Essentials of Foye's Principles of Medicinal Chemistry by Thomas L. Lemke & David A. Williams & Victoria F. Roche & S. William Zito

Author:Thomas L. Lemke & David A. Williams & Victoria F. Roche & S. William Zito [Lemke, Thomas L.]
Language: eng
Format: epub
ISBN: 9781496353832
Publisher: LWW
Published: 2016-04-28T17:00:00+00:00

SAR

• Substitutions and their effects on glucocorticoid activity are summarized in Figure 18.13.

Figure 18.13 SAR effects associated with steroid substitution on glucocorticoid (GC) and mineralocorticoid (MC) activity or receptor affinity.

Table 18.4 Pharmacokinetic Properties of Inhaled and Intranasal Corticosteroids

Physicochemical and Pharmacokinetic Properties

• A comparison of the properties of inhaled and intranasal corticosteroids is difficult due to significant variables. The desired properties include:

• high lipophilicity (i.e., log P ≥ 4, BDP, CIC, mometasone furoate, Flu).

• low bioavailability, high systemic clearance leading to short half-life, high protein binding (Table 18.4).

• rapid systemic clearance with inactive metabolites (see below).

• 10% to 30% of an inhaled dose of the corticosteroid is deposited in the respiratory tract, with the remainder of the dose deposited in the mouth and throat where it is swallowed. The swallowed drug is eliminated in the feces usually without significant absorption.

• The device for administering the drug (metered dose inhaler or dry powder inhaler [DPI], and spacer use), and patient skill produce variable activity.

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