Pharmacology Flashcards
1
Q
Vmax is proportional to
A
the enzyme concentration
2
Q
Km is inversley proportional to
A
the affinity of the enzyme to its substate
3
Q
Enzyme reaction showing a sigmoid curve
A
cooperative kinetics
4
Q
Km =
A
saturation at 1/2 Vmax
5
Q
Michaelis-Mentin kinetics
A
hyperbolic curve shape
6
Q
Lineweaver-Burk plot gradient
A
Km/Vmax
7
Q
How do reversible competitive inhibitors change Vmax and Km?
A
No change
Increase Km
8
Q
How to irreversible competitive inhibitors change Vmax?
A
Decrease Vmax
No change
9
Q
How do noncompetitive inhibitors change Vmx?
A
Decrease Vmax
No change
10
Q
What do reversible compeititve inhibitors do?
A
decrese the potency
11
Q
What do irreversible competitive inhibitors do?
A
decrease efficacy
12
Q
What do noncompetitive inhibitors do?
A
decrease efficacy
13
Q
Volume of distribution
A
volume occupied by drug in body relative to plasma concentration
14
Q
Vd =
A
amount of drug in body/ plasma drug concentration
15
Q
Clearance =
A
rate of elimination/ plasma drug concentration
= Vd x elimination constant
16
Q
Half life =
A
0.693 x Vd / Clearance
17
Q
when is steady state reached?
A
after 4-5 half lives
18
Q
Loading dose =
A
(Cp x Vd) / F
Cp = target plasma concentration
F = bioavailability
Vd = volume of distribution
19
Q
Maintenance dose =
A
(Cp x CL x dosage interval) / F
20
Q
how should loading and maintenance doses change in renal and liver disease?
A
same loading dose, decrease maintenance dose
21
Q
permissive interaction
A
A is required for the full effect of B
22
Q
synergistic interaction
A
the effect of A+B is greater than the sum of the individual effects
23
Q
tachyphylactic interactions
A
acute decrease in drug response after initial/ repeated administration
24
Q
zero order kinetics
A
rate of elimination is always constant
25
first order kinetics
rate of elimination is proportional to drug concentration
26
drugs using zero order kinetics
PEA
Phenytoin
Ethanol
Aspirin
27
Rx for aspirin, methotrexate, phenobarbital OD and why
Bicarbonate
| They are weak acids
28
Rx for amphetamine, TCA OD and why
ammonium chloride
| they are weak bases
29
phase I drug metabolism
reduction, oxidation, hydrolysis
| P-450
30
what phase of drug metabolism is lost first?
phase I
| elderly
31
phase II drug metabolism
conjugation
| --> polar and inactive
32
what will increase the side effects of a drug?
being a slow acetylator
33
what happens in conjucation phase II?
methylation, glucuronidation, acetylation, sulfation
34
efficacy
maximal effect a drug can produce
35
potency
amount of drug needed for a given effect
36
EC50 is
the dose of drug needed to give 50% of the maximum effect
37
theraputic index =
median toxic dose / median effective dose
38
very safe drug theraputic index will be
high
39
sympathetic NS
short pre-synaptic
40
P-ANS
long pre-synaptic
41
P-ANS receptors
Nicotinic ACh
| Muscarinic ACh
42
S-ANS receptors
Nicotinic ACh
| Muscarinic ACh, NE, D, Epinephrine
43
somatic receptors
voluntary motor nerve
| ACh at NMJ
44
how muscarinic ACh receptors work
GPCR
45
sympathetic receptors and g protein classes
a1 - Q
a2 - I
B1, 2, 3 - S
46
action of a1
smooth muscle contraction, mydriasis, intestine and bladder contraction
47
action of a2
decrease sympathetic flow, decrese insulin, decrease lypolysis, increase plt aggregation, decrease aq humour production
48
action of B1
increase HR and contractility, lipilysis, renin release
49
action of B2
vasodilation, bronchodilation, lipolysis, insulin, decrease uterine tone, ciliary muscle relaxation, increase aq humour production
50
B3 action
lipolysis, thermogenesis in skeletal muscle
| be free to take off your clothes and shiver!
51
M1 action
CNS, enteric nervous system
52
M2 action
decrease Hr and contractility of aorta
53
M3 action
exocrine secretion, gut peristalsis, bladder contraction, btonchoconstriction, miosis, accomodation
54
D1 action
relax renal vascular smooth muscle
55
D2 action
modulates transmitter release (brain)
56
H1 action
mucus production, vascular permeability, contraction of bronchioles, pruitus, pain
57
H2 action
gastric acid secretion
58
V1 action
vascular smooth muscle contraction
59
V2 action
H2O reabsorbtion in collecting duct
60
mneumonic for Q g protein class
A Very Quick MuMMy Must Hop
61
mneumonic for I g protein class
2 MAD I's
62
mneumonic for S g protein class
you See, 3 Bees, 2 Honeypots and a Very Victorious Dog
63
action of Gq
phospholipase C --> PIP2 --> DAG --> PKC
| --> IP3 --> Ca2+ rise
64
action of Gs
Adenylyl cyclase --> cAMP --> PKA --> Ca2+ rise, inhibits myosin light chain kinase
65
action of Gi
Inhibits Gs (Adenylyl cyclase --> cAMP --> PKA --> Ca2+ rise, inhibits myosin light chain kinase)
66
hemicholinium
stops formation of ACh
67
vesamicol
stops ACh entering vesicles
68
Botulinum
stops vesicle release
69
stops NA reuptake
cocaine, TCA, amphetamine
70
Increases NA release
amphetamine, ephedrine
71
Stops NA release
Bretylium, guanethidine
72
Reserpine
stops DA moving into vesicles
73
Metryrosine
analog of tyrosine, stops NA being synthesised
74
tyramine excess results in
| why
htn crisis
| excess tyramine displaces NA in vesicles, more NA diffuses into the cleft increasing sympathetic activation
75
cholinomimetics
bethanechol, carbachol, methacholine, pilocarpine
76
methacholine
stimualtes muscarinic receptors in airway
77
carbachol use
miosis for open angle glaucoma
78
bethanechol use
post op ileus, neurogenic ileus, urinary retention
79
anticholinesterases
neostigmine, edrophonium, donepezil, galantamine
80
edrophonium use
dgx myasthenia gravis
81
donepezil, galantamine, rivastigmine use
alzheimer disease
82
neostigmine use
ileus, urinary retention, myasthenia gravis, reverses NMJ block
83
physostigmine use
crosses BBB, anticholinergic toxicity
84
pyridostigmine use
myasthenia gravis
85
what must you be careful with when using cholemimetics?
COPD, asthma, peptic ulcers
86
diarrhoea, urination, miosis, bronchospasm, bradycardia, lacrimation, sweating, salivation
```
anticholinesterase poisoning (neostigmine, edrophonium, donepezil, galantamine)
organophosphates
```
87
Rx anticholinesterase poisoning
atropine + pralidoxime
88
Atropine
muscarinic antagoinst
89
benztropine is, does
muscarinic antagoinst
| parkinson's
90
glycopyrrolate is, does
muscarinic antagoinst
| drooling, peptic ulcer
91
hyoscyamine is, does
muscarinic antagoinst
| antispasm for IBS
92
ipratropium is, does
muscarinic antagoinst
| COPD, asthma
93
oxybutynin, sloifenacin, tolterodine are, do
muscarinic antagoinsts
| reduce urge urinary incontinance
94
scopolamine is, does
muscarinic antagoinst
| motion sickness
95
dry flushed skin, cycloplegia, disorientation
| memory aide
atropine poisoning
| hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter
96
dobutamine is, use
sympathomimetic (B1)
| HF
97
dopamine is, does
sympathomimetic
| bradycardia, HF, shock
98
epinephrine is, effects, for
sympathomimetic
| B > a
99
fenoldopam, is, acts, does
sympathomimetic
D1
post op htn, vasodilator
100
isoproterenol is, does
sympathomimetic
| evaluation of tachyarrhythmias
101
midodrine is, acts on, does
sympathomimetic
a1
postural hOtn
102
NE is, acts on, for
sympathomimetic
a1 > a2 > B1
hOtn, septic shock
103
phenylephrine is, acts on, for
sympathomimetic
a1 > a2
hOtn, decongestant
104
clonidine, guanfacine, is, for
a2 agonist
| htn urgency, ADHD, tourette's
105
a-methyldopa is, for
a2 agonist
| htn in pregnancy
106
prazosin, tamsulosin is, for
a1 blocker
| BPH urinary symptoms, praxosin for htn
107
mirtazapine is, use
a2 blocker
| depression
108
phenoxynenzamine is, for
a blocker
| pheochromocytoma to prevent catecholamine crisis
109
phentolamine is, for
a blocker
| MAO inhibitor patients who eat tyramine rich foods
110
a blockers cause
orthostatic hOtn, reflex tachycardia
111
how are B blockers useful in variceal bleeding?
decrease hepatic venous pressure and portal htn
112
B1 antagonists
acebutol, atenolol, betaxolil, esmolol, metoprolol (1st half of alphabet)
113
non selective B antagonists
nadolol, pindolol, propranolol, timolol (2nd half of alphabet from N)
114
carvedilol, labetalol
a and b antagonists
115
nebivolol
B1 and B3
116
tetrodotoxin
| effect
pufferfish
| binds fast voltage gated Na channels in heart/NS preventing depolarisation
117
ciguatoxin
| effect
reef fish - barracuda, snapper, eel
| opens Na channels, causing depolarisation
118
histamine (scombroid poisoning)
spoiled dark-meat fish
119
action histamine toxin
mimics anaphylaxis
120
amphetamine overdose
NH4Cl
121
antimuscarinic overdose
physostigmine
122
aresenic OD
dimercaprol, succimer
123
benzodiazapine OD
flumazenil
124
B blocker OD
saline, atropine, glucagon
125
Cu OD
penicillamine, trientine
126
Cyanide OD
nitrite + thiosulfate, hydroxocobalamin
127
Digoxin OD
anti-dig Fab fragments
128
Gold OD
Penicillamine, dimercaprol (BAL), succimer
129
Iron OD
deferoxamine, deferasiroz, deferiprone
130
Lead OD
EDTA, dimercaprol, succimer, penicillamine
131
Mercury OD
Dimercaprol, succimer
132
Methanol OD
fomepizol > ethanol, dialysis
133
Methemoglobin OD
methylene blue, vitamin C
134
salicylate OD
NaHCO3, dialysis
135
TCA OD
NaHCO3
136
dilated cardiomyopathy from
doxorubicin, daunorubicin
137
cutaneous flushing caused by
vancomycin, adenosine, niacin, Ca blockers, echinocanidins (VANCE)
138
what can cause hot flashes?
tamoxifen, clomiphene
139
what can cause hyperglycaemia?
tacrolimas, protease inhibitors, niacin, HCTZ, corticosteroids
Note: Taking Pills Causes Hyperglycemia
140
what can cause hypothyroidism?
lithium, amiodarone, sulfonamides
141
what drug can cause acute cholestatic hepatitis?
erythromycin
142
what drug can cause hepatic necrosis?
halothane, amanita phalloides, valproic acid, acetaminophen
143
What drugs can cause hepatitis?
rifampin, isoniazid, pyrazinamide, statins, fibrates
144
what drugs can cause pancreatitis?
didanosine, valproic acid, azathioprine, diuretics - furosemide, HCTZ
Don't HAV Fun
145
What drugs can cause pill-enduced eosophagitis?
tetracyclines, bisphosphonates, potassium chloride
146
what drugs can cause pseudomembranous colitis?
clindamicin, ampicillin, cephalosporins
147
what drugs cause agranulocytosis?
clozapine, carbamexapine, propylthiouracil, methimazole, colchicine, ganciclovir
Can Cause Pretty Major Collapse of Granulocytes
148
what drugs can cause aplastic anaemia?
Carbamazepine, methimazole, NSAIDs, benzene, chloramphenicol, propylthiouracil
Can't Make New Blood Cells Properly
149
What drugs cause hemolytic anaemia, and what type?
direct coombs positive
| methyldopa, penicillin
150
what causes grey baby syndrome?
chloramphenicol
151
what causes hemolysis in G6PDH?
isoniazid, sulfonamides, dapsone, primaquine, aspirin, ibuprofen, nitrofurantoin
Hemolysis IS D PAIN
152
drugs causing megaloblastic anaemia
phenytoin, methotrexate, sulfa drugs
| Having a BLAST with PMS
153
drug causing thrombocytopenia
heparin
154
drugs causing fat redistribution
protease inhibitors, glucocortocoids
| Fat PiG
155
drugs causing gingival hyperplasia
phenytoin, Ca channel blockers, cyclosporine
156
drugs causing gout
pyrazinamide, thiazides, furosemide, niacin, cyclosporine
| Painful Feet Tophi Need Care
157
drugs causing myopathy
fibrates, niacin, colchicine, hydroxychloroquine, interferon-a, penicillamine, statins, glucocorticoids
158
osteoporosis
corticosteroids, heparin
159
photosensitivity
sulfonamindes, amiodarone, tetracyclines, 5-FU
| SAT For photo
160
Steven's Johnson syndrome
anti-epileptics, allopurinol, sulfa dugs, penicillin
161
SLE-like syndrome
sulfa-drugs, hydralazine, isoniazid, procainamide, phenytoin, etanercept
SHIPP-E
162
tendonitis
fluroquinolones
163
ondansetron
5-HT3
164
mechanism acyclovir
incorporates into new DNA
165
side effect of muscarinic antagonism
urinary retention
166
protection against haemorrhagic cystitis
mesna
167
cinchonism
overdose of quinine
168
drugs causing parkinson like symptoms
antipsychotics, reserpine, metoclopramide
| ARM
169
drugs causing seizures
BITE your tongue
| Isoniazid, Bupropion, Imipenem/cilastatin, Tramadol, Enflurane
170
When can isoniazid cause seizures?
with vitamin B6 deficiency
171
What can cause Tardive dyskinesia?
antipsychotics, metoclopramide
172
what drugs can cause diabetes insipidus
lithium, demeclocycline
173
what drugs can cause fanconi syndrome?
tenofovir, ifosfamide
174
what drugs can cause hemorrhagic cystitis?
cyclophosphamide, ifosfamide
175
what drugs can cause interstitial nephritis?
methicillin, NSAIDs, furosemide
176
what drugs can cause SIADH?
carbamazepine, cyclophosphamide, SSRIs
| Can't Concentrate Serum Sodium
177
Which drugs can cause pulmonary fibrosis?
Methotrexate, Nitrofurantoin, Carmustine, Bleomycin, Busulfan, Amiodarone
My Breathing Becomes A Nasty Crackle
178
What drugs have antimuscarinic action?
Atropine, TCA, H1 blockers, antipsychotics
179
What drugs cause a disulfarim like reaction?
metronidazole, certain cephalosporins, griseofulvin, procarbazine, 1st generation sulfonylureas
180
What drugs can cause nephro/oto toxicity?
Aminoglycosides, vancoycin, loop diuretics, cisplatin
| be Very Careful of Little Arteries
181
What may cisplatin toxicity respond to?
amifostine
182
Induce cytochrome P-450
Chronic alcohol, St John's wart, Phenytoin, Phenobarbitol, Nevirapine, Rifampin, Griseofulvin, Carbamazepine
Cytochrome P-450 Needs Regular Stimulation Greeting Circulating Pills
183
P-450 breaks down
Anti-epileptics, Theophylline, Warfarin, OCPs
| metabolised Each One With T
184
P-450 inhibitors
Acute alcohol, ritonavir, Amiodarone, Cimetidine/ciprofloxacin, Ketoconazole, Sulfonamides, Isoniazid, Grapefruit juice, Quinidine, Macrolides
AAA RACKS IN GQ Magazine
185
Macrolide not inhibiting O-450
azithromycin
186
What are sulfa drugs?
sulfonamide antibiotics, sulfasalazine, probenecid, furosemide, acetazolamide, celecoxib, thiazides, sulfonylureas
Scary Sulfa Pharm FACTS
187
fever, urinary infection, rash, hemolytic anaemia, thrombocytopenia, agranulocytosis, urticaria, recent new medication
Sulfa drug
188
-ivir
neuraminidase inhibitor
189
-navir
protease inhibitor
190
-ovir
DNA polymerase inhibitor
191
-bendazole
antiparasitic/antihelminithic
192
-azole
ergosterol synthesis inhibitor
193
-etine
SSRI
194
-triptan
%-HT agonist
195
-chol
cholinergic
196
-curium
nondepolarising paralytic
197
-stigmine
ACHE inhibitor
198
-terol
B2 agonist
199
-zosin
a1 antagonist
200
-afil
PDE-5 inhibitor
201
-sartan
AT II R blocker
202
-glitazone
PPAR-gamma activator
203
-tidine
H2 antagonist
204
-ximab
chimeric mab
205
-zumab
humanized mab
206
cilostazol
decreases platelet activation and vasodilates
