KANISHTHA REDDY

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Blog #11

15 May 2021, 22:15 Publicly Viewable
  • Name an example of each of the three phenothiazine sub-families and state how they differ from one another in terms of potency and side effects.

Phenothiazine with the specific sidechain

Example

Potency

Side-effects

With an aliphatic sidechain

Chlorpromazine

Low

  • Less extrapyramidal side-effects
  • Severe sedation
  • Strong anti-cholinergic effects (dry mouth, visual disturbances, urine retention etc.)
  • Strong α-lytic effects (postural hypotension)

With a piperidine side chain

Periciazine

Low

  • Same as the aliphatic sidechain

With a piperazine side chain

Fluphenazine

High

  • More extrapyramidal side-effects
  • Less sedation
  • Weaker anti-cholinergic effects
  • Weaker α-lytic effects

  • Which receptors in particular are blocked by the typical antipsychotic drugs?

D2 receptors are blocked by typical antipsychotic drugs

  • How does the mechanism of action of the atypical drugs differ from that of the typical drugs?

Atypical drugs block the 5-HT2A receptors whereas typical drugs block the D2 receptors

  • Which of the receptors blocked by the older drugs reduce the risk of extrapyramidal side effects?

The receptors that are blocked by older drugs, that reduce the risk of extrapyramidal side effects, is the D2 receptors. An example would include Sulpiride.

  • Which of the older drugs have a high incidence of extrapyramidal side effects? What is the reason for this?

Fluphenazine has a high incidence of extrapyramidal side effects as it is a potent drug. Potency refers to how likely a drug is to bind to a specific receptor, in this case, fluphenazine is very likely to bind to D2 receptors. The thioxanthenes have a similar pharmacological profile thus they have a high likelihood (but less than fluphenazine) to bind to D2 receptors. Haloperidol is a potent D2 blocker thus producing the most extrapyramidal side-effects.

  • Because of which receptor(s) blockade do the aliphatic group ofdrugs have a high incidence of autonomic side effects?

DA, M, α, histamine and 5-HT receptors.