IP Library › Granted Patent US 12,201,637
Granted Patent B2
US 12,201,637 · App. 18/219,783 · Granted Jan 21, 2025

Dosing regimen for sedation with CNS 7056 (Remimazolam)

Inventors: Karin Wilhelm-Ogunbiyi (Simmermath, DE); Keith Borkett (Houghton Camps, GB); Gary Stuart Tilbrook (Huntingdon, GB); Hugh Wiltshire (Digswell, GB)
Assignee: PAION UK LTD.
A61K31/5517A61K9/0019A61K31/4468A61K45/06
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Quick Facts
Patent No.
US 12,201,637
App. No.
18/219,783
Granted
Jan 21, 2025
Kind
B2
Abstract

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.

Claims (18)

1. A method of sedating an adult human comprising administering intravenously to the adult human an initial dose of a pharmaceutical composition comprising 2.5 mg to 5 mg of 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazol[1,2-a] [1,4] benzodiazepine-4-yl]-propionic methyl ester (formula (I)

or a besylate salt thereof, over a period of about 1 minute.

2. The method of claim 1 , wherein the human is administered 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazol[1,2-a][1,4] benzodiazepine-4-yl]-propionic methyl ester besylate.

3. The method of claim 2 , further comprising administering to the human at least one top-up dose given after the initial dose of the compound of formula (I), or the besylate salt thereof.

4. The method of claim 3 , wherein the at least one top-up dose of the compound of formula (I), or the besylate salt thereof, is administered not less than 2 minutes after the initial dose or a previous top-up dose.

5. The method of claim 3 , wherein the at least one top-up dose given after the initial dose or a previous top-up dose of the compound of formula (I), or the besylate salt thereof, is in an amount of less than 3 mg.

6. The method of claim 5 , wherein the at least one top-up dose of the compound of formula (I), or the besylate salt thereof, is administered not less than 2 minutes after the initial dose.

7. The method of claim 3 , wherein the at least one top-up dose given after the initial dose or after a previous top-up dose of the compound of formula (I), or the besylate salt thereof, is in an amount of between about 2 mg and 3 mg.

8. The method of claim 7 , wherein the at least one top-up dose of the compound of formula (I), or the besylate salt thereof, is administered not less than 2 minutes after the initial dose.

9. The method of claim 1 , wherein the sedation lasts for less than 30 minutes.

10. The method of claim 1 , further comprising maintaining a patient airway or positive pressure ventilation in the human.

11. The method of claim 1 , wherein the pharmaceutical composition comprises saline.

12. The method of claim 1 , wherein the adult human is undergoing an operative procedure.

13. The method of claim 12 , wherein the operative procedure is a diagnostic procedure.

14. The method of claim 13 , wherein the diagnostic procedure is an endoscopic procedure.

15. The method of claim 14 , wherein the endoscopic procedure is colonoscopy.

16. The method of claim 14 , wherein the endoscopic procedure is upper GI endoscopy.

17. The method of claim 12 , wherein the operative procedure is a therapeutic procedure.

Priority Claims (4)
EP 10014366 · Nov 8, 2010 · regional
EP 10014784 · Nov 19, 2010 · regional
EP 10014819 · Nov 22, 2010 · regional
EP 10014972 · Nov 25, 2010 · regional
Continuity (9)
Continuation 16905547 · Jun 18, 2020
Continuation 16457387 · Jun 28, 2019
Continuation 16213879 · Dec 7, 2018
Continuation 16039198 · Jul 18, 2018
Continuation 15792636 · Oct 24, 2017
Continuation 15647143 · Jul 11, 2017
Continuation 15400117 · Jan 6, 2017
Continuation 13883935
Related Publication 20230346796A1 · Nov 2, 2023
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