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Pharmacology Flashcards

1
Q

Dobutamine, Denopamine, Dopamine, Epinephrine, and Isoproterenol are examples of which drug class?

A

Beta 1 receptor (ADRB1) agonists

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2
Q

Atenolol, Metoprolol, Bisoprolol are examples of which drug class?

A

Beta 1 receptor (ADRB1) antagonists. Commonly known as ‘beta blockers’

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3
Q

Is isoproterenol a beta 1 (ADRB1) or beta 2 (ADRB2) agonist?

A

Both. Isoproterenol is a non-selective beta-agonist which stimulates both receptors.

Beta 1 stimulation = increased heart rate and contractile force
Beta 2 stimulation = bronchodilation and vasodilation

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4
Q

Glyceryl Trinitrate
(Class, Use, Mechanism)

A

Class: Nitrovasodilator
Use: Angina, Heart Failure

Mechanism: GTN is converted to nitric oxide in the body. Nitric oxide dilates vessels. Dilated veins reduce preload and dilated arteries reduce afterload. Both actions decrease the hearts oxygen demand.

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5
Q

What are the main precautions when prescribing benzodiazepines to elderly patients? (Diazepam, Lorazepam…)

A

Benzodiazepines increase the risk of falls and impair cognitive function.

*Benzodiazepines are positive allosteric modulators of GABA-A receptors. They enhance GABA’s inhibitory effects.

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6
Q

What is the primary function of glucocorticoids?

A

Cortisol agonists.

Glucocorticoids regulate metabolism and suppress inflammation. Glucocorticoid receptors are located in the cytoplasm of most cells.

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7
Q

Triamcinolone acetonide (Kenalog)
(class, use, mechanism)

A

Class: Glucocorticoid (corticosteroid)

Use: Dermatology, Rheumatology, Allergies

Mechanism: Binds to intracellular glucocorticoid receptors. Enters nucleus. Alters gene transcription. Anti-inflammatory and immunosuppressive effects generated

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8
Q

Lidocaine
(class, use, mechanism)

A

Class: local anaesthetic

Use: Topical anaesthetic for skin procedures. Rapid onset (1-5 mins), intermediate duration (30-60 mins).

Mechanism: Blocks voltage gated Na+ channels, preventing nerve impulse transmission.

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9
Q

Benzocaine
(Class, use, mechanism)

A

Class: local anaesthetic

Use: Topical anaesthetic for mouth ulcers, sore throat, and minor burns. Rapid onset (seconds), short duration (10-15 mins).

Mechanism: Blocks voltage gated Na+ channels, preventing nerve impulse transmission.

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10
Q

When would you use Benzocaine instead of Lidocaine?

A

Both are rapid onset local anaesthetics. Benzoocaine has quicker onset (seconds / minutes) and shorter duration (15m / 30m).

Benzocaine also remains localised with minimal systemic absorption. Lidocaine is therefore better for prolonged anaesthesia.

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11
Q

What are the 8 main classes of antibiotics?

A

‘Antibiotics Can Protect The Queens Men Servants & Guards’

Aminoglycosides
Cephalosporins
Penicillins
Tetracyclines
Quinolones / Fluoroquinolones
Macrolides
Sulfonamides
Glycopeptides

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12
Q

Aminoglycosides
A) mechanism of action?
B) selective toxicity?
C) Other information

A

A) Inhibits protein synthesis. Bactericidal

B) Binds to the 30s ribosomal subunit. Humans (40S & 60S), Bacteria (30S & 50S)

C) Enters bacterial cells via oxygen-dependent active transport. Ineffective against anaerobes and human cells (which lack this mechanism). Mostly gram- effects

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13
Q

Cephalosporins:
A) mechanism of action?
B) selective toxicity?
C) Other information

A

A) Inhibits bacterial wall synthesis. Bactericidal

B) Only bacteria have peptidoglycan cell walls, so human cells are not affected

C) Spectrum broadens with each generation (1-5). Early generations mainly gram+

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14
Q

Penicillins:
A) mechanism of action?
B) selective toxicity?
C) Other information

A

A) Inhibits bacterial cell wall synthesis. Bactericidal.

B) Only bacteria have peptidoglycan cell walls, so human cells are not affected

C) Mainly gram+ effects. Later generations able to tackle gram-

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15
Q

What is cotinine?

A

Cotinine is the primary metabolite of nicotine.

Cotinine is inert and lasts longer in systemic circulation than nicotine, making it a good biomarker for tobacco use.

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16
Q

What is the primary metabolite of caffeine?

A

Paraxanthine (84% of metabolites). Central nervous system stimulant. Responsible for nootropic effects

*Theobromine and Theophylline are the other main metabolites, which conference vasodilatory, bronchodilatory, and diuretic effects.

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17
Q

What is the primary metabolite of ethanol?

A

Acetaldehyde.

A toxic substance and known carcinogen. Further metabolised into acetate and then water and CO2

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18
Q

Tetracyclines:
A) mechanism of action?
B) selective toxicity?
C) Other information

A

A) Inhibits protein synthesis. Bacteriostatic

B) Binds to the 30s ribosomal subunit. Humans (40S & 60S), Bacteria (30S & 50S)

C) Tetracyclines have good tissue penetration (particularly Doxycycline)

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19
Q

In terms of incidence and severity combined, which two antibacterial classes have the greatest side effect risk profile?

A

Sulfonamides:
Frequent hypersensitivity reactions. Bone marrow suppression and hyperkalemia risk.

Fluoroquinolones:
Tendinopathy, CNS toxicity, C
difficile risk

*This is a generic statement, as individual drugs and class subtypes will have different effects. Newer generations of certain classes may mitigate side effects. In general, these two classes have the greatest risk profile

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20
Q

What is the difference in chemical structure between quinolones and fluoroquinolones?

A

Quinolones = original antibiotic compound. No fluorine atom

Fluoroquinolones = quinolone core, plus a fluorine atom

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21
Q

Which antibiotic class has a broader spectrum of activity?

Quinolones, Fluoroquinolones, Vancomycin

A
  1. Fluoroquinolones
    Evolution of quinolones. Broad spectrum. High cell penetration and bacterial DNA binding.
  2. Quinolones
    Earlier antibiotic (1962). Narrow spectrum (mainly gram- urinary pathogens). Largely obsolete class.
  3. Vancomycin
    Not a drug class. Narrow spectrum bactericidal antibiotic. Used primarily for serious Staph. Infections
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22
Q

Quinolones / Fluoroquinolones:
A) mechanism of action?
B) selective toxicity?
C) Other information

A

A) Inhibits topoisomerases, blocking DNA replication. Bacteriocidal

B) Human topoisomerases are structurally different

C) Very broad spectrum. High bacterial penetrance. Risk of tendinopathy present.

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23
Q

Macrolides:
A) mechanism of action?
B) selective toxicity?
C) Other information

A

A) Inhibits protein synthesis. Bacteriostatic

B) Binds to the 50s ribosomal subunit. Humans (40S & 60S), Bacteria (30S & 50S)

C) Gram+ effects (large molecular size)

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24
Q

What are the 4 beta lactams?

A

‘Papal Clothing May Chafe’

Penicillins (Originally G+)
Cephalosporins (Originally G+)
Monobactams (G-)
Carbapenems (Very broad)

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25
Sulfonamides: A) mechanism of action? B) selective toxicity? C) Other information
A) Inhibits enzymatic folate synthesis. Bacteriostatic B) Humans obtain folate from diet, so do not have the enzyme for production C) Broad spectrum. Highest risk of side effects (common and relatively severe)
26
Glycopeptides: A) mechanism of action? B) selective toxicity? C) Other information
A) Inhibits cell wall synthesis. Bactericidal B) Only bacteria have peptidoglycan cell walls, so human cells are not affected C) Gram+ only (due to cell wall)
27
List the 8 common antibiotic classes by mechanism of action?
Aminoglycosides: Inhibits protein synthesis (30s) Cephalosporins: Inhibits cell wall synthesis Penicillins: Inhibits cell wall synthesis Tetracyclines: Inhibits protein synthesis (30s) Quinolones / Fluoroquinolones: Inhibits topoisomerases Macrolides: Inhibits protein synthesis (50s) Sulfonamides: Inhibits folate synthesis Glycopeptides: Inhibits cell wall synthesis
28
How do beta lactams work and what is their clinical significance?
Beta lactams (Penicillins, Cephalosporins, Monobactams, Carbapenams) are bactericidal antibiotics which inhibit cell wall synthesis. Some bacteria have developed resistance by producing beta-lactamases, which degrade the beta lactam ring
29
What is the mechanism of action of beta-lactamase inhibitors?
Medications which prevent bacteria from inactivating beta lactam antibiotics. They are often co-administered with beta lactams to treat resistant bacteria (e.g. co-amoxiclav)
30
A) Outline the mechanism of action for penicillins. B) List 4 common drug examples.
A) Inhibits cell wall synthesis (Beta Lactam) B) Penicillin (G & V), Flucloxacillin, Amoxicillin, Co-Amoxiclav
31
Flucloxacillin, Cefalexin, Meropenam, Aztreonam, and Cefuroxime are all examples of which drug class?
Beta Lactam antiobiotics (Penicillins, Cephalosporins, Monobactams, Carbopenams)
32
Cefuroxamine, Cefalexin, Ertapenam, and Aztreonam are all examples of which drug class?
Beta-Lactam antibiotics (Penicillins, Cephalosporins, Monobactams, Carbopenams)
33
Ertapenam, Meropenam, Ceftriaxone, and Co-Amoxiclav are all examples of which drug class?
Beta-Lactam antibiotics (Penicillins, Cephalosporins, Monobactams, Carbopenams)
34
Outline the mechanism of action for Cephalosporins. List 3 common drug examples
Inhibits cell wall synthesis (Beta Lactam) Cefalexin, Ceftriaxone, Cefuroxime
35
Outline the mechanism of action for Carbapenems. List 2 common drug examples
Inhibits cell wall synthesis (Beta Lactam) Meropenem, Ertapenem
36
Outline the mechanism of action for Monobactams. List a common drug in this class
Inhibits cell wall synthesis (Beta Lactam) Aztreonam
37
Outline the mechanism of action for Macrolides. List 3 common drugs in this class
Inhibits protein synthesis. Binds at the 50s ribosomal subunit. Clarithromycin, Erythromycin, Azithromycin
38
Outline the mechanism of action for Tetracyclines. List 3 common drugs in this class
Inhibits protein synthesis. Binds at the 30s ribosomal subunit. Doxycycline, Tetracycline, Lymecycline
39
Outline the mechanism of action for Aminoglycosides. List 2 common drugs in this class
Inhibits protein synthesis. Binds at the 30s ribosomal subunit. Gentamicin, Amikacin
40
Outline the mechanism of action for Fluoroquinolones. List 3 common drugs in this class
Inhibits topoisomerases, blocking DNA replication. Ciprofloxacin, Levofloxacin, Moxifloxacin
41
Outline the mechanism of action for Sulfonamides. List a common drug in this class
Inhibits enzymatic folate synthesis Trimethoprim
42
Outline the mechanism of action for Glycopeptides. List 2 common drugs in this class
Inhibits cell wall synthesis. Vancomycin, Teicoplanin
43
What is the functional difference between Benzylpenicillin and Phenoxymethylpenicillin?
1. Benzylpenicillin (Penicillin G) - introduced in 1942-45 - requires injection (not stable in stomach acid) 2. Phenoxymethylpenicillin (V) - introduced in 1950s - Oral form (acid stable)
44
Benzylpenicillin (Class, use, mechanism)
Class: Penicillins (Beta Lactam) Use: Main treatment for syphilis Mechanism: Inhibits bacterial cell wall formation. Causes cell lysing
45
Phenoxymethylpenicillin (Class, use, mechanism)
Class: Penicillins (Beta Lactam) Use: strep throat (S. pyogenes). Not effective against beta-lactamase producing bacteria Mechanism: Inhibits bacterial cell wall formation. Causes cell lysing
46
Flucloxacillin (Class, use, mechanism)
Class: Penicillins (Beta Lactam) Use: Staphylococcus infections. Narrow spectrum, beta-lactamase resistant Mechanism: Inhibits bacterial cell wall formation. Causes cell lysis
47
Amoxicillin (Class, use, mechanism)
Class: Penicillins (Beta Lactam) Use: Broad spectrum. Susceptible to beta-lactamases. Used for respiratory infections Mechanism: Inhibits bacterial cell wall formation. Causes cell lysing
48
What is a good rule of thumb when prescribing amoxicillin over flucloxacillin, or vice versa?
Flucloxacillin = Skin Amoxicillin = Respiratory
49
Co-amoxiclav (Class, use, mechanism)
Class: Penicillins (Beta lactam) Use: Broad spectrum, immune to beta-lactamase. Polymicrobial infections Mechanism: Inhibits cell wall synthesis. Causes cell lysis. Clavulanic acid acts as a beta-lactamase inhibitor
50
Ceftriaxone (Class, use, mechanism)
Class: Cephalosporin 3rd gen (beta-lactam) Use: broad spectrum. Good CSF penetration (good for meningitis). Does not cover pseudomonas Mechanism: Inhibits cell wall synthesis. Causes cell lysis
51
Ceftazidime (Class, use, mechanism)
Class: Cephalosporin 3rd gen (beta-lactam) Use: broad spectrum. Covers pseudomonas. Mechanism: Inhibits cell wall synthesis. Causes cell lysis
52
Erythromycin (Class, use, mechanism)
Class: Macrolide Use: Broad spectrum + some atypical coverage (mycoplasma, chlamydophila) Mechanism: Inhibits bacterial protein synthesis (Binds to 50s ribosomal subunit). Bacteriostatic
53
Azithromycin (Class, use, mechanism)
Class: Macrolide Use: Broad spectrum + good atypical effectiveness (more than erythromycin) Mechanism: Inhibits bacterial protein synthesis (Binds to 50s ribosomal subunit). Bacteriostatic
54
What are the suffixes for the 8 main antibiotic classes
Aminoglycosides: -mycin / micin Cephalosporins: cef- / ceph Penicillins: -cillin Tetracyclines: -cycline Quinolones: -floxacin Macrolides: -thromycin Sulfonamides: -sulfa Glycopeptides: -vancin / mycin
55
Ciprofloxacin (Class, use, mechanism)
Class: Fluoroquinolone Use: gram- bacteria (more reliant on gyrase and topoisomerase for DNA stability) Mechanism: Inhibits DNA replication (gyrase and topoisomerase)
56
Doxycycline (Class, use, mechanism)
Class: Tetracycline Use: Broad spectrum. Used for atypical infections (pneumonia, Lyme disease, malaria prophylaxis) Mechanism: Inhibits bacterial protein synthesis (Binds to 30s ribosomal subunit). Bacteriostatic
57
Trimethoprim (Class, use, mechanism)
Class: Seperate. Often classed as a sulfonamide (similar action) Use: Often used as an adjuvinant to sulfonamides to increase potency. Mechanism: Inhibits bacterial folic acid synthesis (higher in the pathway to sulfonamides)
58
Meropenem (Class, use, mechanism)
Class: Carbopenem (beta lactam) Use: broad spectrum. Stable against beta-lactamases Mechanism: Inhibits cell wall synthesis. Causes cell lysis
59
Clarithromycin (Class, use, mechanism)
Class: Macrolide Use: Helicobacter pylori Mechanism: Inhibits bacterial protein synthesis (Binds to 50s ribosomal sub unit). Bacteriostatic
60
Gentamicin (Class, use, mechanism)
Class: Aminoglycoside Use: gram- bacteria Mechanism: Inhibits protein synthesis (Binds to 30s ribosomal sub unit)
61
Vancomycin (Class, use, mechanism)
Class: Glycopeptide Use: MRSA Mechanism: Inhibits cell wall synthesis. Causes cell lysis

BMBS (4 decks)

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