Basic Principles of Pharmacology Flashcards

1
Q

Pharmacokinetics

A

What the body does to the drugs

A-D-M-E

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2
Q

Pharmacokdnamics

A

What the drugs do to the body

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3
Q

ENTERAL includes

A

Oral (PO)
Sublingual (SL)
Buccal
Rectal (BP)

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4
Q

PARENTERAL includes

A

Inhalation

Injection: IV, IM, SQ

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5
Q

TOPICAL includes

A

Transdermal
Nasal spray
Ointment (gold standard)
Increase skin hydration increases absorption

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6
Q

Relationship between first pas effect and bioavailability

A

The greater the first-pass effect, the less drug is available in the circulation thus the lower the bioavailability –> lower therapeutic effect and lower risk of toxicity

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7
Q

Bioavailability

A

the fraction or % of a drug that reaches systemic circulation

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8
Q

Why do we need to increase an oral dose to provide the same effect as an inhaled dose?

A

Oral dose goes through the first-pass effect via liver (more so than lung) thus more systemic circulation –> more systemic bioavailability

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9
Q

Substrates

A

the drug that is being metabolized by other drugs/enzymes

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10
Q

Inhibitors

A

a drug/enzyme that SLOW DOWN the metabolism of a substrate – thus less of that drug/substrate is being excreted –> more remain in circulation –> greater therapeutic effect or toxicity d/t MORE systemic bioavailability

Ex - Cimitidine is an inhibitor to Metformin –> slow down metabolism of Metformin –> more serum metformin –> increase metformin’s effect –> risk of hypoglycemia

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11
Q

Common INHIBITORS

A

G-PACMAN

G = grapefruit
P = Protease inhibitors
A = Azole antifungals 
C = Cimetidine
M = Macrolides (except Azithromycin)
A = Amioadarone 
N = Non-DHP CCBS (Diltiazem, Verapamil)
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12
Q

Common INDUCERS

A

P-CRABS

P = Phenytoin
C = Carbamazepine 
R = Rifampin
A = Alcohol (chronic) 
Barbiturates 
S = St. John's Wort
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13
Q

Inducers

A

Speeds Up metabolism of a substrate/drug
–> generally decrease drug effects

Ex:
-Prednisone is an inducer to Carbamazepine –> reduces serum level of carbamazepine which would leave pts at a higher risk for unanticipated seizures

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14
Q

Narrow Therapeutic Index Drugs (NTI)

A

Examples

  • Anticoagulants (warfarin, heparins)
  • Aminoglycoside antibiotics (Gentamycin, Tobramycin)
  • Digoxin
  • Hypoglycemic agents
  • Levothyroxine sodium
  • Lithium
  • Phenytoin
  • Theophylline
  • TCA
  • Valproic acid
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15
Q

Onset of drug action

A

time between administration and first sign of drug effect

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16
Q

Peak of drug action

A

-Point at which amount of drug being absorbed and distributed is equal to amount being metabolized and excreted.

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17
Q

Duration of drug action

A

Continued entry of drug into body with levels above minimum effective concentration

18
Q

Termination of drug action

A

when drugs stop”working”

19
Q

Therapeutic Range

A

equals MTC - MEC

20
Q

MTC

A

amount to cause toxicity

21
Q

MEC

A

Lowest concentration needed for drugs to work

22
Q

Drug Half-Life

A

Time required for the amount of drug in the body to decrease by 50%
-determine the dosing interval (drugs with short half-life, dosing interval must be correspondingly short. If a long dosing interval were used, drug levels would fall below MEC between doses, and therapeutic effects would be lost)

23
Q

Ligand

A

a molecule that fit into the active site of receptors –> activate those receptors –> propagate signal pathways

24
Q

Agonists

A

Molecules that ACTIVATE receptors

  • Drugs that mimics native ligand and stimulate the typical physiological response at the body natural receptors
  • These drugs have both affinity (allow agonist to bind to receptors) and high intrinsic activity (allows the bound agonist to activate the receptor function)
25
Q

Antagonists

A

Produce pharmacologic effects by preventing the activation of receptors by agonists
-Its effect is determine by the amount of agonist that are present – If there is no agonist present, administration of an antagonist will have no observable effect

  • Have virtually no effects of their own on receptor function
  • These drugs have affinity for a receptor but no intrinsic activity
26
Q

Potency of a drug

A

Strength of a drug at a particular dosage

  • the affinity of a drug for a receptor
  • the amount of drugs require to produce 50% of maximal effect that drug can effect
27
Q

Efficacy

A

Maximum effect that can be achieve by a drug such that after this is reach, no higher dosage can produce any further effect

28
Q

True/False: Two drugs can have the same efficacy but different potency

A

True

29
Q

Pregnancy related Physiologic Changes:

CARDIOVASCULAR

A

Cardio

  • increased BV and CO and
  • decreased systemic vascular resistance
30
Q

Pregnancy related Physiologic Changes:

GI

A
  • Increased pH of intestinal secretion
  • Delayed gastric emptying
  • Decreased gastric acid secretions
  • Decreased intestinal motility
31
Q

Pregnancy related Physiologic Changes:

RENAL

A
  • Increased renal blood flow

- Increase GFR

32
Q

Pregnancy related Physiologic Changes:

GYN/GU

A

-Increase uterine blood flow

33
Q

Pregnancy - ABSORPTION

A

GI:

  • Drugs stay in guts longer → delayed gastric emptying = delayed absorption
  • Reduced gastric acid secretion → decreased absorption of certain medications
  • N/V pregnancy → decreased absorption

Lungs:
-increased absorption of inhaled medications d/t increased blood flow to the lungs

Transdermal:
- increased absorption d/t ↑ peripheral vasodilation and ↑ in total body water (TBW)

34
Q

Pregnancy - DISTRIBUTION

A

1) Water soluble drugs:
- Increase in TBW of 8L during pregnancy = dilution effect → decreased drug concentrations

2) Decreased levels of albumin
- Drugs that are highly bound to albumin, in this case, they will have higher serum concentrations during pregnancy

35
Q

Pregnancy - ELIMINATION

A
  • Increased progesterone stimulates hepatic enzyme systems → increasing elimination of hepatically eliminated medications
  • Increased GFR → increased elimination through the kidneys
36
Q

Pregnancy

Drugs that are more likely to cross the placenta

A
  • Lipids soluble drugs
  • Low molecular weight drugs
  • Free drug (not bound to protein) - not that in pregnancy, there is a lower albumin level
37
Q

Most important determinant of teratogenicity is ____

A

Timing of the exposure , which can be during, before , or after pregnancy

38
Q

Drugs to Avoid in First Trimester

A
Beta blockers
Benzos
Thiazides
ACE-I/ARBs
Anti-epileptics
Estrogen
Warfarin
Topical retinoids
Methotrexate
Lithium 
Cytotoxic drugs
39
Q

Pharmacokinetics & Aging: ABSORPTION

A
  • Decreased in small-bowel surface area -
  • Decreased in GI mobility
  • Increased in pH
40
Q

Pharmacokinetics & Aging: DISTRIBUTION

A
  • Increased body fat –> prolonged action of fat soluble drugs
  • Decreased total body water –> Higher concentration of water-soluble drugs
  • Decreased albumin –> higher concentration of active drugs (unbound/free drugs)
41
Q

Pharmacokinetics & Aging: METOLISM

A

-Decreased hepatic metabolism –> Higher serum concentration

42
Q

Pharmacokinetics & Aging: ELIMINATION

A

-Decreased renal drug clearance, Decrease GFR (even without renal diseases)