Azatadine Maleate.

Azatadine maleate, 6,11-dihydro- 11-(l-methyl-4-piperidylidene)-5H-

benzo-[5,6]cyclo- hepta(1,2-b]pyridine maleate (1:2) (Optimine), is a potent, long-acting
antihistaminic with antiserotonin activity. In early testing, azatadine exhibited more than three
times the potency of chiorpheniramine in the isolated guinea pig ileum screen and more than
seven times the oral potency of chlorpheniramine in protection of guinea pigs against a double
lethal dose of intravenously administered histamine.
Dosage forms: Tablets (1 mg)
Usual dosage: 1 to 2 mg twice daily

Fexofenadine Hydrochloride. Fexofenadine hydrochloride, (6)-4-[1-hydroxy-4-[4-

(hydroxyldiphenyl-methyl)-1-piperinyl]butyl- , -dimethylbenzeneacetic acid (Allegra), occurs as
a white to off-white crystalline powder that is freely soluble in methanol and ethanol, slightly
soluble in chloroform and water, and insoluble in hexane. This compound is marketed as a
racemate and exists as a zwitter-ion in aqueous media at physiological pH.
Fexofenadine is a primary oxidative metabolite of terfenadine. Terfenadine was developed
during a search for new butyrophenone antipsychotic drugs as evidenced by the presence of the
N-phenylbutanol substituent. It also contains a diphenylmethyl-piperidine moiety analogous to
that found in the piperazine antihistamines. Terfenadine is a selective, long-acting (.12 hours)
H1-antihistamine with little affinity for muscarinic, serotonergic, or adrenergic receptors. The
histamine receptor affinity of this compound is believed to be related primarily to the presence of
the diphenylmethylpiperidine moiety. The prolonged action results from very slow dissociation
from these receptors. The lack of anticholinergic, adrenergic, or serotonergic actions appears to
be linked to the presence of the N-phenylbutanol substituent. This substituent contributes to P-
glycoprotein efflux pump affinity, which serves to limit accumulation of terfenadine in the CNS.
Terfenadine undergoes significant first-pass cytochrome P450 (CYP)-based metabolism, with the
predominant metabolite being fexofenadine, an active metabolite resulting from methyl group
oxidation. When drugs that inhibit this transformation, such as the imidazole antifungals and
macrolides, are used concurrently, terfenadine levels may rise to toxic levels, resulting in
potentially fatal heart rhythm problems that were described. The observation that fexofenadine
displays antihistaminic activity comparable with that of terfenadine but is less cardiotoxic led to
its development as an alternative to terfenadine for the relief of the symptoms of seasonal
allergies.
Fexofenadine, like terfenadine, is a selective peripheral H1-receptor ligand that produces no
clinically significant anticholinergic effects or 1-adrenergic receptor blockade at therapeutic
doses. No sedative or other CNS effects have been reported for this drug, and animal studies
indicate that fexofenadine does not cross the BBB. In vitro studies also suggest that unlike
terfenadine, fexofenadine does not block potassium channels in cardiocytes. Furthermore, in
drug interaction studies, no prolongation of the QTc interval or related heart rhythm
abnormalities were detected when fexofenadine was administered concurrently with
erythromycin or ketoconazole.
Fexofenadine is indicated for the treatment of seasonal allergic rhinitis and chronic idiopathic
urticaria. It is rapidly absorbed after oral administration, producing peak serum concentrations in
about 2.5 hours. Fexofenadine is 60% to 70% plasma protein bound. Unlike its parent drug, only
5% of the total dose of fexofenadine is metabolized. The remainder is excreted primarily in the
urine; the mean elimi-nation half-life is about 14 hours.
Dosage form: Tablets (30, 60, and 180 mg), oral disintegrat-ing tablets (30 mg), and an oral
suspension (6 mg/mL)
Usual doses:
 • Chronic idiopathic urticaria: 60 mg twice daily or 180 mg once daily in adults and children;
lower doses are recommended in children
• Seasonal allergic rhinitis: 60 mg twice daily or 180 mg once daily in adults and children;
lower doses are recommended in children

levocabastine
The chemical name for levocabastine hydrochloride is (–)-trans-1-[cis-4-Cyano-4- (p-
fluorophenyl)cyclohexyl]-3-methyl-4-phenylisonipecotic acid monohydrochloride
Levocabastine is a potent, selective histamine H1-antagonist.
Antigen challenge studies performed two and four hours after initial drug instillation indicated
activity was maintained for at least two hours.
In an environmental study, Livostin™ 0.05% (levocabastine hydrochloride ophthalmic
suspension) instilled four times daily was shown to be significantly more effective than its
vehicle in reducing ocular itching associated with seasonal allergic conjunctivitis.
After instillation in the eye, levocabastine is systemically absorbed. However, the amount of
systemically absorbed levocabastine after therapeutic ocular doses is low (mean plasma
concentrations in the range of 1-2 ng/mL).
is indicated for the temporary relief of the signs and symptoms of seasonal allergic
conjunctivitis.
Levocabastine is a synthetic piperidine derivative with antihistamine properties. Levocabastine is
a second generation histamine-1 receptor antagonist. When applied locally into the eye as a
topical solution, this agent reduces itching, rhinorrhea and symptoms of allergic rhinitis or
conjunctivitis.

Terfenadine
Terfenadine is a selective histamine H1-receptor antagonist devoid of central nervous system
depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT
SYNDROME.
White to off-white crystalline powder

astemizol
Antihistaminic puternic si de lunga durata, actionand ca antagonist la nivelul receptorilor H1,
fara efecte centrale, sedative si anticolinergice. Produsul este rapid absorbit din tubul digestiv,
concentratiile sanguine maxime realizandu-se la 30-60 minute dupa administrare. Dupa
metabolizare astemizolul este eliminat prin bila. Doza terapeutica asigura blocarea receptorilor
H1, pentru aproximativ 24 ore. Produsul nu traverseaza membrana hemato-encefalica.
Administrarea unei doze de 6 ori mai mari decat cea terapeutica nu altereaza activitatea mentala.
INDICAŢII
Rinita alergica sezoniera si nesezoniera, conjunctivita alergica, urticaria cronica si alte afectiuni
alergice.

MOD DE ADMINISTRARE
Adulti si copii mai mari de 12 ani: 1 comprimat/zi, copii intre 6-12 an: -5 mg (1/2 comprimat) pe
zi. Copii mai mici de 6 ani: 2 mg/kg corp pe zi.

REACŢII ADVERSE
In cursul tratamentului prelungit, poate determina o crestere ponderala.

Azatadină maleat. Azatadină maleat, maleat de 6,11-dihidro-11- (1-metil-4-piperidiliden) -5H-

benzo [5,6] ciclohepeta [1,2-b] piridină , este un antihistaminic cu activitate antiserotoninergică
puternică și cu durată lungă de acțiune. La testarea timpurie, azatadina a prezentat o potența
orală de șapte ori mai mare decât a clorfeniraminei în protecția porcilor de guineea împotriva
unei doze duble letale de histamină administrată intravenos.
Forme de dozare: Tablete (1 mg)
Doza obișnuită: de la 1 până la 2 mg de două ori pe zi

levocabastină
Denumirea chimică a clorhidratului de levocabastină este monoclorhidratul acidului (-) - trans-1-
[cis-4-cian-4- (p-fluorfenil) ciclohexil] -3- metil- 4- fenilisonipecotic
Levocabastina este un antagonist potent, selectiv al histaminei H1.
Studiile de provocare cu antigen efectuate la două și patru ore după instilația inițială a
medicamentului au indicat că activitatea a fost menținută timp de cel puțin două ore.
Într-un studiu de mediu, Livostin ™ 0,05% (suspensie oftalmică de clorhidrat de levocabastină)
instilită de patru ori pe zi sa dovedit a fi semnificativ mai eficace decât vehiculul său în
reducerea pruritului ocular asociat cu conjunctivita alergică sezonieră.
După instilare în ochi, levocabastina este absorbită sistemic. Cu toate acestea, cantitatea de
levocabastină absorbită sistemic după dozele oculare terapeutice este scăzută (concentrațiile
plasmatice medii în

levocabastină
Denumirea chimică a clorhidratului de levocabastină este clorhidratul acidului [3S-[1(cis),3α,
4β]]-1-4-ciano-4(4-fluorofenil)-ciclohexil]-3-metil-4-fenil-4-piperidincarboxilic.
Levocabastina este un derivat de piperidină sintetic cu proprietăți antihistaminice. Acesta face
parte din a doua generație de antagonişti ai receptorului H1. Atunci când este aplicat local în
ochi ca o soluție topică, acest agent reduce mâncărimea, rinoreea și simptomele de rinită alergică
sau conjunctivită.
După instilare în ochi, levocabastina este absorbită sistemic. Totuși, cantitatea de levocabastină
absorbită sistemic după dozele oculare terapeutice este scăzută (concentrații plasmatice medii în
intervalul 1-2 ng / ml).
Este indicat pentru ameliorarea temporară a semnelor și simptomelor conjunctivitei alergice
sezoniere.