A comparison of bupropion hydrochloride with dexamphetamine and amitriptyline in healthy subjects.

Peck, A. W.; Bye, Carole; Clubley, M; Henson, T; Riddington, C

doi:10.1111/j.1365-2125.1979.tb00988.x

Cited by 83 publications

(44 citation statements)

References 12 publications

(18 reference statements)

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“…It is possible that this apparent elevation after bupropion and nomifensine is spurious and really due to a fortuitously low value obtained after lactose. This increase in heart rate was not seen in the previous study after bupropion 100 mg (Peck et al, 1979) but in that study supine systolic blood pressure was increased compared with lactose after all treatments except bupropion 50 mg. This finding was ascribed to a spuriously low value after lactose and this explanation was probably correct, the finding not being replicated for bupropion in the present study despite the increased dose.…”

Section: Auditory Vigilancecontrasting

confidence: 55%

“…Structurally it resembles amphetamine, but a previous study failed to detect any amphetamine-like activity in healthy subjects using doses up to 100 mg (Peck et al, 1979). Nomifensine (8 amino-2 methyl4 phenyl-1,2,3,4 tetrahydroisoquinoline) is an antidepressant lacking the anticholinergic and sedative properties which result in many of the side effects of the older tricyclic compounds (Hanks, 1977).…”

Section: Bupropionmentioning

confidence: 99%

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Effects of bupropion, nomifensine and dexamphetamine on performance, subjective feelings, autonomic variables and electroencephalogram in healthy volunteers.

Hamilton¹,

Smith²,

Peck³

1983

Brit J Clinical Pharma

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1 Bupropion, a novel antidepressant, has been compared with nomifensine and dexamphetamine in a controlled double blind trial in 12 healthy volunteers. 2 Signals detected in an auditory vigilance test were increased by dexamphetamine 5 and 10 mg when compared with lactose dummy, but unaffected by bupropion 100 and 200 mg and nomifensine 100 mg. Auditory reaction time was decreased by dexamphetamine but unaffected by bupropion and nomifensine. 3 Heart rate was increased after all active treatments but the largest rise followed dexamphetamine 10 mg which differed from both lactose dummy and all other active treatments. Systolic blood pressure was higher after dexamphetamine 10 mg than all other treatments, none of which differed from lactose. No changes occurred in diastolic blood pressure. Pupil size increased after dexamphetamine 10 mg but no changes followed other treatments. 4 Visual analogue scales showed that subjects were more alert, attentive, proficient, excited, interested and elated after dexamphetamine but no changes followed bupropion or nomifensine. Subjects were able to recognise that they had received an active drug only after dexamphetamine 10 mg.5 Increased activity was seen in the 7.5-13.5 Hz and 13.5-26 Hz frequency bands of the electroencephalogram after dexamphetamine 10 mg but not after bupropion or nomifensine. 6 These findings in man suggest that neither of these two, non-sedative antidepressants possess amphetamine-like stimulant activity, and are discussed in relation to the animal pharmacology of the drugs.

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Section: Auditory Vigilancecontrasting

confidence: 55%

Section: Bupropionmentioning

confidence: 99%

Effects of bupropion, nomifensine and dexamphetamine on performance, subjective feelings, autonomic variables and electroencephalogram in healthy volunteers.

Hamilton¹,

Smith²,

Peck³

1983

Brit J Clinical Pharma

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“…In the present study, we examined the effects of binodaline on some baseline autonomic functions (salivation, resting pupil diameter, baseline sweat gland activity), and on tissue responses to cholinoceptor and adrenoceptor stimulants (carbachol-and phenylephrine-evoked sweating). The effects of binodaline were compared with those of placebo and of amitriptyline, an antidepressant with well-documented effects on the autonomic nervous system (Ghose et al, 1974(Ghose et al, , 1976Peck et al, 1979;Szabadi et al, 1980Szabadi et al, , 1981 (Peck, 1959). Three dental rolls (size 2) were used in the present experiment (two rolls were placed bucally and one sublingually).…”

Section: Introductionmentioning

confidence: 99%

Comparison of the effects of binodaline and amitriptyline on peripheral autonomic functions in healthy volunteers.

Longmore¹,

Szabadi²,

Bradshaw³

1985

Brit J Clinical Pharma

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Twelve healthy male volunteers participated in five experimental sessions separated by weekly intervals. At the beginning of each session the subjects received one single oral dose of the following drugs, according to a double‐blind, balanced cross‐over design: binodaline hydrochloride (50 mg or 100 mg); amitriptyline hydrochloride (50 mg or 100 mg); lactose placebo. Salivation and resting pupil diameter were assessed before and 2 h after the ingestion of the drugs; baseline sweating, carbachol‐ or phenylephrine‐evoked sweating were measured 2 h following drug taking. Binodaline, like placebo, had little effect on salivary output, whereas amitriptyline caused a dose‐ dependent decrease in salivation. None of the drugs caused any significant change in resting pupil diameter or in baseline sweating. Carbachol‐evoked sweating did not differ significantly following the ingestion of binodaline or placebo; on the other hand responses to carbachol were significantly reduced following amitriptyline. Phenylephrine‐evoked sweating was reduced by both binodaline and amitriptyline. The lack of effect of binodaline on salivation, resting pupil diameter, baseline and carbachol‐evoked sweating is in agreement with the results of animal experiments indicating the lack of an interaction of this drug with cholinergic mechanisms. The reduction in phenylephrine‐evoked sweating would be indicative of an alpha‐ adrenoceptor blocking property of this drug.

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“…A phase I clinical study in 12 healthy subjects revealed no differences from lactose and it was concluded [50] that bupropion, at the doses studied (of 50 and 100 mg), was devoid of stimulant or sedative properties, or cardiovascular effects.…”

Section: Bupropion J39mentioning

confidence: 92%

Standalone Drugs

Proudfoot

2010

Analogue‐Based Drug Discovery II

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In volume I of Analogue-Based Drug Discovery we focused on analogue drugs with a double similarity, that is, those that are similar to another drug from both chemical and pharmacological viewpoints. These were referred to as structural and pharmacological analogues or, alternatively, full analogues. One special class of these analogues is considered to be direct analogues if they have identical pharmacophores -that is, they can be described by a general structure that includes most of the chemical skeleton. The book also discussed some examples of structural analogues, in which the similarity is limited to their chemical structures since they possess different pharmacological properties. We also proposed the term pharmacological analogues for drugs that have completely different chemical structures but similar pharmacological properties.Analogues are based on following a lead compound, and if this compound were a drug that opened up a new therapeutic treatment then we use the term pioneer drug. Such a drug is often referred to as first in class. One can subdivide pioneer drugs into those that have analogues and those that do not. Thus, the latter group provides a special subclass called standalone drugs,

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A comparison of bupropion hydrochloride with dexamphetamine and amitriptyline in healthy subjects.

Cited by 83 publications

References 12 publications

Effects of bupropion, nomifensine and dexamphetamine on performance, subjective feelings, autonomic variables and electroencephalogram in healthy volunteers.

Effects of bupropion, nomifensine and dexamphetamine on performance, subjective feelings, autonomic variables and electroencephalogram in healthy volunteers.

Comparison of the effects of binodaline and amitriptyline on peripheral autonomic functions in healthy volunteers.

Standalone Drugs

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