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  1. #1
    Join Date
    May 2014

    PROPRANOLOL tutorial (UK, US)

    Hi guys, since I've been on propranolol for 3 years now (anniversary, yeah!! ), I wanted to celebrate this superb event by writing down a propranolol tutorial for anyone out there!

    First things first.... A bit of history
    Propranolol, a chemical substance, was discovered in 1964 in the United Kingdom by a team of scientists lead by a Scottish fellow called Dr James Whyte Black. JW Black then received a Nobel prize for this discovery in 1988. The prize was awarded since Dr Black's propranolol was the first drug after many tens of years which was actually able to control the effects of having angina pectoris - a condition following a heart attack when the heart tissue gets worn and tired due to the original heart attack.

    Propranolol function
    Propranolol belongs to the class of drugs called adrenergics, i.e. drugs with a direct effect on the adrenalin uptake (I will explain the uptake mechanism below) in our body. All these drugs end in -lol suffix, so all the other ones are atenolol, oxprenolol, alprenolol etc. The other drugs from this class differ in their selectivity, in their half-life and in other aspects.

    So what does adrenaline do in our body then?
    When adrenaline gets pumped into the human blood circulation, from the so-called adrenal glands which sit on top of our kidneys, by a split-second command originating in the brain following some stressful or fear-related event, it will eventually 'lock' itself into the cell receptors (I will explain cell reception below) of the heart and lungs tissue which the heart and lungs are made of... Effectively, the presence of adrenaline on and around the tissue of these organs directly causes an increase in the function of these two organs. So, the heart starts beating faster and the lungs start contracting faster. This is the most dominant effect of adrenaline in our body. Effectively, we become perhaps a bit agitated, ready for action, ready to perform, which can be however physically damaging us if this hyper state lasts for days or weeks. People can get really exhausted if this state persists in them.

    What is uptake in human body cells
    On the microscopic level, our whole body (organs, bones, skin, muscles, teeth, hair, simply everything) consists of billions and billions of cells. Each such cell surface, without an exception, has got these so-called receptors, which are simply 'keyholes' onto the cell surface into which certain molecules, with the correct configuration, can lock in. In other words, if around the tissue (consisting of specific cells) flows a certain specific molecule, which has got the correct configuration (shape) to lock into that receptor, then you've got something called the 'uptake', or in other words, that the specific molecule fits into that lock since its configuration/shape fits in perfectly... As if you had the correct key to open the corresponding lock. By our nature, the best uptake of adrenaline is in the heart and in the lungs since the heart tissue and the lung tissue have got the correct receptors (locks) which can accept the adrenaline molecule (key). They simply go well together and they work together. They are also called Beta-receptors. This is the name they gave to the locks of the heart and lungs cells.

    What happens when a molecule fits into a receptor?
    If it fits perfectly, and it is therefore uptaken, then it has got the ability to start a certain reaction inside that very cell where it is locked into. Namely in the case of the heart or lung tissue receptors, these tissues would start contracting in unison! It is funny business, but it really works like that!

    Blockage by propranolol uptake (i.e. not allowing adrenaline uptake, also known as adrenaline inhibition)
    When you take propranolol in tablet or capsule form, within certain time (usually 1-2 hours) it will dissipate inside your tummy (or gut), then it will go directly into your liver (the liver is a gateway to our bloodstream; everything we eat goes through the liver as a first-pass 'safety' mechanism since liver can distinguish between the good and bad stuff). After liver has processed this (with propranolol, up to 90% of the original drug is not accepted and goes directly to kidney and out of the body without any use!), then it finally ends up in the blood where it endlessly circulates. Well, not endlessly because (perhaps with the exception of some heavy metals and radioactive molecules) the duration of the circulation of propranolol in human blood stream (so-called half-life) is between 4-6 hours.... To be completely precise, half-life is half the duration of one substance in the blood stream since it is an accepted premise in medicine that only the first half of the life of the substance in the blood counts towards the actual drug effect since the other half of the overall life of the substance in the blood is much less effective in terms of the desired function of that substance on our body.

    When propranolol locks into the tissue of the heart and the lungs, it will not allow (block/inhibit) any further uptake of adrenaline which naturally flows (following a release from the adrenal glands) in our body and it will therefore not allow activation of the tissue cells (increased heart beat, increased breathing) if there was a sudden increased influx of adrenaline (following a stress and fear situation). Since the most of the locks on the heart and lungs were all taken by propranolol, the human adrenalin will just flow straight out of our body without any use or effect! So what Dr Black actually discovered was a substance resembling the configuration of adrenaline, except for one part which is slightly different to the adrenaline, and which therefore does not cause the cells to start fully working as they would if they were activated by the flowing adrenaline.

    Therapeutic use
    Well, since the main-stream scientists at different state universities are not really willing to research propranolol use further (and similar drugs from this class) in the area of psychiatric medicine (except for a single propranolol study from 1976 by Becker on effects of propranolol on patients with anxiety), we are left with General Practitioners and Physicians prescribing propranolol for various seemingly-unrelated conditions since the time has already proven its effectiveness.

    Most uses are either for situational or long-term anxiety. I reckon you can use any adrenergic drug, which can slow down the heartbeat and the breathing, with any neurotic (emotional, psychological) disease as all emotional and psychological diseases have got in common at least one of these various physical symptoms - high heartbeat, fast breathing, sweating, tension in body, hypervigilance, hyperactivity, and/or emotional outbursts... These are all results of an agitated sympathetic nervous system, ie. a specific nerve system in charge of informing the brain about the function of our heart and lungs, hence any decreased agitation of this nerve circuit by way of controlling and managing the heart and lungs function, which this nervous circuit supervises, can be directly beneficial in the treatment of these diseases (Becker already proved this in 1976; probably not for a full cure because there are always psychological reasons behind any such disease, so counseling is always necessary to achieve such cure). Exceptions could be psychotic diseases where the patients are disillusional, hence the use of adrenergic drugs in this other area might be limited.

    The advantage of propranolol over other adrenergic-class drugs is that propranolol is lipophillic (it can be dissolved around fatty tissue, including brain tissue). This specific characteristic allows propranolol to enter the Central Nervous System (other adrenergic-class drugs are not able to do that), and propranolol has therefore a slight sedative effect.... Since there is no actual scientific study into the physiological reasons for anxiety relief due to use of propranolol, we can only assume that the anxiety-relief benefits are therefore perhaps achieved due to a combination of the effects on the sympathetic nervous system (this nervous circuit with a direct link to the brain gets less employed, and the brain might therefore "feel" less exhausted due to the overall less frequent heartbeat and slower lungs contractions; much different in those patients who are constantly 'on the edge') and for the sedating effect directly in the brain.

    Ethical concerns (really?)
    Since there has been a noticeable rise in prescribing propranolol for such patients in the last 10 years and since the best observers of this rising trend are the financial accountants of the pharmaceutical companies who have been around making ridiculous profits by selling a whole range of other drugs, and since propranolol is indeed very cheap to be made (unlike antidepressants and other what I call brain poisons, such as prozac and neuroleptics, which all just put a blanket on your head, disconnecting you from the real world, really), there has not been any real research into this substance since 1976 (and there perhaps even won't be since the pharmaceutical companies might start losing billions, all of the sudden, if people realized that most of the neurotic diseases indeed carry physical symptoms, and therefore require a primary intervention by way of controlling these physical symptoms, first of all, before any drugs, which disconnect you from the real world around you, unlike propranolol, and which do not address the physical side of neurotic diseases, are prescribed).

    Pharmaceutical companies prefer if their patients were eating prozacs (and other heavy stuff) 24/7, like smarties . Only now, after 40 years, you will no longer find the 24-hour+ propranolol version called INDERAL LA in the UK (the official reasoning by AstraZeneca, the only producer of this 24-hour+ version of propranolol in the whole Europe, which I obtained by enquiring through my local MP, was that this quality propranolol was apparently 'not very popular'....) And only now in the last 2-3 years, whole 40 years after propranolol was daily used by millions of people for different other diseases, there has been a number of scientific "studies" raising, all of the sudden, some new "ethical" concerns over the use of propranolol since they are now pushing this claim that propranolol should be capable of erasing the whole human memory.... Google it.

    Propranolol versions (UK, US)
    In the UK, there are the so-called short-acting tablets (work for 4-6 hours) and long-acting, or also called modified-release capsules (work 10-20 hours). These are:

    PROPRANOLOL tablets (10mg, 40mg, 80mg and 160mg tablets) by companies Actavis, Accord Healthcare, and couple of others (they are all in fact the same thing)

    - one such tablets lasts between 4-6 hours (this is individual, you know that the liver takes up to 90% of the actual pill, so you might get these different results with different people)

    - one such tablet kicks in between 1-2 hours

    PROPRANOLOL capsules (80mg, 160mg) by companies called Sandoz (capsules are called BEDRANOL) and a company called Tillomed (capsules are called BETA PROGANE). These differ much....

    - the Bedranol capsule (80mg, 160mg) lasts between 10-20 hours (I doubt it but that is perhaps because I had an adverse reaction on these), and should start within 1-2 hours

    - the Beta Progane capsule (80mg, 160mg) lasts around 12 hours (sounds more like it) and kicks in only after 5 hours (sounds again, more like it)

    The advantage of these two forms of propranolol are the modified release of propranolol which extends the action of that drug onto the whole day (or a long chunk of the day, at least).... You need to discuss with your doctor what you think will suit you most... Some people, like those with situational fears and anxieties and stress, might prefer the short-acting tablets with an action for 4-6 hours, but other people with generalized anxieties and stress disorders might prefer the whole-day action capsules.

    Again, the response to propranolol is very individual, so each one of us has to try several dosages (max recommended dosage of propranolol is 320mg/day) until the desired therapeutic response is reached (calmness, slowness, etc.)

    In the US (and Canada), you also have got the superb 24-hour action versions, called Innopran XL and Inderal LA, which were available in the UK until January 2014 (no longer available though), which indeed deliver a 24-hour+ action, so I would imagine that people with all day anxieties and stresses go with these.

    I hope you liked the tutorial, I'm sorry if I perhaps used a too complicated language, or maybe too simplistic or exaggerated explanations, but I hope it will help those with anxieties understand many things which the GPs usually don't have much time explaining.

    Take care.
    Last edited by Svojski85; 07-08-14 at 23:30.

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