Paliperidone (Paliperidonum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Neuroleptics

Included in the formulation
  • Invega®
    pills inwards 
    Johnson & Johnson, LLC     Russia
  • Xseplion
    suspension w / m 
    Johnson & Johnson, LLC     Russia
  • Trevikta
    suspension w / m 
    Johnson & Johnson, LLC     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    N.05.A.X   Other antipsychotics

    N.05.A.X.13   Paliperidone

    Pharmacodynamics:

    Paliperidone is a centrally acting antagonist of dopamine D2 receptors, which also has a high antagonism against serotonin 5-HT2 receptors. Besides, paliperidone is an antagonist of α1 and α2-adrenergic receptors and H1-histamine receptors. Paliperidone does not have affinity for cholinergic, muscarinic, and β1- and β2-adrenergic receptors. The pharmacological activity of the (+) and (-) - enantiomers of paliperidone is the same in qualitative and quantitative terms.

    The antipsychotic effect is due to the blockade of D2-dopaminergic receptors of the mesolimbic and mesocortical system. A balanced central antagonism to serotonin and dopamine contributes to a decrease in extrapyramidal side effects and to the expansion of the therapeutic effect of the drug to include negative and productive symptoms of schizophrenia.

    Pharmacokinetics:

    After oral administration, it absorbs up to 28% in the gastrointestinal tract.After intramuscular injection due to low solubility in water is slowly absorbed into the systemic circulation. The maximum concentration in the blood plasma is reached after 13-14 days after intramuscular injection and 24 hours after reception inside. The connection with plasma proteins is 74%.

    Metabolism in the liver.

    The elimination half-life is 23 hours. Elimination by the kidneys (80%) and with feces (20%), unchanged - about 56%.

    Indications:

    It is used to treat schizophrenia and to prevent the recurrence of schizophrenia.

    ICD-10

    V.F20-F29.F20   Schizophrenia

    V.F20-F29.F21   Chrysotile disorder

    V.F20-F29.F22   Chronic delusional disorders

    V.F20-F29.F23   Acute and transient psychotic disorders

    V.F20-F29.F25   Schizoaffective disorder

    V.F20-F29.F29   Inorganic psychosis, unspecified

    Contraindications:

    Individual intolerance.

    Carefully:

    Use with caution in the following diseases: IHD, postinfarction states, conduction disorders of the myocardium, arterial hypotension, epilepsy, diabetes, obesity. It is necessary to adjust the dose for physical exertion associated with increased sweating (dehydration).

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside in the morning on 3-12 mg / sut.

    Intramuscularly (in the deltoid muscle): 150 mg on the first day and 100 mg after 1 week, then 75 mg monthly in the deltoid or gluteus muscle.

    The highest daily dose: 12 mg inwards and 150 mg for intramuscular injection.

    The highest single dose: 12 mg inwards and 150 mg for intramuscular injection.

    Side effects:

    Common reactions: influenza-like intoxication syndrome, a feeling of heaviness in the head, dizziness, bloating, heat stroke.

    Central and peripheral nervous system: sleeplessness at night and drowsiness during the day, tremor, dizziness, suicidal tendencies, nervousness, changes in libido (rising or falling), restless legs syndrome, slowing down mental activity. Rarely - nonsense, obsessive thoughts, depression of consciousness.

    Circulatory system: orthostatic hypotension, arrhythmia, vasovagal syndrome, thrombophlebitis.

    Respiratory system: shortness of breath, pneumonia, hiccough.

    Digestive system: nausea, indigestion, vomiting, caries, swelling of the tongue, incontinence of the stool.

    Sense organs: pain and noise in the ears, dry eye syndrome, loss or perversion of taste, photophobia.

    Musculoskeletal system: myalgia, convulsive syndrome, myasthenia gravis.

    Dermatological reactions: urticaria, dry skin, hyperhidrosis, alopecia, seborrhea.

    Urinary system: urinary incontinence, cystitis, painful erection.

    Allergic reactions.

    Overdose:

    Symtomas: orthostatic collapse, asthenia, tachycardia, extrapyramidal disorders.

    Treatment: symptomatic.

    Interaction:

    Potentiates the effect of α1-adrenoblockers, increases the risk of orthostatic hypotension.

    When the drug is treated with alcohol, it increases the inhibition of the central nervous system.

    When interacting with anticholinergics, the risk of developing hyperthermia increases.

    The risk of toxic effects increases with simultaneous use with intraconazole, ketonazole, fluoxetine, paroxetine.

    Inductors CYP3A4 (carbamazepine) reduce the effectiveness of paliperidone treatment, which requires doubling the dosage.

    Special instructions:

    When treated with paliperidone it is necessary to monitor blood glucose levels, check the condition of the fundus and tendon reflexes.

    Persons receiving the drug on an outpatient basis are forbidden to drive a car and work in production with moving mechanisms.

    Instructions
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