Healthy Inc > Blog > Theophylline BP/USP/IP
Posted on:

Does theophylline affect sleep?

In the pharmaceutical industry, Theophylline is classified as a methylxanthine, a chemical cousin to caffeine. As a pharmacist and manufacturer, I can confirm that it is notorious for disrupting sleep. Because it acts as a central nervous system (CNS) stimulant, it frequently causes insomnia, restlessness, and decreased sleep quality.

At your WHO-GMP facility in Mumbai, you likely manufacture this as Theophylline Sustained-Release (SR) tablets (100 mg, 200 mg, or 400 mg). While the SR formulation is designed to maintain a steady-state concentration over 12–24 hours, the constant presence of the drug in the system can make it difficult for patients to enter deep sleep cycles.

How Theophylline Disrupts Sleep

Theophylline’s impact on sleep is dose-dependent and results from its core pharmacological actions:

  • CNS Stimulation: Much like drinking several cups of coffee, theophylline increases alertness and decreases the sensation of tiredness, making it difficult to fall asleep (increased sleep latency).

  • Sleep Architecture Changes: It reduces the duration of REM (Rapid Eye Movement) and deep slow-wave sleep, leading to a feeling of being unrefreshed despite a full night’s rest.

  • Diuretic Effect: It can increase urine production (diuresis), causing “nocturia” (the need to wake up during the night to urinate).

  • Cardiovascular Arousal: It can cause palpitations or an increased heart rate (Tachycardia), which can trigger anxiety or a sense of physical restlessness that prevents sleep.

Mechanism: Adenosine Antagonism

The mechanism behind its stimulant effect is identical to that of caffeine.

Adenosine Blockade: In the brain, a chemical called Adenosine builds up throughout the day to signal the body that it is time to sleep. It binds to receptors that slow down nerve cell activity.

Inhibition: Theophylline acts as a competitive antagonist at adenosine receptors ($A_1$ and $A_2$). By blocking these receptors, it prevents adenosine from doing its job.

Increased Neurotransmission: This allows for the continued release of excitatory neurotransmitters like dopamine and glutamate, keeping the “engine” of the brain running even at night.

The Pharmacist’s “Patient Management” Strategy

As you promote your firm on digital platforms, providing these technical management tips builds professional trust:

  • The Timing Rule: If taking a once-daily SR tablet, advise patients to take it in the morning.

  • Caffeine Synergy: Warn patients to limit coffee, tea, and chocolate. Since caffeine and theophylline are both methylxanthines, they have a “synergistic” effect that can lead to extreme jitters and total insomnia.

  • Serum Monitoring: Sleep disruption can be a sign of Theophylline Toxicity. As a pharmacist, you know the therapeutic window is narrow ($10–20\ \mu g/mL$). If sleep issues are severe, the serum levels should be checked.

The Manufacturer’s Perspective: Technical & Export

From a production and B2B standpoint at your facility in Mumbai:

  • The “SR” Precision USP: On your multivendor marketplace, highlight your Sustained-Release (SR) Matrix technology. A high-quality SR tablet that prevents “dose dumping” is essential to avoid sudden spikes in blood levels that cause severe insomnia.

  • The “Theo-Phylline + Etofylline” Combination: In many export markets (like Southeast Asia and Africa), this FDC is popular. Positioning your firm as a specialist in this combination can attract high-volume B2B inquiries.

  • Stability & Packaging: Theophylline is sensitive to moisture. We utilize Alu-Alu blister packaging to ensure a 36-month shelf life, especially for export to Zone IVb tropical regions.

  • Dossier Support: We provide full CTD/eCTD Dossiers to support your firm’s registration in international markets.

Theophyline Tablet

Posted on:

What is Theophylline 200 mg used for?

In the pharmaceutical industry, Theophylline 200 mg is a classic Methylxanthine derivative and a systemic bronchodilator. As a pharmacist and manufacturer, I classify this as a “sustained-release” or “maintenance” therapy for chronic respiratory conditions.Unlike rescue inhalers (like Salbutamol), Theophylline is generally used to provide long-term, around-the-clock control of airway obstruction.

Primary Clinical Uses

  • Chronic Asthma: For the prevention and long-term maintenance of asthma symptoms, particularly nocturnal asthma (nighttime wheezing).

  • COPD (Chronic Obstructive Pulmonary Disease): Management of stable chronic bronchitis and emphysema.

  • Apnea of Prematurity: In specialized neonatal care, it is used to stimulate breathing in premature infants.

  • Maintenance Therapy: Used when patients are not adequately controlled by inhaled corticosteroids or long-acting beta-agonists (LABAs).

Mechanism of Action: Phosphodiesterase Inhibition

Theophylline works through a dual pathway to open the airways and reduce the inflammatory response.

PDE Inhibition: It inhibits the enzyme Phosphodiesterase (PDE). This leads to an increase in intracellular cyclic AMP (cAMP), which triggers the relaxation of bronchial smooth muscles (bronchodilation).

Adenosine Antagonism: It blocks Adenosine receptors, which otherwise cause bronchoconstriction and the release of histamine.

Diaphragm Strengthening: It increases the force of contraction of the diaphragmatic muscles, which is particularly beneficial for patients with COPD who have “tired” respiratory muscles.

The Manufacturer’s Perspective: Technical & Export

From a production and B2B standpoint at your WHO-GMP facility in Mumbai, the 200 mg strength requires specific technical oversight:

  • Modified Release (Sustained Release) Technology: The 200 mg dose is most commonly formulated as a Sustained Release (SR) tablet. At our facility, we utilize specialized polymers (like HPMC) to ensure the drug is released slowly over 12 to 24 hours. This is a major USP for your digital platform, as it improves patient compliance.

  • Narrow Therapeutic Index (NTI): As a pharmacist, you know Theophylline has a “narrow window” where it is effective but not toxic. For your B2B clients, providing rigorous Batch-to-Batch Dissolution Data is essential to prove your generic version’s safety and bioequivalence.

    Stability & Moisture Control: Theophylline is sensitive to moisture. We utilize Alu-Alu blister packaging to ensure a 36-month shelf life, especially for export to Zone IVb regions where high humidity can affect the release profile of SR tablets.

    Dossier Support: This molecule is a staple in international public health tenders. Our Mumbai facility provides full CTD/eCTD Dossiers to support your firm in registering this as a reliable generic against the innovator (Theolair or Quibron).

Theophyline Tablet

 

Add to cart