AGIMFAST®120

Composition: Each film-coated tablet contains:
Fexofenadine hydrochloride . . . . . . . . . . .120 mg
Presentation:
Blister of 10 tablets, box of 2 blisters.
Indications:
Agimfast 120 is indicated for the treatment of symptoms associated with seasonal allergic rhinitis, such as sneezing, runny nose, itchy nose, palate and throat, itchy and red eye and watery eyes in adults and children over 12 years of age.

Category:

Additional information

Dosage and administration

Dosage:
Adults and children ³ 12 years of age: 1 tablet/once a day, before the meal.
Patients with kidney failure: The recommended initial dose is 60mg once in 24 hours, dose is adjusted according to renal function. Because Agimfast contains 120mg of fexofenadine, patients should use other product with appropriate strength (containing 30mg or 60mg or taking ½ tablet of Agimfast 120mg) to be able to adjust the dose.
Dose adjustment in patients with impaired hepatic function are not required.
Administration: Agimfast 120® tablets should be orally taken with a glass of water.

Contraindications

Contraindication:
Hypersensitivity to any of the ingredients of Agimfast 120.
Children under 12 years of age.

Warnings and precautions for use

The elderly, patients with hepatic or renal impairment.
Patiens who are driving and operating machinery.
Patients with a history of cardiovascular risk or with pre-existing prolonged QT interval should be monitored cautiously when using fexofenadine.
Do not use concurrently any other antihistamines while taking fexofenadine.
Fexofenadine should be discontinued at least 24-48 hours prior to antigen skin tests.
Fexofenadine may exacerbate psoriasis.
This medicine 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 to the mother outweighs the potential risk to the fetus.
Lactation: It is not known if Agimfast 120 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, because of the safety, caution should be exercised when driving or operating machinery.

Interactions, incompatibilities of medicine

Erythromycin or ketoconazole increases the level of fexofenadine in plasma but does not change QT interval.
Fexofenadine concentrations may be increased by concomitant use of erythromycin, ketoconazole, verapamil, p – glycoprotein inhibitors.
Fexofenadine should not be taken with antacids containing aluminum or magnesium because they decrease the absorption of fexofenadine.
Fexofenadine can increase the concentrations of alcohol, CNS sedative, anticholinergics agents. Fexofenadine may reduce the concentrations of acetylcholinesterase inhibitors (in the CNS), betahistine.
Fexofenadine levels may be reduced by the acetylcholinesterase inhibitors (in the CNS), amphetamine, antacids, grapefruit juice, rifampin.

Undesirable effects (ADRs)

The undesirable effects of Agimfast 120 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.

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 is not an effective means of removing fexofenadine from plasma (only 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 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 120 has fast and prolonged effects because fexofenadine slowly binds to H1 receptor to form a stable complex from which it subsequently slowly dissociates.

Pharmacokinetic properties

Agimfast 120 is well absorbed following oral administration. Peak plasma concentration was achieved after 2-3 hours. The mean Cmax value was approximately 427ng/ml following the administration of a 120mg dose once daily. The administration of fexofenadine with meal decreased plasma peak concentration by 17%, but, the time to reach peak concentration was not slowed down.
Fexofenadine is 60-70% bound to plasma proteins, principally albumin and alpha1-acid glycoprotein. Volume of distribution is 5.4 to 5.8 liters/kg. It is unknown whether fexofenadine crosses the placenta or is excreted in breast milk. However, when terfenadine was used, fexofenadine, a terfenadine metabolites, was found in breast milk. Fexofenadine does not cross the blood-brain barrier.
Approximately 5% of oral dose is metabolized. Approximately 0.5 to 1.5% of dose is metabolized in the liver by the cytochrome P450 microsomal enzyme system to an inactive metabolite. About 3.5% of a fexofenadine dose is metabolized to methyl ester derivative, mainly due to intestinal microbial flora.
The elimination half-life of fexofenadine is about 14.4 hours, it is longer in patients with renal impairment. Fexofenadine is primarily excreted in the feces (approximately 80%), 11-12% of the dose is excreted unchanged in the urine.

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.