Histamine Flashcards
Compounds formed by tissues and act on them are?
Autacoids
What is histamine?
Chemical messenger generated by mast cells
Response of histamine?
- Allergic and inflammatory reactions (act on IgE)
- Gastric acid secretion
- Neurotransmitter.
Synthesis of histamine?
Decarboxylation of histidine by enzyme histidine decarboxylase.
If histamine is not stored in granules, it is inactivated by?
Amine oxidase
Stimuli for histamine release?
Destruction of cell by any trauma
Allergies
Anaphylaxis
MOA of H1 receptors
Smooth muscle contraction
Increasing capillaries permeability
Enhance cytokines release
Pros of 1st generation H1 antihistamine?
More effective and inexpensive
Cons of 1st generation H1 antihistamine?
Cross CNS and causes sedation.
Why are 2nd generation drugs more preferred?
Cannot cross CNS, no sedation
DOC for allergic rhinitis and utricia?
Oral antihistamines
Treatment for allergic conjunctivitis?
Azelastine
Olopatadine
Ketotifen
H1 antihistamine are contraindicated in which condition?
Bronchial asthma
Pts on Monoamine oxidase inhibitors (MAOI) therapy.
Pts undergoing treatment for Alzheimer disease
DOC for acute anaphylactic shock?
Epinephrine
Drugs for motion sickness?
- Diphenhydramine
- Diphenhydrinate (above drug + theophylline)
- Cyclizine
- Meclizine
- Promethazine
- Scopolamine
DOC for vertigo associated with vestibular disorders?
Meclizine
Drugs for insomnia?
- Diphenhydramine
2. Doxylamine
Second generation H1 antihistamine drugs?
- Loratadine
- Fexofrnadine
- Desloratadine
- Cetirizine
H1 antihistamine act on which other receptors?
Cholinergic
Alpha adrenergic
Serotonin
Drug acting on serotonin causing what?
Cyproheptadine causes increase in appetite.
Adverse effects of H1 antihistamine?
- Sedation (fatigue, dizziness, tremors)
- Dryness of nasal passage and mouth (anticholinergic)
- Urinary retention/blurred vision
- Headache
- Contact dermatitis
Overdose of H1 antihistamine cause?
Hallucinations, excitement, ataxia, convulsions, coma.
MOA of H2 antihistamine?
Inhibitors of gastric acid secretion.
H2 antihistamine are used for?
Treatment of ulcers and heartburn
H2 antihistamine drugs?
Cimetidine
Ranitidine
Famotidine
Nizatidine