N301 Pharmacology Drexel Ace

What is pharmacokinetics?
study of drug movement through the body

What are the 4 elements of Pharmacokinetics?
absorption, distribution, metabolism, excretion

What are the 3 ways a drug can cross a membrane?
through channels or pores, aided by a transport system, direct penetration of membrane

What 6 things effect absorption
Rate kid dissolution, surface area, blood flow, lipid solubility, pH partioning, route of administration

What is absorption
Movement of the drug from the site of administration into the blood

Advantages of IV administration?
Rapid onset, control of level of drug, ability to administer large volumes of fluid

What is enteral absorption?
Using GI tract

Advantages of IM administration?
Good for mess with poor water solubility, used for depot administrations

Advantages of oral route?
Easy, convenient, safe

Disadvantages of oral route?
Variability of absorption

What is chemical equivalence?
Contains some amount of an identical compound

What is bioavailability?
2 drugs are equal in bioavailability if they are absorbed at same rate

What is distribution?
Movement of drugs throughout the body

What 3 factors effect distribution?
Blood flow, ability to exit the vascular system, ability of the drug to enter the cells

What 2 pathologic conditions create low blood flow that affects drug distribution?
Abscesses and solid tumors

What 3 ways can drugs exit the vascular system?
Blood brain barrier, placenta, protein binding

What is drug related metabolism?
The enzymatic alteration of drug structure

Where does most metabolism take place?
The liver

What hepatic enzyme metabolizes drugs?
Cytochrome P450

What are the 5 therapeutic consequences of drug metabolism?
Accelerated renal excretion, drug inactivation, increased therapeutic action, activation of prodrugs, changes in toxicity.

What is “first pass effect?”
Rapid inactivation of some oral drugs as they pass through the liver. Little drug is left to work. Parenteral admin bypasses this effect

What is parenteral absorption and the 3 types?
Outside of GI tract, IV, IM, subQ

What are 5 special considerations regarding drug metabolism?
age, induction or inhibition of drug metabolizing enzymes, first pass effect, nutritional status, competition between drugs.

what is excretion?
the removal of drugs from the body

What are the 5 routes of drug excretion?
kidneys (renal) breast milk, bile, lungs, sweat/saliva

What is the main route of excretion?
The kidneys

what 2 factors modify renal drug excretion?
pH-dependent ionization and competition for active tubular transport. alkaline urine can be used to pull acidic drugs out of the body faster.

what is pharmacodynamics?
The study of biochecmical and physiologic actions of drugs and the molecular mechanisms by which effects are produced.

What is maximal efficacy?
largest effect that a drug can produce

what is Relative potency?
the amount of drug given to elicit an effect

What is drug affinity, and how does it effect potency?
the strength of attraction between a drug and its receptor. Higher affinity drugs have a stronger attraction to receptor sites and are more potent.

What is intrinsic activity?
ability of a drug to activate a receptor upon binding. high intrinsic activity leads to high maximal efficacy and intense response

What do agonists do? do they have high or low affinity and intrinsic activity?
mimic endogenous regulators and activate receptors. They have high affinity and high intrinsic activity

What do antagonists do? do they have high or low affinity and intrinsic activity?
block endogenous regulators. high affinity but no intrinsic activity. bind to receptors but do not activate them.

How do noncompetitive antagonists work?
bind irreversibly to receptors, decrease total number of receptors available for binding

How do competitive antagonists work?
block receptors by competing with agonists. If both have equal affinity the receptor will be occupied by whatever has the higher concentration.

What is a partial agonist?
agonist with moderate intrinsic activity. produces less effect than full agonist.

What is receptor desensitization?
Also called refractoriness. cell is less responsive due to continuous exposure of cell receptors to agonist

What is receptor hypersensitivity?
results from continuous exposure of receptors to antagonists

Give 3 examples of drug responses that occur without receptors.
antacids, saline laxatives, chelating agents (bind with poisons)

What does ED50 mean / stand for?
average effective dose. dose required to produce a defined therapeutic response in 50% of the population.

what does ED50:LD50 mean?
therapeutic index, the ratio between the average effective dose and the average lethal dose. Wide is relatively safe.

what are the 3 possibilities of drug-drug interactions?
one drug intensifies the effects of the other (potentiative), one drug reduces the effects of the other (inhibitory), the combination produces a new response seen with either drug alone.

What timing is carsickness for meds that say to take on empty stomach, or to take with a meal?
1 hour before or 2 hours after meals. with a meal, take within 2 hours of eating

what is the grapefruit juice effect and how long can it last?
grapefruit juice inhibits an isoenzyme needed for intestinal metabolism of many drugs. can increase or decrease amount of drug available for use. can last up to 3 days.

Define bioavailability
Amount of active drug that reaches systemic circulation from its site of administration. Different forms of drug can have different bioavailability, primarily in oral preparations. Highest concern in drugs with narrow therapeutic range

Absorption refers to the movement of drug into the bloodstream, with the rate dependent on the physical characteristics of the drug and its formation. Refers to the passage of drug molecules from the site of administration into the circulation. Active …

Dose response curve shows the relationship between the drug response and the dose Free drug compared to drugs that are protein bound, molecules that can produce a pharmacologic effect WE WILL WRITE A CUSTOM ESSAY SAMPLE ON ANY TOPIC SPECIFICALLY …

EC50 the drug concentration giving 50% maximal effect (not binding affinity – the magnitude of a drug effect is not proportional to the proportion of receptors occupied by that drug) a drug with a lower EC50 is more potent (half …

systemic dose relationship has two components: Dose – Plasma concentration relationship -Determined by pharmacokinetics parameters of drug (half life, clearance, volume of distribution) Plasma Concentration – Response relationship -Can be studied using in vitro studies How to Determine a Dose- …

What does it mean that DR interactions are concentration dependent? It means that as the concentration of the drug increases the % of receptors bound increases What does it mean the DR interactions are saturable? At a certain concentration 100% …

Pharmacology The study of substances that interact with living systems through chemical processes, especially by binding to regulatory molecules and activating or inhibiting normal processes Pharmacokinetics “the body’s effects on the drug” Changes in plasma drug concentration over time WE …

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