ANTIPSYCHOTICS

Antipsychotics (also called neuroleptics) are a group of psychoactive drugs commonly but not exclusively used to treat psychosis, which is typified by schizophrenia, but can also be present in severe bipolar disorder, as well as many other conditions. Over time a wide range of antipsychotics have been developed. A first generation of antipsychotics, known as typical antipsychotics, was discovered in the 1950s. Most of the drugs in the second generation, known as atypical antipsychotics, have more recently been developed, although the first atypical anti-psychotic, clozapine, was discovered in the 1950s, and introduced clinically in the 1970s. Both classes of medication tend to block receptors in the brain's dopamine pathways, but antipsychotic drugs encompass a wide range of receptor targets. A number of side effects have been observed in relation to specific medications, including weight gain, agranulocytosis, tardive dyskinesia, tardive akathisia, tardive psychoses, and tardive dysphrenia. The development of new antipsychotics, and the relative efficacy of different ones, is an important ongoing field of research. The most appropriate drug for an individual patient requires careful consideration.

Antipsychotics are broadly divided into two groups, the typical or first-generation antipsychotics and the atypical or second-generation antipsychotics. The typical antipsychotics are classified according to their chemical structure while the atypical antipsychotics are classified according to their pharmacological properties. These include serotonin-dopamine antagonists (see dopamine antagonist and serotonin antagonist), multi-acting receptor-targeted antipsychotics (MARTA, those targeting several systems), and dopamine partial agonists, which are often categorized as atypicals.

Typical antipsychotics are also sometimes referred to as the major tranquilizers, because some of them can tranquilize and sedate. As with the term "neuroleptics," the term "major tranquilizers" is falling out of common and scientific use. The term "tranquilizers" now generally refers to drugs that are primarily intended to sedate—mostly the barbiturates and benzodiazepines, which were once referred to as the "minor tranquilizers."


INDICATIONS:

Antipsychotics
Antipsychotics (also called neuroleptics) are a group of psychoactive drugs commonly but not exclusively used to treat psychosis, which is typified by schizophrenia, but can also be present in severe bipolar disorder, as well as many other conditions. Over time a wide range of antipsychotics have been developed. A first generation of antipsychotics, known as typical antipsychotics, was discovered in the 1950s. Most of the drugs in the second generation, known as atypical antipsychotics, have more recently been developed, although the first atypical anti-psychotic, clozapine, was discovered in the 1950s, and introduced clinically in the 1970s. Both classes of medication tend to block receptors in the brain's dopamine pathways, but antipsychotic drugs encompass a wide range of receptor targets. A number of side effects have been observed in relation to specific medications, including weight gain, agranulocytosis, tardive dyskinesia, tardive akathisia, tardive psychoses, and tardive dysphrenia. The development of new antipsychotics, and the relative efficacy of different ones, is an important ongoing field of research. The most appropriate drug for an individual patient requires careful consideration.

Atypical antipsychotic
The atypical antipsychotics (also known as second generation antipsychotics) are a group of antipsychotic drugs used to treat psychiatric conditions. Some atypical antipsychotics are FDA approved for use in the treatment of schizophrenia. Some carry FDA approved indications for acute mania, bipolar mania, psychotic agitation, bipolar maintenance, and other indications.
Atypicals are a group of unrelated drugs united by the fact that they work differently from typical antipsychotics. Most share a common attribute of working on serotonin receptors as well as dopamine receptors. One drug, amisulpride, does not have serotonergic activity. Instead it has some partial dopamine agonism. Another drug, aripiprazole, also displays some partial dopamine agonism, 5-HT1A partial agonism, and 5-HT2A antagonism.[1]

Antidepressant
Antidepressant, medication used to treat depression, a mood disorder characterized by such symptoms as sadness, decreased appetite, difficulty sleeping, fatigue, and a lack of enjoyment of activities previously found pleasurable. While everyone experiences episodes of sadness at some point in their lives, depression is distinguished from this sadness when symptoms are present most days for a period of at least two weeks. Antidepressants are often the first choice of treatment for depression.

Antianxiety drugs
Antianxiety drugs, also called minor tranquilizers, reduce high levels of anxiety. They may help people with generalized anxiety disorder, panic disorder, and other anxiety disorders. Benzodiazepines, a class of drugs that includes diazepam (Valium), are the most widely prescribed antianxiety drugs. Benzodiazepines can be addictive and may cause drowsiness and impaired coordination during the day.

Antimanic drugs
Antimanic drugs help control the mania that occurs as part of bipolar disorder. One of the most effective antimanic drugs is lithium carbonate, a natural mineral salt (see Lithium). Common side effects include nausea, stomach upset, vertigo, and increased thirst and urination. In addition, long-term use of lithium can damage the kidneys.

ANTIPSYCOTIC DRUGS
Aripiprazole
Brands : Abilify tab
Adverse Drug Reactions
Headache, agitation, insomnia, somnolence; dyspepsia, constipation, pain, nausea, vomiting; asthaenia, dizziness, abdominal pain; dry mouth; anxiety, akathisia; orthostatic hypotension; hypertonia, tremor and blurred vision.

Contraindications
Hypersensitivity. Lactation. Children <18 yr.

Available Dosage Form
5mg tablet; 10mg tablet; 15mg tablet

Pregnancy Category (US FDA)
Category C: Either studies in animals have revealed adverse effects on the fetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus.

Chlorpromazine
Brands : Globazine, Laractyl, Promak
Adverse Drug Reactions
Tardive dyskinesia (on long-term therapy). Involuntary movements of extremities may also occur. Dry mouth, constipation, urinary retention, mydriasis, agitation, insomnia, depression and convulsions; postural hypotension, ECG changes. Allergic skin reaction, amenorrhoea, gynaecomastia, weight gain. Hyperglycaemia and raised serum cholesterol.
Potentially Fatal: Agranulocytosis. Instantaneous deaths associated with ventricular tachyarrhythmias. Marked elevation of body temperature with heat stroke. Neuroleptic malignant syndrome, extrapyramidal dysfunction

Contraindications
Hypersensitivity; preexisting CNS depression, coma, bone-marrow supression; phaeochromocytoma; lactation.

Available Dosage Form
Globazine : 50mg film- coated tablet; 100mg film- coated tablet
Laractyl : 100mg film- coated tablet; 200mg film- coated tablet
Promak : 25mg sugar-coated tablet; 100mg film- sugar tablet

Pregnancy Category (US FDA)
Category C: Either studies in animals have revealed adverse effects on the fetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus.


Levomepromazine (Sold as Nosinan Nozinan, Levoprome) is an aliphatic phenothiazine neuroleptic drug. It is a low-potency antipsychotic (approximately half as potent as chlorpromazine) with strong analgesic and antiemetic properties.
SIDE EFFECTS:
The most common side effect is akathisia.[citation needed] Levomepromazine has prominent sedative and anticholinergic/sympatholytic effects (dry mouth, hypotension, sinus tachycardia, night sweats) and may cause weight gain.
AVAILABLE DOSAGE FORM:
Tablets
Injection
CONTRAINDICATIONS:
Dementia is probably a contraindication for any antipsychotic (fair evidence for increased mortality in long term use) and has an interesting medicolegal potential as it is unclear if following recent changes in datasheets (SPCs) and warnings from the regulatory authorities (eg FDA) any manufacturer will share liability for out of licence use (off license) use in newly commenced patients.
Safety in pregnancy has not been established. There are no absolute contraindications to the use of Levomepromazine in terminal care.
PREGNANCY CATEGORY:
Only if clearly needed.

TRIFLUOPERAZINE
Brand name: Stelazine
SIDE EFFECTS:
Extrapyramidal Symptoms:
These symptoms are seen in a significant number of hospitalized mental patients receiving higher dosages of trifluoperazine (10 mg to 40 mg or more daily). They may be characterized by motor restlessness, may be of the dystonic type, or may resemble parkinsonism.
Motor Restlessness:
Symptoms may include agitation or jitteriness and sometimes insomnia. These symptoms often disappear spontaneously. At times these symptoms may be similar to the original neurotic or psychotic symptoms. Dosage should not be increased until these side effects have subsided. If this condition becomes too troublesome, the symptoms can be controlled by dosage reduction or change of drug. Treatment with antiparkinsonian agents or benzodiazepines may be helpful.
Dystonias:
Symptoms may include spasm of the neck muscles, sometimes progressing to torticollis; extensor rigidity of back muscles; sometimes progressing to opisthotonos; carpopedal spasm, trismus, swallowing difficulty, oculogyric crises and protrusion of the tongue. The onset of the dystonias may be sudden.
Neuroleptic Malignant Syndrome:
As with other neuroleptic drugs, a symptom complex sometimes referred to as neuroleptic malignant syndrome (NMS) has been reported. Cardinal features of NMS are hyperpyrexia, muscle rigidity, altered mental status (including catatonic signs), and evidence of autonomic instability (irregular pulse or blood pressure). Additional signs may include elevated CPK, myoglobinuria (rhabdomyolysis), and acute renal failure. NMS is potentially fatal and requires symptomatic treatment and immediate discontinuation of neuroleptic treatment.
Pseudo-parkinsonism:
Symptoms may include mask-like face, drooling, tremor, pillrolling motion, cogwhell rigidity and shuffling gait. Reassurance and sedation are important. In most cases these symptoms are readily reversible when an antiparkinsonian agent is administered concomitantly.
AVAILABLE DOSAGE FORM:
Oral:

The usual starting dosage is a 1 mg or 2 mg tablet twice daily. In everyday practice it is seldom necessary to exceed 6 mg daily. Because of the inherent long action of trifluoperazine most patients can be effectively controlled on a convenient twice-a-day dosage regimen, and some have been maintained on once-a-day administration.
CONTRAINDICATIONS:
Comatose or greatly depressed states due to central nervous system depressants; blood dyscrasias, bone marrow depression; liver damage.
PREGNANCY CATEGORY: C

PROCHLORPERAZINE


SIDE EFFECTS:Due to the short duration of treatment it is usually well tolerated. It shares in general all side effects of chlorpromazine, but these are seen less frequently so and are less disturbing to the patient, particularly as most patients with the aforementioned conditions are hospitalized. In the treatment of nausea/emesis it might be given together with an antiparkinsonian drug to prevent extrapyramidal side effects of prochlorperazine.

Many individuals are inherently allergic to this medicine. This medicine is known to produce seizures and seizure-like symptoms in individuals who might not have had prior seizures. In such cases, contact health-care facilities for immediate attention. Long-term delays might lead to long-term effects. A common, over-the-counter remedy for side-effects is Diphenhydramine. This product is a blood reactant and can cause permanent circulatory damage when used as an i.v. push drug in emergency room or other use.

AVAILABLE DOSAGE FORM:
Prochlorperazine is available as an oral liquid, tablets, and suppositories, as well as in an injectable form.

Following intramuscular injection the antiemetic action is evident within 5 to 10 minutes and lasts for 3 to 4 hours. Rapid action is also noted after buccal treatment. With oral dosing the start of action is delayed but the duration somewhat longer (approximately 6 hours).

There is an inhaled form of prochlorperazine under development by Alexza Pharmaceuticals, currently in Phase II clinical trials.

CONTRAINDICATIONS:
Prochlorperazine is a phenothiazine drug. Most drugs in this category are used as anti-psychotics (neuroleptics). Neuroleptic means "nerve seizing," and describes the semi-paralyzing effect these drugs have on the brain and nervous system.
PREGNANCY CATEGORY: C


PERPHENAZINE
Brand Names:
  • · Etrafon
  • · Trilafon
  • · Levazine
Common side effects:
  • · Temporary dyskinesia
  • · interferes with the diagnosis
  • · permanant or lasting tardive dyskinesia is a risk
  • · allergic and toxic side-effects of chlorpromazine
  • · early and late extrapyramidal side effects
Available Dosage Forms:
  • · Tablets
Contraindication:
  • · In comatose or greatly obtunded patients and in patients receiving large doses of CNS depressants (barbiturates, alcohol, analgesics or antihistamines); in the presence of blood dyscrasias, bone marrow depression or liver damage; and in patients who have shown hypersensitivity to the components of the injection or related compounds.
  • · It is also contraindicated in patients with suspected or established subcortical brain damage, with or without hypothalamic damage.
Pregnancy Category: Pregnancy category C
Thiothixene
Brand Names:
· Navane
Common Side Effects:
· Drowsiness
· Restlessness
· Agitation
· Insomnia
· weakness or fatigue
Available Dosage Forms:
· Capsule (gelatin)
Contraindications:
· Safety for use in children under 12 years of age has not yet been established.
· Circulatory collapse, comatose states, CNS depression due to any cause and blood dyscrasias.
· Known hypersensitivity to the drug. It is not known whether a cross sensitivity between the thioxanthenes and the phenothiazines exists, but this possibility should be considered.
Pregnancy Category: Pregnancy Category C
Haloperidol
Brand Names:
· Haldol
· Serenase
· Serenace
Common Side Effects:
· facial disfiguring tardive dyskinesia
· anxiety
· dysphoria
· inability to remain motionless
· tremors
Available Dosage Forms:
· Liquid
· Tablets
· Injections
· Depot Injections
Contraindication:
  • Preexisting coma, acute stroke
  • Severe intoxication with alcohol or other central depressant drugs
  • Known allergy against haloperidol or other butyrophenones or other drug ingredients
  • Known heart disease; when combined will tend towards cardiac arrest
Pregnancy Category: Pregnancy Category C

Members:
Querubin, Jan-Reynold O.
Ruiz, Rochelle Ann R.
Ubaldo, Joshua
Mayos, Rocky

78/100 =some don't have brand names; work with a neat/uniform format next time!