Effect of caffeine on intestinal absorption of ergotamine in man

Schmidt, R.; Fanchamps, A

doi:10.1007/bf00560383

Cited by 63 publications

(36 citation statements)

References 9 publications

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“…Caffeine improves the absorption of oral ergotamine tartrate (Schmidt & Fanchamps, 1974). This can, however, hardly explain the discrepancy in plasma concentrations as a total daily dose up to 5 mg ergotamine tartrate tablets containing caffeine did not result in any measurable amount in plasma with the HPLC procedure (Ekbom et al, 1981).…”

Section: Discussionmentioning

confidence: 93%

Low bioavailability of ergotamine tartrate after oral and rectal administration in migraine sufferers.

Ibraheem¹,

Paalzow²,

Tfelt‐Hansen³

1983

Brit J Clinical Pharma

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1 Fifteen migraine patients were administered 2 mg ergotamine tartrate in a partial cross-over design as a single, oral tablet, rectal suppository and rectal solution. Eight of these patients were in a previous investigation given 0.5 mg ergotamine tartrate intravenously. The blood samples were taken up to 54 h after oral and suppository while it was followed for only 3 h after rectal solution. The chemical analysis was performed by applying h.p.l.c. method with a limit of sensitivity of 0.1 ng/ml ergotamine base in plasma.2 No ergotamine was detected in the blood samples after the oral route, whereas small and very variable quantities was found in blood after the rectal route. Regular calculation of bioavailability could therefore not be performed. An estimate of the maximal possible bioavailability was found to yield a mean value of 2% (tablets); 5% (suppositories) and 6% (rectal solution). Rectal solution elicited faster absorption and the extent of absorption was significantly higher (P < 0.05) than for the suppository.

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Section: Discussionmentioning

confidence: 93%

Low bioavailability of ergotamine tartrate after oral and rectal administration in migraine sufferers.

Ibraheem¹,

Paalzow²,

Tfelt‐Hansen³

1983

Brit J Clinical Pharma

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“…The rate and possibly extent of intestinal absorption of ergotamine are enhanced by the simultaneous adminis tration of caffeine. 13 Gangrene of the extremities has been reported in both humans and animals following the ingestion of ergotised grain products, but is quite uncommon fol lowing medicinal ergot poisoning, perhaps due to the intermittent nature of medicinal ergot administration. 4 The animal experiments of Lewis 14 suggested that sec ondary thrombosis of the arteriospastic vessels was necessary before gangrene ensued.…”

Section: Discussionmentioning

confidence: 99%

Transient aortic arch syndrome with dysphasia due to ergotism.

Feneley¹,

Morgan²,

McGrath³

et al. 1983

Stroke

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SUMMARYA 55-year-old woman with an aortic arch syndrome of acute onset and dysphasia, resulting from the excessive administration of ergotamine tartrate suppositories, is described. Complete resolution of symptoms and return of upper limb and carotid artery pulses to normal occurred within four days of cessation of the ergot derivative. Lower limb involvement was conspicuously absent in this case. Stroke, Vol 14, No 5, 1983ARTERIOSPASTIC DISEASE resulting from the ex cessive use of medicinal ergot preparations typically involves the lower limbs 1 ' 2 or less commonly, the mes enteric vessels.3 Although upper limb involvement has been described previously, 4 selective upper limb in volvement with complete sparing of the lower limbs has been only rarely reported. 5-7To our knowledge, there have been only four angiographically document ed cases of ergot-induced carotid arteriospasm.8-" We report the case of a 55-year-old woman with transient, severe, bilateral brachial and internal carotid artery stenoses and expressive dysphasia due to the excessive use of ergotamine tartrate suppositories, but with no evidence of lower limb arteriospasm. Case ReportA 55-year-old woman was referred with a three day history of dizziness and headache of sudden onset. Physical examination revealed absent pulses and unrecordable blood pressure in both upper limbs, which were cool with mild cyanosis of the hands and loud bilateral carotid bruits. The left carotid pulse was not palpable and the bruit on this side had both systolic and diastolic components. The lower limbs were warm and well-perfused and all lower limb pulses were normal. There were no abdominal or femoral bruits. The cardi ac examination, electrocardiogram and chest X-ray were normal. In particular, there was no evidence of mediastinal enlargement. There was no clinical or lab oratory evidence or rheumatoid arthritis, ankylosing spondylitis or other rheumatic disorder. The erythro cyte sedimentation rate was 30 mm/hour. Neurological examination was initially normal, but on the second hospital day expressive dysphasia was noted without other neurological deficit.Doppler orbital blood flow studies showed reversed flow on the right side and low amplitude flow on the left side. Oculoplethysmographically determined oph thalmic artery pressures were 70 mm Hg on both sides. Arch aortography revealed that the aorta and proximal brachiocephalic vessels were normal, but selective an giography demonstrated bilateral internal carotid ar tery stenoses ( fig. 1) brachial artery ( fig. 2). All these stenoses were noted to be long, smooth and tapering. Angiograms of the right brachial artery were not performed because the right brachial artery was palpable at the time of angiog raphy, as was the left carotid pulse, suggesting that the angiographic appearances underestimate the severity of the carotid stenoses present at the time of admission. On the third hospital day, the expressive dysphasia resolved completely, no carotid bruits were audible and all upper limb pulses were palpable....

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“…No other medication beginning 48 h before, no xanthine containing beverages such as tea, coffee and cola beginning 10 h before (caffeine has been shown to modify the absorption of ergot alkaloids: Schmidt & Fanchamps, 1974;Zoglio & Maulding, 1970), and no alcohol beginning 24 h before application and continuing during the blood collection period were allowed. A standard, xanthine-free, low fat breakfast and main meal, each with approximately 250 ml fluid, were given 3 h and 7 h after drug application, respectively.…”

Section: Methodsmentioning

confidence: 99%

Absorption kinetics of dihydroergotoxine following oral administration to man.

Woodcock¹,

Rietbrock²,

Loh³

et al. 1985

Brit J Clinical Pharma

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The absorption characteristics of dihydroergotoxine administered as an oral solution, tablet and retard capsule have been determined in a randomised cross‐over investigation in 12 healthy males. The plasma concentrations of dihydroergotoxine produced by the three preparations, measured using a specific and sensitive radioimmuno‐assay method over 24 h, exceeded 200 pg ml‐1 for approximately 5 h and decayed in a biphasic manner with a slowest measured half‐life of 12‐14 h. The retard capsule differs from the other two preparations in having a low Cmax (50% of that recorded for the solution) and a clearly defined plateau. The bioavailability of the retard capsule was similar to that for the solution indicating that first‐pass metabolism is not significantly increased following a three‐fold prolongation in the absorption rate constant. The 20‐40% greater bioavailability of dihydroergotoxine solution and retard capsule in comparison with the standard tablet may be due to a reduced contact time with gastric secretions achieved by means of rapid absorption from the stomach (solution) or delayed release at pH 1.5 (retard capsule).

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Effect of caffeine on intestinal absorption of ergotamine in man

Cited by 63 publications

References 9 publications

Low bioavailability of ergotamine tartrate after oral and rectal administration in migraine sufferers.

Low bioavailability of ergotamine tartrate after oral and rectal administration in migraine sufferers.

Transient aortic arch syndrome with dysphasia due to ergotism.

Absorption kinetics of dihydroergotoxine following oral administration to man.

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