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    7.3. Obat Stimulan

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    Laras Oktaviani
    1. Xanthine derivatives like caffeine, theophylline, and theobromine are CNS stimulants that are used as bronchodilators, diuretics, and stimulants. They work by inhibiting phosphodiesterase and calcium reuptake. 2. Caffeine specifically can improve alertness and mental performance at low doses but cause anxiety, insomnia, tremors and seizures at high doses. Theophylline is used to treat asthma but can be toxic, sometimes causing seizures. 3. These derivatives are well absorbed orally, distributed throughout the body, and metabolized in the liver. Their effects include stimulating the CNS and heart, relaxing smooth muscles like the bronch

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    7.3. Obat Stimulan

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    Laras Oktaviani
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    1. Xanthine derivatives like caffeine, theophylline, and theobromine are CNS stimulants that are used as bronchodilators, diuretics, and stimulants. They work by inhibiting phosphodiesterase and calcium reuptake. 2. Caffeine specifically can improve alertness and mental performance at low doses but cause anxiety, insomnia, tremors and seizures at high doses. Theophylline is used to treat asthma but can be toxic, sometimes causing seizures. 3. These derivatives are well absorbed orally, distributed throughout the body, and metabolized in the liver. Their effects include stimulating the CNS and heart, relaxing smooth muscles like the bronch

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    1. Xanthine derivatives like caffeine, theophylline, and theobromine are CNS stimulants that are used as bronchodilators, diuretics, and stimulants. They work by inhibiting phosphodiesterase and calcium reuptake. 2. Caffeine specifically can improve alertness and mental performance at low doses but cause anxiety, insomnia, tremors and seizures at high doses. Theophylline is used to treat asthma but can be toxic, sometimes causing seizures. 3. These derivatives are well absorbed orally, distributed throughout the body, and metabolized in the liver. Their effects include stimulating the CNS and heart, relaxing smooth muscles like the bronch

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    123 views16 pages

    7.3. Obat Stimulan

    Uploaded by

    Laras Oktaviani
    1. Xanthine derivatives like caffeine, theophylline, and theobromine are CNS stimulants that are used as bronchodilators, diuretics, and stimulants. They work by inhibiting phosphodiesterase and calcium reuptake. 2. Caffeine specifically can improve alertness and mental performance at low doses but cause anxiety, insomnia, tremors and seizures at high doses. Theophylline is used to treat asthma but can be toxic, sometimes causing seizures. 3. These derivatives are well absorbed orally, distributed throughout the body, and metabolized in the liver. Their effects include stimulating the CNS and heart, relaxing smooth muscles like the bronch

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    of 16

    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

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