Narcotic analgesic agents

Importantly, the narcotic analgesic agents (see Chapter 11) retained an almost comfortable status in this are upto the recent times, such as morphine, hydromorphone, codeine, hydrocodone, methadone and levorphanol. 

Incorporation of the benzylic carbon of phenylacetic acid into a cyclohexane ring affords an agent whose activity is closely related to that of the narcotic analgesics. This activity is particularly noteworthy for the fact that this structure repre-... 

Few studies have explored the efficacy of opioids specifically for OA. The APS recommends against the use of codeine and propoxyphene for OA because of the high incidence of adverse effects and limited analgesic effectiveness. Oxycodone is the most extensively studied of the agents recommended for OA. However, other narcotic analgesics such as morphine, hydromorphone, methadone, and transdermal fentanyl are also effective. 

Where pain is worsened by muscle spasm, oral muscle relaxants may serve as a useful adjunct to therapy.25 These agents include baclofen, metaxalone, methocarbamol, carisoprodol, and cyclobenzaprine. Muscle relaxants may decrease spasm and stiffness associated with either acute or chronic musculoskeletal disorders. These agents should be used with caution because they all may cause sedation, especially in combination with alcohol or narcotic analgesics. 

In the aftermath of World War II, problems with amphetamine abuse began to arise. An epidemic of amphetamine abuse and related cases of amphetamine-induced psychosis arose first in Japan and later in the United States. Since that time, use of amphetamines and other stimulants has been greatly curtailed and as a class are more tightly regulated than virtually any other psychotropic agents, with the exception of narcotic analgesics. 

A not uncommon side effect observed with morphine and some of the other narcotic analgesics is constipation due to decreased motility of the gastrointestinal tract. It proved possible to so modify pethidine as to retain the side effect at the expense of analgesic activity. Relief of diarrhea, it will be realized, is a far from trivial indication. Alkylation of the anion from diphenylacetonitrile (95) with ethylene dibromide gives the intermediate, 96. Alkylation of normeperidine (81) with that halide affords diphenoxylate (97), an antidiarrheal agent. 

HydroNarcotic Analgesic/NSAID] Uses Mod-severe pain (<10 d) Action Narcotic w/ NSAID Dose 1—2 tabs q4-6h PRN Caution [C, M] Renal insuff -1- effect w/ ACE inhibitors diuretics t effect w/ CNS d ressants, EtOH, MAOI, ASA, TCA, anticoagulants Contra Component sensitivity Disp Tabs SE Sedation, fatigue, GI upset see Hydrocodone Acetaminophen Interactions -1- Effects OF ACEIs, diuretics EMS See Hydrocodone Acetaminophen T risk of bleeding w/ heparin use OD See individual agents... 

It is indicated as a narcotic analgesic supplement in general or regional anaesthesia, as an anaesthetic agent with oxygen and skeletal relaxant in selected high risk patients (e.g. open heart surgery). 

MAOIs have the most serious pharmacodynamic interactions of any antidepressant class. As discussed earlier, they can cause a hypertensive crisis and the serotonin syndrome. They potentiate the hypertensive effects of most sympathomimetic amines, as well as tyramine, which is the reason for the avoidance of over-the-counter preparations containing such agents, in addition to the tyramine-free diet ( 508, 509). The serotonin syndrome occurs most often when MAOIs are used in combination with SSRIs and venlafaxine but it can also occur when MAOIs are used with tryptophan, 5-hydroxytryptophan, and some narcotic analgesics. In addition, MAOIs can also significantly potentiate the sedative and respiratory depressant effects of narcotic analgesics. 

Nature has been a potential source of therapeutic agents for thousands of years. An impressive number of modem dmgs have been derived from natural sources. Over the last century, a number of top selling dmgs have been developed from natural products. Anticancer dmg vincristine from Vinca rosea, narcotic analgesic morphine from Papaver somniferum, antimalarial dmg artemisinin from Artemisia annua, anticancer dmg Taxol from Taxus brevifolia and antibiotic peniciUins from Penicillium ssp. are just a few examples. 

It should be noted, however, that the TI is a relative term. Acetaminophen, a nonprescription analgesic, has a TI of approximately 27 (i.e., the ratio of the median toxic dose to the median effective dose equals 27). Prescription agents tend to have lower TIs. For instance, the narcotic analgesic meperidine (Demerol)... 

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