Skip to main content

What is Pharmacokinetic and Pharmacodynamic-Efficacy/Potency

Pharmacokinetics and pharmacodynamics are two pharmacological phenomenon that brings out the effect of the drug when administered in a biological system.

Pharmacokinetics deals with the movement of drug administered which is accomplished in different steps: Absorption, Distribution, Metabolism and Excretion.

Pharmacodynamics deals with the effect that drug shows when it is administered in the biological system.it is dependent on factors like Potency, Efficacy, Bio-equivalent and Bio-availability.

 

Pharmacokinetic and Pharmacodynamic-Efficacy/Potency


Pharmacokinetics: How Drugs Move Through the Body 

Pharmacokinetic is all about the movement of the drug inside the body as kinetic means movement. Once drugs are inside our body, how do they move around, and get to where they need to go? Do they stay in the body indefinitely, or are they eventually removed from the body somehow?

The study of pharmacokinetics deals with precisely these issues, and in learning about this, we can highlight four main processes. Those are

  1. absorption,
  2. distribution,
  3. metabolism and,
  4. excretion.

We want to understand each of these processes, as well as the ways that interactions with food, drink, other drugs, and additional factors can have an influence on them, so let’s get a closer look at these now. As we said, the first step is absorption

 

Absorption 

Generally describes the way the drug moves from its site of administration across one or more membranes, often into the bloodstream, if it was not administered there directly. If a drug is administered topically, this could mean moving through the skin or a mucous membrane, and subsequently through the walls of nearby blood vessels.

If administered orally, this would mean being absorbed through the lining of the stomach or intestines, a process which would be slowed by the presence of food. Some drugs will pass through the cells that comprise these membranes by passive transport, others by active transport, but one way or another they will make it through on the way to their destination. In describing this process, it will be appropriate to review the term “bioavailability”.

This term describes the proportion of a drug that is successfully absorbed into the systemic circulation.

Bioavailability is a bit confusing with Bioequivalence.

Bio-equivalent

Two or more pharmaceutical product is said to be pharmacologically bioequivalent if their bioavailability after administration is in the same molar doges are similar to such a degree that their biological effect on the recipient is expected to be almost the same.

Similar drug may not always be bioequivalent due to the effect of the additional component such as a diluent, stabilizing agent, binder, lubricants etc.

 

Distribution 

Distribution describes its journey through the bloodstream to target cells and specific target molecules within. This is the way that drugs move through the bloodstream, after being absorbed into it, or injected into it. There are many factors that influence this, like the way that the drug interacts with the components of blood, such as plasma proteins.

If the drug binds too tightly to these proteins, it will not be able to reach its target cells. Sometimes, a second drug is administered in conjunction with the first that has a higher affinity for these proteins than the firestone does, thus serving the sole purpose of displacing the primary drug once bound tithe protein, allowing it to be delivered to its destination. Beyond these blood elements, there are other factors that may hinder the movement of a drug. These are anatomical barriers found in certain organs.

This prevents certain substances from passing out of the bloodstream into brain tissue. Some drugs will not be able to surpass this barrier, while others will, such as psychotropic drugs, or those affecting the mind. There is also the blood-placental barrier, that regulates which substances can pass from the bloodstream of a pregnant woman into the fetus. There are, however, a number of substances that are able to pass through this barrier that can still do harm to the fetus, such as alcohol and certain medications.

And then there is the blood-testicular barrier, which prevents many substances from reaching the male testes, therefore making disorders of the testes difficult to treat.

 

Metabolism 

It describes the ways that it eventually gets modified by enzymes and rendered ineffective. This describes any chemical reactions that the drug may participate in, often aimed at inactivating it and targeting it for excretion. If a drug is travelling through the bloodstream, it is highly likely to be metabolized to some degree. This is when Drug Interaction actually occurs.

For example, if a drug is taken orally, it will be absorbed through the intestinal wall, and for this reason, the part of the circulatory system it enters is a collection of blood vessels called the hepatic portal system. These carry blood directly to the liver, where they will be metabolized in some manner. This is called the first-pass effect, referring to the first pass of a drug through the liver, and this will typically greatly reduce the bioavailability of a drug.

In certain cases, metabolism in the liver actually activates a drug, but this is less common, and the first pass effect can inactivate over 90 per cent of an orally administered drug before it is able to reach general circulation. This must be taken into account when determining the appropriate dosage. Of course, drugs eventually reach their target cells, but even then, after enough time elapses, they will be metabolized.

There are many different enzymes in the body that perform these metabolic functions, which are very important because the immune systems only good at dealing with large biological particles like viruses or bacteria. It has no defence against small molecules, so this detoxification mechanism aimed specifically at small molecules had to evolve for life to exist in a chemical world.

Excretion 

It describes the way it then exits the body, typically either through urine or faeces. In excretion, where the drug or its remnants exit the body. This is typically done via exhalation, sweating, urination, or defecation. The kidneys are heavily involved in this process, as they must remove harmful substances from the bloodstream and maintain proper Homeostasis.

Some drugs are metabolized into gaseous form and are thus easily exhaled. Some drugs are excreted through bile, a substance secreted by the liver to aid in digestion, as bile is recirculated back to the liver via enterohepatic recirculation, whereby most of the drug can then be excreted by the kidneys and the rest will exit in the form of faeces.

And as we said, glands that produce fluids such as saliva and sweat can also promote excretion, though this method tends to be less effective. And with that, we have traced the journey of a drug into the body, around the body, and out of the body, which gives us a basic understanding of pharmacokinetics.

Pharmacodynamics: How Drug act inside the Body

Pharmacodynamics- what drug does to body



We just learned about pharmacokinetics, which helped us understand how a drug moves through the body. Through absorption and then distribution, a drug will travel through the bloodstream and eventually arrive at its target cells, where it can elicit its intended effect, prior to being metabolized and excreted. But what is this intended effect? 

Once a drug reaches its target, what exactly does it do, and how does this produce a cellular response? The study of this process is called pharmacodynamics.

So essentially, pharmacokinetics is the study of how our bodies affect a drug, while pharmacodynamics is the study of how a drug affects our bodies. Pharmacodynamics is quite complex, dealing with many advanced concepts in biochemistry. 

Far and away, the vast majority of drugs elicit a physiological response because of the way that they interact with a particular protein. Most often this will be a receptor protein, which may be embedded in the cell membrane, or it may be found inside the cell, whether in the cytoplasm or the nucleus.

Any receptor will have a ligand, which is a molecule that fits into the active site of the receptor, and in essence, turns the receptor on, evoking a conformational change that then propagates the signal in one of several ways. When drugs interact with receptors, there are two main ways that this could go. 

A drug could be an agonist for a particular receptor, meaning that it fits into the active site and mimics the native ligand, eliciting the typical physiological response.

We can call these facilitators. Or, a drug could be an antagonist for this receptor, meaning that it binds to the active site, but does not activate the receptor, thereby locking it in an inactive state. We can call these inhibitors, or sometimes blockers. 

Whichever the case may be, we can represent binding with this very simple equilibrium, which depicts some ligand, L, referring to the drug, and R, referring to the receptor, in equilibrium with LR, which is the receptor-ligand complex, with the ligand bound to the active site. With that understanding, we must now define two terms, potency and efficacy.

Potency 

It refers to the strength of a drug ate particular concentration or dosage, or the amount of a drug that is required to produce a particular effect. And to get more technical, it refers to the concentration or dosage required to produce 50% of the maximal effect that drug can achieve. This can be examined on something called a dose-response curve. 

As we can see, drugs of different potencies will require different doses, or different amounts of the drug being administered, to elicit the drug response it is capable of achieving. So, if a drug is extremely potent, only a very small amount of it will need to be administered in order to achieve its maximum effect.

Efficacy 

It deals with the maximum effect that can be achieved by a drug, such that after this is reached, no higher dose will produce any further effect. Two different drugs may have similar potencies, meaning that the response increases over the same increase in dosage, but one will achieve a more significant response than the other, or a more significant effect, due to its higher efficacy.

And similarly, two drugs can have the same efficacy, but differ in their potency, since one requires a smaller dosage to achieve its maximum effect than the other.

 If the purpose of the drug is to bind to the active site of a receptor or enzyme,

  • How well, does it bind?
  • What is its binding affinity?

If describing binding using this equilibrium from before, how heavily is the forward reaction favoured, the one that produces the LR complex?

Well in order to answer this question, we have to ask a few more.

  • How well does the drug fit into the active site?
  • How many electrostatic interactions are being made, and of what variety?
  • Are there hydrogen bonds?
  • Perhaps even covalent interactions?

If the drug is acting as an inhibitor, then high binding affinity will be crucial in order to have reasonable efficacy, because if the binding affinity is low, then when the native ligand comes along, which is the molecule that is supposed to go in the active site, it will most likely have a higher binding affinity than the drug, and will displace it, thus no inhibition can be achieved.

Sometimes inhibitors will bind irreversibly, meaning that once they’re in, they’re stuck there, which is often the case if covalent bonds are formed between the drug and the protein, although covalent bonds are not necessarily required for binding to be irreversible.

On the other hand, if the drug is acting as an agonist, again binding affinity will be relevant, and it will also have to have the right functional groups necessary to promote the same conformational change in the proteinase the native ligand, so that the protein will produce the same cellular response.

Now that we understand affinity, we can conceptualize potency and efficacy in a slightly different way, using receptors as an example. Potency is the affinity of a drug for a particular receptor. If the affinity is very high, most of the drug will be bound at any given time, and thus very little of the drug will be needed to occupy all the receptors.

Efficacy describes the effect the drug has on the receptor once it is bound or the degree of its ability to act as an agonist or antagonist. So, potency is related to affinity, whereas efficacy is related to the clinical effect of the drug.

Summary

Pharmacokinetic it is the movement of the drug inside the body, or how body react to administered drug.

Pharmacodynamic it is how the drug reacts with the body or simply it is what drug does to the body.

Both of these phenomenon helps in bringing the full effect of drug administered in human to explore its pathological state and physiological condition.

Popular posts from this blog

Scholarship in Nepal for MBBS 2021 Updated-TU/KU/BPKIHS/PAHS/CEE

In Nepal, there are a total of 356 Scholarship seats for the MBBS program. This is as per the provision for a 75% scholarship in a governmental college. This is a total scholarship provided by TU+KU+BPKIHS+PAHS. These seats include both MOE and individual scholarship offered by the respective college. And altogether there are 516 scholarship seats for MBBS including MBBS seats provided by Embassy and Jagdamba Guthi. For the latest {2021 onward} MBBS seats distribution in different Categories by MEC  CLICK HERE . To have look at result of MBBS 2021 Medical Education Common Entrance Examination {MECEE-BL}  DOWNLOAD HERE.   Here we will discuss the scholarship in Nepal for MBBS and seat distribution in these headings: Scholarships for MBBS- by the individual college Scholarships for MBBS – by MOE Scholarships for MBBS-by different Embassy Scholarships for MBBS- by Jagdamba Guthi Common Entrance Exam Scholarships in Nepal for MBBS- by Individual college Institute of Medicine

Scholarship and Open MBBS seats in Nepal 2022 Updated

In Nepal, there are several autonomous medical institutions and Universities which are conducting MBBS programme.  And there are 1835 Medical MBBS seats in Nepal. It includes all the MBBS seats distributed across the Medical institutions and Universities in Nepal . These MBBS seats are further divided into different categories. These are Paying seats and Scholarship seats.  Scholarship seats include both Reservation and Open scholarship seats, whereas other paying seats include both general paying seats and foreign paying seats.   Introduction In Nepal, the MBBS programme has been started in 1978. In the early period of the MBBS study, there were few medical colleges that were running under the affiliation of foreign medical universities Few were autonomous and few were under universities residing in Nepal. Later on, all the operational medical colleges were brought under the affiliation of universities residing in Nepal or made to run autonomously as an independent medical college.  

MECEE-BL 2022 MBBS-BDS-BASLP-Bsc.Nursing Entrance Result PDF Download & Seats

MECEE-BL 2022 MBBS, BDS, BASLP, BSc.Nursing And BPT  entrance exam results has been published on 06 April 2022, via the official website of the Medical Education Commission. In the year 2022, a total of 8687 students has secured passing mark in MBBS, BDS, Bsc.Nursing, BASLP, B.Perf.Technology. This result has arranged the student in merit order based on percentile. You can download the merit list PDF (MECEE-BL 2022 result) below. How Many Seats Are Available For MBBS, BDS, BAMS BSc.MIT, BSc.MLT And B.Optometry In Nepal? In Nepal, there are 18 Medical colleges including private, governmental, and autonomous medical colleges that offer MBBS, BDS, BAMS, BSc.MIT, BSc.MLT and B.Optometry program. There are 1835 medical seats in the MBBS program, 565 medical seats in BDS, 80 medical seats in BAMS, 71 medical seats in BSc. MIT, 445 medical seats in BSc.MLT, and 67 seats in B. Optometry across the different medical colleges in Nepal . Students are selected for these seats in different colleges