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Histamine
And
H1-Antihistaminics
Dr. Mushtaq Ahmed
Associate Professor, Pharmacology
PIMS, Medical College, Jalandhar, Punjab
Autacoids
These are diverse substances produced by wide variety of cells,
having intense biological activity, but act locally at the site of
synthesis and release
 Types of autacoids:
• Amine autacoids
- Histamine, 5-HT (Serotonin)
• Peptide autacoids
- Plasma kinins (Bradykinin, Kallidin), Angiotensinogen
• Lipid autacoids
- Prostaglandins, Leucotrienes, PAF
Histamine & antihistaminics
Histamine & antihistaminics
Storage And Release
• Storage
- Mast cells and Basophils
- Non – mast cell histamine
* Stomach (ELC)
* Brain
• Release
- Immunological
- Chemical & mechanical
Histamine & antihistaminics
Drugs and
Chemicals
Drugs and chemicals causing release of Histamine
Morphine
D-tc, Aminoglycosides etc
Inactivation Pathway of Histamine
Histamine Receptors
• H1 :-
Location: Smooth muscle, exocrine glands, vascular endothelium,
brain; coupled to phospholipase C, leading to IP3 and
diacylglycerol (DAG) production
• H2 :-
Location: Parietal cells, heart, vascular smooth muscle, mast
cells, brain; coupled to cAMP production
• H3 :-
Location: Brain, myenteric plexus (no therapeutic applications,
yet)
MOA of Histamine
• Activation of H1 → ↑ phosphoinositol hydrolysis and ↑ in
intracellular calcium → SM contraction, ↑ in vascular
permeability and mucus secretion
• Activation of H2 → ↑ intracellular CAMP → ↑ gastric acid
secretion
• Activation of H3 → ↓ transmitter release from histaminergic
and other neurons
Pharmacological actions of Histamine
• CNS
- No BBB penetration
- On Intracerebrovascular injection:
* ↑ in BP, cardiac stimulation
* Vomiting, ADH release
• Heart
- Insitu heart – No prominent action
- Isolated heart - ↑ in rate & FOC
Pharmacological actions of Histamine Contd.
• Blood Vessels
- Dilation of smaller Bl. Vessels
- S.C. injection- heat, flushing, ↑ in HR & CO
- Rapid IV injection- ↓ BP
- Intradermal Injection: (Triple Response)
* Red Spot – Capillary dilatation
* Wheal – Exudation of fluid from capillaries and venules
* Flare – Arteriolar dilation
• Viceral Smooth Muscles
- Bronchoconstriction
- Abd. Cramps & colic
• Glands
- ↑ in gastric secretion
• Sensory nerve endings
- IV – itching , Pain
• Autonomic ganglia & Adrenal medulla
- Release of Adrenaline → secondary ↑ in BP
Pharmacological actions (contd.)
Effect of IV histamine on blood pressure
Mediated by H1 receptors on endothelium
Mediated by H2 receptors on vascular smooth muscle
Pathophysiological roles
• Gastric Secretion
• Allergic Phenomena
• As transmitter
• Inflammation
• Tissue growth and repair
SUMMARY OF EFFECTS OF HISTAMINE
Uses Of Histamine
 No Therapeutic Use
• Diagnostic Uses:
* Secreting (Acid) capacity of stomach
* Pheocromocytoma
* Bronchial hyper-reactivity in Asthamatics
 H1 Selective Histamine Analogue:
Betahistine (used to control vertigo in Meniere’s disease)
Histamine & antihistaminics
Antagonists of Histamine
 Physiological antagonists :
Adrenaline – effects are opposite to effects of
histamine
 Histamine release Inhibitors →
Mast cell stabilizers : Cromoglycate
 Histamine receptor blockers :
H1 blockers and H2 blockers
Antihistaminics (H1- Antagonists)
• Classification:
• Highly Sedative:
- Diphenhydramine - Dimenhydrinate
- Promethazine - Hydroxyzine
• Moderately sedative:
- Antazoline - Cyproheptadine
- Buclizine - Pheniramine Melate
• Mild Sedative:
- Chlorphenramine - Cyclizine
- Dimethindine - Methidilazine
• Non Sedative:
- Astemizole - Cetrizine, levocetrizine
- Terfenadine - Loratadine
- Cinnarizine - Fexofenadine
- Mizolastine - Rupatadine
• CNS
- Variable degree of CNS depression
• BP
- IV inj. – cause ↓ BP
• Antagonism of Histamine
- Effectively block:
* Bronchoconstriction
* Contraction of sm. Mus.
* Triple response
• Anti-allergic action
- Type- I reactions are suppressed
Pharmacological actions of
H1-Antihistamines
PK & SE
• PK
- A – Well absorbed
- D - Wide distribution
- M- Metabolized in liver
- E - Excreted through urine
D. O. A : 4-6 hrs 2nd Gen: 12-24 hrs
• SE
- 1st Gen;
- Sedation, Light headedness, Diminished alertness &
concentration, motor in-cordination & fatigue
- 2nd Gen;
- Dryness of mouth, Alteration of bowl movements,
Urinary hesitancy
Therapeutic Uses of H1- Antagonists
• Allergic Disorders
• Pruritus
• Common Cold
• Motion sickness
• Vertigo
• Preanesthetic medication
• Cough
• Parkinsonism
• Acute muscle dystonia
• As sedative, hypnotic and anxiolytic
HISTAIME
↓
Anaphylactic Shock
Histamine & antihistaminics
Histamine & antihistaminics
Anaphylaxis
A medical emergency needs immediate
treatment of:
- Hypotension
- Bronchospasm
- Laryngeal Edema
Treatment of Anaphylactic Shock
• Lay the patient flat & raise the legs
• Attend to the airway
• Inj. Adrenaline
- 0.5 ml (1:1000) IM or 3-5 ml (1:10,000) Slow IV = adult
- 0.01 ml (1:1000) IM or 0.1 ml (1:10,000) Slow IV = children
• Inj. Salbutamol
- For Pts on non-selective β- blockers
• IV Fluids
- To correct hypotension
• Inj. Hydrocortisone Hemisuccinate 100mg - IV
• Antihistaminics
- Do not counter hypotension & bronchospasm
• Inj. Aminophylline IV or Nabulized Salbutamol
• Supportive Measures
- Oxygen & assisted ventilation
Why Adrenaline is DOC for Anaphylactic Shock ?

Epinephrine is a physiological antagonist of
histamine, not a pharmacological antagonist
α-1 = Vasoconstriction
ß-1 = Increased HR
ß-2 = Bronchodilatation
Thank You
Histamine

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Histamine & antihistaminics

  • 1. Histamine And H1-Antihistaminics Dr. Mushtaq Ahmed Associate Professor, Pharmacology PIMS, Medical College, Jalandhar, Punjab
  • 2. Autacoids These are diverse substances produced by wide variety of cells, having intense biological activity, but act locally at the site of synthesis and release  Types of autacoids: • Amine autacoids - Histamine, 5-HT (Serotonin) • Peptide autacoids - Plasma kinins (Bradykinin, Kallidin), Angiotensinogen • Lipid autacoids - Prostaglandins, Leucotrienes, PAF
  • 5. Storage And Release • Storage - Mast cells and Basophils - Non – mast cell histamine * Stomach (ELC) * Brain • Release - Immunological - Chemical & mechanical
  • 7. Drugs and Chemicals Drugs and chemicals causing release of Histamine Morphine D-tc, Aminoglycosides etc
  • 9. Histamine Receptors • H1 :- Location: Smooth muscle, exocrine glands, vascular endothelium, brain; coupled to phospholipase C, leading to IP3 and diacylglycerol (DAG) production • H2 :- Location: Parietal cells, heart, vascular smooth muscle, mast cells, brain; coupled to cAMP production • H3 :- Location: Brain, myenteric plexus (no therapeutic applications, yet)
  • 10. MOA of Histamine • Activation of H1 → ↑ phosphoinositol hydrolysis and ↑ in intracellular calcium → SM contraction, ↑ in vascular permeability and mucus secretion • Activation of H2 → ↑ intracellular CAMP → ↑ gastric acid secretion • Activation of H3 → ↓ transmitter release from histaminergic and other neurons
  • 11. Pharmacological actions of Histamine • CNS - No BBB penetration - On Intracerebrovascular injection: * ↑ in BP, cardiac stimulation * Vomiting, ADH release • Heart - Insitu heart – No prominent action - Isolated heart - ↑ in rate & FOC
  • 12. Pharmacological actions of Histamine Contd. • Blood Vessels - Dilation of smaller Bl. Vessels - S.C. injection- heat, flushing, ↑ in HR & CO - Rapid IV injection- ↓ BP - Intradermal Injection: (Triple Response) * Red Spot – Capillary dilatation * Wheal – Exudation of fluid from capillaries and venules * Flare – Arteriolar dilation
  • 13. • Viceral Smooth Muscles - Bronchoconstriction - Abd. Cramps & colic • Glands - ↑ in gastric secretion • Sensory nerve endings - IV – itching , Pain • Autonomic ganglia & Adrenal medulla - Release of Adrenaline → secondary ↑ in BP Pharmacological actions (contd.)
  • 14. Effect of IV histamine on blood pressure Mediated by H1 receptors on endothelium Mediated by H2 receptors on vascular smooth muscle
  • 15. Pathophysiological roles • Gastric Secretion • Allergic Phenomena • As transmitter • Inflammation • Tissue growth and repair
  • 16. SUMMARY OF EFFECTS OF HISTAMINE
  • 17. Uses Of Histamine  No Therapeutic Use • Diagnostic Uses: * Secreting (Acid) capacity of stomach * Pheocromocytoma * Bronchial hyper-reactivity in Asthamatics  H1 Selective Histamine Analogue: Betahistine (used to control vertigo in Meniere’s disease)
  • 19. Antagonists of Histamine  Physiological antagonists : Adrenaline – effects are opposite to effects of histamine  Histamine release Inhibitors → Mast cell stabilizers : Cromoglycate  Histamine receptor blockers : H1 blockers and H2 blockers
  • 20. Antihistaminics (H1- Antagonists) • Classification: • Highly Sedative: - Diphenhydramine - Dimenhydrinate - Promethazine - Hydroxyzine • Moderately sedative: - Antazoline - Cyproheptadine - Buclizine - Pheniramine Melate • Mild Sedative: - Chlorphenramine - Cyclizine - Dimethindine - Methidilazine • Non Sedative: - Astemizole - Cetrizine, levocetrizine - Terfenadine - Loratadine - Cinnarizine - Fexofenadine - Mizolastine - Rupatadine
  • 21. • CNS - Variable degree of CNS depression • BP - IV inj. – cause ↓ BP • Antagonism of Histamine - Effectively block: * Bronchoconstriction * Contraction of sm. Mus. * Triple response • Anti-allergic action - Type- I reactions are suppressed Pharmacological actions of H1-Antihistamines
  • 22. PK & SE • PK - A – Well absorbed - D - Wide distribution - M- Metabolized in liver - E - Excreted through urine D. O. A : 4-6 hrs 2nd Gen: 12-24 hrs • SE - 1st Gen; - Sedation, Light headedness, Diminished alertness & concentration, motor in-cordination & fatigue - 2nd Gen; - Dryness of mouth, Alteration of bowl movements, Urinary hesitancy
  • 23. Therapeutic Uses of H1- Antagonists • Allergic Disorders • Pruritus • Common Cold • Motion sickness • Vertigo • Preanesthetic medication • Cough • Parkinsonism • Acute muscle dystonia • As sedative, hypnotic and anxiolytic
  • 27. Anaphylaxis A medical emergency needs immediate treatment of: - Hypotension - Bronchospasm - Laryngeal Edema
  • 28. Treatment of Anaphylactic Shock • Lay the patient flat & raise the legs • Attend to the airway • Inj. Adrenaline - 0.5 ml (1:1000) IM or 3-5 ml (1:10,000) Slow IV = adult - 0.01 ml (1:1000) IM or 0.1 ml (1:10,000) Slow IV = children • Inj. Salbutamol - For Pts on non-selective β- blockers • IV Fluids - To correct hypotension • Inj. Hydrocortisone Hemisuccinate 100mg - IV • Antihistaminics - Do not counter hypotension & bronchospasm • Inj. Aminophylline IV or Nabulized Salbutamol • Supportive Measures - Oxygen & assisted ventilation
  • 29. Why Adrenaline is DOC for Anaphylactic Shock ?  Epinephrine is a physiological antagonist of histamine, not a pharmacological antagonist α-1 = Vasoconstriction ß-1 = Increased HR ß-2 = Bronchodilatation