Indomethacin/Prochlorperazine/Caffeine

Hoy, Sheridan M.; Scott, Lesley J.

doi:10.2165/11206740-000000000-00000

Cited by 17 publications

(8 citation statements)

References 33 publications

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“…25,26 Notably, two drug−drug cocrystals involving IND are already known, namely, IND−carbamazepine 27 and IND− lidocaine. 28 CAFF was chosen as a coformer because it can be found together with IND, owing to their synergic effects, 29 in Difmetre, a pharmaceutical containing IND, CAFF, and prochlorperazine dimaleate in a molar ratio 1:5.6:0.07. Difmetreć an be administered as a film-coated or effervescent tablet or as a suppository and is currently used to treat strong migraines, especially hypnic headaches.…”

Section: ■ Introductionsupporting

confidence: 66%

“…IND often has been selected as the main API of many cocrystals found in the literature: − for example, cocrystals of IND with saccharine and with nicotinamide have been extensively investigated to examine their structure and biological effects. , Notably, two drug–drug cocrystals involving IND are already known, namely, IND–carbamazepine and IND–lidocaine . CAFF was chosen as a coformer because it can be found together with IND, owing to their synergic effects, in Difmetré, a pharmaceutical containing IND, CAFF, and prochlorperazine dimaleate in a molar ratio 1:5.6:0.07. Difmetré can be administered as a film-coated or effervescent tablet or as a suppository and is currently used to treat strong migraines, especially hypnic headaches.…”

Section: Introductionmentioning

confidence: 99%

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Engineering Codrug Solid Forms: Mechanochemical Synthesis of an Indomethacin–Caffeine System

Bordignon

Vioglio

Priola

et al. 2017

Crystal Growth & Design

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This article reports on the preparation and solid-state characterization of an indomethacin–caffeine drug–drug cocrystal (or codrug) in a 1:1 stoichiometry. These two active ingredients are frequently coadministered as part of a therapy against strong migraines, in a commercially available fixed dose combination formulation. The X-ray crystal structure of the codrug is characterized by a hydrogen bond interaction between the carboxylic moiety of indomethacin and the purinic nitrogen atom of caffeine. The combination of multinuclear and multidimensional solid-state NMR measurements (1H MAS, 13C and 15N CPMAS, 1H DQ MAS, 13C–1H HETCOR, 14N–1H J- and D-HMQC), as well as IR data, provided spectroscopic evidence about the hydrogen atom position along the hydrogen bond axis, thereby confirming the neutral nature of the cocrystal. Furthermore, dissolution kinetic tests revealed superior bioavailability of indomethacin in the codrug compared to indomethacin alone and to an indomethacin–caffeine physical mixture. On the other hand, the melting point of indomethacin was slightly lower in the cocrystal rather than in the pure drug.

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Section: ■ Introductionsupporting

confidence: 66%

Section: Introductionmentioning

confidence: 99%

Engineering Codrug Solid Forms: Mechanochemical Synthesis of an Indomethacin–Caffeine System

Bordignon

Vioglio

Priola

et al. 2017

Crystal Growth & Design

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“…This data lends support to the notion that caffeine can be absorbed into systemic circulation when administered via the rectum or colon. It has been demonstrated that a single administration of rectal formulation of indomethacin/prochlorperazine/caffeine containing 75 mg of caffeine in adult patients with migraine and episodic tension-type headache exhibited averaged C max⁡ of 5.2 μ g/mL and averaged T max⁡ of 1.9 h [32]. In contrast, the present study revealed that a single administration of 500 mL of coffee enema fluid containing a comparable content of caffeine (107.24 mg) resulted in a remarkably lower extent ( C max⁡ and AUC) but faster T max⁡ (0.30 h or 18 min) of absorbed caffeine.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of Caffeine following a Single Administration of Coffee Enema versus Oral Coffee Consumption in Healthy Male Subjects

Teekachunhatean

Tosri²,

Rojanasthien

et al. 2013

ISRN Pharmacology

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The objective of this study was to determine the pharmacokinetics of caffeine after single administration of a coffee enema versus coffee consumed orally in healthy male subjects. The study design was an open-label, randomized two-phase crossover study. Eleven healthy subjects were randomly assigned either to receive 500 mL of coffee enema for 10 minutes or to consume 180 mL of ready-to-drink coffee beverage. After a washout period of at least 10 days, all the subjects were switched to receive the alternate coffee procedure. Blood samples were collected immediately before and at specific time points until 12 hours after coffee administration in each phase. The mean caffeine content in both the coffee solution prepared for the coffee enema and the ready-to-drink coffee beverage was not statistically different. The C max and AUC of caffeine obtained from the coffee enema were about 3.5 times significantly less than those of the coffee consumed orally, despite having slightly but statistically faster T max. The t 1/2 of caffeine obtained following both coffee procedures did not statistically differ. In summary, the relative bioavailability of caffeine obtained from the coffee enema was about 3.5 times significantly less than those of the coffee consumed orally.

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“…Unilateral headache is a diagnosis feature of both migraine and hemicrania continua (1). A few patients with migraine also benefit from treatment with indomethacin which can further contribute to diagnostic confusion (29,30). However, there remains clear differences between hemicrania continua and migraine.…”

Section: Discussionmentioning

confidence: 99%

Prevalence and clinical features of hemicrania continua in clinic-based studies: A systematic review and meta-analysis

Al-Khazali

Iljazi

et al. 2023

Cephalalgia

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Objective To estimate the relative frequencies of hemicrania continua and its clinical features in adult patients who were evaluated for headache in a clinic-based setting. Methods PubMed and Embase were searched for observational, clinic-based studies published between 1 January 2004 and 1 February 2022, that reported on the relative frequencies of hemicrania continua and its clinical features. Two independent investigators (HMA and SA-K) screened titles, abstracts, and full text-articles. A random-effects meta-analysis was conducted to estimate pooled relative frequencies of hemicrania continua and its clinical features across clinic-based studies. Results Eleven clinic-based studies were deemed eligible for inclusion. Of these, eight studies reported on the relative frequency of hemicrania continua among adult patients (n = 9854) who were evaluated for headache in a tertiary care unit. The pooled relative frequency of hemicrania continua was found to be 1.8% (95% CI; 1.0–3.3). Considerable heterogeneity was noted across studies (I2 = 89.8%). The three most common symptoms associated with hemicrania continua were lacrimation (72.3%), conjunctival injection (69.8%), and restlessness/agitation (60.2%). Conclusion The findings of this meta-analysis suggest that there is limited epidemiologic data on the relative frequencies of hemicrania continua and its clinical features. Standardized data acquisition and reporting are needed to estimate prevalence rates more accurately and to better understand epidemiologic patterns. This, in turn, should increase awareness of the impact that hemicrania continua has in clinical practice.

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Indomethacin/Prochlorperazine/Caffeine

Cited by 17 publications

References 33 publications

Engineering Codrug Solid Forms: Mechanochemical Synthesis of an Indomethacin–Caffeine System

Engineering Codrug Solid Forms: Mechanochemical Synthesis of an Indomethacin–Caffeine System

Pharmacokinetics of Caffeine following a Single Administration of Coffee Enema versus Oral Coffee Consumption in Healthy Male Subjects

Prevalence and clinical features of hemicrania continua in clinic-based studies: A systematic review and meta-analysis

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