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Thread: Lorazepam re: lipid solubility

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    Lorazepam re: lipid solubility 
    #1
    Bluelighter Gormur's Avatar
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    Hopefully this won't be moved to BDD as i often find specific questions of mine left unanswered there...

    So far i know that lorazepam is partially soluble in alcohol & lipid soluble, tho to a small degree. I don't know the B/A. I suppose dosing on an empty stomach helps speed up the process & deter any hindrance to the absorption process

    I drink 20ml WGFJ 30 minutes pre-dose on an empty stomach. After i take the dose (sublingually), i lie there somewhat relaxed but unable to sleep. I know it takes a while to absorb this way, due to the low lipid solubility - which also makes me wonder if by using this MOA i'm wasting much of the active drug

    I thought about plugging, but i suppose we're dealing with the same issue here - lipid solubility

    Please note i have zero tolerance to benzos atm; altho i've been on my fair share over the years & may have a natural tolerance above what is typical

    My script is .5mg ativan - yes it's low. I had to take 2.5mg last night to voluntarily fall asleep - altho i slept well -- altho I do not want to take that much if i can take less without wasting anything & still be effective

    Any suggestions on MOA would be greatly appreciated.

    I'm open to IVing if it's relatively safe & has a higher B/A

    -G

    I found this, regarding intranasal administration of lorazepam:
    http://jcp.sagepub.com/cgi/content/abstract/41/11/1225

    according to this, nasal admin has a high bioavailability- around 77%
    Last edited by Gormur; 12-05-2010 at 23:11.
     

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    #2
    Greenlighter
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    Thanks for the article, I found it quite interesting.

    As with anything, obviously IV will get you the highest B/A and fastest onset.

    SWIM is interested in the specifics of how to prepare IV ativan. It is not soluble in water, and after SWIM did their best scouring forums trying to weed out bs about using isopropyl alcohol and how "it can't be done, just sub-lingual it" I think SWIM will try ethanol (80 proof vodka). You can use higher proof, but all alcohol is diluted and it doesn't really affect anything if you account for the water in it.

    Here is an article regarding solubility http://pubget.com/paper/pgtmp_6a18fb...abaced6c949037 (fyi 303.2 K is approx. 41 deg F)

    In pharm ampoules they use propylene glycol which SWIM will not even attempt to mess with.

    So SWIM will probably use about 15-20 units of 40% ethanol solution ( vodka ) which is about 6-8 units pure alcohol. SWIM should also probably have a micron wheel filter to seperate out as much of the binders and fillers as possible, but SWIM will get one if this method seems viable.

    Another thing I was reading about is the damage of alcohol on veins. The amount of damage done is directly proportional to the concentration of alcohol in the solution and the amount injected. So the key is to try to use the smallest amount of alcohol while still dissolving as much lorazepam as possible.

    So I will report back on how SWIM's little experiment goes...

    If I had your same problem, I would probably insufflate it, as according to your article it has an even faster onset than IM and a good B/A. Best of luck to you and be safe.
     

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    #3
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    This is stupid, lorazepam is well-absorbed orally or sublingually/buccaly.

    IV administration is needlessly risky and painful. It's possible if you use silly mixes of things like propylene glycol, ethanol, and water, but even then it's just stupid to inject etahnol with any sort of frequency!

    Don't inject vodka! It will lead to brusing, swelling, scarred vains, pain, Bad Things, the cops coming to your house, and herping the derp too much.

    Also we don't SWIM here.

    Modes of administration were: A, intravenous injection; B, deltoid intramuscular injection; C, oral tablets in the fasting state; D, sublingual dosage of oral tablets in the fasting state; and E, sublingual dosage of specially formulated tablets in the fasting state. ...
    Absorption of intramuscular lorazepam was rapid. Peak plasma levels were reached at 1.15 hr after dosage, with absorption half-life averaging 14.2 (+/- 4.7) min. Absorption or oral and sublingual lorazepam tended to be less rapid than intramuscular injection, although differences were not significant. Times of peak concentration were 2.37, 2.35, and 2.25 hr postdose for trials C,D, and E, respectively; values of absorption half-life were 32.5, 28.5, and 28.7 min. Absolute systemic availability for trials B, C, D, and E averaged 95.9, 99.8, 94.1, and 98.2%, respectively; none of these differed significantly from 100%. Values of t1/2 beta were highly replicable within individuals regardless of the administration route. Thus, sublingual lorazepam is completely absorbed and is a suitable administration route in clinical practice.
    Tl;dr The only difference between the modes of administration is the time to onset. Lorazepam is 100% absorbed through all routes.
    This thread is getting closed because it's not very advanced at all.
    Last edited by sekio; 07-01-2012 at 03:49.
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    #4
    Administrator Vaya's Avatar
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    You know, there are two benzodiazepines that I get paradoxical effects from - one being, to a mild extent, clonazepam - the other, to a FAR greater extent, is lorazepam (Ativan). It makes me feel as though I've taken some ambien and chosen to stay awake past the 30-minute mark. Restlessness, mild visual disturbances, dysphoria... Maybe this is what you're encountering, unless you've taken it successfully in the past.

    ~ vaya

    Quote Originally Posted by sekio
    IV administration is needlessly risky and painful. It's possible if you use silly mixes of things like propylene glycol, ethanol, and water, but even then it's just stupid to inject etahnol with any sort of frequency!

    Don't inject vodka! It will lead to brusing, swelling, scarred vains, pain, Bad Things, the cops coming to your house, and herping the derp too much.
    Ditto that, my brother.
     

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