38 Questions
What is the term for the ability of a substance to exist in different crystalline forms?
Polymorphism
Which route of administration is most likely to exhibit differences in bioavailability?
Oral
What is the term for a drug that is not bound to plasma proteins?
Free drug
What is the principal site of drug metabolism?
Liver
What is the mechanism of drug excretion via the kidney?
Glomerular filtration
What type of diluent or filler is needed for faster absorption of a hydrophobic drug?
Amphilic
What route of administration bypasses gastrointestinal degradation and hepatic metabolism?
Intravenous injection
What is the major plasma protein involved in the distribution of weak acids?
Albumin
What slows down gastric emptying?
Fatty foods
What is the ratio of the concentration of a drug in two immiscible phases called?
Lipid/water partition co-efficient
What is the result of drug metabolism?
More polar compounds
What happens to drugs that are poorly lipid soluble or extensively ionized at the pH of the blood?
They penetrate the CNS very slowly
What can modify drug absorption?
All of the above
Which statement is FALSE about amorphous and crystalline forms?
The amorphous form has a lower dissolution rate than the crystalline form
Why do poorly lipid soluble drugs have difficulty penetrating the CNS?
They penetrate the CNS very slowly
What is the result of drug metabolism on the oil/water partition coefficient?
It decreases the oil/water partition coefficient
What is the effect on water solubility of a drug when its polarity increases due to the presence of hydrophilic functional groups?
It increases
Which of the following characteristics is NOT associated with facilitated diffusion of drugs?
The transport mechanism becomes saturated at low drug concentrations
Cytochrome is a component of which enzyme system?
Microsomal mixed-function oxidase system
Which type of drugs does alpha-1-glycoprotein bind with?
Basic, highly lipophobic drugs
What is the effect of increasing the polarity of a drug on its blood flow?
It has no effect on blood flow
What is the primary function of cytochrome in the microsomal mixed-function oxidase system?
To activate molecular oxygen
What is the phenomenon where a drug emptied via bile into the small intestine is reabsorbed from the intestinal lumen into systemic circulation?
Enterohepatic recirculation
What is the ratio of the amount of the drug present in the body over the plasma concentration?
Volume of distribution
Which of the following is considered as structurally specific drugs?
Sulfonamides
How does a drug reach the systemic circulation after passing the epithelium of the gastrointestinal mucosa?
Through the bloodstream
What is the phenomenon where the ions of added electrolytes require water for hydration, reducing the amount of water available for the solution of the non-electrolyte?
Salting out
What are drug products that contain the identical therapeutic moiety, or its precursor but not necessarily in the same amount or dosage forms or as the same salt ester?
Pharmaceutical alternates
What are inactive enzymes?
Zymogens
Which of the following pairs is not correct?
Gelatin - coating agent
What is the prerequisite for particle size reduction to enhance drug absorption?
Absorption process is rate limited by dissolution of drugs in GI fluids
What is a prerequisite of drug absorption?
Drug is in aqueous solution
Which theory states that drug effectiveness does not depend on the actual occupation of receptor by the drug?
Hypothesis of Ariens and Stephenson
Which equation is followed by the process of passive diffusion?
Fick's Law
What is a measure of the relative amount of drug from an administered dosage form that enters the systemic circulation?
Bioavailability
What is necessary for a drug to produce its characteristic pharmacologic action?
Achieve adequate concentration at its site of action
What is a type of transport that requires energy?
Active transport
What is the term for the rate at which a drug appears in the bloodstream?
Absorption rate
Study Notes
Pharmacology and Biopharmaceutics
Crystalline Forms
- Crystalline forms of a substance can affect its properties and behavior
- Polymorphism is the ability of a substance to exist in different crystalline forms
Bioavailability
- Bioavailability is affected by the route of administration, with oral administration being a common route
- Subcutaneous and sublingual routes can also affect bioavailability
Drug Metabolism
- The liver is the principal site of drug metabolism
- Drug metabolism can result in more acidic or more polar compounds
- Gastric emptying can be slowed down by certain factors, including vigorous exercise, hot meals, and fatty foods
Drug Absorption
- Drug absorption is affected by factors such as particle size reduction, dissolution rate, and solubility
- The ratio of the concentration of a drug in two immiscible phases is known as the lipid/water partition coefficient
- Pre-requisites for drug absorption include the drug being in an aqueous solution, except in certain absorption mechanisms
Pharmacokinetics
- Bioavailability is the relative amount of drug that enters the systemic circulation and the rate at which it appears in the bloodstream
- Volume of distribution is the ratio of the amount of drug present in the body to its plasma concentration
- Intrinsic clearance, renal clearance, and metabolic clearance are all important pharmacokinetic concepts
Enzymes and Drug Interactions
- Zymogens are inactive enzymes that can be activated to form active enzymes
- Enzymes can affect drug metabolism and interactions
- Certain ions and electrolytes can affect drug solubility and hydration
Pharmaceutical Equivalents and Alternates
- Pharmaceutical equivalents are drug products that contain the same therapeutic moiety, but not necessarily in the same amount or dosage form
- Pharmaceutical alternates are drug products that contain the identical therapeutic moiety, or its precursor, but not necessarily in the same amount or dosage form
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