Clinical Significance of pKa in Pharmacology

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What are the main routes of drug administration mentioned in the text?

Oral, sublingual, rectal, inhalation

Which of the following factors influences drug absorption related to the absorbing surface?

Local blood flow

In which pH environment are acidic drugs more ionized?

Alkaline

Which route of administration is generally the fastest for drug absorption?

Intravenous

What type of drugs are more absorbed: ionized or nonionized?

Nonionized (non polar, non charged) drugs

How does ischemia affect drug absorption?

Decreases absorption

What is the formula for calculating the volume of distribution (Vd) of a drug?

Vd = Total amount of the drug in the body / Plasma concentration of the drug

What does a total Vd of less than 5 L indicate about the drug's distribution in the body?

The drug is present only in the vascular compartment and can be removed by dialysis.

How can toxicity with acidic drugs be treated effectively?

By alkalinization of urine, which renders the drug more ionized in urine and less reabsorbable.

In what pH environment are basic drugs more likely to be trapped in breast milk?

Basic drugs with pKa >7.2 are more likely to be ionized and trapped in breast milk due to its pH of 7.

What does a total Vd greater than 41 L indicate about a drug's distribution in the body?

The drug is highly bound to tissue proteins and cannot be removed by dialysis.

How can toxicity with basic drugs be effectively managed?

By acidification of urine, which renders the drug more ionized in urine and less reabsorbable.

What is the purpose of phase I metabolism in drug metabolism?

Introducing a polar group to render the molecule polar and water soluble for excretion.

Which enzymes are responsible for catalyzing phase I metabolism?

Cytochrome p450, esterases, deaminases.

What is the role of glucuronyl transferase in phase II metabolism?

It catalyzes conjugation reactions with glucuronic acid to form water soluble conjugates.

Define 'First-Pass' Metabolism in the context of drug administration.

Metabolism of drug at the site of administration before it reaches systemic circulation.

What is the bioavailability of a drug administered via the intravenous (IV) route?

100%

How does the bioavailability of atenolol compare to lidocaine, propranolol, and morphine?

Atenolol has complete bioavailability, while lidocaine has partial bioavailability. Propranolol and morphine are in between.

What is the formula to calculate the loading dose needed to attain a desired plasma concentration?

LD = Vd x Cp

Why is it essential to consider drug clearance in pharmacokinetics?

Clearance (Cl) helps determine the rate at which a drug is removed from the body, influencing dosing frequency and overall drug effectiveness.

How does binding of drugs to plasma proteins impact drug efficacy?

The effect of a drug is related only to its free part, as the bound part acts as a reservoir that prolongs the drug's effect.

Which organ is the major site of drug metabolism in the body?

Liver

Give an example of a drug that undergoes metabolism to produce an active metabolite.

Codeine to morphine

How can diseases affecting albumin levels impact drug therapy?

Diseases like chronic liver disease, pregnancy, and renal failure can alter albumin levels, affecting drug binding and potentially leading to drug-related issues.

Learn about the clinical significance of pKa in pharmacology, including the site of drug absorption from the gastrointestinal tract, treatment of drug toxicity through urine alkalinization or acidification, and ion trapping in breast milk. Understand how knowledge of pKa values can impact drug pharmacokinetics and patient treatment strategies.

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