Aripiprazole - instructions for use, dose, side effects, contraindications

Strongly binds to serotonin 5-HT1A- and 5-HT2A-receptors, dopamine D2- and D3-receptors. Moderately binds to 5-HT7-, α1-adrenergic and histamine H1 receptors, dopamine D4-, serotonin 5-HT2C receptors.

Reduces the processes of excitability in the central nervous system, causes orthostatic hypotension.

Pharmacokinetics:

It is taken orally, absorbed into the stomach. Maximum the concentration in the blood plasma comes in 3-4 hours. Bioavailability of the drug is 87%. It binds to blood proteins in 99%.

Half-life is 75 hours for fast metabolites, for slow metabolites, 146 hours, 94 hours for active metabolites.

Metabolized in the liver by hydroxylation, dehydrogenation, N-dealkylation.

The drug is not removed from the blood plasma during hemodialysis.

Elimination with feces in 55%, of them in 18% unchanged with kidneys about 25%, less than 1% - unchanged.

Indications:

It is used for the treatment of endogenous psychoses both at the stage of exacerbation and as a supporting agent during the period of remission of the disease.

ICD-10

V.F20-F29.F20 Schizophrenia

V.F20-F29.F21 Chrysotile disorder

V.F30-F39.F30 Manic episode

V.F30-F39.F31 Bipolar affective disorder

Contraindications:

Individual intolerance.

Carefully:

Use with caution in the following diseases: coronary heart disease, post-infarction states, violations of myocardial conductivity, arterial hypotension, epilepsy, diabetes, obesity. It is necessary to adjust the dose for physical exertion associated with increased sweating (dehydration).

Pregnancy and lactation:

Pregnancy and lactation: recommendations for Food and Drug Administration (US Food and Drug Administration) - Category C. The drug has hepatotoxicity. Pregnant and lactating is contraindicated.

Dosing and Administration:

Dosage is selected individually, the drug is taken orally once a day, regardless of the time of ingestion.

The highest daily dose: 30 mg.

The highest single dose: 30 mg.

Side effects:

Common reactions: flu-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 (increase or decrease), restless legs syndrome, slowing of mental activity. Rarely - nonsense, obsessive thoughts, depression of consciousness.

The 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:

Orthostatic collapse, asthenia, tachycardia, extrapyramidal disorders.

Treatment is symptomatic.

Interaction:

Potentiates the action of α₁- adrenoblockers - the risk of orthostatic hypotension increases.

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 treatment with aripiprazole, which requires doubling the dosage.

Special instructions:

When treating aripiprazole 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

Aripiprazole (Aripiprazolum)