer I would recommend 10-20mg maximum.

THE TEST
[T-00:10] For my test dose I needed at least 3.36ml of vodka to dissolve 80 mg, I dissolved 80mg of diazapam in little blue tablet form, '10mg' a tablet, in 4ml of vodka just to be sure. I would be using 2ml rather thin oral syringes

[T-00:00] Time of dosing: about 22:00
I set up my patch on the floor to begin the experiment, with a pillow for company I lay on my side and lift my leg slightly to make it easier to insert the syringe. Once in almost as far as it could go (syringe roughly 2-3 inches in length), I pushed down on the plunger quickly, which was immediately proceeded by a mild burning sensation up my abdomen which indicated a successful dosing and that the vodka/diazapam solution has been dispersed along rectum and sigmoid colon. The syringe was then washed and this step was then repeated for the remaining 2ml of vodka solution.

[T+00:02] I would continue to lay on my side and then my front as I gave the vodka/diazapam solution time to absorb, and could already begin to feel a heaviness and calmness starting to spread throughout my body, seemingly originating from my abdomen which was still burning slightly, though fading slowly. I also used this time to pour a small amount of cider into the shot glass I had used to mix the vodka and diazapam pills where there was still some residue blue sludge, which I drank down with the cider (let none go to waste!)

[T+00:05] The previously stated feelings continued to build in intensity during this time. After five minutes, the mild burning in my abdomen was completely gone and I felt comfortable enough about not 'spilling' to stand up and make my way to the bath room.
Immediately I noticed drastic decrease in motor control, my mind was blissfully blank, and not subjected at all to my usual anxiety-induced thought loops and feeling of impending doom. I got to the bathroom to clean up and was pleased to see no blue residue on my toilet paper, meaning I hadn't 'lost' any (the vodka/diazapam solution had been made with these little blue 10mg pills, and so the resulting solution was pretty blue).

[T+00:30] At this point I am in divine comfort, I feel as if was peaking on at least 4-5mg of Xanax, but with that beautiful diazapam muscle relaxation. I'm just sitting here in pure contentedness, playing Killing Floor for some shits and giggles, and it was actual a blast - I used to play invite sniper/scout for TF2, so I am pretty good with FPSs - time felt slightly slowed and I felt like I was hitting more headshots due to my patience in aiming.

[T+01:30] I now just feel like I normally would if I have just taken the diazapam dose normally, but with the added feeling of having had a couple of drinks on top.
I completely forget to take my antidepressant/sleep aid 15mg Mirtazapine that night, not that I needed it.

[T+11:00] The next day at 9:00, which is early for me, I wake up still feeling relaxed and content, and feeling more refreshed than usual! I go and make myself a coffee. I feel content and non-anxious for most the day. I would normally take a 10mg diazapam tablet when I wake up, but I didn't feel the need this time, and ended up only using a half tablet, 5mg around 22:00 as I heard of some news that was difficult to cope with, and then about an hour later I took my usual 15mg Mirtazapine before getting into bed

SUMMARY / TL|DR
Rectal administration of diazapam in a vodka solution (for all intents and purposes: 37.5-40.0% ethanol with the remaining water) provided a significantly faster onset than orally administered diazapam with minimal discomfort and had a length of duration the same as orally administered diazapam.
Also anyone who is worried about boofing alcohol, in the volumes used there is no risk of overdosing on 2ml or 4ml of vodka! (Other than it might dry out your butt a bit... although I experienced minimal discomfort).

(Source: HSDB) https://pubchem.ncbi.nlm.nih.gov/compound/Diazepam#section=Solubility

 

[Lynn d]

Can you use isopropyl alcohol?

 

[floopysnow]

Can you use isopropyl alcohol?

I would say yes, but I would be very wary about using isopropyl alcohol, it's not the best stuff to drink, let alone do rectally, it could be really dangerous.
I don't know the bioavailability of isopropyl alcohol nor how much diazapam/other benzos you can dissolve in it, so I wouldn't recommend it - although I would say probably both ethanol and isopropyl would be quite good solvents for benzodiazapines and derivatives regardless.

Your best bet in my opinion is to get either 'pure' ethanol prolly 99% or everclear ('bout 97% if I remember correctly and you can probably by it at your local liquour store for a extortionate price at to buying 'pure' ethanol online and having it delivered). Take their ABV% into mind when dosing. One dose should ideally be, for a single dose, about 1ml of the ethanol containing solution, and then 1ml of water, when using a 2ml syringe, which is my prefered size for rectal dosing, and then go to town! Look up a rectal dosing guide if you want to know the best method.

 

[gaboxadol]

Can you use isopropyl alcohol?

I realize I am reviving an old thread here, but other solvents for benzodiazepines commonly include Propylene Glycol ( PG ) which is often used as the sole solvent in RC benzo oral tinctures and it would work for this type of rectal administration as well, I have done so successfully. I would like to add as well, the IV diazepam USP formulation uses the following recipe as a carrier solution for the drug, which should apply to most typical 1,4-diazepine drugs.

IV Diazepam USP ( source: diazepam injection US pharmacopeia monograph )
Diazepam Injection, USP is a sterile, nonpyrogenic solution intended for intramuscular orintravenous administration. Each milliliter (mL) contains:

• 5 mg diazepam;
• 40% propylene glycol
• 10% alcohol;
  • USP grade uses ethyl alcohol which you could use in the form of 40% vodka or 90% everclear or whatever else you can find locally as long as you do the math on how much water you are adding and subtract it from the amount you use for the solution overall.
• 5% sodium benzoate and benzoic acid added as buffers;
  • Not sure what the pH is like without the buffer, I have made these solutions for IV/IM and rec admin and measured the pH and found it to be inoffensive for infrequent use but adjusting it with a buffer is definitely best practive here. Buffers are acid-conjugate base paired solutions, i.e citric acid + sodium citrate solution in a given ratio, which help said solution resist changes in pH due to the addition of H+ or OH- ions, i.e when you add an acid or base like HCl or NaOH for example, which it can now resist due to the equilibrium of ion concentrations formed by the conjugate acid-base pair's substituent ions.
• 1.5% benzyl alcohol ( added as a preservative )
  • if you are making this solution for rectal administration no sterility is needed, though for immediate IV use, sterilization via heat ( see note below ) or 0.22micron membrane filter.
    • To achieve sterility, a holding time of at least 15 min at 121°C (250 °F) with full exposure to steam/water and at a pressure of 100 kPa / 15 psi. Also, 3 min can be achieved with a temp of 134 °C (273 °F) at the same pressure.
    • And as for membrane filters, Nylon membrane 0.22 micron filters, preferably 25mm diameter though 13mm is doable but slower, are compatible with all compounds in our solution, however the ethanol/water ratio can cause the nylon membrane to swell/shrink and with time dissolve or puncture, PTFE can be used despite it's hydrophobicity due to the mixture with a water-miscible solvent, in our case ethanol/propylene glycol. PES should only be used if the Benzyl Alcohol preservative is ommited as this will cause the filter to break/dissolve and compromise sterility!! 0.22 micron is required for removing sufficient bacterial/viral/particulate contaminants to determine the resulting solution sterile and biocompatible.
• Solution pH of 6.6 (approx. ranging from 6.2 to 6.9).

I have replicated this recipe using other buffers that I happened to have at my disposal at the time of preparation with success but make sure to do all the appropriate calculations for your chosen buffer, i.e citrate buffer, phosphate buffer, For a scalable recipe, the table below contains a breakdown of the milligram quantities of each compound in the example solution totalling 1mL in volume:

Summary:

Compound / Ingredient​	Desired Mass:​	Approx. Volume​
Propylene Glycol: 1 mL × 40% = 0.4 mL Mass = 0.4 mL × 1.036 g/mL ≈ 0.4144 g ≈ 414.4 mg	~414.4 mg​	40% ( 0.400 mL )​
Ethyl Alcohol [1]: 1 mL × 10% = 0.1 mL Mass = 0.1 mL × 0.789 g/mL ≈ 0.0789 g ≈ 78.9 mg [2]	~78.9 mg​	10% ( 0.100 mL )​
pH Buffer: - Sodium Benzoate:​ - Benzoic Acid:​ 1 mL × 5% = 0.05 mL [3] Mass of Sodium Benzoate = 0.025 mL × 1.497 g/mL ≈ 0.0374 g ≈ 37.4 mg Mass of Benzoic Acid = 0.025 mL × 1.265 g/mL ≈ 0.0316 g ≈ 31.6 mg	~37.4 mg ~31.6 mg​	5% ( 0.050 mL ) * combined​
Benzyl Alcohol [4]: 1 mL × 1.5% = 0.015 mL Mass = 0.015 mL × 1.044 g/mL ≈ 0.0157 g ≈ 15.7 mg	~15.7 mg​	1.5% ( 0.015 mL )​
Water ( H2O ) [5]:	~422mg [6]​	43.5% ( 0.435 mL )​
Total [7]:​	~1000mg​	1mL​

Table Notes:
Referenced by [x] notation in table above where X is corresponding to the numbered list order below;

• [1]: Again, can be subbed for Isopropyl Alcohol / Isopropanol of same conc. and numbers are roughly the same, if you're worried do calculations with respective density of isopropanol, but I am sure it's +/- <= 1mg, insignificant. Assumes: an ethanol concentration of 95% w/o drying though anhydrous ( ~99% ) would be preffered for accuracy of the measurements when done either by mass or volume and the resulting ethanol/water/PG ratio; however, small differences here are tolerated both by the body and the solution as well as our given benzo's solubility in it.
• [2]: This calculation assumes 95% ethyl alcohol, generally what it will tend to given it doesn't like to remain anhydrous, so if not using reagent grade undenatured ethanol and assuming no mol seives or magnesium sulfate drying process, for example, was done then this is likely what you possess if it was distilled well. If using a different concentration, adjust the water content accordingly. Again, isopropanol can probably substitute fine here as well and only alters the calculations by +/- 0.5mg likely.
• [3]: Assuming an equal mix of sodium benzoate and benzoic acid, this may need to be adjusted based on empircal measurement of the pH when prepping the solution, i.e tests can be run beforehand without the active ingredient to estimate the ratio of our sodium benzoate / benzoic acid in the buffer. Adjustments can be made to the final solution to perfect the pH to the ideal ~6.5 value for this solution, you could try to get even closer to the rough 7.4 pH value of blood though this would be experimental and there is likely good reason for the USP formulation to have this specified pH value, and it's a widely used medication and is only considered ( in practice and from what I've read/heard & experimented with ) slightly more caustic or irritating to the venous tissue or muscle tissue than say something like 0.9% saline.
  
• [4]: Benzyl alcohol is an optional preservative, recommended in IV/IM multi-dose vial preparations. Conc. >= ~2-3mg/mL can be harmful to health and generally are not more beneficial to long-term sterility of the solution than 0.9% or 1.5% conc. when sealed in a sterile multi-dose vial in a cool, dark location.
• [5]: distilled pure H2O or as close as possible, Addipak unit-dose vials are a good source of sterile water, ensure water source is free of sodium chloride ( i.e don't use saline ), and also from other ions or dissolved minerals as would be found in city water or bottled water, and finally, if using bacteriostatic ensure that you're not adding addition benzyl alcohol which is used there as a preservative though if you do the math to ensure numbers add up you can sub/add to make the same end solution given your starting matertials.
• [6]: dilute to 1mL volumetrically in a grad cylinder as final step in preparation, or if weighing by mass do a final check of the total volume to ensure that the BZD concentration, which is measured volumetrically is accurate to that of the desired concentration. Typically mg/mL concentrations of most BZDs trends towards 2,5, or 10mg/mL due to solubility and potency differences.
  

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• **[7][ IMPORTANT ]**: If you remove either the buffer or preservative, i.e benzoic acid/sodium benzoate (5%) or benzyl alcohol (1.5%) respectively, ensure that their mass/volume percentage is accounted for in the final mass/volume of the solution. An easy way to do this is to replace the roughly 0.65mL or ~75mg of these substances ( assuming both are removed ) with some extra solution of 40% PG + 10% ethyl alcohol + 50% sterile distilled water, or simply 50/50 PG/water can be used.
  • [7.1]: Secondly, but less important, is a note on the fact that the 1g/mL density assumed for our final solution is just for simplicity and volume should be preffered at 20C otherwise use mass when working in non-STP conditions, i.e while heating/stirring to mix.

Assumptions of Densities:
These are the density values in g/mL I used for each given substance when performing these calculations. As the exact type of ethanol and its water contents are not known and vary based on sourced materials available to you, the numbers below and the resulting mass and volume calculations may be slightly different, though any differences will be nominal most likely, as long as you use a milligram scale and grad cylinder and only measure volume after heating solution if that's necessary for dissolution of the benzo.

• Propylene Glycol: ~1.036 g/mL
• Ethyl Alcohol (95%): ~0.789 g/mL
• Sodium Benzoate: ~1.497 g/mL
• Benzoic Acid: ~1.265 g/mL
• Benzyl Alcohol: ~1.044 g/mL
• Water: ~1 g/mL