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Ipratropium

R03B - Other agents for obstructive airway diseases, inhalants ATC R03BB01 Small molecule approved 1986 Topical Natural product

JFDA label: ATROVENT N

Indications

Off-label

  • Pulmonary Disease, Chronic Obstructive

Contraindications

Source: openFDA

  • Ipratropium bromide and albuterol sulfate inhalation solution is contraindicated in patients with a history of hypersensitivity to any of its components, or to atropine and its derivatives. Absolute

Dosing

Source: openFDA

The recommended dose of ipratropium bromide and albuterol sulfate inhalation solution is one 3 mL vial administered 4 times per day via nebulization with up to 2 additional 3 mL doses allowed per day, if needed. Safety and efficacy of additional doses or increased frequency of administration of ipratropium bromide and albuterol sulfate inhalation solution beyond these guidelines has not been studied and the safety and efficacy of extra doses of albuterol sulfate or ipratropium bromide in addition to the recommended doses of ipratropium bromide and albuterol sulfate inhalation solution have not been studied. The use of ipratropium bromide and albuterol sulfate inhalation solution can be continued as medically indicated to control recurring bouts of bronchospasm. If a previously effective regimen fails to provide the usual relief, medical advice should be sought immediately, as this is often a sign of worsening COPD, which would require reassessment of therapy. A Pari-LC-Plus TM nebulizer (with face mask or mouthpiece) connected to a PRONEB TM compressor was used to deliver ipratropium bromide and albuterol sulfate inhalation solution to each patient in one U.S. clinical study. The safety and efficacy of ipratropium bromide and albuterol sulfate inhalation solution delivered by other nebulizers and compressors have not been established. Ipratropium bromide and albuterol sulfate inhalation solution should be administered via jet nebulizer connected to an air compressor with an adequate air flow, equipped with a mouthpiece or suitable face mask.

Warnings & Precautions

Source: openFDA

Warnings & Precautions

Paradoxical Bronchospasm In the clinical study of ipratropium bromide and albuterol sulfate inhalation solution, paradoxical bronchospasm was not observed. However, paradoxical bronchospasm has been observed with both inhaled ipratropium bromide and albuterol products and can be life-threatening. If this occurs, ipratropium bromide and albuterol sulfate inhalation solution should be discontinued immediately and alternative therapy instituted. Do Not Exceed Recommended Dose Fatalities have been reported in association with excessive use of inhaled products containing sympathomimetic amines and with the home use of nebulizers. Cardiovascular Effect Ipratropium bromide and albuterol sulfate inhalation solution, like other beta adrenergic agonists, can produce a clinically significant cardiovascular effect in some patients as measured by pulse rate, blood pressure, and/or symptoms. Although such effects are uncommon for ipratropium bromide and albuterol sulfate inhalation solution at recommended doses, if they occur, the drug may need to be discontinued. In addition, beta agonists have been reported to produce ECG changes, such as flattening of the T-wave, prolongation of the QTc interval, and ST segment depression. The clinical significance of these findings is unknown. Therefore, ipratropium bromide and albuterol sulfate inhalation solution, like other sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension. Immediate Hypersensitivity Reactions Immediate hypersensitivity reactions to albuterol and/or ipratropium bromide may occur after the administration of ipratropium bromide and albuterol sulfate inhalation solution as demonstrated by rare cases of urticaria, angioedema, rash, pruritus, oropharyngeal edema, bronchospasm, and anaphylaxis.

Pregnancy & Lactation

Pregnancy

FDA category B

Safe

Safe inhaled bronchodilator in pregnancy

Lactation

Caution Hale L3

Breastfeeding can be continued during ipratropium therapy.

Chemistry & Properties

2D structure
FormulaC20H30NO3+
Molecular weight332.46 g/mol
IUPAC name[(1R,5S)-8-methyl-8-propan-2-yl-8-azoniabicyclo[3.2.1]octan-3-yl] 3-hydroxy-2-phenylpropanoate
CAS60205-81-4
PubChem CID657309
InChIKeyOEXHQOGQTVQTAT-BHIXFJMTSA-N
logP2.85 (XLogP 2.6)
Polar surface area46.53 Ų
H-bond acceptors / donors3 / 1
Drug-likeness (QED)0.67
Lipinski violations0
SMILESCC(C)[N+]1(C)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(CO)c1ccccc1)C2

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability70.0%
Half-life0.908 h
Volume of distribution4.876 L/kg
Protein binding29.3%
BBB penetrantNo

Enzyme interactions

EnzymeRoleDetail
CYP3A4Substrate

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MATE2 (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OCT1 (Inhibitor)OCT2 (Inhibitor)OCTN2 (Inhibitor)P-gp (Inhibitor)MATE2 (Substrate)OCT(unspecified) (Substrate)OCT1 (Substrate)OCT2 (Substrate)OCTN1 (Substrate)OCTN2 (Substrate)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drugSeverityManagement
Acetylcholine moderate
Aclidinium moderate
Acrivastine moderate
Alimemazine moderate
Amitriptyline moderate
Amoxapine moderate
Aripiprazole moderate
Atropine moderate
Azatadine moderate
Belladonna moderate
Benzatropine moderate
Bethanechol moderate
Biperiden moderate
Brompheniramine moderate
Carbamoylcholine (ophthalmic) moderate
Carbinoxamine moderate
Cevimeline moderate
Chlorcyclizine moderate
Chlorpheniramine moderate
Chlorpromazine moderate
Clemastine moderate
Clidinium moderate
Clomipramine moderate
Clozapine moderate
Cyclizine moderate
Cyclobenzaprine moderate
Cyproheptadine moderate
Darifenacin moderate
Demecarium (ophthalmic) moderate
Desipramine moderate
Dexbrompheniramine moderate
Dicyclomine moderate
Dimenhydrinate moderate
Diphenhydramine moderate
Disopyramide moderate
Doxepin moderate
Doxepin (topical) moderate
Doxylamine moderate
Echothiophate (ophthalmic) moderate
Eluxadoline moderate

Showing 40 of 100+.

Registered Products (13)

BrandForm / strengthPackAgentCitizen (JOD)
Iprovent Child Solution 0.25 mg/2 ml 2 ml Land Of Medicine Drug Store 2.250
Demoren nebulizer solution (0.5+ 2.5)mg/2.5 ml amp Solution 2.5 mg, 0.5 mg 10 ampoule pack varies Al Hilal Drug Store 2.270
Iprovent Adult Solution 0.5 mg/2 ml 2 ml Land Of Medicine Drug Store 2.620
Decozal Complete Solution 0.5 mg/1 ml, 0.6 mg/1 ml 10 ml شركة عمان للصناعات الدوائية / Amman Pharmaceutical Indusries / General 3.700
ATROVENT N Spray anhydrous 20 mcg/Puff 10 ml The Jordan Drugstore Co 4.140
Demoren nebulizer solution (0.5+ 2.5)mg/2.5 ml amp Solution 2.5 mg, 0.5 mg 20 ampoule pack varies Al Hilal Drug Store 4.280
Otrivin Dual Relief nasal spray Spray 0.5 mg, 0.6 mg 10 ml Sukhtian Group 4.630
Duolin Respules Ampoule 500 mcg/2.5 mg 20 amp ORIENT DRUG STORE CO 4.640
Atrovent Vial 250 mcg/2 ml 2 ml The Jordan Drugstore Co 4.900
Demoren nebulizer solution (0.5+ 2.5)mg/2.5 ml amp Solution 2.5 mg, 0.5 mg 30 ampoule pack varies Al Hilal Drug Store 6.420
Atrovent Comp HFA 20mcg/50mcg Spray 20 mcg, 50 mcg 10 ml The Jordan Drugstore Co 6.780
Combivent Unit Dose Vial Vial 3 mg, anhydrous 500 mcg dose 2.5 ml The Jordan Drugstore Co 9.750
Demoren nebulizer solution (0.5+ 2.5)mg/2.5 ml amp Solution 2.5 mg, 0.5 mg 50 ampoule pack varies Al Hilal Drug Store 10.700