Ipratropium use in COPD

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Transcript Ipratropium use in COPD

Short acting anti-cholinergic
Ipratropium
Pharm D student : Eman Youssif
Supervised by : prof. Seham Hafez.
Ipratropium bromide is
a synthetic quaternary
ammonium
antimuscarinic
Chemically
related
to atropine.
Ipratropium use in COPD:
• ipratropium is a first-line maintenance
bronchodilator for relief of chronic (e.g., daily)
symptoms of bronchospasm in patients with mild
COPD.
• fixed combination of albuterol and ipratropium
results in greater bronchodilation following oral
inhalation than either agent given alone in patients
with COPD.
• combined therapy with a β2-agonist bronchodilator
and ipratropium is useful in patients with acute
exacerbations of COPD.
Ipratropium use in COPD:
Ipratrpium is not indicated for the initial treatment of
acute bronchospasm or acute exacerbation of COPD a β2adrenergic agonist may be preferred in such cases.
Orally inhaled ipratropium produce fewer adverse
effects than β2-adrenergic agonist
Ipratropium bromide (36 mcg 4 times daily) oral
inhalation aerosol with chlorofluorocarbon (CFC)
propellants was less effective than tiotropium (18 mcg
once daily) in improving lung function (e.g., as determined
by changes in FEV1 and peak expiratory flow rate [PEFR])
in patients with COPD.
Cholinergic nerve
transmission mediated by
acetylcholine.
Cholinergic muscarinic receptor subtype M1, showing effects
in the target cell mediated by the stimulatory G protein.
PIP2 phosphatidylinositol bisphosphate. DAG diacylglycerol.
Identification and location of muscarinic receptor subtypes M1, M2, and M3 in
the vagal nerve, submucosal gland, and bronchial smooth muscle in the airway,
showing nonspecific blockade by anticholinergic drugs.
•Administration
Ipratropium bromide is administered by oral inhalation using
an oral aerosol inhaler or via nebulization.
Ipratropium bromide is administered in fixed combination
with albuterol sulfate via a metered-dose aerosol inhaler or
via nebulization.
Patients should be advised that ipratropium must be used
consistently throughout the course of therapy for maximum
benefit. In addition, patients should be advised that the drug
will not provide immediate symptomatic relief and should not
be used for the relief of acute bronchospasm
.
If the conjunctiva is exposed to aerosolized anticholinergics (from a nebulizer,
metered-dose inhaler, or powder inhaler) the patient may develop anisocoria. The left
pupil is normal and the right pupil is dilated (mydriatic).
To avoid inadvertent contact of the drug with the eyes and subsequent adverse
effects, patients should be advised to close their eyes during inhalation of ipratropium
aerosol; it also has been suggested that ipratropium aerosol not be administered using
the open-mouth technique in patients at high risk for ocular toxicity
Compairing the efficacy and safety of ipratropium bromide/fenoterol hydrobromide
(IB/FEN; Berodual) delivered from the novel propellant-free Respimat Soft Mist Inhaler
(SMI) with that from a chlorofluorocarbon (CFC) metered-dose inhaler (MDI) plus
spacer in children with asthma. IB/FEN delivered via Respimat1SMI is at least as
effective as, and is as safe as, when delivered via CFC-MDI plus Aerochamber in
children with asthma. Use of Respimat SMI thus enables a 2–4-fold reduction in the
nominal dose of IB/FEN, and obviates the need for a spacer
dosage
Metred dose aerosol:
 a dose of 20–21 mcg of ipratropium bromide
per metered spray, this is the amount released
from the valve stem during actuation of the
inhaler; the dose of ipratropium bromide alone
or in fixed combination with albuterol sulfate
delivered to the patient through the
mouthpiece (actuator) is approximately 17 or 18
mcg, respectively, per metered spray(2 puffs (34
mcg) by inhalation route 4 times per day).
Inhalatin via nebulizer:
 250–500 mcg 3 or 4 times daily .
Pharmacokinetics
Distribution
Quaternary ammonium antimuscarinics are
completely ionized and possess poor lipid solubility;
Side effects: because of the drug’s limited systemic
absorption, oral inhalation of ipratropium bromide
produces anticholinergic adverse effects (e.g.,
increased intraocular pressure, mydriasis, urinary
retention) less frequently than systemically
administered antimuscarinic drugs.
•Pregnancy, and Lactation
• There are no adequate and controlled studies
to date using orally inhaled ipratropium in
pregnant women, and the drug should be
used during pregnancy only when clearly
needed.
• The manufacturer recommends that orally
inhaled ipratropium be used with caution in
nursing women.
•
Drug Interactions
 Concomitant administration of ipratropium
and albuterol via nebulization has been
reported to increase intraocular pressure
(IOP) and precipitate acute angle-closure
glaucoma in susceptible individuals (i.e.,
individuals with untreated or undiagnosed
angle-closure glaucoma),
Stability
- Oral inhalation aerosol should be stored at 25 °C.
- Exposure to excessive humidity should be avoided
- Cooling of the propellants may decrease the internal
pressure of the canister and result in delivery of
particles too large to provide full therapeutic effect.
- Inhalation solutions for nebulization should be
protected from light
- solutions containing ipratropium bromide stable for 1
hour when mixed in a nebulizer prior to
administration.
oxitropium
Oxitropium bromide’s peak bronchodilation may take 60–90 min,
and its duration is 5–8 h. It has been available outside the United
States as Oxivent, in an MDI that delivers 100 g/puff. Oxitropium’s
bronchodilation effect is similar to that of ipratropium bromide, but
oxitropium is longer-lasting.The usual dose is 200 g, 2–3 times daily.
It is considered to have twice the strength of ipratropium per dose.
Although widely used for many years (alone or in combination with
short-acting agonists) for both maintenance treatment of stable
disease and exacerbation of airway obstruction, Boehringer
Ingelheim announced the discontinuation of Oxivent formulations
as of May 2004.
Thank you