Need help with direct liquid micro taper plan

Hello,

 

I’ve read through the boards here about vodka tapering, and I’d like some feedback on the plan I’m developing for my partner. He’s been on 2mg of ethyl loflazepate for 7+ years. It's not commonly prescribed, so here are 2 links with info : http://cdn.neiglobal.com/content/pg/live/loflazepate.pdf and here : http://self.gutenberg.org/articles/benzodiazepine_equivalence

 

2 mg of ethyl loflazepate is equivalent to 10 mg of valium, but he’s not going to switch because loflazepate has a long half-life (51-103 hr), and he doesn’t want to deal with adjusting to a new medication, or finding a sympathetic doctor (unlikely here in Portugal). He’s going to start with a very low daily micro-taper of -.2 ml, and increase to .5ml if possible. If my math is correct, that’s a 5% taper rate per month, working towards a 10% taper if he tolerates it.

 

I’m planning on using a total of 120 ml of liquid per dose. If I understand correctly, I need to find 40% vodka. Absolut brand would work fine I'm guessing ? I dissolve 2 ml of vodka per 1 mg of benzo. So that comes to 4ml of vodka solution + 116 ml of water ?

 

Stahl's Guide (link above) says patients can make a solution with fruit juice. I'm thinking of using apple juice instead of water. Has anyone tried this ?

 

Also I came across this nifty spreadsheet that automatically does the math for you. Has anyone used this before, and if not can you have a look and tell me if it’s legit ?

 

https://docs.google.com/spreadsheets/d/1YAVJk2IqttgwD-wYk9TmKf_Tr2z5rsdCAKUjKypLEKI/edit#gid=0

 

Many thanks ! 

Anybody there ?

Sorry aplusb, I had hoped someone would come along to help you, I'm terrible at this stuff. 

 

Have you seen this tool, if you'll click on liquid, it will take you to another page so you can tap on the read me first in the lower right hand corner.  There is a ton of information there.  I hope this will help you get started until someone smarter than me comes along.

 

http://benzo.alwaysdata.net/             

 

Take a look and let me know what you think.         

Thanks Pamster. I had seen that tool and tried to figure out how to use it, but it's confusing to me. Also, the medication he is on is not on the list unfortunately. I'll just sit tight here, and bump up my post if no one responds in the coming days. Thanks for the support

Hello,

 

I’ve read through the boards here about vodka tapering, and I’d like some feedback on the plan I’m developing for my partner. He’s been on 2mg of ethyl loflazepate for 7+ years. It's not commonly prescribed, so here are 2 links with info : http://cdn.neiglobal.com/content/pg/live/loflazepate.pdf and here : http://self.gutenberg.org/articles/benzodiazepine_equivalence

 

2 mg of ethyl loflazepate is equivalent to 10 mg of valium, but he’s not going to switch because loflazepate has a long half-life (51-103 hr), and he doesn’t want to deal with adjusting to a new medication, or finding a sympathetic doctor (unlikely here in Portugal). He’s going to start with a very low daily micro-taper of -.2 ml, and increase to .5ml if possible. If my math is correct, that’s a 5% taper rate per month, working towards a 10% taper if he tolerates it.

 

I’m planning on using a total of 120 ml of liquid per dose. If I understand correctly, I need to find 40% vodka. Absolut brand would work fine I'm guessing ? I dissolve 2 ml of vodka per 1 mg of benzo. So that comes to 4ml of vodka solution + 116 ml of water ?

 

Stahl's Guide (link above) says patients can make a solution with fruit juice. I'm thinking of using apple juice instead of water. Has anyone tried this ?

 

Also I came across this nifty spreadsheet that automatically does the math for you. Has anyone used this before, and if not can you have a look and tell me if it’s legit ?

 

https://docs.google.com/spreadsheets/d/1YAVJk2IqttgwD-wYk9TmKf_Tr2z5rsdCAKUjKypLEKI/edit#gid=0

 

Many thanks ! 

 

Hello aplusb-

 

Description Ethyl Loflazepate occurs as a whitecrystal-12line powder.13It  is  sparingly  soluble  in acetonitrile,  slightly  soluble  in 14ethanol (99.5), and practically insoluble in water.

 

solubility of ethyl loflazepate

 

Because Ethyl Loflazepate is "barely soluble in water and only slightly soluble in alcohol" I would suggest you make a suspension.

 

A solution of 1mg per 10 ml is all that is needed (.10mg/1ml). To make this use a suspension vehicle such as Ora-Plus or Humco

 

How many mgs are his tablets? Combining tablets along with the liquid may be advantageous.

Hi Gudruna,

 

Thanks a ton for your response!

 

He's taking one 2mg tablet a day since 7 years.

 

Would you suggest crushing it in a mortar and pestle beforehand ?

 

How do you do daily micro-tapers with such a small amount of liquid ? Or is it cut and hold only ?

Yes, crush tablets into a very fine powder.

 

Using 1ml 100 increment syringe and 10ml syringe makes it possible to reduce small amounts daily. So to reduce 5% from 2mg in 30 days one would reduce .003mg per day (2mg x .05 = .10mg/30 days = .003mg reduction per day)

Re: crushing the tablets ...

 

I have no personal experience with this but I did find the article linked below of interest and thought you might as well.  It’s about a formulation for a compounded, 1mg/mL suspension of lorazepam developed by a team of pharmacists at the University of Utah College of Pharmacy, Primary Children’s Medical Center in Salt Lake City, and Children’s Hospital of Philadelphia.

 

Instead of using the traditional approach of grinding tablets in a mortar and pestle, they placed the tablets in a pre-measured, marked amber glass bottle.  Next, they added “the minimum volume of sterile water necessary for tablet dispersion. The bottle was shaken until the tablets were dispersed and a slurry was formed.”  Next, they added the suspending vehicle “QS to volume” (i.e. to the pre-measured mark on the bottle). This method of preparation was selected to reduce drug loss due to surface transfer.

 

As an aside, press-in adapter caps make it easy to draw the correct amount of liquid from a bottle into an oral syringe.

 

For more information and details:

 

Wan-Man Ellaria Lee, Ralph A. Lugo, William J. Rusho, Mark MacKay, and John Sweeley. (2004). Chemical Stability of Extemporaneously Prepared Lorazepam Suspension at Two Temperatures. The Journal of Pediatric Pharmacology and Therapeutics: October 2004, Vol. 9, No. 4, pp. 254-258. Accessed online at: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3469120/pdf/i1551-6776-9-4-254.pdf

Hi Gudruna,

 

I am having a little trouble understanding how to micro-taper. If I understand correctly, I should crush and mix one 2 mg tablet with 20 ml of an oral suspension vehicle. How do I calculate the ml equivalent of .003 mg ? Would that be a reduction of .03 ml per day ? Sorry, my brain is not good with math at the moment.

 

I have already purchased some 1 ml syringes here. Can you verify that is the right size ?[nobbc]https://www.amazon.co.uk/gp/product/B01IF3LDF4/ref=ppx_yo_dt_b_asin_title_o00_s00?ie=UTF8&psc=1[/nobbc]

 

I also got some 10 ml syringes from another website, and a mortar and pestle, so I'm good to go with supplies.

 

Many thanks for your help. This is scary.

 

Edit: Deactivated commercial link.

 

 

Libertas ! Thank you for that link. You BB people are awesome. I will take a close look at it, and may post back here with questions in the coming days. Happy Friday !

Hey there! Have you considered whole fat milk as a binding agent? Theres a youtuber guide on this. I'm at work right now but I would he happy to share that with you if interested.

Hi Zurek. I did consider it, but my partner is not a fan of the milk. Thanks for the suggestion all the same.

Hi Gudruna,

 

I am having a little trouble understanding how to micro-taper. If I understand correctly, I should crush and mix one 2 mg tablet with 20 ml of an oral suspension vehicle. How do I calculate the ml equivalent of .003 mg ? Would that be a reduction of .03 ml per day ? Sorry, my brain is not good with math at the moment.

 

I have already purchased some 1 ml syringes here. Can you verify that is the right size ?[nobbc]https://www.amazon.co.uk/gp/product/B01IF3LDF4/ref=ppx_yo_dt_b_asin_title_o00_s00?ie=UTF8&psc=1[/nobbc]

 

I also got some 10 ml syringes from another website, and a mortar and pestle, so I'm good to go with supplies.

 

Many thanks for your help. This is scary.

 

Edit: Deactivated commercial link.

 

After reading Libertas post above I think this method would be better rather than crushing the tablets with a mortar and pestal.

 

This is how I would prepare my 1ml=.10mg suspension:

1) Put 1 - 2mg tablet in a suitable container

2) Add 2ml distilled water.

3) Once the tablet is dispersed add 12ml of the suspension vehicle and 6ml of water

4) Shake well. Remove and take dose

 

Does the 1ml syringe you ordered have 100 markings on it?(It is hard to tell in the photo) If so, this syringe will work fine.

 

So to get the .003mg daily reduction you simply remove 3 lines using the 1ml 100 increment syringe increasing 3 lines everyday.

 

Click here for a detailed image.

A million thanks to you both. This makes sense now. 

Hey friends,

 

I am having trouble locating an oral suspending vehicle here in Portugal, apart from deliveries from the U.S. that cost a fortune. Maybe I'm not translating it well, but not getting many results in the EU. Is there something available in Europe ? I can have packages sent to me from Belgium, France and the U.K. if I can't locate it here.

Hey friends,

 

I am having trouble locating an oral suspending vehicle here in Portugal, apart from deliveries from the U.S. that cost a fortune. Maybe I'm not translating it well, but not getting many results in the EU. Is there something available in Europe ? I can have packages sent to me from Belgium, France and the U.K. if I can't locate it here.

 

If you are not able to find a suspension agent in your area this is a option for you to consider. Xanthan gum is used as a suspension agent. 

 

click image to enlarge

 

Click here for the link.

 

When I made the Xanthun gum suspension vehicle I only used the Xanthun Gum, warm water & citric acid(preservative)and glycerin. I made it every 5 days so spoilage was not a factor, and did not care about adding a sweetener.

 

Oh dear. I missed this post, aplusb.

 

Have you tried contacting the pharmacies in your area to ask if they could supply you with a suspending agent and/or advise you on where you could purchase same?

 

 

Thank you both. I will look into this. It seems that state-funded compounding pharmacies are very common here, and everyone has access to public healthcare, so that may explain why there is a dearth of oral suspension products readily available for making one's own concoction. I did check with one pharmacy, Libertas, but they did not even know what an oral suspension vehicle was. I will check with a larger one in a last ditch effort, but I may have to take to making my own brew as mention by Gudruna.

Gudruna,

 

Can you give me the exact measurements of the mixture you made ? That sounds pretty easy to me.

Good idea to try a larger pharmacy - perhaps one at a hospital?

 

You mentioned you could get items shipped from the UK.  It looks like Medisca UK stocks OraPlus, OraSweet, and OraBlend (link below).  The catch is that Medisca only sells to compounding pharmacies (not individuals).  Do you know someone in the UK who would be willing to work with a pharmacy in the UK to obtain a supply for you and then ship it to you? 

 

Just brainstorming here ... Gudruna’s suggestion sounds promising.

 

MEDISCA Products | Bases | Pharmaceutical compounding

https://www.medisca.co.uk/products/compounding-bases/oral

Gudruna,

 

Can you give me the exact measurements of the mixture you made ? That sounds pretty easy to me.

 

It is easy...

 

Measurements using a gram scale:

 

.20 grams  of Xanthan Gum (approx. 1/8th of a tsp)

2ml vegetable glycerin (approx. 1/3 tsp)

.10 grams citric acid (preservative)(1/16th of a tsp)

Enough distilled water to make 100ml (1ml=.10mg)

 

How to make a 1ml=.10mg oral suspension:

1) Put 5- 2mg tablets of ethyl loflazepate in a 100ml graduating cylinder

2) Add 10ml distilled water. Let sit until tablets disintegrate

3) Add glycerin, Xanthan gum and citric acid. Shake well

4) Add enough distilled water to bring suspension to the 100ml mark (approx. 90ml)

store in cool dry place.

 

Sample taper reducing 10% of 2mg every 30 days making daily reductions.

Thanks a lot for that Gudruna.

So no need to cook it, warming the distilled water is sufficient?

Also, can you recommend a good gram scale ?

Okay, so hubby went and purchased some Flavor Plus at 50 € a pop for the first couple of months. He seems rather eager to get this thing started, so we'll begin with that, and may switch to making our own concoction a little later in the game. Thanks for all your support and guidance !

Glad to hear that you found a suspension vehicle. Good luck and let us know how it goes

Hello Gudruna. I'm back. My partner has still not started his taper plan. We were unable to obtain a suspension vehicle at a reasonable price, and with the pandemic, it took two months for it to arrive. Fed up, and not willing to make our own concoction and mess with syringes, we're going to switch to a dry taper. Can I turn to you for some advice ?