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PHARM > Pharmacology pt. 2 > Flashcards

Pharmacology pt. 2 Flashcards

1
Q

P-glycoprotein is an ____ found on brain capillary endothelial cells (part of the BBB) that inhibits a wide range of substrates/drugs from entering the brain. Inhibition of p-glycoprotein can improve drug delivery to the CNS.

A

efflux pump

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2
Q

an efflux pump found on brain capillary endothelial cells (part of the BBB) that inhibits a wide range of substrates/drugs from entering the brain.

Inhibition can improve drug delivery to the CNS.

A

P-glycoprotein

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3
Q

Activation of adrenergic receptors results in arrestin binding and receptor ______.

This effect is responsible for the tolerance effect seen with alpha-adrenergic (eg, decongestants, vasopressors) and beta-adrenergic (eg, bronchodilators) agonists.

A

internalization

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4
Q

Activation of adrenergic receptors results in ____ binding and receptor internalization.

A

arrestin

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5
Q

This effect is responsible for the tolerance effect seen with alpha-adrenergic (eg, decongestants, vasopressors) and beta-adrenergic (eg, bronchodilators) agonists.

A

adrenergic receptor internalization

via arrestin

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6
Q

Antibody-drug conjugates improve drug efficacy and minimize toxicity by allowing conventional chemotherapeutic agents to _______ cancer cells while sparing healthy cells (ie, targeted delivery).

A

selectively target and kill

*selectively uptaken by cancer cells

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7
Q

Calcineurin inhibitor nephrotoxicity with resultant impairment of renal function is the most significant adverse effect of

A

cyclosporine

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8
Q

enzyme-replacement therapy is a large molecule that cannot be orally absorbed, the replacement enzyme must be administered ______.
Entry into the cell occurs by endocytosis.

A

intravenously

*except pancreatic enzymes which function in GI tract

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9
Q

has MAOI activity and therefore can precipitate serotonin syndrome with concomitant use of an SSRI, SNRI, or TCAs

A

Linezolid

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10
Q

Heart failure leads to reduced liver and kidney blood flow, resulting in reduced drug ____.

A

clearance

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11
Q

Metformin toxicity causes

A

lactic acidosis

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12
Q

Decreased activity of hepatic ______ results in a diminished ability to metabolize drugs such as isoniazid and sulfonamides, leading to an increased likelihood of toxicity.

A

N-acetyltransferase

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13
Q

Overexpression of p-glycoprotein efflux pump in tumor cells has been identified as a cause of

A

multidrug resistance

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14
Q

Cytochrome P450 polymorphisms occurring in the genes result in various phenotypes that differ in their rates of metabolism; individual differences in phenotype alter treatment ___ and drug toxicity.

A

efficacy

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15
Q

Prevents hemorrhagic cystitis due to cyclophosphamide or ifosfamide. Mesna binds acrolein, the toxic metabolite formed by these agents.

A

Mesna

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16
Q

Hemorrhagic cystitis during therapy with cyclophosphamide or ifosfamide is caused by the urinary excretion of the toxic metabolite _____.

A

acrolein

*treat with Mesna

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17
Q

Drugs that inhibit CYP3A4 like, ____, can cause increased statin drug levels and lead to statin myopathy.

A

Macrolide antibiotics,
ketoconazole,
NDHP-CCBs (Verapamil)
amiodarone

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18
Q

The changes in the log dose-response curve expected for the effect of a reversible competitive antagonist added to a full agonist are (2)

A

1) a parallel RIGHT shift (increased ED50)
2) no change in the maximum effect (Emax).

* Noncompetitive = 
curve height shifts down (decreased Emax)
no change (ED50)
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19
Q

Characteristics of a drug resulting in a low Vd (3-5L):

high molecular __,
___ plasma protein binding,
___ charge,
and hydro____

Trap the drug in the plasma compartment resulting in a low Vd

A

weight
high
high
hydrophilicity

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20
Q

a low Vd is __–__ L

A

3-5 L

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21
Q

can reverse the toxicity of methotrexate in non-cancerous cells in the gastrointestinal mucosa and bone marrow

A

Folinic acid (leucovorin)

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22
Q

a serotonin 5-HT3 receptor inhibitor that is used to treat nausea and vomiting following chemotherapy.

A

Ondansetron

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23
Q

Is used in the treatment of gout and for prevention of tumor lysis syndrome.

A

Allopurinol

*Rasburicase for tumor lysis syndrome also

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24
Q

When used in combination with 5-fluorouracil (5-FU), _____ potentiates the cytotoxic action of 5-FU (by binding thymidylate synthetase) and is frequently included in colorectal cancer chemotherapy regimens.

A

leucovorin

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25
Q

The presence of fast and slow ____ within the same population results in a bimodal distribution of the speed of isoniazid metabolism.

A

acetylators

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26
Q

the higher the Volume of Distribution, the greater the drug distribution into the

A

tissues

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27
Q

The drug concentration (mg/L)

is equal to drug dose (mg) divided by ___.

A

Volume of Distribution (L)

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28
Q

Half life is calculated using the ____

A

drug concentration (mg/L)

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29
Q

First order elimination is ____ DEPENDENT elimination

A

Flow

*downwards exponentially slope

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30
Q

List 3 drugs eliminated by ZERO order kinetics

A

Phenytoin
Ethanol
Aspirin (at high concentrations)

a PEA is round like ZERO

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31
Q

In ZERO order kinetics Phenytoin and Ethanol are eliminated in a ______ amount.

A

Constant amount

Ex:
t1/2 = 2
So elimination would be:
10 – 8 – 6 – 4 – 2 – 0

32
Q

Zero order elimination is ____ limited

A

Capacity

*downwards linear slope

33
Q

Antagonism of Muscarinic Receptors causes what to the pupils and Heart Rate?

A

Mydriasis

Tachycardia

34
Q

are nonspecific and act as antagonists muscarinic acetylcholine receptors. This leads to anticholinergic effects (fever, urinary retention, decreased sweating, altered mental status).

A

First-generation antihistamines

35
Q

are more specific to the histamine H1 receptor and have less permeability through the blood-brain barrier

A

second-generation antihistamines (loratadine)

36
Q

___ adrenoreceptors are located on smooth muscle and neurons.

A

Alpha-1

37
Q

Alpha 1 agonist increases smooth muscle tone of the iris dilator causing ____ and blood vessels causing _____

A

mydriasis

vasoconstriction

38
Q

are not eliminated by hepatic or renal clearance. Therefore, no dose adjustment is necessary with impaired hepatic/renal function or use of cytochrome P450 inducers or inhibitors.

A

Monoclonal antibodies (mAbs)

39
Q

During continuous infusion of a drug metabolized by FIRST-order kinetics, the steady state concentration is reached in ____ half-lives.

A

4 to 5

To calculate the time to reach 95% steady state concentration you have to multiply the drug’s HALF LIFE by 4 or 5.

40
Q

Which characteristic should a drug have if hepatic metabolism and clearance is desired?

A 
High lipophilicity (lipid solubility)
Good CNS penetration
Low first pass metabolism
41
Q

Drug dosing regimens with ____ dosing have lower peak and average drug levels, which can help reduce drug toxicity.

A

more frequent

42
Q

Drugs with a narrow therapeutic window are often dosed _____ to prevent large swings in plasma concentration.

A

more frequently

43
Q

Average plasma drug levels are ___ when a fixed amount of drug is given in more divided doses.

A

lower

44
Q

Average plasma drug levels are lower when a fixed amount of drug is given in ____ doses.

A

more divided

*efficacy is the same

45
Q

_____ is a cholinesterase inhibitor with a tertiary ammonium structure that can reverse both the central and peripheral nervous system symptoms of anticholinergic toxicity (fever, urinary retention, decreased sweating, altered mental status).

A

Physostigmine

46
Q

Neostigmine, edrophonium, and pyridostigmine have a quaternary ammonium structure that limits _____ penetration.

A

central nervous system

47
Q

Anticholinergic Symptoms

Peripheral (3)

A

Tachycardia, Flushed skin, Mydriasis

48
Q

Anticholinergic Symptoms

Central (3)

A

Delirium, coma, and respiratory failure

49
Q

The increased drug half-life seen in certain patients is likely due to increased _____, resulting in a higher volume of distribution.

A

total body weight

50
Q

A drug’s half life increases with a higher ____

A

volume of distribution (VD)

Half life = (.7)VD/CL

51
Q

Metabolites can accumulate in the bloodstream of patients with renal dysfunction and lead to drug ___

A

toxicity

52
Q

The most common side effect of aspirin.

A

Gastrointestinal (GI) mucosal injury & bleeding

53
Q

Aspirin induced GI injury is due to cyclooxygenase-1 inhibition, which results in impaired _____ dependent

GI mucosal defense and

____ platelet aggregation.

A

prostaglandin

decreased

54
Q

The primary adverse effects of ___ include flushing, hyperglycemia, and hepatotoxicity.

A

niacin

55
Q

Medication-induced ______ is a common adverse effect of bisphosphonates.

A

esophagitis

56
Q

Bisphosphonates are also associated with increased risk of

A

osteonecrosis of the jaw

atypical femoral fractures

57
Q

Bisphosphonates decrease ______, thus lowering serum calcium levels. They are sometimes used in the treatment of severe hypercalcemia

A

bone resorption

58
Q

Loading dose is affected by _____ and composition.

A

body weight

59
Q

Isosorbide dinitrate has a low bioavailability due to extensive _____ prior to release in systemic circulation.

A

first-pass hepatic metabolism

60
Q

Sublingual nitroglycerin is absorbed directly from oral mucosa into the venous circulation and has a higher

A

bioavailability

61
Q

causes:
Formation of insoluble compounds with polyvalent cations in the gastrointestinal tract

Decreased absorption of drug

A

Chelation

62
Q

Tetracyclines, Fluoroquinolones and Levothyroxine are susceptible to ____ thus decreased gut absorption

A

chelation

*Chelators: Iron, Ca, Mg, Aluminum

63
Q

Neonates Pharmokinetic parameters:

Blood-brain barrier immaturity
↑ Proportion of \_\_\_
↓ CYP enzyme activity
↓ Hepatic \_\_\_\_\_\_
↓ \_\_\_\_ blood flow
A

body water
glucuronidation
Renal (↓ GFR)

64
Q

Neonates have ↑ Distribution of WATER SOLUBLE drugs thus may need ____ mg/kg dose

A

higher

aminoglycosides, vancomycin
*causes lower plasma concentration of drug

65
Q

Neonates have ↓ Renal blood flow & GFR thus may need ___ doses of renally excreted drugs

A

lower

66
Q

have decreased plasma protein concentrations, which can increase free levels of highly protein-bound drugs like phenytoin and penicillin

A

Neonates

67
Q

___ administration is capable of partially bypassing first-pass metabolism thus increasing the drug’s bioavailability

A

Rectal

*decreases drug’s delivery to the liver

68
Q

In ____ individuals, use of lean body weight or an adjusted body weight may be necessary when dosing hydrophilic drugs (eg, aminoglycosides) that do not distribute into adipose tissue.

A

obese

69
Q

In zero-order kinetics, a constant amount of drug is metabolized per unit of time, independent of ___ levels.

A

serum

*1st order CHANGES with serum levels (aka decreases)

70
Q

A highly lipophilic drug will be rapidly distributed to organs with high blood flow like the brain, liver, kidneys, & lungs.

The drug is then REDISTRIBUTED to tissues with relatively lower blood flow like ___, fat, bone.

A

skeletal muscle

71
Q

Antimuscarinic agents and antihistamines with antimuscarinic action are most effective for ____ prevention.

A

motion sickness

72
Q

The presence of Drug A is required for the full effect of Drug B

A

Permissive

73
Q

Effect of substance A and B together is equal to the sum of their individual effects

A

Additive

74
Q

Drug B with no therapeutic action enhances the therapeutic action of Drug A

A

Potentiation

Carbidopa + levodopa

75
Q

Acute decrease in response to a drug after initial/repeated administration

A

Tachyphylactic

Nitrates, LSD, Fluticortisone

PHARM (11 decks)

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