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1. Cyclizine Hcl
2. Cyclizine Hydrochloride
3. Hcl, Cyclizine
4. Hydrochloride, Cyclizine
5. Marezine
1. 1-benzhydryl-4-methylpiperazine
2. Marezine
3. 82-92-8
4. Nautazine
5. Ciclizina
6. Neo-devomit
7. 1-(diphenylmethyl)-4-methylpiperazine
8. Valoid
9. N-benzhydryl-n'-methylpiperazine
10. N-methyl-n'-benzhydrylpiperazine
11. Cyclizinum
12. Cyclizinum [inn-latin]
13. Ciclizina [inn-spanish]
14. Compound 47-83
15. Piperazine, 1-(diphenylmethyl)-4-methyl-
16. (n-benzhydryl)(n'-methyl)diethylenediamine
17. Wellcome Preparation 47-83
18. 1-benzhydryl-4-methylpiperazin
19. Bw 47-83
20. Cyclizine Chloride
21. Wellcome Prepn. 47-83
22. Cyclizine (inn)
23. Nsc 26608
24. (+-)-1-diphenylmethyl-4-methylpiperazine
25. N-methyl-n'-benzyhydrylpiperazine
26. 1-diphenylmethyl-4-methylpiperazine
27. Nsc-26608
28. Qrw9fcr9p2
29. Chebi:3994
30. 1-benzhydryl-4-methyl-piperazine
31. Emoquil
32. Wellcome
33. Cyclizine [inn]
34. Ne-devomit
35. Wellcome Prepn 47-83
36. Hsdb 3309
37. Ncgc00016421-01
38. Cas-303-25-3
39. Einecs 201-445-5
40. Unii-qrw9fcr9p2
41. Brn 0230441
42. Sr-05000001595
43. Cyclizine [usp:inn:ban:dcf]
44. Emoquil (salt/mix)
45. Marzine (salt/mix)
46. Spectrum_000854
47. Specplus_000917
48. Cyclizine [mi]
49. Cyclizine [hsdb]
50. Prestwick0_000510
51. Prestwick1_000510
52. Prestwick2_000510
53. Prestwick3_000510
54. Spectrum2_001174
55. Spectrum3_000368
56. Spectrum4_000205
57. Spectrum5_001594
58. Cyclizine [vandf]
59. Chembl648
60. Cyclizine [mart.]
61. Cyclizine [who-dd]
62. Schembl4690
63. Oprea1_429421
64. Bspbio_000439
65. Bspbio_002095
66. Kbiogr_000809
67. Kbioss_001334
68. 5-23-01-00232 (beilstein Handbook Reference)
69. Divk1c_007013
70. Spectrum1500211
71. Spbio_001187
72. Spbio_002360
73. Bpbio1_000483
74. Gtpl7151
75. Dtxsid4022864
76. Kbio1_001957
77. Kbio2_001334
78. Kbio2_003902
79. Kbio2_006470
80. Kbio3_001315
81. N-benzhydryl-n-methyl Piperazine
82. Hms1920a20
83. Hms2091i08
84. Pharmakon1600-01500211
85. 1-benzhydryl-4-methylpiperazine #
86. Nsc26608
87. Wln: T6n Dntj Ayr&r& D1
88. Ccg-40322
89. Mfcd00023293
90. Nsc756710
91. Zinc19156872
92. Akos015839079
93. Db01176
94. Nsc-756710
95. Ncgc00016421-02
96. Ncgc00016421-03
97. Ncgc00016421-04
98. Ncgc00016421-09
99. Ncgc00094634-01
100. Ncgc00094634-02
101. Ls-14655
102. Sbi-0052576.p003
103. (+/-)-1-diphenylmethyl-4-methylpiperazine
104. Ab00053084
105. C06930
106. D03621
107. D81845
108. Ab00053084_08
109. L000701
110. Q867308
111. Sr-05000001595-1
112. Brd-k79501723-001-02-0
113. Brd-k79501723-003-03-4
114. Brd-k79501723-003-09-1
| Molecular Weight | 266.4 g/mol |
|---|---|
| Molecular Formula | C18H22N2 |
| XLogP3 | 3.6 |
| Hydrogen Bond Donor Count | 0 |
| Hydrogen Bond Acceptor Count | 2 |
| Rotatable Bond Count | 3 |
| Exact Mass | 266.178298710 g/mol |
| Monoisotopic Mass | 266.178298710 g/mol |
| Topological Polar Surface Area | 6.5 Ų |
| Heavy Atom Count | 20 |
| Formal Charge | 0 |
| Complexity | 253 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
Antiemetics; Histamine H1 Antagonists
National Library of Medicine's Medical Subject Headings online file (MeSH, 1999)
ANTIHISTAMINE USED AS HYDROCHLORIDE & LACTATE IN PREVENTION & TREATMENT OF MOTION SICKNESS (NAUSEA, VOMITING & VERTIGO). IT IS ALSO PROBABLY EFFECTIVE FOR CONTROL OF POSTOPERATIVE NAUSEA & VOMITING.
Osol, A. and J.E. Hoover, et al. (eds.). Remington's Pharmaceutical Sciences. 15th ed. Easton, Pennsylvania: Mack Publishing Co., 1975., p. 747
DURATION OF ACTION IS ABOUT 4 HR.
American Medical Association, AMA Department of Drugs, AMA Drug Evaluations. 3rd ed. Littleton, Massachusetts: PSG Publishing Co., Inc., 1977., p. 1096
...LARGE SCALE STUDY, INCL PREGNANT WOMEN RECEIVING CYCLIZINE DURING 1ST TRIMESTER, FAILED TO CONFIRM THAT DRUG HAD ANY TERATOGENIC EFFECT IN MAN WITH DOSES EMPLOYED.
American Medical Association, AMA Department of Drugs, AMA Drug Evaluations. 3rd ed. Littleton, Massachusetts: PSG Publishing Co., Inc., 1977., p. 1096
For more Therapeutic Uses (Complete) data for CYCLIZINE (7 total), please visit the HSDB record page.
.../DO NOT/ EXCEED 4 TABLETS/DAY. /HYDROCHLORIDE/
Osol, A. and J.E. Hoover, et al. (eds.). Remington's Pharmaceutical Sciences. 15th ed. Easton, Pennsylvania: Mack Publishing Co., 1975., p. 747
.../IT/ SHOULD NOT BE USED IN WOMEN DURING PREGNANCY & THOSE LIKELY TO BECOME PREGNANT UNLESS SPECIFICALLY DIRECTED BY PHYSICIAN.
Osol, A. and J.E. Hoover, et al. (eds.). Remington's Pharmaceutical Sciences. 15th ed. Easton, Pennsylvania: Mack Publishing Co., 1975., p. 747
IN 1965 AN AD HOC COMMITTEE OF US FDA CONCLUDED THAT EVIDENCE OF TERATOGENIC EFFECTS IN HUMAN...WAS NOT SIGNIFICANT, BUT IT MADE NO SPECIFIC MENTION OF EYES.
Grant, W. M. Toxicology of the Eye. 2nd ed. Springfield, Illinois: Charles C. Thomas, 1974., p. 341
...OFFSPRING OF PROBABLY SEVERAL THOUSAND WOMEN WHO HAD RECEIVED APPROX 150 MG CYCLIZINE/DAY DURING PREGNANCY...HAD A VARIETY OF NONOCULAR ABNORMALITIES, BUT STATISTICAL SIGNIFICANCE IN RELATION TO CYCLIZINE WAS UNCERTAIN.
Grant, W. M. Toxicology of the Eye. 2nd ed. Springfield, Illinois: Charles C. Thomas, 1974., p. 341
For more Drug Warnings (Complete) data for CYCLIZINE (8 total), please visit the HSDB record page.
5. 5= EXTREMELY TOXIC: PROBABLE ORAL LETHAL DOSE (HUMAN) 5-50 MG/KG; BETWEEN 7 DROPS & 1 TEASPOONFUL FOR 70 KG PERSON (150) LB.
Gosselin, R.E., H.C. Hodge, R.P. Smith, and M.N. Gleason. Clinical Toxicology of Commercial Products. 4th ed. Baltimore: Williams and Wilkins, 1976., p. II-231
For prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness, and vertigo (dizziness caused by other medical problems).
Cyclizine is a piperazine-derivative antihistamine used as an antivertigo/antiemetic agent. Cyclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus. Although the mechanism by which cyclizine exerts its antiemetic and antivertigo effects has not been fully elucidated, its central anticholinergic properties are partially responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone. It also possesses anticholinergic, antihistaminic, central nervous system depressant, and local anesthetic effects.
Antiemetics
Drugs used to prevent NAUSEA or VOMITING. (See all compounds classified as Antiemetics.)
Histamine H1 Antagonists
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. (See all compounds classified as Histamine H1 Antagonists.)
R - Respiratory system
R06 - Antihistamines for systemic use
R06A - Antihistamines for systemic use
R06AE - Piperazine derivatives
R06AE03 - Cyclizine
BENZHYDROLPIPERAZINES & THEIR N-DEALKYLATION PRODUCTS ARE DISTRIBUTED IN ALL TISSUES OF RAT & ARE TRANSFERRED TO FETUS. /BENZYHYDROLPIPERAZINES/
The Chemical Society. Foreign Compound Metabolism in Mammals. Volume 1: A Review of the Literature Published Between 1960 and 1969. London: The Chemical Society, 1970., p. 194
Cyclizine is metabolised to its N-demethylated derivative, norcyclizine, which has little antihistaminic (H1) activity compared to Cyclizine.
OXIDATIVE N-DEALKYLATION IS MAIN METABOLIC PATHWAY OF BENZHYDROLPIPERAZINES; CYCLIZINE.../IS/ TRANSFORMED INTO NORCYCLIZINE...
The Chemical Society. Foreign Compound Metabolism in Mammals. Volume 1: A Review of the Literature Published Between 1960 and 1969. London: The Chemical Society, 1970., p. 192
WITH A PURIFIED MIXED FUNCTION OXIDASE FROM LIVER MICROSOMES IN PRESENCE OF REDUCED PYRIDINE NUCLEOTIDE & O2.../CYCLIZINE IS/ OXIDIZED TO N-OXIDE.
Casarett, L.J., and J. Doull. Toxicology: The Basic Science of Poisons. New York: MacMillan Publishing Co., 1975., p. 120
20 hours
Vomiting (emesis) is essentially a protective mechanism for removing irritant or otherwise harmful substances from the upper GI tract. Emesis or vomiting is controlled by the vomiting centre in the medulla region of the brain, an important part of which is the chemotrigger zone (CTZ). The vomiting centre possesses neurons which are rich in muscarinic cholinergic and histamine containing synapses. These types of neurons are especially involved in transmission from the vestibular apparatus to the vomiting centre. Motion sickness principally involves overstimulation of these pathways due to various sensory stimuli. Hence the action of cyclizine which acts to block the histamine receptors in the vomiting centre and thus reduce activity along these pathways. Furthermore since cyclizine possesses anti-cholinergic properties as well, the muscarinic receptors are similarly blocked.
.../IT SEEMS/ THAT STIMULATION OF VESTIBULAR APPARATUS IS NECESSARY & SUFFICIENT...& THAT VESTIBULAR CEREBELLAR MIDBRAIN "INTEGRATIVE VOMITING CENTER" & MEDULLARY CHEMORECEPTIVE TRIGGER ZONE ARE...INVOLVED /IN MOTION SICKNESS/. IT IS...PROBABLE THAT EFFECTIVE ANTIHISTAMINES EXERT.../ACTION/ IN THESE CENTERS. /ANTIHISTAMINE/
Goodman, L.S., and A. Gilman. (eds.) The Pharmacological Basis of Therapeutics. 5th ed. New York: Macmillan Publishing Co., Inc., 1975., p. 606
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