OBAT PERANGSANG SSP

( CNS STIMULANTS DRUGS)

Dharma Permana, Apt, PhD

OBAT PERANGSANG SSP

= ANALEPTIK
- dulu : stimulan SSP utk depresi

* E.S >> ( batas keamanan sempit )

Tidak dipakai lagi
perawatan memberikan hasil yg lebih baik

- Obat a.l.

- pikrotoksin
- striknin
- metrazol
- etamiven
- metilfenidat
- Derivat Xantin.. Masih dipakai
- dll

Derivat Xantin
3 golongan:
- Kafein (1,3,7-trimetil xantin )
- Teofilin ( 1,3-dimetil xantin )
- Teobromin (3,7-dimetil xantin )

Sumber:
-Sintetis industri farmasi ( obat & minuman )
- Alami
Kopi Kafein
Teh mengandung kafein, teofilin&
teobromin ( kafein >> )
Coklat teobromin dan kafein

Farmakologi gol Xantin

Xantin

Stimul
an
SSP

Relaksasi
otot Polos
(Bronkus)

Diuresis

Stimulasi
Jantung

Stimulasi
otot Skelet

Dilatasi
koroner

Kafein

Teofilin

Teobromin

Kekuatan: 1>2>3
SSP stimulasi
Ginjal Diuresis
Jantung stimulasi
Otot polos relaksasi

Xanthine Mechanisms of
inhibit cellular calcium reuptake, which increases
action
the free calcium concentration and enhances
cardiac and skeletal muscle contractility
competing for benzodiazepine receptors within
the central nervous system
inhibiting phosphodiesterase, resulting in
increased intracellularcyclic adenosine
monophosphate (cAMP)
Adenosine receptor antagonists, which inhibit
sleepiness-inducing adenosine also leads to
vasoconstriction.
induce acid and pepsin secretions in the GI tract

Pharmacokinetics of Xanthine
Xanthine derivatives are well absorbed orally,
reaching peak distribution within two hours
T1/2 : -Teofilin dws 8-9 jam, anak2 3 jam
- Kafein 3 jam

The compounds are metabolized by the liver (the

cytochrome P-450 enzyme system).
Excreted mostly in urine ( 10% unchanged ),
small amounts excreted in feces, sweat, breast milk
However, in neonates approximately 85 % of a
dose is excreted unchanged in the urine.
Decreased elimination and a prolonged half-life
may increase caffeine toxicity in neonates and
premature infants

1. SSP
Kafein: - ngantuk ( - )
jernih

- berpikir: lbh terang, cepat &

- lelah
- panca indra fgs baik

Hasil kerja efisien ( 1-2 gelas kopi )

Dosis >> : gelisah, gugup, insomnia, tremor,
Dosis>>>: konvulsi ( terutama teofilin )

2. Kardiovaskular
* Jantung freq , kontr
takikardi aritmia
Teofilin : pernah dipakai utk terapi darurat
payah jantung tetapi Toksis
* Pembuluh darah kafein & teofilin
dilatasi - pembuluh darah koroner & pulmonal
- perifer ( tdk stabil)

Sirkulasi Otak : - peningkatan aliran darah & O 2

- vasokontriksi ( vascular cerebral )
Kafein utk migren ( Cafergot )

3. Otot Polos
Relaksasi Otot Polos Bronkus (utk Asma Bronkial)
Teofilin > Teobromin > Kafein
4. Otot Rangka
Kapasitas otot olah raga ( Kafein )
5. Diuresis
meninggikan produksi urin ( terutm teofilin )
6. Sekresi asam lambung
Kafein meningkatkan sekresi as lambung

Intoksikasi
Kafein
- kejang, insomnia, takikardia
Jarang tjd keracunan

Teofilin ; sering
- IV cepat
gjl: kejang terapi dgn diazepam

Xanthine intoxication
Acute Toxicity

Caffeine

In adults, ingestion of 5001000 mg of caffeine may result in

nausea, vomiting, diarrhea, tremors, and agitation. Most
patients have sinus tachycardia and a mild hypertension. The
estimated lethal dose of caffeine in an untreated adult is 510 g

Treatment:
Treatment in all cases is supportive with attention to airway,
breathing, and circulation. Oral activated charcoal, 12 g/kg of
body weight is the primary mode of gastrointestinal
decontamination. Caffeine may produce hypokalemia so
Potassium and other electrolytes should be monitored and
replaced as needed. An antiemetic such as metoclopromide or
ondansetron may be considered if protracted vomiting occurs.
Benzodiazepines such as diazepam and lorazepam should be
given to patients who are agitated, hypertensive, or
tachycardic.

Preparat
Teofilin Asma Bronkial
-tab 125-500 mg
- tab sustaine release
- suppositoriarektum
Aminophylin (garam teofilin) IV
administration
Kafein -campuran obat Flu ( 50 mg )
- minuman energi (50 mg)

Indikasi
Kafein
1.
2.
3.

Campuran analgetik/antipiretik nyaman

Migren
Meng (-) lelah

*Teofilin
- Asma bronkial
- Apnea pada bayi prematur

Xantin pada Minuman

1 gelas Kopi 85 mg kafein
1 gelas Teh 50 mg kafein
1 gelas coklat 250 mg teobromin &
5 mg kafein
* 1 kaleng Coca cola 50 mg kafein

References

- Pharmacology And Pharmacotherapeutics (New

Revised 21 St Ed. 2009)
By R. S. Satoskar, S. D. Bhandarkar &nirmala N. Rege
-Modern Pharmacology with Clinical Applications, 6th ed,
2003
By Charles R. Craig, Robert E. Stitzel
-Farmakologi dan Terapi, ed IV, 2007

Thank you