Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Recombinant or stably-transformed bacterium encoding one or...
Patent
1981-12-18
1984-07-10
Robinson, Douglas W.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Recombinant or stably-transformed bacterium encoding one or...
A61K 3127
Patent
active
044593090
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
This invention relates to a method of treating glaucoma and ocular hypertension in mammals. More particularly, this invention involves a method of lowering intraocular pressure in the mammalian eye by topically applying thereto an ophthalmologically acceptable, effective amount for lowering intraocular pressure of N,N-dimethylaminoethyl carbamate ("N-demethylated carbachol"). The invention further relates to ophthalmic compositions comprising this compound as an active ingredient.
Ocular hypertension is associated with glaucoma, a disease of the eye which is characterized by a progressive increase in intraocular pressure. If the eye is left untreated, such increased pressure will damage the optic nerve head resulting in a corresponding loss of visual field and, ultimately, blindness. Accordingly, a common treatment for glaucoma is the administration to the diseased eye of a substance which is effective in lowering such intraocular pressure.
Basically, there are two types of drugs available for this purpose. One reduces aqueous humor formation and the other increases aqueous humor outflow to reduce the intraocular pressure. Among all of these drugs, pilocarpine, which belongs to the latter type, is the most widely used drug and has been in use for more than a century. Although effective for its intended purpose, when used in the eye pilocarpine and similar drugs produce many unwanted side effects, including local irritation, tearing, burning sensation, ciliary spasm, miosis, and headache. These side effects are thought to be due to two major reasons: (1) instability of the drug at high PH medium necessitating the formulation of pilocarpine-containing ophthalmic solutions at a pH as low as 4.5 to 5.5, and (2) the chemical structure of pilocarpine is entirely different from the natural cholinergic neurotransmitter, acetylcholine, a factor which could produce the sypmtoms of tearing, headache, etc.
It has now been found, according to this invention that intraocular pressure can be reduced in hypertensive eyes without the unwanted side effects commonly associated with pilocarpine and similar drugs.
SUMMARY OF THE INVENTION
Methods are provided for treating open-angle glaucoma by reducing the intraocular pressure in the hypertensive mammalian eye which comprise topically applying to such eye an ophthalmologically acceptable, effective amount for lowering intraocular pressure of a cholinergically active tertiary nitrogen derivative of choline which is capable of being solubilized in aqueous solution and remains stable and active at pH within the range of about 5.5 to about 8.0. In particular, there is provided a method of reducing intraocular pressure in mammals having intraocular hypertension comprising topically administering to a hypertensive eye an opthalmologically acceptable, effective amount for lowering intraocular pressure of a compound selected from N,N-dimethylaminoethyl carbamate (N-demethylated carbachol) and ophthalmologically acceptable acid addition salts thereof. Pharmaceutical compositions comprising an acid addition salt of N-demethylated carbachol and a non-toxic, pharmaceutically acceptable, ophthalmological carrier are particularly suitable for use in accordance with this invention. In a preferred form, such compositions will comprise ophthalmic solutions or ointments, but other known ocular drug delivery means such as, for example, lamella (e.g. a drug containing, water-soluble gel of glycerinated gelatin), polymer inserts, or soft contact lens are also included within the scope of the invention.
BRIEF DESCRIPTION OF DRAWINGS
In the drawings, which are set forth to illustrate the embodiments described in the examples, the figures are as follows:
FIG. 1 is a graph illustrating the time-response relationship of N-demethylated carbachol and pilocarpine effects, respectively, on intraocular pressure in glaucomatous beagles for five days.
FIG. 2 is a graph showing the acute time-response relationship of N-demethylated carbachol effects on intraocular pressure i
REFERENCES:
J. Pharm. Sci., 69, (3), 332-334, (1980), Trzeciakowski et al.
J. Pharm. Sci., 67, (4), 531-535, (1978), Trzeciakowski et al.
Chem. Abst., 93, 422j, (1980), Trzeciakowski et al.
AMA-Drug Evaluation, 2nd ed., (1973), Chapter 69, p. 680.
Robinson Douglas W.
The Texas A&M University System
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