Risperidone

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trade name: Risperdal; drug class: antipsychotic; action: may be related to antagonism for dopamine and serotonin receptors; also has affinity for alpha receptors and histamine (H₁) receptors; use: psychotic disorders.

Brand names: Risperdal®Risperdal® Consta®Risperdal® M-Tab®

Chemical formula:

Drug Forms:
• Risperidone Injection (below)
• Risperidone Oral disintegrating tablet
• Risperidone Oral solution
• Risperidone Oral tablet
• Risperidone Solution for injection

Español:
• Inyección de risperidona
• Risperidona, Tableta de desintegración oral
• Risperidona, Solución oral
• Risperidona, Tableta oral
• Risperidona, Solución para inyección

Risperidone Injection

What is Risperidone Injection?

RISPERIDONE (Risperdal® Consta™) helps to treat schizophrenia. Risperidone can help you to keep in touch with reality and reduce your mental problems. Occasionally risperidone is used to treat other mood disturbances. Generic risperidone injection is not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• frequently drink alcohol or alcohol-containing beverages
• blood disorder or disease
• dementia
• diabetes (increased blood sugar) or a family history of diabetes
• difficulty swallowing
• heart disease
• history of brain tumor or head injury
• history of breast cancer
• irregular heartbeat
• kidney disease
• liver disease
• low blood pressure
• Parkinson's disease
• previous heart attack
• seizures (convulsions)
• an unusual or allergic reaction to risperidone, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Risperidone injection is for injection into a muscle. It is given by a health-care professional in a hospital or clinic setting.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What drug(s) may interact with risperidone?

• alcohol
• arsenic trioxide
• astemizole
• bromocriptine
• cabergoline
• carbamazepine
• clarithromycin
• cimetidine
• cisapride
• droperidol
• erythromycin
• halofantrine
• imatinib, STI-571
• levodopa and other medications for Parkinson's disease
• levomethadyl
• medicines for high blood pressure
• medicines for irregular heartbeats
• medicines for sleep or sedation
• medicines for treating seizures (convulsions)
• other medicines for mental anxiety, depression or psychotic disturbances
• pentamidine
• prescription pain medications
• probucol
• rifampin
• ritonavir
• some medicines for infertility
• some medicines for the hormonal treatment of cancer
• some quinolone antibiotics for treating infections (gatifloxacin, levofloxacin, moxifloxacin, sparfloxacin
• terfenadine

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking risperidone?

Visit your prescriber or health care professional for regular checks on your progress. Do not suddenly stop taking risperidone; you may need to gradually reduce the dose. Only stop taking risperidone on your prescriber's advice.

You may get dizzy or drowsy. Do not drive, use machinery, or do anything that needs mental alertness until you know how risperidone affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol can increase dizziness and drowsiness. Avoid alcoholic drinks. You can get a hangover effect the morning after a bedtime dose.

If you notice an increased hunger or thirst, different from your normal hunger or thirst, or if you find that you must frequently use the restroom (excessive urination), you should contact your health care provider as soon as possible. You may need to have your blood sugar monitored.

Do not treat yourself for colds, diarrhea or allergies. Ask your prescriber or health care professional for advice, some nonprescription medicines may increase possible side effects.

Risperidone may make you more sensitive to sun or ultraviolet light. Keep out of the sun, or wear protective clothing outdoors and use a sunscreen (at least SPF 15). Do not use sun lamps, or sun tanning beds or booths. To protect your eyes wear sunglasses even on cloudy days.

If you are going to have surgery tell your prescriber or health care professional that you are taking risperidone.

What side effects may I notice from taking risperidone?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• aching muscles and joints
• changes in vision
• confusion
• fast or irregular heartbeat (palpitations)
• fainting spells
• increased thirst or hunger
• increased need to pass urine
• inner restlessness, unable to keep still
• loss of balance, difficulty walking or falls
• stiffness, spasms, trembling

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• constipation
• decreased sexual ability
• difficulty sleeping
• drowsiness or dizziness
• headache
• increase or decrease in saliva
• increased sensitivity to the sun
• injection site pain, redness or swelling
• menstrual irregularity
• nausea, vomiting
• stomach pain
• stuffy or runny nose, cough
• unusual tiredness
• weight gain

Where can I keep my medicine?

This does not apply. You will not keep the injection at home.

Last updated: 5/7/2003 9:18:00 AM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Not to be confused with reserpine.

Risperidone
Systematic (IUPAC) name
4-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)- 1-piperidyl]ethyl]-3-methyl- 2,6-diazabicyclo[4.4.0]deca-1,3-dien-5-one
Identifiers
CAS number	106266-06-2
ATC code	N05AX08
PubChem	5073
DrugBank	APRD00187
Chemical data
Formula	C23H27FN4O2
Mol. mass	410.485 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	70% (oral)
Metabolism	Hepatic (CYP2D6-mediated)
Half life	3–20 hours
Excretion	Urinary
Therapeutic considerations
Pregnancy cat.	C
Legal status	℞ Prescription only
Routes	Oral and extended-release intramuscular injection

Risperdal tablets

Risperidone (pronounced Ris-PEAR-rǐ-dōne) is an atypical antipsychotic used to treat schizophrenia (including adolescent schizophrenia), the mixed and manic states associated with bipolar disorder, and irritability in children with autism. The drug was developed by Janssen-Cilag and is sold under the trade name Risperdal in the Netherlands, United States, Canada, the United Kingdom, Portugal, Spain, Turkey and several other countries, Risperdal or Ridal in New Zealand, Sizodon or Riscalin in India, Rispolept in Eastern Europe, and Belivon, or Rispen elsewhere.

Contents 1 Uses 2 Patent status 3 Generic Availability 4 Side effects 5 Pharmacology 6 References 7 External links

Uses

Risperidone was approved by the United States Food and Drug Administration (FDA) in 1993^[1] for the treatment of schizophrenia.

On August 22, 2007, Risperdal was approved as the only drug agent available for treatment of schizophrenia in youth ages 13–18; it was also approved that same day for treatment of bipolar disorder in youth and children ages 10–18, joining lithium. Risperidone contains the functional groups of benzisoxazole and piperidine as part of its molecular structure. In 2003 the FDA approved risperidone for the short-term treatment of the mixed and manic states associated with bipolar disorder. In 2006 the FDA approved risperidone for the treatment of irritability in children and adolescents with autism.^[2] The FDA's decision was based in part on a study of autistic children with severe and enduring problems of violent meltdowns, aggression, and self-injury; risperidone is not recommended for autistic children with mild aggression and explosive behavior without an enduring pattern.^[3] Like other atypical antipsychotics, risperidone has also been used off-label for the treatment of anxiety disorders, such as obsessive-compulsive disorder; severe, treatment-resistant depression with or without psychotic features; Tourette syndrome; disruptive behavior disorders in children; and eating disorders, among others. In two small studies risperidone was reported to successfully treat the symptoms of phencyclidine psychosis due to acute intoxication^[4] and chronic use.^[5]

A 2009 Cochrane Library review found no evidence from randomized controlled trials that risperidone is effective for the treatment of attention-deficit hyperactivity disorder (ADHD) in people with intellectual disabilities.^[6] A multi-year UK study by the Alzheimer's Research Trust suggested that this and other neuroleptic anti-psychotic drugs commonly given to Alzheimer's patients with mild behavioural problems often made their condition worse. The study concluded that:

“

For most patients with AD, withdrawal of neuroleptics had no overall detrimental effect on functional and cognitive status and by some measures improved functional and cognitive status. Neuroleptics may have some value in the maintenance treatment of more severe neuropsychiatric symptoms, but this possibility must be weighed against the unwanted effects of therapy.[7]

”

Patent status

Janssen's patent on Risperdal expired on December 29, 2007, opening the market for cheaper generic versions of the drug from other companies, and Janssen's exclusive marketing rights expired on June 29, 2008 (the result of a pediatric extension.)

Risperidone is available as a tablet in 0.25, 0.5, 1, 2, 3 and 4 mg sizes, as an oral solution (30ml, 1 mg/ml), and as a 25 mg, 37.5 mg and 50 mg ampoule Risperdal Consta, which is a depot injection administered once every two weeks. It is also available as a wafer known in the United States as Risperdal M-Tabs and elsewhere as Risperdal Quicklets.

Generic Availability

Risperidone became available as a generic drug in October 2008 from Teva Pharmaceuticals and Patriot Pharmaceutics. The Patriot generic is Janssen Pharmaceutical's "authorized generic pharmaceutical."

Side effects

Common side effects include severe anxiety, akathisia, sedation, dysphoria, insomnia, sexual dysfunction, low blood pressure, muscle stiffness, muscle pain, tremors, increased salivation, and stuffy nose. Risperidone has been associated with minimal to moderate weight gain, with one study finding that 26 to 38 percent of participants on the drug experienced weight gain.^[8][9]

Occasionally breast tenderness and eventually lactation in both sexes may occur. Many antipsychotics are known to increase prolactin because they inhibit dopamine. However, risperidone is known to increase prolactin to a greater extent than most other antipsychotics, such as quetiapine. Over 40 pituitary neoplasm cases have been reported worldwide. It is thought that once risperidone raises prolactin, it may cause prolactinoma, a benign tumor of the pituitary gland. Tumors, in general, aren't considered reversible. Medical therapy (dopamine agonists) may help reduce tumor size and restore normal reproduction and pituitary function, but if unsuccessful, surgery or radiation treatment may be required. This condition may recur if the patient is switched to a different antipsychotic. Risperidone has been known to cause increased thoughts of suicide.^[10]

Risperidone can potentially cause tardive dyskinesia (TD),^[11] extrapyramidal symptoms (EPS),^[11] and neuroleptic malignant syndrome (NMS).^[11] Risperidone may also trigger diabetes and more serious conditions of glucose metabolism, including ketoacidosis and hyperosmolar coma.^[12]

Pharmacology

This drug belongs to a class of anti-psychotic drugs known as atypical neuroleptics. It is a strong dopamine antagonist. It has high affinity for D₂ dopaminergic receptors. It has actions at several 5-HT (serotonin) receptor subtypes. These are 5-HT_2C, linked to weight gain, 5-HT_2A,linked to its antipsychotic action and relief of some of the extrapyramidal side effects experienced with the typical neuroleptics through action at 5-HT_1A. The latter action may lead to an increased release of dopamine from mesocortical neurones in the brain.

It reaches peak plasma levels quickly regardless of whether it is administered as a liquid or pill. Risperidone is metabolised fairly quickly, so this potential for nausea subsides usually in two to three hours. However, the active metabolite, 9-hydroxy-risperidone, which has similar pharmacodynamics to risperidone, lingers in the body for much longer, and has been developed as an antipsychotic in its own right, called paliperidone.

An intramuscular preparation, marketed as Risperdal Consta, can be given once every two weeks. It is slowly released from the injection site. This method of administration may be used on sanctioned patients who are incompliant, or consenting patients who may have disorganized thinking and cannot remember to take their daily doses.^[13] Doses range from 25 to 50 mg given as an intramuscular injection once every two weeks.

References

1. ^ "Electronic Orange Book". Food and Drug Administration. April 2007. http://www.accessdata.fda.gov/scripts/cder/ob/docs/obdetail.cfm?Appl_No=020272&TABLE1=OB_Rx. Retrieved on 2007-05-24. 
2. ^ FDA (October 2, 2006). FDA approves the first drug to treat irritability associated with autism, Risperdal. Press release. http://www.fda.gov/bbs/topics/NEWS/2006/NEW01485.html. Retrieved on 2006-10-02. 
3. ^ Scahill L (2008). "How do I decide whether or not to use medication for my child with autism? should I try behavior therapy first?". J Autism Dev Disord 38 (6): 1197–8. doi:10.1007/s10803-008-0573-7. PMID 18463973. 
4. ^ AJ Giannini, GL Colapietro, DK Cook. Risperidone therapy in phencyclidine intoxication, Society for Neuroscience Abstracts. 22:77.12, 1996.
5. ^ JF Gabbert,AJ Giannini. Dopaminergic/serotonergic actions of phencyclidine as a model for schizophrenia psychosis. American Journal of Therapeutics. 4:159-164, 1997.
6. ^ Thomson A, Maltezos S, Paliokosta E, Xenitidis K (2009). "Risperidone for attention-deficit hyperactivity disorder in people with intellectual disabilities". Cochrane Database Syst Rev (2): CD007011. doi:10.1002/14651858.CD007011.pub2. PMID 19370667. 
7. ^ Ballard C, Lana MM, Theodoulou M et al. (2008). "A randomised, blinded, placebo-controlled trial in dementia patients continuing or stopping neuroleptics (the DART-AD trial)". PLOS Medicine 5 (4): e76. doi:10.1371/journal.pmed.0050076. PMID 18384230. http://medicine.plosjournals.org/perlserv/?request=get-document&doi=10.1371/journal.pmed.0050076. Lay summary – BBC News (2008-04-01). 
8. ^ Vanina et al. (July 2002). "Body Weight Changes Associated With Psychopharmacology". Psychiatric Services (American Psychiatric Association) 53: 842–847. doi:10.1176/appi.ps.53.7.842. PMID 12096167. http://psychservices.psychiatryonline.org/cgi/content/full/53/7/842#SEC2. 
9. ^ Baldwin, D and Mayers, A. (2003). "Sexual side-effects of antidepressant and antipsychotic drugs". Advances in Psychiatric Treatment (Royal College of Psychiatrists) 9: 202–210. doi:10.1192/apt.9.3.202. http://apt.rcpsych.org/cgi/content/full/9/3/202. 
10. ^ Szarfman A, Tonning J, Levine J, Doraiswamy P (2006). "Atypical antipsychotics and pituitary tumors: a pharmacovigilance study.". Pharmacotherapy 26 (6): 748–58. doi:10.1592/phco.26.6.748. PMID 16716128. 
11. ^ ^{a b c} "Risperdal: Full U.S. Prescribing Information" (PDF). publisher=Ortho-McNeil-Janssen Pharmaceuticals. http://www.risperdal.com/risperdal/shared/pi/risperdal.pdf. Retrieved on 2008-03-06. 
12. ^ FDA (April 19, 2004). FDA Warning Letter. Press release. http://www.fda.gov/foi/warning_letters/archive/g4628d.htm. Retrieved on 2007-05-02. 
13. ^ Antipsychotic Medications, About.com: Mental Health May 30, 2006

External links

• Drugs.com Professional information on risperidone
• Drugs.com Consumer information on risperidone
• Janssen L.P. official web site on Risperdal (risperidone)
• PubChem Substance Summary: Risperidone National Center for Biotechnology Information.

v • d • e Psycholeptics: antipsychotics (N05A) Typicals Phenothiazines Chlorpromazine • Fluphenazine • Mesoridazine • Periciazine • Perphenazine • Prochlorperazine • Promazine • Thioridazine/Sulforidazine • Trifluoperazine • Triflupromazine Indoles Molindone Butyrophenones Azaperone • Benperidol • Bromperidol • Droperidol • Haloperidol • Trifluperidol Thioxanthenes Flupentixol • Chlorprothixene • Thiothixene • Zuclopenthixol Diphenylbutylpiperidines Fluspirilene • Penfluridol • Pimozide Others Amoxapine • Loxapine Atypicals Serotonin antagonists Butyrophenones Melperone Indoles Sertindole • Ziprasidone Other D2 selective Aripiprazole • Asenapine • Iloperidone • Mosapramine • Paliperidone • Perospirone • Quetiapine • Risperidone • Zotepine D4 selective Clozapine • Olanzapine Benzamides Amisulpride • Sulpiride • Remoxipride

v • d • e Serotonergics Receptor Ligands 5-HT1 5-HT1A Agonists: Azapirones: Alnespirone • Binospirone • Buspirone • Gepirone • Ipsapirone • Perospirone • Tandospirone • Tiospirone • Zalospirone; Lysergamides: Dihydroergotamine • Ergotamine • Methysergide • LSD; Phenethylamines: MDA • MDMA; Piperazines: Eltoprazine • Flesinoxan • Flibanserin; Tryptamines: 5-CT • 5-MeO-DMT • 5-MT • DMT • Psilocin • Psilocybin • Rauwolscine • Yohimbine; Atypical Antipsychotics: Aripiprazole • Asenapine • Clozapine • Quetiapine • Ziprasidone; Others: 8-OH-DPAT • F 11440 • F 13640 • Lesopitron • Lu AA21004 • LY-293,284 • LY-301,317 • MKC-242 • Osemozotan • Piclozotan • PRX-00023 • Repinotan • RU-24969 • S-15535 • Sarizotan • SSR-181,507 • Sunepitron • U-92016A • Urapidil • Vilazodone • Xaliproden Antagonists: Beta Blockers: Alprenolol • Cyanopindolol • Iodocyanopindolol • Oxprenolol • Pindobind • Pindolol • Propranolol; Piperazines: Nefazodone • Trazodone • WAY-100,135 • WAY-100,635; Others: AMI-193 • AV965 • BMY-7378 • Dotarizine • GR-46611 • Isamoltane • Lecozotan • Methiothepin • MPPF • NAN-190 • Robalzotan • S-15535 • SB-649915 • SDZ 216-525 • Spiperone • Spiroxatrine • UH-301 • Xylamidine 5-HT1B Agonists: Lysergamides: Dihydroergotamine • Ergotamine • Methysergide; Piperazines: Eltoprazine • TFMPP; Triptans: Eletriptan • Sumatriptan • Zolmitriptan; Tryptamines: 5-CT • 5-MT; Others: CP-93,129 • CP-94,253 • CP-135,807 • RU-24969 Antagonists: Lysergamides: Metergoline • Methiothepin; Tryptamines: Yohimbine; Others: AR-A000002 • GR-127,935 • Isamoltane • SB-216,641 • SB-224,289 • SB-236,057 5-HT1D Agonists: Lysergamides: Dihydroergotamine • Methysergide; Triptans: Almotriptan • Eletriptan • Frovatriptan • Naratriptan • Rizatriptan • Sumatriptan • Zolmitriptan; Tryptamines: 5-CT • 5-MT; Others: CP-135,807 • CP-286,601 • GR-46611 • L-694,247 • L-772,405 • PNU-109,291 • PNU-142,633 Antagonists: Lysergamides: Metergoline • Methiothepin; Tryptamines: Rauwolscine • Yohimbine; Others: BRL-15572 • GR-127,935 • Ketanserin • LY-310,762 • LY-367,642 • LY-456,219 • LY-456,220 • Ritanserin • Ziprasidone 5-HT1E Agonists: Lysergamides: Methysergide; Triptans: Eletriptan; Tryptamines: Tryptamine Antagonists: Methiothepin 5-HT1F Agonists: Triptans: Eletriptan • Naratriptan • Sumatriptan; Tryptamines: 5-MT; Others: LY-334,370 Antagonists: Methiothepin 5-HT2 5-HT2A Agonists: Lysergamides: ALD-52 • Ergonovine • Lisuride • LA-SS-Az • LSD • Lysergic acid 2-butyl amide • Methysergide; Phenethylamines: 25I-NBMD • 25I-NBOH • 25I-NBOMe • 2C-B • 2C-B-FLY • 2C-E • 2C-I • 2C-T-2 • 2C-T-7 • 2C-T-21 • 2CBCB-NBOMe • 2CBFly-NBOMe • Bromo-DragonFLY • DOB • DOC • DOI • DOM • MDA • MDMA • Mescaline • Myristicin • TCB-2 • TFMFly; Piperazines: BZP • Quipazine • TFMPP; Tryptamines: 5-CT • 5-MeO-α-ET • 5-MeO-α-MT • 5-MeO-DET • 5-MeO-DiPT • 5-MeO-DMT • 5-MeO-DPT • 5-MT • α-ET • α-Methyl-5-HT • α-MT • Bufotenin • DET • DiPT • DMT • DPT • Psilocin • Psilocybin; Others: AL-34662 • AL-37350A • PNU-22394 Antagonists: Atypical Antipsychotics: Amperozide • Aripiprazole • Clozapine • Iloperidone • Melperone • Olanzapine • Paliperidone • Pimozide • Quetiapine • Risperidone • Sertindole • Ziprasidone • Zotepine; Typical Antipsychotics: Loxapine • Pipamperone; Antidepressants: Amitriptyline • Amoxapine • Etoperidone • Mianserin • Mirtazapine • Nefazodone • Trazodone; Others: 5-I-R91150 • AC-90179 • Altanserin • AMDA • APD-215 • Blonanserin • Cinanserin • Cyproheptadine • Deramciclane • Dotarizine • Eplivanserin • Fananserin • Flibanserin • Ketanserin • KML-010 • Lubazodone • Methiothepin • Nantenine • Pimavanserin • Pizotifen • Ritanserin • Sarpogrelate • Setoperone • Spiperone • Spiramide • SR-46349B • Volinanserin • Xylamidine • Yohimbine 5-HT2B Agonists: Oxazolines: 4-Methylaminorex • Aminorex; Phenethylamines: Chlorphentermine • DOB • DOC • DOI • DOM • Fenfluramine • MDA • MDMA • Norfenfluramine; Tryptamines: 5-CT • 5-MT • α-Methyl-5-HT; Others: BW-723C86 • Cabergoline • mCPP • Pergolide • PNU-22394 • Ro60-0175 Antagonists: Agomelatine • Asenapine • EGIS-7625 • Ketanserin • Lisuride • LY-272,015 • Rauwolscine • Ritanserin • RS-127,445 • Sarpogrelate • SB-200,646 • SB-204,741 • SB-206,553 • SB-215,505 • SB-221,284 • SB-228,357 • SDZ SER-082 • Tegaserod • Yohimbine 5-HT2C Agonists: Phenethylamines: 2C-B • 2C-E • 2C-I • 2C-T-2 • 2C-T-7 • 2C-T-21 • DOB • DOC • DOI • DOM • MDA • MDMA • Mescaline • Myristicin; Piperazines: Aripiprazole • mCPP • TFMPP; Tryptamines: 5-CT • 5-MeO-α-ET • 5-MeO-α-MT • 5-MeO-DET • 5-MeO-DiPT • 5-MeO-DMT • 5-MeO-DPT • 5-MT • α-ET • α-Methyl-5-HT • α-MT • Bufotenin • DET • DiPT • DMT • DPT • Psilocin • Psilocybin; Others: A-372,159 • AL-38022A • CP-809,101 • Lorcaserin • MK-212 • PNU-22394 • Ro60-0175 • Vabicaserin • WAY-629 • WAY-161,503 • YM-348 Antagonists: Atypical Antipsychotics: Clozapine • Iloperidone • Melperone • Olanzapine • Paliperidone • Pimozide • Quetiapine • Risperidone • Sertindole • Ziprasidone • Zotepine; Typical Antipsychotics: Loxapine • Pipamperone; Antidepressants: Agomelatine • Amitriptyline • Amoxapine • Etoperidone • Fluoxetine • Mianserin • Mirtazapine • Nefazodone • Trazodone; Others: Cinanserin • Deramciclane • Dimebolin • Dotarizine • Eltoprazine • FR-260,010 • Ketanserin • Pizotifen • Ritanserin • RS-102,221 • SB-200,646 • SB-206,553 • SB-221,284 • SB-228,357 • SB-242,084 • SB-243,213 • SDZ SER-082 • Xylamidine 5-HT3 Agonists: Piperazines: BZP • Quipazine; Tryptamines: 2-Methyl-5-HT • 5-CT; Others: Chlorophenylbiguanide • RS-56812 • SR-57,227 • SR-57,227-A • YM-31636 Antagonists: Antiemetics: Alosetron • Azasetron • Batanopride • Bemesetron • Cilansetron • Dolasetron • Granisetron • Lerisetron • Ondansetron • Palonosetron • Ramosetron • Renzapride • Tropisetron • Zacopride • Zatosetron; Atypical Antipsychotics: Clozapine • Olanzapine • Quetiapine; Tetracyclic Antidepressants: Amoxapine • Mianserin • Mirtazapine; Others: BRL-46,470 • ICS-205,930 • Lu AA21004 • MDL-72,222 • Memantine 5-HT4 Agonists: Gastroprokinetic Agents: Cisapride • Metoclopramide • Mosapride • Prucalopride • Renzapride • Tegaserod • Zacopride; Others: 5-MT • BIMU-8 • CJ-033,466 • PRX-03140 • RS-67333 • RS-67506 • TD-5108 Antagonists: GR-113,808 • GR-125,487 • L-Lysine • Piboserod • RS-39604 • RS-67532 • SB-203,186 5-HT5 5-HT5A Agonists: Lysergamides: Ergotamine • LSD; Tryptamines: 5-CT; Others: Valerenic Acid Antagonists: Asenapine • Dimebolin • Methiothepin • Ritanserin • SB-699,551 5-HT5B* Agonists: Lysergamides: Ergotamine • LSD Antagonists: Methiothepin * Note that the 5-HT5B receptor is not functional in humans. 5-HT6 Agonists: Lysergamides: Lisuride • LSD • Metergoline; Tryptamines: 5-CT • 5-MT • E-6801 • E-6837 • EMD-386,088 • EMDT • LY-586,713 • WAY-181,187 • WAY-208,466 Antagonists: Antidepressants: Amitriptyline • Amoxapine • Clomipramine • Doxepin • Mianserin • Nortriptyline; Atypical Antipsychotics: Aripiprazole • Asenapine • Clozapine • Fluperlapine • Iloperidone • Olanzapine • Tiospirone; Typical Antipsychotics: Chlorpromazine • Loxapine; Others: BGC20-760 • BVT-5182 • BVT-74316 • Dimebolin • EGIS-12233 • GW-742,457 • Ketanserin • Methiothepin • MS-245 • PRX-07034 • Ritanserin • Ro 04-6790 • Ro 63-0563 • SB-258,585 • SB-271,046 • SB-357,134 • SB-399,885 5-HT7 Agonists: Lysergamides: LSD; Tryptamines: 5-CT • 5-MT; Others: 8-OH-DPAT • AS-19 • Bifeprunox • LP-12 • LP-44 • Sarizotan Antagonists: Antidepressants: Amitriptyline • Amoxapine • Clomipramine • Imipramine • Maprotiline • Mianserin; Atypical Antipsychotics: Amisulpride • Aripiprazole • Clozapine • Olanzapine • Risperidone • Sertindole • Tiospirone • Ziprasidone • Zotepine; Typical Antipsychotics: Chlorpromazine • Loxapine; Others: EGIS-12233 • LY-215,840 • Mesulergine • Metergoline • Methiothepin • Pimozide • Ritanserin • SB-258,719 • SB-258,741 • SB-269,970 • SB-656,104 • SB-656,104-A • SB-691,673 • SLV-313 • SLV-314 • Spiperone • SSR-181,507 Reuptake Inhibitors Plasmalemmal SERT Inhibitors Selective Serotonin Reuptake Inhibitors (SSRIs): Alaproclate • Citalopram • Dapoxetine • Escitalopram • Femoxetine • Fluoxetine • Fluvoxamine • Indalpine • Litoxetine • Lubazodone • Paroxetine • Sertraline • Vilazodone • Zimelidine; Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs): Bicifadine • Desvenlafaxine • Duloxetine • Milnacipran • Venlafaxine; Serotonin-Norepinephrine-Dopamine Reuptake Inhibitors (SNDRIs): Brasofensine • Diclofensine • DOV 102,677 • DOV 21,947 • DOV 216,303 • NS2359 • SEP-225289 • SEP-227162 • Tesofensine; Tricyclic Antidepressants (TCAs): Amitriptyline • Butriptyline • Cianopramine • Clomipramine • Desipramine • Dosulepin • Doxepin • Imipramine • Lofepramine • Nortriptyline • Protriptyline • Trimipramine; Tetracyclic Antidepressants (TeCAs): Amoxapine; Piperazines: Nefazodone • Trazodone; Tropanes: Cocaine; Antihistamines: Brompheniramine • Chlorpheniramine • Diphenhydramine • Mepyramine/Pyrilamine • Pheniramine • Tripelennamine; Opioids: Meperidine/Pethidine • Methadone • Propoxyphene • Tramadol; Others: Cyclobenzaprine • Dextromethorphan • Mesembrine • SB-649915 • Sibutramine • Ziprasidone TRPC6 Activators Adhyperforin • Hyperforin Vesicular VMAT Inhibitors Ibogaine • Reserpine • Tetrabenazine Releasing Agents Aminoindanes: ETAI • MDAI • MDMAI • MMAI • TAI; Aminopropanes: Indanylaminopropane • Naphthylaminopropane; Benzofurans: 5-APDB; Oxazolines: 4-Methylaminorex • Aminorex; Phenethylamines: 2-Methyl-MDA • 3-Methoxy-4-methylamphetamine • 4-Bromomethcathinone • 4-Fluoroamphetamine • 4-Fluoromethamphetamine • 4-Methylamphetamine • 4-Methylmethamphetamine • 4-Methylthioamphetamine • 5-Methyl-MDA • BDB • BOH • Butylone • Chlorphentermine • Diethylcathinone • Dimethylcathinone • EBDB • Ethylone • Fenfluramine • Flephedrone • MBDB • MDA • MDEA • MDMA (Ecstasy) • MDOH • MDPEA • Mephedrone • Methylone • MMDA • MMDMA • Norfenfluramine • para-Bromoamphetamine • para-Chloroamphetamine • para-Chloromethamphetamine • para-Iodoamphetamine • para-Methoxyamphetamine • para-Methoxyethylamphetamine • para-Methoxymethamphetamine; Quinolines: PK 7059 • Viqualine; Tryptamines: α-ET • α-MT Enzyme Inhibitors Anabolism TPH Inhibitors AGN-2979 • Fenclonine AAAD Inhibitors Benserazide • Carbidopa Catabolism MAO Inhibitors Nonselective: Iproclozide • Iproniazid • Isocarboxazid • Nialamide • Phenelzine • Pheniprazine • Tranylcypromine; MAO-A Selective: Befloxatone • Brofaromine • Cimoxatone • Clorgiline • Harmala Alkaloids • Minaprine • Moclobemide • Pirlindole • Toloxatone • Tyrima Others Precursors L-Tryptophan • 5-HTP Cofactors Iron • Tetrahydrobiopterin • Vitamin B3 (Niacin/Nicotinamide/NADPH) • Vitamin B6 (Pyridoxine/Pyridoxamine/Pyridoxal 5-Phosphate) • Vitamin B9 (Folic Acid/Tetrahydrofolic Acid) • Vitamin C (Ascorbic Acid) • Zinc Others Activity Enhancers: BPAP • PPAP; Reuptake Enhancers: Tianeptine

v • d • e Dopaminergics Receptor Ligands Agonists Benzazepines: Fenoldopam • SKF 38393 • SKF 82958; Ergot-derivatives: Bromocriptine • Cabergoline • Dihydroergocryptine • Lisuride • LSD • Pergolide; Dihydrexidine-derivatives: A-86929 • Dihydrexidine • Dinapsoline • Dinoxyline • Doxathrine; Morphine-derivatives: Apomorphine • Propylnorapomorphine; Piperazines: Aripiprazole • Piribedil • WAY-100,635; Others: A-412,997 • Aplindore • Memantine • Pramipexole • Pukateine • Quinpirole • RDS-127 • Ropinirole • Rotigotine Antagonists Typical Antipsychotics: Acepromazine • Azaperone • Benperidol • Bromperidol • Clopenthixol • Chlorpromazine • Chlorprothixene • Droperidol • Flupentixol • Fluphenazine • Fluspirilene • Haloperidol • Loxapine • Mesoridazine • Methotrimeprazine • Molindone • Penfluridol • Perazine • Periciazine • Perphenazine • Pimozide • Prochlorperazine • Promazine • Sulforidazine • Thioridazine • Thiothixene • Trifluoperazine • Triflupromazine • Trifluperidol • Zuclopenthixol; Atypical Antipsychotics: Amisulpride • Asenapine • Clozapine • Iloperidone • Melperone • Olanzapine • Paliperidone • Perospirone • Quetiapine • Risperidone • Sertindole • Sulpiride • Ziprasidone • Zotepine; Antiemetics: Alizapride • Bromopride • Clebopride • Domperidone • Metoclopramide • Thiethylperazine; Others: Amoxapine • Blonanserin • Buspirone • Butaclamol • Eticlopride • Fananserin • Mosapramine • Nafadotride • Nemonapride • Nuciferine • Raclopride • Remoxipride • SB-277,011-A • SCH 23390 • Spiperone • Spiroxatrine • Stepholidine • Tetrahydropalmatine • Tiapride • UH-232 • Yohimbine Reuptake Inhibitors Plasmalemmal DAT Inhibitors Piperazines: DBL-583 • GBR-12935 • Nefazodone • Vanoxerine; Piperidines: BTCP • Desoxypipradrol • Dextromethylphenidate • Ethylphenidate • HDMP-28 • Methylphenidate • Phencyclidine • Pipradrol; Pyrovalerones: MDPV • Pyrovalerone; Tropanes: β-CPPIT • Altropane • Brasofensine • CFT • Cocaine • Dichloropane • Difluoropine • FE-β-CPPIT • FP-β-CPPIT • Ioflupane • Lometopane • RTI-121 • RTI-126 • RTI-150 • RTI-336 • Tenocyclidine • Tesofensine • Troparil • Tropoxane • WF-11 • WF-23 • WF-31 • WF-33; Others: Amfonelic Acid • Amineptine • Benztropine • Bromantane • BTQ • BTS 74,398 • Bupropion • Cypenamine • Diclofensine • Dimethocaine • Diphenylprolinol • Dizocilpine • DOV 102,677 • DOV 21,947 • DOV 216,303 • Ethcathinone • Fencamfamine • GYKI-52895 • Indatraline • Ketamine • Lefetamine • LR-5182 • Manifaxine • Mazindol • Medifoxamine • Mesocarb • Nisoxetine • Nomifensine • NS2359 • O-2172 • Prolintane • Radafaxine • SEP-225289 • SEP-227162 • Sibutramine • Tametraline • Tripelennamine TRPC6 Activators Adhyperforin • Hyperforin Vesicular VMAT Inhibitors Ibogaine • Reserpine • Tetrabenazine Releasing Agents Alkylamines: Cyclopentamine • Propylhexedrine; Aminopropanes: Indanylaminopropane • Naphthylaminopropane; Oxazolines: 4-Methylaminorex • Aminorex • Pemoline; Phenethylamines: 4-Fluoroamphetamine • 4-Fluoromethamphetamine • Amphetamine • Amphetaminil • Amfepentorex • Benzphetamine • Butylone • Cathine • Cathinone • Clobenzorex • Dextroamphetamine • Diethylcathinone • Dimethylamphetamine • Dimethylcathinone • Ethylamphetamine • Ethylone • Fenethylline • Fenproporex • Flephedrone • Furfenorex • Lisdexamfetamine • MBDB • MDA • MDEA • MDMA • Mefenorex • Mephedrone • Methamphetamine • Methcathinone • Methylone • Phendimetrazine • Phenethylamine • Phenmetrazine • PMA • PMEA • PMMA • Propylamphetamine • Tyramine • Xylopropamine; Piperazines: BZP • MBZP • MeOPP; Others: 4-Benzylpiperidine • Zylofuramine Enzyme Inhibitors Anabolism PAH Inhibitors 3,4-Dihydroxystyrene TH Inhibitors 3-Iodotyrosine • Aquayamycin • Bulbocapnine • Metirosine • Oudenone AAAD Inhibitors Benserazide • Carbidopa Catabolism MAO Inhibitors Nonselective: Iproclozide • Iproniazid • Isocarboxazid • Nialamide • Phenelzine • Pheniprazine • Tranylcypromine; MAO-A Selective: Befloxatone • Brofaromine • Cimoxatone • Clorgiline • Harmala Alkaloids • Minaprine • Moclobemide • Pirlindole • Toloxatone • Tyrima; MAO-B Selective: Lazabemide • Pargyline • Rasagiline • Selegiline COMT Inhibitors Entacapone • Tolcapone DBH Inhibitors Disulfiram • Nepicastat • Tropolone Others Precursors L-Phenylalanine • L-Tyrosine • L-DOPA Cofactors Iron • Tetrahydrobiopterin • Vitamin B3 (Niacin/Nicotinamide/NADPH) • Vitamin B6 (Pyridoxine/Pyridoxamine/Pyridoxal 5-Phosphate) • Vitamin B9 (Folic Acid/Tetrahydrofolic Acid) • Vitamin C (Ascorbic Acid) • Zinc Others Activity Enhancers: BPAP • PPAP; Others: Amantadine • Memantine • Rimantadine

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