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PubMedDate not supplied

Monitoring saliva concentrations of methaqualone, codeine, secobarbital, diphenhydramine and diazepam after single oral doses.

A preliminary investigation was undertaken to determine the feasibility of monitoring saliva levels of drugs for forensic purposes. Single oral doses of the title compounds were administered to healthy volunteers. Plasma and saliva levels were measured and ratios calculated for all drugs except diazepam. Saliva/plasma ratios for methaqualone, diphenhydramine and secobarbital were all less than one and reasonably consistent between collection times and subjects. The saliva/plasma ratios for codeine were more variable, but always greater than one. Although more detailed investigation is necessary, saliva may be a useful medium for forensic monitoring of drug ingestion.

Administration, Oral↗
PubMedDate not supplied

Application of the combined use of fused silica capillary columns and NPD for the toxicological determination of codeine and ethylmorphine in a human overdose case.

The applicability of capillary gas chromatography to the toxicological analysis of extracts of human tissue samples was investigated for codeine and ethylmorphine in a case of drug overdose. After column extraction, the samples were injected onto a fused silica capillary column, using a direct injection technique. The nitrogen-phosphorus detector provided excellent stability and sensitivity without the need for extensive clean-up procedures.

Adult↗
PubMedDate not supplied

Simultaneous determination of codeine and morphine in urine and blood by HPLC.

A procedure is presented for the determination of nanogram quantities of codeine and morphine in biological specimens by HPLC. The quantitative method is based on hydrolysis of the urine samples followed by basic extraction of urine and blood with organic solvents. Separation by liquid chromatography is a reverse phase system on a Spherisorb-CN (5 micron) column with a mobile phase of 40% methanol and phosphate buffer, pH 6.8. The method separated the opiates for screening purposes and was used for confirmation of morphine detected by radioimmunoassay.

Chromatography, High Pressure Liquid↗
PubMed1984

Descriptive epidemiology of mortality in New Jersey due to combinations of codeine and glutethimide.

A review of records of the Toxicology Laboratory of the New Jersey State Medical Examiner's Office yielded a total of 36 deaths attributable to overdose of "hits," an oral combination of codeine and glutethimide, during 1980-1981. During the same period, 126 deaths due to heroin overdose and 46 deaths due to methadone overdose occurred. The majority of hits cases (77.8%) occurred in the Newark vicinity. Demographic features of persons who died of the three agents are presented, and some explanations are advanced for the unexpectedly high mortality due to the oral narcotic combination.

Adult↗
PubMed1996

An assessment of the routes of incorporation of opiates into beard hair after a single oral dose of codeine.

The time course of appearance of immunoreactive opiates was monitored in saliva, sweat, and beard hair in six healthy whites who were not opiate users after oral administration of 60 mg of codeine phosphate. The opiate concentration in saliva peaked within 30 min of drug administration and returned to near the predose level within 24 h. Ninety-one percent of the total secretion of opiates in sweat was collected by the skin-collection patch worn during the first 24 h after drug administration. Detectable material was also present in sweat patches on the following 2 days. Opiates were detected in extracts of alkali digests of beard hair in all subjects on the day after drug administration. Hair concentration peaked on day 3 after dosing and then decreased continuously until day 8. From day 8 until the end of the experiment on day 14, beard hair contained opiate concentrations significantly greater than the predose level. From comparison with cotinine pharmacokinetics, it is proposed that an early and the largest transfer of opiates into beard hair is through sweat. Transfer during hair growth is secondary and of comparable importance to a newly identified contribution of long duration that may involve transfer from storage depots within skin.

Adult↗
PubMed1989

The effects of octreotide, soy polysaccharide, codeine and loperamide on nutrient, fluid and electrolyte absorption in the short-bowel syndrome.

Four agents, which could delay intestinal transit, were tested in six short-bowel patients (jejunal length 30-120 cm) on long-term nutritional/electrolyte replacement therapy. Intestinal transit time of a liquid test meal and nutrient, water and sodium absorption were measured during a control study and with each test agent on separate days. Soy polysaccharide tended to increase transit time, but decreased the absorption of water, sodium and nutrients. Codeine phosphate and loperamide caused inconsistent and clinically unimportant changes. Octreotide, a long-acting analogue of somatostatin, delayed transit and increased water, sodium and calorie absorption from the meal. Octreotide appears to have the potential to reduce the need for electrolyte and nutritional supplements in patients with the short-bowel syndrome.

Codeine↗
PubMed1984

An electromyographic method of objectively assessing cough intensity and use of the method to assess effects of codeine on the dose-response curve to citric acid.

The integrated surface abdominal electromyogram (EMG) has been used as a simple measurement of cough intensity which correlates well with the volume, air flow and noise produced in different coughs. Using the integrated abdominal EMG as a measure of cough intensity, dose response curves to inhaled citric acid can be drawn which are highly reproducible. We have studied the effects of codeine (60 mg) on these curves, and have demonstrated a reduction in cough intensity. It is suggested that this method of testing the effects of an antitussive on such a dose-response curve may be a useful one.

Action Potentials↗
PubMed1991

Differential foetal development of the O- and N-demethylation of codeine and dextromethorphan in man.

1. Codeine and dextromethorphan were N-demethylated in human foetal liver microsomes at high rates which were close to the activities in adult livers. In contrast, foetal liver microsomes did not catalyze the O-demethylation of these drugs at mid-gestation. 2. The metabolic data were in accordance with the absence of P450IID6 and the presence of P450 IIIA as determined by Western blotting with anti-human P450 IID6 (MAb 114/2) and anti-rat P450 IIIA (PCN 2-13-1/C2) monoclonal antibodies, respectively. 3. The inhibitory effects of midazolam and dehydroepiandrosterone support the contention that the N-demethylase is a human foetal form of the cytochrome P450 IIIA family. Consistent with this we found that blotting with the MAb PCN 2-13-1/C2, which recognizes an epitope specific for the P450 III family, correlated well with the N-demethylase activities.

Antibodies, Monoclonal↗
PubMed1998

Solitary rectal ulcer induced by excessive use of analgesic suppositories containing paracetamol, caffeine, and codeine.

We report the case of a 53-yr-old woman who developed an ulcer of the distal rectum with mild stenosis after prolonged use of suppositories containing paracetamol, caffeine, and codeine. After undergoing extensive diagnostic tests with exclusion of other possible causes, she admitted to the abuse of the suppositories. She was treated with frequent endoscopic balloon dilations to prevent progression of the rectal stenosis. Because of severe pain on defecation, she needed a protective colostomy which could be closed after the healing of the ulcer 7 months later. There was no significant residual stenosis. This case is compared to cases described in the past 30 years.

Acetaminophen↗
PubMed1999

Transformations of codeine to important semisynthetic opiate derivatives by Pseudomonas putida m10.

A biotransformation mixture which contained codeine and washed cells of Pseudomonas putida M10 gave rise to a number of transformation products that are of clinical importance which included hydrocodone, dihydrocodeine and 14beta-hydroxycodeine. Incubations with the same organism and codeinone gave rise to 14beta-hydroxycodeinone and 14beta-hydroxycodeine. Cell-free extracts and membrane fractions of P. putida M10 were shown to catalyse the 14beta-hydroxylation of codeinone. In addition, the potent analgesic oxycodone was shown to be produced from 14beta-hydroxycodeinone.

Alcohol Oxidoreductases↗
PubMed1997

Neonatal abstinence syndrome due to codeine.

The neonatal abstinence syndrome (NAS) is a potentially life threatening illness associated with significant morbidity especially in the neonatal period. A case of NAS due to codeine prescribed for pain relief during pregnancy is reported. Clinicians should be aware that narcotic derivatives prescribed in late pregnancy can give rise to this type of problem.

Acetaminophen↗
PubMed1981

A double-blind comparison of ibuprofen, ASA-codeine-caffeine compound and placebo in the treatment of dental surgery pain.

A double-blind randomized clinical trial was conducted in eighty-seven patients with mild, moderate or severe dental surgery pain to evaluate the analgesic activity of a single dose of the following compounds: (i) ibuprofen 400 mg, (ii) ACC-30 (a compound containing ASA 375 mg; codeine phosphate 30 mg; caffeine citrate 30 mg), (iii) placebo. Ibuprofen was significantly better than ACC-30 and placebo on almost all pain intensity, degree of relief and duration of analgesia parameters. ACC-30 was not significantly different from placebo on any analgesic measurement. No serious side-effects were reported with any of the study medications.

Adult↗
PubMed2000

Variable cytochrome P450 2D6 expression and metabolism of codeine and other opioid prodrugs: implications for the Australian anaesthetist.

Codeine is a popular opioid prodrug dependent on the activity of the specific cytochrome P450 enzyme 2D6 (CYP2D6). This enzyme catalyses the production of the potent analgesic metabolite morphine, but genetic studies have demonstrated that individuals from different ethnic groups exhibit considerable variability in the functional capacities of their expressed CYP2D6 enzymes, and pharmacological studies have shown many commonly prescribed drugs can reduce the action of CYP2D6 enzymes. These findings have significant clinical implications for the rational prescription of effective analgesia, especially in a multicultural country like Australia.

Analgesics, Opioid↗
PubMed1997

Comparison of the efficacy of paracetamol versus paracetamol, codeine and promethazine (Painstop) for premedication and analgesia for myringotomy in children.

This prospective double-blinded study compared the analgesic effectiveness and incidence of complications of a compound preparation Painstop (Paedpharm Pty Ltd) containing paracetamol 12 mg, codeine 0.5 mg and promethazine 0.65 mg per 1.0 ml, dosage 1.0 ml/kg, with paracetamol 20 mg/kg. Ninety-five children aged 1 to 12 years, ASA 1-2, scheduled for myringotomy and drain tuber insertion as a day procedure were randomized to receive Painstop or paracetamol 30 to 60 minutes prior to surgery. Preoperative drowsiness and complications on induction and postoperative sedation, pain and times to achieve goals were recorded. The groups were comparable for age, gender, weight, anaesthetic technique and duration of surgery. Times to eye opening (P = 0.05) and first oral intake (P = 0.006) were significantly longer in the Painstop group. There was, however, no difference in times to discharge. Late sedation was more common in the Painstop group (P = 0.03). Pain scores were low and similar in both groups and the need for additional analgesia was uncommon.

Acetaminophen↗
PubMed1983

Paracetamol overdose: protective effect of concomitantly ingested antimuscarinic drugs and codeine.

Twelve cases of paracetamol overdose are reported. Nine patients ingested antimuscarinic agents and/or codeine concomitantly. Our findings indicate that 'mixed' overdose of this type gives rise to marked attenuation of the rate of paracetamol absorption and, apparently, reduced morbidity associated with paracetamol poisoning. It is speculated that suitable antimuscarinic agents may be incorporated into paracetamol formulations to achieve inhibition of gastric emptying and to confer a degree of protection in case of overdose.

Acetaminophen↗
PubMed1983

A suspected case of codeine-induced erythema multiforme.

Erythema multiforme usually presents as an acute inflammatory reaction involving the skin and mucous membranes. Systemic symptoms and organ involvement also can occur. The disease is associated with many illnesses and drugs. A two-year-old child presented to the Family Practice Center with a probable codeine-induced episode of erythema multiforme. The patient had been treated with Actifed-C Expectorant for a suspected viral upper respiratory tract infection. The rash was characteristic of erythema multiforme, but there was no involvement of mucous membranes. The rash quickly abated after the discontinuation of the drug and the administration of hydroxyzine. A viral cause for the rash could not be ruled out. When erythema multiforme is precipitated by a particular drug, discontinuation of the offending agent is necessary. The rash should disappear quickly. Adjunctive use of antihistamines may offer some benefit for the patient. Systemic corticosteroids may be necessary for more severe cases.

Child, Preschool↗