HOME
The Info List - Antihistamines


--- Advertisement ---



Antihistamines are drugs which treat allergic rhinitis and other allergies.[1] Antihistamines can give relief when a person has nasal congestion, sneezing, or hives because of pollen, dust mites, or animal allergy.[1] Typically people take antihistamines as an inexpensive, generic, over-the-counter drug with few side effects.[1] As an alternative to taking an antihistamine, people who suffer from allergies can instead avoid the substance which irritates them.[1] Antihistamines are usually for short-term treatment.[1] Chronic allergies increase the risk of health problems which antihistamines might not treat, including asthma, sinusitis, and lower respiratory tract infection.[1] Doctors recommend that people talk to them before any longer term use of antihistamines.[1] Although typical people use the word “antihistamine” to describe drugs for treating allergies, doctors and scientists use the term to describe a class of drug that opposes the activity of histamine receptors in the body.[2] In this sense of the word, antihistamines are subclassified according to the histamine receptor that they act upon. The two largest classes of antihistamines are H1-antihistamines and H2-antihistamines. Antihistamines that target the histamine H1-receptor
H1-receptor
are used to treat allergic reactions in the nose (e.g., itching, runny nose, and sneezing) as well as for insomnia. They are sometimes also used to treat motion sickness or vertigo caused by problems with the inner ear. Antihistamines that target the histamine H2-receptor are used to treat gastric acid conditions (e.g., peptic ulcers and acid reflux). H1-antihistamines work by binding to histamine H1 receptors in mast cells, smooth muscle, and endothelium in the body as well as in the tuberomammillary nucleus in the brain; H2-antihistamines bind to histamine H2 receptors in the upper gastrointestinal tract, primarily in the stomach. Histamine
Histamine
receptors exhibit constitutive activity, so antihistamines can function as either a neutral receptor antagonist or an inverse agonist at histamine receptors.[3][2][4][5] Only a few currently marketed H1-antihistamines are known to function as inverse agonists.[2][5]

Contents

1 Medical uses 2 Types

2.1 H1-antihistamines

2.1.1 H1 antagonists 2.1.2 H1 inverse agonists

2.2 H2-antihistamines

3 Research

3.1 H3-antihistamines 3.2 H4-antihistamines

4 Related agents

4.1 Histidine decarboxylase
Histidine decarboxylase
inhibitors 4.2 Mast cell
Mast cell
stabilizers

5 History 6 Society and culture 7 Research 8 Special
Special
populations 9 See also 10 References 11 External links

Medical uses[edit] Histamine
Histamine
produces increased vascular permeability, causing fluid to escape from capillaries into tissues, which leads to the classic symptoms of an allergic reaction — a runny nose and watery eyes. Histamine
Histamine
also promotes angiogenesis.[6] Antihistamines suppress the histamine-induced wheal response (swelling) and flare response (vasodilation) by blocking the binding of histamine to its receptors or reducing histamine receptor activity on nerves, vascular smooth muscle, glandular cells, endothelium, and mast cells. Itching, sneezing, and inflammatory responses are suppressed by antihistamines that act on H1-receptors.[2][7] In 2014 antihistamines such as desloratadine were found to be effective as adjuvants to standardized treatment of acne due to their anti-inflammatory properties and their ability to suppress sebum production.[8][9] Types[edit] H1-antihistamines[edit] Main article: H1-antihistamine H1-antihistamines refer to compounds that inhibit the activity of the H1 receptor.[4][5] Since the H1 receptor exhibits constitutive activity, H1-antihistamines can be either neutral receptor antagonists or inverse agonists.[4][5] Normally, histamine binds to the H1 receptor and heightens the receptor's activity; the receptor antagonists work by binding to the receptor and blocking the activation of the receptor by histamine; by comparison, the inverse agonists bind to the receptor and reduce its activity, an effect which is opposite to histamine's.[4] The vast majority of marketed H1-antihistamines are receptor antagonists and only a minority of marketed compounds are inverse agonists at the receptor.[2][5] Clinically, H1-antihistamines are used to treat allergic reactions and mast cell-related disorders. Sedation is a common side effect of H1-antihistamines that readily cross the blood–brain barrier; some of these drugs, such as diphenhydramine and doxylamine, are therefore used to treat insomnia. H1-antihistamines can also reduce inflammation, since the expression of NF-κB, the transcription factor the regulates inflammatory processes, is promoted by both the receptor's constitutive activity and agonist (i.e., histamine) binding at the H1 receptor.[2] A combination of these effects, and in some cases metabolic ones as well, lead to most first-generation antihistamines having analgesic-sparing (potentiating) effects on opioid analgesics and to some extent with non-opioid ones as well. The most commonly used for the purpose include hydroxyzine, promethazine (enzyme induction especially helps with codeine and similar prodrug opioids), phenyltoloxamine, orphenadrine, and tripelennamine; some may also have intrinsic analgesic properties of their own, orphenadrine being an example. Second-generation antihistamines cross the blood–brain barrier to a much lower degree than the first-generation antihistamines. Their main benefit is they primarily affect peripheral histamine receptors and therefore are less sedating. However, high doses can still induce drowsiness through acting on the central nervous system. Some second-generation antihistamines, notably cetirizine, can interact with CNS psychoactive drugs such as bupropion and benzodiazepines.[10] H1 antagonists[edit] Examples of H1 antagonists
H1 antagonists
include:

Acrivastine
Acrivastine
(see Benadryl entry in this section) Azelastine Benadryl is a brand name for different H1 antagonist
H1 antagonist
anitihistamine preparations in different regions: acrivastine is the active component of Benadryl Allergy Relief and cetirizine of Benadryl One a Day Relief in the UK; Benadryl is diphenhydramine in the US and Canada (see http://www.benadryl.ca/adult-allergy-medicine/benadryl-caplets). Bilastine Bromodiphenhydramine Brompheniramine Buclizine Carbinoxamine Cetirizine
Cetirizine
(Zyrtec) Chlorodiphenhydramine Chlorphenamine Clemastine Cyclizine Cyproheptadine Dexbrompheniramine Dexchlorpheniramine Dimenhydrinate
Dimenhydrinate
(most commonly used as an antiemetic) Dimetindene Diphenhydramine
Diphenhydramine
(see Benadryl entry in this section) Doxylamine
Doxylamine
(most commonly used as an over-the-counter drug sedative) Ebastine Embramine Fexofenadine
Fexofenadine
(Allegra) Hydroxyzine
Hydroxyzine
(Vistaril) Loratadine
Loratadine
(Claritin) Meclizine
Meclizine
(most commonly used as an antiemetic) Mirtazapine
Mirtazapine
(primarily used to treat depression, also has antiemetic and appetite-stimulating effects) Olopatadine
Olopatadine
(used locally) Orphenadrine
Orphenadrine
(a close relative of diphenhydramine used mainly as a skeletal muscle relaxant and anti-Parkinsons agent) Phenindamine Pheniramine Phenyltoloxamine Promethazine Quetiapine
Quetiapine
(antipsychotic; trade name Seroquel) Rupatadine
Rupatadine
(Alergoliber) Tripelennamine Triprolidine

H1 inverse agonists[edit] The H1 receptor inverse agonists include:[2][5]

Cetirizine
Cetirizine
(does not cross the blood–brain barrier)

Levocetirizine

Desloratadine
Desloratadine
(does not cross the blood–brain barrier) Pyrilamine
Pyrilamine
(crosses the blood–brain barrier; produces drowsiness)

H2-antihistamines[edit] Main article: H2-antihistamine H2-antihistamines, like H1-antihistamines, occur as inverse agonists and neutral antagonists. They act on H2 histamine receptors found mainly in the parietal cells of the gastric mucosa, which are part of the endogenous signaling pathway for gastric acid secretion. Normally, histamine acts on H2 to stimulate acid secretion; drugs that inhibit H2 signaling thus reduce the secretion of gastric acid. H2-antihistamines are among first-line therapy to treat gastrointestinal conditions including peptic ulcers and gastroesophageal reflux disease. Some formulations are available over the counter. Most side effects are due to cross-reactivity with unintended receptors. Cimetidine, for example, is notorious for antagonizing androgenic testosterone and DHT receptors at high doses. Examples include:

Cimetidine Famotidine Lafutidine Nizatidine Ranitidine Roxatidine Tiotidine

Research[edit] These are experimental agents and do not yet have a defined clinical use, although a number of drugs are currently in human trials. H3-antihistamines have a stimulant and nootropic effect, whereas H4-antihistamines appear to have an immunomodulatory role. H3-antihistamines[edit] Main article: H3-antihistamine An H3-antihistamine is a classification of drugs used to inhibit the action of histamine at the H3 receptor. H3 receptors are primarily found in the brain and are inhibitory autoreceptors located on histaminergic nerve terminals, which modulate the release of histamine. Histamine
Histamine
release in the brain triggers secondary release of excitatory neurotransmitters such as glutamate and acetylcholine via stimulation of H1 receptors in the cerebral cortex. Consequently, unlike the H1-antihistamines which are sedating, H3-antihistamines have stimulant and cognition-modulating effects. Examples of selective H3-antihistamines include:

Clobenpropit,[11] ABT-239[12] Ciproxifan,[13] Conessine A-349,821.[14] Thioperamide

H4-antihistamines[edit] Examples:

Thioperamide JNJ 7777120 VUF-6002

Related agents[edit] Histidine decarboxylase
Histidine decarboxylase
inhibitors[edit] Inhibit the action of histidine decarboxylase:

Tritoqualine Catechin

Mast cell
Mast cell
stabilizers[edit] Main article: Mast cell
Mast cell
stabilizer Mast cell
Mast cell
stabilizers are drugs which prevent mast cell degranulation.

cromolyn sodium Nedocromil β-agonists

History[edit] Currently most people who use an antihistamine to treat allergies use a second generation drug.[1] The first generation of antihistamine drugs became available in the 1930s.[15] This marked the beginning of medical treatment of nasal allergies.[15] Research into these drugs led to the discovery that they were H1 antagonists
H1 antagonists
and also to the development of H2 antagonists, where H1 antihistamines affected the nose and the H2 antihistamines affected the stomach.[16] This history has led to contemporary research into drugs which are H3 receptor antagonist and which affect the Histamine
Histamine
H4 receptor.[16] Society and culture[edit] Antihistamines can vary greatly in cost.[1] Some patients consult with their doctor about drug prices to make a decision about which antihistamine to choose.[1] Many antihistamines are older and available in generic form.[1] Others are newer, still under patent, and generally expensive.[1] The newer drugs are not necessarily safer or more effective.[1] Because so many antihistamines are available, patients can have conversations with their health care provider to choose the right drug for them.[1] The United States government removed two second generation antihistamines, terfenadine and astemizole, from the market based on evidence that they could cause heart problems.[1] Research[edit] Not much published research exists which compares the efficacy and safety of the various antihistamines available.[1] The research which does exist are mostly short term studies or studies which look at too few people to make general assumptions.[1] Another gap in the research is in information reporting the health effects for individuals with long term allergies to take antihistamines for a long period of time.[1] Newer antihistamines have been demonstrated to be effective in treating hives.[1] However, there is not research comparing the relative efficacy of these drugs.[1] Special
Special
populations[edit] Most studies of antihistamines reported on people who are younger, so the effects on people over age 65 are not as well understood.[1] Older people are more likely to experience drowsiness from antihistamine use than younger people.[1] Also, most of the research has been on white people and other ethnicities are not as represented in the research.[1] The evidence does not report how antihistamines affect women differently than men.[1] Different studies have reported on antihistamine use in children, with various studies finding evidence that certain antihistamines could be used by children 2 years of age, and other drugs being safer for younger or older children.[1] See also[edit]

Antileukotriene Immunotherapy

References[edit]

^ a b c d e f g h i j k l m n o p q r s t u v w x y Consumer Reports (2013), Using Antihistamines to Treat Allergies, Hay Fever, & Hives
Hives
- Comparing Effectiveness, Safety, and Price (PDF), Yonkers, New York: Consumer Reports  ^ a b c d e f g Canonica GW, Blaiss M (2011). "Antihistaminic, anti-inflammatory, and antiallergic properties of the nonsedating second-generation antihistamine desloratadine: a review of the evidence". World Allergy Organ J. 4 (2): 47–53. doi:10.1097/WOX.0b013e3182093e19. PMC 3500039 . PMID 23268457. The H1-receptor
H1-receptor
is a transmembrane protein belonging to the G-protein coupled receptor family. Signal transduction from the extracellular to the intracellular environment occurs as the GCPR becomes activated after binding of a specific ligand or agonist. A subunit of the G-protein subsequently dissociates and affects intracellular messaging including downstream signaling accomplished through various intermediaries such as cyclic AMP, cyclic GMP, calcium, and nuclear factor kappa B (NF-κB), a ubiquitous transcription factor thought to play an important role in immune-cell chemotaxis, proinflammatory cytokine production, expression of cell adhesion molecules, and other allergic and inflammatory conditions.1,8,12,30–32 ... For example, the H1-receptor promotes NF-κB
NF-κB
in both a constitutive and agonist-dependent manner and all clinically available H1-antihistamines inhibit constitutive H1-receptor-mediated NF-κB
NF-κB
production ... Importantly, because antihistamines can theoretically behave as inverse agonists or neutral antagonists, they are more properly described as H1-antihistamines rather than H1-receptor antagonists.15  ^ Panula P, Chazot PL, Cowart M, et al. (2015). "International Union of Basic and Clinical Pharmacology. XCVIII. Histamine
Histamine
Receptors". Pharmacol. Rev. 67 (3): 601–55. doi:10.1124/pr.114.010249. PMC 4485016 . PMID 26084539.  ^ a b c d Leurs R, Church MK, Taglialatela M (April 2002). "H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac effects". Clinical and Experimental Allergy. 32 (4): 489–98. doi:10.1046/j.0954-7894.2002.01314.x. PMID 11972592.  ^ a b c d e f "H1 receptor". IUPHAR/BPS Guide to Pharmacology. Retrieved 8 October 2015.  ^ Norrby K (1995). "Evidence of a dual role of endogenous histamine in angiogenesis". Int J Exp Pathol. 76 (2): 87–92. PMC 1997159 . PMID 7540412.  ^ Monroe EW, Daly AF, Shalhoub RF (February 1997). "Appraisal of the validity of histamine-induced wheal and flare to predict the clinical efficacy of antihistamines". The Journal of Allergy and Clinical Immunology. 99 (2): S798–806. doi:10.1016/s0091-6749(97)70128-3. PMID 9042073.  ^ Lee HE, Chang IK, Lee Y, Kim CD, Seo YJ, Lee JH, Im M (2014). "Effect of antihistamine as an adjuvant treatment of isotretinoin in acne: a randomized, controlled comparative study". J Eur Acad Dermatol Venereol. 28 (12): 1654–60. doi:10.1111/jdv.12403. PMID 25081735.  ^ Layton AM (2016). "Top Ten List of Clinical Pearls in the Treatment of Acne
Acne
Vulgaris". Dermatol Clin. 34 (2): 147–57. doi:10.1016/j.det.2015.11.008. PMID 27015774.  ^ "Drug Interaction Report". drugs.com. Retrieved 28 January 2017.  ^ Yoneyama H, et al. (March 2008). "Efficient approaches to S-alkyl-N-alkylisothioureas: syntheses of histamine H3 antagonist clobenpropit and its analogues". The Journal of Organic Chemistry. 73 (6): 2096–104. doi:10.1021/jo702181x. PMID 18278935.  ^ Fox GB, Esbenshade TA, Pan JB, Radek RJ, Krueger KM, Yao BB, Browman KE, Buckley MJ, Ballard ME, Komater VA, Miner H, Zhang M, Faghih R, Rueter LE, Bitner RS, Drescher KU, Wetter J, Marsh K, Lemaire M, Porsolt RD, Bennani YL, Sullivan JP, Cowart MD, Decker MW, Hancock AA (April 2005). "Pharmacological properties of ABT-239
ABT-239
[4-(2- 2-[(2R)-2-Methylpyrrolidinyl]ethyl -benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist". The Journal of Pharmacology
Pharmacology
and Experimental Therapeutics. 313 (1): 176–90. doi:10.1124/jpet.104.078402. PMID 15608077.  ^ Ligneau X, Lin J, Vanni-Mercier G, Jouvet M, Muir JL, Ganellin CR, Stark H, Elz S, Schunack W, Schwartz J (November 1998). "Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist". The Journal of Pharmacology
Pharmacology
and Experimental Therapeutics. 287 (2): 658–66. PMID 9808693.  ^ Esbenshade TA, Fox GB, Krueger KM, Baranowski JL, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan JB, Faghih R, Bennani YL, Williams M, Hancock AA (September 2004). "Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist". Biochemical Pharmacology. 68 (5): 933–45. doi:10.1016/j.bcp.2004.05.048. PMID 15294456.  ^ a b Ostrom, NK (2014). "The history and progression of treatments for allergic rhinitis". Allergy and asthma proceedings. 35 Suppl 1 (3): S3–10. doi:10.2500/aap.2014.35.3758. PMID 25582156.  ^ a b Jones, AW (January 2016). "Perspectives in Drug Development and Clinical Pharmacology: The Discovery of Histamine
Histamine
H1 and H2 Antagonists". Clinical pharmacology in drug development. 5 (1): 5–12. doi:10.1002/cpdd.236. PMID 27119574. 

External links[edit]

Histamine
Histamine
antagonist at the US National Library of Medicine Medical Subject Headings (MeSH) Antihistamine
Antihistamine
information at Allergy UK

v t e

Antihistamines (R06)

Benzimidazoles (*)

Astemizole Azelastine Bilastine Emedastine Mizolastine Talastine

Diarylmethanes

Diarylmethoxyalkylamines: Bromazine
Bromazine
(bromodiphenhydramine) Carbinoxamine Chlorphenoxamine Clemastine Diphenhydramine Diphenylpyraline Doxylamine Ebastine Orphenadrine

Diphenylmethanolpiperidines: Fexofenadine Terfenadine

Diphenylmethylpiperazines: Buclizine Cetirizine

Levocetirizine

Chlorcyclizine Cinnarizine Cyclizine Etodroxizine Hydroxyzine Meclizine Oxatomide

Phenylpyridinylpropanamines: Brompheniramine Chlorphenamine Dexbrompheniramine
Dexbrompheniramine
(+pseudoephedrine) Dexchlorpheniramine
Dexchlorpheniramine
(+betamethasone) Pheniramine

Others: Acrivastine Bamipine Dimetindene Phenyltoloxamine Pyrrobutamine Quifenadine Triprolidine

Ethylenediamines

Antazoline Chloropyramine Histapyrrodine Mepyramine
Mepyramine
(pyrilamine) Methapyrilene Phenbenzamine Thenalidine Tripelennamine
Tripelennamine
(pyribenzamine)

Tricyclics

Dibenzocycloheptenes: Antidepressants (e.g., amitriptyline) Azatadine Cyproheptadine Deptropine Desloratadine Ketotifen Loratadine Rupatadine

Phenothiazines: Alimemazine Fenethazine Hydroxyethylpromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine

Others: Antidepressants (e.g., doxepin, mirtazapine, trimipramine) Epinastine Latrepirdine Mebhydrolin Olopatadine Perlapine Phenindamine Pimethixene

Others

Phenylpiperazines: Antidepressants (e.g., trazodone) Phenbenzamine

For topical use

Bamipine Chloropyramine Chlorphenoxamine Clemastine Dimetindene Diphenhydramine Doxepin Isothipendyl Mepyramine
Mepyramine
(pyrilamine) Promethazine

v t e

Histamine receptor modulators

H1

Agonists: 2-Pyridylethylamine Betahistine Histamine HTMT L-Histidine UR-AK49

Antagonists: First-generation: 4-Methyldiphenhydramine Alimemazine Antazoline Azatadine Bamipine Benzatropine
Benzatropine
(benztropine) Bepotastine Bromazine Brompheniramine Buclizine Captodiame Carbinoxamine Chlorcyclizine Chloropyramine Chlorothen Chlorphenamine Chlorphenoxamine Cinnarizine Clemastine Clobenzepam Clocinizine Cloperastine Cyclizine Cyproheptadine Dacemazine Decloxizine Deptropine Dexbrompheniramine Dexchlorpheniramine Dimenhydrinate Dimetindene Diphenhydramine Diphenylpyraline Doxylamine Embramine Etodroxizine Etybenzatropine
Etybenzatropine
(ethylbenztropine) Etymemazine Fenethazine Flunarizine Histapyrrodine Homochlorcyclizine Hydroxyethylpromethazine Hydroxyzine Isopromethazine Isothipendyl Meclozine Medrylamine Mepyramine
Mepyramine
(pyrilamine) Mequitazine Methafurylene Methapyrilene Methdilazine Moxastine Orphenadrine Oxatomide Oxomemazine Perlapine Phenindamine Pheniramine Phenyltoloxamine Pimethixene Piperoxan Pipoxizine Promethazine Propiomazine Pyrrobutamine Talastine Thenalidine Thenyldiamine Thiazinamium Thonzylamine Tolpropamine Tripelennamine Triprolidine

Second/third-generation: Acrivastine Alinastine Astemizole Azelastine Bamirastine Barmastine Bepiastine Bepotastine Bilastine Cabastinen Carebastine Cetirizine Clemastine Clemizole Clobenztropine Desloratadine Dorastine Ebastine Efletirizine Emedastine Epinastine Fexofenadine Flezelastine Ketotifen Latrepirdine Levocabastine Levocetirizine Linetastine Loratadine Mapinastine Mebhydrolin Mizolastine Moxastine Noberastine Octastine Olopatadine Perastine Pibaxizine Piclopastine Quifenadine
Quifenadine
(phencarol) Rocastine Rupatadine Setastine Sequifenadine (bicarphen) Talastine Temelastine Terfenadine Vapitadine Zepastine

Others: Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, RP-5063, ziprasidone, zotepine) Phenylpiperazine
Phenylpiperazine
antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione) Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline) Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine) Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene)

Unknown/unsorted: Azanator Belarizine Elbanizine Flotrenizine Napactadine Tagorizine Trelnarizine Trenizine

H2

Agonists: Amthamine Betazole Dimaprit Histamine HTMT Impromidine L-Histidine UR-AK49

Antagonists: Bisfentidine Burimamide Cimetidine Dalcotidine Donetidine Ebrotidine Etintidine Famotidine Isolamtidine Lafutidine Lamtidine Lavoltidine
Lavoltidine
(loxtidine) Lupitidine Metiamide Mifentidine Niperotidine Nizatidine Osutidine Oxmetidine Pibutidine Quisultazine (quisultidine) Ramixotidine Ranitidine Roxatidine Sufotidine Tiotidine Tuvatidine Venritidine Xaltidine Zolantidine

H3

Agonists: α-Methylhistamine Cipralisant Histamine Imetit Immepip Immethridine L-Histidine Methimepip Proxyfan

Antagonists: A-349,821 A-423,579 ABT-239 ABT-652 AZD5213 Bavisant Betahistine Burimamide Ciproxifan Clobenpropit Conessine Enerisant GSK-189,254 Impentamine Iodophenpropit Irdabisant JNJ-5207852 MK-0249 NNC 38-1049 PF-03654746 Pitolisant SCH-79687 Thioperamide VUF-5681

H4

Agonists: 4-Methylhistamine α-Methylhistamine Histamine L-Histidine OUP-16 VUF-8430

Antagonists: JNJ-7777120 Mianserin Seliforant Thioperamide Toreforant VUF-6002

See also: Receptor/signaling modulators • Monoamine metabolism modulators • Monoamine reuptake inhibitors

v t e

Pharmacomodulation

Types

♦ Enzyme: Inducer Inhibitor

♦ Ion channel: Opener Blocker

♦ Receptor: Agonist Partial agonist Antagonist Inverse agonist Positive allosteric modulator (PAM) Negative allosteric modulator (NAM)

♦ Transporter [ Reuptake
Reuptake
vs Efflux]: Enhancer (RE) Inhibitor (RI) Releaser (RA)

♦ Miscellaneous: Precursor Cofactor

Classes

Enzyme

see Enzyme
Enzyme
inhibition

Ion channel

Calcium channel blocker
Calcium channel blocker
(CCB) Potassium channel blocker
Potassium channel blocker
(PCB) Sodium channel blocker
Sodium channel blocker
(SCB) Potassium channel opener (PCO)

Receptor & transporter

BA/M

Adrenergic

Adrenergic receptor agonist (α β (1 2)) Adrenergic receptor antagonist (α (1 2) β) Norepinephrine reuptake inhibitor
Norepinephrine reuptake inhibitor
(NRI)

Dopaminergic

Dopamine receptor agonist Dopamine receptor antagonist Dopamine reuptake inhibitor
Dopamine reuptake inhibitor
(DRI)

Histaminergic

Histamine receptor agonist Histamine receptor antagonist (H1 H2 H3)

Serotonergic

Serotonin receptor agonist Serotonin receptor antagonist (5-HT3) Serotonin reuptake inhibitor
Serotonin reuptake inhibitor
(SRI)

AA

GABAergic

GABA receptor agonist GABA receptor antagonist GABA reuptake inhibitor
GABA reuptake inhibitor
(GRI)

Glutamatergic

Glutamate
Glutamate
receptor agonist (AMPA) Glutamate
Glutamate
receptor antagonist (NMDA) Glutamate
Glutamate
reuptake inhibitor

Cholinergic

Acetylcholine
Acetylcholine
receptor agonist (Muscarinic Nicotinic) Acetylcholine
Acetylcholine
receptor antagonist (Muscarinic Nicotinic (Ganglionic Muscular))

Cannabinoidergic

Cannabinoid
Cannabinoid
receptor agonist Cannabinoid
Cannabinoid
receptor antagonist Endocannabinoid enhancer (eCBE) Endocannabinoid reuptake inhibitor (eCBRI)

Opioidergic

Opioid
Opioid
modulator Opioid
Opioid
receptor agonist Opioid
Opioid
receptor antagonist Enkephalinase inhibitor

Other

Adenosine reuptake inhibitor
Adenosine reuptake inhibitor
(AdoRI) Angiotensin II receptor antagonist Endothelin receptor antagonist NK1 receptor antagonist Vasopressin receptor antagonist

Miscellaneous

Cofactor (see Enzyme
Enzyme
cofactors) Precursor

.