Alprenolol, or alfeprol, alpheprol, and alprenololum, is a non-selective beta blocker as well as a 5-HT1A and 5-HT1B receptor antagonist, used in the treatment of angina pectoris. It is no longer marketed by AstraZeneca, but may still be available from ot + some more technical info; chemically it is a secondary amino alcohol with a single stereocenter usually handled and formulated as the racemate, often isolated as a hydrochloride salt for increased stability and aqueous solubility. The molecule combines a lipophilic aryl-allyl moiety with a basic isopropylamino-propanol side chain, producing central nervous system penetration and mixed peripheral and central pharmacology. From a manufacturing perspective the API is produced by aryloxypropanol formation followed by introduction of the dialkylamino side chain, and typical quality control focuses on residual solvents, chirality, assay, and related substances. Formulation and handling notes include attention to hygroscopicity of some salt forms, pH control in aqueous processes to limit degradation, and characterization by HPLC with UV and mass spectrometric detection for related substances.
Parent: Alprenolol
Parent: Alprenolol
Parent: Alprenolol
Parent: Alprenolol / Alprenolol Hydrochloride
Typical API specification examples used in analytical and regulatory dossiers set assay acceptance at about 98.0 to 102.0 percent on a dried basis, with individual related compounds limited to not more than 0.2 to 0.5 percent each and total related substances not exceeding 1.0 percent, consistent with ICH impurity control principles for many small molecule drugs; genotoxic or controlled impurities are held to tighter limits, commonly below 0.05 percent. Known or expected related compounds observed during synthesis and stability studies include N-desalkyl alprenolol (N-dealkylation product), the deaminated/degraded alcohol derivative, allylic oxidation products on the aryl-allyl side chain, and minor epimeric or dehydration products; routine monitoring employs HPLC with reference standards, MS confirmation for peak identity, and limits for residual solvents and heavy metals per pharmacopeial guidance.
Alprenolol is primarily used in the management of angina pectoris and has been used for other cardiovascular indications such as certain arrhythmias and hypertension in some settings; its clinical use declined after withdrawal by the original marketer, though supplies may be available from other manufacturers.
Other names and synonyms include alfeprol, alpheprol, and alprenololum, and it may appear in older literature or alternative supplier catalogs under those names.
Alprenolol has been used off-label in some situations to blunt peripheral adrenergic symptoms of situational anxiety because of its beta blocking effects and central activity, but it is not a first line anxiolytic and clinical evidence is limited; any off-label use should follow clinician assessment.
Alprenolol blocks beta adrenergic receptors non-selectively, reducing heart rate and myocardial contractility, and it antagonizes 5-HT1A and 5-HT1B receptors, which can modulate central serotonergic signaling; the combined actions produce both peripheral cardiovascular effects and some central nervous system activity.
