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Analgesics (Pain Killers) And Sedatives

- by Dr. James Meschino, DC, MS, ROHP

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Analgesic drugs act in various ways on the peripheral and central nervous systems; they include paracetamol (acetaminophen), the non-steroidal anti- inflammatory drugs (NSAIDs) such as the salicylates, narcotic drugs such as morphine, synthetic drugs with narcotic properties such as tramadol, and various others.

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Analgesics (Pain Killers) And Sedatives

Dr. James Meschino, 


1. Acetaminophen and NSAID’s

The exact mechanism of action of paracetamol (acetaminophen) is uncertain, but it appears to be acting centrally.

Aspirin and the other non-steroidal anti-inflammatory drugs (NSAIDs), like ibuprofen (Nurofen, Advil and Motrin) inhibit cyclooxygenases, leading to a decrease in prostaglandin production. This reduces pain and also inflammation (in contrast to paracetamol and the opioids, which do not reduce inflammation, but do reduce pain).

Excessive doses of acetaminophen can lead to kidney and liver damage.

NSAIDs predispose to peptic ulcers, renal failure, allergic reactions, and occasionally hearing loss, and they can increase the risk of hemorrhage by affecting platelet function.

2. Barbiturates

Are drugs that act as central nervous system depressants, producing a wide spectrum of effects, from mild sedation to anesthesia. They are also effective as anxiolytics, hypnotics and as anticonvulsants. They have addiction potential, both physical and psychological.

Barbiturates have now largely been replaced by benzodiazepines mainly due to benzodiazepines being significantly less dangerous in overdose. Barbiturates like pentobarbital and phenobarbital were long used as anxiolytics and hypnotics. Barbituates are thought to work by potentiating the inhibitory effects of GABA, by binding to certain GABA receptors.

3. Benzodiazepine

These also modify GABA receptor activity, slowing down central nervous system activity

Benzodiazepines used more as anxiolytics, for insomnia and as anti- convulsants than for pain control. Some common ones include (suffix “pam” is common):

  • alprazolam
  • bromazepam
  • chlordiazepoxide
  • clonazepam
  • clorazepate
  • diazepam
  • lorazepam 
  • medazepam 
  • nordazepam 
  • oxazepam 
  • prazepam

4. Friorinal For Migraines

Fiorinal and Firoinal-type drugs are a combination analgesic medication consisting of aspirin or acetaminophen, the barbiturate butalbital and caffeine. Some formulations also contain the opioid codeine. It is indicated for the treatment of tension headaches and is often used to treat migraines. The mechanism of action is not well understood. Since butalbital is habit-forming, using fiorinal daily can lead to dependency. Fiorinal #3 contains: 30 mg codeine, 50 mg butalbital, 40 mg caffeine, and 325 mg aspirin.

Other brand names include Fiormor, Fiortal, Fortabs, and Laniroif.

5. Opiates and Morphinomimetics

Morphine and various other substances (e.g. codeine, oxycodone, hydrocodone, diamorphine, pethidine) all exert a similar influence on the cerebral opioid receptor system.

Tramadol and buprenorphine are thought to be partial agonists of the opioid receptors. Dosing of all opioids may be limited by opioid toxicity (confusion, respiratory depression, myoclonic jerks and pinpoint pupils), but there is no dose ceiling in patients who tolerate this.

Codeine (methylmorphine) is an opiate that is used in many pain medications and is often included in cough syrups (antitussives), as it elevates the cough threshold at the level of the medulla. It is by far the most widely used opiate in the world and very likely most commonly used drug overall according to numerous reports.

Oxycodone - a semi-synthetic opioid synthesized from opium-derived thebaine

Percodan – contains oxycodone and aspirin 

Percocet – contains oxycodone and acetominophen 

Combunox – contains oxycodone and ibuprofen

Oxycodone is a narcotic and, even if taken only in prescribed amounts, can cause physical and psychological dependence when taken for a long time.

Common side effects: 






Analgesic Decision-Making

In choosing analgesia, the severity and response to other medication determines the choice of agent.Tthe WHO pain ladder, originally developed in cancer-related pain, is widely applied to find suitable drugs in a stepwise manner. The choice of analgesia is also determined by the type of pain: for neuropathic pain, traditional analgesia is less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants.

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