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INTRODUCTION TO

MEDICINE
Prof. Dr. A. V. Patil
Smt. S. S. Patil College of Pharmacy, Chopda
What is a drug?
“A Chemical Substance that Interacts with a Living
System and Produces a Biological Response”
Definition of a Drug

The term "drug" means [any] articles intended for use in


the diagnosis, cure, mitigation, treatment, or prevention of
disease in man or other animals.
What is a drug?
“A Chemical Substance that Interacts with a Living
System and Produces a Biological Response”
What is a drug?
“A Chemical Substance that Interacts with a Living
System and Produces a Biological Response”

 Good and Bad Drugs?

 Safe Drugs?
What is a drug?
“A Chemical Substance that Interacts with a Living
System and Produces a Biological Response”

 Good and Bad Drugs?

 Safe Drugs?
Morphine (bad?) vs. penicillin (good?)

Curare vs. paracetamol


Drugs are chemical substances that
affect both your mind and your body.
The prolonged use of drug may lead to
physical and/or psychological
dependence. An overdose of any drug
may lead to death.
The Life Cycle of a Drug
(pharmacokinetics)

• Absorption
• Distribution
• Degradation
• Excretion
Slow Absorption

• Orally (swallowed)

• through Mucus Membranes


– Oral Mucosa (e.g. sublingual)
– Nasal Mucosa (e.g. insufflated)

• Topical/Transdermal
(through skin)

• Rectally (suppository)
Faster Absorption

• Parenterally (injection)
– Intravenous (IV)
– Intramuscular (IM)
– Subcutaneous (SC)
– Intraperitoneal (IP)

• Inhaled (through lungs)


Classification of Drug Types
 Ethical drugs
 Generic drugs (no longer under patent)
 “Prescription Only” vs “Over the Counter”
 “Off Label” applications
 Orphan drugs
 Biotechnology products
 Counterfeit drugs
 Street drugs!
What criteria MUST new drugs meet?
 Drugs must address a new need or
provide a significant “added benefit” over
an existing medicine
 Drugs must also meet criteria:
 Must be safe, effective, of high quality
 …cost effective (1980s)
 ……….affordable (1990s)
Major Therapeutic Targets
 Infectious disease – anti-infectives
 Anti-bacterial, anti-viral, anti-parasitic drugs
 Metabolic disease
 cancer, cardiovascular, diabetes,
inflammation, high blood pressure,
neurological disease, pain
 Other aspects of health care
 Hormonal treatments, contraception,
vaccines, immunosuppresents, anaesthetics,
nutraceuticals
How do drugs work?
 The Biological Target - enzyme or receptor
 Where is the target - part of “us” or elsewhere
The “Lock and Key” analogy

Key
Lock
Binding

 Here the KEY is the natural substrate


 Binding of the KEY to the LOCK (an enzyme
or a receptor) then causes a response – a
shape change in the protein/receptor
The “Lock and Key” analogy

Key
Lock
Binding Biological
Response

 Here the KEY is the natural substrate


 Binding of the KEY to the LOCK (an enzyme
or a receptor) then causes a response – a
shape change in the protein/receptor
But when an effective drug is present

Biological response
is altered OR shut down
vs.
Binding of Drug
is preferred

 Drug may bind preferentially to the “active site”


 Antagonist – binds and BLOCKS
A compound inhibits an enzyme from doing its job.
Slows down an enzymatically catalyzed reaction.
 Agonist – binds and ACTIVATES
A compound that does the job of a natural substance.
Does not effect the rate of an enzyme catalyzed reaction.
 Partial agonist – induces a partial response
Who discovers drugs? Doctors?

 Identify biological target - biology


 Prioritise/ validate target – pharmacology and
chemistry
 Identify and optimise lead molecules –
chemistry/pharmacology
 Preclinical studies – chemistry/pharmacology/
toxicology
 Formulation - pharmaceutical sciences
 Clinical evaluation – medicine
 Manufacture - chemical engineering
Getting a drug to market
 Disease target - possible drug candidates
 Pre-clinical testing; R&D (1-3 yrs)
 Toxicology, “ADME”
 Clinical R&D (2-10 yrs; Av. 5yrs)
 Phase 1 – healthy volunteers
 Phase 2 – small patient group
 Phase 3 – larger patient group
 Regulatory approval (2-10(!) yrs)
 Market
 Phase 4 – long term monitoring
Major Therapeutic Targets

CNS
Metabolic
Cardiovascular
Anti-infectives
Respiratory
Gentio-urinary
Musculoskeletal
Oncology
What makes a good drug?
Lipinski's rules (Chris Lipinski – 1997)
In general, an orally active drug will meet most of the
following:
• Not more than 5 hydrogen bond donors (nitrogen or
oxygen atoms with one or more hydrogen atoms)
• Not more than 10 hydrogen bond acceptors (nitrogen or
oxygen atoms)
• A molecular weight under 500 daltons
• An octanol-water partition coefficient log P of less than 5