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Pharma > Board Review > Flashcards

Board Review Flashcards

1
Q

Buspirone, a drug with large first pass effect

Which of the following pharmacokinetic properties of the drug was most likely affected by this large first pass?

A

Oral bioavailability

Amount of concentration of the drug available at that particular time

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2
Q

First pass effect affects

A

Absorption

Bioavailability

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3
Q

Ability of drug to cross the placenta at fastest rate

A

Low molecular weight
Not bound to maternal plasma protein
Least ionized in maternal plasma

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4
Q

Measure that most reliably reflects the total amount of drug reaching the target tissue

A

Area under the curve

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5
Q

Factor that determines how long it will take for the drug to reach a steady-state concentration CSS in blood

A

Half-life

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6
Q

Phase II reaction

a. Glucoronidation
b. Deamination
c. Hydrolysis
d. Reduction

A

Conjugation reaction
Transferase
Glucoronidation

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7
Q

Elimination rate via metabolism catalyzed by alcohol dehydrogenase when the enzyme is saturated

A

Zero order kinetics

Ex. Phenytoin, Aspirin, Warfarin, Theophylline

Already saturated the enzyme
Plateau
Rate of elimination is not proportional to the concetration

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8
Q

Related to zero order kinetics

A

Toxicity

Narrow therapeutic index

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9
Q

Initial rates of drug distribution to different tissues depend primarily on which of the following parameter?

a. blood flow to the tissue
b. fat content of the tissue
c. degree of ionization of the drug un the tissue
d. active transport of the drug out of different cell type

A

INITIAL

blood flow

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10
Q

The pro-drug increases the expression of CYP450 that converts the pro-drug to its active form.

With chronic, long-term administration of the prodrug, which of the following will be observed

a. potency will decrease
b. potency will increase

A

Potency will increase

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11
Q

Antiseizure medication Phenobarbital

Diminished breathing
Low body temperature
Skin reddening

Barbiturate overdose

How does bicarbonate help overcome toxic effects of phenobarbital

A

Bicarbonate is a weak acid and there is overdose
We do not want it to recirculate
We want to trap weak acid (barbiturate) in the urine
It decreases distal tubular reabsorption

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12
Q

Vd

A

protein binding

The more protein-bound, the lesser the binding to tissue

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13
Q

What the drug can induce to body

A

Pharamcodynamics

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14
Q

Loraradine binding to H1 receptor is

A

Affinity

Selective drug
Mass action
Total amount of drug that comes in, it will bind to a receptor

After the drug binds to receptor, receptor activation

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15
Q

Full agonist

A

Maximal efficacy

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16
Q

Two drugs act on the same tissue or organ via activarion of different receptors, resulting in effects that are qualitatively the opposite of one another

An example would be the direct effects of norepinephrine and acetylcholine on heart rate. This represents which of the following types of antagonism?

a. Chemical
b. Competitive
c. Pharmacologic
d. Physiologic

A

Physiologic - yin and yang of pharmacology
Insulin vs Cortisol
Sympa vs Para

Pharmacologic
•Chemical - Heparin vs Protamine sulfate
• Competitive - enzyme not saturable, concentration-dependent

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17
Q

Dopamine, epinephrine and histamine interact with their cellular serpentine receptors

How do they mainly elicit their responses?

a. activating PLC
b. activating adenylate cyclase leading to inc cAMP
c. inducing or inhibiting synthesis of ligand-specific intracelualr proteins
d. opening or closing ligand-gated ion channels
e. regulating intracellular 2nd messengers through G protein-coupled receptors

A

Regulating intracellular 2nd messengers through G protein coupled recetors

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18
Q

Range of doses that have a high probability of therapeutic success

a. Efficacy
b. Potency
c. Therapeutic index
d. Therapeutic window

A

Therapeutic window

LD50/ED50

TILED

Therapeutic index = Lethal dose/ED50

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19
Q

If a drug has no intrinsic activity and bound reversible to B1 receptor, the drug is

a. Full agonist
b. Partial agonist
c. Competitive antagonist
d. Noncompetitive antagonist

A

Competitive antagonist

Non competitive antagonist = covalent, irreversible ex. aspirin (it will take you 7-10 days before aspirin will be eliminated)

Agonist = inherent power of 1
Antagonist = inherent power of 0
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20
Q

TMP-SMZ

Both are bacteriostatic when given alone but bactericidal effect is obtained when the two drugs are given in combination

What do you call this drug interaction?

a. Additive effect
b. Potentiation
c. Synergysm
d. Tolerance

A

Synergism

Potentiation
- no relationship with each other but when given together, they are effective

Co-Amox (beta lactamase) when given together can eliminate beta lactam ring of clavulanic acid instead of amoxicillin (clavulanic is like suicide drug) -
potentiation

Synergysm - both agonist 1 + 1 = 3

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21
Q

Drug with least amount that creates an effect (Potency) but it doesn’t mean that it is equally effective

At a dose of 2mg, it creates + 15 HR
Ar a dose of 10mg, it creates + 22
At a dose of 15mg, it creates + 30HR
At a dose of 20mg, it creates +55HR

Which is the most potent?

A

A dose of 2mg

Which is most effective?
A dose of 20mg

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22
Q

A 51-year old man reported to his physician that in the morning he noticed his urine was cloudy and red.

The man had been taking on oral anticoagulant for 3 weeks to treat a deep venous thrombosis. If the patient’s symptoms were caused by the anticoagulant, which adverse drug reactions as most likely involved?

a. Overdose toxicity
b. Autoimmune reaction
c. Idiosyncratic reaction
d. Hypersensitivity
e. Immediate allergic reaction

A

Overdose

Augmented type of allergic reaction

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23
Q

Non competitive antagonist

a. Alters the mechanism of action of an agonist
b. Alters the potency of an agonist
c. Shifts the dose-response curve of an agonist to the right
d. Decreases the maximum response to antagonist
e. Binds to the same site on the receptor as the agonist

A

Decreases the maximum response to antagonist

ED50 will not be affected by non competitive antagonist

ED 50 will be affected by competitive antagonist by increasing ED50

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24
Q

Mild asthma b2 agonist

Which of the following was most likely the immediate consequence of activation of B2 receptors?

a. conformational change of a G protein
b. Increased synthesis of cAMP
c. Decreased synthesis of cAMP
d. Phosphorylation of a G protein

A

Conformational change of a G protein

Parasympthetic receptors -

M1 - Brain, (Gq) PLC 2nd: IP3 DAG always Ca

M2 - Heart (Gi)

M3 - Bladder and all of the body not supplied by the parasympathetic (Gq) oPLC 2nd: IP3 DAG always Ca

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25
Q

Governs acid production

A

M1 (Gq)

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26
Q

Sympathetic

A

a 1 -Gq IP3 DAG, Ca, vasoconstrict, inc sphincter tone

a 2 - Gi (autoreceptor) in presynapse release of NE from cleft, stimulates autoreceptor creating negative feedback -> inhibition of NE release

Gs - beta receptors

27
Q

Subfamily of CYP450 responsible for the highest fraction of clinically important drug interactions resulting from metabolism

A

CYP3A4 50%

CYP2D6 - prone to polymorphism

28
Q

A japanese man had been receiving a standard dose of warfarin, which is an anticoagulant drug biotransformed by CYP2C9

Which is the most likely cause of the patient’s disorder?

a. Increased protein binding of warfarin
b. Decreased renal excretion of warfarin
c. Inherent polymorphism of CYP2C9
d. Increased metabolism of CYP2C9

A

Inherent polymorphism of CYP2C9

29
Q

African American with weakness, fatigue, yellowing of skin and sclera and slight fever

He was given chloroquine as prophylaxis for malaria
Lab findings confirmed hemolytic anemia likely due to chloroquine use

Due to

A

G6PD deficiency

30
Q

Patient has acute intermittent porphyria. If coma was caused by thiopental, which of the ff drug reactions is likely involved?

A

Idiosyncratic reaction

31
Q

Which of the following drug may prevent absorption of Vit K?

a. Lovastatin
b. Cholestyramine
c. Niacin
d. Gemfibrozil

A

Cholestyramine

Niacin converts cholesterol to VLDL
Gemfibrozil stimulated PPAR-alpha gene transcription stimulating insulin and fat deposition

32
Q

Succinylcholine was given and drug-induced paralysis lasted several hours

Which enzyme polymorphism is responsible to cause this problem?

a. acetylcholinesterase
b. Glucose-6-phosphate dehydrogenase
c. N-acetyltransferase

A

N-acetyltransferase

Non-depolarizing drugs - curare (tobucurarine)

33
Q

Severe allergic reaction to procaine an ester-type local anesthetic provokes allergic or anaphylactic reaction.

Which will also provoke allergic or anaphylactic reaction?

a. Bupivacaine - longest amide
b. Lidocaine - intermediate
c. Mepivacaine -intermediate
d. Prilocaine -intermediate
e. Tetracaine - long acting, lipid solubility amide

A

Tetracaine

Esters - no “i” before caine
Amide - procaine, tetracaine, cocaine (least)

34
Q

A pregnant woman with low RBC and positive direct Coombs test during regular visit

Woman had started treatment with methyldopa because of stage 1

Which most likely mediated the drug-induced reaction?

a. Deficiency of NADH-methemoglobin reductase
b. Product ion of autoantibodies against RBC
c. Drug-induced deficiency of folic acid
d. Drug-induced bone marrow supression
e. Deficiency of G6PD

A

Product ion of autoantibodies against red blood cell

Methyldopa is a good drug for pregnants because it is protein bound does not cross BBB

35
Q

Peripheral neuropathy a known adverse effect of isoniazid, is caused by the patient’s symptoms and signs

a. Rifampin-ibduced inhibition if isoniazid
b. Deficiency of N-acetyltransferase

A

Deficiency of N-acetyltransferase

36
Q

Palpitations, dry mouth, blurred visions and constipation

Depression with use of antidepressant therapy

a. a1 and a2
b. a1 and B1
c. M2 and M3
d. B1 and B2

A

M2 and M3 blockade

37
Q

65 year old, open angle glaucoma underwent ocular surgery

Before the operation, opthalmologist instilled few drops of carbachol in conjunctival sac

Which of the following anatomical structures represents the primary site of action of this drug?

a. Ganglionic neurons
b. Ciliary muscle
c. Lens
d. Radial muscle of iris - dilate

A

Inc IOP, open angle glaucoma has too much aqueous production vs closed angle, there are ciliar muscles that impede canal of schlemm

You need a drug to cause miosis to constrict
Give Carbachol

Contraction of ciliary muscle lead to drainage of aqueous humor to canal of schlemm

Any drug that impede accomodation whether near or far (BOV) anticholinergic agents inhibits M3 receptor of ciliary muscle -> dilation with cyclopegia

Beta blockers can cancel radial muscle but cannot paralyze ciliary muscle since it is controlled by M3

38
Q

Urinary retention neurogenic atonic bladder

Bethanechol was given

Which of the following most likely mediated the therapeutic effectiveness of the drug?

A

Increased tone of the bladder detrusor muscle

39
Q

Neostigmine for MG caused bradycardia

Which molecular mechanism most likely mediated this adverse effect?

a. Opening of ligand-gated K channels
b. Opening of voltage-gated Na channels
c. Increased synthesis of IP3 DAG

A

Opening of ligand gated K channel

Ach slows the heart
Slowing down of the heart rate is caused by opening of K channels

40
Q

GA was induced with thiopental maintained with halothane and nitrous oxide

Tubocurarine, a muscle relaxant

Which is most likely given to reverse muscle paralysis

a. Physostigmine
b. Edrophonium
c. Neostigmine
d. Bethanicol
e. Pralidoxime

A

Neostigmine

Quarternay compound, polar, ionized and water soluble canNOT cross BBB something that will act on peripheral receptor

Physostigmine can cross BBB because it is a tertiary compound

physostigmine c

41
Q

Atropine can control diarrhea because it acts on the

a. histamine secretion by gastric cell
b. inositol triphosphate/diacylglycerol (IP/DAG)
c increase in cAMP

A

Inositol phosphate/DAG

42
Q

Therapeutic effect of scopolamine is blockade of

a. B1 adrenergic
b. D2Dopaminergic
c. M1 cholinergic

A

M1 cholinergic

43
Q

Accidental spraying of ipratropium will most likely cause the following anticholinergic side effect?

a. hallucination
b. increase salivation
c. AV block
d. Difficulty in near vision

A

Difficulty in near vision

44
Q

Mechanism of botulinum toxin

a. Directly activated all muscarinic and nicotinic receptors
b. Inhibits Ach release from all cholinergic nerves

A

Inhibits Ach release from all cholinergic nerves

45
Q

Epinephrine-induced increase duration of lidocaine effect was most likely mediated by activation of the ff adrenoreceptor?

a. B1
b. B2
c. a1
d. a2

A

alpha1

46
Q

Molecular action of the therapeutic effect of dobutamine?

a. Activation of PLA2
b. Increased synthesis of IP3DAG
c. Increased cAMP

A

increased cAMP

47
Q

Albuterol’s therapeutic efficacy is because of

a. Increased microvascular permeability
b. Decreased bronchial secretion
c. Release of histamine from mast cell
d. Increasef mucociliary clearance

A

Increasef mucociliary clearance

48
Q

Acebutalol Type II antiarrythmic and Pindolol are classified as b blockers with intrinsic sympathomimetic activity (ISA)

this means

A

They are partial agonist (mixed agonist/antagonist)

submaximal effect

49
Q

Therapeutic effect of phenoxybenzamine

a. Decreases peripheral vascular resistance
b. Increased cardiac output
c. Decreased epinephrine release from adrenal medulla
d. Increased heart rate

A

Decreased peripheral vascular resistance

Phenoxybenzamine - irreversible covalent binding to alpha receptors

So in a tumor, you need something that will bind permanently (covalently) despite release of tons of vasoconstrictors

Phentolamine is kicked off because it does not bind irreversibly (non-covalent)

50
Q

Weakness
Drowsiness
Palpitation

Diagnosed with bladder obstruction due to BPH
has been taling a drug for 2 weeks

Which is the patient likely taking?

A

Tamsulosin

Block of a1 on trigone sphincter loosens them

51
Q

Prazosin will cause

a. Mydriasis
b. Impaired micturition
c. Pale and cold skin
d. Bronchoconstriction
e. Postural hypotension

A

Postural hypotension

First dose syncope
Vasodilates capacitance vessels less blood going to brain

52
Q

Timolol, open angle glaucoma for 3 months

Treatment stopped progression of optic nerve damage

Which of the following is the most likely site of action of timolol?

a. Uvoscleral vessel
b. Conjunctival vessel
c. Ciliary EPITHELIUM NOT MUSCLE
d. Retinal vessel

A

Ciliary epithelium

53
Q

Parient has hyperthyroidism

Which of the ff drugs is likely included in the therapeutic management of this patient?

a. Albuterol
b. Propranolol
c. Labetalol
d. Prazosin

A

Propranolol

blocks 5’ deiodinade conversion of T4-T3
MSA membrane stabilizing effect highest MSA can cause sedation

54
Q

Atenolol
Verapamil
Digoxin

Which best explains the therapeutic effectiveness of all these drugs in treating atrial fibrillation?

a. Decreased AV conduction
b. Increased intra-atrial conduction
c. Increased ventricular refractoriness
d. Increased myocardial contractility
d. Decreased cardiac preload

A

Decreased atrioventricular conduction

Atenolol - both atria and ventricle
Verapamil - on atria mostly
Digoxin - on atria blocks Na-KATPase; blocks K arm of ATPase no sodium coming in, no depolarization

55
Q

58 MI
Ventricular tachycardia given IV Amiodarone

The therapeutic effect of the drug was most likely mediated by an increase in which of the following electrophysiologic parameter

a. Slope of phase 4
b. Slope of phase 0
c. Action potential duration
d. Length of phase 2

A

Amiodarone is a class III antiarythmic affecting Phase III

Block K channels
Delay depolarization of heart

Increase AP duration by blocking K channels

56
Q

Dry disturbing cough from use of essential hypertension drug

Which caused the sign and symptom?

a. Captopril
b. Clonidine
c. Propranolol
d. Minoxidil
e. Nifedipine

A

Captopril

57
Q

Safest drug to give on pregnant hypertensive patient

a. Captopril
b. Prazosin

A

Prazosin

58
Q

Variant angina appropriate therapy

a. Propranolol
b. Furosemide
c. Verapamil
d. Captopril

A

Verapamil

59
Q

Sublingual nitroglycerine oral isosorbide can cause a potential detrimental side effect of nitrate in prophylactic treatment of exertional angina?

a. Decreased ejection time
b. Increased heart rate

A

Increased heart rate

60
Q

Prevents new stone production after operation?

a. Acetazolamide
b. Hydrochlorthiazide
c. Furosemide
d. Triamterine
e. Spironolactone

A

HCTZ inhibits Na-Ca exchange

Remove sodium reabsorption of Ca

Loop diuretic will aggravate condition, loose calcium too much calcium in tube

61
Q

CHF drug that caused serious allergic reaction to (furosemide)

Which of the ff diuretics was most likely prescribed?

a. Spironolactone
b. Acetazolamide
c. Triamterine
d. Ethacrynic acid
e. Indapamide

A

Ethacrynic acid

Furosemide
HCTZ
sulfa-containing diuretics

62
Q

Captopril for CHF delivers several benefits to CHF because

a. High affinitt for angiotensin II receptors
b. Promotes increased peripheral vascular resistance
c. Decreases CO and increases afterload
d. It causes venodilation and induces natriuresis
e. It increases preload

A

It causes venodilation and natriuresis

63
Q

Drug that acts by multiple mechanism including inhibition of phosphodiesterase in inflammatory cells

a. Tiotropium
b. Albuterol
c. Theophylline

A

Theophylline inc cAMP (symp)
parasympathetic cGMP, inc cGMP ensures bronchodilation

Also acts on heart, inc cAMP goes to brain
Effect on adenosine receptors on heart Gs Beta 1

Effect on inflammatory cells deacetylation

Pharma (26 decks)

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