Drugs Acting on the CNS 1

8/7/2019 Drugs Acting on the CNS 1

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Obat-obat sistem Syaraf Pusat



Gangguan Psikis diklasifikasikan menjadi 3 majorgroups:

Anxiety disorders (phobia and sleepingdisorders).

Effective/mood disorders (depression)

Personality disorders (Schizophrenia)

/gangguan persepsi diri




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:

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)



Diazepam,Lurazepam, Midazolam

Mode of action:

PengikatanG

ABA pada reseptor yang memicu pembukaankonduktansi klorida. Masuknya ion klorida menyebabkanhyperpolarization yang bergerak pasca sinaptik potensi jauhdari ambang menembak dan dengan demikian menghambat pembentukan aksi pembakaran potensial dan saraf

Actions: Reduction of anxiety( pada dosis rendah ) Sedative and hypotonic actions (at higher doses)

Anticonvulsant

Muscle relaxant

Anxiolytic Drugs

(Benzodiazapine)



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:

Dimetabolisme oleh sistem metabolisme hepatik mikrosoma.

Ketergantungan:

At high doses

Results in withdrawal symptoms: Kebingungan, kecemasan, kegelisahan dan ketegangan



Benzodiazapine Efek samping :

Mengantuk dan kebingungan.

Precautions: Hati-hati dalam mengobati pasien dengan penyakit hati



Phenobarbiturate, amobarbiturate

Mekanisme kerja:

Mengganggu transportasi natrium dan kalium di selmembran

Actions: Depresi SSP (pada dosis rendah

Hipnosis dan anestesi (dalam dosis tinggi)

Pernapasan depresi.

Induksi enzim (P-450 enzim mikrosoma dalam hati)

(Barbiturate)



Barbiturate Therapeutic uses: Anestesi

Antikonvulsi Kegelisahan

Pharmacokinetics: Metabolized by the liver

Distributed to:

Splanchnic area

Skeletal muscles

Adipose tissue



Barbiturate Adverse effects:

CNS:

Mengantuk, gangguan konsentrasi dan mental kelesuanDrug hangover

Lelah, mual dan pusing

Addiction:

Tremor, anxiety, tiredness, restlessness, nausea and vomiting

Poisoning: death



Buspirone Berguna dalam pengobatan gangguan kecemasan

umum

Action: Tindakan dimediasi oleh reseptor serotonin

Adverse effects: Pusing

Gugup

Ligthheadness

Tindakan dimediasi oleh reseptor serotonin



Depression and Antidepressant

drugs: depression:

Definition:

Pervasif mengubah mood penyakit yang mempengaruhi energi,tidur, nafsu makan dan kemampuan untuk fungsi.

Symptoms:

Depresi

Kesedihan

Keputusasan

Ketidakmampuan untuk mengalami kenikmatan di aktivitasyang biasa



Amitriptyline, Imipramine

Mode of action:

Menghambat Reuptake saraf norepinefrin dan serotonin ke terminalsaraf, yang mengarah ke presynaptic peningkatan konsentrasimonoamina dalam kunci sinapsis.

Blokir serotonergik, a-adrenergik, dan reseptor histamin muscurinic. Actions:

Meningkatkan suasana hati

Meningkatkan kewaspadaan mental

Meningkatkan aktifitas fisik

Antidepressant Drugs

(Tricyclic/Polycyclic)



Tricyclic/Polycyclic Therapeutic uses: Depresi

Panic disorder Bed-wetting pada anak-anak

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.



Hydralazine, phenelzine

Mode of action:

Reverrsibly or irreversibly inactivate the enzyme, this result in increased norepinephrine, serotonin and dopamine with inthe neuron.

(monoamine oxidase inhibitors)



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 storedcatecholamines from verve terminals resulting in:

Headache

Tachycardia

Nausea

hypertension



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



Personality disorders and antipsycotic

(neuroleptic) Drugs:

schizophrenia

Definition:

Mental disorder caused by some inherited dysfunction of thebrain.

Symptoms:

Delusions

Hallucination

Thinking or speech disturbance



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 andhistamine receptors

(neuroleptic drugs)



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

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Drugs Acting on the CNS 1