Tolfenamic Acid Is as Effective as Ergotamine During Migraine Attacks

Hakkarainen, Heikki; Vapaatalo, Heikki; Gothóni, G.; Parantainen, J.

doi:10.1016/s0140-6736(79)90343-x

Cited by 119 publications

(65 citation statements)

References 13 publications

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“…As expected from earlier studies [87,123], tolerability of NSAIDs was superior to that of ergotamine in several trials [62,84,100,111,112,113], while efficacy was similar. Ergotamine caused more nausea and vomiting, although this was statistically significant only in two trials [84,111].…”

Section: Results Of Randomized Controlled Trialssupporting

confidence: 79%

“…Tolfenamic acid was found effective in three trials [84,85,86] and the rapid release form had an efficacy similar to oral sumatriptan [85]. Tolfenamide was as effective as 500 mg ASA and 1 mg ergotamine [84].…”

Section: Results Of Randomized Controlled Trialsmentioning

confidence: 99%

“…Tolfenamide was as effective as 500 mg ASA and 1 mg ergotamine [84]. A smaller cross-over trial detected a benefit of adding caffeine to tolfenamide [87] but a larger trial showed no difference between tolfenamide+caffeine and tolfenamide alone but detected a slight benefit when tolfenamide was combined with metoclopramide [86].…”

Section: Results Of Randomized Controlled Trialsmentioning

confidence: 99%

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NSAIDs in the Acute Treatment of Migraine: A Review of Clinical and Experimental Data

Párdutz

Schoenen

2010

Pharmaceuticals

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Migraine is a common disabling neurological disorder with a serious socio-economical burden. By blocking cyclooxygenase nonsteroidal anti-inflammatory drugs (NSAIDs) decrease the synthesis of prostaglandins, which are involved in the pathophysiology of migraine headaches. Despite the introduction more than a decade ago of a new class of migraine-specific drugs with superior efficacy, the triptans, NSAIDs remain the most commonly used therapies for the migraine attack. This is in part due to their wide availability as over-the-counter drugs and their pharmaco-economic advantages, but also to a favorable efficacy/side effect profile at least in attacks of mild and moderate intensity. We summarize here both the experimental data showing that NSAIDs are able to influence several pathophysiological facets of the migraine headache and the clinical studies providing evidence for the therapeutic efficacy of various subclasses of NSAIDs in migraine therapy. Taken together these data indicate that there are several targets for NSAIDs in migraine pathophysiology and that on the spectrum of clinical potency acetaminophen is at the lower end while ibuprofen is among the most effective drugs. Acetaminophen and aspirin excluded, comparative trials between the other NSAIDs are missing. Since evidence-based criteria are scarce, the selection of an NSAID should take into account proof and degree of efficacy, rapid GI absorption, gastric ulcer risk and previous experience of each individual patient. If selected and prescribed wisely, NSAIDs are precious, safe and cost-efficient drugs for the treatment of migraine attacks.

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Section: Results Of Randomized Controlled Trialssupporting

confidence: 79%

Section: Results Of Randomized Controlled Trialsmentioning

confidence: 99%

Section: Results Of Randomized Controlled Trialsmentioning

confidence: 99%

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NSAIDs in the Acute Treatment of Migraine: A Review of Clinical and Experimental Data

Párdutz

Schoenen

2010

Pharmaceuticals

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“…Oral ergotamine has been found effective for migraine in double-blind trials (Hakkarainen et al, 1979;Ostfeld, 1961) was not better than placebo, it caused significantly more side-effects than placebo (Waters, 1970 (Knudsen, 1977) and theophylline (Bolme et al, 1979). Since the purpose was the rate of absorption, plasma levels were only followed for 3 h. Rectal solution of ergotamine increased the bioavailability of the drug marginally, but more important ergotamine was detectable in plasma as early as 10 min in eight out of 12 patients which was never the case after administration of suppositories (n = 9).…”

Section: Discussionmentioning

confidence: 99%

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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“…namates, it exerts its pharmacological properties by inhibiting prostaglandin (1) and leukotriene biosynthesis (3) as well as by its antagonistic action on prostaglandin receptors (4). Tolfenamic acid has been found clinically effective in the treatment of rheumatoid arthritis (5,6), dysmenorrhea (7) and migraine (8)(9)(10). Recently, tolfenamic acid has been introduced as a veterinary treatment and it is also used to dope horses (II).…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of tolfenamic acid in pediatric patients after single oral dose

Niopas

Georgarakis

Sidi-Frangandrea

et al. 1995

European Journal of Drug Metabolism and Pharmacokinetics

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The pharmacokinetics of tolfenamic acid, a non-steroidal anti-inflammatory drug, were determined following administration of a 1 mg/kg single oral dose of tolfenamic acid suspension to 6 feverish children. Their ages were from 2-14 years (mean 7.5 years) and their weights were from 12-50 kg (mean 29.2 kg). Tolfenamic acid produced a significant fall in temperature (about 2 degrees C) compared to the initial value before oral intake of the drug and was well tolerated without adverse effects. Blood samples for determination of tolfenamic acid concentrations in plasma were obtained at timed intervals for up to 8 h post-dose. Plasma concentrations of tolfenamic acid were determined using a reversed phase HPLC method and pertinent pharmacokinetic parameters were estimated by model-independent standard methods and were the following: the mean peak plasma concentration (Cmax +/- SEM) was 1.09 +/- 0.44 micrograms/ml (range, 0.65-1.63 micrograms/ml) and the mean time (tmax +/- SEM) to reach peak plasma concentration was 1.4 +/- 0.4 h (range, 0.5-3.0 h). The mean area under the plasma concentration-time curve (AUC0-->infinity +/- SEM) was 4.61 +/- 0.40 micrograms.h/ml (range, 2.74-5.98 micrograms.h/ml), the mean elimination half-life (t1/2 +/- SEM) was 2.82 +/- 0.21 h (range, 2.19-3.40 h) and the mean apparent total clearance (CL/F +/- SEM) was 3.83 +/- 0.41 ml/min/kg (range, 2.79-6.08 ml/min/kg).

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Tolfenamic Acid Is as Effective as Ergotamine During Migraine Attacks

Cited by 119 publications

References 13 publications

NSAIDs in the Acute Treatment of Migraine: A Review of Clinical and Experimental Data

NSAIDs in the Acute Treatment of Migraine: A Review of Clinical and Experimental Data

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

Pharmacokinetics of tolfenamic acid in pediatric patients after single oral dose

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