Index of drugs

Treatment of schizophrenia in adults. Treatment of mania or mixed episodes of moderate intensity in the course of bipolar disorder in adults, children and adolescents from 10 years of age.

1 capsule contains 20 mg, 40 mg, 60 mg or 80 mg of ziprasidone hydrochloride.

An antipsychotic drug. Zyprasidone has a high affinity for type 2 dopaminergic receptors (D.₂) and clearly greater affinity for type 2A serotonergic receptors (5HT_2A). It also works on 5HT serotoninergic receptors_2C, 5HT_1D and 5HT_1Awherein its affinity for the binding sites of these receptors is equal to or greater than the affinity for the D-type receptor₂. Has moderate affinity to neuronal transporters of serotonin and norepinephrine and to histamine H-type receptors₁ and alpha receptors₁. It has negligible affinity for M-muscarinic receptors₁. Ziprasidone was antagonistic to both serotonergic 5HT receptors_2Aas well as dopaminergic D receptors₂. It is believed that the antipsychotic effect is partly due to the association of the above antagonistic activities. After oral administration, the maximum concentration of the drug in the blood serum is observed 6-8 hours after taking the drug. The absolute oral bioavailability of 20 mg is 60%. Studies have shown that the bioavailability of the drug may increase by up to 100% in the presence of food. The average half-life is 6.6 h. The drug is associated with plasma proteins in more than 99%. Zyprasidone used orally is subject to intense metabolic changes and only a small amount of the drug is excreted in the urine (<1%) and faeces (<4%) in unchanged form. Zyprasidone is converted in three metabolic pathways to 4 major metabolites. About 20% of the administered dose is excreted in the urine, about 66% - with faeces. In mild to moderate (Child-Pugh grade A or B) hepatic insufficiency in cirrhosis, after oral administration the level of ziprasidone was 30% higher and the half-life was 2 hours longer than in healthy patients.

Hypersensitivity to ziprasidone or other ingredients of the preparation. QT prolongation found. Congenital prolongation of the QT interval. Fresh myocardial infarction. Uncompensated heart failure. Arrhythmias treated with antiarrhythmic agents from groups IA and III. Concomitant treatment with QT prolonging drugs, such as antiarrhythmics from group IA and III, arsenic trioxide, halofantrine, levometadyl acetate, mesoridazine, thioridazine, pimozide, sparfloxacyna, gatifloxacin, moxifloxacin, dolasetron methanesulfonate, meflox, sertindole, cisapride.

Particularly cautiously use in patients with severe hepatic impairment - there is no experience regarding the use of the drug in these patients. Caution is advised in patients with significant bradycardia, electrolyte disturbances (hypokalaemia, hypomagnesaemia), patients with a history of seizures and patients with risk factors for stroke. In patients with stable cardiac disease before starting treatment, ECG should be considered. If the QT interval_c > 500 it is recommended to stop the drug. In case of symptoms of a neuroleptic malignant syndrome, all antipsychotics, also ziprasidone, should be discontinued. If symptoms of tardive dyskinesia appear, dose reduction or interruption of treatment with ziprasidone should be considered. The safety and efficacy of ziprasidone in pediatric patients with schizophrenia have not been studied. The preparation contains lactose and should not be used in patients with hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

There are no studies in pregnant women. Women of childbearing age should use an effective method of contraception. Pregnancy is not recommended unless the expected benefit to the mother outweighs the potential risk to the fetus.It is not known whether the drug is excreted in milk. You should not breastfeed during treatment with ziprasidone.

Common: restlessness, dystonia, akathisia, extrapyramidal disorder, parkinsonism (including symptom of the toothed wheel, slowness of movement, hypokinesis), tremor, dizziness, sedation, drowsiness, headache, blurred vision, nausea, vomiting, constipation, indigestion, dryness oral mucosa, excessive salivation, musculoskeletal stiffness, weakness, fatigue. Uncommon: increased appetite, agitation, anxiety, feeling of tightness in the throat, nightmares, generalized tonic-clonic convulsions, tardive dyskinesia, dyskinesias, salivation, ataxia, speech disorders, forcible vision with eye rotation, concentration disorders, excessive need sleep, hypoesthesia, paresthesia, lethargy, palpitations, tachycardia, photophobia, dizziness, tinnitus, hypertensive crisis, hypertension, orthostatic hypotension, hypotension, dyspnoea, sore throat, diarrhea, dysphagia, gastritis, discomfort in the cavity abdominal swelling, tongue thickening, bloating, urticaria, rash (also papular-macular), acne, musculoskeletal discomfort, muscle spasms, limb pain, joint stiffness, chest discomfort, gait disturbance, pain, thirst, increased liver enzymes. Rare: rhinitis, hypocalcaemia, panic attacks, depressive symptoms, mental slowness, shallower affectation, anorgasmia, torticollis, paresis, immobility, increased tension, restless legs syndrome, lymphopenia, blurred vision (including amblyopia), pruritus of the eyes, dry eyes , ear pain, systolic hypertension, diastolic hypotension, variable blood pressure, hiccups, gastro-intestinal reflux, loose stools, psoriasis, allergic dermatitis, alopecia, facial edema, erythema, follicular rash, skin irritation, trismus, incontinence, dysuria, erectile dysfunction, increased erections, galactorrhea, gynecomastia, fever, feeling hot, prolonged QT interval_c, abnormal liver function tests, increase in blood lactate dehydrogenase, increase in eosinophil counts. In addition, there was observed: insomnia, mania / hypomania, increased prolactin concentration in the blood, insomnia, neuroleptic malignant syndrome, serotonin syndrome, facial muscle paralysis, arrhythmiastorsade de pointes, fainting, venous thromboembolism, hypersensitivity reactions, anaphylactic reactions, angioneurotic edema, involuntary urination, priapism, neonatal withdrawal syndrome.

Orally.Adults: the recommended dose in schizophrenia and bipolar disorder is 40 mg 2 times a day. Depending on the clinical condition of the patient, this dose may then be increased to a maximum of 80 mg twice daily. If indicated, the highest recommended dose can be used from day 3 of treatment. Do not use doses higher than 160 mg daily. For maintenance treatment, the lowest effective dose should be used in patients with schizophrenia; in many cases a 20 mg twice daily dose may be sufficient.
There is no need to adjust the dose in patients with impaired renal function. In patients with hepatic impairment, a dose reduction should be considered. In the elderly, a reduction in the initial dose is not usually desirable, but should be considered in patients over 65 years of age.Bipolar disorder in children and adolescents from 10 years of age: in acute conditions, 20 mg in a single dose on the first day of treatment. In the following days, the drug should be administered in 2 divided doses, and the daily dose should be increased for 1-2 weeks, until the target values ​​of 120-160 mg / day in patients with m.c. ≥45kg or 60-80 mg / day in patients over m <45kg. In the later period, the dosage should be selected individually in the range of 80-160 mg / day in patients with m.c. ≥45kg or 40-80 mg / day in patients of over 45 kg. In the clinical trial an uneven distribution of divided doses was allowed (the morning dose was 20 or 40 mg lower than the evening dose). Do not exceed the maximum doses of 160 mg / day in patients with m.c. ≥45kg or 80 mg / day in patients of over 45kg.Way of giving. The capsules should be taken with food.