Outline 11, Tetracycline

Front 1

Tetracyclines are yellow powders and have ________ solubility.

Back 1

Low

Front 2

Tetracyclines are _________ in neutral and alkaline.

Back 2

Inactivated

Front 3

True or False
Tetracyclines are resonance stabilized in acidic solutions.

Back 3

True

Front 4

True or False
Tetracyclines act as chelators and bind divalent and trivalent cations.

Back 4

True

Front 5

What is the MOA of tetracycline?

Back 5

Reversibly bind to the 30S ribosomal subunit inhibiting the aminoacyltRNA to mRNA/ribosome complex.

Front 6

True or False
Tetracyclines block the P site, preventing additions to the growing chain.

Back 6

False
A

Front 7

How does tetracycline enter into the cell?

Back 7

Initial rapid uptake via passive diffusion, followed by a slower energy dependent mechanism.

Front 8

Hydrophilic tetracyclines diffuse through ________________________.

Back 8

Pores in the outer membrane.

Front 9

Lipophilic tetracyclines diffuse through ________________________.

Back 9

The lipid matrix.

Front 10

Can tetracyclines affect human protein synthesis?

Back 10

Yes.

Front 11

Group of drugs found in soil samples (strep cultures). Broad spectrum activity on gram +/- organisms.

Back 11

Tetracyclines

Front 12

Are tetracyclines charged in acidic solutions?

Back 12

Yes.

Front 13

True or False
Tetracyclines can acts as chelators binding monovalent and divalent cations.

Back 13

False.
Divalent and Trivalent

Front 14

You should avoid _______ and _______ when taking tetracyclines.

Back 14

Antacids
Diary

Front 15

True or False
Tetracyclines are bacteriocidal agents that irreversibly bind to the 30S ribosomal subunit, thereby inhibiting protein synthesis.

Back 15

False
Tetracyclines are bacteriostatic and they reversibly bind to the 30S ribosomal subunit.

Front 16

Tetracyclines inhibit binding of ______________ to mRNA/ribosome complex.

Back 16

Aminoacyl-tRNA

Front 17

True or False
Tetracyclines block the P site.

Back 17

False
A site

Front 18

True or False
Tetracyclines initially enter microorganisms via passive diffusion until equilibrium is reached and then continue to enter via an energy-dependent process of active transport.

Back 18

True

Front 19

Answer Lipophilic or Hydrophilic
The more _________ tetracyclines pass through pores in the outer membrane, while the more ________ tetracyclines diffuse through the lipid matrix.

Back 19

Hydrophilic
Lipophilic

Front 20

Answer Lipophilic or Hydrophilic

Minocycline, Doxycycline, Tigecycline

Back 20

Lipophilic

Front 21

What are two side effects caused by Calcium binding and chelation of tetracyclines?

Back 21

Retardation of bone growth
Discoloration of teeth via oxidation

Front 22

True or False
Tetracyclines have very poor CNS penetration and should not be taken with food.

Back 22

True

Front 23

Answer Lipophilic or Hydrophilic

Tetracycline, chlorocycline, and oxycyline.

Back 23

Hydrophilic

Front 24

Which is more sensitive to tetracyclines, bacterial or mammalian ribosomes?

Back 24

Bacterial

Front 25

Under what circumstances can tetracyclines interfere with protein synthesis of human cells?

Back 25

If the patient is taking a drug that alters human membrane permeability.
(Amphotericin B and Polymixin B)

Front 26

What are the two most important ways bacteria confer resistance to tetracyclines?

Back 26

1. Impaired influx and increased efflux.
2. Ribosomal protection to decrease binding.

Front 27

What tetracyclines are gram (-) species resistant to? (Caused by an efflux pump)

Back 27

Doxycycline, Demeclocycline, and Minocycline.

Front 28

What tetracyclines are gram (+) staphylococci species resistant to? (Caused by an efflux pump)

Back 28

Tetracycline

Front 29

What tetracyclines are gram (+) species resistant to? (Caused by ribosomal protection protein)

Back 29

Tetracycline, Doxycycline, and Minocycline.

Front 30

Which species are intrinsically resistant to all tetracyclines?

Back 30

Proteus and Pseudomonas aeruginosa.

Front 31

True or False
Use of outdated tetracyclines can cause renal tubular alkalosis.

Back 31

False
Acidosis

Front 32

True or False
Use of tetracyclines can lead to reversible Fanconi syndrome.

Back 32

True

Front 33

What common side effect of tetracyclines is most frequent with demeclocylcine but rare with minocycline? Is it reversible?

Back 33

Phototoxicity
Yes

Front 34

True or False
Superinfections (oral/vaginal candidiasis) are common with tetracycline use.

Back 34

True

Front 35

True or False
Tetracyclines cause GI irritation because they are corrosive, acidic compounds, but the irritation can be lessened by decreasing the dose or taking the drug with food.

Back 35

True

Front 36

Are tetracyclines commonly given via IM injections?

Back 36

No. Solubility issues.

Front 37

What will occur if a tetracycline is repeatedly given IV in the same vein?

Back 37

Thrombophlebitis

Front 38

Used as a treatment for chronic SIADH. Has the greatest affinity for Calcium ions.

Back 38

Demeclocycline.

Front 39

Which tetracycline causes severe photosensitivity and reversible dose-dependent diabetes insipidus syndrome?

Back 39

Demeclocylcline.

Front 40

If a renally impaired patient takes tetracycline or oxytetracycline, what will happen?

Back 40

Half-life increases to 57-120 hours.

Front 41

Which drug is a semisynthetic derivative of oxytetracycline and has the least affinity for calcium ions of all tetracyclines?

Back 41

Doxycycline.

Front 42

Which drug is a semisynthetic derivative of tetracycline and its side effects are more common in women than men?

Back 42

Minocycline

Front 43

Which drug is a semisynthetic derivative of minocycline and contains a glycylamido group?

Back 43

Tigecycline

Front 44

How is tigecycline primarily eliminated?

Back 44

Feces.

Front 45

What are two nontraditional uses of tetracyclines?

Back 45

1. Acne: May cause yellow discoloration.
2. Detection of malignant tumors: high affinity for necrotic tissues and tumors.