Introduction Flashcards

1
Q

Mechanism of action

A

Pharmacodynamics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Type of passive diffusion for large molecules

A

Aqueous diffusion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Type of passive diffusion that is the most important limiting factor for drug permeation

A

Lipid diffusion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Absorption, distribution, metabolism, excretion

A

Pharmacokinetics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Type of antagonist that binds reversibly

A

Competitive antagonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Type of antagonist that binds at the active site or allosteric site

A

Noncompetitive antagonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Type of antagonist that inactivates the agonist by modifying or sequestering it

A

Chemical antagonist (Protamine)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Type of antagonist that either blocks or activates a receptor

A

Physiologic antagonist (adrenergic antagonists)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Measure of the ability of the body to eliminate a drug

A

Clearance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Measure of apparent space in the body available to contain a drug

A

Volume of distribution (Vd)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Type of antagonist that binds to a receptor, competes with, and prevents binding of other molecules

A

Pharmacologic antagonist (Atropine)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Type of agonist that binds at the active site but only produces a partial response

A

Partial agonist (buprenorphine)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Type of transport that requires energy and a carrier; is saturable (low to high)

A

Active transport

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Fractional extent to which a dose of a drug reaches its site of action

A

Bioavailability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Type of drug transport that does not require energy nor a carrier; is non-saturable (high to low)

A

Passive diffusion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

A portion of the drug goes to the portal circulation and is metabolized in the liver resulting to a decreased drug effect before it reaches the systemic circulation

A

First-pass effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Enumerate the CYP inhibitors (decrease in drug metabolism = increase in drug effect)

A

Sodium Valproate, Isoniazid, Cimetidine, Ketoconazole, Fluconazole, Alcohol (acute), Chloramphenicol, Erythromycin, Sulfonamides, Ciprofloxacin, Omeprazole, Metronidazole, Grapefruit juice, Amiodarone, Quinidine (SICKFACES.COM/GAQ)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Type of transport that does not require energy but requires a carrier; is saturable (high to low)

A

Facilitated diffusion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Principal organ in metabolism

A

Liver

23
Q

Enumerate the CYP inducers (increase in drug metabolism = decrease in drug effect)

A

Barbiturates, St. John’s Wort, Carbamazepine, Rifampin, Alcohol (chronic), Phenytoin, Griseofulvin, Phenobarbital, Sulfonylureas (BullShit CRAP GPS)

24
Q

Type of agonist that acts by abrogating the intrinsic activity of the free receptor

A

Inverse agonist

25
Q

Rate and extent of disappearance of a drug from the site of administration and entry into systemic circulation

A

Drug absorption

26
Q

Route of administration that has a 100% bioavailability

A

Intravascular

27
Q

Route of administration that has a less than 100% bioavailability (has a lag phase)

A

Oral

28
Q

The effect where a drug goes into portal circulation and gets metabolized in the liver leading to a decreased drug effect before it reaches systemic circulation

A

First-pass effect

29
Q

A type of preparation that produces a slow, uniformed absorption of the drug for 8 hours or longer

A

Controlled-release preparations (extended-release, sustained-release, prolonged-action)

30
Q

Route of administration that has a direct access to the systemic circulation via SVC (bypasses the liver, protecting it from first-pass effect)

A

Sublingual (Isosorbide dinitrate tablets for angina)

31
Q

Route of administration that has a 50% bioavailability

A

Rectal (Diazepam suppositories for seizures in children)

32
Q

Route of administration used for diagnostic agents

A

Intra-arterial

33
Q

Route of administration to surpass the BBB and blood-CSF barrier

A

Intrathecal

34
Q

Route of administration for non-irritating drugs (has a constant and slow rate of absorption to produce a prolonged effect)

A

Subcutaneous

35
Q

Route of administration where fat composition is a factor in absorption (more fat = less blood vessels = delayed absorption)

A

Intramuscular

36
Q

Route of administration where access to circulation is rapid

A

Inhalation (pulmonary absorption; lungs have a large surface area; salinase for nasal congestion, salbutamol metered-dose inhaler or nebulization for asthma)

37
Q

When 2 (or more) drugs have the same active ingredients, have identical strength or concentration, and are given in the same route of administration

A

Pharmaceutical equivalents

38
Q

Drugs converted into _ _ are more water-soluble and are more readily excreted

A

Inactive metabolites

39
Q

Drugs converted into _ _ have the same effect but of longer duration

A

Active metabolites (Diazepam to Nordiazepam)

40
Q

A compound that has no activity

A

Prodrug (Salicylic acid undergoes acetylation into AcetylSalicylic Acid or Aspirin)

41
Q

Phase I of metabolism

A

Oxidation, reduction, hydrolysis -> addition of a functional group -> drug inactivation

42
Q

Phase II of metabolism

A

Conjugation -> use of phase I by-product -> increased hydrophilicity -> elimination

43
Q

Enzyme system for microsomal metabolism

A

Cytochrome P450 enzyme system (found in the liver, GIT, lungs, kidneys)

44
Q

The time when half of the initial drug’s dose or concentration is reached or decreased

A

Half-life (t1/2)

45
Q

The amount of drug present inside the body

A

Area Under the Curve (AUC)

46
Q

Organ in drug excretion

A

Kidneys (also bile duct, lungs, skin)

47
Q

A constant fraction of the drug is eliminated per unit time and t1/2 is constant (half of the drug is eliminated every x hours)

A

First-order elimination (most drugs follow this)

48
Q

A constant amount of the drug is eliminated per unit time and t1/2 is variable (a specific amount of the drug is eliminated every x hours)

A

Zero-order elimination (ethanol in high blood levels, phenytoin in high doses, salicylates in toxic doses)

49
Q

Refers to the volume of blood cleared of drug per unit time

A

Clearance (Cl) (constant in first-order)

50
Q

The rate when the drug comes in which is equal to the rate the drug goes out (availability rate = elimination rate)

A

Steady state (usually 4-5 half-lives)