Drug/Small Molecule:
caffeine

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

Links to Unannotated Labels

These links are to labels associated with caffeine that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105080

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA CYP1A2 *1A N/A N/A N/A
VIP No VIP available No VIP available CYP1A2 *1C N/A N/A N/A
VIP CA VA CYP1A2 *1F N/A N/A N/A
VIP No VIP available VA CYP1A2 *1K N/A N/A N/A
No VIP available No VIP available VA CYP2A6 *1A N/A N/A N/A
No VIP available No VIP available VA CYP2A6 *4A N/A N/A N/A
VIP No VIP available VA CYP2A6 *7 N/A N/A N/A
VIP No VIP available VA CYP2A6 *9A N/A N/A N/A
No VIP available No VIP available VA CYP2A6 *10 N/A N/A N/A
No VIP available No VIP available VA CYP2A6 *11 N/A N/A N/A
VIP No VIP available No VIP available CYP2A6 *1X2A N/A N/A N/A
No VIP available No VIP available VA NAT2 *4 N/A N/A N/A
No VIP available No VIP available VA NAT2 *5A N/A N/A N/A
No VIP available No VIP available VA NAT2 *5B N/A N/A N/A
No VIP available No VIP available VA NAT2 *5C N/A N/A N/A
No VIP available No VIP available VA NAT2 *6 N/A N/A N/A
No VIP available No VIP available VA NAT2 *7 N/A N/A N/A
No VIP available No Clinical Annotations available VA
CYP1A2 high activity phenotype N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs1110976 113284519T>G, 16846935T>G, 66483A>C, 724-914A>C, 810+578A>C
T > G
Intronic
No VIP available No Clinical Annotations available VA
rs11704959 24820483C>A, 4211052C>A
C > A
Not Available
rs2069514 (-2964)G>A, 28338G>A, 3860G>A, 45828777G>A, 75038220G>A, CYP1A2*1C
G > A
Not Available
No VIP available No Clinical Annotations available VA
rs2070676 1156-118G>C, 135351137G>C, 15271G>C, 6585068G>C
G > C
Intronic
No VIP available No Clinical Annotations available VA
rs2198843 45791787C>G, 75001230C>G
C > G
Not Available
No VIP available No Clinical Annotations available VA
rs2267076 24830595T>C, 332+891T>C, 4221164T>C, 575-2193A>G, ADORA2A: g.4221164T>C
T > C
Intronic
No VIP available CA VA
rs2298383 -275+1797C>T, 2235A>A, 24825511C>T, 4216080C>T, ADORA2A: g.4216080C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2470890 +, 1548C>T, 295T>C, 37544C>T, 45837983C>T, 75047426C>T, Asn516=, CYP1A2*1B, CYP1A2:1545T>C, CYP1A2:1548T>C, CYP1A2:5347T>C, CYP1A2:Asn516Asn, CYP1A2:Ex7
C > T
Synonymous
Asn516Asn
No VIP available No Clinical Annotations available VA
rs2470893 -1694G>A, 45810006C>T, 75019449C>T, 9567C>T
C > T
5' Flanking
No VIP available No Clinical Annotations available VA
rs2472299 23518A>G, 45823957A>G, 75033400A>G
A > G
Not Available
No VIP available No Clinical Annotations available VA
rs2472304 1042+43G>A, 34356G>A, 45834795G>A, 75044238G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs3032740 1285+221_1285+222insAAAAA, 24835040_24835041insTTTTT, 333-1511_333-1510insTTTTT, 4225609_4225610insTTTTT, 574+2919_574+2920insAAAAA
- > TTTTT
Not Available
No VIP available No Clinical Annotations available VA
rs35320474 *453_*454insT, 1011+49_1011+50insA, 24837910_24837911insT, 2592C>Tins, 4228479_4228480insT, 574+49_574+50insA, ADORA2A:2592T/-, Exon 5; 2592 Ins/DelT
- > T
Not Available
No VIP available No Clinical Annotations available VA
rs35694136 -1635delT, 29731delT, 45830170delT, 75039613delT
T > -
5' Flanking
No VIP available No Clinical Annotations available VA
rs3761422 -274-2427T>C, 1398+208A>G, 24826672T>C, 4217241T>C, ADORA2A: g.4217241T>C
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs4410790 17274577T>C, 17284577T>C
T > C
Not Available
No VIP available No Clinical Annotations available VA
rs4646421 -26-728C>A, -26-728C>G, -26-728C>T, 45806749G>A, 45806749G>C, 45806749G>T, 6310G>A, 6310G>C, 6310G>T, 75016192G>A, 75016192G>C, 75016192G>T
G > A
G > T
G > C
Intronic
No VIP available No Clinical Annotations available VA
rs4822492 24843594C>G, 4234163C>G, 426-5486G>C, 862+4585G>C
C > G
Intronic
No VIP available No Clinical Annotations available VA
rs5751862 140775G>A, 24802564G>A, 286-4992G>A, 3088-4992G>A, 3088-6052G>A, 4193133G>A
G > A
Intronic
No VIP available CA VA
rs5751876 1011+659A>G, 1083T>C, 24837301T>C, 4227870T>C, 574+659A>G, ADORA2A:1083T>C, ADORA2A:1976T>C, Tyr361=
T > C
Synonymous
Tyr361Tyr
No VIP available No Clinical Annotations available VA
rs5760405 *3250C>T, 152052C>T, 24813841C>T, 4204410C>T
C > T
3' Flanking
rs762551 -9-154C>A, 32035C>A, 45832474C>A, 75041917C>A, CYP1A2*1F, CYP1A2:734C>A
C > A
Intronic
VIP No Clinical Annotations available No Variant Annotations available
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
No VIP available No Clinical Annotations available VA
rs8192766 -1515T>G, 135339385T>G, 3519T>G, 6573316T>G, CYP2E1(-1515)G>T
T > G
5' Flanking
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • 1,3,7-trimethylxanthine
  • 137X
  • CFF
  • Cafeina
  • Caffein
  • Caffeine Pure
  • Caffeine, Anhydrous
  • Caffeine, Monohydrate
  • Caffeine, Synthetic
  • Compound 65
  • Methyltheobromide
  • Methyltheobromine
  • Monomethyl Derivative of Theophylline
  • Theobromine ME
  • Theophylline ME
Trade Names
  • Alert-Pep
  • Anoquan
  • Cafamil
  • Cafcit
  • Cafecon
  • Cafergot
  • Caffedrine
  • Caffedrine Caplets
  • Caffine
  • Cafipel
  • Coffein
  • Coffeine
  • Darvon Compound
  • Darvon Compound-65
  • Dasin
  • Dexitac
  • Dexitac Stay Alert Stimulant
  • Dhc Plus
  • Diurex
  • Durvitan
  • Eldiatric C
  • Enerjets
  • Ercatab
  • Esgic
  • Esgic-Plus
  • Femcet
  • Fioricet
  • Fiorinal
  • Guaranine
  • Hycomine
  • Invagesic
  • Invagesic Forte
  • Keep Alert
  • Kofein
  • Koffein
  • Lanorinal
  • Mateina
  • Maximum Strength Snapback Stimulant Powders
  • Medigesic Plus
  • Migergot
  • Miudol
  • Natural Caffeinum
  • Nix Nap
  • No-Doz
  • Nodaca
  • Nodoz Maximum Strength Caplets
  • Norgesic
  • Norgesic Forte
  • Organex
  • Orphengesic
  • Orphengesic Forte
  • Pep-Back
  • Phensal
  • Propoxyphene Compound 65
  • Propoxyphene Compound-65
  • Quick Pep
  • Refresh'n
  • SK 65 Compound
  • Stim
  • Synalgos-Dc
  • Thein
  • Theine
  • Triad
  • Ultra Pep-Back
  • Vivarin
  • Wake-Up
  • Wigraine
Brand Mixture Names
  • 217 (Acetylsalicylic Acid + Caffeine Citrate)
  • 217 Strong Tab (Acetylsalicylic Acid + Caffeine Citrate)
  • 222 Tablet (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  • 282 Mep (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate + Meprobamate)
  • 282 Mep Tab (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate + Meprobamate)
  • 282 Tab (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  • 282 Tablets (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  • 292 Tab (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  • 292 Tablets (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  • 692 Tab (Acetylsalicylic Acid + Caffeine + Dextropropoxyphene Hydrochloride)
  • 692 Tablet (Acetylsalicylic Acid + Caffeine + Dextropropoxyphene Hydrochloride)
  • A & C Tablets with Codeine 15mg (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • A & C Tablets with Codeine 30mg (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • A C and C Tab 0.125gr (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • A.C. & C 8mg Tab (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • A.C. & C Tablets (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • AC and C Tab 1/8gr (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • AC&C Tablets (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • ASA, Caffeine & 8mg Codeine Phosphate (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • Acet 2 (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acet 3 (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen 300 Mg with Caffeine & Codeine Caplet (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen 500mg Cmpd Tab with Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen Caffeine & 8mg Cod Phos Tab (Acetaminophen + Caffeine + Codeine (Codeine Phosphate))
  • Acetaminophen Caffeine & 8mg Cod. Phos. Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen Compound Caplets with Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen Compound Tablets with Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen Compound Tablets with Codeine 8mg (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen Extra Strength with Caf & Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen with Caffeine and Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen with Codeine - Caplet (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen with Codeine Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen, Caffeine & 8mg Codeine Phosphate (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen, Caffeine & 8mg Codeine Phosphate Tablets (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen, Caffeine and 8 Mg of Codeine Phosphate Tablets (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetaminophen, Caffeine, and 8mg of Codeine Phosphate Tablets (Acetaminophen + Caffeine + Codeine Phosphate)
  • Acetylsalicylic Acid Caffeine & 8mg Cod Phos (Acetylsalicylic Acid + Caffeine + Codeine (Codeine Phosphate))
  • Acetylsalicylic Acid, Caffeine & 8 Mg Codeine Phosphate Tablets (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • Acetylsalicylic Acid, Caffeine and 8mg Codeine Phosphate (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • Alka-Seltzer Morning Relief (Acetylsalicylic Acid + Caffeine)
  • Anacin Caplet (Acetylsalicylic Acid + Caffeine)
  • Anacin Caplets (Acetylsalicylic Acid + Caffeine)
  • Anacin Extra Strength Caplet (Acetylsalicylic Acid + Caffeine)
  • Anacin Extra Strength Tablet (Acetylsalicylic Acid + Caffeine)
  • Anacin Tab (Acetylsalicylic Acid + Caffeine)
  • Anacin Tablet (Acetylsalicylic Acid + Caffeine)
  • Anacin with Codeine Tab (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • Antidol Tablets (Acetylsalicylic Acid + Caffeine)
  • Arco Pain Tab (Acetylsalicylic Acid + Caffeine Citrate)
  • Astone Cap (Acetylsalicylic Acid + Caffeine)
  • Atasol 15 Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • Atasol 30 Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • Atasol 8 Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • C T Acetylsalicylic Acid Codeine and Caf Tab (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • C-2 Buffered with Codeine (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • C2 Buffered Tab (Acetylsalicylic Acid + Aluminum Hydroxide + Caffeine + Magnesium Hydroxide)
  • C2 Buffered with Codeine Tab (Acetylsalicylic Acid + Aluminum Hydroxide + Caffeine + Codeine Phosphate + Magnesium Hydroxide)
  • C2 Tab with Codeine (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • Cafergot PB Sup (Belladonna + Caffeine + Ergotamine (Ergotamine Tartrate) + Pentobarbital)
  • Cafergot PB Tab (Belladonna + Caffeine + Ergotamine (Ergotamine Tartrate) + Pentobarbital Sodium)
  • Cafergot Sup (Caffeine + Ergotamine Tartrate)
  • Cafergot Tab (Caffeine + Ergotamine Tartrate)
  • Calmine Tab (Acetylsalicylic Acid + Caffeine)
  • Codamin No2 (Acetaminophen + Caffeine + Codeine Phosphate)
  • Codamin No3 (Acetaminophen + Caffeine + Codeine Phosphate)
  • Codaminophen Tab 1/8gr (Acetaminophen + Caffeine + Codeine Phosphate)
  • Corytab (Acetaminophen + Caffeine + Diphenylpyraline Hydrochloride)
  • Cotabs (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • Darvon N Compound Pulvule 405 (Acetylsalicylic Acid + Caffeine + Dextropropoxyphene Napsylate)
  • Dolomine 37 (Acetylsalicylic Acid + Caffeine)
  • Dristan Capsules (Acetylsalicylic Acid + Caffeine + Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  • Emercidin D Tab (Acetaminophen + Caffeine + Diphenylpyraline Hydrochloride + Phenylpropanolamine Hydrochloride)
  • Emertabs Tab (Acetaminophen + Caffeine + Phenylpropanolamine Hydrochloride)
  • Ergodryl Cap (Caffeine Citrate + Diphenhydramine Hydrochloride + Ergotamine Tartrate)
  • Excedrin (Acetaminophen + Caffeine)
  • Excedrin Extra-Strength (Acetaminophen + Caffeine)
  • Excedrin Tab (Acetaminophen + Caffeine)
  • Exdol 15tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • Exdol 30tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • Exdol 8 Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • Exdol-15 Tablets (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • Exdol-30 Tablets (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • Exdol-8 Tablets (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • Extra Strength Acetaminophen, Caffeine & 8mg Codeine Phosphate Caplets (Acetaminophen + Caffeine + Codeine Phosphate)
  • Extra Strength Midol (Acetylsalicylic Acid + Caffeine)
  • Fiorinal C1/2 Cap (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate)
  • Fiorinal C1/4 Cap (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate)
  • Fiorinal Cap (Acetylsalicylic Acid + Butalbital + Caffeine)
  • Fiorinal Tab (Acetylsalicylic Acid + Butalbital + Caffeine)
  • Gravergol Capsules (Caffeine + Dimenhydrinate + Ergotamine Tartrate)
  • Herbopyrine Tab 325mg (Acetylsalicylic Acid + Caffeine Citrate)
  • Instantine - Tab (Acetylsalicylic Acid + Caffeine)
  • Instantine - Tablets (Acetylsalicylic Acid + Caffeine)
  • Instantine Tab (Acetylsalicylic Acid + Caffeine)
  • Madelon (Acetylsalicylic Acid + Caffeine)
  • Megral Tabs (Caffeine + Cyclizine Hydrochloride + Ergotamine Tartrate)
  • Midol - Caplet (Acetylsalicylic Acid + Caffeine + Cinnamedrine)
  • Midol Extra Strength Gelcaps (Acetaminophen + Caffeine + Pyrilamine Maleate)
  • Midol Extra Strength Menstrual (Acetaminophen + Caffeine + Pyrilamine Maleate)
  • Midol Menstrual Formula - Caplet (Acetylsalicylic Acid + Caffeine)
  • Midol Multi-Symptom Caplets Extra Strength (Acetaminophen + Caffeine + Pyrilamine Maleate)
  • Midol Multi-Symptom Gelcap Extra Strength (Acetaminophen + Caffeine + Pyrilamine Maleate)
  • Midol Regular (Acetylsalicylic Acid + Caffeine)
  • Midol Tab (Acetylsalicylic Acid + Caffeine + Cinnamedrine)
  • Neo Tigol Tab (Acetylsalicylic Acid + Aluminum Hydroxide + Caffeine + Magnesium Hydroxide + Passion Flower + Valerian)
  • Nervine (Acetylsalicylic Acid + Caffeine)
  • Nervine Tab (Acetylsalicylic Acid + Caffeine)
  • Norgesic Forte Tab (Acetylsalicylic Acid + Caffeine + Orphenadrine Citrate)
  • Norgesic Tab (Acetylsalicylic Acid + Caffeine + Orphenadrine Citrate)
  • Novo AC and C 8mg Tab (Acetylsalicylic Acid + Caffeine + Codeine Phosphate)
  • Novo-Gesic C15 (Acetaminophen + Caffeine + Codeine Phosphate)
  • Novo-Gesic C30 (Acetaminophen + Caffeine + Codeine Phosphate)
  • Novo-Gesic-C8 (Acetaminophen + Caffeine + Codeine Phosphate)
  • Novo-Propoxyn Compound Cap (Acetylsalicylic Acid + Caffeine + Dextropropoxyphene Hydrochloride)
  • Oradrine 2 Tab (Acetaminophen + Caffeine + Diphenylpyraline Hydrochloride + Phenylpropanolamine Hydrochloride)
  • Oradrine Tablets (Acetaminophen + Caffeine + Codeine Phosphate + Diphenylpyraline Hydrochloride + Phenylpropanolamine Hydrochloride)
  • Oradrine-2 Tab (Acetaminophen + Caffeine + Diphenylpyraline Hydrochloride + Phenylpropanolamine Hydrochloride)
  • Pain Aid (Acetylsalicylic Acid + Caffeine)
  • Painex Tab 0.25gr (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  • Painex Tab 0.5gr (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate)
  • Ratio-Lenoltec No 1 (Acetaminophen + Caffeine + Codeine Phosphate)
  • Ratio-Lenoltec No 2 (Acetaminophen + Caffeine + Codeine Phosphate)
  • Ratio-Lenoltec No 3 (Acetaminophen + Caffeine + Codeine Phosphate)
  • Ratio-Tecnal (Acetylsalicylic Acid + Butalbital + Caffeine)
  • Ratio-Tecnal C 1/2 (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate)
  • Ratio-Tecnal C1/4 (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate)
  • Sinugex 38 (Acetaminophen + Caffeine + Diphenylpyraline Hydrochloride)
  • Triaminicin Colds & Flu Caplets (Acetaminophen + Caffeine + Pheniramine Maleate + Phenylpropanolamine Hydrochloride + Pyrilamine Maleate)
  • Trianal Capsules (Acetylsalicylic Acid + Butalbital + Caffeine)
  • Trianal Tablet (Acetylsalicylic Acid + Butalbital + Caffeine)
  • Trianal-C 1/2 Capsule (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate)
  • Triatec-8 Fort Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • Triatec-8 Tab (Acetaminophen + Caffeine Citrate + Codeine Phosphate)
  • Tylenol No 1 Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  • Tylenol No.1 Caplets (Acetaminophen + Caffeine + Codeine Phosphate)
  • Tylenol No.1 Forte Caplets (Acetaminophen + Caffeine + Codeine Phosphate)
  • Tylenol No1 Forte Tablets with Codeine (Acetaminophen + Caffeine + Codeine Phosphate)
  • Tylenol Ultra Relief (Acetaminophen + Caffeine)
  • Tylenol with Codeine No. 2 - Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  • Tylenol with Codeine No. 3 - Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  • Tylenol with Codeine No2 Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  • Tylenol with Codeine No3 Tab (Acetaminophen + Caffeine + Codeine Phosphate)
  • Ultra Headache Relief (Acetaminophen + Caffeine)
  • Wigraine Suppositories (Belladonna + Caffeine + Ergotamine Tartrate)
  • Wigraine Tab (Belladonna + Caffeine + Ergotamine Tartrate)

PharmGKB Accession Id:
PA448710

Description

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.

Source: Drug Bank

Indication

For management of fatigue, orthostatic hypotension, and for the short term treatment of apnea of prematurity in infants.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Caffeine stimulates medullary, vagal, vasomotor, and respiratory centers, promoting bradycardia, vasoconstriction, and increased respiratory rate. This action was previously believed to be due primarily to increased intracellular cyclic 3',5'-adenosine monophosphate (cyclic AMP) following inhibition of phosphodiesterase, the enzyme that degrades cyclic AMP. It is now thought that xanthines such as caffeine act as antagonists at adenosine-receptors within the plasma membrane of virtually every cell. As adenosine acts as an autocoid, inhibiting the release of neurotransmitters from presynaptic sites but augmenting the actions of norepinephrine or angiotensin, antagonism of adenosine receptors promotes neurotransmitter release. This explains the stimulatory effects of caffeine. Blockade of the adenosine A1 receptor in the heart leads to the accelerated, pronounced "pounding" of the heart upon caffeine intake.

Source: Drug Bank

Pharmacology

Caffeine, a naturally occurring xanthine derivative like theobromine and the bronchodilator theophylline, is used as a CNS stimulant, mild diuretic, and respiratory stimulant (in neonates with apnea of prematurity). Often combined with analgesics or with ergot alkaloids, caffeine is used to treat migraine and other headache types. Over the counter, caffeine is available to treat drowsiness or mild water-weight gain.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic cytochrome P450 1A2 (CYP 1A2) is involved in caffeine biotransformation. About 80% of a dose of caffeine is metabolized to paraxanthine (1,7-dimethylxanthine), 10% to theobromine (3,7-dimethylxanthine), and 4% to theophylline (1,3-dimethylxanthine).

Source: Drug Bank

Protein Binding

Low (25 to 36%).

Source: Drug Bank

Absorption

Readily absorbed after oral or parenteral administration. The peak plasma level for caffeine range from 6-10mg/L and the mean time to reach peak concentration ranged from 30 minutes to 2 hours.

Source: Drug Bank

Half-Life

3 to 7 hours in adults, 65 to 130 hours in neonates

Source: Drug Bank

Toxicity

LD 50=127 mg/kg (orally in mice)

Source: Drug Bank

Route of Elimination

In young infants, the elimination of caffeine is much slower than that in adults due to immature hepatic and/or renal function.

Source: Drug Bank

Volume of Distribution

Source: Drug Bank

Chemical Properties

Chemical Formula

C8H10N4O2

Source: Drug Bank

Isomeric SMILES

Cn1cnc2c1c(=O)n(c(=O)n2C)C

Source: OpenEye

Canonical SMILES

CN1C=NC2=C1C(=O)N(C)C(=O)N2C

Source: Drug Bank

Average Molecular Weight

194.1906

Source: Drug Bank

Monoisotopic Molecular Weight

194.080375584

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Caffeine Pathway, Pharmacokinetics
    Stylized liver cell showing candidate genes involved in the metabolism of caffeine.
  1. Theophylline Pathway, Pharmacokinetics
    Schematic representation of theophylline metabolism in human liver.

External Pathways

Links to non-PharmGKB pathways.

  1. Aromatic amines can be N-hydroxylated or N-dealkylated by CYP1A2 - (Reactome via Pathway Interaction Database)

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ADORA1 (source: Drug Bank)
ADORA2A (source: Drug Bank)
PDE4B (source: Drug Bank)
RYR1 (source: Drug Bank)

Drug Interactions

Drug Description
caffeine The quinolone increases the effect and toxicity of caffeine (source: Drug Bank)
caffeine The quinolone increases the effect and toxicity of caffeine (source: Drug Bank)
caffeine Caffeine increases the effect and toxicity of clozapine (source: Drug Bank)
caffeine Caffeine increases the effect and toxicity of clozapine (source: Drug Bank)
caffeine The quinolone increases the effect and toxicity of caffeine (source: Drug Bank)
caffeine The quinolone increases the effect and toxicity of caffeine (source: Drug Bank)
caffeine Caffeine decreases serum levels of lithium (source: Drug Bank)
caffeine Caffeine decreases serum levels of lithium (source: Drug Bank)
caffeine The quinolone increases the effect and toxicity of caffeine (source: Drug Bank)
caffeine The quinolone increases the effect and toxicity of caffeine (source: Drug Bank)
caffeine Caffeine, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Caffeine is initiated, discontinued, or dose changed. (source: Drug Bank)
caffeine Caffeine, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Caffeine is initiated, discontinued, or dose changed. (source: Drug Bank)
caffeine Terbinafine may increase the plasma concentration of Caffeine. (source: Drug Bank)
caffeine The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Caffeine by decreasing Caffeine metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Caffeine if Thiabendazole is initiated, discontinued or dose changed. (source: Drug Bank)
caffeine Caffeine may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
caffeine Caffeine may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
caffeine The CYP3A4 inhibitor, Caffeine, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Caffeine is initiated, discontinued or dose changed. (source: Drug Bank)
caffeine The CYP3A4 inhibitor, Caffeine, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Caffeine is initiated, discontinued or dose changed. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to caffeine: 86

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for N-acetyltransferase 2. Pharmacogenetics and genomics. 2014. McDonagh Ellen M, et al. PubMed
Comparison of N-acetyltransferase-2 enzyme genotype-phenotype and xanthine oxidase enzyme activity between Swedes and Koreans. Journal of clinical pharmacology. 2012. Djordjevic Natasa, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for cytochrome P-450, family 2, subfamily A, polypeptide 6. Pharmacogenetics and genomics. 2012. McDonagh Ellen M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: caffeine pathway. Pharmacogenetics and genomics. 2012. Thorn Caroline F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
alcohol, smoking, and caffeine in relation to fecundability, with effect modification by NAT2. Annals of epidemiology. 2011. Taylor Kira C, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
ADORA2A Gene Variation, Caffeine, and Emotional Processing: A Multi-level Interaction on Startle Reflex. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2011. Domschke Katharina, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP1A2. Pharmacogenetics and genomics. 2011. Thorn Caroline F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Impact of Smoking, Smoking Cessation, and Genetic Polymorphisms on CYP1A2 Activity and Inducibility. Clinical pharmacology and therapeutics. 2011. Dobrinas M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
N-Acetyltransferase-2 (NAT2) gene polymorphisms and enzyme activity in Serbs: unprecedented high prevalence of rapid acetylators in a White population. Journal of clinical pharmacology. 2011. Djordjevic Natasa, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Sequence variants at CYP1A1-CYP1A2 and AHR associate with coffee consumption. Human molecular genetics. 2011. Sulem Patrick, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Caffeine activates tumor suppressor PTEN in sarcoma cells. International journal of oncology. 2011. Miwa Shinji, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genistein alters caffeine exposure in healthy female volunteers. European journal of clinical pharmacology. 2011. Chen Yao, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Genome-Wide Meta-Analysis Identifies Regions on 7p21 (AHR) and 15q24 (CYP1A2) As Determinants of Habitual Caffeine Consumption. PLoS genetics. 2011. Cornelis Marilyn C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Coffee, ADORA2A, and CYP1A2: the caffeine connection in Parkinson's disease. European journal of neurology : the official journal of the European Federation of Neurological Societies. 2011. Popat R A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Methylxanthines and pain. Handbook of experimental pharmacology. 2011. Sawynok Jana. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association of the anxiogenic and alerting effects of caffeine with ADORA2A and ADORA1 polymorphisms and habitual level of caffeine consumption. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2010. Rogers Peter J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Caffeine, selected metabolic gene variants, and risk for neural tube defects. Birth defects research. Part A, Clinical and molecular teratology. 2010. Schmidt Rebecca J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Higher serum caffeine in smokers with schizophrenia compared to smoking controls. Drug and alcohol dependence. 2010. Gandhi Kunal K, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Induction of CYP1A2 by heavy coffee consumption is associated with the CYP1A2 -163C>A polymorphism. European journal of clinical pharmacology. 2010. Djordjevic Natasa, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Polymorphisms of caffeine metabolism and estrogen receptor genes and risk of Parkinson's disease in men and women. Parkinsonism & related disorders. 2010. Palacios N, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
In vivo evaluation of CYP2A6 and xanthine oxidase enzyme activities in the Serbian population. European journal of clinical pharmacology. 2010. Djordjevic Natasa, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
A Phenotype-Genotype Approach to Predicting CYP450 and P-Glycoprotein Drug Interactions With the Mixed Inhibitor/Inducer Tipranavir/Ritonavir. Clinical pharmacology and therapeutics. 2010. Dumond J B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
VKORC1, CYP2C9 and CYP4F2 genetic-based algorithm for warfarin dosing: an Italian retrospective study. Pharmacogenomics. 2010. Zambon Carlo-Federico, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effects of caffeine in Parkinson's disease: from neuroprotection to the management of motor and non-motor symptoms. Journal of Alzheimer's disease : JAD. 2010. Prediger Rui D S. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
A mathematical model to improve on phenotyping for molecular genetic research in malignant hyperthermia. Pharmacogenetics and genomics. 2009. Ginz Hans F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Coffee intake, variants in genes involved in caffeine metabolism, and the risk of epithelial ovarian cancer. Cancer causes & control : CCC. 2009. Kotsopoulos Joanne, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Coffee consumption, genetic susceptibility and bladder cancer risk. Cancer causes & control : CCC. 2009. Villanueva Cristina M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association between ADORA2A and DRD2 polymorphisms and caffeine-induced anxiety. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2008. Childs Emma, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Coffee, caffeine-related genes, and Parkinson's disease: a case-control study. Movement disorders : official journal of the Movement Disorder Society. 2008. Facheris Maurizio F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacokinetics/genotype associations for major cytochrome P450 enzymes in native and first- and third-generation Japanese populations: comparison with Korean, Chinese, and Caucasian populations. Clinical pharmacology and therapeutics. 2008. Myrand S P, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The relative contribution of human cytochrome P450 isoforms to the four caffeine oxidation pathways: an in vitro comparative study with cDNA-expressed P450s including CYP2C isoforms. Biochemical pharmacology. 2008. Kot Marta, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Caffeine reverses antinociception by amitriptyline in wild type mice but not in those lacking adenosine A1 receptors. Neuroscience letters. 2008. Sawynok Jana, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Structure/function evaluations of single nucleotide polymorphisms in human N-acetyltransferase 2. Current drug metabolism. 2008. Walraven Jason M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Variation in CYP1A2 activity and its clinical implications: influence of environmental factors and genetic polymorphisms. Pharmacogenomics. 2008. Gunes Arzu, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Functional characterization of human xanthine oxidase allelic variants. Pharmacogenetics and genomics. 2008. Kudo Mutsumi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Caffeine as a marker substrate for testing cytochrome P450 activity in human and rat. Pharmacological reports : PR. 2008. Kot Marta, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Association between caffeine intake and risk of Parkinson's disease among fast and slow metabolizers. Pharmacogenetics and genomics. 2007. Tan Eng-King, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Coffee, CYP1A2 genotype and risk of myocardial infarction. Genes & nutrition. 2007. El-Sohemy Ahmed, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacokinetic and pharmacodynamic interactions between zolpidem and caffeine. Clinical pharmacology and therapeutics. 2007. Cysneiros R M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
The 1976C>T polymorphism in the adenosine A2A receptor gene does not affect the vasodilator response to adenosine in humans in vivo. Pharmacogenetics and genomics. 2007. Riksen Niels P, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Genetic polymorphism of the adenosine A2A receptor is associated with habitual caffeine consumption. The American journal of clinical nutrition. 2007. Cornelis Marilyn C, et al. PubMed
Comparisons of CYP1A2 genetic polymorphisms, enzyme activity and the genotype-phenotype relationship in Swedes and Koreans. European journal of clinical pharmacology. 2007. Ghotbi Roza, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
The CYP1A2 genotype modifies the association between coffee consumption and breast cancer risk among BRCA1 mutation carriers. Cancer epidemiology, biomarkers & prevention : a publication of the American Association for Cancer Research, cosponsored by the American Society of Preventive Oncology. 2007. Kotsopoulos Joanne, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
A genetic variation in the adenosine A2A receptor gene (ADORA2A) contributes to individual sensitivity to caffeine effects on sleep. Clinical pharmacology and therapeutics. 2007. R├ętey J V, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Development of the "Inje cocktail" for high-throughput evaluation of five human cytochrome P450 isoforms in vivo. Clinical pharmacology and therapeutics. 2007. Ryu J Y, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
In vivo evaluation of CYP1A2, CYP2A6, NAT-2 and xanthine oxidase activities in a Greek population sample by the RP-HPLC monitoring of caffeine metabolic ratios. Biomedical chromatography : BMC. 2007. Begas E, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Concordance between the deduced acetylation status generated by high-speed: real-time PCR based NAT2 genotyping of seven single nucleotide polymorphisms and human NAT2 phenotypes determined by a caffeine assay. Clinica chimica acta; international journal of clinical chemistry. 2007. Rihs Hans-Peter, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Appropriate phenotyping procedures for drug metabolizing enzymes and transporters in humans and their simultaneous use in the "cocktail" approach. Clinical pharmacology and therapeutics. 2007. Fuhr U, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Coffee, CYP1A2 genotype, and risk of myocardial infarction. JAMA : the journal of the American Medical Association. 2006. Cornelis Marilyn C, et al. PubMed
Cyp2a6 is a principal enzyme involved in hydroxylation of 1,7-dimethylxanthine, a main caffeine metabolite, in humans. Drug metabolism and disposition: the biological fate of chemicals. 2005. Kimura Miyuki, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Caffeine intake, CYP1A2 polymorphism and the risk of recurrent pregnancy loss. Molecular human reproduction. 2005. Sata Fumihiro, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Re-investigation of the concordance of human NAT2 phenotypes and genotypes. Archives of toxicology. 2005. Bolt Hermann M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Nonresponse to clozapine and ultrarapid CYP1A2 activity: clinical data and analysis of CYP1A2 gene. Journal of clinical psychopharmacology. 2004. Eap Chin B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Phenotyping of N-acetyltransferase type 2 by caffeine from uncontrolled dietary exposure. European journal of clinical pharmacology. 2004. Jetter Alexander, et al. PubMed
Genetic polymorphism of CYP1A2 in Ethiopians affecting induction and expression: characterization of novel haplotypes with single-nucleotide polymorphisms in intron 1. Molecular pharmacology. 2003. Aklillu Eleni, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association between A2a receptor gene polymorphisms and caffeine-induced anxiety. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2003. Alsene Karen, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Polymorphisms in the CYP1A2 gene and theophylline metabolism in patients with asthma. Clinical pharmacology and therapeutics. 2003. Obase Yasushi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Association of caffeine intake and CYP1A2 genotype with ovarian cancer. Nutrition and cancer. 2003. Goodman Marc T, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Update on caffeine consumption, disposition and action. Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association. 2002. Mandel H G. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The interindividual differences in the 3-demthylation of caffeine alias CYP1A2 is determined by both genetic and environmental factors. Pharmacogenetics. 2002. Rasmussen Birgitte B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Inducibility of CYP1A2 by omeprazole in vivo related to the genetic polymorphism of CYP1A2. British journal of clinical pharmacology. 2002. Han Xing-Mei, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Analysis of six SNPs of NAT2 in Ngawbe and Embera Amerindians of Panama and determination of the Embera acetylation phenotype using caffeine. Pharmacogenetics. 2002. Jorge-Nebert Lucia F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Molecular action of methotrexate in inflammatory diseases. Arthritis research. 2002. Chan Edwin S L, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Caffeine metabolism and the risk of spontaneous abortion of normal karyotype fetuses. Obstetrics and gynecology. 2001. Signorello L B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Med-psych drug-drug interactions update. Psychosomatics. 2002. Armstrong Scott C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Correlation between acetylation phenotype and genotype in Chinese women. European journal of clinical pharmacology. 2000. Zhao B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Prospective evaluation of detoxification pathways as markers of cutaneous adverse reactions to sulphonamides in AIDS. Pharmacogenetics. 2000. Wolkenstein P, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Reversal of the antiinflammatory effects of methotrexate by the nonselective adenosine receptor antagonists theophylline and caffeine: evidence that the antiinflammatory effects of methotrexate are mediated via multiple adenosine receptors in rat adjuvant arthritis. Arthritis and rheumatism. 2000. Montesinos M C, et al. PubMed
Functional significance of a C-->A polymorphism in intron 1 of the cytochrome P450 CYP1A2 gene tested with caffeine. British journal of clinical pharmacology. 1999. Sachse C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Genetic polymorphism in the 5'-flanking region of human CYP1A2 gene: effect on the CYP1A2 inducibility in humans. Journal of biochemistry. 1999. Nakajima M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Rate of caffeine metabolism and risk of spontaneous abortion. American journal of epidemiology. 1998. Fenster L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Meta-analysis of phenotype and genotype of NAT2 deficiency in Chinese populations. Pharmacogenetics. 1997. Xie H G, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
N-acetylation among HIV-positive patients and patients with AIDS: when is fast, fast and slow, slow?. Clinical pharmacology and therapeutics. 1997. O'Neil W M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Imipramine demethylation in vivo: impact of CYP1A2, CYP2C19, and CYP3A4. Clinical pharmacology and therapeutics. 1997. Madsen H, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
N-acetyltransferase 2 polymorphism in patients infected with human immunodeficiency virus. Clinical pharmacology and therapeutics. 1996. Kaufmann G R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Predictors of N-acetyltransferase activity: should caffeine phenotyping and NAT2 genotyping be used interchangeably in epidemiological studies?. Cancer epidemiology, biomarkers & prevention : a publication of the American Association for Cancer Research, cosponsored by the American Society of Preventive Oncology. 1996. Le Marchand L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Sympathomimetic effects of paraxanthine and caffeine in humans. Clinical pharmacology and therapeutics. 1995. Benowitz N L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
CYP2D6, N-acetylation, and xanthine oxidase activity in cystic fibrosis. Pharmacotherapy. 1996. Bosso J A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Arylamine N-acetyltransferase (NAT2) mutations and their allelic linkage in unrelated Caucasian individuals: correlation with phenotypic activity. American journal of human genetics. 1995. Cascorbi I, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The use of caffeine for enzyme assays: a critical appraisal. Clinical pharmacology and therapeutics. 1993. Kalow W, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Biotransformation of caffeine, paraxanthine, theobromine and theophylline by cDNA-expressed human CYP1A2 and CYP2E1. Pharmacogenetics. 1992. Gu L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Acetylation pharmacogenetics. The slow acetylator phenotype is caused by decreased or absent arylamine N-acetyltransferase in human liver. The Journal of clinical investigation. 1990. Grant D M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
N-acetylation pharmacogenetics. Pharmacological reviews. 1985. Weber W W, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
A simple test for acetylator phenotype using caffeine. British journal of clinical pharmacology. 1984. Grant D M, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
63323-406-03
DrugBank:
DB00201
PDB:
CFF
ChEBI:
27732
KEGG Compound:
C07481
KEGG Drug:
D00528
PubChem Compound:
2519
PubChem Substance:
148854
46506408
IUPHAR Ligand:
407
Drugs Product Database (DPD):
2241831
BindingDB:
10849
ChemSpider:
2424
HET:
CFF
Therapeutic Targets Database:
DAP000099
FDA Drug Label at DailyMed:
b4fb7c77-1e82-48b7-83c5-dd04ec7c5c4e

Clinical Trials

These are trials that mention caffeine and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.