caffeine, an adenosine a1, a2a, and a2b receptor antagonist, is frequently used as an adjuvant analgesic in combination with non steroidal anti-inflammatory drugs or opioids. the aim of this study was to evaluate the effects of caffeine on preventing the development of morphine tolerance and analgesia in mice. in this study, different groups of mice received morphine (30 mg/kg) + saline (10 ml/...

In view of the potent analgesia exhibited by the apparent structurally dissimilar morphine-6-O-glucuronide (M6G) and morphine-6-O-sulfate (M6S) conjugates of morphine, we have examined the effect of structural modification of M6S on analgesic activity, using the tail-flick test. Changes in the M6S structure were made that would affect the lipophilicity and polarity of the molecule. Subcutaneous...

The chemical stability of an intrathecally administered analgesic combination may influence the frequency of pump refills necessary to maintain safe and effective analgesia. Previous work has shown that the stability of ziconotide at body temperature is reduced substantially by the presence of morphine sulfate 35 mg/mL. The current study was performed to evaluate the chemical stability of admix...

Mu-opioids (i.e. morphine, oxycodone, hydrocodone) are considered to be the primary drugs for treatment of moderate to severe acute, chronic and cancer pain. Despite their analgesic effectiveness they have several clinically significant side-effects (cognitive, motor, respiratory, cardiovascular, gastrointestinal). They also have a limited spectrum of action, being more effective for nociceptiv...

A series of 3-O-acyl-6-O-sulfate esters of morphine, dihydromorphine, N-methylmorphinium iodide, codeine, and dihydrocodeine were prepared and evaluated for their ability to bind to mu-, delta-, kappa(1)-, kappa(2)-, and kappa(3)-opiate receptors. Several compounds exhibited good affinity for the mu-opiate receptor. Morphine-3-O-propionyl-6-O-sulfate had four times greater affinity than morphin...

Morphine is still the mainstay in treatment of severe pain and is metabolized in the liver mainly by glucuronidation, partly to the pharmacologically active morphine-6-glucuronide (M6G). The sulfation pathway has attracted much less attention but may also form active metabolites. The aim of the present study was to study two sulfate metabolites of morphine in humans. Urine and plasma from newbo...

OBJECTIVE A review of the English language literature was performed to determine the sensitivity and specificity of morphine sulfate-augmented hepatobiliary imaging for acute cholecystitis. Twenty publications, involving 914 patients, were reviewed from journals published between 1984 and 1999. The analysis of these patients has resulted in the largest combined review study to date. The sensiti...

BACKGROUND Patterns of therapy switching in patients receiving long-acting opioids have not been well documented. OBJECTIVE To compare therapy switching among patients beginning treatment with controlled-release (CR) oxycodone, transdermal fentanyl, or CR morphine sulfate. METHODS Using a US healthcare claims database, we identified patients beginning treatment with CR oxycodone, transderma...

objective(s):this study was carried out to evaluate the effect of maternal morphine exposure during gestational and lactation period on pyramidal neurons of hippocampus in 18 and 32 day mice offspring. materials and methods: thirty female mice were randomly allocated into cases and controls. in case group, animals received morphinesulfate 10 mg/kg.body weight intraperitoneally during 7 days bef...