Pharmacology &

Pharmacognosy
BTC-3084
Patricio Rojas Silva y Antonio Machado
*What are drugs?
*Which are the sources?
 What are drugs?
Chemicals that act on
living systems and may
be used in the
diagnosis, treatment,
or prevention of a
disease.
https://www.pharmacologyeducation.org/drugs
 What is
pharmacology?

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Pharmacogenetics/genomics

Pharmacovigilance

Pharmacognosy

Pharmacy

https://www.pharmacologyeducation.org/pharmacology
 What is
pharmacology?
The study of how drugs act in living systems.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Pharmacogenetics/genomics

Pharmacovigilance

Pharmacognosy

Pharmacy

https://www.pharmacologyeducation.org/pharmacology
 Pharmacokinetics (PK)

Quantitative study of drug movement in,

through and out of the body.
 Pharmacokinetics (PK)

Drug absorption:
*Process of delivering a drug into the blood
stream.

*Orally, rectally, intramuscularly,

subcutaneously, inhalation, topically, etc.

*If a drug is administered intravenously

(placed directly into the blood stream), the
need for absorption is bypassed entirely.

*Most drugs: weak acids or bases.

 Drug half-Life (t½)
The time it takes a drug to lose half its original concentration or activity after being
introduced into the body. Drug half-life is considered when determining drug dosing.
https://clinicalinfo.hiv.gov/en/glossary/half-life-t-12
 Pharmacokinetics (PK)

Drug distribution:
*Process of delivering a drug from the
bloodstream to the tissues, especially the
tissue(s) where its actions are needed.

*Drugs can bind non-specifically to albumin

and other proteins in the plasma or tissues.

*Drugs will be more quickly distributed to

areas of the body that receive large amounts
of blood flow.
 Pharmacokinetics (PK)

Drug metabolism:

*Primary objective: facilitate a drug’s

excretion by increasing its water
solubility (hydrophilicity).

*Covert a prodrug: codeine to

morphine.
*70% clinical drugs are removed by
the body’s metabolic system.

*Hepatic enzymes: cytochromes P450

(CYPs).

Wang D, et al. 2020. Deep Learning Based Drug Metabolites Prediction. Front. Pharmacol. 10:1586. doi: 10.3389/fphar.2019.01586
 Pharmacokinetics (PK)

Drug excretion:

*The kidney is the principal drug-

excreting organ.

*In most people renal drug excretion

decreases with age.

*Other ways:
Bile (Feces)
Milk (problem with lactation)
Sweat (minimal)
Tears (minimal)

https://www.youtube.com/watch?v=VZRVt9r4oSM
 Pharmacokinetics (PK)
Drug excretion: clearance

https://tmedweb.tulane.edu/pharmwiki/doku.php/pharmacokinetics https://www.youtube.com/watch?app=desktop&v=csywV3MYHDg
 Pharmacodynamics (PD)

* It is the study of how drugs have effects on the body or cells.

* The most common mechanism is by the interaction of the drug with tissue receptors
located either in cell membranes or in the intracellular fluid.
* Agonists & antagonists.

https://www.pharmacologyeducation.org/pharmacology/pharmacodynamics
 Drug-protein interaction: binding
Nicotinic agonist binding interactions
Acetylcholine binding protein (AChBP) from Lymnaea stagnalis

Ethan B. Van Arnam and Dennis A. Dougherty. Functional Probes of Drug–Receptor Interactions Implicated by Structural Studies: Cys-Loop Receptors Provide a Fertile Testing Ground
Miniperspective. Journal of Medicinal Chemistry 2014 57 (15), 6289-6300 DOI: 10.1021/jm500023m https://pubs.acs.org/doi/10.1021/jm500023m
 Factors affecting the pharmacokinetics and pharmacodynamics of a drug.

The effects of a drug are determined by:

* Physico-chemical/ molecular
characteristics, &
* The properties of the biological
systems involved.

Heterogenous conditions such as:

* gender,
* genetic background,
* tissue,
* age,
* diet,
* disease,
*other drug treatments
*+ etc.,
result in considerable inter-individual
and intra-individual variation!

de Lange Fluids and Barriers of the CNS 2013, 10:12 http://www.fluidsbarrierscns.com/content/10/1/12

 Pharmacovigilance
It is the science and activities
relating to the detection,
assessment, understanding and
prevention of adverse effects or
any other medicine-related
problem with an approved drug.
FDA (EEUU), EMA (UE), ARCSA
(Ecuador), OMS (WHO).

https://www.ema.europa.eu/en/human-regulatory/overview/pharmacovigilance-overview
 Pharmacovigilance

Nisha Jha et al. Need for involving consumers in Nepal's pharmacovigilance system. Australasian Medical Journal May 2014 DOI: 10.4066/AMJ.2014.2011
 Pharmacognosy
Pharmacognosy deals
with the natural drugs
obtained from organisms
such as plants, microbes,
and animals.

Orhan IE. Pharmacognosy: Science of natural products in drug

discovery. Bioimpacts. 2014;4(3):109-10. doi: 10.15171/bi.2014.001
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4204033/
 Artemisininas
Avermectinas
Artemisia annua
(ivermectina)
(Chinese
Streptomyces avermitilis
pharmacopea)
https://www.nature.com/articles/nature.2015.18507
Individualised Medicine - Prerequisites and Consequences
https://www.researchgate.net/publication/280577359_Individualised_Medicine_-_Prerequisites_and_Consequences
 Clinical trials or studies
• The discovery of small molecule drugs is:
• Time-consuming: timelines of 10–20 years.
• Expensive: US$0.5 billion to US$2.6 billion
• Labor-intensive.
• In addition to economic and technical reasons:
• Almost 50% of drug candidate drugs failed in clinical trials.
• Up to 25% of compounds were withdrawn due to metabolic, pharmacokinetic,
or toxic problems.
• Drug metabolism can produce metabolites with physicochemical and
pharmacological properties, which are significantly different from the physical
and pharmacological properties of parent drugs.

Wang D, et al. 2020. Deep Learning Based Drug Metabolites Prediction. Front. Pharmacol. 10:1586. doi: 10.3389/fphar.2019.01586
http://www.worksure.org/clinical-trial-drug-4-phases-required-documents/