Antipsychotic Drugs

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General Information

This group of drugs constitutes the major treatment for some of the most disturbed patients seen by psychiatrist. Anti psychotics drugs are mainly used to treat acute schizophrenic episodes and to prevent reemergence of psychotic syndrome in schizophrenic patients.

These compounds also are useful for other psychotic condition, including mania, psychotic disorder due to a general medical condition; substance induced psychotic disorder, and Tourette's Disorder.

Adverse effect

Antipsychotic drugs produce a board range of side effects.

Atypical antipsychotic drugs

Two currently available antipsychotic drugs, Clozapine (chloral) and Risperidon are considered atypical because they produce little or no extrapyramidal side effects.

Cloaapine

Clozapine differs from all other available antipsychotic drugs, which have their major effects -as antagonists of DA receptors, particularly D2 receptors. Clozapine has a high affinity for the serotonin type 2 (5-hydroxytryptamine [5-HT2]), and a-adrenergic, cholinergic (muscarinic), and histamine type 1 (Hl) receptors. Moreover clozapine's DA type 1 (D1) antagonist activity is much greater than its D2 antagonist activity.

Adverse effects

The two most serious adverse effects associated with Clozapine use are agranulocytisis and seizures.

Risperidon

Risperidon is an antipsychotic drug with significant antagonist activity at the 5- HT2 receptor and at the D2 receptor. researchdata indicate that it may be more effective than currently available dopamine receptor antagonists at treating both the positive and the negative symptoms of schizophrenia. The studies used dosages ranging of 2-16 mg a day of Risperidon compared with a placebo and up to 20mg a day of haldol.

Adverse effects

Risperidon use may be associated with anxiety, insomnia, somnolence, dizziness, constipation, nausea, dyspepsia, rhinitis, rash and tachycardia. Dose-related side effects include sedation, fatigue, accommodation disturbances, Orthostatic dizziness, weigh gain, diminished sexual desire and erectile dysfunction.

Tricyclic antidepressants

The tricyclic antidepressant Imipramine was discovered during clinical testing for antipsychotic drugs. The tricyclic and tetracycline antidepressants inhibit the neuronal reuptake of both NE and 5-HT, thus increasing the amount of these neurotransmitters in the synapse.

Tetracycline

Two antidepressants that are sterilely and pharmacologically similar to the tricyclics are amoxapine (asendin) and maprotiline (ludiomil)

Amoxapine

Amoxapine is an analogue of loxapine, a potent antipsychotic Drug. Amoxapine has clinically significant dopamine-blocking activity. Each 100mg of amoxapine is equivalent to about 0.5-1.Omg of Haloperidol in antipsychotic activity.

Maprotiline (ludiomil)

Maprotiline is the most selective inhibitor of Nereuptake. It is structurally and pharmacologically similar to desipramine, the second most selective NE blacker.

Fluoxetine

Fluoxetine has a half-life of up to 4-6 days and an active metabolic that has a half-life of up to 16 day

Sertraline

Sertraline is the most selective of the SSRIs, although the relevance of this property is not established. Sertraline also possesses some dopamine reuptake blocking activity.

Paroxetine

Paroxetine exhibits the greatest potency in 5-HT reuptake inhibitions, but is not as selective as Sertraline. The clinical significance goes these distinctions are not known. Paroxetine has a half-life of 1 day and has no active metabolites.

Fluvoxamine

Fluvoxamine is an SSRI that is not markedly different from other drugs of this class but that is approved only for the treatment of obsessive-compulsive disorder by the FDA.

Phenylpiperazines

Two Phenylpiperazines agents, trazodone and nefazodone, are unique among the antidepressant drugs in that they are potent antagonists of the 5-HT2receptor. They are, however, different in their profile of side effects.

  1. Trazodone-trazodone is a highly specific 5-HT reuptake blacker in vitro. Its therapeutic effects are due to its activity as a 5-HT reuptake inhibitor and a 5-HT2 antagonist.
  2. Nefazodone-although and analogue of trazodone, nefazodone has a distinct combination of pharmacological effects and as a consequence, a different side effect profile. Like trazodone, nefazodone is a potent antagonist of postsynaptic 5-HT2A receptors and an inhibitor of presynaptic 5 Htreuptake.

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