Degradation Situations That Can Affect the Safety of Drug Products
| Product | Degradation | Effect | Reference |
|---|---|---|---|
| Tetracycline | Epimerization under acidic conditions forms anhydrotetracycline and 4-epitetracycline | Reversible Fanconi syndrome | (71, 72) |
| Meropenem (solution) | Alkaline conditions and thermal degradation may yield 4-methyl-3- (1H-pyrrol-3-ylsulfanyl)-5H-pyrrole-2-carboxylic acid and other degradants | High concentrations of degraded samples demonstrate in vitro cytotoxic activity in mononuclear cells after 48h | (73) |
| Chloramphenicol | Photo-oxidation | Inhibition of antibiotic activity | (74) |
| Isoniazid | Hydrolytic degradation at high temperatures forms hydrazine | Genotoxicity and carcinogenicity in animal models | (75, 32) |
| Ibuprofen | Oxidation and photodegradation can result in the generation of 1-(4-isobutylphenyl)-1-ethanol | Cytotoxicity to fibroblasts at concentrations above 1mM | (76, 77) |
| Ascorbic acid | Dehydration and hydrolysis under anaerobic conditions may yield furfural | Hepatotoxity in rats | (78) |
| Enalapril maleate (tablets) | High temperature and humidity can form enalaprilat and a diketopiperazine derivative | Change in the dissolution profile, impairment of drug bioavailability and decrease in the effectiveness | (79) |
| Pethidine | Hydrolytic degradation of an ester group can generate N-methyl-4-phenyl-1,2,3,6 tetrahydropyridine (MPTP) | Severe and irreversible symptoms of Parkinson's disease | (80) |
| Lidocaine | Hydrolytic degradation generates 2.6-xylidine | Anoxia and damage to the hematopoietic system | (81–83) |
| Gabapentin | Intramolecular cyclization can form the β-lactam 3,3-pentamethylene-4-butyrolactam(2-azaspiro[4,5]decan-3-one) | Induction of seizures in animal models | (84) |