Doxofylline

Doxofylline belongs to the pharmacological class Methyl xanthine. Doxofylline appears to have a bronchodilatory effect in the pulmonary system.

Doxofylline has been found to be approved for relieving symptoms and for the treatment and maintenance of episodes of chronic asthma, chronic bronchitis, and Chronic Obstructive Pulmonary Disease.

Doxofylline is absorbed with an absolute bioavailability of 63 ± 25%. Doxofylline is said to have a short distribution phase which is followed by the 100mg intravenous administration of Doxofylline. Doxofylline undergoes extensive hepatic metabolism, which is followed by a clearance of 90%. The metabolite called as β-hydroxymethyltheophylline has been found in the urine, although it does not have any pharmacological activity.

The common side effects associated with Doxofylline are irregular nausea, insomnia, headache, stomach irritability.

Doxofylline is available in the form of oral capsules. Doxofylline is available in U.S., Canada,E.U. , India, Australia, Japan.

Doxofylline belongs to the pharmacological class Methyl xanthine. Doxofylline appears to have a bronchodilatory effect in the pulmonary system.

Doxofylline is said to attenuate inflammatory action, bronchoconstriction, and also thromboxane A2 when it is challenged by the platelet-activating factor.

Doxofylline has been foudn to be approved for relieving symptoms and for the treatment as well as maintenance of episodes of chronic asthma, chronic bronchitis, and Chronic Obstructive Pulmonary Disease.

The Cmax of Doxofylline was found to be about 5.78 to 20.76 mcg/mL after oral administration. The Tmax is found to be 1.19 ± 0.19 hours after the oral administration.

Duration of action of Doxofylline lasts upto about 10 to 11 hours.

Doxofylline can be used in the treatment of:

• Chronic Asthma
• Chronic Bronchitis
• Chronic Obstructive Pulmonary Disease.

Doxofylline is approved for use in the following clinical indications:

• Chronic Asthma
• Chronic Bronchitis
• Chronic Obstructive Pulmonary Disease.

Oral capsule: To be swallowed as a whole with water 2-3 times a day as per physicians’ instructions.

Oral Capsule: 400mg

Oral dosage form capsule

Maintaining health and smoking cessation and is a must.

In take of Caffeine is to be avoided or limited to use as it may lead to the risk of nervousness, rapid heartbeat, nausea, palpitationsetc.

Alcohol should be avoided in the patient especially in pateints with an underlying liver disorder or liver dysfunction

Diet containing food with a salt, preservatives, refined and high energy-dense foods, high glycemic index, red and processed meat, added sugar, saturated and trans fat food, low fiber, low antioxidants, and vitamins is to be restricted.

The dietary restrictions should be individualized as per the patient's requirements.

Doxofylline may be contraindicated under the following conditions:

• Hypersensitivity to the ingredients of the medication
• Heart problems such as low blood pressure and heart attack.

The adverse reactions related to Doxofylline can be categorized as:

Common

• Nausea
• Fast heart rate
• Stomach irritability
• Headache
• Vomiting

Less common

• Throat Irritation
• Inflammation Or Infection Of The Vagina
• Decreased Appetite
• Diarrhea
• Upper Abdominal Pain Rare
• Peeling, Blistering or loosening of the skin

Rare

• Hives
• Pancreatitis
• Angioedema
• Anaphylaxis
• Hepatitis
• Steven Johnson syndrome
• Decreased blood platelets

The clinically relevant drug interactions of Doxofylline is briefly summarized here:

• Lincomycin
• Other xanthine derivatives
• Propranolol
• Ranitidine
• Troleandomycin
• Allopurinol
• Anti flu vaccine
• Cimetidine
• Clindamycin
• Ephedrine

The common side effects of Doxofylline include the following:

• Insomnia
• Fast Heart rate
• Headache
• Nausea
• Vomiting
• Stomach irritability

Pharmacodynamics

Doxofylline is said to be a methylxanthine bronchodilator with potent bronchodilator activity whixh is comparable to that of theophylline. In animal studies, it has been demonstrated doxofylline can attenuate inflammatory actions ,bronchoconstriction, and the release of thromboxane A2 when challenged with platelet-activating factor.

Doxophylline only displays an inhibitory action against PDE2A1 and antagonism at adenosine A(2A) at high concentrations. A study demonstrated that doxofylline is found to interact with β2-adrenoceptors to induce blood vessel relaxation as well as airway smooth muscle relaxation. In dog studies, doxofylline cuased decreased airway responsiveness at a dose that did not affect heart rate and respiratory rate.

Pharmacokinetics

• Absorption

Following repeated administrations , doxofylline is found to reach the steady-state in about four days. Following oral administration of 400 mg doxofylline two times a day for five days in adults with chronic bronchitis, the peak plasma concentrations i.e.Cmax at steady state is foudn to be ranging from 5.78 to 20.76 mcg/mL. The time to reach maximum concentration i.e.Tmax was found to be 1.19 ± 0.19 hours. The absolute bioavailability of doxofylline was found to be 63 ± 25% .

• Distribution

Doxofylline is foudn to demonstrate a short distribution phase following intravenous administration of about 100 mg of Doxophylline given in adults with chronic bronchitis. As methylxanthines are foudn to be distributed to all body compartments, doxofylline might be detected in breast milk and placenta.

• Metabolism

Doxofylline is found to undergo hepatic metabolism, which accounts for about 90% of total drug clearance. β-hydroxymethyltheophylline had been detected in the serum and urine after the oral administration of 400 mg Doxophylline given in healthy subjects. The circulating metabolite was found to be devoid of any significant pharmacological activity.

• Elimination

Ist has been found that less than 4% of an orally administered dose of Doxophylline is excreted in unchanged in the urine due to the extensive hepatic metabolism.

• https://cdn.caymanchem.com/cdn/insert/18746.pdf
• https://www.ndrugs.com/?s=doxofylline&t=overdose
• https://www.webmd.com/drugs/2/drug-14449/doxycycline-oral/details/list-sideeffects
• https://mrmjournal.biomedcentral.com/counter/pdf/10.1186/s40248-019-0189-0.pdf
• https://go.drugbank.com/drugs/DB09273