U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1 - 10 of 12 results

Tigecycline (INN) is an antibiotic used to treat a number of bacterial infections. It is a first in class glycylcycline that is administered intravenously. For the treatment of infections caused by susceptible strains of the designated microorganisms in the following conditions: Complicated skin and skin structure infections caused by Escherichia coli, Enterococcus faecalis (vancomycin-susceptible isolates only), Staphylococcus aureus (methicillin-susceptible and -resistant isolates), Streptococcus agalactiae, Streptococcus anginosus grp. (includes S. anginosus, S. intermedius, and S. constellatus), Streptococcus pyogenes and Bacteroides fragilis. Complicated intra-abdominal infections caused by Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Klebsiella oxytoca, Klebsiella pneumoniae, Enterococcus faecalis (vancomycin-susceptible isolates only), Staphylococcus aureus (methicillin-susceptible isolates only), Streptococcus anginosus grp. (includes S. anginosus, S. intermedius, and S. constellatus), Bacteroides fragilis, Bacteroides thetaiotaomicron, Bacteroides uniformis, Bacteroides vulgatus, Clostridium perfringens, and Peptostreptococcus micros. Tigecycline, a glycylcycline, inhibits protein translation in bacteria by binding to the 30S ribosomal subunit and blocking entry of amino-acyl tRNA molecules into the A site of the ribosome. This prevents incorporation of amino acid residues into elongating peptide chains. Tigecycline carries a glycylamido moiety attached to the 9-position of minocycline. The substitution pattern is not present in any naturally occurring or semisynthetic tetracycline and imparts certain microbiologic properties to tigecycline. In general, tigecycline is considered bacteriostatic; however, TYGACIL has demonstrated bactericidal activity against isolates of S. pneumoniae and L. pneumophila. In vitro studies have not demonstrated antagonism between tigecycline and other commonly used antibacterials.
Status:
First approved in 1959
Source:
Declomycin by Lederle
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Demeclocycline hydrochloride is an antibiotic isolated from a mutant strain of Streptomyces aureofaciens. It inhibits protein synthesis by binding with the 30S and possibly the 50S ribosomal subunit(s) of susceptible bacteria. Demeclocycline has antimicrobial activity against a wide range of gram-negative and gram-positive organisms. Demeclocycline is indicated in the treatment of infections caused by susceptible strains of the designated microorganisms. Demeclocycline is currently used to treat hyponatremia in patients with the syndrome of inappropriate antidiuretic hormone secretion (SIADH). Demeclocycline mainly attenuates hyponatremia in SIADH by reducing adenylate cyclase 5/6 expression and, consequently, cAMP generation, AQP2 gene transcription, and AQP2 abundance in the renal inner medulla, coinciding with a reduced vasopressin escape response in other collecting duct segments.
Status:
US Approved OTC
Source:
21 CFR 333.110(c) first aid antibiotic:ointment chlortetracycline hydrochloride
Source URL:
First approved in 1948
Source:
Aureomycin Calcium by Lederle
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Chlortetracycline (trade name Aureomycin, Lederle) is a tetracycline antibiotic, the first tetracycline to be identified. It was discovered in 1945 by Benjamin Minge Duggar working at Lederle Laboratories under the supervision of Yellapragada Subbarow. Duggar identified the antibiotic as the product of an actinomycete he cultured from a soil sample collected from Sanborn Field at the University of Missouri. The organism was named Streptomyces aureofaciens and the isolated drug, Aureomycin, because of their golden color. Chlortetracycline inhibits cell growth by inhibiting translation. It binds to the 16S part of the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. In veterinary medicine, chlortetracycline is commonly used to treat conjunctivitis in cats.
Status:
US Previously Marketed
Source:
RONDOMYCIN by MEDPOINTE PHARM HLC
(1966)
Source URL:
First approved in 1966

Class (Stereo):
CHEMICAL (ABSOLUTE)



Methacycline is a tetracycline antibiotic. Similar to other tetracyclines, it has a wide spectrum of antimicrobial action. It is active against most Gram-positive bacteria (pneumococci, streptococci, staphylococci) and Gram-negative bacteria (E. coli, salmonella, shigella, etc.), and towards agents causing onithosis, psittacosis, trachoma, and some Protozoa. Like other tetracyclines, the general usefulness of methacycline has been reduced with the onset of bacterial resistance. Methacycline inhibits the binding of aminoacyl-tRNA to the mRNA-ribosome complex. Methacycline inhibits cell growth by inhibiting translation. It binds to the 16S part of the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. Methacycline is mostly used for the treatment of acute bacterial exacerbations of chronic bronchitis.
Status:
US Previously Marketed
Source:
Syntetrin by Bristol
(1959)
Source URL:
First approved in 1959
Source:
Syntetrin by Bristol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Rolitetracycline, launched in the late 1950s, was the first of the semi -synthetic tetracyclines. Rolitetracycline is formed by a Mannich condensation of formaldehyde and pyrrolidine with tetracycline. Rolitetracycline is a pro -drug of tetracycline, in which the pyrrolidine moiety improves bioavailability compared with tetracycline. Rolitetracycline has broad spectrum Gram positive activity in vivo, but pH instability limits use to parenteral administration. Rolitetracycline passively diffuses through porin channels in the bacterial membrane and reversibly binds to the 30S ribosomal subunit, preventing binding of tRNA to the mRNA-ribosome complex, and thus interfering with protein synthesis.
Status:
Possibly Marketed Outside US
Source:
Penimepicyclina by Elenco Farmaci
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Penimepicycline is a salt of beta-lactam antibiotic penicillin V and tetracycline antibiotic pipacycline. Penimepicycline exerts a bactericidal action on the streptococci, and a bacteriostatic action on various gram-positive and gram-negative bacilli, as well as on the penicillin-resistant staphylococci. In the 1960s it was studied in Japan for the treatment of urological, respiratory, gynecological and other infections.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Clomocycline is the approved name of a methylol derivative of chlortetracycline. Clomocycline is a tetracycline antibiotic that is commonly prescribed by medical doctors for infections and to treat acne. It may also be used to treat urinary tract infections, gum disease, and other bacterial infections such as gonorrhea and chlamydia. Clomocycline is also used commonly as a prophylactic treatment for infection by Bacillus anthracis (anthrax). It is also effective against Yersinia pestis and malaria and is also prescribed for the treatment of Lyme disease. Clomocycline inhibits cell growth by inhibiting translation. It binds to the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. The binding is reversible in nature. Clomocycline is lipophilic and can easily pass through the cell membrane or passively diffuses through porin channels in the bacterial membrane. This drug has been reported to be noticeably free of side-effects such as nausea, vomiting, and diarrhea.
Status:
Possibly Marketed Outside US
Source:
NCT01661985: Phase 4 Interventional Unknown status Urethritis
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Lymecycline is a tetracycline broad-spectrum antibiotic marketed by the pharmaceutical company Galderma. It is approximately 5,000 times more soluble than tetracycline base and is unique amongst tetracyclines in that it is absorbed by an active transport process across the intestinal wall, making use of the same fast and efficient mechanism by which carbohydrates are absorbed. Lymecycline's side effects can include rash, headache, diarrhoea, ulcerative colitis, nausea, vomiting, dermatitis, dysphasia, inflammation of the liver, hypersensitive reactions, and visual disturbances. When taken for a long period of time, it can cause reflux oesophagitis.
Minocycline is a tetracycline analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant staphylococcus infections. Minocycline has many brand names one of them is minocin, Minocin is indicated in the treatment of the following infections due to susceptible isolates of the designated bacteria: Rocky Mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsialpox and tick fevers caused by rickettsiae. Respiratory tract infections caused by Mycoplasma pneumoniae. Lymphogranuloma venereum caused by Chlamydia trachomatis. Psittacosis (Ornithosis) due to Chlamydophila psittaci etc. Minocycline is indicated for the treatment of infections caused by the following Gram-negative bacteria when bacteriologic testing indicates appropriate susceptibility to the drug: Escherichia coli. Enterobacter aerogenes. Shigella species etc. MINOCIN also is indicated for the treatment of infections caused by the following Gram-positive bacteria when bacteriologic testing indicates appropriate susceptibility to the drug: Upper respiratory tract infections caused by Streptococcus pneumoniae. Skin and skin structure infections caused by Staphylococcus aureus (Note: Minocycline is not the drug of choice in the treatment of any type of staphylococcal infection, etc. When penicillin is contraindicated, minocycline is an alternative drug in the treatment of the following infections: Meningitis due to Neisseria meningitidis. Syphilis caused by Treponema pallidum subspecies pallidum. Yaws caused by Treponema pallidum subspecies pertenue, etc. Minocycline passes directly through the lipid bilayer or passively diffuses through porin channels in the bacterial membrane. Minocycline inhibits protein synthesis by binding to 30S and possibly 50S ribosomal subunits of susceptible bacteria.
Doxycycline hyclate (Vibramycin, Periostat, Vibra-Tabs) is salt of tetracycline antibiotic Doxycycline, that used to treat many kinds of infections, like dental, skin, respiratory, and urinary tract infections. It also treats acne, Lyme disease, malaria, and certain sexually transmitted diseases. Doxycycline hyclate is a light-yellow crystalline powder which is soluble in water, while doxycycline monohydrate is very slightly soluble in water. Doxycycline is bacteriostatic, inhibiting bacterial protein synthesis due to disruption of transfer RNA and messenger RNA at ribosomal sites. Doxycycline hyclate is indicated for use in the treatment of chronic adult periodontitis for a gain in clinical attachment, reduction in probing depth, and reduction in bleeding on probing.

Showing 1 - 10 of 12 results