Peringatan Keamanan

The oral LD50 of caffeine in rats is 192 mg/kg.MSDS An acute fatal overdose of caffeine in humans is about 10–14 grams (equivalent to 150–200 mg/kg of body weight).T722

Caffeine overdose

In the case of caffeine overdose, seizures may occur, as caffeine is a central nervous system stimulant. It should be used with extreme caution in those with epilepsy or other seizure disorders.L9851 Symptoms of overdose may include nausea, vomiting, diarrhea, and gastrointestinal upset. Intoxication with caffeine is included in the World Health Organization’s International Classification of Diseases (ICD-10). Agitation, anxiety, restlessness, insomnia, tachycardia, tremors, tachycardia, psychomotor agitation, and, in some cases, death can occur, depending on the amount of caffeine consumed. Overdose is more likely to occur in individuals who do not consume caffeine regularly but consume energy drinks.A187721

Overdose management

For a mild caffeine overdose, offer symptomatic treatment. In the case of a severe overdose, intubation for airway protection from changes in mental status or vomiting may be needed. Activated charcoal and hemodialysis can prevent further complications of an overdose and prevent absorption and metabolism. Benzodiazepine drugs can be administered to prevent or treat seizures. IV fluids and vasopressors may be necessary to combat hypotension associated with caffeine overdose. In addition, magnesium and beta blocking drugs can be used to treat arrhythmias that may occur, with defibrillation and resuscitation if the arrhythmias are lethal. Follow local ACLS protocols.T716

Caffeine

DB00201

small molecule approved

Deskripsi

Caffeine is a drug of the methylxanthine class used for a variety of purposes, including certain respiratory conditions of the premature newborn, pain relief, and to combat drowsiness. Caffeine is similar in chemical structure to Theophylline and Theobromine.A187691,L9851 It can be sourced from coffee beans, but also occurs naturally in various teas and cacao beans, which are different than coffee beans.T716 Caffeine is also used in a variety of cosmetic products and can be administered topically, orally, by inhalation, or by injection.T716

The caffeine citrate injection, used for apnea of the premature newborn, was initially approved by the FDA in 1999.L9863 According to an article from 2017, more than 15 million babies are born prematurely worldwide. This correlates to about 1 in 10 births. Premature birth can lead to apnea and bronchopulmonary dysplasia, a condition that interferes with lung development and may eventually cause asthma or early onset emphysema in those born prematurely.A187694 Caffeine is beneficial in preventing and treating apnea and bronchopulmonary dysplasia in newborns, improving the quality of life of premature infants.T716

Struktur Molekul 2D

Berat 194.1906
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) In an average-sized adult or child above the age of 9, the half-life of caffeine is approximately 5 hours. Various characteristics and conditions can alter caffeine half-life. It can be reduced by up to 50% in smokers. Pregnant women show an increased half-life of 15 hours or higher, especially in the third trimester. The half-life in newborns is prolonged to about 8 hours at full-term and 100 hours in premature infants, likely due to reduced ability to metabolize it. Liver disease or drugs that inhibit CYP1A2 can increase caffeine half-life.[T716,T722]
Volume Distribusi Caffeine has the ability to rapidly cross the blood-brain barrier. It is water and fat soluble and distributes throughout the body.[T716,T722,L9851] Caffeine concentrations in the cerebrospinal fluid of preterm newborns are similar to the concentrations found in the plasma. The mean volume of distribution of caffeine in infants is 0.8-0.9 L/kg and 0.6 L/kg in the adult population.[L9851]
Klirens (Clearance) The clearance of caffeine varies, but on average, is about 0.078?L/kg/h (1.3?mL/min/kg).[A187730,T722]

Absorpsi

Caffeine is rapidly absorbed after oral or parenteral administration, reaching peak plasma concentration within 30 minutes to 2 hours after administration.A187730 After oral administration, onset of action takes place within 45 to 1 hour.L9827 Food may delay caffeine absorption. The peak plasma level for caffeine ranges from 6-10mg/L.L9851 The absolute bioavailability is unavailable in neonatesL9851, but reaches about 100% in adults.T716

Metabolisme

Caffeine metabolism occurs mainly in the liver via the cytochrome CYP1A2 enzyme.A187730 The products of caffeine metabolism include paraxanthine, theobromine, and theophylline. The first step of caffeine metabolism is demethylation, yielding paraxanthine (a major metabolite), followed by theobromine, and theophylline, which are both minor metabolites. They are then excreted in urine as urates after additional metabolism.A187730,T716,L9851 The enzymes xanthine oxidase and N-acetyltransferase 2 (NAT2) also participate in the metabolism of caffeine.A187730

Rute Eliminasi

The major metabolites of caffeine can be found excreted in the urine.T716 About 0.5% to 2% of a caffeine dose is found excreted in urine, as it because it is heavily absorbed in the renal tubules.T722,A187730

Farmakogenomik

1 Varian
CYP1A2 (rs762551)

Patients with this genotype have increased risk of a non-fatal myocardial infarction with caffeine

Interaksi Obat

674 Data
Deferasirox The serum concentration of Caffeine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Caffeine can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Caffeine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Caffeine can be decreased when it is combined with Teriflunomide.
Regadenoson Caffeine may decrease effectiveness of Regadenoson as a diagnostic agent.
Adalimumab The serum concentration of Caffeine can be decreased when it is combined with Adalimumab.
Adenosine The therapeutic efficacy of Adenosine can be decreased when used in combination with Caffeine.
Allopurinol The serum concentration of Caffeine can be increased when it is combined with Allopurinol.
Carbamazepine The serum concentration of Caffeine can be decreased when it is combined with Carbamazepine.
Cimetidine The metabolism of Caffeine can be decreased when combined with Cimetidine.
Disulfiram The serum concentration of Caffeine can be increased when it is combined with Disulfiram.
Febuxostat The serum concentration of the active metabolites of Caffeine can be increased when Caffeine is used in combination with Febuxostat.
Fluvoxamine The metabolism of Caffeine can be decreased when combined with Fluvoxamine.
Formoterol The risk or severity of hypokalemia can be increased when Caffeine is combined with Formoterol.
Indacaterol The risk or severity of adverse effects can be increased when Caffeine is combined with Indacaterol.
Isoniazid The serum concentration of Caffeine can be increased when it is combined with Isoniazid.
Lithium citrate The serum concentration of Lithium citrate can be decreased when it is combined with Caffeine.
Lithium carbonate The serum concentration of Lithium carbonate can be decreased when it is combined with Caffeine.
Lithium hydroxide The serum concentration of Lithium hydroxide can be decreased when it is combined with Caffeine.
Mexiletine The metabolism of Caffeine can be decreased when combined with Mexiletine.
Olodaterol Caffeine may increase the hyperkalemic activities of Olodaterol.
Pancuronium The therapeutic efficacy of Pancuronium can be decreased when used in combination with Caffeine.
Pentoxifylline The serum concentration of Caffeine can be increased when it is combined with Pentoxifylline.
Phenytoin The serum concentration of Caffeine can be decreased when it is combined with Phenytoin.
Propafenone The serum concentration of Caffeine can be increased when it is combined with Propafenone.
Quinine The serum concentration of Caffeine can be increased when it is combined with Quinine.
Quinidine The serum concentration of Caffeine can be increased when it is combined with Quinidine.
Riociguat Caffeine may increase the hypotensive activities of Riociguat.
Thiabendazole The metabolism of Caffeine can be decreased when combined with Thiabendazole.
Ticlopidine The metabolism of Caffeine can be decreased when combined with Ticlopidine.
Zafirlukast The serum concentration of Zafirlukast can be decreased when it is combined with Caffeine.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Caffeine.
Probenecid The serum concentration of Caffeine can be increased when it is combined with Probenecid.
Agomelatine The serum concentration of Agomelatine can be increased when it is combined with Caffeine.
Pirfenidone The metabolism of Pirfenidone can be decreased when combined with Caffeine.
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Caffeine.
Abiraterone The serum concentration of Caffeine can be increased when it is combined with Abiraterone.
Isoprenaline The serum concentration of Caffeine can be decreased when it is combined with Isoprenaline.
Cyproterone acetate The metabolism of Caffeine can be increased when combined with Cyproterone acetate.
Amphetamine The risk or severity of adverse effects can be increased when Amphetamine is combined with Caffeine.
Phentermine The risk or severity of adverse effects can be increased when Phentermine is combined with Caffeine.
Midodrine The risk or severity of adverse effects can be increased when Midodrine is combined with Caffeine.
Norepinephrine The risk or severity of adverse effects can be increased when Norepinephrine is combined with Caffeine.
Labetalol The risk or severity of adverse effects can be increased when Labetalol is combined with Caffeine.
Metaraminol The risk or severity of adverse effects can be increased when Metaraminol is combined with Caffeine.
Epinephrine The risk or severity of adverse effects can be increased when Epinephrine is combined with Caffeine.
Methoxamine The risk or severity of adverse effects can be increased when Methoxamine is combined with Caffeine.
Orciprenaline The risk or severity of adverse effects can be increased when Orciprenaline is combined with Caffeine.
Phenmetrazine The risk or severity of adverse effects can be increased when Phenmetrazine is combined with Caffeine.
Dobutamine The risk or severity of adverse effects can be increased when Dobutamine is combined with Caffeine.
Benzphetamine The risk or severity of adverse effects can be increased when Benzphetamine is combined with Caffeine.
Ritodrine The risk or severity of adverse effects can be increased when Ritodrine is combined with Caffeine.
Terbutaline The risk or severity of adverse effects can be increased when Terbutaline is combined with Caffeine.
Oxymetazoline The risk or severity of adverse effects can be increased when Oxymetazoline is combined with Caffeine.
Diethylpropion The risk or severity of adverse effects can be increased when Diethylpropion is combined with Caffeine.
Dopamine The risk or severity of adverse effects can be increased when Dopamine is combined with Caffeine.
Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Caffeine.
Lisdexamfetamine The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with Caffeine.
Fenoterol The risk or severity of adverse effects can be increased when Fenoterol is combined with Caffeine.
Ephedrine The risk or severity of adverse effects can be increased when Ephedrine is combined with Caffeine.
Mephentermine The risk or severity of adverse effects can be increased when Mephentermine is combined with Caffeine.
Procaterol The risk or severity of adverse effects can be increased when Procaterol is combined with Caffeine.
Clenbuterol The risk or severity of adverse effects can be increased when Clenbuterol is combined with Caffeine.
MMDA The risk or severity of adverse effects can be increased when MMDA is combined with Caffeine.
Midomafetamine The risk or severity of adverse effects can be increased when Midomafetamine is combined with Caffeine.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Caffeine.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Caffeine.
Tenamfetamine The risk or severity of adverse effects can be increased when Tenamfetamine is combined with Caffeine.
Chlorphentermine The risk or severity of adverse effects can be increased when Chlorphentermine is combined with Caffeine.
Methylenedioxyethamphetamine The risk or severity of adverse effects can be increased when Methylenedioxyethamphetamine is combined with Caffeine.
Dextroamphetamine The risk or severity of adverse effects can be increased when Dextroamphetamine is combined with Caffeine.
Metamfetamine The risk or severity of adverse effects can be increased when Metamfetamine is combined with Caffeine.
Celiprolol The risk or severity of adverse effects can be increased when Celiprolol is combined with Caffeine.
Nylidrin The risk or severity of adverse effects can be increased when Nylidrin is combined with Caffeine.
Tetryzoline The risk or severity of adverse effects can be increased when Tetryzoline is combined with Caffeine.
Tyramine The risk or severity of adverse effects can be increased when Tyramine is combined with Caffeine.
Isoxsuprine The risk or severity of adverse effects can be increased when Isoxsuprine is combined with Caffeine.
Etilefrine The risk or severity of adverse effects can be increased when Etilefrine is combined with Caffeine.
Synephrine The risk or severity of adverse effects can be increased when Synephrine is combined with Caffeine.
Hydroxyamphetamine The risk or severity of adverse effects can be increased when Hydroxyamphetamine is combined with Caffeine.
Iofetamine I-123 The risk or severity of adverse effects can be increased when Iofetamine I-123 is combined with Caffeine.
Racepinephrine The risk or severity of adverse effects can be increased when Racepinephrine is combined with Caffeine.
Ritobegron The risk or severity of adverse effects can be increased when Ritobegron is combined with Caffeine.
Bucindolol The risk or severity of adverse effects can be increased when Bucindolol is combined with Caffeine.
Tramazoline The risk or severity of adverse effects can be increased when Tramazoline is combined with Caffeine.
Mephedrone The risk or severity of adverse effects can be increased when Mephedrone is combined with Caffeine.
Fenozolone The risk or severity of adverse effects can be increased when Fenozolone is combined with Caffeine.
Methoxyphenamine The risk or severity of adverse effects can be increased when Methoxyphenamine is combined with Caffeine.
Tretoquinol The risk or severity of adverse effects can be increased when Tretoquinol is combined with Caffeine.
Gepefrine The risk or severity of adverse effects can be increased when Gepefrine is combined with Caffeine.
Epanolol The risk or severity of adverse effects can be increased when Epanolol is combined with Caffeine.
Prenalterol The risk or severity of adverse effects can be increased when Prenalterol is combined with Caffeine.
Mefenorex The risk or severity of adverse effects can be increased when Mefenorex is combined with Caffeine.
2,5-Dimethoxy-4-ethylthioamphetamine The risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylthioamphetamine is combined with Caffeine.
Esmolol The risk or severity of adverse effects can be increased when Esmolol is combined with Caffeine.
Betaxolol The risk or severity of adverse effects can be increased when Betaxolol is combined with Caffeine.
Atenolol The risk or severity of adverse effects can be increased when Atenolol is combined with Caffeine.
Timolol The risk or severity of adverse effects can be increased when Timolol is combined with Caffeine.
Propranolol The risk or severity of adverse effects can be increased when Propranolol is combined with Caffeine.
Bisoprolol The risk or severity of adverse effects can be increased when Bisoprolol is combined with Caffeine.

Target Protein

Adenosine receptor A1 ADORA1
5'-nucleotidase NT5E
Adenosine receptor A2a ADORA2A
Adenosine receptor A2b ADORA2B
Adenosine receptor A3 ADORA3
Phosphodiesterase enzymes PDE4D
3',5'-cyclic-AMP phosphodiesterase 4B PDE4B
Ryanodine receptor 1 RYR1
Cyclic nucleotide phosphodiesterase PDE4A
DNA-dependent protein kinase catalytic subunit PRKDC
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform PIK3CD
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform PIK3CA
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform PIK3CB
Inositol 1,4,5-trisphosphate receptor ITPR1
Serine-protein kinase ATM ATM

Referensi & Sumber

Synthesis reference: Kaspar Bott, "Preparation of caffeine." U.S. Patent US4380631, issued December, 1976.
Artikel (PubMed)
  • PMID: 1356551
    Nehlig A, Daval JL, Debry G: Caffeine and the central nervous system: mechanisms of action, biochemical, metabolic and psychostimulant effects. Brain Res Brain Res Rev. 1992 May-Aug;17(2):139-70.
  • PMID: 22113078
    Ding R, Shi J, Pabon K, Scotto KW: Xanthines down-regulate the drug transporter ABCG2 and reverse multidrug resistance. Mol Pharmacol. 2012 Mar;81(3):328-37. doi: 10.1124/mol.111.075556. Epub 2011 Nov 23.
  • PMID: 24761278
    Kole J, Barnhill A: Caffeine Content Labeling: A Missed Opportunity for Promoting Personal and Public Health. J Caffeine Res. 2013 Sep;3(3):108-113. doi: 10.1089/jcr.2013.0017.
  • PMID: 30574005
    Michael Z, Spyropoulos F, Ghanta S, Christou H: Bronchopulmonary Dysplasia: An Update of Current Pharmacologic Therapies and New Approaches. Clin Med Insights Pediatr. 2018 Dec 11;12:1179556518817322. doi: 10.1177/1179556518817322. eCollection 2018.
  • PMID: 28589122
    Collins JJP, Tibboel D, de Kleer IM, Reiss IKM, Rottier RJ: The Future of Bronchopulmonary Dysplasia: Emerging Pathophysiological Concepts and Potential New Avenues of Treatment. Front Med (Lausanne). 2017 May 22;4:61. doi: 10.3389/fmed.2017.00061. eCollection 2017.
  • PMID: 29067618
    Lipton RB, Diener HC, Robbins MS, Garas SY, Patel K: Caffeine in the management of patients with headache. J Headache Pain. 2017 Oct 24;18(1):107. doi: 10.1186/s10194-017-0806-2.
  • PMID: 1544897
    Schneider E, Freundlieb S, Tapio S, Boos W: Molecular characterization of the MalT-dependent periplasmic alpha-amylase of Escherichia coli encoded by malS. J Biol Chem. 1992 Mar 15;267(8):5148-54.
  • PMID: 26074744
    Cappelletti S, Piacentino D, Sani G, Aromatario M: Caffeine: cognitive and physical performance enhancer or psychoactive drug? Curr Neuropharmacol. 2015 Jan;13(1):71-88. doi: 10.2174/1570159X13666141210215655.
Menampilkan 8 dari 11 artikel.
Textbook
  • Justin Evans; Amanda S. Battisti (2019). Caffeine. Stat Pearls Publishing.
  • IARC Working Group on the Evaluation of Carcinogenic Risk to Humans (1991). Coffee, Tea, Mate, Methylxanthines and Methylglyoxal. International Agency for Research on Cancer.
  • Institute of Medicine (US) Committee on Military Nutrition Research. (2001). Caffeine for the Sustainment of Mental Task Performance: Formulations for Military Operations.. National Academic Press.

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