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).
Effective/mood disorders (depression)
Personality disorders (Schizophrenia)

Drugs acting on the CNS 1

Anxiolytic Drugs:

Antidepressant Drugs:

Benzodiazepines(BDZ)
Barbiturate.
Buspirone

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:

Fate:

Short, intermediate and long acting.

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:

Drug hangover

Tiredness, nausea and dizziness

Addiction:

Drowsiness, impaired concentration and mental sluggishness

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

Butyrophenones

Fluphenazine
Promethazine

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:

Extrapyramidal effects:

By blocking dopaminergic receptors.

Antimuscarinic effects:

Parkinson syndrome by blocking the dopamine receptors in the

nigrostriatal pathway.

Antiemetic effects:

Reduce hallucinations by blocking dopamine receptors.

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