General Principles of Pharmacology

18 important questions on General Principles of Pharmacology

List the non-receptor drug mechanisms

Antacids
Mannitol
Bulk & lubricating laxatives
Bile acid binding resins
Metal chelators
Purine/pyrimidine or folic acid structural analogues

What do bile acid binding resins do?

Bile acid binding resins (cholestyramine, colestipol) bind to bile acid and cholesterol in the intestine to prevent reabsorption.

What do metal chelators do?

Metal chelators bind to specific metal ions to reduce metal overload
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What are purine/pyrimidine or folic acid structural analogues?

Purine/pyrmidine or folic acid structural analogues incorporate into DNA to either alter function or inhibit precursor synthesis

What is the role of agonists?

Agonists mimic endogenous ligand, eliciting a response.

What is the role of antagonists?

Antagonists occupy a receptor without intrinsic activity, inhibiting agonists from binding to the receptor. Consequently, no response is elicited.

What are the three events that are altered by conformational change of the receptor due to the binding of the drug to the receptor?

1. Receptor interaction with other proteins
2. Ion channel open probability
3. Enzyme activity

What are the direct effects of conformational change from formation of drug-receptor complex?

1. Drug acts as competitive antagonist by mimicing and competing with endogenous ligand for binding site on receptor
2. Drug acts as competitive inhibitor by binding to receptor to obstruct substrate access to enzyme active site

What are the indirect effects of conformational change from formation of drug-receptor complex?

1. Allosteric regulation via conformation change caused by binding of drug somewhere else on receptor, which modulates receptor function or enzyme activity
2. Modulation of downstream events

What is the cause of side effects from drugs?

Since drugs not only interact with its target receptor but also with its non-target receptors, it produces side effects

What should the affinity (Ka) for target receptors of a drug be greater than to reduce side effects?

Ka for target receptors should be greater than Ka for other receptors to reduce side effects

What is the relationship between drug concentration (dose) and side effects?

Greater drug concentration leads to increase in drug side effects because more non-target receptors are likely to be bound to the drug.

List the factors to consider when prescribing medications

Correct clinical diagnosis
Underlying pathophysiology
Drugs with potentially useful action
Monitoring therapeutic response
Risks vs. Benefits
Communication with patient in making decision to treat

At which level do drugs act on living systems?

Drugs act on living systems at molecular level

What are the four types of drug names

1. Formal chemical name - indicates drug's exact molecular structure
2. Code name - short alphanumeric identifier (ex: D-365)
3. Generic name - official name of drug
4. Trade/proprietary name - marketed name (one drug can have multiple trade names)

What is the key difference between generic and trade names of drugs?

Generic drug names are usually written in all lower case. Trade drug names start with a capital letter.

What are the three variable factors in drug molecules?

1. Size (usually between 300-500 daltons)
2. Shape & charge (does it complement to the binding site on receptor?)
3. Chemistry (most drugs are weak acids or weak bases)

Which ionization form of drug molecules cross membranes more easily?

Unionized form of drug molecules cross membranes more readily.

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