Pharmacology - NSAIDs & PROSTAGLANDIN ANALOGS (MADE EASY)

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NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) are painkillers commonly used to treat pain, fever, and inflammation. Prostaglandin analogs are simply mimickers of endogenous prostaglandins, which are hormone-like substances involved in numerous body functions including the dilation and constriction of blood vessels, control of blood pressure, modulation of inflammation, and the contraction and relaxation of smooth muscle. This pharmacology lecture covers topics such as the role of cyclooxygenases (COX-1 & COX-2) in inflammation, thromboxane, prostaglandins; mechanism of action, therapeutic uses and side effects of NSAIDs and various prostaglandin analogs. Drugs mentioned include; Selective COX-1 inhibitors; Ketorolac, Flurbiprofen, Ketoprofen, Indomethacin, low-dose Aspirin; Non-selective COX inhibitors; Naproxen, Ibuprofen, Piroxicam, Diflunisal; Selective COX-2 inhibitors; Meloxicam, Diclofenac, Celecoxib, Etodolac; Prostaglandin E1 analogs; Alprostadil, Lubiprostone, Misoprostol; Prostaglandin F2α analogs; Bimatoprost, Latanoprost, Travoprost; Prostacyclin analogs; Iloprost, and Treprostinil.

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0:00 Arachidonic acid cascade
1:35 Nonsteroidal anti-inflammatory drugs (NSAIDs)
5:57 Prostaglandin analogs
10:18 Prostacyclin analogs

[SpeedPharmacology]

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[markyounger]

When he said that COX 1 inhibition had "highest risk" he should have added "higher GI risk" but less cardiovascular risk. COX 2 inhibition has higher cardiac risk.

[ritikasrivastava]

your 11 mins lecture is wayy far better then my faculty"s 1 hr lecture
respect from india

[dropapebble]

One of the best things you do is start off with the normal pathways and mechanisms of the body these drugs affect. It really helps understanding to start there and not just 'memorise fact A is A because it's A". It makes SENSE this way.

[TewodrosEriga]

I like pharmacy department when I was seen this channel

[sahilkakran]

Aspirin is an selective COX 2 inhibitor at low dose but at high dose it loses it's selectivity and also inhibit the COX 1 so not given in hypertension patient at high dose

[HarlequinDolls]

“Babies before birth”. It’s a fetus. Babies are born. They are neonatal.

[chemistrybyap]

Indomethacin and keterolac is classifed as Non-selective COX inhibitor in indian author book K.d tripathi.
What is correct please anybody clear it. Which source this channel use for making videos?

[ammarali]

Ketorolac and indomethacin are non-selective not only work on cox-1 as mentioned in the video

[nigelnyoni]

Inflammatory response:
Following tissue injury/irritation, Phospholipase A2 (PLA2) is released. It converts c.s. memb phospholipids into Arachidonic acid.

Arach. acid can be broken down by Cyclo-Oxygenase enzymes 1, 2 (and 3).

COX 1 is ubiquitous and perennial in body. it prods thromboxane & prostaglandins stimulating normal body functions
- secretion of protective gastric mucous,
- regulation of gastric acid,
- promotion of platelet aggregation,
- maintenance of renal blood flow
COX 1 make Thromboxane (TXA2) which promotes platelet aggregation.

COX 2 is induced at sites of inflammation. the prostaglandins it produces mediate inflammation, pain and fever. It produces Prostacyclin which is anti -platelet aggregation. Prostacyclin keeps blood CYCLIN
..
NSAIDs inhibit cox enzymes, preventing prostaglandin production, hence anti-inflam and ainti-pyretic, and analgesic effects

3 major groups of NSAIDs
1. selective COX 1 inhibitors
Ketorolac, Flurbiprofen, Ketoprophen, Indomethacin, Low-doses of Aspirin

2. non-selective COX inhibitors
Naproxen, Ibuprofen, Piroxicam, Diflunisal

3. selective COX inhibitors
Meloxicam, Diclofenac, Celecoxib, Etodolac

.
ADRs of NSAIDs

ADR 1: GI tract bleeding and peptic ulcers
COX-1 mediated prod. of Prostaglandin E2 (PGE2) an Prostacyclin (PGI2) usually stim. synth, of protective mucous and regulate normal gastric blood flow.
COX 1 inhibition has ADRs = increased risk of GI bleeding, and peptic ulcers.
.
ADR 2: Increased risk of bleeding
COX-1 mediated Thromboxane A2 (TXA2) prod promotes platelet aggregation.
TXA2 promotes platelet agg.; inhibition of it's prod. has anti-platelet effect, increasing risk of bleeding.

ASPIRIN IRREVERSIBLY INHIBITS COX-1 in platelets.
platelets haven't got nuclei, so no new COX-1 can be synth'ed, so effects last until new platelets form.
.
ADR 3: Compromised renal health
Renal prostaglandins (PGE2 and PGI2) dilate renal efferent arteriole (maintains GFR). They usally have minimal effect on renal perfusion. In old age and heart failure, their production increases due to compromise kidney fnxn. NSAIDs decrease this prod. and increase risk of kidney injury in people with compromised kidney health.
.
ADR 4: increased risk of Cardiovascular events
Agents with high COX-1 selectivity protect cardiovascular health due to their antiplatelet effects. Anti-cox-2 drugs do the opposite.
In coronary blood vessels, prostacyclin vs TXA2 is usually balanced:
Prostacyclin (PGI2) prod by COX-2 in endothelium causes vasodilation & inhibition of platelet activation
Thromboxane A2 (TXA2) prod by COX-1 in platelets causes vasoconstriction and promotion of platelet aggregation.

Selective inhib of cox 2 decreases PGI2 and increases TXA2 by contrast, => vasoconstriction and platelet activation being more likely to occur => CV events more likely (MIs and Strokes)

[barbarvssa]

There is no selective cox1 inhibiter, only preferential activity on cox1. (Inhibition is more on cox1 but not exclusive)

[kotsiaschris]

not sure if there exist cox 1 selective inhibitors ???

[jesseoneill]

Diclofenac is not a selective Cox 2 inhibitor. It inhibites Cox 1 and Cox 2 with equipotency

[ComPasPharm]

How could Indometacin, Ketorolac and Flubiprofen be selective COX1 inhibitors if they are NSAIDs? To be an NSAID a drug definetely has to inhbit COX2 enzime and the production of prostaglandins...
Its a mistake here... we could say about nonselective COX1 and COX2 with a higher or lesser inhibiting activity toward COX1 vs COX2 but deffinetly not to call NSAIDs selective COX1 inhibitors.
With all respect, here s a mistake that can easely lead to misunderstanding.

[francisanukur]

Extremely perfect, I love your lecture...

[yashgarg]

but speed sir google is saying that ketorolac is a non-selective cox inhibitor

[zelda]

maybe in COX 1 u mean thromboxane and leukotrienes ?

[sangbarafavour]

your videos are always the best
Thank you

[Simplensweett]

Ur classes are different from others.same every time and very clear.learning is easy with you.

[johnsadek]

isnt ketoprofen cox 1 and 2 inhibitor? not selective cox 1? 3:30