Sublingual drugs, pharmacokinetic

Caille G, Spenard J, Lacasse Y, et al Pharmacokinetics of two lorazepam formulations, oral and sublingual, after multiple doses. Biopharm Drug Dispos 4 31—42, 1983... 

Motwani, J.G. and Lipworth, B.J. (1991) Clinical pharmacokinetics of drugs administered buccally and sublingually. Clin. Pharmacokin., 21 83-94. 

Other nitrates are similar to nitroglycerin in their pharmacokinetics and pharmacodynamics. Isosorbide dinitrate is another commonly used nitrate it is available in sublingual and oral forms. Isosorbide dinitrate is rapidly denitrated in tbe liver to isosorbide mononitrate, which is also active. Isosorbide mononitrate is available as a separate drug for oral use. Several other nitrates are available for oral use and, like the oral nitroglycerin preparation, have an intermediate duration of action (4-6 hours). Amyl nitrite is a volatile and rapidly acting vasodilator that was used for angina by the inhalational route but is now rarely prescribed. 

Because it is easy to administer and has satisfactory pharmacokinetics, sublingual tacrolimus is an attractive option when the oral route is prohibited. In a retrospective analysis of 17 lung and heart transplant patients, tacrolimus was administered sublingually and 90% of blood concentrations were within the target range [153 ]. Acute rejection episodes, renal toxicity, and drug interactions were not observed. 

---