Antipsychotics and Risk of Bleeding

Antipsychotics and Risk of Bleeding

 

BM Verdel et al (1) assessed several classes of serotonergic drugs in order to evaluate whether they constitute a risk factor for hospitalization for bleeding (gastrointestinal, intracranial, or in the female genital tract). 

They classified serotonergic medications according to their affinity for the 5-HTT (serotonin reuptake transporter) and the 5-HT2A receptors:-

    • High: Ki <10nmol/l;

 

    • Medium: Ki 10–1,000nmol/l; and

 

  • Low: Ki >1,000nmol/l.

 

Antipsychotics

Affinity for 5HTT

Affinity for 5-HT2A

Chlorpromazine

1,296

42.4

Fluphenazine

5,950

29.4

Perphenazine

5.6

Prochlorperazine

15

Thioridazine

1,259

17.9

Haloperidol

> 1,000

96.7

Risperidone

> 1,000

1.21

Clozapine

> 1,000

7.9

Olanzapine

> 1,000

5.2

Quetiapine

> 1,000

344

Aripiprazole

> 1,000

21.9

Note: Information on ziprasidone not available in this article.

Based on this Ki information in above table:-

  • Haloperidol and Fluphenazine among first generation antipsychotics and Quetiapine among second generation antipsychotics makes more sense as a first choice, if benefits outweighs risk for treatment.

But according to above article’s results and conclusions:

    • The risks of gastrointestinal and intracranial bleeding were higher in new users of antipsychotic medications as compared with those who were already receiving these drugs.

 

  • No clear association was found between the degree of affinity for the serotonin (5-hT) transporter or the 5-hT2a receptor and the risk of any type of bleeding.

 

Please do correct me if I am wrong with my understanding of Ki here.

Also do post relevant articles on this topic here.

Source: Clin Pharmacol Ther. 2011 Jan;89(1):89-96.

Please do post your questions or comments below. 


Dr. Harvinder Singh, M.D. (Admin)


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