摘要:
Sexual dysfunction in human females can be ameliorated, without substantial undesirable side effects, by sublingual administration of apomorphine dosage forms. Administration of apomorphine increases nerve stimulated clitoral intracavernosal blood flow and vaginal wall blood flow for enhanced clitoral erection and vaginal engorgement in a female. A plasma concentration of apomorphine of no more than about 5.5 nanograms per milliliter is preferably maintained.
摘要:
The treatment of sexual dysfunction in human patients by an oral therapy regimen of administration of apomorphine and sildenafil is disclosed. This treatment optimizes the efficacy of each drug and substantially minimizes the undesirable side effects associated individually therewith. Apomorphine and sildenafil can be co-administered with a combination dosage unit or administered sequentially in separate dosage units, substantially prior to sexual activity. Other erectogenic agents can be administered along with apomorphine and sildenafil.
摘要:
A process for the synthesis of arylpiperidine carbinol intermediates and derivatives is disclosed. A preferred process embodiment provides the synthesis of intermediate compounds of structural formula (I) and structural formula (II), where X is halogen, C1-C10 alkyl, C1-C10 alkoxy, C1-C10 haloalkyl, hydroxy, or hydrogen; and R2 and R3 each is C1-C4 alkyl and R2 and R3 are the same. The compound of structural formula (I) is made by condensing a corresponding cinnamonitrile with a corresponding diester malonate. The compound of structural formula (II) in the (±)-trans configuration is obtained by hydrogenating the compound of structural formula (I). The compounds of structural formula (I) and structural formula (II) are useful chemical intermediates for synthesizing 4-arylpiperidine-3-carbinols and their derivatives in (-)-trans configuration.
摘要:
Symptoms of Parkinson's disease and psychogenic male erectile dysfunction (MED) can be ameliorated through the use of apomorphine. The adverse side effects of apomorphine administration, such as nausea, vomiting, yawning, and cardiovascular effects, can be significantly reduced by a dose escalating method of acclimatization. An initial dose of apomorphine is administered to the patient, and subsequently increased over a period of time until a final apomorphine dose in excess of a desired therapeutic dose has been received by the patient. Thereafter a therapeutic dose of apomorphine, less than the final apomorphine dose, is administered to the patient with attendant reduced side effects.
摘要:
A free-flowing, amorphous paroxetine hydrochloride-ethanol composition suitable as a therapeutic agent for premature ejaculation can be prepared by dissolving paroxetine free base in a hydrochloric acid-ethanol solution followed by drying. In a preferred embodiment, the amount of ethanol present in the amorphous product is in the range of 1 to 4 weight percent based on paroxetine hydrochloride. The amorphous product is stable and substantially non-hygroscopic.
摘要:
A free-flowing, amorphous paroxetine hydrochloride composition suitable as a therapeutic agent for premature ejaculation can be prepared by dissolving paroxetine free base in a hydrochloric acid-ethanol solution followed by drying. The present compositions comprise amorphous paroxetine hydrochloride and at least one hydroxyl-bearing compound. In one preferred embodiment, the hydroxyl-bearing compound is ethanol and the amount of ethanol present in the amorphous product is in the range of 1 to 4 weight percent based on paroxetine hydrochloride. The amorphous product is stable and substantially non-hygroscopic.