Codeine indications

Metabolic studies of codeine indicate that approximately 10 percent of codeine (whose chemical name is methylmor-phine) is converted to its active metabolite, morphine it is this small fraction of morphine that provides codeine s analgesic effect. 

The presence of a significant amount of in the codeine indicates that the methyl ether can be demethylated in opium poppies) 0.49 ( H)... 

It is known that not all reactions proceed in the same manner on all adsorbent layers because the material in the layer may promote or retard the reaction. Thus, Ganshirt [209] was able to show that caffeine and codeine phosphate could be detected on aluminium oxide by chlorination and treatment with benzidine, but that there was no reaction with the same reagent on silica gel. Again the detection of amino acids and peptides by ninhydrin is more sensitive on pure cellulose than it is on layers containing fluorescence indicators [210]. The NBP reagent (. v.) cannot be employed on Nano-Sil-Ci8-100-UV2S4 plates because the whole of the plate background becomes colored. 

The -elimination of a thiyl radical (RS ) terminated a remarkably productive tandem radical bicyclization in Parker s formal total syntheses of ( )-codeine and ( )-morphine (see Scheme 14).29 Subjection of aryl bromide 72 to the conditions indicated generates transient aryl radical 73, an intermediate which engages the substi-... 

Monochromator 663, 791 Monodentate ligand 51 Morphine (and codeine) D. of (fu) 740 Mortar agate, 155 mullite, 155 percussion, 155 synthetic sapphire, 155 Muffle furnace 97 Multielement analysis 174, 184, 775 Multiple range indicators 268 Murexide 316... 

In the case of heroin, the indicator used is nonexclusive of heroin consumption, as it is also excreted to a high extent after administration of therapeutic morphine and in minor proportions after use of other opioids, such as codeine, pholcodine, and ethylmorphine. In order to obtain comparable results to previous studies [25, 31], an average medical administration of morphine of 10 mg/capita/year [45] and an excretion rate of 85% of morphine after therapeutic use [25, 31] were considered in the calculations. 

Codeine, dextromethorphan and pholcodine are opioid cough suppressants indicated for dry cough. Sedating antihistamines, such as diphenhydramine, tend to have an antitussive action as well. Vitamin C is not used in the management of cough but may be used as a prophylaxis against colds. 

One of the main side-effects of opioid analgesics, such as codeine and tramadol, is constipation. Amitriptyline (tricyclic antidepressant) and orphenadrine tend to have antimuscarinic properties, resulting in side-effects such as constipation. Senna is a stimulant laxative indicated in constipation. 

Three samples of codeine are analysed as described earlier, which indicate whether the TLC limit tests shown below pass or fail the samples. Solutions 1-3 appear in numerical order from left to right. 

Like morphine, codeine is a naturally occurring opioid found in the poppy plant. Codeine is indicated for the treatment of mild to moderate pain and for its antitussive effects. It is widely used as an opioid antitussive because at antitussive doses it has few side effects and has excellent oral bioavailability. Codeine is metabolized in part to morphine, which is believed to account for its analgesic effect It is one of the most commonly used opioids in combination with nonopioids for the relief of pain. The administration of 30 mg of codeine in combination with aspirin is equivalent in analgesic effect to the administration of 65 mg of codeine. The combination of the drugs has the advantage of reducing the... 

Hydrocodone (Hycodan), oxycodone (Roxicodone), dihydrocodeine, hydromorphone (Dilaudid), and oxy-morphone (Numorphan) are derivatives of codeine and morphine. All are indicated for the relief of mild to severe pain or for their antipyretic effects they are often used in combination with nonopioid analgesics. The drugs vary in potency, but their pharmacological effects do not differ significantly from those of codeine or morphine. 

Propoxyphene (dextropropoxyphene Darvon) is structurally related to methadone but is much less potent as an analgesic. Compared with codeine, propoxyphene is approximately half as potent and is indicated for the treatment of mild pain. It is not antipyretic or antiinflammatory like aspirin and is less useful than aspirin in most cases of mild pain. Toxicity from propoxyphene, especially in combination with other sedatives, such as alcohol, has led to a decrease in its use. Death following ingestion of alcohol in combination with propoxyphene can occur rapidly (within 20 minutes to 1 hour). The drug is not indicated for those with histories of suicide or depressive illnesses. 

Pharmacokinetic properties Codeine (Sindrup and Brosen, 1995) has a good oral bioavailability. The compound is extensively metabolized by O- and N-demethylation followed by glucuronidation. The main metabolites are norcodeine, morphine and hydrocodeine and their glucuronides. There are indications (Yue et al., 1997), that the analgesic effect is reduced in persons with low CYP2D6 activity (poor metabolizers). 

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. 

Semi-synthetic and synthetic opioids (meperidine, hydrocodone, fentanyl, etc.) are the result of many attempts to produce effective yet safer analgesics. The fact that both morphine and codeine are still widely used indicates that the newer opioids have been only moderately successful. However, current knowledge of the opioid system makes the goal of producing the perfect... 

Codeine plays a relatively minor role in the overall picture of opioid prescription drug abuse. Evidence indicates that proper prescribing of codeine for legitimate medical concerns does not greatly increase the risk of addiction and abuse. Those in the medical community agree that more education is needed on both sides to help prevent the potential for abuse and addiction, so that patients tmly in need are not denied access to codeine based on misperceptions and fear. The benefits for individuals and society are great when chronic pain is treated safely and effectively. 

Meperidine was first synthesized in the late 1930s, and was one of the first synthetic opioids. The fact that both morphine and codeine are still widely used, though, indicates that meperidine, along with all of the opioids produced since that time, have been only modest successes. Research continues with the hope of discovering the perfect opioid analgesic. 

A survey published in 2001 shows that primary care physicians would much rather prescribe Schedule III pain relievers—such as acetaminophen with codeine—for chronic pain not due to cancers. Thirty-five percent of the 161 doctors responding to the mailed survey stated they would never prescribe Schedule II opioids to be used around-the-clock by patients in persistent pain. Those who would be willing to give the Schedule II drugs were those who also indicated a lower degree of concern about... 

Pentazocine is a potent analgesic of the benzo-morphan series with a 50 rag oral dose equivalent to 60 rag of codeine. It is also a weak narcotic antagonist with about one-fiftieth the activity of nalorphine. Pentazocine is indicated in the treatment of moderate to severe pain. It is also used as a preanesthetic and anesthetic supplement (1,2). 

Hamilton Application Catalog 13. p.8 (1992) resolved from morphine, codeine, thebaine. cocaine, reserpine. and methadone also plant extract [565]. p. 67 HPLC [569.705. p. 215] TLC [656] Sterisomers [757] Stability indicating [755] also [206]... 

W. R. Sisco, C. T. Rittenhouse, and L. A. Everhart, Simultaneous high-performance liquid chromatographic stability-indicating analysis of acetaminophen and codeine phosphate in tablets and capsules, J. Chromatogr., 348 253 (1985). 

---