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Painkiller Drug Information

Painkillers, also known as analgesics, are a class of drugs used to relieve pain. They work by blocking pain signals or by interfering with the brain’s interpretation of pain. There are two kinds of painkillers: Non-narcotics and Narcotic.

Non-Narcotic Painkillers:

Acetaminophen (in more than 600 over-the-counter and prescription medications, including Tylenol, Excedrin, Paracetemol, Vicodin, Percocet, etc.)

Acetaminophen is the most commonly used over-the-counter, non-narcotic analgesic.  The parent compound to acetaminophen was discovered to reduce fevers in the late 1800s, but due to its high toxicity it was not used in medicine. But in 1949 it was found that a compound called phenacetin converted to its metabolite, acetaminophen in the body. Acetaminophen began to be used and became widely available as an ingredient in many non-prescription and prescription drugs to relieve migraines and tension headaches. Acetaminophen does not have anti-inflammatory activity and will not effect blood clotting (homeostasis). Its pain relieving ability is about equal to that of aspirin.

Acetaminophen is completely absorbed from the gastrointestinal tract and reaches peak plasma concentrations in less than an hour. Once in the blood stream, it relieves pain by increasing your body’s threshold to the sensation of pain. It also reduces fever by eliminating excess heat.  Ultimately the blood filters through the liver where the majority of the acetaminophen is broken down (metabolized), then excreted in the urine. 

In the United States, Acetaminophen toxicity is the most common cause of liver failure, and is responsible for nearly 50% of all cases. This far surpasses the numbers for hepatitis.

Acetaminophen is contained in more than 100 products, and is known as paracetamol and N-acetyl-p-aminophenol (APAP). The liver breaks down most of the drug into safe components that can be removed from the body in urine. However, a small amount of Acetaminophen metabolizes into a harmful by-product called N-acetyl-p-benzoquinoneimine (NAPQI). When this toxic chemical is produced greater than the body can remove it, the main cells of the liver are destroyed. This largely occurs because of the depletion of Glutathione.   Glutathione, the master antioxidant of the body is required for the safe detoxification of Acetaminophen (paracetamol) and other harmful toxins.  Glutathione converts fat-soluble toxins into water-soluble forms for safe and efficient elimination by the body. But Acetaminophen not only depletes Glutathione, but it blocks the production of Glutathione, allowing the NAPQI to build up and react with cellular proteins, killing the cells in the process. Chronic use of Acetaminophen is known to cause liver damage.

Acetaminophen should only be used in the recommended doses only. Considering more than 100 products contain acetaminophen, its important to add the amounts from each item.  In 2009 the recommendations for the maximum adult daily dose for acetaminophen was reduced from 4,000 mg per day to 3,250 mg.  The recommendations also limited the strength of immediate release versions of the drug and placed greater controls on the use of acetaminophen in liquid formulations for children.

Narcotic Painkillers: There are two types of narcotic analgesics (painkillers): Opiates and the Opiods (derivatives of Opiates)

  • Codeine (Tylenol #2, 3, 4)
  • Darvocet (Propoxyphene & Acetaminophen)
  • Darvon (Propoxyphene
  • Duragesic (Fentanyl Patch)
  • Hydromorphone (Palladone, Dilaudid)
  • Morphine (MSContin, Oramorph)
  • Oxycodone (Oxycontin, Roxicodone)
  • Percocet (Oxycodone & Acetaminophen)
  • Percodan (Oxycodone & Aspirin)
  • Talwin NX (Pentazocine & Naloxone)
  • Ultram (Tramadol)
  • Vicodine (Hydrocodone & Acetaminophen)

The human body naturally produces its own opiate-like substances and utilizes them as neurotransmitters. They are called the Endogenous Opiods (endorphins, enkephalins and dynorphin) that modulate our reactions to pain and regulate vital functions such as hunger and thirst, but they are also involved in mood control, immune response and other body processes.

Among the brain’s numerous functions, it is the natural chemist of the body. The brain produces more than 50 identified active drugs that are associated with memory, intelligence and relaxation. Endorphin is our natural painkiller that is 3 times more potent than morphine.

The reason opiates affect us so powerfully is that they bind to the same receptors as our natural opiods, decreasing GABA and increasing Dopamine. In addition, three kinds of receptors that open the ion channels to reduce the excitability of the neurons are widely distributed throughout the brain (mu, delta, and kappa receptors). This reduced excitability is partially the source of euphoria experienced by opiates.  But the euphoric effect also appears to involve GABA, the inhibitory neurotransmitter. When opiates attach to the GABA receptor, they reduce the amount of GABA released.  Normally, GABA reduces the amount of dopamine released, but by reducing the amount of GABA, opiates actually increase the amount of dopamine, and therefore the amount of pleasure felt.

Stimulating dopamine turns on the brains reward system. In addition to inducing euphoria, Dopamine stimulates the memory centers of the brain. Research from the Harvard School of Medicine suggests that because Opiates stimulate the release of Dopamine and Dopamine stimulates memory, there may be a memory component to addiction that triggers memories that remind us of the good feelings produced by the drug. Within this system, morphine activate opiate receptors in the mid-brain, the drug and reward circuitry of the brain; the nucleus accumbens, where reward, pleasure, laughter, addiction, aggression, fear and the placebo effect is believed to exist; and the cerebral cortex, the area connected to memory, attention, perceptual awareness, thought, language and consciousness.

Unfortunately, prolonged opiate use may cause the brain to adapt, and it then becomes dependent on the drug to function normally.  If the drug is removed, the person experiences the opposite of pleasure – anxiety, irritability, low mood, pain, nausea, chills, cramping and sweating.

Opiates also act directly on the respiratory center where they cause a slowdown in activity and decrease the breathing rate. Excessive amounts of an opiate, like heroin, can cause the respiratory center to shut down breathing completely. During an overdose of heroin, it is the action of heroin in the brainstem respiratory centers that can cause the individual to stop breathing and die.

Side Effects May Include: Nausea, Vomiting, Drowsiness, Dry mouth, Miosis (contraction of the pupil), Orthostatis hypotension (blood pressure lowers upon standing), Urinary retention, Constipation and/or fecal impaction, Confusion, Hallucinations, Delirium, Hives, Itching, Hypothermia, Bradycardia (slow heart rate), Tachycardia (rapid heart rate), Raised intracranial pressure, Urinary spasm, Muscle rigidity, Flushing, Respiratory depression, Fatal overdose

Synthetic Opiods

- Methadone (Symoron, Dolophine, Amidone, Methadose, Physeptone, Heptadon)

- Suboxone

Methadone is a synthetic opiate synthesized by a German pharmaceutical during WWII as a painkiller.  Currently Methadone is used primarily to treat opiate addiction, but has been used as a painkiller with more frequency. But Methadone has a much longer half-life (length of time the drug stays in the body) than Opiates.  Adverse reactions including death, happen at the beginning of treatment in methadone programs due to excessive doses and subsequent toxicity. Many erroneously estimate the amount of Methadone required for the desired effect. Like heroin, high doses of Methadone can stop the respiratory center causing death.  Many describe addiction to Methadone as much more challenging than any Opiate, including heroin.

Side Effects May Include: Muscle spasms, Difficulty breathing, Slow, shallow and labored breathing, Pinpoint pupils, Bluish skin - fingernails - lips, Stomach spasms and/or intestinal tract, Constipation, Weak pulse, Low blood pressure, Drowsiness, Disorientation, Coma

Suboxone is a combination of Buprenorphine and Naloxone. Buprenorphine is an opiod partial agonist-antagonists and naloxone is in a class called opioid antagonist. It is believed that Suboxone blocks the opiate receptor, preventing the body from responding to opiates and endorphins. While some have expressed success using Suboxone to quit Opiates, others deem it a greater challenge.

It is advised not to combine Suboxone with antidepressants, sedatives, tranquilizers, or sleeping pills. But additional caution is advised with herbal products, acetaminophen, antifungals, oral contraceptives, some blood pressure and heart medications, niacin, and other medications. Check with your pharmacist.

Side Effects May Include: Headache, Dizziness, Difficulty Breathing, Stomach pain, Vasodilation (widening of the blood vessels), Constipation, Diarrhea, Nausea, Stuffy Nose, Sweating, Fever, Anxiety, Depression, Insomnia, Dizziness, Runny eyes


    *While great care has been taken in organizing and presenting the material throughout this website, please note that it is provided for informational purposes only and should not be taken as Medical Advice. More...

    *Because these drugs can cause severe withdrawal reactions, do not stop taking any medication without first consulting your physician. The decision to quit any medication should be discussed with your doctor and with their consent and support. More...*Because these drugs can cause severe withdrawal reactions, do not stop taking any medication without first consulting your physician. The decision to quit any medication should be discussed with your doctor and with their consent and support. More...