CHAPTER I INTRODUCTION
Air enters the lungs through the main airways (bronchi) and then go into the smaller airways (bronchioles), then into the alveoli. Difficulty breathing include shortness of breath, coughing and wheezing, which is normally as a result of narrowing of the lumen of the bronchioles so that the air space to pass more narrow.
(1.2) Bronchodilators are drugs used to treat breathing difficulties caused by asthma, bronchitis, bronchiolitis, pneumonia and emphysema. Bronchodilators dilate the bronchi and bronchioles that increase airflow. Bronchodilators may be endogenous substance or a medicine used to treat breathing difficulties.(1,2)
CHAPTER II
Drugs Bronchodilators Main types of bronchodilators:
1. Adrenergic
Used is b2-sympathomimetic (short b2-mimetic) the following: salbutamol, terbulatine, tretoquinol, fenoterol, rimiterol, prokaterol (Meptin), and klenbuterol (Spriropent). After all, a long-acting drug that is rather new, the salmoterol and formoterol (dorudil). These substances work more or less selective for the receptor b2 Adrenergis and not practical to receptors- b1 (cardiac stimulation). Drugs with effects on both receptors should not be used anymore in its effect on the heart, such as ephedrine, inprenalin, orsiprenalin and heksoprenalin. The exception is adrenaline (receptors and b) are very effective in the state of chaos. Its mechanism of action is through stimulation of b2 receptors in the trachea (windpipe) and bronchi, which causes activation of adenilsiklase. This enzyme conversion strengthen adenosintrifosat (ATP) into energy-rich cyclic adenosine monophosphate-(cAMP) with the release of energy that is used for processes in the cell. Increased levels of cAMP in the cells produced some inhibitory effect bronchodilatasi and mediator release by mast cells. Its use initially as monotherapy continuous, which turns gradually increase the HRB and ultimately worsen lung function, because it does not address the inflammation and increased sensitivity to allergens in allergic patients. Therefore, since a few years only used to counter attack as maintenance or in combination with preventive medications, such as corticosteroids and cromoglycate. Pregnancy and lactation. Salbutamol and terbutaline can be used by pregnant women, as well as fenoterol and heksoprenalin after the 16th week. salbutamol. Terbutaline, and salmeterol reach the breast milk. Of other drugs have not been there enough data to assess its safety; in animal experiments, it turns salmeterol fetal harm (3,4). Adrenergic drugs are often used as a bronchodilator:
Adrenergic substances with alpha + beta effect is strongest bronchodilator with rapid but short of work and is used for a great asthma attack. Often these compounds combined with tranquillizer orally to fight the fear and anxiety that accompanies an attack. Orally, adrenaline is not active. Side effects include central effects (restlessness, tremor, headache) and the heart palpitations, arrhythmias), especially at higher doses. Hyperglikemia also occur, due to the effects of oral antidiabetika weakened. Dose on asthma attacks i.v. 0.3 ml of a solution of 1: 1,000 which can be repeated twice every 20 meters (tartrate) (3,4).
Derivatives - The adrenaline has a central effect is stronger with effect bronchodilatation lighter and last longer (4 hours). Ephedrine can be administered orally it is widely used as an asthma medication (bounded free without prescription) in a variety of popular preparations, although side effects can be harmful. resorption well and within ¼ - 1 hour already occurred bronchodilatation. In the liver, partly overhauled substances mainly through urine excretion as a whole. Plasma her 3-6 ½ hours. Side effects, in people who are sensitive, ephedrine in low doses was able to cause trouble sleeping, tremors, anxiety and urinary disorders. At the overdose, arising adverse effects on the CNS and the heart (palpitations) (3,4).
This derivative has the effect of b1 + b2 bronchodilatation adrenergics and has good power but resorption in poor and irregular bowel. resorption of mouth (as tablets or solution oromucosal somewhat better and faster, and the effect has been raised after a few minutes and last up to 1 hours. Its use as an asthma drug has been driven by adrenergika with specific properties without the effects of beta-1 (heart), so the more rare side effects. Similarly, the decline, as mentioned below, should not be used again (3.4).
Are isomers of isoprenaline with better resorption, the effect starts slower (15-20 min after oral but last longer, up to 4 hours. Begin working through inhalation or injection is after 10 minutes. 4 dose dd 20 mg (sulfate), i.m. or s.c. 0.5 mg which can be repeated after ½ hour, inhalation 3-4 dd 2 sprays (3.4).
Derivatives isoprenaline is first adrenergik (1986) that the usual dose has less power over the specific work to b2 receptors. besides helpless bronchodilatation good, salbutamol also has a weak effect on the stabilization mastcell, it is very effective in preventing or eliminating asthma attack. Today this drug is commonly used in the form of an aerosol dose-effect since rapidly with milder side effects than oral use. At the time of inhalation seruk halsu or solution, approximately 80% to reach the trachea, but only 7 -8% of the tiniest (1-5 microns) arrived in bronchioli and lung. Side effects are rare and usually include headache, dizziness, nausea, and hand tremors. At the overdose can occur b-1 receptor stimulation with cardiovascular effects: tachycardia, palpitations, arrhythmias, and hypotension. It is therefore very important to give instructions carefully in order not to repeat the inhalation in a very short time, because it can happen tachyfylaxis (drug effect decreases rapidly in use too often). Dose of 2-4 dd mg 3-4 (sulfate) inhalation 3-4 dd of 2 sprays 100 mcg, 2 puffs on an acute attack can be repeated after 15 minutes. In the onslaught i.m. or s.c. 250-500 mcg, which can be repeated after 4 hours (3,4).
Methyl derivative of orciprenaline (1970) is also efficacious selective b2. Orally, started working after 1-2 hours, while his long ca 6 hours. More often result in tachycardia. Doses 2-3 dd of 2.5-5 mg (sulfate) inhalation 3-4 dd of 1-2 sprays 250 mcg, maximum 16 puffs a day, sc 250 mcg, a maximum of 4 times a day (3.4).
Terbutaline is a derivative of the power and use of the same work. The effect was stronger and lasted ca 6 hours, longer than salbutamol (ca 4 h). Dose: 3 dd 2.5-5 mg (bromide), 15 mg suppository night, and inhalation 3-4 dd of 1-2 sprays 200 mcg (3.4).
2. Antikolinergika
In the smooth muscle cells there is a balance between system adrenergis and cholinergic systems. If for whatever reason the system adrenergis b2 receptors are blocked, then the cholinergic system will power the bronchokonstriksi result. Antikolimengika block muscarine receptors on cholinergic nerves in the smooth muscle of the bronchi, until adrenergis nerve activity becomes dominant with bronchodilatasi effect. Use primarily for maintenance therapy HRB, but also useful to exclude an acute asthma attack (via inhalation with rapid effect). Undesirable side effect is that it is thicken phlegm and tachycardia, which often interfere with therapy. Which is also known atropine effects, such as dry mouth, obstipation, difficulty urinating, and blurred vision due to disturbance of accommodation. Its use as an inhalation relieve these side effects (3,4).
Examples of anticholinergic drugs are often used as a bronchodilator: Ipratropium:
Atrovent -N-propyl derivatives of this atropine (1974) bronchodilatasi efficacious, as against the formation of cGMP that cause constriction. Ipratropin helpless reduce hypersecretion in the bronchi, the drying effect of the drug antikolinergika, it is very effective in patients who spend a lot of phlegm. In particular is used as inhalation, the effect begins more slowly (15 minutes) of the b2-mimetika. The maximum effect is achieved after 1-2 hours and lasted an average of 6 hours. Very effective as a preventive medicine and maintenance, especially in chronic bronchitis. Now, these substances are not used (anymore) as monotherapy (maintenance), but always with kortikosteroida-inhalation. Combination with b2-mimetika strengthening effect (addition). Resorpsinya orally bad (like all quaternary ammonium compounds). In tracheal just local work and practically not absorbed. The advantage is that these substances can also be used by cardiac patients who can not tolerate adrenergika. The side effects are rare and usually a dry mouth, nausea, headache, and dizziness. Dose inhaled 3-4 dd of 20 mcg 2 sprays (bromide) (3.4).
3. Derivatives Xanthin: theophylline, aminophylline
Bronchorelaksasinya power is estimated based on the blockade of adenosine receptors. In addition, theophylline as cromoglycate prevent increased hiperektivitas and prophylaxis based on this work. Resorption of theophylline derivatives is very different; it is best to theophylline microfine (particle size 1-5 microns) and their salts and kolinteofilinat aminophylline. Its use continuous maintenance therapy was effective in reducing the frequency and great attack. In the acute situation (infection aminophylline) may be combined with other acidic drugs, but the combination with b2-mimetika should be used with caution relate these two types of mutually reinforcing effects of drugs on the heart. Combination with ephedrine (Asmadex, Asmasolon) practically does not increase bronchodilatasi effect, whereas the effect on the heart and central effects of highly amplified. Because of this, the combination of such preparations is not recommended, especially for the elderly. Sustanined release tablets (125-250 mg retard Euphyllin) is efketif to obtain a constant blood levels, especially at bedtime and thus prevent attacks midnight and morning dip (3.4).
Pregnancy and lactation
Theophylline is safe for pregnant women. Because it can reach the breast milk, mothers should breastfeed their babies before ingesting this drug (3,4). Xanthin class of drugs that are often used as a bronchodilator
This alkaloids (1908) are shared kofein (trimethylxanthine) in tea leaves (Yuntheos = God, phykllon = leaf) and has a number of benefits including spasmolitis powerless against smooth muscle, especially the bronchi muscles, stimulates the heart inotropic positive effect) and dilate. Theophylline also stimulates the central nervous system and respiratory, as well as a weak diuretic and speedy work. Kofein also has all these properties although weaker, except for the effect of a stronger central stimulation. Now, the drug is widely used as a drug prevention and treatment of asthma attack. Bronchodilatasinya effects did not correlate well with the dose, but showed a clear relationship with levels in blood and saliva levels. Terapeutisnya narrowly wide, meaning that the effective dose is located adjacent to toksisnya dose. Required for optimal effect in the blood levels of 10-15 mcg / ml, whereas at 20 mcg / ml have toxic effects occur. Therefore, it is recommended to assign individual doses based on demand levels in the blood. This is especially necessary in children under 2 years of age and in the elderly over 60 years, which is very sensitive to overdose, also in patients with liver and kidney disorders. Treatment with theophylline should be guided by the determination of levels in the blood. Resorpsinya in poor and irregular bowel. That is why this old bronchodilator (1935), formerly rarely used. Only in the 1970s, it is known that complete resorption can be when used in the form of microfine seruk. (particle size of 5-10 microns) as well as on the use of the solution, which is 20% alcohol added as necessary. Plasma t ½ of her 3-7 hours, lasting as acid excretion through the urinary metilurat and only 10% in one piece. Theophylline should be used as preparation 'sutanined release' which provide a constant resorption and levels in the blood more regularly. The most important side effects include nausea and vomiting, both in the use of oral or rectal or parenteral. At the overdose occurred central effects (anxiety, sleeplessness, tremors, and convulsions) and respiratory disorders, as well as cardiovascular effects, such as tachycardia, arrhythmia, and hypotension. Small children are very sensitive to the side effects of theophylline. doses 3-4 dd 125-250 mg microfine (retard). 1 mg teofilin 0 aq = 1,1 g teofilin 1 aq = 1,17 g aminofilin 0 aq = 1,23 g aminofilin 1 aq (3,4).
Is the salt in the blood release theophylline back. This salt is alkaline and highly stimulating the mucous membrane, thus often resulting orally gastric disorders (nausea, vomiting), as well as on the use of the suppository and intramuscular injection (pain). In an asthma attack, the drug is used as an iv injection
Air enters the lungs through the main airways (bronchi) and then go into the smaller airways (bronchioles), then into the alveoli. Difficulty breathing include shortness of breath, coughing and wheezing, which is normally as a result of narrowing of the lumen of the bronchioles so that the air space to pass more narrow.
(1.2) Bronchodilators are drugs used to treat breathing difficulties caused by asthma, bronchitis, bronchiolitis, pneumonia and emphysema. Bronchodilators dilate the bronchi and bronchioles that increase airflow. Bronchodilators may be endogenous substance or a medicine used to treat breathing difficulties.(1,2)
CHAPTER II
Drugs Bronchodilators Main types of bronchodilators:
- Adrenergic
- Anticholinergics
- Xanthin
1. Adrenergic
Used is b2-sympathomimetic (short b2-mimetic) the following: salbutamol, terbulatine, tretoquinol, fenoterol, rimiterol, prokaterol (Meptin), and klenbuterol (Spriropent). After all, a long-acting drug that is rather new, the salmoterol and formoterol (dorudil). These substances work more or less selective for the receptor b2 Adrenergis and not practical to receptors- b1 (cardiac stimulation). Drugs with effects on both receptors should not be used anymore in its effect on the heart, such as ephedrine, inprenalin, orsiprenalin and heksoprenalin. The exception is adrenaline (receptors and b) are very effective in the state of chaos. Its mechanism of action is through stimulation of b2 receptors in the trachea (windpipe) and bronchi, which causes activation of adenilsiklase. This enzyme conversion strengthen adenosintrifosat (ATP) into energy-rich cyclic adenosine monophosphate-(cAMP) with the release of energy that is used for processes in the cell. Increased levels of cAMP in the cells produced some inhibitory effect bronchodilatasi and mediator release by mast cells. Its use initially as monotherapy continuous, which turns gradually increase the HRB and ultimately worsen lung function, because it does not address the inflammation and increased sensitivity to allergens in allergic patients. Therefore, since a few years only used to counter attack as maintenance or in combination with preventive medications, such as corticosteroids and cromoglycate. Pregnancy and lactation. Salbutamol and terbutaline can be used by pregnant women, as well as fenoterol and heksoprenalin after the 16th week. salbutamol. Terbutaline, and salmeterol reach the breast milk. Of other drugs have not been there enough data to assess its safety; in animal experiments, it turns salmeterol fetal harm (3,4). Adrenergic drugs are often used as a bronchodilator:
- Adrenaline epinephrine Lidonest 2%.
Adrenergic substances with alpha + beta effect is strongest bronchodilator with rapid but short of work and is used for a great asthma attack. Often these compounds combined with tranquillizer orally to fight the fear and anxiety that accompanies an attack. Orally, adrenaline is not active. Side effects include central effects (restlessness, tremor, headache) and the heart palpitations, arrhythmias), especially at higher doses. Hyperglikemia also occur, due to the effects of oral antidiabetika weakened. Dose on asthma attacks i.v. 0.3 ml of a solution of 1: 1,000 which can be repeated twice every 20 meters (tartrate) (3,4).
- Ephedrine: * Asmadex, * Asmasolon, * Bronchicum "
Derivatives - The adrenaline has a central effect is stronger with effect bronchodilatation lighter and last longer (4 hours). Ephedrine can be administered orally it is widely used as an asthma medication (bounded free without prescription) in a variety of popular preparations, although side effects can be harmful. resorption well and within ¼ - 1 hour already occurred bronchodilatation. In the liver, partly overhauled substances mainly through urine excretion as a whole. Plasma her 3-6 ½ hours. Side effects, in people who are sensitive, ephedrine in low doses was able to cause trouble sleeping, tremors, anxiety and urinary disorders. At the overdose, arising adverse effects on the CNS and the heart (palpitations) (3,4).
- isoprenaline: Isuprel Aleudrin
This derivative has the effect of b1 + b2 bronchodilatation adrenergics and has good power but resorption in poor and irregular bowel. resorption of mouth (as tablets or solution oromucosal somewhat better and faster, and the effect has been raised after a few minutes and last up to 1 hours. Its use as an asthma drug has been driven by adrenergika with specific properties without the effects of beta-1 (heart), so the more rare side effects. Similarly, the decline, as mentioned below, should not be used again (3.4).
- Orsiprenalin (metaproterenol, Alupent, Silomat comp)
Are isomers of isoprenaline with better resorption, the effect starts slower (15-20 min after oral but last longer, up to 4 hours. Begin working through inhalation or injection is after 10 minutes. 4 dose dd 20 mg (sulfate), i.m. or s.c. 0.5 mg which can be repeated after ½ hour, inhalation 3-4 dd 2 sprays (3.4).
- Salbutamol: ventolin, salbuven
Derivatives isoprenaline is first adrenergik (1986) that the usual dose has less power over the specific work to b2 receptors. besides helpless bronchodilatation good, salbutamol also has a weak effect on the stabilization mastcell, it is very effective in preventing or eliminating asthma attack. Today this drug is commonly used in the form of an aerosol dose-effect since rapidly with milder side effects than oral use. At the time of inhalation seruk halsu or solution, approximately 80% to reach the trachea, but only 7 -8% of the tiniest (1-5 microns) arrived in bronchioli and lung. Side effects are rare and usually include headache, dizziness, nausea, and hand tremors. At the overdose can occur b-1 receptor stimulation with cardiovascular effects: tachycardia, palpitations, arrhythmias, and hypotension. It is therefore very important to give instructions carefully in order not to repeat the inhalation in a very short time, because it can happen tachyfylaxis (drug effect decreases rapidly in use too often). Dose of 2-4 dd mg 3-4 (sulfate) inhalation 3-4 dd of 2 sprays 100 mcg, 2 puffs on an acute attack can be repeated after 15 minutes. In the onslaught i.m. or s.c. 250-500 mcg, which can be repeated after 4 hours (3,4).
- Terbutaline: Bricasma, Bricanyl
Methyl derivative of orciprenaline (1970) is also efficacious selective b2. Orally, started working after 1-2 hours, while his long ca 6 hours. More often result in tachycardia. Doses 2-3 dd of 2.5-5 mg (sulfate) inhalation 3-4 dd of 1-2 sprays 250 mcg, maximum 16 puffs a day, sc 250 mcg, a maximum of 4 times a day (3.4).
- fenoterol (berotec)
Terbutaline is a derivative of the power and use of the same work. The effect was stronger and lasted ca 6 hours, longer than salbutamol (ca 4 h). Dose: 3 dd 2.5-5 mg (bromide), 15 mg suppository night, and inhalation 3-4 dd of 1-2 sprays 200 mcg (3.4).
2. Antikolinergika
In the smooth muscle cells there is a balance between system adrenergis and cholinergic systems. If for whatever reason the system adrenergis b2 receptors are blocked, then the cholinergic system will power the bronchokonstriksi result. Antikolimengika block muscarine receptors on cholinergic nerves in the smooth muscle of the bronchi, until adrenergis nerve activity becomes dominant with bronchodilatasi effect. Use primarily for maintenance therapy HRB, but also useful to exclude an acute asthma attack (via inhalation with rapid effect). Undesirable side effect is that it is thicken phlegm and tachycardia, which often interfere with therapy. Which is also known atropine effects, such as dry mouth, obstipation, difficulty urinating, and blurred vision due to disturbance of accommodation. Its use as an inhalation relieve these side effects (3,4).
Examples of anticholinergic drugs are often used as a bronchodilator: Ipratropium:
Atrovent -N-propyl derivatives of this atropine (1974) bronchodilatasi efficacious, as against the formation of cGMP that cause constriction. Ipratropin helpless reduce hypersecretion in the bronchi, the drying effect of the drug antikolinergika, it is very effective in patients who spend a lot of phlegm. In particular is used as inhalation, the effect begins more slowly (15 minutes) of the b2-mimetika. The maximum effect is achieved after 1-2 hours and lasted an average of 6 hours. Very effective as a preventive medicine and maintenance, especially in chronic bronchitis. Now, these substances are not used (anymore) as monotherapy (maintenance), but always with kortikosteroida-inhalation. Combination with b2-mimetika strengthening effect (addition). Resorpsinya orally bad (like all quaternary ammonium compounds). In tracheal just local work and practically not absorbed. The advantage is that these substances can also be used by cardiac patients who can not tolerate adrenergika. The side effects are rare and usually a dry mouth, nausea, headache, and dizziness. Dose inhaled 3-4 dd of 20 mcg 2 sprays (bromide) (3.4).
3. Derivatives Xanthin: theophylline, aminophylline
Bronchorelaksasinya power is estimated based on the blockade of adenosine receptors. In addition, theophylline as cromoglycate prevent increased hiperektivitas and prophylaxis based on this work. Resorption of theophylline derivatives is very different; it is best to theophylline microfine (particle size 1-5 microns) and their salts and kolinteofilinat aminophylline. Its use continuous maintenance therapy was effective in reducing the frequency and great attack. In the acute situation (infection aminophylline) may be combined with other acidic drugs, but the combination with b2-mimetika should be used with caution relate these two types of mutually reinforcing effects of drugs on the heart. Combination with ephedrine (Asmadex, Asmasolon) practically does not increase bronchodilatasi effect, whereas the effect on the heart and central effects of highly amplified. Because of this, the combination of such preparations is not recommended, especially for the elderly. Sustanined release tablets (125-250 mg retard Euphyllin) is efketif to obtain a constant blood levels, especially at bedtime and thus prevent attacks midnight and morning dip (3.4).
Pregnancy and lactation
Theophylline is safe for pregnant women. Because it can reach the breast milk, mothers should breastfeed their babies before ingesting this drug (3,4). Xanthin class of drugs that are often used as a bronchodilator
- Theophylline: 1.3 dimryilkdsnyin, Quibron-T / SR Theobron.
This alkaloids (1908) are shared kofein (trimethylxanthine) in tea leaves (Yuntheos = God, phykllon = leaf) and has a number of benefits including spasmolitis powerless against smooth muscle, especially the bronchi muscles, stimulates the heart inotropic positive effect) and dilate. Theophylline also stimulates the central nervous system and respiratory, as well as a weak diuretic and speedy work. Kofein also has all these properties although weaker, except for the effect of a stronger central stimulation. Now, the drug is widely used as a drug prevention and treatment of asthma attack. Bronchodilatasinya effects did not correlate well with the dose, but showed a clear relationship with levels in blood and saliva levels. Terapeutisnya narrowly wide, meaning that the effective dose is located adjacent to toksisnya dose. Required for optimal effect in the blood levels of 10-15 mcg / ml, whereas at 20 mcg / ml have toxic effects occur. Therefore, it is recommended to assign individual doses based on demand levels in the blood. This is especially necessary in children under 2 years of age and in the elderly over 60 years, which is very sensitive to overdose, also in patients with liver and kidney disorders. Treatment with theophylline should be guided by the determination of levels in the blood. Resorpsinya in poor and irregular bowel. That is why this old bronchodilator (1935), formerly rarely used. Only in the 1970s, it is known that complete resorption can be when used in the form of microfine seruk. (particle size of 5-10 microns) as well as on the use of the solution, which is 20% alcohol added as necessary. Plasma t ½ of her 3-7 hours, lasting as acid excretion through the urinary metilurat and only 10% in one piece. Theophylline should be used as preparation 'sutanined release' which provide a constant resorption and levels in the blood more regularly. The most important side effects include nausea and vomiting, both in the use of oral or rectal or parenteral. At the overdose occurred central effects (anxiety, sleeplessness, tremors, and convulsions) and respiratory disorders, as well as cardiovascular effects, such as tachycardia, arrhythmia, and hypotension. Small children are very sensitive to the side effects of theophylline. doses 3-4 dd 125-250 mg microfine (retard). 1 mg teofilin 0 aq = 1,1 g teofilin 1 aq = 1,17 g aminofilin 0 aq = 1,23 g aminofilin 1 aq (3,4).
- Aminophylline (theophylline-ethylenediamine, Phyllocomtin continus, Euphylllin)
Is the salt in the blood release theophylline back. This salt is alkaline and highly stimulating the mucous membrane, thus often resulting orally gastric disorders (nausea, vomiting), as well as on the use of the suppository and intramuscular injection (pain). In an asthma attack, the drug is used as an iv injection
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