cns

• (mental disorder that is characterized by distortions in thinking, Perception, emotions, language, sense of self, behavior) Schizophrenia
• Schizoaffective Disorders - combination of symptoms of schizophrenia with mood distortions
• Bipolar Affective Disorder (AKA Manic depression)
• Tourette's Syndrome (Minor ticks), uncontrolled and characterized by minor and major tics
• Senile dementia of Alzheimer type ▪ (Mental deterioration) (Loss off mental ability)
• Antiemetic


  Prochlorperazine, Benzquinamine
• . Psychiatric indications

  • Schizophrenia
  • Schizoaffective Disorders
  • Bipolar Affective Disorder
  • Tourette's Syndrome
  • Senile dementia of Alzheimer type
• Neuropsychiatric indications

  • Antiemetic
  • Antihistamines
  • Preoperative Sedatives
  • Neuroleptanesthesia
• Antihistamines


  Phenothiazines
• Preoperative Sedatives


  Promethazine
• Neuroleptanesthesia


  (Droperidol +Fentanyl + Nitrous Oxide)
• Typical Antipsychotic Agents


  : 1 st generation,
• Atypical APA


  2 nd generation
• 1. PHENOTHIAZINES

  • ALIPHATIC SIDE CHAIN
  • PIPERIDINE SIDE CHAIN
  • PIPERAZINE SIDE CHAIN
• ALIPHATIC SIDE CHAIN


  Chlorpromazine
• Chlorpromazine

  • for intractable hiccups
  • ADR: associated with seizure, orthostatic hypotension, corneal depositnagkakaron ng deposit ng chlorpromazine sa cornea
  • first to be developed as Surgical anesthetic
  • NMS (neuroleptic malignant syndrome)
• PIPERIDINE SIDE CHAIN


  Thioridazine
• Thioridazine

  • Deposits to retina that can cause blindness
  • cardiotoxic
  • low potency
• PIPERAZINE SIDE CHAIN

  • Trifluoperazine
  • Fluphenazine
• Trifluoperazine


  More potent than chlorpromazine
• high potency; associated with EPS

  • Perphenazine
  • Fluphenazine
• Fluphenazine


  available in the market as salt (FLUPHENAZINE DECANOIC)
• . BUTYROPHENONE

  • Haloperidol
  • Droperidol
• BUTYROPHENONE


  Available as slow-release preparation
• Haloperidol

  • prototype drug of butyrophenone
  • adr: EPS(tremor), NMS(high fever, sweating)
• Droperidol

  • strong sedating effect
  • has anti-emetic property
  • mixed in neurolept anesthesia (fentanyl)
• THIOXANTHENE


  Thiothexene & Chlorprothixene
• Typical Antipsychotic Agents: 1 st generation

  • PHENOTHIAZINES
  • BUTYROPHENONE
  • THIOXANTHENE
• ANTIEMETIC AGENTS

  1. Prochlorperazine
  2. 2. Promethazine- anti-pruritic
  3. 3. Droperidol- sedative, antipsychotic, antiemetic
• 3 COMMON MOA


  -DOPAMINE II BLOCKER

  -ADRENERGIC ALPHA RECEPTOR BLOCKER

  -ANTICHOLINERGIC EFFECT
• Cardiovascular effects.

  • Anticholinergic effects produce tachycardia.
  • Alpha-adrenergic blockade causes orthostatic hypotension.
  • With very large overdoses of some agents, quinidine-like membrane depressant effects on the heart may occur.
• Central nervous system effects

  1. CNS depression caused by centrally mediated sedation and anticholinergic effects
  2. Alpha-adrenergic blockade causes small pupils
  3. Central dopamine receptor blockade produces extrapyramidal dystonic reactions (EPS), low dopamine
• Possible even at therapeutic dose

  -extrapyramidal reactions

  -anticholinergic effects,

  -and orthostatic hypotension are often seen with therapeutic doses
• serious CNS depression and hypotension may occur after ingestion of 200-1000 mg of chlorpromazine in children or 3-5 g in adults.
• MILD INTOXICATION of TCA CAUSES

  • Sedation

  • Small pupils

  • Orthostatic hypotension
• ANTICHOLINERGIC MANIFESTATIONS INCLUDE:


  • Dry mouth

  • Absence of sweating

  • Tachycardia

  • Urinary retention
• SEVERE INTOXICATION MAY CAUSE:

  • Coma

  • Seizures

  • Respiratory arrest

  • Hypothermia

  • hypotension
• EXTRAPYRAMIDAL DYSTONIC EFFECTS


  • Torticollis

  o Spasm of the muscles in one side of the neck which causes the head to twist to that side. Straightening of the head usually causes pain

  • Jaw muscle spasm

  • Oculogyric crisis

  o spasm of extraocular muscle (muscle sa mata)

  • Rigidity

  • Bradykinesia

  o Extremely slow movement

  • Pill-rolling tremor
• Qualitative screening may easily detect phenothiazines in urine or gastric juice, but butyrophenones such as haloperidol are usually not included in toxicologic screens.
• OTHER USEFUL LABORATORY STUDIES

  Electrolytes, glucose, BUN, creatinine, creatine phosphokinase (CPK), arterial blood gases or oximetry, abdominal x-ray (to look for radiopaque pills), chest x-ray