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Fall 2014 - Pharm Intro Unit > Pharm 1 > Flashcards

Pharm 1 Flashcards

1
Q

Pharmacology

A

the study of drugs and their origin, nature, properties, and effects upon living organisms

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2
Q

Pharmacotherapy

A

the use of medicine in the treatment of disease

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3
Q

What 4 ideal characteristics does a pharmacotherapy resource have?

A
  • current
  • complete
  • easy to use
  • unbiased
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4
Q

Why should one not use more than 1 medication if 1 alone is adequate?

A
  • cost

- fewer possible side effects or drug interactions

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5
Q

Why should one use newly approved medications only when there are clear advantages over older medications?

A
  • new are more expensive (no generic)

- we have more history/knowledge of the old meds

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6
Q

Why consider lifestyle modification when indicated before medication therapy?

A
  • avoid negative side effects of drug

- some people prefer not to take meds

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7
Q

What are some possible reasons for the failure of medication regimens?

A
  • adherence/compliance: patients don’t take or don’t do it correctly
  • don’t fill scrip
  • wrong diagnosis = wrong med = med “failure”
  • interaction w/ another drug or food
  • environmental factors
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8
Q

Pharmacokinetics

A

the study of the action of the body on drugs

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9
Q

Pharmacodynamics

A

the study of the action of drugs on the body

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10
Q

Therapeutic Range

A
  • the “sweet spot”: drug is effective w/o causing too many adverse effects
  • above this range, risk of side effects outweighs the benefits
  • below this range, therapeutic benefits are not seen
  • varies from individual to individual
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11
Q

Bioavailability (F)

A

-the fraction or percentage of the drug dose that reaches the systemic circulation

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12
Q

What is the bioavailability of a drug where 50 mg of the 100 mg dose reaches the systemic circulation?

A

F = 50%

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13
Q

First Pass Effect

A
  • blood from GI tract pases through the liver before systemic circulation
  • some drugs are significantly metabolized by the liver before reaching the systemic circulation
  • first pass effect can decrease bioavailability
  • eg nitro: given sublingual, transdermal or IV b/c it has a very high first pass effect so you don’t want to give it orally
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14
Q

Transport from the GI Tract

  1. Passive diffusion
  2. Active diffusion
A
  1. high concentration to low concentration; lipid soluble drugs are absorbed across GI more rapidly than water soluble
  2. specific carrier proteins and saturable kinetics (only so many carrier proteins to transport drug = can limit the drug dose given at one time b/c extra won’t be absorbed
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15
Q

List 4 drug-associated factors that influence absorption.

A
  1. ionization state: non-ionized cross more readily
  2. molecular weight: smaller pass faster than large
  3. solubility/lipophilicity: lipophilic cross more readily than hydrophilic
  4. formulation (solution vs. tablet vs. sustained release): solution faster than chewable faster than swallowed tablet faster than enteric coating
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16
Q

List 4 patient-associated factors that influence absorption.

A
  1. presence of food in GI tract: food can slow down absorption or prevent stomach upset
  2. stomach acidity: usually around 2 but lower pH around mealtimes; some drugs destroyed if pH too low
  3. blood flow to the GI tract: decreased blood to GI = decreased absorption
  4. gastric emptying time: 50 min in 26 y.o. vs. 120 min in 74 y.o.
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17
Q

Oral Route: Abbreviation

A

PO

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18
Q

Oral Route: Advantages

A
  • patient convenience

- easy storage (pills @ room temp)

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19
Q

Oral Route: Disadvantages

A
  • non-emergent

- must pass through GI tract (first pass effect)

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20
Q

Sublingual Route: Abbreviation

A

SL

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21
Q

Sublingual Route: Advantages

A
  • avoid first pass effect

- rapidly absorbed by capillary bed under tongue

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22
Q

Sublingual Route: Disadvantages

A

-limited by volume and sublingual absorption

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23
Q

Sublingual Route: Example

A

Nitroglycerin

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24
Q

Rectal Route: Abbreviation

A

PR

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25
Q

Rectal Route: Advantages

A
  • unconscious or vomiting patients
  • children
  • primarily treat local conditions
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26
Q

Rectal Route: Disadvantages

A
  • comfort

- unreliable absorption

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27
Q

Rectal Route: Examples

A
  • valium/diazepam
  • MS contin tablets (morphine sulfate)
  • enemas
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28
Q

Intravenous Route: Abbreviation

A

IV

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29
Q

Intravenous Route: Advantages

A
  • rapid onset
  • F = 100%
  • emergency
  • NPO patients
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30
Q

Intravenous Route: Disadvantages

A
  • must be soluble in water

- increased risk

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31
Q

Intravenous Route: Examples

A
  • IV push: atropine (heart conditions)
  • slow IV: phenytoin
  • IV infusion: vancomycin
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32
Q

Intramuscular Route: Abbreviation

A

IM

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33
Q

Intramuscular Route: Advantages

A
  • quick onset

- avoids stomach

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34
Q

Intramuscular Route: Disadvantages

A
  • erratic absorption
  • increased risk
  • pain
35
Q

Intramuscular Route: Examples

A

-benzathine pen G vs. procain pen G

36
Q

Subcutaneous Route: Abbreviation

A

SubQ, SC

37
Q

Subcutaneous Route: Advantages

A

-less painful than IV or IM

38
Q

Subcutaneous Route: Disadvantages

A
  • slower
  • sometimes erratic absorption
  • limited volume
39
Q

Subcutaneous Route: Example

A

insulin

40
Q

Inhalation: Advantages

A
  • rapid onset

- local effect

41
Q

Inhalation: Disadvantages

A
  • technique is important

- potential alveolar irritant

42
Q

Inhalation: Examples

A
  • albuterol MDI

- nitrous oxide

43
Q

Intranasal: Advantages

A

-local effect

44
Q

Intranasal: Disadvantages

A

-comfort

45
Q

Intranasal: Example

A

Flonase

46
Q

Topical: Advantages

A

-local delivery

47
Q

Topical: Disadvantages

A

-patient ease of use

48
Q

Topical: Examples

A

dermatologic and ophthalmic

49
Q

Transdermal: Advantages

A
  • avoids GI

- convenience

50
Q

Transdermal: Disadvantages

A

local irritation

51
Q

Transdermal: Examples

A
  • nicotine

- fentanyl

52
Q

What are the parenteral routes of drug administration?

What does that mean?

What is the problem with these routes?

A
  1. IV, IM, subQ
  2. go around/avoid the GI tract
  3. increased risk of infection
53
Q

List 5 determinants used in drug formulation.

A
  1. barriers drug needs to pass: eg oral vs. IV
  2. setting of use: eg OR vs. home
  3. urgency of medical situation: eg emergent vs. non-emergent
  4. stability of drug: acid labile (does an acidic enviro break down the drug? take on empty stomach)
  5. first pass effect
54
Q

A new med is developed to treat prolonged seizures. It has a high first pass effect and is acid labile. Which is the LEAST appropriate route of administration? Which is the BEST?

a. SL b. PO c. SC d. IM e. PR

A
  • least appropriate: PO (don’t want to use oral if there is a high first pass effect and will be broken down by stomach acid)
  • best: IM (avoids GI system)
  • the best would probably be IV if it was an option, but it’s not in this particular question
55
Q

List 3 factors that influence drug distribution.

A
  • blood flow to area of action
  • membrane permeability: lipophilic drugs readily cross BBB
  • plasma protein binding: higher protein binding decreases the unbound/”free” drug in the blood; only unbound drug can exert pharmacological effect
56
Q

Define volume of distribution (give words and math equation).

A
  • the apparent volume into which a drug distributes in the body at equilibrium
  • OR the volume that would be required to contain the administered dose if that dose was evenly distributed in blood or plasma

-Vd = amount in body (mg) / plasma drug concentration (mg/L)

57
Q
  1. What does a small Vd indicate?

2. What does a large Vd indicate?

A
  1. hydrophilic (trapped in plasma) so it has a more difficult time distributing
  2. lipophilic so it has an easier time distributing to tissues
58
Q

Metabolism

A
  • most drugs are biotransformed or metabolized (primarily by the liver) before they can be eliminated
  • this process usually makes the drug more water soluble
59
Q

Phase I Metabolism Reactions

A

-drug oxidized or reduced to more polar form by cytochrome P450 system

60
Q
  1. Substrate
  2. Inducer
  3. Inhibitor
A
  1. drug metabolized by cytochrome P450 system (most lipophilic drugs)
  2. drug that causes more rapid metabolism of substrate drugs (eg chronic EtOH)
  3. drug that causes slower metabolism of substrate drugs
61
Q

Phase II Metabolism Reactions

A

-polar group is conjugated to the drug –> increased polarity

62
Q

Prodrug

also give a couple examples

A
  • inactive substance metabolized to an active substance w/in the body
  • prednisone –> prednisolone
  • codeine –> morphine
63
Q

Active Metabolite

A
  • metabolite that also has therapeutic activity

- primidone –> phenobarbital

64
Q

What are 3 factors that influence metabolism?

A
  • hepatic dysfunction (most metabolism is done by liver)
  • severe CHF (heart and brain get priority blood flow and liver gets less)
  • advanced age
65
Q

Elimination

A
  • drugs are excreted from the body after being metabolized to a more polar form
  • others are excreted unchanged, usually in the urine
66
Q

Filtration

A

-drugs diffuse from blood to nephron (small, unbound, nonionic)

67
Q

Secretion

A

-active transport of drug into nephron

68
Q

Reabsorption

A

-drugs reabsorbed into the blood stream by diffusion from the nephron tubule (small, nonionic)

69
Q

What factor influences elimination?

A

renal dysfunction (can be affected by age, blood flow)

70
Q

Half Life (t1/2)

A

-the time it takes the plasma concentration of a drug to decrease by 50% after a given dose

71
Q

How is half life related to dosing frequency?

A

-the longer the 1/2 life, the longer the dosing interval (lower frequency dosing)

72
Q

How is Vd related to half life?

A

-the smaller the Vd, the shorter the 1/2 life

73
Q

Steady State

A
  • absorption = elimination
  • the drug in the body is in a state of homeostasis
  • steady state is generally reached in 5 half lives
74
Q
  1. If the half life of a drug is 1.5 hrs, what is the steady state?
  2. For a drug with half life 40 hrs?
A
  1. 7.5 hrs (1.5*5)

2. 200 hrs (40*5)

75
Q

Receptor

A

-the component of a cell or organism that interacts with a drug and initiates the chain of biochemical events leading to the drug’s observed effects

76
Q
  1. Agonist

2. Antagonist

A
  1. alters cell physiology by binding to plasma membrane or intracellular receptors
  2. inhibit or block responses caused by agonists
77
Q

Describe 3 dose-response relationships.

A
  1. usually lower doses produce smaller responses and higher doses increase the response b/c more receptors are occupied by the drug
  2. effect plateaus when the amount of drug exceeds # of available receptors
  3. affinity for receptors also plays role (high affin = high potency)
78
Q

List 6 factors that can affect pharmacokinetics and pharmacodynamics.

A
  • genetics: metabolic differences
  • age: kinetic and dynamic differences in v young and v old
  • gender: body composition, hormonal levels
  • ethnicity: hepatic enzymes, habits/traditions, home remedies
  • diet and nutrition: key food-drug interactions
  • pathophysiology: disease affects kinetics and dynamics
79
Q

Pharmacokinetic drug interactions are caused by alterations in…

A
  1. absorption: increase or decrease amount of drug absorbed
  2. distribution: plasma protein binding competition –> transient increase of unbound drug then gets metabolized
  3. metabolism: induction or inhibition of P450
  4. elimination: decrease or increase elimination of drug
80
Q

What are the 4 types of pharmacodynamic interactions?

A
  1. addition: 1 + 1 = 2 (2 drugs do similar things)
  2. synergism: 1 + 1 = 3 (get more than expected out of combo)
  3. potentiation: 0 + 1 = 2 (substance w/o therapeutic activity helps drug work better)
  4. antagonism: 1 + 1 = 0 (effects cancel)
81
Q

Bioequivalence

A

drugs that have the same effect on the body and a nearly identical chemical structure

82
Q

Therapeutic Equivalence

A

drugs that have essentially the same effect on the body, but do not have an identical chemical structure

83
Q

Loading Dose

A

an initial dose that is larger than subsequent doses for the purpose of achieving therapeutic drug concentrations more rapidly

84
Q

Maintenance Dose

A

dose of drug that attempts to maintain a steady state plasma concentration in the therapeutic range

Fall 2014 - Pharm Intro Unit (5 decks)

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