Obat-obat sistem Syaraf

Pusat
 Obat-obat sistem Syaraf
PusatPsikis diklasifikasikan menjadi 3 major
Gangguan
groups:
Anxiety disorders (phobia and sleeping
disorders).
Effective/mood disorders (depression)
Personality disorders (Schizophrenia)
/gangguan persepsi diri
 Obat-obat sistem Syaraf
PusatDrugs:
Anxiolytic
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:
Keadaan yang tidak nyaman atau rasa takut yang
meningkat akibat sesuatu yang tidak jelas (kecemasan)
Symptoms:
Tachycardia(denyut jantung berlebih)
Sweating (berkeringat)
Palpitations (jantung berdebar)
Sympathetic activation (aktivasi sistem sympatik)
 Anxiolytic Drugs
(Benzodiazapine)
Diazepam,Lurazepam, Midazolam
Mode of action:
Binding of GABA (gama aminobutirat acid ) to its
receptor trigger an opening of chloride conductance.
The influx of chloride ions causes hyperpolarization,
terjadi peningkatan re up take dari neurotrasnmiter di
otak (seperti:Ne, E, dan serotonin)
Actions:
Reduction of anxiety( at low doses)
Sedative and hypotonic actions (at higher doses)
Anticonvulsant
Muscle relaxant
 Benzodiazapine
Therapeutic uses:
Anxiety disorders (gangguan cemas)
Muscular disorders
Seizures (kebingungan)
Sleep disorders (gangguan tidur)
Pharmacokinetics:
Absorption and distribution:
Lipophilic (suka lemak/larut dalam lemak)
Rapidly absorbed (cepat diabsorpsi)
 Benzodiazapine
Pharmacokinetics:
Duration of action:
Short, intermediate and long acting.
Metabolisme
Metabolized by the hepatic microsomal metabolism system.
Dependence: (ketergantungan)
At high doses
Results in withdrawal symptoms: (menimbulkan
withdrawal syndrome), yaitu gangguan akibat
penurunan dosis tiba-tiba
Confusion(bingung), anxiety(cemas), restlessness(lelah)
and tension (TD yang tinggi).
 Benzodiazapine
Adverse effects:
Drowsiness (mengantuk) and confusion (bingung).
PrecautionsPerhatian)
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: (efek samping)
CNS:
Drowsiness
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. (berguna untuk mengobati kecemasan
umum)
Action:
The action is mediated by serotonin receptors.
Adverse effects:
Dizziness (bingung)
Nervousness (gugup)
Ligthheadness (kunang-kunang)
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
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