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74 Cards in this Set

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On the log enzyme kinetics graph, y-intercept is equal to?
1/Vmax
The lower the Km,
the _____ the affinity.
higher
On the log kinetics graph:
Competitive inhibitors cross each other competitively.
T/F
T
They all cross on 1/Vmax
On the log kinetics graph:
Noncompetitive inhibitors do not cross each other.
T/F
T
they have different Km's
Vd = ?
amt of drug in body /
plasma drug concentration
t1/2 = ?
0.7 * Vd / clearanc
A drug infused at a constant rate reaches about 94% of steady state after x half-lives?
x = 4
Loading dose = ?
Cp * Vd/F

Cp = target plasma conc.
F = bioavailability: =1 per IV
Phase 1 metabolism involves?

yields?
reduction, oxidation, hydrolysis
cytochrome P450
yields slightly polar, still-active water-soluble metabolites
Geriatrics lost this first
Phase 2 metabolism involves?

yields?
acetylation, glucuronidation, sulfation, conjugation
yields very polar, inactive metabolites
Potency = ?
Efficacy = ?
Potency = amt needed for a given effect

Efficacy = maximal effect
Therapeutic index =
TD50 /
ED50

(median toxic dose /
median effective dose)
Skeletal Muscle.
N or M?
neurotransmitter?
N
ACh
PNS: Cardiac & Smooth Muscle, gland cells.
N or M?
neurotransmitter?
N-------M (2 neurons)
Ach Ach
All sympathetic @ ganglion.
N or M?
neurotransmitter?
N
ACh
Sympathetic 2nd neuron @ sweat glands:
N or M?
neurotransmitter?
M
ACh
Sympathetic @ cardiac and smooth muscle, gland cells, nerve terminals

neurotransmitter?
NE @ alpha or beta
Sympathetic at Renal vascular smooth muscle

receptor??
D1
Sympathetic @ adrenal medulla

N or M?
neurotransmitter?
N, ACh
G-protein-linked 2nd messengers:
α1 ->

G-prot class?
functions?
q
↑vascular smooth muscle contraction
G-protein-linked 2nd messengers:
α2
i
↓sympathetic outflow
↓insulin release
G-protein-linked 2nd messengers:
β1
s
↑HR, ↑contactility
↑renin release
↑lipolysis
↑aq. humor formation
G-protein-linked 2nd messengers:
β2
s
vasodilation, bronchodilation
↑glucagon release
G-protein-linked 2nd messengers:
M1
q
CNS
G-protein-linked 2nd messengers:
M2
i
↓HR
G-protein-linked 2nd messengers:
M3
q
↑exocrine gland secretions
G-protein-linked 2nd messengers:
D1
s
relaxes renal vascular smooth muscle
G-protein-linked 2nd messengers:
D2
i
modulates transmitter release, esp in brain
G-protein-linked 2nd messengers:
H1
q
↑nasal/bronchial mucus
bronchconstriction
pruritis
pain
G-protein-linked 2nd messengers:
H2
s
↑gastic acid secretion
G-protein-linked 2nd messengers:
V1
contracts vascular smooth muscle
G-protein-linked 2nd messengers:
V2
↑H20 permeability & reabsorption in the collective tubules
HAV 1 M&M

G-prot class?
cell signals?
H1A1V1 M1M3
Gq → Phoslipase C → PIP2 → ↑Ca ⇉
IP3 → inc Ca
DAG → PKC
BB DOne I HV2

G-prot class?
cell signals?
B1, B2, D1, H2, V2
Gs → adenylcyclase → ↑cAMP → pkA
MAD2's
M2, A2, D2
Gi → adcyclase → ↓cAMP → ↓pkA
Guanethidine
decreases NE release
Metyrosine
decreases DOPA formation from tyrosine
Reserpine
inhibits reuptake of NE; causing its depletion
Amphetamine
blocks DOPA transporter reuptake; in addition causes DA reflux
primary reinforcing and behavioral-stimulant effects are linked to enhanced dopaminergic activity in the mesolimbic DA system
Bethanechol

clin?
action?
cholinomimetic direct agonist
clin: postop & neurogenic ileus & urinary retention
action: activates Bowel & Bladder smooth muscle; resistant to AChE
Carbachol

clin?
action?
Cholinomimetic direct agonist
clin: glaucoma, pupillary contraction, & release of intraocular pressure
act: contracts ciliary muscle of eye (open angle), pupillar sphincter (narrow angle); resistant to AChE
Pilocarpine
cholinomimetic direct agonist
potent stimulator of sweat, tears, saliva
Methacholine
cholinomimetic direct agonist
challenge test for dx of asthma
stimulates muscarinic receptors
Neostigmine
cholinomimetic indirect agonist
clin: postop & neurogenic ileus & urinary retention, myasthenia gravis, reversal of nueromuscular junction blockade(postop)
act: ↑endogenous ACh; no CNS penetration
Pyridostigmine
cholinomimetic indirect agonist
myasthenia gravis, increases strength
act: ↑endogenous ACh; no CNS penetrance
Edrophonium
cholinomimetic indirect agonist
dx of Myasthenia G (extremely short acting)
act: ↑endogenous ACh;
Physostigmine
cholinomimetic indirect agonist
glaucoma (crosses BBB to CNS) and atropine OD
act: ↑endogenous ACh;
Echothiophate
cholinomimetic indirect agonist
glaucoma
act: ↑endogenous ACh;
Cholinesterase inhibitor poisoning symptoms:
antidote?

DUMBBELSS
Diarrhea
Urination
Miosis
Bronchospasm
Bradycardia
Excitation of skeletal muscle and CNS
Lacrimation
Sweating
Salivation (also abd cramps)

ANTIDOTE: atropine (muscarinic antagonist) plus pralidoxime (chemical antagonist used to regenerate active cholinsterase)
homatropine
tropicamide
atropine
cholinoreceptor blockers
produces mydriasis & cycloplegia
Benztropine
cholinoreceptor blockers
parkinson's dz (2nd line)
Scopolamine
cholinoreceptor blockers
motion sickness
Ipratropium
cholinoreceptor blockers
Asthma, COPD
Methscopolamine,
oxybutin,
glycopyrrolate
cholinoreceptor blockers
reduces urgency in mild cystitis and reduces bladder spasms
Glaucoma
epinephrine

mech?
tox?
mech: alpha agonist
↑outflow of aqueous humor

SE:
mydriasis, stinging, DO NOT USE IN CLOSED-ANGLE GLAUCOMA
Glaucoma
brimonide

mech?
tox?
mech: alpha agonist
↓aqueous humor synth

SE: no pupillary or vision changes
Glaucoma
betaxolol, timolol, carteolol

mech?
tox?
mech: beta-blocker
↓aqueous humor secretion

SE: no pupillary or vision changes
Glaucoma
Acetazolamide

mech?
tox?
mech: diuretic
↓aqueous humor secretion via inhibition of carbonic anydrase

SE: no pupillary or vision changes
Glaucoma
pilocarpine, carbachol, physostigmine, echothiophate

mech?
tox?
mech: cholinomimetic
↑outflow of aqueous humor; contracts ciliary muscle -->
opens trabecular meshwork
use pilocarpine in emergencies as it is very effetive at opening canal of Schlemm

SE: miosis, cyclospasm
Glaucoma
Latanoprost

mech?
tox?
mech: prostaglandin
↑outflow of aqueous humor;

tox: darkens color of iris (browning)
ATROPINE

uses?
Muscarinic antagonist

EYE: ↑pupil dilation, cycloplegia
AIRWAY: ↓secretions
Stomach: ↓acid secretion
Gut: ↓motility
Bladder: ↓urgency in cystitis

BLOCKS SLUD:
Salivation
Lacrimation
Urination
Defecation
ATROPINE

tox?
TOX:
↑body temp; rapid pulse; dry mouth; dry, flushed skin; cycloplegia; constipation; disorientation

can cause acute angle-closure glaucoma in elderly, urinary retention in men w/prostatic hypertrophy, and hyperthermia in infants
Hot as a...
Hot as a hare
Dry as a bone,
red as a beet,
blind as a bat
mad as a hatter
Hexamethonium
mech: nicotinic ACh receptor antagonist
clin: ganglionic blocker. Used in exp models to prevent vagal reflexz response to changes in BP--e.g. prevents reflex bradycardia caused by NE
Sympathomimetic selectivity
Epi
α₁ α₂ β₁ β₂
low doses selective for β₁

uses: anaphylaxis, glaucoma(open angle), asthma, hypoTN
Sympathomimetic selectivity
NE
α₁ α₂ > β₁
↑SBP, DBP --> reflex bradycardia

clin:
hypoTN(but ↓renal perfusion)
Sympathomimetic selectivity
Iso
β₁=β₂ > α₁ α₂
↓SBP, DBP
↑HR

clin: AV block (rare)
Sympathomimetic selectivity
Dopa
D1=D2 > β₁ β₂ > α₁ α₂

clin:
shock(increases renal perfusion), HF
Sympathomimetic selectivity
Dobu
α₁ α₂ β₁ β₂
Phenoxybenzamine (irrev)
phentolamine (rev)
nonsel. α-blocker

clin: pheochromocytoma
tox: orthostatic HTN
reflex tachycardia
Prazosin, terazosin, doxazosin
α₁ selective

clin: HTN, BPH
tox: 1st dose orthoHTN, dizziness, headache
Mirtazapine
α₂ selective

clin: depression
tox: sedation, ↑serum chol, ↑appetite
olol's

clin & tox?
Beta-blockers
HTN: ↓CO, ↓renin secretion
Angina: ↓HR/contractility, resulting in ↓O2 use
MI: ↓mortality
SVT: ↓AV conduction velocity
CHF: slows progression of CHF
Glaucoma (timolol): ↓aq humor secretion

TOX: impotence, exacerabtion of asthma, CV adverse effects, CNS adverse effects
olol's

non selective & selective(A BEAM of b1 blockers)?
nonselective: propranolol, timolol, nadolol, pindolol (partial agonist), labetalol (partial agonist)
Beta1 selective: Acetbutolol (partial), betaxolol, Esmolol (short acting), Atenolol, Metroprolol