ChemiCals in mediCines

introduCtion:

The words ‘medicine’ and 'drug' are often used in our country to mean the same
substances: any substance, manufactured artificially, which can help recovery from sickness,
relieve symptoms or modify a natural process in the body. A medicine is often a mixture of
several chemical compounds. Even if it has only one active component compound often
other substances are used as fillers or binders to give it bulk. Chemistry, the science related to
chemical substances, provides us the tools to make and study the substances that are the
constituents of almost all medicines. The past hundred years or so, ever since the advent of
organic chemistry, many chemical compounds have been discovered in nature that are
effective for curing diseases. Modern chemistry has also made it possible to synthesize
several medicines using methods of organic chemistry.

The most common medicines can be classified into few groups, e.g. antibiotics, antiseptics,
analgesics, tranquillizers, antipyretics, hormonal, steroids etc.
There are very many medicines that come under each of these groups. Often several
chemical compounds that make a particular group of medicines, say antibiotics have similar
chemical structure. Since the medicines in a particular group are effective for treating a
particular type of ailment or disease, their mode of action can also be very similar. But, the
methods used to isolate a medicine from its natural sources or to synthesize it are most often
very different.The development of pharmaceuticals has been a groundbreaking endeavor
throughout human history, transforming the landscape of healthcare and significantly
extending life expectancy. At the heart of this revolution lie chemicals – the active ingredients
within medicines that interact with the body to treat, manage, or prevent various medical
conditions. This introduction delves into the fundamental role of chemicals in medicines,
exploring the intricate relationship between chemistry and healthcare.

**1. ** Historical Perspective: The use of chemicals in medicines dates back centuries, with
ancient civilizations employing natural substances like plants and minerals for therapeutic
purposes. Over time, the understanding of these substances evolved, paving the way for the
systematic synthesis and design of chemicals tailored to target specific diseases.

**2. ** Chemical Basis of Pharmaceuticals: Medicines are essentially chemical compounds

designed to interact with biological systems in a way that produces a therapeutic effect.
These compounds, known as active pharmaceutical ingredients (APIs), are carefully selected
and synthesized to exhibit the desired pharmacological activity.

**3. ** Drug Discovery and Development: The process of bringing a new medicine to market
involves an intricate journey of drug discovery and development. Chemists play a pivotal role
in this process, identifying potential drug candidates, optimizing their chemical structures for
efficacy and safety, and ensuring their compatibility with the human body.

**4. ** Modes of Action: Chemicals in medicines exert their effects through diverse
mechanisms. This can range from targeting specific proteins or enzymes involved in disease
processes to modulating cellular pathways. Understanding the molecular interactions is crucial
for both drug design and predicting potential side effects.

**5. ** Therapeutic Classes and Applications: Pharmaceuticals encompass a wide array of

therapeutic classes, addressing an extensive range of medical conditions. From antibiotics
combating infections to analgesics alleviating pain, each class of drugs relies on specific
chemical properties to achieve therapeutic goals.

**6. ** Challenges and Innovations: The field of medicinal chemistry faces ongoing challenges,
including the need for increased efficacy, reduced side effects, and novel approaches to
drug delivery. Recent innovations, such as nanotechnology and computational drug design,
showcase the evolving landscape of chemical interventions in healthcare.

**7. ** Ethical Considerations: The use of chemicals in medicines also raises ethical
considerations, from the responsible handling of pharmaceutical waste to addressing issues of
access and affordability. Striking a balance between innovation, safety, and ethical
considerations is a critical aspect of advancing healthcare through chemistry.
ANTIBIOTICS

Introduction:

Antibiotics are a class of potent medications crucial in the battle against bacterial infections.
Since the discovery of the first antibiotic, penicillin, by Alexander Fleming in 1928, these drugs
have revolutionized medicine, saving countless lives and mitigating the impact of bacterial
diseases. This theoretical overview aims to provide a concise understanding of antibiotics,
their mechanisms of action, classifications, and the challenges associated with their use.

1. Mechanisms of Action:

Antibiotics act through various mechanisms to inhibit bacterial growth or eliminate bacteria
entirely. Broadly, these mechanisms can be categorized into:

• Inhibition of Cell Wall Synthesis: Many antibiotics, such as penicillins and

cephalosporins, disrupt the synthesis of bacterial cell walls, leading to cell lysis.
• Inhibition of Protein Synthesis: Antibiotics like tetracyclines and macrolides interfere
with bacterial protein synthesis by targeting ribosomes, preventing the formation of
essential proteins.
• Disruption of Nucleic Acid Synthesis: Quinolones and rifamycins interfere with DNA or
RNA synthesis, impeding bacterial replication.
• Inhibition of Metabolic Pathways: Sulphonamides and trimethoprim inhibit specific
enzymes involved in bacterial metabolic pathways, disrupting essential cellular
functions.

2. Antibiotic Classes:

Antibiotics are classified based on their chemical structure, mechanism of action, and
spectrum of activity:

• Penicillins and Cephalosporins: These antibiotics target bacterial cell walls and are
effective against a broad range of gram-positive bacteria.
• Tetracyclines and Macrolides: These antibiotics interfere with protein synthesis, and
their spectrum includes both gram-positive and gram-negative bacteria.
• Quinolones and Rifamycins: These antibiotics disrupt nucleic acid synthesis and are
particularly effective against gram-negative bacteria.
• Aminoglycosides: Known for their efficacy against aerobic gram-negative bacteria,
these antibiotics inhibit protein synthesis.

3. Challenges and Concerns:

Despite their significant contributions to medicine, antibiotics face challenges that threaten
their efficacy and sustainability:

• Antibiotic Resistance: Prolonged or inappropriate antibiotic use has led to the

emergence of antibiotic-resistant strains of bacteria, posing a global threat to public
health.
 • Side Effects: Antibiotics may have adverse effects on the host, ranging from mild
gastrointestinal disturbances to severe allergic reactions.
• Overuse and Misuse: Inappropriate prescribing and overuse of antibiotics contribute
to resistance and jeopardize the long-term effectiveness of these drugs.

4. Future Directions and Innovations:

Addressing the challenges associated with antibiotics involves ongoing research and
innovation:

• Development of New Antibiotics: The discovery and development of novel antibiotics

with different mechanisms of action are crucial to combat emerging resistant strains.
• Antibiotic Stewardship: Implementing antibiotic stewardship programs to optimize the
use of antibiotics, reduce unnecessary prescriptions, and minimize the development of
resistance.

Our body and our domestic animals, can serve as hosts to a wide variety of diseasecausing
organisms (pathogens): These are:
• bacteria
• viruses
• fungi
• protozoon’s

An antibiotic (Greek anti, "against"; bios, "life"), is a chemical substance produced by one
organism that is destructive to another. This process traditionally has been called antibiosis and
is the opposite of symbiosis. More specifically, an antibiotic is a type of chemotherapeutic
agent that has a toxic effect on certain types of disease-producing microorganisms without
acting dangerously on the patient. The definition most used for antibiotics is: any substance
produced by a microorganism which harms or kills another microorganism. However,
antibiotics DO NOT harm viruses. Doctors often prescribe antibiotics when you may have a
viral infection because of the possibility that you may also acquire a bacterial infection
because you are so ill with a virus - being ill places a person at risk for certain bacterial
infections that are normally handled without any problem.

The overwhelming majority of antibiotic substances are natural products that certain
bacteria and fungi (molds) produce and send outside of their cells. About 90% of the
antibiotics in use today, are isolated from bacteria. There are a few antibiotics, however,
which are completely synthetic... that is, are made from scratch in the laboratory. These
particular antibiotics are designed to inhibit some process previously identified to be
completely unique to bacteria, and necessary for the bacterium to remain alive. An
antibiotic can be most often classified into any one of the following categories of chemical
compound:

1. Amino glycosides
2. Glycopeptides

3. Beta Lactams also known as Penicillin’s

 4. Tetracycline

5. Quinolines

6. Sulfonamides

Amino glycosides

Amino glycosides are antibiotics that are often administered into veins or muscle to treat
serious bacterial infections. Some amino glycosides are also used orally to treat intestinal
infections or topically to treat eye infections. Some very popular examples of this group of
antibiotics are

• Streptomycin
• Kanamycin Neomycin
• Gentamycin

They are the inhibitors of protein synthesis, ↓ 30S ribosomal subunit, but some abnormal
proteins insert in cell membrane & form pores, thus become bactericidal The chemical
structure of this group of antibiotics is:

Glycopeptides

Glycopeptide antibiotics are a class of antibiotic drugs. They consist of a

glycosylated cyclic or polycyclic nonribosomal peptide. Important
glycopeptide antibiotics include vancomycin, teicoplanin, ramoplanin,
and decaplanin.

This class of drugs inhibits the synthesis of cell walls in susceptible microbes
by inhibiting peptidoglycan synthesis. Bacterial cell wall contains
peptidoglycan strands
• Peptidoglycan is composed of UDP-N-acetyl-muramic acid, UDP-N-
acetylglucosamine & a pentapeptide
• Cycloserine, resembles to alanine & inhibits addition of alanine into
peptide chain

• Vancomycin inhibits transglycosidase enzyme & prevents

peptidoglycan chain elongation

Due to their toxicity, their use is restricted to those patients who are
critically ill or who have a demonstrated hypersensitivity to the β-lactams.
The chemical structure of a glycopeptide antibiotic is
Penicillin

Penicillin is one major class of antibiotics. They are used to treat strep throat and countless
other infections. Examples of various kinds of penicillin include Amoxicillin, Ampicillin,
Carbenicillin, Cloxacillin, Dicloxacillin, Flucloxacillin..

They are the inhibitors of cross linking of peptidoglycan strands:

• Inhibit transpeptidase enzyme, involved in cross linking of peptidoglycan strands

• Also called as transpeptidation reaction & strengthens cell wall.
• Defects in the synthesis of cell wall cause wholes in cell wall & changes in permeability
• Leading to bacterial swelling & lysis
• Hence cell wall synthesis inhibitors are bactericidal

Common structural features of Beta-Lactams;

Tetracycline

Tetracyclines are another category of antibiotics. In addition to being used to treat infections,
they are often used to manage acne. A few of the tetracyclines frequently used are:
Achromycin V (Tetracycline)
Minocin (Minocycline)
Vibramycin (Doxycycline)

They are the inhibitors of protein synthesis, ↓ 30S ribosomal subunit & are bacteriostatic

The chemical structure of most tetracycline is related to the following structure. The name is
derived from the fact that it is made up of four rings (cycles).

Quinolones

The quinolones are a family of broad-spectrum antibiotics. The parent of the group is nalidixic
acid. The majority of quinolones in clinical use belong to the subset of fluoroquinolones, which
have a fluoro group attached the central ring system. Quinolones and fluoroquinolones are
bactericidal drugs, actively killing bacteria. Quinolones inhibit the bacterial DNA gyrase or the
topoisomerase II enzyme, thereby inhibiting DNA replication and transcription.

They are the inhibitors of DNA replication & mitosis, inhibit bacterial topisomerase-II [ in gram
(-) bacteria] & topoisomerase IV [in gram (+) bacteria], inhibit DNA replication & are
bactericidal

The common chemical structure is as follows

Sulfonamides

Sulfonamide drugs (known widely as "sulfa drugs") were the first antibacterial antibiotics, and
paved the way for the antibiotic revolution in medicine. The first sulfonamide was trade named
Prontosil, which is a prodrug. Experiments with Prontosil began in 1932 in the laboratories of the
Bayer Corporation, a component of the huge German chemical trust IG Farben. The dye-
based drug was synthesized by Bayer chemist
Josef Klarer and tested in animals under the direction of physician/researcher Gerhard
Domagk. Domagk quickly won the 1939 Nobel Prize in Medicine and Physiology, an honor that
Hitler forbade him to accept.

They are the inhibitors of DNA & cell division, can affect microbial DNA & cell division in
following ways:

• Inhibit DNA synthesis

a) Inhibitors of folate synthesis- Sulfonamides & sulfones inhibit dihydro- pteroate
synthase (DHPS) enzyme

Trimethoprim inhibits dihydro-folate reductase (DHFR) enzyme (bacterial

DHFR more than human)

b) Inhibitors of thymidylate synthesis- Flucytosine: is a cytosine analogue & inhibits

thymidylate synthase (TS)

• Converted in fungi & GI flora to 5-fluorouracil (5-FU)

• 5-FU converted to 5-FdUMP

• 5-FdUMP incorporated to DNA

Some examples of sulfonamide antibiotics are:

Mafenide, Sulfacetamide, Sulfamethizole, Sulfanilimide, Trimethoprim etc.

How Antibiotics act.

Antibiotics attack a metabolic pathway found in the bacterium but not in the host. This is not
an insurmountable problem for bacterial pathogens because they differ in many respects
from eukaryotes.

Thus pencillins (beta-lactams) work by interfering with the synthesis of the bacterial cell walls
— a structure that is not found in eukaryotes. The walls of bacteria are made of a complex
polymeric material called peptidoglycan. It contains both amino acids and amino sugars.
The amino sugars are of two kinds N-acetylglucosamine (NAG) and its close relative N-
acetylmuramic acid (NAM).

These two form a linear polymer of NAG alternating with NAM. They are linked by a glycosidic
bond between the #1 and #4 carbons (this is the linkage attacked by lysozyme) and are
oriented in the same way they are in cellulose. Side chains containing 4 or 5 amino acids are
attached to each NAM. These form covalent bonds with amino acids in adjacent chains. The
bonds may
• be direct to the next chain or
• include additional peptide cross bridges (e.g., 5 glycine residues) which
• extend to chains in the same plane (shown here) as well as to chains above and below.
This elaborate, covalently cross-linked structure provides the great strength of the cell wall. It
also leads to the remarkable conclusion that the bacterial cell wall meets the definition of a
single molecule!

The beta-lactam antibiotics bind to and inhibit enzymes needed for the synthesis of the
peptidoglycan wall. While they have little effect on resting bacteria, they are lethal to dividing
bacteria as defective walls cannot protect the organism form bursting in hypotonic
surroundings.

The aminoglycosides bind to the 30S subunit of the bacterial ribosome, because the bacterial
ribosome differs in several ways from the eukaryotic ribosome and thus interferes with the
formation of the initiation complex , causing misreading of the mRNA.

Tetracyclines also bind to the 30S subunit of the bacterial ribosome. They prevent the transfer
of activated amino acids to the ribosome so protein synthesis is halted.

The fluoroquinolones block the action of two bacterial topoisomerases — enzymes that relieve
the coils that form in DNA when the helix is being opened in preparation for replication or
transcription or repair.

block the synthesis of folic acid. Mammals ignore PABA and its analogs and thus can tolerate
sulfa drugs.
The mode of action of Sulfonamides is a bit different. Both bacteria and their human hosts
require folic acid for nucleic acid synthesis (it is converted into prunes and thymidine) as well
as protein synthesis (precursor of the amino acids methionine and glycine). However, bacteria
synthesize their folic acid starting with para-aminobenzoic acid (PABA), while we must ingest
our folic acid already formed; that is, for us it is a vitamin.

Production of antibiotics

Since the first pioneering efforts of Florey and Chain in 1939, the importance of antibiotics to
medicine has led to much research into discovering and producing them. The process of
production usually involves screening of wide ranges of microorganisms, testing and
modification. Production is carried out using fermentation; a process that is important in
anaerobic conditions when there is no oxidative phosphorylation to maintain the production
of ATP by glycolysis.
ANTISEPTICS

Antiseptics are antimicrobial substances that are applied to living tissue/skin to reduce the
possibility of infection, sepsis, or putrefaction. They should generally be distinguished from
antibiotics that destroy microorganisms within the body, and from

disinfectants, which destroy microorganisms found on non-living objects.

Some antiseptics are true germicides, capable of destroying microbes
(bactericidal), whilst others are bacteriostatic and only prevent or inhibit
their growth. Antibacterial are antiseptics that only act against bacteria.

Some chemical compounds/groups of chemical substances that are often

used as antiseptics are:

Alcohols
Most commonly used is ethanol (60-90%), 1-propanol (60-70%) and
2propanol/isopropanol (70-80%) or mixtures of these alcohols. They
are commonly referred to as "surgical alcohol". Used to disinfect the
skin before injections are given, often along with iodine (tincture of
iodine) or some cationic surfactants (benzalkonium chloride 0.05 -
0.5%, chlorhexidine 0.2 - 4.0% or octenidine dihydrochloride 0.1 -
2.0%).
Quaternary ammonium compounds
They include the chemicals benzalkonium chloride (BAC), cetyl
trimethylammonium bromide (CTMB), cetylpyridinium chloride ,
cetylpyridinium chloride (CPC) and benzethonium chloride (BZT).
Benzalkonium chloride is used in some pre-operative skin
disinfectants (conc. 0.05 - 0.5%) and antiseptic towels. The
antimicrobial activity of Quats is inactivated by anionic surfactants,
such as soaps. Related disinfectants include chlorhexidine and
octenidine.
Boric acid
Used in suppositories to treat yeast infections of the vagina, in
eyewashes, and as an antiviral to shorten the duration of cold sore
attacks. Put into creams for burns. Also common in trace amounts in
eye contact solution. Though it is popularly known as an antiseptic, it
is in reality only a soothing fluid, and bacteria will flourish comfortably
in contact with it.
Chlorhexidine Gluconate
A biguanidine derivative, used in concentrations of 0.5 - 4.0% alone
or in lower concentrations in combination with other compounds,
such as alcohols. Used as a skin antiseptic and to treat inflammation
of the gums (gingivitis). The microbicidal action is somewhat slow.

Hydrogen peroxide
Used as a 6% (20Vols) solution to clean and deodorise wounds and
ulcers. More common 1% or 2% solutions of hydrogen peroxide have
been used in household
first aid for scrapes, etc. However, even this less potent form is no
longer recommended for typical wound care as the strong
oxidization causes scar formation and increases healing time. Gentle
washing with mild soap and water or rinsing a scrape with sterile
saline is a better practice.
Iodine
Usually used in an alcoholic solution (called tincture of iodine) or as
Lugol's iodine solution as a pre- and post-operative antiseptic. No
longer recommended to disinfect minor wounds because it induces
scar tissue formation and increases healing time. Gentle washing
with mild soap and water or rinsing a scrape with
sterile saline is a better practice. Novel iodine antiseptics containing
iodopovidone/PVP-I (an iodophor, complex of povidone, a water-
soluble polymer, with triiodide anions I3-, containing about 10% of
active iodine, with the commercial name Betadine) are far better
tolerated, don't affect wound healing negatively and leave a depot
of active iodine, creating the so-called "remanent," or persistent,
effect. The great advantage of iodine antiseptics is the widest scope
of antimicrobial activity, killing all principle pathogens and given
enough time even spores, which are considered to be the most
difficult form of microorganisms to be inactivated by disinfectants
and antiseptics.
Mercurochrome
Not recognized as safe and effective by the U.S. Food and Drug
Administration
(FDA) due to concerns about its mercury content. Another obsolete
organomercury antiseptics include bis-(fenylmercury)
monohydrogenborate .
Phenol (carbolic acid) compounds
Phenol is germicidal in strong solution, inhibitory in weaker ones. Used
as a "scrub" for pre-operative hand cleansing. Used in the form of a
powder as an antiseptic baby powder, where it is dusted onto the
belly button as it heals. Also used in mouthwashes and throat
lozenges, where it has a methadone-like painkilling effect as well as
an antiseptic one. Example: TCP. Other phenolic antiseptics include
historically important, but today rarely used (sometimes in dental
 surgery) thymol, today obsolete hexachlorophene, still used triclosan
and sodium 3,5-dibromo-4-hydroxybenzenesulfonate (Dibromol).

Sodium chloride
Used as a general cleanser. Also used as an antiseptic mouthwash.
Only a weak antiseptic effect, due to hyperosmolality of the solution
above 0.9%.
Sodium hypochlorite
Used in the past, diluted, neutralised and combined with potassium
permanganate in the Daquin's solution. Nowadays used only as
disinfectant.
DISINFECTANTS

By the middle of the nineteenth century, post-operative sepsis infection accounted for the
death of almost half of the patients undergoing major surgery.
In 1839 the chemist Justin von Liebig had asserted that sepsis was a kind of combustion caused
by exposing moist body tissue to oxygen. It was therefore considered that the best prevention
was to keep air away from wounds by means of plasters, collodion or resins.

ANTACIDS
Antacids perform a neutralization reaction, i.e. they buffer gastric acid, raising the pH to
reduce acidity in the stomach. When gastric hydrochloric acid reaches the nerves in the
gastrointestinal mucosa, they signal pain to the central nervous system. This happens when
these nerves are exposed, as in peptic ulcers. The gastric acid may also reach ulcers in the
esophagus or the duodenum.
Other mechanisms may contribute, such as the effect of aluminum ions inhibiting smooth
muscle cell contraction and delaying gastric emptying.

Calcium Carbonate
CALCIUM CARBONATE is a calcium salt. calcium carbonate, CaCO3, white chemical
compound that is the most common nonsiliceous mineral. It occurs in two crystal forms:
calcite, which is hexagonal, and aragonite, which is rhombohedral. Calcium carbonate is
largely insoluble in water but is quite soluble in water containing dissolved carbon dioxide,
combining with it to form the bicarbonate Ca(HCO3)2. Such reactions on limestone (which is
mainly composed of calcite) account for the formation of stalactites and stalagmites in caves.
Iceland spar is a pure form of calcium carbonate and exhibits birefringence, or double
refraction.
It is used as an antacid to relieve the symptoms of indigestion and heartburn. It is also used to
prevent osteoporosis, as a calcium supplement, and to treat high phosphate levels in patients
with kidney disease.
Antacids are usually taken after meals and at bedtime, or as directed by your doctor or
health care professional. Take your medicine at regular intervals. Do not take your medicine
more often than directed. Need to take care before taking this:
•constipation
•dehydration
•high blood calcium levels
•kidney disease
•stomach bleeding, obstruction, or ulcer
•an unusual or allergic reaction to calcium carbonate, other medicines, foods, dyes, or
preservatives
•pregnant or trying to get pregnant
•breast-feeding

Interaction with medicines

Do not take this medicine with any of the following medications:

•ammonium chloride
•methenamine

This medicine may also interact with the following medications:

•antibiotics like ciprofloxacin, tetracycline
•captopril
•delavirdine
•gabapentin
•iron supplements
•medicines for fungal infections like ketoconazole and itraconazole
•medicines for seizures like ethotoin and phenytoin
•mycophenolate
•quinidine
•rosuvastatin
•sucralfate
•thyroid medicine.

ANTIHISTAMINES

A histamine antagonist is an agent which serves to inhibit the release of histamine.

The term antihistamine usually refers to the classical H1 receptor blockers. Reversible &
competitive H1 receptor antagonists block the binding of histamine to its receptors.
These compounds do not influence the formation or release of histamine. [Cromolyn which
inhibits the release of histamine from mast cells and is useful in the treatment of asthma.]

1. Introduction
 • Definition and Function: Antihistamines are a class of drugs that counteract the effects
of histamine, a compound involved in allergic reactions. They play a crucial role in
managing allergies, hay fever, and certain skin conditions.

2. Types of Antihistamines

• First-Generation Antihistamines:
• Structure and Mechanism of Action: Agents like diphenhydramine and
chlorpheniramine, which antagonize histamine receptors.
• Central Nervous System Effects: The ability to cross the blood-brain barrier and
induce sedation.
• Second-Generation Antihistamines:
• Structure and Mechanism of Action: Drugs like cetirizine and loratadine,
designed for selective peripheral histamine receptor blockade.
• Minimized Central Nervous System Penetration: Reduction of sedative side
effects through structural modifications.

3. Histamine Receptors and Signaling Pathways

• Histamine Receptor Subtypes:

• H1, H2, H3, and H4 receptors: Distribution and functions.
• Selective Targeting: How different antihistamines interact with specific receptor
subtypes.
• Signal Transduction Pathways:
• Activation of G-protein-coupled receptors and downstream effects.
• Modulation of Intracellular Calcium: Impact on cellular responses.

4. Structural Chemistry of Antihistamines

• Arylalkylamine Class:
• Structure-Activity Relationships: Influence of side chain variations on
pharmacological properties.
• Binding Interactions with Histamine Receptors: Molecular docking studies and
binding affinity.
• Ethylenediamine Class:
• Alkylamine vs. Ethylenediamine: A comparison of structural features.
• Stereochemistry Effects: Influence of chiral centers on drug activity.

5. Pharmacokinetics and Metabolism

• Absorption and Distribution:

• Bioavailability and Factors Influencing Absorption.
• Tissue Distribution: Penetration into target tissues.
• Metabolism and Elimination:
• Hepatic Metabolism: Involvement of cytochrome P450 enzymes.
• Metabolites and Active Compounds: How metabolites contribute to therapeutic
effects.
6. Adverse Effects and Safety Considerations

• First-Generation Antihistamines:
• Sedation and Central Nervous System Effects.
• Anticholinergic Side Effects: Dry mouth, blurred vision, and constipation.
• Second-Generation Antihistamines:
• Reduced Sedative Effects: Advantages over first-generation drugs.
• Safety in Special Populations: Considerations for children, elderly individuals, and
pregnant women.

7. Drug Interactions and Clinical Considerations

• Cytochrome P450 Interactions:

• Potential interactions with other drugs metabolized by the same enzymes.
• Clinical Implications: Adjustments in dosage or choice of antihistamine.
• Combination Therapies:
• Use of antihistamines in combination with decongestants or other allergy
medications.
• Synergistic Effects and Limitations: Balancing benefits and risks.

8. Future Developments and Innovations

• Novel Drug Targets:

• Exploration of non-histaminergic pathways for allergy management.
• Targeting Histamine Receptor Subtypes: Development of subtype-specific drugs.

Histamine
Basic amine autacoid stored in granules of mast cells and basophils.
IgE-dependent release
IgE-independent release (C3a and C5a, or drugs (e.g., d-tubocurarine).
Acts as neurotransmitter in histaminergic nerves

TRANQUILLISERS

1. Introduction

• Definition and Purpose: Tranquilizers, also known as anxiolytics or sedatives, are a class
of drugs primarily used to manage anxiety, promote calmness, and induce sleep. They
act on the central nervous system, modulating neurotransmitters to achieve their
therapeutic effects.

2. Types of Tranquilizers

• Benzodiazepines:
• Structure and Mechanism of Action: Benzodiazepines, such as diazepam and
lorazepam, enhance the inhibitory effects of the neurotransmitter GABA
 (gamma-aminobutyric acid) by binding to specific receptors on GABA-A
receptors.
• Therapeutic Uses: Anxiety disorders, insomnia, muscle spasms.
• Chemistry Behind Different Benzodiazepines: Variations in chemical structure
and their impact on pharmacological properties.
• Barbiturates:
• Structure and Mechanism of Action: Barbiturates, like phenobarbital, act on
GABA-A receptors and also directly on ion channels.
• Historical Significance: Early use and development of barbiturates.
• Safety Concerns and Decline in Usage: Barbiturate-related risks and the shift
towards safer alternatives.
• Non-Benzodiazepine Sedative-Hypnotics:
• Structure and Mechanism of Action: Drugs like zolpidem and eszopiclone, which
interact with GABA receptors but have a different chemical structure from
benzodiazepines.
• Selectivity and Reduced Side Effects: Design considerations for improved safety
and efficacy.

3. Molecular Targets and Receptor Interactions

• GABA-A Receptors:
• Detailed Mechanism: Interaction of tranquilizers with specific sites on GABA-A
receptors.
• Subunit Specificity: Variations in receptor subunits and their impact on drug
effects.
• Neurotransmitter Modulation:
• Impact on Neurotransmitter Release: How tranquilizers regulate the release and
action of neurotransmitters like GABA and glutamate.

4. Pharmacokinetics and Metabolism

• Absorption and Distribution:

• Lipophilicity and Blood-Brain Barrier: Factors influencing drug penetration into
the central nervous system.
• Distribution in Body Tissues: Variations in drug distribution due to chemical
properties.
• Metabolism and Elimination:
• Liver Enzyme Involvement: Cytochrome P450 enzymes and drug metabolism.
• Metabolites and Active Compounds: How drug metabolism produces active or
inactive compounds.

5. Adverse Effects and Tolerance

• Dependency and Tolerance:

• Biochemical Basis: Changes in neurotransmitter sensitivity and receptor
downregulation.
• Withdrawal Symptoms: Molecular mechanisms behind withdrawal symptoms.
• Cognitive Impairment and Sedation:
 • Impact on Neurotransmission: How tranquilizers induce sedation and affect
cognitive function.
• Balance Between Therapeutic and Side Effects: Challenges in designing drugs
with minimal cognitive side effects.

6. Future Directions and Innovations

• Targeted Drug Design:

• Development of drugs with improved specificity and reduced side effects.
• Exploration of Novel Targets: Research on alternative neurotransmitter systems
for anxiety and sedation management.

Tranquillizers also known as sedatives are man-made drugs, they are usually prescribed by
doctors as short-term treatments for depression, anxiety, stress and insomnia (difficulty in
sleeping).

The most commonly prescribed tranquillizers are from the class of drugs called
benzodiazepines (benzos) and are known as minor tranquillizers. There are various benzos and
they are usually known by their brand names, a few of the well known products include:

• Valium the generic name is diazepam.

• Ativan the generic name is lorazepam.
• Mogadon the generic name is nitrazepam. On the street they may be called moggies.
• Normison the generic name is temazepam. On the street they may be called jellies or
eggs.
• Rohypnol the generic name is flunitrazepam. On the street they may be called roofies,
rope or the forget-pill.

Drugs of abuse

The easy availability of tranquillizers has made them common as drugs of abuse. Some drug
abusers take tranquillizers to bring them down after using stimulants such as ecstasy or
cocaine. Others take them to enhance the effect of alcohol.

Temazepam has become a street drug as a substitute for heroin and Rohypnol is the
tranquilizer most associated with "date rape" as it has been known to be used to spike drinks.
The victim is often unaware that they have been slipped a drug and while under the influence
they are vulnerable to sexual abuse and rape.

Immediate effects of tranquillizers

Tranquillisers calm the user down and reduce feelings of agitation and restlessness, they also
slow down mental activity and produce drowsiness. Tranquillisers can have a relaxing effect
on the muscles. High doses of tranquillizers can make users forgetful, dizzy and can induce
sleep.
Long-term effects of taking tranquillizers

A low dosage of tranquillizers prescribed for a short period of time is unlikely to pose any greater
risk to health. However, if you take tranquillizers regularly a tolerance can develop, so you will
need to take more to get the same effect and you may also find you become dependent on
them. Therefore it is recommended that tranquillizers are not used for long periods, and should
not be taken for more than a 2-4 week period. If you are taking them for insomnia a 2-3 night
break from the tranquillizers each week is recommended.

ANTI FERTILITY DRUGS/ ORAL CONTRACEPTIVE PILLS

The combined oral contraceptive pill (COCP), often referred to as the birth-control pill or simply
"the pill", is a birth control method that includes a combination of an estrogen and
progestogen. When taken by mouth every day, these pills inhibit female fertility.
Mechanism of action

Combined oral contraceptive pills were developed to prevent ovulation by suppressing the
release of gonadotropins. Combined hormonal contraceptives, including COCPs, inhibit
follicular development and prevent ovulation as their primary mechanism of action.

Progestagen negative feedback decreases the pulse frequency of gonadotropin-releasing

hormone (GnRH) release by the hypothalamus, which decreases the release of
folliclestimulating hormone (FSH) and greatly decreases the release of luteinizing hormone (LH)
by the anterior pituitary. Decreased levels of FSH inhibit follicular development, preventing an
increase in estradiol levels. Progestagen negative feedback and the lack of estrogen positive
feedback on LH release prevent a mid-cycle LH surge. Inhibition of follicular development and
the absence of a LH surge prevent ovulation.

Estrogen was originally included in oral contraceptives for better cycle control (to stabilize the
endometrium and thereby reduce the incidence of breakthrough bleeding), but was also
found to inhibit follicular development and help prevent ovulation. Estrogen negative
feedback on the anterior pituitary greatly decreases the release of FSH, which inhibits follicular
development and helps prevent ovulation.

A secondary mechanism of action of all progestagen-containing contraceptives is inhibition

of sperm penetration through the cervix into the upper genital tract (uterus and fallopian
tubes) by decreasing the amount of and increasing the viscosity of the cervical mucus.

Drug interactions

Some drugs reduce the effect of the Pill and can cause breakthrough bleeding, or increased
chance of pregnancy. These include drugs such as rifampicin, barbiturates, phenytoin and
carbamazepine. In addition cautions are given about broad spectrum antibiotics, such as
ampicillin and doxycycline, which may cause problems "by impairing the bacterial flora
responsible for recycling ethinylestradiol from the large bowel"
STEROIDS

Introduction:

Steroids, a class of organic compounds with a characteristic structure, play diverse and
essential roles in the biological systems of both plants and animals. These molecules,
characterized by a specific arrangement of four interconnected carbon rings, serve as key
signaling molecules, structural components, and regulators in various physiological
processes. This overview explores the chemistry of steroids, encompassing their structure,
classification, and biological significance.

**1. ** Chemical Structure: At the core of steroids is a tetracyclic carbon structure known as
the steroid nucleus, consisting of three six-membered rings (labeled A, B, and C) and one
five-membered ring (labeled D). This unique arrangement imparts distinct chemical and
physical properties to steroids.

**2. ** Functional Groups: Steroids exhibit a variety of functional groups that contribute to
their biological activities. Hydroxyl (-OH) groups, ketones (C=O), and double bonds are
common features, with the specific arrangement influencing a steroid's function.

**3. ** Classification: Steroids are broadly classified into different types based on their
biological origin and function:
 • Corticosteroids: Derived from the adrenal cortex, these steroids include
glucocorticoids and mineralocorticoids involved in metabolism and electrolyte
balance.
• Sex Hormones: Estrogens, androgens, and progestogens are sex hormones that
regulate reproductive processes and secondary sexual characteristics.
• Sterols: Cholesterol, a vital component of cell membranes, is an example of a sterol
that also serves as a precursor for the synthesis of other steroids.

**4. ** Biosynthesis: The biosynthesis of steroids occurs through complex enzymatic processes,
often starting with precursor molecules like squalene. The diverse array of steroids results from
variations in the enzymatic pathways and modifications during synthesis.

**5. ** Biological Significance: Steroids play pivotal roles in various physiological processes:

• Regulation of Metabolism: Glucocorticoids influence glucose metabolism and immune

response.
• Reproductive Function: Sex hormones control the development of sexual
characteristics and play a crucial role in reproduction.
• Cell Membrane Structure: Sterols contribute to the fluidity and stability of cell
membranes.

**6. ** Pharmaceutical Applications: Synthetic steroids, such as corticosteroids and anabolic

steroids, find extensive use in medicine. Corticosteroids are employed for their anti-
inflammatory properties, while anabolic steroids are sometimes used to promote muscle
growth.

**7. ** Challenges and Controversies: The use of steroids, especially in the context of sports
and bodybuilding, has raised ethical and health-related concerns. Misuse and abuse of
steroids can lead to adverse effects on physical and mental health.
Conclusion: Unraveling the Chemistry of Medicines
In the pursuit of understanding the intricate tapestry of chemicals in medicines, our
expedition has taken us through the vast landscapes of molecular structures, biochemical
pathways, and therapeutic applications. From the ancient remedies rooted in nature to the
cutting-edge pharmaceuticals meticulously designed in laboratories, the journey has
showcased the profound impact of chemistry on the realm of healthcare.

As we navigated the diverse classes of medicines, each with its unique chemical fingerprint,
a common thread emerged — the pivotal role of chemical interactions in alleviating,
managing, or preventing various medical conditions. Corticosteroids, with their nuanced
modulation of inflammation, stood as guardians against immune-related disorders.
Antibiotics, the stalwarts in the battle against bacterial foes, showcased the elegance of
chemical warfare on a microscopic scale.

Venturing into the world of tranquilizers, we witnessed the delicate balance between
chemical design and therapeutic efficacy, where structural nuances could mean the
difference between sedation and relief. The antihistamines, with their targeted antagonism
of histamine receptors, demonstrated the fine art of disrupting allergic cascades at the
molecular level.

Beyond the mechanisms of action, our exploration delved into the pharmacokinetics and
metabolism, uncovering the journeys these chemicals embark upon within the human body.
Metabolites and active compounds, absorption and distribution patterns — each aspect
unfolded a chapter in the saga of how chemicals transform from pharmaceutical
formulations to therapeutic agents.

However, this journey also revealed challenges and ethical considerations. Antibiotic
resistance looms as a global threat, urging us to tread cautiously in the realm of antimicrobial
warfare. The potential for dependency and tolerance with tranquilizers echoed a cautionary
tale about the delicate equilibrium between therapeutic benefits and risks.

As we conclude this expedition through the chemical landscapes of medicines, it is evident

that the synergy between chemistry and medicine continues to shape the narrative of
human health. The future holds promises of novel drug targets, innovative therapies, and a
deeper understanding of the intricate dance between chemicals and biological systems.

In closing, our odyssey into the chemistry of medicines invites us to marvel at the intricacies,
respect the cautions, and embrace the ongoing quest for safer, more effective, and
ethically sound pharmaceutical interventions. The chemistry of medicines, a symphony of
atoms and molecules orchestrated to heal, stands as a testament to the ceaseless pursuit of
a healthier, chemically harmonized world.