Other Opiate Pain Relievers

Among the remedies which it has pleased Almighty God to give to man to relieve his sufferings, none is so universal and so efficacious as opium. 

If pain is moderate, a doctor might consider prescribing an NSAID 

4000 b.c. Reference to the opium poppy is found in ancient Sumerian texts and Egyptian art. 

3200-2600 b.c. Fossilized opium poppies have been found 

dating back to Neolithic settlements in what is now Switzerland. Alexander the Great, king of Macedonia, introduces opium to Persia and India. 

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The gold standard of opiate pain relievers is morphine. It was one of the first compounds extracted, isolated, and purified from the opium poppy, and it continues to be one of the most widely used pain relievers today. Morphine and other opiate drugs such as heroin, codeine, oxycodone, and hydrocodone have very similar chemical structures (Figure 3.2). However, other opiates such as fentanyl and meperidine (Demerol) have a slightly different structure (Figure 3.3). 

As seen in Figure 3.7, the most widely abused opiate pain relievers are Darvocet , Darvon , and Tylenol with codeine , followed by Vicodin, Lortab , and Lorcet . Methadone is the least addicting of the opiate pain relievers and stays in the body the longest. Because of this, methadone is often used as a substitute for morphine, heroin, and other more addictive opiates to wean people off the drug to which they are addicted. 

In addition, morphine has served as a point of departure for the discovery of many medically usefnl derivatives. These inclnde codeine, a pain reliever and cough suppressant, levophanol, an orally active analgesic (morphine is not active when given orally and is nsnally given by injection), and many other modem and highly potent opiate analgesics. 

A final note The opiate-containing poppy seeds that many people consume as part of their morning muffin or bagel have no pain-relieving or other psychoactive effect because the dose is far too low. Nonetheless, it is possible to detect traces of... 

Doctors are most likely to prescribe morphine or other opiates when pain is severe and expected to be short-lasting (a few days to a week), such as after injury or major surgery. This is because short-term use of opiates is less likely to lead to tolerance (loss of potency with repeated use of the drug) and dependence (addiction). However, the problem becomes more complex when the severity of the pain requires the use of pain-relieving medication for more than a few weeks, because this is when tolerance and addiction to opiates tend to develop (see the section on Opiate Addiction on page 48). 

In Chapter 10 we discussed the use of opiate drugs in the treatment of pain. But the use of opiates for pain relief is usually reserved for severe cases. Many effective painkillers are available over the counter, and aspirin is the most widely known and used. Acetylsalicylic acid (aspirin) is closely related to a chemical found in the bark of the willow and other trees (salicylic acid). Willow bark was used in the treatment of painful conditions and fever by the ancient Greeks and by Native Americans. Salicylic acid was isolated and used as a pain reliever in Europe, but it causes severe stomach distress. It was not until the late 19th century that acetylsalicylic acid was synthesized and named aspirin by the. Bayer Company of Germany. Aspirin has come to be one of the most important drugs in medicine. It is marketed under the brand names Anacin, Bufferin, and Excedrin to name just a few, and more than 10,000 tons of aspirin are consumed in the United States every year (Julien, 2005). 

Incidence and prevalence of opiate nse are widely variable depending on the drug. In 2002, there were 166,000 current heroin users. Collectively, use of opiates other than heroin is far more common. An estimated 4.4 million people used narcotic pain relievers and 1.9 million persons ages 12 or older used what SAMHSA classified as OxyContin nonmedically at least once in their fifetime." ... 

The discovery of a naturally occurring peptide called endorphin in the brain led to a search for pain-killing drugs that would be less addictive than morphine or other opiates used to relieve pain. The new drugs would be as natural as endorphin, and they could provide new insight into the molecular processes of addiction. 

The opium alkaloid morphine is representative for this group of opiates and also for other opioid analgesics. Morphine is a full agonist for both the jx and the k receptors. It is used to relieve severe acute pain, or chronic pain in terminally ill patients. Its oral bioavailability varies from 15% to 35% and its... 

Morphine Morphine (C17H19NO3), a habit forming Class A analgesic drug, is the major bioactive constituent of opium poppy seeds. Like other opium constituents (opiates), e.g. heroin, morphine acts directly on the CNS to relieve pain. Morphine is used for the treatment of post-surgical pain and chronic pain (e.g. cancer pain), and as an adjunct to general anaesthesia, and... 

Chlorzoxazone (Paraflex, Parafon Forte DSC, Others) [Skeletal Muscle Relaxant/ANS Drug] Uses Adjunct to rest physical therapy to relieve discomfort associated w/ acute, painful musculoskeletal conditions Action Centrally acting skeletal muscle relaxant Dose Adults. 250-500 mg PO tid-qid Peds. 20 mg/kg/d in 3-4 + doses Caution [C, ] Avoid EtOH CNS depressants Contra Severe liver Dz Disp Tabs SE Drowsiness, tach, dizziness, hepatotox, angioedema Interactions T Effects W/ antihistamines, CNS depressants, MAOIs, TCAs, opiates, EtOH, watercress EMS Use of CNS depressants and concurrent EtOH use can T sedation urine may turn reddish purple or orange OD May cause N/V/D, dizziness, HA, X deep tendon reflexes, hypotension and resp depression symptomatic and supportive, activated charcoal may be effective... 

For the relief of pain arising from spasm of smooth muscle, as in renal or biliary colic, morphine is frequently employed. Other measures including antispasmodics such as atropine, atropine substitutes, theophylline, nitrites, and heat may be employed first however, if they are ineffective, meperidine, methadone, or opiates must be used. Morphine relieves pain only by a central action and may aggravate the condition producing the pain by exaggerating the smooth muscle spasm. Morphine may also be indispensable for the relief of pain due to acute vascular occlusion, whether this be peripheral, pulmonary, or coronary in origin. In painful acute pericarditis, pleurisy, and spontaneous pneumothorax, morphine is likewise indicated. Carefully chosen and properly spaced doses of codeine or morphine may occasionally be necessary in pneumonia to control pain, dyspnea, and restlessness. Traumatic pain arising from fractures, bums, etc., frequently requires morphine. In shock, whether due to trauma, poisons, or other causes, morphine may be required to relieve severe pain. 

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