Use of guaifenesin in the treatment of urologic disorders
Publication number EP0271127 A2
Publication type Application
Application number EP19870202148
Publication date Jun 15, 1988
Filing date Nov 5, 1987
Priority date Nov 7, 1986
Also published as DE3785555D1, DE3785555T2, EP0271127A3, EP0271127B1, US4822610
Inventors Irving M. Bush
Applicant Irving M. Bush
Export Citation BiBTeX, EndNote, RefMan
Patent Citations (2), Non-Patent Citations (2), Referenced by (2), Classifications (6), Legal Events (22)
External Links: Espacenet, EP Register
Use of guaifenesin in the treatment of urologic disorders
EP 0271127 A2
ABSTRACT
A novel method for the treatment of prostatitis, seminal vesiculitis, benign prostatic hypertrophy, prostatic abscess, bladder neck hypertrophy, urinary tract infection including urethritis and decreased liquification of semen by administering a
pharmaceutically acceptable dosage of guaifenesin, or guaifenesin including zinc sulfate.
CLAIMS(7)
1. A method for the treatment of the urologic conditions selected from the group consisting of prostatitis, seminal vesiculitis, benign prostatic hypertrophy, prostatic abscess, bladder neck hypertrophy, urinary tract infection including urethritis and
decreased liquification of semen, which comprises administering orally to the patient in need of such treatment a pharmaceutically acceptable dosage of guaifenesin.
2. A method for the treatment of the urologic conditions selected from the group consisting of prostatitis, seminal vesiculitis, benign prostatic hypertrophy, prostatic abscess, bladder neck hypertrophy, urinary tract infection including urethritis and
decreased liquification of semen, which comprises administering orally to the patient in need of such treatment a pharmaceutically acceptable dosage of guaifenesin, wherein the active agent is administered in a dosage of 50-1200mg once per day for 3 days,
then twice a day for one week, and then 150-200mg a day in divided dosages. 3. A method according to claim 1 wherein the dosage incorporates 5-30mg of pharmaceutically acceptable zinc sulfate.
4. The method according to claim 2 wherein the dosage incorporates 5-30mg of pharmaceutically acceptable zinc sulfate.
5. A pharmaceutical composition useful for treating the urological conditions selected from the group known as prostatitis, seminal vesiculitis, benign prostatic hypertrophy, prostatic abscess, bladder neck hypertrophy, urinary tract infection including
urethritis and decreased liquification of semen, which comprises a pharmaceutically acceptable oral dosage of guaifenesin and zinc sulfate.
6. A method according to claim 1 wherein the active agent is administered in a dosage not exceeding 50mg per day in patients who have a relatively low tolerance to said agent.
7. A method according to claim 2 wherein said active agent is administered for 2 weeks in acute problems, up to 3 months in recurring problems, and up to one year in chronic problems.
DESCRIPTION
BACKGROUND OF THE INVENTION
[0001]
This application is a continuation-in-part of my copending U.S. patent application Serial No. 06/928,313, filed November 7, 1986.
[0002]
The present invention relates to a novel method for the treatment of the urologic conditions known as prostatitis (P), seminal vesiculitis (SV), benign prostatic hypertrophy (BPH), prostatic abscess (PA), bladder neck hypertrophy (BNH), urinary tract
infection (UTI) including urethritis and decreased liquification of semen (DLS).
[0003]
These diseases of the urinary and genital tract of males and females are among the most common diseases (8%) seen in medical practice. They are often recurring, debilitating or persistent and take a great toll in patient morbidity. Many of the symptoms
associated with P, SV, BPH, PA, BNH, UTI and DLS are related to the inability of associated organs to drain their mucoid or mucopurulent secretions which may or may not contain bacteria that are often resistent to many antibiotics. This inability to
drain has been solved at the present time only through painful massage by the treating physician.
[0004]
Guaifenesin C₁₀H₁₄O₄ 1,2 - Propanediol, 3 (2 methoxyphenoxy)-3-(o-Methoxyphenoxy)-1,2-propanediol has in the past and at present been used as an expectorant. By increasing respiratory tract fluid (mucus) guaifenesin reportedly reduces the
viscosity of tenacious secretions leading to removal of the offending materia. Guaifenesin may also reduce respiratory tract adhesiveness and surface tension promoting ciliary action. It therefore has been used in the management of coughs associated with
the common cold, bronchitis, laryngitis, pharyngitis, pertussis, influenza, measles and chronic paranasal sinusitis, all of which are diseases of the upper respiratory tract.
[0005]
Mucolytic cough medications such as Robitussin (active ingredient guaifenesin) have been used to liquify cervical secretions in infertility problems on and off for many years. In 1980 we utilized Robitussin to liquify viscid semen in infertility problems,
but some of the patients complained about the effect of the alcohol. In early 1983 a patient with a chronic prostatic abscess was given guaifenesin by capsule (without alcohol) to encourage drainage of the thick purulent material normally expressed by
vigorous prostatic massage once a week. Two phenomena occurred over the next 4 months. The secretions became slightly thinner and massage needed to be performed only once a month, as his prostate seemed distinctly smaller by rectal examination. In
addition, there was no alcohol effect on the prostate.
[0006]
This led to a prospective study of 158 patients with male infertility, prostatitis, seminal vesiculitis, prostatic abscess, benign prostatic hypertrophy and urinary tract infection. The men were given 400 to 600mg of guaifenesin for 2 to 14 months.
Results included a decrease in: (a) semen viscosity; (b) white blood cell count, pH, bacterial content of ejaculated semen, an increase in semen zinc content and semen antibacterial factors as tested against known bacterial strains and (c) sperm mobility.
Two unexpected findings were: 1. The reduction, in some patients, of their sperm counts; and 2. A decrease in prostatic size in selected long-term patients as measured by rectal exam, voiding studies, residual bladder urine and bladder and prostatic
ultrasound. Side effects in these patients included rash, chronic cough, initial increased dysuria, constipation, sleeplessness and gastric upset. Further studies indicate that certain of these patients could tolerate the drug at 50 milligrams per day
with similar results over a longer period of treatment.
[0007]
The effect of concurrent zinc therapy (5-30mg of zinc sulfate per day) in a significant number of these patients was beneficial.
SUMMARY OF THE INVENTION
[0008]
In accordance with the present invention, it has now surprisingly been found that guaifenesin with and without zinc is of use for the treatment of prostatitis (P), seminal vesiculitis (SV), benign prostatic hypertrophy (BPH), prostatic abscess (PA),
bladder neck hypertrophy (BNH), urinary tract infection (UTI) including urethritis, and decreased liquification of semen (DLS). This use in the treatment of P, SV, BPH, PA, BNH, UTI and DLS has not been previously suggested and has not been reported. The
object of the treatment is to encourage the drainage of the byproducts of infections and inflammations of the associated organ glands by increasing prostate, seminal vesicle, bladder neck, and urethral fluid secretion, and to reduce surface tension and
adhesiveness of the mucosal lining of the prostate, seminal vesicle, bladder neck and urethra in males, and bladder neck and urethra in females. Testing of 30 patients with other mucolytic agents, including iodonated products, has not been effective.
DETAILED DESCRIPTION OF PREFERRED EMBODIMENT
[0009]
Guaifenesin occurs as a white to slightly grey crystalline powder, having a bitter taste. Guaifenesin may have a slight characteristic odor. The powder tends to become lumpy on storage. It is soluble in alcohol and in water. It is also known as glyceryl
guaiacolate or a-Glyceryl Guaracol Ether and is not a natural product, being manufactured by a chemical process. Its formula is Guaifenesin C₁₀H₁₄O₄ [198.22] 1.2 - Propanediol, 3-(2-methoxyphenoxy)-3-(o Methoxyphenoxy)-1,2-propanediol. The drug
can be identified by several chemical methods. It melts between 78° to 82°F and has a pH between 5.0 and 7.0 in a solution of 1 to 100.
[0010]
In treating patients with P, SV, BPH, PA, BNH, UTI and DLS, guaifenesin may, for example, be given 50-200mg once a day for 3 days, then twice a day for one week, then 150-1200mg a day in divided doses (three to six capsules). It can be administered by
syrup but in the above conditions is preferred to be administered by 50mg to 200mg tablets or capsules. When produced with 5-30mg of zinc sulfate it is best provided by capsule.
[0011]
It would be administered for 2 weeks in acute problems; up to 3 months in recurring problems; and up to one year in chronic problems. Prophylactic use would be employed in long term patients. This would include certain patients with low tolerance for
guaifenesin but who could tolerate a 50mg per day dosage over a long period of time.
[0012]
If the agent acts by lysing thick prostatic and seminal vesicle secretions, one would expect that theoretically trapped bacteria would "pour" forth and cause increased dysuria and frequency in patients with prostatic and seminal vesicle infections. This
in fact does occur in at least one-third of the patients to some degree and most patients should be covered by antibacterial agents initially. This is also seen in women with elevated bladder necks given this agent.
[0013]
At times the dysuria and frequency in certain patients may be so severe that the medication has to be abandoned. In some patients, stopping the medication has caused a gradual return to pre-treatment symptoms and findings. Significant reduction of sperm
counts in males in the reproductive age would also necessitate the stopping of medication.
PATENT CITATIONS
Cited Patent Filing date Publication date Applicant Title
EP0055313A1 * Dec 30, 1980 Jul 7, 1982 Ed. Geistlich Söhne Ag Für Chemische Industrie Guaiacol and derivatives; compositions thereof and use in a method of treatment
US3314852 * Oct 4, 1963 Apr 18, 1967 Bristol Myers Co Method of producing ataraxic, anticonvulsant activity and skeletal muscle relaxation
* Cited by examiner
NON-PATENT CITATIONS
Reference
1 * Arch. Sci. Med., Vol. 120, No. 1, 1965, pages 58-69; R. FIOCCARDI: "Ritenzione urinaria postoperatoria"
2 * Fertility and Sterility, Vol. 37, No. 5, May 1982, pages 707-708, The American Fertility Society, US; J.H. CHECK et al.: "Improvement of cervical factor with guaifenesin"
* Cited by examiner
REFERENCED BY
Citing Patent Filing date Publication date Applicant Title
WO2005018528A2 * Aug 12, 2004 Mar 3, 2005 Kuno Kirschfeld Method for the treatment prophylaxis and differential diagnosis of prostatitis
WO2005018528A3 * Aug 12, 2004 Apr 7, 2005 Kuno Kirschfeld Method for the treatment prophylaxis and differential diagnosis of prostatitis
* Cited by examiner
CLASSIFICATIONS
International Classification A61K31/09, A61K33/30
Cooperative Classification A61K33/30, A61K31/09
European Classification A61K31/09, A61K33/30
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