GREEN PACOP BIOCHEM

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Questions and Answers

What is a consideration regarding the proper handling of Nitroglycerin tablets?

They are explosive in certain formulations

They are affected by temperature changes

They are sensitive to light (correct)

They are sensitive to humidity

Which of the following nitrovasodilators has a bioavailability of about 100%?

Amyl nitrite

Isosorbide dinitrate

Glyceryl trinitrate

Isosorbide mononitrate (correct)

What is the primary mechanism of action of nitrovasodilators?

Nitrate ion released upon denitrification stimulating the production of prostacylin

Denitrification by glutathione S-transferase leading to increase cGMP (correct)

Nitrate ion released upon denitrification directly stimulating outward K-channels

Denitrification by glutathione S-transferase leading to increase cAMP

Which of the following tissues exhibit the greatest sensitivity to nitrovasodilators at the lowest effective doses?

Myocardial tissues Signup and view all the answers

Why do sublingual tablets of Nitroglycerin lose their potency when stored in plastic containers?

Because they react with the plastic material Signup and view all the answers

What is the effect of denitrification of nitrovasodilators?

Release of nitrite ion, which is then converted to nitric oxide Signup and view all the answers

What is the effect of nitric oxide on vascular smooth muscles?

It leads to relaxation Signup and view all the answers

Which of the following is NOT a characteristic of Nitroglycerin tablets?

They are affected by temperature changes Signup and view all the answers

What is the substrate for the synthesis of cAMP?

ATP Signup and view all the answers

What is generated as a secondary messenger when a Beta-adrenoceptor is stimulated?

cAMP Signup and view all the answers

What is the mechanism of action of Sildenafil?

Inhibits PDE leading to increase cGMP Signup and view all the answers

What ion's intracellular levels increase due to drugs that activate the phospholipase C-inositol phosphate system?

Calcium Signup and view all the answers

What characterizes competitive antagonism?

Shift of the agonist log concentration-effect curve to the right without a change on the slope or amplitude Signup and view all the answers

What is the minimum dose that produces the maximum achievable response known as?

E-max Signup and view all the answers

What generates cAMP as a secondary messenger?

Adenylyl Cyclase Signup and view all the answers

What is the effect of stimulating a G-protein-linked receptor?

Generation of cAMP Signup and view all the answers

Which of the following substances is absorbed significantly by pinocytosis?

Cyanocobalamin Signup and view all the answers

What is the apparent lipid-water partition coefficient of the drug in the given scenario?

4 Signup and view all the answers

What is the primary factor that determines the time to reach the steady-state concentration for a drug given at a constant rate?

Biologic half-life Signup and view all the answers

How much of the drug will remain in the body 12 hours after a single dose, given a biologic half-life of 4 hours?

25% Signup and view all the answers

What is the characteristic of a one-compartment model of drug behavior?

An AUC above the explored line that is less than 5% of the total AUC Signup and view all the answers

What is the required rate of infusion of Theophylline to achieve a desired plasma concentration of 10ug/mL in a 70kg patient?

0.6mL/minute Signup and view all the answers

What is the significance of the biologic half-life in pharmacokinetics?

It determines the time to reach the steady-state concentration Signup and view all the answers

What is the process by which the body eliminates a drug?

Clearance Signup and view all the answers

What is the most important toxicity associated with pyrazolone derivatives like Phenylbutazone?

Hematologic toxicities Signup and view all the answers

Which NSAID is most useful as an analgesic and has been used to replace morphine in mild to moderate post-surgical pain?

Ketorolac Signup and view all the answers

What is the primary advantage of drugs like Celecoxib and Etoricoxib?

Less incidence of gastric irritation or ulceration Signup and view all the answers

What is the primary reason for the withdrawal of certain COX-2 inhibitors from the market?

They increase the risk of thrombosis and cardiac deaths Signup and view all the answers

Which of the following agents is currently used as a first-line DMARD in the management of Rheumatoid Arthritis?

Methotrexate Signup and view all the answers

What is a benefit of using Ketorolac with an opioid?

It decreases the opioid requirement by 25-50% Signup and view all the answers

What is a common adverse effect of NSAIDs?

Gastric ulceration Signup and view all the answers

Why were some NSAIDs withdrawn from the market?

They increase the risk of thrombosis and cardiac deaths Signup and view all the answers

What is the maximum serum level of Theophylline above which toxicities and side effects occur?

20mg/L Signup and view all the answers

Which group of individuals has a faster clearance of Theophylline?

Neonates, young infants, and adults Signup and view all the answers

What happens to the clearance of Theophylline among chronic smokers?

It decreases Signup and view all the answers

What is the serum level of Theophylline above which seizures and arrhythmias are more common?

40mg/L Signup and view all the answers

What is true about the use of anti-cholinergic agents in COPD and bronchial asthma?

They are available as tertiary ammonium compounds Signup and view all the answers

What is the mechanism of action of Nedocromil?

Increase inward chloride conductance leading to hyperpolarization of mast cell membrane Signup and view all the answers

What is the mechanism of action of Zafirlukast and Montelukast?

Pharmacologic antagonism of Luekotriene D4 action Signup and view all the answers

What is not a characteristic of the use of anti-cholinergic agents in COPD and bronchial asthma?

They are more effective than beta-2 agonists in COPD Signup and view all the answers

Study Notes

Pharmacology Study Notes

Cyclic Adenosine Monophosphate (cAMP)

cAMP is generated as a secondary messenger by the action of the enzyme Adenylyl Cyclase
The substrate for the synthesis of cAMP is ATP (Adenosine Triphosphate)

Beta-adrenoceptor Stimulation

Stimulation of Beta-adrenoceptor, a G-protein-linked receptor, involves the generation of a secondary messenger known as cAMP
This is in contrast to IP3 (Inositol Triphosphate), DAG (Diacylglycerol), and calcium ions, which are secondary messengers involved in other receptor stimulation

Sildenafil (Viagra) Mechanism of Action

Sildenafil, a drug popularly known as Viagra, inhibits Phosphodiesterase (PDE) leading to an increase in cGMP (Cyclic Guanosine Monophosphate)

Phospholipase C-Inositol Phosphate System

Activation of alpha-adrenergic agonists like phenylephrine primarily causes an increase in intracellular calcium ion levels

Competitive Antagonism

Competitive antagonism is characterized by a shift of the agonist log concentration-effect curve to the right without a change in slope or amplitude
This is in contrast to other types of antagonism, which exhibit different effects on the agonist log concentration-effect curve

Pharmacological Principles

Potency refers to the minimum dose that produces the maximum achievable response
ED50 (Effective Dose 50) is the dose required to produce 50% of the maximum response

Drug Absorption and Distribution

Pinocytosis is a mechanism of absorption for certain substances, including Vitamin K and Cyanocobalamin
The apparent lipid-water partition coefficient of a drug can be calculated based on its concentration in an aqueous solution and octanol

Pharmacokinetics

The rate of infusion of a drug to achieve a desired plasma concentration depends on the clearance of the drug
The biologic half-life of a drug determines the time it takes for the drug concentration to decrease by half
Compartmental analysis of serum drug concentration versus time plots can be used to determine the pharmacokinetic behavior of a drug

Nitrovasodilators

Nitrovasodilators, such as nitroglycerin, have a bioavailability of about 100% when administered sublingually
The primary mechanism of action of nitrovasodilators involves the release of nitric oxide, which activates guanylyl cyclase leading to an increase in cGMP
Nitrovasodilators exhibit the greatest sensitivity in veins, followed by arterioles and arteries

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

Pyrazolone derivatives like Phenylbutazone are associated with hepatotoxicity and hematologic toxicities
Ketorolac is an NSAID that is useful as an analgesic and has been used successfully to replace morphine in some situations involving mild to moderate post-surgical pain
COX-2 inhibitors like Celecoxib and Etoricoxib have a lower incidence of gastric irritation or ulceration compared to traditional NSAIDs

Disease Management

Methotrexate is currently used as a first-line DMARD (Disease-Modifying Anti-Rheumatic Drug) in the management of Rheumatoid Arthritis
Anti-cholinergic agents are used in COPD and bronchial asthma, but their use is limited due to side effects

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Description

This quiz assesses knowledge of physiology and biochemistry concepts, including hormone regulation and secondary messenger systems.