How Do Painkillers Work.... And What Are The Real Risks?

'Sometimes The Drugs Really Don't Work...Sometimes They Do Make You Worse...'

Popping pills may be a quick fix to pain relief, but can they do more harm than good? Are they in fact the 21st centuries’ biggest danger to your overall health? Here we ask how do painkillers work and how does this help you because not all painkillers are built the same…..

How Do Painkillers Work?

Taking an ibuprofen when you suffer .

Indeed, it is fair to say painkillers today are a major part of most people’s treatment – whether it be fighting the impact of a degenerative disease such as arthritis, recovering from a physical injury, battling the impact of cancer or recovering following surgery.

Since the early 90’s their use has really expanded, with many drugs now available as ‘over the counter options’. But are they really the ‘lightbulb treatment’ we all once thought?

Taking a balanced viewpoint…

While there are undoubted benefits to the use of painkillers, there are also substantial downsides and any sensible usage really has to be undertaken with a sound knowledge of the long term effects of painkillers, as well as those felt today.

Unfortunately, this is not always the case. In a poll by The National Safety Council, 9 out of 10 prescription opioid users were not concerned about addiction, despite nearly 60% having a family link to addiction.

Painkiller Types

Painkillers work by blocking the pain messages sent to the brain for processing. Exactly how they work depends on the type of painkiller used (which in turn should depend on the type of pain being experienced). Painkillers can however broadly be broken down in to three basic categories –

1. Non-Steroidal Anti-Inflammatory Drugs (or NSAIDs)

Examples include – Aspirin, Ibuprofen, Diclofenac and Piroxicam

As the same would suggest, NSAIDs are designed to be particularly effective when targeting pain caused by inflammation.

This could be inflammation of the joints or from an injury where the main pain is caused by inflammation that has created increased sensitivity of the pain receptors to performing normally painless mechanical functions (moving).

NSAIDs work by inhibiting prostaglandin production through preventing the COX enzymes (cyclooxygenase) converting arachidonic acid. We’ll stop there because the chemistry isn’t relevant here – suffice to say that NSAIDs work where inflammation is a fundamental cause of the pain sensation.

This class of painkiller is also known as ‘non-narcotic analgesics’. However, while we list Aspirin here since it is technically an NSAID, it has a different mode of action with a very different risk/ benefit profile, so when we list the pros/ cons of each, we will deal with Aspirin as a fourth type of painkiller.

2. Acetaminophen (Paracetamol)

Examples – Numerous brand names for Paracetamol.

Paracetamol is similar to the NSAIDs in that they are all non-narcotic analgesics, but Paracetamol does not have the anti-inflammatory impact of the NSAIDs. As such, it can only work at helping to mask the pain, not actually treat the potential cause. It is commonly used for mild to moderate headaches, toothaches or mild joint pains.

3. Narcotic Opioid Painkillers

Examples include – Morphine and Codeine (natural narcotics) or Tramadol, Fentnyl, Trimeperidine, Butorphanol (synthetic narcotics)

The first key difference with narcotic painkillers lies in their mode of action – narcotics specifically bind to opioid receptors in the Central Nervous System, fundamentally blocking the feeling of pain by preventing it’s transmission to the brain.

The second key difference lies in their therapeutic effect – narcotic painkillers are much more effective at blocking out all types of pain. That is not to say they are the always the correct type of painkiller – as discussed above, in instances where inflammation is the primary course of pain, then NSAIDs are often a better solution.

Similarly, if the pain is very mild, a simple does of paracetamol may suffice. As your pain increases up the scale, and depending on the cause, one of the ‘narcotic opioid painkillers’ is likely to be prescribed.

Narcotic painkillers are much more likely to be prescription-only whereas some NSAIDs (aspirin, Ibuprofen etc) are normally available over the counter from a pharmacy.

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The Risks and Benefits of Using Painkillers

Obviously the main benefit of painkillers lies in the name – they are designed to give you time free from pain. In end-of-life circumstances, there is not a price that can be put on this, where the strongest (morphine) is most commonly used.

Indeed, after surgery and other major trauma’s they also play an absolutely essential role in your early recovery.

It is in their longer, continued use that many of the most recent warnings and much of the current debate is centred around.

Some studies have actually shown additional benefits to your health of using certain painkillers, although this is very selective depending on the type of painkiller. When evaluating the long-term case for/ against you deciding to use painkillers we have to consider the potential benefits as well.

Here we try to look at the various options in isolation to ascertain how strong the case for the short and long-term use of painkillers really is.

Acetaminophen/ Paracetamol –

The no1 used painkiller has been the stalwart of many a families’ drug cabinet. Ask anybody of it’s benefits and they will tell you it’s cheap, it’s safe and it’s effective.

It has a wide range of uses and has been adopted as the no1 after concerns surfaced around the safety profile of it’s major competitors – Aspirin and Ibuprofen. But all is not always quite what is seems. New research has poured considerable scorn on the idea of it’s effectiveness as a simple painkiller too.

Take away safety and effectiveness from Acetaminophen/ Paracetamol and suddenly it is not the friend you thought it was.

However, the summary findings were clear – a large part of paracetamol’s effectiveness has been called in to question after it failed to outscore the ‘placebo’ in a number of clinical trials (a placebo is a fake drug with no active ingredient, designed to measure the ‘mental benefit’ of taking the drug).

Placebos are used to counter the phenomenon that patients start getting better, simply because they think they are going to, rather than because of the actual drug.

Furthermore, in successive clinical trials, paracetamol or acetaminophen caused just as much internal bleeding as Ibuprofen and the other NSAIDs, while also in a few cases, causing kidney and liver problems.

Of course, the risk is all relative. For your average person taking a low dose once in a while, the risks are low and so any benefit, real or otherwise, is of considerable value.

But it certainly opened our eyes as we started to research the safety of a drug we all considered the ‘gold standard’

Aspirin –

One of the most talked about (and widely used) painkillers is Aspirin. As mentioned earlier, officially this could be included with the NSAIDs as it is still classed as a non-steroidal Anti-Inflammatory Drug. However it’s behaviour as a drug is very different to the other NSAIDs and so we’ll deal with it separately when looking at the risks/ benefits.

Aspirin was originally marketed principally to relieve the pain of headaches but has since been revealed to have some surprising longer-term benefits too.

It’s most prominent benefit lies in it’s ability to thin the blood. These blood thinning properties help prevent blood clots forming that can cause heart attacks and stroke among other things. Hence, it’s connection to a healthy heart and lower blood pressure. It has also been found in certain cases, to reduce the risk of getting some cancers.

However, balanced against this is the fact that aspirin was not designed to be an anti-coagulant and so does not offer the level of control that the new class of drug that specialises in anti-coagulation can offer.

There is then the very real danger of thinning the blood at the wrong time that can also cause hemorrhagic strokes (typically the most fatal type of stroke) and major, life-threatening bleeds.

We reviewed the benefits and risks in more detail here, but typically clinicians have now turned against recommending aspirin for anything more than short-term use.

And given the relative risk reduction in rates of cancer is small, and better drugs exist if you are at genuine risk of stroke/ heart attack, then there is no reason to challenge this – aspirin certainly has a place but only short-term for mild short-term pain relief.

NSAIDs –

The biggest single advantage of NSAIDs over other drugs is the fact that they are specifically designed to lower inflammation.

Ibuprofen, one of the most popular NSAIDs, can be given to both adults and children in the right doses – making its pain reducing qualities available to everyone.

People with arthritis can also gain long-term benefit from using NSAIDs to control painful inflammation. The other big advantage is that they are cheap to purchase as a quick over the counter solution.

However, once again, NSAIDs are also linked to an increased chance of having a heart attack. This has decreased since the Vioxx scandal which saw one type of NSAID (the Cox-2 inhibitors) voluntarily withdrawn from the market, with the exception of Celebrex.

Indeed, many governing bodies started issuing strict health warnings against even short-term use of Ibuprofen, Diclofenac etc. As the furore calmed down, Ibuprofen has resumed it’s place as a short-term pain reliever for mild-moderate pain with a caution. They even have some usage long-term but this is very much done under regular medical monitoring only and should certainly not be decided by yourself.

Narcotic Opioids –

In truth with these much stronger painkillers, there is little debate that the short-term benefits are purely around pain relief, but long-term use carries some very substantial downsides.

They are perfect for use when recovering from surgery (when they are reviewed every 5 days or so) or in the case of a terminal illness, because the long-term outlook is far less important than the short-term impact on quality of life.

However, gradually narcotic opioids such as morphine have increasingly been used in the long-term management of chronic pain conditions such as back pain.

When doing this, your clinician needs to be extremely pro-active in monitoring all the signs of your health to ensure that any potential side effects can be immediately countered before they become even more severe than the pain you are trying to control.

Obviously this all depends on a wide range of factors, and we have taken a more in-depth look specifically at these and the general debate raging around use of narcotic opioids (morphine, codeine etc) here

The Final Word –

Painkillers of any sort are never a perfect solution to pain. Putting any chemical in your body can have an impact on your blood, your liver and ultimately your life.

However, in short doses, and particularly in cases where there are no alternatives, they offer a haven of pain free time. But this pain relief always comes at a price – how severe that price is largely depends on how frequently you use them, what you use and a certain portion of luck.

Every time you take a drug to control your pain you roll a dice as to the possible side effects. With some drugs these risks are of course much greater than others, but with any chemical there is always still a risk. A clinician will always balance the likely benefit vs the % risk.

However, some doctors are still set in their ways and only really consider the traditional solutions of drug prescriptions. This is where you need to know how painkillers work and what the real risks are associated with them.

Even with over-the-counter medications, there is still a risk that increases disproportionately over time. Obviously, painkillers play a crucial role in the right circumstances and for short-term usage, but wherever possible the safest route always seems to be to try other non-chemical alternatives in the long run.

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References Used –

1. (2019). Few Understand Risks of Prescription Painkiller Addiction. The National Safety Council.

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