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What Are Analgesics (Painkillers)?

A Painkiller (also called pain killers, pain medications, pain relievers) and medically known as an Analgesic is defined as a drug used to relieve pain, or achieve analgesia, by blocking pain signals going to the brain or by interfering with the brain's interpretation of the signals.
An analgesic (also known as a painkiller) is any member of the diverse group of drugs used to relieve pain (achieve analgesia). The word analgesic derives from Greek an- ("without") and -algia ("pain"). 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. Many studies have shown that properly managed medical use of pain killer compounds is safe and rarely causes addiction. Taken exactly as prescribed, opioids can be used to manage pain effectively.

How do Analgesics (Painkillers) work ?

It is not fully understood how painkillers work. Damaged or inflamed body tissues produce various chemicals which send signals through the nervous system to the brain. The brain produces the sensation of pain. Different painkillers act at different points in this process. For example, NSAIDS may act at the point of injury , whereas others act on the nerves or brain.

In choosing analgesia, the severity and response to other medication determines the choice of agent; the 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.

According to recent figures from the US Drug Enforcement Administration (DEA), in the last ten years the number of painkillers sold and distributed in the United States by hospitals, retail pharmacies, and doctors has risen by 600%. Most of the increased sales are painkiller pills that contain oxycodone, the active ingredient in the painkiller OxyContin, once known as "hillbilly heroin".

Morphine, the archetypal opioid, 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. Opioids, while very effective analgesics, may have some unpleasant side-effects. Up to 1 in 3 patients starting morphine may experience nausea and vomiting (generally relieved by a short course of antiemetics). Pruritus (itching) may require switching to a different opioid. Constipation occurs in almost all patients on opioids, and laxatives (lactulose, macrogol-containing or co-danthramer) are typically co-prescribed. When used appropriately, opioids and similar narcotic analgesics are otherwise safe and effective, however risks such as addiction and the body becoming used to the drug (tolerance) can occur. The effect of tolerance means that drug dosing may have to be increased if it is for a chronic disease this is where the no ceiling limit of the drug comes into play. However what must be remembered is although there is no upper limit there is a still a toxic dose even if the body has become used to lower doses.

Analgesics are frequently used in combination, such as the paracetamol and codeine preparations found in many non-prescription pain relievers. They can also be found in combination with vasoconstrictor drugs such as pseudoephedrine for sinus-related preparations, or with antihistamine drugs for allergy sufferers. The use of paracetamol, as well as aspirin, ibuprofen, naproxen, and other NSAIDS concurrently with weak to mid-range opiates (up to about the hydrocodone level) has been shown to have beneficial synergistic effects by combatting pain at multiple sites of action—NSAIDs reduce inflammation which, in some cases, is the cause of the pain itself while opiates dull the perception of pain—thus, in cases of mild to moderate pain caused in part by inflammation, it is generally recommended that the two be prescribed together.

Common side effects and adverse reactions of painkillers:

nausea
vomiting
drowsiness
dry mouth
miosis (contraction of the pupil)
orthostatic
hypotension (blood pressure lowers upon sudden standing)
urinary retention
constipation and/or fecal impaction
Less common side effects and adverse reactions:
confusion
hallucinations
delirium
hives
itch
hypothermia
bradycardia (slow heart rate)
tachycardia (rapid heart rate)
raised intracranial pressure
ureteric or biliary spasm
muscle rigidity
flushing
Most severe side effects and adverse reactions:
respiratory depression
fatal overdose

Chronic use of pain killers can result in tolerance to the medications so that higher doses must be taken to obtain the same initial effects. Long-term use also can lead to physical addiction—the body adapts to the presence of the substance and withdrawal symptoms occur if use is reduced abruptly. Individuals taking prescribed pain killer medications should not only be given these medications under appropriate medical supervision, but also should be medically supervised when stopping use in order to reduce or avoid withdrawal symptoms. Symptoms of withdrawal can include restlessness, muscle and bone pain, insomnia, diarrhea, vomiting, cold flashes with goose bumps (“cold turkey”), and involuntary leg movements.

Individuals who become addicted to pain killers can be treated.

Options for effectively treating pain killer addiction to prescription opioids are drawn from research on treating heroin addiction.

Prolonged use of these drugs eventually changes the brain in fundamental and long-lasting ways, explaining why people cannot just quit on their own, and why treatment is essential. In effect, drugs of abuse take over the brain's normal pleasure and motivational systems, moving drug use to the highest priority in the individual's motivational hierarchy, thereby overriding all other motivations and drives. These brain changes, then, are responsible for the compulsion to seek and use drugs that we have come to define as addiction. This is likely the state people are in when they are reportedly "doctor shopping," feigning illnesses, and stealing from pharmacies to obtain the drug.

Fortunately, we have a number of effective options to treat pain killer addiction to prescription opioids and to help manage the sometime severe withdrawal syndrome that accompanies sudden cessation of drug use. These options are drawn from experience and clinical research regarding the treatment of heroin addiction. They include medications, such as methadone and LAAM (levo-alpha-acetyl-methadol), and behavioral counseling approaches.

Caution: The United States FDA estimates that 200,000 Americans are hospitalized every year because of overdoses of painkillers and side effects of normal doses by causing gastrointestinal problems and liver damage, they also cause thousands of deaths a year. Use of Tylenol, particularly with alcohol, can readily cause hepatitis and liver failure. In people aged over 60, the most common cause of gastritis, peptic ulcers and upper gastrointestinal bleeding is the use of NSAIDs (Non-steroidal anti-inflammatory drugs).

At least half a million people receive treatment and rehabilitation for painkiller addiction and abuse per year. All painkillers have potential side effects so you need to weigh up the advantages against the disadvantages.

Common Opioids based painkillers:

ULTRAM™ (tramadol hydrochloride) and ULTRACET™ (tramadol with acetaminophen) are prescription painkillers used to treat medium to moderately severe pain. Side effects may include: dizziness, drowsiness, or headache, anxiety; nausea, vomiting, constipation, diarrhea, nervousness, tremor, itching, dry mouth, and sweating. Tramadol can be addictive and withdrawal effects are possible if the painkillers are stopped suddenly after long or higher dosages.

Oxycodone - Used as an analgesic and can be made into other pharmaceuticals including OxyContin™ (a controlled-release painkiller) and with aspirin (Percodan™) or with acetaminophen (Percoset™). These drugs are prescribed for pain relief. They all require a doctor's prescription and are prescribed for moderate to severe pain.

Vicodin™ - A hydrocodone mixed with acetaminophen. Hydrocodone is a semi-synthetic opioid similar in effects to morphine and when abused, can lead to dependence, tolerance, and/or addiction. Vicodin™ is one of the most frequently prescribed painkillers. Other similiar products include Vicoprophen™, Tussionex™, and Lortab™.

Cocaine - A stimulant crystalline tropane alkaloid that is obtained from the leaves of the coca plant. It is a stimulant of the central nervous system and an appetite suppressant. Because of the way it affects the mesolimbic reward pathway, cocaine is addictive. Cocaine is used in medicine as a topical anesthetic for pain, even in children, specifically in eye, nose and throat surgery. The major disadvantages of this use are cocaine's side effects and intense vasoconstrictor activity and potential for cardiovascular toxicity.