Unit 4

Week 5
Siti Ma’rufah

Drugs acting on the CNSI

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)

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:
 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)
 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
 Therapeutic uses:
 Anxiety disorders
 (Muscular disorders
 Seizures
 Sleep disorders
 Pharmacokinetics:
 Absorption and distribution:
 Lipophilic
 Rapidly absorbed
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.
Benzodiazapine
 Adverse effects:
 Drowsiness and confusion.
 Precautions:
 Cautiously in treating patients with liver disease.
 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
 Therapeutic uses:
 Anesthesia
 Anticonvulsant
 Anxiety
 Pharmacokinetics:
 Metabolized by the liver
 Distributed to:
 Splanchnic area
 Skeletal muscles
 Adipose tissue
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
 Welcome
Buspirone
 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
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)
 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
 Therapeutic uses:
 Depression
 Panic disorder
 Bed-wetting in children
 Pharmacokinetics:
 Absorption and distribution:
 Lipophilic
 Low bioavailability
 Metabolized by hepatic microsomal system
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.
 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
 Therapeutic uses:
 Depression
 Phobic states
 Pharmacokinetics:
 Effect require 2 to 4 weeks
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
 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

 Pharmacokinetics:
 Slowly cleared from the body
 Potent inhibitor of a hepatic cytochrome P-450.
 Adverse effects:
 Nausea
 Anxiety
 Insomnia
 Sexual dysfunction
 Weight loss
 tremors
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)
 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 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 drugs
 Therapeutic uses:
 Schizophrenia
 Prevention of severe nausea
 Treatment of severe pain
 Adverse effects:
 Tremors
 Postural hypotension
 Constipation
 Urinary retention
 Confusion
 Sexual dysfunction
Thank You Team