1. Chlorpiprazine
2. Perfenazine
3. Trilafon
1. 58-39-9
2. Trilafon
3. Perphenazin
4. Etaperazine
5. Perfenazine
6. Ethaperazine
7. Etaperazin
8. Fentazin
9. Chlorpiprazine
10. Perphenan
11. Thilatazin
12. Decentan
13. Chlorperphenazine
14. Emesinal
15. Perfenazina
16. Tranquisan
17. Trifaron
18. Trilifan
19. Triphenot
20. F-mon
21. Perphenazinum
22. 2-(4-(3-(2-chloro-10h-phenothiazin-10-yl)propyl)piperazin-1-yl)ethanol
23. Sch 3940
24. 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol
25. 4-[3-(2-chlorophenothiazin-10-yl)propyl]-1-piperazineethanol
26. 4-(3-(2-chlorophenothiazin-10-yl)propyl)-1-piperazineethanol
27. Pzc
28. Gamma-(4-(beta-hydroxyethyl)piperazin-1-yl)propyl-2-chlorophenothiazine
29. Nsc 150866
30. 4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]-1-piperazineethanol
31. 1-(2-hydroxyethyl)-4-(3-(2-chloro-10-phenothiazinyl)propyl)piperazine
32. 2-{4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]piperazin-1-yl}ethan-1-ol
33. Fta7xxy4ez
34. Chembl567
35. Nsc-150866
36. 2-chloro-10-3-(1-(2-hydroxyethyl)-4-piperazinyl)propyl Phenothiazine
37. 2-{4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]piperazin-1-yl}ethanol
38. 2-chloro-10-(3-(4-(2-hydroxyethyl)piperazin-1-yl)propyl)phenothiazine
39. 2-chloro-10-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl]phenothiazine
40. Mls000069637
41. Chebi:8028
42. 1',1-(2-idrossietil)-4,3-(2-cloro-10-fenotiazil)propilpiperazina
43. 1-piperazineethanol, 4-(3-(2-chloro-10h-phenothiazin-10-yl)propyl)-
44. 1-piperazineethanol, 4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]-
45. 2-(4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]-1-piperazinyl)ethanol
46. Nsc150866
47. Cas-58-39-9
48. Ncgc00015826-02
49. Perfenil
50. Smr000058180
51. Perfenazina [italian]
52. 1-piperazineethanol, 4-(3-(2-chlorophenothiazin-10-yl)propyl)-
53. 1-(2-hydroxyethyl)-4-[3-(2-chloro-10-phenothiazinyl)propyl]piperazine
54. Dsstox_cid_3441
55. Piperazineethanol, 4-(3-(2-chloro-10h-phenothiazin-10-yl)propyl)-
56. Dsstox_rid_77031
57. Dsstox_gsid_23441
58. Perfenazina [inn-spanish]
59. Perphenazinum [inn-latin]
60. Perphenazine Maleate [jan]
61. 1-piperazineethanol, 4-[3-(2-chlorophenothiazin-10-yl)propyl]-
62. 2-chloro-10-3-[1-(2-hydroxyethyl)-4-piperazinyl]propyl Phenothiazine
63. Hsdb 3379
64. Sr-01000000137
65. Unii-fta7xxy4ez
66. Einecs 200-381-5
67. Mfcd00056798
68. Ai3-50151
69. Piperazineethanol, 4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]-
70. .gamma.-(4-(.beta.-hydroxyethyl)piperazin-1-yl)propyl-2-chlorophenothiazine
71. .gamma.-[4-(.beta.-hydroxyethyl)piperazin-1-yl]propyl-2-chlorophenothiazine
72. 2-(4-(3-(2-chloro-10h-phenothiazin-10-yl)propyl)piperazin-1-yl)ethan-1-ol
73. Perphenazine [usp:inn:ban:jan]
74. 2-chloro-10-(3-(1-(2-hydroxyethyl)-4-piperazinyl)propyl)phenothiazine
75. Sch-3940
76. Prestwick_536
77. 1',1-(2-idrossietil)-4,3-(2-cloro-10-fenotiazil)propilpiperazina [italian]
78. Etrafon (salt/mix)
79. Spectrum_001610
80. Opera_id_1161
81. Prestwick0_000125
82. Prestwick1_000125
83. Prestwick2_000125
84. Prestwick3_000125
85. Spectrum2_001602
86. Spectrum3_000758
87. Spectrum4_000843
88. Spectrum5_001493
89. Lopac-p-6402
90. Perphenazine [mi]
91. Perphenazine [inn]
92. Perphenazine [jan]
93. P 6402
94. Perphenazine [hsdb]
95. Perphenazine [vandf]
96. Lopac0_000930
97. Oprea1_603835
98. Regid_for_cid_4748
99. Schembl42125
100. Bspbio_000170
101. Bspbio_002376
102. Gtpl209
103. Kbiogr_001445
104. Kbioss_002090
105. Perphenazine [mart.]
106. Mls001146929
107. Mls002548897
108. 5,7-eicosadiynoicacid
109. Bidd:gt0150
110. Divk1c_000880
111. Perphenazine [usp-rs]
112. Perphenazine [who-dd]
113. Spectrum1503934
114. Spbio_001603
115. Spbio_002109
116. Bpbio1_000188
117. Dtxsid1023441
118. Component Of Triavil (salt/mix)
119. Hms502l22
120. Kbio1_000880
121. Kbio2_002090
122. Kbio2_004658
123. Kbio2_007226
124. Kbio3_001596
125. Perphenazine (jp17/usp/inn)
126. Ninds_000880
127. Hms1568i12
128. Hms1922m14
129. Hms2093m15
130. Hms2095i12
131. Hms2232d21
132. Hms3259c09
133. Hms3262j22
134. Hms3370o14
135. Hms3712i12
136. Hms3885h20
137. Perphenazine [orange Book]
138. Pharmakon1600-01503934
139. Perphenazine [ep Monograph]
140. Hy-a0077
141. Perphenazine [usp Monograph]
142. Perphenazine 1.0 Mg/ml In Methanol
143. Tox21_110233
144. Tox21_500930
145. 1-piperazineethanol, Trihydrochloride
146. Bdbm50130273
147. Ccg-39060
148. Nsc758649
149. S4731
150. Stk019818
151. Zinc19228902
152. Akos000664046
153. Tox21_110233_1
154. Cs-5137
155. Db00850
156. Etrafon-a Component Perphenazine
157. Ks-5105
158. Lp00930
159. Nc00472
160. Nsc-758649
161. Sdccgsbi-0050904.p004
162. Idi1_000880
163. Mrf-0000509
164. Ncgc00015826-01
165. Ncgc00015826-03
166. Ncgc00015826-04
167. Ncgc00015826-05
168. Ncgc00015826-06
169. Ncgc00015826-07
170. Ncgc00015826-08
171. Ncgc00015826-09
172. Ncgc00015826-10
173. Ncgc00015826-13
174. Ncgc00015826-20
175. Ncgc00024092-03
176. Ncgc00024092-04
177. Ncgc00024092-05
178. Ncgc00024092-06
179. Ncgc00261615-01
180. Ac-12196
181. Perphenazine Component Of Etrafon-a
182. Sbi-0050904.p003
183. Db-053200
184. Ab00052390
185. Eu-0072164
186. Eu-0100930
187. Ft-0603244
188. P1970
189. C07427
190. D00503
191. D82041
192. Ab00052390_17
193. A831863
194. L000919
195. Q423520
196. Sr-01000000137-2
197. Sr-01000000137-4
198. Sr-01000000137-5
199. Sr-01000000137-8
200. W-105390
201. Brd-k10995081-001-05-5
202. Brd-k10995081-001-15-4
203. Wln: T C666 Bn Isj Eg B3- At6n Dntj D2q
204. Z1945707494
205. Perphenazine, British Pharmacopoeia (bp) Reference Standard
206. Fluphenazine Dihydrochloride Impurity E [ep Impurity]
207. Perphenazine, European Pharmacopoeia (ep) Reference Standard
208. Perphenazine, United States Pharmacopeia (usp) Reference Standard
209. 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]-piperazin-1-yl]ethanol
210. 2-(4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]-1-piperazinyl)ethanol #
211. Perphenazine For System Suitability, European Pharmacopoeia (ep) Reference Standard
| Molecular Weight | 404.0 g/mol |
|---|---|
| Molecular Formula | C21H26ClN3OS |
| XLogP3 | 4.2 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 5 |
| Rotatable Bond Count | 6 |
| Exact Mass | 403.1485113 g/mol |
| Monoisotopic Mass | 403.1485113 g/mol |
| Topological Polar Surface Area | 55.2 Ų |
| Heavy Atom Count | 27 |
| Formal Charge | 0 |
| Complexity | 463 |
| 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 |
| 1 of 2 | |
|---|---|
| Drug Name | Perphenazine |
| PubMed Health | Perphenazine (By mouth) |
| Drug Classes | Antiemetic, Antipsychotic |
| Drug Label | Perphenazine (4-[3-(2-chlorophenothiazin-10-yl)propyl]-1-piperazineethanol), a piperazinyl phenothiazine, having the chemical formula, C21H26CIN3OS. It is available as oral tablets containing 2 mg, 4 mg, 8 mg, and 16 mg of perphenazine.Inactive ingre... |
| Active Ingredient | Perphenazine |
| Dosage Form | Tablet |
| Route | Oral |
| Strength | 8mg; 4mg; 2mg; 16mg |
| Market Status | Prescription |
| Company | Vintage Pharms; Sandoz |
| 2 of 2 | |
|---|---|
| Drug Name | Perphenazine |
| PubMed Health | Perphenazine (By mouth) |
| Drug Classes | Antiemetic, Antipsychotic |
| Drug Label | Perphenazine (4-[3-(2-chlorophenothiazin-10-yl)propyl]-1-piperazineethanol), a piperazinyl phenothiazine, having the chemical formula, C21H26CIN3OS. It is available as oral tablets containing 2 mg, 4 mg, 8 mg, and 16 mg of perphenazine.Inactive ingre... |
| Active Ingredient | Perphenazine |
| Dosage Form | Tablet |
| Route | Oral |
| Strength | 8mg; 4mg; 2mg; 16mg |
| Market Status | Prescription |
| Company | Vintage Pharms; Sandoz |
Antipsychotic Agents, Phenothiazine; Dopamine Antagonists
National Library of Medicine's Medical Subject Headings online file (MeSH, 2009)
Perphenazine is indicated for use in the treatment of schizophrenia and for the control of severe nausea and vomiting in adults. /Included in US product label/
US Natl Inst Health; DailyMed. Current Medication Information for Perphenazine (perphenazine) tablet, film coated (April 2010). Available from, as of July 8, 2010 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6633
Perphenazine has not been shown effective for the management of behavioral complications in patients with mental retardation. /Included in US product label/
US Natl Inst Health; DailyMed. Current Medication Information for Perphenazine (perphenazine) tablet, film coated (April 2010). Available from, as of July 8, 2010 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6633
The US Food and Drug Administration (FDA) currently advises clinicians that antipsychotic agents are not approved for the treatment of dementia-related psychosis. FDA further advises clinicians that no drugs currently are approved for the treatment of patients with dementia-associated psychosis and that other management options should be considered in such patients. /Phenothiazine General Statement/
American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 2509
VET: ...To help control intractable animals, relieve pain, control motion sickness, and as preanesthetic agent.
Rossoff, I.S. Handbook of Veterinary Drugs. New York: Springer Publishing Company, 1974., p. 434
/BOXED WARNING/ WARNING: Increased Mortality in Elderly Patients with Dementia-Related Psychosis Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Analyses of seventeen placebo-controlled trials (modal duration of 10 weeks), largely in patients taking atypical antipsychotic drugs, revealed a risk of death in drug-treated patients of between 1.6 to 1.7 times the risk of death in placebo-treated patients. Over the course of a typical 10-week controlled trial, the rate of death in drug-treated patients was about 4.5%, compared to a rate of about 2.6% in the placebo group. Although the causes of death were varied, most of the deaths appeared to be either cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia) in nature. Observational studies suggest that, similar to atypical antipsychotic drugs, treatment with conventional antipsychotic drugs may increase mortality. The extent to which the findings of increased mortality in observational studies may be attributed to the antipsychotic drug as opposed to some characteristic(s) of the patients is not clear. Perphenazine is not approved for the treatment of patients with dementia-related psychosis.
US Natl Inst Health; DailyMed. Current Medication Information for Perphenazine (perphenazine) tablet, film coated (Updated: August 2012). Available from, as of April 24, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5fbfe9da-26e8-4705-98f3-42acd3d7b439
... Extrapyramidal reactions ... fairly common, usually 3 types ... Parkinsonian-like syndrome ... dystonia and dyskinesia, including torticollis, tics, and other involuntary muscle movements ... akathisia, shown by restlessness ... hyperreflexia, reported in newborn ... ./Phenothiazines/
Osol, A. and J.E. Hoover, et al. (eds.). Remington's Pharmaceutical Sciences. 15th ed. Easton, Pennsylvania: Mack Publishing Co., 1975., p. 1021
Perphenazine products are contraindicated in comatose or greatly obtunded patients and in patients receiving large doses of central nervous system depressants (barbiturates, alcohol, narcotics, analgesics, or antihistamines); in the presence of existing blood dyscrasias, bone marrow depression, or liver damage; and in patients who have shown hypersensitivity to perphenazine tablets, their components, or related compounds.
US Natl Inst Health; DailyMed. Current Medication Information for Perphenazine (perphenazine) tablet, film coated (April 2010). Available from, as of July 8, 2010 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6633
Perphenazine products are also contraindicated in patients with suspected or established subcortical brain damage, with or without hypothalamic damage, since a hyperthermic reaction with temperatures in excess of 104 F may occur in such patients, sometimes not until 14 to 16 hours after drug administration. Total body ice-packing is recommended for such a reaction; antipyretics may also be useful.
US Natl Inst Health; DailyMed. Current Medication Information for Perphenazine (perphenazine) tablet, film coated (April 2010). Available from, as of July 8, 2010 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6633
For more Drug Warnings (Complete) data for Perphenazine (47 total), please visit the HSDB record page.
For use in the management of the manifestations of psychotic disorders and for the control of severe nausea and vomiting in adults.
FDA Label
Perphenazine is a piperazinyl phenothiazine, acts on the central nervous system, and has a greater behavioral potency than other phenothiazine derivatives whose side chains do not contain a piperazine moiety. It is a member of a class of drugs called phenothiazines, which are dopamine D1/D2 receptor antagonists. Perphenazine is 10 to 15 times as potent as chlorpromazine; that means perphenazine is a highly potent antipsychotic. In equivalent doses it has approximately the same frequency and severity of early and late extrapypramidal side-effects compared to Haloperidol.
Dopamine Antagonists
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME. (See all compounds classified as Dopamine Antagonists.)
Antipsychotic Agents
Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)
N - Nervous system
N05 - Psycholeptics
N05A - Antipsychotics
N05AB - Phenothiazines with piperazine structure
N05AB03 - Perphenazine
Absorption
Absolute bioavailability is 40% following oral administration.
Route of Elimination
Perphenazine is extensively metabolized in the liver to a number of metabolites by sulfoxidation, hydroxylation, dealkylation, and glucuronidation.
Phenothiazines are generally well absorbed from the GI tract and from parenteral sites; however, absorption may be erratic, particularly following oral administration. Considerable interindividual variations in peak plasma concentrations have been reported. The variations in peak plasma concentrations may result from genetic differences in the rate of metabolism, biodegradation of the drug in the GI lumen, and/or metabolism of the drug during absorption (in the GI mucosa) and first pass through the liver. /Phenothiazine General Statement/
American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 2511
Following oral administration of perphenazine tablets, mean peak plasma perphenazine concentrations were observed between 1 to 3 hours. ... In a study in which normal volunteers (n=12) received perphenazine 4 mg q8h for 5 days, steady-state concentrations of perphenazine were reached within 72 hours.
US Natl Inst Health; DailyMed. Current Medication Information for Perphenazine (perphenazine) tablet, film coated (April 2010). Available from, as of July 8, 2010 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6633
Phenothiazines and their metabolites are distributed into most body tissues and fluids, with high concentrations being distributed into the brain, lungs, liver, kidneys, and spleen. /Phenothiazine General Statement/
American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 2511
Phenothiazines are highly bound to plasma proteins. /Phenothiazine General Statement/
American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 2511
For more Absorption, Distribution and Excretion (Complete) data for Perphenazine (10 total), please visit the HSDB record page.
Hepatic.
Perphenazine is extensively metabolized in the liver to a number of metabolites by sulfoxidation, hydroxylation, dealkylation, and glucuronidation.
US Natl Inst Health; DailyMed. Current Medication Information for Perphenazine (perphenazine) tablet, film coated (April 2010). Available from, as of July 8, 2010 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6633
Most metabolites of phenothiazines are pharmacologically inactive; however, certain metabolites (eg, 7-hydroxychlorpromazine, mesoridazine) show moderate pharmacologic activity and may contribute to the action of the drugs. There is limited evidence to indicate that some phenothiazines (eg, chlorpromazine) may induce their own metabolism. /Phenothiazine General Statement/
American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 2511
The pharmacokinetics of a single oral dose of 6 mg perphenazine was studied in a group of six slow and six rapid hydroxylators of debrisoquin. Peak serum concentrations of perphenazine were significantly higher in slow hydroxylators than they were in rapid hydroxylators (2.4 +/- 0.6 versus 0.7 +/- 0.3 nmol/L, p less than 0.001). The AUC(0-12) was also higher in slow hydroxylators than it was in rapid hydroxylators (18.5 +/- 6.2 versus 4.5 +/- 2.5 nmol.L-1.hr, p less than 0.001). The data suggest that the disposition of the antipsychotic drug perphenazine covaries with polymorphic debrisoquin hydroxylation.
PMID:2743709 Dahl-Puustinen ML et al; Clin Pharmacol Ther 46 (1): 78-81 (1989)
After chronic administration of piperazine-substituted phenothiazine drugs ... to rats, tissues contained drug metabolites, in which piperazine ring fission by multiple oxidative n-dealkylation had occurred to give substituted ethylenediamine. Thus, n-[gamma-(2-chlorophenothiazinyl-10)-propyl]ethylenediamine ... from ... perphenazine ...
The Chemical Society. Foreign Compound Metabolism in Mammals Volume 3. London: The Chemical Society, 1975., p. 255
Perphenazine has known human metabolites that include N-Dealkylated perphenazine and Perphenazine sulfoxide.
S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560
8-12 hours, but ranges up to 20 hours.
The plasma elimination half-life of perphenazine was independent of dose and ranged between 9 and 12 hours.
US Natl Inst Health; DailyMed. Current Medication Information for Perphenazine (perphenazine) tablet, film coated (April 2010). Available from, as of July 8, 2010 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6633
...The average terminal half-life of PPZ was approximately 9.5 hours. ...
PMID:973987 Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1428936 Eggert Hansen C et al; Br J Clin Pharmacol 3 (5): 915-23 (1976)
Peak 7-hydroxyperphenazine concentrations were observed between 2 to 4 hours with a terminal phase half-life ranging between 9.9 to 18.8 hours.
US Natl Inst Health; DailyMed. Current Medication Information for Perphenazine (perphenazine) tablet, film coated (April 2010). Available from, as of July 8, 2010 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6633
Binds to the dopamine D1 and dopamine D2 receptors and inhibits their activity. The mechanism of the anti-emetic effect is due predominantly to blockage of the dopamine D2 neurotransmitter receptors in the chemoreceptor trigger zone and vomiting centre. Perphenazine also binds the alpha andrenergic receptor. This receptor's action is mediated by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
The principal pharmacologic effects of "perphenazine" are similar to those of chlorpromazine. "Perphenazine" has moderate anticholinergic effects, weak to moderate sedative effects, and strong extrapyramidal effects. "Perphenazine" has strong antiemetic activity.
American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 2516
The development of phenothiazine derivatives as psychopharmacologic agents resulted from the observation that certain phenothiazine antihistaminic compounds produced sedation. In an attempt to enhance the sedative effects of these drugs, promethazine and chlorpromazine were synthesized. Chlorpromazine is the pharmacologic prototype of the phenothiazines. The pharmacology of phenothiazines is complex, and because of their actions on the central and autonomic nervous systems, the drugs affect many different sites in the body. Although the actions of the various phenothiazines are generally similar, these drugs differ both quantitatively and qualitatively in the extent to which they produce specific pharmacologic effects. /Phenothiazine General Statement/
American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 2510
In the CNS, phenothiazines act principally at the subcortical levels of the reticular formation, limbic system, and hypothalamus. Phenothiazines generally do not produce substantial cortical depression; however, there is minimal information on the specific effects of phenothiazines at the cortical level. Phenothiazines also act in the basal ganglia, exhibiting extrapyramidal effects. The precise mechanism(s) of action, including antipsychotic action, of phenothiazines has not been determined, but may be principally related to antidopaminergic effects of the drugs. There is evidence to indicate that phenothiazines antagonize dopamine-mediated neurotransmission at the synapses. There is also some evidence that phenothiazines may block postsynaptic dopamine receptor sites. However, it has not been determined whether the antipsychotic effect of the drugs is causally related to their antidopaminergic effects. Phenothiazines also have peripheral and/or central antagonistic activity against alpha-adrenergic, serotonergic, histaminic (H1-receptors), and muscarinic receptors. Phenothiazines also have some adrenergic activity, since they block the reuptake of monoamines at the presynaptic neuronal membrane, which tends to enhance neurotransmission. The effects of phenothiazines on the autonomic nervous system are complex and unpredictable because the drugs exhibit varying degrees of alpha-adrenergic blocking, muscarinic blocking, and adrenergic activity. The antipsychotic activity of phenothiazines may be related to any or all of these effects, but it has been suggested that the drugs' effects on dopamine are probably most important. It has also been suggested that effects of phenothiazines on other amines (eg, gamma-aminobutyric acid [GABA]) or peptides (eg, substance P, endorphins) may contribute to their antipsychotic effect. Further study is needed to determine the role of central neuronal receptor antagonism and of effects on biochemical mediators in the antipsychotic action of the phenothiazines and other antipsychotic agents. /Phenothiazine General Statement/
American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 2510
Although the exact mechanism(s) of action has not been conclusively determined, phenothiazines have an antiemetic effect. The antiemetic activity may be mediated via a direct effect of the drugs on the medullary chemoreceptor trigger zone (CTZ), apparently by blocking dopamine receptors in the CTZ. Phenothiazines inhibit the central and peripheral effects of apomorphine and ergot alkaloids. Phenothiazines generally do not inhibit emesis caused by the action of drugs at the nodose ganglion or by local action on the GI tract. /Phenothiazine General Statement/
American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 2511
For more Mechanism of Action (Complete) data for Perphenazine (14 total), please visit the HSDB record page.
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