Adenosine A1 antagonist
Adenosine A1 receptor antagonist
- Primary effect of caffeine
- ↑ HR and AV conduction
- Enhanced wakefulness/alertness
- Afferent arteriolar vasoconstriction → ↑ glomerular filtration rate (GFR)
- Diuretic effect
- Lipolysis
- ↓ seizure threshold
Drugs with this mechanism (9)
- Aminophylline — Soluble theophylline; a bronchodilator with a narrow therapeutic index.
- Caffeine — The world's most-used stimulant; adenosine antagonist, OTC.
- Carbamazepine — Anticonvulsant/mood stabilizer and potent autoinducer; HLA-B*1502 rash risk.
- Carbamazepine ER capsules — Bead-filled extended-release carbamazepine capsule that can be opened and sprinkled.
- Carbamazepine ER (Equetro) — Carbamazepine ER capsule - the only carbamazepine approved for acute bipolar mania.
- Oxcarbazepine — Carbamazepine analog with less enzyme induction; hyponatremia risk.
- Oxcarbazepine XR — Extended-release oxcarbazepine for focal seizures; hyponatremia and enzyme induction complicate use.
- Carbamazepine XR — Extended-release carbamazepine for seizures and trigeminal neuralgia; potent enzyme inducer.
- Theophylline — Old methylxanthine bronchodilator; narrow index, largely supplanted.
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