Prior authorization is required for the brand, unless a particular form of that drug (for example, tablet, capsule, or liquid) does not have an FDA “A”-rated generic equivalent.Smart PA: Claims for desloratadine tablets will usually process at the pharmacy without a PA request if the member has Mass Health medical claims for allergic rhinitis or chronic idiopathic urticaria and a history of paid pharmacy claims for ≥14 days out of the last 180 days of one intranasal corticosteroid and two of the following: loratadine tablets or liquid, cetirizine tablets or liquid, levocetirizine tablet.Generally the broader action that these compounds have at blocking receptors, the more sedatibg they will be.I know this thread is a little old, but I thought I'd chime in anyways.You can't compare all of these because they all have very different effects around the body.Sure, they may all antagonize H1, but antagonization of H1 is not the only thing that produces sedation!Smart PA: Claims for a combination antihistamine/decongestant agents listed above will usually process at the pharmacy without a PA request if the member has Mass Health medical claims for allergic rhinitis or chronic idiopathic urticaria and a history of paid pharmacy claims for ≥ 14 days out of the last 180 days of loratadine/pseudoephedrine, cetirizine/pseudoephedrine and an intranasal corticosteroid.
My only interest here is to know what works acutely and is not going to pussyfoot around.) Serotonin transporter (IC50 = 100n M) Norepinephrine transporter (IC50 = 260n M) Dopamine transporter (IC50 = 1,000n M) Haloperidol - antagonist at the following receptors: α1-adrenergic (Ki = 12n M) Alpha Adrenergic 2a (Ki = 1130n M) Alpha Adrenergic 2b (Ki = 480n M) Alpha Adrenergic 2c (Ki = 550n M) D1 (Ki = 10-15n M) D5 (Ki = 15-17n M) D2 (Ki = 1.55n M) D3 (Ki = 0.74n M) H1 (Ki = 1800n M) 5HT2A (Ki = 53n M) 5HT2C (Ki = 10,000n M) 5HT6 (Ki = 3666n M) 5HT7 (Ki = 377.2n M) M1 (Ki = 10,000n M) NR1\NR2B Subunit containing NMDA receptor antagonist Ifenprodil site (IC50 = 2m M) And also acts on the following: D4 inverse agonist (Ki = 5-9n M) 5HT1A agonist (Ki = 1927n M) Sigma 1 Irreversible inactivation by HPP (Ki = 3n M) Sigma 2 agonist (Ki = 54n M) Trazodone - antagonist at the following receptors: α1-adrenergic (Kd = 39 n M) α2-adrenergic (Kd = 405 n M) H1 (Kd = 725 n M) 5-HT2A (Ki = 13 n M) 5-HT2B (Ki = 74 n M) 5-HT2C (Ki = 192 n M) Also has the following actions: 5-HT1A receptor partial agonist (Kd = 78 n M) SERT transporter inhibitor (Kd = 160 n M) So, if one is able to understand these, you can see from the numbers why some are more effective than others for sedation, likelihood of unwanted side effects, and why dose is so important. Doxylamine has been shown to be a more effective sedative than babiturates.I don't doubt that Seroquel etc are just as good though.Dose is very important, because an antihistamine is not just an antihistamine, it will have varying binding affinities for other receptors and you want a dose that gives you a decent amount of histamine antagonism yet little activation of other receptors that are stimulating.Most people's problem with antihistamines for sleep is they take too high a dose, assuming more is better. And when tolerance builds, taking more is not going to help because then you get more of the other stuff like anticholinergic effects.Tolerance to sedation from antihistamines can build very rapidly.