Geodon Ziprasidone

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Ziprasidone 40 mg belongs to the group of antipsychotic drugs, indole derivatives. The therapeutic effect is ensured by using Ziprasidone Hydrochloride Monohydrate as the active ingredient. Due to its affinity with dopamine and serotonin receptors, the drug is used to treat schizophrenia in adults.

Pharmacological features

A positron emission tomography study of the drug's efficacy was conducted to trace the effects on the receptors. Twelve hours after taking 40 mg of Ziprasidone, the blocking of type 2A serotonin receptors was increased by 80%. Blocking of D2 receptors was increased by more than 50%. The drug also acts on the 5HT2C, 5HT1D and 5HT1A receptors, and this action is greater than for the D2 receptors. It has weaker effects on the neuronal serotonin and norepinephrine transporters, histamine H(1)- and alpha(1)-receptors. It also has a weak effect on the muscarinic M(1) receptors.

The antipsychotic effect is due not only to the above effects, but also to the antagonistic effect on serotonin type 2A receptors (5HT2A) and dopamine type 2 receptors (D2). The effect on the nervous system is also caused by the antagonistic effect on the 5HT2C and 5HT1D receptors, the agonistic effect on the 5HT1A receptors and the inhibition of neuronal reuptake of noradrenaline and serotonin.

Pharmacokinetics action

Ziprasidone (Geodon) reaches maximum plasma concentrations 6-8 hours after administration. Efficacy and digestibility are increased when taking the drug simultaneously with food. Therefore, it's recommended to take the drug exactly with a meal. About 99% of the drug binds with the plasma proteins, which leads to effect on the body.

The elimination half-life is 6.6 hours on average. The excretion of the active substance from the body occurs in the following ratio: 20% in the urine and 60% in the feces. The drug is almost completely metabolized, and only less than 1% is excreted unchanged. During biotransformation, 4 active metabolites of benzisothiazol piperazine sulfoxide, benzisothiazol piperazine sulfone, ziprasidone sulfoxide and S-methylhydroziprazidone are formed.

Age and bad habits such as smoking have no effect on the action of Ziprasidone Geodon. Patients with impaired liver function have 30% higher blood concentrations than patients with a healthy liver.

Indications

Ziprasidone (Geodon) is prescribed for the treatment of schizophrenia in the form of tablets, but if oral administration is not enough, then the drug is used in the form of injections. In addition to schizophrenia, the drug has shown effectiveness in treating patients with bipolar disorder.

Contraindications

  • Allergy to the underlying component and excipients.
  • Congenital and established QT interval prolongation.
  • Abnormal functioning of the cardiovascular system: heart failure and myocardial infarction.
  • Treatment of arrhythmias with class 1 and class 3 antiarrhythmic agents.

Dosage of Ziprasidone

To get the effect of using the drug, 40 mg of Ziprasidone is prescribed twice a day. This dosage can be used as early as the third day of treatment. If there is no desired effect, you can increase the dose to 80 mg twice a day. A higher dose is not recommended because of the lack of data on the effect of the drug. The initial and maintenance dose is 20 mg twice a day. The recommended daily dose is reduced for patients with impaired liver function and if the patient is older than 65 years. No dose adjustment is required for patients with impaired renal function.

Interaction of Ziprasidone

The drug may potentiate the effects of antihypertensive drugs, so blood pressure should be monitored during such combinations. Ziprasidone Geodon may alter the pharmacokinetics of oral contraceptives, which also requires monitoring. Ketoconazole increases the blood concentration of an antipsychotic. With serotonergic agents, an adverse body reaction may occur.

Ziprasidone: weight gain

The drug may cause weight gain or loss, these phenomena are side effects with frequent occurrence. To avoid this happening before starting treatment, you need to undergo a comprehensive examination and not self-medicate.

Ziprasidone and alcohol

The drug cannot be combined with alcohol, but if the patient took a dose of alcohol before or after taking the drug, it's necessary to monitor the condition. In case of a negative reaction after such a combination, immediately take a sorbent and call your GP.

If a severe allergic reaction develops, an antiallergic drug must be injected immediately.

Ziprasidone for anxiety

The drug eliminates the negative reactions of the body caused by schizophrenia and bipolar disorder. Ziprasidone (Geodon) is prescribed to eliminate the symptoms of anxiety caused by these very diseases. To understand the cause of the anxiety, it is necessary to undergo an examination. If the anxiety is not caused by a mental disorder, the drug may not be effective.

Ziprasidone vs. Risperidone

Ziprasidone works better on dopamine, adrenergic, and serotonin receptors, but it lacks action on alpha2-adrenergic receptors, whereas risperidone has a 55.5 index of such action. Risperidone causes an increase in body weight to a greater extent. If with Zyprazidone this index is only 0.04 kg in 10 weeks, with risperidone this figure is 2.1 kg in 10 weeks. Only the treating physician can choose which drug will be effective in each individual case.

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Geodon Ziprasidone
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Geodon Ziprasidone