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Pharm Flashcards

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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
M1
Gq mediates higher cognitive functions Stimulate enteric nervous system
26
M2
Gi | decrease HR and contractility of atria
27
M3
Gq increase exocrine gland secretions, increase gut peristalsis, increase bladder contraction, bronchoconstriction, miosis, ciliary M contraction, increase insulin, endothelium mediated vasodilation
28
D1
Gs | relax renal vascular smooth M, activate direct pathway of striatum
29
D2
Gi | modulate transmitter release in brain, inhibits indirect pathway of the striatum
30
H1
Gq | increase nasal and bronchial mucus production, increase vascular permeability, bronchoconstriction, pruritus, pain
31
H2
Gs | increase gastric acid secretion
32
V1
Gq | increase vascular smooth muscle contraction
33
V2
Gs | increase H2O permeability and reabsorption via up-regulating Aquaporin 2 in collecting tubules, increase release of vWF
34
Chilinomimetic agents
Watch for COPD, asthma and peptic ulcer
35
Bethanechol
activate bladder smooth muscle, resistant to AChE | Used for urinary retention
36
Carchachol
ACh but resistant to AChE | constricts pupil and relieves intraocular pressure in open angle glaucoma
37
Methacholine
stimulate M receptors in airway when inhaled | challenge test for asthma Dx
38
Pilocarpine
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)
39
Donepezil, rivastigmine, galantamine
increase ACh | Alzheimers
40
Edrophonium
increase ACh | diagnose MG
41
Neostigmine
increase ACh No CNS penetration postop and neurogenic ileus and urinary retentions, MG, reversal of NMJ blockade
42
Physostigmine
increase ACh Cross BBB Antidote for anticholinergic tox
43
Pyridostigmine
increase ACh increase muscle strength used with glycopyrrolate, hysocyamine or propantheline to control side effects used for MG (long lasting)
44
Muscarinic anti AChE poisoning
``` Diarrhea Urination Miosis Bronchospasm Brady Emesis Lacrimation Sweating Salivation REVERSED BY ATROPINE ```
45
Nicotinic anti AChE poisoning
neuromuscular blockade | REVERSED BY PRALIDOXIME
46
CNS effects AChE poisoning
Respiratory depression, lethargy, seizures, coma
47
Produce mydriasis and cycoplegia
Atropine Homatropine, tropicamide
48
Parkinson Disease Acute Dystonia
Benzotropine trihexyphenidyl
49
Parenteral: preop use to reduce airway secretion Oral: drooling, peptic ulcer
Glycopyrrolate
50
Antispasmodics for IBS
Hyoscyamine | Dicyclomine
51
COPD, asthma
ipratropiu | tiotropium
52
Reduce bladder spasms and urge urinary incontinence (overactive bladder)
Oxybutynin Solifenacin tolterodine
53
Motion sickness
Scopolamine
54
Adverse effects of Atropine use
increase body temp, increase HR, dry mouth, flushed skin, cyclopegia, constipation, disorientation
55
Albuterol, salmeterol, terbutaline
``` B2>B1 increase heart rate Albuterol for acute COPD/asthma Salmeterol for long term COPD/ asthma Terbutaline for bronchospasm in asthma and tocolysis ```
56
Dobutamine
B1>B2, a increase HR and CO used in HF, cardiogenic shock, cardiac stress test
57
Dopamine
D1=D2>B>a increase BP, HR and CO used in unstable brady, HF, shock
58
Epinephrine
B>a increase BP, HR and CO used for anaphylaxis, asthma, open angle glaucoma
59
Fenoldopam
D1 decrease BP, increase HR and CO post op HTN, vasodilator. Promote natiuresis
60
Isoproterenol
B1=B2 | decrease BP, increase HR and CO
61
Midodrine
a1 increase BP, decrease HR used in autonomic insufficiency and postural hypotension
62
Mirabegron
B3 | used in urinary urgency or incontinence or overactive bladder
63
Norepinephrine
a1>a2>B1 increase BP and HR used in.hypotension, septic shock
64
Phenylephrine
a1>a2 increase BP decrease HR used in hypotension, ocular procedures, rhinitis, ischemic priapism
65
Amphetamine
indirect agonist, reuptake inhibitor, release catecholamine stores used in narcolepsy, obesity, ADHD
66
Cocaine
indirect agonist, reuptake inhibitor causes vasoconstriction and local anesthesia If given B blockers --> extreme hypertension
67
Ephedrine
indirect agonist, releases catecholamine stores | used in nasal decongestion, urinary incontinence, hypotension
68
NE vs isoproterenol
NE causes reflex brady due to a1 effects | isoproterenol causes vasodilation and increased HR
69
Clonidine, guanfacine
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
a methyldopa
a2 agonist used in HTN in pregnancy Adverse: direct Coombs hemolysis, drug indcled lupus, hyperprolactinemia
71
Tizanidine
a2 agonist used for relief of spasticity Adverse: hypotenion, weakness, xerostomia
72
Phenoxybenzamine
Irreversible a blocker Pheochromocytoma to prevent catecholamine crisis adverse: orthostatic hypotension, reflex tachy
73
Phentolamine
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
Prozasoin, terazosin, doxazosin, tamsulosin
a1 blockers used in urinary symptoms of BPH, PTSD hypertension adverse: 1st does, orthostatic hypotension, dizzy, HA
75
Mirtazapine
a2 blocker used in depression adverse: sedation, increase serum cholesterol, increase appetite
76
B blockers on angina pectoris
decrease HR and contractility --> low O2 consumption
77
Glaucoma
Timolol | decrease aqueous humor production
78
Heart Failure
Bisoprolol, Carvedilol, Metoprolol | decrease mortality
79
B blockers of HTN
decrease CO, decrease renin secretion
80
Hyperthyroidism
Propanolol | symptom control
81
B blockers on Hypertrophic cardiomyopathy
decrease HR --> increase filling time, relieve obstruction
82
B blockers for MI
decrease O2 demand, decrease mortality
83
Supraventricular tachy
metoprolol, esmolol | decrease AV conduction velocity
84
Variceal bleeding
Nadolol, propanolol, carvedilol | decrease hepatic venous pressure gradient and portal HTN
85
Adverse for B blockers
ED, cardiovascular, CNS, dyslipidemia and asthma/COPD exacerbation
86
B blocker B1>B2
acebutolol, atenolol, betaxolol, bisoprolol, esmolol, metoprolol
87
Nonselective B blockers
nadolol, propanolol, timolol, pindolol
88
Nonselective a and B antagonists
carvedilol, labetolol
89
Theophylline
Nonspecific PDE inhibitor decrease cAMP hydrolysis --> increase cAMP --> bronchial smooth muscle relaxation --> dilation used in COPD/ asthma adverse: cardiotox, ab pain, neurotox
90
PDE5 inhibitors
-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
PDE4 inhibitors
roflumilast increase cAMP in neutrophils, granulocytes, bronchial epithelium used in severe COPD adverse: ab pain, weight loss, mental disorders
92
PDE3 inhibitors
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
Platelet inhibitors PDE inhibitor
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
Histamine Scromboid poisoning
Eating spoiled dark meat fish Bacterial histidine decarboxylase converts histidine to histamine Anaphylaxis symptoms Treat with antihistamines, albuterol and epi if needed
95
Tetrodotoxin
puffer fish bind to VGNaC in nerve tissues preventing depolarization Nausea diarrhea, paresthesias, weakness, dizzy, loss of refelxes
96
Ciguatoxin
reef fish open Na channels cause depolarization Nausea, vomiting, diarrhea, perioral numbness, reversal of hot and cold sensations, brady, heart block, hypotension
97
Beers criteria
``` Dont give elderly a blockers anticholinergics, antidepressant, antihistamines or opioids benzos NSAIDs PPIs ```
98
Treat acetaminophen poisoing
NAC --> replenish glutathione
99
Treat AChE inhibitors, organophosphate
Atropine > pralidoxime
100
Antimuscarininc, anticholinergic tox
physiostigmine
101
Arsenic tox
Dimercaprol, succimer
102
Benzo tox
flumazenil
103
B blocker tox
atropine, glucagon, saline
104
CO tox
100% O2, hyperbaric O2
105
Copper tox
penicillamine, trientine
106
CN tox
Hydroxocobalamin, nitrates + sodium thiosulfate
107
Digitalis tox
Digoxin Ab fragments
108
Heparin tox
protamine sulfate
109
Iron tox
deferoxamine, deferasirox, deferiprone
110
Lead tox
EDTA, dimercaprol, succimer, penicillamine
111
Mercury tox
dimercaprol, succimer
112
Methanol tox (antifreeze)
fomepizole > ethanol, dialysis
113
methoglobin tox
methylene blue, vit C
114
opioid tox
naloxone
115
Salicylates tox
NaHCO3
116
TCA tox
NaHCO3
117
Warfarin tox
vitamin K, PCC/FFP
118
Drugs that cause coronary vasospasm
Cocaine, amphetamines, sumatriptan, ergot alkaloids
119
Drugs that cause cutaneous flushing
vancomycin, adenosine, Niacin, CCB, echinocandins, Nitrates | Red man syndrome via vancomycin. Tx with diphenhydramine
120
Drugs that cause dilated cardiomyopathy
Doxorubicin and Daunorubicin | treat with dexrazoxane
121
Drugs that cause Torsades
``` Class 1A and III antiarrhythmics antibiotics (macrolides) antipsychotics antidepressants antiemetics ```

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