Drug intelligence / Profile preview

caffeine + propranolol

Development stage
Phase 2
Lead developer
Stanford University
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Caffeine + propranolol is a combination of two active pharmaceutical ingredients, caffeine and propranolol. Caffeine is a central nervous system stimulant of the methylxanthine class, commonly used to promote wakefulness and as an adjuvant in pain relief medications. Propranolol is a non-selective beta-adrenergic receptor antagonist (beta blocker) used primarily for the treatment of hypertension, angina pectoris, arrhythmias, migraine prophylaxis, essential tremor, and anxiety. The combination does not have a widely recognized or marketed fixed-dose formulation but may be co-administered in clinical practice for specific indications such as migraine management or to counteract certain side effects (e.g., performance anxiety with fatigue). Caffeine acts by antagonizing adenosine receptors leading to increased alertness and mild vasoconstriction; propranolol blocks beta-1 and beta-2 adrenergic receptors resulting in decreased heart rate, contractility, blood pressure reduction, and inhibition of sympathetic nervous system activity[3][4][7][8]. There are no major direct pharmacological interactions between these two drugs; however, caffeine can reduce the antihypertensive effect of propranolol due to its pressor action[2][9].

02

Targets

ADORA1 (Adenosine receptor A1 subtype)ADORA2A (Adenosine A₂A Receptor)ADORA2B (Adenosine A2B receptor)ADORA3 (Adenosine A3 receptor)ADRB1 (β1)ADRB2 (β2)ADRB3 (β3)ADOR (Adenosine receptors)

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