Pharmacology prelim Flashcards
it is THE STUDY OF DRUGS
pharmacology
articles USED IN PREVENTION, DIAGNOSIS, MITIGATION, CURE, AND TREATMENT OF DISEASE
drugs
what the drug does to the body/ effects of human body
pharmacodynamics
study of processes a drug undergoes as it reaches and leaves the site of action
pharmacokinetics
- integration of PD and PK
- study of the RATIONAL USE OF DRUGS in the management of diseases
- study of the physiologic and biochemical effects of drugs in the living systems
pharmacodynamics
biological sites of action or active sites
target protein mediated
made of alpha and beta tubulin
functions: keep organelles in place and axonal transport/release of neurotransmitter
microtubules
it is a CELL MOVEMENT
chemotaxis
medicine for ANTIFUNGAL
griseofulvin
treatment for INFECTION OF SKIN AND APPANDAGES
dermatomycosis
inhibition of cell division of fungal cell
MOA
absorption is increased by?
fatty foods
stimulate metabolism of another drug if they combine together
enzyme inducer
Colchicine is a medicine for?
acute gout and chronic gout with allupurinel
inhibits movement of inflammatory cells to immune cells
MOA: inhibit chemotaxis
what are the 3 mitotic spindle inhibitors/antimitotics?
- Vincas (perwinke plants)
- vincristine
- vinblastine
- vinorebline
- vindesine - taxanes (bark pacific new tree)
- pclitaxel
- docetaxel
- cabazitaxel - estramustine
what are the REGULATORY PROTEINS?
- channel
- enzymes
- carriers
- receptors
detect changes in the environment
channel (voltage gated)
Voltage gated sodium channels inhibited by CLASS 1 ANTIARRHYTHMIC CHANNELS
IA
IB
IC
prolong the action potential
IA
disypramide guideline procainamide
IA
shortens the action potential
IB
tocainide, mexiletine, lidocraine, pheytoxin
IB
no effect on the action potential
IC
maritizin, fleanide, propaferone, encainide
IC
LOCAL ANESTHETICS
- ester type; amide type 2 ii - liducaine
iii - procraine
anticonvulsants
- phenytoin, carbamazepine
voltage gated potassium channels inhibited by CLASS 3 ANTIARRHYTHMIC DRUGS and SULFONYLUREAS (for type 2 DM)
class 3 - amiodarone, bretylium, sotanol, donederone, ibutilide, dofetelide
sulfonylureas - glibenclamide, glipizide, chlorproramide
calcium channel blockers
dihydropyridines (dhps) - ex; amlodopine, nicardipine, nifedapine
important for CONTRACTION/DEPULIRIZATION
NAT sodium
anti-inflammatory drugs
NSAIDS
ex; mefenamic acid, ibuprofen, aspirin
anti-platelet clotting
aspirin
reversible inhibitor of MAO
Moclubemide
selective MAO inhibitor
selegiline and rosagiline
non-selective MAO inhibitor
Phenelzine
Isocarbozacid
Tranylcypromine
antibacterial with MAO blocking effect
linezolid
drug for partensons
tolcapone
entacapone
cell membrane proteins with specific binding sites that undergo conformational change
carriers
drug for heart failure
- failure of the heart to contract
digoxin
increase force/strength of contraction
inotropism
decrease heart rate
chronotropism
decrease conduction velocity through the atrioventricular (AV node)
dromotropism
a typical ANTI-PYSYCHOTIC
aripiprazole
functional macromolecular cell components with specific stereochemical configuration with which a ligand interacts usually in a lock and key fashion
receptors
any substance that binds to a receptor
ligand
associated with ligand-gated ion channels
location; cell membrane
type 1 (Ionotropic) receptor
inhibitory neurotransmitter
GABA
increase frequency of chloride channel opening
benzodiazepines
increase duration of chloride channel opening
barbiturates
its effects is INCREASE/DECREASE concentration of metabolites
type 2 (metabotropic) receptor
types of G proteins
ADREGENERIC
1. Gq- alpha 1 - contraction
2. Gi - alpha 2 - decrease camp
3. Gs - beta 1 - increase pump
4. Gs - beta 2
5. Gs - beta 3
MUSCARMIC
1. Gq - meta 1
2. Gi- meta 2
3. Gq - meta 3
it is a SECONDARY MESSENGER
CAMP
- stimulation of glucokinase
- translocation of glucose transporters into the cell membrane
type 3 enzyme linked/ insulin receptor (tyrosine kinase)
properties of solutions dependent on the number of solute particles
colligative properties
for heavy metals poisoning
chelation
ability of drug to bind to a receptor
affinity
constitutive activity of the receptor. reducing pharmacologic effects
intrinsic activity
types of ligands based on the effect on intrinsic activity of the receptor
- agonist
- antagonist
- inverse agonist
binds to the receptor, produce effects. -
-increase activity
agonist
binds to the receptor, blocking the effect
- no activity
antagonist
anti- histamine drug
antagonist
a site other than the agonist binding site
allosteric activity
enhances agonist binding
- it will adjust to fit the agonist
allosteric agonist
inhibits against binding
allosteric antagonist
produce the maximal effects/ full spectrum of effects associated with the receptor
full agonist
produces some of the effects associated with the receptor
partial agonist
aka: mixed agonist-antagonist
produces opposite effects by binding to the SAME RECEPTOR
pharmacologic antagonist
produces opposite effects by binding to the DIFFERENT RECEPTOR
physiologic antagonist
temporary bond (noncovalent)
NMT 24 hours
ex. organophosphate nerve gasses
reversible
permanent bond (covalent)
24 hours
irreversible
effect CAN BE FULLY OVERCOME by increasing agonist concentration
ex. morphine analgesic
competitive/ surmountable
effect CANNOT BE FULLY OVERCOME by an increasing agonist concentration
noncompetitive/ insurmountable
maximum achievable response
efficacy/ceiling effect
smallest dose that produces the maximum response
ceiling dose/limit dose
dose that produces 50% of the efficacy
ex. cologne
potency
degree of change in response with a change in the dose
midslope
a slight change of dose will produce dramatic change
steeper
dose that produces the BENEFICIAL OUTCOME in 50% of the study population
ED50 - median effective dose
dose that produces the TOXIC OUTCOME in 50% of the study population
TD50 - median toxic dose
measure of relative safety
- the higher the TI, the safer the drug
therapeutic index
pharmacokinetics process
- transport process
- liberation
- absorption
- distribution
- metabolism
- excretion
mechanism of drug movement across the cell membrane
basic requirement - drug in aqueous solution
transport process
release of a drug from the dosage form
liberation
breaking of solid
disintegration
from solid to solution
dissolution
physiologic rate and extent of disappearance of a drug from the site of administration
absorption
energy requiring or ATP
- agonist a concentration gradient
- low to high concentration
active transport
non energy requiring
- a long a concentration gradient
- vitamin b12
facilitated transport
preparation for passive diffusion
- for large ions
ion-pair transport
drug passes through water-filled pores
- movement is through solvent drug
convective transport
-vesicle mediated
- vitamin ADEK, Griseofulvin