Receptor Bindng Profile Side Effects

Question 1

Dopamine D2 receptor

Answer 1

Dopamine D2: improvement of positive symptoms, induction of extrapyramidal symptoms (EPS) and tardive dyskinesia (TD), increased prolactinemia

Question 2

Seretonin 5HT2A receptor

Answer 2

improvement of negative symptoms, of depressive symptoms, of quality of sleep, of cognitive symptoms, and of aggressive/impulsive symptoms; decrease in Extra pyramidal symptoms

Question 3

Serotonin 5-HT2C

Answer 3

İncreased appettite and weight gain

Question 4

Adrenergic a1 antagonism

Answer 4

orthostatic hypotension, dizziness, falling down, tachycardia,
sexual side effects, potentiation of antipsychotic effect, sedation and anti-agitation

Question 5

Histamine H1 antagonism:

Answer 5

sedation, somnolence, weight gain

Question 6

Acetylcholine antagonism:

Answer 6

decreased cognitive functioning (mainly memory) and Extrapyramidal symptoms.
although potentially more TardiveDyskinesia; delirium, dry mouth, blurred vision, urinary retention, nausea, vomiting, constipation, glaucoma, sexual problems.

Question 7

D2 receptor blocker pharmacodynamics

Answer 7

Blocking the D2 receptors is the cornerstone of the antipsychotic effect but it is also responsible for some of the side effects. In addition to the antipsychotic effect, most of the antipsychotics have a sedative effect. While sedation is most pronounced at the start of treatment, it may be permanent and sometimes useful.
Despite the sedative effects these drugs should preferably not be used to treat pure anxiety or sleep disorders, in particular because of the severe side effects (see below).
The old term “neuroleptics” refers to the inhibiting effect on the patient’s initiative, the loss of interest in the environment and the decreased expression of emotions. Nonetheless, the patient remains approachable and communicative, and there is little negative impact on the cognitive skills. These effects usually appear before the typical antipsychotic effects (such as the reduction of hallucinations, of delusions and of chaotic thinking).
Nowadays, the term “neuroleptics” is only used to describe the characteristic neurological effects; the term “antipsychotics” is preferred to this outdated term.

Question 8

Antipsychotic side effects.: common ones

Answer 8

The most frequent cardiovascular side effect of antipsychotics is orthostatic hypotension, which
can lead to syncope and falling down.
Many antipsychotics cause arrhythmias (elongation of QT-interval, torsade de pointes, cardiac arrest). Therefore, concomitant administration of antipsychotics and other drugs with known or potential cardiotoxicity (such as antiarrhythmic drugs or tricyclic antidepressants) should be avoided. Furthermore, patients with existing cardiac problems should not take antipsychotics, if possible.

The metabolic side effects may also increase the cardiovascular morbidity and mortality.