Ziprasidone; Indications/Uses, Dosage, Side effects, Drug Interaction, Pregnancy

Ziprasidone








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Ziprasidone Hydrochloride is the hydrochloride salt form of ziprasidone, a benzothiazolylpiperazine derivative and an atypical antipsychotic agent with an antischizophrenic property. Ziprasidone hydrochloride functions as an antagonist at the dopamine D2 and serotonin 5-HT2A and 5-HT1D receptors, and as an agonist at the 5-HT1A receptor. Ziprasidone hydrochloride also inhibits synaptic reuptake of serotonin and norepinephrine. The mechanism of action by which ziprasidone hydrochloride exerts its antischizophrenic effect is unknown but is potentially mediated through a combination of dopamine D2 and serotonin 5-HT2 antagonism. This agent also has antagonistic activity against histamine H1 and alpha-1-adrenergic receptors.

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Ziprasidone is the fifth atypical antipsychotic which is used for the treatment of schizophrenia as well as acute mania and mixed states associated with bipolar disorder. Ziprasidone is Food and Drug Administration (FDA) approved for the treatment of schizophrenia, and the intramuscular injection form of ziprasidone is approved for acute agitation in schizophrenic patients. Ziprasidone has also received approval for acute treatment of mania associated with bipolar disorder. Its immediate release intramuscular injection form is approved for acute agitation in people with schizophrenia. Ziprasidone is also used off-label for depression, bipolar maintenance, and post-traumatic stress disorder (PTSD).

Mechanism of Action of Ziprasidone

Ziprasidone’s antipsychotic activity is likely due to a combination of its antagonistic function at D2 receptors in the mesolimbic pathways and at 5HT2A receptors in the frontal cortex. Ziprasidone is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Ziprasidone acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Ziprasidone. Ziprasidone’s antagonism of muscarinic M1-5 receptors may explain its anticholinergic effects. Ziprasidone’s antagonism of histamine H1 receptors may explain the somnolence observed with this drug. Ziprasidone’s antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug. Ziprasidone functions as an antagonist at the Dopamine D2 , 5HT-2A , and 5HT-1D receptors, and as an agonist at the 5HT-1A receptor. Alleviation of positive symptoms is due to antagonism at D2 receptors while relief of negative symptoms are due to 5HT2A antagonism.

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Ziprasidone is a benzisothiazolyl piperazine-derivative antipsychotic agent that is chemically unrelated to other currently available antipsychotic agents (eg, butyrophenones, phenothiazines) and has been referred to as an atypical or second-generation antipsychotic agent. The exact mechanism of antipsychotic action of ziprasidone has not been fully elucidated but, like that of other atypical antipsychotic agents (eg, olanzapine, risperidone), may involve antagonism of central type 2 serotonergic (5-HT2) receptors and central dopamine D2 receptors. As with other drugs that are effective in bipolar disorder, the precise mechanism of antimanic action of ziprasidone has not been fully elucidated. Antagonism of various other receptors (eg, histamine H1 receptors, alpha1-adrenergic receptors) may contribute to other therapeutic and adverse effects (eg, orthostatic hypotension, somnolence) observed with ziprasidone.

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Indications of Ziprasidone

Contra Indications of Ziprasidone

Dosage of Ziprasidone

Strengths: 40 mg; 20 mg; 60 mg; 80 mg

Schizophrenia

Oral

  • Initial dose: 20 mg orally twice a day
  • Maintenance dose: Adjust as clinically indicated at intervals of not less than 2 days
  • Maximum dose: 100 mg twice a day
  • A dose greater than 80 mg twice a day is generally not recommended.

Intramuscular

  • Recommended dose: 10 to 20 mg IM; may repeat 10 mg IM every 2 hours or 20 mg IM every 4 hours up to the maximum daily dose
  • Maximum dose: 40 mg IM per day
  • Duration of therapy: Use beyond 3 consecutive days has not been studied

 Bipolar Disorder

Acute Treatment of Manic or Mixed Episodes

  • Initial dose: 40 mg orally twice daily
  • Increase dose to 60 mg or 80 mg twice daily on the second day; subsequently adjust dose based on tolerance and efficacy within the dose range of 40 to 80 mg orally twice a day.
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Maintenance Treatment (as the adjunct to lithium or valproate)

  • Once stabilized, continue on the same dose within the range of 40 to 80 mg orally twice daily.

Side Effects of Ziprasidone

The most common

More common

Rare

Drug Interactions of Ziprasidone

Ziprasidone may interact with following drug, supplements, & may change the efficacy of the drug

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Pregnancy Catagory of Ziprasidone

FDA Pregnancy Category C

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

It is not known if ziprasidone passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.The safety and effectiveness of using this medication have not been established for children less than 18 years of age.

References

  1. https://pubchem.ncbi.nlm.nih.gov

 

Ziprasidone

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