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This paper highlights the abuse potential of the codeine containing cough syrups, which may take two forms. One, experimental abuse in school or college students which later persists in a dependent pattern. Two, pre-existing opioid abusers, as a substitute which starts after the school or college years. The short term treatment outcome is better in the former group in that they are able to maintain abstinence for a relatively longer period.
We encountered a terminal lung cancer patient with severe back pain and dyspnea who refused the use of morphine, and succeeded in home palliative care with the use of an original prescription (CA), the main ingredient of which was codeine phosphate.
Discrepancies exist between reports arising from single-dose and multiple-dose studies intended to compare the efficacy of oral analgesics. D Differences in the pharmacokinetic characteristics of these drugs account for much of the discord. Codeine and fenoprofen rapidly achieve their ultimate plasma equilibrium levels (on a q. 6h. schedule), whereas, propoxyphene requires a longer period, doubtless due to its longer half-life and proportionately smaller maintenance dose. If the drugs are not to be compared during the steady state, then administration of appropriate loading doses permits satisfactory single dose comparisons at steady-state concentrations.
In the anesthetized dog, codeine causes a combination of pulmonary vasoconstriction and systemic vasodilation. Pulmonary blood flow is either increased or decreased, relating to a primary stimulation or depression of myocardial contractility. The overall effect is an elevation in pulmonary arterial pressure largely due to vasoconstriction of the pulmonary blood vessels.
We evaluated the tolerance to NIM in patients with adverse reactions to NSAIDs, expressed by urticaria-angioedema, bronchial asthma or erythema polymorphous on 92 patients among which 32 atopics affected by asthma, rhinitis or contact dermatitis. Challenge test has been performed with increasing amounts of NIM per os every 2 hrs to a maximum of 100 mg/dose. The last dosage was repeated every 12 hrs for 4 times more. No reactions were observed in 86 patients (93.4%). Moreover we evaluated the efficacy of NIM in modulating pomphoid cutaneous reaction to histamine (HIS) and codeine (COD). Three subjects were prick tested with HIS and COD solutions at different concentrations (0.1 to 10 mg/ml), before and after a 5 days therapy with NIM at different dosages/kg/die. At NIM dosages of 3.7 and 2.7 mg/kg/die we observed a strong reduction of pomphoid activity of both HIS and COD. No clear effects were detected at 2.2 mg/kg/die dosage. We assume a dose-related in vivo inhibitory effect of NIM on cutaneous mast cells releasability or a direct anti-histaminic effect. We point out the possible therapeutic role of NIM in the treatment of allergic flogosis at steroid and cromon's side.
We have recently found that codeinone, an oxidation metabolite of codeine, induced apoptosis, characterized by internucleosomal DNA fragmentation and mitochondrial cytochrome c release in HL-60 human promyelocytic leukemic cell lines, most effectively among 10 opioids. These findings prompted us to investigate whether codeinone induces apoptosis in other human cancer cells and possible changes in mitochondrial enzyme. FACS analysis demonstrated that codeinone induced the production of ANNEXIN-positive apoptotic cells in three different human cancer cells (HL-60, MCF7, A549). The apoptotic cells were visualized by microscopical observation after staining with Hoechst (H)-33342. Fluorometric assay showed that codeinone time-dependently activated caspase 3 and caspase 9, but not caspase 8, suggesting the activation of intrinsic apoptotic signaling pathway via mitochondria. Western blot analysis demonstrated that codeinone enhanced the Pro-apoptotic Bax protein expression, but reduced the anti-apoptotic Bcl-2 protein expression. Codeinone did not significantly change the manganese superoxide dismutase (MnSOD) activity nor its mRNA expression. This apoptosis-inducing activity, in conjunction with antinociceptive activity, further substantiated the antitumor potential of codeinone.
In a single-dose, parallel group, randomized block treatment allocation study, the relative analgesic efficacy of flurbiprofen, a nonsteroidal antiinflammatory drug, was compared to acetaminophen 650 mg with codeine 60 mg, zomepirac sodium 100 mg, and placebo. A total of 226 post-surgical dental patients (146 females and 80 males) participated in the study. Flurbiprofen in 50 mg and 100 mg dosages demonstrated effective analgesic activity with the 100 mg dosage being at least as effective as the acetaminophen/codeine combination. The results of this study support previous work on flurbiprofen.
The regulatory effects of various endocrine factors on allergic processes have been widely studied. The clinical importance of hyperthyroidism in asthma and in chronic urticaria has been demonstrated in several cases. These observations may be attributed to modulatory effects of thyroid hormones on mast cell releasability and/or on other target organs as blood vessels. To evaluate the effects of thyroid hormones on mast cell releasability and on the cutaneous vasculature, we analyzed the wheal and flare response to compound 48/80, to codeine, and to histamine in patients with hyperthyroidism and in a control group. No significant difference was found between the two groups. We could not demonstrate any in vivo effect of the thyrotoxic state on the cutaneous response to these substances.
Nine healthy subjects were given 1 mg ketotifen orally and were skin tested with histamine (4, 10, and 20 micrograms/mL), codeine (0.001%, 0.01%, and 0.1%) and normal saline at varying time intervals up to 96 hours. Seven subjects allergic to tree and dust allergens were studied in the same way and were skin tested with both allergens. The suppression of skin responses in both studies occurred maximally between 4 and 24 hours, and did not disappear until 72 hours. The control subjects not taking ketotifen did not show any suppression. These results suggest that oral ketotifen should be withheld for 72 hours prior to immediate type hypersensitivity skin tests.
Abuse of the oral combination of glutethimide (DORIDEN) and codeine, commonly referred to as "sets", in the northwest Pennsylvania area is reviewed. Nine fatalities have been reported in the Erie area from 1985-87 due to acute toxicity with this combination. The glutethimide/codeine combination reportedly produces a euphoric effect comparable to intravenous heroin but is longer lasting. Age of the victims ranged from 18 to 37 years. In all cases there was a history of chronic intentional "sets" abuse by the victims prior to death. The 9 fatalities due to this combination of prescription drugs is unusually high for this area considering the population and rural nature of the Erie community. Although the use of "sets" has been reported occasionally in other localized areas of the country, no other significant use has been reported in Pennsylvania.
In a double-blind control study, oral doses of placebo, propoxyphene napsylate (50 or 100 mg), or codeine sulfate (30 or 60 mg) were administered to 46 postepisiotomy patients, grouped by severity of pain reported at first-dose drug administration. Eight hourly observations by a trained observer provided estimates of analgesia. The analgesia scores for placebo treatments were significantly lower than for the lesser doses of either drug (P less than .05) as well as for the greater doses (P less than .01). At both dose levels, the analgesia scores for both drugs were almost identical. Analgesia with the higher doses was greater than with the lower, but not to a statistically significant extent. The difference in patient responses increased following the second dose. No serious adverse reactions occurred; the elicited and volunteered reports of minor side effects were similar for all five treatments.
In a double-blind, single-dose study, the analgesic effect of a combined ibuprofen-codeine phosphate preparation was compared with those of zomepirac and placebo in 127 patients with moderate or severe postepisiotomy pain. Both the combination and zomepirac were significantly more effective than placebo for up to six hours, but the onset of action of the combination was more rapid than that of zomepirac. The study was notable for the virtual absence of side effects.
This paper evaluates the dose-response relationship of several doses of fenoprofen calcium, between 12.5 and 300 mg, and their relationship to 60 mg of codeine sulfate and placebo. Three separate parallel studies are included in this evaluation, including a total of 867 patients. The types of pain were cesarean section, episiotomy wound, uterine cramping, and general surgery. This paper shows that a significant increasing relationship exists between efficacy and dose of fenoprofen, suggesting that relatively larger doses of fenoprofen will achieve greater amounts of efficacy.
A twenty-year-old white male subject without a history of psychiatric disorder developed hallucinations and paranoid symptoms following ingestion of 540 mg codeine over a period of 36 hr. The symptoms reached an intensity where hospitalization became necessary but no specific treatment was required. In less than 72 hr, the patient completely recovered from his symptoms and was subsequently discharged. In view of the available data on the neurochemical effects of opiates and non-narcotic analgesics, it was concluded that inhibition of prostaglandin biosynthesis or interference with its action might have caused the psychotic symptoms reported.
A simple and accurate spectrophotometric procedure for the analysis of a mixture of acetaminophen, salicylamide, and codeine phosphate is described. Determination of the first 2 components depends on pH-induced differential spectral changes of their nitroso derivatives. The third component is assayed by the acid dye method. The proposed procedure was successfully applied to the analysis of laboratory-made and commercial tablets containing the ternary drug mixture.
We have modified our radiometric assay for ethylmorphine N-demethylase to examine the metabolism of codeine. We find that the current assay gives excellent separation of metabolites with a zero time activity of 0.08%. The N- and O-demethylations are linear for up to 30 min with up to 1 mg/ml of microsomal protein. The pH profiles show slightly different maxima (N-demethylation, pH 8.0; O-demethylation, pH 7.8). The kinetic parameters for N-demethylation were markedly higher (Vmax = 5.6 nmol/min/mg protein; KM = 714 microM) than those for O-demethylase (Vmax = 0.75 nmol/min/mg protein; KM = 149 microM). These data suggest that the HCHO results primarily from the N-demethylase. Further, the differences in the kinetic parameters and the pH profile suggest that these two activities are catalyzed by different enzymatic systems.
One hundred and eighty patients (American Society of Anesthesiologists rating 1-2) received one of three oral analgesics--ciramadol (Wy. 15705) 20 mg, ciramadol 60 mg or codeine 60 mg--on a double-blind random basis for the relief of pain 24-48 hours after major general surgical, gynaecological or orthopaedic operations. All three analgesics proved equally effective and caused mild sedation only. No patient showed signs of clinical cardiorespiratory depression, and other side-effects were infrequent. Ciramadol may therefore prove a useful clinical alternative to conventional oral analgesics provided its lack of respiratory depressant properties and addiction potential in monkeys can be substantiated in humans.
A 3-year-old White child was admitted to the critical care unit in a coma after a generalized convulsion. Codeine and salicylic acid were present in his plasma. The possible aetiology and management are discussed.