Friday, February 16, 2018

IPRATROPIUM BROMIDE- Anticholinergic drug side effects and its therapeutic uses

DESCRIPTION


PHARMACOLOGY-

Ipratropium exhibits bronchiolytic action by reducing cholinergic influence on the bronchial musculature. It blocks muscarinic acetylcholine receptors, without specificity for subtypes, and therefore promotes the degradation of cyclic guanosine monophosphate (cGMP), resulting in a decreased intracellular concentration of cGMP.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 not considered a short-acting bronchodilator and should never be used in place of salbutamol (albuterol) as a rescue medication.

MECHANISM OF ACTION-
Ipratropium bromide is an anticholinergic agent. It blocks muscarinic cholinergic receptors, without specificity for subtypes, resulting in a decrease in the formation of cyclic guanosine monophosphate (cGMP). Most likely due to actions of cGMP on intracellular calcium, this results in decreased contractility of smooth muscle.


SIDE EFFECTS-

If ipratropium is inhaled, side effects resembling those of other anticholinergics are minimal. However, dry mouth and sedation have been reported. Also, effects such as skin flushing, tachycardia, acute angle-closure glaucoma, 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.Urinary retention has been reported in patients receiving doses by nebulizer. As a result, caution may be warranted, especially by men with prostatic hypertrophy.

DRUG-DRUG INTERACTION-
1.The therapeutic efficacy of Ipratropium bromide can be decreased when used in combination with 1,10-Phenanthroline.
2. The metabolism of Ipratropium bromide can be decreased when combined with Abiraterone.
3.Aclidinium may increase the anticholinergic activities of Ipratropium bromide.
4.The risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Aclidinium.
5.The risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Alfentanil.
6.The risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Alphacetylmethadol.
7.The therapeutic efficacy of Ipratropium bromide can be decreased when used in combination with Ambenonium.

USES-
1,Ipratropium is administered by inhalation for the treatment of chronic obstructive pulmonary disease (COPD). For that purpose it is supplied in a canister for use in an inhaler or in single dose vials for use in a nebulizer.
2.It is also used to treat and prevent minor and moderate bronchial asthma, especially asthma that is accompanied by cardiovascular system diseases.
3.It is also combined with salbutamol under the trade names Combivent (metered-dose inhaler or MDI) and Duoneb (nebulizer) for the management of COPD and asthma, and with fenoterol for the management of asthma.
4. Ipratropium as a nasal solution sprayed into the nostrils can reduce rhinorrhea but will not help nasal congestion.
5.Combination with beta-adrenergic agonists, increases the dilating effect on the bronchi.


REFERENCE- Tripathi K.D. "Essentials of Medical Pharmacology", 7th Edition, page no- 116




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