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Pharmacology Of Diltiazem Hydrochloride Essay

576 words - 3 pages

Diltiazem Hydrochloride, nondihydropyridine-derivative, is a member of the group of drugs known as benzothiazepines, which are a class of calcium channel blockers, used in the treatment of hypertension, angina pectoris, and some types of arrhythmia. It is a class III anti-anginal drug, and a class IV antiarrhythmic [1]. Diltiazem Hydrochloride exerts its pharmacological action through inhibiting trans-membrane influx of extracellular calcium ions across the membranes of myocardial cells and vascular smooth muscle cells, without changing serum calcium concentrations. It is a peripheral arterial vasodilator that acts directly on vascular smooth muscle causing reduction in peripheral vascular resistance and blood pressure. It possesses substantial inhibitory effects on the cardiac conduction system, acting principally at the atrioventricular (AV) node to slow conduction time and prolong AV nodal refractoriness. In spite of being a corner stone in the treatment and management of hypertension, angina and arrhythmia, it experiences a major pharmacokinetic problem. Despite the fact that following oral administration of diltiazem hydrochloride conventional tablets, approximately 80% of a dose is rapidly absorbed from the gastrointestinal tract, its absolute bioavailability is about 40%. It undergoes extensive first-pass metabolism, where it is rapidly and almost completely metabolized in the liver principally via Cytochrome-P enzyme system, mainly CYP3A4 [2-7].
Intranasal administration represents a viable option for local and systemic delivery of diverse therapeutic compounds [8-16]. The large surface area of the nasal mucosa affords a rapid onset of therapeutic effect, potential for direct-to-central nervous system delivery, no first-pass metabolism, and non-invasiveness; all of which may maximize patient convenience, comfort, and compliance. Drug permeation and systemic bioavailability via the nasal route is influenced by a variety of structural, biochemical,...

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