Drugs in the treatment of asthma

Svedmyr, N; Simonsson, Bo G.

doi:10.1016/s0306-039x(78)90005-3

Cited by 13 publications

(12 citation statements)

References 247 publications

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“…In man, the therapeutic effect of theophylline for obstructive pulmonary diseases is well correlated to plasma concentration of the drug, 10-20 pg/ml being the effective range (Svedmyr & Simonsson, 1978;Rall, 1980;Weinberger & Hendeles, 1980), and adverse effects are frequent at levels above 20 pglml (Weinberger & Hendeles, 1980). Horses suffering from obstructive pulmonary disease are often treated with theophylline and a wide range of dosage regimens is used.…”

Section: Discussionmentioning

confidence: 99%

“…Adverse effects, such as central nervous symptoms, sweating and muscle tremor, have been reported in horses with plasma concentrations of theophylline slightly above 15 yglml . In man, the therapeutic range of theo-phylline in plasma is between 10 and 20 pg/ ml and adverse effects are uncommon with plasma concentrations less than 20 pg/ml (Svedmyr & Simonsson, 1978;Rall, 1980;Weinberger & Hendeles, 1980). The xanthine derivatives have also been used in doping of racehorses (Tobin, 1981).…”

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetics and cardio‐respiratory effects of oral theophylline in exercised horses

Ingvast-Larsson

Kallings

Persson

et al. 1989

Vet Pharm & Therapeutics

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The pharmacokinetics of theophylline at rest and the effects on cardio-respiratory and blood lactate responses to exercise were investigated after repeated oral administrations in six healthy Standardbred horses. A dose of 5 mg/kg body weight was administered every 12 h. The binding of theophylline to plasma protein was also determined. There was good agreement between predicted and observed plasma concentrations of theophylline at steady state. The mean half-life of elimination was shown to be 17.0 +/- 2.5 h, the mean half life of absorption was 1.6 +/- 1.8 h, the apparent volume of distribution was 852 +/- 99.0 ml/kg and total plasma clearance 0.61 +/- 0.08 ml/kg/min. Theophylline showed very low plasma protein binding (12%). The heart rate and blood lactate levels, during and after exercise, were significantly increased during theophylline-treatment. There was an increase of the arterial oxygen tension after exercise and the arterial carbon dioxide values before and after exercise were significantly lower than the premedication values. No severe adverse effects of the drug were noted. The recommended oral dose is therefore 5 mg/kg every 12 h but due to inter-individual variation, an adjustment of the dose may be necessary. The changes in the studied exercise parameters indicate that the performance capacity may be impaired by theophylline in the healthy horse.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics and cardio‐respiratory effects of oral theophylline in exercised horses

Ingvast-Larsson

Kallings

Persson

et al. 1989

Vet Pharm & Therapeutics

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“…This has in fact been shown in a number of animal studies, both in vivo and in vitro (reviews 25,35), and also in human bronchial muscles in vitro (32,34). This has in fact been shown in a number of animal studies, both in vivo and in vitro (reviews 25,35), and also in human bronchial muscles in vitro (32,34).…”

Section: Discussionmentioning

confidence: 72%

Effects of Oral Theophylline Combined with Oral and Inhaled β₂‐Adrenostimulants in Asthmatics

Svedmyr¹

1982

Allergy

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The acute ventilatory, cardiovascular and tremorogenic effect of a high oral dose of terbutaline (5 mg) was compared with that of half the dose (2.5 mg) combined with 280 mg anhydrous theophylline orally in the randomized, double-blind, cross-over study in eight asthmatics. After 120 min, when steady-state bronchodilation was achieved, five terbutaline inhalations (1.25 mg terbutaline sulphate) were added to both treatment regimens. The mean maximum plasma concentration of theophylline was then 7 micrograms/ml (39 mumol/l). Inhalation of a beta 2-adrenostimulant had a very good additional effect without increasing side effects in these patients with good inhalation technique. The oral low-dose combination gave significantly better bronchodilation than the high dose of terbutaline alone and caused significantly less tremor. Although the combination only had an additive bronchodilating effect, it may offer important clinical advantages. If the patient cannot use the metered dose aerosol, an oral low dose combination should be preferred to a single high dose of either theophylline or beta 2-adrenostimulants. In patients with good inhalation technique but not controlled by inhalation from a metered dose aerosol alone, a combination of oral theophylline and terbutaline in "sub-optimal" dose and an inhaled beta 2-agonist in individually titrated optimal dose gave a maximal bronchodilating effect with minimum side effects.

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“…They have a fairly selective β 2 stimulating effect; tachycardia is the dose-limiting side effect in only a few per cent of the patients. [10] Salbutamol sulphate has site-specific absorption in stomach and upper part of the small intestine. [3] The objective of the present study is to formulate and evaluate the press coated tablets of salbutamol sulphate for time controlled release of the drug.…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of press coated tablets of salbutamol sulphate for time controlled release

Hasan¹,

Chaitanya²,

Someshwar³

et al. 2014

Asian J Pharm

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T he objective of the present study was to formulate and evaluate a press coated pulsatile drug delivery system of salbutamol sulphate in order to attain a time controlled release for treatment of nocturnal asthma. The core was prepared by direct compression, while press coating technique was used in coating the outer layer there by preparing a press coated tablet. The immediate release core formulations comprised of salbutamol sulphate and disintegrants like crospovidone, croscarmellose sodium and sodium starch glycolate in different ratios with the drug. The outer coat formulations were prepared using a hydrophilic (HPMC) and hydrophobic (EC) polymer of similar viscosity. The polymers were reviewed individually for their influence on lag time further obtaining the lag time using polymer combinations were assessed by employing central composite design. All the preliminary trials were evaluated for various post compression parameters along with the dissolution study that was performed using USP paddle method at 50 rpm in 0.1 N HCl and phosphate buffer pH 6.8. The formulation containing 300 mg of EC N50 and 75-100 mg of HPMC E50 may be regarded as the minimum quantity required in outer press coat so as to attain a predetermined lag time of 6 h.

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Drugs in the treatment of asthma

Cited by 13 publications

References 247 publications

Pharmacokinetics and cardio‐respiratory effects of oral theophylline in exercised horses

Pharmacokinetics and cardio‐respiratory effects of oral theophylline in exercised horses

Effects of Oral Theophylline Combined with Oral and Inhaled β₂‐Adrenostimulants in Asthmatics

Formulation and evaluation of press coated tablets of salbutamol sulphate for time controlled release

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Drugs in the treatment of asthma

Cited by 13 publications

References 247 publications

Pharmacokinetics and cardio‐respiratory effects of oral theophylline in exercised horses

Pharmacokinetics and cardio‐respiratory effects of oral theophylline in exercised horses

Effects of Oral Theophylline Combined with Oral and Inhaled β2‐Adrenostimulants in Asthmatics

Formulation and evaluation of press coated tablets of salbutamol sulphate for time controlled release

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Effects of Oral Theophylline Combined with Oral and Inhaled β₂‐Adrenostimulants in Asthmatics