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pharm cards Flashcards

2
Q

List the 4 most important pharmacokinetics equations: (Vd, Cl, LD, MD)

A

1) Vd = (amount of drug given)/([drug] in plasma)2) Cl = (Vd X 0.7)/t1/23) LD = Css X Vd4) MD = Css X Cl

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3
Q

competitive vs noncompetitive inhibitors:1) Resemble substrate?2) Overcome by increased [S]?3) Bind active site?4) Effect on Vmax?5) Effect on Km?6) Pharmacodynamics: effect on potency? efficacy?

A

Competitive inhibitors:1) Yes2) Yes3) Yes4) Vmax does not change5) Km increases6) decreased potency (increased Km, decreased potency); no effect on efficacyNoncompetitive inhibitors:1) No2) No3) No4) Vmax decreases5) Km does not change6) decreased efficacy (decreased Vmax, decreased efficacy); no effect on potentcy

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4
Q

Zero-order elimination

A

rate of elimination of drug is constant, regardless of the plasma concentration; Cp decreases linearly with time.Examples = PEA: Phenytoin, Ethanol, Aspirin

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5
Q

First-order elimination

A

Rate of elimination is proportional to drug concentration (a constant fraction of the drug is eliminated per unit time); the plasma concentration decreases exponentially with time.

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6
Q

Phase I vs Phase 2 metabolism:Which phase do geriatric patients lose first?

A

Phase I: -reduction, oxydation, hydrolysis-usually yields slightly polar, water-soluble metabolites (often still active)-cytochrome P-450Phase II:-GAS: Glucuronidation, Acetylation, Sulfation-usually yields very polar, inactive metabolites (renally excreted)*Geriatric patients lose phase 1 first

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7
Q

Efficacy vs Potency

A

Efficacy: -proportional to Vmax (increase Vmax, increase efficacy)-maximal effect a drug can produce-high efficacy drugs: analgesics, antibiotics, antihistamines, decongestantsPotency:-inversely proportional to Km (increase Km, decrease potency)-amount of drug needed for a given effect-increased potency, increased affinity for receptor-highly potent drugs: chemo drugs, anti-hypertensive drugs, antilipid drugs

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8
Q

Pharmacodynamics: Effects of adding competitive antagonists, noncompetitive antagonists, and partial agonists to an agonist on pharmacodynamic curves:

A

1) Competitive antagonist + agonist –> shift curve to the right = decreased potency (increased Km); no change on efficacy2) Noncompetitive antagonist plus agonist: shift curve down = decreased efficacy (decreased Vmax); no effect on potency3) Partial agonist: acts at the same site as a full agonist, but with reduced maximal effect. Get decreased efficacy (decreased Vmax); potency is variable, can be either increased or decreased.

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9
Q

Therapeutic Index: What is it? What’s the equation? Is it safer to have a higher or lower TI?*Examples of drugs with low TI?

A

TI = measurement of drug safetyTI = LD50/ED50 = median lethal dose/median effective dose(“TILE”)Safer drugs have higher TI valuesExamples of drugs with low TI (must monitor these patients!):-Phenobarbital-Lithium-Digoxin-Coumadin/Warfarin

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10
Q

Nicotinic vs Muscarinic ACh receptors

A

Nicotininc ACh receptors = Na+/K+ channelsMuscarinic ACh receptors = G-protein-coupled receptors, act through 2nd messengers; 5 subtypes = M1, M2, M3, M4, M5

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11
Q

Gq:-what receptors stimulate it?-what are its effects?

A

-Stimulated by alpha 1, M1, M3, H1, V1-stimulates phospholipase C, which stimulates lipid conversion to PIP2, which stimulates increased diacylglycerol and increased inositol triphosphate. –> increased DAG leads to increased protein kinase C–> increased

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12
Q

Gs:-what receptors stimulate it?-what are its effects?

A

-stimulated by: B1, B2, D1, H2, V2-stimulates adenylyl cyclases –> increases cAMP –> increases protein kinase A –> increased intracellular Calcium *lots of bacterial toxins use this mechanism!

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13
Q

Gi:-what receptors stimulate it?-what are its effects?

A

-stimulated by: alpha 2, M2, D2-inhibits adenylyl cyclase (so decreased cAMP and decreased protein kinase A)…

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14
Q

alpha 1 receptor:-which G-protein class?-Major functions?

A

GqFunctions:-increase vascular smooth muscle contraction (increase BP)-mydriasis-increase intestinal and bladder sphincter muscle contraction

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15
Q

alpha 2 receptor:-G-protein class?-major functions?

A

GiMajor functions:-decrease sympathetic outflow (decrease NE secretion)-decrease insulin release-decrease BP (vasodilation)-increase glucagon secretion from alpha cells in pancreas

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16
Q

Beta 1 receptor:-G-protein class?-Major functions?

A

GsFunctions:-increase HR-increase contractility-increase renin release-increase lipolysis

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17
Q

Beta 2 receptor:-G-protein class?-Major functions?

A

GsFunctions:-vasodilation-bronchodilation-increase HR (compensatory to increase BP)-increase contractility-increase lipolysis-increase insulin release-decrease uterine tone

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18
Q

M1 receptor:-G protein?-Functions?

A

GqFunctions:-CNS, enteric nervous system

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19
Q

M2 receptor:-G-protein?-Functions?

A

GiFunctions:-decreased HR and contractility of atria

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20
Q

M3 receptor: -G-protein?-Functions?

A

GqFunctions:-increase exocrine gland secretions (ie sweat, gastric acid)-increase gut peristalsis-increase bladder contraction-bronchoconstriction-increase miosis-accommodation (ciliary muscle contraction)

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21
Q

D1 receptor:-G-protein?-Functions?

A

GsFunctions:-relaxes renal vascular smooth muscle

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22
Q

D2 receptor:-G protein?-Functions?

A

GiFunctions:-modulates transmitter release, especially in brain

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23
Q

H1 receptor:-G protein?-Functions?

A

GqFunctions:-increase nasal and bronchial mucus production-bronchiole contraction-pruritus-pain

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24
Q

H2 receptor:-G protein?-Functions?

A

GsFunctions:-increase gastric acid secretion

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25
Q

V1 receptor:-G protein?-Functions?

A

GqFunctions:-increase vascular SM contraction

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26
Q

V2 receptor:-G protein?-Functions?

A

GsFunctions:-increase H20 permeability and reabsorption in the collecting tubules of the kidney(“V2 is found in the 2 kidneys”)

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27
Q

What class of drugs are these:Bethanochol, Carbachol, Pilocarpine, Methacholine?

A

Cholinomimetic agents: Direct agonists

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28
Q

What class of drugs are these:Neostigmine, Pyridostigmine, Edrophonium, Physostigmine, Echothiophate, Donepezil

A

Cholinomimetic agents: Indirect agonists = anti-cholinesterases

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29
Q

What class of drugs are these:Atropine, homatropine, tropicamide, benztropine, scopolamine, ipratropium, oxybutynin, glycopyrrolate, methscopolamine, pirenzepine, propantheline

A

muscarinic antagonists = cholinergic antagonists

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30
Q

List the direct agonists/cholinomimetic agents (X4):

A

NAME?

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31
Q

List the indirect agonists/cholinomimetic agents = anticholinesterases (X6)

A

NAME?

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32
Q

List the muscarinic antagonists;

A

NAME?

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33
Q

Cholinesterase inhibitor poisoning symptoms (ie excess parasympathetic activity): Antidote to anti-AchE poisoning?

A

NAME?

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34
Q

What’s parathion?

A

Parathion = insecticide = organophosphate; causes cholinesterase-inhibitor poisoning (DUMBBELSS)

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35
Q

When do you give atropine + pralidoxime?

A

Give as an antidote to organophosphate poisoning/ Cholinesterase-inhibitor poisoning

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36
Q

Atropine:-class of drug?-clinical uses?-effects on eyes, airway, stomach, gi, bladder?-toxicity?

A

atropine = muscarinic antagonistused to treat bradycardia and for ophthalmic applicationseffects: blocks DUMBBELSS!-Eye–> increases mydriasis, cycloplegia-Airway–>decreases secretions-stomach –> decreases acid secretions-GI –> decreases motility-bladder –> decreases urgency in cystitis*Toxicity: Hot as a hare, Dry as a bone, Red as a beet, Blind as a bat, Mad as a hatter, Bloated as a toad:-increased body temp, decreased sweating-rapid pulse-dry mouth; dry/flushed skin-cycloplegia (blurry, near vision)-constipation (and urinary retention in men with prostatic hyperplasia)-disorientation-acute angle-closure glaucoma in elderly-hyperthermia in infants

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37
Q

What sympathomimetic should be used to treat:-anaphylactic shock?-cardiogenic shock?-septic shock?

A

NAME?

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38
Q

Epinephrine:-type of drug-what receptors does it act on?-clinical applications

A

-direct sympathomimetic-acts on alpha 1, alpha 2, beta 1, beta 2-use for anaphylaxis, open angle glaucoma, asthma, hypotension (anaphylactic shock)

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39
Q

norepinephrine:-type of drug-what receptors does it act on?-applications

A

-direct sympathomimetic-acts on alpha 1, alpha 2, beta 1-use for hypotension (septic shock)

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40
Q

isoproterenol:-type of drug-what receptors does it act on?-applications

A

-direct sympathomimetic-acts equally on beta 1 and beta 2 receptors-used for AV block

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41
Q

dopamine:-type of drug-what receptors does it act on?-applications

A

-direct sympathomimetic-acts on all receptors, but its effects vary by dose:low dose –> acts on D1medium dose –> acts on B1 > B2*high dose –> acts on alpha 1 and alpha 2-used for shock (increases renal perfusion), heart failure

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42
Q

dobutamine:-type of drug-what receptors does it act on?-applications

A

-direct sympathomimetic-acts on Beta 1 mostly (also, slightly on alpha 1, alpha 2, beta 2)-used for heart failure, cardiac stress testing, cardiogenic shock

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43
Q

phenylephrine:-type of drug-what receptors does it act on?-applications

A

-direct sympathomimetic-acts on alpha 1 mostly (and a little on alpha 2)-used for pupillary dilation, vasoconstriction, nasal decongestion; good for stopping epistaxis

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44
Q

Metaproterenol, Albuterol, Salmeterol, Terbutaline:-types of drugs?-what receptors do they act on?-Applications

A

-direct sympathomimetics-B2-agonists (also act very slightly on B1)-Metaproterenol and Albuterol –> used for acute asthma-Salmeterol –> for long-term treatment of asthma-Terbutaline –> to reduce premature uterine contractions

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45
Q

Ritodrine:-type of drug-what receptors does it act on?-applications

A

-direct sympathomimetic-acts on B2 receptors ONLY!-used to reduce premature uterine contractions

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46
Q

List 3 indirect sympathomimetics:-What are their actions?-What are their clinical applications?

A

1) Amphetamines:-indirect general sympathetic agonist; release stored catecholamines-used for narcolepsy, obesity, ADD2) Ephedrine:-indirect general sympathetic agonist-release stored catecholamines-used for nasal decongestion, urinary incontinence, hypotension3) cocaine:-indirect general sympathetic agonist; uptake inhibitor-causes vasoconstriction and local anesthesia

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47
Q

clonidine and alpha-meythldopa:-type of drugs?-act on what type of receptor?-applications?

A

NAME?

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48
Q

-azole =

A

anti-fungal (ie ketoconazole)

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49
Q

-cillin =

A

penicillin (ie methicillin)

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50
Q

-cycline =

A

antibiotic, protein synthesis inhibitor (ie tetracycline)

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51
Q

-navir =

A

protease inhibitor (HIV trtmt) (ie saquinavir)

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52
Q

-triptan =

A

5-HT1B/1D-agonists (for migraines) (ie sumatriptan)

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53
Q

-ane=

A

inhalational general anesthetic (ie halothane)

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54
Q

-caine=

A

NAME?

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55
Q

-operidol=

A

butyrophenone (neuroleptic) (ie haloperidol)

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56
Q

-azine =

A

phenothiazine (neuroleptic, antiemetic) (ie chlorpromazine)

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57
Q

-barbital =

A

barbiturate (ie phenobarbital)

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58
Q

-zolam =

A

benzodiazepine (ie alprazolam)

59
Q

-azepam =

A

benzodiazepine (ie diazepam)

60
Q

-etine =

A

SSRI (ie fluoxetine)

61
Q

-ipramine =

A

TCA (ie imipramine)

62
Q

-triptyline =

A

TCA (ie amitriptyline)

63
Q

-olol =

A

beta-antagonist (ie propranolol)

64
Q

-terol =

A

beta2-agonist (ie albuterol)

65
Q

-zosin =

A

alpha 1-antagonist (ie prazosin)

66
Q

-oxin =

A

cardiac glycoside (inotropic agent) (ie digoxin)

67
Q

-pril =

A

ACE-inhibitor (ie captopril)

68
Q

-afil =

A

erectile dysfunction (ie sildenafil)

69
Q

-tropin =

A

pituitary hormone (ie somatotropin)

70
Q

-tidine =

A

H2-antagonist (ie cimetidine)

71
Q

-dronate =

A

bisphosphonate (for osteoporosis) (ie alendronate)

72
Q

-sartan =

A

Ang II-receptor-antagonist (ie losartan, valsartan)

73
Q

-chol =

A

cholinergic/muscarinic agonist (ie bethanechol, carbachol)

74
Q

-curium or -curonium =

A

paralytic drugs (non-depolarizing NM-blocking drugs; reversed with neostigmine) (ie atracurium, vecuronium)

75
Q

-stigmine =

A

anti-cholinesterase (ie neostigmine, physostigmine, pyridostigmine)

76
Q

-mustine =

A

nitrosureas (cross BBB, used to treat brain cancers)

77
Q

-statins =

A

HMG-coA reductase inhibitors (ie atorvastatin)

78
Q

-glitazones =

A

increase target cell response to insulin (ie rosiglitazone, pioglitazone)

79
Q

-bendazoles=

A

anti-parasitic (esp anti-helminthic)

80
Q

-dipine =

A

Ca-channel blockers (specifically dihyropyridine CCB’s) (ie nifedipine, amlodipine)

81
Q

-prost =

A

prostaglandin analogues (treat glaucoma) (ie unoprostone)

82
Q

-mab =

A

monoclonal antibody (ie infliximab, daclizumab)

83
Q

alpha 1 blockage leads to?alpha 2 blockage leads to?

A

alpha1-blockage –> vasodilationalpha2-blockage –> vasoconstriction

84
Q

phenoxybenzamine:-type of drug?-application?-toxicity?

A

-nonselective alpha-blocker (irreversible/non-competitive)-used for pheochromocytoma (use phenoxybenzamine before removing tumor)-toxicity: orthostatic hypotension, reflex tachycardia

85
Q

Phentolamine:-type of drug-application?

A

-nonselective alpha-blocker (reversible/competitive)-give to patients on MAO-inhibitors who eat tyramine-containing foods

86
Q

prazosin, terazosin, doxazosin:-types of drugs?-applications?-toxicity?

A

-alpha-1-selective-blockers-used for hypertension, urinary retention in BPH-toxicities: orthostatic hypotension with first dose; dizziness, headache (should give pts first dose before bed, while lying down)

87
Q

mirtazapine:-type of drug-application-toxicity

A

NAME?

88
Q

List the B1-selective antagonists (A BEAM):

A

Acebutolol (partial agonist)BetaxololEsmolol (short-acting)AtenololMetoprolol

89
Q

List the nonselective Beta-antagonists (Please Try Not being Picky)

A

PropranololTimololNadololPindolol

90
Q

List the partial beta-agonists (PAPA):

A

PindololAcebutolol

91
Q

Nonselective alpha and beta -antagonists:

A

CarvelidolLabetalol

92
Q

Clinical applications of beta-blockers:

A

-hypertension (decrease CO, decrease renin secrtion - by beta-receptor blockade on JGA cells)-angina pectoris (decrease HR and contractility, so have decreased O2 consumption of myocardium)-MI (metoprolol and carvedilol –> decrease mortality from MIs)-SV

93
Q

Toxicity of Beta-blockers

A

-impotence!-exacerbates asthma-CV adverse effects (bradycardia, AV block, CHF)-CNS adverse effects (sedation, sleep alterations)-use caustiously with diabetics! (b/c B-blockers block sympathetically-mediated symptoms of hypoglycemia; so, patient won’t be

94
Q

Bethanechol applications

A

Bethanecol = direct cholinomimetic-used for postoperative and neurogenic ileus and urinary retention (activates Bowel and Bladder)

95
Q

Carbachol applications

A

carbachol = direct cholinomimetic-used for glaucoma, pupillary contraction, relief of intraocular pressure

96
Q

Pilocarpine applications

A

-pilocarpine = direct cholinomimetic-used to stimulate sweat, tears, saliva (“cry, spit, sweat on your pillow”)

97
Q

Which cholinomimetics are resistant to AChE?

A

Bethanechol, Pilocarpine

98
Q

Methacholine applications?

A

methacholine = direct cholinomimetic-used as a challenge test to diagnose asthma

99
Q

Neostigmine applications?

A

neostigmine - anticholinesterase (indirect cholinomimetic)-used for postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of NM jxn blockade-increases endogenous ACh; does not penetrate the CNS

100
Q

Pyridostigmine applications?

A

pyridostigmine = anticholinesterase (indirect cholinomimetic)-used for myasthenia gravis (gets RID of MG)-does not penterate CNS-increases endogenous ACh

101
Q

Edrophonium applications

A

endrophonium = anticholinesterase (indirect cholinomimetic)-used to diagnose myasthenia gravis-increases endogenous Ach

102
Q

Physostigmine applications

A

physostigmine = anticholinesterase (indirect cholinomimetic)-used to treat glaucoma and atropine overdose (“phyxes” atropine OD)-crosses the BBB!-increases endogenous Ach

103
Q

Echothiophate applications

A

echothiphate = anticholinesterase (indirect cholinomimetic)-used to treat glaucoma-increases endogenous Ach

104
Q

Donepezil applications

A

donepezil = anticholinesterase (indirect cholinomimetic)-used to treat Alzheimer’s disease-increases endogenous Ach!

105
Q

pKa = acid dissociation constant = ?

A

pKa = pH at which amount of the non-protonated form = the amount of the protonated form

106
Q

if pH < pKa…

A

acidic environment; have more of the protonated form (so, basic drugs get trapped)

107
Q

if pH > pKa…

A

basic environment; have more of the nonprotonated form (acidic drugs get trapped)

108
Q

Treat acidic drug OD (ie slicylates) with?

A

NaHCO3 (traps the acidic drug in the basic urine)

109
Q

Treat basic drug OD (ie amphetamines) with?

A

NH4Cl (ammonium chloride; traps basic drug in the acidic urine)

110
Q

What class of drugs can cause excess parasympathetic activity (ie DUMBBELSS symptoms)?

A

Cholinomimetic agents

111
Q

What drug regenerates AchE after organophosphate poisoning?

A

Pralidoxime (regenerates active AchE) (also, give atropine to treat symptoms!)

112
Q

What are the symptoms of inhibiting parasympathetic activity?

A

(ie atropine side effects)Hot as a hareDry as a boneRed as a beetBlind as a batMad as a hatterBloated as a toad

113
Q

In what populations is atropine contraindicated?

A

-Glaucoma (because don’t want to dilate eyes)-BPH or any urinary retention-GI obstruction (ie ileus)-Dementia or Elderly (because can cause delirium)-Infant with fever (because can cause hyperthermia)-

114
Q

List 4 classes of drugs with anti-cholinergic side effects:

A

1) First generation H1-Blockers (diphenhydramine, doxylamine, chlorpheniramine)2) Traditional neuroleptics3) TCAs4) Amantadine

115
Q

List 4 treatment options for Myasthenia Gravis:

A

1) Anti-cholinesterases (indirect cholinergic agonists)2) Corticosteroids (because MG = autoimmune disease)3) Thymectomy (often curative)4) Plasmapheresis

116
Q

What are the 5 classes of drugs used to treat glaucoma?

A

1) alpha-agonists2) beta-blockers3) Diuretics (Carbanic anhydrase inhibtors and mannitol)4) cholinomimetics5) prostaglandins

117
Q

P-450 Inducers

A

Barb Steals Phen-phen and Refuses Greasy Carbs Chronically:BarbituratesSt. John’s wortPhenytoinRifampinGriseofulvinCarbamazepineChronic alcohol use

118
Q

P-450 inhibitors

A

Q-MAGIC RACKS:QuinidineMacrolidesAmiodaroneGrapefruit juiceIsoniazidCimetidineRitonavirAcute alcohol abuseCiprofloxacinKetoconazoleSulfonamides

119
Q

acetaminophen antidote? (toxic dose = 4 g/day = 8 extra-strength tablets)

A

N-acetylcysteine (replenishes glutathione)

120
Q

salicylates (ie aspirin) antidote?

A

NaHCO3 (alkalinizes urine)Dialysis

121
Q

amphetamines antidote

A

NH4Cl (acidifies urine)

122
Q

anti-acetylcholinesterase and organophosphates antidote?

A

Atropine + Pralidoxime

123
Q

antimuscarinic, anticholinergic agents (ie atropine) antidote?

A

physostigmine salicylate

124
Q

beta-blockers antidote?

A

(same as verapamil antidote!) = glucagon, calcium, atropine (all increase HR)

125
Q

Iron antidote

A

deferoxamine

126
Q

lead antidote

A

CaEDTA (in adults)Dimercaprolsuccimer (in kids)penicillamine

127
Q

mercury, arsenic, gold antidote

A

-dimercaprol (BAL) (dimes = money = gold; merc = mercury!)-succimer

128
Q

copper, arsenic, gold antidote

A

penicillamine (copper pennies!)

129
Q

cyanide antidote

A

(may get cyanide poisoning from nitroprusside, used for malignant HTN; also, from house fires – see CN toxicity along with CO poisoning)-nitrite-hydroxocobalamin-thiosulfate

130
Q

Carbon monoxide antidote

A

100% O2Hyperbaric O2

131
Q

opioids antidote

A

naloxone/naltrexone

132
Q

benzodiazepines antidote

A

flumazenil

133
Q

TCAs antidote

A

NaHCO3 (plasma alkalinization)

134
Q

Heparin antidote

A

protamine (H+ = Proton-amine!)

135
Q

Warfarin antidote

A

vitamin Kfresh frozen plasma

136
Q

tPA, streptokinase, urokinase antidote?

A

Aminocaproic acid

137
Q

theophylline antidote

A

Beta-blocker(theophylline is an option for COPD pts; it has a low TI with cardio-toxicity; so, give beta-blockers for the cardio-toxic effects)

138
Q

Verapamil antidote

A

same as beta-blocker antidote! = glucagon, calcium, atropine (all increase HR)

139
Q

Digitalis antidote

A

-Normalize K+ and Mg2+-lidocaine (if there’s tachyarrhythmia) -anti-dig fab fragments (if there’s arrhythmia)-atropine (if there’s bradycardia)

140
Q

methemoglobin antidote

A

-methylene blue-vitamin C

141
Q

methanol, ethylene glycol (anti-freeze) antidote

A

-Fomepizole = 1st choice! (inhibits alcohol dehydrogenase)-2nd choices = ethanol, dialysis

FirstAID (24 decks)

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