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ANTIPSYCHOTICS

Antipsychotics are a group of powerful psychoactive drugs thought to block specific receptors in the brain that affect the central nervous system. Antipsychotics are intended to treat psychosis, which some scientists think stems from problems with brain chemistry, although that has never been proven scientifically.

Psychosis means 'an abnormal mental condition'. It is a broad psychiatric term for a mental state usually described as involving a 'loss of contact with reality'. People suffering from psychosis are said to be 'psychotic', possibly experiencing delusions, hallucinations, bizarre behavior and other odd personality changes.

Because of their widely different action on different people, and their often severe mental and physical side effects, antipsychotics are not widely seen as a good treatment but rather as the only medication available.

MOST-COMMON ANTIPSYCHOTICS

NEUROTRANSMITTERS

Antidepressants create specific effects on various neurotransmitters, which are special chemicals in your brain that relay, amplify and modulate signals between a neuron—a special nerve cell—and another cell. In other words, neurotransmitters help nerve cells communicate.

Antidepressants are thought to increase the amount of time that one or more of the neurotransmitters called serotonin, norepinephrine, or dopamine remain active in your brain.

Neurotransmitters are thought, by some researchers, to play a role in depression. Other scientists point to the fact that there is no medical test to determine if increasing the amount of time that neurotransmitters remain active in the brain is needed or even occurs and question if these drugs  play any role at all in addressing depression.

Antidepressants  can cause significant changes in brain chemistry but many researchers believe that any apparent relief of depression is due to other factors and not to the affect of antidepressants on the neurotransmitters.

Some studies have shown that placebo pills, which have no effect on neurotransmitters or anything else in the brain or body, are just as effective at relieving depression, and in some cases, even better at it. The same is often true for exercise, changes in diet, various vitamins, minerals and herbs, and other holistic approaches.

In other words, there is no exact science proving that neurotransmitters  or any type of chemical imbalance have anything to do with depression, or that antidepressants themselves are measurably doing anything to relieve depression that other therapies couldn’t accomplish without the antidepressant's side effects.

THREE MAIN TYPES OF ANTIPSYCHOTICS

There are three ‘generations’ of antipsychotics. The first generation is often called ‘typical’ antipsychotics, and a second, or newer generation, is called ‘atypical’. The latest drugs, some still in development and called third generation, are also often referred to as ‘atypical’. There are no published lists of ‘most prescribed’ antipsychotics.

Most common first generation ‘typical’ antipsychotics

  • Haloperidol (Haldol)
  • Loxapine (Loxitane, Loxapac)
  • Fluphenazine (Prolixin)
  • Perphenazine (Trilafon)
  • Thioridazine (Mellaril)
  • Molindone (Moban)
  • Trifluoperazine (Stelazine)
  • Mesoridazine (Serentil)
  • Thiothixene (Navane)
  • Chlorpromazine (Thorazine)

Most common Second generation ‘atypical’ antipsychotics

  • Clozapine (Clozaril)
  • Olanzapine (Zyprexa)
  • Risperidone (Risperdal)
  • Quetiapine (Seroquel)
  • Ziprasidone (Geodon)
  • Amisulpride (Solian) (Approved in other countries, not approved by FDA)
  • Paliperidone (Invega)
  • Asenapine

Most common Third generation antipsychotics (often called ‘atypical’ as well)

  • Aripiprazole (Abilify)
  • Under clinical development: Bifeprunox, norclozapine

Typical antipsychotics are sometimes called tranquilizers, because some of them act as sedatives. The term tranquilizer is not widely used because it suggests a connection to benzodiazepines, the largest family of tranquilizers.

A Note About Psychosis

People who are said to be suffering from psychosis may be experiencing any number of mental problems that affect their thinking, behavior, and ability to ‘be in the now’ and understand what’s going on around them, and can relate to others in abnormal, unpredictable ways.

A typical, well-known psychosis is schizophrenia, which can include abnormalities in perception of reality, auditory hallucinations, paranoid or bizarre delusions and beliefs, disorganized speech and thinking, and significant disability in relating to others.

People labeled as psychotic may not be experiencing hallucinations or have delusional beliefs, but suffer other personality changes, perform unusual or bizarre behavior. Generally they are unable to easily perform the simple activities of daily life.

Dopamine and Antipsychotics

Both kinds of antipsychotics, the ‘typical’ and newer ‘atypical’ type discussed above, are said to block receptors in the brain's ‘dopamine pathways’ in the brain—special nerve connections that transmit the neurotransmitter called ‘dopamine’ from one region of the brain to another. Many of the atypical antipsychotics also seek to block the serotonin receptors, another important neurotransmitter that is thought to increase a normal person's feeling of calm and well-being.

A ‘receptor’ is a special protein molecule which receives signal molecules sent to it. A dopamine pathway is the route dopamine takes as it binds to a receptor.

Neurotransmitters are brain chemicals that relay, amplify and modulate signals between a neuron— a special nerve cell— and another cell. In other words, neurotransmitters help nerve cells communicate.

Dopamine is one of the brain’s important chemical neurotransmitters. It has many functions in the brain. Research scientists say it plays important roles in behavior, motor activity, cognition, sleep, mood, motivation and reward, attention, learning, and other functions.

By blocking dopamine from reaching and attaching to a receptor, more dopamine remains circulating in the brain. The theory is that blocking dopamine receptors and keeping more dopamine circulating helps control psychotic experiences.

Antipsychotics were discovered not by learning the cause of psychosis and developing medicine that cured it, but by observing the effects of drugs on behavior. As everyone knows, drugs that affect one’s brain chemistry and/or nervous system can definitely alter one’s behavior, sometimes in bizarre and unpredictable ways. It was observed that certain drugs, which later came to be called antipsychotics, slowed down or helped control some of the symptoms of some psychoses.

Unfortunately, the antipsychotic drugs which target dopamine pathways which seem to help some psychotic episodes also target a wide range of other receptors in the brain. The numerous unpredictable, definitely unwanted, even dangerous and disabling side effects this produces is the major problem with antipsychotic medications.

This problem, of course, is in addition to the fact that a person taking antipsychotics is depending on powerful psychoactive drugs to feel or act normal, when there may be other, far less dangerous ways to treat the condition.

A large number of studies on the efficacy of both typical and atypical antipsychotics show that responses to any given antipsychotic are so variable from person to person that trial and error is the standard approach—finding one that has the least side effects. Also the lowest dose possible is always preferred.

Other studies have shown that people with similar conditions who did not take antipsychotics had more favorable outcomes than those who did.

More research is needed on the causes of psychosis, so that treatments that are less invasive, disabling and risky can be found.

SIDE EFFECTS OF ANTIPSYCHOTICS

Antipsychotics deaden a person’s perceptions of pleasure, severely reducing feelings of desire, thoughtfulness, motivation, and the ability to be surprised or amazed. At one time, some of the earlier antipsychotics were described as causing a ‘chemical lobotomy’ or were used as ‘chemical straightjackets’.

The word ‘zombie’ is often used to describe this side effect of many antipsychotics.

Because of the seriousness of these and many other side effects, many people stop taking them -- two-thirds of people in controlled drug trials -- due at least in part to the adverse effects. Some side effects have even been seen to appear long after a person has stopped taking the drug, effects that last for years, or for life. This suggests that some antipsychotics cause permanent, irreversible brain damage.

Many side effects from antipsychotics have been studied and observed, so many and so serious that much of the research in the field has been trying to find drugs that cause fewer side effects.

Side effects are different depending on the specific drug, but generally, to one degree or another, can include, but are not limited to, the following:

  • Diabetes

  • Pancreatitis—inflammation of the pancreas

  • Serious weight gain or weight loss

  • Agranulocytosis—a dangerous decrease in white blood cells

  • Seizures

  • Parkinsonism—rigidity and tremors

  • Acute dystonias -- movement disorder with sustained muscle contractions, twisting and repetitive movements or abnormal postures

  • Hyperprolactinaemia—abnormally-high levels of prolactin in the blood

    • Prolactin is a hormone associated with lactation. This side effect may cause spontaneous flow of breast milk, disruptions in normal menstrual cycles, hypogonadism, infertility, and erectile dysfunction in men.
  • Tardive dyskinesia

    • Tardive means the condition continues, or even appears for the first time, after the drugs are no longer being taken.

    • Dyskinesia is involuntary, uncontrollable and repetitive movements.

  • Tardive akathisia

    • Akathisia is an eerie, uncontrollable restlessness, ranging from a feeling of inner disquiet, often localized in the muscles, to an inability to sit still or lie quietly.

  • Tardive dysphrenia and psychoses -- any number and any kind of psychosis. In other words, a medication for psychosis causes psychosis, even after stopping taking it.

  • Tardive tourettism—a tic disorder that closely mimics Tourette Syndrome.

    • Tourettes is characterized by the presence of multiple physical (motor) tics and at least one vocal (phonic) tic.
  • Tachycardia -- accelerated heart rates

  • Hypotension -- dangerously low blood pressure

  • Impotence

  • Lethargy

  • Dysphoria—sadness and depression

  • Tooth decay—primarily from the ‘dry mouth’ effect of antipsychotics

  • Intense dreams or nightmares

  • Sudden dangerous rise in body temperature

  • Sudden death in Alzheimer’s patients

  • Central nervous system damage— associated with irreversible tardive akathisia and/or tardive dysphrenia

Many studies indicate that chronic treatment with antipsychotics affects the brain at a structural level, causing permanent loss of brain tissue and shrinkage of the brain. Some side effects are also irreversible (permanent), even after taking the drug just a few times, or even once according to some reports..

DEPENDENCE, ADDICTION AND WITHDRAWAL

PHYSICAL DEPENDENCE

Antipsychotic medications create some physical and psychological withdrawal symptoms when discontinued -- this is called dependence. But they are not considered addictive.

The common practice is to ‘wean’ patients off antipsychotics by slowly decreasing their dosage over a period of time.

Medical drug detox, called medically assisted withdrawal, can offer advantages.

ADDICTION

A person is addicted who is continues drug use to ‘get high’ or experience some other drug effect, who do things they would not normally do, and will go to almost any lengths to get more drugs. Addiction is not commonly associated with antipsychotics.

MEDICALLY ASSISTED WITHDRAWAL

Medical detox facilities use proper nutrition, hydration and other means to help the withdrawal from antipsychotics to be safer, more comfortable, and much faster than other means

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