Integrated Pharmaceutical Sciences 1: Organic Medicinal Chemistry

Questions and Answers

What was the primary source for the discovery of morphine?

Poppy juice (correct)

Synthetic medicinal chemicals

Plant extracts

Animal fluids

Which scientist is credited with the discovery of penicillin?

Ernst Chain

Norman Heatley

Alexander Fleming (correct)

Howard Flory

Which of the following properties is NOT associated with aspirin?

Analgesic

Anticoagulant

Antiviral (correct)

Antipyretic

What is a common method used in drug discovery for identifying new compounds with biological activity?

Screening large libraries of natural products Signup and view all the answers

What is the significance of preclinical safety and toxicity testing in drug development?

To assess safety before clinical trials Signup and view all the answers

Which of the following is a method of drug discovery based on modifying existing molecules?

Chemical modification resulting in me-too analogs Signup and view all the answers

What contribution did Howard Flory, Ernst Chain, and Norman Heatley make to penicillin?

They isolated and purified the active compound. Signup and view all the answers

Which of the following is an example of a natural product used in drug discovery?

Fermentation broths Signup and view all the answers

What is the primary use of Pilocarpine?

Narrow angled glaucoma Signup and view all the answers

Which of the following is an indirect-acting parasympathomimetic?

Echothiophate Signup and view all the answers

What class of drugs does Atropine belong to?

Antimuscarinics Signup and view all the answers

What effect does Atropine toxicity typically have?

Dilated pupils and dry skin Signup and view all the answers

Which of the following is a cholinesterase regenerator?

Pralidoxime Signup and view all the answers

Which substances are included in the group of cholinesterase inhibitors?

Parathion and Malathion Signup and view all the answers

What condition is treated with ganglionic blockers like Hexamethonium?

Hypertension in emergencies Signup and view all the answers

What is the general effect of sedative-hypnotics?

Dose-dependent CNS depressant effects Signup and view all the answers

What is the primary mechanism of action of benzodiazepines?

They increase the frequency of GABA-mediated chloride ion channel opening. Signup and view all the answers

Which agent is classified as an antagonist that can reverse the effects of benzodiazepines?

Flumazenil Signup and view all the answers

Which of the following benzodiazepines is classified as short-acting?

Triazolam Signup and view all the answers

What is one of the primary concerns associated with the use of barbiturates?

They can interact adversely with other CNS depressants. Signup and view all the answers

Which of the following is NOT a characteristic of barbiturates?

They bind to the same site as benzodiazepines on GABAA receptors. Signup and view all the answers

What is the duration of action for Phenobarbital?

Long acting Signup and view all the answers

Which of the following drugs is considered an atypical sedative-hypnotic?

Glutethimide Signup and view all the answers

Which of the following statement about benzodiazepines and barbiturates is true?

Benzodiazepines can be reversed by flumazenil, while barbiturates cannot. Signup and view all the answers

What is a key characteristic of salicylates?

They have potent anti-inflammatory activity. Signup and view all the answers

Which compound is primarily indicated for treating ankylosing spondylitis?

Indomethacin Signup and view all the answers

What is the mechanism of action for Sulindac?

Prodrug with the same mechanism as indomethacin. Signup and view all the answers

Which class of NSAIDs is primarily indicated for post-op pain?

Pyrrole acetic acids Signup and view all the answers

What distinguishes COX-2 selective inhibitors from other NSAIDs?

They have a sulfonamide component that binds to a hydrophilic region on COX-2. Signup and view all the answers

Which drug is considered a non-selective COX inhibitor?

Tolmetin Signup and view all the answers

Which property is characteristic of propionic acid derivatives?

The alpha-methyl substituent increases COX inhibition. Signup and view all the answers

What is a common use for mefenamic acid?

Mild analgesic for dysmenorrhea Signup and view all the answers

Which class of medications produces hypotension as a side effect?

Phenothiazines Signup and view all the answers

What is the primary mechanism of action for second generation antihistamines?

Selective H1-receptor antagonism Signup and view all the answers

Which drug is considered a primary acid metabolite of hydroxyzine?

Cetirizine Signup and view all the answers

What characterizes dual acting antihistamines?

They block mast cell release and act on H1 receptors Signup and view all the answers

Which mast cell stabilizer is used topically for inflammatory diseases of the eye?

Lodoxamide tromethamide Signup and view all the answers

What effect do piperazine antihistamines like Cetirizine have on the blood-brain barrier?

They have limited ability to cross the BBB Signup and view all the answers

What is a notable side effect of dopamine antagonists?

Increased prolactin release Signup and view all the answers

What is a characteristic feature of the second generation antihistamines compared to first generation?

Reduced affinity for non-H1 receptors Signup and view all the answers

Study Notes

Organic Medicinal Chemistry Overview

Focuses on the discovery and development of novel natural and synthetic organic compounds.
Examines the effects of physiochemical properties on drug therapy.

Drug Discovery Process

Natural Products: Includes fermentation broths, plant extracts, and animal fluids like snake venoms.
Synthetic Medicinal Chemicals: Derived from project medicinal chemistry and combinatorial chemistry.

Historical Drug Discoveries

Morphine: Alkaloid from poppy juice, discovered by Friedrich Wilhelm Sertürner in 1815.
Penicillin: Discovered by Alexander Fleming in 1928 from mold; isolated by Howard Flory, Ernst Chain, and Norman Heatley in 1939, enabling clinical tests.
Aspirin: Analgesic, anti-inflammatory drug derived from willow tree bark used since Hippocrates’ time for pain relief.

Drug Classification and Mechanism of Action

Parasympatholytics: Include antimuscarinics which block muscarinic receptors; Atropine is a prototype used for cholinergic poisoning and bradycardia management.
Cholinesterase Reactivators: Pralidoxime, used for organophosphate poisoning.

Sedative-Hypnotics

Classified into benzodiazepines, barbiturates, and atypical agents.
Benzodiazepines: Enhance GABA-mediated chloride ion channel opening; divided into short, intermediate, and long-acting categories.
Barbiturates: Previously common sedatives with low safety margins; different durations of action including ultra-short, short, intermediate, and long-acting.

Anti-inflammatory Drugs

Salicylates: Potent anti-inflammatories mainly targeting COX-1.
Propionic Acid Derivatives: NSAIDs with analgesic and antipyretic properties; Naproxen shows slight COX-2 selectivity.
Aril and Heteroaryl Acetic Acids: Indomethacin treats various arthritic conditions, while sulindac acts as a prodrug.

COX Inhibitors

Selective COX-2 Inhibitors: Diaryl-5-membered heterocycles with similar therapeutic effects as NSAIDs; indicated for osteoarthritis, rheumatoid arthritis, and acute pain.

Antihistamines

First vs. Second Generation: Second-generation antihistamines have reduced affinity for non-histamine receptors and are more selective for H1-receptors.
Dual Acting Antihistamines: Block histamine release and action; examples include azelastine and ketotifen.

Mast Cell Stabilizers

Cromolyn Sodium: Inhibits mast cell degranulation, used prophylactically for asthma.
Lodoxamide Tromethamine: Prevents antigen-induced calcium influx leading to histamine release.

Notable Drug Examples

Phenothiazines: Used as sedatives and antiemetics; includes Promethazine and Cyproheptadine.
Benzodiazepine Reversal: Flumazenil acts as a benzodiazepine antagonist to reverse CNS effects.

Summary of Actions and Uses

Sedative-Hypnotics: Induce CNS depressant effects through various mechanisms; essential for managing anxiety, insomnia, and convulsions.
Antibiotics and Analgesics: Achieve therapeutic effects through inhibition of specific biological pathways; essential in pain management and infection control.

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Description

This quiz covers the essentials of Organic Medicinal Chemistry, focusing on the discovery and development of novel natural and synthetic organic compounds. It explores the effects of physiochemical properties on drug therapy and examines various sources of drugs, including natural products and synthetic methods.