Pharm Flashcards
1
Q
Km
A
=[S] at 1/2 Vmax; inverse to affinity for substrate
2
Q
Vmax
A
Directly proportional to enzyme concentration (V of saturation)
3
Q
Competitive inhibitor
A
Same Vmax, lower Km (takes longer to reach vmax); reversible
4
Q
Noncompetitive inhibitor
A
Higher Km, lower Vmax
5
Q
Cooperative kinetics
A
Sigmoid curve (like hemoglobin)
6
Q
Most enzymes have a ____ curve
A
Hyperbolic
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
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
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
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
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
12
Q
Vd=
A
Amount drug in body/plasma drug conc
13
Q
Low Vd compartment and type
A
Intravascular large/charged molecules often bound to plasma proteins
14
Q
Medium Vd compartment and type
A
ECF small hydrophilic molecules
15
Q
High Vd compartment and type
A
All tissues including fat, small lipophilic molecules, esp if bound to tissue protein
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)
17
Q
How many half lives to reach steady state in 1st order kinetics?
A
4-5
18
Q
How many half lives to reach 90% of steady state in first order kinetics?
A
3.3
19
Q
T1/2 in first order kin=
A
(0.693*Vd)/CL
20
Q
Loading dose=
A
(Cp*Vd)/F
Where Cp is conc. at steady state
F is bioavailability
21
Q
Maintenance dose=
A
(CpCLt)/F
Where Cp is conc at steady state
F is bioavailability
t is dosage interval
22
Q
In renal and liver disease, how do maintenance doses change?
A
Maintenance goes down
23
Q
In renal and liver disease, how do loading doses change?
A
Loading dose doesn’t change (trick q)
24
Q
Additive drug effect
A
Effect of A+B=sum of individual effects
25
Permissive drug effect
Need A for proper fxn of B
26
Synergistic drug effect
A+B together > sum of their effects individually
27
Tachyphlactic drug interaction
Acute decrease in reponse to drug after initial/repeated admin
28
Zero order elim
Rate of elim constant regardless of Cp; eg Phenytoin, ethanol, aspirin at high conc. (constant AMOUNT)
29
First order elim
Rate of elim directly proportional to drug conc. (constant FRACTION), Cp decreases exponentially w/ time; e.g. most drugs
30
Weak acids and how to get rid of them in overdose
Ex: phenobarb, methotrexate, aspirin
| Trapped in basic environments -- give sodium bicarb to alk the urine
31
Weak bases and how to get rid of them in overdowse
Ex: amphetimines, TCAs
| Trapped in acidic environments -- give ammonium Cl to acidify urine
32
Phase I metabolism
Reduction, oxidation, hydrolysis w P50 --> slightly polar, water soluble metabolites (often still active)
33
First type of metabolism lost w/ age
Phase I
34
Phase II metabolism
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
35
Efficacy
Maximal effect a drug can produce (Vmax)
36
Partial agonist efficacy vs full agonist efficacy
Partial
37
Potency
Amount of drug needed for a given effect (EC50 -- i.e. 50% of maximal effect)
38
Left shift in potency=
Lower EC50, higher potency, less drug needed for an effect
39
Competitive antagonist
Right shift in curve --i.e. lower potency, but same efficacy and can be overcome by increased substrate conc
40
Noncompetitive antagonist
Shifts curve down (lower efficacy) -- not able to be overcome by a higher [S]
41
Partial agonists
Same site as a full agonist, decreases efficacy, potency independent
42
Therapeutic index
Measurement of drug safety
| TD50/ED50 (toxic median dose/effective median dose)
43
Therapeutic window
Dosage range to safely/effectively treat disease
44
Lower TI drugs
Require monitoring; eg Warfarin, theophylline, dig, Li,
| "Warning These Drugs are Lethal!"
45
All first synapses are
Ach on Nicotinic receptors
46
PNS has long/short pre synaptic
Long
47
SNS has long/short pre synaptic
Short
48
Exception to SNS rules
Sweat glands -- Ach on M like PNS
49
alpha1
Gq
| Vascular smooth muscle contraction, pupillary dilator contracts (mydriasis); intestinal/bladder sphincter contraction
50
alpha2
Gi
| Less sympathetic outflow, less insulin release, less lipolysis, increased platelet agg, less aqueous humor made
51
beta1
Gs
| Increased heart rate, increased contractility, renin released, increased lipolysis
52
beta2
Gs
Vasodilation, bronchodilation, increased lipolysis, increased insulin release, less uterine tone (tocolysis), ciliary muscle relaxation, more aqueous humor
53
beta3
Gs
| Increased lipolysis, thermogenesis in skeletal m, bladder relaxation
54
M1
Gq
| Higher cognitive fxns, stimulates enteric nervous system
55
M2
Gi
| Lower heart rate, less atrial contractility
56
M3
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
57
D1
Gs
| Relaxes renal vascular smooth muscle, activates direct pathway of striatum
58
D2
Gi
Modulates transmitter release (esp in brain), inhibition of indirect pathway of striatum
(GI, Inhibition Indirect path)
59
H1
Gq
| Nasal and bronchial muscus production, vascular permeability, contraction of bronchioles, pruritus, pain
60
H2
Gs
| Gastric acid secretion
61
V1
Gq
| Vascular smooth muscle contraction
62
V2
Gs
| H2O permeability and reabsorption in collecting tubules of kidney
63
Gq receptor examples and effector enzyme
H1, alpha1, V1, M1, M3
"HAVe 1 M&M"
Works via PLC (Ca/PKC)
64
Gs receptor examples and effector enzyme
B1, B2, B3, D1, H2, V2
Works via AC upregulation
65
Gi receptor examples and effector enzyme
M2, alpha2, D2
Works via AC downregulation
66
NE self regulation
Via alpha2 autoreceptors
67
Selective beta blockers (6)
B1 -- acebutolol (partial agonist), atenolol, betaxolol, bisoprolol, esmolol, metoprolol
68
Non selective beta blockers (4)
Nadolol, pindolol (partial agonist), propanolol, timolol
69
Nonselective beta/alpha blockers
Labetolol, carvedilol
70
Special beta blockers
Nebivolol -- cardiac selective B1, stim of B3 in vasculature --> NO synthase --> reduces SVR
71
B blockers that reduce mortality in HF
Bisoprolol, carvedilol, metoprolol
72
B blocker partial agonists
Pindolol, acebutalol (don't use in heart failure)
73
Tetrodotoxin -- source, action, symptoms, tx
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)
74
Ciguatoxin -- source, action, symptoms, tx
Reef fish (barracuda, snapper, moray eel) --> opens Na channels --> depolarization --> NVD, perioral numbness, reversal of hot/cold sensations, bradycardia, heart block, hypotension (tx supportive)
75
Histaime (scombroid poisoning) -- source, action, symptoms, tx
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)
76
Beers drugs
- 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
Acetaminophen overdose tx
N-acetylcystein (replenishes glutathione)
78
AChE inhibitors, organophosphates overdose tx
Atropine > pralidoxime (muscle)
79
Antimuscarinic, anticholinergic agents overdose tx
Physostigmine, control hyperthermia
80
Arsenic overdose tx
Dimercaprol, succimer
81
Benzos overdose tx
Flumazenil
82
B blockers overdose tx
Glucagon, atropine
83
CO overdose tx
100%/hyperbaric O2
84
Cu overdose tx
Penicillamine, trientine
85
Cyanide overdose tx
Nitrate + thiosulfate, hydroxocobalamin
86
Dig overdose tx
Anti-dig Fab fragments
87
Heparin overdose tx
Protamine sulfate
88
Fe overdose tx
Deferoxamine, deferasirox, deferiprone
89
Pb overdose tx
EDTA, dimercaprol, succimer, penicillamine
90
Mercury overdose tx
Dimercaprol, succimer
91
Methanol, ethylene glycol (antifreeze) overdose tx
Fomepizole>ethanol, dialysis
92
Methemoglobin overdose tx
Methylene blue, vit C
93
Opioids overdose tx
Naloxone
94
Salicylates overdose tx
NaHCO3 (alkalinize urine), dialysis
95
TCAs overdose tx
NaHCO3 (alkalinize urine)
96
Warfarin overdose tx
VIt K (delayed effect), FFP (immediate)
97
Drugs causing coronary vasospasm
Amphetamines, cocaine, ergot alkaloids, sumatriptan
98
Drugs causing cutaneous flushing
Vanco, Adenosine, Niacin, Nitrates, Ca2+ channel blockers, Echinocandins
VANNCE
99
Drugs causing dilated cardiomyopathy
Anthracyclines (doxorubicin, daunorubicin), prevent w/ dexrazoxane
100
Drugs causing torsades
AntiArrhythmics (Class Ia, III), antiBiotics (macrolides), anti"C"ycotics (haloperidol), antiDepressants (TCAs), antiEmetics (ondansetron)
ABCDE
101
Drugs causing adrenocortical insufficiency
HPA suppression 2o to glucocorticoid w/drawal
102
Drugs causing diabetes insipidis
Li, demeclocycline
103
Drugs causing hot flashes
Tamoxifen, clomiphene
104
Drugs causing hyperglycemia
Tacrolimus, Protease inhibs, Niacin, HCTZ, Corticosteroids
| Taking Pills Necessitates Having Blood Checked
105
Drugs causing hypothyroidism
Li, amiodarone, sulfonamides
106
Drugs causing SIADH
Carbamazepine, Cyclophosphamide, SSRIs
Can't Concentrate Serum Sodium
107
Drugs causing acute cholestatic hepatitis/jaundice
Erythromycin
108
Drugs causing diarrhea
Acamprosate, acarbose, cholinesterase inhibs, colchicine, erythromycin, ezetimibe, metformin, misoprostol, orlistat, pramlintide, quinidine, SSRIs
109
Drugs causing focal-massive hepatic necrosis
Halothane, Amanita phalloides, Valproic acid, ACetaminophen
Liver HAVAC
110
Drugs causing hepatitis
Rifamipin, isoniazid, pyrazinamide, statins, fibrates
111
Drugs causing pancreatitis
Didanosine, Corticosteroids, Alcohol, Valproic acid, Azathioprine, Diuretics (furosemide, HCTZ)
Drugs Causing A Violent Abdominal Distress
112
Drugs causing pill-induced esophagitis
Bisphosphonates, ferrous sulfates, NSAIDs, KCl, tetracyclines
(Minimize w/ upright posture and water intake)
113
Drugs causing pseudomembranous colitis
Ampicillin, cephalosporins, clindamycin, fluoroquinolones
114
Drugs causing agranulocytosis
Clozpine, Carbamazepine, PTU, Methimazole, Colchicine, Ganciclovir
Can Cause Pretty Major Collapse of Granulocytes
115
Drugs causing aplastic anemia
Carbemazepine, Methimazole, NSAIDs, Benzene, Chloramphenicol, PTU
Can't Make New Blood Cells Properly
116
Drugs causing direct Coombs positive hemolytic anemia
Methyldopa, penicillin
117
Drugs causing DRESS
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
Drugs causing gray baby syndrome
Chloramphenicol
119
Drugs causing hemolysis in G6PD def
Isoniazid, Sulfonamides, Dapsone, Primaquine, Aspirin, Ibuprofen, Nitrofurantoin
Hemolysis IS D PAIN
120
Drugs causing megaloblastic anemia
HydroxYUREa, Phenytoin, Methotrexate, Sulfa drugs
YURE having a MEGABLAST with PMS
121
Drugs causing thrombocytopenia
Heparin
122
Drugs causing thrombotic complications
Combined OC, hormone replacement therapy, SERMs (tamoxifen, raloxifene, clomiphene) -- estrogen mediated
123
Drugs causing fat redistribution
Protease inhibitors, Glucocorticoids
| Fat PiG
124
Drugs causing gingival hyperplasia
Phenytoin, Ca channel blockers, cyclosporine
125
Drugs causing hyperuricemia
Pyrazinamide, Thiazides, Furosemides, Niacin, Cyclosporine
| Painful Tophi Feed Need Care
126
Drugs causing myopathy
Statins, fibrates, niacin, colchicine, daptomycin, hydrozychloroquine, IFN alpha, penicillamine, glucocorticoids
127
Drugs causing osteoporosis
Corticosteroids, depot medrozyprogesterone acetate, GnRH agonists, aromatase inhibitors, anticonvulsants, heparin
128
Drugs causing photosensitivity
Sulfonamides, Amiodarone, Tetracyclines, 5 Fu
SAT For Photo
129
Drugs causing rash (SJS)
Antiepileptics (esp lamotrigine), allopurinol, sulfa drugs, penicillin
Steven Johnson has epileptic allergy to sulf drugs and penicillin
130
Drugs causing SLE like syndrome
Sulfa drugs, Hydralazine, Isoniazid, Procainamide, Phenytoin, Etanercept
Having lupus is SHIPP-E
131
Drugs causing teeth discoloration
Tetracyclines (teethracyclines)
132
Drugs causing tendonitis, tendon rupture, and/or cartilage damage
Fluoroquinolones
133
Drugs causing cinchonism
Quinidine, quinine (tinnitus, hearing/vision loss, psychosis, cognitive impairment)
134
Drugs causing parkinson-like syndrome
Antipsychotics, Reserpine, Metoclopramide
Cogwheel rigidity of ARM
135
Drugs causing seizures
Isoniazid (in B6 def), Bupropion, Imipenem/cilastin, Tramadol, Enflurane
with seizures I BITE my tongue
136
Drugs causing tardive dyskinesia
Antipsychotics, metoclopramide
137
Drugs causing Fanconi syndrome
Cisplatin, ifosfamide, expired tetracyclines, tenofovir
138
Drugs causing hemorrhagic cystitis
Cyclophosphamide, isofosfamide (prevent by coadmin of mesna)
139
Drugs causing interstitial nephritis
Penicillins, furosemides, NSAIDs, PPIs, sulfa drugs
140
Drugs causing dry cough
ACE inhibs
141
Drugs causing pulmonary fibrosis
Methotrexate, Nitrofurantoin, Carmustine, Bleomycin, Busulfan, Amiodaron
My Nose Cannot Breate Bad Air
142
Drugs causing antimuscarinic side effects
Atropine, TCAs, H1 blockers, antipsychotics
143
Drugs causing disulfiram like reaction
1st gen Sulfanureas, Procarbazine, some Cephalosporins, Griseofulvin, Metronidazole
Sorry Pals Can't Go Mingle
144
Drugs causing nephro/ototoxicity
Aminoglycosides, vanco, loop diuretics, cisplatin, amphotericin B (cisplatin tox may respond to amifostine)
145
P450 inducers (8)
```
Chronic alcohol use
St johns wort
Phenytoin
Phenobarbitol
Nevirapine
Rifampin
Griseofulvin
Carbamazepine
```
Chronic alcoholics STeal PHEN PHEN and Never Refurse GReasy CARBs
146
P450 substrates
Antiepileptics
Theophylline
Warfarin
OCPs
Always Think When Outdoors
147
P450 Inhibitors (12)
```
Sodium valproate
Isoniazid
Cimetidine
Ketoconazole
Fluconazole
Acute EtOH abuse
Chloramphenicol
Erythromycin (macrolides)
Sulfonamides
Ciprofloxacin
Omeprazole
Metronidazole
```
SICKFACES.COM
148
Sulfa drugs (8)
Sulfonamide abx, Sulfasalazine, Probenecid, Furosemides, Acetazolamide, Celecoxib, Thiazides, Sulfonylureas
Scary Sulfa Pharm FACTS
149
-azoles
Ergosterol synthesis inhibitor
150
-bendazole
Antiparasitic/antihelminthic
151
-cillin
TTPase (PBP)
152
-cycline
Protein synth inhibitor
153
-ivir
Neuraminidase inhibitor
154
-navir
Protease inhibitor
155
-ovir
DNA polymerase inhibitor
156
-thromycin
Macrolide abx
157
-ane
Inhalational general anesthetic
158
-azine
Typical antipsychotic
159
-barbital
Barbiturate
160
-caine
Local anesthetic
161
-etine
SSRI
162
-imipramine
TCA
163
-triptyline
TCA
164
-triptan
5HT1B/1D agonist
165
-zepam
Benzo
166
-zolam
Benzo
167
-chol
Cholinergic agonist
168
-curium
Nondepolarizing paralytic
169
-curonium
Nondepolarizing paralytic
170
-olol
B blocker
171
-stigmine
AchE inhib
172
-terol
B2 agonist
173
-zosin
A1 antagonist
174
-afil
PDE5 inhib
175
-dipine
DHP Ca channel blocker
176
-pril
ACE inhib
177
-sartan
AngIIRB
178
-statin
HMG-CoA reductase inhib
179
-xaban
Direct factor Xa inhib
180
-dronate
Biphosphonate
181
-glitazone
PPAR-gamma activator
182
-prazole
PPI
183
-prost
Prostaglandin analog
184
-tidine
H2 antagonist
185
-tinib
TK inhib
186
-tropin
Pituitary hormone
187
-ximab
Chimeric MAb
188
-zumab
Humanized MAb
