** Ipratropium bromide:
- (Anti muscarinic bronchodilator)
** Amphetamine act as:
- (INDIRECT-ACTING ADRENERGIC AGONIST)
** Increase plasma HDL Level:
- (Reduce Risk of Atherosclerosis)
** Waraferin act as:
- (inhibited blood clot ) anticoagulant.
bronchodilators:
1- The cholinergic system in the bronchi. Muscarinic receptors:
The cholinergic system is present at the bronchial level via the vagus nerve (X). This one takes its origin at the bulbar level.
It is composed of pre-ganglionic fibers connecting the parasympathetic centers (PΣ) to the P gang ganglia of the bronchi and postganglionic fibers joining the neuroeffective synapses at the different bronchial structures: smooth muscle, secretory glands, vessels ...
It includes 3 types of muscarinic receptors called M1, M2, M3, M1 receptors provide transmission to the ganglia, together with nicotinic receptors N1. M2 receptors are present at the presynaptic level of neuro-effector synapses.
They are stimulated by the acetylcholine released in the synaptic space and inhibit the release of the latter (negative feedback).
M3 receptors are postsynaptic and cause the systemic effects of acetylcholine: bronchoconstriction, bronchial hypersecretion, vasodilatation, plasma exudation etc ...
The cholinergic system is brought into play under the influence of the stimulation of the receptors for irritation, located in the bronchi under the influence of irritating agents (chlorine, tobacco smoke, SO2 ...) or mediators of the 'inflammation.
It is therefore possible to interrupt the cholinergic transmission with substances blocking M3 muscarinque receptors at the post-synaptic neuro-effector level or M1 at the ganglion level.
Theoretically, an M2 antagonist might facilitate the release of acetylcholine, but many studies have shown that the postsynaptic M2 receptor, coupled to adenylcyclase by a Gi protein, could inhibit the effects of β2 stimulants.
The currently marketed cholinergic antagonists for the treatment of asthma, ipratropium and oxytropium, are non-specific M1 M2 M3 antagonists.
A new drug should be marketed soon.
It is tiotropium, a long-acting M3 antagonist, a short-acting M2 antagonist.
In addition to asthma, the drug is interesting in the treatment of COPD.
2- Properties of anticholinergics:
Anticholinergics cause bronchodilatation since in humans the parasympathetic exerts a permanent bronchocontrictor effect.
Anticholinergics partially inhibit bronchospasm caused by various bronchoconstrictor agents via the receptors for irritation that require a cholinergic component (muscarinic receptors).
This action predominates on large bronchi (> 2 mm).
Asthma that best responds to anticholinergics are those in which the irritative component is important, such as exercise asthma. An effect on the inhibition of mast cell degranulation is envisaged.
Bronchial secretions do not appear to be significantly modified.
3- Route of administration:
inhaled route (refer to the text of the section beta2-adrenergic agonists).
4- Indications:
- Symptomatic treatment of the asthma attack, in addition to a beta2mimetic of rapid action and short duration by inhalation (1 to 2 puffs at the first symptoms)
- Symptomatic treatment of exacerbations during asthmatic disease or chronic obstructive bronchitis, in addition to a fast-acting, short-acting beta2 mimetic by inhalation (1 to 2 puffs at the first symptoms)
- Continuous symptomatic treatment of reversible bronchospasm of chronic obstructive pulmonary disease (1 to 2 puffs 2 to 4 times / daily).
Do not exceed 16 puffs / day
There are specialties that combine an anticholinergic and a short and fast-acting β2-stimulant (suspension for inhalation and powder for inhalation), also indicated in the prevention of exercise asthma and the treatment of COPD.
5- Undesirable effects:
Dryness of the mouth, pharyngeal irritation, coughing, paradoxical bronchospasm triggered by inhalation which contraindicate further treatment.
The systemic effects of inhaled anticholinergics are small because of the poor passage and the quaternary ammonium function which limits the crossing of the blood-brain barrier (little or no effect on the CNS).
- (Anti muscarinic bronchodilator)
** Amphetamine act as:
- (INDIRECT-ACTING ADRENERGIC AGONIST)
** Increase plasma HDL Level:
- (Reduce Risk of Atherosclerosis)
** Waraferin act as:
- (inhibited blood clot ) anticoagulant.
bronchodilators:
1- The cholinergic system in the bronchi. Muscarinic receptors:
The cholinergic system is present at the bronchial level via the vagus nerve (X). This one takes its origin at the bulbar level.
It is composed of pre-ganglionic fibers connecting the parasympathetic centers (PΣ) to the P gang ganglia of the bronchi and postganglionic fibers joining the neuroeffective synapses at the different bronchial structures: smooth muscle, secretory glands, vessels ...
It includes 3 types of muscarinic receptors called M1, M2, M3, M1 receptors provide transmission to the ganglia, together with nicotinic receptors N1. M2 receptors are present at the presynaptic level of neuro-effector synapses.
They are stimulated by the acetylcholine released in the synaptic space and inhibit the release of the latter (negative feedback).
M3 receptors are postsynaptic and cause the systemic effects of acetylcholine: bronchoconstriction, bronchial hypersecretion, vasodilatation, plasma exudation etc ...
The cholinergic system is brought into play under the influence of the stimulation of the receptors for irritation, located in the bronchi under the influence of irritating agents (chlorine, tobacco smoke, SO2 ...) or mediators of the 'inflammation.
It is therefore possible to interrupt the cholinergic transmission with substances blocking M3 muscarinque receptors at the post-synaptic neuro-effector level or M1 at the ganglion level.
Theoretically, an M2 antagonist might facilitate the release of acetylcholine, but many studies have shown that the postsynaptic M2 receptor, coupled to adenylcyclase by a Gi protein, could inhibit the effects of β2 stimulants.
The currently marketed cholinergic antagonists for the treatment of asthma, ipratropium and oxytropium, are non-specific M1 M2 M3 antagonists.
A new drug should be marketed soon.
It is tiotropium, a long-acting M3 antagonist, a short-acting M2 antagonist.
In addition to asthma, the drug is interesting in the treatment of COPD.
2- Properties of anticholinergics:
Anticholinergics cause bronchodilatation since in humans the parasympathetic exerts a permanent bronchocontrictor effect.
Anticholinergics partially inhibit bronchospasm caused by various bronchoconstrictor agents via the receptors for irritation that require a cholinergic component (muscarinic receptors).
This action predominates on large bronchi (> 2 mm).
Asthma that best responds to anticholinergics are those in which the irritative component is important, such as exercise asthma. An effect on the inhibition of mast cell degranulation is envisaged.
Bronchial secretions do not appear to be significantly modified.
3- Route of administration:
inhaled route (refer to the text of the section beta2-adrenergic agonists).
4- Indications:
- Symptomatic treatment of the asthma attack, in addition to a beta2mimetic of rapid action and short duration by inhalation (1 to 2 puffs at the first symptoms)
- Symptomatic treatment of exacerbations during asthmatic disease or chronic obstructive bronchitis, in addition to a fast-acting, short-acting beta2 mimetic by inhalation (1 to 2 puffs at the first symptoms)
- Continuous symptomatic treatment of reversible bronchospasm of chronic obstructive pulmonary disease (1 to 2 puffs 2 to 4 times / daily).
Do not exceed 16 puffs / day
There are specialties that combine an anticholinergic and a short and fast-acting β2-stimulant (suspension for inhalation and powder for inhalation), also indicated in the prevention of exercise asthma and the treatment of COPD.
5- Undesirable effects:
Dryness of the mouth, pharyngeal irritation, coughing, paradoxical bronchospasm triggered by inhalation which contraindicate further treatment.
The systemic effects of inhaled anticholinergics are small because of the poor passage and the quaternary ammonium function which limits the crossing of the blood-brain barrier (little or no effect on the CNS).
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