Fexofenadine , sold under the trade name Allegra of which is an antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as fever and urticaria. Therapeutically, fexofenadine is a peripheral selective H1-blocker.
Fexofenadine is classified as a second generation antihistamine because it is less able to cross the blood-brain barrier and cause sedation, compared to first-generation antihistamines. This is also called third generation antihistamine, although there is some controversy associated with the use of the term.
Fexofenadine has been produced in generic form since 2011.
Video Fexofenadine
Medical use
Fexofenadine is used to relieve the physical symptoms associated with seasonal allergic rhinitis and for the treatment of chronic urticaria. It does not heal but prevents the aggravation of allergic rhinitis and chronic idiopathic urticaria and reduces the severity of symptoms associated with the condition, providing relief from recurrent sneezing, runny nose, itchy eyes or skin, and general body fatigue.
Maps Fexofenadine
Side effects
The most common side effects demonstrated in adults are headache, but some also have back and muscle pain, proper miosis or pupils, nausea, drowsiness, and menstrual cramps. There are also reports of rare anxiety and insomnia. The most common side effects shown during clinical trials are cough, upper respiratory tract infection, fever, and otitis media for children aged 6 to 11 years and fatigue for children ages 6 months to 5 years.
Overdose
The fexofenadine safety profile is quite beneficial, as no cardiovascular or sedative effects are proven to occur even when taking 10 times the recommended dosage. Research in humans ranged from a single dose of 800 mg, with a dose of 690 mg daily for a month, with no clinically significant side effects, when compared with placebo. No deaths occurred in the test in mice, weighing 5000Ã, mg/kg, which is a hundred times the maximum ten (110x) dose recommended for adult humans. If overdose occurs, supportive action is recommended. Theoretically, overdose can appear as dizziness, dry mouth, and/or drowsiness, consistent with excessive side effects commonly occurring. It does not appear that hemodialysis is an effective way to remove fexofenadine from the blood.
Action mechanism
Fexofenadine is a peripheral selective H1-blocker. Blockage prevents the activation of H1 receptors by histamine, preventing symptoms associated with allergies from occurring. Fexofenadine is not easy to cross the blood-brain barrier and is therefore less likely to cause drowsiness than other antihistamines ready to cross the blood-brain barrier (ie, first-generation antihistamines such as diphenhydramine). In general, fexofenadine takes about an hour to apply, although this may be influenced by the choice of dosage form and the presence/absence of certain foods.
Fexofenadine also showed no effect of blocking anticholinergic receptors, antidopaminergic, alpha1-adrenergic, or beta-adrenergic-receptor.
Pharmacokinetics
- Absorption: After oral application, maximum plasma concentration is reached after two to three hours. Fexofenadine should not be consumed with high fatty foods, because the concentration of fexofenadine in the bloodstream is seen to decrease from 20-60% depending on the form of the drug (tablet, ODT, or suspension).
- Distribution: Fexofenadine is 60-70% bound to plasma proteins, mostly albumin.
- Metabolism: Fexofenadine is a CYP3A4 substrate. However, only about 5% is metabolized by the liver, indicating that the role of liver metabolism is relatively small in its leeway from the body.
- Elimination: Most of the substance removed does not change through the feces (80%) and urine (11-12%).
Interactions
Taking erythromycin or ketoconazole while taking fexofenadine does not increase plasma plasma levels of fexofenadine, but this increase does not affect QT interval. The reasons for this effect are probably due to transport-related effects, especially those involving p-glycoprotein (p-gp). Both erythromcin and ketoconazole are p-gp inhibitors, a transporting protein involved in preventing intestinal uptake of fexofenadine. When p-gp is inhibited, fexofenadine may be better absorbed by the body, increasing plasma concentrations more than what is intended.
Fexofenadine should not be taken with apple juice, oranges, or wine as it may reduce the absorption of the drug and therefore should be taken with water. Grapefruit juice can significantly reduce plasma concentrations of fexofenadine.
Antacids containing aluminum or magnesium should not be taken in 15 minutes of fexofenadine because they reduce the absorption of fexofenadine by almost 50%. This is not to be regarded as a change in pH (in fact, absorption may actually increase below the increasingly alkaline pH), but rather because of the formation of metal complexes with polar groups in fexofenadine. As suggested by Shehnaza et al (2014), various sites of molecules are considered responsible for this interaction, including nitrogen piperidine, carboxylic acid group (-COOH), and both hydroxyl (- OH) groups.
Foods with high amounts of fat reduces the absorption of fexofenadine by about 50%.
Custom population
Fexofenadine is the category of pregnancy C and should only be used if the benefits outweigh the risks.
No research has been done to evaluate the presence of fexofenadine in breast milk. Therefore, nursing women are urged to be careful when using fexofenadine.
No sufficient study has been done in patients over the age of 65. Therefore, it is recommended that elderly patients use liver when using fexofenadine, especially when there is concern for kidney disorders.
History
An older antihistamine agent known as terfenadine was found to metabolize into the corresponding carboxylic acid, fexofenadine. Fexofenadine is found to retain all the biological activity of its mother while providing fewer adverse reactions in the patient, so that terfenadine is replaced in the market by its metabolite. Fexofenadine was originally synthesized in 1993 by the Massachusetts-based biotech company Sepracor, which then sold development rights to Hoechst Marion Roussel (now part of Sanofi-Aventis), and then approved by the Food and Drug Administration (FDA) in 1996 Albany Molecular Research Inc. (AMRI) holds patents for intermediates and production of HCl fexofenadine along with Roussel. Since then, it has achieved a blockbuster drug status with global sales of $ 1.87 billion in 2004 (with $ 1.49 billion USD coming from the United States). AMRI received royalty payments from Aventis that enabled AMRI growth.
On January 25, 2011, the FDA approved the sale of fexofenadine sold freely in the United States, and the Sanofi Aventis' version became available on March 4, 2011.
Other brand names
Fexofenadine yang Dipasarkan di banyak nama-nama merk di seluruh dunia by December 2017, termasuk: Agimfast, Alafree, Alanil, Alercas, Alerfedine, Alerix, Alertam Alexia Allegix, Allegra, Allegratab, Allemax, Aller nyata, Allerf, Allerfexo, Allergo, Allergy , Allenphast, Alrin, Alterreal Altifex, Altiva, Aspen, Axodin, Axofen, Bixin, Bosnum, Dinafex, Ewofex, Fastel, Fastofen, Fastway, Fe Min, Feksine, Fenadex, Terfenadine, Fenafex, Phenax, Fenofex, Fentradol, Fesler, Fexadyne, Fexal, Fexalar, Fexaway, Fexetra, Fexgen, Fexidine, Fexigra, Fexin, Fexo, Fexodane, Fexodine, Fexodis, Fexofast, Fexofen, Fexofenaderm, Fexofenadine, Fexofenadin, Fexofenadine, Fexofà © nadine, Fexofep, Fexofin, Fexogen, Fexomin , Fexon, Fexona, Fexonadinea, Fexoquit, Fexoral, Fexoril, Fexostad, Fexotin, Fexovid, Fixal, Fixit, Fixodin, Flexofen, Foxin, Fynadin, Glossas, Hasalfast, Histafree, Imexofen, Kofixir, Lai Duo Fei, Mayfex, Minie Jie, Nefoxef, Neofex, Nolargy, Nosedex, Odafen, Oregra, Radifex, Ral Tiva, Rapido, Rhinogan, Ridrinal, Rhinofen, Rinolast, Ritch, Rui Fei, Sailexi, Tefodine, Telfadin, Telfast, Telfastin, Telfexo, Tellerge, Terfemax, Ternafast, Tocimat, Tofexo, Torfast, Vifas, Vifasesh, X-Dine, Xergic , then Zefeksal.
In January 2017 it is marketed as a combination drug with pseudoephedrine under brand name including: Alerfedine D, Allegra-D, Allergyna-D, Altiva-D, Dellegra, Fexo Plus, Fexofed, Fixal Plus, Ridrinal D, and Rinolast D.
In January 2017 it is marketed as a combination drug with brand name montelukast including Fexokast, Histakind-M, Monten-FX, Montolife-FX, and Novamont-FX.
See also
- Terfenadine
References
External links
- Fexofenadine (UK patient information leaflet)
- "fexofenadine" at medicinenet.com
Source of the article : Wikipedia
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