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Painkillers - Which one should you choose and when

Painkillers are some of the most commonly available over-the-counter drugs in the world. Whether it's for muscle cramp, a twisted ankle, an aching tooth or a nasty fall that required stitches, pain killers are literal life savers for many, if not all of us.


When there are so many options to choose from, which one do you go with? While every single ache or cramp isn't probably a visit-the-doctor situation, it's still necessary to be informed about the type of painkiller you need, how it works and when to take it.


Painkillers or analgesics are pharmacologically classified into opioid and non-opioid drugs.


Opioid drugs: are narcotics which are mainly used for moderate to high levels of pain. They can be naturally occurring, like morphine and codeine, synthetic (made by humans), like fentanyl and tramadol or semi-synthetic (man-made from naturally found compounds) like oxycodone. Opioids are heavily regulated drugs and require a doctor's evaluation and prescription because of their addictive properties.


Apart from opioids, we have the non-opioid drugs which are used to manage mild to moderate pain and are more available OTC, but still be used with precautions and preferably with a doctor's guidance (especially for chronic use)


Non-opioids can be classified very broadly into NSAIDs and Acetaminophen. We'll cover what each of these is and when they're used below.


1. NSAIDs: short for Non-Steroidal Anti-Inflammatory Drugs, they're your regular ibuprofens and aspirins. NSAIDs can be of different types, like non-selective (Salicylates like aspirin, ibuprofen), preferential (diclofenac, aceclofenac) and selective (etoricoxib), etc.


How do they act: In the human body, when there's an injury to a tissue, or an infection or inflammation, a compound called arachidonic acid is released. Arachidonic acid is then converted into prostaglandins (which are basically pain and fever promoters) and thromboxanes (which are used in blood clotting by clumping platelets). This conversion is promoted by enzymes called cyclooxygenases, or COX for short. Now, NSAIDs act by inhibiting these COX enzymes, thereby blocking the production of prostaglandins or thromboxanes, either temporarily or permanently. There are two different types of COXs - 1 and 2, which have different functions. You may have noticed some people being prescribed aspirin as a blood thinner for particular heart conditions - this is because aspirin inhibits the thromboxanes, which interfere with the process of blood clotting, thus preventing life-threatening clots.


When can NSAIDs be used: They can be taken for mild to moderate pain levels, for example, to relieve a headache, a period, a muscle cramp, a backache or a joint pain.


Dosages vary depending on the type of NSAID.


Side effects: Some prostaglandins have a gastroprotective effect, meaning they help prevent the GI tract from injury. Taking too many NSAIDs can take away this protective effect and lead to toxicity, GI ulcers, etc. It's important to be aware that NSAIDs must not be taken long-term without a doctor's approval, as they can cause ulcers, excessive bleeding (especially if on other blood thinners as well), and kidney damage, among many others. Consult a doctor if you're using NSAIDs for more than 5 days or if your pain has not subsided or is increasing.


2. Acetaminophen: commonly known as paracetamol. It's one of the most widely used painkillers worldwide and is efficient in treating mild to moderate pain such as regular headaches, muscle pain, fever or toothaches.


How does it act: Unlike NSAIDs, the way paracetamol acts hasn't been completely understood yet. Research suggests that it also acts on the COXs like NSAIDs, but to a weaker effect and it is also widely believed that it acts on the chemicals in the brain which control pain and body temperature.


When can it be used: Paracetamol is usually the most recommended drug as the first line of management for pain. Paracetamol can also be used to reduce fever, as it is an antipyretic. Common symptoms like headaches, migraines, muscle cramps, toothaches, back pain, etc., can be cured with a simple Acetaminophen.


Dosage: The recommended safe dosage of paracetamol is no more than 2g (2000 mg) per day. It should be spaced out to 500mg or 0.5g every 6 hours (dosage can vary by weight).


Side effects: Mainly liver toxicity along with associated organ damage, such as the kidneys. Paracetamol is primarily metabolised or broken down in the liver. It releases a metabolite, NAPQI, which directly damages liver cells.


So when should I choose paracetamol over ibuprofen?


Not every pain requires the same treatment, let alone both. Some milder conditions, like a pesky headache or a fever, can respond well to paracetamol, while inflammatory pain is better treated with an NSAID.


Stronger pain meds like opioids can be given by a healthcare professional when the pain is more severe and warrants a higher level of pain management.


How to use painkillers the right way?

Painkillers should always be used within the recommended dosage. Dosages are usually calculated by body weight and pre-existing conditions. They shouldn't be combined without proper guidance, as they can lead to serious side effects. If your pain is persistent, severe, or unclear in cause, it is important to seek medical advice rather than depending entirely on pain medication alone.


References:


2. Paracetamol (acetaminophen): A familiar drug with an unexplained mechanism of action - PMC https://share.google/fXz5LZiAFLcWoo3ON


3. Pain Management Medications - StatPearls - NCBI Bookshelf https://share.google/0cUcTCbfZUJSIlwGb


4. Analgesics Class of Medications (Painkillers & NSAIDs) https://share.google/wCIoN1VXJHILG1vol


Image: Google


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