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Preventive And Social Medicine II > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What the body does to the drug

A

Pharmacokinetics

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2
Q

What is the movement of drug into, through and out the body?

A

Pharmacokinetics

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3
Q

What is the flow of the drug?

A

ABDME

  • Absorption
  • Bioavailability
  • Distribution
  • Metabolism
  • Excretion
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4
Q

Pharmacokinetics is determined by the drug’s

A

1) physiochemical properties
2) formulation
3) route of administration

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5
Q

How do drugs cross the membranes?

A 
By:
      Passive diffusion
      Facilitated passive diffusion
      Active transport
      Pinocytosis
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6
Q

What are the 3 primary processes of pharmacokinetics?

A

IDE

Input
Distribution
Elimination

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7
Q

It is the amount of drug in the body in relation to the concentration of drug in the plasma.

A

Volume of Distribution

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8
Q

Where is the drugs with very high VD concentrated?

A

Extravascular tissue

than vascular compartment not homogeneously distributed

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9
Q

Why is VD generally uneven?

A

D/t the differences in blood perfusion, tissue binding, regional pH, and permeability of cell membranes.

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10
Q

What is the factor that predicts the rate of elimination in relation to the drug concentration?

A

Clearance

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11
Q

Clearance: first-order

A

Elimination - not saturable

Rate of elimination directly proportional to concentration

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12
Q

It is also known as:

Mixed-order
Saturable
Dose or conc dependent
Nonlinear
Michaelis Menten Elimination
A

Capacity-limited elimination

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13
Q

What is saturable and also called Vmax?

A

Maximum elimination capacity

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14
Q

It is the Km-drug conc at wc rate of elimination is 50% of Vmax.

A

Capacity limited elimination

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15
Q

Conc that are high relative to the elimination rate is almost independent of

A

Conc state of “pseudo-zero order” elimination

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16
Q

What if dosing rate exceeds elimination capacity?

A

Steady state cannot be achieved

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17
Q

Relationship of conc and dosing

A

Conc will keep rising as long as dosing continues

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18
Q

Where does the elimination of drugs depend?

A

Primarily on the rate of drug delivery to the organ of elimination

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19
Q

What is the main determinant of drug delivery?

A

Bld flow to the organ

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20
Q

Any conc of drug, most of the drug in bld perfusing the organ is eliminated on the

A

First pass of the drug through it

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21
Q

What is the time required to change the amount of drug in the body by one-half during elimination?

A

Half-life

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22
Q

Also time req to attain 50% of steady state or to decay 50% from steady state conditions after a change in the rate of drug administration

A

Half-life

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23
Q

Fraction remaining can be predicted from the dosing interval and t1/2

A

Drug accumulation

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24
Q

Fraction of unchanged drug reaching the systemic circulation following administration by any route

A

Bioavailability

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25
What has the most rapid onset?
IV (100% Bioavailability)
26
Large volume, often feasible, may be painful, 75-100%, 90°
IM - most common: deltoid (5mL) - glutes (10mL)
27
Smaller vol than IM, may be painful, 75-100%, 45° | E.g vaxx, insulin
SC
28
Most convenient, 5-100%, first pass effect may be impt
Oral
29
Less first pass effect than oral, 30-<100%
Rectal
30
<100%, often very rapid onset
Inhalation
31
Usually very slow absorption, used for lack 1st pass effect, prolonged duration of action, 80-100%
Transdermal
32
What refers to extent and rate at wc active moiety (drug/metabolite) enters systemic circulation thus accessing site of action?
Bioavailability
33
What are drug products that contain the same active cmpd in the same amt and meet current official std? Same cmpd, diff brand names
Chemical equivalence
34
What are drug products when given to same px in same dose result in equivalent concs of drug in plasma and tissues
Bioequivalence
35
What are drug products that when given to same px in same dose have same therapeutic and adverse effects?
Therapeutic equivalence
36
What is the principal site of drug met?
Liver
37
Inactive/weakly active subs that has an active metabolite
Prodrug
38
What is the goal of drug met/drug brkdwn?
Make drug easier to excrete
39
Formation of a new/modified fxnal grp or cleavage (oxidation, redxn, hydrolysis)
Phase I
40
Conjugation with an endogenous substance
Phase II
41
What is determined by site of administration and drug formation?
Rate of absorption
42
Rate is independent of amt of drug remaining in the gut
Zero-order | - eg det by rate of gastric emptying tume or by ctrlled-release formulation
43
Dose us dissolved in GI fluids
First order | - e.g rate of absorption proportional to GI fluid conc
44
Produced the desired therapeutic effect
Target conc
45
Steady state of drug Most impt to consider-clearance Dosing rate = rate of elimination (clearance x target conc)
Maintenance dose
46
Dose that promptly raises the conc of drug in plasma to the target conc
Loading dose (antibiotics)
47
What is the single most impt factor determining drug conc?
Clearance
48
What are the factors affecting protein binding?
- albumin conc (low in many dse states) - a1-acid glycoprotein conc (inc in acute inflam dis) Quinidine, Lidocaine, Propanolol - capacity-limited protein binding - binding to rbc
49
What are the factors affecting protein binding?
- albumin conc (low in many dse states) - a1-acid glycoprotein conc (inc in acute inflam dis) Quinidine, Lidocaine, Propanolol - capacity-limited protein binding - binding to rbc
50
What is the principal organ for drug excretion?
Kidneys
51
Small amount of drug is excreted into:
Int, saliva, sweat, breast milk, lungs
52
Influence of drug conc on the magnitude of the response
Pharmacodynamics
53
Component of the biologic sys to wc a drug binds to bring about a change in fxn of the system
Receptor
54
A drug that activates its receptor upon binding
Agonist
55
Component of the biologic sys that accomplishes the biologic effect afte being activated by the receptor; often a channel or enz
Effector
56
A drug that binds to its receptor w/o activating it
Pharmacologic antagonist
57
A pharma antagonist that can be overcome by increasing the dose of agonist e.g beta blockers
Competitive antagonist
58
A pharma antagonist that cannot be overcome by inc the dose of agonist
Irreversible antagonist
59
A drug that counters the effects of another by binding to a different receptor and causing opposing effects
Physiologic antagonist
60
A drug that counters the effects of another by binding the drug and preventing its action, drugs for OD or poisoning (eg antedote)
Chemical antagonist
61
Effects of AchE
Mimicked by muscarine and nicotine | Blocked by atropine
62
No requirement for highly specific chemical structure
Mannitol
63
Conc of drug increase, magnitude of pharmacologic effect also increase
Graded dose response relations
64
Response is continuous and gradual
Response-graded effect
65
Drug-receptor interaction characterized by
- Binding of drug to receptor - Gov by affinity - Potent drugs-elicit a response by binding to a number of particular receptor type at low conc (high affinity)
66
Characterize one drug vs another
Relative efficacy
67
Magnitude of response is equal to
Amt of receptors bound or occupied
68
Occurs when all receptors are bound
Emax
69
Controlled by receptor density, efficacy, affinity, and efficiency of the stimulus-response mechanism of the tissue
Potency
70
What is the conc (EC50) or dose (ED50) of a drug required to produce 50% of that drug's maximal effect?
Potency
71
The extent or degree of an effect that can be achieved in the px Impt for making clin decisions when large doses are needed
Maximal efficacy
72
What is the dose required to produce a particularly toxic effect in 50% of animals?
Median toxic dose (TD50)
73
Dose required to produce a desired effect to that wc produces an undesired effect
Therapeutic index | - tells u the safety of the drug
74
In animals the ratio is
TD50:ED50
75
Its normal fxn is to act as receptors for endogenous regulatory ligands
Proteins
76
What are drugs that bind to physiologic receptors and mimic the regulatory effects of the endogenous signaling compounds?
Agonist
77
What stabilize the receptor in its inactive conformation?
Inverse agonists
78
What bind to receptors w/o regulatory effect, but their binding blocks the binding of the endogenous agonist?
Antagonists
79
High affinity for receptor | Form covalent bonds w receptor
Irreversible antagonist
80
Need not be present in unbound form to inhibit agonist responses once the receptor has been occupied
Irreversible antagonist
81
Duration of action Independent: rate of elimination More dependent: turnover of receptor mol.
Irreversible antagonist
82
What is an example of irreversible antagonist?
Phenoxybenzamine - irreversible alpha-adrenoceptor antagonist - usee to ctrl HPN c/b pheochromocytoma
83
Decrease in actual num of receptors in the cell/tissue Generally occurs only after prolonged or repeated exposure to agonist (over hrs or dayz)
Down-regulation
84
Parts of a prescription
``` 1 superscription 2 inscription 3 subscription 4 avoid confusion 5 proper px info 6 all prescription written in ink 7 date of prescription 8 choice of drug product 9 prescriber's ID 10 errors in drug orders should be minimized ```
85
Parts of Superscription
``` Date Name Address Wt Age Rx ```
86
Parts of Inscription
Name of drug Amt Strength to be dispensed (write generic name) Official gen and approved brand name
87
Parts of Subscription
``` Instructions to pharmacist Signa/sig - how to take prescription - English - avoid abbrev or symbols ```
88
Prescriber's ID
``` Physician's name and professional degree Add Phone number License number PTR number S2 license number (aka dangerous drugs license) ```
89
SCHEDULE I
- High potential for abuse - No accepted med use in US - Heroin, methylene dioxymethamphetamine, lysergic acid diethylamide, mescaline
90
SCHEDULE II
- High pot for abuse - Has currently accepted medical use in US - Abuse may lead to severe psychological/physical dependence - Morphine, oxycodone, fentanyl, meperidine, dextroamphetamine, cocaine, amobarbital
91
SCHEDULE III
- Abuse potential less than I and II - Has currently acceptable med use - Abuse may lead to mod or low physical dependence or high psychological dependence - Anabolic steroids, nalorphine, ketamine, certain sched II in suppositories, mixtures limited amnts per dosage unit
92
SCHEDULE IV
- Abuse potential
93
SCHEDULE V
- Low potential for abuse - Some may be sold in limited amnts w/o a prescription - Buprenorphine, products cont a low dose of an opiod plus a non narcotic s/a codeine and guaifenesin
94
Oral orders
3, 4 & 5 2 if emergency
95
Refills
3 & 4 - orally or in writing, not >5 refills or 6 months after issue date 2 - NOT to be refilled under any circumstance
96
What is the best documented barrier to compliance?
Px w multiple drugs, multiple illness, chronic dse
96
What is the best documented barrier to compliance?
Px w multiple drugs, multiple illness, chronic dse
97
Most common barrier to compliance
High cost

Preventive And Social Medicine II (32 decks)

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