Mucosal delivery systems of antihypertensive drugs: A practical approach in general practice

Abstract

Patients who are unable to receive oral medication (p.o.) are a major problem in outpatient settings, especially in home health care systems. Mucosal administration of drugs offers an alternative to the oral route, especially when the parenteral mode cannot be used. There are three main pathways of mucosal administration: sublingual/buccal, intranasal and rectal. We discuss the possibility of mucosal delivery of antihypertensive drugs. Perindopril arginine and Amlodipine besylate are registered in the EU as orodispersible tablets for oromucosal delivery, however, they are not available in all countries. For this reason, we describe other drugs suitable for mucosal delivery: Captopril and Nitrendipine in the sublingual system and Metoprolol tartrate, Propranolol and Furosemide by the transrectal route. Based on the published data and common clinical practice we discuss the use of mucosal delivery systems of all these antihypertensive drugs with special attention to their pharmacokinetics. We illustrate this mini-review with a case report of the prolonged-term use of mucosal delivery of sublingual Captopril and Nitrendipine combined with rectal Metoprolol tartrate and Furosemide in a patient with severe hypertension unable to receive medication p.o. This is also a report on the first human use of Furosemide-containing suppositories as well as prolonged-term transmucosal administration of these four drugs, describing a practical approach leading to successful control of severe hypertension with four antihypertensive drugs delivered via the mucosal route. The treatment was effective and without side effects; however, the long-term safety and efficacy of such therapy must be confirmed by randomized clinical trials.

Rate of change of circulating 25-hydroxyvitamin D following sublingual and capsular vitamin D preparations

“…A limitation to this study is that we cannot show definitive absorption of the sublingual supplement. However, sublingual routes of drug delivery are established in pharmacokinetic studies 19,20 . Recent research presented by Satia and colleagues found superior sublingual absorption compared to capsules in patients with malabsorption issues 21 preparations.…”

A case report of high-output heart failure due to arteriovenous shunt without bowel: how to address?

“…A recent review has studied the sublingual/buccal and rectal administration of antihypertensive drugs, with the sublingual administration of perindopril and captopril being of the most clinical interest for our case. 10 While perindopril is a prodrug and needs to be activated in the liver into the active metabolite, captopril is not, which may result in faster absorption and higher bioavailability. 10 Sublingually administered drugs reach the systemic circulation by diffusing through the highly vascularized mucosa of the oral cavity, thereby bypassing the gastrointestinal tract and first-pass metabolism in the liver.…”

“… 10 While perindopril is a prodrug and needs to be activated in the liver into the active metabolite, captopril is not, which may result in faster absorption and higher bioavailability. 10 Sublingually administered drugs reach the systemic circulation by diffusing through the highly vascularized mucosa of the oral cavity, thereby bypassing the gastrointestinal tract and first-pass metabolism in the liver. 11 Pharmacokinetic studies of captopril have shown a shorter T max (45 vs. 75 min) for the sublingual administration compared to oral administration, with no significant difference in C max and area under the curve.…”

<p>Bucco-Adhesive Film as a Pediatric Proper Dosage Form for Systemic Delivery of Propranolol Hydrochloride: In-vitro and in-vivo Evaluation</p>

“…As the development of appropriate formulations for kids is a major challenge, various studies have focused on developing new dosage forms for propranolol hydrochloride including buccal formulations in an attempt to overcome these problems. [1][2][3][4] The buccal route has been regularly adopted for the systemic delivery of drugs experiencing hepatic first-pass metabolism 5 or to extend drug release. 6 This route has arisen as an attractive site for pediatrics systemic drug administration.…”