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  • venoconstriction  (3)
  • venous compliance  (2)
  • beta-blockade  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 7 (1974), S. 137-139 
    ISSN: 1432-1041
    Keywords: Dihydroergotamine ; phentolamine ; venoconstriction ; venous compliance ; α-adrenoceptor blockade
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of dihydroergotamine on superficial veins of the hand has been investigated in healthy volunteers. The compliance of the veins was assessed by measurement of their diameter at a standard congestion pressure. Direct local infusion into the vein under study of 0.4 µg and 2.0 µg dihydroergotamine reduced venous compliance by 15±5% and 30±3%, respectively. Local infusion of phentolamine 20 µg, an α-adrenoceptor blocking drug, did not affect venous compliance, but markedly inhibited the venoconstrictor effect of dihydroergotamine 2 µg. It was concluded that the venoconstrictor effect of dihydroergotamine demonstrated in this experiment was mainly due to α-adrenoceptor stimulation. Venous compliance also decreased after oral administration of dihydroergotamine 10 mg; after 150 min, venous diameter was reduced by 30±5%.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: pindolol ; beta-blockade ; slow release tablet ; plasma levels ; urinary excretion ; pharmacokinetics ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 10 healthy volunteers the time course of cardiac beta-adrenoceptor blocking activity, plasma levels and cumulative urinary excretion of pindolol were compared during a 4-day course of pindolol 5 mg (Visken®) t. d. s., and one tablet of pindolol 20 mg retard (Visken® retard) once a day. After oral administration of the 20 mg retard tablet, plasma concentrations of pindolol higher than half the maximum value (1/2 Cp (tmax)) were maintained about 2.5 times as long as after administration of the conventional 5 mg tablet. This is evidence for an important and marked retardation of drug release. During treatment with pindolol 20 mg retard once daily, cardiac beta-adrenoceptor blockade, measured by the reduction in exercise-induced tachycardia and in the exercise-induced rise in systolic blood pressure, at almost all times throughout the 24 h period was at least as great as during treatment with pindolol 5 mg t. d. s. This suggests that patients successfully treated with pindolol 5 mg t. d. s. can be maintained with the same beta-adrenoceptor blockade by a single tablet of pindolol 20 mg retard once daily.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 30 (1986), S. 581-584 
    ISSN: 1432-1041
    Keywords: dihydroergotamine ; venoconstriction ; nasal spray ; healthy volunteers ; i.m. administration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A parenteral formulation of dihydroergotamine (DHE) is the only galenical form now available for the treatment of acute attacks of migraine in which a rapid onset of action is required. A recently developed nasal spray of DHE has been compared with intramuscular DHE for its venoconstrictor activity. In a randomised double-blind, cross-over trial, 9 healthy male volunteers received a single dose of DHE 1 mg intranasally, DHE 0.5 mg i.m. or placebo (intranasally and i.m.) on three different occasions, with an interval of at least 1 week between doses. Both active treatments, but not placebo, produced marked venoconstriction as shown by reduced compliance of superficial hand veins. The effect persisted for more than 8 h. The maximum venoconstrictor effect of 1 mg DHE intransally was 40±12% (mean ± SEM) and after 0.5 mg i.m. it was 52±15%. The time course of the venoconstrictor effect was similar after both routes of administration. Blood pressure and heart rate changes in these normotensive subjects were almost identical after dihydroergotamine and placebo. The results suggest that the nasal spray could be used as an alternative to parenteral DHE, permitting self-administration of the drug for the treatment of acute attacks of migraine.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 26 (1984), S. 239-242 
    ISSN: 1432-1041
    Keywords: dihydroergotamine ; venoconstriction ; 8′ hydroxy-dihydroergotamine ; main metabolite in man ; time course
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The time course of the venoconstrictor effect of dihydroergotamine and its main metabolite 8′ hydroxy-dihydroergotamine was investigated in a placebo-controlled study in seven healthy male volunteers, after direct local infusion of 0.08 and 0.4 µg into superficial hand veins. Both dihydroergotamine and 8′ hydroxy-dihydroergotamine elicited a similar, marked venoconstrictor effect. The time course of the venoconstrictor action was similar for both compounds; about one third of the effect was present at the end of the infusion, which lasted for 10 min, and it took about a further 20 min for the effect to reach its maximum. The effect then remained fairly constant for the rest of the period of observation of 180 min from the start of the infusion. The data indicate that the pharmacological activity of oral dihydroergotamine is due not only to the unchanged drug but also to its main metabolite, 8′ hydroxy-dihydroergotamine, which occurs in plasma in concentrations about 5–7 times higher than those of dihydroergotamine itself. The absolute bioavailability of unchanged dihydroergotamine, therefore, does not reflect the markedly higher bioavailability of pharmacologically active drug.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 25 (1983), S. 759-762 
    ISSN: 1432-1041
    Keywords: pizotifen ; ergotamine ; venous tone ; 5-hydroxytryptamine ; noradrenaline ; venous compliance ; venous constriction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of locally infused pizotifen (80 ng) and ergotamine (16 ng and 4 ng) on the compliance of superficial hand veins in man, and their interactions with the venoconstrictor effects of noradrenaline and 5-hydroxytryptamine (5-HT), were investigated in a placebo-controlled study in healthy volunteers. Pizotifen alone reduced venous compliance and produced a parallel displacement to the right of the 5-HT dose-response curve suggestive of competitive antagonism. The venoconstrictor effect of noradrenaline was not influenced by pizotifen. This confirms the selective antagonism of 5-HT by pizotifen and supports the existence of specific 5-HT receptors on human veins. After infusion of 16 ng ergotamine, which by itself reduced venous compliance, the venoconstrictor effects of the lower doses of 5-HT and of all doses of noradrenaline were larger but still never exceeded the arithmetic sum of the separate effects of noradrenaline or 5-HT and ergotamine. A lower dose of ergotamine (4 ng) induced only a small venoconstriction and did not influence the constrictor effect of noradrenaline. Therefore, in contrast to previous observations, no potentiation of the venoconstrictor effect of noradrenaline by ergotamine was observed under the present experimental conditions. The additive effect of noradrenaline and ergotamine may well explain its therapeutic action in the treatment of migraine.
    Type of Medium: Electronic Resource
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