How Do Painkillers Kill Pain? It’s About Meeting The pain Where It’s At

Without the ability to feel pain, life is more dangerous. To avoid injury, pain tells us to use a hammer more gently, wait for the soup to cool or put on gloves in a snowball fight. Those with rare inherited disorders that leave them without the ability to feel pain are unable to protect themselves from environmental threats, leading to broken bones, damaged skin, infections, and ultimately a shorter life span.

In these contexts, pain is much more than a sensation: It is a protective call to action. But pain that is too intense or long-lasting can be debilitating. So how does modern medicine soften the call?

As a neurobiologist and an anesthesiologist who study pain, this is a question we and other researchers have tried to answer. Science’s understanding of how the body senses tissue damage and perceives it as pain has progressed tremendously over the past several years. It has become clear that there are multiple pathways that signal tissue damage to the brain and sound the pain alarm bell.

Interestingly, while the brain uses different pain signaling pathways depending on the type of damage, there is also redundancy to these pathways. Even more intriguing, these neural pathways morph and amplify signals in the case of chronic pain and pain caused by conditions affecting nerves themselves, even though the protective function of pain is no longer needed.

Painkillers work by tackling different parts of these pathways. Not every painkiller works for every type of pain, however. Because of the multitude and redundancy of pain pathways, a perfect painkiller is elusive. But in the meantime, understanding how existing painkillers work helps medical providers and patients use them for the best results.

Anti-inflammatory painkillers

A bruise, sprain, or broken bone from an injury all lead to tissue inflammation, an immune response that can lead to swelling and redness as the body tries to heal. Specialized nerve cells in the area of the injury called nociceptors sense the inflammatory chemicals the body produces and send pain signals to the brain.

Common over-the-counter anti-inflammatory painkillers work by decreasing inflammation in the injured area. These are particularly useful for musculoskeletal injuries or other pain problems caused by inflammation such as arthritis.

Nonsteroidal anti-inflammatories like ibuprofen (Advil, Motrin), naproxen (Aleve), and aspirin do this by blocking an enzyme called COX that plays a key role in a biochemical cascade that produces inflammatory chemicals. Blocking the cascade decreases the amount of inflammatory chemicals, and thereby reduces the pain signals sent to the brain. While acetaminophen (Tylenol), also known as paracetamol, doesn’t reduce inflammation as NSAIDs do, it also inhibits COX enzymes and has similar pain-reducing effects.

Prescription anti-inflammatory painkillers include other COX inhibitors, corticosteroids, and, more recently, drugs that target and inactivate the inflammatory chemicals themselves.

Because inflammatory chemicals are involved in other important physiological functions beyond just sounding the pain alarm, medications that block them will have side effects and potential health risks, including irritating the stomach lining and affecting kidney function. Over-the-counter medications are generally safe if the directions on the bottle are followed strictly.

Corticosteroids like prednisone block the inflammatory cascade early on in the process, which is probably why they are so potent in reducing inflammation. However, because all the chemicals in the cascade are present in nearly every organ system, long-term use of steroids can pose many health risks that need to be discussed with a physician before starting a treatment plan.

Topical medications

Many topical medications target nociceptors, the specialized nerves that detect tissue damage. Local anesthetics, like lidocaine, prevent these nerves from sending electrical signals to the brain.

The protein sensors on the tips of other sensory neurons in the skin are also targets for topical painkillers. Activating these proteins can elicit particular sensations that can lessen the pain by reducing the activity of the damage-sensing nerves, like the cooling sensation of menthol or the burning sensation of capsaicin.

Because these topical medications work on the tiny nerves in the skin, they are best used for pain directly affecting the skin. For example, a shingles infection can damage the nerves in the skin, causing them to become overactive and send persistent pain signals to the brain. Silencing those nerves with topical lidocaine or an overwhelming dose of capsaicin can reduce these pain signals.

Nerve injury medications

Nerve injuries, most commonly from arthritis and diabetes, can cause the pain-sensing part of the nervous system to become overactive. These injuries sound the pain alarm even in the absence of tissue damage. The best painkillers in these conditions are those that dampen that alarm.

Antiepileptic drugs, such as gabapentin (Neurontin), suppress the pain-sensing system by blocking electrical signaling in the nerves. However, gabapentin can also reduce nerve activity in other parts of the nervous system, potentially leading to sleepiness and confusion.

Antidepressants, such as duloxetine and nortriptyline, are thought to work by increasing certain neurotransmitters in the spinal cord and brain involved in regulating pain pathways. But they may also alter chemical signaling in the gastrointestinal tract, leading to an upset stomach.

All these medications are prescribed by doctors.

Opioids

Opioids are chemicals found or derived from the opium poppy. One of the earliest opioids, morphine, was purified in the 1800s. Since then, medical use of opioids has expanded to include many natural and synthetic derivatives of morphine with varying potency and duration. Some common examples include codeine, tramadol, hydrocodone, oxycodone, buprenorphine and fentanyl.

Opioids decrease pain by activating the body’s endorphin system. Endorphins are a type of opioid your body naturally produces that decreases incoming signals of injury and produces feelings of euphoria—the so-called “runner’s high.” Opioids simulate the effects of endorphins by acting on similar targets in the body. Although opioids can decrease some types of acute pain, such as after surgery, musculoskeletal injuries like a broken leg, or cancer pain, they are often ineffective for neuropathic injuries and chronic pain.

Because the body uses opioid receptors in other organ systems like the gastrointestinal tract and the lungs, side effects and risks include constipation and potentially fatal suppression of breathing. Prolonged use of opioids may also lead to tolerance, where more drug is required to get the same painkilling effect. This is why opioids can be addictive and are not intended for long-term use. All opioids are controlled substances and are carefully prescribed by doctors because of these side effects and risks.

Cannabinoids

Although cannabis has received a lot of attention for its potential medical uses, there isn’t sufficient evidence available to conclude that it can effectively treat pain. Since the use of cannabis is illegal at the federal level in the US, high-quality clinical research funded by the federal government has been lacking.

Researchers do know that the body naturally produces endocannabinoids, a form of the chemicals in cannabis, to decrease pain perception. Cannabinoids may also reduce inflammation. Given the lack of strong clinical evidence, physicians typically don’t recommend them over FDA-approved medications.

Matching pain to drug

While sounding the pain alarm is important for survival, dampening the klaxon when it’s too loud or unhelpful is sometimes necessary.

No existing medication can perfectly treat pain. Matching specific types of pain to drugs that target specific pathways can improve pain relief, but even then, medications can fail to work even for people with the same condition. More research that deepens the medical field’s understanding of the pain pathways and targets in the body can help lead to more effective treatments and improved pain management.

Source: How do painkillers kill pain? It’s about meeting the pain where it’s at | Ars Technica

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How To Move With Migraines

Migraines are the most common form of headache that can cause severe throbbing pain – usually on one side of the head – and severely affect quality of life. A migraine attack can last hours or days and often comes with nausea, vomiting and extreme sensitivity to light and sound.

According to a 2018 Deloitte Access Economics Report, almost 5 million people in Australia live with migraine, with 7.6% of them – around 400,000 people – experiencing chronic migraine, which means more than 15 migraine days per month.

Migraines are much more common in women than men and more prevalent in working-age people.

“During a flare, all people want to do is lie in a cold dark room and not do anything,” says Adnan Asger Ali, a physiotherapist and the deputy national chair at Musculoskeletal Physiotherapy Australia. But research shows regular exercise may have a preventive effect in reducing the number and intensity of migraines. One of the main reasons physical activity may help relieve migraines, says Ali, is that the body releases endorphins (natural painkillers) during exercise.

“Physical therapy can complement the pharmacological management of migraines,” he says. “It might mean that they take two Panadol instead of two codeine, and that’s still going to be a win because they’re not taking the hard stuff.”

A proper physical assessment is necessary to tailor a treatment plan to the individual, and individuals should consult with a health professional before embarking on a new exercise regime, but here are some suggestions on physical exercise that might help manage migraine.

The class: yoga and tai chi

Ali says slow movements, meditation and relaxation have significant beneficial effects on people who suffer from migraines. That includes activities such as yoga and tai chi.

In a recent randomized clinical trial that involved 114 patients aged 18 to 50 years with a diagnosis of episodic migraine, researchers found that people who practised yoga as an add-on therapy had less frequent and less intense migraines than those who received medical treatment alone.

Tai chi can also serve as a preventive measure for migraines. In a 2018 randomised controlled trial of 82 Chinese women with episodic migraines, researchers found that after 12 weeks of tai chi training, the women experienced significantly fewer migraine attacks.

The move: chin tuck

Neck stiffness and postural issues can be a driver for migraines, says Ali. He suggests the chin tuck, or cervical retraction, exercise to strengthen neck muscles and improve mobility.

The chin tuck exercise can be performed standing or sitting. Begin by sitting upright and looking straight ahead, keeping your neck and shoulders relaxed. Place a finger on your chin and gently glide your chin down – tuck your chin to your neck. Don’t hold your breath, move your head up or down or bend your neck forward.

You might feel a gentle pull at the base of the head and top of the neck. Hold the position for about five seconds and repeat the exercise 10 times – as long as it doesn’t cause any pain.

The activity: walking, jogging, running and cycling

Aerobic exercises such as walking, jogging, running and cycling might help mitigate migraine.

A systematic review of studies on exercise and migraine published in The Journal of Headache and Pain in 2019 found that moderate-intensity exercise – physical activities that elevate your heart rate and cause you to breathe harder but still allow you to carry on a conversation – can decrease the number of migraine days.

“Any activity that people will do consistently and that they enjoy will be good for them,” says Ali.

The hard pass: high-intensity interval training

Ali warns against HIIT workouts, which alternate short bursts of intense cardio exercise with rest or lower-intensity exercise. “Very high-intensity exercise is discouraged if it triggers your migraine,” he says.

In some people, high-intensity exercise can trigger a migraine attack. But research has shown that regular HIIT workouts might be more beneficial than moderate exercise for others, highlighting the importance of a personalized exercise plan.

By: Manuela Callari

Source: How to move: with migraines | Life and style | The Guardian

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Definition:

The main symptom of a migraine is usually an intense headache on 1 side of the head. The pain is usually a moderate or severe throbbing sensation that gets worse when you move and prevents you carrying out normal activities. In some cases, the pain can occur on both sides of your head and may affect your face or neck.

Additional symptoms

Other symptoms commonly associated with a migraine include:

  • feeling sick
  • being sick
  • increased sensitivity to light and sound, which is why many people with a migraine want to rest in a quiet, dark room

Some people also occasionally experience other symptoms, including:

Not everyone with a migraine experiences these additional symptoms and some people may experience them without having a headache. The symptoms of a migraine usually last between 4 hours and 3 days, although you may feel very tired for up to a week afterwards.

Symptoms of aura

About 1 in 3 people with migraines have temporary warning symptoms, known as aura, before a migraine.

These include:

  • visual problems – such as seeing flashing lights, zig-zag patterns or blind spots
  • numbness or a tingling sensation like pins and needles – which usually starts in 1 hand and moves up your arm before affecting your face, lips and tongue
  • feeling dizzy or off balance
  • difficulty speaking
  • loss of consciousness – although this is unusual

Aura symptoms typically develop over the course of about 5 minutes and last for up to an hour. Some people may experience aura followed by only a mild headache or no headache at all.

When to get medical advice

You should see a GP if you have frequent or severe migraine symptoms that cannot be managed with occasional use of over-the-counter painkillers, such as paracetamol. Try not to use the maximum dosage of painkillers on a regular or frequent basis as this could make it harder to treat headaches over time.

You should also make an appointment to see a GP if you have frequent migraines (on more than 5 days a month), even if they can be controlled with medicine, as you may benefit from preventative treatment. You should call 999 for an ambulance immediately if you or someone you’re with experiences:

References:

  • Paralysis or weakness in 1 or both arms or 1 side of the face
  • stroke or meningitis, and should be assessed by a doctor as soon as possible.

 

Expert Pharmacist GEMMA FROMAGE Reveals How To Save £200-a-Year On Everyday Essentials

For every condition, there is often a branded over-the-counter remedy we instinctively reach for. And yet there will be a cheaper version with identical contents that could save you a small fortune. Pharmacist GEMMA FROMAGE reveals the definitive guide to the best buys to fill your medicine cabinet.

Painkillers 

Best buys: Aspar Paracetamol 500mg, 16 caplets, 25p, sainsburys.co.uk; Bell’s Ibuprofen 200mg, 16 tablets, 45p, lloydspharmacy.comAnnual saving: £55.20* (Based on the average person buying eight packs of paracetamol a year, and for women, 12 packs of ibuprofen — one for each menstrual period.)

Some branded versions have special coatings, or are contained in soft capsules, and may dissolve more quickly in the body — however, the difference in speed of pain relief will be minimal

Some branded versions have special coatings, or are contained in soft capsules, and may dissolve more quickly in the body — however, the difference in speed of pain relief will be minimal

Expert says: The price of painkillers can vary hugely, yet the own-brand or cheaper versions will contain the same active ingredient in the exact same doses. As a result, they will do the exact same job as any expensive, branded options despite being up to ten times cheaper in some cases.

Some branded versions have special coatings, or are contained in soft capsules, and may dissolve more quickly in the body — however, the difference in speed of pain relief will be minimal.

Also, despite some products claiming to be designed for a specific type of pain, such as migraine or back pain, oral painkillers do not target one type alone, they work throughout the body so it won’t be targeted relief (but gels may offer this, see below).

Paracetamol and ibuprofen work differently: paracetamol can reduce a fever and ease cold and flu symptoms, whereas ibuprofen (which may also ease some of these problems) is an anti-inflammatory and so is beneficial for muscle aches and period pain. 

Antibacterial mouthwash 

Wisdom Chlorhexidine Antibacterial Mouthwash fresh mint

Best buy: Wisdom Chlorhexidine Antibacterial Mouthwash fresh mint, 300ml, £1.49, groceries.asda.com Annual saving: £35.10 (Based on going through ten bottles a year.)

Expert says: Studies have shown that chlorhexidine is the most effective mouthwash ingredient for killing bacteria that cause plaque and lead to gum disease (specifically gingivitis).

Despite the difference of more than £3.50 for the same size bottle of the branded version, the cheapest product contains the same active ingredient and will be just as effective in easing inflammation, swelling and bleeding associated with gum disease.

As with all mouthwash, use at a different time from brushing, as slooshing straight after will wash away most of the protective fluoride in toothpaste.

Allergy tablets

Best buys: Galpharm Cetirizine Hayfever And Allergy Relief, 30 tablets, £1.45, cooppharmacy.coop

Annual saving: £34.20 (Based on getting through four boxes over a year.)

Expert says: With an astounding £8.55 difference in price compared to the leading brand, it is hard to believe that the products contain the exact same 30 tablets of cetirizine at the same dose.

This medicine blocks the effects of histamine in your body, which immune cells release during an allergic response to a perceived irritant, such as pollen, which in turn causes symptoms such as sneezing and a runny nose. Take one a day.

Rehydration sachets  

Best buy: Asda Rehydration Treatment blackcurrant flavour, six sachets, £2.25, asda.com Annual saving: £6.16 (Based on buying a box four times a year.)

Asda Rehydration Treatment blackcurrant flavour

Asda Rehydration Treatment blackcurrant flavour

Expert says: Rehydration sachets — which you dissolve in a glass of water — contain electrolytes, vital salts such as sodium citrate and potassium chloride which keep the muscles and nervous system functioning properly (as well as sugar for energy). The body loses these as a result of diarrhoea, through dehydration, causing symptoms such as dizziness, headaches and tiredness.

Rehydration salts restore the natural balance of salts and fluid in the body, and help eliminate symptoms of dehydration.

There may be slight differences in the salts themselves, from one more expensive product to the next (and prices can be more than double this Asda option), but the overall effect will be the same.

Adults should mix one sachet with water and drink immediately after a loose bowel motion. (Do not give to children under two unless told to do so by a doctor.) If symptoms persist for more than 48 hours, seek medical advice.

LloydsPharmacy Chloramphenicol Eye Ointment

LloydsPharmacy Chloramphenicol Eye Ointment

Eye ointment

Best buy: LloydsPharmacy Chloramphenicol Eye Ointment, 4g, £4.99, lloydspharmacy.com

Annual saving: £5.22 (Based on buying two tubes a year.)

Expert says: Eye infections such as bacterial conjunctivitis are common, and the ointment used to treat them contains the active ingredient chloramphenicol, an antibiotic which stops the bug from growing and spreading.

There are many versions on pharmacy shelves, but the ointment always contains 1 per cent chloramphenicol (the drops always contain 0.5 per cent).

You apply a small amount to the infected eye three to four times a day for five days. A tube has to be binned 28 days after opening.

Nasal spray

Wilko Decongestant Nasal Spray

Wilko Decongestant Nasal Spray

Best buy: Wilko Decongestant Nasal Spray, 15ml, £1.75, wilko.com

Annual saving: £10.56 (Based on using four a year.)

Expert says: As part of the immune response during a cold, blood vessels swell, membranes become congested, and as a result the nose feels blocked.

Decongestant nasal sprays contain oxymetazoline hydrochloride which can help relieve symptoms by narrowing the small blood vessels in the nose. This brings down the swelling and helps open up the nasal passages to make breathing easier.

All sprays should work within minutes and the effects last for up to 12 hours. Identical sprays can cost up to four times as much.

Cold sore cream

Best buy: Bell’s Lipsore, 2g, £1, wilko.com Annual saving: £20.80 (Based on needing four a year.)

Expert says: At some point an estimated seven in ten of us will be infected with the virus HSV-1 (also known as herpes simplex virus type 1), which causes cold sores.

And once you have the virus, it is always in your body, where it lies dormant and is reactivated by triggers such as sunlight, stress and cold weather.

Treatments can speed up healing or try to halt outbreaks.

One of the most effective over-the-counter remedies is acyclovir, which stops the virus from reproducing, and in turn reduces the duration and severity of blisters.

Some products cost more than six times as much as this cut-price option, for the same size bottle with the same active dose.

Simply apply to the affected area with a cotton bud five times a day. 

Bell’s Lipsore

For cystitis 

Galpharm Cystocalm cystitis relief

Galpharm Cystocalm cystitis relief

Best buy: Galpharm Cystocalm cystitis relief, pack of six, £1.20, wilko.com

Annual saving: £7.40 (Based on using two packets a year.)

Expert says: Cystitis is an inflammation of the bladder, usually caused by a bladder infection, which causes acidic urine, irritation and an unpleasant burning sensation when passing water.

An effective remedy like this contains sodium citrate, which will make the urine less acidic, thus providing relief of the symptoms in a few hours — but some remedies can cost four times as much.

Mix with water and drink three times a day.

If you have no improvement in symptoms in three days, suffer regularly, or have blood in your urine, then see your GP. 

Ibuprofen gel 

Best buy: Tesco Ibuprofen Gel, 35g, £1.85, tesco.com

Annual saving: £12.42 (Based on buying three a year.)

Expert says: This anti-inflammatory gel contains 5 per cent ibuprofen — but identical versions can cost from £1.85 to £6 for the same size tube.

The gels are beneficial for massaging into muscular aches and pains.

Unlike oral painkillers, which get into the bloodstream and travel around the body, the ibuprofen in the gel is locally absorbed into the skin where it is applied.

This means that pain relief can be accurately targeted.

Massage the gel into the skin until fully absorbed, up to a maximum of three times a day.

Expert says: This anti-inflammatory gel contains 5 per cent ibuprofen — but identical versions can cost from £1.85 to £6 for the same size tube

Expert says: This anti-inflammatory gel contains 5 per cent ibuprofen — but identical versions can cost from £1.85 to £6 for the same size tube

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Tesco Health Chesty Cough Relief

Tesco Health Chesty Cough Relief

Cough syrup

Best buy: Tesco Health Chesty Cough Relief, 300ml, £2.25, tesco.com

Annual saving: £11.48 (Based on using two bottles a year.)

Expert says: A common ingredient in cough syrups is guaifenesin, which reduces chest congestion caused by colds or infections. It does this by loosening phlegm and making it easier to cough out.

Differences in these cough mixtures tends to be due to ingredients that make it taste better. However, this has no effect on how the product works, yet can cost four times more. 

Cold and flu remedy 

Asda Max Strength Cold & Flu Relief sachets blackcurrant

Asda Max Strength Cold & Flu Relief sachets blackcurrant

Best buy: Asda Max Strength Cold & Flu Relief sachets blackcurrant, pack of ten, £1.59, asda.com

Annual saving: £10.40 (Based on using four boxes a year.)

Expert says: There are several cold and flu sachets on the market and the most effective — such as this Asda option — will contain the painkiller paracetamol and decongestant phenylephrine, which reduces inflammation of the nasal tissue to open the airway. 

Yet some can cost up to four times as much for the same effect. Mix with boiling water and drink every six hours. Don’t use with other medicines containing paracetamol.

Arjun Olive Oil Ear Drops

Arjun Olive Oil Ear Drops

Ear drops

Best buy: Arjun Olive Oil Ear Drops, 10ml, £1.99, weldricks.co.uk

Annual saving: £7.08 (Based on needing three bottles a year.)

Expert says: Ear drops can contain medical-grade olive oil (which, unlike that in your kitchen, is licensed for use in the body) to soften hardened ear wax gently and make it easier to remove via syringing. 

Despite containing just this basic ingredient, some cost up to four times as much.

✱ Annual savings based on a comparison with the most expensive branded products at time of writing. Advertisement Read more:

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Painkillers Like Paracetamol Should Not Be Prescribed For Chronic Pain

US-HEALTH-OPIOID-OXYCODON-ILLUSTRATION

Painkillers such as paracetamol, ibuprofen, aspirin and opioids can do “more harm than good” and should not be prescribed to treat chronic pain, health officials have said.

Draft guidance from the National Institute for Health and Care Excellence (Nice) said that there was “little or no evidence” the commonly used drugs for chronic primary pain made any difference to people’s quality of life, pain or psychological distress.

But the draft guidance, published on Monday, said there was evidence they can cause harm, including addiction.

Chairman of the guidance committee Nick Kosky said that, while patients expected a clear diagnosis and effective treatment, the complexity of the condition means GPs and specialists can find it very “challenging” to manage.

The consultant psychiatrist at Dorset HealthCare NHS University Foundation Trust added: “This mismatch between patient expectations and treatment outcomes can affect the relationship between healthcare professionals and patients, a possible consequence of which is the prescribing of ineffective but harmful drugs.

“This guideline, by fostering a clearer understanding of the evidence for the effectiveness of chronic pain treatments, will help to improve the confidence of healthcare professionals in their conversations with patients.

“In doing so it will help them better manage both their own and their patients’ expectations.”

Chronic primary pain is a condition in itself which cannot be accounted for by another diagnosis or as a symptom of an underlying condition, Nice said.

It is characterized by significant emotional distress and functional disability with examples including chronic widespread pain and chronic musculoskeletal pain, it added.

Nice said an estimated third to half of the population may be affected by chronic pain while almost half of people with the condition have a diagnosis of depression and two-thirds are unable to work because of it.

The draft guidance, which is open to public consultation until August 14, said that people with the condition should be offered supervised group exercise programs, some types of psychological therapy, or acupuncture.

It also recommends that some antidepressants can be considered for people with chronic primary pain.

But it said that paracetamol, non-steroidal anti-inflammatory drugs such as aspirin and ibuprofen, benzodiazepines or opioids should not be offered because there was little or no evidence that they made any difference to people’s quality of life, pain or psychological distress.

There was evidence that they can cause harm, including possible addiction, it added.

The draft guideline also said that antiepileptic drugs including gabapentinoids, local anaesthetics, ketamine, corticosteroids and antipsychotics should not be offered to people to manage chronic primary pain because, again, there was little or no evidence that these treatments work but could have possible harms.

Paul Chrisp, director of the centre for guidelines at Nice, said: “”When many treatments are ineffective or not well tolerated, it is important to get an understanding of how pain is affecting a person’s life and those around them because knowing what is important to the person is the first step in developing an effective care plan.

“Importantly the draft guideline also acknowledges the need for further research across the range of possible treatment options, reflecting both the lack of evidence in this area and the need to provide further choice for people with the condition.”

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