Introduction to NSAIDs and Analgesics

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Questions and Answers

What is the primary precursor for all eicosanoids in the biosynthesis pathway?

Thromboxane

Arachidonic acid (correct)

Leukotriene A4

Prostaglandin PGG2

Which of the following is NOT a function of eicosanoids?

Modulating pain

Reducing bronchoconstriction (correct)

Inhibiting inflammation

Regulating platelet aggregation

What effect do NSAIDs have on prostaglandin production?

They inhibit COX-1 and COX-2, reducing PGG2 production (correct)

They increase the production of PGG2

They enhance the activity of phospholipase A2

They convert PGG2 to thromboxane

What result occurs when phospholipase A2 acts on cell membrane phospholipids?

Conversion to arachidonic acid Signup and view all the answers

Which of the following statements about leukotrienes is true?

Excess leukotrienes can lead to airway edema and bronchoconstriction. Signup and view all the answers

What is the primary role of an agonist in pharmacology?

Enhance cellular activity Signup and view all the answers

Which of the following best describes the concentration-effect relationship in pharmacodynamics?

Sigmoidal curve representation Signup and view all the answers

What are the two main processes described by pharmacokinetics (PK) and pharmacodynamics (PD)?

What drug does to the body and what body does to the drug Signup and view all the answers

Which route of administration bypasses first-pass metabolism?

Intravenous (IV) Signup and view all the answers

What is the significance of drug elimination in pharmacology?

It influences drug effects in cases of organ dysfunction Signup and view all the answers

Why should children not be dosed as small adults?

They are more vulnerable to adverse effects Signup and view all the answers

What stage follows drug discovery in the drug development process?

Clinical development Signup and view all the answers

What is the advantage of generic medicines compared to brand-name drugs?

Generics are cheaper due to existing research on the formula Signup and view all the answers

What is the primary effect of NSAIDs on COX enzymes?

Inhibit COX only Signup and view all the answers

Which prostaglandin is important for heart protection and is made by COX-2?

Prostacyclin I Signup and view all the answers

What is a potential side effect of acetanilide and phenacetin?

Hemolytic anemia Signup and view all the answers

What is the predominant mechanism of action of paracetamol in the central nervous system?

Agonism at cannabinoid receptors Signup and view all the answers

Why does paracetamol lack anti-inflammatory activity?

It works only at COX-3 in the CNS Signup and view all the answers

What is the resultant compound formed when paracetamol is metabolized?

AM404 Signup and view all the answers

Why might children experience different effects when taking paracetamol?

Their liver is not fully developed Signup and view all the answers

What do NSAIDs primarily prevent in the body?

Inflammation Signup and view all the answers

What is the primary role of proteins and nucleic acids in biochemical processes?

They form critical links in biochemical processes. Signup and view all the answers

Which process is primarily influenced by the absorption of a drug?

Bioavailability Signup and view all the answers

In drug development, which stage focuses on testing the efficacy and safety of a drug in humans?

Phase I Clinical Trials Signup and view all the answers

What characteristic of a drug is primarily affected by its stereochemistry?

Its mechanism of action Signup and view all the answers

What is the main function of antagonists in pharmacodynamics?

To inhibit the action of agonists Signup and view all the answers

Which method of drug discovery focuses on the utilization of natural compounds?

Natural Products Signup and view all the answers

Which factor is least likely to influence drug response?

The color of the drug Signup and view all the answers

What is the primary purpose of drug regulation?

To ensure the safety and effectiveness of drugs. Signup and view all the answers

Which of the following best describes biotransformation?

The process where drugs are chemically modified by the body. Signup and view all the answers

What aspect of pharmacokinetics primarily influences the duration of a drug's effect?

Metabolism rate Signup and view all the answers

What effect does adding other lipophilic groups to the rings have on the structure?

It becomes non coplanar and enhances activity. Signup and view all the answers

What does the suffix 'ac' or 'cin' imply about a compound?

The compound contains two carbon atoms, indicating acetic acid. Signup and view all the answers

Which of the following is NOT a property shared among the NSAIDs analyzed by Novartis?

All contain a 3-carbon chain. Signup and view all the answers

What is the partition coefficient of Diclofenac?

13.4 Signup and view all the answers

What does the introduction of an a-methyl group in carboxylic side chain result in for aryl propionic acids?

A chiral carbon and existence of enantiomers. Signup and view all the answers

What is the primary challenge associated with drugs in the profen class?

They have rapid epimerization of enantiomers. Signup and view all the answers

How does Diclofenac bind to proteins in the body?

Similar to the way aspirin binds to serine. Signup and view all the answers

What was the primary aim of Novartis during the development of Diclofenac?

To create an NSAID with high activity and tolerance. Signup and view all the answers

Study Notes

Introduction to Non-Steroidal Anti-inflammatory Drugs (NSAIDs)

NSAIDs are a class of drugs that reduce pain, fever, and inflammation.
They work by inhibiting the production of prostaglandins, which are chemicals that cause pain, fever, and inflammation.
NSAIDs are often used to treat conditions like arthritis, headaches, and menstrual cramps.

Analgesics

Analgesics are drugs that relieve pain.
They can be divided into two main categories: narcotic and non-narcotic.
Narcotic analgesics, such as morphine, are derived from the opium poppy and are highly effective at relieving pain.
Non-narcotic analgesics, such as NSAIDs, are not as potent as narcotics but are generally safer.

Eicosanoids

Eicosanoids are a group of lipids that play a role in inflammation, pain, and other physiological processes.
They are derived from arachidonic acid, a fatty acid found in cell membranes.
Different types of eicosanoids, such as leukotrienes, thromboxanes, and prostaglandins, have different effects on the body.

Eicosanoids Biosynthesis

Phospholipase A2 is an enzyme that converts phospholipids in cell membranes into arachidonic acid.
Arachidonic acid is the precursor to all eicosanoids.
Lipooxygenases (LOX) enzymes convert arachidonic acid into leukotrienes, which are involved in airway edema and bronchoconstriction (asthma).
Cyclooxygenase (COX) enzymes convert arachidonic acid into prostaglandins, which modulate pain, inflammation, and fever.

NSAID Mechanism of Action

NSAIDs inhibit COX-1 and COX-2 enzymes, which prevents the production of prostaglandins.
This reduces inflammation and pain.
However, inhibiting COX enzymes can also increase the production of leukotrienes, which can worsen asthma symptoms.
Steroidal drugs inhibit the production of arachidonic acid, preventing the production of all eicosanoids, including leukotrienes.

Paracetamol (Acetaminophen)

Paracetamol is an effective analgesic and antipyretic but lacks anti-inflammatory activity.
It is a prodrug that is metabolised in the body to form AM404, which is an agonist at cannabinoid receptors.
Paracetamol also inhibits COX-3, but only in the central nervous system, which explains its lack of anti-inflammatory effects.

Arylalkonoic Acids

Arylalkonoic acids are a large group of NSAIDs that includes acetic and propionic acid derivatives.
Acetic acid derivatives have two carbon atoms and include drugs like diclofenac and indomethacin.
Propionic acid derivatives have three carbon atoms and include drugs like ketoprofen and ibuprofen.

Indomethacin Development

Indomethacin was discovered in 1963 and is a potent anti-inflammatory and antipyretic.
It is used for short-term treatment of acute gout, ankylosing spondylitis, and osteoarthritis.

Diclofenac Development

Diclofenac was developed by Novartis and is a potent NSAID with good tolerability.
Its structure is similar to other effective NSAIDs, including phenylbutazone, mefenamic acid, and indomethacin.

Ibuprofen Development

Ibuprofen is a chiral molecule, with two enantiomers (R- and S-isomers).
Most ibuprofen formulations are marketed as a racemate (mixture of R- and S-isomers) because the R-enantiomer quickly converts to the S-enantiomer in the body.

NSAID Binding

Diclofenac binds to serine residues in the COX enzyme in a similar way to aspirin.

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Description

This quiz explores the fundamentals of Non-Steroidal Anti-inflammatory Drugs (NSAIDs) and analgesics. Learn how these drugs function in pain relief, fever reduction, and inflammation control. Understand the differences between narcotic and non-narcotic analgesics and their applications.