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Medichem Unit-1 Remaining Notes

This document discusses histamine receptors and antihistamines. It describes the four types of histamine receptors (H1, H2, H3, H4), their distribution in the body, and actions. First and second generation antihistamines are classified based on their development and side effect profiles. First generation antihistamines are more likely to cause drowsiness while second generation have fewer side effects. The document also briefly discusses H2 receptor antagonists, antineoplastic agents, and the mechanisms of action of mechlorethamine and methotrexate.

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19 views

Medichem Unit-1 Remaining Notes

This document discusses histamine receptors and antihistamines. It describes the four types of histamine receptors (H1, H2, H3, H4), their distribution in the body, and actions. First and second generation antihistamines are classified based on their development and side effect profiles. First generation antihistamines are more likely to cause drowsiness while second generation have fewer side effects. The document also briefly discusses H2 receptor antagonists, antineoplastic agents, and the mechanisms of action of mechlorethamine and methotrexate.

Uploaded by

arunpandey651
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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HISTAMINE RECEPTORS:

Since histamine is a chemical mediater which is produced locally, act locally and
metabolized locally. So, histamine is also called as autocoid or local harmone. This histamine
is synthesized in secretory granules of mast cells present in our body. When this histamine is
released from mast cell as a immune response of allergic reaction, tissue injury, drugs and
foreign substance, it binds with its respective receptor to produce the effect as a immune
response. Histamine receptors belong to family of G- Protein Coupled Receptors. These
histamine receptors are of four types as given below-

(i) H1 - Receptor
(ii) H2 - Receptor
(iii) H3 – Receptor
(iv) H4 – Receptor

Out of the above all four histamine receptors H1, H2 and H3 recptors are well specified and
explained in literatures while H4 recptor is not much explored yet. H4 receptor is somewhat
related to immune system. We can sumurise all these four histamine receptors in following
table based on their type/ mode of action, distribution , action and effect.

S.No. Name of H- Type/mode of Distribution Action and Effect


Receptor action
1. H1 - Receptor GPCR(IP3/DAG -Blood vessels -Vasodialation
Pathway) endothelium
-Smooth muscle(lung) -Bronchoconstriction
-Sensory nerve ending -Pain and itching
-Brain
-Wakefullness and loss
of appetite
2. H2 - Receptor GPCR(CAMP -Parietal cell of gastric -Increased acid
Pathway) mucosa secretion
-SA node of heart -Impulse generation,
increased force of
contraction, increased
heart rate
3. H3 - Receptor GPCR (CAMP -CNS -As an Autoreceptor
Pathway) -Presynaptic cleft ,Suppression of
- Nasal submucosal norepinephrine release
gland at nerve endings
-Airways -Stimulate gastric
- GI Tract nasal gland secretion.

4. H4 - Receptor GPCR (CAMP Basophil, Eosinophils, -Immune response


Pathway) Neutrophils, Bone -Chemotaxis of Mast
Marrow cell and eosiophils
-Resgulation of WBC
Production
Antihistaminic Agents:
Antihistamines are a class of drugs that are used to treat a variety of allergic and
inflammatory conditions. They work by blocking the effects of histamine, a chemical
released by the body in response to allergens and other triggers. Antihistamines can be
classified in several ways based on their generation, mechanism of action, and other
characteristics. Here's a basic classification of antihistaminic agents:
Antihistamines can be categorized into two generations based on their development and
characteristics.
a. First-generation antihistamines:
These are the older antihistamines.
Examples include diphenhydramine, chlorpheniramine, and promethazine.
They are more likely to cause drowsiness and have a sedative effect.
Their use is often associated with side effects such as dry mouth and blurred vision.
b. Second-generation antihistamines:
These are newer antihistamines.
Examples include loratadine, cetirizine, and fexofenadine.
They are less likely to cause drowsiness and sedation.
Second-generation antihistamines are preferred for allergic conditions due to their improved
side effect profile.

About first generation antihistamines:

i) Amino alkyl ether derivative(Diphenhydramine):

Uses:
Diphenhydramine is a first-generation antihistamine used to treat a number of
conditions including allergic symptoms and itchiness, the common
cold, insomnia, motion sickness, and extrapyramidal symptoms.
ii) Ethylene diamine derivative ( Tripelenamine)

Uses: Tripelennamine is a histamine H1 antagonist used to treat


hypersensitivity reactions, coughs, and the common cold. A histamine H1
antagonist with low sedative action but frequent gastrointestinal irritation. It is
used to treat asthma; HAY fever; urticaria; and rhinitis; and also in veterinary
applications.
iii) Cyclic basic chain derivative (Chlorcyclizine)

Uses: Chlorcyclizine is a first generation phenylpiperazine class antihistamine


used to treat urticaria, rhinitis, pruritus, and other allergy symptoms.
iv) Propylamine derivative(Pheniramine,Triprolidine)

Pheniramine
Uses: Pheniramine is an antihistamine used to treat allergic rhinitis and
pruritus.
v) Phenothiazine derivative (Promethazine)

Uses:
Promethazine is a medication used to manage and treat allergic conditions,
nausea and vomiting, motion sickness, and sedation.
vi) Dibenzocycloheptadine (Azatidine)

Uses:
It has a role as a H1-receptor antagonist and an anti-allergic agent.
vii) Miscellaneous:

Fexofenadine
Uses:
Fexofenadine is a piperidine-based anti-histamine compound. It has a role as
a H1-receptor antagonist and an anti-allergic agent.

Antazoline
Uses:

It is used to relieve nasal congestion. It is also formulated as eye drops with naphazoline to
relieve allergic conjunctivitis.

H2- Antagonists:
H2- antagonists also known as H2 blockers or H2- receptor antagonists. Two well known H2-
antaginists are cimetidine and ranitidine.

1. Cimetidine:
Structure:

Use:
 In the treatment of GERD( Gastroesophageal Reflux Disease)
 Used to treat peptic ulcers, gastric and duodenal ulcers.
 Zollinger-Ellison syndrome.
2. Ranitidine:
Structure:

Uses:
 In the treatment of GERD( Gastroesophageal Reflux Disease)
 Used to treat peptic ulcers, gastric and duodenal ulcers.

Antineoplastic Agents
Antineoplastic agents, also known as anticancer agents or chemotherapeutic agents, are a
class of medications and therapies used to treat cancer. These agents work to inhibit or kill
cancer cells, slow down their growth, or prevent their spread to other parts of the body. They
are an essential component of cancer treatment and can be administered in various ways,
including orally, intravenously, or topically, depending on the specific drug and the type of
cancer being treated.

Classification of Antineoplastic agents:


Synthesis of Mechlorethamine:

Mechanism of action of Mechlorethamine:


Mechanism of Action of Methotrexate:

Methotrexate is a type of antimetabolite, specifically an antimetabolite of folic acid. Its main


mechanism of action involves interfering with the metabolism of folic acid, which is essential
for the synthesis of DNA, RNA, and proteins. Methotrexate inhibits dihydrofolate reductase,
an enzyme involved in the conversion of dihydrofolic acid to tetrahydrofolic acid, which is
needed for DNA and RNA synthesis. By blocking this enzyme, Methotrexate disrupts the
synthesis of these important cellular components, ultimately inhibiting the growth and
division of cells.

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