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Brand Name :
Nuplazid
Synonyms :
pimavanserin
Class :
Atypical antipsychotics, second Generation
Dosage forms & Strengths
Tablet
10mg
Capsule
34mg
Safety and efficacy not established.
pimavanserin carries a black box warning for increased mortality with dementia-related psychosis in elderly patients.
Geriatric patients with dementia associated psychosis treated with antipsychotic medications, including pimavanserin, are at an increased risk of death compared to placebo.
may decrease the therapeutic effect when combined with anti-parkinson agents
may decrease the therapeutic effect when combined with anti-parkinson agents
may decrease the therapeutic effect when combined with anti-parkinson agents
may decrease the therapeutic effect when combined with anti-parkinson agents
may decrease the therapeutic effect when combined with anti-parkinson agents
may enhance the risk of hypertension when combined
may enhance the risk of hypertension when combined
may enhance the risk of hypertension when combined
may enhance the risk of hypertension when combined
may enhance the risk of hypertension when combined
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
aluminum hydroxide/magnesium carbonate
may diminish the absorption of Antacids
may decrease the therapeutic effect of each other when combined
may decrease the therapeutic effect when combined with antipsychotic agents
CYP3A strong enhancers of the small intestine may reduce the bioavailability of pimavanserin
may decrease the therapeutic effect of cabergoline
metoclopramide increases the toxicity of antipsychotic agents
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the adverse effect of amphetamines
may increase the adverse effect of amphetamines
may increase the adverse effect of amphetamines
may increase the adverse effect of amphetamines
may increase the adverse effect of amphetamines
may increase the levels of serum concentration of pimavanserin
may increase the levels of serum concentration of pimavanserin
may increase the levels of serum concentration of pimavanserin
may increase the levels of serum concentration of pimavanserin
may increase the levels of serum concentration of pimavanserin
may have an increased neurotoxic effect when combined with antipsychotic agents
may have an increased neurotoxic effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with beta-blockers
may have an increased hypotensive effect when combined with beta-blockers
may have an increased hypotensive effect when combined with beta-blockers
may diminish the therapeutic effect of the drug
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
CYP3A4 inhibitors increase the concentration of pimavanserin in serum
it may increase the neurotoxic effect of antipsychotic agents
It may increase the neurotoxic effect of Antipsychotic Agents
seizure lowering agents increase the toxic or adverse effects of other antipsychotic agents
seizure lowering agents increase the toxic or adverse effects of other antipsychotic agents
it may increase the risk of adverse effect of amphetamines
it may increase the risk of adverse effect of amphetamines
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the hypotensive effects
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may diminish the therapeutic effect of antipsychotic agents
may diminish the therapeutic effect of antipsychotic agents
may diminish the therapeutic effect of antipsychotic agents
may diminish the therapeutic effect of antipsychotic agents
may diminish the therapeutic effect of antipsychotic agents
may decrease the absorption of antipsychotic agents
may decrease the absorption of antipsychotic agents
may decrease the absorption of antipsychotic agents
may decrease the absorption of antipsychotic agents
may decrease the absorption of antipsychotic agents
may enhance the hypotensive effect of antipsychotic agents
may enhance the hypotensive effect of antipsychotic agents
may enhance the hypotensive effect of antipsychotic agents
may enhance the hypotensive effect of antipsychotic agents
may enhance the hypotensive effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may increase the hypotensive effect of beta blockers
may increase the hypotensive effect of beta blockers
may increase the toxic effect of amphetamines
may increase the hypotensive effect of blood pressure-lowering agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the toxic effect of seizure threshold-lowering potential agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may increase the hypotensive effect of Blood Pressure Lowering Agents
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may increase the hypotensive effect of Blood Pressure Lowering Agents
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increasingly adverse effect when combined with antipsychotic agent
they decrease the absorption of antipsychotic agents
they decrease the absorption of antipsychotic agents
antipsychotic agents increase the effect of beta-blockers
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
Could potentially amplify the toxicity of antipsychotic agents
The efficacy of guanethidine could be reduced by the presence of antipsychotic agents
Could potentially amplify the toxicity of antipsychotic agents
may have an increased neurotoxic effect when combined with antipsychotic agents
may have an increased neurotoxic effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
cimetidine: they may decrease the therapeutic effect of antipsychotics
topiramate: they may decrease the therapeutic effect of antipsychotics
barbiturates: they may decrease the therapeutic effect of antipsychotics
barbiturates: they may decrease the therapeutic effect of antipsychotics
barbiturates: they may decrease the therapeutic effect of antipsychotics
barbiturates: they may decrease the therapeutic effect of antipsychotics
barbiturates: they may decrease the therapeutic effect of antipsychotics
may have an increasingly adverse effect when combined with antipsychotic agents
Actions and Spectrum:
pimavanserin is a medication used to treat and symptoms related with PD psychosis. It is a selective serotonin inverse agonist and antagonist (SSIA) of the 5-HT2A receptor, which means it blocks the activity of serotonin at this receptor site.
pimavanserin has a high affinity for the 5-HT2A receptor and does not have significant affinity for other receptors, such as dopamine or adrenergic receptors, which distinguishes it from other antipsychotic medications. This selective activity at the 5-HT2A receptor allows pimavanserin to improve psychosis symptoms without worsening motor symptoms in patients with Parkinson’s disease.
pimavanserin is generally not approved for the treatment of other forms of psychosis, such as schizophrenia or bipolar disorder. Overall, pimavanserin has a narrow spectrum of action and is used only for the treatment of Parkinson’s disease psychosis. Its selective activity at the 5-HT2A receptor makes it a unique and important option for patients with this condition.
Frequency defined
1-10%
Peripheral edema (7%)
Nausea (7%)
Constipation (4%)
Confusional state (6%)
Gait disturbance (2%)
Hallucinations (5%)
Black Box Warning:
pimavanserin carries a black box warning for increased mortality with dementia-related psychosis in elderly patients. Geriatric patients with dementia associated psychosis treated with antipsychotic medications, including pimavanserin, are at an increased risk of death compared to placebo.
pimavanserin is generally not approved for the treatment of dementia-related psychosis and is only indicated for the treatment of delusions and hallucinations associated with Parkinson’s disease psychosis.
Healthcare providers should carefully evaluate the risks and benefits of using pimavanserin in elderly patients with dementia-related psychosis and consider alternative treatments when possible.
Contraindication/Caution:
Contraindication
Caution
Pregnancy consideration:
US FDA pregnancy category: Not assigned.
Lactation:
Excreted into human milk is Not known.
Pregnancy category:
Pharmacology:
pimavanserin is a selective serotonin 5-HT2A receptor inverse agonist and antagonist. It acts as an inverse agonist at the 5-HT2A receptor, meaning that it reduces the activity of the receptor below its basal level, and as an antagonist, meaning that it blocks the activity of the receptor in response to its natural ligands.
The 5-HT2A receptor is believed to play a role in the development of symptoms related with PD psycosis. By blocking the activity of this receptor, pimavanserin reduces the activity of the brain circuits that contribute to these symptoms.
Pharmacodynamics:
Mechanism of action: pimavanserin has selective activity as both an inverse agonist (inhibitor) and an antagonist (blocker) of serotonin specifically targeting the 5-HT2A receptors in the brain. These receptors are thought to be significant in the development of psychotic symptoms.
Pharmacokinetics:
Absorption
The peak plasma concentration of the drug occurs approximately 6 hours after administration, with a range of 4 to 24 hours. It takes about 6 hours for the drug to be metabolized into its active form.
Distribution
The drug is highly protein-bound, with approximately 95% of the drug binding to plasma proteins. The apparent volume of distribution (Vd) is 2173 liters, indicating that the drug is extensively distributed throughout the body.
Metabolism
The drug is primarily metabolized by the enzymes CYP3A4 and CYP3A5, with additional contributions from CYP2J2, CYP2D6, and other CYP and FMO enzymes. The major active metabolite (AC-279) is predominantly formed by the action of CYP3A4.
Elimination and Excretion
The half-life of the drug pimavanserin is 57 hours, while the half-life of its active metabolite is much longer at 200 hours. After 10 days, approximately 0.55% of the drug is excreted unchanged in urine, and 1.53% is excreted unchanged in feces. Less than 1% of the administered dose and active metabolite are recovered in urine.
Administration:
Oral administration
pimavanserin is available as an oral tablet and is typically taken one time a day with or without food.
It is key to follow the dosing instructions provided by the healthcare provider and to take the medication as directed. pimavanserin should not be crushed, chewed, or broken, and should be swallowed whole with a glass of water.
If a dose of pimavanserin is missed, it should be taken as soon as possible, but should not be doubled to make up for a missed dose. It is important to maintain a regular dosing schedule to ensure the medication is effective.
If a patient experiences any new or worsening symptoms while taking pimavanserin, they should contact their healthcare provider immediately. This could include changes in mood, behavior, or thinking, as these could be signs of a serious condition.
Patient information leaflet
Generic Name: pimavanserin
Pronounced: [ PIM-a-VAN-ser-in- ]
Why do we use pimavanserin?
pimavanserin is a medication that is used to treat delusions and hallucinations associated with Parkinson’s disease psychosis.It is a non-motor symptom of Parkinson’s disease that affects up to 50% of patients and can significantly impact their quality of life. The symptoms of Parkinson’s disease psychosis can include visual hallucinations, auditory hallucinations, and delusions.
pimavanserin is the first and only FDA-approved medication for the treatment of Parkinson’s disease psychosis. It works by selectively blocking serotonin 5-HT2A receptors in the brain, which are believed to be involved in the development of hallucinations and delusions.
By treating these symptoms, pimavanserin can help in improving overall quality of life for patients with Parkinson’s disease psychosis and their caregivers. It may also reduce the burden of caregiving and potentially delay the need for nursing home placement. It is important to note that pimavanserin is not approved for the treatment of other types of hallucinations or delusions, such as those associated with schizophrenia or bipolar disorder.