Comparative pharmacokinetics of theophylline and aminophylline in man.

Aslaksen, Aslak; Om, Bakke; T, Vigander

doi:10.1111/j.1365-2125.1981.tb00533.x

Cited by 22 publications

(14 citation statements)

References 14 publications

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“…Serum rapidly loses CO2 resulting in an increase in pH. In our experiments with ungassed, previously frozen serum, pH was in the range 8.1-8.3 and the binding of theophylline, as determined by ultrafiltration or by dialysis against ungassed Krebs Ringer bicarbonate buffer, was about 58-60%, results which are similar to those reported in other studies in which pH control was not described (Mangione et al, 1978;Simons et al, 1979;Koysooko et al, 1974;Lesko et al, 1981;Aslaksen et al, 1981).…”

Section: Discussionsupporting

confidence: 81%

“…The degree of binding observed in this study is similar to that reported by Fleetham et al (1979), for healthy subjects, but much lower than that reported by Mangione et al (1978), Simons et al (1979), Koysooko et al (1974), Lesko et al (1981) and Aslaksen et al (1981). Vallner et al (1978) observed that the binding of theophylline in serum is pH-dependent.…”

Section: Discussionsupporting

confidence: 70%

“…The data on protein binding of theophylline in human serum is conflicting. In healthy subjects, binding varies from 30-80% in different studies (Mangione et al, 1978;Lesko et al, 1981;Piafsky et al, 1977;Simons et al, 1979;Aslaksen et al, 1981). This imposes considerable uncertainty upon the judgement of dosage regimen based on plasma concentration measurement in individual patients.…”

Section: Introductionmentioning

confidence: 99%

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Binding of theophylline in human serum determined by ultrafiltration and equilibrium dialysis.

Brørs¹,

Sager²,

Sandnes³

et al. 1983

Brit J Clinical Pharma

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1 Binding of theophylline (80 ,tmol/l) was determined in serum from healthy subjects by equilibrium dialysis and by ultrafiltration, using [3H]-theophylline, at 22°C and at different pH-values. pH was regulated by gassing with CO2 or by dialysing the serum against a phosphate buffer before use. 2 Binding of theophylline in serum was 34-38% determined by equilibrium dialysis and 41-45% determined by ultrafiltration at pH 7.4-7.5. The protein concentration in serum decreased by 12-16% during equilibrium dialysis and increased by 20% during ultrafiltration. The intersubject variation in binding was small. 3 Binding of theophylline in serum was pH-dependent with 25-30% bound at pH 7.0 and 58-60% bound at pH 8.1-8.3. Binding was significantly correlated to the fraction of ionized theophylline. 4 The binding of theophylline in normal human serum is about 35 40% at pH 7.4 and 22°C. The difference in binding observed between equilibrium dialysis and ultrafiltration may be explained by the opposite changes in protein concentration during the experiment. 5 Control of pH is necessary to obtain physiologically relevant data on drug binding in serum.

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Section: Discussionsupporting

confidence: 81%

Section: Discussionsupporting

confidence: 70%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Binding of theophylline in human serum determined by ultrafiltration and equilibrium dialysis.

Brørs¹,

Sager²,

Sandnes³

et al. 1983

Brit J Clinical Pharma

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“…Aminophylline has a terminal half-life of approximately 7 hours, shorter than that of dipyridamole. 6,9 Historically, aminophylline had been advocated for bradyasystolic cardiac arrest, based on the assumption that such patients may have elevated levels of endogenous adenosine. Despite promising small studies, a large randomized, placebo-controlled Canadian trial by Abu-Laban and colleagues found an increase in nonsinus tachyarrhythmias but no increase in return of spontaneous circulation from aminophylline in prehospital patients with bradyasystolic cardiac arrest.…”

Section: Discussionmentioning

confidence: 99%

Surviving a stressful MIBI scan

Gooch

Bryski

Courvoisier-Grzywacz

2013

CJEM

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Dipyridamole/technetium sestamibi scans (more commonly known as MIBI scans, an acronym for methoxyisobutyl isonitrile) are used commonly for the diagnosis and risk stratification of coronary artery disease. Adverse events from MIBI scans are extremely rare. We present the case of a 64-year-old man who was successfully resuscitated after two asystolic episodes following dipyridamole infusion for a MIBI scan. The second asystolic episode occurred in the emergency department 40 minutes after the patient had been transferred from the Cardiac Stress Test Laboratory. To our knowledge, there are no previous reports of patients having two discrete asystolic episodes or an asystolic episode as delayed as we report after a MIBI scan. Our case illustrates why emergency physicians should be aware of the potential for asystole following MIBI scanning and why aminophylline, the antidote for dipyridamole, should be readily available in emergency departments that could see patients after pharmacologic stress testing. Patients who become asystolic following dipyridamole infusion likely require prolonged cardiac monitoring, given the potential for further episodes after periods of hemodynamic stability. RÉ SUMÉLes scintigraphies au dipyridamole-techné tium sestamibi (mieux connues sous le nom de scintigraphies au MIBI, acronyme anglais de mé thoxy-isobutyl-isonitrile) servent souvent au diagnostic et à la classification du risque de maladie coronarienne. Les é vé nements indé sirables dé coulant des scintigraphies au MIBI sont extrê mement rares. Nous exposons le cas d'un homme de 64 ans qui a é té ré animé avec succè s à la suite de deux é pisodes d'asystole, consé cutifs à la perfusion de dipyridamole en vue d'une scintigraphie au MIBI. Le deuxiè me é pisode est survenu au service des urgences, 40 minutes aprè s la mutation du patient du laboratoire d'é preuves d'effort cardiaque. À notre connaissance, il n'existe pas de rapport anté rieur de deux é pisodes distincts d'asystole ou tout au moins d'un é pisode d'asystole survenu aussi tardivement aprè s une scintigraphie au MIBI. Le cas dé crit dé montre trè s bien pourquoi les mé decins d'urgence devraient ê tre conscients du risque d'asystole à la suite d'une scintigraphie au MIBI et pourquoi il faudrait que les services d'urgence susceptibles de recevoir des patients aprè s une é preuve d'effort mé dicamenteuse aient à la porté e de la main de l'aminophylline, l'antidote du dipyridamole. Il ne fait aucun doute que les patients qui subissent un é pisode d'asystole aprè s une perfusion de dipyridamole doivent faire l'objet d'une surveillance cardiaque prolongé e, compte tenu du risque d'é pisodes ulté rieurs d'arrê t cardiaque aprè s des pé riodes de stabilité hé modynamique.Keywords: aminophylline, asystole, dipyridamole, MIBI Dipyridamole/technetium sestamibi scans (more commonly known as MIBI scans, an acronym for methoxyisobutyl isonitrile) are used commonly for the diagnosis and risk stratification of coronary artery disease. Adverse events from MIBI scans are extre...

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“…Teofilin sangat sukar larut dalam air, akan tetapi kelarutannya dapat meningkat setelah ditambah etilendiamin dalam bentuk kompleks garam aminofilin. 3 Berdasarkan Daftar Obat Esensial Nasional (DOEN) tahun 2013, aminofilin termasuk ke dalam salah satu terapi yang digunakan pada saat terjadinya eksaserbasi asma. 4 Aminofilin/ teofilin merupakan suatu bronkodilator yang poten dengan aksi antiinflamasi yang ringan, 5 sehingga dapat digunakan untuk pengobatan serangan asma.…”

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Effectiveness and Toxicity Risk of Intravenous Aminophylline in Exacerbation Asthma Treatment

Lorensia

Ikawati

Andayani

et al. 2018

Indones J Clin Pharm

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4Program Studi Apoteker, Fakultas Farmasi Universitas Surabaya, Surabaya AbstrakAsma merupakan penyakit inflamasi kronis pada saluran pernafasan yang mempunyai prevalensi global yang cukup besar. Perburukan penyakit asma berupa serangan asma yang menyebabkan peningkatan gejala asma dan penurunan fungsi paru secara progresif. Salah satu obat asma yang masih sering digunakan di Indonesia adalah aminofilin intravena. Aminofilin merupakan obat dengan rentang terapi sempit yang berisiko menyebabkan toksisitas obat, namun data perbandingan keuntungan efektivitas dan keamanan obat tersebut belum memadai. Penelitian ini bertujuan untuk mengetahui efektivitas aminofilin intravena pada pengobatan awal serangan asma berupa perbaikan gejala asma dan kejadian toksisitas terkait gejala yang muncul dan kadar teofilin dalam darah di suatu rumah sakit di Surabaya, Indonesia. Penelitian ini menggunakan metode pra-eksperimental yang dilaksanakan sejak 2014 hingga 2016. Sebanyak 27 pasien terlibat dalam penelitian ini. Terapi yang diberikan adalah aminofilin intravena selama satu jam. Metode sampling yang digunakan adalah consecutive sampling dengan teknik analisis deskriptif dan jum. Semua subjek penelitian menunjukkan perbaikan gejala serangan asma dengan terapi aminofilin intravena selama satu jam, dan tidak ada yang mengalami toksisitas karena kadar teofilin dalam darah di bawah rentang terapi. Aminofilin masih efektif dalam mengurangi gejala pada serangan asma dan tidak menunjukkan risiko toksisitas.Kata kunci: Aminofilin, efektivitas, serangan asma, toksisitas Effectiveness and Toxicity Risk of Intravenous Aminophylline in Exacerbation Asthma Treatment AbstractAsthma is a chronic inflammatory disease in the respiratory tract that has a considerable global prevalence. The worsening of asthma is an asthma attack that causes asthma symptoms to increase and decreased lung function progressively. One of the most commonly used asthma medications in Indonesia is intravenous aminophylline. Aminophylline is a drug with a narrow range of therapies that is at risk of causing drug toxicity, but the comparative data on the efficacy and safety benefits of the drug are inadequate. This study aimed to determine the effectiveness of aminophylline intravenously in the early treatment of asthma attacks in the form of improvements in asthma symptoms and toxicity events related to the symptoms that appear and blood theophylline levels in a hospital in Surabaya, Indonesia. This study used a pre-experimental method which was carried out from 2014 to 2016. A total of twenty seven patients were involved in the study. The therapy given was aminophylline intravenously for one hour. The sampling method used was consecutive sampling with descriptive analysis technique. All subjects showed improved symptoms of asthma attacks with intravenous aminophylline therapy for one hour, and none had toxicity due to theophylline levels in the blood below the therapeutic range. Aminophylline is still effective in reducing symptoms in asthma attacks and does not indic...

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Comparative pharmacokinetics of theophylline and aminophylline in man.

Cited by 22 publications

References 14 publications

Binding of theophylline in human serum determined by ultrafiltration and equilibrium dialysis.

Binding of theophylline in human serum determined by ultrafiltration and equilibrium dialysis.

Surviving a stressful MIBI scan

Effectiveness and Toxicity Risk of Intravenous Aminophylline in Exacerbation Asthma Treatment

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