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Pharm Flashcards

1
Q

Km

A

=[S] at 1/2 Vmax; inverse to affinity for substrate

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2
Q

Vmax

A

Directly proportional to enzyme concentration (V of saturation)

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3
Q

Competitive inhibitor

A

Same Vmax, lower Km (takes longer to reach vmax); reversible

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4
Q

Noncompetitive inhibitor

A

Higher Km, lower Vmax

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5
Q

Cooperative kinetics

A

Sigmoid curve (like hemoglobin)

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6
Q

Most enzymes have a ____ curve

A

Hyperbolic

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7
Q

On a lineweaver burk plot

A

High y intercept = lower V max (1/V on Y axis); further right x intercept (closer to zero) –> higher Km, lower affinity

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8
Q 
Reversible competitive inhibitors -- 
Resemble substrate
Overcome by increased [S]
Bind active site
Effect on Vmax
Effect on Km
Pharmacodynamics
A 
Resemble substrate: yes
Overcome by increased [S]: yes
Bind active site: yes
Effect on Vmax: no change
Effect on Km: increased
Pharmacodynamics: decreased potency
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9
Q 
Irreversible competitive inhibitors --
Resemble substrate
Overcome by increased [S]
Bind active site
Effect on Vmax
Effect on Km
Pharmacodynamics
A 
Resemble substrate: yes
Overcome by increased [S]: no
Bind active site: yes
Effect on Vmax: decreased
Effect on Km: no change
Pharmacodynamics: decreased efficacy
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10
Q 
Noncompetitive inhibitors --
Resemble substrate
Overcome by increased [S]
Bind active site
Effect on Vmax
Effect on Km
Pharmacodynamics
A 
Resemble substrate: yes
Overcome by increased [S]: no
Bind active site: yes
Effect on Vmax: decreased
Effect on Km: no change
Pharmacodynamics: decreased efficacy
Compared to uncompetitive -- binds equally well no matter whether substrate is bound
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11
Q

Uncompetitive inhibitor

A

Only binds to an enzyme bound to substrate

Decreases Vmax, decreases Km (increased sticking in enzyme); parallel on LB plot

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12
Q

Vd=

A

Amount drug in body/plasma drug conc

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13
Q

Low Vd compartment and type

A

Intravascular large/charged molecules often bound to plasma proteins

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14
Q

Medium Vd compartment and type

A

ECF small hydrophilic molecules

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15
Q

High Vd compartment and type

A

All tissues including fat, small lipophilic molecules, esp if bound to tissue protein

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16
Q

CL=

A

rate of elimination/plasma drug conc. (volume of plasma cleared of drug per unit of time)
aka Vd*Ke (elimination const)

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17
Q

How many half lives to reach steady state in 1st order kinetics?

A

4-5

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18
Q

How many half lives to reach 90% of steady state in first order kinetics?

A

3.3

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19
Q

T1/2 in first order kin=

A

(0.693*Vd)/CL

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20
Q

Loading dose=

A

(Cp*Vd)/F
Where Cp is conc. at steady state
F is bioavailability

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21
Q

Maintenance dose=

A

(CpCLt)/F
Where Cp is conc at steady state
F is bioavailability
t is dosage interval

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22
Q

In renal and liver disease, how do maintenance doses change?

A

Maintenance goes down

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23
Q

In renal and liver disease, how do loading doses change?

A

Loading dose doesn’t change (trick q)

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24
Q

Additive drug effect

A

Effect of A+B=sum of individual effects

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25
Q

Permissive drug effect

A

Need A for proper fxn of B

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26
Q

Synergistic drug effect

A

A+B together > sum of their effects individually

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27
Q

Tachyphlactic drug interaction

A

Acute decrease in reponse to drug after initial/repeated admin

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28
Q

Zero order elim

A

Rate of elim constant regardless of Cp; eg Phenytoin, ethanol, aspirin at high conc. (constant AMOUNT)

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29
Q

First order elim

A

Rate of elim directly proportional to drug conc. (constant FRACTION), Cp decreases exponentially w/ time; e.g. most drugs

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30
Q

Weak acids and how to get rid of them in overdose

A

Ex: phenobarb, methotrexate, aspirin

Trapped in basic environments – give sodium bicarb to alk the urine

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31
Q

Weak bases and how to get rid of them in overdowse

A

Ex: amphetimines, TCAs

Trapped in acidic environments – give ammonium Cl to acidify urine

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32
Q

Phase I metabolism

A

Reduction, oxidation, hydrolysis w P50 –> slightly polar, water soluble metabolites (often still active)

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33
Q

First type of metabolism lost w/ age

A

Phase I

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34
Q

Phase II metabolism

A

Conjugation (Methylation, glucuronidation, acetylation, sulfation) –> very polar inactive metabolites that can be renally excreted
Slow acetylators have increased side effects from some drugs due to slower metabolism

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35
Q

Efficacy

A

Maximal effect a drug can produce (Vmax)

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36
Q

Partial agonist efficacy vs full agonist efficacy

A

Partial

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37
Q

Potency

A

Amount of drug needed for a given effect (EC50 – i.e. 50% of maximal effect)

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38
Q

Left shift in potency=

A

Lower EC50, higher potency, less drug needed for an effect

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39
Q

Competitive antagonist

A

Right shift in curve –i.e. lower potency, but same efficacy and can be overcome by increased substrate conc

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40
Q

Noncompetitive antagonist

A

Shifts curve down (lower efficacy) – not able to be overcome by a higher [S]

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41
Q

Partial agonists

A

Same site as a full agonist, decreases efficacy, potency independent

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42
Q

Therapeutic index

A

Measurement of drug safety

TD50/ED50 (toxic median dose/effective median dose)

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43
Q

Therapeutic window

A

Dosage range to safely/effectively treat disease

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44
Q

Lower TI drugs

A

Require monitoring; eg Warfarin, theophylline, dig, Li,

“Warning These Drugs are Lethal!”

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45
Q

All first synapses are

A

Ach on Nicotinic receptors

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46
Q

PNS has long/short pre synaptic

A

Long

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47
Q

SNS has long/short pre synaptic

A

Short

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48
Q

Exception to SNS rules

A

Sweat glands – Ach on M like PNS

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49
Q

alpha1

A

Gq

Vascular smooth muscle contraction, pupillary dilator contracts (mydriasis); intestinal/bladder sphincter contraction

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50
Q

alpha2

A

Gi

Less sympathetic outflow, less insulin release, less lipolysis, increased platelet agg, less aqueous humor made

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51
Q

beta1

A

Gs

Increased heart rate, increased contractility, renin released, increased lipolysis

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52
Q

beta2

A

Gs
Vasodilation, bronchodilation, increased lipolysis, increased insulin release, less uterine tone (tocolysis), ciliary muscle relaxation, more aqueous humor

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53
Q

beta3

A

Gs

Increased lipolysis, thermogenesis in skeletal m, bladder relaxation

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54
Q

M1

A

Gq

Higher cognitive fxns, stimulates enteric nervous system

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55
Q

M2

A

Gi

Lower heart rate, less atrial contractility

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56
Q

M3

A

Gq
Increases exocrine gland secretions (lacrimal, sweat, salivary, gastric acid), causes gut peristalsis, bladder contraction, bronchoconstriction, pupillary muscle contraction (miosis), ciliary muscle contraction (accomodation), increases release of insulin

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57
Q

D1

A

Gs

Relaxes renal vascular smooth muscle, activates direct pathway of striatum

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58
Q

D2

A

Gi
Modulates transmitter release (esp in brain), inhibition of indirect pathway of striatum

(GI, Inhibition Indirect path)

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59
Q

H1

A

Gq

Nasal and bronchial muscus production, vascular permeability, contraction of bronchioles, pruritus, pain

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60
Q

H2

A

Gs

Gastric acid secretion

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61
Q

V1

A

Gq

Vascular smooth muscle contraction

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62
Q

V2

A

Gs

H2O permeability and reabsorption in collecting tubules of kidney

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63
Q

Gq receptor examples and effector enzyme

A

H1, alpha1, V1, M1, M3
“HAVe 1 M&M”
Works via PLC (Ca/PKC)

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64
Q

Gs receptor examples and effector enzyme

A

B1, B2, B3, D1, H2, V2

Works via AC upregulation

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65
Q

Gi receptor examples and effector enzyme

A

M2, alpha2, D2

Works via AC downregulation

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66
Q

NE self regulation

A

Via alpha2 autoreceptors

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67
Q

Selective beta blockers (6)

A

B1 – acebutolol (partial agonist), atenolol, betaxolol, bisoprolol, esmolol, metoprolol

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68
Q

Non selective beta blockers (4)

A

Nadolol, pindolol (partial agonist), propanolol, timolol

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69
Q

Nonselective beta/alpha blockers

A

Labetolol, carvedilol

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70
Q

Special beta blockers

A

Nebivolol – cardiac selective B1, stim of B3 in vasculature –> NO synthase –> reduces SVR

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71
Q

B blockers that reduce mortality in HF

A

Bisoprolol, carvedilol, metoprolol

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72
Q

B blocker partial agonists

A

Pindolol, acebutalol (don’t use in heart failure)

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73
Q

Tetrodotoxin – source, action, symptoms, tx

A

Pufferfish – highly potent, binds voltage gated Na channels in heart/nerve –> prevents depolarization –> leads to nausea, diarrhea, paresthesias, weakness, dizziness, lost of reflexes (tx supportive)

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74
Q

Ciguatoxin – source, action, symptoms, tx

A

Reef fish (barracuda, snapper, moray eel) –> opens Na channels –> depolarization –> NVD, perioral numbness, reversal of hot/cold sensations, bradycardia, heart block, hypotension (tx supportive)

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75
Q

Histaime (scombroid poisoning) – source, action, symptoms, tx

A

From spoiled dark-meat fish like tuna, mahimahi, mackerel, bonito –> bacterial histidine decarboxylase causes histadine –> histamine –> mimics anaphylaxis (tx: antihistamines, albuterol and epi if needed)

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76
Q

Beers drugs

A
  • Anticholinergics, antihistamines, antidepressants, benzos, opioids (increase risk of delirium, sedation, falls, constipation, urinary retention)
  • Alpha blockers (increases risk of hypotension)
  • PPs (increase c diff risk)
  • NSAIDs (increased risk of GI bleeds, esp w anticoags)
77
Q

Acetaminophen overdose tx

A

N-acetylcystein (replenishes glutathione)

78
Q

AChE inhibitors, organophosphates overdose tx

A

Atropine > pralidoxime (muscle)

79
Q

Antimuscarinic, anticholinergic agents overdose tx

A

Physostigmine, control hyperthermia

80
Q

Arsenic overdose tx

A

Dimercaprol, succimer

81
Q

Benzos overdose tx

A

Flumazenil

82
Q

B blockers overdose tx

A

Glucagon, atropine

83
Q

CO overdose tx

A

100%/hyperbaric O2

84
Q

Cu overdose tx

A

Penicillamine, trientine

85
Q

Cyanide overdose tx

A

Nitrate + thiosulfate, hydroxocobalamin

86
Q

Dig overdose tx

A

Anti-dig Fab fragments

87
Q

Heparin overdose tx

A

Protamine sulfate

88
Q

Fe overdose tx

A

Deferoxamine, deferasirox, deferiprone

89
Q

Pb overdose tx

A

EDTA, dimercaprol, succimer, penicillamine

90
Q

Mercury overdose tx

A

Dimercaprol, succimer

91
Q

Methanol, ethylene glycol (antifreeze) overdose tx

A

Fomepizole>ethanol, dialysis

92
Q

Methemoglobin overdose tx

A

Methylene blue, vit C

93
Q

Opioids overdose tx

94
Q

Salicylates overdose tx

A

NaHCO3 (alkalinize urine), dialysis

95
Q

TCAs overdose tx

A

NaHCO3 (alkalinize urine)

96
Q

Warfarin overdose tx

A

VIt K (delayed effect), FFP (immediate)

97
Q

Drugs causing coronary vasospasm

A

Amphetamines, cocaine, ergot alkaloids, sumatriptan

98
Q

Drugs causing cutaneous flushing

A

Vanco, Adenosine, Niacin, Nitrates, Ca2+ channel blockers, Echinocandins

VANNCE

99
Q

Drugs causing dilated cardiomyopathy

A

Anthracyclines (doxorubicin, daunorubicin), prevent w/ dexrazoxane

100
Q

Drugs causing torsades

A

AntiArrhythmics (Class Ia, III), antiBiotics (macrolides), anti”C”ycotics (haloperidol), antiDepressants (TCAs), antiEmetics (ondansetron)
ABCDE

101
Q

Drugs causing adrenocortical insufficiency

A

HPA suppression 2o to glucocorticoid w/drawal

102
Q

Drugs causing diabetes insipidis

A

Li, demeclocycline

103
Q

Drugs causing hot flashes

A

Tamoxifen, clomiphene

104
Q

Drugs causing hyperglycemia

A

Tacrolimus, Protease inhibs, Niacin, HCTZ, Corticosteroids

Taking Pills Necessitates Having Blood Checked

105
Q

Drugs causing hypothyroidism

A

Li, amiodarone, sulfonamides

106
Q

Drugs causing SIADH

A

Carbamazepine, Cyclophosphamide, SSRIs

Can’t Concentrate Serum Sodium

107
Q

Drugs causing acute cholestatic hepatitis/jaundice

A

Erythromycin

108
Q

Drugs causing diarrhea

A

Acamprosate, acarbose, cholinesterase inhibs, colchicine, erythromycin, ezetimibe, metformin, misoprostol, orlistat, pramlintide, quinidine, SSRIs

109
Q

Drugs causing focal-massive hepatic necrosis

A

Halothane, Amanita phalloides, Valproic acid, ACetaminophen

Liver HAVAC

110
Q

Drugs causing hepatitis

A

Rifamipin, isoniazid, pyrazinamide, statins, fibrates

111
Q

Drugs causing pancreatitis

A

Didanosine, Corticosteroids, Alcohol, Valproic acid, Azathioprine, Diuretics (furosemide, HCTZ)

Drugs Causing A Violent Abdominal Distress

112
Q

Drugs causing pill-induced esophagitis

A

Bisphosphonates, ferrous sulfates, NSAIDs, KCl, tetracyclines
(Minimize w/ upright posture and water intake)

113
Q

Drugs causing pseudomembranous colitis

A

Ampicillin, cephalosporins, clindamycin, fluoroquinolones

114
Q

Drugs causing agranulocytosis

A

Clozpine, Carbamazepine, PTU, Methimazole, Colchicine, Ganciclovir

Can Cause Pretty Major Collapse of Granulocytes

115
Q

Drugs causing aplastic anemia

A

Carbemazepine, Methimazole, NSAIDs, Benzene, Chloramphenicol, PTU

Can’t Make New Blood Cells Properly

116
Q

Drugs causing direct Coombs positive hemolytic anemia

A

Methyldopa, penicillin

117
Q

Drugs causing DRESS

A

Allopurinol, anticonvulsants, abx, sulfa drugs

Potentially fatal and delayed, 2-8 wk latency –> fever, morbilliform rash, multiorgan involvement – tx w/ w/drawal and coricosteroids

118
Q

Drugs causing gray baby syndrome

A

Chloramphenicol

119
Q

Drugs causing hemolysis in G6PD def

A

Isoniazid, Sulfonamides, Dapsone, Primaquine, Aspirin, Ibuprofen, Nitrofurantoin

Hemolysis IS D PAIN

120
Q

Drugs causing megaloblastic anemia

A

HydroxYUREa, Phenytoin, Methotrexate, Sulfa drugs

YURE having a MEGABLAST with PMS

121
Q

Drugs causing thrombocytopenia

122
Q

Drugs causing thrombotic complications

A

Combined OC, hormone replacement therapy, SERMs (tamoxifen, raloxifene, clomiphene) – estrogen mediated

123
Q

Drugs causing fat redistribution

A

Protease inhibitors, Glucocorticoids

Fat PiG

124
Q

Drugs causing gingival hyperplasia

A

Phenytoin, Ca channel blockers, cyclosporine

125
Q

Drugs causing hyperuricemia

A

Pyrazinamide, Thiazides, Furosemides, Niacin, Cyclosporine

Painful Tophi Feed Need Care

126
Q

Drugs causing myopathy

A

Statins, fibrates, niacin, colchicine, daptomycin, hydrozychloroquine, IFN alpha, penicillamine, glucocorticoids

127
Q

Drugs causing osteoporosis

A

Corticosteroids, depot medrozyprogesterone acetate, GnRH agonists, aromatase inhibitors, anticonvulsants, heparin

128
Q

Drugs causing photosensitivity

A

Sulfonamides, Amiodarone, Tetracyclines, 5 Fu

SAT For Photo

129
Q

Drugs causing rash (SJS)

A

Antiepileptics (esp lamotrigine), allopurinol, sulfa drugs, penicillin

Steven Johnson has epileptic allergy to sulf drugs and penicillin

130
Q

Drugs causing SLE like syndrome

A

Sulfa drugs, Hydralazine, Isoniazid, Procainamide, Phenytoin, Etanercept

Having lupus is SHIPP-E

131
Q

Drugs causing teeth discoloration

A

Tetracyclines (teethracyclines)

132
Q

Drugs causing tendonitis, tendon rupture, and/or cartilage damage

A

Fluoroquinolones

133
Q

Drugs causing cinchonism

A

Quinidine, quinine (tinnitus, hearing/vision loss, psychosis, cognitive impairment)

134
Q

Drugs causing parkinson-like syndrome

A

Antipsychotics, Reserpine, Metoclopramide

Cogwheel rigidity of ARM

135
Q

Drugs causing seizures

A

Isoniazid (in B6 def), Bupropion, Imipenem/cilastin, Tramadol, Enflurane

with seizures I BITE my tongue

136
Q

Drugs causing tardive dyskinesia

A

Antipsychotics, metoclopramide

137
Q

Drugs causing Fanconi syndrome

A

Cisplatin, ifosfamide, expired tetracyclines, tenofovir

138
Q

Drugs causing hemorrhagic cystitis

A

Cyclophosphamide, isofosfamide (prevent by coadmin of mesna)

139
Q

Drugs causing interstitial nephritis

A

Penicillins, furosemides, NSAIDs, PPIs, sulfa drugs

140
Q

Drugs causing dry cough

A

ACE inhibs

141
Q

Drugs causing pulmonary fibrosis

A

Methotrexate, Nitrofurantoin, Carmustine, Bleomycin, Busulfan, Amiodaron

My Nose Cannot Breate Bad Air

142
Q

Drugs causing antimuscarinic side effects

A

Atropine, TCAs, H1 blockers, antipsychotics

143
Q

Drugs causing disulfiram like reaction

A

1st gen Sulfanureas, Procarbazine, some Cephalosporins, Griseofulvin, Metronidazole

Sorry Pals Can’t Go Mingle

144
Q

Drugs causing nephro/ototoxicity

A

Aminoglycosides, vanco, loop diuretics, cisplatin, amphotericin B (cisplatin tox may respond to amifostine)

145
Q

P450 inducers (8)

A 
Chronic alcohol use
St johns wort
Phenytoin
Phenobarbitol
Nevirapine
Rifampin
Griseofulvin
Carbamazepine

Chronic alcoholics STeal PHEN PHEN and Never Refurse GReasy CARBs

146
Q

P450 substrates

A

Antiepileptics
Theophylline
Warfarin
OCPs

Always Think When Outdoors

147
Q

P450 Inhibitors (12)

A 
Sodium valproate
Isoniazid
Cimetidine
Ketoconazole
Fluconazole
Acute EtOH abuse
Chloramphenicol
Erythromycin (macrolides)
Sulfonamides
Ciprofloxacin
Omeprazole
Metronidazole

SICKFACES.COM

148
Q

Sulfa drugs (8)

A

Sulfonamide abx, Sulfasalazine, Probenecid, Furosemides, Acetazolamide, Celecoxib, Thiazides, Sulfonylureas

Scary Sulfa Pharm FACTS

149
Q

-azoles

A

Ergosterol synthesis inhibitor

150
Q

-bendazole

A

Antiparasitic/antihelminthic

151
Q

-cillin

A

TTPase (PBP)

152
Q

-cycline

A

Protein synth inhibitor

153
Q

-ivir

A

Neuraminidase inhibitor

154
Q

-navir

A

Protease inhibitor

155
Q

-ovir

A

DNA polymerase inhibitor

156
Q

-thromycin

A

Macrolide abx

157
Q

-ane

A

Inhalational general anesthetic

158
Q

-azine

A

Typical antipsychotic

159
Q

-barbital

A

Barbiturate

160
Q

-caine

A

Local anesthetic

161
Q

-etine

162
Q

-imipramine

163
Q

-triptyline

164
Q

-triptan

A

5HT1B/1D agonist

165
Q

-zepam

166
Q

-zolam

167
Q

-chol

A

Cholinergic agonist

168
Q

-curium

A

Nondepolarizing paralytic

169
Q

-curonium

A

Nondepolarizing paralytic

170
Q

-olol

171
Q

-stigmine

A

AchE inhib

172
Q

-terol

A

B2 agonist

173
Q

-zosin

A

A1 antagonist

174
Q

-afil

A

PDE5 inhib

175
Q

-dipine

A

DHP Ca channel blocker

176
Q

-pril

177
Q

-sartan

178
Q

-statin

A

HMG-CoA reductase inhib

179
Q

-xaban

A

Direct factor Xa inhib

180
Q

-dronate

A

Biphosphonate

181
Q

-glitazone

A

PPAR-gamma activator

182
Q

-prazole

183
Q

-prost

A

Prostaglandin analog

184
Q

-tidine

A

H2 antagonist

185
Q

-tinib

186
Q

-tropin

A

Pituitary hormone

187
Q

-ximab

A

Chimeric MAb

188
Q

-zumab

A

Humanized MAb

STEP (15 decks)

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