Bosnum/Bosnum 180

Bosnum/Bosnum 180

fexofenadine

Manufacturer:

Unison

Distributor:

Health Alliance
Full Prescribing Info
Contents
Fexofenadine hydrochloride.
Description
Each film coated tablet contains: Fexofenadine hydrochloride 60 mg.
Each film coated tablet contains: Fexofenadine hydrochloride 180 mg.
Action
Pharmacology: Fexofenadine is an antihistamine with selective peripheral H1-receptor antagonist activity. It inhibits antigen-induced bronchospasm in sensitized guinea pigs and histamine release from peritoneal mast cells in rats.
Pharmacokinetics: Absorption: Rapid following oral administration. The bioavailabilities of Fexofenadine capsule and tablet formulations are equivalent when administered in equal doses.
Bioavailability of Fexofenadine was shown to be reduced by 36% by fruit juices such as grapefruit and orange based on the results from three clinical studies including a population pharmacokinetic analysis. The same effects may be extrapolated to other fruit juices such as apple juice.
The pharmacokinetics of Fexofenadine are linear for oral doses up to 240 mg a day (120 mg twice a day).
Distribution: Volume of distribution (Vd) 5.4 to 5.8 liters/kilogram.
Tissue distribution studies in rats using radiolabeled Fexofenadine show that it does not cross the blood-brain barrier.
Protein binding: High (60 to 70%) predominantly to albumin and alpha1-acid glycoprotein.
Biotransformation: About 5% of the total dose is metabolized; approximately 0.5 to 1.5% by cytochrome P450 3A4 isoenzyme metabolism and 3.5% transformed to a methyl ester metabolite by intestinal microflora.
Elimination: 14.4 hours in healthy subjects; in patients with mild renal impairment (creatinine clearance of 41 to 80 mL per minute) and severe renal impairment (creatinine clearance of 11 to 40 mL per minute), the mean elimination half-life was 59% and 72% longer, respectively, than in healthy subjects. In patients on dialysis, half-life was 31% longer than in healthy subjects.
Onset of action: Within 1 hour, as determined by a reduction in rhinitis symptoms following administration of a single 60-mg dose to patients exposed to ragweed pollen and by human histamine skin wheal and flare studies following administration of single and twice-daily doses of 20 and 40 mg of Fexofenadine.
Peak serum concentration: 209 ng/mL after a single 60-mg dose as an oral solution in healthy volunteers.
142 ng/mL after a single 60 mg tablet in healthy volunteers.
494 ng/mL after a single 180 mg oral tablet in healthy volunteers.
286 ng/mL after 10 doses of 60-mg as an oral solution every 12 hours in healthy volunteers.
Time to peak effect: 2 to 3 hours, as determined by human histamine skin wheal and flare studies following administration of single and twice-daily doses of 20 and 40 mg of Fexofenadine.
Duration of action: Effect evident 12 hours after administration, as determined by clinical studies in patients with seasonal allergic rhinitis given a single 60-mg dose, and by human histamine skin wheal and flare studies in patients given single and twice-daily doses of 20 and 40 mg of Fexofenadine.
Note: Tolerance to the antihistamine effect of Fexofenadine was not demonstrated following 28 days of dosing.
Elimination: Renal: Renal clearance: 3 to 4 L per hour; approximately 11% of a radioactive Fexofenadine dose is excreted in the urine.
Fecal: Approximately 80% of a radioactive Fexofenadine dose is excreted in the feces, however, it is unclear whether this represents unabsorbed drug or is the result of biliary excretion.
Indications/Uses
Rhinitis, seasonal allergic (treatment): Fexofenadine is indicated to relieve symptoms that are associated with seasonal allergic rhinitis in adults and children 6 years of age and older (for Bosnum). Symptoms treated effectively were sneezing, rhinorrhea, itchy eyes, nose, and throat, and red, watery eyes.
Urticaria (treatment): Fexofenadine is indicated for the treatment of uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 years of age and older (for Bosnum). It significantly reduces pruritus and the number of wheals.
Dosage/Direction for Use
Usual adult and adolescent dose: Bosnum: Rhinitis, seasonal, allergic (treatment): 60 mg two times a day, or 180 mg once a day with water.
Urticaria (treatment): 60 mg two times a day or 180 mg one time a day with water.
Note: For patients with decreased renal function, an initial dose of 60 mg once a day is recommended.
Usual adult and adolescent (12 years of age or older) dose: Bosnum 180: Rhinitis, seasonal, allergic (treatment): 180 mg once a day with water.
Urticaria (treatment): 180 mg once a day with water.
For patients with decreased renal function, an initial dose of 60 mg once a day is recommended.
Usual adult and adolescent (12 years of age or older) prescribing limits: Bosnum: 60 mg two times a day, or 180 mg once a day with water.
Bosnum 180: 180 mg once a day with water.
Usual pediatric dose: Bosnum: Rhinitis, seasonal, allergic (treatment) & Urticaria (treatment): Children 12 years of age and older: See Usual adult and adolescent dose as previously mentioned.
Children 6 to 11 years of age: Oral, 30 mg two times a day with water.
Children up to 6 years of age: Safety and efficacy have not been established.
Note: For pediatric patients with decreased renal function, an initial dose of 30 mg once a day is recommended.
Usual Pediatric prescribing limits: Bosnum: 30 mg two times a day with water.
Usual Geriatric Dose: Bosnum: See Usual adult and adolescent dose as previously mentioned.
Bosnum 180: Same as adult dose.
Note: For 60 mg dosing, another preparation containing Fexofenadine hydrochloride 60 mg per unit dose should be used.
Overdosage
Clinical effects of overdose: Signs and Symptoms: Dizziness; Drowsiness; Dry mouth.
Treatment of overdose: To decrease absorption consider standard measures to remove any unabsorbed drug.
Hemodialysis does not effectively remove fexofenadine from the blood (up to 1.7% removed).
There is no known antidote to fexofenadine. Treatment is generally symptomatic and supportive.
Patients in whom intentional overdose is confirmed or suspected should be referred for psychiatric evaluation.
Contraindications
Except under special circumstances, this medication should not be used when the following medical problem exists: Hypersensitivity to Fexofenadine or any of its ingredients.
Risk-benefit should be considered when the following medical problems exist: Renal function impairment (based upon increases in the bioavailability and half-life of Fexofenadine, once-daily administration is recommended initially in patients with impaired renal function).
Special Precautions
Carcinogenicity/Tumorigenicity: Fexofenadine showed no carcinogenic potential in 18- and 24-month studies in mice and rats given oral Terfenadine doses of 50 and 150 mg per kg of body weight (mg/kg) per day, respectively. These doses resulted in area under the plasma concentration-time curve (AUC) values for Fexofenadine of up to four times the human therapeutic value based on the recommended dosage.
Mutagenicity: Fexofenadine was not mutagenic in in vitro (Bacterial Reverse Mutation, CHO/HGPRT Forward Mutation, and Rat Lymphocyte Chromosomal Aberration assays) studies and in vivo (Mouse Bone Marrow Micronucleus assay) studies.
Fertility: Dose-related reductions in implants and increases in post implantation losses were seen in rats given oral doses of Terfenadine 150 mg/kg. These doses resulted in AUC values for Fexofenadine of three times the human therapeutic value based on the recommended dosage. In mice, Fexofenadine hydrochloride produced no effect on male or female fertility at average dietary doses up to 4438 mg/kg (approximately 10 times the maximum recommended human daily oral dose).
Use in Children: Bosnum: In clinical trials, 438 children 6 to 11 years of age were safely treated for seasonal allergic rhinitis with Fexofenadine 30 mg twice daily, for up to 2 weeks. These studies have not demonstrated pediatrics-specific problems that would limit the usefulness of Fexofenadine in children. However, the safety and efficacy of Fexofenadine in children up to 6 years of age have not been established.
Use in Elderly: Although appropriate studies on the relationship of age to the effects of Fexofenadine have not been performed in the geriatric population, no geriatrics-specific problems have been documented to date. However, elderly patients are more likely to have age-related renal function impairment which may require care in dose selection and monitoring of renal function.
Use In Pregnancy & Lactation
Pregnancy: Adequate and well-controlled studies in humans have not been done. Fexofenadine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Fexofenadine was not teratogenic in studies in which rats or rabbits were given oral doses of Terfenadine of up to 300 mg/kg per day.
These doses resulted in AUC values for Fexofenadine of up to 4 and 37 times the human therapeutic value based on the recommended dosage, respectively. In mice, no adverse effects and no teratogenic effects during gestation were observed with Fexofenadine at doses up to 3730 mg/kg (approximately 15 times the maximum recommended human daily oral dose).
In rats given oral doses of Terfenadine 150 mg/kg, dose-related decreases in pup weight and survival were observed. These doses resulted in AUC values for Fexofenadine of three or more times the human therapeutic value based on the recommended dosage, respectively.
Breast-feeding: It is not known whether Fexofenadine is distributed into breast milk. Because many drugs are distributed into human milk, caution should be exercised when administering Fexofenadine to a nursing woman.
Adverse Reactions
Those indicating need for medical attention: Incidence rare: Observed during clinical practice: Anaphylaxis and hypersensitivity reactions (chest tightness; feeling of warmth redness of the face, neck, arms and occasionally, upper chest; large, hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, sex organs; shortness of breath, difficult or labored breathing).
Those indicating need for medical attention only if they continue or are bothersome: Incidence less frequent: Back pain; coughing- observed in pediatric patients only; dizziness; drowsiness; dysmenorrhea (painful menstrual bleeding); dyspepsia (stomach upset); fatigue (unusual feeling of tiredness); fever- observed in pediatric patients only; headache; myalgia (joint pain; swollen joints; muscle aching or cramping; muscle pains or stiffness; difficulty in moving); nasopharyngitis (stuffy or runny nose; muscle aches; unusual tiredness or weakness; fever; sore throat; headache); nausea; otitis media (earache; ringing or buzzing in ears)- observed in pediatric patients only; pain in extremity (pain in arms or legs); sinusitis (headache; pain or tenderness around eyes or cheekbones; runny or stuffy nose); upper respiratory tract infection (ear congestion; nasal congestion; chills; cough, fever, sneezing, or sore throat; body aches or pain; headache; loss of voice; runny nose; unusual tiredness or weakness; difficulty in breathing); viral infections such as cold and flu.
Incidence rare: Observed during clinical practice: Nervousness; rash (urticarial and pruritic); sleep disorders (sleeplessness; terrifying dreams; trouble sleeping).
Drug Interactions
Combinations containing any of the following medications, depending on the amount present, may also interact with this medication: Antacids, aluminum and magnesium hydroxide-containing (administration of Fexofenadine within 15 minutes of dosing with an aluminum and magnesium hydroxide-containing antacid has decreased the Fexofenadine area under the time-concentration curve by 41% and Cmax by 43%).
Storage
Store at temperature not more than 30°C.
ATC Classification
R06AX26 - fexofenadine ; Belongs to the class of other antihistamines for systemic use.
Presentation/Packing
FC tab 60 mg x 10 x 10's. 180 mg x 10 x 10's.
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