ORAL PREPARATIONS:
--------------------------------------------------------------------------------
x
ORAL ANTIBIOTICS/ANTIBACERIALS
Use of Antimicrobials in Food Animals
(Special Report by AABP)
"The antibiotic era is barely 60 years old, yet the inappropriate use of these drugs threatens our ability to cope with infections"
Drs. R.P. Wenzel and M.B. Edmond
Virginia Commonwealth University
Sulfonamides
Drug Family: Folic Acid Inhibitors
References Sulfonamides
Sulfonamides are broad-spectrum antimicrobials inhibiting both gram-positive and gram-negative bacteria, as well as some protozoa, such as coccidia. Sulfonamides are widely distributed throughout the body, and cross the placenta (some teratogenic effects have been seen when very high doses were given to pregnant mice and rats).
NOTE: Sulfaquinoxaline is minimally absorbed systemically and is referred to as an enteric sulfonamide.
Resistance of animal pathogens to sulfonamides is widespread as a result of more than 50 years of therapeutic use and this limits their effectiveness. Cross-resistance between sulfonamides is considered complete. BACTERIOSTATIC.....
--------------------------------------------------------------------------------
Sulfamethoxazole/Trimethoprim & Sulfadiazine/Trimethoprim combo's listed becuase they are so frequently used.
Data and studies indicate that
Trimethoprim is inactivated after oral administration in ruminants.
This occurs also with the sulfa-trimethoprim combinations that have been used orally in extralabel applications (Byrne, personal communic. 1999) in ruminants.
. TRIMETHOPRIM/SULFAMETHOXAZOLE - Rx item
BRAND NAMES : Septra® Uroplus® SS
TMP/SMX Sulfamethoprim® Cotrim® (Canada & US)
TMP/SMZ Sulfatrim® Cotrim® DS(Canada & US)
Bactrim® Sulfatrim® DS Di-Trim® (Canada & US)
Septra® DS Uroplus® DS
Antibacterial, systemic --Sulfadiazine and Trimethoprim; Sulfamethoxazole and Trimethoprim
Antiprotozoal --Sulfamethoxazole and Trimethoprim
TRIMETHOPRIM/SULFADIAZINE- Rx item
BRAND NAMES : TMP/SDZ Tribrissen®
Cotrim® (Canada Cotrim® DS (Canada) Di-Trim® (Canada)
Antibacterial, systemic --Sulfadiazine and Trimethoprim; Sulfamethoxazole and Trimethoprim
--------------------------------------------------------------------------------
DOSE : 30mg/kg (665mg/50 pounds) twice daily . The most common tablets are 960mg. = one 960mg tablet per 70-75 pounds twice daily.
Plasma levels are achieved in approximately 6 hours following oral dosage.
A broad spectrum antioibiotic and sulfa combination with a wide spectrum of activity against gram neagtive and positive organisims. Sulfonamides (sulfadiazine and sulfamethoxazole) are bacteriostatic and trimethoprim is bacteriocidal. In combination, they are bacteriocidal.
Effective against Actinomyces spp., B. anthracis, Bordetella, Brucella, Clostridia, Corynebacterium, e-coli , Haemophillus, Klebsiella, pasturella, Proteus, Salmonella spp., Staphylococci. Streptococci and Vibro spp.
For respiratory, urinary tract, skin, and gastrointestinal infections, and infections with coccidia.
There is some question about the oral use of trimethoprim in ruminents. Some thoughts are that it is perhaps significantly degraded in the rumen.
CONTRAINDICATIONS : Untreated dehydration.
CAUTION: Prolonged use may decrease thyroid function and affect tear production in the eye.
Store at room temperature in a tight container.
Not approved for lactating animals in the US.
WITHDRAWAL (cattle) (Canada) - 3 days for T/sulfadiazine, 10 days T/sulfadoxine.
MILK DISCARD (cattle) (Canada) - 96 hours for T/sulfadiazine or T/sufladoxine.
--------------------------------------------------------------------------------
Vet. Res. 32 (2001) 261-273
(Received 7 December 2000; accepted 7 February 2001)
Resistance to trimethoprim and sulfonamides
Ola Sköld
Division of Microbiology, Department of Pharmaceutical Biosciences, Biomedical Center, Uppsala University, PO Box 581, SE-751 23 Uppsala, Sweden
Abstract
Sulfonamides and trimethoprim have been used for many decades as efficient and inexpensive antibacterial agents for animals and man. Resistance to both has, however, spread extensively and rapidly. This is mainly due to the horizontal spread of resistance genes, expressing drug-insensitive variants of the target enzymes dihydropteroate synthase and dihydrofolate reductase, for sulfonamide and trimethoprim, respectively. Two genes, sul1 and sul2, mediated by transposons and plasmids, and expressing dihydropteroate synthases highly resistant to sulfonamide, have been found. For trimethoprim, almost twenty phylogenetically different resistance genes, expressing drug-insensitive dihydrofolate reductases have been characterized. They are efficiently spread as cassettes in integrons, and on transposons and plasmids. One particular gene, dfr9, seems to have originally been selected in the intestine of swine, where it was found in Escherichia coli, on large plasmids in a disabled transposon, Tn5393, originally found in the plant pathogen Erwinia amylovora . There are also many examples of chromosomal resistance to sulfonamides and trimethoprim, with different degrees of complexity, from simple base changes in the target genes to transformational and recombinational exchanges of whole genes or parts of genes, forming mosaic gene patterns. Furthermore, the trade-off, seen in laboratory experiments selecting resistance mutants, showing drug-resistant but also less efficient (increased Ks) target enzymes, seems to be adjusted for by compensatory mutations in clinically isolated drug-resistant pathogens. This means that susceptibility will not return after suspending the use of sulfonamide and trimethoprim.
--------------------------------------------------------------------------------
.. SULFAQUINOXALINE [20% solution] - Coccidia treatment.
DOSE 6mg/lb daily for 5 days.
for SULFAQUINOXALINE 20% solution (200 mg per mL) :
Drench: 2ml/50 lbs orally for 5 days.
Water: 1oz/10 gallons (animals will need to drink 1 quart of solution for each 25 lbs of body weight to get an effective dose).
NOTE: Sulfaquinoxaline is minimally absorbed systemically and is referred to as an enteric (Of, relating to, or being within the intestine) sulfonamide.
--------------------------------------------------------------------------------
PRODUCT RECALL: June 2000 -
PRODUCT Hess & Clark brand 20% Sulfaquinoxaline Sodium Solution, in 16-ounce bottles, product is added to drinking water to teat infections in chickens, turkeys, cattle and calves.
CODE Lot #07397 EXP OCT 02.
MANFACTURER Hess & Clark Inc., Ashland, Ohio.
DISTRIBUTION Alabama, Oklahoma, Missouri, Hawaii, Pennsylvania, Iowa, Kansas, Ohio, and Texas.
QUANTITY 27 cases (12 bottles per case) were distributed.
REASON An extended expiration date was used on the label. Stability data existed only for 2 years as packaged in 16-ounce bottles.
--------------------------------------------------------------------------------
VETERINARY PRODUCTS/BRAND NAMES :
note the different strengths
34.4 mg per mL (OTC) [liquid Sulfa-Nox].Dose: 11.5mL/50 lbs
200 mg per mL (OTC) [Sulfa-Q20%; GENERIC] Dose: 2mL/50 lbs
286.2 mg per mL - (29% solution) (OTC) [Sulquin 6-50] Dose: 1.4 (1.5)mL/50 lbs
340 mg per mL (OTC) [34% Sul-Q-Nox]. Dose: 1.1mL/50 lbs
.MEAT WITHOLDING: 10 days.
...... ALBON® & DI-METHOX® [both are sulfadimethoxine]. For coccidia and scours.
DOSE : 25 mg of sulfadimethoxine per pound (55mg/kg) day one, 12.5mg per lb (27mg.kg) days 2-5.
Also used for pneumonia and misc. bacterial infectious processes.
See injectable Albon (Albon Injection-40%) information under Injectable Antibiotics.
WITHDRAWAL (boluses) : Meat 7 days. Milk discard 60 hours.
Albon®[ Albon 12.5% solution ]Dose rateof the 12.5% oral solution is 10ml/50 lbs on day 1 then 5ml/50 lbs days 2-5.
Albon®[ Albon boluses -5 gm and 15 gmDose rate - 1 gm per 40 lbs day 1 then reduce dosage by half for days 2-5.
Albon®[ Albon soluble powder ] in 107 gm pkts - Labeled for drinking water. One 107 gm pkt medicates 50 gallons of water. As a drench, disolve one pkt (107 gms) in two cups of water, dose at 13 ml/cc per 100 pounds on day 1 and 6.5 ml/cc days 2-5, or, 1.5 cc/ml per 10 pounds day 1 then 3/4 cc/ml days 2-5 (keep refrigerated).
top
References Sulfonamides
OTHER COMMONLY USED BRAND NAMES OR VETERINARY LABELED SULFA PRODUCTS
Albon-S.R. [Sulfadimethoxine]
Albon Tablets [Sulfadimethoxine]
Bovazine SR Calf Bolus [Sulfamethazine] Bovazine SR Cattle Bolus [Sulfamethazine]
Calfspan [Sulfamethazine]
CalfSpan [Sulfamethazine]
Di-Methox 12.5% Oral Solution [Sulfadimethoxine]
Di-Methox Injection-40% [Sulfadimethoxine]
Hava-Span [Sulfamethazine]
Liquid Sulfa-Nox [Sulfaquinoxaline]
Powder 21 [Sulfamethazine and Sulfathiazole]
S-125 [Sulfadimethoxine]
S-250 [Sulfadimethoxine]
S-M-T [Sulfamethazine and Sulfathiazole]
Sulfa 2 [Sulfamethazine and Sulfathiazole] Sulfa "25" [Sulfamethazine]
Sulfa 25% [Sulfamethazine]
Sulfalean [Sulfamethazine and Sulfathiazole]
Sulfa-Max III [Sulfamethazine]
Sulfa-Max III Calf Bolus [Sulfamethazine] 2 Sulfamed [Sulfamethazine and Sulfathiazole]
Sulfa MT [Sulfamethazine and Sulfathiazole]
Sulfa-Q20% [Sulfaquinoxaline]
Sulfasol [Sulfadimethoxine]
Sulfasure [Sulfamethazine]
Sulfasure SR [Sulfamethazine]
Sulfasure SR Calf Bolus [Sulfamethazine]
SulfaTech Calf Bolus [Sulfamethazine]
SulfaTech Cattle Bolus [Sulfamethazine]
Sulforal [Sulfadimethoxine] Sulmet Drinking Water Solution [Sulfamethazine]
Sulmet Oblets [Sulfamethazine]
Sulmet Soluble Powder [Sulfamethazine] 34% Sul-Q-Nox [Sulfaquinoxaline]
Sulquin 6-50 [Sulfaquinoxaline]
Suprasulfa III Calf Bolus [Sulfamethazine]
Suprasulfa SR [Sulfamethazine]
Sustain III [Sulfamethazine]
Sustain III Calf Bolus [Sulfamethazine]
Triple Sulfa Bolus [Sulfamethazine, Sulfanilamide, and Sulfathiazole]
Vetisulid [Sulfachlorpyridazine]
Vetisulid Boluses [Sulfachlorpyridazine]
Vetisulid Powder [Sulfachlorpyridazine
References for Page 4
--------------------------------------------------------------------------------
x
ORAL ANTIBIOTICS/ANTIBACERIALS
Use of Antimicrobials in Food Animals
(Special Report by AABP)
"The antibiotic era is barely 60 years old, yet the inappropriate use of these drugs threatens our ability to cope with infections"
Drs. R.P. Wenzel and M.B. Edmond
Virginia Commonwealth University
Sulfonamides
Drug Family: Folic Acid Inhibitors
References Sulfonamides
Sulfonamides are broad-spectrum antimicrobials inhibiting both gram-positive and gram-negative bacteria, as well as some protozoa, such as coccidia. Sulfonamides are widely distributed throughout the body, and cross the placenta (some teratogenic effects have been seen when very high doses were given to pregnant mice and rats).
NOTE: Sulfaquinoxaline is minimally absorbed systemically and is referred to as an enteric sulfonamide.
Resistance of animal pathogens to sulfonamides is widespread as a result of more than 50 years of therapeutic use and this limits their effectiveness. Cross-resistance between sulfonamides is considered complete. BACTERIOSTATIC.....
--------------------------------------------------------------------------------
Sulfamethoxazole/Trimethoprim & Sulfadiazine/Trimethoprim combo's listed becuase they are so frequently used.
Data and studies indicate that
Trimethoprim is inactivated after oral administration in ruminants.
This occurs also with the sulfa-trimethoprim combinations that have been used orally in extralabel applications (Byrne, personal communic. 1999) in ruminants.
. TRIMETHOPRIM/SULFAMETHOXAZOLE - Rx item
BRAND NAMES : Septra® Uroplus® SS
TMP/SMX Sulfamethoprim® Cotrim® (Canada & US)
TMP/SMZ Sulfatrim® Cotrim® DS(Canada & US)
Bactrim® Sulfatrim® DS Di-Trim® (Canada & US)
Septra® DS Uroplus® DS
Antibacterial, systemic --Sulfadiazine and Trimethoprim; Sulfamethoxazole and Trimethoprim
Antiprotozoal --Sulfamethoxazole and Trimethoprim
TRIMETHOPRIM/SULFADIAZINE- Rx item
BRAND NAMES : TMP/SDZ Tribrissen®
Cotrim® (Canada Cotrim® DS (Canada) Di-Trim® (Canada)
Antibacterial, systemic --Sulfadiazine and Trimethoprim; Sulfamethoxazole and Trimethoprim
--------------------------------------------------------------------------------
DOSE : 30mg/kg (665mg/50 pounds) twice daily . The most common tablets are 960mg. = one 960mg tablet per 70-75 pounds twice daily.
Plasma levels are achieved in approximately 6 hours following oral dosage.
A broad spectrum antioibiotic and sulfa combination with a wide spectrum of activity against gram neagtive and positive organisims. Sulfonamides (sulfadiazine and sulfamethoxazole) are bacteriostatic and trimethoprim is bacteriocidal. In combination, they are bacteriocidal.
Effective against Actinomyces spp., B. anthracis, Bordetella, Brucella, Clostridia, Corynebacterium, e-coli , Haemophillus, Klebsiella, pasturella, Proteus, Salmonella spp., Staphylococci. Streptococci and Vibro spp.
For respiratory, urinary tract, skin, and gastrointestinal infections, and infections with coccidia.
There is some question about the oral use of trimethoprim in ruminents. Some thoughts are that it is perhaps significantly degraded in the rumen.
CONTRAINDICATIONS : Untreated dehydration.
CAUTION: Prolonged use may decrease thyroid function and affect tear production in the eye.
Store at room temperature in a tight container.
Not approved for lactating animals in the US.
WITHDRAWAL (cattle) (Canada) - 3 days for T/sulfadiazine, 10 days T/sulfadoxine.
MILK DISCARD (cattle) (Canada) - 96 hours for T/sulfadiazine or T/sufladoxine.
--------------------------------------------------------------------------------
Vet. Res. 32 (2001) 261-273
(Received 7 December 2000; accepted 7 February 2001)
Resistance to trimethoprim and sulfonamides
Ola Sköld
Division of Microbiology, Department of Pharmaceutical Biosciences, Biomedical Center, Uppsala University, PO Box 581, SE-751 23 Uppsala, Sweden
Abstract
Sulfonamides and trimethoprim have been used for many decades as efficient and inexpensive antibacterial agents for animals and man. Resistance to both has, however, spread extensively and rapidly. This is mainly due to the horizontal spread of resistance genes, expressing drug-insensitive variants of the target enzymes dihydropteroate synthase and dihydrofolate reductase, for sulfonamide and trimethoprim, respectively. Two genes, sul1 and sul2, mediated by transposons and plasmids, and expressing dihydropteroate synthases highly resistant to sulfonamide, have been found. For trimethoprim, almost twenty phylogenetically different resistance genes, expressing drug-insensitive dihydrofolate reductases have been characterized. They are efficiently spread as cassettes in integrons, and on transposons and plasmids. One particular gene, dfr9, seems to have originally been selected in the intestine of swine, where it was found in Escherichia coli, on large plasmids in a disabled transposon, Tn5393, originally found in the plant pathogen Erwinia amylovora . There are also many examples of chromosomal resistance to sulfonamides and trimethoprim, with different degrees of complexity, from simple base changes in the target genes to transformational and recombinational exchanges of whole genes or parts of genes, forming mosaic gene patterns. Furthermore, the trade-off, seen in laboratory experiments selecting resistance mutants, showing drug-resistant but also less efficient (increased Ks) target enzymes, seems to be adjusted for by compensatory mutations in clinically isolated drug-resistant pathogens. This means that susceptibility will not return after suspending the use of sulfonamide and trimethoprim.
--------------------------------------------------------------------------------
.. SULFAQUINOXALINE [20% solution] - Coccidia treatment.
DOSE 6mg/lb daily for 5 days.
for SULFAQUINOXALINE 20% solution (200 mg per mL) :
Drench: 2ml/50 lbs orally for 5 days.
Water: 1oz/10 gallons (animals will need to drink 1 quart of solution for each 25 lbs of body weight to get an effective dose).
NOTE: Sulfaquinoxaline is minimally absorbed systemically and is referred to as an enteric (Of, relating to, or being within the intestine) sulfonamide.
--------------------------------------------------------------------------------
PRODUCT RECALL: June 2000 -
PRODUCT Hess & Clark brand 20% Sulfaquinoxaline Sodium Solution, in 16-ounce bottles, product is added to drinking water to teat infections in chickens, turkeys, cattle and calves.
CODE Lot #07397 EXP OCT 02.
MANFACTURER Hess & Clark Inc., Ashland, Ohio.
DISTRIBUTION Alabama, Oklahoma, Missouri, Hawaii, Pennsylvania, Iowa, Kansas, Ohio, and Texas.
QUANTITY 27 cases (12 bottles per case) were distributed.
REASON An extended expiration date was used on the label. Stability data existed only for 2 years as packaged in 16-ounce bottles.
--------------------------------------------------------------------------------
VETERINARY PRODUCTS/BRAND NAMES :
note the different strengths
34.4 mg per mL (OTC) [liquid Sulfa-Nox].Dose: 11.5mL/50 lbs
200 mg per mL (OTC) [Sulfa-Q20%; GENERIC] Dose: 2mL/50 lbs
286.2 mg per mL - (29% solution) (OTC) [Sulquin 6-50] Dose: 1.4 (1.5)mL/50 lbs
340 mg per mL (OTC) [34% Sul-Q-Nox]. Dose: 1.1mL/50 lbs
.MEAT WITHOLDING: 10 days.
...... ALBON® & DI-METHOX® [both are sulfadimethoxine]. For coccidia and scours.
DOSE : 25 mg of sulfadimethoxine per pound (55mg/kg) day one, 12.5mg per lb (27mg.kg) days 2-5.
Also used for pneumonia and misc. bacterial infectious processes.
See injectable Albon (Albon Injection-40%) information under Injectable Antibiotics.
WITHDRAWAL (boluses) : Meat 7 days. Milk discard 60 hours.
Albon®[ Albon 12.5% solution ]Dose rateof the 12.5% oral solution is 10ml/50 lbs on day 1 then 5ml/50 lbs days 2-5.
Albon®[ Albon boluses -5 gm and 15 gmDose rate - 1 gm per 40 lbs day 1 then reduce dosage by half for days 2-5.
Albon®[ Albon soluble powder ] in 107 gm pkts - Labeled for drinking water. One 107 gm pkt medicates 50 gallons of water. As a drench, disolve one pkt (107 gms) in two cups of water, dose at 13 ml/cc per 100 pounds on day 1 and 6.5 ml/cc days 2-5, or, 1.5 cc/ml per 10 pounds day 1 then 3/4 cc/ml days 2-5 (keep refrigerated).
top
References Sulfonamides
OTHER COMMONLY USED BRAND NAMES OR VETERINARY LABELED SULFA PRODUCTS
Albon-S.R. [Sulfadimethoxine]
Albon Tablets [Sulfadimethoxine]
Bovazine SR Calf Bolus [Sulfamethazine] Bovazine SR Cattle Bolus [Sulfamethazine]
Calfspan [Sulfamethazine]
CalfSpan [Sulfamethazine]
Di-Methox 12.5% Oral Solution [Sulfadimethoxine]
Di-Methox Injection-40% [Sulfadimethoxine]
Hava-Span [Sulfamethazine]
Liquid Sulfa-Nox [Sulfaquinoxaline]
Powder 21 [Sulfamethazine and Sulfathiazole]
S-125 [Sulfadimethoxine]
S-250 [Sulfadimethoxine]
S-M-T [Sulfamethazine and Sulfathiazole]
Sulfa 2 [Sulfamethazine and Sulfathiazole] Sulfa "25" [Sulfamethazine]
Sulfa 25% [Sulfamethazine]
Sulfalean [Sulfamethazine and Sulfathiazole]
Sulfa-Max III [Sulfamethazine]
Sulfa-Max III Calf Bolus [Sulfamethazine] 2 Sulfamed [Sulfamethazine and Sulfathiazole]
Sulfa MT [Sulfamethazine and Sulfathiazole]
Sulfa-Q20% [Sulfaquinoxaline]
Sulfasol [Sulfadimethoxine]
Sulfasure [Sulfamethazine]
Sulfasure SR [Sulfamethazine]
Sulfasure SR Calf Bolus [Sulfamethazine]
SulfaTech Calf Bolus [Sulfamethazine]
SulfaTech Cattle Bolus [Sulfamethazine]
Sulforal [Sulfadimethoxine] Sulmet Drinking Water Solution [Sulfamethazine]
Sulmet Oblets [Sulfamethazine]
Sulmet Soluble Powder [Sulfamethazine] 34% Sul-Q-Nox [Sulfaquinoxaline]
Sulquin 6-50 [Sulfaquinoxaline]
Suprasulfa III Calf Bolus [Sulfamethazine]
Suprasulfa SR [Sulfamethazine]
Sustain III [Sulfamethazine]
Sustain III Calf Bolus [Sulfamethazine]
Triple Sulfa Bolus [Sulfamethazine, Sulfanilamide, and Sulfathiazole]
Vetisulid [Sulfachlorpyridazine]
Vetisulid Boluses [Sulfachlorpyridazine]
Vetisulid Powder [Sulfachlorpyridazine
References for Page 4