Universal reference book for medicines
Product name: ZELDOX В® (ZELDOX В® )

Active substance: ziprasidone

Type: Antipsychotic drug (antipsychotic)

Manufacturer: PFIZER IRELAND PHARMACEUTICALS (Ireland) manufactured by BEN VENUE Laboratories (USA)
Composition, form of production and packaging
Lyophilizate for the preparation of a solution for intravenous administration of
white or almost white;
the applied solvent is a clear, colorless liquid; reconstituted solution - transparent colorless.
1 f.

ziprasidone mesylate trihydrate 40.93 mg,

which corresponds to the content of ziprasidone 30 mg

Excipients: cyclodextrin sodium sulfobutylate (SBECD).

Solvent: water d / and - 1.4 ml (taking into account the necessary excess of 0.2 ml for a guaranteed withdrawal of 1.2 mg).

Vials of colorless glass (1) complete with a solvent (amp 1 pc.) - packs of cardboard.


Description of the drug approved by the manufacturer for the printed edition of 2012.


Ziprasidone is an antagonist of both serotonin 2 A (5-HT 2A ) type receptors and type 2 dopaminergic receptors (D 2 ), which determines the antipsychotic activity of the drug.

Ziprasidone is also a potent 5-HT 2c , 5-HT ID antagonist and potent 5-HT 1A receptor agonist (the affinity of the drug for these receptors is comparable to or greater than that of D 2 receptors) and inhibits the reuptake of coradrenaline and serotonin in neurons.
Serotonergic activity of ziprasidone and its effect on the reuptake of neurotransmitters in neurons are associated with antidepressant activity. The agonism of 5-HT 1A receptors causes anxiolytic effects. The pronounced antagonism to 5-HT 2c receptors determines possible antipsychotic activity. Ziprasidone depresses the reverse neuronal seizure of serotonin and norepinephrine. An affinity for H 1 -gistamine and alfa-adrenoreceptors was also noted. Antagonism to these receptors causes the possibility of developing drowsiness and orthostatic gynotension, respectively. Ziprasidone practically does not interact with m-cholinergic receptors (antagonism to these receptors is associated with memory impairment).
According to the positron emission tomography (PET) data, the degree of blockade of the 2 A type SSR is 12% after 12 hours after a single oral dose of 40 mg is 80%, and the number of receptors is 50%.

A significant improvement in the state of psychomotor agitation is observed in patients after 15 minutes and is kept from 1 to 2 hours after administration of 10 mg of ziprasidone and from 30 minutes to 4 hours after the administration of 20 mg of ziprasidone.


Bioavailability of ziprasidone with intramuscular injection is 100%.

After a single intramuscular injection, the serum concentration reaches a maximum in about 60 minutes or earlier.
The average half-life period ranges from 2 to 5 hours. The concentration of the drug increases in accordance with the increase in the dose, and after a 3-day intramuscular application, cumulation is negligible.
The average systemic clearance of ziprasidone for intravenous administration is 7.5 ml / min / kg, and the volume of distribution is 1.5 l / kg.
Ziprasidone more than 99% binds to serum proteins and the degree of binding does not depend on the concentration of the drug.
There are 3 ways of biotransformation of ziprasidone, which lead to the formation of 4 main metabolites - benzisothiazole piperazine (BITP) sulfoxide, BITP sulfone, ziprasidone sulfoxide and S methyl dihydroziprasidone.
Approximately 20% of the dose is excreted by the kidneys and approximately 66% by the intestine. The proportion of unchanged ziprasidone from the total drug and its metabolites in the serum is about 44%.
Isozyme CYP3A4 (the most important of the cytochromes P450) catalyzes the oxidative conversion of ziprasidone.
S-methyldihydroziprasidone is formed as a result of 2 reactions catalyzed by aldehyde oxidase and thiol methyltransferase.
Ziprasidone, S-methyldihydroziprasidone and ziprasidone sulfoxide have similar properties that can cause prolongation of the QT interval.
S-methyldihydrosiprasidone is excreted primarily by the intestine and by transformations catalyzed by the CYP3A4 isoenzyme. Ziprasidone sulfoxide is excreted by renal excretion and secondary metabolism under the action of the CYP3A4 isoenzyme.
Clinically significant dependence of the pharmacokinetics of ziprasidone on age or sex with oral administration was not noted.

Significant changes in the pharmacokinetics of ziprasidone in patients with severe and moderate impairment of kidney function when taken orally compared to healthy volunteers have not been identified.

In patients with mild or moderate impairment of liver function (Child-Pugh class A or B), the serum ziprasidone concentrations are 30% higher than in healthy volunteers and the half-life is approximately 2 hours longer with cirrhosis.


- suppression of psychomotor agitation in patients with schizophrenia.


Only for intramuscular injection.
Do not administer intravenously!

The recommended dosage is from 10 mg to 20 mg (maximum 40 mg / day).
Doses of 10 mg can be administered every 2 hours; a dose of 20 mg can be administered every 4 hours (maximum 40 mg / day). The efficacy of ziprasidone for intramuscular administration for more than 3 days has not been studied.
If long-term therapy is required, the patient should be transferred from the intramuscular injection as soon as possible to receive ziprasidone capsules inside.

Application for violations of liver function

In patients with hepatic insufficiency, the dose of the drug should be reduced in proportion to the severity of the disease.

Application for smokers

Dose changes in smokers are not required.

Instructions for preparing a solution.

The contents of the vial are dissolved in 1.2 ml of the supplied water for injection;
the concentration of the resulting solution is 20 mg of ziprasidone per ml. The vial is shaken until the powder is completely dissolved. You can use only a transparent solution that does not contain any visible inclusions. From each vial, you should only take one dose of the drug, and the remainder must be poured.

The most frequent adverse reactions were nausea, sedation, dizziness, pain at the injection site, headache and drowsiness.

All undesirable reactions are listed with the distribution of classes and frequency: very often (> 1/10), often (> 1/100, but <1/10), infrequently (> 1/1000, but <1/100) and rarely <1/1000).

The undesirable reactions listed below could also be associated with concomitant pathology and / or concomitant medications.

System-Organ Class Undesirable drug reactions

Disorders of nutrition and metabolism

Uncommon Anorexia

Mental disorders

Uncommon Agitation, antisocial behavior, psychotic disorder, insomnia, tics.

Disturbances from the nervous system

Often, akathisia, dizziness, dystopia, headache, sedation, drowsiness.

Uncommon Muscular rigidity as a "cogwheel", postural dizziness, dysarthria, dyskinesia, dyspraxia, parkinsonism, tremor.

Cardiological disorders

Infrequently Bradycardia.
Disturbances from the organs of hearing and balance

Infrequently Dizziness.

Disorders of the vas from the side of the vascular system

Often, hypertension.

Infrequent hyperemia, orthostatic hypotension.

Respiratory, thoracic and mediastinal disorders

Infrequently loring-spasm

Disorders of her side of the digestive system

Often Nausea, vomiting.

Uncommon Constipation, diarrhea, dry mouth.

Disturbances from the skin and subcutaneous tissue

Infrequently Hyperhidrosis.

Disturbances from the musculoskeletal system and connective tissue

Often Rigidity of muscles.

Systemic disorders and complications at the site of administration

Often asthenia, burning at the injection site, pain at the injection site.

Infrequent withdrawal syndrome, fatigue, flu-like syndrome, discomfort at the injection site, irritation at the injection site.

Abnormalities detected in laboratory studies

Infrequent Reduction of blood pressure, increased activity of liver enzymes.

The most frequent cardiovascular adverse events reported in clinical studies of intramuscular administration of fixed doses of ziprasidone were dizziness (10 mg - 11%, 20 mg - 12%), tachycardia (10 mg - 4%, 20 mg - 4% ), postural dizziness (10 mg - 2%, 20 mg - 2%), orthostatic hypotension (20 mg - 5%) and lowering blood pressure (10 mg -2%).

In pre-registration clinical studies of intramuscular administration of fixed doses of ziprasidone, an increase in blood pressure was noted in 2.2% of patients receiving the drug at a dose of 10 mg;
In addition, an increase in blood pressure was registered in 2.8% of patients treated with ziprasidone at a dose of 20 mg.
Malignant neuroleptic syndrome (CNS) with the use of antipsychotic agents observed cases of NSA, which is a rare but potentially fatal complication.
Clinical manifestations of CNS are fever (hyperpyrexia), muscle rigidity, changes in mental status and signs of instability in the autonomic nervous system (fluctuations in heart rate or changes in blood pressure, tachycardia, profuse sweating, arrhythmias). Additional signs may include increased activity of creatine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure. If the patient develops symptoms that can be attributed to signs of the NSH, or if a high body temperature suddenly appears, not accompanied by the emergence of the remaining symptoms of the NSA, all antipsychotics, including ziprasidone, should be immediately discontinued.
The cases of CNS are noted in the post-marketing application of Zeldox.
Late dyskinesia
With prolonged use of ziprasidone, as well as other antipsychotics, there is a risk of developing tardive dyskinesia and other distant extrapyramidal syndromes.
When there are signs of late dyskinesia, it is advisable to reduce the dose of ziprasidone or to cancel it.
An increase in the incidence of death on the background of the use of neuroleptics in elderly patients with dementia, combined with psychosis.

In elderly patients with psychosis caused by dementia, the risk of death is increased with the use of some neuroleptics compared with placebo.
The results obtained during the research of ziprasidone do not allow to conclude that the risk of death in elderly patients with psychosis caused by dementia on the background of taking the drug increases. However, ziprasidone is not recommended for treatment of this category of patients.

- hypersensitivity to ziprasidone or any other component of the drug;

- prolongation of the QT interval in the history, including congenital syndrome of the extended QT interval;

- acute and subacute stage of myocardial infarction;

- heart failure in the stage of decompensation;

- joint administration of drugs that extend the QT interval, in particular antiarrhythmics of classes 1A and III, arsenic anhydride, halofantrine, methadone, mesoridazine, thioridazine, pimozide, sparfloxacin, gatifloxacin, moxifloxacin, dolasatron, mefloquine, sertindole or cisapride;

- Patients with psychosis due to dementia.

- the efficacy and safety of ziprasidone in patients under the age of 18 years and in the elderly over 65 years are not established.

With caution :

QT interval prolongation, myocardial infarction, unstable angina It is believed that there is a relationship in the occurrence of QT interval elongation and paroxysmal ventricular arrhythmia (torsade des pointes), which is potentially life-threatening (a similar effect is caused by some drugs, including class I and III antiarrhythmics section Contraindications)).
When observing the symptoms that confirm the occurrence of arrhythmia during the treatment with ziprasidone, a heart function test should be performed. If the QTc interval exceeds 500 ms, it is recommended to stop treatment (see Contraindications section). There were rare cases of paroxysmal ventricular arrhythmia (torsade de pointes) in patients with multiple mixed risk factors taking ziprasidone during post-marketing use, although there was no causal relationship with the drug.
Ziprasidone should be administered with caution to patients with the following risk factors that may aggravate the occurrence of such an arrhythmia:


- Electrolyte imbalance;

- use with other drugs that extend the QT interval.

Caution should be exercised when prescribing ziprasidone to patients who have recently undergone myocardial infarction, as well as to patients with unstable angina, as the efficacy and safety of ziprasidone in patients with these diseases has not been established.


Application in pregnancy

Women of reproductive age should use a reliable method of contraception.
Given the limited experience of using the drug in humans, ziprasidone is not recommended to be administered during pregnancy, except when the expected benefit of treatment for the mother justifies the possible risk to the fetus.
Application when breastfeeding

It is not known whether ziprasidone is excreted in breast milk.
In the treatment of ziprasidone, women should be cautioned against stopping breastfeeding.

Patients with impaired renal function intramuscularly ziprasidone should be used with caution, because cyclodextrin, as an auxiliary component of the drug, is able to be excreted by glomerular filtration.


The experience of using ziprasidone in patients with severe hepatic insufficiency is absent, therefore, the drug should be used cautiously in this group.


The efficacy and safety of ziprasidone in patients under the age of 18 years is not established.


The efficacy and safety of ziprasidone in patients over the age of 65 years is not established.


After relieving psychomotor agitation, it is advisable to transfer patients to oral intake of the drug.

Impact on the ability to drive vehicles and manage mechanisms

Like other psychotropic drugs, ziprasidone causes drowsiness and other side effects that can affect the ability to drive vehicles, etc. This should be prevented by patients who can drive a car or dangerous machinery.


Information about an overdose of ziprasidone is limited.
In the case of a maximum confirmed dose of 12800 mg, extrapyramidal symptoms and prolongation of the QT interval to 446 ms (without cardiac dysfunction) were noted. The main symptoms of overdose are extrapyramidal disorders, drowsiness, tremors and anxiety. If you suspect an overdose, you should consider the possibility of interaction of several drugs.
There is no specific ziprasidone antidote.
In acute overdose, it is necessary to restore and maintain airway patency and provide adequate ventilation and oxygenation.The oppression of consciousness, the possibility of cramps or dystonic reaction of the neck muscles after an overdose create a threat of aspiration with induced vomiting. It is necessary to immediately begin monitoring the function of the cardiovascular system, including continuous registration of the ECG in order to identify possible arrhythmias. Given that ziprasidone is largely bound to plasma proteins, hemodialysis in case of an overdose is not indicated. The patient must remain under medical supervision until the symptoms of intoxication disappear completely.

Antiarrhythmic agents 1A and III class and other drugs that extend the interval QT

See section "Contraindications".

Drugs acting on the central nervous system / alcohol

Ziprasidone has a depressing effect on the central nervous system, so care must be taken when it is used in combination with alcohol and other drugs that affect the central nervous system, including drugs acting on dopaminergic and serotonergic systems.

All studies on drug interaction were conducted using ziprasidone for oral administration.

The effect of other drugs on ziprasidone

Ziprasidone is metabolized by aldehyde oxidase and, to a lesser extent, isoenzyme CYP3A4.
Clinically significant inhibitors or inducers of aldehyde oxidase are unknown. The inhibitor of the isoenzyme CYP3A4 ketoconazole (400 mg / day) increased the concentration of ziprasidone in serum by less than 40%. The concentration of S-methyldihydrosiprasidone in serum at the expected time point Tmax ziprasidone was increased by 55%. No additional elongation of the QT interval was observed. The likelihood of a change in the pharmacokinetics of ziprasidone when co-administered with inhibitors of the CYP3A4 isoenzyme is small, so no correction of the doses of both agents is required in this case. The use of carbamazepine (200 mg twice daily), the inductor of the isoenzyme CYP3A4, leads, in turn, to a decrease in the area under the concentration-time curve (AUC) by 36%, which is also unlikely to be of clinical significance.
Cimetidine - has no significant effect on the pharmacokinetics of ziprasidone.
Benzatropin, propranolol, lorazepam - do not have a clinically significant effect on the pharmacokinetic parameters of ziprasidone concentration in serum.

In accordance with the results of in vitro studies and clinical studies on healthy volunteers, ziprasidone was shown to have no effect on the metabolism of dextromethorphan and its main metabolite, dextrorphan, via the isozyme CYP2D6.


Ziprasidone does not affect the pharmacokinetics of lithium preparations when combined.

Protein binding
Ziprasidone is largely bound to plasma proteins. Ziprasidone protein binding in vitro blood plasma was not changed under the influence of warfarin or propranolol - two drugs highly bound to plasma proteins; ziprasidone also did not change the binding of drugs to proteins of human blood plasma. Thus, the interaction of drugs with ziprasidone caused by the displacement of the connection with proteins, it is unlikely.
Pharmaceutical properties
Incompatibility drug can not be mixed with other drugs or solvents, except water for injection.

On prescription.


In the dark place at a temperature not higher than 30 В° C.
Keep out of the reach of children. The vials were stored in the original carton. Shelf life - 3 years.
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