Mandibular and parotid salivary excretion of procainamide and N-acetylprocainamide after intravenous administration of procainamide to rats

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Abstract
Flow rate, protein level and pH of mandibular and parotid saliva samples in rats were almost stabilized 2h after induction of salivation with pilocarpine (9ṁ0 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 = 0ṁ108X + 1ṁ96 (r = 0ṁ795) for mandibular and Y = 0ṁ917X (r = 0ṁ974) for parotid glands]. The mean saliva to plasma concentration ratio (S/P ratio) was significantly higher in parotid (0ṁ974 ± 0ṁ243) than in mandibular (0ṁ284 05119) 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.