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Tetracyclines & Sulfonamides
Pharamocolgy Chapter32
61
Nursing
Undergraduate 1
10/12/2009

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Term

 

Is the following statement True or False?
Tetracyclines and sulfonamides are older bacteriostatic medications that are rarely used for systemic infections.
Definition

 

True.
Tetracyclines and sulfonamides are older, broad-spectrum, bacteriostatic medications that are rarely used for systemic infections because of microbial resistance and the development of more effective or less toxic drugs.
Term

 

Tetracyclines and Sulfonamides
Definition

 

Older, broad-spectrum bacteriostats
Rarely used for systemic infections
Due to microbial resistance
Development of more effective/less toxic medications
Urinary antiseptics
Used only in UTIs
Term

 

Tetracyclines
Definition

 

Effective against wide range of gram(+) and gram(-) microbes
Not usually drug of choice
Widely distributed into most body tissues and fluids
Older medications are excreted mainly in urine
Doxycycline eliminated in urine and feces
Minocycline eliminated mainly by liver
Term

 

Doxycycline
Definition
  • Well absorbed:
  • Highly lipid soluble reaches therapuetic levels in CSF the eye and prostate gland
  • smaller dosage than tetracycline eliminated in urine and feces
Term
Doxycycline is given by 
Definition

po/IV 100-200mg

older adults po

Term

 

Minocycline
Definition
  • well absorbed after oral
  • like doxycline, readily penetrates the CSF
  • metabolized more than other tetracyclines, and smaller
  • eliminted by the liver
Term
Minocycline is given by 
Definition

po, 200mg initially then 100mg q12h

older 8y: po, 4 mg/kg initially, then 2 mg/kg q12

Term
Tetracyclines treats 
Definition

richettsiae

chlamydia

protoza

spirochetes

Brucella

vibrio cholerae

Term

 

Doxycycline treat
Definition

Bacillus anthracis (anthrax)

Chlamydia trachomatis

Respiratory tract infection due to mycoplasma pneumiae

Term
Tetracycline (achromycin)
Definition
  • UTI
  • Prototype drug
  • Marketed under generic and numerous
Term
Tetracycline (achromycine) treat by
Definition

po 250-500 mg q6h

older than 8 years po 25-50 mg/kg/d in 4 divide doses

Term

 

Demeclocycline (Declomycin)
Definition
  • tetraycline most likely to cause photosensitivity
  • primarily used to treat inappropriate secretion of antidiuretic horome
  • no longer recommend for treatment of gonorrhea
Term
Demeclocycline (Declomycin)
Definition

po 150 mg q6h or 300 mg q12h

older than 8years po 8-12 mg/kg/d in 2-4 divided doses

Term
Demeclocycline (Declomycin)
Definition
may be used to inhibit antidiuretic horomone in the treatment of chronic inappropriate antidiuretic hormone secrection
Term

 

Sulfonamides
Definition

 

Bacteriostatic against wide range of gram(+) and gram(-) microbes
Increasing resistance, decreasing efficacy
Susceptibility should be documented by culture and sensitivity testing
Some can be used in treatment of systemic infections
Others exert only local effects
Term

 

Sulfonamides
 
Sulfadiazine
Definition
  • A short-acting rapidly absorbed & excreted agent for systemic infections
  • The addition of folinic acid may be recommended
Term
Sulfadiazine clinical Indications 
Definition

Nocardiosis

Toxoplasmosis

Term
Sulfadiazine routes and Dosage Range
Definition

adults toxoplasmosis po 2-6 daily

in dived doses q 6h in conjunction w/ pyrimethamine

Nocardiosis 4-8 b/ day for minimum of 6 weeks

Term
Sulfadiazine routes and Dosage Range
Definition
childern toxoplasmosis older than 2 mo po75mg/kg initially, then 150 mg/kg/d in conjunction with pyri methamine in 4-6 divide doses maximal daily dose, 6g
Term

 

Sulfasalazine (Azulfidine)
Definition
  • porly absobed
  • dose not alter normal bacterial in the intestine
  • effectiveness in ulcerative colitis may be due to antibacterial
Term
Sulfasalazine (Azulfidine) Clinical Indications 
Definition

Ulcerative colitis/ Crohn's disease

Rheumatoid arthritis

Term
Sulfasalazine (Azulfidine) Routes and Dosage Ranges 
Definition

Adults Ulcerative colitis po 3-4g daily in 4 divided doses intially 2g daily in divided doses for maintenance maximal daily dose 4 g

Rheumatoid arthritis maintenance po 2g daily in divided doses q12h

Term
Sulfasalazine (Azulfidine) Routes and Dosage Ranges 
Definition
Childern  po 30-60mg/kg/d in 2-6 divided doses intially followed by 30mg/kg/d in 4 divided doses maximum daily dose 2g
Term

 

Sulfisoxazole
Definition
  • Rapidly absorbed rapidly excreted
  • Highly soluble and less likely to cause crystalluria than most other sulfonamides
Term
Sulfisoxazole Clinical indications 
Definition

UTI

Ocular infections

Term
Sulfisoxazole Routes and Dosage ranges
Definition
Adult po 2-4g initially then 4-8g daily in 4-6 divided doses
Term
Sulfisoxazole Routes and Dosage ranges
Definition
Childern  older than 2 mounths po 75mg/kg of body weight initially then 120-150mg/kg/d in 4-6 divided doses; maximal daily dose 6g
Term

 

Trimethoprim sulfamethoxazole (Bactrim)
Definition

May exhibit synergistic effectiveness against many organisms (verifysusceptibility first)

including streptococci (S. viridans) staphylococci (S. epidermidis, S aureus) Escherichia coli, Salmonella, Shigella, Serrtia Klebsiella, Nocardia, and others

Term
Trimethoprim sulfamethoxazole (Bactrim) Clinical Indications
Definition
  • Acute and chronic UTI
  • Acute exacerbations of chronic bronchitis
  • Acute otitis media caused by susceptible strains of hemophilus influenzae and Streptococcus pneumoniae
  • Shigellosis
  • Infection by pneumocystis jiroveci (prevention and treatment)
Term
Trimethoprim sulfamethoxazole (Bactrim) Routes and Dosage Ranges 
Definition
  • UTI trimethoprim 160mg and sulfamethoxazole 800 mg po q12h for 10-14 days
  • Shigellosis same doses as above for 5 d
  • Sever UTI , IV, 8-10 mg (trimethoprin component) kg/d in 2-4 divided doses, up to 14 d
Term
Trimethoprim sulfamethoxazole (Bactrim) Routes and Dosage Ranges 
Definition

Childern UTI and otitis media, po 8 mg/kg trimethoprim and 40 mg/ kg sulfamethoxazole in 2 divided doses q12h for 10d

Shigellosis same dose as above for 5 d

Sever Uti IV8-10mg (trimethoprim component )/kg in 2-4 divided doses, q 6-8hor q12, up to 14d

Term

 

Mafenide (Sulfamylon)
Definition
  • Effective against most gram - negative and gram-negative and gram-positive organisms especially Pseudomonas aeruginosa
  • Application cause pain and burning
  • Mafenide is absorbed systemically and may produce metabolic acidosis
Term
Mafenide (Sulfamylon) Clinical Indications
Definition
Prevention Of bacterial colonization and infection of severe burns
Term
Mafenide (Sulfamylon) Routes and Dosage Ranges
Definition

Topical application to burn area,onece or twice daily in a thin layer

In childern is the same as in adults

Term

 

Silver sulfadiazine (Silvadene)
Definition
Effective against most pseudomonas species the most common pathogen in severe burn sepsis E coli Klebsiella proteus Staphylococci and streptococci
Term

 

Silver sulfadiazine (Silvadene) Clinical Indications 
Definition
SAme as mafenide usually the preferred drug
Term
Silver sulfadiazine (Silvadene) Routres and Dosage Ranges 
Definition
Adults 1-2 times daily cover burned area w/ cream In childern is the same as in adults
Term

 

Urinary Antiseptics
Definition

 

May be bactericidal because of local effects produced by high concentration levels in renal tubules and urine
Not used for systemic infections
Do not attain therapeutic plasma levels
Term

 

Mechanisms of Action
Definition

 

Tetracyclines
Penetrate microbial cells, inhibiting protein synthesis
Sulfonamides
Halt multiplication of new bacteria
Do not kill mature, fully formed bacteria
Term

 

Is the following statement True or False?
Phenazopyridine is an antimicrobial used in the treatment of UTIs.
Definition

 

False.
Phenazopyridine is not an antimicrobial medication; it is administered to relieve pain associated with UTIs.
Term

 

Tetracycline Indications for Use
Definition

 

Drug of choice in specific infections
Cholera, Rocky Mountain spotted fever, syphilis, typhus, H. pylori, etc
Useful in animal bites, lyme disease
Chlamydia infections; adjunct in STD treatment; prophylaxis/treatment of anthrax
Long-term acne treatment; substitute for PCN in hypersensitivity
Term

 

Sulfonamide Indications for Use
Definition

 

UTI caused by E. coli, Proteus, Klebsiella organisms
In combination to treat chronic bronchitis
Ulcerative colitis, other uncommon infections
Topically
Prevention of burn wound infections
Ocular and other soft tissue infections
Term

 

Urinary Antiseptic Indications for Use
Definition

 

Urinary antiseptics are used only for UTIs
Term

 

Urinary Antiseptics
Definition

 

Fosfomycin (Monurol)
Methenamine mandelate (Mandelamine)
Methenamine hippurate (Hiprex)
Nalidixic acid (NegGram)
Nitrofurantoin (Furadantin, Macrodantin)
Phenazopyridine (Pyridium)
Term

 

Nitrofurantoin (Furadantin, Macrodantin)
Definition
  • Antibacterial activity against Ecoil and most other organisms that cause UTI
  • Used for short-term treatment of UTI or long-term suppression of bacteria in chronic, recurrent UTI
  • Bacterial resistance develops slowly and to a limited degree
  • Contraindicated in severe renal disease
Term
Nitrofurantoin (Furadantin, Macrodantin) Routes and Dosage 
Definition

Macrodantin: PO 50-100 mg 4 times daily; Macrobid 100

mg q12h for 7 d

Prophylaxis of recurrent UTI in women Macrodantin PO 50-100mg at bedtime

Term
Nitrofurantoin (Furadantin, Macrodantin) Routes and Dosage 
Definition

In childern: older than 12 years Dual-release capsules 100mg q12h for 7 days

Childern: i mounths and older PO macrocrystal capsules 5-7mg/kg/d in 4 divided dose for 7 days

Term

 

Phenazopyridine (Pyridium)
Definition
  • An azo dye that acts as a urinary tract analgesic and relives sysmptoms of dysuria, burning, and frequency and urgency of urination, which occur with UTI
  • It has no anti-infective action
  • It turns urine orange- red which may be mistaken as blood
  • It is contraindicated in renal insufficiency and sever hepatitis
Term
Phenazopyridine (Pyridium) Routes and Dosage Ranges 
Definition

Adults PO 100-200mg 3 times Daily after meals

Childern: 6-12 years 12mg/kg/day in 3 divided doses after meals

Term

 

Contraindications for Use 
Tetracyclines and sulfonamides
 
 
Definition

 

Clients with renal failure
Tetracyclines
Pregnant women
Children aged <8 years
Can discolor tooth enamel and depress bone growth
Term

 

Principles of Therapy 
Tetracyclines
 
Definition

 

Culture and susceptibility studies needed before therapy begun
Due to drug resistance
Oral route is effective and preferred
Decompose with age, light exposure, extreme heat and humidity
Medications must be stored correctly
Term

 

Principles of Therapy 
Sulfonamides and urinary antiseptics
 
Definition

 

Culture and susceptibility studies needed before therapy begun
Loading dose produces therapeutic blood levels more quickly
Loading dose = twice maintenance dose
Urine pH important in pharmacotherapy
Term

 

Is the following statement True or False?
Tetracyclines can be prescribed for the treatment of specific STDs.
Definition

 

True.
Tetracyclines can be prescribed for the treatment of certain chlamydial infections, pelvic inflammatory disease, and sexually transmitted diseases.
Term

 

Special Population Use
Definition

 

Children
Older adults
Renal impairment
Hepatic impairment
Critical illness
Term
Special Population Use IN Childern 
Definition
Tetracyclines should not be used in children younger than 8 years of age because of their effectes on teeth and bones.
Term
Special Population In Adults
Definition
  •  A major concern with the use of tetracyclines and sulfonamides in older adults is renal impairment
  • In younger adsults a fluid intake of 2 liters daily is needed to reduce formation of crystals & stones in the urinary tract.
  • Severe skin reactions and bone marrow depression are most often reported w/ combination of trimethoprin-sulfamethoxazole
Term
Special Population With Renal Impairment
Definition
  • As discussed previously, most tetracyclines are contraindicated in patients w/ renal impairment. High concentrations of tetracyclines inhibit protein synthesis in human cells.

 

Term
Special Population With Renal Impairment
Definition

Azotemia increased blood urea nitrogen, hyperphosphatemia, hyperkalemia, & acidosis.

Acute renal failure (ARF) has occurred when the drugs or their metabolites precipitated in renal tubules and caused obstruction. ARF is rarely associated with newer sulfonamides.

Term

 

USE In Patients With Hepatic impairment
Definition
Tetracyclines are generally contraindicated in pregnant women because they may cause fatal heptic necrosis in the mother as fetus.
Term

 

Critical illness
Definition
Tetracyclines may be used to treat sepsis caused by rickettsial, chlamydial, or mycoplasma infection and pulmonary infection caused by M. pneumoniae or Legionella pneumophila
Term
Doxycycline or Minocycline
Definition
Given to renal patients and critical ill
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