      Document 0109
 DOCN  DRG0109
 UNIQUE IDENTIFIER        DRG-0138
 NAME OF SUBSTANCE        Dronabinol [USAN 1996]
 REGISTRY NUMBER          1972-08-3
 STANDARD CHEMICAL NAME   6H-Dibenzo(b,d)pyran-1-ol,6a,7,8,10a
                          -tetrahydro-6,6,9-trimethyl-3-pentyl-,
                          (6aR-trans)- [USAN 1996]
 SYNONYMS                 Marinol [USAN 1996]
 SYNONYMS                 delta-9-Tetrahydrocannabinol [PDR 1995]
 SYNONYMS                 delta-9-THC [PDR 1995]
 SYNONYMS                 Deltanyne [USAN 1990]
 PROTOCOL ID NUMBERS      NIAID DATRI 004
 SECONDARY SOURCE ID      NSC-134454 [USAN 1996]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Cannabinoid receptors in
                          neural tissues may mediate the effects of
                          dronabinol. Forms numerous metabolites,
                          including 11-hydroxy-tetrahydrocannabinol,
                          which is psychoactive and is the principal
                          active metabolite. Maximum plasma
                          concentration of dronabinol and several
                          metabolites occurs approximately 2-3 hours
                          after oral dosing. Biliary excretion is the
                          major route of elimination. The elimination
                          phase exhibits biphasic kinetics with an
                          alpha half-life of about 4 hours and a
                          terminal half-life of 25-36 hours. The
                          terminal plasma half-life for the principal
                          active metabolite is approximately 15-18
                          hours. [PDR 1995]
 DISEASES STUDIED/TREATED FDA approved 12/23/92 for appetite
                          stimulation and the prevention of weight loss
                          in HIV-infected patients [AmFAR Tx Dir
                          1995;7(4)] [USP DI 1995]
 CLASSIFICATION CODE      Appetite stimulant [AmFAR Tx Dir 1995;7(4)]
 CLASSIFICATION CODE      Antiemetic [USAN 1996]
 OTHER MAJOR USES         Nausea and vomiting associated with cancer
                          chemotherapy [PDR 1995]
 SUBSTANCE INTERACTIONS   May interact with barbiturates, disulfiram,
                          theophylline, sympathomimetics and hypnotics
                          and sedatives. May delay absorption of
                          alcohol. [Drug Interactions and Side Effects
                          Index 1992] [PDR 1995]
 ADVERSE EFFECTS          The most frequently reported adverse
                          reactions involved the central nervous
                          system. In decreasing order of frequency
                          these events were drowsiness, dizziness,
                          muddled thinking and brief impairment of
                          coordination, sensory and perceptual
                          functions. Easy laughing, elation and
                          heightened awareness, often termed a high,
                          was observed in 24% of patients. [PDR 1995]
 CONTRAINDICATIONS        Contraindicated in pregnant and nursing
                          women, in patients whose nausea and vomiting
                          arise from any cause other than cancer
                          chemotherapy, and in patients with known
                          hypersensitivity to either dronabinol or
                          sesame oil. Should be used with caution in
                          patients with hypertension or heart disease;
                          in manic, depressive, or schizophrenic
                          patients; and in patients receiving other
                          psychoactive drugs. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Synthetically manufactured
                          version of the active substance in marijuana,
                          delta-9-tetrahydrocannabinol [AmFAR Tx Dir
                          1995;7(4)]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Light yellow resinous
                          oil [PDR 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C21H30O2 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 314.47 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Insoluble in water, formulated in
                          sesame oil [PDR 1995]
 CHEMICAL/PHYSICAL DATA   PHYSICAL COMMENT: pKa 10.6 [USP DI 1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: 2.5, 5, and 10 mg soft gelatin
                          capsules. [PDR 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral. [PDR 1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Store between 8 and 15 C (46 and 59
                          F). Protect from freezing. [PDR 1995]
 MANUFACTURERS            Roxane Laboratories, Incorporated
 REFERENCES               Beal JE, Olson R, Laubenstein L, Morales JO,
                          Bellman P, Yangco B, Lefkowitz L, Plasse TF,
                          Shepard KV. Dronabinol as a treatment for
                          anorexia associated with weight loss in
                          patients with AIDS. J Pain Symptom Manage.
                          1995 Feb;10(2):89-97.
 REFERENCES               Beal J, Flynn N. AIDS-associated anorexia. J
                          Physicians Assoca AIDS Care. 1995
                          Jan;2(1):19-22.
 REFERENCES               Cat LK, Coleman RL. Treatment for HIV wasting
                          syndrom. Ann Pharmacother. 1994
                          May;28(5):595-597.
 REFERENCES               Struwe M, Kaempfer SH, Geiger CJ, Pavia AT,
                          Plasse TF, Shepard KV, Ries K, Evans TG.
                          Effect of dronabinol on nutritional status in
                          HIV infection. Ann Pharmacother. 1993
                          Jul-Aug;27(7-8):827-831.
 REFERENCES               Struwe M, Kaempfer SH, Pavia AT, Geiger CJ,
                          Shepard KV, Plasse TF, Evans T. Randomized
                          study of dronabinol in HIV related weight
                          loss. Int Conf AIDS. 1992 Jul 19-24;8(3):137
                          (abstract no. PuB 7531).
 REFERENCES               Plasse T, Conant M, Gorter R, Shepard KV.
                          Dronabinol stimulates appetite and causes
                          weight gain in HIV patients. Int Conf AIDS.
                          1992 Jul 19-24;8(3):122 (abstract nol PuB
                          7442).
 REFERENCES               Flynn J, Hanif N. Nabilone for the management
                          of intractable nausea and vomiting in
                          terminally staged AIDS. J Palliat Care. 1992
                          Summer;8(2):46-7.
 REFERENCES               Plasse TF, Gorter RW, Krasnow SH, Lane M,
                          Shepard KV, Wadleigh RG. Recent clinical
                          experience with dronabinol. Pharmacol Biochem
                          Behav. 1991 nov;40(3):695-700.
 ENTRY MONTH              9203
 LAST REVISION DATE       960111
 

SOURCE: National Library of Medicine, Bethesda, MD.  Distributed by AEGIS.
