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Antipsychotic Drug Information


Originally prescribed for schizophrenia and psychosis, but recently they have been prescribed for insomnia as well as an adjunct with Antidepressant therapy at an alarming rate.

28% of seniors in retirement homes are taking antipsychotics, despite the FDA warning of increased death risk.  Children and adolescents antipsychotic use has increased 5-fold, yet warnings exist for obesity and type-2 diabetes.

Antipsychotics are among the largest selling and most profitable medications, and generated $22 billion in global sales in 2008. The number of prescriptions for children and adolescents doubled between 2003 and 2006.

In October 2009, AstraZeneca, the manufacturer of the atypical antipsychotic, Seroquel agreed to pay a billion dollars to settle two two whistle-blower lawsuits and two federal investigations for promoting off-label uses. Sales of Seroquel continue to soar.

Typical Antipsychotics:

  • Chlorpromazine (Largactil)
  • Droperidol (Droleptan, Thalamonal)
  • Flupenthixol (Depixol, Fluanxol)
  • Fluphenazine (Modecate, Moditen, Motipress, Motival)
  • Haloperidol (Haldol, Serenace)
  • Thioridazine (Melleril)
  • Trifluoperazine (Stelazine, Parstelin)
  • Zuclopenthixol (Clopixol)

Atypical Antipsychotics:

  • Ariprazole (Abilify)
  • Clozapine (Clozaril)
  • Olanzapine (Zyprexa, Zalasta, Zolafren, Olzapin, Rexapin, Zypadhera)
  • Risperidone (Risperdal)
  • Quetiapine (Seroquel)
  • Ziprasidone (Geodon, Zeldox)

It is theorized that Schizophrenia is caused by too much Dopamine in the brain, and antipsychotics work by blocking the effects of Dopamine in the central nervous system, but they exert their strongest effect in the limbic system while also effecting the cortex. The limbic system is involved in our feelings of pleasure related to our survival, such as eating and sex, and is also involved in memory.  The cortex also plays a key role in memory, attention, perceptual awareness, thought, language and consciousness.

Anti-psychotics are divided into two classifications – typical, or first-generation, which are classified by their chemical structure; and atypical, or second-generation, which are classified by their pharmacological properties. The first generation known as typical antipsychotics, were discovered in the 1950s, with Chlorpromazine (Thorazine) being synthesized and developed as a surgical anesthetic. It was used as a psychiatric medication due to its powerful calming effect and at the time was regarded as a “chemical lobotomy”. Both generations of antipsychotics block receptors in the brain’s Dopamine pathways. But antipsychotics encompass a wide range of receptor targets and some can interfere with the release of Dopamine and also block the Dopamine receptors so the cells cannot recognize Dopamine.

Dopamine is commonly known as a chemical that relates to the sensation of pleasure. It regulates virtually all bodily functions, including heartbeat, breathing and eye movement. There are multiple types of Dopamine in the body that must exist in carefully balanced amounts in order for these functions to be properly controlled. With low levels of Dopamine, movement becomes difficult. Parkinson’s disease is one result of low levels of Dopamine. Too much Dopamine results in an inability to remain still. The most extreme form of this excited state is tardive dyskinesia, a disorder caused by medications that involves involuntary movements, particularly of the lower face. Tardive dyskinesia began to surface in the early 1960, as the use of the antipsychotics increased.

Understanding Dopamine:

The Dopamine receptor involved in emotion and behavior is very specific. However, the drugs used to control them are not always successful in targeting the precise receptor. Antipsychotic medications affect a range of Dopamine receptors, including those for regulating voluntary muscle function. One Dopamine receptor plays a significant role in the more intense and primitive emotional states, such as fear and rage. It is the one targeted by antipsychotics, but the medications can also affect other Dopamine receptors. This can cause the symptoms associated with tardive dyskinesia, and in some cases, suicidal and/or violent behavior.  

The prevalence of Diabetes has become a serious public health problem, and the use of antipsychotics has been associated with a disruption of the glucose metabolism that causes blood sugar to increase significantly. The most significant risk factor for weight gain from antipsychotics is the strong blocking of the histaminergic receptors.  Histamine is an organic nitrogen compound involved in the immune response. It also regulates physiological function in the gut and acts as a neurotransmitter. Histamine triggers the inflammatory response and as part of an immune response to foreign invaders it increases the permeability of the capillaries to white blood cells and other proteins. This allows the foreign invaders to be surrounded in the affected tissues.  Histamine is found in virtually all body cells. Histamine also regulates appetite, so artificially increasing levels cause a patient to require more food. 

Johns Hopkins brain scientists recently connected antipsychotics to natural brain chemicals that trigger appetite. They identified a significant increase in AMPK activity (an enzyme that plays a role in balancing cellular energy) caused by antipsychotics, which increases food intake and cravings. The study showed that mice given the antipsychotic clozapine had quadrupled the AMPK activity compared to activity measured pre-drug.

In humans, drugs that reduce Dopamine activity have been shown to reduce motivation, cause an inability to experience pleasure, and long term use has been associated with tardive dyskinesia, large weight gain, diabetes, lactation, abnormally large mammary glands, drooling, fatigue, an increase in depression, anxiety, irritability or restlessness, sexual dysfunction, and heart rhythm problems.

Side Effects May Include: Weight gain, Enlarged breasts and milk discharge in men and women, Lowered white blood cell count, Involuntary repetitive body movements (tardive dyskinesia), Diabetes, Sexual dysfunction , Neuroleptic malignant syndrome (severe muscle stiffness), Constipation, Dizziness, Drowsiness, Dry mouth, Increased appetite, Nasal congestion, Nausea, Sore throat, Stomach pain or upset, Tiredness, Vomiting, Weakness, Headache, Agitation, Psychosis, Hallucinations, Diabetes

DISCLAIMER:

    *While great care has been taken in organizing and presenting the material throughout this website, please note that it is provided for informational purposes only and should not be taken as Medical Advice. More...

    *Because these drugs can cause severe withdrawal reactions, do not stop taking any medication without first consulting your physician. The decision to quit any medication should be discussed with your doctor and with their consent and support. More...*Because these drugs can cause severe withdrawal reactions, do not stop taking any medication without first consulting your physician. The decision to quit any medication should be discussed with your doctor and with their consent and support. More...