Pharmacology Flashcards
It describes the actions of a drug on the body
and the influence of drug concentrations on the
magnitude of the response
Pharmacodynamics
It act as signals
Drugs
It act as signal detectors
Receptor
It is responsible for selectivity of
drug action
Receptor
Receptors mediate the actions of pharmacologic __ and ___
Agonists and
antagonists
What does the Agonist do to the ureter? It acts as…
Diuretic
What does the Antagonist do to the ureter? It acts as…
Antidiuretic
What does Inverse Agonist do to the brain?
Depress CNS
What does Inverse Agonist do to the brain?
Stimulating the
negative response
Gs activates what?
Adenylyl cyclase
Gs increases what?
Increase cAMP
Gi inhibits what?
Adenylyl cyclase
Gi decreases what ?
cAMP
Gq activates…
Phospholipase C
Gq increases…
IP3, DAG, and Calcium
What is cAMP?
Cyclic adenosine monophosphate
What is DAG?
diacylglycerol
What is IP3?
Inositol triphosphate
De-phosporylation results to…
Relaxation
Actions of effector molecules
Interplay among signaling
mechanisms
powerfully amplifies the initial regulatory signal by recording a molecular memory that the pathway has been activated
Phosphorylation
erases the memory, taking a longer time to do so than is required for dissociation of an allosteric ligand
De-phosphorylation
It is a measure of the amount of drug necessary to produce an effect of a given
magnitude
Potency
The concentration of drug producing 50% of the maximum effect (EC50) is usually used to determine potency
EC50
magnitude of response a drug causes when it interacts with a receptor
Efficacy
dependent on the number of drug–receptor complexes formed and the intrinsic activity of the drug
Efficacy
ability to activate the receptor and cause a cellular response
Intrinsic activity
refers to the movement of drug into, through, and out of the body
Pharmacokinetics
Transfer of a drug from the site of administration to the bloodstream
Absorption
ADME
Absorption
Distribution
Metabolism
Excretion
Absorption of acidic drugs occur in the…
Stomach
Absorption of basic drugs occur in the…
Small intestine
LUNA
Lipophilic
Nonpolar
Unionized
Absorption
Ionized Drugs are..
Water Soluble and Polar
The process in which an atom/molecule acquires a positive/negative charge by losing or gaining electrons
Ionization
Unionized Drugs
Lipid soluble and Nonpolar
the adding of a proton
Protonation
Form if pH is less than pKa
drugs are in protonated forms
Acidic protonated drugs are found in what organ?
Stomach
Form if pH is greater than pKa
drugs are in deprotonated forms
High vascularized organs (3)
Brain, Heart, and Liver
Factors affecting Distribution
Capillary Permeability
Protein Binding
Lipohilicity
Basic deprotonated drugs are found in what organ?
Small intestine
actors affecting Distribution
Volume of Distribution
Types of Capillaries
Continuous, Fenestrated and Discontinuous
Continuous
Fat
muscle
nervous system
Fenestrated
Kidney glomeruli
intestinal villi
endocrine glands
Discontinuous
Liver
bone marrow
spleen
Drugs should be ___ enough to pass
Small
Protein Binding results to
Inhibition of distribution
Lipophilic drugs can…
Readily cross membranes
Blood flow affects its
distribution
Formula in determining Volume of Distribution
Vd = dose/Plasma conc.
Hydrophilic drugs do not readily ______
Penetrate membranes
What happens to the concentration in the tissue if the Vd is high
Increases
Effect of Vd on Drug half life
Increase Vd = Increase half life
Goal of Metabolism
to degrade and water solubility
What happens to the metabolism of the drug if it binds with CYP450
Degrades
What are the 2 phases of Metabolism
Phase 1: Functionalization
Phase 2: Conjugation
Reactions that occurs in Phase 1
Oxidation
Reduction
Hydrolysis
Reactions that occurs in Phase 2
Glucuronidation
Sulfation
Methylation
Acetylation
GSH conjugation
Glycine conjugation
7 Enzyme Inducers
Carbamazepine
Rifampicin
Alcohol
Phenytoin
Griseofulvin
Phenobarbital
Sulfonylureas
12 Enzyme Inhibitors
Sodium valproate
Isoniazid
Cimetidine
Ketoconazole
Fluconazole
Alcohol & grapefruit juice
Chloramphenicol
Erythromycin
Sulfonamides
Ciprofloxacin
Omeprazole
Metronidazole