Pharmacokinetics of moxisylyte in healthy volunteers after intracavernous injection of increasing doses

Bressolle, Françoise; Costa, P.; Rouzier-Panis, Régine; Marquer, C.

doi:10.1007/bf00203788

Cited by 7 publications

(5 citation statements)

References 12 publications

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“…9,28 Moxisylyte is a pro-drug that is immediately converted to ®ve metabolites, four of which exhibit biological activities. 28 …”

Section: Moxisylyte (Thymoxamine)mentioning

confidence: 99%

Current perspectives on intracavernosal pharmacotherapy for erectile dysfunction

Porst¹

2000

Int J Impot Res

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Thirty percent of males af¯icted with erectile dysfunction (ED) do not respond to oral drugs, another 15% reveal contraindications to currently available therapy, and a subset of patients actually prefer injection therapy due to its predictable short time-to-onset of erection and reliable rigidity compared to oral drugs. This paper provides both a historical and current perspective on intracavernosal therapy and reviews the popular injectable therapeutic agents that are currently used for the treatment of ED. Emphasis is placed on the ef®cacy, mechanism of action and side effect pro®les of approved and experimental injectable pharmacotherapy for ED.

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“…9,28 Moxisylyte is a pro-drug that is immediately converted to ®ve metabolites, four of which exhibit biological activities. 28 …”

Section: Moxisylyte (Thymoxamine)mentioning

confidence: 99%

Current perspectives on intracavernosal pharmacotherapy for erectile dysfunction

Porst¹

2000

Int J Impot Res

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“…tions of the conjugates were shown to increase nonlinearly with the dose after oral administration; DAM-S reached saturation between 120 and 240 mg and MDAM-S between 240 and 480 mg, whereas DAM-G increased more than proportionally 1251. However, after intracavernous administration, except for DAM-G between 10 and 30 mg, the AUC of the four metabolites increased linearly with the dose [4]. N o modification of the metabolism of moxisylyte occurs in repeated-dose regimens.…”

Section: Metabolismmentioning

confidence: 93%

“…When moxisylyte was injected in the corpus cavernosum, DAM increased rapidly in the systemic circulation to reach a peak at 10 min, at C,,, values lower than after intravenous injection [4,7, 8, 10, 151. However, based on C,,, and T,,, values, its pharmacokinetics was linear between 10 and 30 mg [4]. In the two reported comparative studies [ 10, 151, the difference between the mean intravenous and intracavernous MRT values was about 15 to 20 min.…”

Section: Zntracavernous Injectionmentioning

confidence: 93%

“…The general tolerance was also excellent; whatever the dose, no significant decrease in arterial pressure was reported in the above-mentioned efficacy studies. However, two cases of asymptomatic hypotension occurred in two healthy volunteers (one at 10 mg, the other at 20 mg) taking part in a dose-increasing pharmacokinetic study [4]. On each occasion, the values returned to normal after 1 h.…”

Section: Tolerabilitymentioning

confidence: 98%

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Moxisylyte: A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in impotence

Marquer¹,

Bressolle

1998

Fundamemntal Clinical Pharma

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Moxisylyte is a competitive noradrenaline antagonist, acting preferentially on post-synaptic alpha-1 adrenoceptors. It was introduced more than thirty years ago for the treatment of cerebro-vascular disorders and shown more recently effective in the urological field due to its ability to modulate the urethral pressure. Renewal of interest in this drug has been observed in recent years since the demonstration of the possibilities of vasoactive drugs in evaluation and treatment of erectile dysfunctions. Moxisylyte is a prodrug, rapidly transformed into an active metabolite in plasma (Deacetylmoxisylyte or DAM). Elimination of the active metabolite occurs by N-demethylation, sulpho- and glucuroconjugation. The N-demethylated metabolite is sulphoconjugated only. Urine is the main route of excretion. The metabolites of moxisylyte can be determined in biological fluids by various methods using high-performance liquid chromatography. Their pharmacokinetics is dependent on the route of administration. By the oral route, the concentrations of the active metabolite are low, and the glucuroconide of DAM predominates over the sulphates. After intravenous and intracavernous injection, the active metabolite is proportionally higher, the two sulphates are equivalent and in larger amounts than the glucuronide. In the treatment of impotence, intracavernous injection of moxisylyte at 10, 20 or 30 mg can induce an erection adequate for intercourse in most of the patients. Compared to inducing agents such as papaverine and prostaglandin E1, moxisylyte must be considered as a facilitator of male erection, its interest lying in the low rate of adverse effects, either general or local.

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“…Η μοξισυλάτη είναι ένας εκλεκτικός αναστολέας των αι-αδρενεργικών υποδοχέων, με πιθανή αντιισταμινική δράση. Η μοξισυλάτη είναι ένα προφάρμακο που μετατρέπεται αμέσως σε πέντε μεταβολίτες, εκ των οποίων οι τέσσερις έχουν βιολογική δράση [786]. Οι αρχικές μελέτες έδειξαν ότι η ενδοσηραγγώδης χορήγηση του φαρμάκου (10-30mg) διευκολύνει τη στύση προκαλώντας κυρίως διόγκωση σε ποσοστό έως και 70% [7871.…”

Section: μοξισυλάτη (θυμοξαμίνη)unclassified

Παθοφυσιολογία Του Μηχανισμού Της Στύσης

Χατζημουρατίδης¹

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αναστόμωσης της κάτω επιγαστρίου ή μηριαίας αρτηρίας με τη ραχιαία ή τη σηραγγώδη αρτηρία του πέους........ 166 11.2.2.3 Επεμβάσεις αναστόμωσης της κάτω επιγαστρίου αρτηρίας με την εν τω βάθει ραχιαία φλέβα του πέους_________ ______ ...166 11.2.2.4 Αποτελέσματα των επεμβάσεων στους περιφερικούς αρτη ριακούς κλάδους.

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Pharmacokinetics of moxisylyte in healthy volunteers after intracavernous injection of increasing doses

Abstract: The pharmacokinetics of moxisylyte in humans following intracavernous administration were linear in the dose range 10 to 30 mg.

Cited by 7 publications

References 12 publications

Current perspectives on intracavernosal pharmacotherapy for erectile dysfunction

Current perspectives on intracavernosal pharmacotherapy for erectile dysfunction

Moxisylyte: A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in impotence

Παθοφυσιολογία Του Μηχανισμού Της Στύσης

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