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ANTIHISTAMINES
DR.FOUZIA
HISTAMINE
1-It is a chemical produced in mast cells.
Histidine  Histamine MAO
2-It mediates cellular responses like:
A- Allergic and inflammatory reactions
B- Gastric acid secretion
C- Neurotransmission in brain.
3-It has no clinical applications
4- Antihistamines have therapeutic applications.
HISTAMINE RECEPTORS
H1:
Pain and itching in the skin, bronchoconstriction, vasodilation
H2:
Gastric acid secretion by parietal cells in stomach, Cardio stimulant,
To ↓ histamine release from mast cells
H3:
Presynaptic modulation of histamine in CNS
H4:
Leukocytes (eosinophil), mast cells Chemotactic responses
CLASSIFICATION OF ANTI-HISTAMINES
H1-Antagonist:
First generation anti-histamines: (More sedation)
Chlorpheniramine
Brompheniramine
Cyclizine
Meclizine
Promethazine
Dimenhydrinate
Diphenhydramine
Carbinoxamine
CLASSIFICATION OF ANTI-HISTAMINES
H1-Antagonist:
Second generation anti-histamines:(Less sedation)
Fexofanadine
Loratidine
Desloratidine
Cetrizine
ANTIHISTAMINES
Mechanism of action:
1-H1 blockers are competitive antagonists of histamine at the H1-R
2-No effect on histamine release from storage sites
First generation
H1-R
Muscarinic-R
α1-R
Serotonin-R
Second generation
H1-R
CLINICAL USES OF ANTIHISTAMINES
1-Allergic and inflammatory conditions:
Allergic rhinitis
Hay fever
Allergic conjunctivitis
Urticaria
2-Anti-motion sickness:
Diphenhydramine, dimenhydrinate, cyclizine, meclizine, promethazine
3-Chemotherapy-induced vomiting
Diphenhydramine
CLINICAL USES OF ANTIHISTAMINES
4-Morning sickness in pregnancy:
Doxylamine
5-Drug-induced parkinsonism:
Diphenhydramine( parentrally)
Acute suppression of extrapyramidal symptoms associated with
antipsychotics
6-As local anesthetics:
Diphenhydramine, Promethazine
ADVERSE EFFECTS OF ANTI-HISTAMINES
First generation
1-Sedation
2-Antimuscarinic effects
Dry mouth and blurred vision, urinary retention, tachycardia
3-Alpha-adrenoceptor blockade
Orthostatic hypotension (Promethazine)
4-Contact dermatitis
Diphenhydramine
5-Excitation and convulsions in children
ADVERSE EFFECTS OF ANTI-HISTAMINES
Second generation:
Headache
Arrhythmias (Terfenadine)
SEROTONIN
It is a local hormone, neurotransmitter
Receptors: 1-7
Clinical uses:
Serotonin agonist
1-BuspironeAnxiolytic
2-SumatriptanMigraine
3-Cisapride Gastro esophageal reflex and motility disorders
4-Tegaserod Irritable bowel syndrome
SEROTONIN
Clinical uses:
Serotonin antagonist
Cyproheptadine
1-Carcinoid tumor
2-Cold induced urticaria
Ondansetron
For nausea and vomiting associated with surgery and chemotherapy

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ANTIHISTAMINES.pptx

  • 2. HISTAMINE 1-It is a chemical produced in mast cells. Histidine  Histamine MAO 2-It mediates cellular responses like: A- Allergic and inflammatory reactions B- Gastric acid secretion C- Neurotransmission in brain. 3-It has no clinical applications 4- Antihistamines have therapeutic applications.
  • 3. HISTAMINE RECEPTORS H1: Pain and itching in the skin, bronchoconstriction, vasodilation H2: Gastric acid secretion by parietal cells in stomach, Cardio stimulant, To ↓ histamine release from mast cells H3: Presynaptic modulation of histamine in CNS H4: Leukocytes (eosinophil), mast cells Chemotactic responses
  • 4. CLASSIFICATION OF ANTI-HISTAMINES H1-Antagonist: First generation anti-histamines: (More sedation) Chlorpheniramine Brompheniramine Cyclizine Meclizine Promethazine Dimenhydrinate Diphenhydramine Carbinoxamine
  • 5. CLASSIFICATION OF ANTI-HISTAMINES H1-Antagonist: Second generation anti-histamines:(Less sedation) Fexofanadine Loratidine Desloratidine Cetrizine
  • 6. ANTIHISTAMINES Mechanism of action: 1-H1 blockers are competitive antagonists of histamine at the H1-R 2-No effect on histamine release from storage sites First generation H1-R Muscarinic-R α1-R Serotonin-R Second generation H1-R
  • 7. CLINICAL USES OF ANTIHISTAMINES 1-Allergic and inflammatory conditions: Allergic rhinitis Hay fever Allergic conjunctivitis Urticaria 2-Anti-motion sickness: Diphenhydramine, dimenhydrinate, cyclizine, meclizine, promethazine 3-Chemotherapy-induced vomiting Diphenhydramine
  • 8. CLINICAL USES OF ANTIHISTAMINES 4-Morning sickness in pregnancy: Doxylamine 5-Drug-induced parkinsonism: Diphenhydramine( parentrally) Acute suppression of extrapyramidal symptoms associated with antipsychotics 6-As local anesthetics: Diphenhydramine, Promethazine
  • 9. ADVERSE EFFECTS OF ANTI-HISTAMINES First generation 1-Sedation 2-Antimuscarinic effects Dry mouth and blurred vision, urinary retention, tachycardia 3-Alpha-adrenoceptor blockade Orthostatic hypotension (Promethazine) 4-Contact dermatitis Diphenhydramine 5-Excitation and convulsions in children
  • 10. ADVERSE EFFECTS OF ANTI-HISTAMINES Second generation: Headache Arrhythmias (Terfenadine)
  • 11. SEROTONIN It is a local hormone, neurotransmitter Receptors: 1-7 Clinical uses: Serotonin agonist 1-BuspironeAnxiolytic 2-SumatriptanMigraine 3-Cisapride Gastro esophageal reflex and motility disorders 4-Tegaserod Irritable bowel syndrome
  • 12. SEROTONIN Clinical uses: Serotonin antagonist Cyproheptadine 1-Carcinoid tumor 2-Cold induced urticaria Ondansetron For nausea and vomiting associated with surgery and chemotherapy

Editor's Notes

  1. First generation more lipid soluble and more effects on autonomic receptors
  2. Second generation: Less lipid soluble, less effects on autonomic receptors
  3. Second generation: Allergic rhinitis, chronic urticaria (DOC)