Principles of Pharmacology
9 important questions on Principles of Pharmacology
Define ‘pharmacokinetics’ and list the 4 phases of the pharmacokinetic route through the body.
- ● = the movement of drugs in the body.
- ● Absorption, distribution, metabolism,. excretion.
- Define ‘pharmacodynamics’ and state 3 topics that are treated under the heading of pharmacodynamics.
- ● = the study of the biochemical and physiological effects of drugs on the body.
- ● Affinity (= the STRENGTH of binding between a drug and its receptor)
Efficacy (= the degree to which a drug is able to induce max. effects),
Potency (= the amount of drug required to produce 50% of the max. response that the drug is capable of inducing).
- What makes a molecule hydrophilic, and what makes it lipophilic?
- ● A hydrophilic molecule is one that is typically charged/polarized and capable of hydrogen bonding.
- ● A lipophilic molecule is one that is typically noncharge/polarized and not capable of hydrogen bonding.
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- State 3 pharmacokinetic differences between hydrophilic and lipophilic molecules.
Membrane permeability/fat tissue storage (l), brain barrier permeability (l), kidneys excretion (h), metabolism/biotransformation (h).
What is the practical (clinical) relevance of the solubility of drug molecules?
● Hydrophilic drugs:
Hardly permeate membranes, except when there are:
Aqueous channels.
Carriers.
- ○ Hardly reach brain.
- ○ Easily excreted by kidney.
● Lipophilic drugs:- ○ Are ‘slippery’ >> pass membranes easily.
- ○ Reach brain well.
- ○ May accumulate in fatty tissue or lungs.
- ○ Hard to remove from body >> need biotransformation to increase polarity.
- ○ Are ‘slippery’ >> pass membranes easily.
- Which drugassociated factors influence absorption? What type of molecule is most readily absorbed?
- ● Drugassociated factors that influence absorption:
- ○ ionization state.
- ○ solubility (lipophilicity).
- ○ molecular weight.
- ○ formulation (solution vs. tablet).
- ○ ionization state.
- ● In general, absorption is better with: lipophilic molecules, nonionized state, low molecular weight, high degree of dispersion.
- Which patientassociated factors influence absorption? Give at least 2 examples.
- ● Presence of food in the GI tract.
- ● Stomach acidity and blood flow to the GI tract.
- Give a short description of the following mechanisms of drug transport across membranes: passive diffusion; facilitated diffusion; active transport.
- ● Passive diffusion: no energy, no carrier, lipophilic/nonionic/small molecules favored.
- ● Facilitated diffusion: no energy, with carrier, drugs bind to carrier by noncovalent mechanisms, competition for carrier between chemically similar drugs.
- ● Active transport: with energy, with carrier, identical to facilitated diffusion except that ATP powers drug transport against concentration gradient.
What are ‘aqueous channels’ and which type of transport do they subserve?
● Aquaporin = protein membrane channel through which water can diffuse.
● Porins are proteins that cross a cellular membrane and act as a pore through which molecules can diffuse. They are large enough to allow passive diffusion.
● Aqueous channels: no energy, no carrier, small hydrophilic drugs diffuse along concentration gradient by passing through aqueous channels (pores).
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