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Step 1 > Pharm > Flashcards

Pharm Flashcards

1
Q

Competitive inhibitor Reversible

A 
Resemble substrate, bind at active site
Overcome by increase substrate
Vmax: unchanged
Km: increased
decrease potency
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2
Q

Competitive inhibitor Irreversible

A 
Resemble substrate, bind at active site
NOT overcome by increase substrate
Vmax: decreased
Km: unchanged
decrease efficacy
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3
Q

Noncompetitive inhibitor

A 
Resemble substrate, DOES NOT bind at active site
NOT overcome by increase substrate
Vmax: decreased
Km: unchanged
decrease efficacy
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4
Q

Bioavailability

A

Fraction of administered drug reaching systemic circulation unchanged.
IV= 100%
F= AUC oral/ AUC IV

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5
Q

Volume of distribution

A

Theoretical volume occupied by the total amount of drug in the body relative to its plasma concentration.
Can be altered by liver and kidney disease (high Vd)
Vd= amount of drug in body / plasma concentration
Low –> intravascular
Medium –> ECF
High –> all tissues

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6
Q

Clearance

A

The time required to change the amount of drug in the body by 1/2 during elimination
First order- t1/2 = (.7*Vd) / CL

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7
Q

Loading dose

A

Cp*Vd/F

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8
Q

Maintenance dose

A

(Cp * CL *dosage interval) / F

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9
Q

Zero Order elimination

A

rate of elimination is constant regardless of Cp
Cp decreased linearly with time
Phenytoin, Ethanol, Aspirin

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10
Q

First order elimination

A

Directly proportional to drug concentration

Most drugs

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11
Q

Efficacy

A

Maximal effect a drug can produce

Vmax

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12
Q

Potency

A

Amount of drug needed for a given effect.

EC50

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13
Q

Competitive antagonist

A

Decrease potency
No change in efficacy
Can be overcome by increase agonist concentration

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14
Q

Noncompetitive antagonist

A

No change in potency
Decrease efficacy
Cannot be overcome by increase agonist concentration

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15
Q

Partial agonist

A

Independent of potency

Efficacy decreases

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16
Q

Therapeutic index

A

Measure of drug safety
TD50/ ED50
Safe drugs have high therapeutic index

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17
Q

Bladder control

A

Sympathetics: increase urinary retention
Parasympathetics: increase urine voiding

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18
Q

Urgency incontinence Meds

A 
Muscarinic antagonists (-M3 --> relax detrusor M --> decrease overactivity) Oxybutynin
Sympathomimetics (+B3 --> relax detrusor muscle --> increase bladder capacity) Miragegron
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19
Q

Urinary Retention meds

A

Muscarinic agonist (+M3 –> contract detrusor –> increase bladder emptying) Bethanechol

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20
Q

BPH meds

A 
a1 blockers (-a1 --> relax smooth muscle --> decrease urinary obstruction)
Tamsulosin
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21
Q

a1

A

Gq

increase vascular smooth muscle contraction, Mydriasis, increase intestinal and bladder sphincter muscle contraction

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22
Q

a2

A

Gi
decrease sympathetics, decrease insulin, decrease lipolysis, increase platelet aggregation, decrease aqueous humor production

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23
Q

B1

A

Gs

increase HR, contractility, renin, lipolysis

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24
Q

B2

A

Gs
vasodilation, bronchodilation, increase lipolysis, insulin, glycogenolysis, decrease uterine tone, increase aqueous humor production, increase cellular K+ intake

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25
Q

M1

A

Gq
mediates higher cognitive functions
Stimulate enteric nervous system

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26
Q

M2

A

Gi

decrease HR and contractility of atria

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27
Q

M3

A

Gq
increase exocrine gland secretions, increase gut peristalsis, increase bladder contraction, bronchoconstriction, miosis, ciliary M contraction, increase insulin, endothelium mediated vasodilation

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28
Q

D1

A

Gs

relax renal vascular smooth M, activate direct pathway of striatum

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29
Q

D2

A

Gi

modulate transmitter release in brain, inhibits indirect pathway of the striatum

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30
Q

H1

A

Gq

increase nasal and bronchial mucus production, increase vascular permeability, bronchoconstriction, pruritus, pain

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31
Q

H2

A

Gs

increase gastric acid secretion

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32
Q

V1

A

Gq

increase vascular smooth muscle contraction

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33
Q

V2

A

Gs

increase H2O permeability and reabsorption via up-regulating Aquaporin 2 in collecting tubules, increase release of vWF

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34
Q

Chilinomimetic agents

A

Watch for COPD, asthma and peptic ulcer

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35
Q

Bethanechol

A

activate bladder smooth muscle, resistant to AChE

Used for urinary retention

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36
Q

Carchachol

A

ACh but resistant to AChE

constricts pupil and relieves intraocular pressure in open angle glaucoma

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37
Q

Methacholine

A

stimulate M receptors in airway when inhaled

challenge test for asthma Dx

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38
Q

Pilocarpine

A

contract ciliary muscle of eye, pupillary sphincter
Resistant to AChE
can cross BBB
used to stimulate sweat, tears and saliva (Sjogrens, open and closed angle glaucoma)

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39
Q

Donepezil, rivastigmine, galantamine

A

increase ACh

Alzheimers

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40
Q

Edrophonium

A

increase ACh

diagnose MG

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41
Q

Neostigmine

A

increase ACh
No CNS penetration
postop and neurogenic ileus and urinary retentions, MG, reversal of NMJ blockade

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42
Q

Physostigmine

A

increase ACh
Cross BBB
Antidote for anticholinergic tox

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43
Q

Pyridostigmine

A

increase ACh
increase muscle strength
used with glycopyrrolate, hysocyamine or propantheline to control side effects
used for MG (long lasting)

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44
Q

Muscarinic anti AChE poisoning

A 
Diarrhea
Urination
Miosis
Bronchospasm
Brady
Emesis
Lacrimation
Sweating
Salivation
REVERSED BY ATROPINE
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45
Q

Nicotinic anti AChE poisoning

A

neuromuscular blockade

REVERSED BY PRALIDOXIME

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46
Q

CNS effects AChE poisoning

A

Respiratory depression, lethargy, seizures, coma

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47
Q

Produce mydriasis and cycoplegia

A

Atropine Homatropine, tropicamide

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48
Q

Parkinson Disease Acute Dystonia

A

Benzotropine trihexyphenidyl

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49
Q

Parenteral: preop use to reduce airway secretion
Oral: drooling, peptic ulcer

A

Glycopyrrolate

50
Q

Antispasmodics for IBS

A

Hyoscyamine

Dicyclomine

51
Q

COPD, asthma

A

ipratropiu

tiotropium

52
Q

Reduce bladder spasms and urge urinary incontinence (overactive bladder)

A

Oxybutynin
Solifenacin
tolterodine

53
Q

Motion sickness

A

Scopolamine

54
Q

Adverse effects of Atropine use

A

increase body temp, increase HR, dry mouth, flushed skin, cyclopegia, constipation, disorientation

55
Q

Albuterol, salmeterol, terbutaline

A 
B2>B1
increase heart rate
Albuterol for acute COPD/asthma
Salmeterol for long term COPD/ asthma
Terbutaline for bronchospasm in asthma and tocolysis
56
Q

Dobutamine

A

B1>B2, a
increase HR and CO
used in HF, cardiogenic shock, cardiac stress test

57
Q

Dopamine

A

D1=D2>B>a
increase BP, HR and CO
used in unstable brady, HF, shock

58
Q

Epinephrine

A

B>a
increase BP, HR and CO
used for anaphylaxis, asthma, open angle glaucoma

59
Q

Fenoldopam

A

D1
decrease BP, increase HR and CO
post op HTN, vasodilator. Promote natiuresis

60
Q

Isoproterenol

A

B1=B2

decrease BP, increase HR and CO

61
Q

Midodrine

A

a1
increase BP, decrease HR
used in autonomic insufficiency and postural hypotension

62
Q

Mirabegron

A

B3

used in urinary urgency or incontinence or overactive bladder

63
Q

Norepinephrine

A

a1>a2>B1
increase BP and HR
used in.hypotension, septic shock

64
Q

Phenylephrine

A

a1>a2
increase BP decrease HR
used in hypotension, ocular procedures, rhinitis, ischemic priapism

65
Q

Amphetamine

A

indirect agonist, reuptake inhibitor, release catecholamine stores
used in narcolepsy, obesity, ADHD

66
Q

Cocaine

A

indirect agonist, reuptake inhibitor
causes vasoconstriction and local anesthesia
If given B blockers –> extreme hypertension

67
Q

Ephedrine

A

indirect agonist, releases catecholamine stores

used in nasal decongestion, urinary incontinence, hypotension

68
Q

NE vs isoproterenol

A

NE causes reflex brady due to a1 effects

isoproterenol causes vasodilation and increased HR

69
Q

Clonidine, guanfacine

A

a2 agonist
Used in hypertensive urgency, ADHD, Tourette syndrome, symptom control in opioid withdrawal
Adverse: CNS depression, brady, hypotension, respiratory depression, miosis, rebound HTN with abrupt cessation

70
Q

a methyldopa

A

a2 agonist
used in HTN in pregnancy
Adverse: direct Coombs hemolysis, drug indcled lupus, hyperprolactinemia

71
Q

Tizanidine

A

a2 agonist
used for relief of spasticity
Adverse: hypotenion, weakness, xerostomia

72
Q

Phenoxybenzamine

A

Irreversible a blocker
Pheochromocytoma to prevent catecholamine crisis
adverse: orthostatic hypotension, reflex tachy

73
Q

Phentolamine

A

reversible a blocker
given to patients on MAO inhibitors who eat tyramine containing foods for severe cocaine induced hypertension
adverse: orthostatic hypotension, reflex tachy

74
Q

Prozasoin, terazosin, doxazosin, tamsulosin

A

a1 blockers
used in urinary symptoms of BPH, PTSD hypertension
adverse: 1st does, orthostatic hypotension, dizzy, HA

75
Q

Mirtazapine

A

a2 blocker
used in depression
adverse: sedation, increase serum cholesterol, increase appetite

76
Q

B blockers on angina pectoris

A

decrease HR and contractility –> low O2 consumption

77
Q

Glaucoma

A

Timolol

decrease aqueous humor production

78
Q

Heart Failure

A

Bisoprolol, Carvedilol, Metoprolol

decrease mortality

79
Q

B blockers of HTN

A

decrease CO, decrease renin secretion

80
Q

Hyperthyroidism

A

Propanolol

symptom control

81
Q

B blockers on Hypertrophic cardiomyopathy

A

decrease HR –> increase filling time, relieve obstruction

82
Q

B blockers for MI

A

decrease O2 demand, decrease mortality

83
Q

Supraventricular tachy

A

metoprolol, esmolol

decrease AV conduction velocity

84
Q

Variceal bleeding

A

Nadolol, propanolol, carvedilol

decrease hepatic venous pressure gradient and portal HTN

85
Q

Adverse for B blockers

A

ED, cardiovascular, CNS, dyslipidemia and asthma/COPD exacerbation

86
Q

B blocker B1>B2

A

acebutolol, atenolol, betaxolol, bisoprolol, esmolol, metoprolol

87
Q

Nonselective B blockers

A

nadolol, propanolol, timolol, pindolol

88
Q

Nonselective a and B antagonists

A

carvedilol, labetolol

89
Q

Theophylline

A

Nonspecific PDE inhibitor
decrease cAMP hydrolysis –> increase cAMP –> bronchial smooth muscle relaxation –> dilation
used in COPD/ asthma
adverse: cardiotox, ab pain, neurotox

90
Q

PDE5 inhibitors

A

-fil
decrease hydrolysis of cGMP –> increases cGMP –> increase smooth muscle relaxation by enhancing NO activity –> pulmonary vasodilation and increase blood blow to corpus cavernosum
used in erectile dysfunction, pulm HTN, BPH
adverse: flushing, HA, dyspepsia, hypotension in patients taking nitrites

91
Q

PDE4 inhibitors

A

roflumilast
increase cAMP in neutrophils, granulocytes, bronchial epithelium
used in severe COPD
adverse: ab pain, weight loss, mental disorders

92
Q

PDE3 inhibitors

A

Mirinone
in cardiomyocytes increase cAMP –> Ca influx –> increase ionotropy and chronotropy
in vascular smooth M increase cAMP –> MLCK inhibition –> vasodilation –> decrease preload and afterload
used in acute decompensated HF with cardiogenic shock
adverse: tachy, ventricular arrhythmias, hypotension

93
Q

Platelet inhibitors PDE inhibitor

A

Cilostazol, Dipyridamole
increase cAMP –> inhibit platelet aggregation
used in intermittent claudication, stroke or TIA prevention, cardiac stress test, prevent coronary stent restenosis
Adverse: nausea, HA, facial flushing, hypotension, ab pain

94
Q

Histamine Scromboid poisoning

A

Eating spoiled dark meat fish
Bacterial histidine decarboxylase converts histidine to histamine
Anaphylaxis symptoms
Treat with antihistamines, albuterol and epi if needed

95
Q

Tetrodotoxin

A

puffer fish
bind to VGNaC in nerve tissues preventing depolarization
Nausea diarrhea, paresthesias, weakness, dizzy, loss of refelxes

96
Q

Ciguatoxin

A

reef fish
open Na channels cause depolarization
Nausea, vomiting, diarrhea, perioral numbness, reversal of hot and cold sensations, brady, heart block, hypotension

97
Q

Beers criteria

A 
Dont give elderly
a blockers
anticholinergics, antidepressant, antihistamines or opioids
benzos
NSAIDs
PPIs
98
Q

Treat acetaminophen poisoing

A

NAC –> replenish glutathione

99
Q

Treat AChE inhibitors, organophosphate

A

Atropine > pralidoxime

100
Q

Antimuscarininc, anticholinergic tox

A

physiostigmine

101
Q

Arsenic tox

A

Dimercaprol, succimer

102
Q

Benzo tox

A

flumazenil

103
Q

B blocker tox

A

atropine, glucagon, saline

104
Q

CO tox

A

100% O2, hyperbaric O2

105
Q

Copper tox

A

penicillamine, trientine

106
Q

CN tox

A

Hydroxocobalamin, nitrates + sodium thiosulfate

107
Q

Digitalis tox

A

Digoxin Ab fragments

108
Q

Heparin tox

A

protamine sulfate

109
Q

Iron tox

A

deferoxamine, deferasirox, deferiprone

110
Q

Lead tox

A

EDTA, dimercaprol, succimer, penicillamine

111
Q

Mercury tox

A

dimercaprol, succimer

112
Q

Methanol tox (antifreeze)

A

fomepizole > ethanol, dialysis

113
Q

methoglobin tox

A

methylene blue, vit C

114
Q

opioid tox

A

naloxone

115
Q

Salicylates tox

A

NaHCO3

116
Q

TCA tox

A

NaHCO3

117
Q

Warfarin tox

A

vitamin K, PCC/FFP

118
Q

Drugs that cause coronary vasospasm

A

Cocaine, amphetamines, sumatriptan, ergot alkaloids

119
Q

Drugs that cause cutaneous flushing

A

vancomycin, adenosine, Niacin, CCB, echinocandins, Nitrates

Red man syndrome via vancomycin. Tx with diphenhydramine

120
Q

Drugs that cause dilated cardiomyopathy

A

Doxorubicin and Daunorubicin

treat with dexrazoxane

121
Q

Drugs that cause Torsades

A 
Class 1A and III antiarrhythmics
antibiotics (macrolides)
antipsychotics
antidepressants
antiemetics

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