Pharmacodynamic methods for investigating antiasthma drugs in healthy volunteers.

The investigation of bronchoactive drugs in healthy volunteers may be divided into studies on the drug effects on basal airway calibre, the effects on induced bronchoconstriction and the examination of the pharmacokinetic and side effect profile of new chemical entities. In the studies presented in this paper, whole body plethysmography was used to assess the pharmacological activity of three new development compounds. In the first example, bronchodilatation was measured after administration of an anticholinergic drug.

Phase I clinical trials with WAL 2014, a new muscarinic agonist for the treatment of Alzheimer's disease.

The safety, tolerability and pharmacological activity of WAL 2014, a new centrally-acting M1 agonist were examined in two clinical studies (0.5-80 mg and 100-160 mg). Single increasing p.

Neuroendocrine and side effect profile of pramipexole, a new dopamine receptor agonist, in humans.

The effects and tolerability of pramipexole, a new dopamine D2-receptor agonist, on prolactin, human growth hormone, thyrotropin, cortisol, and corticotropin levels were investigated in a randomized, double-blind, crossover study in 12 healthy volunteers. Single oral doses of 0.1, 0.

Pharmacodynamics, pharmacokinetics and safety profile of the new platelet-activating factor antagonist apafant in man.

Platelet-activating factor (PAF) is a unique phospholipid mediator with multifunctional properties. Evidence generated in experimental studies suggests that PAF plays a pathogenetic role in anaphylactic, inflammatory and immunogenic reactions. Apafant (WEB 2086, CAS 105219-56-5), a novel synthetic PAF receptor antagonist, was administered to a total of 101 healthy volunteers within 5 studies to investigate its pharmacologic activity, pharmacokinetic behaviour and safety profile.

Antihistaminic activity and side effect profile of epinastine and terfenadine in healthy volunteers.

New H1-receptor antagonists are assessed not only for their H1 antihistaminic activity but also for their central nervous system (CNS) side effects. Fifteen healthy subjects received a once daily dose of 5 mg, 10 mg or 20 mg of epinastine, or a twice daily dose of 60 mg of terfenadine or placebo in a randomized double-blind (double-dummy) crossover study. The response to histamine-induced skin wheals was compared.