Midterm Flashcards
Term for the chemical forces that cause drug to associate with receptor.
affinity
Term for chemical structure (nature) or a drug that causes the receptor to change when the drug is bound.
Efficacy (intrinsic activity)
What is the equation for standard safety margin?
LD1/ED99
What is the equation for therapeutic index?
LD50/ED50
What is used instead of therapeutic index for non lethal drugs?
Therapeutic ratio: Toxic conc/Effective conc
Molecule that associates and dissascoiates freely and competes with an agonist ppresent for available binding sites?
competitive antagonist (reversible)
Molecule that binds more aggressively and do not disassociate freely. Receptors are unavailable for competitive binding to agonist molecules.
Irreversible antagonists (non-competitive)
What type of antagonism is when two drugs, an agonist and an antagonist bind to the same receptor?
receptor antagonism (pharmacological)
What type of antagonism inolves receptors in opposing systems simultaneously?
physiologic antagonism (functional)
What type of antagonism is when a drug forms bonds with 2 or more molecules?
chemical antagonism
What is the term for acute diminished response in an organ after repeated exposure to an agonist?
tachyphylaxis
What is pharmacokinetics?
quantitative study of the time course of drug absorption, distribution, metabolism, and excretion (What body does to drug)
What is pharmacodynamics?
what drug does to body
Liquid oral dosage form that is in aqueous suspensions.
magmas
What is the injectable drug form that is to be reconstituted with sterile water ust priior to admin?
lyophilized form
What injectable drug form is designed to use IM or SQ and absorption is prolonged?
repository
What are the 3 factors for absorption of a drug IM and SC?
SA of capillaries, blood flow, and solubility in interstitial fluids
What pH are weak acids ionized at?
pH above their pKa
What pH are weak bases ionized at?
ionized at pH below their pKa
What are the 3 major reactions involved in phase 1 metabolism?
Oxidation, reduction, and hydrolysis
What major reaction is involved in phase 2 metabolism?
conjugation
What pharmacokinetic model is used if elimination mechanisms of a drug are saturated?
zero-order process (non linear kinetics)
What pharmacokinetic model is used to show the rate of transfer between compartments and elimination is proportional to drug in body?
first order or linear kinetics
What is the equation for volume of distribution?
Vd = IV dose/C0
What is the equation for biological half life?
t1/2 = 0.693/k
What is the equation for systemic clearance?
Cls = IV dose/AUC0-inf
What are the 2 choline esters?
carbachol and bethanechol
What 2 problems is bethanacol used to treat?
tx of urinary retiontion in cats and dogs and a prokinetic in horses
What are the side effects of choline esters?
SLUD - salivation, lacrimation, urination, defecation
What are the 3 naturally occuring cholinomimetic alkaloids?
pilocarpine, muscarine, arecoline
What are the 5 directly acting cholinomimetic drugs?
carbachol, bethanechol, pilocarpine, muscarine, arecoline
What are the 4 reversible anticholinesterases?
physostigmine, neostigmine, edrophonium, pyridostigmine
What group of drugs produces irreversibile inhibition of cholinesterase?
organophosphates
Which reversible anticholinesterase is used primarily orally?
pyridostigmine
Can reversible cholinesterase inhibitors treat nondepolarizing NM blockers or depolarizing NM blockers??
only nondepolarizing
not depolarizing due to SYNERGISM
What drug is used to diagnose myasthenia gravis in dogs and cats?
edrophonium
What 2 drugs are used to treat myasthenia gravis in dogs and cats?
neostigmine and pyridostigmine
What reversibile cholinesterase inhibitor is a topical miotic agent and reduces intraocular pressure?
physostigmine
What are organophosphate compounds treated with?
atropine (competitive antagonist to AcH)
What drug can dissosociate organophosphates with the AchE enzyme?
pralidoxime (2-pam, protopam)
Which species have a short half life of atropine?
rabbits and goats - have atropinase
What can atropine treat in the GI tract?
antispasmodic - GI hypermotility
When is atropine contraindicated in the eye?
KCS - decreased tear production
What drug is 2-4 times more potent than atropine but less likely to penetrate BBB?
glycopyrrolate
What antispasmodic and anticholinergic drug is used for IV in horses with colic?
N-butylscopolammonium bromide
What are the 2 synthetic catecholamines?
isoproterenol and dobutamine
What are the presnyaptic and postsynaptic actions of alppha 2 receptors?
pre- stops norepinephrine release
post - stimulates systemic vasoconstriction, platelet aggregation, etc
Where are beta 3 receptors found?
on adipocytes, mediates lipolysis