Anti-histamine

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All Medicinal Chemistry 2 Flashcards on Anti-histamine, created by Majd Fawaz on 22/05/2021.
Majd Fawaz
Flashcards by Majd Fawaz, updated more than 1 year ago
Majd Fawaz
Created by Majd Fawaz almost 4 years ago
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Question Answer
- Betahistine - H-3 antagonist and H-1 weak agonist - Direct and indirect agonist (cause of the negative feedback of H-3) - Only B-aminoethyl heterocyclic compound with agonstic activity - Antivertigo drug (Meniere's disease)
- Khelline - Chromone that causes bronchodilation (inhibits histamine release) but does not reverse bronchoconstriction
- Nedocromil - Lacks antihistamine effect - Lacks bronchodilatory effect - Poor oral bioavailability - Given by inhalation for asthma, nasal for rhinitis, topically for conjugtivites - Chronic use might cause tolerance
- Chromolyn sodium - Lacks antihistamine effect - Lacks bronchodilatory effect - Poor oral bioavailability - Given by inhalation for asthma, nasal for rhinitis, topically for conjugtivites - Chronic use might cause tolerance
- Lodoxamide - Mast cell stabilizer - Used topically for conjunctivitis
- Pemirolast - Pyrimidinone derivative - Used topically for conjunctivitis - Inhibits release of histamine and leukotrienes
- Phenbenzamine - Ethylenediamine derivatives - was 1st class of anti-hist - Spacer: 2C - X: N
- Tripelennamine - Ethylenediamine derivatives - 1st Gen H-1
- Thonzylamine - Ethylenediamine derivatives - 1st Gen H-1 - Sedation, drowsiness, may impair mental activity
- Cyclazine - Piperazine derivative (Ethylenediamine) - Moderatly potent - Longer DOA - Has anti-choli effects - For nausea and vomiting - Lactate form for IM
- Chlorcyclazine - Piperazine derivative (Ethylenediamine) - Moderatly potent - Longer DOA - Has anti-choli effects - More lipophilic - Less likely to be metabolized - For urticaria and hay fever
- Hydroxyzine - Piperazine derivative (Ethylenediamine) - Moderatly potent - Longer DOA - Has anti-choli effects - market sedation - Used for pruritus - At higher doses for anxiety
- Meclezine - Piperazine derivative (Ethylenediamine) - Moderatly potent - Longer DOA - Has anti-choli effects - Used for nausea and vomiting due to motion sickness and radiation sickness
- Buclizine - Piperazine derivative (Ethylenediamine) - Moderatly potent - Longer DOA - Has anti-choli effects - Used for nausea and vomiting due to motion sickness and radiation sickness
- Oxatomide - Piperazine derivative (Ethylenediamine) - Moderatly potent - Longer DOA - Has anti-choli effects - Antihistamine - Antimuscarine - Mast stabilizer (given before time)
- Diphenhydramine - Marked sedation - Antitussive - Antiemitic -Antihistaminic - Anticholinergic - p-methyl --> Increase antihistamine - o-methyl --> Increase anticholinergic - 3*N --> 4*N increase anticholinergic
- Dimenhydrinate - 8-chlorothiophyline salt of diphenhydramine - Indicated for motion sickness
- Bromodiphenhydramine - More lipo --> More potent
- Chlorodiphenhydramine - More lipo --> More potent
- Carbinoxamine - Potent antihisamine - Levo > dextro
- Doxylamine - Same potency and diphenhydramine but more CNS depression --> given hypnotic agent
- Climastine - Propylamine derivative (aminoalkyl ether) - Potent antihistamine - R,R most potent - Long DOA - Less anticholinergic effect - Less sedation
- Pheniramine - P-chloro is x10 more potent - dextro>levo - Longer acting - P-Bromo is equipotent - Longer DOA than Chloro - dextro>levo
- Triprolidine - Potent antihistamine - Long DOA - E>Z - Distance between the N and the aromatic ring is important
- Pyrrobutamine - Potent antihistamine - Long DOA - E>Z - Distance between the N and the aromatic ring is important
What are the Characteristics of TC anti-histamines phenothiazines - Moderatly potent - Long DOA - Sedation - Analgesia - Drowsiness - Antianxiety
- Promethazine - TC antihistamine (ethylene diamine) - Used for allergic rhinits+pruritus
- Pimethexine - If you replace the N with sp2 C --> orally active anti-histamine - Thioxanthine derivative
- Methixine - If you replace the N with sp3 C --> moderate potent + Anticholinergic (antiparkinson)
- Cyproheptadine - Anti Cholinergic+histaminic+sertoninergic - Apetite stimulant --> good for anorexia
- Azatedine - Aza isostere of 10,11 dihydrocyproheptadine - Anti cholinergic+histaminic - Long acting
- Ketotifen - Thiophene 9,10 dihydro 10 keto cyproheptadine - Potent anti histamine - Mast cell stabilizer
What are the characteristics of the 2nd Gen H1 Antihistamine - Less sedation - Less Anticholinergic effects - Less adrenergic - Less serotoninergic - Selective H1
- Terfenadine - First H1 antagonist with no sedation - Cardiotoxic so discontinued - Active non toxic metabolite (COOH instead of CH3)
- Ebastine - Benzhydryl ether - H1 antagonist - Potent - Long Acting - Non sedative
- Ceterizine - CA metabolite of Hydroxyzine - Levo x30> Dextro
- Loratadine - Ethyl carbamate derivative of azatedine - Long acting - Non sedative - Low affinity to CNS transport protein --> Less CNS side effects - Active metabolite --> Desloratadine
- Acrivastine - Triprolidine analogue - Same activity without CNS
What are the topical anti histamines? - astine - adine - Keto Fumarate - Used for seasonal allergic conjunctivitis - Used for seasonal allergic rhinitis
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