Drugs Soluble in Ethanol - Pharmacokineticists Help

I have access to clenbuterol in ethanol suspension.

I am cautious with dosing stimulants, how accurate will this suspension be?
Is there any data suggesting ethanol holding the drug “homogeneously”?

Since the dosing of clen is in order of mcg, I would appreciate some peace of mind.

Thanks guys

Your terminology worries me. You have a solution of clen in EtOH or a suspension? Clen is soluble in organic solvents. See here for example:

I’d drop the whole thing if you have no idea what you are doing. But I’d drop the whole thing and I know what I am doing. The solubilities stated above indicate you have little margin for error especially if you don’t know what you are working with.

If you want a second reference you could go here:
image

image

image

Yeah that’s my mistake.
Clenbuterol dissolved in ethanol to form a solution.
So x dose/unit volume.

I guess my question is what are the margins for uncertainty.
Since we are working with roughly 250 mcg/ml, and the bottle is 10ml.

This is all from a lab I do trust. (I am not mixing any products)
I would just appreciate more information of how accurate solutions are with the distribution of the drug.

1 Like

I would think that adding more ethanol would make dosing more accurate (edit: precise is the right word here).

For example, it is easier to do 40 mcg dose from 50 mcg/mL solution, than it is to do it from 250 mcg/mL solution.

Also, if you turn your 250 mcg/mL 10 mL solution into 5 50 mcg/mL 10 mL solution containers, the risk of settling and getting way more than you want towards the bottom is minimized, since each container contains less total clen.

1 Like

Why would observing a suspension in the vial at room temp be a huge red flag based on what i posted above and the presumed stated concentration?

I know this forum is for fun* and entertainment* but you guys need to be more careful or do more study before you mess with this stuff.

:man_facepalming:

image

I have never worked with oral solutions (as I corrected above not a suspension).
I was just curious if anyone could share data or information about how accurate dosing an oral solution is.

No need to be a dickhead about it.

Abstract

Clenbuterol is an oral β2-agonist utilized as an illicit substance for performance-enhancement or weight loss. We report a case of a 23-year-old male who presented with anxiety and chest tightness after intentional ingestion of 5000 μg of clenbuterol (125 times the recommended adult dose) to lose weight. His electrocardiogram showed sinus tachycardia and diffuse nonspecific repolarization abnormalities with mild inferolateral ST-segment depression. Bloodwork revealed a potassium of 2.0 mmol/L, peak lactate of 9.4 mmol/L, and peak troponin of 5.39 μg/L. A transthoracic echocardiogram was normal except for hyperdynamic left ventricular function. He was treated with intravenous fluids and oral metoprolol. His tachycardia and electrocardiogram abnormalities resolved after 48 h. Clenbuterol has gained notoriety in recent years as a drug of abuse and cases of toxicity will likely continue to increase due to its relative attainability and readily accessible online dosing information. Patients often present with agitation, palpitations, tachycardia, hypokalemia, and hyperglycemia. Treatment is supportive with intravenous fluids, β-blockers, and potassium supplementation.

< Learning objective: Clenbuterol, an oral β2-agonist, can be utilized as an illicit substance for performance-enhancement or weight loss. Cardiac toxicity and type II myocardial infarction can occur with clenbuterol overdoses. Associated symptoms include agitation, palpitations, tachycardia, hypokalemia, and hyperglycemia. Treatment is supportive primarily with intravenous fluid, β-blockers, and potassium supplementation.>

good lord, I wonder how the guy decided 5mg of clen was a good idea

1 Like

I wonder what is worse…intentionally or unintentionally ingesting 5 mg of clen? Your heart probably can’t tell the difference.

I am hopeful someone can see the latter scenario is plausible from what was discussed above.

1 Like

Well I guess if it was intentional, you can rest assured that you’re the dumbass, and you didn’t necessarily get improperly dosed gear.

At one point in time there was a case study posted about, I believe, a situation in which someone unintentionally ingested wayyyyyy too much clen because it was improperly dosed, and I believe it killed that person.

So both of these scenarios are certainly possible

1 Like

The dickhead has some questions:

The solvent is ethanol and the solute is clen hcl. At room temp you notice solid particles after vigorously swirling the suspension. They don’t go away. You filter the suspension. What is the solution concentration of clen based on what I shared above or from your own study of clen solubility in EtOH at room temperature?

Why is this last question important to answer? How far apart is your estimated concentration from the advertised concentration of 250 mcg/ml?

Ok, let’s move on from the suspension/solution stuff. You corrected the terminology, got it.

You want to understand how to accurately and precisely administer certain volumes of liquid? Or you want someone on the internet to tell you if what you possess is accurately labeled?

1 Like

many years back i heared the story that some dude ate a whole bottle of fat burner and also died - and they banned that fat burner or smth…

But dosed improperly would usually be under-dosed imo… that would be a rare thing to dose MORE than you agreed to sell, haha.
Imagine getting like 10mg anavar tabs that are like 100mg anavar tabs. The whole factory goes out of business in a month :smiley:
Reminds me how long time ago when people didnt know shit, some people believed that protein powders are spiked with steroids, so they would produce results.
No idea who tought that protein manufacturers would give away free steroids with their protein :smiley:

1 Like

It’s been a while since I read the case study, but I think the clen tabs were improperly dosed individually, but an analysis showed that the average dosing against several tabs was accurate to the label claim.

Unless you have highly specialized equipment, I don’t know how you can accurately dose mcg in tab/pill/capsule form.

I recently made up some anastrazole, but I made it a liquid oral. I dissolved it into grain alcohol, then mixed it into Ora-plus/ora-sweet. There’s no way I could accurately dose capsules at .25mg, or even 1 mg.

2 Likes

Clenbuterol was mostly taken in the veterinary liquid or gel form (24 exposures) at a median of 2 mL (range, 0.5–20 mL) or two “scoops” (range, 1–2 scoops). The actual dose is highly variable between liquid formulations. Two people took tablets (one and three tablets, respectively) and of the eight episodes in which the dose was known, the median dose was 0.8 mg (range, 0.08–5000 mg).

More info brought to you by dickhead…

Case Report

A 31-year-old man presented to the emergency department approximately 30 minutes after ingesting 1.5 ml (a tenfold dosing error) of Ventipulmin® syrup (72.5 mcg/ml clenbuterol HCl). The product was brought to the emergency department (ED) by the patient. He reported no current use of anabolic steroids. He presented in an anxious state with complaints of palpitations and shortness of breath. Vital signs upon examination were as follows: BP, 122/77 mmHg (16.3/10.3 kPa); HR 254 bpm; RR, 22 bpm; Temperature, 97.1°F (36°C); and oxygen saturation, 100% on ambient air. His electrocardiogram (ECG) demonstrated supraventricular tachycardia with a ventricular rate of 254 bpm. Esmolol was recommended for rate control after the unsuccessful use of adenosine and diltiazem. Laboratory studies showed potassium, 2.1 mmol/L; magnesium, 1.3 mg/dL (0.54 mmol/L); phosphorus, 1.0 mg/dL (0.32 mmol/L); serum glucose, 209 mg/dL (11.6 mmol/L); creatinine, 0.8 mg/dL (70.7 μmol/L); AST, 20 U/L; ALT, 55 U/L; hemoglobin, 12.6 g/dL (126 g/L); CPK total, 87 U/L; and troponin I, 0.23 μg/L. The patient’s urine was negative for any drugs of abuse. Clenbuterol levels were not obtained. A second ECG, 16 hours post ingestion, reflected atrial fibrillation with a ventricular rate of 125 to 147 bpm. On hospital day 3, he was electively cardioverted to sinus rhythm; heart rate and rhythm returned to normal, and he was discharged with oral metoprolol.

Also change your title. We haven’t even got the drug in your body yet. What you need is a basic competent bench chemist.

It is supposed to be a solution.

But if to much solute (clen) is present, it will be a suspension, right?

Lowering the solute amount per mL, should ensure a solution, right?

Also, I would start very low dose with Clen, like 20 mcg. Dosing accurately with a 1 mL syringe 20 mcg out of a 250 mcg/mL is such a small amount that I think a lower concentration would be easier to do.

Maybe I am an idiot? IDK, I don’t actually plan on doing this. I tried to dissolve some adex, but didn’t trust it and threw it away. Perhaps the particulate at the bottom was just pill filler, but it was unsettling, so I didn’t use it.

This is the level you are working with here haha.

image

2 Likes

I have the accurately dosed product.
My question was more so about possible irregularities in dosing.
ie. is the drug evenly distributed to what % accuracy?
Theoretical dose assuming 100% even distribution vs realistic - how they hold up.

That is all.

It is a medical dropper that dispenses a tiny volume per drop. (consistent volume nonetheless and therefore the mg/drop is consistent - in theory)

Edit: I am also not doing this myself - I bought the product in liquid form all ready from a trusted research lab and was curious about the accuracy of this from a pharmaceutical perspective.

1 Like

https://inchem.org/documents/jecfa/jecmono/v38je02.htm

2.3 Observations in humans

A single blinded cross-over study was carried out to examine the
acute bronchospasmolytic effect and possible side-effects following
oral administration of placebo and three doses of clenbuterol (1, 2.5
and 5 µg/day) in patients (three male and three female) with chronic
obstructive airway disease over a 3 day period. The drug was given
orally, diluted with water. Observations were carried out over a
2-hour period following dosing. The average age of the patients was
55.7 years and they had an average body weight of 73.16 kg.

None of the 3 doses produced any clear, consistent effects on
bronchial resistance, thoracic gas volume, radial pulse frequency or
blood pressure, and no side effects were seen.

The pharmacological NOEL in this study was 5 µg/day, equivalent
> to 0.08 µg/kg bw per day (Kaik, 1978).

The bronchospasmolytic effect was examined in two groups of
patients:

Group A: ten patients aged 46-75 years with chronic obstructive
respiratory disease resulting from pulmonary tuberculosis.

Group B: five patients aged 56-67 years with chronic obstructive
respiratory disease not related to tuberculosis, plus five
patients aged 34-57 with bronchial asthma.

The bronchospasmolytic effect was examined after single oral doses of
1, 2.5, 5, 10, 20, 25 or 30 µg/person, and after a placebo dose.

In Group A patients, intrathoracic gas volume was significantly
reduced and vital capacity and pneumometer values significantly
increased at all dose levels. In Group B patients, airway resistance
was significantly reduced, but no dose relationship could be
demonstrated. No significant placebo effect was seen in either group.
When compared with placebo values, a significantly greater increase
for both vital capacity and pneumometer values was observed in Group
A, even at the lowest dose used in this group (5 µg). However, at the
two lowest doses used in Group B (1 and 2.5 µg), there were no
significant differences from placebo values. The pharmacological NOEL
> in this study was 2.5 µg, equivalent to 0.042 µg/kg bw (Nolte &
> Laumen, 1972; Nolte, 1980).

Children who consumed between 0.05-0.075 mg of clenbuterol showed
> only mild tachycardia. A 30-year-old woman who consumed 30 tablets
equivalent to 0.6 mg clenbuterol (10 µg/kg approximately) developed
tachycardia and slight hypertension approximately 1 hour after
consumption. No tablet remains were found on gastric lavage, and
medicinal charcoal and a saline laxative were given. The following
day, the patient’s pulse rate and blood pressure had returned to
normal (Boehringer, 1991a).

Patients (100+) administered doses of 20-60 µg/day (0.3-1.0 µg/kg
bw per day) for up to 1 year or 20 µg/day (0.3 µg/kg bw per day) for
up to 6 months showed no adverse effects except for slight tremor and
occasional, mild tachycardia (Laumen, 1978; Tullgren & Lins, 1987).

In humans, clenbuterol produced a bronchiolytic effect when a
single dose of 10 µg (0.167 µg/kg bw) was given by the inhalation
route, but no evidence of tachycardia was seen at this dose. With oral
doses of clenbuterol of up to 5 µg/day (0.08 µg/kg bw per day) over a
3-day period, there were no effects on bronchial resistance, thoracic
gas volume, cardiac rate or blood pressure. The NOEL in this study was
5 µg/day (0.08 µg/kg bw per day). In a study to investigate the
bronchospasmolytic effect in humans, patients with obstructive lung
disease were given oral doses of up to 30 µg per person. Patients
administered doses of 5 µg or more exhibited bronchospasmolytic
effects, and the pharmacological NOEL in this study was 2.5 µg per
person, equivalent to 0.04 µg/kg bw.

  1. EVALUATION

    The Committee considered the most relevant study for determining
    the ADI to be that concerning the bronchospasmolytic effect in humans.
    The patients had chronic obstructive airway disease and thus were
    likely to be a very sensitive population for this effect. The NOEL
    identified in this study (2.5 µg per person, equivalent to 0.04 µg/kg
    bw) is approximately 25% of the dose in another study in which the
    inhalation route was used, but in which cardiac effects were not
    observed. This NOEL is approximately 50% of the oral dose used in
    another study where, again, cardiac effects did not occur. Hence, this
    NOEL for the bronchospasmolytic effect offers an additional safety
    margin for cardiac effects. The Committee therefore established an ADI
    > of 0-0.004 µg/kg bw, based on the NOEL of 0.04 µg/kg bw per day for
    > pharmacodynamic effects in humans and a safety factor of 10.

Then you got your answer.

http://chemistry.elmhurst.edu/vchembook/170solutions.html

https://employees.csbsju.edu/hjakubowski/classes/Chem%20and%20Society/IMF_Solutions/olIMF_solutions.htm

https://genchem1.chem.okstate.edu/1515SP17/Personal/Lecture/Chapter13/Lec91201.html

1 Like