What is Risperidone?
Risperidone is an active ingredient used for Schizophrenia and moderate to severe manic episodes associated with bipolar disorder.
The brand names of Risperidone in United States are Risperdal, Risperdal Consta, Perseris and Risperdal M-Tab.
Risperidone Mechanism of Action (MOA)
Selective monoaminergic antagonist, with high affinity for serotonergic 5-HT2 and dopaminergic D2 receptors.
Therapeutic indications, uses and benefits of Risperidone
Oral use:
- Schizophrenia.
- Moderate to severe manic episodes associated with bipolar disorder.
- Short-term treatment (up to 6 weeks) of persistent aggression in patients with moderate to severe Alzheimer’s type dementia who do not respond to other non-pharmacological measures and when there is a risk of harm to them or others.
- Short-term treatment (up to 6 weeks) of persistent aggression in behavioral disorders in children ≥ 5 years and adolescents with below-average intellectual functioning or mental retardation diagnosed according to the DSM-IV criterion, in which the severity of the aggression or other disruptive behaviors requires pharmacological treatment.
Parenteral:
- Maintenance of schizophrenia in patients currently stabilized with oral antipsychotics.
Posology of Risperidone
Oral:
– Schizophrenia, adults: initial, 2 mg/day (one dose or in 2), increase to 4 mg on the second day; then maintain or individualize if necessary.
Most benefit from doses of 4-6 mg/day. Maximum 16 mg/day.
Elderly: initial 0.5 mg 2 times/day; individualize in increments of 0.5 mg, 2 times/day, up to 1-2 mg, 2 times/day.
Children < 18 years: not recommended.
– Manic episode in bipolar disorder, adults: start at 2 mg/day, increase by 1 mg/day, if required.
Recommended dose, 1 to 6 mg/day.
Elderly: initial 0.5 mg 2 times/day; individualize in increments of 0.5 mg, 2 times/day to 1-2 mg, 2 times/day.
Children < 18 years: not recommended.
– Persistent aggression in patients with moderate to severe Alzheimer’s type dementia: initial 0.25 mg 2 times/day; adjust, if necessary, with increments of 0.25 mg 2 times/day on alternate days.
– Behavioural disorders in children aged 5-18 years:
≥ 50 kg: initial, 0.5 mg/day, individual adjustment with an increase of 0.5 mg/day, often no more than every other day; dose range 0.5-1.5 mg/day.
< 50 kg: initial, 0.25 mg/day, individual adjustment with an increase of 0.25 mg/day, often no more than every other day; dose range 0.5-0.75 mg/day.
Children < 5 years: not recommended.
Renal insufficiency and hepatic insufficiency: regardless of the indication, both initial and consecutive doses should be reduced by half.
Parenteral:
Adults. Intramuscular, initial: 25 mg every 2 weeks, for doses of ≤ 4 mg of oral risperidone (2 or more weeks), with higher doses titrate doses of 37.5 mg.
After the first injection an antipsychotic coverage with oral risperidone or the antipsychotic previously used must be guaranteed for the first 3 weeks.
Maintenance: 25 mg every 2 weeks, may be increased to 37.5 or 50 mg at a frequency not < 4 weeks. Maximum 50 mg/2 weeks.
Children < 18 years: not recommended.
Method of administration of Risperidone
Buccodispersible tablets: place on the tongue, it will begin to disintegrate in seconds; water can be used if desired.
Oral solution: drink with a non-alcoholic beverage, except tea.
Contraindications of Risperidone
Hypersensitivity to risperidone.
Warnings and Cautions with Risperidone
Cardiovascular disease, family history of prolonged QT interval and concomitant use with originating medications, bradycardia, electrolytic disorders (hypokalemia, hypomagnesemia), history of seizures.
Elderly people, renal insufficiency, hepatic insufficiency, patients with risk of cerebral attack, pre-existing hyperprolactinemia and prolactin-dependent tumors.
Situations that contribute to a rise in body temperature, risk factors for venous thromboembolism.
Due to its antiemetic effect, it can mask signs and symptoms of overdose of certain medications or disorders such as intestinal obstruction, Reye’s syndrome and brain tumors.
Evaluate risk/benefit in Parkinson’s disease or dementia of Lewis bodies.
Monitor symptoms of hyperglycemia in all patients and especially in diabetics.
Monitor weight.
Stop treatment if signs of MNS and/or tardive dyskinesia or stroke appear.
If there is a risk of orthostatic hypotension, reduce the dose.
In elderly with dementia, treatment alone or in combination with furosemide was associated with increased mortality, assess risk/benefit.
Analyze physical and social causes of aggressive behavior and control sedative effect by learning capacity problem before administering to children.
Risk of developing intraoperative flaccid iris syndrome during and after cataract surgery.
Risk of leukopenia, neutropenia and agranulocytosis, monitor.
With severe neutropenia interrupt treatment and control white blood cell levels until recovery.
Injectable: Anaphylactic reactions have rarely been reported in patients who have previously tolerated oral risperidone.
Liver failure
Caution. Regardless of the indication, both initial and consecutive doses should be reduced by half (oral).
Kidney failure
Caution. Regardless of the indication, both initial and consecutive doses should be reduced by half (oral).
Interactions with Risperidone
- Risk of increased sedation with: alcohol, opiates, antihistamines, and benzodiazepines.
- Plasma concentration decreased by: carbamazepine, phenytoin, rifampicin, phenobarbital.
- Plasma concentration increased by: fluoxetine, paroxetine, verapamil, phenothiazines, tricyclic antidepressants, some ß-blockers, itraconazole.
- May antagonize effect of: levodopa and other dopamine agonists.
- Risk of hypotension with: antihypertensive.
- Not recommended for use with: paliperidone.
Pregnancy and Risperidone
It was not teratogenic in animal studies, but other types of reproductive toxicity were observed.
The possible risk to humans is unknown. Therefore, it should not be used unless clearly necessary.
Breastfeeding
In animal studies, risperidone and 9-hydroxy-risperidone are excreted in milk. It has been shown that they are also excreted in small amounts in human milk.
No data on adverse effects in infants are available. Therefore, the benefit of breastfeeding should be weighed against the possible risks to the child.
Effects on driving ability
Risperidone acts on the central nervous system and can cause: drowsiness, dizziness, visual disturbances and decreased ability to react.
These effects as well as the disease itself make it advisable to be cautious when driving vehicles or operating dangerous machinery, especially until each patient’s particular sensitivity to the medication has been established.
Adverse reactions and side effects of Risperidone
Upper respiratory tract infection, pneumonia, bronchitis, sinusitis, urinary tract infection, flu.
Hyperprolactinemia; hyperglycemia, weight gain, increased appetite, decreased weight, decreased appetite.
Insomnia, depression, anxiety, sleep disorders, agitation.
Parkinsonism, headache, sedation/somnolence, akathisia, dystonia, dizziness, dyskinesia, tremor.
Blurred vision; tachycardia; hypotension, hypertension.
Dyspnea, pharyngeal pain, cough, nasal congestion.
Abdominal pain, abdominal discomfort, vomiting, nausea, constipation, gastroenteritis, diarrhea, dyspepsia, dry mouth, toothache.
Exanthema; muscle spasms, musculoskeletal pain, back pain, arthralgia.
Urinary incontinence; erectile dysfunction, amenorrhea, galactorrhea.
Edema, pyrexia, chest pain, asthenia, fatigue, pain.
Increased transaminases, increased gammaglutamyltransferase; falls.
Intramuscular: anemia, pain at the injection site, reaction at the injection site.
⭐⭐⭐⭐⭐ VIDEO OF RISPERIDONE/RISPERDAL (DRUG)
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
Resources:
UNII: L6UH7ZF8HC
ChemIDplus
DrugPortal
PubChem CID: 5073
NCI Thesaurus: C29416