Telfast 120 Mg 7 Film-coated Tablets

Telfast (120 Mg 7 Coated Tablets)

Fexofenadine hydrochloride

ACTION AND MECHANISM

- Antiallergic. Fexofenadine is the carboxylated metabolite of terfenadine. It is a piperidine derivative that blocks H1 receptors in a powerful, competitive and specific way, reducing the systemic effects of histamine for a long time. The unblocking of the receptors is very slow, so the antagonism is practically irreversible, depending on the dose administered. It leads to vasoconstriction and decreased vascular permeability, reducing redness and edema associated with allergy. Partially mitigates symptoms associated with allergic processes such as eye redness or nasal congestion. It also produces a slight bronchodilator effect and a decrease in dermal itching.Clinical experience also seems to show that fexofenadine is capable of preventing the release of histamine from mast cells.

Fexofenadine is barely able to cross the blood-brain barrier and thus has virtually no significant sedative effects. It shows great selectivity for H1 receptors, lacking important anticholinergic effects. It has been found that fexofenadine is not capable of blocking the potassium channels involved in the repolarization of the cardiac fiber, so it will not have a cardiotoxic effect.

PHARMACOKINETICS

Linear pharmacokinetics in doses up to 120 mg, 2 times a day. At higher doses (240 mg twice daily) the AUC increases 8.8% above normal.

- Absorption: Fexofenadine is rapidly absorbed from the intestine after oral administration. The Cmax obtained after administering a dose of 120 mg and 180 mg is 427 ng / ml and 494 ng / ml, respectively. The Tmax is 2.6 h. The antihistamine effect appears after 1 h, is maximum at 6 h and lasts for 24 h.

Effect of food : The administration of fexofenadine together with food can lead to a decrease in Cmax of 17%, which is not clinically significant.

- Distribution: 60-70% plasma protein binding, mainly albumin and alpha-1-acid glycoprotein. It is widely distributed throughout the tissues, although it does not appear to cross the blood-brain barrier. It is unknown whether it crosses the placenta. Fexofenadine appears to be excreted with milk, although the amount excreted by this route is unknown. Fexofenadine is a substrate for P-gp.

- Metabolism: minimal (<5%), leading to small amounts of inactive compounds.

- Elimination: in feces (80%, mostly unchanged) by biliary excretion. Small amounts (10%) in urine. The t1 / 2 is 11-15 h.

Pharmacokinetics in special situations :

- Children: AUC is 56% higher in children 7-12 years than in adults.

- Elderly: Cmax is 99% higher in> 65 years than in those between 19-45 years. Also the AUC is higher in elderly patients, but these values ​​are considered within acceptable limits.

- Renal insufficiency: in mild to moderate insufficiency (ClCr 41-80 ml / min) and in those with severe renal insufficiency (ClCr 11-40 ml / min) the Cmax was 87% and 111% higher respectively, while the Clr was 59% and 72% higher, when compared to patients with normal kidney function.

INDICATIONS

"PRESENTATIONS 120 mg"

- Relief of symptoms associated with [SEASONAL ALLERGIC RHINITIS] in adults and adolescents from 12 years of age.

POSOLOGY

- Adults: 1 tablet, once a day.

- Children and adolescents under 18 years of age:

* Adolescents from 12 years old: the same as adults.

* Children <12 years: not recommended.

- Elderly: does not require dosage adjustment.

Missed dose : administer the next dose at the usual time. Do not double the next dose.

DOSAGE IN KIDNEY INSUFFICIENCY

It does not require dosage adjustment.

DOSAGE IN LIVER INSUFFICIENCY

It does not require dosage adjustment.

RULES FOR CORRECT ADMINISTRATION

Swallow the tablets with water.

Administration with food : administer before a meal.

CONTRAINDICATIONS

- Hypersensitivity to fexofenadine or to any component of the drug. There may be cross reactions with other antihistamines, so it is not recommended to use any H1 antihistamine in patients who have presented hypersensitivity to any compound in the group.

PRECAUTIONS

- [CARDIAC ARRHYTHMIA]. Antihistamines have been associated with the development of tachycardia and palpitations.

- Limitations in clinical experience. Its efficacy and safety in patients with [KIDNEY FAILURE] or [HEPATIC FAILURE] have not been evaluated. Although no specific dosage recommendations have been established, caution is advised.

ADVICE TO THE PATIENT

- Take your medication at approximately the same time every day. If you forget to take a dose, take the next one at the usual time. Do not double a dose to make up for a forgotten one.

SPECIAL WARNINGS

- Due to the antiallergic effects of this medicine, it could give false negatives in dermal tests of hypersensitivity to antigenic extracts. It is recommended to suspend the administration of this medicine at least 72 hours before the test.

INTERACTIONS

- Antacids. Co-administration of fexofenadine and antacids with magnesium or aluminum could decrease the absorption of fexofenadine. It is recommended to distance the taking of both medications at least 2 h.

- Erythromycin and ketoconazole: the administration of either of these two drugs together with fexofenadine, can lead to an organic accumulation of the antihistamine, leading to toxic effects.
- Grapefruit juice: possible decrease in the absorption of fexofenadine.
- Pollen: a loss of reliability of the pollen diagnostic test may occur. It is recommended to leave an interval of 2-3 days after the last intake of short-acting antihistamines and 8 weeks with long-acting ones.
- Rifampicin: possible decrease in the organic levels of fexofenadine and, as a consequence, in its therapeutic activity.
- Cabozantinib: co-administration with P-glycoprotein substrates, including fexofenadine, may lead to an increase in adverse reactions.

PREGNANCY

Safety in animals : fexofinadine was not teratogenic in rats and rabbits (Cp 4-31 times higher than in humans). Administration in rats of 150 mg / kg (Cp 3 times higher than in humans) was associated with decreased birth weight and neonatal survival of the progeny.

Safety in humans : There are no adequate and well-controlled studies in humans. Its administration is only accepted if there are no safer therapeutic alternatives, and the benefits outweigh the possible risks.

Effects on Fertility : No specific studies have been performed in humans. Fexofenadine did not affect fertility in mice.

LACTATION

Animal safety : no data available.

Safety in humans : fexofenadine is excreted in human milk, although there are no data regarding the amount of drug excreted. Its administration is not recommended during lactation.

KIDS

Fexofenadine can be used in adolescents from 12 years of age, at the same doses as in adults.

Safety and efficacy have not been evaluated in children <12 years of age, so it is recommended to avoid its use.

SENIORS

No specific problems have been described in the elderly that require a dosage adjustment.

EFFECTS ON DRIVING

It does not seem likely that it could lead to significant effects. However, drowsiness, dizziness, or headache are common.

ADVERSE REACTIONS

Adverse reactions are described according to each frequency range, being considered very common (> 10%), common (1-10%), uncommon (0.1-1%), rare (0.01-0.1%) , very rare (<0.01%) or of unknown frequency (cannot be estimated from the available data).

- Immune system disorders: frequency unknown [HYPERSENSITIVITY REACTIONS] with manifestations such as [ANGIOEDEMA], [THORACIC OPPRESSION], [DYSNEA], [SOFOCUS] and [ANAPHYLAXIA].

- Psychiatric disorders: frequency unknown [INSOMNIA], [NERVIOSISM], [SLEEP DISORDERS] or [NIGHTMARES] / excessive dreams ([PARANOIA]).

- Nervous system disorders: common [HEADACHE], [Drowsiness], [DIZZINESS].

- Cardiac disorders: unknown frequency [TACHYCARDIA], [PALPITATIONS].

- Gastrointestinal disorders: common [NAUSEAS]; frequency unknown [DIARRHEA].

- Skin and subcutaneous tissue disorders: frequency unknown [EXANTEMATIC ERUPTIONS], [URTICARIA], [PRURITO].

- General disorders and administration site conditions: uncommon [FATIGUE].

OVERDOSE

Symptoms : Dizziness, drowsiness, fatigue and dry mouth have been reported from overdose with fexofenadine. Single doses up to 800 mg, and doses up to 690 mg twice daily for one month or 240 mg once daily for one year have been administered to healthy adults without the development of clinically significant adverse effects compared to placebo. The maximum tolerated dose of fexofenadine has not been established.

Measures to be taken :

- Antidote: there is no specific antidote.

- General elimination measures: common measures to eliminate unabsorbed drug. Hemodialysis does not effectively remove fexofenadine from the blood.

- Monitoring: patient monitoring does not seem necessary.

- Treatment: symptomatic.

Telfast 120 Mg 7 Coated Tablets Leaflet