Antihistamines Flashcards
Antihistamines
Adverse effects
Primarily due to antihistamine effects: sedation or CNS stimulation, anticholinergic effects( anti -slud)
-dizziness, tinnitus, uncoordinated, blurry vision, nervousness, insomnia, tremors
-loss of appetite, N/V, constipation
, diarrhea, increase appetite or weight gain
First generation antihistamines
Fast onset across the BBB
Around longer (old)
More sedating vs second generation
Second generation antihistamines
DONT cross the BBB
Actions similiar to 1st generation; primarily H1 antagonist actions
Newer
Better tolerated; less AEs
Non-sedating: less likely to make you sleepy
Less CNS penetration
Diphenhydramine (Benadryl) Dimenhydrinate (Dramamine) Clemastine (tavist) Carbinoxamine (rondec) Pyrilamine (poly-histine-D) Tripelennamine (PBZ) Hydroxyzine (atarax, vistaril) Cyclizine Meclizine (antivert) Phenidamine (nolahist) *cyproheptidine (periactin) *chlorpheniramine (Chlor-trimenton) * brompheniramine (bromphen) *doxepin *promethazine
First generation antihistamines
Acrivastine (semprex-D) *certirizene (zyrtec) Levocertirizine (xyzal) Azelastine (astelin, astepro) Loratidine (Claritin) Desloratadine (clarinex) Fexofenadine (Allegra)
Second generation antihistamines
Antihistamines
MOA
Actions primarily due to H1 antagonist actions
- active on many histamine effects: vasodilation, capillary permeability, itching and redness
- mixed effects on sexretions
- sedating and CNS stimulating effects
- anticholinergic effects (ANTI-SLUD)
- actions may last longer than drugs t1/2
Cyproheptidine (periactin)
1st generation
Some anti serotonin effects (5-HT)
Treatment for serotonin syndrome
Chlorpheniramine (Chlor-trimenton)
Brompheniramine (bromphen)
1st generation
Less sedating possibly more CNS stimulation
Halogenated
* less sedating of all the 1st generations
Doxepin
1st gen Tricyclic antidepressant Strongest * High potency High anticholinergic effects High sedation
Promethazine
1st gen Phenothiazine typical antipsychotic Anticholinergic effects High sedation *largely used as an antiemetic
Certirizene (zyrtec)
2nd generation
* most sedating of second gen