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Besides rebound congestion, persistent use of a decongestant entails the risk of atrophic damage caused by prolonged hypoxia of the nasal mucosa. ?-Sympatholytics (B). The interaction of norepinephrine with ?-adrenoceptors can be inhibited by ?-sympatholytics ( ?-adrenoceptor antagonists, ?- blockers).
Having entered the blood, drugs may bind to the protein molecules that are present in abundance, resulting in the formation of drug-protein complexes. Protein binding involves primarily albumin and, to a lesser extent, ?-globulins and acidic glycoproteins. Other plasma proteins serve specialized functions in connection with specific substances.

 

Biotransformation begins either at substituents on the diazepine ring (diazepam: N-dealkylation at position 1; midazolam: hydroxylation of the methyl group on the imidazole ring) or at the diazepine ring itself. Hydroxylated midazolam is quickly eliminated following glucuronidation (t1/2 ~ 2 h).
Capsules usually consist of an oblong casing — generally made of gelatin — that contains the drug in powder or granulated form (See. p. 9, C). In the case of the matrix-type tablet, the drug is embedded in an inert meshwork from which it is released by diffusion upon being moistened.

 

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