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Pharm 2 > Lecture 1/23/23 > Flashcards

Lecture 1/23/23 Flashcards

1
Q

Drug effect relates to

A

number of bound receptors

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2
Q

Ion bonding

A

electrovalent => oppositely charged ions

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3
Q

Hydrogen Bonding

A

to a very electronegative atom

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4
Q

Van der Waals interaction

A

the sum of attractive or repulsive forces; creates orbital shift

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5
Q

Competitive antagonism shifts the dose response sure to the __________

A

Right, more drug is needed to get the same response

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6
Q

What are some examples of how the number of receptors are not static

A
  • Tolerance [tachyphylaxis => rapid tolerance => ephedrine]
  • Albuterol treatment for asthma => downregulation of receptors due to repetition
  • Pheochromocytoma => decreased β receptors in response to catecholamines
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7
Q

What types of receptors (classified by location) do we have?
What is a drug that binds to each of those types of receptors?

A

Lipid bilayer:
* Common for anesthesia drugs
* Membrane bound
* Opioids, bzd [benzos], b-blockers, catecholamines, NMBD

Intracellular proteins:
* Insulin, steroids, milrinone

Circulating proteins:
* Anticoagulants
* Age decreases proteins
* => more unbound drug => free drug
* => more anticoagulant [drug] effects
* => Bleeding

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8
Q

Central compartment

A

What dilutes the drug in the first minute following injection
Venous blood in arm, inferior vena cava, right heart, pulmonary vessels, lungs, left heart, aorta
movement based on CO and vessel-rich groups

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9
Q

Plasma proteins bind most drugs in 2 categories

A
  • Acidic drugs primarily to albumin
  • Alkalotic drugs primarily to a1-acid glycoprotein
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10
Q

Only ________ can determine the concentration available to the receptor (potency)

A

free drug

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11
Q

What conditions cause decreased proteins?

A

Age, Hepatic disease, Renal disease, Pregnancy, Burns, sepsis

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12
Q

If the normal free fraction of the drug is 5% but this. the patient has lost 50% of their plasma proteins what free drug concentration will this pt have?

A

10%

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13
Q

If a drug is poorly protein bound and lipophilic if will have a __________ Vd

A

high, ie Thiopental

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14
Q

What is phase 1 in metabolism

A
  • Increase polarity and prepare for Phase II reactions
  • Oxidation
  • Reduction
  • Hydrolysis
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15
Q

What is phase 2 in metabolism

A
  • Covalently link with a highly polar molecule to become water soluble
  • Conjugation
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16
Q

how many isoform of CYP450

A

10

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17
Q

CYP450 participate in what phase of metabolism and more specifically what subcategory

A

Phase 1, oxidation and reduction

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18
Q

most common CYP enzyme

A
  • CYP3A4:
  • Most common for anesthetic drugs
  • Up to 60% of CYP450 activity
  • Metabolizes > 50% of drugs: opioids, BZP, LA, immunosuppressants, antihistamines
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19
Q

Phenobarbital ___________ enzymes => _____________ metabolism of drugs, causing __________effectivness of other drugs

A

Induces, increases, decreased

20
Q

What is a well-known CYP inhibitor and what effect does it have on other drugs?

A

Grapefruit juice => increases the concentration of drugs/toxicity levels by inhibiting their metabolism
* More drug left around, might cause OD

21
Q

Rate of drug metabolism

A
  • Rate is proportional to the concentration
  • More drug/more clearance
    R = Q (C inflow – C outflow)
    Q= flow so low CO will affect Rare of metabolism
22
Q

Three Methods of Renal Clearance

A

Glomerular filtration
* GFR and amount of protein bound drug controls amount of drug entering tubule

Active tubular secretion
* From peritubular capillaries
* Active transport process
* PCNs

Passive tubular reabsorption
* Increased if drug lipid soluble
* ie. thiopental
* Almost zero for water-soluble drugs => excreted in urine

23
Q

Elimination ½ Time

A
  • Time necessary to eliminate 50% of the drug from PLASMA after a bolus dose. Measured by peak and troughs and random blood draws.
24
Q

What is Context Sensitive Half-Time

A
  • Time to a 50% decrease after infusion discontinued
  • Assumes a constant concentration
  • Roughly relates to ½ life
  • Increases the longer the infusion increases
  • Accumulation in peripheral tissues
  • Propofolfalls to 50% quickly even with long infusion times when you discontinue the drug
  • Fentanyl takes a little longer with a longer infusion
  • Need to stop early to get breathing back in time for the patient to wake up

https://www.youtube.com/watch?v=Asf97N69rME&ab_channel=MikeLoughren

25
Q

Are local anesthetics weak bases or acids

A

bases

26
Q

Acids are ionized in __________ pH

A

Alkaline pH

27
Q

Bases are ionized at __________pH

A

Acidic

28
Q

Non-ionized => ____________ and will cross cell membranes

A

lipid soluble

29
Q

To be renal excreted you want the drug to be _________.

A

ionized

30
Q

How can you tell if a weak acid will be ionized in a given pH

A

pH - pK = …
Aaaaacids pK go AAAfter pH
if the number is positive then it will be ionized
if the number is negative it will be unionized

31
Q

How can you tell a weak base will be ionized in a given pH?

A

pK - pH = …..
Bbbbbbases pK go Before pH
if the number is positive then it will be ionized
if the number is negative it will be unionized

32
Q

What is ion trapping?

A

When a drug enters an isolated environment and becomes ionized based on its surroundings and then can not get back to its original environment.
ie: fetal ion trapping

ie: urine ion trapping. Ion trapping alters the urine pH to inhibit the reabsorption of toxins across the renal tubular membranes. The principle behind this approach is to “trap” the toxin in its ionized form in the urine where it can be excreted.

33
Q

the more acidic the environment the _________ a local anesthetic will work

A

Less. weak Base
* In ischemic tissue 8.0 (lido pK) – 6.6 (pH) = +1.4 (very ionized)

34
Q

What is pharmacodynamics and what is a drug that has different pharmacodynamics at different concentrations

A

“What the drug does to the body,” Dopamine

35
Q

What is potency?

A

Concentration vs response, Less drug with more effect = more potent

36
Q

What is efficacy?

A

The ability of a drug to produce a clinical effect
* “How much of the effect can I get?”

37
Q

Why is it important to understand the time to drug effect?

A
  • Lag time between administration (plasma concentration) and effect
  • So we don’t re-dose inappropriately
    ie: fentanil has a 5 min delay from when you administer in plasma to when we see a tissue effect. Alfentanil has almost an immediate effect and no lag between administration and effect
38
Q

Therapeutic index

A

LD50 / ED50
* ED50 : Dose required to produce effect in 50% of patients
* LD50 : Dose required to produce death in 50% of patients

The Wider the ratio the safer the medication
* Less side effects
* Gives area for caution

39
Q

Chiral compounds

A
  • Molecules with asymmetric centers [Center carbon]
  • Usually related to way carbon molecules are bonded
40
Q

Stereochemistry

A

How drug molecules are structured in 3 dimensions

41
Q

What is an enantiomer?

A
  • Chemically identical
  • Mirror images
  • Can’t be superimposed
  • Can’t be placed on top of each other
42
Q

Enantiomers that rotate light to the right are called

A

Dextrorotary
Rectur

43
Q

Enantiomers that rotate light to the Left are called

A

Levorotatary
Sinister

44
Q

What is a 50/50 mixture called?

A

Racemic,
each enantiomer can exibit different ADME
* One enantiomer is active => other inactive or side effects
* Albuterol vs. Xopenex
* Xopenex has the same effect as albuterol, but no tachycardia
* 1/3 of drugs are racemic => should decrease in future

45
Q

the ____ enantiomer of ketamine more potent with less delirium

A

S- enantiomer

46
Q
  • Cisatracurium, the isomer of atracurium, lacks _______ effects
A

histamine
* Histamine => inflammation, vasodilation => hypotension

Pharm 2 (8 decks)

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