Introduction to Risperidone

Developed in the late 1980's and approved for sale in 1993, risperidone is used to treat schitzophrenia, bipolar disorder and irritability in autism. It is the only drug approved for the treatment of schitzphrenia in youth's aged 13-17. It is on the World Health Organisation's list of essential medicines and is available in several generic forms.

Using Risperidone

Ways of Administration

Oral, tablet or liquid solution
Intra-muscular injection. [2]

Dose

Oral/Daily

Column 1	Column 2
Threshold	mg
Light	2mg
Medium	6mg
Strong	16mg

IM Injection/Fortnightly

Column 1	Column 2
Threshold	mg
Light	25mg
Medium	37.5mg
Strong	50mg

Effects of Risperidone

Risperidone combinations

Recreational drug combinations with Risperidone

Concurrent use with stimulants (Amphetamines, MDMA, Cocaine) may reduce the efficacy of either or both risperidone and the stimulant drug. [3]

Dangerous interactions with Risperidone

No dangerous combinations with Risperidone have been added to this wiki yet.

Medication interactions with Risperidone

May antagonise the effects of Levodopa and other dopamine agonists.
Caution should be exercised when coadministered with medications that increase QT interval or are known to cause electrolyte imbalance and inhibitors of hepatic metabolism of risperidone.
Carbamazepine has been shown to decrease plasma levels of risperidone and 9-hydroxy-risperidone. This may be the case with other CYP 3A4 hepatic enzyme inducers.
Fluoxetine and paroxetine increase plasma concentrations of risperidone, but less so of 9-hydroxy-risperidone.
Topiramate modestly reduced the bioavailability of risperidone.
Phenothiazones, tricyclic antidepressants and some beta blockers may increase plasma concentrations of risperidone.[4]

Potentiators of Risperidone

No Potentiation combinations with Risperidone have been added to this wiki yet.

Different Uses for Risperidone

Risperidone has shown efficacy in the treatment of obsessive compulsive disorder in combination with an SSRI. [5]

Recreational use of Risperidone

Using Risperidone for ...

Using Risperidone for ...

Pharmacology of Risperidone

General

Risperidone is a selective monoaminergic antagonist.

Targets, Enzymes, and Transporters

Targets

Target​
	Action​
Serotoninergic 5HT2	Antagonist, high affinity
Dopaminergic D2	Antagonist, high affinity
Alpha1-adrenergic	Antagonist, moderate affinity
H1-Histamine	Antagonist, low affinity
Alpha2-adrenergic	Antagonist, low affinity

Enzymes

Enzyme​
	Action​

Transporters

Transporter​
	Action​

Chemistry of Risperidone

Property​
	Values​
Systematic(IUPAC) name:	3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one
Synonyms:	Consta, Risperdal, R64766, Risperidone.
Molecular Formula:	C23H27FN4O2
Molar mass:	410.485g/mol.
CAS Registry Number:	106266-06-2
Melting Point:	170 ℃
Boiling Point:	No data
Flash Point:	No data
Solubility:	2.8mg/L
Additional data:
Notes:
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[6]

Reagent test results of Risperidone

The Dangers of Risperidone

General Warnings

Increased mortality in elderly patients with dementia compared to placebo.
Higher instances of cerebrovascular events such as stroke in elderly patients with dementia compared to placebo.

Side Effects and Interactions

Potential Side Effects

Nasopharyngitis
Upper respiratory tract infection
Sinusitis
Urinary tract infection
Anaemia
Hypersensitivity
Insomnia
Anxiety
Nervousness
Parkinsonism
Akathisia
Somnolence
Dizziness
Sedation
Tremor
Dystonia
Lethargy
Dizziness postural
Dyskinesia
Syncope
Vision blurred
Ear pain
Tachycardia
Orthostatic hypotension
Hypotension
Nasal congestion
Dyspnoea
Epistaxis
Sinus congestion
Nausea
Constipation
Dyspepsia
Vomiting
Diarrhoea
Salivary hypersecretion
Dry mouth
Abdominal discomfort
Abdominal pain
Stomach discomfort
Abdominal pain upper
Rash
Dry skin
Dandruff
Seborrhoeic dermatitis
Hyperkeratosis
Back pain
Arthralgia
Pain in extremity
Urinary incontinence
Ejaculation failure
Fatigue
Asthenia
Pyrexia
Chest pain

Potential Drug Interactions

Levodopa and other dopamine agonists.
Medications that increase QT interval or are known to cause electrolyte imbalance and inhibitors of hepatic metabolism of risperidone.
Carbamazepine and other CYP 3A4 hepatic enzyme inducers.
Fluoxetine and paroxetine
Topiramate
Phenothiazones, tricyclic antidepressants and some beta blockers

Potential Food Interactions

Oral solution is not compatible with Tea or Cola.

Physical Health Risks

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<Physical Problem 2 - Please Identify and Add Others As Necessary>

Mental Health Risks

<Mental Health Risk 1 - Please Identify and Add Others As Necessary>

<Mental Health Risk 2 - Please Identify and Add Others As Necessary>

Overdose

Most reported signs and symptoms of overdose have been an exageration of the known effects of risperidone. QT-prolongation and convulsions have been reported.

Reported Deaths

No data.

Producing Risperidone

Forms of Risperidone

Risperidone is available in oral tablet, oral solution and intra-muscular injection forms.

Legal Status of Risperidone

United Nations

USA

Unscheduled but prescription only.

EU

Other Countries

History of Risperidone

Study of risperidone began in the late 1980s and it was approved for sale in the United States in 1993. It is on the World Health Organisation's list of essential medicines.

Insights for Risperidone

Risperidone

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References

1. ^U.S. National Library of Medicine. (2015). Risperidone.
2. ^US food and drug administration. (2016). Risperidone.
3. ^Dean, A. (2006). Illicit drugs and drug interactions. Australian Pharmacist. 25 9. 684-689.
4. ^Medsafe. (2015). Data Sheet Risperidone Tablets.
5. ^Dold, M, Aigner, M, Lanzenberger, R, Kasper, S. (2013). International Journal of Neuropsychopharmacology. Antipsychotic augmentation of serotonin reuptake inhibitors in treatment-resistant obsessive-compulsive disorder: a meta-analysis of double-blind, randomized, placebo-controlled trials .
6. ^National Center for Biotechnology Information. PubChem Compound Database; CID=5073.

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