Medicinal Chemistry Question

[Green Xenon]

Hi:

 

Let's say there is a pill of long-acting Inderal [propanolol]. This pill is opened up and the powder inside is put into a glass cup; boiling water is then poured into the cup and the powder is mixed with the hot water. Ice cubes are then added to this concoction to cool it down to drinkable temperature. Will this "Inderal drink" have the same medical effects of the Inderal pill or will the high-temperature of the boiling-water denature the propanolol and cause it to lose it's medicinal properties? OR will the previously long-acting Inderal now become short-acting due to thermal destruction of the components that are meant to slow the release of propanolol into the bloodstream?

 

Any medicinal compound has a certain temperature above which it will inactivate -- due to the effect of the excessive heat on the molecule of the medication's active ingredient. What is the deactivation temperature for propanolol? Is boiling water hot enough to inactivate propanolol?

 

This thermal-deactivation of medications is analogous to enzymes in biological systems. Enzymes are proteins and when such a protein is heated above a certain temperature, it is denatured. A denatured enzyme is chemically-unreactive and thus no longer interacts with substrates.

 

 

Thanks,

 

GX

[John Cuthber]

This sounds like a fairly effective way to overdose on propranolol.

Is that the intention?

[Suxamethonium]

The following advice is my own and information is to the best of my knowledge- but I suggest confirming it with your own research anyway.

 

Do NOT remove the drug from its packaged form, unless told to do so by your pharmacist. For information about the drug or dosage from, talk to your pharmacist.

 

Most simple structured drugs are not analogous to proteins/enzymes. Denaturing of an enzyme happens because for some reason it changes conformation (changes shape), unfolds or falls apart. When this happens, it can no longer perform its function. Simple molecules like propranolol however do not behave this way, if they are effected by heat then it is a distinct chemical reaction and how it effects it's medicinal action is dependant on the type of product formed. As for the temperature required to decompose propranolol, I don't know specifically.

 

If you feel that a different dosage form (such as liquid preparation) is required, talk to your pharmacist.

 

As previously mentioned, this has the potential to pose a significant health risk to yourself (or others), particularly as propranolol acts on both beta adrenoceptors in the heart and airways- once again, Do NOT take this medication like this (unless specifically instructed to do so by your pharmacist).

[Green Xenon]

This sounds like a fairly effective way to overdose on propranolol.

Is that the intention?

 

No, the intent is to cancel the long-acting effect of the medication and make it immediate-release.

[John Cuthber]

Do you understand that getting, for example, a weeks worth of drug in one dose would be bad for you?

Do you realise that making a "slow release" version of a drug into an "immediate release" version is the same sort of thing?

[Suxamethonium]

I use capitals here because I am trying to stress the very important parts of what I am about to say.

 

THIS IS A QUESTION FOR YOUR PHARMACIST!! There is a reason these meds are prescription, and there is a reason why you have been prescribed the drugs you have been given. Please ask yourself if you have a pharmacist accreditation, and whether or not this makes you more qualified than the pharmacist who approved your medication when they dispensed it to you TO BE TAKEN AS DIRECTED.

[ewmon]

You're thinking of playing with fire. What part of "dead" don't you understand? You need to follow directions.

 

Do not crush, chew, break, or open an extended-release capsule. Swallow it whole.

source

 

Although propranolol is mostly used for circulatory system disorders and migraine headaches, it also reduces anxiety. Most people have no problem going back to their doctor about physical problems, such as migraines, but balk at going back about psychological problems, such as anxiety. I suspect that your goal is to provide quick relief from anxiety.

 

I've worked with this sort of thing. You need to take a long, hard look at what's called ADME -- Absorption, Distribution, Metabolism and Excretion -- because what you propose can, and probably will, overwhelm every one of these stages of how your body manages a chemical. When you start violating the verified formulation of medications, you enter into serious, unknown territory where even pharmaceutical companies don't go. When you start doing this, the characteristics of ADME can change dramatically and unexpectedly. What might seem to work okay, can backfire on you for obscure reasons that even the experts could not have foreseen, and you end up in intensive care or the morgue.

 

The only answer is this -- go back to the doctor that issued you the prescription, and openly and honestly discuss the problem you want addressed.

[Suxamethonium]

The only answer is this -- go back to the doctor that issued you the prescription, and openly and honestly discuss the problem you want addressed.

 

Or pharmacist- they are afterall the experts in medications (I say this because a doctor may not know what other preparations are available at this persons particular pharmacy that can better address the specific issue that they are having- the pharmacist will).

 

 

Edit: Pharmaceutics is highly involved, such advice should only be given by a PHARMACIST due to the ease in the ability for mistakes to end with fatal consequences. Hence, why I am really stressing the 'go to the pharmacist' point, particularly if you have already been taking your medication like this (do not panic about it- If you are worried about this and live in australia- you can call 13 11 26 - the poisons information centre if not google a number for one in your country) but talk to your pharmacist.

Edited March 13, 2012 by Suxamethonium