Pharmacology 2 Flashcards
1
Q
What is the specific clinical use of Indomethacin in neonates?
A
Indomethacin is used to close a patent ductus arteriosus.
2
Q
What is used to reverse the action of Heparin?
A
Protamine Sulfate is used for rapid reversal of heparinization (positively charged molecule that binds to negatively charged heparin).
3
Q
What patients are at risk for life threatening hypotension when taking Sildenafil (Viagra)?
A
Those patients who are taking nitrates.
4
Q
What process does Zafirlukast interfere with?
A
Leukotrienes increasing bronchial tone.
5
Q
What type of gout is treated with Allopurinol?
A
Chronic gout.
6
Q
What type of gout is treated with Colchicine?
A
Acute gout.
7
Q
What type of gout is treated with Probenacid?
A
Chronic gout.
8
Q
What type of patient should not take Misoprostol and why?
A
Misoprostol is contraindicated in women of childbearing potential because it is an abortifacient.
9
Q
Which H2 Blocker has the most toxic effects and what are they?
A
Cimetidine is a potent inhibitor of P450; it also has an antiandrogenic effect and decreases renal excretion of creatinine. Other H2 blockers are relatively free of these effects.
10
Q
Why are the Sulfonylureas inactive in IDDM (type-1)?
A
Because they require some residual islet function.
11
Q
Acetaldehyde is metabolized by Acetaldehyde dehydrogenase — which drug inhibs this enzyme?
A
-Disulfram & also sulfonylureas — metronidazole
12
Q
Explain pH dependent urinary drug elimination?
A
-Weak Acids>Alkinalize urine(CN3) to remove more -Weak bases>acidify urine to remove more
13
Q
How do you treat coma in the ER (4)?
A
-Airway -Breathing -Circulation -Dextrose (thiamine & narcan) -ABCD
14
Q
In coma situations you rule out what (7)?
A
-Infections -Trauma -Seizures -CO -Overdose -Metabolic -Alcohol (IT’S COMA)
15
Q
List some specifics of lead poisoning(4)?
A
-A57Blue lines in gingiva & long bones -Encephalopathy & Foot drop -Abdominal colic / -Sideroblastic anemia
16
Q
List the specific antidote for this toxin: Acetaminophen
A
-N-acetylcystine
17
Q
List the specific antidote for this toxin: Amphetamine
A
-Ammonium Chloride
18
Q
List the specific antidote for this toxin: Anticholinesterases (organophosphate.)
A
-Atropine & pralidoxime
19
Q
List the specific antidote for this toxin: Antimuscarinic (anticholinergic)
A
-Physostigmine salicylate
20
Q
List the specific antidote for this toxin: Arsenic (all heavy metals)
A
-Dimercaprol — succimer
21
Q
List the specific antidote for this toxin: Benzodiazepines
A
-Flumazenil
22
Q
List the specific antidote for this toxin: Beta Blockers
A
-Glucagon
23
Q
List the specific antidote for this toxin: Carbon monoxide
A
-100% oxygen — hyperbaric
24
Q
List the specific antidote for this toxin: Copper
A
-Penicillamine
25
List the specific antidote for this toxin: Cyanide
-Nitrate --- hydroxocobalamin thiosulfate
26
List the specific antidote for this toxin: Digitalis
-Normalize K+ --- Lidocaine --- & Anti-dig Mab
27
List the specific antidote for this toxin: Heparin
-Protamine
28
List the specific antidote for this toxin: Iron
-Deferoxamine
29
List the specific antidote for this toxin: Lead
-EDTA --- dimercaprol --- succimer --- & penicillamine
30
List the specific antidote for this toxin: Methanol & Ethylene glycol
-Ethanol --- dialysis --- & fomepizole
31
List the specific antidote for this toxin: Methemoglobin
-Methylene blue
32
List the specific antidote for this toxin: Opioids
-B51Naloxone / naltrexone (narcan)
33
List the specific antidote for this toxin: Salicylates
-Alkalinize urine & dialysis
34
List the specific antidote for this toxin: TPA & Streptokinase
-Aminocaproic acid
35
List the specific antidote for this toxin: Tricyclic antidepressants
-NaHCO3
36
List the specific antidote for this toxin: Warfarin
-Vitamin K & fresh frozen plasma
37
What are the products and their toxicities of the metabolism of ethanol by / alcohol dehydrogenase?
-Acetaldehyde -Nausea --- vomiting --- headache --- & hypotension
38
What are the products and their toxicities of the metabolism of Ethylene Glycol by / alcohol dehydrogenase?
-Oxalic acid -Acidosis & Nephrotoxicity
39
What are the products and their toxicities of the metabolism of Methanol by / alcohol dehydrogenase?
-Formaldehyde & formic acid -severe Acidosis & retinal damage
40
Which drug(s) cause this reaction: Adrenocortical Insufficiency
-Glucocorticoid withdrawal
41
Which drug(s) cause this reaction: Agranulocytosis (3)?
-Cloazapine -carbamazapine -colchicine -PTU
42
Which drug(s) cause this reaction: Anaphylaxis?
-penicillin
43
Which drug(s) cause this reaction: Aplastic anemia (5)?
-Chloramphenicol -benzene -NSAIDS -PTU -phenytoin
44
Which drug(s) cause this reaction: Atropine-like side effects?
-Tricyclic antidepressants
45
Which drug(s) cause this reaction: Cardiac toxicity?
-Daunorubicin & Doxorubicin
46
Which drug(s) cause this reaction: Cinchonism (2)?
-Quinidine -quinine
47
Which drug(s) cause this reaction: Cough?
-ACE inhibitors (Losartan>no cough)
48
Which drug(s) cause this reaction: Cutaneous flushing (4)?
-Niacin -CA++ channel blockers -adenosine -vancomycin
49
Which drug(s) cause this reaction: Diabetes insipidus?
-Lithium
50
Which drug(s) cause this reaction: Disulfram-like reaction (4) ?
-metronidazole -certain cephalosporins -procarbazine -sulfonylureas
51
Which drug(s) cause this reaction: Drug induced Parkinson's (4) ?
-Haloperidol -chlorpromazine -reserpine -MPTP
52
Which drug(s) cause this reaction: Extrapyramidal side effects (3)?
-chlorpromazine -thioridazine -Haloperidol
53
Which drug(s) cause this reaction: Fanconi's syndrome?
-Tetracycline
54
Which drug(s) cause this reaction: Focal to massive hepatic necrosis (4)?
-Halothane -Valproic acid -acetaminophen -Amantia phalloides
55
Which drug(s) cause this reaction: G6PD hemolysis(8)?
-Sulfonamides -INH -ASA -Ibuprofen -primaquine -nitrofurantoin /-pyrimethamine -Chloramphenicol
56
Which drug(s) cause this reaction: Gingival hyperplasia?
-phenytoin
57
Which drug(s) cause this reaction: Gray baby syndrome?
-Chloramphenicol
58
Which drug(s) cause this reaction: Gynecomastia (6)?
-Cimetidine -ketoconazole -spironolactone -digitalis -EtOH -estrogens
59
Which drug(s) cause this reaction: Hepatitis?
-Isoniazid
60
Which drug(s) cause this reaction: Hot flashes?
-Tamoxifen
61
Which drug(s) cause this reaction: Neuro and Nephrotoxic?
-polymyxins
62
Which drug(s) cause this reaction: Osteoporosis (2)?
-Corticosteroids -heparin
63
Which drug(s) cause this reaction: Oto and Nephrotoxicity (3)?
-aminoglycosides -loop diuretics -cisplatin
64
Which drug(s) cause this reaction: P450 induction(6)?
-Barbiturates -phenytoin -carbamazipine -rifampin -griseofulvin -Quinidine
65
Which drug(s) cause this reaction: P450 inhibition(6)?
-Cimetidine -ketoconazole -grapefruit juice -erythromycin -INH -Sulfonamides
66
Which drug(s) cause this reaction: Photosensitivity(3)?
-Tetracycline -amiodarone -Sulfonamides
67
Which drug(s) cause this reaction: Pseudomembranous colitis?
-Clindamycin
68
Which drug(s) cause this reaction: Pulmonary fibrosis(3)?
-Bleomycin -amiodarone -busulfan
69
Which drug(s) cause this reaction: SLE-like syndrome?
-Hydralazine -Procainamide -INH -phenytoin
70
Which drug(s) cause this reaction: Stevens-Johnson syn. (3)?
-Ethosuxamide -Sulfonamides -lamotrigine
71
Which drug(s) cause this reaction: Tardive dyskinesia?
-Antipsychotics
72
Which drug(s) cause this reaction: Tendonitis and rupture?
-Fluoroquinolones
73
Which drug(s) cause this reaction: Thrombotic complications?
-Oral Contraceptives
74
Which drug(s) cause this reaction: Torsade de pointes (2)?
-Class III antiarrhythmics (sotalol) -Class IA (Quinidine)
75
Which drug(s) cause this reaction: Tubulointerstitial Nephritis (5)?
-Sulfonamides -furosemide -methicillin -rifampin -NSAIDS (ex. ASA)
76
Describe first-order kinetics?
Constant FRACTION eliminated per unit time.(exponential)
77
Describe Phase I metabolism in liver(3)?
-reduction --- oxy --- & hydrolysis -H2O sol. Polar product -P450
78
Describe Phase II metabolism in liver(3)?
-acetylation --- glucuron. --- & sulfation -Conjugation -Polar product
79
Explain differences between full and partial agonists(2).
- Act on same receptor - Full has greater efficacy
80
Explain potency in relation to full and partial agonists(2).
- partial agonist can have increased --- decreased --- /A21or equal potency as full agonist. - Potency is an independent factor.
81
How do spare receptors effect the Km?
- ED 50 is less than the Km (less than 50% of receptors)
82
How do you calculate maintenance dose?
Md= (CpxCL)/F Cp= plas. Conc. CL=clear. F=bioaval.
83
How does a competitive antagonist effect an agonist?
-Shifts the curve to the right -increases Km
84
How does a noncompetitive antagonist effect an agonist?
- Shifts the curve down -reduces Vmax
85
Name the steps in drug approval(4)?
-phase I (clinical tests) -phase II -phase III -PhaseIV (surveillance)
86
Steady state concentration is reached in __ number of half-lifes
In 4 half-lifes= (94%) T1/2 = (0.7x Vd)/CL
87
What is the definition of zero-order kinetics? Example?
-Constant AMOUNT eliminated per unit time. -EtOH & ASA
88
What is the formula for Clearance (CL)
CL= (rate of elimination of drug/ Plasma drug conc.)
89
What is the formula for Volume of distribution (Vd)
Vd= (Amt. of drug in body/ Plasma drug conc.)
90
What is the loading dose formula?
Ld= (CpxVd)/F Cp=plasma conc. F= Bioaval.
91
A 12yo patient was treated for a reaction to a bee sting --- what drug provides the best coverage of sympathomimetic receptors?
Epinephirine(Alpha1 ---2 and Beta 1 ---2)
92
A 57 yo heart failure pt develops cardiac decompensation --- what drug will give you adequate perfusion of his kidneys as well as tx for his Hypotension
Dopamine
93
A fellow passenger on a Carnival cruise ship looks pale and diaphoretic --- what antimuscarinic agent would you give them?
scopolamine
94
A group of pts are rushed into the ER complaining of excessive sweating --- tearing --- salivation --- HA --- N and V --- muscle twitching --- difficulty breathing and diarrhea. What drug would be the most effective immediate tx
Atropine pts are suffering from Cholinestrase inhibitor poisining (Nerve gas/Organophosphate poisining)
95
As an Anes you want to use a depolarizing neuromuscular blocking drug on your pt --- what do you use
Succinylcholine
96
MOA of Succinylcholine
Prevents the release of Ca from SR of skeletal muscle
97
Clonidine is the preferred sym pathomimetic tx of HTN in pts with renal disease --- why??
Centrally acting alpha agonist --- thus causing a decrease in central adrenergic outflow --- spairing renal blood flow
98
Cocaine casues vasoconstriction and local anesthesia by what mechanism
Indirect agonist --- uptake inhibitor
99
Cocaine shares is mechanism of action with what antidepressant
TCA
100
Dobutamine used for the tx of shock acts on which receptors
Beta1 more than B2
101
Guanethidine enhances the release of Norepi?
No --- it inhibits the release of Nor Epi
102
How does angiotensin II affect NE release?
It acts presynaptically to increase NE release.
103
How does botulinum toxin result in respiratory arrest?
Prevents the release of ACh --- which results in muscle paralysis.
104
How does dantrolene work?
Prevents the release of calcium from the sarcoplasmic reticulum of skeletal muscle.
105
How does NE modulate its own release? What other neurotransmitter has this same effect?
NE acts presynaptically on alpha-2 receptors to inhibit its own release. ACh also acts presynaptically through M1 receptors to inhibit NE release.
106
How would hemicholinium treatment affect cholinergic neurons?
Hemicholinium inhibits the transport of choline into the nerve --- thus inhibiting formation of ACh.
107
How would you reverse the effect of a neuromuscular blocking agent?
Give an antichloinesterase - neostigmine --- edrophonium --- etc
108
If a patient is given hexamethonium --- what would happen to his/her heart rate?
It would increase to ~ 100 beats/min. Both sympathetic and vagal stimulation would be knocked out --- but the SA node has an intrinsic pace of 100 beats/min --- which is normally checked by vagal stimulation.
109
Isopoterenol was given to a patient with a developing AV block --- why?
Stimulates beta adrenergic receptors
110
Norepi feedbacks and inhibits the presynaptic receptor by what mechanism
Binding to the presynaptic alpha 2 release modulating receptors
111
Reserpine will block the syntheis of this drug and but not its precursor.
Blocks Norepi --- but not Dopamine
112
These drugs acts indirectly by releasing strored catecholamines in the presynaptic terminal
Amphetamine and Ephedrine
113
What anticholinesterase crosses the blood-brain-barrier?
physostigmine
114
What antimuscarinic agent is used in asthma and COPD?
Ipratropium
115
What antimuscarinic drug is useful for the tx of asthma
Ipratropium
116
What are the classic symptoms of cholinesterase inhibitor poisoning (parathion or other organophosphates)?
Diarrhea --- Urination --- Miosis --- Bronchospasm --- Bradycardia --- Excitation of skeletal muscle and CNS --- Lacrimation --- Sweating --- and Salivation = DUMBBELS; also abdominal cramping
117
What are the clinical indications for bethanechol?
Activates cholinergic receptors on bladder and bowel smooth muscle --- alleviating post-op and neurogenic ileus and urinary retention.
118
What are the clinical indications for neostigmine?
Post-op and neurogenic ileus and urinary retention --- myasthenia gravis --- and reversal of neuromuscular junction blockade (post-op) through anticholinesterase activity.
119
What are the indications for using amphetamine?
narcolepsy --- obesity --- and attention deficit disorder (I wouldn't recommend this)
120
What are the nondepolarizing neuromuscular blocking drugs?
Tubocurarine --- atracurium --- mivacurium --- pancuronium --- vecuronium --- rapacuronium
121
What are the phases of succinylcholine neuromuscular blockade?
Phase 1 = prolonged depolarization --- no antidote --- effect potentiated by anticholinesterase; Phase 2 = repolarized but blocked --- an anticholinesterase is the antidote for this phase.
122
What are two indirect acting adrenergic agonists?
amphetamine and ephedrine
123
What beta 2 agonist will help your 21yo Astma pt?
Albuterol --- tertbutaline
124
What cholinergic inhibitor acts by directly inhibiting Ach release at the presynaptic terminal
Botulinum
125
What cholinomimetic is useful in the diagnosis of Myasthenia Gravis
Edrophonium
126
What cholinomimetics might your pt be taking for his glaucoma
Carbachol --- pilocarpine --- physostigmine --- echothiophate
127
What class of drug is echothiophate? What is its indication?
anticholinesterase glaucoma
128
What conditions would you use dantrolene?
In treatment of malignant hyperthermia --- due to concomitant use of halothane and succinylcholine. Also in neuroleptic malignant syndrome --- a toxicity of antipsychotic drugs.
129
What drug is used to diagnose myasthenia gravis?
edrophonium (extremely short acting anticholinesterase)
130
What drugs target anticholinesterase
Neostigmine --- pyridostigmine edrophonium --- physostigmine echothiophate
131
What effect would atropine have on a patient with peptic ulcer disease?
Theoretically it could be used to block the cephalic phase of acid secretion (vagal stimulation).
132
What effect would atropine have on the preganglionic sympathetic activation of sweat glands? Would this person sweat?
None. No --- because atropine would block the postganglionic muscarinic receptors involved in sweat gland stimulation.
133
What enzyme is responsible for the breakdown of ACh in the synaptic cleft?
Acetylcholinesterase; ACh is broken down into choline and acetate.
134
What enzyme is responsible for the degredation of Ach
Acetylcholine esterase
135
What enzyme is responsible for the production of Ach from Acetyl CoA and Choline
Choline acetyltransferase
136
What is the clinical utility of clonidine?
Treatment of hypertension --- especially with renal disease (lowers bp centrally --- so flow is maintained to kidney).
137
What is the clinical utility of cocaine?
The only local anesthetic with vasoconstrictive properties.
138
What is the difference between the affinity for beta receptors between albuterol/terbutaline and dantroline?
Dobutamine has more of an affintiy for beta-1 than beta-2 --- and is used for treating heart failure and shock. Albuterol and terbutaline is the reverse --- and is used in treatment of acute asthma.
139
What is the difference in receptor affinity of epinephrine at low doses? High doses?
Prefers beta's at low doses --- but at higher doses alpha agonist effects are predominantly seen.
140
What is the effect of epinephrine infusion on bp and pulse pressure?
Increased systolic and pulse pressure --- decreased diastolic pressure --- and little change in mean pressure.
141
What is the effect of guanethidine on adrenergic NE release?
It inhibits release of NE.
142
What is the effect of norepinephrine on bp and pulse pressure?
Increases mean --- systolic --- and diastolic bp --- while there is little change in pulse pressure.
143
What is the effect of TCA's on the adrenergic nerve?
They inhibit reuptake of NE at the nerve terminal (as does cocaine).
144
What is the only depolarizing neuromuscular blocking agent?
Succinylcholine
145
What is the receptor affinity and clinical use of isoproterenol?
It affects beta receptors equally and is used in AV heart block (rare).
146
What physiological effects was the Anes using Atropine to tx
SLUD (salivation --- Lacrimation --- urination --- Defecation)as well as airway secretion --- GI motility --- acid secretions
147
What reversal agent could a Anes give to reverse the effects of Atropine
Bethanechol --- Neostigmine --- physostigmine
148
What side effect of using atropine to induce pupillary dilation would you expect?
Atropine would also block the receptors in the ciliary muscle --- causing an impairment in accommodation (cycloplegia).
149
What sympathomimetic would you not prescribe for hypotension in a pt with renal artery sclerosis.
Norepinephrine (Alpha1 ---2 and beta 1)
150
What type of neurological blockade would hexamethonium create?
Hexamethonium is a nicotinic antagonist --- and thus is a ganglionic blocker.
151
What would be the effect on blood pressure with infusion of the alpha -2 agonist clonidine?
Initially vasoconstriction would increase bp --- but then it acts on central alpha-2 receptors to decrease adrenergic outflow resulting in decreased bp.
152
Which antimuscarinic agents are used in producing mydriasis and cycloplegia?
atropine --- homatropine --- tropicamide
153
Which drug increases Sys BP w/o affecting Pulse Pressure
Epinephrine
154
Which of epi --- norepi --- or isoproterenol results in bradycardia?
Norepinephrine
155
Which of the following would atropine administration cause? Hypothermia --- bradycardia --- excess salivation --- dry flushed skin --- or diarrhea
Dry flushed skin --- due to inhibition of sympathetic post-ganglionic blockade on muscarinic receptors of sweat glands. All others are opposite of what would be expected.
156
Which of these three drugs will cause a reflex bradycardia in your pt (Norepi --- Epi --- or Isoporterenol)
Norepinephrine
157
Which receptors does phenylephrine act upon?
alpha-1 > alpha-2; used as a pupil dilator --- vasoconstrictor --- and for nasal decongestion
158
While at a tail gait party --- you bite into a sandwich that a yellow jacket is also enjoying. Knowing your allergy to this creature --- what should you do?
Epinephrine to treat anaphylaxis. Also useful if you have open angle glaucoma --- asthma --- or hypotension.
159
Why are albuterol and terbutaline effective in tx of acute asthmatic attacks?
These B-2 agonists cause respiratory smooth muscle to relax.
160
Why does atropine dilate the pupil?
Blocking muscarinic receptors in the circular fibers of the eye --- results in unopposed action of radial muscles to dilate.
161
Why does NE result in bradycardia?
NE increases bp --- which stimulates baroreceptors in the carotid sinus and the aorta. The CNS signals through vagal stimulation to decrease heart rate.
162
Why is carbachol and pilocarpine useful in treatment of glaucoma?
They activate the ciliary muscle of the eye (open angle) and pupillary sphincter (narrow angle).
163
Why is pyridostigmine effective in the treatment of myasthenia gravis?
As an anticholinesterase it increases endogenous ACh and thus increases strength.
164
Why is reserpine effective in treating HTN?
Reserpine inhibits dopamine transport into vesicles --- attenuating its conversion to NE by dopamine beta-hydroxylase.
165
Why is there a drop in systolic --- mean --- and diastolic bp with infusion of isoproterenol?
Stimulating beta receptors stimulates heart rate --- but beta receptor induced vasodilation reduces peripheral resistance.
166
Why would a patient with cog-wheel rigidity and a shuffling gait be given benztropine?
Parkinson patients benefit from antimuscarinic agents through its inhibitory action within the indirect pathway.
167
Why would dopamine be useful in treating shock?
Receptors = D1=D2>beta>alpha --- thus increasing heart rate (beta) and blood pressure (alpha vasoconstriction) while maintaining kidney perfusion (dopamine receptors)
168
Why would you give a drug like pancuronium or succinylcholine?
Useful in muscle paralysis during surgery or mechanical ventilation.
169
Why would you use pralidoxime after exposure to an organophosphate?
Pralidoxime regenerates active cholinesterase.
170
Will Hemicholinum affect the release of stored Ach during Cholinergic Stimulation
No --- hemicholinum block the uptake of Choline and thus Ach synthesis
171
Would blockade of muscarininc receptors in the bladder be useful in treating urinary retention?
No. Atropine is used to reduce urgency in mild cystitis. So it would aggravate the urinary retention.
172
Your patient wants an effective drug to treat his motion sickness --- what would you prescribe
Scopolamine
