Pharm Flashcards
Km
inversely related to the affinity of the enzyme. Km = [S] at 1/2Vmax
if Km is bigger, means the enzyme doesn’t bind as well to the substrate, since you need more enzyme to achieve 1/2 max velocity
how long does it take for a drug infused at a constant rate to reach steady state?
4-5 half-lives
half-life equation
(0.693 x Vd) / CL
Clearance
volume of plasma cleared of drug / time
rate of drug elimination / plasma drug concentration = Vd X elimination constant
loading dose
(target plasma concentration x volume of distribution) / (bioavailability)
maintenance dose
(Cp x CL x dosage interval) / bioavailability
zero-order elimination + examples
rate of elimination constant, regardless of time. Cp dec. linearly w/ time.
Phenytoin, Ethanol, Aspirin
1st order elimination
constant fraction drug eliminated per unit time
competitive antagonist + example
1) dec. potency, but doesn’t change efficacy (shift right)
ex: diazepam + flumazenil
noncompetitive antagonist + examples
dec. efficacy –> shift curve down
ex: norepinephrine + phenoxybenzamine (note: phenoxy = irreversible competitive antagonist)
partial agonist
acts at same site as full agonist. lower efficacy –> shift down
morphine vs. buprenorphine
Nictoinic vs. muscarinic AcH receptors
1) nicotinic = ligand-gated Na/K channels
2) muscarinic = G-protein coupled receptors w/ 2nd messengers
Parasympathetic
1) cardiac + smooth muscle, gland cells, nerve terminals (muscarinic; M2 = cardiac, M3 = everywhere else)
Sympathetic innervation
1) sweat glands (muscarinic)
2) cardiac / smooth muscle: NE on alpha/beta
3) renal vasculature: D1 / D2
a1
incr:
- vascular smooth muscle
- pupillary dilator contraction
- intestinal / blader sphincter contraction
a2
dec:
- symp. outflow
- insulin release
- lipolysis
incr:
-platelet aggregation
b1
incr:
- HR
- contractility
- renin release
dec. :
- lipolysis
b2:
vasodilation, bronchodilation.
incr. :
- HR
- contractility
- lipolysis
- insulin release
- aqueous humor
dec. :
- uterine tone
M1
CNS / enteric nervous system
M2
dec. HR / atrial contraction
M3
incr:
- exocrine gland secretions (lacrimal, salivary, gastric acid)
- gut peristalsis
- bladder contraction / bronchoconstriction
- pupillary sphincter contraction
D1
renal vascular smooth muscle
D2
modulates transmitter release in brain
H1
incr:
- nasal / bronchial mucous production
- vascular permeability
contraction of bronchioles, pruritis, pain
H2
incr:
-gastric acid secretion
V1
Incr. vascular smooth muscle contraction
V2
incr. H2O permeability + reabsorption in collecting tubules of the kidney
Gq downstream
phospholipase C –> Dag:
1) protein kinase C
2) IP3 –> incr. ca2 –> smooth muscle contraction