Compositions of opioid antagonists and methods for treating conditions caused by the varicella-zoster virus therewith
Provided are compositions comprising opioid antagonists, such as naltrexone naloxone, or nalmefene, or their pharmaceutically acceptable salts, and methods for treating conditions caused by the varicella-zoster virus therewith.
1. A method for treating a vesicular eruption caused by the varicella-zoster virus, the method comprising topically administering to a subject in need thereof an effective amount of naltrexone or a pharmaceutically-acceptable salt thereof, wherein the naltrexone or the pharmaceutically-acceptable salt thereof is administered in the form of a pharmaceutical composition comprising:
a) the naltrexone or the pharmaceutically-acceptable salt thereof in an amount of about 0.1% to about 5% by weight of the pharmaceutical composition;
b) an emulsifying agent in an amount of about 2% to about 5% by weight of the pharmaceutical composition;
c) a stiffening agent in an amount of about 1% to about 45% by weight of the pharmaceutical composition;
d) a surfactant in an amount of about 0.5% to about 2.5% by weight of the pharmaceutical composition;
e) a preservative in an amount of about 0.01% to about 0.6% by weight of the pharmaceutical composition;
f) a humectant in an amount of about 1% to about 15% by weight of the pharmaceutical composition;
g) alkalizing or buffering agent in an amount of about 0.01% to about 3% by weight of the pharmaceutical composition;
h) an emollient in an amount of about 1% to about 50% by weight of the pharmaceutical composition; and
i) a solvent,
wherein the vesicular eruption regresses within 5 days of administration of the pharmaceutical composition.
2. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof has less than about 10% by weight of other stereoisomers.
3. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof has less than about 5% by weight of other stereoisomers.
4. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is present in an amount of about 0.5% to about 2% by weight of the pharmaceutical composition.
5. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is present in an amount of about 1% by weight of the pharmaceutical composition.
6. The method of claim 1 , wherein the pharmaceutical composition is in the form of a gel, cream, ointment, liquid, suspension, solution, emulsion, foam, or aerosol.
7. The method of claim 1 , wherein the pharmaceutical composition is administered to the subject by spreading or spraying the composition onto the affected area.
8. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is administered in a total daily dose of up to about 150 mg/cm 2 of skin.
9. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is administered in a total daily dose of about 10 mg/cm 2 to about 100 mg/cm 2 of skin.
10. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is administered in a total daily dose of about 50 mg/cm 2 of skin.
11. The method of claim 1 , wherein the pharmaceutical composition is administered 1, 2, 3, 4, or 5 times daily.
12. The method of claim 1 , further comprising administering to the subject one or more additional agents effective to treat the vesicular eruption.
13. The method of claim 12 , wherein the additional agent is acyclovir, valacyclovir, or famciclovir.
14. The method of claim 1 , wherein the administration blocks an opioid receptor in the subject.
15. The method of claim 14 , wherein the opioid receptor that is blocked is a mu (μ) opioid receptor.
16. The method of claim 14 , wherein the opioid receptor that is blocked is a delta (δ) opioid receptor.
17. The method of claim 14 , wherein the opioid receptor that is blocked is a kappa (κ) opioid receptor.
18. The method of claim 1 , wherein the method further comprises treating post-herpetic neuralgia caused by varicella-zoster virus in the subject.
19. The method of claim 1 , wherein a pain of the subject associated with the varicella-zoster virus regresses within 3 days of administration.
20. The method of claim 1 , wherein an itching of the subject associated with the varicella-zoster virus regresses within 3 days of administration.
21. The method of claim 1 , wherein a hyperesthesis of the subject associated with the varicella-zoster virus regresses within 3 days of administration.
22. The method of claim 1 , wherein an itching, pain, and hyperesthesis of the subject associated with the varicella-zoster virus regresses within 3 days of administration.
23. The method of claim 1 , wherein no additional treatment is required to treat the vesicular eruption.
24. The method of claim 1 , wherein the administration produces no side-effect in the subject.
25. The method of claim 1 , wherein the administration occurs daily.
26. The method of claim 1 , wherein the administration occurs three times daily.
27. The method of claim 1 , wherein the naltrexone or the pharmaceutically-acceptable salt thereof is administered in a total daily amount of about 1 g.
28. The method of claim 1 , wherein the pharmaceutical composition comprises:
a) the naltrexone or the pharmaceutically-acceptable salt thereof in an amount of about 0.5% to about 2% by weight of the pharmaceutical composition;
b) the emulsifying agent in an amount of about 2% to about 5% by weight of the pharmaceutical composition;
c) the stiffening agent in an amount of about 2% to about 5% by weight of the pharmaceutical composition;
d) the surfactant in an amount of about 0.5% to about 1.5% by weight of the pharmaceutical composition;
e) the preservative in an amount of about 0.01% to about 0.6% by weight of the pharmaceutical composition;
f) the humectant in an amount of about 2% to about 10% by weight of the pharmaceutical composition;
g) the alkalizing or buffering agent in an amount of about 0.01% to about 3% by weight of the pharmaceutical composition;
h) the emollient in an amount of about 15% to about 30% by weight of the pharmaceutical composition; and
i) the solvent.
29. The method of claim 1 , wherein the pharmaceutical composition comprises:
a) the naltrexone or the pharmaceutically-acceptable salt thereof in an amount of about 1% by weight of the pharmaceutical composition;
b) the emulsifying agent, wherein the emulsifying agent is cetyl alcohol in an amount of about 3.6% by weight of the pharmaceutical composition, and carboxypolymethylene in an amount of about 0.2% by weight of the pharmaceutical composition;
c) the stiffening agent in an amount of about 3.6% by weight of the pharmaceutical composition, wherein the stiffening agent is stearyl alcohol;
d) the surfactant in an amount of about 0.8% by weight of the pharmaceutical composition, wherein the surfactant is sodium lauryl sulfate;
e) the preservative, wherein the preservative is nipagin in an amount of about 0.1% by weight of the pharmaceutical composition, and nipasol in an amount of about 0.05% by weight of the pharmaceutical composition;
f) the humectant in an amount of about 5% by weight of the pharmaceutical composition, wherein the humectant is propylene glycol;
g) the alkalizing or buffering agent in an amount of about 0.03% by weight of the pharmaceutical composition, wherein the alkalizing or buffering agent is sodium hydroxide;
h) the emollient, wherein the emollient is white vaseline in an amount of about 13.5% by weight of the pharmaceutical composition, and liquid vaseline in an amount of about 5.4% by weight of the pharmaceutical composition; and
i) the solvent, wherein the solvent is water.