Ipratropium
Ipratropium Uses, Dosage, Side Effects, Food Interaction and all others data.
Ipratropium Bromide is a quaternary ammonium compound with anticholinergic properties. It appears to inhibit vagal reflexes by antagonising the action of acetylcholine (the transmitter agent released from the vagus nerve). Anticholinergics prevent the increase in intracellular concentration of cyclic guanosine monophosphate (cyclic GMP) caused by interaction of acetylcholine with the muscarinic receptor on bronchial smooth muscle.
Ipratropium is a short-acting agent that inhibits the parasympathetic nervous system at the level of the airway which then produces bronchodilatation. The effect of this agent starts after 1-2 hours and it is known to last only from 4 to 6 hours. As part of the effect, ipratropium relaxes the bronchial airways which reverse the narrowing that accounts for wheezy breathing, chest tightness, cough and abnormal gas exchange.
In clinical trials where ipratropium was used in the initial management of status asthmaticus, it was demonstrated a clear benefit in pulmonary function in children and adults. However, the continuous use of ipratropium after an acute asthmatic attack is not proven to be significantly advantageous nor the prophylactic administration of this agent.
| Trade Name | Ipratropium |
| Availability | Prescription only |
| Generic | Ipratropium |
| Ipratropium Other Names | bromuro de ipratropio, Ipratropium ion |
| Related Drugs | Trelegy Ellipta, ProAir Digihaler, prednisone, Symbicort, Breo Ellipta, Ventolin, Xopenex, Ventolin HFA, Spiriva, Dulera |
| Weight | 250mcg/ml, , 21mcg/inh, 42mcg/inh |
| Type | Respirator Solution, Inhalation Solution, Nasal Spray |
| Formula | C20H30NO3 |
| Weight | Average: 332.463 Monoisotopic: 332.22202025 |
| Protein binding | The protein binding of ipratropium is very low as the level of circulating ipratropium is very minimal. The bound state represents only from 0-9% of the administered dose. |
| Groups | Approved, Experimental |
| Therapeutic Class | Anticholinergic bronchodilators |
| Manufacturer | Chemist Laboratories Limited |
| Available Country | Bangladesh, United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Ipratropium Nebuliser Solution is used for a bronchodilator for maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease, including chronic bronchitis and emphysema.
Ipratropium is also used to associated treatment for these conditions: Acute Exacerbation of Asthma, Asthma, Bronchospasm, Chronic Obstructive Pulmonary Disease (COPD), Nasal Congestion Associated With the Common Cold, Non-Allergic Rhinitis, Perennial Allergic Rhinitis (PAR), Rhinitis
How Ipratropium works
Ipratropium acts as an antagonist of the muscarinic acetylcholine receptor. This effect produces the inhibition of the parasympathetic nervous system in the airways and hence, inhibit their function. The function of the parasympathetic system in the airway is to generate bronchial secretions and constriction and hence, the inhibition of this action can lead to bronchodilation and fewer secretions.
At the cellular level, the diameter of the airways is controlled by the release of acetylcholine into the muscle cells causing them to contract and producing a narrow airway. Thus administration of ipratropium stops the activity of acetylcholine in the smooth muscle preventing the contraction and producing relaxed airways.
Dosage
Ipratropium dosage
Children over 3 years: The usual dose is 0.4-2.0 ml Ipratropium Bromide Solution (100-500 micrograms) up to three times daily.
Adults (including elderly and adolescents) over 12 years of age: The usual dose is 0.4-2.0 ml Ipratropium Bromide Solution (100-500 micrograms) up to four times daily.
Side Effects
Allergic-type reactions such as skin rash, angio-oedema of the tongue, lips and face, urticaria (including giant urticaria), laryngospasm and anaphylactic reactions have been reported, with positive rechallenge in some cases.
Toxicity
The reported LD50 in mice after oral administration of ipratropium is 1500 mg/kg. However, overdosage is not very likely due to the poor absorption of ipratropium.
Ipratropium was not shown to present carcinogenesis, teratogenesis not mutagenesis potential and it did not present effects on fertility. The only effect after high administration of ipratropium was a reduction in the conception rate.
Precaution
Ipratropium Bromide should be used with caution in patients predisposed to narrow-angle glaucoma, or with prostatic hyperplasia or bladder-neck obstruction.
Food Interaction
No interactions found.Ipratropium Drug Interaction
Moderate: tiotropium, tiotropiumUnknown: fluticasone / salmeterol, fluticasone / salmeterol, furosemide, furosemide, polyethylene glycol 3350, polyethylene glycol 3350, albuterol, albuterol, montelukast, montelukast, budesonide / formoterol, budesonide / formoterol, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol
Ipratropium Disease Interaction
Volume of Distribution
Ipratropium has a volume of distributions of 4.6 L/kg and hence, it is known to be highly distributed in the tissues.
Elimination Route
Ipratropium is a topically active but poorly absorbed agent. The lack of absorption potential in the mucosal surfaces is associated with the presence of a charge in the 5-valent nitrogen. The molecule itself presents very large topic effectiveness however, it does not produce detectable blood levels nor systemic effects.
Serum levels of ipratropium after oral or inhaled administration are very low, corresponding to only 1-2% of the administered dose. These low levels peak after 1-2 hours and it presents a low bioavailability of 2%.
Half Life
Ipratropium presents a short half-life of about 1.6 hours.
Clearance
The average clearance rate of ipratropium is of 2.3 L/min with a renal clearance of 0.9 L/min.
Elimination Route
About 80-100% of the administered dose of ipratropium is excreted in the urine leaving less than 20% of the dose to be eliminated through the feces. From the urine eliminated portion, almost all the drug is found unchanged.
However, when ipratropium is orally administered, due to its low absorption, most of the dose is recovered in the feces with a very minimal amount found in the urine.
Pregnancy & Breastfeeding use
The safety of Ipratropium Bromide during human pregnancy has not been established. The benefits of using Ipratropium Bromide during a confirmed or suspected pregnancy must be weighed against possible hazards to the unborn child. It is not known whether Ipratropium Bromide is excreted into breast milk.
Contraindication
Ipratropium Bromide solution should not be taken by patients with known hypersensitivity to atropine or its derivatives or to any other component of the product.
Storage Condition
Should be stored in cool and dry place
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