Drugs that influence caffeine pharmacokinetics
Data according to Soto et al. (1994), Amchin et al. (1999), Schmider et al. (1999), Carrillo and Benitez (2000 and references therein), Granfors et al. (2004), Culm-Merdek et al. (2005), Backman et al. (2006), Cysneiros et al. (2007), Darwish et al. (2008), Dinger et al. (2016), Yamazachi et al. (2017).
| Drug Class | Name | Effect on Caffeine Half-Life |
|---|---|---|
| Oral contraceptives | All | About +40% |
| Quinolone antibiotics | Ami- and difloxacin | +21% |
| Ciproflacin | +70% | |
| Enoxacin | +75% | |
| Fleroxacin | No effect | |
| Grepafloxacin | +50% | |
| Lomeflaxin | +23% | |
| Nalidixic acid | +67% | |
| Norfloxacin | +35% | |
| Ofloxacin | No effect | |
| Pefloxacin | +22–47% | |
| Pipemidic acid | +59% | |
| Rufloxacin | No effect | |
| Temafloxacin | No effect | |
| Tosufloxacin | +34% | |
| Trovafloxacin | No effect | |
| Cardiovascular drugs | Mexiletine (anti-arrhythmic) | +30%–50% |
| Diltiazem (calcium antagonist) | +22% | |
| Verapamil (calcium antagonist) | +20% | |
| Propafenone (anti-arrhythmic) | Increase | |
| Propranolol (beta-blocker) | Increase | |
| Triamterene (diuretic) | Increase | |
| Warfarin (anticoagulant) | Increase | |
| CNS drugs | Clozapine (antidepressant) | Variable, up to +26% |
| Fluvoxamine (antidepressant) | −80%; decreases caffeine half-life by sixfold | |
| Venlafaxine (antidepressant, serotonin-norepinephrine reuptake inhibitor (SNRI) | No significant effect | |
| Alprazolam (anti-anxiety) | No significant effect | |
| Olanzapine (antipsychotic) (Shirley et al. 2003) | Slows clearance, interindividual variability | |
| Tryptamine derivatives (psychoactive) | Slows caffeine clearance to various degrees | |
| Armodafinil (wakefulness promoting) | No significant effect | |
| Tacrine (cholinesterase inhibitor) | Slows slightly clearance | |
| Zolpidem (Hypnotic) | No significant effect | |
| Anti-inflammatory drugs | Idrocilamide | Half-life increased up to 63 h |
| Rofecoxib | Decreased clearance | |
| Antifungal medication | Fluconazole | + 25% |
| Isavuconazole | No effect | |
| Ketoconazole | + 11% | |
| Terbinafine | + 21% | |
| Proton pump inhibitors | Cimetidine | −31% |
| Lansoprazole | No effect | |
| Omeprazole | −41% | |
| Pantoprazole | No effect | |
| Ondansetron (anti-vomiting) | Slows clearance | |
| Psoralens, anti-psoriasis and anti-eczema drugs | Methoxsalen | −70% |
| 5-Methoxypsoralen | −31% | |
| Bronchodilators | Furafylline | Increases caffeine half-life up to 10-fold |
| Theophylline | Slows caffeine clearance, twofold |