Sulphanomides

Question 1

What type of antiinfectives are sulphanomides?

Answer 1

Antibacterics - chemotherapeutics

Question 2

Characterize sulphanomides:

Answer 2

Complex synthetic organic chemical compounds.
Bacteriostatic activity.

Question 3

Spectrum of action of sulphanomides:

Answer 3

• Gram positive and Gram negative bacteria: streptococcus, staphylococcus, haemophilius, bacteroides, brucella, corynebacterium, chlamydia and toxoplasma gondii
• wide using
• plasmid mediated resistance in G+ and G- bacteria: enterococcus, campylobacter, pseudomonas, mycoplasma, mycobacterium

Question 4

Farmacokinetics of sulphanomides:

Answer 4

• bind to plasma albumin
• high doses application
• unbounded molecules can penetrate into tissues, organs, placenta, milk
• eliminated in urine, perspiration, tears, bile, milk

Question 5

Minimum therapeutic concentration in blood for reaching bacteriostatic effect:

Answer 5

2-10 mg%

Question 6

Mechanism of action of sulphanomides:

Answer 6

Structural analogs of PABA
- competitively inhibit dihydropteroate synthase –> reduced synthesis of dihydrofolic acid –> levels of tetrahydrofolate diminish –> suppression of protein synthesis –> impairment of metabolic processes –> inhibition of microbial growth and multiplication
BACTERIOSTATIC

Question 7

Mechanism of action of potentiated sulfanomides:

Answer 7

diaminopyrimidine used in combination competively inhibits dihydrofolate reductase enzyme to prevent the formation of folinic acid, required for the synthesis of DNA
BACTERICIDAL

Question 8

Trimethoprim and sulfanomides used separately have which effect?
And which effect does the combination have?

Answer 8

Bacteriostatic, but becomes bactericidal when used in combination

Question 9

What is the standard use of sulfanomides?

Answer 9

• upper and lower respiratory tract infections
• urogenital system
• erysipelas, septicemia, pyemia
• secondary bacterial infections in viral diseases
• coccidosis
  D: 1-4 x daily. 120-150 mg/kg p.o., 60-75 mg/kg s.c., i.m.
  (potentiated are administered as 1/2 or 1/3)

Question 10

Classify sulfanomides according to duration of action:

Answer 10

1. Short-acting: above 50 ug/ml <12h (sulfadiazine)
2. Intermediate-acting: above 50 ug/ml for 12-24 h (sulfamethoxazole)
3. Long-acting: 50 ug/ml obtained after 24h after dosing (sulfadoxine, sulfamethopyrazine)

Question 11

Name short-acting sulphanomides:

Answer 11

sulfathiazole, sulfacetamide

Question 12

Name long-acting sulphanomides:

Answer 12

sulfamidine, sulfadiazine, sulfamerazine, sulfaqmetoxazole

Question 13

Name long-acting sulphanomides:

Answer 13

sulfamethoxypyridazine, sulfadoxine, sulfadimethoxine

Question 14

Divide sulphanomides according to solubility/or administration:

Answer 14

Highly soluble - urinary tract infections
Poorly soluble - intestinal infection:
- ulcerative colitis in dog
- caecal and intestinal coccidosis (sulfaquinoxaline and sulfaclozine)
Topical sulfanomides:
- ophtalmic infections
- burn wounds

Question 15

Name adverse and undesired effects of sulphanomides:

Answer 15

Hepatitis, hypersensitivity, bone marrow depression
Nausea and vomiting, disorders in digestion and urinary tract
Crystalluria - impairment of kidney tubules (in low pH)
Cyanosis
Hemorrhagic syndrome (vit. K synthesis)
Reduction of vit. B synthesis (suppression of gut microflora)

Question 16

Contraindications of sulphanomides:

Answer 16

Hypersensitivity, severe renal or hepatic impairment
Hepatic disease
Urolithiasis

Question 17

Name enteric and local sulphanomides:

Answer 17

phthalylsulfatiazole (Streptonamid), sulfaclozinum (Klozanit)

Question 18

How does quinolones and fluoroquinolones act?

Answer 18

Inhibition of bacterial DNA synthesis - bactericidal

In-vitro bactericidal effect on G- microorganisms

High concentrations in urine but low in blood and tissues

Question 19

Mechanism of action of quinolones:

Answer 19

Inhibit replication of bacterial DNA by blocking the ligase domain of bacterial DNA gyrase (topoisomerase II); some also inhibit topoisomerase IV.
These enzymes relax DNA supercoils and enable DNA replication and repair
- Bactericidal

Question 20

Mechanism of action of fluoroquinolones:

Answer 20

Inhibit two enzymes (DNA topoisomeres) involved in bacterial DNA synthesis.
Human cells lack these enzymes, and they are essential for bacterial DNA replication.
Both specific and bactericidal.

Question 21

Indications of quinolones:

Answer 21

Urinary tract infections: acute cystitis, prevention of chronic infections
Enteric infections: shigellosis, bacterial enterocolitis

Question 22

Indications of fluoroquinolones:

Answer 22

Upper respiratory tract infections
Enteric infections
Anthrax
Infections of the urogenital system
Infections of skin, soft tissues, bones and joints
Eye infections
Meningitis by G- bacteria
Sepsis
Tuberculosis

Question 23

Division of quinolones:

Answer 23

4 generations:
1. gen - quinolones
2. - 4. gen. - fluoroquinolones

Question 24

Name some quinolones:

Answer 24

nalidixid acid, oxalin acid, flumechin, cinoxacin, flumexil 5% inj a.u.v, flumigal 4% plv. a.u.v.