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Musculoskeletal Exam 2 > Pharmacology - Chloramphenicol, Tetracycline, Clindamycin > Flashcards

Pharmacology - Chloramphenicol, Tetracycline, Clindamycin Flashcards

1
Q

How are tetracylines formulated and how does this effect them metabolically?
What factor decreases GI absorption?
What is the mechanism of action of tetracyclines?

A
  • They are formulated as hydrochlorides which allow them to be water soluble.
  • GI absorption is decreased by the presence of food in the GI and a high pH
  • Reversibly blocks the 30s ribosome to prevent protein synthesis
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2
Q

What is the spectrum of anti-microbial activity for tetracycline?

A
  • Broad spectrum with activity against many gram positive and gram negative (Chlamydia, mycoplasmas, Rickettsiae and L-forms. They are also effective against protozoa like amebas.
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3
Q

How do tetracyclines enter susceptible bacteria?

What alternatives are there to fight microbials with tetracycline resistant efflux pumps?

A
  • In part by simple diffusion and through active transport

Doxycucline, minocycline, and tigecycline

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4
Q

What are 3 general ways that resistance can be developed to tetracycline?

A

1) Impaired influx or enhanced efflux (of tetracycline) by an active transport protein pump
2) Ribosome protection
3) Enzymatic inactivation of the drugs

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5
Q

What is soo freaking special about Tigecycline’s ability to knock off bacteria?

A
  • It is effective even against the Tet (A) efflux-expressing gram negative strains having resistance to the older tetracyclines/
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6
Q

What 3 drugs can overcome Tet (K) resistance to tetracyclines.

A

doxycyclines, minocycline, or tigecycline

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7
Q

What 3 drugs can overcome Tet (M) ribosomal protection expressed by gram positive strains confers resistance to tetracyclines.

A

Doxycycline, minocycline, and tigecycline

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8
Q

How is Tigecycline absorbed?

What is the percentage of Doxycline and Minocycline absorption?

A
  • through IV (100%)

- 95-100%

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9
Q

What two tetracyclines are not impaired by food in the GI tract?
What food products or Cations can impair the GI absorption of tetracycline?

A
  • Doxycyline and minocycline

- Concurrent ingestion of dairy products, antacids or the cations like Ca+, Mg2+, Fe2+, or Al3+

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10
Q

What is the distribution range of Tetracyclines?

What is its effects on fetuses and kids?

A
  • Everywhere - except the CNS where only a small portion is present
  • Crosses the placenta, found in breast milk, bind calcium and damage bones and teeth especially in children, not good for children younger than 8 years old due to active epiphysis.
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11
Q

What drug attains high concentrations in saliva and tears making it useful for eradication of the meningococcal carrier state?

A
  • Minocycline
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12
Q

How are tetracyclines mainly excreted?

What two tetracyclines are excreted via non-renal mechanisms?

A
  • excreted mainly in the urine and in the bile with enterohepatic circulation.
  • Doxycycline and tigecycline
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13
Q

What is the range of T1/2 for some of the top lasting tetracyclines?

A
  • Tigecycline (36 hrs)
  • Doxycycline and minocycline (16-18 hrs)
  • Demeclocycline and methacycline (12 hrs)
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14
Q

What types of infections is tetracyclines useful in?

A
  • Infections involving Mycoplasma, pneumoniae, Rickettsiae (Rocky mountain fever), Chlamydia, Trachoma, Antrax, and some Spirochetes
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15
Q
A
  • Helcobacter pylori-induced ulcers
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16
Q

What disease caused by vibrio does tetracycline have a rapid response to?

A
  • Cholera
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17
Q

What is Tetracycline’s effects in STDs?

A
  • Effective against most Chlamydial infections but is no longer indicated for gonoccal infections due to resistance.
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18
Q

Tetracyclines are used in combination with aminoglycosides to treat what?
- What Protozoal infections are indicated with tetracyclines?
What tetracycline might be used to treat ADH secreting tumors?

A

plague, tularemia, and brucellosis

  • Entramoeba histolytica or Plasmodium falciparum
  • Demeclocycline
19
Q

What are some other diseases treated with Tetracyclines?

A
  • Acne
  • exercitation of bronchitis
  • community acquired pneumonia
  • Lyme disease
  • relapsing fever
  • leptospirosis
  • Mycobacterium marinum
20
Q

What types of activity does Tigecycline have against resistant bacteria?

A
  • Coagulase negative staphylococci and Staphylococci aureus and methicillin -resistant strains. Streptococci, penicillin susceptible and resistant, enterococci, vancomycin-resistant strains and gram negative rods. Effective against Enterobacteriacae, multiple resistant strains of Acenitobacter species, Rickettsiae, chlamydia, and legionella.
  • ** Proteus and Pseudomonas aeruginosa are resistant
21
Q

What are the 6 main uses for tetracyclines?

A
  • Cholera
  • Malaria
  • Parrot Fever
  • Lyme Disease
  • Rocky mountain spotted fever
  • Q-fever
22
Q

What are the adverse effects of Tetracyclines on the GI tract?
Due to disruption of normal flora giving rise to overgrowth of bacteria what might result?

A
  • nausea, vomiting, and diarrhea

- Anal pruritus, vaginal, or oral candidiasis

23
Q

Where are tetracyclines deposited in kids less then 8 yrs and pregnant women?
- Administered in high doses could effect intravenously could effect what?

A
  • Deposited in the bones and the teeth

- The liver resulting in hepatic necrosis

24
Q

Tetracyclines cause nitrogen resulting in the renal buildup of all tetracyclines except?
What does local tissue toxicity result in?

A

Doxycycline and tigecycline

- Venous thrombosis, pain, and local irritation in muscles

25
Q

What tetracycline especially has photosensitivity?

What vestibular reaction can result?

A
  • Demeclocycline

- Dizziness, vertigo, nausea, and vomiting have been noted particularly with doxycycline.

26
Q

What is the Mechanism of action of Clindamycin?

What microbes are susceptible to Clindamycin and what are resistance?

A
  • Binds exclusively to the 50S ribosome and inhibits protein synthesis
  • Susceptible: Streptococci, staphylococci, pneumococci, and bacteriodes species
    Resistant: enterococci and gram negative aerobic organisms
27
Q

What mechanism of resistance is used against Clindamycin?

A

1) Mutation of the ribosomal receptor site
2) Constitutive expression of METHYLASE–> modification of the receptors
3) Enzymatic inactivation of clindamycin
- Gram negative aerobic species are intrinsically resistant due to poor permeability of the outer cell wall.

28
Q

What is the % of protein binding in Clindamycin?

- What type of cells does clindamycin concentrate in?

A
  • 90% protein bound and has good penetration in to the tissues (except for the CNS)
  • Concentrates in phagocytic cells via active transport
29
Q

Where is Clindamycin metabolized in, excreted with, and does an adjustment need to occur with renal insufficiency?

A
  • metabolized in the liver, excreted in the urine and bile, and dose adjustment is not necessary in renal insufficiency
30
Q

What types of infection are treated with clindamycin?

Clindamycin is used in combination with cephalosporin or aminoglycosides to treat what?

A
  • Anaerobic infections by bacteroide species

- To treat penetrating wound of the abdomen

31
Q

Clindamycin provides prophylaxis against what in patients with valvular hear diseases?
What Clindamycin is combined with what drug does it form an effective alternative to trimethoprim-sulfamethozazole against moderate to severe pneumocystitis jirovei in AIDS patients?

A
  • Prophylaxis against endocarditis

- Primaquine

32
Q

Clindamycin is also used in combination with pyrimethamine for AIDS-related what of the brain?

A

toxoplasmosis

33
Q

What are the adverse effects of Clindamycin?

A
  • Diarrhea, nausea, vomiting, and skin rashes
  • Impaired liver function (possible jaundice) and NEUTROPENIA may also occur
  • SEVERE DIARRHEA and PSEUDO MEMBRANOUS COLITIS have been reported following admin. of clindamycin most likely due to Clostridium difficile
34
Q

What is the mechanism of action of chloramphenicol?

What is Chloramphenicol’s spectrum range?

A
  • inhibits bacterial 50S ribosomes and prevent protein synthesis
  • Has a broad spectrum with activity against both gram negative and gram positive bacteria
35
Q

What microbacteria is Chloramphenicol active against?

A
  • Active against Rickettsia but not Chlamydia. Active against haemophilus influenza, N. meningitis and some strands of bacteriodes are highly susceptible.
36
Q

What is resistance to chloramphenicol due to?

A

The production of CHLORAMPHENICOL ACYL TRANSFERASE, a plasmid encoded enzyme

37
Q 
Where is Chloramphenicol distributed?
- Where is it metabolized and excreted?
- How does dosing change with renal 
insufficiency?
- How would dosing be reduced in newborns and premature infants?
A
  • Widely distributed throughout the body including the CNS and body fluids.
  • Conjugated in the liver (glucuronic acid) and eliminated in urine.
  • Dosing MUST be reduced in hepatic but not renal insufficiency.
  • Dose must also be reduced in newborns and premature infants
38
Q

How does chloramphenicol treatment effect cholera, Rickettsia diseases?
- What is disease is it an alternative to beta-lactam?

A
  • It is a second line drug for cholera, and is indicated for serious Rickettsial infection such as typhus and Rocky Mountain Spotted Fever
  • Meningococcal meningitis (in patients either hypersensitive to penicillin or if the infection is penicillin-resistant
39
Q

Used for Brain abscesses and topically for treatment of eye infection.

A

Just didn’t feel like making a questions out of that!!

40
Q

What are the adverse effects in the GI tract?

A
  • Adults (no kids) commonly develop nausea, vomiting, and diarrhea
  • Risk of oral or vaginal candidiasis may occur due to alteration of normal flora
41
Q

What bone marrow disturbances might occur with chloramphenicol?

A
  • Bone marrow disturbances: decreased production of red blood cells. Aplastic anemia (idiosyncratic - no explanation) may be reversible but could be fatal
42
Q

What is the toxicity in newborn infants?

A
  • Gray baby syndrome ( vomiting flaccidity, hypothermia, gray color shock and collapse). Must be used with caution in infants
43
Q

What are the drug interactions of Chloramphenicol?

A
  • (Chloramphenicol is a CYP inhibitor that reduces the rate of metabolism of) phenytoin, tolbutamide, chlorpropamide, and warfarin, thereby increasing their half lives
  • Can also antagonize the effect of penicillin and aminoglycosides.

Musculoskeletal Exam 2 (8 decks)

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