Drug Metabolism Made Simple *ANIMATED*
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- Опубликовано: 19 окт 2024
- metabolism is the protective biochemical process by which our bodies alter xenobiotics either enzymatically or nonenzymatically. generally, drug metabolism begins with hydrophobic drug and converts it to a more hydrophilic metabolite to facilitate its elimination.
an understanding of the drug metabolism process and the potential outcomes is critical for developing safe and useful pharmaceuticals.
drug metabolism can result in one of two products, an inactive metabolite and an active metabolite.
inactive metabolites of the drugs basically have no pharmacological activity of the original drug. an example of that would be the hydrolysis of procaine into para aminobenzoic acid and diethylethanolamine which results in the loss of the anesthetic activity of procaine.
on the other hand, an active metabolite can mean that a metabolite can retain the same activity of the parent drug, that's apparent when codeine is demthylated to a more active drug which is morphine.
however, in some cases we notice a result known as bioactivation where the parent drug is inactive and the metabolite would have a pharmacological activity, in this case the inactive parent drug is called a prodrug.
an example of a prodrug is enalapril which has no activity as an antihypertensive, but upon hydrolysis it becomes enalaprilat which is a potent antihypertensive drug.
bioactivation of a drug can also lead to toxic metabolites, the widely used acetaminophen has a metabolite that is called n-acetyl-p-benzoquinone imine which is hepatoxic, I explained the mechanism of the toxicity and the antidote in my previous video which I linked in the description below.
The liver has the highest concentration of drug-metabolizing enzymes, because of it’s location between the gastrointestinal tract and the systemic circulation.
Based on the reactions involved in the metabolism process we can classify the metabolic pathways into phase I metabolism and phase II.
Phase I metabolism is characterized as a functionalization reaction, where they add or reveal a functional group by oxidation, reduction, or hydrolysis, hence, leading to increase in overall polarity of the drug which facilitates its excretion in the urine
Oxidation is the most common phase I reaction,
Cytochrome p450 is a superfamily of oxidases that are responsible for the majority of oxidation reactions, it’s found in very high concentrations in the liver.
Oxidation can also happen through alcohol dehydrogenase which is an enzyme that oxidizes alcohols into aldehydes from primary alcohols and to ketones from secondary.
Aldehydes can be oxidized from to carboxylic acid by the enzyme aldehyde dehydrogenase. We can see that in the example of the conversion of acetaldehyde to acetic acid in the metabolism of ethanol.
Another phase I reaction is the reduction reaction, there are several reductase enzymes common reduction reactions include the reduction of disulfide bonds, in which the disulfides would be reduced to free sulfhydryls. Another reduction reaction is done by the aldo-keto reductases which reduce carbonyl containing compounds back to alcohol in a process opposite to the oxidation done by alcohol dehydrogenase.
The last type of phase I metabolism reaction is hydrolysis, hydrolysis is basically the addition of water across a bond resulting in a more water-soluble metabolite. A great example of hydrolysis is ester hydrolysis which is performed by the enzyme esterase found throughout the body, esterase is responsible for the hydrolysis of an ester into a more soluble alcohol or carboxylic acid.
Phase II
Phase II reactions are commonly called conjugation reaction owing to the fact they add a functional group on the drug for the purpose of increasing its polarity. The conjugation process requires an enzyme generally termed as transferase, that transfers the large polar molecule called a co-factor onto the drug,
Examples of phase II reactions:
glucuronidation is the most common phase II reaction, glucuronosyltransferase is the enzyme that uses UDP-GA as the cofactor to transfer glucuronic acid to several functional groups like hydroxyl groups, carboxylic acid ,and hydroxylamines. The glucuronic acid adds a significant amount of hydrophilicity to the molecules facilitating it’s excretion process.
Another popular reaction is glutathione conjugation which results from the addition of glutathione molecule to an electrophilic substrate. Being a nucleophile glutathione generally acts to detoxify electrophiles.
Glutathione-s-transferase is the enzyme responsible for the reaction of glutathione with electrophiles like epoxides and halides. After the conjugation, the product is excreted as mercapturic acid in the urine.
Paracetamol antidote video: • 5 ANTIDOTES EVERY PHAR...
Hey guys thank you for watching, what videos do you like to see next, tell me here if you would like me to cover a specific topic!! ☺️☺️☺️
Thank you for the video. However, I found the style of animation rather annoying and unnecessary.
This is honestly amazing, I have 2 powerpoint lectures consisting of 90 lecs altogether on drug metabolism, and you've summarised that into 8mins of pure simplicity! Keep up the amazing work, lookng forward to future vids. Definitely subscribed
Thank you so much
YESSSS!!!
This is actually very nicely summarized, short and brief but contains all the most important information. Saved me time from my 1.5hr lecture xDDDDD
this is an amazing video!!! covers everything in good detail but still simple!
one of the simplest explanation that i have seen..thanks..keep it up. It can be used in class room.
Thank you sir I really appreciate it
This is a very condensed but valuable explanation. The author's style captures attention. Compare the written script with the animated presentation and for me, the animated presentation enable the script. The effort and time to create this presentation was not humble.
+Edward Tobe wow, you sir humble me with your praise. thanks alot, comments like this push me foreward.
fantastic video!! now i feel confident for my exam!
Thanks a lot for making me understand a concept that I struggled with throughout my 5 years of med school...Finally!
Most welcomed, my pleasure.
This was phenomenal! Very concise and informative. Thank you!!
Several typos? Glutathion -> Glutathione
Easter Hydrolysis -> Ester Hydrolysis
t=326
Thanks for the video. It was assigned reading for grad school. I will say that the hand didn't add anything and just gave us less time to absorb the material. But that's for providing the video.
outstanding viedo, 8 minutes of pure education, amazing, well done!
Appreciate it
Great video, but maybe use a little bit of space between your CAPITALIZED words, so it is easier to read?
Was wondering if you have reference to this, it is really nice how you made it quite simple but easy to understand. Thank you
His explanation is direct to the point.💞
Solid video sir, thank you
Thank you
Truly an amazing explanation-!! So calm as well. Im trying to find out why im not feeling my meds!
Just to be clear... If im more sensitive to "uppers" does that mean its the same for "downers" ?
help me understand ! 💖🌟⭐🌠🌌thank you so much
Sir what is the enzyme in which disulfide is reduced to free disulfydryl?
I don't know how to thank this explain so well, great job.
You're most welcomed
This Animation is Very useful for me. Thanks to you. Keep it up...
Hey tnk u sooo much u just save my brain
Thank you!
Your teaching way is v nice v simple and perfect I get my complete lecture from ur video thanks..
Please can explain the details of metabolism of linagliptin as hypoglycemic drug ,thank you
Wow probably paused and rewinded that a hundred times. Still a little confused as to how carboxylic acid plays a roll in the oxidation of aldehydes?
Thank you so much !
It's been over 25 years since I studied Chemistry in high school so I don't remember much of it. I watch these type of videos just out of curiosity, I'm not even a student in the field. That being said, I would like to ask a question. Do med students have to know the IUPAC nomenclaturure and all that aldehyde, ester, aminas stuff in order to pass the exams on drug metabolism?
Not really, but pharmacists must
really very well explained, one can easily understand ....
Thank you for your amazing feedback ❤️
Woww you made it sooo easy and simple for me thanks for this amazing video ❤
Very well explained, thank you
Really very very helpful...thanks...
Wow amazing ❤️❤️
Well explained👍
I love your videos please continue
Thankyou so so much❤ it was more than awesome 🔥
Thank you for your feedback 🥰
I love this video.Please keep it up.
Thank you
Thank you so much for this.
Thanks
this guy stole my keyword search hahahaha😊
thanks so much for this
thank you is much it really helped me
At 3:14 there is a typo for "Oxidation".
Please upload more videos....
Any suggestions on the subject ?
At 3:50, There is another typo "Responsible"
Great job!
Amazing! Thank you!
Please make more video of pharma
Very helpful
Thank you
Helpful
+Waqar Ahmad Lone glad to hear that
awesome ......very helpful video please make more alike videos
Thank you!!
well explained ..... thank you sir
You're most welcomed
Brother plz make video on types of receptor s
Thank you sir
All the best
Great
To improve your videos even further.. please check the spelling in your animation.
It's very distracting when there is a spelling error.
Great job doing the video though
I will, thank you for your feedback
At 5:22, you spelled easter, but it should be ester
+Natan Glauber filippi thank you for noticing
Thanks million times...sir
يعطيك العافيه
الله يعافيك
really thanx
Can u make videos on Drugs acting on automic nervous system?
+Vishwa patel I will soon
Vishwa pate
Thnx
excellent, but many TYPOS - please fix
Very good explanation....keep it up
+Vishwa patel thank you so much , I will
Nice
superb lecture
Thank u
Welcome and thank you for watching 😁
Receptors
What about microsomal and non-microsomal enzymes?
You completely missed that part 😒
Very helpfull thkyou sir
Fantastic
Thank you
Pill Whiteboard illustrate. The metabolic path ways for tow phase 1 metabolites and one phase2 metabolit of Diphenhydramine
So the what's function of cytochrome p450 in metabolism?
It's the enzyme that facilitates the oxidation of molecules resulting in easier excretion
Okay but please some describe CYP450
Pill Whiteboard can u help me
tnq so much sir 😊...
My pleasure
Drug biotransformation phase I makes drugs ____ polar for metabolism and phase II makes drugs ____ polar for excretion. *
More; Less
More; More
Less; Less
Less; More
can someone help me with this?
I guess ..More ; Less .. what's the answer??
Bestttttt
It must be ester and not easter
Am I able to contact you via an email address?
Of course, abqourrr@gmail.com
Parasympahomimetics
😊
200000 viewer
Thank you
You speak english with an arabic accent ^_^
I am arabic 😊
Thank you so much!
You're welcome!