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Anesthesia and analgesia and the curse of Eve
Published in Michael J. O’Dowd, The History of Medications for Women, 2020
Encouraging reports by Gilbert and Dixon (1943 p. 320) and others soon appeared in the American literature and in England Cripps et al. (1944 p. 498) and Barnes (1947 p. 437) published similar results. The maternal and fetal respiratory depressant side-effects of pethidine could be counteracted by levallorphan tartrate (Lorphan), a drug synthesized by Schneider and Hellerbach in 1950. Levallorphan 1.25 mg was combined with pethidine 100 mg and marketed as pethilorphan. Although popular for a while, petMorphan had reduced analgesic potency and could actually increase respiratory depression.
Classes of Drugs Needed for the Successful Management of Addictions
Published in Frank Lynn Iber, Alcohol and Drug Abuse as Encountered in Office Practice, 2020
Used intravenously, the opiate antagonists promptly reverse respiratory depression caused by opioid drugs, even in neonates, and reverse many of the other effects of overdose of opiates and many related compounds. Although there are many subtypes of opiate receptors (see Chapter 2), naloxone interferes with the receptors in the respiratory center as well as all other types and in this fashion removes nearly all opioid effects and may precipitate withdrawal. Naloxone has no agonist activity, whereas levallorphan has some. The agonist effects of naloxone are much less than levallorphan, making the former the drug of choice.
Historical Notes
Published in Albert A. Kurland, S. Joseph Mulé, Psychiatric Aspects of Opiate Dependence, 2019
Albert A. Kurland, S. Joseph Mulé
As the studies with cyclazocine were in progress, N-allylnoroxymorphone (naloxone), a pure antagonist was synthesized that had none of the disadvantages associated with cyclazocine. The theoretical background on which this synthesis had been based was the knowledge that the substitution of the methyl group of the basic nitrogen of narcotic analgesics with an allyl group may produce compounds capable of antagonizing the respiratory and other pharmacological effects of narcotics. Thus, the narcotic antagonists, N-allylnormorphine (nalorphine) and 1-3hydroxy-N-allylmorphinan (levallorphan) were developed as N-allyl derivatives of morphine and Levorphan,® respectively. N-allyl-14-hydroxy dihydronormorphinone (naloxone) hydrochloride, was structurally related to the potent narcotic analgesic Num orphan® (oxymorphone) and was also synthesized on this theoretical basis.
Synthesis and in‐vivo taste assessment of meloxicam pivalate
Published in Drug Development and Industrial Pharmacy, 2019
Bandoo C. Chatale, Mariam S. Degani
Previous research revealed that bitter compounds possess several variations of structural aspects, responsible for bitterness, so it is difficult to simplify the molecular requirements; however, it is reported that polar amino group and hydroxyl group are often responsible for bitter taste of drugs [22–24]. Blocking of bitter functionality through structural chemical modification has been proven to decrease bitterness significantly. Bitter drugs like nalbuphine, naloxone, naltrexone, oxymorphone, butorphanol, and levallorphan, have been esterified at phenolic hydroxyl group, thereby reducing their bitterness [25].