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Pharm Flashcards

1
Q 
Michaelis-Menten Kinetics 
Equation 
Vmax
Km
Curve
A

v = (Vmax[S])/(Km + [S])
Vmax directly proportional to enzyme concentration
Km inversely related to the affinity of the enzyme for its substrate
At 1/2 Vmax, Km=[S]
Hyperbolic

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2
Q

What kind of enzymatic reactions do not follow Michaelis-Menten Kinetics?

A

Enzymes that show cooperative kinetics (hemoglobin) have sigmoid curves

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3
Q 
Lineweaver-Burk Plot 
y axis
x axis
slope
y intercept 
x intercept
A 
1/V
1/[S]
Km/Vmax
1/Vmax. As y-intercept ↑, Vmax ↓
-1/Km. As x-intercept moves further to the right, ↑Km (lower affinity)
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4
Q

Lineweaver-Burk Plot
Competitive inhibitor
Noncompetitive inhibitor

A

Vmax stays the same as Km moves closer to the right. ↑Km (lower affinity)
y-intercept increases (↓Vmax) but Km (x-intercept) stays the same

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5
Q 
Competitive Inhibitors 
Resemblance to substrate
Over come by ↑[S]
Bind active site
Effect on Vmax
Effect on Km
Pharmacodynamics
A 
Resemble substrate 
Overcome by ↑[S]
Binds active site 
Vmax unchanged 
Km ↑
↓ potency
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6
Q 
NonCompetitive Inhibitors 
Resemblance to substrate
Over come by ↑[S]
Bind active site
Effect on Vmax
Effect on Km
Pharmacodynamics
A 
No resemblance to substrate 
Not overcome by ↑[S]
Doesn't binds active site 
Vmax ↓ 
Km unchanged 
↓ efficacy
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7
Q

Bioavailability
Variable
What is it?
When is it 100%

A

F
Fraction of administered dose that reaches systemic circulation unchanged
IV dose

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8
Q 
Volume of distribution 
Variable 
What is it?
When can it be altered?
Equation
A

Vd
Theoretical fluid volume required to maintain the total absorbed drug amount at plasma concentration
Vd of plasma-protein bound drugs can be altered by liver and kidney disease (↓ protein binding, ↑ Vd)
(Amount of drug in body)/(plasma drug concentration)

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9
Q

Low Vd
Volume
Distribution
Drug types

A

4-8L
Blood
Large/charged molecules; plasma protein bound

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10
Q

Medium Vd
Distribution
Drug types

A

ECF

Small hydrophilic molecules

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11
Q

High Vd
Distribution
Drug types

A

All tissues

Small lipophilic molecules, especially if bound to tissue protein

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12
Q

A drug infused at a steady state takes how many half lives to reach steady state?

A

4 to 5

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13
Q

Half Life
Property of…
Equation

A

First Order Elimination

(.7Vd)/CL

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14
Q 
Clearance 
Variable 
What is it?
Impaired with defect in what organ functions?
Equation (2)
A

CL
Relates rate of elimination to the plasma concentration
Impaired with defect in cardiac, hepatic, or renal function
(Rate of elimination)/(Plasma drug concentration) = Vd x Ke (elimination constant)

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15
Q

Loading dose

A 
Cp x (Vd/F)
Cp = target plasma concentration
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16
Q

Maintenance dose

A 
Cp x (CL/F)
Cp = target plasma concentration
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17
Q

What happens to loading dose and maintenance dose in liver or renal disease?

A

Loading dose remains the same

Maintenance dose ↓

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18
Q

Time to steady state depends primarily on

A

Half life

Independent of dosing frequency or size

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19
Q

Zero-Order Elimination
What is it?
How does Cp change?
Examples

A

Rate of elimination is constant regardless of Cp. Constant amount of drug eliminated per unit time
“PEA looks like a 0”
Phenytoin, EtOH, Aspirin (at high concentrations)

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20
Q

First-Order Elimination
What is it?
How does Cp change?
Description

A

Rate of elimination is directly proportional to the drug concentration. Constant fraction of drug eliminated per unit time
Cp ↓ exponentially with time
Flow-Dependent Elimination

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21
Q

Ionized vs non-Ionized species in the urine?
Weak Acids? What happens? Examples
Weak Bases? What happens? Examples

A

Ionized species trapped in the urine and cleared quickly. Neutral forms can be reabsorbed
Trapped in basic environments so treat OD with bicarb. Phenobarbital, Methotrexate, Aspirin
Trapped in acidic environments. Treat OD with Ammonium chloride. Amphetamines

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22
Q 
Drug Metabolism Phase 1
Reactions 
Mediator
Metabolites 
Lost in what kind of pt
A

RedOx or hydrolysis
Cytochrome P450
Usually yields slightly polar water soluble metabolites (often still active)
Lost in geriatric pts

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23
Q 
Drug Metabolism Phase 2
Reactions 
Metabolites
Excretion  
Decreased in what kind of pt
A 
"GAS"
Conjugation (Glucuronidation, Acetylation, Sulfation)
Very polar inactive metabolites 
Renally excreted 
Slow acetylators
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24
Q

Efficacy
Definition
Examples

A

Maximal effect a drug can produce

Analgesics, Antibiotics, Decongestants

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25
Q

Potency
Definition
Mechanism
Examples

A

Amount of drug needed for a given effect
↑ potency –> ↑ receptor affinity
Chemotherapeutic drugs, AntiHTN, AntiLipid

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26
Q 
Competitive Antagonist 
Shifts effect vs dose curve?
Potency 
Efficacy 
How can it be overcome?
Examples
A 
Shifts curve to Right
Potency ↓
No change in efficacy 
↑ [agonist]
Diazepam and Flumazenil @ GABA Receptor
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27
Q 
NonCompetitive Antagonist 
Shifts effect vs dose curve? 
Efficacy 
How can it be overcome?
Examples
A

Shifts curve down
Efficacy ↓
Cannot be overcome by ↑ [agonist]
NE and Phenoxybenzamine @ α receptors

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28
Q 
Partial Agonist
Where and how does it act? 
Shifts effect vs dose curve?
Potency 
Efficacy 
Examples
A

Acts at same site as full agonist but with reduced maximal effect
Left shift at low concentrations but then levels off sooner and at lower concentration
Variable
Efficacy ↓
Buprenorphine @ μ

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29
Q 
Therapeutic index
Measure of...
Formula 
Safe drugs have what kind of TI?
Unsafe drug examples
A

Measure of drug safety
“TILE”
(Median Lethal dose)/(Median Effective dose)
Safer drugs have high TI
Low TI: Digoxin, Li, Theophylline, Warfarin

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30
Q

Therapeutic Window
Measure of what?
What is it?
Safe drugs have…

A

Measure of clinical drug safety
Range of minimum effective dose to minimum toxic dose
Safe drugs have large TW

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31
Q

Antidote for Salicylates

A

NaHCO3 (alkalinize urine), Dialysis

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32
Q

Antidote for Amphetamines

A

NH4Cl (acidify urine)

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33
Q

Antidote for AChE Inhibitors and Organophosphates

A

Atropine, Pralidoxime

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34
Q

Antidote for AntiMuscarinics and AntiCholinergics

A

Physostigmine Salicylate and Control Hyperthermia

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35
Q

Antidote for β blockers

A

Glucagon

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36
Q

Antidote for Digitalis

A

“stay “KALM”

Normalize K, Anti dig Fab Fragment, Lidocaine, Mg

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37
Q

Antidote for Fe?

A

DeFEroxamine, deFErasirox

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38
Q

Antidote for Pb

A

EDTA, Dimercaprol, Succimer, Penicillamine

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39
Q

Antidote for Hg, Arsenic, or Gold?

A

Dimercaprol, Succimer

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40
Q

Antidote for Cu, Arsenic, or Gold

A

Penicillamine

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41
Q

Antidote for Cyanide

A

Nitrite + Thiosulfate, Hydroxocobalamin

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42
Q

Antidote for Methemoglobin

A

Methylene Blue, VitC

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43
Q

Antidote for CO

A

100% O2, Hyperbaric O2

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44
Q

Antidote for Methanol, Ethylene Glycol

A

Fomepizole, EtOH, Dialysis

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45
Q

Antidote for Opioids

A

Naloxone, Naltrexone

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46
Q

Antidote for Benzodiazepines

A

Flumazenil

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47
Q

Antidote for TCAs

A

NaHCO3 (plasma alkalinization)

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48
Q

Antidote for Heparin

A

Protamine Sulfate

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49
Q

Antidote for Warfarin

A

VitK, Fresh Frozen Plasma

50
Q

Antidote for tPA, Streptokinase, Urokinase

A

Aminocaproic Acid

51
Q

Antidote for Theophylline

A

β blockers

52
Q

Drugs that can cause Coronary Vasospasms

A

Cocaine, Sumatriptan, Ergot Alkaloids

53
Q

Drugs that can cause Cutaneous Flushing

A

“VANC”

Vancomycin, Adenosine, Niacin, Ca channel blockers

54
Q

Drugs that can cause Dilated Cardiomyopathy

A

Doxorubicin (Adriamycin), Daunorubicin

55
Q

Drugs that can TdP

A

Class III (Sotalol) and Class IA (Quinidine)

56
Q

Drugs that can cause Agranulocytosis

A

“Agranulocytosis Could Certainly Cause Pretty Major Damage”

Clozapine, Carbamazepine, Colchicine, Propylthiouracil, Methimazole, Dapsone

57
Q

Drugs that can cause Aplastic Anemia

A

Chloramphenicol, Benzene, NSAIDs, Propylthiouracil, Methimazole

58
Q

Drugs that can cause Direct Coombs + test

A

MethyDOPA, Penicillin

59
Q

Drugs that can cause Gray Baby Syndrome

A

Chloramphenicol

60
Q

Drugs that can cause Hemolysis in G6PD deficient pts

A

“Hemolysis IS PAIN”

Isoniazid, Sulfonamides, Primaquine, Aspirin, Ibuprofen, Nitrofurantoin

61
Q

Drugs that can cause Megaloblastic Anemia

A

“Having a blast with PMS”

Phenytoin, Methotrexate, Sulfa drugs”

62
Q

Drugs that cause thrombotic complications

A

OCP (estrogen)

63
Q

Drugs that can cause Cough

64
Q

Drugs that can cause Pulmonary Fibrosis

A

“BLAB”

Bleomycin, Amiodarone, Busulfan

65
Q

Drugs that can cause Acute Cholestatic Hepatitis, Jaundice

A

Erythromycin

66
Q

Drugs that can cause Focal to Massive Hepatic Necrosis

A

“Liver HAVAc”

Halothane, Amanita Phalloides, Valproic Acid, Acetaminophen

67
Q

Drugs that can cause Hepatitis

68
Q

Drugs that can cause Pseudomembranous Colitis

A

Clindamycin and Ampicillin

69
Q

Drugs that can cause Adrenocortical Insufficiency

70
Q

Drugs that can cause Gynecomastia

A

“Some Drugs Create Awkward Enormous Knockers”

Spironolactone, Digitalis, Cimetidine, Alcohol, Estrogen, Ketoconazole

71
Q

Drugs that can cause Hot Flashes

A

Tamoxifen, Clomiphene

72
Q

Drugs that can cause Hyperglycemia

A

Niacin, Tacrolimus, Protease Inhibitors, HCTZ, Corticosteroids

73
Q

Drugs that can cause Hypothyroidism

A

Li, Amiodarone, Sulfonamides

74
Q

Drugs that can cause Fat redistribution

A

Steroids, Protease Inhibitors

75
Q

Drugs that can cause Gingival Hyperplasia

A

Phenytoin, Verapamil

76
Q

Drugs that can cause Gout

A

Furosemide, Thiazides, Niacin, Cyclosporine

77
Q

Drugs that can cause Myopathies

A

“Fish N CHIPS Give you myopathies”

Fibrates, Niacin, Colchicine, Hydroxychloroquine, IFNα, Penacillamine, Statins, Glucocorticoids

78
Q

Drugs that can cause Osteoporosis

A

Glucocorticoids, Heparin

79
Q

Drugs that can cause Photosensitivity

A

“SAT for a photo”

Sulfonamides, Amiodarone, Tetracycline

80
Q

Drugs that can cause Stevens-Johnsons Syndrome

A

“bad rash for a PEC SLAPP”

Penicillin, Ethosuximide, Carbamazepine, Sulfa drugs, Lamotrigine, Allopurinol, Phenytoin, Phenobarbital

81
Q

Drugs that can cause SLE-like syndrome

A

“HIPP”

Hydralazine, INH, Procainamide, Phenytoin

82
Q

Drugs that can cause Teeth in kids

A

Tetracyclines

83
Q

Drugs that can cause Tendonitis, Tendon Rupture, or Cartilage Rupture

A

Fluoroquinolones

84
Q

Drugs that can cause DI

A

Li, Demeclocycline

85
Q

Drugs that can cause Fanconi’s Syndrome

A

Expired Tetracycline

86
Q

Drugs that can cause Hemorrhagic Cystitis

A

Cyclophosphamide, Ifosfamide

Prevented by Mesna

87
Q

Drugs that can cause Interstitial Nephritis

A

Methicillin, NSAIDs, Furosemide

88
Q

Drugs that can cause SIADH

A

Carbamazepine, Cyclophosphamide

89
Q

Drugs that can cause Cinchonism

A

Quinidine, Quinine

90
Q

Parkinsons-Like Syndrome

A

Antipsychotics, Reserpine, Metoclopramide

91
Q

Drugs that can cause Seizures

A

“during seizures I BITE My tongue”

Isoniazid, Bupropion, Imepenem/cilastatin, Tramadol, Enflurane, Metoclopramide

92
Q

Drugs that can cause Tardive Dyskinesia

A

Antipsychotics

93
Q

Drugs that can cause Antimuscarinic effects

A

Atropine, TCAs, H1 blockers, Neuroleptics

94
Q

Drugs that can cause Disulfiram-like reaction

A

Metronidazole, Cephalosporins, Procarbazine, 1st gen Sulfonylureas

95
Q

Drugs that can cause Nephrotoxicity and Ototoxicity

A

Aminoglycosides, Vancomycin, Loop Diuretics, Cisplatin

96
Q

P450 Inducers

A

“Momma Barb Steals Phen-phen and Refuses Greasy Carbs Chronically”

Modafinil, Barbiturates, St John’s wort, Phenytoin, Rifampin, Griseofulvin, Carbamazepine, Chronic EtOH

97
Q

P450 Inhibitors

A

“MAGIC RACKS in GQ”

Macrolides, Amiodarone, Grapefruit juice, Isoniazid, Cimetidine, Ritonavir, Acute EtOH abuse, Ciprofloxacin, Ketoconazole, Sulfonamides, Gemfibrozil, Quinidine

98
Q

Sulfa Drugs

A

“Popular FACTSSS”

Probenecid, Furosemide, Acetazolamide, Celecoxib, Thiazides, Sulfonamide Antibiotics, Sulfasalazine, Sulfonylureas

99
Q

Allergy to Sulf Drugs Presentation

A

Fever, UTI, Pruritic rash, Stevens-Johnson Syndrome, Hemolytic Anemia, Thrombocytopenia, Agranulocytosis, Urticaria

100
Q

-azole

A

Antifungal

101
Q

-cillin

A

Penicillin

102
Q

-cycline

A

Antibiotic that inhibits protein synthesis

103
Q

-navir

A

Protease Inhibitor

104
Q

-triptan

A

5HT 1B/1D agonist

105
Q

-ane

A

Inhalation general anesthetic

106
Q

-caine

A

Local anesthetic

107
Q

-operidol

A

Butyrophenone (neuroleptic)

108
Q

-azine

A

Phenothiazine (antiemetic)

109
Q

-barbital

A

Barbituate

110
Q

-zolam

A

Benzodiazepine

111
Q

-azepam

A

Benzodiazepine

112
Q

-etine

113
Q

-ipramine

114
Q

-triptyline

115
Q

-olol

A

β antagonist

116
Q

-terol

A

β2 agonist

117
Q

-zosin

A

α1 antagonist

118
Q

-oxin

A

Cardiac Glycoside

119
Q

-pril

A

ACE Inhibitor

120
Q

-afil

A

Erectile Dysfunction

121
Q

-tropin

A

Pituitary Hormone

122
Q

-tidine

A

H2 antagonist

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