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