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55 Cards in this Set

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Zero order kinetics
Phenytoin, Ethanol, Aspirin (high dose)
First phase of metabolism to become deficient in elderly
Phase I
Phase of metabolism that lags in development in neonates/infants
Phase II
Spare R: Kd vs. EC50
EC50 < Kd
Vd =
dose / []p
CL =
rate of excretion / []p
t1/2 =
.7 * Vd/CL
Loading dose =
[]p * Vd / F
Maintenance dose =
[]p * CL / F
Therapeutic index =
TC50 / EC 50 = median toxic dose / median effective dose
Phase I Drug Development
Normal volunteers. Safe? Pharmacokinetics
Phase II Drug Development
Small patient sample. Vs. placebo. Efficacy? (and safety)
Phase III Drug Development
Larger patient sample. Vs. control drug. Double Blind. Efficacy? (and safety)
Phase IV Drug Development
Postmarketing surveillance
alpha 1
Q. vasoconstriction. Dec GU/GI motility. Gluconeogenosis/glycogenolysis.
alpha 2
I. dec sympathetic outflow. dec insulin release.
beta 1
S. inc (HR, contractility, AV conduction v), renin, lipolysis, aqueous humor.
beta 2
S. vasodilation, bronchodilation, glucagon relase.
M1
Q. CNS.
M2
I. Dec HR.
M3
Q. Exocrine glands.
D1
S. Renal vasodilation.
D2
I. Brain.
H1
Q. nasal/bronchial mucus, bronchioconstriction, pruritis, pain
H2
S. Gastric acid.
V1
Q. Vasoconstrction.
V2
S. Aquaporin in apical collecting tubules membrane.
IP3
Ca2+
DAG
PKC
Vesamicol
inh ACh => vesicle "vesamicol=>vesicle". ~ reserpine except for Ach
Hemicholinium
inh ACh reuptake
Reserpine
inh VMAT (N => vesicle). ~ vesamicol except for NE.
Cocaine
inh NET (and DAT, 5HTT). ~TCA
Guanethidine
Displace NE from vesicles. (Acute: indirect sympathomimmetic. Chronic: dec NE signaling).
Bethanechol
Muscarinic agonist. Bladder + Bowel (postop + neurogenic ileus. ~neostigmine but diff mech).
Carbachol
Muscarinic agonist. AChE R. Glaucoma
Pilocarpine
Muscarinic agonist. AChE R. Glaucoma
__stigmine
AChE inh
Neostigmine
AChE inh. Neo = fresh out of Op: Bowel + bladder (Postop, neurogenic ileus), rev NMJ block. MG.
Pyridostigmine
AChE inh. MG.
Edrophonium
AChE inh. Dx MG (short)
Physostigmine
AChE inh. Glaucoma. CNS. Atropine poisoning. "ph-eye-sostigmine"
Echothiophate
Ach inh. Glaucoma. "Echoth-eye-ophate"
__tropine
~atropine
Atropine
ACh antagonist. Mydriasis, cycloplegia.
Homatropine
ACh antagonist. Mydriasis, cycloplegia. "_tropine"
Tropicamide
Ach antagonist. Mydriasis, cycloplegia. "atropine drops/trops"
Benztropine
ACh antagonist. CNS. parkinson's dz (reduce pinrolling tremor). "_tropine"
Scopalamine
M ACh antagonist. CNS. motion sickness.
Isatropium
M ACh antagonist. Respiratory: asthma, COPD.
Methscopalamine
M ACh antagonist. GU. dec urgency in mild cystitis, dec bladder spasms. ~ oxybutin, glycopyrrolate
Oxybutin
M ACh antagonist. GU. dec urgency in mild cystitis, dec bladder spams. ~ methscopalamine, glycopyrrolate.
Glycopyrrolate
M ACh antagonist. GU. dec urgency in mild cystitis, dec bladder spams. ~ methscopalamine, glycopyrrolate.
Atropine tox
Acute angle-closure glaucoma in elderly. Urinary retention in BPH. Hyperthermia in infants.
Hexamethonium
Nicotinic AChR antagonist (ganglions too). Research animals.