Ronald R. Tuttle - Plantation FL Ross Dixon - Boca Raton FL Maciej M. Smulkowski - Gainesville FL
Assignee:
Ivax Laboratories, Inc. - Miami FL
International Classification:
A61K 3170 C07H 1524
US Classification:
514 27
Abstract:
Intestine-specific delivery of an opioid antagonist can be accomplished without substantial central nervous system effects by administering the antagonist orally in the form of the glucuronide derivative.
Provided is a method of orally treating a child having a tendency to be overactive to the extent of requiring an external control which comprises orally administering to said child a pharmaceutically effective amount of 6-methylene-6-desoxy-N-cyclopropylmethyl-14-hydroxydihydronormorphone to said patient, whereby the patient tends to reduce his food intake.
A method of orally treating a child having a tendency to be overactive to the extent of requiring an external control which comprises orally administering to said child a pharmaceutically effective amount of (-)-17-(cyclopropylmethyl)-4,5-alpha-epoxy-3,14-dihydroxymorpinan-6-one to said patient, whereby the attention span of the child lengthened. An oral sustained release dosage unit containing (-)-17-(cyclopropylmethyl)-4,5-alpha-epoxy-3,14-dihydroxymorpinan-6-one is disclosed also.
A method for increasing cardiac contractility in a warm-blooded animal suffering from acutely depressed cardiac contractility which comprises administering to said animal an effective amount of a compound of the formula ##STR1## wherein R is hydrogen or isobutyrate, or a pharmaceutically acceptable acid addition salt thereof.
Cardiac contractility agents are provided which are 3,4-di-isobutyryloxy-N-�3-(4-isobutyryloxyphenyl)-1-methyl-n-propyl!-beta- phenethylamine, preferably orally deliverable forms which are cyclodextrin complexes.
A method is provided for orally treating a patient suffering from senile dementia which comprises the periodic oral delivery of a pharmaceutically effective amount of 6-methylene-6-desoxy-N-cyclopropylmethyl-14-hydroxydihydronormorphone to said patient, whereby the patient tends to reduce his food intake. Also provided is an oral sustained release dosage unit form suitable for treating a patient suffering from obesity which permits a prolonged interval between administration to said patient, said oral dosage unit formulation comprising a plurality of granules which together constitute a pharmaceutically effective amount of 6-methylene-6-desoxy-N-cyclopropylmethyl-14-hydroxydihydronormorphone to provide a sustained action over said prolonged interval, said plurality of granules each comprising a polymeric matrix to permit a substantially even release of said 6-methylene-6-desoxy-N-cyclopropylmethyl-14-hydroxydihydronormorphone to permit the necessary sustained release over the prolonged period of time.
Cardiac contractility agents are provided which are 3,4-dihydroxy-N-[3-(4-hydroxyphenyl)-1-methyl-n-propyl]-beta-phenethylamin e cyclodextrin complexes.