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Unit 8 Week 5 Dr.Mohammed Hassan. Drugs acting on the CNSI. Al-Hamadi , Drugs acting on the CNSI . 4medstudents.com 2003. Drugs acting on the CNS 1 . The psychotic disorders are classified into 3 major groups: Anxiety disorders (phobia and sleeping disorders).

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drugs acting on the cnsi

Unit 8

Week 5

Dr.Mohammed Hassan

Drugs acting on the CNSI

Al-Hamadi , Drugs acting on the CNSI. 4medstudents.com 2003

drugs acting on the cns 1
Drugs acting on the CNS 1
  • The psychotic disorders are classified into 3 major groups:
      • Anxiety disorders (phobia and sleeping disorders).
      • Effective/mood disorders (depression)
      • Personality disorders (Schizophrenia)
slide3

Drugs acting on the CNS 1

  • Anxiolytic Drugs:
      • Benzodiazepines(BDZ)
      • Barbiturate.
      • Buspirone
  • Antidepressant Drugs:
    • Tricyclic/Plycyclic
    • Monoamine oxidase inhibitors
    • Selective serotonin-reuptake inhibitors (SSRI)
  • Neurolytic Drugs:
    • Phenothiazin
    • Buteopheanol
anxiety and anxiolytic drugs
Anxiety and Anxiolytic Drugs:
  • Anxiety:
    • Definition:
      • Unpleasant state of tension or a fear that seems to arise from an unknown source.
    • Symptoms:
      • Tachycardia
      • Sweating
      • Palpitations
      • Sympathetic activation
anxiolytic drugs benzodiazapine
Anxiolytic Drugs(Benzodiazapine)
  • Diazepam,Lurazepam, Midazolam
  • Mode of action:
    • Binding of GABA to its receptor trigger an opening of chloride conductance. The influx of chloride ions causes hyperpolarization that moves the post synaptic potential away from its firing threshold and thus inhibits the formation of action potential and neural firing>
  • Actions:
    • Reduction of anxiety( at low doses)
    • Sedative and hypotonic actions (at higher doses)
    • Anticonvulsant
    • Muscle relaxant
benzodiazapine
Benzodiazapine
  • Therapeutic uses:
    • Anxiety disorders
    • (Muscular disorders
    • Seizures
    • Sleep disorders
  • Pharmacokinetics:
    • Absorption and distribution:
      • Lipophilic
      • Rapidly absorbed
benzodiazapine1
Benzodiazapine
  • Pharmacokinetics:
    • Duration of action:
      • Short, intermediate and long acting.
    • Fate:
      • Metabolized by the hepatic microsomal metabolism system.
  • Dependence:
    • At high doses
    • Results in withdrawal symptoms:
      • Confusion, anxiety, restlessness and tension.
benzodiazapine2
Benzodiazapine
  • Adverse effects:
    • Drowsiness and confusion.
  • Precautions:
    • Cautiously in treating patients with liver disease.

Goodbye BDZ

welcome barbiturate
Welcome (Barbiturate)
  • Phenobarbiturate, amobarbiturate
  • Mode of action:
    • Interfere with sodium and potassium transport across cell membranes.
  • Actions:
    • Depression of CNS (at low doses)
    • Hypnosis and anesthesia ( at high doses)
    • Respiratory depression.
    • Enzyme induction (P-450 microsomal enzyme in liver)
barbiturate
Barbiturate
  • Therapeutic uses:
    • Anesthesia
    • Anticonvulsant
    • Anxiety
  • Pharmacokinetics:
    • Metabolized by the liver
    • Distributed to:
      • Splanchnic area
      • Skeletal muscles
      • Adipose tissue
barbiturate1
Barbiturate
  • Adverse effects:
    • CNS:
      • Drowsiness, impaired concentration and mental sluggishness
    • Drug hangover
      • Tiredness, nausea and dizziness
    • Addiction:
      • Tremor, anxiety, tiredness, restlessness, nausea and vomiting
    • Poisoning:
      • death

Goodbye Barbiturate

welcome buspirone
WelcomeBuspirone
  • Useful in the treatment of generalized anxiety disorders.
  • Action:
    • The action is mediated by serotonin receptors.
  • Adverse effects:
    • Dizziness
    • Nervousness
    • ligthheadness
    • The action is mediated by serotonin receptors

Goodbye all Anxiolytic Drugs

depression and antidepressant drugs
Depression and Antidepressant drugs:
  • depression:
    • Definition:
      • Pervasive mood altering illness affecting energy, sleep, appetite and the ability to function.
    • Symptoms:
      • Depression
      • Sadness
      • Hopelessness
      • Inability to experience pleasure in usual activity
antidepressant drugs tricyclic polycyclic
Antidepressant Drugs(Tricyclic/Polycyclic)
  • Amitriptyline, Imipramine
  • Mode of action:
    • Inhibit the neuronal reuptake of norepinephrine and serotonin into presynaptic nerve terminals which leads to increased concentration of monoamine in the synaptic clef.
    • Blocking serotonergic,a-adrenergic, histamine and muscurinic receptors.
  • Actions:
    • Elevate moods
    • Improve mental alertness
    • Increase physical activity
tricyclic polycyclic
Tricyclic/Polycyclic
  • Therapeutic uses:
    • Depression
    • Panic disorder
    • Bed-wetting in children
  • Pharmacokinetics:
    • Absorption and distribution:
      • Lipophilic
      • Low bioavailability
      • Metabolized by hepatic microsomal system
tricyclic polycyclic antidepressant
Tricyclic/Polycyclic antidepressant
  • Adverse effects:
    • Anti muscarinic effects:
      • Blurred vision, dry mouth, urinary retention and constipation
    • Increase cardiovascular stimulation
    • Sedation
    • Orthostatic hypotension:
      • By blocking a-adrenergic receptors.

Goodbye tricyclic/polycyclic

welcome monoamine oxidase inhibitors
Welcome (monoamine oxidase inhibitors)
  • Hydralazine, phenelzine
  • Mode of action:
    • Reverrsibly or irreversibly inactivate the enzyme, this result in increased norepinephrine, serotonin and dopamine with in the neuron.
monoamine oxidase inhibitors
monoamine oxidase inhibitors
  • Therapeutic uses:
    • Depression
    • Phobic states
  • Pharmacokinetics:
    • Effect require 2 to 4 weeks
monoamine oxidase inhibitors1
monoamine oxidase inhibitors
  • Adverse effects:
    • Inability to degraded tyramine obtained from the gut
      • Cheese
      • Chicken liver

Tyramine causes the release of large amounts of stored catecholamines from verve terminals resulting in:

      • Headache
      • Tachycardia
      • Nausea
      • hypertension

Goodbye MAO Inhibitors

welcome selective serotonin reuptake inhibitors
Welcome (Selective Serotonin-Reuptake Inhibitors)
  • Fluoxetine
  • Actions:
    • Inhibit serotonin reuptake ( selective for serotonin)
  • Therapeutic uses:
    • Depression
    • Panic disorders
    • Pre menstrual syndrome
selective serotonin reuptake inhibitors
Selective Serotonin-Reuptake Inhibitors
  • Pharmacokinetics:
    • Slowly cleared from the body
    • Potent inhibitor of a hepatic cytochrome P-450.
  • Adverse effects:
    • Nausea
    • Anxiety
    • Insomnia
    • Sexual dysfunction
    • Weight loss
    • tremors

Goodbye SSRI

personality disorders and antipsycotic neuroleptic drugs
Personality disorders and antipsycotic (neuroleptic) Drugs:
  • schizophrenia
    • Definition:
      • Mental disorder caused by some inherited dysfunction of the brain.
    • Symptoms:
      • Delusions
      • Hallucination
      • Thinking or speech disturbance
neuroleptic drugs
(neuroleptic drugs)
  • Five important classes. Most important classes are:
    • Phenothiazines
      • Fluphenazine
      • Promethazine
    • Butyrophenones
      • Haloperidol
      • Doroperidol
  • Mode of action:
    • Block dopamine and serotonin receptor in the brain
    • Many of these drugs also block cholinergic, adrenergic and histamine receptors
neuroleptic drugs1
neuroleptic drugs
  • Actions:
    • Antipsychotic actions:
      • Reduce hallucinations by blocking dopamine receptors.
    • Extrapyramidal effects:
      • Parkinson syndrome by blocking the dopamine receptors in the nigrostriatal pathway.
    • Antiemetic effects:
      • By blocking dopaminergic receptors.
    • Antimuscarinic effects:
      • Blurred vision, dry mouth, sedation and confusion.
    • Other effects:
      • Hypotension and lightheadedness by blocking a-adrenergic receptors
neuroleptic drugs2
neuroleptic drugs
  • Therapeutic uses:
    • Schizophrenia
    • Prevention of severe nausea
    • Treatment of severe pain
  • Adverse effects:
    • Tremors
    • Postural hypotension
    • Constipation
    • Urinary retention
    • Confusion
    • Sexual dysfunction

Goodbye Neuroleptic Drugs