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 Relaksasi Diuresis Stimulasi Stimulasi Dilatasi

an otot Polos Jantung otot Skelet koroner
SSP (Bronkus)
Kafein 1 3 3 3 1 3
Teofilin 2 1 1 1 2 1
Teobromin 3 2 2 2 3 2

Kekuatan: 1>2>3
SSP stimulasi
Ginjal Diuresis
Jantung stimulasi
Otot polos relaksasi
Xanthine Mechanisms of action
inhibit cellular calcium reuptake, which increases 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, distributed to all body
tissues , crosses placenta barrier and BBB
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 ( - )
- berpikir: lbh terang, cepat & jernih
- lelah
- panca indrafgs 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 & O2

- 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
Caffeine
Acute Toxicity
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.
 Use of Caffeine in Pregnancy

> 300 mg/day increased risk of spontaneous abortion

> 600 mg/day increased risk of spontaneous abortion
no/little evidence of teratogenic effects
caffeine passes into nursing infant in breast milk --- increased irritability,
insomnia, colic in infant
 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. Campuran analgetik/antipiretik nyaman
2. Migren
3. 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