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NDEB- Sayuri > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What’s pharmacokinetics?

A

Body does to the drug

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2
Q

Pharmacokinetics processes

A

Absorption
Distribution
Metabolism
Excretion

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3
Q

Routes of drug admin

A

Enteral
Parenteral
Inhalation
topical
Transdermal - patch, onset 15min. I.e: Fentanyl patch

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4
Q

Types of enteral admin

A

Buccal/ sublingual
Oral - slowest. Absorbed best in duodenum
Rectal

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5
Q

Types of parental admin

A

IV - fastest. Only one 100% bioavailability
IM - Deepest. 5min. Site: upper lateral quadrant of the gluteal muscle
SC - 15min

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6
Q

What’s bioavailability

A

Amount of drug that reaches site of action

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7
Q

Lipophilic & acidic drugs are easier to absorb. TRUE/FALSE

A

True.

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8
Q

What’s “hepatic 1st pass effect”?

A

Drug gets metabolized in the liver - through the Hepatic portal syst- an amount will become inactive

Only PO and rectal will pass this pathway. I.e: Pen G- completely inactive if PO - best route: IV/IM

> H < bioavailability

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9
Q

What are the absorption mechanisms?

A

Passive transfer -no energy
Active transport

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10
Q

Types of passive transfer

A

Simple passive diffusion - gradient. Hydrophobic/Lipophilic/non-ionized
Filtration - Hydrophilic/Lipophobic/ionized
Facilitated diffusion - carrier-based

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11
Q

Types of active transport

A

Needs ATP
Against gradient
I.e: Glucose
Needs carrier

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12
Q

Osmosis

A

Similar to filtration

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13
Q

lipid-soluble compounds get through BBB? T/F

A

True
Non-ionized drugs have higher lipid solubility
I.e: Thiopental, ultra-short barbiturate

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14
Q

Factors affecting distribution

A

Rate of blood flow

Protein binding - albumin (plasma protein) highest ability to bind to drugs - < distribution

Permeability - leaky capillary >distribution. In BBB <distribution

Gastric emptying time

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15
Q

> blood flow >concentration of a drug?
T/F

A

True.
Most important factor
I.e: brain, kidneys, liver

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16
Q

What’s bio transformation of a drug?

A

Lipophilic to lipophobic
Active to inactive
It gets easily excreted by kidneys

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17
Q

Types of biotransformation

A

Inactivation

Formation of active metabolite from active drug. I.e: Digitoxin - Digoxin

Activation of inactive drug - Prodrugs. I.e: Levodopa (inactive) - Dopamine (active)

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18
Q

Where does Phase I rx occurs and kind of rx?

A

Liver - Hepatocytes - CYP450 (Cytochromes) system
Oxidation, reduction, hydrolysis

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19
Q

Which cytochrome causes genetic polymorphism

A

CYP2D6
Rapid metabolizer - < therapeutic effect. I.e: Codeine
Slow metabolizer - > toxicity

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20
Q

Examples of CYP450 inducers

A

Rifampicin
Phenytoin
Carbamazepine
Chronic alcohol

If taken w/Warfarin - > risk of clotting

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21
Q

Examples of CYP450 inhibitors

A

Grapefruit juice
Ketoconazole (all azoles)
Cimetidine (heartburn)
Acute alcohol

If taken w/Warfarin - risk of bleeding

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22
Q

Where does Phase II rx occurs and kind of rx?

A

Liver and kidney
Rx: Conjugation rx like:
Glucuronidation - glucuronide
Acetylation
Sulfation

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23
Q

Sites for drug of elimination

A

Kidneys and liver
Also lungs - Halothane, N2O , bile - cat ionic, anionic, steroid-like , feces

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24
Q

Factors affecting renal excretion

A

GFR - plasma protein bound drug isn’t filtered

Kidney tubular reabsorption - pH. I.e: ASA (weak acid) easily reabsorbed in acid conditions

Active secretion
Changes: [plasma protein/binding]
Blood flow
#functional nephrons, renal disease
Volume of distribution

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25
Q

Types of drug clearance/elimination

A

Zero-order
1st-order

26
Q

How is the elimination in each type?
(Zero/1st order)

A

Zero order - linear. I.e: alcohol, phenytoin, ASA (toxic)

1st order - exponential. Most drugs

27
Q

What’s a drug half life and how many does it take to eliminate it from the body

A

Time required [drug] to decrease by 50%

4-5 half lives

28
Q

What’s therapeutic index

A

How safe a drug is
Comparison Therapeutic & toxic effect
Lethal dose for 50% of animals to the effective dose for 50% of animals

29
Q

Formula for Therapeutic index

A

Ti = LD50 / ED50

LD - lethal dose
ED - effective dose

30
Q

What’s the therapeutic window

A

Range Desired/ adverse response
Narrow therapeutic window >monitoring >risk of side effects

31
Q

What are the intrinsic activities in pharmacodynamics

A

Agonist
Antagonist
Agonist-antagonist

32
Q

What’s pharmacodynamics?

A

What the drug does to the body

33
Q

Types of Agonist intrinsic activities

A

Full Agonist - full response

Partial Agonist - partial response

34
Q

What’s an agonist drug? And examples

A

Drug bonds yo receptor and mímica effect of agent/neurotransmitter

NE, EPi, Ventolin, Albuterol

35
Q

What’s an antagonist drug? Examples

A

Drug binds to receptor and prevents effect to happen

Atropine, Benadryl

36
Q

Type of antagonist

A

Competitive - binds are weak. >agonist = response

Non-competitive - binds too strong. > agonist = No response

37
Q

What’s an agonist-antagonist

A

Acts as both. I.e: Opiods

38
Q

What’s efficacy

A

receptors for max response

39
Q

What affects the efficacy of a drug?

A

Affinity - how strong drug binds to receptor

Intrinsic activity - how strong it can produce desire effect

Drug w/both has high efficacy

40
Q

What’s potency?

A

Strength

41
Q

Important factors determining appropriate dosage of a drug?

A

MH
Age
Weight

42
Q

<EC50>Potency >Affinity
T/F
</EC50>

A

True

43
Q

Drug effects?

A

Additive - combination 2 drugs = No enhancement

Cumulative - >drug = > [drug] achieved

Synergistic - combination 2 drugs = > effect

44
Q

Drugs adverse rx

A

Toxicity- excessive dosage of drug for pt

Allergy - immune rx

Side effect - rx within therapeutic window

Idiosyncratic- unusual, unpredictable rx

Teratogenicity- fetal abnormalities

45
Q

Drug abuse

A

Can result in addiction

46
Q

Tolerance

A

Chronic response
>dose <response/effect

47
Q

Physical/psychological dependence

A

Physical - continued use of drug to avoid withdrawals

Psychological - repeated use of a drug w/o increase dosage

48
Q

Perception of acute and chronic pain involves the dame regions of the brain (CNS) T/F

A

True

49
Q

Dimensions of pain

A

Sensory - location, intensity, quality

Affective - emotions

50
Q

Categories of pain

A

Somatic - periodontal, alveolar

Visceral - pulpal

51
Q

Criteria when selecting analgesic

A

Severity of pain
Age
Current meds
Pregnancy

52
Q

Which intensity of pain rx Acetaminophen

A

Mild- mod

53
Q

Mechanism of action acetaminophen

A

Inhibits CNS cyclooxygenase

54
Q

Action of acetaminophen

A

Analgesic
Antipyretic

55
Q

Acetaminophen antidote

A

NAC - N-acetylcysteine

56
Q

Reason acetaminophen is rx to pt w/ hx ulcers and bleeding disorders

A

Doesn’t affect inflammatory response
Platelets function
Coagulation pathway

57
Q

Max dose for adult and kids /day

A

Adult - 4gr/day
* in alcoholics 2gr/day
Kids - 2.6gr/day (75mg/kg)

58
Q

What condition can increase risk of hepatotoxicity and lead to renal toxicity

A

Pt w/liver dysfunction (cirrhosis, chronic alcoholism)

Is not a contraindication is this pt

59
Q

Contraindications of Acetaminophen

A

Allergy

Relative contraindications:
- hepatic/renal dysfunction
- alcohol abuse
- warfarin

60
Q

Side effects of Acetaminophen

A

Headache
Sweating
Nausea/vomiting
Rash
Abdominal pan
Dark urine

NDEB- Sayuri (3 decks)

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