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Caffeine

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Definition: A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes SMOOTH MUSCLE, stimulates CARDIAC MUSCLE, stimulates DIURESIS, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling.     
Pharmacological Action Central Nervous System Stimulants; Phosphodiesterase Inhibitors; Purinergic P1 Receptor Antagonists 		Other names Vivarin; Thompson Brand 2 of Caffeine; Thompson Brand 1 of Caffeine; Seid Brand of Caffeine; Republic Drug Brand of Caffeine; Quick-Pep; Pierre Fabre Brand of Caffeine; Percutaf+¬ine; Percoffedrinol N; Passauer Brand of Caffeine; No Doz; Merck dura Brand of Caffeine; GlaxoSmithKline Brand of Caffeine; Durvitan; Dexitac; Coffeinum Purrum; Coffeinum N; Caffedrine; Bristol-Myers Squibb Brand of Caffeine; Berlin-Chemie Brand of Caffeine
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
cellucare  0   *Caffeine *Hyaluronic Acid Drug Combinations. J Cosmet Laser Ther. 2011 Aug;13(4):142-53.
Keganmin  0   *Aminopyrine *Caffeine *Phenacetin Drug Combinations. Guang Pu Xue Yu Guang Pu Fen Xi. 1997 Feb;17(1):123-5
caffeine, chlorcyclizine, codeine, ergotamine drug combination  0   *Caffeine *Codeine *Ergotamine *Piperazines Drug Combinations.
Pharma Action Analgesics
Indoprocaf  0   *Caffeine *Indomethacin *Prochlorperazine Drug Combinations Migraine Disorders. Int J Clin Pract. 2007 Aug;61(8):1256-69
(1,3,7,9-tetramethylxanthine-8-ylidene)silver acetate  0   *Organometallic Compounds Caffeine/*analogs & derivatives Silver. J Med Chem 2006 Nov 16;49(23):6811-8
LM11A-24  0   Caffeine/*analogs & derivatives Apoptosis. Eur J Neurosci 2006 Sep;24(6):1575-80
hydroxycut  0   *Plant Preparations Caffeine. Pharmacotherapy 2001 May;21(5):647-51
caffeinol  0   *Ethanol *Caffeine Drug Combinations. Stroke 2005 Jan;36(1):129-34
8-nitrocaffeine  0   Caffeine/*analogs & derivatives. Gan To Kagaku Ryoho 2004 Apr;31(4):522-5
lipokinetix  0   *Benzofurans *Caffeine *Diiodothyronines *Phenylpropanolamine *Yohimbine. Ann Intern Med 2002 Apr 16;136(8):590-5
KF 21213  155271-17-3   Caffeine/*analogs & derivatives Ligands. Nucl Med Biol 2000 Aug;27(6):541-6
Shin Ruru A  0   *Acetaminophen *Caffeine *Guaiacol *Muramidase Drug Combinations Nonprescription Drugs. J Dermatol 2000 Jun;27(6):401-4
3-methyl-7-(7-oxooctyl)-1-propargylxanthine  0   Caffeine. J Med Chem 1999 Jul 15;42(14):2527-34
1,3-dimethyl-7-(7-hydroxyoctyl)xanthine  0   Caffeine. J Med Chem 1999 Jul 15;42(14):2527-34
1,3-dimethyl-7-(5-ethylcarboxypentyl)xanthine  0   Caffeine. J Med Chem 1999 Jul 15;42(14):2527-34
valcophen  0   *Aspirin *Caffeine *Phenobarbital Drug Combinations. Fiziol Zh 1998;44(5-6):102-5
acetaminophen, aspirin, caffeine drug combination  0   *Acetaminophen *Aspirin *Caffeine Drug Combinations.
Pharma Action Anti-Inflammatory Agents, Non-Steroidal 		J Pharm Pharmacol 1997 Dec;49(12):1260EXCEDRIN (MIGRAINE); ACETAMINOPHEN, ASPIRIN AND CAFFEINE; CODEINE, ASPIRIN, APAP FORMULA NO. 3; ACETAMINOPHEN, ASPIRIN, AND CODEINE PHOSPHATE; CODEINE, ASPIRIN, APAP FORMULA NO. 4; CODEINE, ASPIRIN, APAP FORMULA NO. 2
8-cyclohexylcaffeine  0   Caffeine/*analogs & derivatives Receptors, Purinergic P1/antagonists & inhibitors. Pharmacol Toxicol 1997 Jun;80(6):295-300
L 5409709  0   *Acetaminophen *Caffeine *Ibuprofen Drug Combinations. Pain 1997 Apr;70(2-3):253-66
caffeine, codeine, acetaminophen, propyphenazone drug combination  0   *Acetaminophen *Caffeine *Codeine Antipyrine/*analogs & derivatives Drug Combinations.
Pharma Action Analgesics 		Zh Neuropatol Psikhiatr Im S S Korsakova 1997;97(4):48-9
proksifein  80539-94-2   Caffeine/*analogs & derivatives DNA Repair. Tsitologiia 1996;38(11):1203-10
cofpropamine  0   Caffeine/*analogs & derivatives Poly(ADP-ribose) Polymerases/antagonists & inhibitors. Gen Pharmacol 1996 Oct;27(7):1215-8
guarana powder  0   *Caffeine *Theobromine *Theophylline Sapindaceae. Analyst 1994 Dec;119(12):2701-3
tert-butyloxycarbonyl-mononitrosamidocaffeidine  145439-00-5   *Nitrosamines Caffeine/*analogs & derivatives. Mutat Res 1993 Aug;292(1):41-9
dinitrosocaffeidine  145438-97-7   *Nitrosamines Caffeine/*analogs & derivatives. Mutat Res 1993 Aug;292(1):41-9
mononitrosocaffeidine  145438-96-6   *Nitrosamines Caffeine/*analogs & derivatives. Mutat Res 1993 Aug;292(1):41-9
Kinuya-chinnetsu  0   *Acetaminophen *Caffeine Drug Combinations. Chest 1993 Jul;104(1):291-2
8-(3-chlorostyryl)caffeine  148589-13-3   Caffeine/*analogs & derivatives. FEBS Lett 1993 May 24;323(1-2):141-4
dixaphen  0   *Benzamides *Caffeine *Ephedrine Drug Combinations. Vopr Onkol 1992;38(2):148-53
caffeidine acid  54536-15-1   Caffeine/*analogs & derivatives. Chem Res Toxicol 1993 Jan-Feb;6(1):50-8
K1 protocol  0   *Antineoplastic Combined Chemotherapy Protocols Caffeine Cisplatin Doxorubicin Methotrexate. J Cancer Res Clin Oncol 1992;118(8):567-9
8-chlorocaffeine  4921-49-7   Caffeine/*analogs & derivatives. Carcinogenesis 1991;12(10):1781
pircophen  8075-94-3   *Aminopyrine *Caffeine *Phenacetin Drug Combinations. Klin Med (Mosk) 1990;68(8):91
8-methoxycaffeine  569-34-6   Caffeine/*analogs & derivatives Cross-Linking Reagents. Boll Soc Ital Biol Sper 1990;66(6):587
Impletol  8013-38-5   *Caffeine *Procaine Drug Combinations. Nippon Jibinkoka Gakkai Kaiho 1989;92(12):2023
caffeine, chlorpheniramine, dihydrocodeine, methylephedrine drug combination  0   *Caffeine *Chlorpheniramine Codeine/*analogs & derivatives Drug Combinations Ephedrine/*analogs & derivatives. Arukoru Kenyuto Yakubutsu Ison 1989;24(5):417
acetaminophen, butalbital, caffeine drug combination  0   *Acetaminophen *Barbiturates *Caffeine Drug Combinations.
Pharma Action Anti-Inflammatory Agents, Non-Steroidal 		Clin Ther 1987;10(1):69ESGIC; FIORICET W/ CODEINE; TRIAD; ANOQUAN; BUTALIBITAL, ACETAMINOPHEN AND CAFFEINE; FIORICET; FEMCET; PHRENILIN WITH CAFFEINE AND CODEINE; BUTALBITAL, ACETAMINOPHEN AND CAFFEINE; BUTALBITAL, ACETAMINOPHEN, CAFFEINE AND CODEINE PHOSPHATE; MEDIGESIC PLUS; ESGIC-PLUS
Vasobral  94423-99-1   *Caffeine *Dihydroergotoxine Drug Combinations. Arm Radiol 1987;30(6):425
caffeidine  20041-90-1   Caffeine/*analogs & derivatives. Chem Pharm Bull (Tokyo) 1986;34(9):3573
Sig 8304  123283-88-5   *Benzoates *Caffeine Antipyrine/*analogs & derivatives Drug Combinations. Clin Ter 1986;117(6):469
acetaminophen, caffeine, guaifenesin drug combination  0   *Acetaminophen *Caffeine *Guaifenesin Drug Combinations. Act Nerv Super (Praha) 1986;28(2):153
aspirin, caffeine, codeine drug combination  0   *Aspirin *Caffeine *Codeine Drug Combinations. Can Dent Assoc J 1986;52(4):325SYNALGOS-DC
Propain  138230-30-5   *Acetaminophen *Caffeine *Codeine *Diphenhydramine Drug Combinations. Br J Clin Pract 1985;39(1):21
Migril  86498-65-9   *Caffeine *Cyclizine *Ergotamine Drug Combinations. Practitioner 1984;228(1390):444
impletol depot Bayer  95017-34-8 Benzoic acid, 4-amino-, 2-(diethylamino)ethyl ester, mixt. with 3,7-dihydro-1,3,7-trimethyl-1H-purine-2,6-dione and 1-ethenyl-2-pyrrolidinone homopolymer  *Caffeine *Povidone *Procaine Drug Combinations Delayed-Action Preparations. Reumatologia 1983;21(2):167
Norgesic forte  88566-80-7 Benzoic acid, 2-(acetyloxy)-, mixt. with 3,7-dihydro-1,3,7-trimethyl-1H-purine-2,6-dione and N,N-dimethyl-2-((2-methylphenyl)phenylmethoxy)ethanamine 2-hydroxy-1,2,3-propanetricarboxylate (1:1)  *Aspirin *Caffeine *Orphenadrine Drug Combinations. Ther Drug Monit 1983;5(4):401INVAGESIC FORTE; ORPHENADRINE CITRATE, ASPIRIN, AND CAFFEINE; ORPHENGESIC; INVAGESIC; NORGESIC FORTE; NORGESIC; ORPHENGESIC FORTE
2-methylcaffeine  0   Caffeine/*analogs & derivatives. Toxicol Appl Pharmacol 1983;71(2):237
6-thiocaffeine  13182-58-6   Caffeine/*analogs & derivatives. Pharmacol Res Commun 1983;15(2):131
caffeine, ergotamine drug combination  0   *Caffeine *Ergotamine Drug Combinations. Clin Pediatr (Phila) 1983;22(3):226CAFERGOT; WIGRAINE; MIGERGOT; ERGOTAMINE TARTRATE AND CAFFEINE
1-methylcaffeine  77196-81-7 1H-Purine-2,6-dione, 3,7-dihydro-3,7-dimethyl-1-(methyl-14C)  Caffeine/*analogs & derivatives. Drug Metab Dispos 1982;10(4):417
Midol  83514-22-1 Benzoic acid, 2-(acetyloxy)-, mixt. with 3,7-dihydro-1,3,7-trimethyl-1H-purine-2,6-dione, N-(4-ethoxyphenyl)acetamide and alpha-(1-(methyl(3-phenyl-2-propenyl)amino)ethyl)benzenemethanol hydrochloride  *Aspirin *Caffeine *Phenacetin Drug Combinations Ephedrine/*analogs & derivatives. Arch Intern Med 1982;142(8):1583MIDOL
solpadeine  82400-20-2 Morphinan-6-ol, 7,8-didehydro-4,5-epoxy-3-methoxy-17-methyl-, (5alpha,6alpha)-, phosphate (1:1) (salt), mixt. with 3,7-dihydro-1,3,7-trimethyl-1H-purine-2,6-dione and N-(4-hydroxyphenyl)acetamide  *Acetaminophen *Caffeine Codeine/*analogs & derivatives Drug Combinations. J Int Med 1982;10(2):109ACETAMINOPHEN, CAFFEINE, AND DIHYDROCODEINE BITARTRATE; DHC PLUS; SYNALGOS-DC-A
cofplaton  80539-95-3 Platinate(2-), hexachloro-, (OC-6-11)-, dihydrogen, compd. with 8-(3-(dimethylamino)propoxy)-3,7-dihydro-1,3,7-trimethyl-1H-purine-2,6-dione (1:2)  *Organoplatinum Compounds Caffeine/*analogs & derivatives Platinum. Naturwissenschaften 1981;68(12):628
caffeine, ephedrine drug combination  0 1H-Purine-2,6-dione, 3,7-dihydro-1,3,7-trimethyl-, mixt. with (R-(R*,S*))-alpha-(1-(methylamino)ethyl)benzenemethanol  *Caffeine *Ephedrine Drug Combinations. Int J Obes 1981;5(2):183
Syndol  79953-81-4 Morphinan-6-ol, 7,8-didehydro-4,5-epoxy-3-methoxy-17-methyl-, (5alpha,6alpha)-, phosphate (1,1) (salt), mixt. with 3,7-dihydro-1,3,7-trimethyl-1H-purine-2,6-dione, N,N-dimethyl-2-(1-phenyl-1-(2-pyridinyl)ethoxy)ethanamine butanedioate (1,1) and N-(4-hydr  *Acetaminophen *Caffeine *Doxylamine Codeine/*analogs & derivatives Drug Combinations. Br Dent J 1981;150(7):187
Migraine-Kranit  77193-78-3 Acetamide, N-(4-hydroxyphenyl)-, mixt. with 1-((3,4-diethoxyphenyl)methyl)-6,7-diethoxyisoquinoline hydrochloride, 1,2-dihydro-1,5-dimethyl-4-(1-methylethyl)-2-phenyl-3H-pyrazol-3-one, 3,7-dihydro-1,3,7-trimethyl-1H-purine-2,6-dione and 5-ethyl-5-phenyl  *Acetaminophen *Caffeine *Phenobarbital Antipyrine/*analogs & derivatives Drug Combinations Papaverine/*analogs & derivatives. Arzneim Forsch 1981;31(1):105
caffeine citrate  69-22-7   *Caffeine *Citrates Apnea.
Pharma Action Central Nervous System Stimulants 		Indian J Exp Biol 1980;18(1):99CAFCIT; CAFFEINE CITRATE
caffeine, sodium benzoate drug combination  5743-17-9   *Caffeine *Benzoates Drug Combinations.
Pharma Action Antimutagenic Agents ; Analgesics, Non-Narcotic 		Radiobiologiia 1980;20(4):598
Aspirin-oxycodone hydrochloride-oxycodone terephthalate combination  64336-56-7   *Aspirin *Caffeine *Oxycodone *Phenacetin Drug Combinations. Kidney Int 1980;17(2):250PERCODAN; ROXIPRIN; PERCODAN-DEMI; OXYCODONE AND ASPIRIN; OXYCODONE AND ASPIRIN (HALF-STRENGTH); CODOXY
bucetin, caffeine, dibenzoylthiamine, ethenzamide drug combination  0   *Caffeine *Salicylamides Drug Combinations Phenetidine/*analogs & derivatives Thiamine/*analogs & derivatives. Dent Outlook 1978;52(5):911
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