Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-10-16
1994-08-09
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 31505
Patent
active
053366786
DESCRIPTION:
BRIEF SUMMARY
The present invention concerns the use of minoxidil for the preparation of a medicament useful for the treatment of erectile impotence.
The treatment of most erectile impotences presently relies on the injection in corpora cavernosa of drugs which, directly acting on the arterial smooth muscles and on cavernous muscles, cause the relaxation thereof, allowing and/or making the hematic repletion and therefore erection, easier.
The drug-induced erection by means of intracavernous injection allow (in cases selected by the papaverine test) a normal sexual intercourse immediately after the injection whereas the normal erections are improved by periodical injections.
Papaverine by the intracavernous route has therefore found wide clinical applications, with a substantial improvement in the therapy of erectile impotence.
Several clinical and experimental research efforts have been paid to the search of new drugs having the same effectiveness of papaverine but lower risks and drawbacks.
It has been recently shown that the erection first induced by the relaxation of corpora cavernosa muscle tissue and of the penis arterial system (Ann. Urol. 19, 327, 1985 e 22, 49, 1988). Myorelaxant or alpha-blocker drugs are therefore potentially useful as erection inducers (Lancet 2, 938, 1982; Br. J. Psychometr. 143, 332, 1983; Br. J. Psych. 149, 210, 1986).
The drugs up-to-now studied belong to three different classes, according to the administration route:
1) orally active drugs: yohimbine
2) drugs active by intracavernous injection: papaverine, phentolamine, PGE.sub.1 etc.
3) Topical drugs: nitroglycerine.
The drugs for local use ( intracavernous and topical) share, as a mechanism of action, the relaxing of smooth muscle fibers and of the arterio-arteriolar system of the penis, causing therefore the first and fundamental event of the erection, as shown by recent studies on the physiology of the erection.
However, none of the presently available drugs is completely satisfactory: for instance, yohimbine is not active against organic impotence whereas the intracavernous administration of drugs such as papaverine, phentolamine, PGE.sub.1 has a low compliance because of pain and psychological problems, sometimes even impairing the drug-induced erection. This route involves also substantial risks of priapism and sclerosis of corpora cavernosa after long-term treatment. Finally, topically applied nitroglycerine has been found to induce cephalalgia, hypotension and burning on the application site, typical side-effects of organic nitrates.
It has now been found that topically applied minoxidil is able to make erection easier, side-effects and problems connected with the use of the previously known drugs.
Minoxidil is a vasodilator agent mainly acting on the arterial wall. Its use as antihypertensive is well-established and, more recently, topical applications of minoxidil have been found to be useful for the treatment of androgenetic alopecia Minoxidil, when topically applied, is poorly absorbed from healthy cutis, an average of only 1.4% (range: 0.3-4.5%) of the administered dose being found in the systemic circulation. Thus, the application of 1 ml of 2% Minoxidil solution, corresponding to 20 mg of drug, gives absorption of 0.28 mg (Rep. Farm. H., 1990), very far from the recommended maximum daily antihypertensive dose (100 mg).
A double-blind controlled study has been carried cut on 42 patients effected by impotence of different origin, diagnosed by a complete clinical, psychological and instrumental evaluation. The patients affected by uncontrolled diabetes, prepuce sclerosis, La Peyronie disease, recent myocardial infarction, orthostatic hypotension or treated with organic nitrates and minoxidil in the 4 months before the study were not tested.
The etiology is shown in Table 1.
Each patient was given on 3 different days: 2.5 g of 2% nitrogylcerine ointment (Nitrocor.RTM.); 1 ml of 2% minoxidil; 2.5 g of urethral lubrificant as placebo (K-J.RTM.).
The patients were randomized in three groups of 14, each receiving both nitroglycer
REFERENCES:
patent: 4596812 (1986-06-01), Chidsey et al.
patent: 4801587 (1989-01-01), Voss et al.
British Journal of Uroiogy, 1988, 62(J) p. 466 (Watters et al.) "Effect on Pharmacological Agents of Erectile Responses in the Dog".
Cintins Marianne M.
Jarvis William R. A.
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