Mandibular and parotid salivary excretion of procainamide and N-acetylprocainamide after intravenous administration of procainamide to rats.
Flow rate, protein level and pH of mandibular and parotid saliva samples in rats were almost stabilized 2 h after induction of salivation with pilocarpine (9.0 mg h-1 kg-1). Salivary excretion profiles of procainamide, 50 mg kg-1 i.v., and its metabolite N-acetylprocainamide (NAPA) were then investigated. Plasma and salivary procainamide levels declined bi-exponentially with time almost in parallel. Salivary procainamide levels (Y) from both types of gland were correlated with the plasma level (X) over a wide concentration range [Y = 0.108X + 1.96 (r = 0.795) for mandibular and Y = 0.917X (r = 0.974) for parotid glands]. The mean saliva to plasma concentration ratio (S/P ratio) was significantly higher in parotid (0.974 +/- 0.243) than in mandibular (0.284 +/- 0.119) saliva samples. Similar correlations and S/P ratios were observed for NAPA. Procainamide and NAPA mean S/P ratios for saliva from both glands were fairly consistent with the calculated value according to the pH-partition hypothesis.
D000120:Acecainide / Q000097:blood / Q000493:pharmacokinetics*; D000818:Animals; D007275:Injections, Intravenous; D008297:Male; D010306:Parotid Gland / Q000378:metabolism; D011342:Procainamide / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism / Q000493:pharmacokinetics*; D051381:Rats; D011919:Rats, Inbred Strains; D012463:Saliva / Q000378:metabolism*; D013363:Submandibular Gland / Q000378:metabolism
D000120:Acecainide; D011342:Procainamide