Hydroxyzine

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Prescription and use

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Hydroxyzine is both an antihistamine and anxiolytic (see below) and its use as a mild tranquilizer is especially common in dentistry and it retains some popularity in obstetrics, where for many years it was especially preferred for its ability to boost the effectiveness of opioids as well as permit later use of scopolamine or benzodiazepines better than other drugs might. recliner massage

Hydroxyzine is prescribed when the onset of an organic disease state manifests through anxiety, as general anxiety disorder, or in other more serious cases as psychoneurosis, and is therefore prescribed as a means of regulating normal function. Hydroxyzine has shown to be as effective as the benzodiazepine drug bromazepam in the treatment of generalised anxiety disorder. Hydroxyzine can also be used for the treatment of allergic conditions, such as chronic urticaria, atopic or contact dermatoses, and histamine-mediated pruritus. These have also been confirmed in both recent and past studies to have no adverse effects on the liver, blood, nervous system or urinary tract.[citation needed] chair cushion massager

Use of hydroxyzine for premedication as a sedative has no effects on belladonna alkaloids, such as atropine, but may, following general anesthesia, potentiate meperidine and barbiturates, and use in pre-anesthetic adjunctive therapy should be modified depending upon the state of the individual.[citation needed]

In other cases, the usage of hydroxyzine is as a form of non-barbiturate tranquilizer used in the pre-operative sedation and treatment of neurological disorders, such as psychoneurosis and other forms of anxiety or tension states.

For dentistry and obstetrics as well as other surgeries and procedures and acute pain situations like accidents, hydroxyzine is useful as a first line anxiolytic and opioid adjunct because it lacks both antagonism and synergy with benzodiazepines and scopolamine, allowing either of these agents to be used simultaneously or later in the procedure if need be.

Hydroxyzine is not thought to be an effective treatment for anxiety if used for a period of over 4 months, and it is therefore a prerequisite of any medical professional prescribing such drugs, to re-assess the usefulness for the individual patient. Rather than its use as an anxiety-reducing agent, hydroxyzine should be reconsidered if the patient has more intense anxiety or other psychoneurosis; then other compounds specifically designed for such conditions should be considered.[citation needed]

Animal research

Aside from its prescription as an antihistamine, hydroxyzine has also shown slight possibilities for use in other species, such as dogs, from results and effects observed in rats with "learned helplessness" induced through the use of random inescapable shocks (max 0.8 mA) administered in 1 minute intervals for a period of 15 seconds for an hour. After the condition was induced, rats were then given a conditioned stimulus of a light, and shocked if unable to move to safety from the area producing the current within 3 seconds. Those unable to move were determined as having a conditioned stimulus of expecting shocks from the initial random condition.

In the initial treatment to this condition, rats were given hydroxyzine as a curative treatment for the shocks received and as a treatment for the prevention of learned helplessness by injection beforehand; results indicating that hydroxyzine decreased the overall amount of escape failures by a similar amount to those observed in diazepam, which achieved similar results, however, with side effects of amnesia. Despite the fact that hydroxyzine clearly increased the ability of the rats to avoid stimuli, it had almost no effect on the rats' ability to respond to the shocks nor remove "stress" after exposure to shocks.

Clinical description

Metabolism and pharmacokinetics

Hydroxyzine can be administered orally or via intramuscular injection. When given orally, hydroxyzine is rapidly absorbed from the gastro-intestinal tract. The effect of hydroxyzine is notable in 30 minutes.

Pharmacokinetically, hydroxyzine is rapidly absorbed and distributed in oral and intramuscular administration, and is metabolised in the liver; the main metabolite (45%) through oxidation of the alcohol moiety to a carboxylic acid, is cetirizine and overall effects are observed within one hour of administration. It has a half-life observed on average of around 710 hours in adults, 67 hours in children, and 1821 hours in the elderly, or those with renal insufficiency, with higher concentrations found in the skin than in the plasma. Cetirizine, although less sedating, is non-dialyzable and possesses similar anti-histaminergic properties. "In animals, hydroxyzine and its metabolites are excreted in feces via biliary elimination." "The extent of renal excretion of VISTARIL has not been determined" Administration in geriatrics differs from the administration of hydroxyzine in younger patients; according to the FDA, there have not been significant studies made (2004), which include population groups over 65, which provide a distinction between elderly aged patients and other younger groups. Hydroxyzine should be administered carefully in the elderly with consideration given to possible reduced elimination.[citation needed] Similarly, the use of sedating drugs alongside hydroxyzine can cause over-sedation and confusion if administered in large amountsny form of treatment alongside sedatives should be done under supervision of the patient.[citation needed]

Contraindications

The administration of hydroxyzine in large amounts by ingestion or intramuscular administration during the onset of pregnancy can cause fetal abnormalitieshen administered to pregnant rats, mice and rabbits, hydroxyzine caused abnormalities with doses significantly above that of the human therapeutic range.[citation needed] In terms of humans, a significant dose has not yet been established in studies, and by default, the FDA has introduced contraindication guidelines in regard to hydroxyzine. Similarly the use in those at risk from or showing previous signs of hypersensitivity is also contraindicated.[citation needed]

Other contraindications include the administration of hydroxyzine alongside depressants and other compounds which affect the central nervous system. and if absolutely necessary, it should only be administered concomitantly in small doses. If administered in small doses with other substances, such as mentioned, then patients should refrain from using dangerous machinery, motor vehicles or any other practice requiring absolute concentration, in accordance with safety law.

Studies have also been conducted which show that long-term prescription of hydroxyzine can lead to tardive dyskinesia after years of use, but effects related to dyskinesia have also anecdotally been reported after periods of 7.5 months, such as continual head rolling, lip licking and other forms of athetoid movement. In certain cases, elderly patients' previous interactions with phenothiazine derivatives or pre-existing neuroleptic treatment may have had some contribution towards dyskinesia at the administration of hydroxyzine due to hypersensitivity caused due to the prolonged treatment, and therefore some contraindication is given to the short-term administration of hydroxyzine to those with previous phenothiazine use.

Adverse reactions

For a full list of side effects, consult the full technical specification of hydroxyzine.

Several reactions have been noted in manufacturer guidelines deep sleep, incoordination and dizziness have been reported in children and adults, as well as others such as hypotension, tinnitus and headaches. Gastro-intestinal effects have also been observed, as well as less serious effects such as dryness of the mouth and constipation caused by antimuscarinic properties of hydroxyzine.

Central nervous system problems such as hallucinations or confusion have been observed in rare cases, attributed mostly to overdosage. Such properties have been attributed to hydroxyzine in several cases, particularly in patients treated for neuropsychological disorders, as well as in cases where overdoses have been observed. While there are reports of the "hallucinogenic" or "hypnotic" properties of hydroxyzine, several clinical data trials have not reported such side effects from the sole consumption of hydroxyzine, but rather, have described its overall calming effect described through the stimulation of areas within the formatio reticularis. The description of hallucinogenic or hypnotic properties have been described as being an additional effect from overall central nervous system suppression by other CNS agents, such as lithium or alcohol.

The effect of hydroxyzine has also been tested on the ability of humans in the registration and storage of memory, and was used in comparison with relatively safe drugs, such as hydroxyzine, to illustrate the effects of benzodiazepines, which are thought to have adverse effects on the capacity of memory storage. Hydroxyzine was found to have no adverse effects on memory in relation to lorazepam, which caused several deficiencies in the capacity of memory storage.

In a comparative study with lorazepam on memory effects, patients who had taken hydroxyzine experienced sedative effects similar to drowsiness, but recalled that they felt capable, attentive and able to continue with a memory test under these conditions. Conversely, those under the effects of lorazepam felt unable to continue due to the fact they felt out of control with its effects; 8 out of 10 patients describing tendencies of problems with balance and control of simple motor functions.

Somnolence with or without vivid dreams or nightmares may occur in users with antihistamine sensitivities in combination with other CNS depressants. Hydroxyzine exhibits anxiolytic and sedative properties in many psychiatric patients. Other studies have suggested that hydroxyzine acts as an acute hypnotic, reducing sleep onset latency and increasing sleep duration also showing that some drowsiness did occur. This was observed more in female patients, who also had greater hypnotic response.

Some users may report shortness of breath or wheezing, a result of a mild allergic reaction to the medication itself.

In contrast to drugs in the benzodiazepine class, (i.e. alprazolam, diazepam) which carry a potential for abuse and dependence, hydroxyzine is very unlikely to cause any dependence due to its relative strength compared to other substances.

Because of potential for more severe side effects, this drug is on the list to avoid in the elderly. (See NCQA HEDIS Measure: Use of High Risk Medications in the Elderly, http://www.ncqa.org/Portals/0/Newsroom/SOHC/Drugs_Avoided_Elderly.pdf).

References

^ a b RxList, et al. (2004)

^ Llorca PM, Spadone C, Sol O, et al. (November 2002). "Efficacy and safety of hydroxyzine in the treatment of generalized anxiety disorder: a 3-month double-blind study". J Clin Psychiatry 63 (11): 10207. PMID 12444816. http://www.psychiatrist.com/privatepdf/2002/v63n11/v63n1112.pdf. 

^ a b United States Food & Drug Administration, (2004), p1

^ a b c Dolan, C. M., (1958)

^ a b c d e f g United States Food & Drug Administration, (2004), p2

^ a b Porsolt, R. D.; P. Martin, A. Lenegre, S. Frornage, and C.E. Giurgea (1989), p229

^ a b c Porsolt, R. D.; P. Martin, A. Lenegre, S. Frornage, and C.E. Giurgea (1989), p228

^ a b Porsolt, R. D.; P. Martin, A. Lenegre, S. Frornage, and C.E. Giurgea (1989), p230

^ a b c United States Food & Drug Administration, (2004), p3

^ a b c Clark, B. G., Araki, M., et al. (1976)

^ a b c UCB South-Africa, et al., (2004)

^ Anderson, P. O., Knoben, J. E., et al. (2002), p794-796

^ Brabander, A. DE, Debert, W., (1990), p1

^ a b Brabander, A. DE, Debert, W., (1990), p3

^ Alford, C.; N. Rombautt, J. Jones, S. Foley, C. Idzikowskit and I. Hindmarch (1992).

Print sources

Hutcheon, D. E.; D.L. Morris, A. Scriabine (December 1956). "Cardiovascular action of hydroxyzine (Atarax)". J Pharmacol Exp Ther. 118 (4): 451460. PMID 13385806. 

Dolan, C. M. (June 1958). "Management of emotional disturbances -- Use of Hydroxyzine (Atarax) in General Practice". Calif Med. 88 (6): 443444. PMID 13536863. PMC 1512309. http://www.pubmedcentral.nih.gov/picrender.fcgi?artid=1512309&blobtype=pdf. Retrieved 2007-03-09. 

Pfizer Labs, Division of Pfizer Inc, NY, NY 10017 (2004) (pdf). Vistaril (hydroxyzine pamoate) Capsules and Oral Suspension. United States Food and Drug Administration. http://www.fda.gov/cder/ogd/rld/11795s16.pdf. Retrieved 2007-03-09. 

Anderson, Philip O.; James E. Knoben, William G. Troutman (2002). Handbook of Clinical Drug Data. McGraw-Hill Medical. ISBN 0071363629. 

de Brabander, A.; W. Deberdt (1990). "Effect of Hydroxyzine on Attention and Memory". Human Psychopharmacology (John Wiley & Sons) 5 (4): 357362. doi:10.1002/hup.470050408. http://www3.interscience.wiley.com/cgi-bin/abstract/109710652/ABSTRACT?CRETRY=1&SRETRY=0. Retrieved 2007-03-09. 

Clark, B. G.; M. Araki, H. W. Brown (1982). "Hydroxyzine-Associated Tardive Dyskinesia". Ann Neurol. 11 (4): 435. doi:10.1002/ana.410110423. PMID 7103423. 

Porsolt, R. D.; P. Martin, A. Lenegre, S. Frornage, and C.E. Giurgea (1989). "Prevention of earned Helplessness in the Rat by Hydroxyzine". Drug Dev. Res. 17 (3): 227236. doi:10.1002/ddr.430170306. http://www3.interscience.wiley.com/cgi-bin/abstract/109670961/ABSTRACT?SRETRY=0. Retrieved 2007-03-10. 

Alford, C.; N. Rombautt, J. Jones, S. Foley, C. Idzikowskit and I. Hindmarch (1992). "Acute Effects of Hydroxyzine on Nocturnal Sleep and Sleep Tendency the Following Day: a C-EEG Study". Human Psychopharmacology 7 (1): 2535. doi:10.1002/hup.470070104. http://www3.interscience.wiley.com/cgi-bin/abstract/109711163/ABSTRACT. Retrieved 2007-03-10. 

Internet-based

RxList , et al. (2004). "Atarax Indications, Dosage, Storage, Stability". RxList - The internet drug index. http://www.rxlist.com/cgi/generic/hydrox_ids.htm. Retrieved 2007-03-09. 

Medscape (2004). "Vistaril Oral: Monograph - Hydroxyzine Hydrochloride, Hydroxyzine Pamoate". medscape.com. http://www.medscape.com/druginfo/monograph?cid=med&drugid=6144&drugname=Vistaril+Oral&monotype=monograph&print=1. Retrieved 2007-03-09. 

pfizer (2004). "Non-print version of vistaril fact sheet." (PDF). http://www.pfizer.com/pfizer/download/uspi_vistaril.pdf. Retrieved 2007-07-03. 

Drug information pamphlets

UCB South-Africa, et al., (2004). ATERAX 25 mg TABLETS; ATERAX 100 mg TABLETS; ATERAX SYRUP (Manufacturing guidance package insert) Pharmacare Ltd, (a division of Aspen Pharmacare Ltd)

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Anxiolytics (N05B)

GABAA PAMs

Benzodiazepine

Adinazolam Alprazolam Bretazenil Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam Ethyl Loflazepate Etizolam Fludiazepam Halazepam Imidazenil Ketazolam Lorazepam Medazepam Nordazepam Oxazepam Pinazepam Prazepam Tofisopam

Carbamates

Emylcamate Mebutamate Meprobamate (Carisoprodol, Tybamate) Phenprobamate Procymate

Nonbenzodiazepines

Abecarnil Adipiplon Alpidem CGS-9896 CGS-20625 Divaplon ELB-139 Etifoxine GBLD-345 Gedocarnil ICI-190,622 L-838,417 NS-2664 NS-2710 Ocinaplon Pagoclone Panadiplon Pipequaline RWJ-51204 SB-205,384 SL-651,498 TP-003 TP-13 TPA-023 Tracazolate Y-23684 ZK-93423

Others

Chlormezanone Etazolate Ethanol (Alcohol) Kavalactones (Kava Kava) Skullcap Valerenic Acid (Valerian)

2 VDCC Blockers

Gabapentin Pregabalin

5-HT1A Agonists

Azapirones: Buspirone Gepirone Tandospirone; Others: Flesinoxan Oxaflozane

H1 Antagonists

Diphenylmethanes: Captodiame Hydroxyzine; Others: Brompheniramine Chlorpheniramine Pheniramine

CRF1 Antagonists

Antalarmin CP-154,526 Pexacerfont Pivagabine

NK2 Antagonists

GR-159,897 Saredutant

MCH1 antagonists

ATC-0175 SNAP-94847

mGluR2/3 Agonists

Eglumegad

mGluR5 NAMs

Fenobam

TSPO agonists

DAA-1097 DAA-1106 Emapunil FGIN-127 FGIN-143

1 agonists

Afobazole Opipramol

Others

Benzoctamine Carbetocin Demoxytocin Mephenoxalone Oxytocin Promoxolane Trimetozine WAY-267,464

v  d  e

Cholinergics

Receptor

Ligands

mAChR

Agonists: 77-LH-28-1 AC-42 AC-260,584 Aceclidine Acetylcholine AF30 AF150(S) AF267B AFDX-384 Alvameline AQRA-741 Arecoline Bethanechol Butyrylcholine Carbachol CDD-0034 CDD-0078 CDD-0097 CDD-0098 CDD-0102 Cevimeline cis-Dioxolane Ethoxysebacylcholine LY-593,039 L-689,660 LY-2,033,298 McNA343 Methacholine Milameline Muscarine NGX-267 Ocvimeline Oxotremorine PD-151,832 Pilocarpine RS86 Sabcomeline SDZ 210-086 Sebacylcholine Suberylcholine Talsaclidine Thiopilocarpine Vedaclidine VU-0029767 VU-0090157 VU-0152099 VU-0152100 VU-0238429 WAY-132,983 Xanomeline YM-796

Antagonists: 3-Quinuclidinyl Benzilate 4-DAMP Anisodamine Anisodine Atropine Atropine Methonitrate Benactyzine Benzatropine (Benztropine) Benzydamine BIBN 99 Biperiden Bornaprine CAR-226,086 CAR-301,060 CAR-302,196 CAR-302,282 CAR-302,368 CAR-302,537 CAR-302,668 CS-27349 Cyclobenzaprine Cyclopentolate Darifenacin DAU-5884 Dimethindene Dexetimide DIBD Dicyclomine (Dicycloverine) Ditran EA-3167 EA-3443 EA-3580 EA-3834 Elemicin Etanautine Etybenzatropine (Ethylbenztropine) Flavoxate Himbacine HL-031,120 Ipratropium J-104,129 Hyoscyamine Mamba Toxin 3 Mamba Toxin 7 Mazaticol Mebeverine Methoctramine Metixene Myristicin N-Ethyl-3-Piperidyl Benzilate N-Methyl-3-Piperidyl Benzilate Orphenadrine Otenzepad Oxybutynin PBID PD-102,807 Phenglutarimide Phenyltoloxamine Pirenzepine Piroheptine Procyclidine Profenamine RU-47,213 SCH-57,790 SCH-72,788 SCH-217,443 Scopolamine (Hyoscine) Solifenacin Telenzepine Tiotropium Tolterodine Trihexyphenidyl Tripitamine Tropatepine Tropicamide WIN-2299 Zamifenacin; Others: 1st Generation Antihistamines (Brompheniramine Chlorpheniramine, Cyclizine, Cyproheptadine, Dimenhydrinate, Diphenhydramine, Doxylamine, Hydroxyzine, Meclizine, Mepyramine/Pyrilamine, Phenindamine, Pheniramine, Tripelennamine, Triprolidine, etc) Tricyclic Antidepressants (Amitriptyline, Doxepin, Trimipramine, etc) Tetracyclic Antidepressants (Amoxapine, Maprotiline, etc) Typical Antipsychotics (Chlorpromazine, Thioridazine, etc) Atypical Antipsychotics (Clozapine, Olanzapine, Quetiapine, etc)

nAChR

Agonists: 5-HIAA A-84,543 A-366,833 A-582,941 A-867,744 ABT-202 ABT-418 ABT-560 ABT-894 Acetylcholine Altinicline Anabasine AR-R17779 Butyrylcholine Carbachol Cotinine Cytisine Decamethonium Desformylflustrabromine Dianicline Dimethylphenylpiperazinium Epibatidine Epiboxidine Ethoxysebacylcholine EVP-4473 EVP-6124 Galantamine GTS-21 Ispronicline Lobeline MEM-63,908 (RG-3487) Nicotine NS-1738 PHA-543,613 PHA-709,829 PNU-120,596 PNU-282,987 Pozanicline Rivanicline Sazetidine A Sebacylcholine SIB-1508Y SIB-1553A SSR-180,711 Suberylcholine TC-1698 TC-1734 TC-1827 TC-2216 TC-5214 TC-5619 TC-6683 Tebanicline Tropisetron UB-165 Varenicline XY-4083

Antagonists: 18-Methoxycoronaridine -Bungarotoxin -Conotoxin Alcuronium Anatruxonium Atracurium Bupropion (Amfebutamone) Chandonium Chlorisondamine Cisatracurium Coclaurine Coronaridine Dacuronium Decamethonium Dextromethorphan Dextropropoxyphene Dextrorphan Diadonium DHE Dimethyltubocurarine (Metocurine) Dipyrandium Dizocilpine (MK-801) Doxacurium Duador Esketamine Fazadinium Gallamine Hexafluronium Hexamethonium (Benzohexonium) Ibogaine Ketamine Kynurenic Acid Levacetylmethadol Malouetine Mecamylamine Memantine Methadone Methorphan (Racemethorphan) Methyllycaconitine Metocurine Mivacurium Morphanol (Racemorphanol) Neramexane Pancuronium Pempidine Pentamine Pentolinium Phencyclidine Pipecuronium Radafaxine Rapacuronium Rocuronium Surugatoxin Suxamethonium (Succinylcholine) Toxiferine Trimethaphan Tropeinium Tubocurarine Vecuronium

Reuptake

Inhibitors

Plasmalemmal

CHT Inhibitors

Hemicholinium-3 (Hemicholine)

Vesicular

VAChT Inhibitors

Vesamicol

Enzyme

Inhibitors

Anabolism

ChAT Inhibitors

1-(-Benzoylethyl)pyridinium 2-(-Naphthoyl)ethyltrimethylammonium 3-Chloro-4-stillbazole 4-(1-Naphthylvinyl)pyridine Acetylseco Hemicholinium-3 Acryloylcholine AF64A B115 BETA CM-54,903 N,N-Dimethylaminoethylacrylate N,N-Dimethylaminoethylchloroacetate

Catabolism

AChE Inhibitors

Reversible: Carbamates: Aldicarb Bendiocarb Bufencarb Carbaryl Carbendazim Carbetamide Carbofuran Chlorbufam Chloropropham Ethienocarb Ethiofencarb Fenobucarb Fenoxycarb Formetanate Furadan Ladostigil Methiocarb Methomyl Miotine Oxamyl Phenmedipham Pinmicarb Pirimicarb Propamocarb Propham Propoxur; Stigmines: Ganstigmine Neostigmine Phenserine Physostigmine Pyridostigmine Rivastigmine; Others: Ambenonium Donepezil Edrophonium Galantamine Huperzine A (Huperzia Serrata) Minaprine Tacrine Zanapezil

Irreversible: Organophosphates: Acephate Azinphos-Methyl Bensulide Cadusafos Chlorethoxyfos Chlorfenvinphos Chlorpyrifos Chlorpyrifos-Methyl Coumaphos Cyclosarin (GF) Demeton Demeton-S-Methyl Diazinon Dichlorvos Dicrotophos Diisopropyl Fluorophosphate (Guthion) Diisopropylphosphate Dimethoate Dioxathion Disulfoton EA-3148 Echothiophate Ethion Ethoprop Fenamiphos Fenitrothion Fenthion Fosthiazate GV Isofluorophate Isoxathion Malaoxon Malathion Methamidophos Methidathion Metrifonate Mevinphos Monocrotophos Naled Novichok Agent Omethoate Oxydemeton-Methyl Paraoxon Parathion Parathion-Methyl Phorate Phosalone Phosmet Phostebupirim Phoxim Pirimiphos-Methyl Sarin (GB) Soman (GD) Tabun (GA) Temefos Terbufos Tetrachlorvinphos Tribufos Trichlorfon VE VG VM VR VX; Others: Demecarium Onchidal (Onchidella Binneyi)

BChE Inhibitors

Many of the acetylcholinesterase inhibitors listed above act as butyrylcholinesterase inhibitors.

Others

Precursors

Choline (Lecithin) Citicoline Dimethylethanolamine Glycerophosphocholine Phosphatidylcholine Phosphatidylethanolamine Phosphorylcholine

Cofactors

Acetic Acid Acetyl-L-Carnitine Acetyl-Coenzyme A Vitamin B5 (Pantothenic Acid, Pantethine, Pantetheine, Panthenol)

Others

Acetylcholine Releasing Agents: -Latrotoxin -Bungarotoxin; Acetylcholine Release Inhibitors: Botulinum Toxin (Botox); Acetylcholinesterase Reactivators: Pralidoxime obidoxime

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Histaminergics

Receptor

Ligands

H1

Agonists: 2-Pyridylethylamine Betahistine Histamine HTMT UR-AK49

Antagonists: 1st Generation: 4-Methyldiphenhydramine Alimemazine Antazoline Azatadine Bamipine Benzatropine (Benztropine) Bepotastine Bromazine Brompheniramine Buclizine Captodiame Carbinoxamine Chlorcyclizine Chloropyramine Chlorothen Chlorpheniramine Chlorphenoxamine Cinnarizine Clemastine Clobenzepam Clocinizine Cyclizine Cyproheptadine Dacemazine Deptropine Dexbrompheniramine Dexchlorpheniramine Dimenhydrinate Dimetindene Diphenhydramine Diphenylpyraline Doxylamine Embramine Etybenzatropine (Ethylbenztropine) Etymemazine Histapyrrodine Hydroxyethylpromethazine Hydroxyzine Iproheptine Isopromethazine Isothipendyl Meclizine Mepyramine (Pyrilamine) Mequitazine Methafurylene Methapyrilene Methdilazine Moxastine Niaprazine Orphenadrine Oxatomide Oxomemazine Phenindamine Pheniramine Phenyltoloxamine Pimethixene Promethazine Propiomazine Pyrrobutamine Talastine Thenalidine Thenyldiamine Thiazinamium Thonzylamine Tolpropamine Tripelennamine Triprolidine; 2nd Generation: Acrivastine Astemizole Azelastine Cetirizine Clemizole Clobenztropine Dimebolin Ebastine Emedastine Epinastine Ketotifen Levocabastine Loratadine Mebhydrolin Mizolastine Olopatadine Rupatadine Setastine Terfenadine; 3rd Generation: Desloratadine Fexofenadine Levocetirizine; Miscellaneous: Tricyclic Antidepressants (Amitriptyline, Doxepin, Trimipramine, etc) Tetracyclic Antidepressants (Mianserin, Mirtazapine, etc) Serotonin Antagonists and Reuptake Inhibitors (Trazodone, Nefazodone) Typical Antipsychotics (Chlorpromazine, Thioridazine, etc) Atypical Antipsychotics (Clozapine, Olanzapine, Quetiapine, etc)

H2

Agonists: Amthamine Betazole Dimaprit Histamine HTMT Impromidine UR-AK49

Antagonists: Cimetidine Famotidine Lafutidine Metiamide Niperotidine Nizatidine Ranitidine Roxatidine

H3

Agonists: -Methylhistamine Cipralisant Histamine Imetit Immepip Immethridine Methimepip Proxyfan

Antagonists: A-349,821 A-423,579 ABT-239 Betahistine Burimamide Ciproxifan Clobenpropit Conessine GSK-189,254 Impentamine Iodophenpropit JNJ-5,207,852 MK-0249 NNC-38-1,049 SCH-79,687 Thioperamide Tiprolisant VUF-5,681

H4

Agonists: 4-Methylhistamine Histamine VUF-8,430

Antagonists: JNJ-7,777,120 Thioperamide VUF-6,002

Reuptake

Inhibitors

Plasmalemmal

.....

Vesicular

VMAT Inhibitors

Ibogaine Reserpine Tetrabenazine

Enzyme

Inhibitors

Anabolism

HDC Inhibitors

-FMH Brocresine Catechin Cyanidanol-3 McN-A-1293 ME Meciadanol Naringenin Thiazol-4-yimethoxyamine Tritoqualine Zy-15,029

Catabolism

HNMT Inhibitors

Amodiaquine BW-301U Diphenhydramine Harmaline Metoprine Quinacrine SKF-91,488 Tacrine

DAO Inhibitors

1,4-Diamino-2-butyne Aminoguanidine

Others

Precursors

L-Histidine

Cofactors

Vitamin B6 (Pyridoxine, Pyridoxamine, Pyridoxal Pyridoxal Phosphate)

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Piperazines

1-Cyclohexylpiperazine  2C-B-BZP  Acaprazine  Almitrine  Alnespirone  Aminoethylpiperazine  Amoxapine  Antrafenine  Aripiprazole  Atevirdine  Azaperone  Azimilide  Befuraline  Bifeprunox  Binospirone  BRL-15572  Buclizine  Buspirone  BZP  Chlorbenzoxamine  Chlorcyclizine  Cinepazet  Cinnarizine  Ciprofloxacin  Clocinizine  Clopenthixol  Clozapine  CPPene  Cyclizine  Dasatinib  DBL-583  DBZP  Dibenzylpiperazine  Diethylcarbamazine  Dimethylphenylpiperazinium  Dotarizine  DPI-3290  Dropropizine  EGIS-12233  Eltoprazine  Ensaculin  Etoperidone  Fipexide  Flesinoxan  Flibanserin  Flupentixol  Fluphenazine  Fluprazine  GBR-12935  Gepirone  HEPPS  Hexocyclium  Hydroxyzine  Imatinib  Indinavir  Ipsapirone  Itraconazole  JNJ-7777120  Ketoconazole  Levodropropizine  Lidoflazine  Loxapine  Lurasidone  Manidipine  MBZP  mCPP  MDBZP  Meclizine  MeOPP  Nefazodone  Niaprazine  Olanzapine  Opipramol  Oxatomide  Oxypertine  PB28  Perazine  Perospirone  Perphenazine  pFPP  Piberaline  Piperazine  PIPES  Pirenzepine  Piribedil  Posaconazole  Prochlorperazine  PRX-00023  Quipazine  Ranolazine  S-15535  SA 4503  SB-258,585  SB-271,046  SB-357,134  SB-399,885  Sildenafil  Tandospirone  TFMPP  Thiethylperazine  Thiothixene  Tirilazad  Trazodone  Trelibet  Trifluoperazine  Trimazosin  Trimetazidine  Vanoxerine  Vardenafil  Vesnarinone  Vilazodone  VUF-6002  WAY-100,135  WAY-100,635  Zalospirone  Zipeprol  Ziprasidone  Zuclopenthixol

Categories: Drugboxes which contain changes to watched fields | Analgesics | Antiemetics | Anxiolytics | H1 receptor antagonists | Sedatives | Piperazines | Organochlorides | Ethers | AlcoholsHidden categories: Articles needing additional references from August 2009 | All articles needing additional references | All articles with unsourced statements | Articles with unsourced statements from October 2009