SlideShare a Scribd company logo
1 of 46
Download to read offline
ANTI-PSYCHOTIC DRUGS




 http://crisbertcualteros.page.tl
ANTI – PSYCHOTIC DRUGS

• NEUROLEPTIC DRUGS
• ANTI-SCHIZOPHRENIC DRUGS
• MAJOR TRANQUILIZERS
• DOPAMINE RECEPTOR
 ANTAGONISTS
TYPES OF PSYCHOSIS

  • SCHIZOPHRENIA
  • AFFECTIVE DISORDERS
    (DEPRESSION/MANIA)
  • ORGANIC PSYCHOSES
    (CAUSED BY HEAD INJURY,
    ALCOHOLISM, OTHERS)
THE NATURE OF SCHIZOPHRENIA
• Begins at an early age
• Strong hereditary factor
POSITIVE SYMPTOMS
 Delusions / Hallucinations
Thought disorder
NEGATIVE SYMPTOMS
Withdrawal from social contacts
Flattening of emotional responses
THE DOPAMINE HYPOTHESIS
• SCHIZOPRENIA: WITH EXCESSIVE
    DOPAMINIERGIC ACTIVITY
1. ANTIPSYCHOTIC DRUGS BLOCK
    POSTSYNAPTIC D2 RECEPTORS IN CNS

2. DRUGS THAT INCREASE DOPA
   AGGRAVATE SCHIZOPHRENIA
THE DOPAMINE HYPOTHESIS
3. DOPAMINE RECEPTOR DENSITY ↑ in
  schizophrenia

4. POSITRON EMISSION TOMOGRAPHY
  (PETS) ↑ DRD

5. HOMAVANILLIC ACID (HAV) change in
  amount
CLASSIFICATION OF ANTIPSYCHOTIC DRUGS

1. TYPICAL ANTIPSYCHOTICS
a. Phenothiazine derivatives
• Aliphatic Derivative: CHLORPROMAZINE
• Piperidine Derivative: THIORIDAZINE
• Piperazine Derivative: FLUPENAZINE,
    PERPHENAZINE, TRIFLUOPERAZINE
b. Thioxanthene Derivative: THIOTHIXENE
c. Butyrophenone: HALOPERIDOL
CLASSIFICATION OF ANTIPSYCHOTIC DRUGS

  2. ATYPICAL ANTIPSYCHOTICS
  • CLOZAPINE             LOXAPINE
  • OLANZAPINE
    QUETIAPINE
  • RISPERIDONE
    MOLINDONE
  • ZIPRASIDONE
  • SERTINDOLE
    ARIPIPRAZOLE
PHARMACOKINETICS
• READILY BUT INCOMPLETELY
  ABSORBED
• FIRST PASS METABOLISM
• HIGHLY LIPID SOLUBLE
• LARGE V d > 7 L / kg
• PROTIEN BOUND
• COMPLETELY METABOLIZED
• LITTLE EXCRETED UNCHANGED
• T ½ is 10 -24 hours
MECHANISM OF ACTION
• DOPAMINE RECEPTOR-BLOCKING
 ACTIVITY IN THE BRAIN

• SEROTONIN RECEPTOR-BLOCKING
 ACTIVITY IN THE BRAIN

• BLOCK CHOLINERGIC,
 ADRENERGIC & HISTAMINERGIC
 RECEPTORS
DOPAMINERGIC SYSTEM
• MESOLIMBIC-MESOCORTICAL :
   substancia nigra………>limbic system
    BEHAVIOR
2. NIGROSTRIATAL            : substancia
   nigra,,,……...>caudate & putamen
    VOLUNTARY MOVEMENTS
3.TUBEROINFUNDIBULAR: arcuate
   nuclei & periventricular neurons,,,>
   hypothalamus & post pituitary;
   INHIBITS PROLACTIN SECRETION
DOPAMINERGIC SYSTEM
4.MEDULLARY-PERIVENTRICULAR :
  motor nuclei of the vagus
  EATING BEHAVIOR

5. INCERTOHYPOTHALAMUS : from
  the medial zona incerta to the
  hypothalamus and the amygdala
  REGULATE THE ANTICIPATORY
  MOTIVATIONAL PHASE OF
  COPULATORY BEHAVIOR IN RATS
DOPAMINE RECEPTORS
• D1: CHROMOSOME 5; ↑ cAMP…>
  activation of adenyl cyclase
• D5 : CHROMOSOME 4; ↑ cAMP
• D2: CHROMOSOMES 11: ↓ cAMP…>
  blocks Ca ++ channels…> opens K +
           channels
• D3: CHROMOSOME 11: ↓ cAMP
• D4: ↓ cAMP
DIFFERENCES AMONG
ANTIPSYCHOTIC DRUGS

CHLORPROMAZINE: a1=5HT2 >D2 >D1

HALOPERIDOL: D2>D1=D4>a1>5HT2

CLOZAPINE : D4=a1>5HT>D2=D1
DIFFERENCES AMONG
ANTIPSYCHOTIC DRUGS

 OLANZAPINE: 5HT2A >D4 >D2 >a1 >D1

ARIPIPRAZOLE: D2 = 5HT 2A > D4 > a1
            =H1 > > D1

QUETIAPINE: H1 >a1 > M1,3 > D2 > 5
  HT2a
ANTIPSYCHOTIC AGENTS
• PSYCHOLOGICAL EFFECTS
> sleepiness, restlessness, impaired
  performance & judgment
• NEUROPHYSIOLOGIC EFFECTS
> hypersyncrony focal /unilateral
• ENDOCRINE EFFECTS
> amenorrhea, galactorrhea, increase libido,
  false( +) pregnancy tests
• ↓ libido in males, gynecomastia
ANTIPSYCHOTIC AGENTS
• CARDIOVASCULAR EFFECTS
orthostatic hypotension
 high resting pulse rate
↑ PR, ↓ stroke volume, ↓ mean
 arterial pressure,
↓ peripheral resistance
NAUSEA & VOMITING
Block the chemoreceptor trigger zone
CLINICAL INDICATIONS
A. PSYCHIATRY INDICATIONS
• SCHIZOPHREMIA
• SCHIZOAFFECTIVE DISORDERS
• MANIC EPISODES IN BIPOLAR
    DISORDERS
• GILLES DE TOURETTE SYNDROME
• SENILE DEMENTIA
B. NONPSYCHIATRIC INDICATIONS
>ANTI-EMETIC EFFECT (prochlorperazine)
>ANTI-PRURITIC EFFECTIphenothiazines)
>PREOPERATIVE
    ANESTHESIA.promethazine
>NEUROLEPTIC ANESTHESIA..droperidol
SIDE EFFECTTS OF NEUROLEPTIC
DRUGS
A. NEUROLOGIC EFFECTS
  1. ACUTE DYSTONIA : Spasm of muscles
  tongue, face, neck, back, may mimic
  seizures
• During the first 1 -5 days of Rx
• Mechanism unknown
• Rx: antiparkinson’s agents
  2. AKATHISIA : Motor restlessness
• 5 -60 days
• Mechanism unknown; Rx with
  diphenhydramine
3. PARKINSONISM
 bradykinesia, rigidity, tremor, mask facies,
  shuffling gait seen in 5-30 days
Mechanism is antagonism of Dopamine
Rx: Antiparkinson’s Agents
4. NEUROLEPTIC MALIGNANT SYNDROME:
catatonia, stupor, fever, unstable BP,
  myoglobulinemia after weeks of treatment
Mechanism: Antagonism of Dopamine
Rx: Stop neuroleptic immediately; Dandrolene;
  Bromocriptine, Antiparks not effective
5. PERIODIC TREMOR (RABBIT SYNDROME)
Perioral tremors
 after months or years of treatment
Mechanism : unknown
Rx Antiparkinson’s Drugs
6. TARDIVE DYSKINESIA
oral-facial dyskinesia, choreoathetosis, dystonia
After months or years of Rx
Worse on withdrawal
Mechanism: excess function of dopamine
Rx: prevention crucial Rx unsatisfactory
ADVERSE EFFECTS
II. BEHAVIORAL EFFECTS:
• Pseudo-depression; toxic confusional state
III. AUTONOMIC NERVOUS SUSTEM EFFECTS :
• urinary retention,dry mouth, loss of
   accommodation, constipation (MUSCARINIC
   CHOLINERGIC BLOCKADE)
• orthostatic hypotension, impotence, failure to
   ejaculate ( ALPHA ADRENORECEPTOR
   BLOCKADE)
ADVERSE EFFECTS
IV. METABOLIC & ENDOCRINE EFFECTS
Weight gain, hyperglycemia, hyper -
prolactenemia, amenorrhea-galactorrhea
  syndrome, infertility, impotence in males
V. TOXIC OR ALLERGIC REACTIONS
Agranulocytosis (clozapine) , cholestatic
  jaundice, skin eruptions
VI. CARDIAC TOXICITY
Ventricular arrythmias (thioridazine)
VII. OCULAR COMPLICATIONS: “ browning
  of vision”
ANTIMANIC AGENTS
• MOOD STABILIZING AGENT
• BIPOLAR DISORDERS (MANIC-
  DEPRESSIVE)
• DISORDER WITH PREPONDERANCE OF
  CATHECHOLAMINE RELATED ACTIVITY
• LITHIUM CARBONATE
• CARBAMAZEPINE, VALPROIC ACID
LITHIUM P’KINETICS
ABSORPTION           :     virtually complete
 within 6 -8 hrs; peak plasma levels in 30 min
 to 2 hrs
DISTRIBUTION: in total body water; slow
 entry into intracellular compartment. No
 protein binding
METABOLISM: None
EXCRETION: virtually entirely in urine; plasma
 half life is about 20 hours
LITHIUM ‘ DYNAMICS
• EFFECTS ON ELECTROLYTES & IONS
  TRANSPORT:
Substitute for sodium
• EFFECTS ON NEUROTRANSMITTER
 enhance effects of serotonin?
Decrease norepinephrine & dopamine
  turnover
Block dopamine receptor
  supersensitivity
Augment synthesis of acetylcholine?
LITHIUM PHARMACODYNAMICS
 • EFFECTS ON SECOND MESSENGER
 effect on IP3/ DAG

 EFFECTS ON PHOSPHOINOSITOL
  TURNOVER…..> EARLY RELATIVE
  REDUCTION OF MYOINOSITOL IN HUMAN
  BRAIN
LITHIUM ADVERSE EFFECTS
1. CNS EFFECTS; dizziness, mild ataxia
2. NEUROMUSCULAR EFECTS: fine tremors
3. CV EFFECTS: ventricular arrythmias
4. GIT EFFECTS: nausea, vomiting,
   diarrhea
5. GUT EFFECTS: polyuria
6. ENDOCRINE EFFECTS: hypothyroidism
7. ALLERGIC REACTION: pruritus, rash
8. OVERDOSE TOXICITY: vomiting,
   drowsiness, decrease consciousness
   seizures
Rx: dialysis
LITHIUM CONTRAINDICATION
A. MARKED DEHYDRATION OR
  SODIUM DEPLETION
B.SIGNIFICANT RENAL OR CARDIAC
  DISEASES
C. PREGNANCY(W)
D. RENAL CONCENTRATION
  ABILITY(W)
• Nephrogenic diabetes insipidus with
  polyuria
DRUG INTERACTIONS
A. THIAZIDE DIURETICS: ↓ RENAL
   CLEARANCE OF LITHIUM
B. NSAID: ↓ LITHIUM CLEARANCE
C. ANTIPYSCHOTIC AGENTS:
   ↑ NEUROTOXICITY
DEPRESSION
I.REACTIVE OR SECONDARY DEPRESSION
Core Depression Syndrome: depression, anxiety,
     tension, bodily complaints, guilt (> 60%)
II.ENDOGENOUS DEPRESSION
Core Depression Syndrome plus ABNORMAL VS
     rhythm of sleep, motor activity, livido,
     decrease appetite ( 25%)
III. DEPRESSION ASSOCIATED WITH BIPOLAR
     AFFECTIVE DISORDER
       (10-15%)
ANTIDEPRESSANTS
I.TRICYCLIC ANTIDEPRESSANTS
    IMIPRAMINE. AMITRYPTYLINE, DOXAPIN,
    NORTRIPTYLLINE ,DESIPRAMINE.
    CLOMIPRAMINE , PROTIPTYLINE,
    TRIMIPRAMINE
B. HETEROCYCLIC, SECOND & THIRD
    DEGENERATIONS
1. SECOND GENERATIONS
    AMOXAPINE, MAPROTILINE
    TRAZODON, BUPROPION
2. THIRD GENERATIONS
    MIRTAZAPINE, VENLAFAZINE
    NEFAXODONE
ANTIDEPRESSANTS
C. SELECTIVE SEROTONIN REUPTAKE
  INHIBITORS (SSRI)
• FLUOXETINE       FLUVOXAMINE
• PAROXETINE       ESCITALOPRAM
• SERTRALINE       CITALOPRAM
D. MONOAMINE OXIDASE
  INHIBITORS (MAOI)
• PHENELZINE, TRANYLCYPROMINE
• MOCLOBEMIDE
ANTIDEPRESSANTS PHARMADYNAMICS
A. ACTION OF ANTIDEPRESSANTS ON
  BIOGENIC AMINE
  NEUROTRANSMITTERS
 TRICYCLICS: BLOCK AMINE REUPTAKE
  PUMPS
 MAOI: BLOCK DEGRADATIVE PATHWAY
  FOR THE AMINE NEUROTRANSMITTERS
 TRAZODON, NEFAZODONE &
  MIRTAZAPINE: SERETONIN RECEPTORS
  ANTAGONIST
B.RECEPTOR & POSTRECEPTOR
     EFFECTS
• SSRI: ↓ in norepinephrine cAMP &
  in beta -adrenoreceptor binding
• MAOI: mixed action with
  norepinephrine & serotonin
• ↑ serotonergic transmission
  mediated through diverse
  mechanisms
Drug            Sedati Muscar NE        5HT reuptake
                ve     inicrBl reuptake block
                       ock     Block
Amitryptyline   +++ +++       ++       +++

Imipramine      ++  +         +        ++
Amoxapine       ++  +         ++       +
Bupropion       -     -         -        -
Trazodone       +++ -            -       ++
Mirtazepine     +++     -       -        -
Venlafaxine      -      -      +++      ++
Fluoxetine      -       +       -      +++
PHARMACOKINETICS
• A. TRICYCLICS
Incompletely reabsorbed
First pass metabolism
Large Vd
Metabolized
HETEROCYCLICS
Variable bioavailabilitiy
High protein binding
Variable and large Vd
Active metabolites
PHARMACOKINETICS
• SSRI : FLUOXETINE
• Well absorbed
• PPC: 4 – 8 hrs
• Inhibits drug metabolizing enzymes
• MAOI
• Readily absorbed
CLINICAL INDICATIONS
A. DEPRESSION
B. PANIC DISORDER
C. OBSESSIVE COMPULISVE
D. ENURESIS
E. CHRONIC PAIN
F. OTHERS: Eating Disorder(Bulemia)
Cataplexy asstd with Narcolepsy,
   School Phobia, Attention Deficit
   Syndrome
ADVERSE EFFECTS
• TRICYCLICS
Sedation:            Sleepiness
Synpathomimetic;       tremors,
                         insomnia
Antimuscarinic;       blurred vision.
                constipation
 confusion,
                 urinary
 incontinence
TRICYCLICS
Psychiatric:   psychoses
                  aggravated
CVS:          orthostatic
                  hypotension
Neurologic:         Seizures
Metabolic-Endocrine: weight
 gain,            sexual
 disturbance
ADVERSE EFFECTS
MAO INHIBITORS
headache, drowsiness, dry mouth,
 weight gain, postural hypotension,
 sexual distn
AMOXAPIN
 Tricyclic & antipsychotic effects
MAPROTILINE
Tricyclic Effects
ADVERSE EFFECTS
TRAZODONE & NEFAZODONE:
 drowsiness, dizziness, insomnia,
 nausea, agitation
BUPROPION
dizziness, dry mouth, tremor
FLUOXETINE
Anxiety, insomnia, tremors, decr
 libido, GIT effects
Foods that interact with MAOI
• High in tyramine content:
BEER.
BROAD BEANS, LAVA BEANS
CHEESE.
CHICKEN LIVER
 SAUSAGES
 SNAILS WINE, RED WINE
YEAST
Drugs that Interact with MAOI
A.INDIRECTLY ACTING
  SYMPATHOMIMETICS: amphetamines,
  ephedrine, metaraminol,
  phenylpropanolamine
B. OTHER ADRENORECEPTOR AGENTS &
  RELATED AGENTS: levodopa, methyldopa,
  guanethidine, reserpine
C. OPIOID ANALGESICS &
  DERIVATIVES: morphine, codeine,
  meperidine, dextromethorpham
D.MISCELLANEOUS DRUGS: buspirone,
  fluoxetine, LSD
anti-psychotic drugs

More Related Content

What's hot

What's hot (20)

Antipsychotics
AntipsychoticsAntipsychotics
Antipsychotics
 
Antidepressants -pharmacology
Antidepressants -pharmacologyAntidepressants -pharmacology
Antidepressants -pharmacology
 
Antipsychotics
AntipsychoticsAntipsychotics
Antipsychotics
 
Antipsychotic drugs
Antipsychotic drugsAntipsychotic drugs
Antipsychotic drugs
 
ANTIDEPRESSANTS
ANTIDEPRESSANTSANTIDEPRESSANTS
ANTIDEPRESSANTS
 
Antidepressants - Pharmacology
 Antidepressants - Pharmacology Antidepressants - Pharmacology
Antidepressants - Pharmacology
 
Selective serotonin reuptake inhibitors 2016
Selective serotonin reuptake inhibitors 2016Selective serotonin reuptake inhibitors 2016
Selective serotonin reuptake inhibitors 2016
 
Antipsychotic drugs ppt
Antipsychotic drugs pptAntipsychotic drugs ppt
Antipsychotic drugs ppt
 
Antidepressants
AntidepressantsAntidepressants
Antidepressants
 
Schizophrenia and Antipsychotic Drugs
Schizophrenia and Antipsychotic DrugsSchizophrenia and Antipsychotic Drugs
Schizophrenia and Antipsychotic Drugs
 
Antianxiety drugs
Antianxiety drugsAntianxiety drugs
Antianxiety drugs
 
Antipsychotics and updates
Antipsychotics and updatesAntipsychotics and updates
Antipsychotics and updates
 
Levodopa
LevodopaLevodopa
Levodopa
 
Sedatives & hypnotics
Sedatives & hypnoticsSedatives & hypnotics
Sedatives & hypnotics
 
Antidepressants
Antidepressants Antidepressants
Antidepressants
 
Drug Therapy of Depression
Drug Therapy of Depression Drug Therapy of Depression
Drug Therapy of Depression
 
Anti-Parkinsonism Drugs / Drugs Used in the treatment of Parkinson's Disease
Anti-Parkinsonism Drugs / Drugs Used in the treatment of Parkinson's DiseaseAnti-Parkinsonism Drugs / Drugs Used in the treatment of Parkinson's Disease
Anti-Parkinsonism Drugs / Drugs Used in the treatment of Parkinson's Disease
 
Typical antipsychotics
Typical   antipsychoticsTypical   antipsychotics
Typical antipsychotics
 
Antimanic drugs and its pharmacology
Antimanic drugs and its pharmacologyAntimanic drugs and its pharmacology
Antimanic drugs and its pharmacology
 
ANTIDEPRESSANTS
ANTIDEPRESSANTSANTIDEPRESSANTS
ANTIDEPRESSANTS
 

Viewers also liked

Viewers also liked (6)

Sedative hypnotic drugs
Sedative hypnotic drugsSedative hypnotic drugs
Sedative hypnotic drugs
 
Sedative hypnotics.ppt - dr dhriti
Sedative hypnotics.ppt - dr dhriti Sedative hypnotics.ppt - dr dhriti
Sedative hypnotics.ppt - dr dhriti
 
Sedative Hypnotic
Sedative HypnoticSedative Hypnotic
Sedative Hypnotic
 
Antipsychotics
AntipsychoticsAntipsychotics
Antipsychotics
 
Sedative-Hypnotic Drugs
Sedative-Hypnotic DrugsSedative-Hypnotic Drugs
Sedative-Hypnotic Drugs
 
Antipsychotic drugs
Antipsychotic drugsAntipsychotic drugs
Antipsychotic drugs
 

Similar to anti-psychotic drugs

Antidepressants BY Dise.pptx
Antidepressants BY Dise.pptxAntidepressants BY Dise.pptx
Antidepressants BY Dise.pptxXavier875943
 
pharmacology of Antipsychotic Agents & Lithium.ppt
pharmacology of Antipsychotic Agents & Lithium.pptpharmacology of Antipsychotic Agents & Lithium.ppt
pharmacology of Antipsychotic Agents & Lithium.pptNorhanKhaled15
 
Skeletal muscle relaxants & Spasmolytics dr abdul azeem
Skeletal muscle relaxants & Spasmolytics dr abdul azeemSkeletal muscle relaxants & Spasmolytics dr abdul azeem
Skeletal muscle relaxants & Spasmolytics dr abdul azeemHassan Ahmad
 
Drugs Acting on Autonomic Nervous System
Drugs Acting on Autonomic Nervous SystemDrugs Acting on Autonomic Nervous System
Drugs Acting on Autonomic Nervous SystemAbhijeet Lokras
 
Anti depressants
Anti depressantsAnti depressants
Anti depressantsraj kumar
 
Antidepressants /certified fixed orthodontic courses by Indian dental academy
Antidepressants  /certified fixed orthodontic courses by Indian dental academy Antidepressants  /certified fixed orthodontic courses by Indian dental academy
Antidepressants /certified fixed orthodontic courses by Indian dental academy Indian dental academy
 
Mydriatics & cycloplegics
Mydriatics & cycloplegicsMydriatics & cycloplegics
Mydriatics & cycloplegicsVinitkumar MJ
 
Emetics, antiemetics and prokinetic agents.pptx
Emetics, antiemetics and prokinetic agents.pptxEmetics, antiemetics and prokinetic agents.pptx
Emetics, antiemetics and prokinetic agents.pptxsapnabohra2
 

Similar to anti-psychotic drugs (20)

Anti Psychoticdoncua
Anti PsychoticdoncuaAnti Psychoticdoncua
Anti Psychoticdoncua
 
Antidepressants BY Dise.pptx
Antidepressants BY Dise.pptxAntidepressants BY Dise.pptx
Antidepressants BY Dise.pptx
 
Psychopharmacology
PsychopharmacologyPsychopharmacology
Psychopharmacology
 
Anti emetics
Anti emeticsAnti emetics
Anti emetics
 
Antiemetics
AntiemeticsAntiemetics
Antiemetics
 
pharmacology of Antipsychotic Agents & Lithium.ppt
pharmacology of Antipsychotic Agents & Lithium.pptpharmacology of Antipsychotic Agents & Lithium.ppt
pharmacology of Antipsychotic Agents & Lithium.ppt
 
Neuroleptics and Tranquilazers
Neuroleptics and TranquilazersNeuroleptics and Tranquilazers
Neuroleptics and Tranquilazers
 
Cholinergic drugs
Cholinergic drugsCholinergic drugs
Cholinergic drugs
 
Skeletal muscle relaxants & Spasmolytics dr abdul azeem
Skeletal muscle relaxants & Spasmolytics dr abdul azeemSkeletal muscle relaxants & Spasmolytics dr abdul azeem
Skeletal muscle relaxants & Spasmolytics dr abdul azeem
 
Drugs Acting on Autonomic Nervous System
Drugs Acting on Autonomic Nervous SystemDrugs Acting on Autonomic Nervous System
Drugs Acting on Autonomic Nervous System
 
DEPRESSION.pptx
DEPRESSION.pptxDEPRESSION.pptx
DEPRESSION.pptx
 
Antidepressants_Hand Out.pdf
Antidepressants_Hand Out.pdfAntidepressants_Hand Out.pdf
Antidepressants_Hand Out.pdf
 
Anti depressants
Anti depressantsAnti depressants
Anti depressants
 
Antidepressants /certified fixed orthodontic courses by Indian dental academy
Antidepressants  /certified fixed orthodontic courses by Indian dental academy Antidepressants  /certified fixed orthodontic courses by Indian dental academy
Antidepressants /certified fixed orthodontic courses by Indian dental academy
 
Mydriatics & cycloplegics
Mydriatics & cycloplegicsMydriatics & cycloplegics
Mydriatics & cycloplegics
 
Antipsychotics agents
Antipsychotics agents Antipsychotics agents
Antipsychotics agents
 
9. antipsychotics
9. antipsychotics9. antipsychotics
9. antipsychotics
 
Anticholinergics
AnticholinergicsAnticholinergics
Anticholinergics
 
NEUROTRANSMITTERS 1.pptx
NEUROTRANSMITTERS 1.pptxNEUROTRANSMITTERS 1.pptx
NEUROTRANSMITTERS 1.pptx
 
Emetics, antiemetics and prokinetic agents.pptx
Emetics, antiemetics and prokinetic agents.pptxEmetics, antiemetics and prokinetic agents.pptx
Emetics, antiemetics and prokinetic agents.pptx
 

More from DJ CrissCross

2019 Novel Coronavirus
2019 Novel Coronavirus2019 Novel Coronavirus
2019 Novel CoronavirusDJ CrissCross
 
Aspirin for Primary Prevention of Cardiovascular Disease
Aspirin for Primary Prevention of Cardiovascular DiseaseAspirin for Primary Prevention of Cardiovascular Disease
Aspirin for Primary Prevention of Cardiovascular DiseaseDJ CrissCross
 
Acute Myocardial Infarction
Acute Myocardial InfarctionAcute Myocardial Infarction
Acute Myocardial InfarctionDJ CrissCross
 
Syndrome of inappropriate anti diuretic hormone secretion (siadh)
Syndrome of inappropriate anti diuretic hormone secretion (siadh)Syndrome of inappropriate anti diuretic hormone secretion (siadh)
Syndrome of inappropriate anti diuretic hormone secretion (siadh)DJ CrissCross
 
Vitamin B12 Deficiency
Vitamin B12 DeficiencyVitamin B12 Deficiency
Vitamin B12 DeficiencyDJ CrissCross
 
Clostridium difficile infection
Clostridium difficile infectionClostridium difficile infection
Clostridium difficile infectionDJ CrissCross
 
Hydrocarbon Toxicity
Hydrocarbon ToxicityHydrocarbon Toxicity
Hydrocarbon ToxicityDJ CrissCross
 
Amyotrophic Lateral Sclerosis
Amyotrophic Lateral SclerosisAmyotrophic Lateral Sclerosis
Amyotrophic Lateral SclerosisDJ CrissCross
 
Emergencies In Oncology
Emergencies In OncologyEmergencies In Oncology
Emergencies In OncologyDJ CrissCross
 
Sjogren’s syndrome
Sjogren’s syndromeSjogren’s syndrome
Sjogren’s syndromeDJ CrissCross
 
Approach to a patient with JAUNDICE
Approach to a patient with JAUNDICEApproach to a patient with JAUNDICE
Approach to a patient with JAUNDICEDJ CrissCross
 
Paraneoplastic Endocrine Syndrome
Paraneoplastic Endocrine SyndromeParaneoplastic Endocrine Syndrome
Paraneoplastic Endocrine SyndromeDJ CrissCross
 
Physical Examination
Physical ExaminationPhysical Examination
Physical ExaminationDJ CrissCross
 
Diagnosis of Hyponatremia
Diagnosis of HyponatremiaDiagnosis of Hyponatremia
Diagnosis of HyponatremiaDJ CrissCross
 

More from DJ CrissCross (20)

2019 Novel Coronavirus
2019 Novel Coronavirus2019 Novel Coronavirus
2019 Novel Coronavirus
 
Aspirin for Primary Prevention of Cardiovascular Disease
Aspirin for Primary Prevention of Cardiovascular DiseaseAspirin for Primary Prevention of Cardiovascular Disease
Aspirin for Primary Prevention of Cardiovascular Disease
 
CURB - 65
CURB - 65CURB - 65
CURB - 65
 
Epilepsy
EpilepsyEpilepsy
Epilepsy
 
Acute Myocardial Infarction
Acute Myocardial InfarctionAcute Myocardial Infarction
Acute Myocardial Infarction
 
Syndrome of inappropriate anti diuretic hormone secretion (siadh)
Syndrome of inappropriate anti diuretic hormone secretion (siadh)Syndrome of inappropriate anti diuretic hormone secretion (siadh)
Syndrome of inappropriate anti diuretic hormone secretion (siadh)
 
Vitamin B12 Deficiency
Vitamin B12 DeficiencyVitamin B12 Deficiency
Vitamin B12 Deficiency
 
Stroke
StrokeStroke
Stroke
 
Clostridium difficile infection
Clostridium difficile infectionClostridium difficile infection
Clostridium difficile infection
 
Hydrocarbon Toxicity
Hydrocarbon ToxicityHydrocarbon Toxicity
Hydrocarbon Toxicity
 
Amyotrophic Lateral Sclerosis
Amyotrophic Lateral SclerosisAmyotrophic Lateral Sclerosis
Amyotrophic Lateral Sclerosis
 
Emergencies In Oncology
Emergencies In OncologyEmergencies In Oncology
Emergencies In Oncology
 
Esophageal Cancer
Esophageal CancerEsophageal Cancer
Esophageal Cancer
 
Diabetes Mellitus
Diabetes MellitusDiabetes Mellitus
Diabetes Mellitus
 
Sjogren’s syndrome
Sjogren’s syndromeSjogren’s syndrome
Sjogren’s syndrome
 
Approach to a patient with JAUNDICE
Approach to a patient with JAUNDICEApproach to a patient with JAUNDICE
Approach to a patient with JAUNDICE
 
Paraneoplastic Endocrine Syndrome
Paraneoplastic Endocrine SyndromeParaneoplastic Endocrine Syndrome
Paraneoplastic Endocrine Syndrome
 
Emergencies in ENT
Emergencies in ENTEmergencies in ENT
Emergencies in ENT
 
Physical Examination
Physical ExaminationPhysical Examination
Physical Examination
 
Diagnosis of Hyponatremia
Diagnosis of HyponatremiaDiagnosis of Hyponatremia
Diagnosis of Hyponatremia
 

Recently uploaded

Female Reproductive Physiology Before Pregnancy
Female Reproductive Physiology Before PregnancyFemale Reproductive Physiology Before Pregnancy
Female Reproductive Physiology Before PregnancyMedicoseAcademics
 
AUTONOMIC NERVOUS SYSTEM organization and functions
AUTONOMIC NERVOUS SYSTEM organization and functionsAUTONOMIC NERVOUS SYSTEM organization and functions
AUTONOMIC NERVOUS SYSTEM organization and functionsMedicoseAcademics
 
Physiology of Smooth Muscles -Mechanics of contraction and relaxation
Physiology of Smooth Muscles -Mechanics of contraction and relaxationPhysiology of Smooth Muscles -Mechanics of contraction and relaxation
Physiology of Smooth Muscles -Mechanics of contraction and relaxationMedicoseAcademics
 
Clinical Research Informatics Year-in-Review 2024
Clinical Research Informatics Year-in-Review 2024Clinical Research Informatics Year-in-Review 2024
Clinical Research Informatics Year-in-Review 2024Peter Embi
 
power point presentation of Clinical evaluation of strabismus
power point presentation of Clinical evaluation  of strabismuspower point presentation of Clinical evaluation  of strabismus
power point presentation of Clinical evaluation of strabismusChandrasekar Reddy
 
"Radical excision of DIE in subferile women with deep infiltrating endometrio...
"Radical excision of DIE in subferile women with deep infiltrating endometrio..."Radical excision of DIE in subferile women with deep infiltrating endometrio...
"Radical excision of DIE in subferile women with deep infiltrating endometrio...Sujoy Dasgupta
 
DNA nucleotides Blast in NCBI and Phylogeny using MEGA Xi.pptx
DNA nucleotides Blast in NCBI and Phylogeny using MEGA Xi.pptxDNA nucleotides Blast in NCBI and Phylogeny using MEGA Xi.pptx
DNA nucleotides Blast in NCBI and Phylogeny using MEGA Xi.pptxMAsifAhmad
 
SGK ĐIỆN GIẬT ĐHYHN RẤT LÀ HAY TUYỆT VỜI.pdf
SGK ĐIỆN GIẬT ĐHYHN        RẤT LÀ HAY TUYỆT VỜI.pdfSGK ĐIỆN GIẬT ĐHYHN        RẤT LÀ HAY TUYỆT VỜI.pdf
SGK ĐIỆN GIẬT ĐHYHN RẤT LÀ HAY TUYỆT VỜI.pdfHongBiThi1
 
pA2 value, Schild plot and pD2 values- applications in pharmacology
pA2 value, Schild plot and pD2 values- applications in pharmacologypA2 value, Schild plot and pD2 values- applications in pharmacology
pA2 value, Schild plot and pD2 values- applications in pharmacologyDeepakDaniel9
 
MedMatch: Your Health, Our Mission. Pitch deck.
MedMatch: Your Health, Our Mission. Pitch deck.MedMatch: Your Health, Our Mission. Pitch deck.
MedMatch: Your Health, Our Mission. Pitch deck.whalesdesign
 
historyofpsychiatryinindia. Senthil Thirusangu
historyofpsychiatryinindia. Senthil Thirusanguhistoryofpsychiatryinindia. Senthil Thirusangu
historyofpsychiatryinindia. Senthil Thirusangu Medical University
 
SGK RỐI LOẠN TOAN KIỀM ĐHYHN RẤT HAY VÀ ĐẶC SẮC.pdf
SGK RỐI LOẠN TOAN KIỀM ĐHYHN RẤT HAY VÀ ĐẶC SẮC.pdfSGK RỐI LOẠN TOAN KIỀM ĐHYHN RẤT HAY VÀ ĐẶC SẮC.pdf
SGK RỐI LOẠN TOAN KIỀM ĐHYHN RẤT HAY VÀ ĐẶC SẮC.pdfHongBiThi1
 
Pharmacokinetic Models by Dr. Ram D. Bawankar.ppt
Pharmacokinetic Models by Dr. Ram D.  Bawankar.pptPharmacokinetic Models by Dr. Ram D.  Bawankar.ppt
Pharmacokinetic Models by Dr. Ram D. Bawankar.pptRamDBawankar1
 
Trustworthiness of AI based predictions Aachen 2024
Trustworthiness of AI based predictions Aachen 2024Trustworthiness of AI based predictions Aachen 2024
Trustworthiness of AI based predictions Aachen 2024EwoutSteyerberg1
 
ORAL HYPOGLYCAEMIC AGENTS - PART 2.pptx
ORAL HYPOGLYCAEMIC AGENTS  - PART 2.pptxORAL HYPOGLYCAEMIC AGENTS  - PART 2.pptx
ORAL HYPOGLYCAEMIC AGENTS - PART 2.pptxNIKITA BHUTE
 
AORTIC DISSECTION and management of aortic dissection
AORTIC DISSECTION and management of aortic dissectionAORTIC DISSECTION and management of aortic dissection
AORTIC DISSECTION and management of aortic dissectiondrhanifmohdali
 
CONNECTIVE TISSUE (ANATOMY AND PHYSIOLOGY).pdf
CONNECTIVE TISSUE (ANATOMY AND PHYSIOLOGY).pdfCONNECTIVE TISSUE (ANATOMY AND PHYSIOLOGY).pdf
CONNECTIVE TISSUE (ANATOMY AND PHYSIOLOGY).pdfDolisha Warbi
 
Using Data Visualization in Public Health Communications
Using Data Visualization in Public Health CommunicationsUsing Data Visualization in Public Health Communications
Using Data Visualization in Public Health Communicationskatiequigley33
 
Generative AI in Health Care a scoping review and a persoanl experience.
Generative AI in Health Care a scoping review and a persoanl experience.Generative AI in Health Care a scoping review and a persoanl experience.
Generative AI in Health Care a scoping review and a persoanl experience.Vaikunthan Rajaratnam
 

Recently uploaded (20)

Female Reproductive Physiology Before Pregnancy
Female Reproductive Physiology Before PregnancyFemale Reproductive Physiology Before Pregnancy
Female Reproductive Physiology Before Pregnancy
 
AUTONOMIC NERVOUS SYSTEM organization and functions
AUTONOMIC NERVOUS SYSTEM organization and functionsAUTONOMIC NERVOUS SYSTEM organization and functions
AUTONOMIC NERVOUS SYSTEM organization and functions
 
Physiology of Smooth Muscles -Mechanics of contraction and relaxation
Physiology of Smooth Muscles -Mechanics of contraction and relaxationPhysiology of Smooth Muscles -Mechanics of contraction and relaxation
Physiology of Smooth Muscles -Mechanics of contraction and relaxation
 
Clinical Research Informatics Year-in-Review 2024
Clinical Research Informatics Year-in-Review 2024Clinical Research Informatics Year-in-Review 2024
Clinical Research Informatics Year-in-Review 2024
 
American College of physicians ACP high value care recommendations in rheumat...
American College of physicians ACP high value care recommendations in rheumat...American College of physicians ACP high value care recommendations in rheumat...
American College of physicians ACP high value care recommendations in rheumat...
 
power point presentation of Clinical evaluation of strabismus
power point presentation of Clinical evaluation  of strabismuspower point presentation of Clinical evaluation  of strabismus
power point presentation of Clinical evaluation of strabismus
 
"Radical excision of DIE in subferile women with deep infiltrating endometrio...
"Radical excision of DIE in subferile women with deep infiltrating endometrio..."Radical excision of DIE in subferile women with deep infiltrating endometrio...
"Radical excision of DIE in subferile women with deep infiltrating endometrio...
 
DNA nucleotides Blast in NCBI and Phylogeny using MEGA Xi.pptx
DNA nucleotides Blast in NCBI and Phylogeny using MEGA Xi.pptxDNA nucleotides Blast in NCBI and Phylogeny using MEGA Xi.pptx
DNA nucleotides Blast in NCBI and Phylogeny using MEGA Xi.pptx
 
SGK ĐIỆN GIẬT ĐHYHN RẤT LÀ HAY TUYỆT VỜI.pdf
SGK ĐIỆN GIẬT ĐHYHN        RẤT LÀ HAY TUYỆT VỜI.pdfSGK ĐIỆN GIẬT ĐHYHN        RẤT LÀ HAY TUYỆT VỜI.pdf
SGK ĐIỆN GIẬT ĐHYHN RẤT LÀ HAY TUYỆT VỜI.pdf
 
pA2 value, Schild plot and pD2 values- applications in pharmacology
pA2 value, Schild plot and pD2 values- applications in pharmacologypA2 value, Schild plot and pD2 values- applications in pharmacology
pA2 value, Schild plot and pD2 values- applications in pharmacology
 
MedMatch: Your Health, Our Mission. Pitch deck.
MedMatch: Your Health, Our Mission. Pitch deck.MedMatch: Your Health, Our Mission. Pitch deck.
MedMatch: Your Health, Our Mission. Pitch deck.
 
historyofpsychiatryinindia. Senthil Thirusangu
historyofpsychiatryinindia. Senthil Thirusanguhistoryofpsychiatryinindia. Senthil Thirusangu
historyofpsychiatryinindia. Senthil Thirusangu
 
SGK RỐI LOẠN TOAN KIỀM ĐHYHN RẤT HAY VÀ ĐẶC SẮC.pdf
SGK RỐI LOẠN TOAN KIỀM ĐHYHN RẤT HAY VÀ ĐẶC SẮC.pdfSGK RỐI LOẠN TOAN KIỀM ĐHYHN RẤT HAY VÀ ĐẶC SẮC.pdf
SGK RỐI LOẠN TOAN KIỀM ĐHYHN RẤT HAY VÀ ĐẶC SẮC.pdf
 
Pharmacokinetic Models by Dr. Ram D. Bawankar.ppt
Pharmacokinetic Models by Dr. Ram D.  Bawankar.pptPharmacokinetic Models by Dr. Ram D.  Bawankar.ppt
Pharmacokinetic Models by Dr. Ram D. Bawankar.ppt
 
Trustworthiness of AI based predictions Aachen 2024
Trustworthiness of AI based predictions Aachen 2024Trustworthiness of AI based predictions Aachen 2024
Trustworthiness of AI based predictions Aachen 2024
 
ORAL HYPOGLYCAEMIC AGENTS - PART 2.pptx
ORAL HYPOGLYCAEMIC AGENTS  - PART 2.pptxORAL HYPOGLYCAEMIC AGENTS  - PART 2.pptx
ORAL HYPOGLYCAEMIC AGENTS - PART 2.pptx
 
AORTIC DISSECTION and management of aortic dissection
AORTIC DISSECTION and management of aortic dissectionAORTIC DISSECTION and management of aortic dissection
AORTIC DISSECTION and management of aortic dissection
 
CONNECTIVE TISSUE (ANATOMY AND PHYSIOLOGY).pdf
CONNECTIVE TISSUE (ANATOMY AND PHYSIOLOGY).pdfCONNECTIVE TISSUE (ANATOMY AND PHYSIOLOGY).pdf
CONNECTIVE TISSUE (ANATOMY AND PHYSIOLOGY).pdf
 
Using Data Visualization in Public Health Communications
Using Data Visualization in Public Health CommunicationsUsing Data Visualization in Public Health Communications
Using Data Visualization in Public Health Communications
 
Generative AI in Health Care a scoping review and a persoanl experience.
Generative AI in Health Care a scoping review and a persoanl experience.Generative AI in Health Care a scoping review and a persoanl experience.
Generative AI in Health Care a scoping review and a persoanl experience.
 

anti-psychotic drugs

  • 2. ANTI – PSYCHOTIC DRUGS • NEUROLEPTIC DRUGS • ANTI-SCHIZOPHRENIC DRUGS • MAJOR TRANQUILIZERS • DOPAMINE RECEPTOR ANTAGONISTS
  • 3. TYPES OF PSYCHOSIS • SCHIZOPHRENIA • AFFECTIVE DISORDERS (DEPRESSION/MANIA) • ORGANIC PSYCHOSES (CAUSED BY HEAD INJURY, ALCOHOLISM, OTHERS)
  • 4. THE NATURE OF SCHIZOPHRENIA • Begins at an early age • Strong hereditary factor POSITIVE SYMPTOMS  Delusions / Hallucinations Thought disorder NEGATIVE SYMPTOMS Withdrawal from social contacts Flattening of emotional responses
  • 5. THE DOPAMINE HYPOTHESIS • SCHIZOPRENIA: WITH EXCESSIVE DOPAMINIERGIC ACTIVITY 1. ANTIPSYCHOTIC DRUGS BLOCK POSTSYNAPTIC D2 RECEPTORS IN CNS 2. DRUGS THAT INCREASE DOPA AGGRAVATE SCHIZOPHRENIA
  • 6. THE DOPAMINE HYPOTHESIS 3. DOPAMINE RECEPTOR DENSITY ↑ in schizophrenia 4. POSITRON EMISSION TOMOGRAPHY (PETS) ↑ DRD 5. HOMAVANILLIC ACID (HAV) change in amount
  • 7. CLASSIFICATION OF ANTIPSYCHOTIC DRUGS 1. TYPICAL ANTIPSYCHOTICS a. Phenothiazine derivatives • Aliphatic Derivative: CHLORPROMAZINE • Piperidine Derivative: THIORIDAZINE • Piperazine Derivative: FLUPENAZINE, PERPHENAZINE, TRIFLUOPERAZINE b. Thioxanthene Derivative: THIOTHIXENE c. Butyrophenone: HALOPERIDOL
  • 8. CLASSIFICATION OF ANTIPSYCHOTIC DRUGS 2. ATYPICAL ANTIPSYCHOTICS • CLOZAPINE LOXAPINE • OLANZAPINE QUETIAPINE • RISPERIDONE MOLINDONE • ZIPRASIDONE • SERTINDOLE ARIPIPRAZOLE
  • 9. PHARMACOKINETICS • READILY BUT INCOMPLETELY ABSORBED • FIRST PASS METABOLISM • HIGHLY LIPID SOLUBLE • LARGE V d > 7 L / kg • PROTIEN BOUND • COMPLETELY METABOLIZED • LITTLE EXCRETED UNCHANGED • T ½ is 10 -24 hours
  • 10. MECHANISM OF ACTION • DOPAMINE RECEPTOR-BLOCKING ACTIVITY IN THE BRAIN • SEROTONIN RECEPTOR-BLOCKING ACTIVITY IN THE BRAIN • BLOCK CHOLINERGIC, ADRENERGIC & HISTAMINERGIC RECEPTORS
  • 11. DOPAMINERGIC SYSTEM • MESOLIMBIC-MESOCORTICAL : substancia nigra………>limbic system BEHAVIOR 2. NIGROSTRIATAL : substancia nigra,,,……...>caudate & putamen VOLUNTARY MOVEMENTS 3.TUBEROINFUNDIBULAR: arcuate nuclei & periventricular neurons,,,> hypothalamus & post pituitary; INHIBITS PROLACTIN SECRETION
  • 12. DOPAMINERGIC SYSTEM 4.MEDULLARY-PERIVENTRICULAR : motor nuclei of the vagus EATING BEHAVIOR 5. INCERTOHYPOTHALAMUS : from the medial zona incerta to the hypothalamus and the amygdala REGULATE THE ANTICIPATORY MOTIVATIONAL PHASE OF COPULATORY BEHAVIOR IN RATS
  • 13. DOPAMINE RECEPTORS • D1: CHROMOSOME 5; ↑ cAMP…> activation of adenyl cyclase • D5 : CHROMOSOME 4; ↑ cAMP • D2: CHROMOSOMES 11: ↓ cAMP…> blocks Ca ++ channels…> opens K + channels • D3: CHROMOSOME 11: ↓ cAMP • D4: ↓ cAMP
  • 14. DIFFERENCES AMONG ANTIPSYCHOTIC DRUGS CHLORPROMAZINE: a1=5HT2 >D2 >D1 HALOPERIDOL: D2>D1=D4>a1>5HT2 CLOZAPINE : D4=a1>5HT>D2=D1
  • 15. DIFFERENCES AMONG ANTIPSYCHOTIC DRUGS OLANZAPINE: 5HT2A >D4 >D2 >a1 >D1 ARIPIPRAZOLE: D2 = 5HT 2A > D4 > a1 =H1 > > D1 QUETIAPINE: H1 >a1 > M1,3 > D2 > 5 HT2a
  • 16. ANTIPSYCHOTIC AGENTS • PSYCHOLOGICAL EFFECTS > sleepiness, restlessness, impaired performance & judgment • NEUROPHYSIOLOGIC EFFECTS > hypersyncrony focal /unilateral • ENDOCRINE EFFECTS > amenorrhea, galactorrhea, increase libido, false( +) pregnancy tests • ↓ libido in males, gynecomastia
  • 17. ANTIPSYCHOTIC AGENTS • CARDIOVASCULAR EFFECTS orthostatic hypotension  high resting pulse rate ↑ PR, ↓ stroke volume, ↓ mean arterial pressure, ↓ peripheral resistance NAUSEA & VOMITING Block the chemoreceptor trigger zone
  • 18. CLINICAL INDICATIONS A. PSYCHIATRY INDICATIONS • SCHIZOPHREMIA • SCHIZOAFFECTIVE DISORDERS • MANIC EPISODES IN BIPOLAR DISORDERS • GILLES DE TOURETTE SYNDROME • SENILE DEMENTIA B. NONPSYCHIATRIC INDICATIONS >ANTI-EMETIC EFFECT (prochlorperazine) >ANTI-PRURITIC EFFECTIphenothiazines) >PREOPERATIVE ANESTHESIA.promethazine >NEUROLEPTIC ANESTHESIA..droperidol
  • 19. SIDE EFFECTTS OF NEUROLEPTIC DRUGS A. NEUROLOGIC EFFECTS 1. ACUTE DYSTONIA : Spasm of muscles tongue, face, neck, back, may mimic seizures • During the first 1 -5 days of Rx • Mechanism unknown • Rx: antiparkinson’s agents 2. AKATHISIA : Motor restlessness • 5 -60 days • Mechanism unknown; Rx with diphenhydramine
  • 20. 3. PARKINSONISM  bradykinesia, rigidity, tremor, mask facies, shuffling gait seen in 5-30 days Mechanism is antagonism of Dopamine Rx: Antiparkinson’s Agents 4. NEUROLEPTIC MALIGNANT SYNDROME: catatonia, stupor, fever, unstable BP, myoglobulinemia after weeks of treatment Mechanism: Antagonism of Dopamine Rx: Stop neuroleptic immediately; Dandrolene; Bromocriptine, Antiparks not effective
  • 21. 5. PERIODIC TREMOR (RABBIT SYNDROME) Perioral tremors  after months or years of treatment Mechanism : unknown Rx Antiparkinson’s Drugs 6. TARDIVE DYSKINESIA oral-facial dyskinesia, choreoathetosis, dystonia After months or years of Rx Worse on withdrawal Mechanism: excess function of dopamine Rx: prevention crucial Rx unsatisfactory
  • 22. ADVERSE EFFECTS II. BEHAVIORAL EFFECTS: • Pseudo-depression; toxic confusional state III. AUTONOMIC NERVOUS SUSTEM EFFECTS : • urinary retention,dry mouth, loss of accommodation, constipation (MUSCARINIC CHOLINERGIC BLOCKADE) • orthostatic hypotension, impotence, failure to ejaculate ( ALPHA ADRENORECEPTOR BLOCKADE)
  • 23. ADVERSE EFFECTS IV. METABOLIC & ENDOCRINE EFFECTS Weight gain, hyperglycemia, hyper - prolactenemia, amenorrhea-galactorrhea syndrome, infertility, impotence in males V. TOXIC OR ALLERGIC REACTIONS Agranulocytosis (clozapine) , cholestatic jaundice, skin eruptions VI. CARDIAC TOXICITY Ventricular arrythmias (thioridazine) VII. OCULAR COMPLICATIONS: “ browning of vision”
  • 24. ANTIMANIC AGENTS • MOOD STABILIZING AGENT • BIPOLAR DISORDERS (MANIC- DEPRESSIVE) • DISORDER WITH PREPONDERANCE OF CATHECHOLAMINE RELATED ACTIVITY • LITHIUM CARBONATE • CARBAMAZEPINE, VALPROIC ACID
  • 25. LITHIUM P’KINETICS ABSORPTION : virtually complete within 6 -8 hrs; peak plasma levels in 30 min to 2 hrs DISTRIBUTION: in total body water; slow entry into intracellular compartment. No protein binding METABOLISM: None EXCRETION: virtually entirely in urine; plasma half life is about 20 hours
  • 26. LITHIUM ‘ DYNAMICS • EFFECTS ON ELECTROLYTES & IONS TRANSPORT: Substitute for sodium • EFFECTS ON NEUROTRANSMITTER  enhance effects of serotonin? Decrease norepinephrine & dopamine turnover Block dopamine receptor supersensitivity Augment synthesis of acetylcholine?
  • 27. LITHIUM PHARMACODYNAMICS • EFFECTS ON SECOND MESSENGER effect on IP3/ DAG EFFECTS ON PHOSPHOINOSITOL TURNOVER…..> EARLY RELATIVE REDUCTION OF MYOINOSITOL IN HUMAN BRAIN
  • 28. LITHIUM ADVERSE EFFECTS 1. CNS EFFECTS; dizziness, mild ataxia 2. NEUROMUSCULAR EFECTS: fine tremors 3. CV EFFECTS: ventricular arrythmias 4. GIT EFFECTS: nausea, vomiting, diarrhea 5. GUT EFFECTS: polyuria 6. ENDOCRINE EFFECTS: hypothyroidism 7. ALLERGIC REACTION: pruritus, rash 8. OVERDOSE TOXICITY: vomiting, drowsiness, decrease consciousness seizures Rx: dialysis
  • 29. LITHIUM CONTRAINDICATION A. MARKED DEHYDRATION OR SODIUM DEPLETION B.SIGNIFICANT RENAL OR CARDIAC DISEASES C. PREGNANCY(W) D. RENAL CONCENTRATION ABILITY(W) • Nephrogenic diabetes insipidus with polyuria
  • 30. DRUG INTERACTIONS A. THIAZIDE DIURETICS: ↓ RENAL CLEARANCE OF LITHIUM B. NSAID: ↓ LITHIUM CLEARANCE C. ANTIPYSCHOTIC AGENTS: ↑ NEUROTOXICITY
  • 31. DEPRESSION I.REACTIVE OR SECONDARY DEPRESSION Core Depression Syndrome: depression, anxiety, tension, bodily complaints, guilt (> 60%) II.ENDOGENOUS DEPRESSION Core Depression Syndrome plus ABNORMAL VS rhythm of sleep, motor activity, livido, decrease appetite ( 25%) III. DEPRESSION ASSOCIATED WITH BIPOLAR AFFECTIVE DISORDER (10-15%)
  • 32. ANTIDEPRESSANTS I.TRICYCLIC ANTIDEPRESSANTS IMIPRAMINE. AMITRYPTYLINE, DOXAPIN, NORTRIPTYLLINE ,DESIPRAMINE. CLOMIPRAMINE , PROTIPTYLINE, TRIMIPRAMINE B. HETEROCYCLIC, SECOND & THIRD DEGENERATIONS 1. SECOND GENERATIONS AMOXAPINE, MAPROTILINE TRAZODON, BUPROPION 2. THIRD GENERATIONS MIRTAZAPINE, VENLAFAZINE NEFAXODONE
  • 33. ANTIDEPRESSANTS C. SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI) • FLUOXETINE FLUVOXAMINE • PAROXETINE ESCITALOPRAM • SERTRALINE CITALOPRAM D. MONOAMINE OXIDASE INHIBITORS (MAOI) • PHENELZINE, TRANYLCYPROMINE • MOCLOBEMIDE
  • 34. ANTIDEPRESSANTS PHARMADYNAMICS A. ACTION OF ANTIDEPRESSANTS ON BIOGENIC AMINE NEUROTRANSMITTERS  TRICYCLICS: BLOCK AMINE REUPTAKE PUMPS  MAOI: BLOCK DEGRADATIVE PATHWAY FOR THE AMINE NEUROTRANSMITTERS  TRAZODON, NEFAZODONE & MIRTAZAPINE: SERETONIN RECEPTORS ANTAGONIST
  • 35. B.RECEPTOR & POSTRECEPTOR EFFECTS • SSRI: ↓ in norepinephrine cAMP & in beta -adrenoreceptor binding • MAOI: mixed action with norepinephrine & serotonin • ↑ serotonergic transmission mediated through diverse mechanisms
  • 36. Drug Sedati Muscar NE 5HT reuptake ve inicrBl reuptake block ock Block Amitryptyline +++ +++ ++ +++ Imipramine ++ + + ++ Amoxapine ++ + ++ + Bupropion - - - - Trazodone +++ - - ++ Mirtazepine +++ - - - Venlafaxine - - +++ ++ Fluoxetine - + - +++
  • 37. PHARMACOKINETICS • A. TRICYCLICS Incompletely reabsorbed First pass metabolism Large Vd Metabolized HETEROCYCLICS Variable bioavailabilitiy High protein binding Variable and large Vd Active metabolites
  • 38. PHARMACOKINETICS • SSRI : FLUOXETINE • Well absorbed • PPC: 4 – 8 hrs • Inhibits drug metabolizing enzymes • MAOI • Readily absorbed
  • 39. CLINICAL INDICATIONS A. DEPRESSION B. PANIC DISORDER C. OBSESSIVE COMPULISVE D. ENURESIS E. CHRONIC PAIN F. OTHERS: Eating Disorder(Bulemia) Cataplexy asstd with Narcolepsy, School Phobia, Attention Deficit Syndrome
  • 40. ADVERSE EFFECTS • TRICYCLICS Sedation: Sleepiness Synpathomimetic; tremors, insomnia Antimuscarinic; blurred vision. constipation confusion, urinary incontinence
  • 41. TRICYCLICS Psychiatric: psychoses aggravated CVS: orthostatic hypotension Neurologic: Seizures Metabolic-Endocrine: weight gain, sexual disturbance
  • 42. ADVERSE EFFECTS MAO INHIBITORS headache, drowsiness, dry mouth, weight gain, postural hypotension, sexual distn AMOXAPIN  Tricyclic & antipsychotic effects MAPROTILINE Tricyclic Effects
  • 43. ADVERSE EFFECTS TRAZODONE & NEFAZODONE: drowsiness, dizziness, insomnia, nausea, agitation BUPROPION dizziness, dry mouth, tremor FLUOXETINE Anxiety, insomnia, tremors, decr libido, GIT effects
  • 44. Foods that interact with MAOI • High in tyramine content: BEER. BROAD BEANS, LAVA BEANS CHEESE. CHICKEN LIVER  SAUSAGES  SNAILS WINE, RED WINE YEAST
  • 45. Drugs that Interact with MAOI A.INDIRECTLY ACTING SYMPATHOMIMETICS: amphetamines, ephedrine, metaraminol, phenylpropanolamine B. OTHER ADRENORECEPTOR AGENTS & RELATED AGENTS: levodopa, methyldopa, guanethidine, reserpine C. OPIOID ANALGESICS & DERIVATIVES: morphine, codeine, meperidine, dextromethorpham D.MISCELLANEOUS DRUGS: buspirone, fluoxetine, LSD