Optra Hfa

Optra Hfa Uses, Dosage, Side Effects, Food Interaction and all others data.

Optra Hfa 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.

Optra Hfa 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 Optra Hfa
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 20mcg
Type Inhaler
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 Getz Pharma Pakistan (pvt) Ltd,
Available Country Pakistan
Last Updated: September 19, 2023 at 7:00 am
Optra Hfa
Optra Hfa

Uses

Optra Hfa Nebuliser Solution is used for a bronchodilator for maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease, including chronic bronchitis and emphysema.

Optra Hfa 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 Optra Hfa works

Optra Hfa 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

Optra Hfa dosage

Children over 3 years: The usual dose is 0.4-2.0 ml Optra Hfa 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 Optra Hfa 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.

Optra Hfa 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

Optra Hfa 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.

Volume of Distribution

Optra Hfa has a volume of distributions of 4.6 L/kg and hence, it is known to be highly distributed in the tissues.

Elimination Route

Optra Hfa 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

Optra Hfa 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 Optra Hfa Bromide during human pregnancy has not been established. The benefits of using Optra Hfa Bromide during a confirmed or suspected pregnancy must be weighed against possible hazards to the unborn child. It is not known whether Optra Hfa Bromide is excreted into breast milk.

Contraindication

Optra Hfa 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

Innovators Monograph

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*** Taking medicines without doctor's advice can cause long-term problems.
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