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xD2 Pharm Exam 6 > Beardsley Material > Flashcards

Beardsley Material Flashcards

1
Q

High risk patients for drug interactions

A

elderly, young, sick, multiple diseases, multiple drug therapies, renal or liver impairment

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2
Q

What are three general classes of drug-drug interactions?

A
  1. Preadmin
  2. Pharmacokinetic
  3. Pharmacodynamic
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3
Q

What are two characteristics of high risk drugs for interactions?

A
  1. Low (narrow) therapeutic index

2. Recognized enzyme inhibitor or inducer

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4
Q

What are 4 types of pharmacokinetic drug interactions?

A
  1. Drug absorption
  2. Drug displacement (protein binding)
  3. Drug biotransformation (metabolic)
  4. Drug excretion (from cells or body)
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5
Q

What are 5 general mechanisms of drug absorption interactions?

A
  1. Change in GI pH
  2. Drug binding in GI tract
  3. Change in GI flora
  4. Change in GI motility
  5. Malabsorption caused by other drugs
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6
Q

What happens if tetracyclines and quinolone antibiotics are taken with calcium food, vitamins and supplements?

A

Chelate the divalent and trivalent cationsto make acomplex that is poorly absorbed

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7
Q

If you administer Warfarin and NSAIDs together, their competition for protein receptors causes what?

A

More warfarin to be active

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8
Q

If a drug is an enzyme inducer, it will do what to the other drug?

A

Decrease its effects

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9
Q

If a drug is an enyzme inhibitor, it will do what to the other drug?

A

Increase its effects

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10
Q

What do all parts of CYP450 nomenclature mean?

A

Cyp = superfamily/ 3 - family/ A = subfamily / 4 = individual gene

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11
Q

Cytochrome enzyme involved in the greatest number of drug biotransformations

A

CYP3A4

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12
Q

5 CYP enzymes responsible for drug metabolism

A 
CYP2E1
CYP1A2
CYP2C9
CYP2D6
CYP3A4
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13
Q

Where is the cytochrome P450 system located?

A

The lipid bilayer of smooth ER and hepatocytes in liver and enterocytes of small intestine

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14
Q

What CYP450 enzyme will ciprofloxacin inhibit, and what drugs can then potentiate?

A

CYP1A2, tacrine, theophylline, imipramine, flu

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15
Q

Which drug would be potentiated if CYP1A2 was inhibited by erythromycin?

A

Theophylline

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16
Q

Grapefruit juice inhibits which CYP450 enzyme?

A

CYP34A

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17
Q

2 Drugs metabolized by CYP2D6 where the inhibition of the enzyme decreases the drugs’ net effects

A
  1. Tramadol

2. Codeine

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18
Q

What are 2 kinds of general drug excretion interactions?

A
  1. One drug impairs the renal excretion of another

2. Affects on permeability of the glycoprotein

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19
Q

What occurs if thiazide diuretics are given to someone on Lithium?

A

Will cause lithium to be retained and accumulated

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20
Q

Which CYP 450 is affected by the same drugs that PGP is?

A

CYP 34A

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21
Q

What are 2 possible specific interactions that opiates can have with local anesthetics?

A
  1. Opiate induced respiratory acidosis

2. Elevation arterial carbon dioxide tensions leading to convlusions

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22
Q

Drugs to be aware of when administering prilocaine to minimize the induction of methemoglobinemia

A
  1. Nitroglycerine
  2. Dapsone
  3. Solfonamides
  4. Phenacetin
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23
Q

Possible side effect of giving patient epinephrine while on a beta blocker

A

Their B2 vasodilation is blocked and EPI stimulates the A1 vasoconstrictors unopposed causing hypertension

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24
Q

What is a concern for a patient taking NSAIDS and SSRIs?

A

Increased bleeding risk due to decreased platelet aggregation

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25
Q

Is the NSAID/SSRI interaction additive?

A

No it is synergistic

26
Q

How are local anesthetics different from general anesthetics?

A

Local applied to target site and block pain by depressing peripheral nerves and their axonal conduction while general administered sytemically and depresse CNS and block pain by stopping transmission across synapses

27
Q

What are 8 properties of ideal local anesthetic?

A
  1. Nonirritating
  2. No permanent alteration of nerve
  3. Low systemic toxicity
  4. Effective topically or by injection
  5. Short onset time
  6. Appropriate duration of action
  7. Non-allergenic
  8. Sufficiently potent
28
Q

What are 3 domains of a local anesthetic?

A
  1. Lipophilic
  2. Alkyl link
  3. Hydrophilic
29
Q

What domain determines the anesthetic classification, its metabolism and its toxicity?

A

The alkyl group (amide or ester)

30
Q

What is the primary determinant of local anesthetic potency?

A

Lipid solubility (the more lipid soluble, the more potent)

31
Q

What is the primary determinant of duration of action of local anesthetics?

A

Protein binding (great the protein binding, the longer the duration of action)

32
Q

What are the 2 most influential determinants of onset of action of local anesthetics?

A

Neuron Fiber size and pKa of local

33
Q

What is the most common site of action for local anesthetics?

A

Bind receptor in the sodium channel to block sodium influx

34
Q

What is pKa?

A

The measure of inherent acidity of alkalinty of a molecule. it is the pH at which the cation and the base species are equal

35
Q

Only what form of the anesthetic binds the receptor?

A

Ionized form (cation = positively charged)

36
Q

Which fibers are generally affected by local first: pain or motor?

A

Pain because sensory fibers normally are smaller than motor

37
Q

What happens to local pH in inflamed tissue and its affect on the speed of onset for local?

A

Tissue pH decreases. This causes more cations of the local (i.e. less base) which increases the amount of time it takes to diffuse, and takes longer for onset

38
Q

How are ester anesthetics (e.g. Procaine) metabolized?

A

In blood by pseudocholinesterase

39
Q

How are amide anesthetics metabolized?

A

Liver

40
Q

Which class of local anesthetic would more likely produce a hypersensitivity reaction?

A

Ester

41
Q

What metabolite is the likely cause of the hypersensitivity reaction?

A

p-aminobenzoic acid (PABA)

42
Q

What percentage of patient is likely to have a hypersensitivity reaction to local?

A

less than 1 percent

43
Q

What is the major organ of excretion for both ester and amide locals?

A

Kidneys: urine and feces as various metabolites

44
Q

What are 5 Amide local anesthetics

A 
(First part has an I in it)
Lidocaine
Etidocaine
Mepivicaine
Bupivicaine
Prilocaine
45
Q

What are 5 ester local anesthetics?

A 
(No I other than the "caine" part)
Procaine
Benzocaine
Propoxycaine
Tetracaine
Cocaine
46
Q

Where do tetrodotoxin and Saxitoxin (local anesthetic-like poisons) bind?

A

Irreversibly bind external membrane of nerve near the sodium channel

47
Q

What are 7 general factors influencing Local Anesthetic Toxicity?

A
  1. Drug Type
  2. Concentration
  3. Route of administration
  4. Rate of injection
  5. Vascularity
  6. Patient’s weight
  7. Rate of metabolism and excretion
48
Q

What is methemoglobinemia?

A

Drug-induced cyanosis caused by a metabolite oxidizing Ferrous (Fe+++) oxygen-carrying hemoglobin to Ferric (Fe+++) non oxygen-carrying hemoglobing (methemoglobin)

49
Q

What is the majory local anesthetic that can cause methemoglobinemia and the metabolite that causes it?

A

Prilocaine, O-toluidine

50
Q

What is the treatment for methemoglobinemia?

A

Slow IV administration of methylene blue which reduces methemoglobin to hemoglobin by acting as an electron receptor

51
Q

What are the components of oraqix?

A

1:1 Lidocaine to Prilocaine (2.5% Lidocaine, 2.5% Prilocaine, 92% water, 3% inert stabilizers)

52
Q

What are 2 primary indications for Bupivicaine?

A
  1. Lengthy dental procedures

2. Post-operative pain management (longer onset but also longer duration)

53
Q

What is the general idea of an isomer approach?

A

The (+) and (-) isomers of a molecule may have different properties though they have the same number and kind of atoms. One isomer can be isolated and exploited to advantage.

54
Q

What is an example of the isomer approach?

A

(-) istom of bupivicaine is less cardiotoxic than racemic bupivicaine. Therefore, market (-) isomer as Ropivicaine.

55
Q

What is the term for a mix between a local anesthetic with an absorbable iodized fatty acid (used to use peanut oil)?

A

Iophendylates Depot Prep

56
Q

What is the term for a mix between a local anesthetic with hydrophobic triglycerides and encapsulating in a layer of phospholipids?

A

Lipospheres Depot Prep

57
Q

What is the term for a mix between local anesthetic, a lipid, and an emulsifier sonicated in a liquid producing micelles of lipid bilayer called liposomes, containing local anesthetic and water within their cavity?

A

Liposome depot prep

58
Q

Tetraethylammonium (TEA) is what?

A

Selective potassium ion channel blocker

59
Q

What are 2 biotoxin local anesthetics?

A
  1. Tetrodotoxin

2. Saxitotoxin

60
Q

Where do tetrodotoxin and saxitoxin bind and what do they block?

A

Bine to external membrane, irreversibly block sodium channels

61
Q

What is the positive aspect of biotoxins?

A

Selective for sodium channels, and selective to block neural over cardiac tissue

xD2 Pharm Exam 6 (2 decks)

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