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Intro To Pharmacology Flashcards

(58 cards)

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1
Q

Pharmacokinetics

A

ADME, target site = drug efifets

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2
Q

Drugs are _ in the liver and- - in the kidneys

A

Metabolism occurs in liver and elimination occurs in liver/kidney

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3
Q

Pharmacologic effect

A

Occurs when drug reaches the therapeutic site of action

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4
Q

Once drug is absorbed into body, where does it go?

A

Is in the circulatory system can go anywhere, unwanted, side of action or two receptors ( bound or free)

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5
Q

Dose-concentration~ how fast and how long target is exposed to drug
VS
concentration affect ~ drugs affect at certain concentration

A

Kinetics
Vs
dynamics

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6
Q

Therapeutic drug monitoring is based on what, used for what

A

Measure of drug serum concentration to optimize dose regimens
Based on absorption rate distribution in elimination

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7
Q

Therapeutic range of drug

A

Range between the minimum toxic concentration in the minimum effective concentration

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8
Q

What affects the rate and efficiency of absorption of medicine a.k.a. when it’s taken orally versus IV

A

medicine administer IV equals 100% to circulatory system

Extravascular must be absorbed through G.I. tract

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9
Q

What can impact oral drug absorption?

A

Drug formulation – immediate versus extended release
Lipophilicity or hydrophilic
Drug concentration
Blood
Other medication
Disease state/gastric pH
Gender/age

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10
Q

What does an increased lipophilicity do for absorption?

A

Increases the ability to cross the cell membrane due to livid by layer no ionized drugs cannot cross cell membrane

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11
Q

Why is it important to know how drug is absorbed into cell?

A

For example, if methotrexate uses folic acid transport system and fully levels are low absorption will be decreased unless supplemented

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12
Q

Bioavailability F

A

Proportion of medications do that reaches circulatory system
Ranges 0-1
IV is always 100%

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13
Q

Why would bioavailability F be less than one?

A

Medication failed to enter circulation could be metabolized in G.I. track or liver in solubility or incomplete release of dosage

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14
Q

What is the benefit of switching from IV to PO medication?

A

You can take pills at home, non-invasive, lower infection, risk, safer for body to reject, often cheaper

Look at bio availability to understand what dosage to give

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15
Q

What is required for distribution of a drug?

A

The vascular system must have good blood flow, solubility, drugs, level of binding, to tissues proteins receptors

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16
Q

What do plasma proteins do?

Name them

A

They are inert binding sites (don’t cause rxn) that medication bind to when remain in blood end up with protein, bound, drug and unbound drug

Albumin and Alpha one acid glycoprotein

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17
Q

What is drug protein binding affected by?

A

Other medications, disease, state, chronic kidney or liver disease

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18
Q

How does local toxicity occur?

A

When tissue bound drugs, spine to a receptor with a high affinity and accumulate in certain area

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19
Q

Why are lipophilic medications used in high doses to reach the blood pain barrier in central nervous system

A

Medications will take time to distribute to these areas, prolongation of action

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20
Q

What is volume of distribution and its equation?

A

Amount of drug in the body to the serum concentration – blood concentration, helpful to determine loading dose and how long men will stay in body

Vd equals amount of drug and body divided by plasma drug concentration

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21
Q

What does a small volume of distribution mean versus large?

A

Water soluble, high plasma, protein binding, low tissue binding equals small
Large equals lipid, soluble, low ionization, high tissue binding, not homogenously distributed

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22
Q

If volume of distribution equals5 , x ,x….

A

five – blood
10 – extra cellular fluid
25 – intracellular fluid
40 – whole body
Greater than 100 equals deep tissue

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23
Q

If a drug works by inhibiting channels in the heart, what does the volume of distribution need to be?

A

Large because it needs to go to a specific organ

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24
Q

What are the common membrane transporters to get drugs across the cell membrane?

Study These Flashcards
A

P-glycoprotein P-gp = E flux pump, reduces drug absorbent brain penetration, active

Organic anion transporters OAT = influx, transporter into cells, especially in kidneys, facilitated diffusion

Considered substrate of proteins

25
Where does majority of metabolism occur?
In the liver also occurs in kidneys G.I. track
26
What’s the difference between an active metabolite and a prodrug metabolite
Active metabolism retains pharmacologic activity like parent drug while road drug metabolite becomes active parent drug inactive
27
What is issue with lipophilic drugs
Trouble removing from body because reabsorbed back into kidney need to be in more water soluble form
28
What occurs in phase one versus phase 2 of metabolism?
Phase one become less active more polar due to more soluble functional group versus phase 2 inactivates drug makes hydrophilic, conjunction, the facilitates excretion
29
These one metabolism uses what enzyme
Cytochrome P450 (CYP450) primarily in liver throughout body
30
A drug may be a substrate, inducer, and or inhibitor of a blank enzyme
CYP450 enzyme not highly selective Substrate means metabolized by enzyme specifically Inducer means enhance rate of synthesis of CYP, accelerates metabolism of drug Inhibitor decreases slows activity of CYP, inhibits metabolism of drug
31
What drug drug interactions lead to
Alters, pharmacokinetics and anticipated, therapeutic response, adverse effects, toxicity, increased\ decreased efficacy (desired effect)
32
How do genetic polymorphisms affect metabolism?
Can lead to CYP enzymes, differing, rapid or slow metabolism – can test for this
33
Why isn’t codeine recommended for kids?
Due to a CYP2D6 polymorphism leading to ultra rapid metabolizers of codeine Metabolize codeine into morphine quickly
34
Phase 2 of metabolism helps what
Increases water solubility to facilitate excretion
35
Phase 2 metabolism occurs where and uses what enzyme
In the liver uses UGT to facilitate glucuronidation
36
What is the first pass affect?
When drugs are taken orally, they absorb through the liver before entering the blood A high first packed effect will have less active drugs available to exert effects
37
What administering roots bypass first pass effect?
IV, I am, sub, Q, transdermal Otherwise, higher doses are required for oral alternate routes or pro drugs used
38
How does high first pass affect relate to bioavailability?
By availability is the amount in blood for the amount given so if there’s a high first pass rate, then less medication is going into the blood, oral drug may not be worth it
39
Where does most excretion occur?
Kidneys also bio elimination or breastmilk
40
What is clearance in its calculation?
Clearance describes volume of plasma cleared of giving medication overtime can be linear or non-linear CL equals right of elimination of drug divided by plasma drug concentration
41
What does a high clearance mean?
Low plasma concentration
42
Elimination half-life and how it’s determined
Describes the time required for serum concentration on a drug decrease by 1/2 Affected by volume of distribution clearance
43
As volume of distribution increases and clearance decreases, the half life will blank
The half-life will increase because more drug tissues, not blood, longer to get out of body
44
Terminal half-life
The flow process that prolongs to half life as drug penetrate deep peripheral compartment Can occur after prolonged course of medicine
45
Half-life equation
T 1/2 equals 0.693 times volume distribution divided by clearance
46
Steady state
Win rate of drug administration equals the rate of drug elimination – consistent value Reached after five half-life needs to be continuous administration
47
What is study state used for?
Determine patient response in dose regiments
48
Study state changes by what each half life
Concentration changes by 50% after each half-life see larger change at beginning
49
How does the loading dose effect study state
Takes the same time to reach study state just has higher therapeutic concentration reaches it sooner commonly used with antibiotics
50
First order versus zero order elimination
Most drugs follow first order elimination, which is proportional decreases by 50% each time  Zero elimination order is a constant rate by 2.5 units each time drugs don’t have a consistent high life, more likely to produce toxicity these affect the duration of action for drugs
51
What are drugs that follow zero order elimination? Why are they dangerous?
Ethanol – intoxication last longer takes longer to clear Phenytoin  aspirin at High toxic concent
52
First order elimination is blank of drug concentration and half life is blank on initial drug concentration
Dependent of drug concentration  Half life independent on initial drug concentration
53
Zero order elimination is blank of drug concentration and half life is blank on initial drug concentration
Elimination is independent of drug concentration half-life is dependent on initial drug concentration
54
What do medication’s rely on for elimination? How do we assess this?
Rely on kidneys can test glomerular filtration rate (GFR) and creatinine clearance (clcr)
55
What is creatinine clearance important for? What is creatinine
Determining appropriate medication doses with renal impairment creatinine is the product of muscle skeletal breakdown
56
Cockcroft Gault equation for Creatinine Clearance (CrCl) What is considered good/bad?
(IBW in kg) x (140-age) ------------------------------ x (0.85 for females) 72 x (Scr in mg/dL) Normal” CrCl is 90-120 mL/min Bad is <30
57
What is Ideal Body Weight (IBW calculation
IBW Females: 45.5kg + (2.3)(# of inches > 5 ft) • IBW Males: 50kg + (2.3)(# of inches > 5 ft)
58
Medication’s like Ciprofloxacin are cleared by the kidneys so what do you need to do?
Know kidney function, CrCl calculation

Pharmacology (3 decks)

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