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

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Status:
Possibly Marketed Outside US
Source:
Japan:Bopindolol Malonate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Bopindolol (4-[benzoyloxy-3-tertbutylaminopropoxy]-2-methylindole hydrogen malonate) is an indole beta-adrenoceptor antagonist bearing a benzoyl ester residue on the beta-carbon atom of the propanolamine side chain. Bopindolol is metabolized by esterase to benzoic acid and an active metabolite, 18-502 [4-(3-t-butylamino-2-hydroxypropoxy)-2-methyl indole], which is further metabolized to 20-785 [4-(3-t-butylaminopropoxy)-2-carboxyl indole]. Bopindolol produces sustained blockade of beta 1- and beta 2-adrenoceptors, has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is used in the treatment of hypertension. In limited trials bopindolol has also successfully reduced symptoms in patients with angina pectoris, anxiety and essential tremor.
Status:
Possibly Marketed Outside US
Source:
Japan:Meprylcaine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Meprylcaine (also known as Epirocaine and Oracaine) is a local anesthetic with stimulant properties that is structurally related to dimethocaine. Meprylcaine has a relatively potent inhibitory action on the monoamine transporter and inhibits the reuptake of dopamine, norepinephrine and serotonin. Oracaine is commonly used as the hydrochloride salt and is compatible with the known vasoconstrictors. It has a slightly more rapid onset than procaine with a slight increase in potency. The earliest symptoms of a toxic overdose are stimulation to the central nervous system, thus following the same symptoms as procaine. Not more than 400 mg. (20 ml. of a 2 per cent solution) should be used at any one time for the ambulatory patient. Oracaine, like metycaine, may be used for patients sensitive to the para-aminobenzoic acid derivatives. Oracaine hydrochloride is used at present mainly by the dental profession and in dermatologic surgery.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)



Acedoben (4-acetamidobenzoic acid) is a benzoic acid derivative and a metabolite of benzocaine. It is a component of immunomodulatory drug inosine pranobex, which is used to treat mucocutaneous infections due to herpes simplex virus (type 1 and/or type II), genital warts as adjunctive therapy to podophyllin or carbon dioxide laser, and subacute sclerosing panencephalitis.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Pitofenone is a spasmolytic agent. It exerts anticholinesterase and antimuscarinic activities. Pitofenone is used to relieve pain and spasms of smooth muscles. Pitofenone is also used for the treatment of back pain, sprains, and strains. Pitofenone is used in combination along with fenpiverinium bromide, and metamizole sodium. The drug is currently sold in Eastern Europe and India under various trade names. The combined preparation possesses strong analgesic, spasmolytic, cholinolytic and anti-inflammatory effects on the smooth muscles predominantly of the gastrointestinal and urogenital tract. Indications are strong pain in gastric or intestinal colic, kidney and gallstones, and for painful menstruation. Pitofenone hydrochloride present in the combination exerts papaverin-like spasmolytic effect on the vascular and extra-vascular smooth muscles of the stomach, intestines, urinary tract, biliary tract, and uterus.
Status:
Possibly Marketed Outside US
Source:
Japan:p-Butylaminobenzoyldiethylaminoethyl Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


p-Butylaminobenzoyldiethylaminoethyl hydrochloride (T-cain) was the most frequently used local anesthetic for spinal anesthesia in Japan in the 1940s–1960s. The market for spinally administered T-cain is almost ended. T-cain is still used for topical/infiltrative anesthesia in some specialties. T-cain may also be used as an alternative in patients who are allergic to lidocaine or bupivacaine. The side effects reported for spinal use of Neo Percamin S (T-cain with dibucaine) were hypotension, bradycardia, respiratory arrest, and allergy.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Zofenopril is an inhibitor of Angiotensin Converting Enzyme (ACE), which is approved in Europe for the treatment of hypertension and acute myocardial infarction.
Gentamicin C1 is a part of gentamicin C complex, containing gentamicin C1, gentamicin C1a, and gentamicin C2 which compose approximately 80% of gentamicin and have been found to have the highest antibacterial activity. Commercial gentamicin C is a mixture of gentamicin C1, C1a, and C2. Gentamicin C1 has a methyl group in the 6' position of the 2-amino-hexose ring and is N methylated at the same position. Gentamicin is a broad spectrum aminoglycoside antibiotic. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses. Aminoglycosides like gentamicin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically gentamicin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes. Gentamicin complex is used for treatment of serious infections caused by susceptible strains of the following microorganisms: P. aeruginosa, Proteus species (indole-positive and indole-negative), E. coli, Klebsiella-Enterobactor-Serratia species, Citrobacter species and Staphylococcus species (coagulase-positive and coagulase-negative).