Analgesics


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Analgesics

 

Definition

Analgesics are medicines that relieve pain.

Purpose

Analgesics are those drugs that mainly provide pain relief. The primary classes of analgesics are the narcotics, including additional agents that are chemically based on the morphine molecule but have minimal abuse potential; nonsteroidal anti-inflammatory drugs (NSAIDs) including the salicylates; and acetaminophen. Other drugs, notably the tricyclic antidepressants and anti-epileptic agents such as gabapentin, have been used to relieve pain, particularly neurologic pain, but are not routinely classified as analgesics. Analgesics provide symptomatic relief, but have no effect on the cause, although clearly the NSAIDs, by virtue of their dual activity, may be beneficial in both regards.

Description

Pain has been classified as "productive" pain and "non-productive" pain. While this distinction has no physiologic meaning, it may serve as a guide to treatment. "Productive" pain has been described as a warning of injury, and so may be both an indication of need for treatment and a guide to diagnosis. "Nonproductive" pain by definition serves no purpose either as a warning or diagnostic tool.
Although pain syndromes may be dissimilar, the common factor is a sensory pathway from the affected organ to the brain. Analgesics work at the level of the nerves, either by blocking the signal from the peripheral nervous system, or by distorting the interpretation by the central nervous system. Selection of an appropriate analgesic is based on consideration of the risk-benefit factors of each class of drugs, based on type of pain, severity of pain, and risk of adverse effects. Traditionally, pain has been divided into two classes, acute and chronic, although severity and projected patient survival are other factors that must be considered in drug selection.

Acute pain

Acute pain is self limiting in duration, and includes post-operative pain, pain of injury, and childbirth. Because pain of these types is expected to be short term, the long-term side effects of analgesic therapy may routinely be ignored. Thus, these patients may safely be treated with narcotic analgesics without concern about possible addiction, or NSAIDs with only limited concern for the risk of ulcers. Drugs and doses should be adjusted based on observation of healing rate, switching patients from high to low doses, and from narcotic analgesics to non-narcotics when circumstances permit.
An important consideration of pain management in severe pain is that patients should not be subject to the return of pain. Analgesics should be dosed adequately to ensure that the pain is at least tolerable, and frequently enough to avoid the anxiety that accompanies the anticipated return of pain. Analgesics should never be dosed on an as needed basis, but should be administered often enough to assure constant blood levels of analgesic. This applies to both the narcotic and non-narcotic analgesics.

Chronic pain

Chronic pain, pain lasting over three months and severe enough to impair function, is more difficult to treat, since the anticipated side effects of the analgesics are more difficult to manage. In the case of narcotic analgesics this means the addiction potential, as well as respiratory depression and constipation. For the NSAIDs, the risk of gastric ulcers limit dose. While some classes of drugs, such as the narcotic agonist/antagonist drugs bupronophine, nalbuphine and pentazocine, and the selective COX-2 inhibitors celecoxib and rofecoxib represent advances in reduction of adverse effects, they are still not fully suitable for long-term management of severe pain. Generally, chronic pain management requires a combination of drug therapy, life-style modification, and other treatment modalities.

Key terms

Acute pain — Pain that is usually temporary and results from something specific, such as a surgery, an injury, or an infection.
Analgesic — Medicine used to relieve pain.
Chronic pain — Pain that lasts more than three months and threatens to disrupt daily life.
Inflammation — Pain, redness, swelling, and heat that usually develop in response to injury or illness.
Osteoarthritis — Joint pain resulting from damage to the cartilage.

Narcotic analgesics

The narcotic analgesics, also termed opioids, are all derived from opium. The class includes morphine, codeine, and a number of semi-synthetics including meperidine (Demerol), propoxyphen (Darvon) and others. The narcotic analgesics vary in potency, but all are effective in treatment of visceral pain when used in adequate doses. Adverse effects are dose related. Because these drugs are all addictive, they are controlled under federal and state laws. A variety of dosage forms are available, including oral solids, liquids, intravenous and intrathecal injections, and transcutaneous patches.
NSAIDs are effective analgesics even at doses too low to have any anti-inflammatory effects. There are a number of chemical classes, but all have similar therapeutic effects and side effects. Most are appropriate only for oral administration; however ketorolac (Toradol) is appropriate for injection and may be used in moderate to severe pain for short periods.
Acetaminophen is a non-narcotic analgesic with no anti-inflammatory properties. It is appropriate for mild to moderate pain. Although the drug is well tolerated in normal doses, it may have significant toxicity at high doses. Because acetaminophen is largely free of side effects at therapeutic doses, it has been considered the first choice for mild pain, including that of osteoarthritis.
Topical analgesics (topical being those that are applied on the skin) have become much more popular in recent years. Those applied for local effect include capsaicin, methylsalicylate, and transdermal lidocaine. Transdermal fentanyl may be applied for systemic (the entire body in general) effect. In some cases, these topical agents reduce the need for drug therapy. Sales of pain relief patches have increased substantially in recent years. They are particularly useful for elderly patients who may not want to take a lot of tablets.

Recommended dosage

Appropriate dosage varies by drug, and should consider the type of pain, as well as other risks associated with patient age and condition. For example, narcotic analgesics should usually be avoided in patients with a history of substance abuse, but may be fully appropriate in patients with cancer pain. Similarly, because narcotics are more rapidly metabolized in patients who have used these drugs for a long period, higher than normal doses may be needed to provide adequate pain management. NSAIDs, although comparatively safe in adults, represent an increased risk of gastrointestinal bleeding in patients over the age of 60.

Precautions

Narcotic analgesics may be contraindicated in patients with respiratory depression. NSAIDS may be hazardous to patients with ulcers or an ulcer history. They should be used with care in patients with renal insufficiency or coagulation disorders. NSAIDs are contraindicated in patients allergic to aspirin.

Side effects

Each drug's adverse effects should be reviewed individually. Drugs within a class may vary in their frequency and severity of adverse effects.
The primary adverse effects of the narcotic analgesics are addiction, constipation, and respiratory depression. Because narcotic analgesics stimulate the production of enzymes that cause the metabolism of these drugs, patients on narcotics for a prolonged period may require increasing doses. This is not the same thing as addiction, and is not a reason for withholding medication from patients in severe pain.
NSAIDs can lead to ulcers and may cause kidney problems. Gastrointestinal discomfort is common, although in some cases, these drugs may cause ulcers without the prior warning of gastrointestinal distress. Platelet aggregation problems may occur, although not to the same extent as is seen with aspirin.

Interactions

Interactions depend on the specific type of analgesic.

Resources

Periodicals

"Analgesics: No Pain, No Gain." Chemist & Druggist (September 11, 2004): 38.
Kuritzky, Louis. "Topical Capsaicin for Chronic Pain." Internal Medicine Alert (September 29, 2004): 144.
"Pain Relief Patches Are Flying Off Store Shelves." Chain Drug Review (August 16, 2004): 15.
References in periodicals archive ?
Based on the description above, the researchers are interested in studying the side effects of analgesics and pain management of side effects and postoperative analgesia in patients in the Jakarta Islamic Hospital.
An important finding of this study was that in comparison to group P,the mean time until intake of the first dose of rescuemedication was longer in group T, submucosal tramadol resulted in the decrease of postoperative analgesics use which is also in accordance with the other studies5,17, providing evidence of the analgesic effectiveness of this kind of intervention.
Conclusively, attention must be given to the rational use of analgesics as irrational use by the patients and the irrational prescribing by practitioners has been observed.
The oral analgesics segment held about half of the market share in2015, and is anticipated to maintain this trend throughout the forecast period.
Analgesics is expected to increase in value at a CAGR of 6% at constant 2015 prices over the forecast period, with this positive performance set to be largely due to improvements in the Cameroonians economy and the anticipated decline in the prevalence of fake and substandard drugs in the country.
Analgesics is set to continue capitalising on the increasingly hectic lifestyles of many Italian consumers over the forecast period as high level of stress are often linked to tension headaches.
Additionally, as the Mintel report observes, "There is growing interest in analgesics with natural ingredients, supported by the 84 percent of consumers who express interest in buying these products.
During the same period, deaths involving opioid analgesics increased from 179 in 2003 to 883 in 2012 (Table).
Analgesics is expected to register a positive value CAGR at constant 2013 prices over the forecast period.
The wide variety of drugs in development includes opioid receptor ligands, bradykinin antagonists, mPGES-1 inhibitors, glutamate receptor antagonists, substance P and neurokinin receptor antagonists, norepinephrine transporter inhibitors,P2X2 neuron receptor antagonists and nitric oxide-based analgesics.
Compared with the 151 subjects who didn't use any acute antimigraine medication, those who used single analgesics for that purpose had an adjusted 61% Iower risk of progressing to chronic headache.
LONDON--Using any acute antimigraine medication--be it single or combination analgesics, or triptans--exerted a protective effect against developing chronic migraine in a large, prospective study of episodic migraineurs.