Dosing regimen for sedation with CNS 7056 (Remimazolam)
The invention relates to a dosing regimen for sedation with the fast-acting benzodiazepine CNS 7056 in combination with an opioid, in particular fentanyl, whereas CNS 7056 is given in a dose of 2 to 20 mg, preferably between 4 and 9 mg and most preferably between 5 and 8 mg.
1. A method for conducting a procedure involving sedation in a subject comprising:
(a) administering intravenously to the subject one or more fixed doses of a pharmaceutical composition in an amount sufficient to sedate the subject, wherein the pharmaceutical composition comprises 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]-propionic methyl ester of formula (I)
or a pharmaceutically acceptable salt thereof; and
(b) passing an endoscope into the subject.
2. The method of claim 1 , wherein the subject is 18 years or older.
3. The method of claim 1 , wherein one or more doses of an opioid is administered to the subject prior to the administration of the pharmaceutical composition to the subject.
4. The method of claim 3 , wherein the opioid is fentanyl.
5. The method of claim 1 , wherein the procedure is an upper GI endoscopy.
6. The method of claim 1 , wherein the procedure is a colonoscopy.
7. The method of claim 1 , wherein the one or more fixed doses of the pharmaceutical composition is administered to the subject over a time period of one minute or less.
8. The method of claim 1 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 2 mg to about 10 mg of the compound of formula (I), or a pharmaceutically acceptable salt thereof.
9. The method of claim 8 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 10 mg of the compound of formula (I), or a pharmaceutically acceptable salt thereof.
10. The method of claim 9 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 9 mg of the compound of formula (I), or a pharmaceutically acceptable salt thereof.
11. The method of claim 10 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 5 mg to about 9 mg of the compound of formula (I), or a pharmaceutically acceptable salt thereof.
12. The method of claim 8 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 2 mg to about 10 mg of the compound of formula (I).
13. The method of claim 12 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 10 mg of the compound of formula (I).
14. The method of claim 13 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 9 mg of the compound of formula (I).
15. The method of claim 13 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 5 mg to about 8 mg of the compound of formula (I).
16. The method of claim 15 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises about 5 mg of the compound of formula (I).
17. The method of claim 1 , wherein the one or more doses of the pharmaceutical composition comprise an amount of the compound of formula (I), or a pharmaceutically acceptable salt thereof, to achieve an MOAA/S score of less than or equal to 4 in the subject.
18. The method of claim 1 , wherein the pharmaceutical composition comprises the besylate salt of the compound of formula (I).
19. A method for conducting a procedure involving sedation in a subject comprising:
(a) administering intravenously to the subject one or more fixed doses of a pharmaceutical composition in an amount sufficient to sedate the subject, wherein the pharmaceutical composition comprises the besylate salt of 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]-propionic methyl ester of formula (I)
and wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 2 mg to about 10 mg of the besylate salt of the compound formula (I); and
(b) passing an endoscope into the subject.
20. The method of claim 19 , wherein the subject is 18 years or older.
21. The method of claim 19 , wherein one or more doses of an opioid is administered to the subject prior to the administration of the pharmaceutical composition to the subject.
22. The method of claim 21 , wherein the opioid is fentanyl.
23. The method of claim 19 , wherein the procedure is an upper GI endoscopy.
24. The method of claim 19 , wherein the procedure is a colonoscopy.
25. The method of claim 19 , wherein the one or more fixed doses of the pharmaceutical composition is administered to the subject over a time period of one minute or less.
26. The method of claim 19 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 10 mg of the besylate salt of the compound of formula (I).
27. The method of claim 26 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 9 mg of the besylate salt of the compound of formula (I).
28. The method of claim 27 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 5 mg to about 9 mg of the besylate salt of the compound of formula (I).
29. The method of claim 19 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 5 mg to about 8 mg of the compound of formula (I).
30. The method of claim 29 , wherein each fixed dose of the pharmaceutical composition administered to the subject comprises about 5 mg of the compound of formula (I).
31. The method of claim 19 , wherein the one or more doses of the pharmaceutical composition comprise an amount of the besylate salt of the compound of formula (I) sufficient to achieve an MOAA/S score of less than or equal to 4 in the subject.
32. A method for conducting a procedure involving sedation in a subject comprising:
(a) administering to the subject one or more doses of a pharmaceutical composition, wherein each dose of the pharmaceutical composition comprises 5 mg of 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]-propionic methyl ester of formula (I)
or a pharmaceutically acceptable salt thereof; and
(b) passing a colonoscope into the subject.
33. The method of claim 1 , wherein the procedure is a diagnostic procedure.
34. The method of claim 19 , wherein the procedure is a diagnostic procedure.
35. The method of claim 32 , wherein the procedure is a diagnostic procedure.