Search summary:
Session ID: 65099d7982a8c2a271f593cc8a780ca2
Search Type: drug
Started at: 2009-11-10 11:19:21
Finished at: 2009-11-10 11:21:17
| Field | Result | Source |
|---|---|---|
| Name | ||
| chlorpromazine | External | |
| Drugbank ID | ||
| DB00477 | DrugBank | |
| Description | ||
| According to one study of the effects on the reproductive system in rats treated with chlorpromazine there were significant decreases in the weight of the testis, epididymis, seminal vesicles, and prostate gland. This was accompanied by a decline in sperm motility, sperm counts, viability, and serum levels of testosterone in chlorpromazine rats compared to control rats. It has been reported that a change in either the absolute or relative weight of an organ after a chemical is administered is an indication of the toxic effect of the chemical. Therefore, the observed change in the relative weight of the testis and other accessory reproductive organs in rats treated with chlorpromazine indicates that the drug might be toxic to these organs at least during the period of treatments. Furthermore, the weights of the kidney, heart, liver, and adrenal glands of these treated rats were not affected both during administration of the drug and recovery periods, suggesting that the drug is not toxic to these organs. | Wikipedia | |
| Additionally, chlorpromazine is a presynaptic inhibitor of dopamine reuptake, which may lead to (mild) antidepressive and antiparkinsonian effects. This action could also account for psychomotor agitation and amplification of psychosis (very rarely noted in clinical use). | Wikipedia | |
| Antipsychotic drugs may cause priapism, a pathologically prolonged and painful penile erection, which is usually unassociated with sexual desire or intercourse. Although this effect is rare it is a potentially serious complication that can lead to permanent impotence and other serious complications. | Wikipedia | |
| Chlorpromazine is a psychotropic agent indicated for the treatment of schizophrenia. It also exerts sedative and antiemetic activity. Chlorpromazine has actions at all levels of the central nervous system-primarily at subcortical levels-as well as on multiple organ systems. Chlorpromazine has strong antiadrenergic and weaker peripheral anticholinergic activity | DrugBank | |
| Chlorpromazine is a very effective antagonist of D2 dopamine receptors and similar receptors, such as D3 and D5. Unlike most other drugs of this genre, it also has a high affinity for D1 receptors. Blocking these receptors causes diminished neurotransmitter binding in the forebrain, resulting in many different effects. Dopamine, unable to bind with a receptor, causes a feedback loop that causes dopaminergic neurons to release more dopamine. Therefore, upon first taking the drug, patients will experience an increase in activity of dopaminergic neural activity. Eventually, dopamine production of the neurons will drop substantially and dopamine will be removed from the synaptic cleft. At this point, neural activity decreases greatly; the continual blockade of receptors only compounds this effect. | Wikipedia | |
| Chlorpromazine is an antagonist to H1 receptors (provoking antiallergic effects), H2 receptors (reduction of forming of gastric juice), M1 and M2 receptors (dry mouth, reduction in forming of gastric juice) and some 5-HT receptors (different anti-allergic/gastrointestinal actions). | Wikipedia | |
| Chlorpromazine largely replaced electroconvulsive therapy, psychosurgery, and insulin shock therapy. The development and marketing of antipsychotic drugs was one of the forces that propelled deinstitutionalization, which is the systematic removal of people with severe mental illness from institutions like psychiatric hospitals. In 1955 there were 558,922 resident patients in American state and county psychiatric hospitals. By 1970 the number dropped to 337,619; by 1980 to 150,000; and by 1990 between 110,000 to 120,000 patients. | Wikipedia | |
| Doses of antipsychotics that are considered therapeutically low are sufficient to trigger an epileptic seizure in particularly vulnerable patients for example those with an abnormally low genetically determined seizure threshold. The drug dose ability to provoke seizures is presumably due to a reduced seizure threshold. The incidence of the first unprovoked seizure in the general population is 0.07 to 0.09%, whereas the incidence rates have been reported to range from 0.1 to 1.5% in patients treated with therapeutic doses of the most commonly used antipsychotic drugs. Furthermore, the seizure risk rises markedly to a range of 4 to 30% in patients who have taken an overdose. This most notable variability among studies may possibly be due to methodological differences which makes the research data that much harder to interpret. The risk of a seizure being provoked during antipsychotic drug medication is greatly influenced by the individuals inherited seizure threshold and particularly by the presence of a history of epilepsy, brain damage or other conditions. There is an agreement however that seizures triggered by drugs are a dose-dependent adverse effect. | Wikipedia | |
| In addition to influencing the neurotransmitters dopamine, serotonin, epinephrine, norepinephrine, and acetylcholine it has been reported that antipsychotic drugs could achieve glutamatergic effects. This mechanism involves direct effects on antipsychotic drugs on glutamate receptors. By using the technique of functional neurochemical assay chlorpromazine and phenothiazine derivatives have been shown to have inhibitory effects on NMDA receptors that appeared to be mediated by action at the Zn site. It was found that there is an increase of NMDA activity at low concentrations and suppression at high concentrations of the drug. No significant difference in glutamate and glycine activity from the effects of chlorpromazine were reported. Further work will be necessary to determine if the influence in NMDA receptors by antipsychotic drugs contributes to their effectiveness. | Wikipedia | |
| Other reported side effects are rare, though severe; these include a reduction in the number of white blood cells—referred to as leukopenia—or, in extreme cases, even agranulocytosis, which may occur in 0.01% of patients and lead to death via uncontrollable infections and/or sepsis. Chlorpromazine is also known to accumulate in the eye—in the posterior corneal stroma, lens, and uveal tract. Because it is a phototoxic compound, the potential exists for it to cause cellular damage after light exposure. Research confirms a significant risk of blindness from continued use of chlorpromazine, as well as other optological defects such as color blindness and benign pigmentation of the cornea. | Wikipedia | |
| Chemical Kingdom | ||
| Organic | BioSpider | |
| Chemical Class | ||
| Not Available | Not Applicable | |
| Chemical Species | ||
| aromatic compound | Checkmol | |
| aryl chloride | Checkmol | |
| heterocyclic compound | Checkmol | |
| tertiary aliphatic amine (trialkylamine) | Checkmol | |
| tertiary aliphatic/aromatic amine (alkylarylamine) | Checkmol | |
| tertiary amine | Checkmol | |
| thioether | Checkmol | |
| Synonym | ||
| 10-(3-Dimethylaminopropyl)-2-chlorophenothiazine | Pubchem | |
| 10H-Phenothiazine-10-propanamine, 2-chloro-N, N-dimethyl- | NCI | |
| 10H-Phenothiazine-10-propanamine, 2-chloro-N,N-dimethyl- | NIST | |
| 2-Chloro-10-(3-(dimethylamino)propyl)phenothiazine | Pubchem | |
| 2-Chloro-10-[3-(Dimethylamino)propyl]phenothiazine | NIST | |
| 2-Chloro-10-[3-(dimethyamino)propyl]phenothiazine | NIST | |
| 2-Chloro-N,N-dimethyl-10H-phenothiazine-10-propanamine | Pubchem | |
| 2-Chloropromazine | NIST | |
| 2-Cloro-10 (3-dimetilaminopropil)fenotiazina | NIST | |
| 2-Cloro-10 (3-dimetilaminopropil)fenotiazina [Italian] | Pubchem | |
| 2-chloro-10-(3-(dimethylamino)propyl)-phenothiazine | Pubchem | |
| 2-chloro-10-[3-(dimethylamino)propyl]- | Pubchem | |
| 3-(2-chlorophenothiazin-10-yl)-N,N-dimethyl-propan-1-amine | Pubchem | |
| 3-(2-chlorophenothiazin-10-yl)-N,N-dimethylpropan-1-amine | Pubchem | |
| 4560 Rp hydrochloride | Pubchem | |
| 69-09-0 (HYDROCHLORIDE) | Pubchem | |
| AB | Pubchem | |
| Aminasine | NIST | |
| Aminazin | NIST | |
| Aminazin monohydrochloride | Pubchem | |
| Aminazine | NIST | |
| Ampliactil | NIST | |
| Ampliactil monohydrochloride | Pubchem | |
| Amplicitil | NIST | |
| Amplictil | NIST | |
| Apo Chlorpromazine Tab 100mg | DPD | |
| Apo Chlorpromazine Tab 25mg | DPD | |
| Apo Chlorpromazine Tab 50mg | DPD | |
| CPZ | NIST | |
| CPZ (van) | NCI | |
| Chlor-PZ | NIST | |
| Chlor-promanyl | NIST | |
| Chloractil | Pubchem | |
| Chlorazine | Pubchem | |
| Chlordelazin | Pubchem | |
| Chlordelazine | Pubchem | |
| Chlorderazin | NIST | |
| Chloro-2-dimethylamino-3 propyl-10 phenothiazine | NIST | |
| Chloro-3 (dimethylamino-3 propyl)-10 phenothiazine | Pubchem | |
| Chloro-3 (dimethylamino-3 propyl)-10 phenothiazine (FRENCH) | NCI | |
| Chloro-3 (dimethylamino-3 propyl)-10 phenothiazine [French] | Pubchem | |
| Chloropromazine | NIST | |
| Chlorpromados | NIST | |
| Chlorpromazin | NIST | |
| Chlorpromazine (usp/inn) | Pubchem | |
| Chlorpromazine Hcl Inj 25mg/Ml Usp | DPD | |
| Chlorpromazine [usan:inn:ban] | Pubchem | |
| Chlorpromazine hydrochloride | Pubchem | |
| Chlorpromazine hydrochloride injection | DPD | |
| Chlorpromazinium chloride | Pubchem | |
| Chlorpromazinum | Pubchem | |
| Chlorpromazinum [inn-latin] | Pubchem | |
| Chlropromados | Pubchem | |
| Clorpromazina | NIST | |
| Clorpromazina [inn-spanish] | Pubchem | |
| Clorpromazina [italian] | Pubchem | |
| Contomin | NIST | |
| Cromedazine | NIST | |
| Elmarin | NIST | |
| Esmind | NIST | |
| Fenactil | NIST | |
| Fenactil monohydrochloride | Pubchem | |
| Fenaktyl | NIST | |
| Flavin mononucleotide semiquinone | Pubchem | |
| Fraction | Pubchem | |
| Fraction ab | NIST | |
| Hebanil | Pubchem | |
| Hibanil | NIST | |
| Hibernal | NIST | |
| Hybernal | Pubchem | |
| Klorproman | Pubchem | |
| Klorpromex | Pubchem | |
| Largactil | NIST | |
| Largactilothiazine | NIST | |
| Largactyl | NIST | |
| Lomazine | Pubchem | |
| Lopac-C-8138 | Pubchem | |
| Megaphen | NIST | |
| N-(3-Dimethylaminopropyl)-3-chlorophenothiazine | Pubchem | |
| Neurazine | Pubchem | |
| Norcozine | Pubchem | |
| Novo-Chlorpromazine Tab 100mg | DPD | |
| Novo-Chlorpromazine Tab 25mg | DPD | |
| Novo-Chlorpromazine Tab 50mg | DPD | |
| Novomazina | NIST | |
| Pentanitrine | NIST | |
| Phenactyl | NIST | |
| Phenathyl | NIST | |
| Phenothiazine | Pubchem | |
| Phenothiazine hydrochloride | Pubchem | |
| Phenothiazine, 2-chloro-10-(3-(dimethylamino)propyl)- | Pubchem | |
| Phenothiazine, 2-chloro-10-[3-(dimethylamino)propyl]- | NIST | |
| Phenothiazine, {2-chloro-10-[3-(dimethylamino)propyl]-} | NCI | |
| Plegomasine | NIST | |
| Plegomazin | NIST | |
| Prazil | NIST | |
| Prazilpromactil | NIST | |
| Proma | NIST | |
| Promachel | Pubchem | |
| Promacid | Pubchem | |
| Promactil | NIST | |
| Promapar | Pubchem | |
| Promazil | NIST | |
| Promexin | Pubchem | |
| Propaphen | Pubchem | |
| Propaphenin | NIST | |
| Prozil | NIST | |
| Prozin | NIST | |
| Psychozine | NIST | |
| Sanopron | NIST | |
| Sonazine | Pubchem | |
| Thiazenone | NIST | |
| Thorazine | NIST | |
| Thorazine (TN) | Pubchem | |
| Thorazine hydrochloride | Pubchem | |
| Thorazine suppositories | Pubchem | |
| Torazina | NIST | |
| Tranzine | Pubchem | |
| UNII-U42B7VYA4P | Pubchem | |
| Unitensen | Pubchem | |
| WLN: T C666 BN ISJ B3N1&1 EG | Pubchem | |
| Wintermin | NIST | |
| [3-(2-Chloro-phenothiazin-10-yl)-propyl]-dimethyl-amine | Pubchem | |
| {2-Chloro-10-[3-(dimethylamino)propyl]phenothiazine} | NCI | |
| Brand Mixture | ||
| Not Available | Not Applicable | |
| CAS | ||
| 50-53-3 | DrugBank | |
| InChI Identifier | ||
InChI=1/C17H19ClN2S/c1-19(2)10-5-11-20-14-6-3-4-7-16(14)21-17-9-8 -13(18)12-15(17)20/h3-4,6-9,12H,5,10-11H2,1-2H3 |
World Wide Molecular Matrix | |
| IUPAC | ||
| 3-(2-chlorophenothiazin-10-yl)-N,N-dimethylpropan-1-amine | DrugBank | |
| Chemical Formula | ||
| C17H19ClN2S | PubChem | |
| Chemical Structure | ||
![]() |
Molconvert | |
| Average Molecular Weight (g/mol) | ||
| 318.864160 | BioSpider | |
| Monoisotopic Molecular Weight (g/mol) | ||
| 318.095750 | BioSpider | |
| SMILES (Isomeric) | ||
Clc2cc1N(c3c(Sc1cc2)cccc3)CCCN(C)C |
ChemSpider | |
| SMILES (Canonical) | ||
CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl |
PubChem | |
| Kegg Drug | ||
| D00270 | DrugBank | |
| Kegg Compound | ||
| C06906 | DrugBank | |
| Pubchem Compound ID | ||
| 2726 | DrugBank | |
| Pubchem Substance ID | ||
| 10347421 | Pubchem | |
| 10486704 | Pubchem | |
| 10524433 | Pubchem | |
| 10588932 | Pubchem | |
| 11110990 | Pubchem | |
| 11110991 | Pubchem | |
| 11120337 | Pubchem | |
| 11120825 | Pubchem | |
| 11121313 | Pubchem | |
| 11335799 | Pubchem | |
| 11361038 | Pubchem | |
| 11363036 | Pubchem | |
| 11364725 | Pubchem | |
| 11365598 | Pubchem | |
| 11367287 | Pubchem | |
| 11368160 | Pubchem | |
| 11369849 | Pubchem | |
| 11371331 | Pubchem | |
| 11372890 | Pubchem | |
| 11373945 | Pubchem | |
| 11375449 | Pubchem | |
| 11376322 | Pubchem | |
| 11378013 | Pubchem | |
| 11462010 | Pubchem | |
| 11466092 | Pubchem | |
| 11467212 | Pubchem | |
| 11484847 | Pubchem | |
| 11485904 | Pubchem | |
| 11488972 | Pubchem | |
| 11490162 | Pubchem | |
| 11492098 | Pubchem | |
| 11493956 | Pubchem | |
| 12014508 | Pubchem | |
| 148556 | Pubchem | |
| 14923746 | Pubchem | |
| 24398080 | Pubchem | |
| 26611657 | Pubchem | |
| 26680205 | Pubchem | |
| 26747094 | Pubchem | |
| 26747095 | Pubchem | |
| 26751620 | Pubchem | |
| 26751621 | Pubchem | |
| 29221882 | Pubchem | |
| 36519388 | Pubchem | |
| 36519771 | Pubchem | |
| 4332427 | Pubchem | |
| 441206 | Pubchem | |
| 46508395 | Pubchem | |
| 47364978 | Pubchem | |
| 47364979 | Pubchem | |
| 47588791 | Pubchem | |
| 47588792 | Pubchem | |
| 47662070 | Pubchem | |
| 47662071 | Pubchem | |
| 47736247 | Pubchem | |
| 47885204 | Pubchem | |
| 47959525 | Pubchem | |
| 48034879 | Pubchem | |
| 48184787 | Pubchem | |
| 48184788 | Pubchem | |
| 48184789 | Pubchem | |
| 48415768 | Pubchem | |
| 49698686 | Pubchem | |
| 50006354 | Pubchem | |
| 50100209 | Pubchem | |
| 50104291 | Pubchem | |
| 53801065 | Pubchem | |
| 56312009 | Pubchem | |
| 56312819 | Pubchem | |
| 56313671 | Pubchem | |
| 56313735 | Pubchem | |
| 56314330 | Pubchem | |
| 57287810 | Pubchem | |
| 57321419 | Pubchem | |
| 57825665 | Pubchem | |
| 602724 | Pubchem | |
| 747132 | Pubchem | |
| 7847336 | Pubchem | |
| 78487736 | Pubchem | |
| 7978926 | Pubchem | |
| 81091924 | Pubchem | |
| 8149253 | Pubchem | |
| 8151764 | Pubchem | |
| 841999 | Pubchem | |
| 85209020 | Pubchem | |
| 9123 | Kegg | |
| OMIM ID | ||
| Not Available | Not Applicable | |
| ChEBI | ||
| 3647 | Chebi | |
| BioCyc | ||
| Not Available | Not Applicable | |
| PharmGKB | ||
| PA448964 | DrugBank | |
| HET ID | ||
| Not Available | Not Applicable | |
| DPD ID | ||
| 00232807 | DPD | |
| 00232823 | DPD | |
| 00232831 | DPD | |
| 00312673 | DPD | |
| 00312681 | DPD | |
| 00312703 | DPD | |
| 00743518 | DPD | |
| 01933272 | DPD | |
| Rxlist Link | ||
| http://www.rxlist.com/cgi/generic3/chlorpromazine.htm | DrugBank | |
| Wikipedia | ||
| chlorpromazine | Wikipedia | |
| Pdr Health Link | ||
| http://www.pdrhealth.com/drugs/rx/rx-mono.aspx?contentFileName=chl2054.html&contentName=Chlorpromazine&contentId=164 | PDRHealth | |
| Melting Point | ||
| < 25 oC | PhysProp | |
| State | ||
| Solid | BioSpider | |
| MSDS Link | ||
| 1257877233.pdf | www.sciencelab.com | |
| FDA Label | ||
| Not Available | Not Applicable | |
| Experimental Water Solubility | ||
| 0.00255 mg/mL at 24 oC [YALKOWSKY,SH & DANNENFELSER,RM (1992)] | PhysProp | |
| Predicted Water Solubility | ||
| 0.00417 mg/mL [Predicted by ALOGPS] | Alogps | |
| Experimental LogP | ||
| 5.41 [AVDEEF,A (1995)] | PhysProp | |
| Predicted LogP | ||
| 5.18 [Predicted by ALOGPS] | Alogps | |
| pKa | ||
| 9.3 | DrugBank | |
| SDF File | ||
| 1257877181.sdf | Pubchem | |
| Mol File | ||
| 1257877164.mol | Molconvert | |
| Pdb File | ||
| 1257877237.pdb | Molconvert | |
| Mass Spec File | ||
| Not Available | Not Applicable | |
| Associated Disorder | ||
| Not Available | Not Applicable | |
| Pathway | ||
| map07028 - Antipsychotics | Kegg Drug | |
| map07029 - Phenothiazines | Kegg Drug | |
| map07212 - Histamine receptor antagonists | Kegg Drug | |
| map07213 - Dopamine receptor agonists/antagonists | Kegg Drug | |
| Category | ||
| Not Available | Not Applicable | |
| ATC Code | ||
| N05AA01 | DPD | |
| AHFS Code | ||
| 28:16.08.24 | DPD | |
| Schedule | ||
| SCHEDULE F (Canada) | DPD | |
| Indication | ||
| Chlorpromazine is able to cross the placental barrier and it has been shown that drug doses higher than 500 mg daily in late pregnancy are associated with an increased incidence of respiratory distress in newborns. One case study reported that a newborn who was not breast fed but was exposed to CPZ in utero had detectably large amounts of the drug in its urine. This indicated the drug can in fact cross the placental barrier and is slowly cleared out of the body due to the infant's immature liver. Pregnant women and nursing mothers should thus be advised of the effects of CPZ on their newborn's health. | Wikipedia | |
| Chlorpromazine is occasionally used off-label for treatment of severe migraine. Sometimes it is used in small doses to improve the nausea that opioid-treated cancer patients encounter and to intensify and prolong the analgesic action of the opioids given. It remains controversial whether or not chlorpromazine has its own analgesic properties. Analgesic properties may result from a central action on the hypothalamus; the patient may feel pain much less than before. Other mechanisms may be an interaction with opioid receptors centrally and/or in the spinal cord. Some experts even say that chlorpromazine, like other phenothiazines, may even have antianalgesic properties. Chlorpromazine has been proposed as useful in newborns for the treatment of opioid withdrawal, if the mother was opioid-dependent. The latter indication remains highly controversial. | Wikipedia | |
| Chlorpromazine is primarily used as an antiemetic in dogs and cats. It is also sometimes used as a preanesthetic and muscle relaxant in cattle, swine, sheep, and goats. It is generally contraindicated for use with horses, due to a high incidence of ataxia and altered mentation. Its use in food-producing animals has been banned in the EU according to the Council's regulation 2377/90. Dosage and administration | Wikipedia | |
| Differential expression of various CYP isoforms in specific brain locations leads to the conclusion that antipsychotic drugs could be metabolized to different products in different regions of the brain. The varying levels of expression of the CYP isoforms between individuals and for each particular antipsychotic as well as the possibility of differential metabolism in the brain provides one possible reason why there is such a wide range of adverse effects and therapeutic effects of chlorpromazine and the other antipsychotic drugs in the population of patients currently using. | Wikipedia | |
| For the treatment of schizophrenia, control nausea and vomiting, For relief of restlessness and apprehension before surgery, adjunct in the treatment of tetanus, control the manifestations of the manic type of manic-depressive illness. | DrugBank | |
| It can be used to treat amphetamine overdose. | Wikipedia | |
| The lowest dosage compatible with good therapeutic effect should be given. Dosage in ambulatory patients should be particularly low (minimizing sedation and hypotension). Intravenous injection of undiluted solution is contraindicated due to risk of massive fall in blood pressure, cardiovascular collapse. For i.v.-infusion of dilutions the (hospitalized) patient should be lying and the infusion rate should be as slow as possible. Afterwards the patient should rest in the lying position for at least 30 minutes. | Wikipedia | |
| Pharmacology | ||
| Chlorpromazine is a psychotropic agent indicated for the treatment of schizophrenia. It also exerts sedative and antiemetic activity. Chlorpromazine has actions at all levels of the central nervous system-primarily at subcortical levels-as well as on multiple organ systems. Chlorpromazine has strong antiadrenergic and weaker peripheral anticholinergic activity | DrugBank | |
| Mechanism Of Action | ||
| Additionally, chlorpromazine is a presynaptic inhibitor of dopamine reuptake, which may lead to (mild) antidepressive and antiparkinsonian effects. This action could also account for psychomotor agitation and amplification of psychosis (very rarely noted in clinical use). | Wikipedia | |
| Because it acts on so many receptors, chlorpromazine is often referred to as a "dirty drug", whereas the atypical antipsychotic amisulpride, for example, acts only on central D2 and D3 receptors and is therefore a "clean drug". Research still needs to be done to understand the implications of this fact. Adverse effects | Wikipedia | |
| Chlorpromazine acts as an antagonist (blocking agent) on different postsynaptic receptors: dopamine receptors (subtypes D1, D2, D3 and D4), which account for its different antipsychotic properties on productive and unproductive symptoms;in the mesolimbic dopamine system accounts for the antipsychotic effect whereas the blockade in the nigrostriatal system produces the extrapyramidal effects serotonin receptors (5-HT1 and 5-HT2), with anxiolytic, and antiaggressive properties as well as an attenuation of extrapyramidal side effects, but also leading to weight gain, fall in blood pressure, sedation and ejaculation difficulties), histamine receptors (H1 receptors, accounting for sedation, antiemetic effect, vertigo, fall in blood pressure and weight gain), α1- and α2-adrenergic receptors (antisympathomimetic properties, lowering of blood pressure, reflex tachycardia, vertigo, sedation, hypersalivation and incontinence as well as sexual dysfunction, but may also attenuate pseudoparkinsonism—controversial), and M1 and M2 muscarinic acetylcholine receptors (causing anticholinergic symptoms such as dry mouth, blurred vision, constipation, difficulty or inability to urinate, sinus tachycardia, electrocardiographic changes and loss of memory, but the anticholinergic action may attenuate extrapyramidal side effects). | Wikipedia | |
| Chlorpromazine acts as an antagonist (blocking agent) on different postsysnaptic receptors -on dopaminergic-receptors (subtypes D1, D2, D3 and D4 - different antipsychotic properties on productive and unproductive symptoms), on serotonergic-receptors (5-HT1 and 5-HT2, with anxiolytic, antidepressive and antiaggressive properties as well as an attenuation of extrapypramidal side-effects, but also leading to weight gain, fall in blood pressure, sedation and ejaculation difficulties), on histaminergic-receptors (H1-receptors, sedation, antiemesis, vertigo, fall in blood pressure and weight gain), alpha1/alpha2-receptors (antisympathomimetic properties, lowering of blood pressure, reflex tachycardia, vertigo, sedation, hypersalivation and incontinence as well as sexual dysfunction, but may also attenuate pseudoparkinsonism - controversial) and finally on muscarinic (cholinergic) M1/M2-receptors (causing anticholinergic symptoms like dry mouth, blurred vision, obstipation, difficulty/inability to urinate, sinus tachycardia, ECG-changes and loss of memory, but the anticholinergic action may attenuate extrapyramidal side-effects). Additionally, Chlorpromazine is a weak presynaptic inhibitor of Dopamine reuptake, which may lead to (mild) antidepressive and antiparkinsonian effects. This action could also account for psychomotor agitation and amplification of psychosis (very rarely noted in clinical use). | DrugBank | |
| Chlorpromazine is a very effective antagonist of D2 dopamine receptors and similar receptors, such as D3 and D5. Unlike most other drugs of this genre, it also has a high affinity for D1 receptors. Blocking these receptors causes diminished neurotransmitter binding in the forebrain, resulting in many different effects. Dopamine, unable to bind with a receptor, causes a feedback loop that causes dopaminergic neurons to release more dopamine. Therefore, upon first taking the drug, patients will experience an increase in activity of dopaminergic neural activity. Eventually, dopamine production of the neurons will drop substantially and dopamine will be removed from the synaptic cleft. At this point, neural activity decreases greatly; the continual blockade of receptors only compounds this effect. | Wikipedia | |
| Chlorpromazine is an antagonist to H1 receptors (provoking antiallergic effects), H2 receptors (reduction of forming of gastric juice), M1 and M2 receptors (dry mouth, reduction in forming of gastric juice) and some 5-HT receptors (different anti-allergic/gastrointestinal actions). | Wikipedia | |
| In addition to influencing the neurotransmitters dopamine, serotonin, epinephrine, norepinephrine, and acetylcholine it has been reported that antipsychotic drugs could achieve glutamatergic effects. This mechanism involves direct effects on antipsychotic drugs on glutamate receptors. By using the technique of functional neurochemical assay chlorpromazine and phenothiazine derivatives have been shown to have inhibitory effects on NMDA receptors that appeared to be mediated by action at the Zn site. It was found that there is an increase of NMDA activity at low concentrations and suppression at high concentrations of the drug. No significant difference in glutamate and glycine activity from the effects of chlorpromazine were reported. Further work will be necessary to determine if the influence in NMDA receptors by antipsychotic drugs contributes to their effectiveness. Peripheral effects | Wikipedia | |
| Absorption | ||
| Bioavailability : Only about 32% of the administered dose is available to the systemic circulation in the active form | Wikipedia | |
| Chlorpromazine is slowly absorbed from the intramuscular injection site with the peak plasma concentration occurring 6–24 hours after administration of the drug | Wikipedia | |
| Intramuscular administration is generally not recommended due to the unpredictable absorption and hence widely varying effect | Wikipedia | |
| Oral, 30 to 50% (interindividual variations 10–70%) | Wikipedia | |
| Over time and multiple administrations, bioavailability may drop to 20% | Wikipedia | |
| The anticholinergic properties only slightly influence chlorpromazine's absorption from the gastrointestinal tract, compared to other antipsychotics such as fluphenazine | Wikipedia | |
| The oral bioavailability is estimated to be 30–50% that of intramuscular doses and about 10% that of intravenous doses due to extensive first pass metabolism in the liver | Wikipedia | |
| Protein Binding | ||
| 40% | DrugBank | |
| Approximately 95-98% of the drug is bound in the plasma; 85% of the drug is bound to the plasma protein albumin | Wikipedia | |
| Half Life | ||
| 16 to 30 hours. In long term treatment, CPZ induces its own metabolism | Wikipedia | |
| Biotransformation | ||
| Differential expression of various CYP isoforms in specific brain locations leads to the conclusion that antipsychotic drugs could be metabolized to different products in different regions of the brain | Wikipedia | |
| Toxicity | ||
| Agitation, coma, convulsions, difficulty breathing, difficulty swallowing, dry mouth, extreme sleepiness, fever, intestinal blockage, irregular heart rate, low blood pressure, restlessness | DrugBank | |
| Cardiac arrhythmia and apparent sudden death have been associated with therapeutic doses of chlorpromazine, however they are rare cases | Wikipedia | |
| Furthermore if plasma levels are monitored then any form of drug induced toxicity can be suspected as well as controlling for the lack of compliance by the patient. Chlorpromazine impairs the metabolism of tricyclic antidepressants which can thus increase the risk of toxicity. Combination with other antidopaminergic agents such as metoclopramide and prochlorperazine increases the risk of extrapyramidal symptom effects. Chlorpromazine can enhance the central nervous system depression produced by other CNS depressent drugs | Wikipedia | |
| Furthermore, the seizure risk rises markedly to a range of 4 to 30% in patients who have taken an overdose | Wikipedia | |
| Other uses It has also been used in porphyria and as part of tetanus treatment. It still is well recommended for short term management of severe anxiety and aggressive episodes. Resistant and severe hiccups, severe nausea/emesis and preanesthetic conditioning have been other indications in the past. It can be used to treat amphetamine overdose. It has also been used to stimulate the appetite of patients with eating disorders, as most anti-psychotics make patients feel hungrier. Off-label and controversial uses Chlorpromazine is occasionally used off-label for treatment of severe migraine | Wikipedia | |
| Plumb's Veterinary Drug Handbook (Blackwell, 5th Edition, 2005) "Methods of Execution" | Wikipedia | |
| Research confirms a significant risk of blindness from continued use of chlorpromazine, as well as other optological defects such as color blindness and benign pigmentation of the cornea. Chlorpromazine is the antipsychotic drug with the highest rates (0.5% to 1%) of liver toxicity of the cholestatic type. The sedation effect combined with indifference to physical stimuli, anecdotally known as the "thorazine shuffle," has long been associated with the drug | Wikipedia | |
| Some side effects seem to appear more frequently during the first months of therapy (sedation, hypotension, liver damage) while others do not (e.g | Wikipedia | |
| The dose required to treat psychotic symptoms is smaller and therefore less sedative than is commonly depicted. In some rare cases psychosis or death can result from the paradoxical lowering of blood pressure, or death due to cardiac arrest attributed to dysrhythmia. Cardiotoxic effects of phenothiazines in overdose are similar to that of the tricyclic antidepressants | Wikipedia | |
| These major cardiac arrhythmias that are lethal are a potential hazard even in patients without heart disease who are receiving therapeutic doses of antipsychotic drugs | Wikipedia | |
| http://www.clarkprosecutor.org/html/death/methods.htm | Wikipedia | |
| Dosage | ||
| Liquid (Intravenous) | DPD | |
| Tablet (Oral) | DPD | |
| Patient Information | ||
| 1257877268.html | RxList | |
| Interactions | ||
| Not Available | Not Applicable | |
| Contraindications | ||
| Not Available | Not Applicable | |
| Targets | ||
P02768[ UniProt | Analyze ] |
DrugBank | |
P14416[ UniProt | Analyze ] |
DrugBank | |
P28223[ UniProt | Analyze ] |
DrugBank |


