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  • BDD Moderators: Keif’ Richards | negrogesic

The Basics of Drugs

LearntYoung

Bluelighter
Joined
Jun 26, 2014
Messages
2,902
Location
Netherlands
Intro:
Even though it was only one person who gave me notice of his interest in a topic with drug basics in general, I promised to create it. Afterwards I had forgotten about it, until today, when I suddenly realised my promise and decided it was time to put in the time and effort it deserves.


I'm a 21 year old first year university pharmacy student, that has (ab)used drugs ever since I was 16. My interest in drugs grew larger as I grew older, but the chemistry part came really late, since I had a terrible chemistry teacher at first. After changing school, I suddenly realised chemistry was not only really interesting to me, I was also really good at it. I've studied one year of chemistry, but had to quit due to a lack of study credits, caused by my constant absance. Now I'm more serious with my study and it's going a lot better. Next to study related knowledge, I've also been browsing both forums and scientific articles from the moment I started using.


If you feel like amphetamine is used too often in the examples of this topic, you're out of luck. It's my drug of choice and I don't have to look up any properties when writing about that.


This topic is created with the knowledge I've gathered over the years combined with a few sources, which will be mentioned below. Some parts of the text will be simply copied from things I wrote earlier. If you have any suggestions of stuff I should add or questions, please let me know. However, note that this topic isn't about in-depth drug knowledge. If you have more complicated questions, please PM me, I might know them, but I don't think they belong here.


Contents:
1. Bioavailability
2. Route of Administration
3. Drug Action (Neurotransmitters)
4. Percentages (Salts)
5. Washing Away Cuts
6. Nasal Spray and other Gadgets
7. Guidelines & Risks
8. Source


1. Bioavailability
Simply said, the bioavailability (BA) is the percentage of a drug that is absorbed and therefore active. The BA is determined by a lot of different variables, but most important are the route of administration(ROA), solubility and pKa.


Different pKa values and solubilities determine what ROA results in the largest BA. Next to that it's also important to keep in mind that only oral use involves first-pass metabolism, which is important for some drugs' effects.


Even though it's a lot more complicated, on average drugs that are easily soluble in water have a high BA when insufflated. Hydrophobic substances on the other hand, should be taken either sublingually or rectally.


Oral, inhaled and IM/IV are not mentioned above as they differ from that rule of thumb. For oral use, the pKa plays a big role, because of the stomach's acid and it's state in the blood's pH. In general, weak acids have a high oral BA and weak bases a low one.


For inhaled substances, two things are important: The drug shouldn't burn, but melt when heated to vaporize and poorly water soluble substances get absorbed most easily.


Finally IM and IV are both very direct methods, but differ slightly in absorption. IV always has a 100% BA and IM has a faster absorbance for more soluble drugs.


2. Route of Administration
Different routes of administration have already been mentioned above, but only the BA aspect has been covered. Here I'll simply comment on some pros and cons.


Oral: Easiest method, clearly, but often a low BA and more factors come into play, like the amount and time of your last meal. (Long duration)
Sublingual: The method of bypassing the first-pass metabolism with the lowest risk. (Medium duration)
Nasal: Faster and stronger onset, but can easily ruin your nose. (Medium duration)
Smoked: Very fast and strong onset and often a great absorbance, but the complications with lung damage are risky. (Short duration)
Rectal: Biggest downside is that it's uncomfortable and weird, but it can result in a high and fast absorbance with a strong onset. (Medium duration)
IM/IV: Prevent going here at all cost. If decide to go here anyway, you get a very quick and intense high, with insane risks. (Very short duration)


When insufflating, don't inhale firmly, but gently. The drug shouldn't get to your lungs or stomach.
For more detailed info, look here. Since there was already a topic about it, I didn't feel like elaborating more.

3. Drug Mechanism (Neurotransmitters)
I won't go into much detail here, since I will be learning most of this later. I'll just cover the surface.
What determines what effect a drug results in and what is it that induces the effects you experience?


The effects of a drug are based on it's structure. Not only do different polarities and electronegativities of certain parts play a huge role, the way it's metabolized is also a major factor.


The metabolism isn't easily predicted, since it's proteins that carry out this proces and their effectiveness and routes don't have an easy 1-2-3 method of predicting. What I'll cover concerning metabolism is that atoms with strong attraction towards eachother are less likely to break their bond. Also keep in mind that metabolites can form a risk that hadn't been predicted based on the drug's own structure.


The primary effect is based on what is called 'affinity.' Different drugs have a higher affinity for certain receptors, based on their structure, even the isomeric properties have influence. Most of the times, the Levo (bends light counter-clockwise, left) isomer is often most potent, but once again, it's unpredictable what the actual effect will be.


Neurotransmitters transform this drug interaction into a respons from the body. They're basically the body's regulation system, consisting of different messengers. Each messenger's concentration in the synaptic cleft effects the way you feel and the way your body functions. The most important neurotransmitters for recreational drugs are Serotonin, Dopamine, NMDA, Noradrenaline, Adrenaline and GABA.


A drug could effect this system by affecting the release, the reuptake or even activating the receptor by itself.[/spoiler]


4. Percentages (Salts)
Maximum purities of a freebase chemical is always 100%. When in salt form, however, this percentage is different. The explaination is quite simple, shown by this example:


Amphetamine (135.21 g/mol) is sold as the Sulphate (96.06 g/mol) salt, which due to it's double negative charge, can hold 2 Amphetamine molecules in the salt structure. Resulting in a total molecular mass of (2 × 135.21) + (1 × 96.06) = 366.43 g/mol. Therefore, the maximum percentage of Amphetamine is 270.42 / 366.43 × 100 = 73.80%.


Methamphetamine (149.24 g/mol) is sold as the Hydrochloride (36.46 g/mol) salt, which can only hold 1 Methamphetamine molecule in the salt structure. Same steps: 149.24 + 36.46 = 185.70 g/mol, 149.24 / 185.70 × 100 = 80.37%.


5. Washing Away Cuts
If you know your drug is cut with something and know what this something is, you can use the physical properties to filter the cuts from the drug. Most commonly used would be solubility in different solvents.


For example, to wash caffeine from amphetamine sulfate, you can use (anhydrous!) acetone, which dissolves caffeine, but not the speed. By simply pouring the mixture on a coffee filter, the ampetamine is left on top and the acetone with caffeine goes through. Let the any leftover acetone in the speed evaporate and it's done.


From the top of my head, levamisol can be filtered from cocaine with chloroform, but more easily you can 'clean' cocaine by turning it into freebase (and back if you want.)


6. Nasal Spray and other Gadgets
Spray
After using for a long time I came across inconveniences and solutions. My favorite of which, the (meth)amphetamine nasal spray. Here's a guide to make your own.
First of all, you'll need a spray bottle. You can either purchase an empty, easily refillable one or buy a saline solution spray. If you choose the second choice, the bottle most likely won't have a screw cap, so be sure to examine if the top is removable at all. If it is, the easiest way to pop it open is by using a bottle opener, like this one:
Aluminium%2Bflesopener-00.jpg



If you have an open spray bottle, empty it if not yet empty and fill it with a measured amount of water. (eg. 10mL) Put the top back on and count how many sprays you can get out of it until it's empty. Repeat this step and use the average for a more precise dosing.


For the solution there are 2 types to choose from and an optional addition. You could make (1) a solution with only meth in it or (2) a solution with meth and some salt added. Both having its own advantage and disadvantage. Optionally, you could add a sweetener, like sorbitol, to make it taste a bit better. (500mg sorbitol would be plenty for 10mL solution)


Advantages:
(1) The lack of salt will create a favourable osmotic pressure, causing a higher absorbance.
(2) The salt will act as a decongestant, so you won't have a clogged nose.
The choice is yours. When adding salt, never add more than 9mg / mL. I'd recommend just 4mg / mL or so, to reduce it's influence on the absorption rate.


All choices made, except for one, your dosing. Especially for the first time, I'd recommend to not make a lot of solution, since you might not like the method and it's a bitch to get the meth out again. Read this first, before actually making the solution, as I'm explaining that in the next paragraph.
Let's say you used 10mL to determine the amount of sprays and got 90 sprays out of that. A simple calculation (10 / 90) would tell you each spray consists of 0.111mL. Meth is freely soluble in water, so you won't have to worry about it not dissolving when adding too much, but you just need to decide what dose you'd like. Dissolving 1 gram of meth, would get you 100mg / mL and 11.11mg per spray. 1.5g meth > 16.67mg /spray and so on.


To make the solution, get some water boiling and let it cool down. Put the desired contents and amounts, chosen from the description above, in the empty bottle and add the amount of distilled water prefered. Add the cap and shake it for a while to mix everything properly. Always shake before use for optimal effect.


Other
Other useful stuff or solutions (somethings obvious), which I won't go into detail with, is listed below.
-Cut straws into pieces for snorting tubes. Cheap, easy and no chance of infections.
-A precission scale, preferably 0.001g. It's safer and very practical from time to time.
-Precise dosing by dissolving and using a syringe. (Shake before use!)
-You can make a vapirozer from a light bulb. It looks crappy, but it's really useful.
-Sitting down and whistling helps against the inability to pee.
-The thought of having benzodiazepines as a backup when you have a bad trip (psychedelic) is often enough.


7. Guidelines & Risks
Different drugs have different risks and require a different approach, however when you start drugs, it's wise to set up rules for yourself beforehand to minimize the risks and keep your use responsible. Even in the long run.


Think about:
-Never use for any practical reasons.
-Prevent having a strict pattern.
-Don't use when feeling down.
-Keep in mind Tolerance, Damage and Dependence for your frequency.
-Set yourself a minimal period inbetween use and NEVER use again before that. (One exception leads to multiple)
-Think of cross-tolerance (and damage) - E.g. MDMA and 6-APB are both heavy serotonergic drugs. When recovering from MDMA, don't do 6-APB.
-Think of interactions when combining.


8. Source
http://www2.courses.vcu.edu/ptxed/m2/powerpoint/download/Lamb Drug Absorption.PDF


This is the first time I made a topic like this, so feedback is appreciated.
 
Last edited:
The precise definition of bioavailability is the amount of drug that reaches systemic circulation not the amount absorbed. Absorption is the process which drugs permeate biological membranes and while related, bioavailability (often abbreviated as F) has other determining factors. For instance take the first pass effect you mentioned. A drug may be said to be completely absorbed, but pass into the portal circulation, be extensively metabolized via the liver, then enter the systemic circulation. So absorption is high but F is low.

Also keep in mind when we speak of low F of orally administered drugs, we are speaking of relative bioavailability. This is the amount of drug reaching systemic circulation via oral or any other ROA compared to IV administration. I think you get this but is important to realize that F via oral administration needs to be compared to something otherwise we can say that whatever does reach the blood could be considered 100% F.

Also while pka and whether a drug is a weak acid or base are important in many PK measures, the single biggest factor determing absorption is the surface area and permeability of the membrane. The small intestine far exceeds the stomach in both so even weak acids are more extensively absorbed there even though the pH is around 4 to 5, as opposed to 2 in the stomach.

Please explain what you mean about metabolism not being a 1-2-3 process. The biotransformation of many drugs is rather well understood via both phase I and II metabolism. Both tend to increase the polarity of the parent compound with I adding a functional group and II a conjugate which enhances excretion.

But not a bad start for 1st year student. More than I knew.
 
Honestly, I knew that first part, but I thought:
"Would the average member here understand the difference between absorption and what reaches the systemic circulation? Or would using those words make it more difficult than necessary for the purpose of this topic?"
The purpose of this topic is to educate new users and users that aren't interested in the complicated science behind drugs about the basics. I decided to write up a topic, because there are often quite a few misconceptions caused by the lack of insight in the amount of different variables involved. Also, I've mentioned some things that could be useful for the beginning user, since I think life would've been a lot different for me if I had known these things from the start instead of figuring them out along the way.

The second part, about the surface area, I didn't know, even though it sound very logical now that you mention it, I'll check if I can edit & credit today ;)

What I meant by that 1-2-3 process, is that there are way too many things involved in determining what a drug will be metabolized like to write it in a simple 1-2-3 step guide or something for a novice to predict the result of substances he's interested in. Therefore, elaborating any further than I did would serve no cause other than to show what I know, while messing up the topic's simple, straight forward style.

This isn't all I know and I've learned most of it by studying drug info, since I screwed up when I just started, by not educating myself. Afterwards, I was stubborn, thinking I had to be an exception, since I ignored the knowledge present from the start (at first out of ignorance) and never experienced any of the described problems that could occur. What my young, teenage brain couldn't imagine yet was that the moment you notice the problems, it's already developed to a stage where it has done more to you and has more control over you than you'd be willing to admit.
 
I see. I figured you were trying to be a bit of a mix between technical and layman. It is unlikely someone will understand pka, electronegativity and even what mol stands for if they are just starting to learn about drugs from scratch, too. I thought it was more of an exercise for yourself than for others.

Oh and I should have mentioned the intestine starts at pH 4-5 but progressively increases to over 8. I made it sound like the whole small intestine is at pH 4-5.
 
Still can't edit though... It deletes the post and if I paste it in there again and adjust it, it gives an error...
 
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