Prophylactic oral ibuprofen or ibuprofen-codeine versus placebo for postoperative pain after primary hip arthroplasty

The postoperative analgesic effect of ibuprofen was compared with a combination of ibuprofen and codeine versus placebo. The study was prospective, randomized, double blind with 123 consecutive hip arthroplasly operations. All the patients received oral diazepam as premedication and spinal anaesthesia with bupivacaine 5 mg/ml 3–4 ml.
Postoperatively, when the spinal anaesthesia started to wear off, the patients were randomly assigned to one of three groups; the ibuprofen group (n=48) received 800 mg of ibuprofen orally. The ibuprofen/codeine group (IC, n=48) received 800 mg of ibuprofen combined with 60 mg of codeine. The placebo group (P, n=25), received oral placebo medication. The patients were observed for the need of additional opioid (e.g. ketobemidone), pain score (verbal and VAS), bleeding and side effects for five hours. The patients in the placebo group (P) had significantly higher pain scores ( P >0.05) compared with the two other groups after 2 and 4 hours, with no significant differences after 1, 3 and 5 hours. The P group also received 45% more opioids ( P <0.001) compared with the two other groups during the same period. No significant differences in bleeding or side-effects were observed between the groups. There were no significant differences between the ibuprofen group and the ibuprofen/codeine group.
We conclude that a prophylactic dose of 800 mg ibuprofen orally has an opioid sparing effect with a tendency of less pain experience during the first hours after hip arthroplasty.     

Reinforcing properties of some opiates and opioids in rhesus monkeys with histories of cocaine and codeine self-administration

Rhesus monkeys were conditioned to press a key to selfadminister intravenous injections of either cocaine (8 monkeys) or codeine (7 monkeys). Every tenth lever press resulted in an injection of 50 mcg/kg/inj. cocaine or codeine during daily 3 h sessions. Equal doses of cocaine and codeine generated regular comparable rates of self-administration responding. After responding stabilized, different narcotic and non-narcotic analgesics (morphine, codeine, detropropoxyphene, propiramfumarate, pentazocine and nalorphine) were substituted for cocaine or codeine. At appropriate doses all drugs except for nalorphine, maintained self-administration responding. Monkeys with a codeine self-administration history self-administered higher numbers of injections and showed less intraindividual variability than monkeys with a cocaine self-administration history.Parts of these experiments were presented on the 33rd Meeting of the Committee on Problems of Drug Dependence Toronto, Februar 1971.     

The pharmacology of medieval sedatives: The “Great Rest” of the Antidotarium Nicolai

Ethnopharmacological relevance

Past practices of compound drugs from different plant ingredients enjoyed remarkable longevity over centuries yet are largely dismissed by modern science as subtherapeutic, lethal or fanciful.

Aim of the study

To examine the phytochemical content of a popular medieval opiate drug called the “Great Rest” and gauge the bioavailability and combined effects of its alkaloid compounds (morphine, codeine, hyoscyamine, scopolamine) on the human body according to modern pharmacokinetic and pharmacodynamic parameters established for these compounds.

Calculations and theory

We reviewed the most recent studies on the pharmacodynamics of morphine, codeine, hyoscyamine and scopolamine to ascertain plasma concentrations required for different physiological effects and applied these findings to dosage of the Great Rest.

Results

Given the proportional quantities of the alkaloid rich plants, we calculate the optimal dose of Great Rest to be 3.1±0.1–5.3±0.76 g and reveal that the lethal dose of Great Rest is double the therapeutic concentration where all three alkaloid compounds are biologically active.

Conclusion

This study helps establish the effective dose (ED₅₀), toxic dose (TD₅₀) and lethal dose (LD₅₀) rates for the ingestion of raw opium, henbane and mandrake, and describes their probable combined effects, which may be applied to similar types of pre-modern pharmaceuticals to reveal the empirical logic behind past practices.     

高效液相色谱-质谱联用分析磷酸可待因及其精氨酸布洛芬复方中的有关物质

建立了高效液相色谱法检查磷酸可待因、磷酸可待因与精氨酸布洛芬复方的有关物质,并采用HPLC-TOF／MS和LC—MS／MS对磷酸可待因及两种复方药物产生的降解产物进行了结构鉴定。色谱柱为ClR（250mm×4．6mm,5μm）,柱温50℃,流速1mL／min,检测波长245nm,醋酸铵（0．04M,用醋酸调pH6．0）-乙腈（92：8,v／v）为流动相A,乙腈为流动相B,梯度洗脱。磷酸可待因在氧化条件下很不稳定产生了两个N-氧可待因异构体,在碱性破坏中得到了新的杂质,其结构可能为6-羟基-3-甲氧基-17-甲基-7,8-双脱氢吗啡-5-醇。在酸性破坏条件下磷酸可待因和精氨酸布洛芬可发生酯化反应。所建立的HPLC方法灵敏、准确,可有效测定磷酸可待因、磷酸可待因与精氨酸布洛芬复方的有关物质,并对产生的降解产物进行了结构鉴定,为更好的控制磷酸可待因与磷酸可待因复方药物的质量提供了依据。     

磷酸可待因片的细胞毒性研究

目的：比较两个企业的磷酸可待因片剂的处方优劣。方法：检测两个企业的磷酸可待因的片剂、原料和辅料的细胞毒性。结果：A企业片剂的IC50值为0.169 mg·ml^-1,B企业片剂的IC50值为0.140 mg·ml^-1,两企业片剂的IC50值差异有统计学意义（P〈0.05）;两企业原料的IC50值差异无统计学意义（P〉0.05）。结论：两企业磷酸可待因片剂的细胞毒性差异主要由辅料不同导致,A企业处方优于B企业。     

Purple drank prevalence and characteristics of misusers of codeine cough syrup mixtures

A mixture of codeine cough syrup with alcohol and/or a soft drink known as “purple drank” has gained media attention in recent years as a drug associated with professional athletes and southern rap music. The existing research on purple drank consumption has primarily utilized samples of African Americans residing in the Houston, Texas area. This is the first scholarly study of purple drank use outside of the Houston, Texas area among a general population of young adults, and indicates that purple drank use is not limited to African American males. The findings depict higher odds of the use of purple drank among other racial and ethnic groups, males, and homosexual, bisexual, and transgender college students from urban areas.     

Allergic urticarial rash from oral codeine

A case of an urticarial rash from delayed-type allergy to orally administered codeine is presented. The literature on contact allergy to codeine is reviewed, and the rôle of patch testing in drug eruptions discussed.