Pharmacology Flashcards
1
Q
What is the K, Vmax, of Micehalis-menton kinetics?
A
Km is inversely related to the affinity of the enzyme for its substrate
Vmax: directly proportional to the enzyme concentration
2
Q
What type of enzyme reaction do most medication follow?
A
Hyperbolic curve
Some enzyme reactions exhibit sigmoid
3
Q
Which type of inhibitor can be overcome by increasing the substrate concentration?
A
1) Only reversible competitive inhibitors (irreversible compeitive and non competitive cannot)
4
Q
What is the effect of Km depending on the type of inhibitor?
A
Competitive inhibitor reverible (Increased)
Comp. non revers. unchanged
Non. comp: unchanged
5
Q
Effect on Vmax?
A
Comp In (rev.) unchanged Comp in (irr) decreased Non. irr decreased
6
Q
What is bioavilability of IV dose?
A
F= 100
7
Q
What is the bioavailability of PO dose?
A
Less then 100% due to incomplete absorbtion and first pass metabolism
8
Q
What is the volume distribution?
A
Amount of drug in the body relative to its plasma concentration
9
Q
What can affect the volume of distribution?
A
Altered by liver or kidney disease
10
Q
How to calculate the volume of distribution?
A
Vd= Amount of drug in the body/plasma drug concentration
11
Q
what are characteristics of low volume of distribution?
A
Compartment: blood (drug: large charged molebules) with plasma protein bound
12
Q
What are characteristic of medium distribution?
A
ECF
Small, hydrophilic molecules
13
Q
What are characteristics of high distribution?
A
All tissues including fat
Small, lipophilic molecules, especially bound by tissue protein.
14
Q
How to determine the clearance ?
A
CL = rate of elimination of the drug/plasma drug concentration = Vd X Ke
15
Q
What is the half time?
A
Time required for the body to 1/2 elimination
T1/2 = ).693 X Vd/ CL
16
Q
What is meant by the different number of half times?
A
1 half life: 50%
2 half life: 25%
3 half life: 12.5%
4 half life: 6.25%
17
Q
How to calculate a loading dose?
A
Cp X Vd / F
Cp=target plasma concentration at steady state
Vd is volume distribution
F = bioavilability
18
Q
How to calculate the maintenece dose?
A
Maintence dose=Cp X Cl X t/F
Cp (target plasma steady state)
T= dosage interval (if not administered continuousely
19
Q
What happens to the loading dose if have liver or kidney disease?
A
The loading dose is usually unchanged, but the maintence dose is decreased
20
Q
What determines the time to the steady state?
A
The T1/2 is independent of dose, and of dosing frequency
21
Q
What is an additive drug interaction, and what is an example?
A
effect of substance A and B is equal to sum of their individual effects (ASA and acetaminophen)
22
Q
What is a permissive effect of drugs?
A
Presence of substance A needed to get full effect of B (cortisol on catecholamine effect)
23
Q
what is a synergistic effect of drugs?
A
Effect of substance A and B is greater then the sum of individual effects
24
Q
What is tachyphylactic drug interaction?
A
Acute decrease in response to the drug after initial administration
MDMA and LSD
25
What is zero order drug?
Constant amount of drug eliminated regardless of unit of time (graph is a straight line)
26
What are examples of drugs that are zero order?
Phenytoin
Ethanol
ASA
27
What is first order elimination?
Rate of elimination is directly proportional to the concentration of the drug (graph is a curved line)
28
How does urine pH affect the drug elimination?
Ionized species are trapped in urine and eliminated quickly
Neutral forms can be reabsorbed
29
How do weak acids work?
| Examples of weak acids?
1) Trapped in basic environment (treat with bicarbonate)
| 2) Examples: phenobarbitol methrotrexate, ASA
30
How do weak bases work?
How to treat overdose?
What are some examples?
1) Trapped in acideic environment (treat overdose with ammonia chloride)
2) Amphetamines and TCA's
31
What are the two phases of drug metabolism?
Phase 1: Reduction, oxidation, hydrolysis with cytochrome p-450 (Geriatric patients lose phase 1 first)
Phase 2: conjugation (methylation, acetylation) usually yeilds very polar inactive metabolits that are renally excreted
32
What is the efficacy of a drug?
Maximal effect a drug can produce
Represented by the y value (V max)
Partial agnosits have less efficiency then full agonist
33
What is the potency of a drug?
1) Amount of drug needed for a given effect
| 2) Rpresented by the EC 50
34
What happens whe the EC 50 has a left shift?
A left shift will increase the potency
| Will decrease the amount of drug needed for a given effect
35
what happens when agonist is placed with competitive antagonist? What is the effect?
1) Shifts the curve to the right
2) Decrease the potency
3) Can be overcome by increasing the concentration of the agonist substrate
Ex. Diazepm with flumazenil (competitive on GABA receptor)
36
What happens when agonist with non-competitive antagonist?
1) Shifts curve down (decrease efficiency)
2) Cannot be overcome by increasing the agonist substrate concentration
3) example: Norepi and alpha receptor
37
What happens when partial agonist is places with agonist?
1) Acts at the same site as full agonist
2) Lower maximal effect (decrease of efficiency)
3) Potency is independent variable
Ex Morphine vs burenorphine
38
How is the safety of drug measured?
TD 50/ ED50
```
TD 50 (median toxic dose)
ED 50 (median effective dose)
```
39
What is therapeutic window?
Dosage range that can safetly and effectvely be used to treat the disease
40
What is the TI of a safer drug?
Usually have a higher TI
41
What is the TI of a more dangerous drug?
| What needs to be done with less safe drugs?
1) More dangerous drug will have lower TI
2) Will need more monitoring
3) Examples include: digoxin, lithium, theophylline
42
What is the difference between the parasympathetic and sympathetic system?
Parasympathetic: controls rest and digest and hemostatic
Sympathetic: In charge of the fight or flight response
43
Where does the parasympathetic vs sympathetic system originate?
Para: spinal cord and medulla
Sympathetic: Spinal cord, thoracic and lumber spine
44
How does the trajectory of the nerves para vs sympa?
Para are long neurons (slow pathways)
| Symp are short neurons (fast pathways)
45
What are effects of para and sympa (cardio, lungs, muscles, glycogen, urinary?
Para: decrease heart rate, bronchial constrict, muscles relax, no effect on glycogen, increase urinary output
Sympa: Increase contraction and heart rate, bronchials releax, muscle contract, glycogen to glucose, decrease urinary output
46
What are the types of ach receptors, and where are they found?
Nictonic: Na-K+ ligated Nn (found in autonomic ganglia/adrenal medulla)
Nm (found in neuromuscular junction of muscle)
Muscarinic: G-coupled receptors (act through second messengers) there are 5 types (Smooth muscle, brain, exocrne, sweat glands)
47
What are the two types of alpha receptos, and their functions?
1) Alpha 1: increase smooth muscle contraction,pupil dilates, increase the intestinal and bladder sphincter
2) Alpha 2: Decrease sympathetic outflow, decrease insulin release, decrease lipolysis increase platelet aggregation
48
What are the Beta receptors and their functions?
Beta 1: Increase heart rate, contractility, and renin, and lipolysis
Beta 2: Vasodilation, bronchodilation, increase lipolysis, increase insulin release
Beta 3: Increase lipolysis, increase thermogenesis
49
What are the parasympathetic M receptors?
1) M1: CNS, enteric nervous system
2) M2: decrease heart rate, and contractility of the atria
3) M3: Increase exocrine gland secretion, increase gut peristalsis, increase bladder contraction, bronchoconstriction
50
What are the dopamine receptors?
1) D1: relaxes the renal vascular smooth muscle
| 2) D2: Modulates transmitter release in the brain
51
What are the histamine receptors?
1) H1: increase the nasal and bronchial mucus production
| 2) H2: increased gastric acid secretion
52
What are the receptors of vasopressin?
1) V1: increase smooth muscle contraction
| 2) V2: increased H2O permeability and reabsorption in the collecting tubules
53
How does botulism work (postsynaptic membrane)?
Blocks the release of the ACH from the presynaptic membrane
54
How does amphetamine and ephedrine work?
increase the NE
55
How does cocaine, TCA, and amphetamine work?
Decrease the reuptake of NE by the presynaptic membrande
56
How does ingestion of tyramine and MAO inhibitors cause hypertensive crisis?
Wine, cheese cause more tryamine, and diaplaces NE, releases more active presynaptic neurotransmittos, increase diffusion of neurotransmittors into the synaptic cleft, leads to increase stimulation, and HTN
57
Name 4 cholinomimetic agents, and their applications?
1) Bethanechol: Activates bowl and bladder (for postoperative ileus, and neurogenic urinary retention)
2) Carbachol (copy of acetylcholine: constrics the pupil, and relieves intraocular pressure in open angle glaucoma)
3) Methacoline: (stimulates muscarinic receptors) Challenge test for asthma
4) Pilocarpine contracts the ciliary muscle of the eye :stimulates the production of sweat, tears, and saliva (Sjogren)
58
What are the medications used to treat Alzehimers?
1) Donepezil
2) Galantamine
3) Rivastigmine
59
What is edrophonium used for?
1) Increase Ach
2) Diagnosis for mysanthia gravis
3) Mysanthia gravis now diagnosed by anti-acetycholine test
60
What is neostigmine used for?
1) Increased ACH
2) For neurogenic ileus and urinary retntion
3) For mysanthia gravis
4) For reversal of neuromuscular junction blockade/
61
What is physostigmine used for?
1) Increases ACH
2) used to fixed atropine overdose
3) Used when have anticholinergic toxicity (crosses blood, brain barrier)
62
What does pyridostigmine used for?
1) Increase ACH
2) Increases muscle strength
3) Used for mysanthia gravis
63
How are cholinesterase inhibitor poisoning treated?
1) Usually due to organophosphates ( components of insecticides)
2) Treat with atropine
64
What are signs of cholinesterase inhibitor poisoning?
1) Diarrhea
2) Bronchospasm
3) Sweating
4) Salivation
5) Urination
6) Miosis
65
What is atropine, homatropine, tropicamide used for?
1) Eye
| 2) Produce mydriasis and cycloplegia
66
What is Benztropine used for?
1) Parkinsons disease
| 2) Acute dystonia
67
what are glycopyrrolate used for?
GI and resp
To reduce the airway secretions
Oral: drooling or peptic ulcer
68
What is hyoscyamine and dicyclomine used for?
GI
| Antispasmodics for irritable bowel syndrome
69
What is ipratropium and tiotropium used for?
COPD and asthma
70
What is oxybutin, solifernacine, and tolterodine used for?
Bladderspasms
Urge of urinary incontinence
Overactive bladder
71
What is scopalamine used for?
1) CNS
| 2) Motion sickness
72
What are the actions of atropine?
1) Incease pupil dilations
2) Decrease secretions
3) Decrease gastric acid
4) Decrease motility
```
Sideeffecects:
Hot as a hare
Dry as a bone
Red as a beet
Blind as a bat
Mad as a hatter
```
73
Actions and applications of Benztropine?
Parkinson disease
| Acute dystonia
74
Actions of glycopyrrolate?
GI and respiratory
Reduce airway secretions
Drooling, peptic ulcer
75
Actions of Hyoscyamine and dicyclomine>
Anti-sposmodics for irritable bowel
76
Actions of Ipratropium and tiotropium?
Respiratory
| COPD and asthma
77
Actions of oxybutynin and solifenacin?
Reduce bladder spasm and urge urinary continence
78
Actions of scopolamine?
Motion sickness
79
Receptors of albuterol and salmeterol?
B2 more then B1
| Albuterol for acute asthma or COPD
80
What are the actions for dobutamine?
B1 more then B2
some alpha effects
Heart failure (inotropic more then chronotropic)
81
Dopamine?
D1 and D2 equal (more the Beta or alpha)
82
Action of epinephrine?
```
Beta more then alpha
Anaphylaxis
Asthma
Open angle glaucoma
More Beta effect then norephinenrine
```
83
What is the action of fenoldopam?
```
D1
Post operative HTN and HTN crisis
Vasodilation
Promotes Natriureses
Can cause hypotension and tachycardia
```
84
Action of isoproterenol?
B1 and B2 are the same
Used for electrophysiological evaluation of tachyarrythmias
Can make ischemia worst
85
Action of midodrine?
Alpha 1 action
Autonomic insufficiency and postural hypotenion
Can exacerbate supine hypertension
86
Action of norepinephrine?
Alpha 1 more then alpha 2 more then B1
| Use in hypotension and septic shock
87
Action of phenyephrine?
Alpha 1 more then alpha 2
| Hypotension (vasocrontriction) occular pressure, rhinitis (decongestant)
88
Mechanism of action of amphetamine ? And applications?
1) Indirect general agonist
2) Reuptake inhibitor
3) Release stored catecholamines
4) Narcoplepsy, obesity and ADHD
89
Mechanism of Cocaine?
1) Indirect general agonist
2) Reuptake inhibitor
Causes vasoconstriction and local anesthesi
Do NOT give B blockers if cocaine intoxication is suspected *can lead to extreme hypotension*
90
What is Ephedrine cause?
Indirect, general agonsist
Release stored catecholamins
Used for nasal decongestion, urinary incontinence and hypotension
91
What are the differences between norepinephrine and isoproterenol?
Norepinephrine: Increase systolic and diastolic presssure as a result of alpha mediated vasocronstriction
Isoproterenol very little alpha effect
Can cause B2 vasodilation, with decrease in mean arterial pressure and increase in heart rate through B1 and reflex activity.
92
Uses for clonidine and guanfacine?
Hypertensive emergency
ADHD, Tourette
Adverse effect: CNS depression, bradycardia, hypotension, respiratory depression, miosis
93
Uses for alpha-methyldopa?
HTN in pregnancy
Direct commbs + hemolysis
SLE-like syndrome
94
Action and use of penoxybenzamineÉ
Pheochromocytoma (to prevent catecholamine surge)
HTN crisis (orthostatic hypotension and reflex tachycardia)
Alpha blocker
95
Action and use of Phentolamine?
Give patients MAO inhibitors who eat tyramine containing foods.
Used for Orthostatic hypotension
Reflex tachycardia
96
What are the alpha selective (-osin drugs)? Prazosin, terazosin, doxazosin, tamsulosin?
1) Urinary symptoms of BPH
| 2) Side effects can be hypotension, dizziness, headache
97
What does the alpha 2 selective inhibitor do? (Mirtazapine)
Used to treat depression
| Adverse effect include sedation, increase serum cholesterole, increase appetite
98
```
What are the effects of B-blocker on Angina?
effect on MI
SVT
HTN
HF
Glaucoma
Variceal bleeding
```
Angina:
decrease heart rate
decrease contractility
decrease O2 consumption
Effect on MI:
Decrease mortality
Effect on SVT
Decrease AV conduction
99
What are adverse effects of B blockers?
1) erectile dysfunction
2) Bradycarida, HF
3) CNS seizures, and sedation, dyslipidemia
100
Which B-blockers are selective antagonists? B1 > B2 ?
```
Acebutolol
Atenolol
Betaxolol
Esmolol
Metoprolol
```
101
Which are non-selective antagonists? B1=B2?
Nadolol
Pindolol
Propranolol
Timolol
102
Which are non-selective alpha and beta antagonists?
Carvedilol
| Labetalol
103
What is the unique property of Nebivolol?
Combines cardiac-selective B1 adergenic with stimulation of B3 receptors
104
What is the effect/ symptoms of tetrodoxotoxin?
Source: pufferfish
Action: potent toxin, voltage gated Na + channels
Symptoms: nausea, diarrhea,paresthesis, weakness, dizziness
Treatment: Supportive
105
What are the effect/symptoms of Ciguatoxin?
1) Source is barracuda, snapper, moray eel
2) Opens Na+ channels causing depolarization
3) Symptoms are like cholinergic poisoning.
4) Primarily supportive
106
what is sombroid poisoning?
1) Source is spoiled dark red meat (tuna, mahi-mahi, mackereal)
2) Bacterial histadine (decarboxylase converts histidie to histamine0
3) Frequently misdiagnosed as a fish allergy
107
Acetominophen toxicity and treatment?
N-acetylcysteine
108
Ace/organophosphate toxicity?
Atropine> pralidoxine
109
Amphetamine toxicity?
NH4Cl (acidify the urine)
110
Antimuscarinic, anticholinergic agent?
Physostigmine
| control hyperthermia
111
Arsenic poisoing?
Dimercaprol
| Succiner
112
Benzodiazepine poisoning?
Flumazenil
113
B Blocker poisoning?
Saline, atropine, glucagon
114
Carbon monoxide poisoning?
100% hyperbaric O2 chamber
115
Copper poisoning?
Pencillamine, trientine
116
Cyanide poisoning?
Nitirite and thiosulfate, hydroxocobalamine
117
Gold poisoning?
Penicillamine, dimercaprol, succimer
118
Heparine poisoning?
Protamine sulfate
119
Iron poisoning?
Deferoxamine
Deferasirox
Deferiprone
120
Lead poisoning?
EDTA
Dimercaprol
Succimer
Penicillamine
121
Mercury poisioning?
Dimercaprol
| Succimer
122
Methanol, ethylene glycol (antifreeze)?
Fomepizole
| Dialysis
123
Methemoglobin poisoning?
Methylene blue
| Vitamine C
124
Opiods poisoning?
Naloxone
125
Salicylates poisoning?
NaHCos (dialysis)
126
Warfarin poisoning?
```
Vitamin K (delayed effect)
Can give FFP
```
127
What drugs cause coronary vasospasm?
Cocaine
Sumatriptan
Ergot Alkaloids
128
Drugs cause cutaneous flushing?
```
Vancomycin
Adenosine
Niacine
Ca+ channel blockers
Echinocandins
```
129
Drugs causes dilated cardiomyopathy?
Anthracyclins (doxorubicin) prevent with dexrazoxone
130
Drugs causing Torsades de points?
```
Anti-arrythmics (class 1A and III)
Antibiotics (macrolides)
Anti-psychotics (haloperidol)
Anti-depressants (TCA)
Anti-emetics (ondansetron)
```
131
Drugs causing adrenocrotical insufficiency?
Glucocorticoid withdrawl
132
Causing hot flashes?
Tamoxifen
| Clomphene
133
Causing hyperglycemia?
```
Tacrolimus
Protease inhibitirs
Niacin
HCTX
Corticosteroids
```
134
Causing hypothryoidism?
Lithium
Amiodarone
Sulfonamides
135
Causing cholestatic hepatitis and jaunedice?
Erythromycin
136
Causing diarrhea?
Acanorosate
Acarbose
Cholinesterase
Colchicine
137
Causing hepatic necrosis?
Halothane
Amanita phalloides
Valporic acid
Acetaminophen
138
Causing hepatitis?
Rifampin
Isoniazid
Pyraszinamide
Statins
139
Causing pancreatitis?
```
Didansine
Corticosteroids
Alcohol
Valporic Acid
Azithipine
Diuretics
```
140
Causing esophagitis?
Tetracyclnes
Bisphosphonates
Potassium Chloride
141
Causing pseudomembraneous colitis?
Clindamycin
Ampicillin
Cephalosporins
142
Causing agranulocytosis?
```
Clozapine
Carbamazepine
Propylthiouricil
Methimazole
Colchicinine
Ganicyclovir
```
143
Causing Aplastic anemia?
```
Carbamazepine
Methimazole
NSAIDS
Benzene
Chloramphenicol
```
144
Cause direct coombs hemolytic anemia?
Methyldopa, penicillin
145
Gray baby syndrome?
Chloramphenicol
146
Hemolysis of G6PD?
```
Isoniazid
Sulfonamides
Dapsone
Primaquine
ASA
Nitrofurantoin
Ibuprofen
```
147
Causes megaloblastic anemia?
Phenytoin
Methrotrexate
Sulfa drugs
148
Causing Thrombocytopenia?
Heparine
149
Thrombotic complications?
Oral contracpetives
| Hormone replacement
150
Changes in fat distribution?
Protease inhibitors
| Glucocorticoids
151
Causing gingival hyperplasia?
Phenytoin
Calcium channel blocker
Cyclosporine
152
Causing hyperuricemia?
```
Pyrazamide
Thiazides
Furosamide
Niacin
Cyclosporine
```
153
Causing myopathy?
```
Fibrates
Niacn
Cholcine
Hydroychloroquine
interferon alpha
penicillamine
statins
glucocorticoids
```
154
Causing osteoporosis?
Corticosteroids
| Heparine
155
Causing photosenstivity?
Sulfonamides
Amiodarone
Tetracyclines
5-FU
156
Causing Stevens-Johnson syndrome?
Anti-epileptic syndrome
Allp[urional
Sulfa
Penicilleine
157
Causing SLE like syndrome?
```
Sulfa
Hydralazine
Isoniazid
Procainamide
Phenytoin
Etanercept
```
158
Causing teeth discoloration?
Tetracycline
159
Causing tendonitis, tendon rupture, cartilage damage?
Fluoroquinolones
160
Drugs (causing cinchonism? (flushed and sweaty skin, tinnitus, blurred vision, hearing imparied, confusion, hearing loss, headache, abdominal pain)
quinidine
161
Parkinson like syndrome?
Antipsychotics
Reserpine
Metoclopramide
(Cogwheel of the arm)
162
Seizures?
```
Isoniaizid
Bupropion
Imipenum
Tramadol
enflurane
```
163
Tardive dyskinesia?
Antipsychotics
| Metoclopamide
164
Drugs causing diabtetes insipidus?
Lithium
| Demeclocycline
165
Drugs causing Fanconi syndrome?
Tenofovir
| Ifosfamide
166
Drugs causing hemorraghic cysts?
Cyclophasphamide
| ifosfamide
167
Drugs causing interstitial nephritis?
Methicillin
NSAIDS
Furosemide
168
Drugs causing SIADH?
Carbamazepine
Cyclophosphamide
SSRI
169
Drugs causing dry cough?
ACE inhibitors
170
Drugs causing pulmonary fibrosis?
```
Methotrexate
Nitrofurantoin
Carmystine
Bleomycin
Busilfan
Amiodarone
```
171
Drugs causing antimuscarinic?
Atropine
TCA
H1 blockers
Antipsychotics
172
Drugs causing disulfiram-like reactions?
```
Metronidazole
Cephalosporins
Griseofulvin
Procarbazine
Sulfonylurea
```
173
Drugs causing nephrotoxicity and ototoxicity?
Aminoglycosides
Vancomycin
Loop diuretics
Cisplatin
174
Inhibitos of anti-epileptics?
ETOH
175
Onhibitos of theophylline?
Ritonavir
176
Inhibitors of warfarin?
Amiodarone
177
Inhibitos of OCP?
```
Cimentidine
Cipro
Ketocanozole
Sulfamides
Isoniaziad
Grapefruit
Quinidine
Macrolides (Not azithromycin)
```
178
Inducers of anti-epiletpics?
Chronic ETOH (acute ETOH inhibits it)
179
Inducers of theophyylline?
St John's Wart
180
Inducers of warfarin?
Phenytoin
181
Inducers of OCP?
```
Phenobarbital
Nevirapine
Rifampin
Griseoflulvin
Carbamazepine
```
182
Name some sulfa drugs?
```
Sulfonamide antibiotics
Sulfasaoazine
Probenecid
Furoseamide
Acetazolamide
Celecoxib
Thiazides
Sulfonylureas
```
183
What are side effects of sulfa drugs?
```
Fever
UTI
Stevens-Johnson
Hemolytic anemia
Thrombocytopenia
Agranulocytosis
Urticaria
```
184
Drugs ending with -azole?
Ergosterol synthesis inhibitor (ketoconazole)
185
Drugs with bendazole?
Antiparasitic/antihelaminths
| Mebendazole
186
Drugs with cillin?
Peptidoglycans synthesis inhibitor ?
| Ampicillin
187
Durgs with cycline?
Protein synthesis inhibitor
| Tetracycline
188
Drugs with ivir?
Osetlamavir
| Neuramindase
189
Drugs with navir?
Protease inhibitor
| Ritonavir
190
Drugs ending in ovir?
Acyclovir
| DNA polymerase inhibitor
191
Drugs with thormycin?
Macrolide antibiotic
| Azithromycine
192
Drugs with ending azine?
Typical antipsychotic
193
Drugs ending with barbital?
Barbituate
| Phenobarbital
194
Drugs with glitazone?
PPAR activator
| Rosiglitazone
195
Drugs with prazole?
Proton pump inhibitor
196
Drugs with zumab?
Humanized monoclonal antibody
| Daclizumab
197
Drugs with zosin?
Alpha antagonist
| Prazosin
198
Drugs with zumab ending?
Humanized monoclonal antibodies
| Daclizumab
199
Drugs with ximab ending?
Chimeric monoclonal AB (Basiliximab)
