The effect on ileostomy function of codeine phosphate, Lomotil, or Isogel was tested in 20 subjects at home living a normal life, studied over two three-day periods on and off treatment. Codeine phosphate 60 mg three times daily was associated with a reduction in the mean total weight of ileostomy output and the ileostomy outputs of water, sodium, and potassium (p < 0.05). The proportion of fae...

In 2009 we reported the fatal case of a toddler who had received codeine after adenotonsillectomy for obstructive sleep apnea syndrome. The child was an ultra-rapid metabolizer of cytochrome P4502D6 (CYP2D6). We now report 3 additional fatal or life-threatening cases from North America. In the 2 fatal cases, functional gene duplications encoding for CYP2D6 caused a significantly greater product...

Administering codeine to breast-feeding mothers had been considered safe until the recent death of a breast-fed neonate whose mother had been prescribed codeine. We investigated the risk of opioid poisoning to breast-fed neonates using coupled physiologically based pharmacokinetic models for the mother and child. Neonatal morphine plasma concentrations were simulated for various combinations of...

Smoking is predisposed by social, environmental and genetic factors including variation in CYP2A6, CYP2D and CYP2B6, which encode nicotine and codeine metabolizing enzymes. In early adolescence, CYP2A6-induced slow nicotine metabolism was related with higher dependence and reduced cigarette consumption. Our commentary has fully extended prior work illustrating that slow nicotine metabolism medi...

16 Alkaloids including galanthamine (1) and codeine (2) are reported to be positive allosteric 17 modulators of nicotinic acetylcholine receptors (nAChRs) but the binding sites responsible 18 for this activity are not known with certainty. Analogues of galanthamine (1), codeine (2) and 19 morphine (3) with reactivity towards cysteine thiols were synthesised including conjugated 20 enone derivat...

Codeine has been prescribed to pediatric patients for many decades as both an analgesic and an antitussive agent. Codeine is a prodrug with little inherent pharmacologic activity and must be metabolized in the liver into morphine, which is responsible for codeine's analgesic effects. However, there is substantial genetic variability in the activity of the responsible hepatic enzyme, CYP2D6, and...

To determine whether the antidiarrheal action of opiate drugs in humans is due to enhanced intestinal absorption rates, as suggested by recent experiments in animals, or is due to altered intestinal motility, as traditionally thought, we studied the effect of therapeutic doses of codeine on experimental diarrhea and on the rate of intestinal absorption of water and electrolytes in normal human ...

We report the production and comparative specificities of antisera raised to different immunogens containing codeine, morphine, and oxycodone. Antisera raised to bovine serum albumin (BSA) conjugates of codeine-6-hemisuccinate, ethylmorphine-6-hemisuccinate, or oxycodone-6-carboxymethyloxime had greatest recognition of structural changes around the piperidine ring nitrogen atom and th 14-positi...

Postmortem samples from 14 cases of suspected heroin overdose were subjected to a preliminary systematic toxicological analysis in order to highlight the presence of unknown exogenous compounds (e.g., drugs of abuse, alcohol) that may have played a role in the mechanism of death. This analysis unveiled histories of poly-drug use in seven of the cases under investigation. Moreover, the concentra...

The present study aimed to investigate the stability of morphine, morphine-3-β-glucuronide (M3G), morphine-6-β-glucuronide (M6G), 6-acetylmorphine (6-AM) from heroin metabolites, and codeine, codeine-6-glucuronide, nor-codeine, fentanyl, norfentanyl, paracetamol, caffeine its adulterants at room temperature for 24 hours in order understand effect instability postmortem redistribution (PMR). m...