Ipratropium
Encyclopedia
Ipratropium bromide is an anticholinergic
drug used for the treatment of chronic obstructive pulmonary disease
and acute asthma
. It blocks the muscarinic acetylcholine receptor
s in the smooth muscles of the bronchi in the lungs, opening the bronchi.
(COPD).
Ipratropium is also combined with salbutamol
(albuterol, USA) under the trade names Combivent (metered-dose inhaler or MDI) and Duoneb (nebulizer
) for the management of COPD and asthma
, and with fenoterol
(trade names Duovent and Berodual N) for the management of asthma.
Ipratropium can reduce rhinorrhea
but will not help nasal congestion.
to atropine
and related substances. For oral administration, contraindications are similar to other anticholinergics; they include narrow angle glaucoma
and obstructions in the gastrointestinal tract
and urinary system
.
s are minimal. However, dry mouth and sedation have been reported. Also, effects such as skin flushing, tachycardia, acute angle ocular dislocure, nausea, palpitations and headache have been observed. Inhaled ipratropium does not decrease mucociliary clearance
. The inhalation itself can cause headache and irritation of the throat in a few percent of patients.
Some studies suggest that patients with peanut allergies may have a anaphylactic response to atrovent.
Urinary retention has been reported in patients receiving doses by nebulizer. As a result, caution may be warranted, especially by in men with prostatic hypertrophy.
(cGMP), resulting in an increase of cGMP concentration. Most likely due to actions of cGMP on intracellular calcium, this results in decreased contractility of smooth muscle in the lung, inhibiting bronchoconstriction
and mucus
secretion
. It is a nonselective muscarinic antagonist
, and does not diffuse into the blood, which prevents systemic side effects. Ipratropium is a derivative of atropine
but is a quaternary amine and therefore does not cross the blood-brain barrier
, which prevents central side effects (anticholinergic syndrome). Ipratropium is considered a short-acting bronchodilator.
and other xanthine
derivatives, increases the dilating effect on the bronchi. Interactions with other anticholinergics like tricyclic antidepressant
s, antiparkinson drugs and quinidine
, which theoretically increase side effects, are clinically irrelevant when ipratropium is administered as an inhalant.
Anticholinergic
An anticholinergic agent is a substance that blocks the neurotransmitter acetylcholine in the central and the peripheral nervous system. An example of an anticholinergic is dicycloverine, and the classic example is atropine....
drug used for the treatment of chronic obstructive pulmonary disease
Chronic obstructive pulmonary disease
Chronic obstructive pulmonary disease , also known as chronic obstructive lung disease , chronic obstructive airway disease , chronic airflow limitation and chronic obstructive respiratory disease , is the co-occurrence of chronic bronchitis and emphysema, a pair of commonly co-existing diseases...
and acute asthma
Asthma
Asthma is the common chronic inflammatory disease of the airways characterized by variable and recurring symptoms, reversible airflow obstruction, and bronchospasm. Symptoms include wheezing, coughing, chest tightness, and shortness of breath...
. It blocks the muscarinic acetylcholine receptor
Muscarinic acetylcholine receptor
Muscarinic receptors, or mAChRs, are acetylcholine receptors that form G protein-coupled in the plasma membranes of certain neurons and other cells...
s in the smooth muscles of the bronchi in the lungs, opening the bronchi.
Uses
It is administered by inhalation for the treatment of chronic obstructive pulmonary diseaseChronic obstructive pulmonary disease
Chronic obstructive pulmonary disease , also known as chronic obstructive lung disease , chronic obstructive airway disease , chronic airflow limitation and chronic obstructive respiratory disease , is the co-occurrence of chronic bronchitis and emphysema, a pair of commonly co-existing diseases...
(COPD).
Ipratropium is also combined with salbutamol
Ipratropium/salbutamol
The combination preparation ipratropium bromide/salbutamol is a formulation containing ipratropium bromide and salbutamol sulfate used in the management of chronic obstructive pulmonary disease and asthma...
(albuterol, USA) under the trade names Combivent (metered-dose inhaler or MDI) and Duoneb (nebulizer
Nebulizer
In medicine, a nebulizer is a device used to administer medication in the form of a mist inhaled into the lungs....
) for the management of COPD and asthma
Asthma
Asthma is the common chronic inflammatory disease of the airways characterized by variable and recurring symptoms, reversible airflow obstruction, and bronchospasm. Symptoms include wheezing, coughing, chest tightness, and shortness of breath...
, and with fenoterol
Fenoterol
Fenoterol is an asthma medication designed to open up the airways to the lungs. It is classed as sympathomimetic beta2 agonist.Fenoterol is produced and sold by Boehringer Ingelheim as Berotec N and in combination with ipratropium as Berodual N....
(trade names Duovent and Berodual N) for the management of asthma.
Ipratropium can reduce rhinorrhea
Rhinorrhea
Rhinorrhea or rhinorrhoea is a condition where the nasal cavity is filled with a significant amount of mucous fluid. The condition, commonly known as "runny nose", occurs relatively frequently and is not usually considered dangerous. Rhinorrhea is a common symptom of allergies or certain diseases,...
but will not help nasal congestion.
Contraindications
There are no contraindications for inhaled ipratropium, apart from hypersensitivityHypersensitivity
Hypersensitivity refers to undesirable reactions produced by the normal immune system, including allergies and autoimmunity. These reactions may be damaging, uncomfortable, or occasionally fatal. Hypersensitivity reactions require a pre-sensitized state of the host. The four-group classification...
to atropine
Atropine
Atropine is a naturally occurring tropane alkaloid extracted from deadly nightshade , Jimson weed , mandrake and other plants of the family Solanaceae. It is a secondary metabolite of these plants and serves as a drug with a wide variety of effects...
and related substances. For oral administration, contraindications are similar to other anticholinergics; they include narrow angle glaucoma
Glaucoma
Glaucoma is an eye disorder in which the optic nerve suffers damage, permanently damaging vision in the affected eye and progressing to complete blindness if untreated. It is often, but not always, associated with increased pressure of the fluid in the eye...
and obstructions in the gastrointestinal tract
Gastrointestinal tract
The human gastrointestinal tract refers to the stomach and intestine, and sometimes to all the structures from the mouth to the anus. ....
and urinary system
Urinary system
The urinary system is the organ system that produces, stores, and eliminates urine. In humans it includes two kidneys, two ureters, the bladder and the urethra.-Kidney:...
.
Side effects
If ipratropium is inhaled, side effects resembling those of other anticholinergicAnticholinergic
An anticholinergic agent is a substance that blocks the neurotransmitter acetylcholine in the central and the peripheral nervous system. An example of an anticholinergic is dicycloverine, and the classic example is atropine....
s are minimal. However, dry mouth and sedation have been reported. Also, effects such as skin flushing, tachycardia, acute angle ocular dislocure, nausea, palpitations and headache have been observed. Inhaled ipratropium does not decrease mucociliary clearance
Mucociliary Clearance
Mucociliary clearance, also referred to as mucociliary apparatus or mucociliar clearance , derived from mucus , cilia and clearance describes the self-clearing mechanism of the bronchi.The main bronchi down to the alveoli are lined with a respiratory epithelium...
. The inhalation itself can cause headache and irritation of the throat in a few percent of patients.
Some studies suggest that patients with peanut allergies may have a anaphylactic response to atrovent.
Urinary retention has been reported in patients receiving doses by nebulizer. As a result, caution may be warranted, especially by in men with prostatic hypertrophy.
Pharmacology
It blocks muscarinic acetylcholine receptors, without specificity for subtypes, and therefore inhibits degradation of cyclic guanosine monophosphateCyclic guanosine monophosphate
Cyclic guanosine monophosphate is a cyclic nucleotide derived from guanosine triphosphate . cGMP acts as a second messenger much like cyclic AMP...
(cGMP), resulting in an increase of cGMP concentration. Most likely due to actions of cGMP on intracellular calcium, this results in decreased contractility of smooth muscle in the lung, inhibiting bronchoconstriction
Bronchoconstriction
Bronchoconstriction is the constriction of the airways in the lungs due to the tightening of surrounding smooth muscle, with consequent coughing, wheezing, and shortness of breath. Bronchoconstriction can also be due to an accumulation of thick mucus....
and mucus
Mucus
In vertebrates, mucus is a slippery secretion produced by, and covering, mucous membranes. Mucous fluid is typically produced from mucous cells found in mucous glands. Mucous cells secrete products that are rich in glycoproteins and water. Mucous fluid may also originate from mixed glands, which...
secretion
Secretion
Secretion is the process of elaborating, releasing, and oozing chemicals, or a secreted chemical substance from a cell or gland. In contrast to excretion, the substance may have a certain function, rather than being a waste product...
. It is a nonselective muscarinic antagonist
Receptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
, and does not diffuse into the blood, which prevents systemic side effects. Ipratropium is a derivative of atropine
Atropine
Atropine is a naturally occurring tropane alkaloid extracted from deadly nightshade , Jimson weed , mandrake and other plants of the family Solanaceae. It is a secondary metabolite of these plants and serves as a drug with a wide variety of effects...
but is a quaternary amine and therefore does not cross the blood-brain barrier
Blood-brain barrier
The blood–brain barrier is a separation of circulating blood and the brain extracellular fluid in the central nervous system . It occurs along all capillaries and consists of tight junctions around the capillaries that do not exist in normal circulation. Endothelial cells restrict the diffusion...
, which prevents central side effects (anticholinergic syndrome). Ipratropium is considered a short-acting bronchodilator.
Interactions
Combination with beta-adrenergic agonists, as well as theophyllineTheophylline
Theophylline, also known as dimethylxanthine, is a methylxanthine drug used in therapy for respiratory diseases such as COPD and asthma under a variety of brand names. Because of its numerous side-effects, the drug is now rarely administered for clinical use. As a member of the xanthine family, it...
and other xanthine
Xanthine
Xanthine , is a purine base found in most human body tissues and fluids and in other organisms. A number of stimulants are derived from xanthine, including caffeine and theobromine....
derivatives, increases the dilating effect on the bronchi. Interactions with other anticholinergics like tricyclic antidepressant
Tricyclic antidepressant
Tricyclic antidepressants are heterocyclic chemical compounds used primarily as antidepressants. The TCAs were first discovered in the early 1950s and were subsequently introduced later in the decade; they are named after their chemical structure, which contains three rings of atoms...
s, antiparkinson drugs and quinidine
Quinidine
Quinidine is a pharmaceutical agent that acts as a class I antiarrhythmic agent in the heart. It is a stereoisomer of quinine, originally derived from the bark of the cinchona tree.-Mechanism:...
, which theoretically increase side effects, are clinically irrelevant when ipratropium is administered as an inhalant.
See also
- EpinephrineEpinephrineEpinephrine is a hormone and a neurotransmitter. It increases heart rate, constricts blood vessels, dilates air passages and participates in the fight-or-flight response of the sympathetic nervous system. In chemical terms, adrenaline is one of a group of monoamines called the catecholamines...
- Beclometasone dipropionateBeclometasone dipropionateBeclometasone dipropionate or beclomethasone dipropionate , also referred to as beclometasone , is a potent glucocorticoid steroid. In the form of an inhaler , a wide number of brands of which are available, it is used for the prophylaxis of asthma. As a nasal spray Beclometasone dipropionate (INN...
- SalbutamolSalbutamolSalbutamol or albuterol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. It is marketed as Ventolin among other brand names....
- Ipratropium/salbutamolIpratropium/salbutamolThe combination preparation ipratropium bromide/salbutamol is a formulation containing ipratropium bromide and salbutamol sulfate used in the management of chronic obstructive pulmonary disease and asthma...