Buclizine Hydrochloride

MOA: BliiBuclizine is a hithistam ine H1 antagon ist with an tieme tic and antivertigo properties. It also exhibits anticholinergic, centltral nervous system dtdepressant, and lllocal anesthe ticeffect s.

Uses: It is used in the symp toma tic tttreatmen t of motion sickness and control of vertigo associated with vestibular system diseases. Chlorpheniramine maleate

MOA: Chlorpheniramine binds to the histamine H1 receptor. This bloc kstheactionof endogenous histamine, whhhich subsequently leads to temporary relief of the negative symptoms bhbroughtonby histamine. Uses: Used for the symptomatic relief of hypersensitivity reactions, coughs, and the common cold. Triprolidine

MOA: Triprolidine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subseqqyuently leads to temppyorary relief of the negative symptoms brought on by histamine. Uses: Used for the syypmptomatic relief of hypersensitivity reactions, coughs, and the common cold. PhenindamineTartarate

3

MOA: Phenindamine blocks the effects histamine in the body. It appear to compete with histamine for histamine H1- receptor sites on effector cells. The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release. Uses: It is used to treat sneezing, runny nose, itching, watery eyes, hives, rashes, itching, and other symptoms of allergies and the common cold. Promethazine Hydrochloride MOA: oPromethazine is a an antagonist of histamine H1, post- synaptic mesolimbic dopamine, alpha adrenergic, muscarinic, and NMDA receptors. oThe antihistamine action is used to treat allergic reactions. Antagonism of muscarinic and NMDA receptors contribute to its use as a sleep aid, as well as for anxiety and tension. oAntagonism of histamine H1, muscarinic, and dopamine receptors in the medullary vomiting center make promethihazine useflful inthe treatment of nausea and vomiiiting. Uses: to treat rhinitis, allergic conjj,unctivitis, allergic reactions to blood or plasma, dermographism, anaphylactic reactions, sedation, nausea, vomiting, pp,ain, motion sickness, and allergic skin reactions. Trimeprazine Tartarate

9 1 8 S COOH 7 2 . OH 6 3 OH N 4 5 10 CH3 COOH CH2 CH CH2 N 1 2 3 CH3 CH3

MOA: Trimeprazine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative syypmptoms brought on by histamine. Uses: Used for the symptomatic relief of hypersensitivity reactions, pruritus ((g)itching) and urticaria (some allergic skin reactions). Cyproheptadine hydrochloride 10 11 9 1 8 2

7 5 3 6 4 4 5 3 2 6 N 1 CH3 MOA: ChdiCyproheptadine competes w it h free histam ine for bin ding at HA- receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite. Uses: Allerg ic rhin it is, rhin it is, urtiiicariaand angidioedema and dermatographism.