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Pharmacology Flashcards

1
Q

Michaelis Menten kinetics

  • Km
  • Vmax
  • curve
A
  • related to affinity of enzyme for substrate; on x axis
  • directly proportional to enzyme concentration; on y axis
  • hyperbolic, sigmoid
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2
Q

Lineweaver-burk plot

  • vmax
  • Km
  • competitive inhibitors
  • noncompetitive inhibitors
A
  • y intercept, higher the intercept lower the vmax
  • x intercept, further to the right the greater the Km and lower the affinity
  • cross each other, and increased Km
  • do not cross each other
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3
Q

Pharmacodynamics

  • competitive inhibitor, reversible: resemble substrate, overcome by [s], bind active site, effect on vmax, effect on Km, pharmacodynamics
  • competitive inhibitors, irreversible: resemble substrate, overcome by [s], bind active site, effect on vmax, effect on Km, pharmacodynamics
  • noncompetitive inhibitors: resemble substrate, overcome by [s], bind active site, effect on vmax, effect on Km, pharmacodynamics
A
  • resemble substrate, overcome by increase in [substrate], bind active site, do not change vmax, increase Km, decrease potency
  • resemble substrate, not overcomed by [substrate], bind active site, decrease vmax, Km unchanged, decreased efficacy of pharmacodynamics
  • do not resemble substrate, not overcome by [substrate], do not bind active site, decrease Vmax, do not change Km, decrease efficacy
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4
Q

Pharmacokinetics

  • bioavailability
  • volume of distribution
  • clearance
  • half life
  • dosage calculation
A
  • fraction of administered drug reaching systemic circulation
  • volume of total amount of drug in body relative to plasma concentration
  • volume of plasma cleared of drug per unit time; rate of elimination of drug // plasma drug concentration
  • the time required to change the amount of drug in body by 1/2 during elimination, 1-50, 2-25, 3-12.5, 4-6.25
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5
Q

Types of drug interactions

  • additive
  • permissive
  • synergistic
  • tachyohylactic
A
  • effect of substance A and B together is equal to sum of individual effects
  • presence of substance A is required for full effect of substance B
  • effect of substance A and B together is greater that the sum of their individual
  • acute decrease in response to drug after initial/repeated administration
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6
Q

Elimination of drugs

  • zero order
  • first order
A
  • rate of elimination is constant

- rate of elimination is proportional to drug concentration

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7
Q

Urine pH and drug elimination

- what happens

A
  • ionized species are trapped in urine and cleared while neutral forms can be reabsorbed
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8
Q

Drug metabolism

  • phase I
  • phase II
A
  • reduction, oxidation hydrolysis w/ cytochrome p450

- conjugation, usually yields very polar inactive metabolites

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9
Q

Efficacy vs potency

  • efficacy
  • potency
A
  • max effect drug can produce, represented by increase in vmax
  • amount of drug needed for given effect, represented by middle of x
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10
Q

Therapeutic index

  • what is it
  • equation
  • therapeutic window
A
  • measurement of drug safety; high is safe and low needs to be monitored
  • median toxic dose // median effective dose
  • dosage range that can safely and effectively treat disease
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11
Q

Autonomic receptors

  • parasympathetic
  • sympathetic
A
  • Ach on nicotinic, and Ach on muscarinic

- Ach on nicotinic, and Epi on alpha/beta

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12
Q

Acetylcholine receptors

  • nicotinic MOA
  • nicotinic subtypes
  • muscarinic MOA
  • muscarinic location
A
  • ligand gated Na/K channels
  • Nn found in autonomics and Nm found in NMJ
  • gPCR -> act through second messengers
  • muscle , brain, exocrine gland, sweat gland
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13
Q

G-protein linked second messengers sympathetic

  • alpha 1
  • alpha 2
  • beta 1
  • beta 2
  • beta 3
A
  • q; increase vascular SM contractions, increase pupillary dilator contraction, increase intestinal and bladder sphincter contraction
  • i; decrease sympathetic outflow (epi will bind back on pre-synaptic nerve to modulate release of epi), decrease insulin release, decrease lipolysis, increase platelet aggregation, decrease AQH production
  • s; increase heart rate, contractility, renin release, lipolysis
  • s; vasodilation, bronchodilation, increase lipolysis, increase insulin release, increase AQH production
  • s; increase lipolysis, thermogenesis and bladder relaxation
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14
Q

G-protein linked second messengers parasympathetic

  • M1
  • M2
  • M3
A
  • q; mediates higher cog functions and stimulates enteric nervous system
  • i; decrease heart rate and contractility of atria
  • q; increase exocrine gland secretions, increase gut peristalsis, increase bladder contraction, bronchoconstriction
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15
Q

G-protein linked second messengers dopamine

  • D1
  • D2
A
  • s; relaxes renal vascular SM, activated direct pathway of striation
  • i; modulates transmitter release, especially in brain
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16
Q

G-protein linked second messengers histamine

  • H1
  • H2
A
  • q; increase nasal and bronchial mucus, vascular permiability, bronchoconstriction, pruritis, pain
  • s; increase gastric secretion
17
Q

G-protein linked second messengers vasopressin

  • V1
  • V2
A
  • q; increase vascular SM contractions

- s; increase H2O permeability and reabsorbtion via upregulating aq-2 in CT

18
Q

Amphetamines MOA

A
  • use NE transporter on presynaptic cleft to get into pre-synaptic neuron, then use vesicular monoamine transporter to enter neurosecretory vesicles and displace NE, when NE builds up in the pre-synaptic neuron `the NE transporter that normally reuptakes NE from post synaptic cleft starts releasing it
19
Q

Direct cholinergic agonists

  • bethanechol: action, indication
  • Cabarchol
  • methacholine
  • pilocarpine
A
  • activates bladder smooth muscle
  • carbon copy of Ach but resistant to AchE; constricts pupils and relieves intraocular pressure
  • stimulates muscarinic receptors in airway when inhaled; challenge test for asthma
  • contracts ciliary muscles of eye, pupillary sphincter, can cross BBB; potent stimulator of sweat, tears, and saliva, open and closed angle glaucoma
20
Q

Indirect cholinergic agonists

  • donepezil
  • edrophonium
  • neostigmine
  • physostigmine
  • pyridostigmine
A
  • increase Ach, 1st line for alzheimers
  • increase Ach, used to test for Myasthenia Gravis
  • increase Ach, post-op and neuro ileus and urinary retention, reversal of NMJ blockade
  • increase Ach, antidote to anticholinergic tox
  • increase Ach and muscle strength; tx for myasthenia gravis
21
Q

Acetylcholinesterase poisoning

  • caused by
  • muscarinic effects: sxs, reversal
  • nicotinic effects: sxs, reversal
  • CNS effects
A
  • organophosphates (insecticides) that irreversibly inhibit AchE; seen in farmers
  • diarrhea, urination, miosis, bronchospasm, bradycardia, emesis, lacrimation, sweating, salivation; atropine
  • NM blockade; reversed by pralidoximine
  • resp depression, lethargy, seizure, coma
22
Q

Muscarinic antagonists

  • atropine
  • benztrpoine
  • glycopyrrolate
  • hyoscyamine
  • ipatropium
  • oxybutynin
  • scopolamine
A
  • eye; produce mydriasis and cycloplegia
  • CNS; parkinson dx
  • GI/ resp; preoperative to reduce airway secretions
  • GI; anti-spasmodics for IBS
  • resp; COPD, asthma
  • GU; reduce bladder spasms and urge urinary incontinence
  • CNS; motion sickness
23
Q

Atropine effects

  • eye
  • airway
  • stomach
  • gut
  • bladder
A
  • increase pupil dilation
  • bronchodilation, decrease secretions
  • decrease acid secretion
  • decrease motility
  • decrease urgency in cystitis
24
Q

Direct sympathomimetics

  • albuterol: which receptor, indication
  • dobutamine
  • dopamine
  • epinephrine
  • fenoldopam
  • isoproterenol
  • midodrine
  • mirabegron
  • nor-epi
  • phenyl-epi
A
  • binds beta 2 more than beta 1; for acute asthma
  • binds beta 1 more than beta 2; heart failure, cardiogenic shock, cardiac stress test
  • dopamine 1 and 2; unstable bradycardia, HF, shock
  • Beta more than alpa; anaphylaxis, asthma, open angle glaucoma
  • D1; post op HTN, hypertensive crisis
  • B1 = B2; elctrophysiologic eval of tachyarrythmias
  • alpha 1; auto insuff and postural hypotension
  • beta 3; urinary urge incontinence or overactive bladder
  • alpha 1> 2> Beta 1; hypotension
  • alpha 1> 2; hypotension, ocular procedures, rhinitis
25
Q

Indirect sympathomimetics

  • amphetamine: MOA
  • cocaine
  • ephedrine
A
  • indirect general agonist, reuptake inhibitor and releases stored catecholamines; narcolepsy, obesity, ADHD
  • indirect general agonist, reuptake inhibitor; causes vasoconstriction and local anesthesia
  • indirect general agonist, releases stored catecholamines; nasal decongestion, urinary incontinence, hypotension
26
Q

Sympatholytics: indications, side effects

  • clonidine
  • alpha-methyldopa
  • tizanidine
A
  • hypertensive urgency, ADHD, tourettes, symptom control for opioid withdrawal; CNS depression, bradycardia, hypotension, resp depression
  • hypertension in pregnancy; direct coombs + hemolysis, drug induced lupus
  • relief of spasticity; hypotension, weakness
27
Q

Nor-epi vs isoproterenol

  • nor epi
  • isoproterenol
A
  • acts on alpha 1; vasoconstriction, increase mean arterial pressure, reflex bradycardia
  • acts on beta; 2- vasodilation, decrease in mean arterial pressure and 1- increase heart rate and reflex activity
28
Q

Alpha blockers non selective

  • phenoxybenzamine
  • phentolamine
A
  • irreversible, pheochromocytoma to prevent catecholamine crisis
  • reversible, given to pts on MAO inhibitors who eat tyramine containing foods and for cocaine induced hypertension
29
Q

Alpha blockers a1 selective

- prazosin, terazo, doxazo, tamulo

A
  • urinary sxs from BPH

- orthostatic hypotension, dizziness, headache

30
Q

Alpha blockers a2 selective

- mirtazapine

A
  • depression
31
Q

Beta blockers

  • angina; how does it help
  • glaucoma; how does it help, which med
  • heart failure; effect
  • hypertension; how does it help
  • hyperthyroidism; how does it help, med
  • HCM
  • MI: how does it help
  • SVT: how does it help
  • variceal bleeding: how does it help, med
A
  • decrease HR and contraction resulting in decreased O2 consumption
  • decrease production of AQH; timolol
  • decrease mortality
  • decrease cardiac output, renin secretion
  • symptom control, thyroid storm; propranolol
  • decreased HR-> increase filling time, relieving obstruction
  • decrease O2 demand and mortality
  • decrease AV conduction velocity
  • decrease hepatic venous pressure gradient and portal HTN; Nadolol
32
Q

Ingested seafood toxins

  • histamine: source, action, sxs, tx
  • tetrodotoxin
  • ciguatoxin
A
  • spoiled dark meat fish; bacterial histidine decarboxylase converts histidine to histamine, misdiagnosed as fosh allergy; mimics anaphylaxis, acute burning sensation of mouth, flushing of face; antihistamine, albuterol and epi
  • pufferfish; highly potent toxin, binds fast voltage gated Na channels in cardiac and nerve tissues; nausea, diarrhea, paresthesia, weakness, dizziness, loss of reflexes; supportive
  • reef fish (barracuda, snapper, moray eel); open Na channels causing depolarization; nausea, vomiting, diarrhea, perioral numbness, reversal of hot and cold sensation; supportive
33
Q

Beers criteria

  • what does it do
  • meds
A
  • developed to reduce potentially inappropriate prescribing and harmful polypharmacy in geriatric population
  • alpha blocker, anticholinergics, anti depressants, antihistamine, opioids, benzos, NSAIDs, PPIs

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