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Theophylline Anhydrous for Asthma: A Comprehensive Study

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Theophylline anhydrous is routinely advocated as a curative intervention for asthma. Continue reading to know more.

Medically reviewed by

Dr. Kaushal Bhavsar

Published At May 14, 2024
Reviewed AtMay 14, 2024

Overview:

Theophylline anhydrous is widely proposed for asthma (difficult breathing) treatment. It ameliorates asthma symptoms. The United States Food and Drug Administration extended marketing accreditation for Theophylline anhydrous in asthma patients. Moreover, Theophylline anhydrous is also advocated for other breathing troubles and respiratory illnesses. However, considering Theophylline’s ability to associate with a wide range of drugs, its practical applicability has been knocked down.

Drug Group:

The methylxanthine drug class accommodates Theophylline anhydrous. This class of drugs is specifically recognized for its potential to effectuate bronchodilation. The bronchodilatory attributes of methylxanthines render Theophylline anhydrous therapeutic efficacies in tackling asthma.

Available Doses and Dosage Forms:

1. Dosage Forms:

  • Oral Formulations: Tablet (slow or rapid-release), oral suspension, and capsule (slow or rapid-release) forms.

  • Intravenous Formulation: Dispensed into the vein.

2. Available Doses:

  • Theophylline anhydrous pills of strength 600 and 400 milligrams (mg).

For Patients:

What Is Asthma?

Asthma is a familiar lung condition that attenuates the air passage, affecting the lungs and the nose. It is this air passage that channels the breathing gasses. In asthma, the air passage lumen, which guides breathing air to the lung, shrinks down. Consequently, it limits the air stream that one's air passage can accommodate, making breathing laborious. The swelling of the breathing tract or mucus (phlegm) gathering collapses the lumen dimension drastically. It poses challenges for one to inspire as well as expire. Despite labored breathing, asthma often accompanies other manifestations like chest discomfort, noisy breathing (wheezing), coughing, and short breaths.

Certain elements can evoke or instigate asthmatic episodes. Some of the frequently recognized triggers include the following:

  • Exercise.

  • Cold weather.

  • Pollutants.

  • Irritant fumes.

  • Allergic particles.

  • Pollen grains.

Asthmatic exacerbation exposes one to breathing challenges. It dampens the respiratory patency and oxygen flow. Such instances call for timely interventions to reinstate unhindered breathing and oxygen availability.

How Does Theophylline Anhydrous Work?

Constriction or choking of the breathing track is encountered during asthma. Theophylline anhydrous, being a potent bronchodilator, mitigates choking by the bronchodilation mechanism. The bronchodilation is the process by which Theophylline opens out the breathing track. Widening happens by loosening up and unwinding the muscles that drape and frame the breathing tract. Theophylline signals the muscles to wind down, thus easing the passage and accommodating more air. This widening enables more breathing gasses to stream into the lungs. This is how Theophylline anhydrous works to tackle asthmatic manifestations.

What Is the Dosage of Theophylline Anhydrous?

400 to 600 milligrams (mg) is the proposed daily dose of theophilline. However, the patient’s Theophylline tolerance, therapeutic requirement, and asthma severity must be considered for definitive dose determination. The patient should heed the prescribed dose. Adhering to an apt dosage safeguards one from exposure to Theophylline toxicity issues.

How Effective Is Theophylline Anhydrous?

Response to Theophylline therapy is not uniform, and it projects individual variations. This individual variance may govern Theophylline’s clinical applicabilities. Furthermore, the patient response, the ailment being addressed, and its severity are the decisive parameters that pilot Theophylline’s potency. Theophylline anhydrous has been an assuring intervention for lung ailments encompassing chronic obstructive pulmonary disease (COPD - disorders that impede breathing). But, presently, with the invention of targeted modalities, Theophylline’s therapeutic usage elicited a drastic downfall. Many newer medicines surpassed the Theophylline’s therapeutic potencies and secured their positions as first-line interventions. However, Theophylline anhydrous is still advocated for specific asthma cases.

What Are the Things to Inform the Doctor Before Taking the Drug?

The following are some critical patient data that the doctor should be vigilant about:

  • Allergy History: Instances where the patient has had an allergic response to Theophylline.

  • Drug Allergy: Any other medicines or pills that prompted exaggerated reactivity or abnormalities.

  • Medical History: Relevant and irrelevant data about one’s health, including comorbidities and surgeries undergone.

  • Drug History: Comprehension of all the medicinal therapy one is undergoing, embracing dietary supplements, plant-based medicines, and others.

  • Pregnancy: One should determine their pregnancy status in advance for Theophylline therapy.

  • Lactation: Informing the doctor concerning the potential patient’s nursing status is imperative.

  • Smoking Habit: Tobacco can mitigate Theophylline’s potency. Therefore, one should expose one's tobacco usage habits well in advance.

How Is Theophylline Anhydrous Administered?

Since there are different Theophylline drug forms, the administration proceedings do vary. There are diverse pharmacological formulations in which Theophylline is being marketed. Theophylline in oral suspension and pill formulations is devoted to oral delivery. Concerning intravenous formulations, the drug dispensation has to be through veins. Intravenously delivered Theophylline directly strikes the circulation and facilitates its dissemination.

Ensuring uniformity concerning Theophylline delivery time and its co-ingestion with edibles or food around the course is a high priority. One can choose whether to have Theophylline alongside food or not. Having said that, whatever the person chooses should be adhered to till Theophylline drug course completion. If Theophylline is delivered to a starving gut (preferred mode of Theophylline intake), ensure the pill has been ingested with six to eight ounces of water (200 to 250 milliliters). Grinding or crumbling the slow-release Theophylline pill can facilitate and expedite theophylline uptake. This would bring out an abrupt ascent in Theophylline concentration, effectuating toxicity.

What Are the Side Effects of Theophylline Anhydrous?

Theophylline anhydrous can gravitate to certain side effects. Some of the frequently encountered side effects concerning Theophylline therapy encompass:

  • Trouble sleeping.

  • Headache.

  • Not feeling hungry.

  • Indigestion.

  • Stomach discomfort.

  • Diarrhea.

  • Uneasiness.

  • Impatience.

Heart racing, destabilized heart rate, awful vomiting, seizure (anomalous brain activity), labored breathing, and extensive skin reactions are encountered to be Theophylline’s grave responses, which necessitates a speedy intervention.

Dietary Considerations:

Certain foodstuffs, notably coffee, cola, tea, chocolate, and cocoa, could accentuate Theophylline's nervous excitation. One should withhold these drinkables and edibles until Theophylline therapy is wrapped up.

Missed Dose:

At times, one may miss the Theophylline dose delivery. In such instances, one can continue with the skipped dose if the upcoming dose ingestion time is not close enough. Likewise, if the next Theophylline dose is close, giving up that particular dose is prudent. In case one requires specifics on missed dose scenarios, seek medical advice.

Overdose:

Theophylline anhydrous holds an augmented potential for overdose. Even if the ingested Theophylline dose surpasses the prescribed amount in negligible proportion or margin, it may call forth Theophylline overdose. Ingesting the slow-release Theophylline pill in the wrong way by powdering it can also effectuate overdose even if the ingested pill is of the prescribed dose.

Storage:

Theophylline anhydrous pills are retailed in pet bottles and strip packets. 68 to 77 degrees Fahrenheit (20 to 25 degrees Celsius) is gauged to be the apt temperature range under which Theophylline pills can be housed. High-up areas should be chosen to store the Theophylline pill bottle to prevent access to kids.

For Doctors:

Indications:

  • Reversible airflow obstruction (asthma and COPD).

Dose:

Theophylline’s therapeutic dosing window advocates a daily dose within the 300 to 600 mg range. Considering slow-release Theophylline pills, the daily dose can be served out via a single pill. On the contrary, with the rapid-release Theophylline pill, the estimated daily dose is often served as two doses of half the estimated daily dosing value.

The apt dose must be gauged individually, given every person’s Theophylline tolerance and clearance variances. It is executed by weighing up Theophylline’s blood concentration, which gets reflected with a specific Theophylline dose. Correspondingly, theophylline dose titration, either upregulation or downregulation, is advocated to secure a safe dose of theophylline for that particular person.

Dosing Considerations:

Theophylline dosing considerations are advocated for beings with:

  • Undermined Theophylline clearance.

  • Serum Theophylline concentration tracking is impractical.

A different dosing strategy should be adhered to in each of the above scenarios:

  • 12 to 15 Years of Age: 16 milligrams per kilogram of body weight per day (mg/kg/day), capped at 400 mg daily.

  • 16 Years and Above: Not surpassing 400 mg per day.

What Are the Pharmacological Aspects of Theophylline Anhydrous?

1. Mechanism of Action: In asthmatic conditions, Theophylline anhydrous elicits its therapeutic out-turn through non-bronchodilator prophylactic effects and bronchodilatation. Non-bronchodilator prophylactic effects refer to the tampering of “stimuli evoked respiratory tract reactions. Certain triggers can pilot reversible airway impediments by triggering reactions in the airway tract. Theophylline anhydrous clamps down those reactions and curtails the body’s response. Theophylline molecules hinder and hold back the adenosine receptor and phosphodiesterase enzyme functions. Bronchodilation is precipitated as the collaborative output of Theophylline’s adenosine receptor and phosphodiesterase enzyme inactivation sequel.

2. Pharmacodynamics: Apart from Theophilline’s actions over adenosine receptors and phosphodiesterase enzymes, it also inflates the serum calcium proportion. Calcium inflation is attained by facilitating calcium dispensation. Serum calcium tends to leverage bronchodilatation under Theophylline’s pull. Theophylline could also trigger breathing centers and intensify ventilation.

3. Pharmacokinetics: Theophylline’s ingestion is escorted by swift gut uptake. Gut uptake patterned first-order kinetics. Theophylline’s ingested dose and utmost concentration reflected a direct correlation. Theophylline’s distribution and dissemination are executed through its alliance with plasma proteins—liver cytochrome enzymes, mainly the cytochrome P450 enzyme system, process Theophylline anhydrous molecules. The expulsion of Theophylline, either in its original structure or as fragmented products, comes off through urine.

Toxicity:

Theophylline’s highly restrictive therapeutic window adds to its toxicity potency. Even the slightest heightened Theophylline dose cannot be approved. Theophylline overdose projects the following manifestations:

  • Incessant vomiting.

  • Abdominal pain.

  • Irritability.

  • Hypotension.

  • Restlessness.

  • Seizures.

  • Acute lung injury.

  • Tachypnea.

  • Hallucinations.

Clinical Studies:

Clinical study reports concerning Theophylline anhydrous were opposing and clashing. Certain controlled trials with Theophylline elicited no specific therapeutic benefit. Instead, incorporating theophylline heightened the side effect profile encountered in such patients. Few other studies have underscored the benefits of augmented asthma recovery with Theophylline.

What Are the Contraindications of Theophylline Anhydrous?

Theophylline anhydrous should not be advocated for the following cases:

  • Reported Theophylline allergy.

  • Reported exaggerated reactivity with constituents in Theophylline pills or infusion formulation.

Warnings and Precautions:

  • Underlying Disease Exacerbation: While advocating Theophylline therapy to one with other coexisting disorders, there is a better prospect for the underlying disease to inflame. Seizures, peptic ulcers, epilepsy, and arrhythmias are the ones that are discerned to be on the red list when considering Theophylline anhydrous therapy.

Likewise, certain coexisting maladies temper and tone down the Theophylline clearance. Such cases prompted an augmented vulnerability for Theophylline toxicity. Acute hepatitis, congestive heart failure, cor-pulmonale, hypothyroidism, and acute pulmonary edema underscore the need for vigilance.

  • Neonates and Elderly Usage: Theophylline therapy in seniors (beyond 65 years) and babies (under one year) requires close tracking of Theophylline clearance. Due to their compromised clearance potential, these categories are exposed to theophylline toxicity encounters.

  • Concurrent Drug Therapy: Drugs that can attenuate Theophylline processing, when advocated in unison with Theophylline therapy, expose one to Theophylline overdose.

  • Theophylline Dose Revisions: No abrupt Theophylline dose inflation is advocated through the therapy if asthmatic worsening is precipitated amidst the course. Theophylline dose revisions should be pulled off only after confirming Theophylline’s serum concentration. No dose inflation can be achieved if the serum concentration exceeds 10 micrograms per milliliter (mcg per ml).

  • Tracking Theophylline’s Serum Concentration: Theophylline serum concentration tracking is imperative to expose the appropriateness of the ongoing dosing.

What Are the Drug Interactions of Theophylline Anhydrous?

Theophylline anhydrous elicits interactions with a broad range of other medicines. Some of the notably flagged Theophylline drug association encompasses the following:

  • Medications like Erythromycin, Ciprofloxacin, Enoxacin, Fluvoxamine, Tacrine, or Cimetidine, when advocated in conjunction with Theophylline anhydrous, can set back Theophylline’s processing. It can eventually reinforce the potential for theophylline toxicity and heighten the vulnerability.

  • Theophylline’s breakdown and processing get amplified and encouraged by Rifampin, Aminoglutethimide, Phenobarbital, and Carbamazepine. Thus, bring down Theophylline’s potency.

  • Theophylline depletes Adenosine and Diazepam’s potency by masking adenosine receptors.

Specific Considerations:

1. Theophylline Anhydrous in Expectant Women: Theophylline anhydrous marks its position under “pregnancy category C.” Animal studies concerning Theophylline brought its teratogenicity to light. However, asthma in pregnant women is also a matter that could call forth fetal harm. Both prospects must be scrutinized before advocating Theophylline to a conceiving lady.

2. Theophylline Anhydrous in Nursing Women: A notable proportion of Theophylline gets reflected in a Theophylline ingested lactating woman’s breastmilk. Babies nursed by those undergoing Theophylline therapy are liable to Theophylline toxicity. Serum and breastmilk Theophylline proportions were estimated to be analogous.

3. Theophylline Anhydrous in Pediatric Patients: Theophylline therapy is endorsed in pediatric patients. Nevertheless, owing to immaturity, pediatric patients’ Theophylline clearance rate might be compromised, which further deepens their toxicity vulnerabilities.

4. Theophylline Anhydrous in Geriatric Patients: Aging triggers oddities in how theophylline anhydrous is processed. Just like pediatric patients, older ones also elicit poor Theophylline clearance. Notable adverse effects encounters will get precipitated in geriatric patients through Theophylline therapy.

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Dr. Kaushal Bhavsar
Dr. Kaushal Bhavsar

Pulmonology (Asthma Doctors)

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