Histamines Antagonist

HISTAMINE
ANTAGONISTS
Dr. NDAYISABA CORNEILLE

CEO of CHG
MBChB,DCM,BCSIT,CCNA
Supported BY
Histamine
 Is a protein substance manufactured & found in
human tissues
 Its also a component of some venoms & secretions
of stinging insects
Storage of histamine
 In tissue mast cells (mainly)
 In basophils
 Enterochromaffin-like (ECL) cells of fundus of the
stomach
 Within tissues mast cells are found at sites likely to
be damaged like;
 Nose & respiratory mucosa
 Mouth
 Feet
 Internal body surfaces
 Blood vessels
NB; No mast cells are found in brain

Histamine release from mast cells;
 Its released in response to;
1.Direct chemical /physical trauma to tissue mast

cells
2. Drugs like morphine which displace histamine
from their storage sites
3. Immunologic reactions esp the type 1allergic
reactions coz degranulation of mast cells
Mechanism of action of histamine
 Actions of histamine are mediated via histamines
receptors found on cell membranes of different
tissues
Types of histamine receptors;
1. H1 receptors
2. H₂ receptors
3. H₃ receptors
4. H₄ receptors
Location of the various histamine receptors
1. H1 receptors
 Smooth muscle cells
 Endothelium
 Brain
2. H₂ receptors
 Gastric mucosa cells
 Cardiac muscle
 Mast cells
 Brain
3. H₃ receptors
 Presynaptic: brain, myenteric plexus, other neurons
4. H₄ receptors
 Eosinophils
 Neutrophils
 CD4 T cells
Physiological effects of histamine
1. Acts as a neurotransmitter in brain with resultant;
 Neuroendocrine control
 Cardiovascular regulation
 Thermal & body weight regulation
 Control of arousal
2. It promotes HCl production after it binds to
H-2 receptors on parietal cells of the gastric
mucosa
3. It mediates inflammation by binding to H-1

receptors on blood vessels, nerve cells,
leading to sneezing, vasodilatation,
swelling ,pruritus, nasal discharge etc
Histamine antagonists
Definition
 Are drugs that inhibit the actions of histamine
by blocking histamine receptors
Types /classification of histamine antagonists
1. H1-receptor antagonists
2. H2 receptor antagonists
3. H3- & H4-receptor antagonists

1. H1-receptor antagonists
 Are drugs commonly referred to antihistamines

 Thus a term antihistamines refers only to H1
receptor antagonists
 Are drugs which block H1-receptors located on

vessel smooth muscle cells, brain ,heart etc
 Clinically
 H1 antagonists are used mainly to treat

allergic reactions
Mechanism of action
Bind & block H-1 receptors thus relieving Sxs of
inflammation like swelling, nasal discharge
pruritus, sneezing etc
Drugs bind to & block H1 receptors found on ;
a. Smooth muscle cells of blood vessels
b. Brain
c. Nerves
d. Glandular cells
e. Endothelium & mast cells

 This inhibits histamine-induced wheal
(swelling) & vasodilation (flare)
response
 Itching & sneezing are suppressed by
antihistamine blockage of H1-receptors
on nasal sensory nerves
Pharmacokinetic aspects H1-receptor antagonists
 Most anti-histamines;
 Are given orally & are well absorbed from gut
 Reach their peak effect in 1-2 hours
 Are effective for 3-6 hours
 Are widely distributed thru out the body
 Some do not penetrate BBB e.g non-sedative anti-
histamines
 Are metabolised in liver & excreted in urine
Types of H-1 anti-histamines
Sedating H1 antihistamines And Non sedating antihistamines
1. Sedating H1 antihistamines
 Are also known as;
 1st generation antihistamines
 Older antihistamines
 They coz sedation
 This sedating activity is some times used to manage pruritus
associated with some allergies
Examples
 Promethazine (phenergan)
 Chlorphenamine (piriton)
 Cyclizine
 Alimemazine
NB; Little evidence occurs some sedating

antihistamines are superior to the other
Clinical indications of Chlorphenamine (piriton)
1.Symptomatic relief of allergies like;
 Hay fever/allergic rhinitis
 Rashes due to drug hypersensitivity
 Urticaria
2.Used in combination with adrenaline in emergency
tx of anaphylactic reactions
3. Symptomatic relief of pruritus due to chicken pox

Contraindications & cautions of PIRITON
 This drugs are contraindicated or used with caution in;
1. Pregnancy
2. Breast feeding
3. Pylorodeudenal obstruction
4. Benign prostatic hypertrophy
5. Urine retention
6. Angle closure glaucoma
7. Pts with epilepsy

Indications of Promethazine (phenergan)
1. Symptomatic relief of allergies like;
 Hay fever
 Urticaria
2. Emergency tx of anaphylactic shock
3. Treatment of nausea & vomiting (anti-emetic)

4. Induction of sedation
Contraindications & cautions of prometazine
 These drugs are contraindicated or used with
caution in ;
1. Children < 2 years
2. Severe coronary artery disease
3. Pregnancy
4. Breast feeding
7. Urine retention

2. Non sedating antihistamines
 These are also known as;
 2nd generation antihistamines
 Newer anti-histamine
 They coz less; sedation & psychomotor impairment
bcoz they poorly penetrate the BBB
 Examples
 Cetrizine
 Levocetrizine
 Loratadine
 Desloratadine
 Fexofenadine
 Mizolastine
 Etc
Clinical indications of Cetrizine
1. Symptomatic relief of allergies like

 Hay fever
 Chronic idiopathic urticaria
 Angioedema
 Atopic dermatitis in which drug reduces
awareness of itching
2. In UTRI due to rhinovirus infection to reduce

inflammation
Clinical indications of H-1 antihistamines
1. Treatment & prevention of allergic conditions like;

 Seasonal allergic rhinitis (hay fever)
 Pruritus
 Drug hypersensitivity reactions
 Insect & bee stings
 Urticaria rashes
2.Emergency Tx of angioedema & anaphylactic shock in
combination with adrenaline
3. Treatment of occasional insomnia
Common unwanted effects of older anti-histamines
1. Drowsiness –very common

2. Headaches
3. Psychomotor impairment
4. Anti-muscarinic (blockage of Parasympathetic NS) S/Es like

 Urine retention
 Dry mouth
 Constipation
 Blurring of vision
 Palpitations
Other rare S/Es of all anti-histamines
1. CNS
 Extra pyramidal S/Es
 Dizziness
 Confusion
 Restlessness
 Depression
 Tremors
 Seizures
2. CVS
 Palpitations
 Cardiac arrhythmias
 Hypotension
3.GIT
 Liver disorders
4. Hypersensitivity reactions like
 Bronchospasms
 Angioedema
 Anaphylactic shock
 Rash
 Photosensitivity reactions
NB; What is defined as 'unwanted' will depend to a

certain extent on what the drugs are used for
Contraindications & cautions
 These drugs are contraindicated or used with caution
in pts with conditions like;
2. Urine retention

6. Liver disease
7. Acute porphyria
8.Pregnancy
9.Breast feeding
10.Renal failure
Dr Ndayisaba Corneille
2. H2 receptor antagonists;
 Drugs that bind to & block histamine-2 receptors
located on parietal cells of gastric mucosa
Mechanism of action
 Blockage of histamine-2 receptors located on
parietal cells of stomach mucosa leading to ↓ HCl
production
Indications
 Tx of acid reflux disease (heart burn)
 Tx of gastric ulcers
Examples
 Cimetidine ,Ranitidine
 Nizatidine, Famotidine
 Lafutidine
 Roxatidine
3. H3 & H4-receptor antagonists
 Drugs that block H3- & H4-receptors
 These are still experimental drugs

 These do not yet have a defined clinical use
END
BY
DR NDAYISABA CORNEILLE
MBChB,DCM,BCSIT,CCNA,Cyber Security
contact: [email protected] ,
[email protected]
whatsaps :+256772497591 /+250788958241
THANKS FOR LISTENING

Dr Ndayisaba Corneille

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HISTAMINE

Dr. NDAYISABA CORNEILLE

NB; No mast cells are found in brain

1.Direct chemical /physical trauma to tissue mast

Types of histamine receptors;

3. It mediates inflammation by binding to H-1

3. H3- & H4-receptor antagonists

 Are drugs commonly referred to antihistamines

 Are drugs which block H1-receptors located on

 H1 antagonists are used mainly to treat

a. Smooth muscle cells of blood vessels

e. Endothelium & mast cells

NB; Little evidence occurs some sedating

3. Symptomatic relief of pruritus due to chicken pox

7. Pts with epilepsy

3. Treatment of nausea & vomiting (anti-emetic)

8. Angle closure glaucoma

1. Symptomatic relief of allergies like

2. In UTRI due to rhinovirus infection to reduce

1. Treatment & prevention of allergic conditions like;

1. Drowsiness –very common

4. Anti-muscarinic (blockage of Parasympathetic NS) S/Es like

NB; What is defined as 'unwanted' will depend to a

3. Angle closure glaucoma

 Drugs that bind to & block histamine-2 receptors

located on parietal cells of gastric mucosa

 Blockage of histamine-2 receptors located on

parietal cells of stomach mucosa leading to ↓ HCl

 These are still experimental drugs

whatsaps :+256772497591 /+250788958241

THANKS FOR LISTENING

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