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125 Cards in this Set
- Front
- Back
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What is Phase 1 metabolism
Phase 2? Which one is lost first in geriatric patients |
Phase 1 - cytochrome P450 (reduction, oxidation, hydrolysis)
Phase 2- conjugation (acetylation, glucoronidation, sulfation) Phase 1 lost first in geriatrics |
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What is the sympathetic receptor on renal vascular smooth muscle? sweat gland?
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renal: D1 receptors
sweat gland: Ach muscarinic 3 |
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What conditions affect volume distribution of plasma protein-bound drugs
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liver and kidney disease
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What is a property of first-order elimination in terms of half-life
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a drug infused at a constant rate reaches ~94% of steady state at 4 t(1/2) (half-lives)
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What is the equation for loading dose
for maintenance dose |
Loading: Cp x (Vd / F)
Maintenance: Cp x (CL/F) Cp = target plasma [ ] F = bioavailability CL = clearance |
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What happens to loading/maintenance dose in impaired liver and kidney disease
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loading dose same
maintenance dose decreases |
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What drugs have zero-order elimination
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PEA
Phenytoin, Ethanol, Aspirin (at high or toxic concentrations) |
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How do you treat a weak acid overdose
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trx w/bicarbonate
-ion is trapped in a basic environment ex: phenobarbital, methotrexate, TCAs, aspirin |
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How do you treat a weak base overdose
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trx w/ammonium chloride
-ion trapped in an acidic env't ex: amphetamines |
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What effect does a competitive antagonist have
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decreases potency and increases EC50 (effective concentration for producing a given effect)
Increase Km |
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What effect does a noncompetitive antagonist have
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decreases efficacy (lower Vmax)
Km is the same |
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Compare a full and partial agonist
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partial agonist acts on the same receptor system, but has a lower maximal efficacy (regardless of dose)
but potency is independent (can be higher, lower or the same) |
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How do you calculate therapeutic index
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LD50/ED50
measures drug safety. Drugs w/higher TI values are safer |
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Describe Nicotinic ACh receptors
Describe Muscarinic ACh receptors |
Nicotinic: ligand-gated Na/K channels
(Nn found in autonomic ganglia; Nm found at the NMJ) Muscarinic: G-protein-coupled receptors acting thru 2nd messengers |
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What is volume of distribution (Vd)?
Clearance (CL)? |
Vd = amt of drug / drug plasma conc
Low Vd: only in plasma med Vd: in extracellular space or body water high Vd: in tissue CL = rate of elimination/drug plasma conc = Vd x Ke |
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P450 Inducers?
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Queen Bar Steals Phen-phen and Refuses Greasy Carbs Chronically.
Quinidine Barbiturate St. John's Worts Phenytoin Rifampin Griseofulvin Carbamazepine Chronic etOH |
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P450 Inhibitors?
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"SIC from KEG"
Sulfonamide Isoniazid Cimetidine Ketoconazole Erythromycin Grapefruit juice acute EtOH |
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Gq receptors?
Hint: ANS, DA, Histamine, ADH |
HAVe 1 M&M
H1, alpha 1, V1, M1, M3 |
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Gs receptors?
Gi receptors? Hint: ANS, DA, histamine, ADH |
Gs: Beta 1, beta 2, D1, H2, V2
Gi: "MAD 2's"; M2, alpha 2, D2 |
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Major functions of alpha 1 sympathetic receptors?
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Vasoconstriction, mydriasis, intestinal and bladder sphincter contraction
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Major functions of beta 1 sympathetic receptors?
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Increase: HR, contractility, conduction velocity
Increase renin and lipolysis |
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Major functions of Beta 2 sympathetic receptors?
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Bronchodilation, vasodilation
Increase: HR, contractility Lipolysis, insulin release uterine relaxation |
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major functions of muscarinic 2 receptors?
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decrease HR and contractility of ATRIA
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Major functions of muscarinic 3 receptors?
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Increase exocrine secretion (sweat, gastric acid)
Increase: gut motility, bronchoconstriction Miosis and accomodation |
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Major functions of H1 and H2 receptors?
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H1: increase nasal/bronchial mucus secretion, bronchoconstriction, pruiritis and pain (think type 1 hypersensitivity)
H2: gastric acid secretion |
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Cholinergic transmission modulators (3)
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Hemicholium, vesamicol, and botulinum
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Hemicholium
vesamicol botulinum |
Hemicholium: blocks choline reuptake
vesamicol: blocks VAT and inhibit Ach storage Botulinum: block Ach release |
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Adrenergic tranmission modulators (5)
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Guanethidine
Reserpine Amphetamine Cocaine TCAs |
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Metyrosine
Reserpine Guanethidine |
adnergic transmission blockers
Metyrosin: blocks tyrosine hydroxylase Reserpine: blocks vesicular transport Guanethidine: blocks release of NE |
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Amphetamine
TCAs Cocaine |
all block reuptake of NE
amphetamine induces release of NE |
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Bethanechol
Carbachol Pilocarpine Methacholine |
direct cholinomimetics
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Bethanechol
indication? Action? |
direct cholinomimetics
for postoperative and neurogenic ileus and urinary retention activates Bowels and Bladder smooth muscle |
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carbachol
indication? |
direct cholinomimetics
glaucoma, pupillary contraction, and release of intraocular pressure |
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Pilocarpine
indication? Action? |
direct cholinomimetics
potent stimulator of sweat, tears, and saliva contracts ciliary muscle eye (open angle), pupillary sphincter (narrow angle) resistant to AchE |
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Methacholine
indication? Action? |
direct cholinomimetics
challenge test for dx of asthma stimulates muscarinic receptors when inhaled |
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Neostigmine
Pyridostigmine edrophonium physostigmine echothiphate |
anticholinesterases
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Neostigmine
indication? action? |
anticholinesterases
postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular jxn blockade (postoperative) increase endogenous Ach; no CNS penetration |
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Pyridostigmine
indication? action? |
anticholinesterases
Myasthenia gravis (long acting) does not penetrate CNS increase strength |
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edrophonium
indication? action? |
anticholinesterases
aka tensilon dx of myathenia gravis (very short acting) |
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physostigmine
echotiophate indication? action? |
anticholinesterases
glaucoma (crosses CNS) and atropine overdose |
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Toxicity of choinesterase inhibitor? (9)
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DUMBBELSS
Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation of skeletal muscle Lacrimination Sweating Salivation (abdomen cramping) |
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Antidotes for cholinesterase inhibitors
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atropine: M antagonist
Pralidoxime: regenerates active cholinsterase |
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Atropine, homatropine, tropicamide
class? targeted organ? application? |
Muscarinic antagonist
eye produce mydriasis and cycloplegia |
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Benztropine
class? targeted organ? application? |
Muscarinic antagonist
CNS to reduce the sx of Parkinson's disease |
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Scopolamine
class? targeted organ? application? |
muscarinic antagonist
CNS motion sickness and sx of Parkinson's |
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Ipratropium
class? targeted organ? application? |
Muscarinic antagonist
respiratory Asthma, COPD |
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Oxybutynin, glycopyrrolate
class? targeted organ? application? |
Muscarinic antagonist (M3)
genitourinary reduce urgency in mild cystitis and reduce bladder spasm |
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Methscopolamine, pirenzepine, propantheline
class? targeted organ? application? |
Muscarinic antagonist
Gastrointestinal peptic ulcer tx |
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toxicity of atropine
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Hot as a hare
dry as a bone red as a beet blind as a bat mad as a hatter increased body temperature rapid pulse dry mouth dry flushed skin cycloplegia constipation disorientation can cause acute angle-closure glaucoma in elderly urinary retention in men with prostatic hyperplasia hyperthermia in infants |
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Hexamethonium
class? indication? toxicity |
nicotinic antagonist
Ganglionic blocker used in experimental models to prevent vagal reflex responses to changes in BP (prevent reflex bradycardia caused by NE) severe orthostatic hypotension blurred vision constipation sexual dysfxn |
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Succinycholine
class? Indications? complications? |
Depolarzing neuromuscular blockers (blocks nicotinic receptor)
used for muscle paralysis in surgery or mechanical ventilation can cause hypercalcemia and hyperkalemia |
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Tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium
Class? indication? |
nondepolarzing neuromuscular blockers
competitive nicotinic ach receptor blockers used for muscle paralysis for surgery or mechanical ventilation |
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How do you reverse the ganglionic blockers?
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use cholinesterase inhibitors
e.g. neostigmine, edrophonium |
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Dantrolene
MOA? indication? |
prevent release of Ca from sarcoplasmic ER of skeletal muscle
used in malignant hyperthermia, which is caused by inhalation of anesthetics and succinycholine neurleptic malignant syndrome (a toxicity of antipsychotic drugs) |
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Epinephrine
mechanism/selectivity? applications? effects on BP and HR? |
alpha1/2, and beta 1/2
Low doses selective for beta 1 for anaphylaxis, glaucoma (open angle), asthma, hypotension BP: increased systolic (due to beta 1), decreased diastolic (due to beta 2), and same PP heart rate: increased HR due to Beta 1 |
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Norepinephrine
Mechanism/selectivity applications HR and BP changes? |
alpha1/2 > beta 1
hypotension but decreased renal perfusion BP: increased systolic (beta 1), diastolic (alpha 1), and PP HR: decreased due to reflex bradycadia |
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Isoproterenol
Mechanism/selectivity applications HR and BP changes? |
Beta 1 = beta 2
AV block (rare) BP: Systolic (mildly decreased due to beta 1), diastolic (decreased due to beta 2), decreased PP HR: increased due to beta 1 |
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Dopamine
mechanism/selectivity applications |
D1 = D2 > beta > alpha
shock (increase renal perfusion), heart failure |
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dobutamine
mechanism/selectivity applications |
beta 1> beta 2 sympathomimetics; inotropic but no chronotropic
shock, heart failure, cardiac stress testing |
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Phenylephrine
MOA? clinical indications? |
alpha 1 > alpha 2
pupillary dilation, vasoconstriction, nasal decongestion |
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Metaproterenol, Albuterol, Salmeterol, Terbutaline
mechanism/selectivity applications |
selective beta 2 agonists
"MAST" Metaproterenol and albuterol: fo acute asthma Salmeterol: for long term tx Terbutaline: to reduce premature uterine contractions |
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Ritodrine
mechanism/selectivity applications |
Beta 2 agonist
reduce premature uterine contractions |
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Amphetamine
mechanism/selectivity applications |
indirect general agonist, releases stored catecholamine
narcolepsy, obesity, ADD |
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Ephedrine
mechanism/selectivity applications |
indirect general agonist, releases stored catecholamine
Nasal decongestion, urinary incontinence, hypotension |
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Cocaine
mechanism/selectivity applications |
indirect general agonist, uptake inhibitor of catecholamine
causes vasoconstriction and local anesthesia |
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Clonidine, alpha methyldopa
Mechanism/selectivity applications |
centrally acting alpha 2 agonists, decreased central adrenergic outflow
hypertension, especially with renal disease (no decrease in blood flow to kidney) |
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What happens to BP when alpha blockade is applied after a large dose of epi? how about phenylephrine?
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Epi: increased BP (systolic, diastolic, PP) initially with epi (net pressor effect) and then net depressor effect with alpha blockade
Phenylephrine: net pressor effect initially and then suppressino of pressor effect with alpha blockade |
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Phenoxybenzamine and phentolamine
class application toxicity |
nonselective alpha blockers
pheochromocytoma (phenoxybenzamine, irreversible, before removing tumor b/c high levels of released catecholamines will not be able to overcome blockage) orthostatic hypotension and reflex tachycardia |
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Prazosin, terazosin, and doxazosin
class application toxicity |
alpha 1 blockers (-zosin ending)
htn, urinrary retention in BPH (by relexing the urinary sphincter) first dose orthostatic hypotension, dizziness, and headache |
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Mirtazapine
class application toxicity |
alpha2 blocker
depression with insomnia sedation, increased serum cholesterol, and increased appetite |
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propranolol, timolol, nadolol, pindolol, labetalol
selectivity? |
nonselective beta antagonists
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Acebutolol, betaxolol, esmolol, atenolol, metoprolol
selectivity? |
A BEAM of beta 1 blockers
acebutolol: partial agonists Esmolol: short acting |
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Carvediolol, labetalol
selectivity? |
nonselective alpha and beta antagonists
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Pindolol, acebutulol
what is common b/t above 2 drugs? |
partial beta agonists
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applications of B blockers
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HTN, angina pectoris, MI, SVT, CHF, glaucoma
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What 2 beta blockers are used for SVT?
What beta blocker is used for glaucoma |
SVT: propranolol, esmolol
Glaucoma: timolol |
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Iron poisoning
mechanism? sxs? |
cell death due to peroxidation of membrane lipids
acute: gastric bleeding chronic: metabolic acidosis, scarring leading to GI obstruction |
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What is accumulated in the following alcohol toxicity? sxs?
Ethylene glycol? Methanol? Ethanol? |
Ethylene glycol: oxalic acid --> acidosis, nephrotoxicity
Methanol: formaldehyde and formic acid --> severe acidosis and retinal damage ethanol: acetaaldehyde --> nausea, vomiting, headache, and hypotension |
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Formepizole
Disulfiram MOA? |
Formepizole: etOH dehydrogenase inhibitor
Disulfiram: acetaaldehyde dehydrogenase inhibitor |
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antidote/treatment for the following toxins?
Acetaminophen Salicyclates Amphetamines |
Acetaminophen: N-acetylcysteine
Salicyclates: NaHCO3 (alkalinize urine), dialysis Amphetamines: NH4Cl (acidify urine) |
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antidote/treatment for the following toxins?
Anticholinersterases inhibitors, organophosphates Antimuscarinic, anticholinergic agents Beta blockers digitalis |
Anticholinersterases inhibitors, organophosphates: atropine, pralidoxime (regenerates active cholinesterase)
Antimuscarinic, anticholinergic agents: physostigmine salicylate Beta blockers: glucagon digitalis: stop dig, normalize K, lidocaine, anti-dig Fab fragments, Mg |
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antidote/treatment for the following toxins?
Iron Lead Mercury, arsenic, gold copper, arsenic gold |
Iron: deferoxamine
Lead: CaEDTA, dimercaprol (for severe toxicity), succimer (agent of choice), penicillamine Mercury, arsenic, gold: dimercaprol (BAL), succimer copper, arsenic gold: penicillamine |
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antidote/treatment for the following toxins?
Cyanide Methemoglobin Carbonmonoxide |
Cyanide: nitrite, hydroxocobalamin, thiosulfate
Methemoglobin: methylene blue, vitamin c Carbonmonoxide: 100% O2, hyperbaric O2 |
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antidote/treatment for the following toxins?
Methanol, ethylene glycol (antifreeze) Opioids Benzodiazepines TCAs |
Methanol, ethylene glycol (antifreeze): ethanol, dialysis, femopizole
Opioids: naloxone/naltrexone Benzodiazepines: flumazenil TCAs: NaHCO3 to alkalize serum |
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antidote/treatment for following toxins?
Heparin Warfarin tPA, streptokinase Theophylline |
Heparin: protamine
Warfarin: vitamin K, fresh frozen plasma tPA, streptokinase: aminocaproic acid Theophylline: beta blocker |
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What drug reaction is induced by the following drugs?
TCAs |
atropine like side effects
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What drug reaction is induced by the following drugs?
cocaine, sumatriptan |
coronary vasospasm
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What drug reaction is induced by the following drugs?
Vancomycin, Adenosine, Niacin, Ca channel blockers |
VANC
cutaneous flushing |
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What drug reaction is induced by the following drugs?
doxorubicin, daunorubicin |
dilated cadiomyopathy
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What drug reaction is induced by the following drugs?
soltalol, quinidine, antiarrhythmics |
torsade de pointes
anything that prolongs QT interval --> torsades Jervell-Lange Nielson syndrome: congenital defect where QT interval is prolonged |
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What drug reaction is induced by the following drugs?
Clozapine, carbamazepine, colchicine, propylthiouracil, methimazole, dapsone |
agranulocytosis
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What drug reaction is induced by the following drugs?
chloramphenicol, benzene, NSAIDs, propylthiouracil, methimazole |
aplastic anemia
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What drug reaction is induced by the following drugs?
methydopa |
direct Coombs positive hemolytic anemia
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What drug reaction is induced by the following drugs?
chloramphenicol |
gray baby syndrome
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What drug reaction is induced by the following drugs?
Isoniazid, Sulfonamides, Primaquine, Aspirin, Ibuprofen, Nitrofurantion |
hemolysis in G6PD deficient pts
hemolysis IS PAIN (intrinsic hemolytic normocytic anemia) also fava beans |
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What drug reaction is induced by the following drugs?
Phenytoin, methotrexate, Sulfa drugs |
megaloblastic anemia
"having a BLAST with PMS" |
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What drug reaction is induced by the following drugs?
OCPs (estrogens and progestins) |
thrombotic complications
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What drug reaction is induced by the following drugs?
ACE inhibitors |
cough
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What drug reaction is induced by the following drugs?
Bleomycin, Amiodarone, Busulfan |
pulmonary fibrosis
it's hard to BLAB when you have pulmonary fibrosis |
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What drug reaction is induced by the following drugs?
Macrolides |
acute cholestatic hepatitis, GI discomfort (most common cause of noncompliance)
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What drug reaction is induced by the following drugs?
Halothane, valproic acid, acetaminophen, amanita phalloides |
focal to massive hepatic necrosis
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What drug reaction is induced by the following drugs?
INH |
hepatitis
neurotoxicity (by competing with B6 -> deplete tryptophan -> decrease niacin) |
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What drug reaction is induced by the following drugs?
Clinidamycin, ampicillin |
pseudomembranous colitis via C. difficile infection
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What drug reaction is induced by the following drugs?
Glucocorticoid withdrawal |
adrenocritical insufficiency due to HPA suppression
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What drug reaction is induced by the following drugs?
spironolactone, digitalis, cimetidine, chronic alcohol abuse, estrogens, ketoconazole |
gynecomastia
Some Drugs Create Awesome Knockers |
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What drug reaction is induced by the following drugs?
Tamoxifen, clomiphne |
hot flashes
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What drug reaction is induced by the following drugs?
Lithium, amiodarone |
hypothyroidism
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What drug reaction is induced by the following drugs?
phenytoin |
gingival hyperplasia, megaloblastic anemia, teratogenesis (fetal hydantoin syndrome), SLE-like syndrome
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What drug reaction is induced by the following drugs?
furosemide, thiazides |
Gout
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What drug reaction is induced by the following drugs?
Corticosteroids, heparin |
osteoporosis
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What drug reaction is induced by the following drugs?
Sulfonamides, Amiodarone, Tetracyline |
photosensitivity
SAT for photo |
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What drug reaction is induced by the following drugs?
Ethosuximide, lamotrigine, carbamazepine, phenobarbital, phenytoin, sulfa drugs, penicillin, allopurinol |
Rash (Stevens-Johnson syndrome)
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What drug reaction is induced by the following drugs?
Hydralazine, INH, Procainamide, Phenytoin |
SLE-like syndrome
it's not HIPP to have lupus |
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What drug reaction is induced by the following drugs?
Flouroquinolones |
Tendonitis, tendone rupture, and cartilage damage
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What drug reaction is induced by the following drugs?
Expired tetracycline |
Fanconi's syndrome
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What drug reaction is induced by the following drugs?
Methicillin, NSAIDs, furosemide |
interstitial nephritis
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What drug reaction is induced by the following drugs?
how do you prevent? Cyclophosphamide, ifsfamide |
hemorrhage cystitis
prevent with mesna |
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What drug reaction is induced by the following drugs?
quinidine, quinine |
cinchonism: headache, tinnitus
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What drug reaction is induced by the following drugs?
lithium, demeclocyline |
diabetes insipidus
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What drug reaction is induced by the following drugs?
haloperidol, chlorpromazine, reserpine, metoclopramide |
parkinson like syndrome
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What drug reaction is induced by the following drugs?
bupropion, imipenem/cilastatin, isoniazid |
seizures
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What drug reaction is induced by the following drugs?
antipsychotics |
tardive dyskinesia
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What drug reaction is induced by the following drugs?
metronidazole, certain cephalosporins, procarbazine, first gene sulfonyureas |
disulfiram like reaction
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What drug reaction is induced by the following drugs?
polymyxins |
nephrotoxicity/neurotoxicity
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What drug reaction is induced by the following drugs?
aminoglycosides, vancomycin, loop diuretics, cisplatin |
nephrotoxicity and neurotoxicity
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