Inhalation administration salbutamol

The transformation of a drug into a medicinal product is a complex process that is controlled by a range of competing factors. The formulator must amalgamate the preformulation information and the clinical indication, which may suggest a particular route of administration (e.g. inhalation of salbutamol. Table 2.2), with toxicology and biopharmaceutical data determining... 

The P2 selective adrenergic agonists are most widely used drugs for the treatment of asthma. They are effective after oral and inhaled administration and have a longer duration of action. Albuterol (salbutamol), salmeterol, bitolterol, pir-buterol are available as aerosol pack in metered dose. 

Disposition in the Body. Rapidly absorbed after oral administration and after inhalation. About 60 to 90% of a dose is excreted in the urine in 24 hours, of which approximately 50% is unchanged salbutamol and 50% is the 4 -0-sulphate of salbuta-mol. Up to about 12% is eliminated in the faeces. 

The effects of single inhaled doses of salmeterol 0.1, 0.2, and 0.4 mg and salbutamol 0.4 mg from a multidose pressurized inhaler have been compared in healthy volunteers (10). At all doses tested, salmeterol produced statistically significant changes in pulse rate, tremor, blood glucose, and plasma potassium concentrations. Tremor, awareness of heartbeat, and headache were reported by the subjects after salmeterol administration. 

After administration of vinorelbine, chest pain occurs in up to 5% of patients. However, subsequent analysis showed that most patients had underlying cardiovascular disease or a tumor in the chest, making interpretation difficult (2,20). Three patients developed acute cardiopulmonary toxicity after vinorelbine therapy (25). The symptoms mimicked acute cardiac ischemia, but with no electrocardiographic changes or raised cardiac enzymes. In two patients, tachypnea, rales, wheezing, and severe dyspnea responded to inhaled salbutamol. One patient developed pulmonary edema and bilateral pleural effusions, which contained no malignant cells when drained. 

Salbutamol (4) has been extensively studied by oral (4 mg), inhalation (200 pg),2 intravenous,2 and intramuscular22 administration and found to be effective in the inhibition of exercise induced bronchospasm.2 No drug tolerance was observed in chronically pre-treated guinea pigs.28... 

A report briefly describes a case of tachycardia and apprehension in a patient taking phenelzine when salbutamol (albuterol) was started [route of administration not stated]. Hypomania has been described in a patient taking phenelzine in the few weeks after starting inhaled isoetarine 680 micrograms up to every 4 hours. ... 

Conner WT, Dolovich MB, Frame RA, Newhouse MT. Rehahle salbutamol administration in 6- to 36-month-old children by means of a metered dose inhaler and Aerochamber with mask. Pediatr Pulmonol 1989 6 263-267. 

Carbuterol has been shown to produce safe and effective bronchodilatation but of less magnitude than that produced by salbutamol. Tremulousness was the only side effect seen in 1 patient out of 15 given carbuterol 300 HS by inhalation. It occurred 2 and 4 hours after administration. Minor T-wave changes follow higher doses (lO ). A significant increase in heart rate and blood pressure occurred in 9 patients with bronchial asthma or chronic bronchitis when given carbuterol 4 mg orally. Two complained of headache and tremulousness that lasted for 1-2 hours (11 ). 

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