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168 Cards in this Set
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What is Km?
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then conc. of the substrate at which enzyme is at 1/2Vmax
reflects the affinity of an enzyme for it's substrate |
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Which has higher affinity, a low or high Km?
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lower Km = higher affinity
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What does a non-competitive inhibitor do to the enzyme's kinetics?
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It decreases the enzyme's Vmax but doesn't affect it's affinity for substrate (Km unchanged)
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What does a competitive inhibitor do to the enzyme's kinetics?
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It decreases the enzyme's affinity for substrate (bigger Km) but the Vmax stays the same
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What do competitive antagonists do to the pharmacodynamics?
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Decrease potency
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right shit on curve - more agonist needed to achieve same effect |
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What do non-competitive antagonists do to the pharmacodynamics?
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Decrease efficacy
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down shift on curve. lower maximum effect of agonist |
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What is volume of distribution (Vd)?
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amt of drug deliver (mg)/conc. in blood (mg/L)
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units are in L |
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What is a low Vd?
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~4L-8L ==> indicates most of the drug stayed in the blood
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what is the formula for half-life?
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(0.7xVd)/CL
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What is the formula for loading dose?
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(Cp x Vd)/F
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Cp = target plasma conc. F = bioavailability of drug (=1 when given IV) |
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What is the formula for maintenance dose?
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(Cp x CL) /F
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Cp = target plasma conc. F=bioavailability of drug |
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What is the formula for clearance of a drug?
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CL = rate of elimination of drug/plasma drug conc.
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also =VdxKe where Ke=elimination constant |
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What is zero-order elimination?
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Rate of elimination is constant regardless of plasma concentration
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constant amount of drug eliminated per time |
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What are examples of drugs with zero-order elimination?
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alcohol
aspirin |
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What is a first order elimination?
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rate of elimination is proportion to the drug concentration
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constant fraction eliminated per unit time |
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How do you speed up elimination of a drug (as in during overdose)?
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You give them something to cause the drug to go into it's ionized form.
Ionized molecules can be filtered but not readily reabsorbed so they will be more likely to pee it out |
If the drug is a weak acid ==> treat with bicarbonate (raise pH, make pee more basic) If the drug is a weak base ==> treat with ammonium chloride to lower the pH (make pee more acidic) |
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What are examples of drugs that are weak acids that might be overdosed?
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methotrexate
phenobarbital aspirin |
treat with bicarb to make them pee it out |
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What is a Phase 1 reaction?
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P-450 in liver causes reduction, oxidation, hydrolysis ==> slightly polar, water soluble metabolites that are often still active
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this is what you loose with age |
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What is a Phase 2 reaction?
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acetylation, glucuronidation and sulfation yielding very polar, inactive metabolites that can be renally excreted
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What is the difference between efficacy and potency?
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efficacy is the max effect a drug can have
potency is how much drug you need to give to achieve a given effect |
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What does a partial agonist do to the pharmacodynamics of a reaction?
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It decreases the efficacy and can either raise or lower the potency
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what is therapeutic index?
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median lethal dose/median effective dose
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safer drugs have higher TI values |
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What does it mean if a drug has a low therapeutic index?
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It has a very narrow therapeutic window. You have to careful because the toxic dose may not be much higher than the effective dose.
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Nicotinic receptors work how/where?
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Na+/K+ ligand-gated Ach receptor in autonomic ganglin (Nn) and skeletal muscle (Nm)
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How do Muscarinic receptors work (generally)?
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they are G-protein couple receptors found in the parasympathetic branch the autonomic nervous system.
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What do alpha-1 receptors do?
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inc. vascular SM contraction
inc. pupillary dilator muscle contraction (mydriasis) Inc. intestinal bladder and sphincter muscle contraction |
Gq-->phospholipace C ==> PIP2 ==> IP3/Dag ==> inc. Ca2+ and PKC |
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What do alpha-2 receptors do?
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dec. sympathetic outflow
dec. insulin release |
Gi ==> inhibits adenylyl cyclase ==> dec. cAmp ==> dec. PKA |
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What do beta-1 receptors do?
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inc. HR
inc. contractility inc. renin release inc. lipolysis |
Gs ==> activated adenylyl cyclase ==> inc. cAMP ==> inc. PKA |
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What do beta-2 receptors do?
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Vasodilation
Bronchodilation inc. HR inc. contractility inc. lipolysis inc. insulin release dec. uterine tone |
Gs (same as Beta-1) |
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What do M1 receptors do?
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?? found in CNS and enteric nervous system
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Gq |
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What do M2 receptors do?
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dec. HR
dec. contractility of atria |
Gi |
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What do M3 receptors do?
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inc. exocrine glad secretion
inc. gut peristalsis inc. bladder contractions bronchoconstriction inc. pupillary sphincter muscle contraction (miosis) ciliary muscle contraction (accommodation) |
Gq (like M1) |
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What do D1 receptors do?
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relaxes renal vascular smooth muscle
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Gs |
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What do D2 receptors do?
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modulated transmitter release, especially in the brain
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Gi |
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What do H1 receptors do?
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inc. nasal and bronchial mucus production
contraction of bronchioles pruritus pain |
Gq |
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What do H2 receptors do?
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Inc. gastric acid secretion
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Gs |
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What do V1 receptors do?
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inc. vascular smooth muscle contraction
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Gq |
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What do V2 receptors do?
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inc. H20 permeability and reabsorption in the collecting tubules of the kidney
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Gs |
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Which receptors are Gq coupled?
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H1, alpha-1, V1, M1, M3
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HAVe 1 M&M |
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Which receptors are Gs coupled?
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B1, B2, D1, H2, V2
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Which receptors are Gi coupled?
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M2, alpha-2, D2
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MAD 2's |
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Bethanechol MOA
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cholinomimetic, Ach direct agonist at muscarinic receptors - activates bladder and bowel
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Bethanechol clinical use
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post-operative neurogenic ileus and urinary retention
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Carbachol MOA
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cholinomimetic, Ach direct agonist at muscarinic receptors - causes pupillary sphincter muscle contraction
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Carbachol clinical use
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glaucoma
relief of intraocular pressure |
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Pilocarpine MOA
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cholinomimetic, Ach direct agonist at muscarinic receptors - contracts ciliary muscle of the eye (so opens the angle), contracts the pupillary sphincter (accomodation)
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Pilocarpine clinical use
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potent stimulator of sweat, tears, saliva
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Methacholine MOA
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cholinomimetic, Ach direct agonist at muscarinic receptors (M3 receptors in airway SM causes bronchoconstriction)
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Methacholine clinical use
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challenge test of asthma diagnosis
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Neostigmine MOA
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anti-cholinesterase (indirect agonist of Ach - cholimimetic)
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can not penetrate BBB |
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Neostigmine clinical use
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postoperative and neurogenic ileus and urinary retention
myasthenia gravis reversal of neuromuscular junction blockade (post-surgery) |
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Pyridostigmine MOA
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anti-cholinesterase (indirect Ach agonist - cholimimetic) so inc. endogenous Ach by keeping it around in the synaptic junction
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no CNS penetration |
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Pyridostigmine clinical use
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myasthenia gravis (long acting)
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Physostigmine MOA
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anti-cholinesterase (indirect Ach agonist - cholimimetic) so inc. endogenous Ach by keeping it around in the synaptic junction
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Physostigmine clinical use
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glaucoma
atropine overdose (outc |
crosses BBB |
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Echothiophate MOA
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anti-cholinesterase (indirect Ach agonist - cholimimetic) so inc. endogenous Ach by keeping it around in the synaptic junction
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Echothiophate clinical use
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glaucoma
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Cholinesterase inhibitor poising symptoms
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Diahrrea/urination
miosis bronchospasm bradycardia excitation of skeletal muscle and CNS lacrimation/sweating/salivation |
caused by organophosphates used in fertilizers and insecticides |
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Organophosphate poisoning antidote
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Atropine + pralidoxime
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The atropine blocks the Ach while the pralidoxime helps regenerate the AchE |
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What is organophosphate poisoning?
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The chemical irreversibly inhibits AchE so there is too much Ach in the synapse causing too much parasympathetic activation
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What are the direct agonist cholimimetics?
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Bethanechol
Carbachol Pilocarpine Methacholine |
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Atropine clinical use
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Muscarinic antagonist: produces mydriasis (pupillary dilation) and cycloplegia (inability to accommodate) for ophtho exam
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Homatropine
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Muscarinic antagonist eye drop: produces mydriasis (pupillary dilation) and cycloplegia (inability to accommodate) for ophtho exam
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Tropicamide
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Muscarinic antagonist eye drop: produces mydriasis (pupillary dilation) and cycloplegia (inability to accommodate) for ophtho exam
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Benztropine
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Muscarinic antagonist - blocks Ach in CNS
used for Parkinson's |
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Scopolamine
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blocks Ach in CNS
used for motion sickness |
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Ipratropium
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Muscarinic antagonist - blocks Ach in the respiratory system preventing bronchoconstriction
Used for asthma and COPD |
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Oxybutynin
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Muscarinic antagonist - blocks Ach in genitourinary system so prevents bladder contraction
used for cystitis and OBS |
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Glycopyrrolate
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same as oxybutynin:
Muscarinic antagonist - blocks Ach in genitourinary system so prevents bladder contraction used for cystitis and OBS |
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Methscoplamine
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Muscarinic antagonist - block Ach affect on stomach so dec. H+ secretion
used for peptic ulcers |
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Pirenzepine
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Muscarinic antagonist - block Ach affect on stomach so dec. H+ secretion
used for peptic ulcers |
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Propantheline
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Muscarinic antagonist - block Ach affect on stomach so dec. H+ secretion
used for peptic ulcers |
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What are the symptoms of atropine poisoning?
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block parasympathetic response:
inc. temp (due to dec. sweating) rapid pulse dry mouth dry, flushed skin cycloplegia constipation disorientation |
Hot as a hare Dry as a bone Red as a beet Blind as a bat Mad as a hatter |
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Hexamethonium
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nicotinic antagonist - Ach blocker at the ganglion
not used clinically |
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Epinephrine MOA
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stimulates alpha1, alpha2, beta1, beta2
at low doses it is beta2 selective |
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Epinephrine clinical use
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anaphylaxis
open angle glaucoma asthma severe hypotension (shock) |
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Norepinepherine MOA
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alpha1/2 > B1
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Norepinepherine clinical use
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Hypotension (but not really because it dec. renal perfusion too)
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Isoproterenol MOA
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beta-adrenergic direct agonist
B1=B2 |
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Isoproterenol clinical use
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AV block (rarely used)
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Dopamine MOA
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D1/D2 > beta1/2 > alpha 1/2
inotropic and chronotropic |
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Dopamine clinical use
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inotropic and chronotropic and relaxes renal vascular smooth muscle so good for:
shock (also inc. renal perfusion) heart failure |
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Dobutamine MOA
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beta-1 > beta-2
inotropic but not chronotropic |
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Dobutamine clinical use
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heart failure
cardiac stress testing |
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Phenylephrine MOA
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alpha-1 > alpha-2
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Phenylephrine clinical use
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pupillary dilation
vasoconstriction nasal decongestion |
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Metaproterenol MOA
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Selective Beta-2 agonist (B2>B1)
stimulates bronchodilation |
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Metaproterenol clinical use
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acute asthma
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Terbutaline MOA/clinical use
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selective beta-2 agonist
decreases uterine vascular tone used to slow contractions in premature labor |
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Ritodrine MOA/clinical use
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beta-2 agonist
reduces premature uterine contractions |
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Pseudephedrine side effect
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urinary retention (cuz it's a general agonist releasing stored catecholamines, which includes stimulating urinary sphincter contraction)
bad for men with BPH, e.g |
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What does exogenous NE do to blood pressure?
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Widens the pulse pressure
Beta-1 effects raise systolic Alpha-1 effects lower the diastolic |
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What does exogenous NE do to heart rate?
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reflex bradycardia
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What does isoproterenol do to blood pressure?
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lowers it (slightly) cuz beta>alpha
the Beta-2 causes vasodilation |
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What does isoproterenol do to heart rate?
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reflex tachycardia
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Clonidine MOA
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centrally acting alpha-2 agonist ==> dec. central adrenergic outflow
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alpha-methyldopa MOA
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centrally acting alpha-2 agonist ==> dec. central adrenergic outflow
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Clonidine clinical use
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to treat hypertension (esp. in renal disease cuz doesn't dec. renal perfusion)
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alpha-methyldopa clinical use
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to treat hypertension (esp. in renal disease cuz doesn't dec. renal perfusion)
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Phenoxybenzamine - MOA/use/toxicity
|
non-selective, irreversible alpha-blocker
used pre-operatively for pheochromocytoma |
orthostatic hypotension reflex tachycardia |
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Phentolamine MOA/use/toxicity
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non-selective, reversible alpha-blocker
used in pheochromocytoma (esp. pre-op) |
toxicity includes orthostatic hypotension and reflex tachycardia |
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Prazosin/terazosin/doxazosin
MOA/use/toxicity |
alpha-1 selective antagonists
used for HTN treats urinary retention in men with BPH |
toxicity: 1st dose orthostatic hypotension dizziness headache |
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Mirtazipine MOA/use/toxicity
|
alpha-2 selective antagonist
used for depression |
toxicity: inc. sedation inc. serum cholesterol inc. appetite |
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What happens to BP if you give a large dose of epi and then phentolamine
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the blood pressure will raise due to the alpha effect from the epi but then lower to below baseline after the phentolamine because there is an alpha but no beta blockade
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What happens to BP if you give a large dose of phenylephrine and then phentolamine
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The blood pressure will rise from the alpha-response induced by phenylephrine and then lower back to baseline due to alpha-blockade of phentolamine
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How do beta-blockers treat HTN?
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dec. cardiac output
dec. renin secretion (Beta-1 on JGA cells) |
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How do beta-blockers treat angina?
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dec. HR and contractility resulting in dec. O2 consumption
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How do beta-blockers treat SVT?
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dec. AV conduction velocity
(class II anti-arrhythmic) |
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What do beta-blockers treat?
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HTN
CHF angina MI SVT glaucoma |
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How do beta-blockers treat glaucoma?
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dec. secretion of aqueous humor
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What are the side effects of beta-blockers?
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impotence
exacerbation of asthma bradycardia AV block CHF worsening sedation/sleep alterations use with caution in diabetics |
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Which are the non-selective Beta-blockers?
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propranolol
timolol nadolol pindolol |
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Which are the Beta-1 selective beta-blockers?
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Atenolol
Metoprolol Esmolol (short-acting) Betaxolol |
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Which are the nonselective alpha- and beta-antagonists?
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Carvedilol
labetalol |
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Which are the partial beta-agonists?
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Pindolol
Acebutlol |
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antidote for acetaminophen overdose
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N-acetylcysteine
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antidote for salicylates overdose
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Bicarb
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alkalinize the urine |
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antidote for amphetamines overdose
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NH4Cl
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acidify the urine |
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antidote for Organophosphate overdose
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atropine + pralidoxime
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antidote for Antimuscarine/anticholinesterase overdose
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physostigmine (direct Ach agonist)
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B-blocker overdose antidote
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glucagon
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Digitalis overdose antidote
|
normalize K+
lidocaine anti-dig Fab Mg2+ |
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Iron overdose antidote
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Deferoxamine
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Lead poisoning antidote
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CaEDTA, dimercaprol, succimer, penicillamine
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Mercury/arsenic/gold poisoning antidote
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dimercaprol, succimer
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Copper, arsenic poisoning antidote
|
penicillamine
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cyanide poisoning antidote
|
nitrite, hydroxocobalamin, thiosulfate
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Methemoglobin poisoning antidote
|
Methylene blue, vitamin C
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TCA's overdose antidote
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Bicarb
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Heparin overdose antidote
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Protamine
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Warafin overdose antidote
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Vitamin K, fresh frozen plasma
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tPA, streptokinase overdose antidote
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aminocaproic acid
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Theophylline overdose antidote
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Beta-blocker
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Drugs that cause atropine-like side effects
|
TCAs
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Drugs that cause cutaneous flushing
|
Vancomycin
Adenosine Niacin Calcium-channel blockers |
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Drugs that cause torsades de pointes
|
Class III antiarrhythmics (sotalol)
Class IA antiarrhythmics (quinidine) |
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Drugs that cause agranulocytosis
|
clozapine
carbamazepine colchicine propylthiouracil methimazole dapsone |
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Drugs that cause aplastic anemia
|
chloramphenicol
benzene NSAIDs PTU methimazole |
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Drugs that cause hemolysis in G6PD deficient patients
|
Isoniazid
Sulfonamides Primaquine Aspiring Ibuprofen Nirtofurantoin |
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Drugs that cause megaloblastic anemia
|
Phenytoin
Methotrexate Sulfa drugs |
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Drugs that cause pulmonary fibrosis
|
Bleomycin
Amiodarone Busulfan |
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Drugs that cause hepatotoxicity
|
Halothane
Calproic acid Acetaminophen INH |
|
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Drugs that cause gynecomastia
|
Spironolactone
Digitalis Cimetidine Alcohol Ketoconazole |
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Drugs that cause hypothyroid
|
Lithium
Amiodarone |
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Drugs that cause gout
|
furosemide
thiazides |
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Drugs that cause osteoporosis
|
Corticosteroids
Heparin |
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Drugs that cause photosensitivity
|
Sulfonamides
Amiodarone Tetracyclines |
|
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Drugs that cause severe rash (Stevens-Johnson syndrome)
|
Ethosuximide
Lamotrigine Carbamazepine Phenobarbital Phenytoin Sulf drugs Penicillin Allopurinol |
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Drugs that cause SLE-like syndrome
|
Hydralazine
INH Procainamide Phenytoin |
|
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Drugs that cause interstitial nephritis
|
Methicillin
NSAIDs Furosemide |
|
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Drugs that cause pulmonary fibrosis
|
Bleomycin
Amiodarone Busulfan |
|
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Drugs that cause hepatotoxicity
|
Halothane
Calproic acid Acetaminophen INH |
|
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Drugs that cause gynecomastia
|
Spironolactone
Digitalis Cimetidine Alcohol Ketoconazole |
|
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Drugs that cause hypothyroid
|
Lithium
Amiodarone |
|
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Drugs that cause gout
|
furosemide
thiazides |
|
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Drugs that cause osteoporosis
|
Corticosteroids
Heparin |
|
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Drugs that cause photosensitivity
|
Sulfonamides
Amiodarone Tetracyclines |
|
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Drugs that cause severe rash (Stevens-Johnson syndrome)
|
Ethosuximide
Lamotrigine Carbamazepine Phenobarbital Phenytoin Sulf drugs Penicillin Allopurinol |
|
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Drugs that cause SLE-like syndrome
|
Hydralazine
INH Procainamide Phenytoin |
|
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Drugs that cause interstitial nephritis
|
Methicillin
NSAIDs Furosemide |
|
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Drugs that cause diabetes insipidus
|
Demeclocycline
Lithium |
|
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Drugs that cause Parkinsonian effects
|
Haloperidol
Chlorpromazine Reserpine Metoclopramide |
|
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Drugs that cause seizures
|
Buproprion
Imipenem/cilastatin Isoniazid |
|
|
Drugs that cause disulfram-like reactions
|
Metronidazole
Cephalosporins (some) Procarbazine 1st generation sulfonylureas |
|
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Drugs that cause nephro- and ototoxicity
|
Aminoglycosides
Vancomycin Loop diuretics Cisplatin |
|
|
P-450 inducers
|
Quinidine
Barbituates St. John's wort Phenytoin Rifampin Griseofulvin Carbamazepine Chronic alcohol use |
Queen Barb Steals Phen-phen and Refuses Greasy Carbs Chronically makes drugs wear-off quicker |
|
P-450 inhibitors
|
HIV protease inhibitors
Ketoconazole Erythromycin Grapefruit juice Acute alcohol use sulfonamides isoniazid cimetidine |
"inhibit yourself from drinking beer from a KEG because it makes you Acutely SICk" makes drugs more potent and/or stay around longer |
|
What are the symptoms of sulfa-drug allergies?
|
fever
pruritic rash urticuria Steven-Johnson syndrome hemolytic anemia thrombocytopenia agranulocytosis |
