AGIMFAST®180

Composition: Each tablet contains:
Fexofenadine hydrochloride. . . . . . . . . . . 180 mg
Presentation:
Cardboard box with 2 blisters of 10 film coated tablets.
Indications:
Agimfast tablets (Fexofenadine) are indicated for the relief of symptoms associated with seasonal allergic rhinitis such as sneezing; runny nose; itchy nose/palate/and throat; itchy red and watery eyes; chronic idiopathic urticaria.

Category:

Additional information

Dosage and administration

Dosage:
– Adults and children aged 12 years and over: 1 tablet/once a day.
– In patients with hepatic impairment, a dose reduction is not recommended.
– In patients with mild to moderate renal impairment (Clcr: 41-80 ml/min) or severe (Clcr: 11-40 ml/min), the recommended initial dose is 60mg once in 24 hours. Then, other products with appropriate strength can be taken.
Administration: Agimfast 180 is orally taken once daily with or without food. It should not be used along with various fruit juices.

Contraindications

Hypersensitivity to fexofenadine and any of the ingredients of Agimfast 180 tablets.
Children under 12 years of age.

Warnings and precautions for use

Fexofenadine hydrochloride should be administered with care in the elderly, patients with renal or hepatic impairment.
Caution should be exercised in people who are driving and operating machinery.
Fexofenadine hydrochloride should be administered with care in patients with a history of or ongoing cardiovascular disease or with a pre-existing prolonged QT interval.
Fexofenadine should not be used concurrently with other antihistamine agents.
This drug contains lactose: Patients with rare genetic problems with galactose intolerance, Lapp lactase enzyme deficiency or glucose-galactose malabsorption should not take this medicine.

Recommendation for pregnancy and breastfeeding

Pregnancy: There are no adequate data on fexofenadine use during pregnancy. Fexofenadine hydrochloride should be used during pregnancy only if the potential benefit outweighs the potential risk to the fetus.
Lactation: It is not known if Agimfast®180 is excreted in human milk; therefore, fexofenadine should be used cautiously in nursing mothers.

Effects on ability to drive and use machines

Although fexofenadine rarely causes drowsiness, caution should be exercised when driving or operating machinery.

Interactions, incompatibilities of medicine

Co-administration of fexofenadine with either ketoconazole or erythromycin led to increased plasma levels of fexofenadine and area-under-the plasma concentration versus time curve [AUC], the mechanism may be due to increased absorption and decreased excretion of fexofenadine. However, this interaction is not clinically meaningful.
Antacids containing alumimium or magnesium reduce bioavailability of fexofenadine if they are taken concurrently. It is advisable to leave 2 hours between administration of fexofenadine hydrochloride and these antacids.

Undesirable effects (ADRs)

The undesirable effects of Agimfast®180 are not affected by the dose, age, sex and race of patients.
Common, ADR > 1/100:
Nervous system disorders: Drowsiness, fatigue, headache, insomnia, dizziness.
Gastrointestinal disorders: Nausea, indigestion.
Others: Viral infection (cold, flu), dysmenorrhoea, upper respiratory tract infections, itchy throat, cough, fever, otitis media, sinusitis, back pain.
Uncommon: 1/1000 < ADR < 1/100:
Nervous system disorders: Nervousness, sleep disorders, nightmares.
Gastrointestinal disorders: Dry mouth, abdominal pain.
Rare: ADR < 1/1000:
Skin: Rash, urticaria, pruritus.
Hypersensitivity: Angioedema, chest tightness, dyspnoea, flushing and systemic anaphylaxis.
Management of ADRs
ADRs of fexofenadine are mild, only 2.2% of fexofenadine patients have to stop taking the drug due to adverse drug reactions.

Overdose and management

Overdose:
Information on acute toxicity of fexofenadine is limited. However, drowsiness, dizziness and dry mouth have been reported.
Management:
Standard measures should be considered to remove the unabsorbed medicines from the gastrointestinal tract. Symptomatic and supportive treatment is recommended.
Haemodialysis reduces plasma concentrations insignificantly (1.7%). There is no specific antidote.

Pharmacodynamic properties

Fexofenadine is a second-generation antihistamine with specific, selective peripheral H1-receptor antagonist activity. Fexofenadine is an active metabolite of terfenadine and without the cardiotoxic effects of terfenadine because it does not block potassium channel involved in repolarization of cardiac cells. Fexofenadine has no significant acetylcholine and dopamine antagonist activity and exhibits no alpha1-adrenergic or beta-adrenergic-receptor blocking effects.
At therapeutic doses, no sedative or other central nervous system effects are observed.
Agimfast®180 has fast and prolonged effects because fexofenadine slowly binds to H1 receptor to form a stable complex from which it dissociates slowly is separated slowly.

Pharmacokinetic properties

Absorption: Agimfast®180 tablet is well absorbed following oral administration. After taking one 60mg tablet, peak plasma concentration was achieved after 2-3 hours. Peak plasma concentration is about 494 nanograms/ml after taking one 180mg tablet once daily. High fat diets decrease peak plasma levels by approximately 17% and prolong the time to attain maxima plasma concentration (up to about 4 hours). Antihistaminic effects persist for more than 12 hours.
Distribution: Fexofenadine is 60-70% plasma protein bound, predominantly to albumin and α1-acid glycoprotein. It is unknown whether it crosses the placenta or is distributed in breast milk, but, when terfenadine is used, fexofenadine is discovered as a terfenadine metabolite in breast milk. Fexofenadine does not cross the blood brain barrier.
Metabolism: Fexofenadine undergoes negligible metabolism (approximately 5% of the dose is metabolized in intestinal mucosa. Only 0.5-1.5% is metabolized in the liver by the cytochrome P450 microsomal enzyme system to an inactive metabolite). Approximately 3.5% of the fexofenadine dose is metabolized by a second metabolic pathway (unrelated to the cytochrome P450 enzyme system) to the methyl ester derivative. This metabolite of fexofenadine is found only in faeces, so it is possible that the intestinal flora are involved in this metabolism.
Elimination: Elimination half-life of fexofenadine is approximately 14.4 hours, prolonged (31 – 72% longer than those observed in healthy individuals) in patients with renal impairment. The drug is mainly excreted in the feces (approximately 80%); 11-12% of the dose is excreted in urine as unchanged form.
Pharmacokinetics in patients with renal impairment compared to healthy individuals:
Clcr: 41 – 80 ml/min: Peak concentration is 87% higher, elimination half life is 59% longer.
Clcr: 11 – 40 ml/min: Peak concentration is 111% higher, elimination half life is 72% longer.
Clcr ≤ 10 ml/min (in patients undergoing dialysis): Peak concentration is 82% higher, elimination half life is 31% longer than that observed in healthy people.
Hemodialysis does not effectively remove fexofenadine from blood.
Pharmacokinetics in patients with hepatic impairment:
The pharmacokinetics of fexofenadine hydrochloride in patients with hepatic disease did not differ substantially from that observed in healthy patients.

Storage conditions, shelf-life, quality specification of the medicine

Storage conditions: Protect from humidity and light, below 30 degrees C.
Shelf – life: 36 months from the manufacture date.
Quality specification: In house specification.