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HIJ Drug Manufacturing Factory

H N. O. Cl. HIJ Drug Manufacturing Factory. Ketamine. 6S Chu Man Hin, Hinson (9) Chung Siu Wa, Jennifer (10) Lau Yuk Ping, Isa (14). Lead Compound Discovery.

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HIJ Drug Manufacturing Factory

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  1. H N O Cl HIJ Drug Manufacturing Factory Ketamine 6S Chu Man Hin, Hinson (9) Chung Siu Wa, Jennifer (10) Lau Yuk Ping, Isa (14)

  2. Lead Compound Discovery cause hallucinations(幻覺), neurotoxicity(神經毒性) and seizures(癲癇) phencyclidine (PCP) Ph A kind of an anesthetic (麻醉藥) N Ketamine for replacement

  3. Laboratory Session

  4. Molecular Modification Ketamine PCP Cyclohexamine Year 1959 1958 1962

  5. MgBr Cl Drug synthesis CN Step 1 Cyclopentylmagnesium bromide 2-chlorobenzonitrile

  6. Cl Drug synthesis O Step 2 Br2 1-(2-chlorobenzoyl) cyclopentane

  7. Cl Drug synthesis O Br Step 3 CH3NH2 + H2O

  8. Cl Drug synthesis N OH Step 4 Decalin (C10H18) Methylimino derivative

  9. H N Drug synthesis O Cl Ketamine made!!

  10. Formulation Development

  11. Injection 10% ketoprofen 5% Lidocaine 10% ketamine

  12. Injection cyclobenzaprine tramadol clonidine These are all longer-acting local anaesthetics(麻醉藥)

  13. Liquid Aerosol Formulation carriers diluents solubilizing or emulsifying agents excipients surfactants

  14. Liquid Aerosol Formulation carriers • Examples : • Soya lecithin (大豆豆黃素) • oleic acid (油酸) • sorbitan trioleate (山梨糖醇酐三油酸 • 酯) = Preferred

  15. Liquid Aerosol Formulation diluents • Examples : • Sterile water • Saline(鹽水) • Buffered saline • Dextrose(葡萄糖)solution • In Specific embodiment: • phosphate buffered saline • buffered saline solution generally between the pH 7.0-8.0 range • water

  16. Liquid Aerosol Formulation They are useful for 1) pH maintenance 2) solution stabilization 3) regulating osmotic pressure solubilizing or emulsifying agents excipients surfactants

  17. Liquid Aerosol Formulation Benzodiazepine (苯二氮平類藥物) narcotic analgesic (麻醉止痛劑)

  18. Aerosol Dry Powder Formulation a dispersing agent ketamine a bulking agent (eg. lactose, sucrose)

  19. Aerosol Dry Powder Formulation Dispersing agent facilitates the dispersal of the powder from the device May include another therapeutically effective drug like benzodiazepine and narcotic analgesic

  20. Safety Tests According to several research and studies: 1) tolerance and/or dependence to the drug 2) great deal in common with other drugs linked with dependence including stimulants, opiates, alcohol, and cannabis 3) indulges in excessive amounts over a short period of time

  21. Human Trials The drug was first given to American soldiers during the Vietnam War. A 2-year prospective audit of sedation practicewas undertaken by the Department of EmergencyMedicine.

  22. Midazolam Ketamine Propofol 107people 18people 85people Test 51% 40% 9% Total people involved : 210

  23. Results Time/ min

  24. Results Percentage/ % 14.6 % 22.2 %

  25. Results • Apnoea(窒息) and hypoxia(缺氧) most often occurred with midazolam and propofol • hypertension(過度緊張) and hypertonicity(張力過高)were encountered more frequently with ketamine • 19.5% of patients given ketamine suffered from the reemergence phenomenon.

  26. Conclusion 1) Ketamine is both safe and effective 2) Ketamine compares favourably with midazolam as an agent forprocedural sedation 3) Ketamine may be particularly useful ingroups of patients at high risk of adverse effects with midazolam

  27. Market Approval 1) In 1970, the FDA approved ketamine for human use 2) It was (and still is) legally sold as (i) Ketalar (Parke-Davis, for humans) (ii) Ketaset (For Dodge, for animals), (iii) other brands (like Ketamine Hydrochloride)

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