Complex Compound of Diphenhydramine and Its Therapeutic Activity
Abstract Generated abstract
This paper describes the preparation and preliminary therapeutic evaluation of a mercury-containing complex compound of dimedrol, an antihistamine, with potassium mercuric rhodanide for potential use in psoriasis. The authors synthesize the compound by combining aqueous dimedrol with potassium mercuric rhodanide, obtaining a water-insoluble resinous product with a mercury content consistent with a 1:1 composition. Pharmacological testing indicated low toxicity, and preliminary clinical use as a 2 to 5 percent ointment in 11 psoriasis patients suggested reduction of itching and an antipsoriatic effect without observed undesirable side effects.
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COMPLEX COMPOUND OF DIMEDROL AND ITS THERAPEUTIC ACTIVITY
A. G. Pechenkin, S. D. Yaroslavleva
(Presented by Prof. Dr. Chem. Sci. T. P. Kuleva)
Some of the mercury-containing complex compounds of the acridine and quinoline series synthesized by us proved effective against psoriasis [1]. However, while producing a general therapeutic effect, these compounds only slowly relieve the itching from which patients with psoriasis suffer greatly. To reduce itching, patients are given dimedrol internally. Dimedrol belongs to the antihistamine drugs; it reduces the organism’s reaction to histamine, has a desensitizing effect, and is used for urticaria, pruritic dermatoses, etc. [2].
It seemed of interest to obtain complex compounds of mercury salts with dimedrol and to test them in the form of ointments for psoriasis. From complex compounds of this kind we expected an antipruritic action combined with a general antipsoriatic effect.
We obtained complex compounds of potassium mercuric rhodanide with dimedrol in the following way.
To 7.3 g of dimedrol (a pharmacopoeial preparation), dissolved in 100 ml of water, with stirring is added a solution of potassium mercuric rhodanide (12.8 g in 100 ml of water), prepared according to the prescription [3]. With continued stirring, a product is formed in the form of a pink resin, which, after decantation and washing with water, is dried to constant weight over calcium chloride. The complex compound obtained is insoluble in water, dissolves in alcohol, and contains 25.9% mercury, which corresponds to a composition of 1:1 (mole of dimedrol per mole of potassium mercuric rhodanide)
\[ \begin{aligned} &\text{[structural formula of dimedrol]}\cdot K_2Hg(CNS)_4 \end{aligned} \]
Pharmacological tests showed that the preparation is of low toxicity.
In the clinic of skin diseases of the Tomsk Medical Institute, under the direction—
under Professor I. S. Beirakh, the preparation was tested for psoriasis in the form of a 2–5% ointment. Preliminary data from clinical trials (11 subjects) indicate that the preparation reduces itching and exhibits an antipsoriatic effect without causing undesirable side effects.
REFERENCES
- A. G. Pechenkin, S. D. Yaroslavtseva, Complex compounds of 8-hydroxyquinoline and their therapeutic activity (article included in this collection).
- M. D. Mashkovsky, Medicinal Agents, 1960.
- A. Rosenheim, R. Cohen, Z. Anozg. Chem., 27, 285 (1901).