Morphine suppositories

Takatori T, Yamamoto K, Yamaguchi T, Higaki K, Kimura T. Design of controlled -release morphine suppositories containing polyglycerol ester of fatty acid. Biol Pharm Bull 2005 28(8) 1480-1484. 

Rectal Administration. The administration of drugs by a solid rectal dosage form (i.e., suppositories) results in a wide variability in the rate and extent of absorption in children [79]. This fact, coupled with the inflexibility of a fixed dose, makes this a route that should not be promoted for pediatric patients. At least one death involving a 7-month-old infant can be directly attributed to the use of solid rectal dosage form of a therapeutic dose of morphine [80]. 

Show how you would prepare 15 morphine hydrochloride suppositories containing 25 mg of the drug in each suppository. Assume that you are required to use cocoa butter base. 

Opium Street Names Auntie Emma, big O. black stuff, block, gum, hop, ope, tar (brand generic called tincture of opium, laudanum, paregoric (CIII), B O suppositories [CIII]) Use Some medical uses (antidiarrheal, antitussive, antispas-modic) illegally used to produce morphine and h oin can be swallowed or smoked Actions Narcotic contains morphine Effects Pain relief, euphoria, drowsiness/N, constipation, confusion, sedation, resp dqjression and arrest, tol -ance, addiction, unconsciousness, coma, death... 

Dosages and routes of administration Morphine is available in different salt forms but the hydrochloride and sulfate (Vermeire and Remon, 1999) are used preferentially. The compound can be administered by the oral, parenteral or intraspinal route. Oral application is preferred for chronic pain treatment and various slow release forms have been developed to reduce the administration frequency to 2-3 times per day (Bourke et al., 2000). Parenteral morphine is used in intravenous or intramuscular doses of 10 mg, mostly for postoperative pain and self-administration devices are available for patient-controlled analgesia (PCA). Morphine is additionally used for intraspinal (epidural or intrathecal) administration. Morphine is absorbed reasonably well in the lower gastrointestinal tract and can be given as suppositories. 

FIGURE 8.3 Bioavailability of morphine after rectal administrations of Witepsol H-15 hollow-type suppositories containing morphine hydrochloride (MH) and CyDs in rabbits. Each value represents the mean SE of three rabbits. p < 0.05, compared with MH alone. 

Kondo, T., T. Irie, and K. Uekama. 1996. Combination effects of a-cyclodextrin and xanthan gum on rectal absorption and metabolism of morphine from hollow-type suppositories in rabbits. Biol Pharm Bull 19 280. 

Uekama, K., et al. 1995. Modification of rectal absorption of morphine from hollow-type suppositories with a combination of a-cyclodextrin and viscosity-enhancing polysaccharide. 

Morgan, D.J., et al. 1992. Prolonged release of morphine alkaloid from a lipophilic suppository base in vitro and in vivo. Int J Clin Pharmacol Ther Toxicol 30 576. 

Dihydromorphinone is used in the same manner as morphine for the relief of pain but in much smaller doses — usually 1 to 2 mg. For cough, a dose about half that size is used. Administered orally, dihydromorphinone, is more effective than morphine, and it may also be administered in a rectal suppository. It is principally indicated for acute pain of short duration. 

Oxymorphone (Numorphan ), dihydromorphinone hydrochloride, is also about ten times as active as morphine and has a rapid onset of action that lasts for about 6 h. It is administered subcutaneously or intramuscularly in doses of 1 ml (1.5 mg) or as a rectal suppository (2 and 5 mg). 

Morphine is available by prescription in many forms. It can be taken orally as a liquid or as pills, and by injection under the skin, into the veins, or into the space surrounding the spinal cord. Rectal suppositories for pain control provide longer-lasting relief with less potential for nausea. As an abused drug, morphine can be smoked and sniffed as well as swallowed. 

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