New Page 25

Bethanechol

Bethanechol is a very useful medication for counteracting the dry mouth and bladder inhibition side-effects of tricyclic anti-depressants and other psychiatric medications. It also reportedly helpful for the constipation and orgasmic difficulties sometimes caused by anti-cholinergic side-effects. Unfortunately, it is rarely used by American psychiatrists. Indeed, thanks to lax regulation by the federal government, the cost of bethanechol has skyrocketing from a few cents per 25 mg tablet to $1.50 per tablet. Fortunately, it can be legally obtained with the prescription of an American physician from a pharmacy in England for roughly 23 cents per tablet.

Bethanechol is a cholinergic medication, so it counteracts anti-cholinergic side-effects. While bethanechol can cause frequent side-effects of its own when used for dry mouth or constipation not due to anti-cholinergic side-effect, in my experience with over 100 patients, I have never had a single side-effect reported to me. In other words, as long as bethanechol is correcting an anti-cholinergic imbalance, side-effects are extremely unlikely. Bethanechol is unable to cross the blood-brain barrier, so it is not a psychotropic and has no effect on a person's mental state.

Bethanechol for Dry Mouth: Xerostomia after radiation therapy to the head and neck. Bethanechol possesses muscarinic and nicotinic-cholinergic activity that likely accounts for its mode of action. Bethanechol (25 mg, three times daily) was not associated with significant side effects. Statistically significant increases in whole resting saliva (p = 0.003) and whole stimulated saliva (p = 0.001) Oral Surg Oral Med Oral Pathol 1994 Jun;77(6):610-4;

Bethanechol for Dry Mouth, Constipation, Bladder Inhibition: Use of bethanechol chloride to relieve side effects, including salivary inactivation, constipation, and bladder inhibition, which result from the anticholinergic action of tricyclic antidepressants. He suggests that the use of cholinergic medication during antidepressant therapy may extend the use of the tricyclics to patients who find anticholinergic side effects especially troublesome. Everett, Am J Psychiatry 1975 Nov;132(11):1202-4

Female Anorgasmia Common; Bethanechol Might Help: As of 1989, psychotropics reported to inhibit female orgasm: antipsychotics (thioridazine, trifluoperazine and fluphenazine), combination perphenazine/amitriptyline, antidepressants (phenelzine, isocarboxazid, tranylcypromine, amoxapine, clomipramine, imipramine, nortriptyline and desipramine) and anxiolytics (diazepam, flurazepam and alprazolam). Try discontinuation of the drug, reduction of dosage, a wait for spontaneous remission. Bethanechol chloride and cyproheptadine have been successful in resolving anorgasmia while on antidepressants. Shen, St.Louis U, J Reprod Med 1990 Jan;35(1):11-4. Bethanechol, a cholinergic drug, was found to give total relief of impotence in two men and of anorgasmy in one woman; none of the subjects suffered side effects. Am J Psychiatry 1982 Sep;139(9):1193-4

Bethanechol 1 Hour Before Sex for Tricyclic Ejaculatory Dysfunction: 43-year-old man who experienced profound dose-related erectile and ejaculatory dysfunction without loss of libido on three separate tricyclic antidepressants. Bethanechol chloride 20 mg taken 1 to 2 hours prior to sexual activity permitted satisfactory erection and ejaculation during sexual intercourse, while the patient continued to take protriptyline, a tricyclic (Vivactyl). Bethanechol chloride can reverse erectile and ejaculatory dysfunction induced by tricyclic antidepressants and mazindol: case report. Yager J. J Clin Psychiatry 1986 Apr;47(4):210-1

Bethanechol for Tricyclic Impotence and Anorgasmia: The anticholinergic properties of tricyclic antidepressants sometimes cause sexual dysfunction. Bethanechol, a cholinergic drug, was found to give total relief of impotence in two men and of anorgasmy in one woman; none of the subjects suffered side effects. Reversal by bethanechol of sexual dysfunction caused by anticholinergic antidepressants. Gross MD. Am J Psychiatry 1982 Sep;139(9):1193-4

Bethanechol Helps Nortriptyline Dry Mouth in DB: 26 pt DB PC. 26 elderly depressed patients being treated with nortriptyline. Patients receiving bethanechol had reduced subjective complaints of anticholinergic side effects and showed a trend toward improvement on an objective measure of salivary flow. U Pitt, Treatment of nortriptyline's side effects in elderly patients: a double-blind study of bethanechol. Rosen J, Pollock BG, Altieri LP, Jonas EA. Am J Psychiatry 1993 Aug;150(8):1249-51

Bethanechol Mentioned for Anti-Depressant Sexual Inhibition: "Adjunctive medications (such as cyproheptadine, bethanechol, yohimbine, and amantadine, as well as other antidepressants) to counteract the adverse sexual effects." Provides no data or experience. Clinical implications of antidepressant drug effects on sexual function. Harvey KV, Balon R. Ann Clin Psychiatry 1995 Dec;7(4):189-201

Bethanechol 1 Hour Before Sex for Ejaculatory Dysfunction: 43-year-old man who experienced profound dose-related erectile and ejaculatory dysfunction without loss of libido on three separate antidepressants and on the anorectic agent mazindol is described. Bethanechol chloride 20 mg p.o., taken 1 to 2 hours prior to sexual activity, permitted satisfactory erection and ejaculation during sexual intercourse, while the patient continued to take protriptyline or mazindol. Bethanechol chloride can reverse erectile and ejaculatory dysfunction induced by tricyclic antidepressants and mazindol: case report. Yager J. J Clin Psychiatry 1986 Apr;47(4):210-1

Bethanechol for Anti-Depressant Impotence and Anorgasmia: The anticholinergic properties of currently available antidepressants sometimes cause sexual dysfunction. Bethanechol, a cholinergic drug, was found to give total relief of impotence in two men and of anorgasmy in one woman; none of the subjects suffered side effects. Reversal by bethanechol of sexual dysfunction caused by anticholinergic antidepressants. Gross MD. Am J Psychiatry 1982 Sep;139(9):1193-4

Bethanechol Mode of Action: It stimulates the parasympathetic nervous system, stimulating gastric motility, peristalsis, bladder emptying. muscarinic effects are prominent with little nicotinic effects. Little effect on heart, BP, circulation. It "does not cross the blood-brain barrier because of its charged quaternary amine moiety." It starts working in 30-60 minutes and works for about an hour. Side-effects are rare from oral administration. The oral dosage is 10-50 mg 3-4 times a day. PDR 2003, pg 2104 Merck. Cost = $52 for 100 25mg via myprescription.com in Canada. Best deal is to buy scored 50mg tabs 100 for $62 and break in half. Urecholine brand $163 for 100 25mg. $18.50 for 100 25mg from www.mastersmarketing.com in UK.

Pilocarpine (Salagen) Alternative: Used for dry mouth 5-10 mg TID or 5 mg QID. Half-life of 5 mg is 45 min., and 10mg 1.5 hr. Onset occurs in 20 min, and peaks at 30 min., lasting 3-5 hours. PDR. Cost $114 per 100 5 mg tab via SavRx.com.

Cevimeline (Evoxac) Alternative: New cholinergic medicine for Sjogren’s Syndrome at 30mg tid for dry mouth. (1-866-3EVOXAC). It has muscarinic effects on the gastrointestinal, urinary and reproductive systems and other tissues at the doses approximately 10-fold higher than the doses needed for saliva secretion. General pharmacological profile of the novel muscarinic receptor agonist SNI-2011, a drug for xerostomia in Sjogren's syndrome. 4th communication: Effects on gastrointestinal, urinary and reproductive systems and other effects. Arisawa H, Fukui K, Imai E, Fujise N, Masunaga H. Arzneimittelforschung 2002;52(4):225-32; DB PC study. muscarinic agonist activity prominently affecting the M1 and M3 receptors prevalent in exocrine glands. 60 mg tid OK but more side-effects and 30 tid fine. Cevimeline for the treatment of xerostomia in patients with Sjogren syndrome: a randomized trial. Fife RS, Chase WF, Dore RK, Wiesenhutter CW, Lockhart PB, Tindall E, Suen JY. Indiana Univ Med School, Arch Intern Med 2002 Jun 10;162(11):1293-300; Cost = $124 for 100 30mg tabs via SavRx.com

Reasons Given by Researchers for Not Using Bethanechol: 1) It’s a psychotropic and therefore not allowed by research protocol [not a psychotropic], 2) Dry mouth a minor side-effect and not worth bothering with [#1 side-effect of imipramine and nortriptyline and bethanechol also helps urinary retention, and is reported to help anti-cholinergic constipation and sexual dysfunction too], 3) It would break the double-blind [It would probably help protect the double-blind. The dry mouth breaks the double-blind], 4) The researcher no longer prescribes tricyclics in his practice and either does anyone else because tricyclics are no longer worth considering in research or practice [The research had just published a study using a tricyclic as the comparator medication and in the article pointed out its high rate of side-effects! Patients in the study were not given bethanechol or anything else to relieve the discomfort].