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Status:
US Previously Marketed
Source:
TENATHAN by ROBINS AH
(1981)
Source URL:
First approved in 1981
Source:
TENATHAN by ROBINS AH
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Bethanidine is a post-ganglionic adrenergic neurone-blocking agent which exerts a marked postural hypotensive effect. The precise mechanism whereby bethanidine causes blockade of adrenergic neurones is unknown. An initial sympathomimetic effect has been demonstrated in man and animals, possibly due to release of catecholamines.
Status:
US Previously Marketed
Source:
MEZLIN by BAYER PHARMS
(1982)
Source URL:
First approved in 1981
Source:
MEZLIN by BAYER PHARMS
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Bayer developed MEZLOCILLIN (previously known as BAYPEN); it is a semisynthetic ampicillin-derived penicillin. Mezlocillin is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The bactericidal activity of mezlocillin results from the inhibition of cell wall synthesis and is mediated through mezlocillin binding to penicillin binding proteins (PBPs). Mezlocillin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases and cephalosporinases and extended spectrum beta-lactamases. Mezlocillin was poorly absorbed orally and was given either intramuscularly or intravenously. This drug was discontinued in the U.S.
Status:
US Previously Marketed
Source:
PAXIPAM by SCHERING
(1981)
Source URL:
First approved in 1981
Source:
PAXIPAM by SCHERING
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Halazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Halazepam is used to relieve anxiety, nervousness, and tension associated with anxiety disorders. Halazepam (Paxipam) is no longer commercially available in the United States. Common adverse effects are: hypotension, nausea, xerostomia, confusion, headache. Alcohol should be avoided while taking Paxipam as it causes drowsiness as well. Medications that also cause drowsiness should not be taken along with Paxipam. These include: Antidepressants, Pain relievers, Seizure medications, Muscle relaxants, Antihistamines, Sleeping pills and sedatives.
Status:
US Previously Marketed
Source:
CHOLOVUE by BRACCO
(1981)
Source URL:
First approved in 1981
Source:
CHOLOVUE by BRACCO
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Iodoxamic acid (previously sold under the brand name Cholovue) is an organoiodine compound that was used as a contrast medium. It is intravenous cholecystocholangiographic
agent. It features both a high iodine content as well as several hydrophilic groups.
Status:
US Previously Marketed
Source:
EMCYT by PHARMACIA AND UPJOHN
(1981)
Source URL:
First approved in 1981
Source:
EMCYT by PHARMACIA AND UPJOHN
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Estramustine is an antineoplastic agent indicated in the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate. Estramustine is a combination of estradiol with nitrogen mustard. In vivo, the nitrogen-mustard moiety becomes active and participates in alkylation of DNA or other cellular components. This causes DNA damage in rapidly dividing cancerous cells leading to cell death and ideally, tumor shrinkage. Also, due to the drugs estrogen component, it can bind more selectively to active estrogen receptors. Used for the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate.
Status:
US Previously Marketed
Source:
MECLAN by JOHNSON AND JOHNSON
(1980)
Source URL:
First approved in 1980
Source:
MECLAN by JOHNSON AND JOHNSON
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Meclocycline is a tetracycline antibiotic. It is used topically for skin infections treatment. Tetracyclines are broad-spectrum bacteriostatic agents and act by inhibiting protein synthesis by blocking the binding of aminoacyl tRNA (transfer RNA) to the mRNA (messenger RNA) ribosome complex. Meclocycline might increase sensitivity to light when it is used with Aminolevulinic acid.
Status:
US Previously Marketed
Source:
SPECTROBID by PFIZER
(1980)
Source URL:
First approved in 1980
Source:
SPECTROBID by PFIZER
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
Conditions:
Bacampicillin is a penicillin antibiotic. It is a prodrug of ampicillin with improved oral bioavailability. It exerts bactericidal activity via inhibition of bacterial cell wall synthesis by binding one or more of the penicillin binding proteins (PBPs). Spectrobid is used to treat bacterial infections such as tonsillitis, pneumonia (lung infection), bronchitis (inflammation of airway), urinary tract infections, gonorrhea, and infections of the skin. Adverse effects are: anemia, thrombocytopenia, neutropenia, agranulocytosis, seizures, nephrotoxicity, Jarisch-Herxheimer Reaction (fever, chills, sweating, tachycardia, hyperventilation, flushing, and myalgia). Drug interactions: Contraceptives - decreased contraceptive effectiveness; Live Typhoid Vaccine - decreased immunological response to the typhoid vaccine; Probenecid - increased bacampicillin levels.
Status:
First approved in 1980
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Ritodrine (trade name Yutopar) is beta-2 adrenergic agonist used to stop premature labor. Ritodrine binds to beta-2 adrenergic receptors on the outer membrane of the myometrial cell, activates adenyl cyclase to increase the level of cAMP which decreases intracellular calcium and leads to a decrease of uterine contractions. In addition to stimulating the beta-2–adrenergic receptors of the uterine smooth muscle, ritodrine stimulates beta-adrenergic receptors of bronchial and vascular smooth muscles. The cardiostimulatory effects, including increased cardiac output, increased maternal and fetal heart rates, and widening of the maternal pulse pressure, are probably due to relaxation of the vascular smooth muscle. Relaxation of vascular smooth muscle stimulates the beta-1–adrenergic receptors and the reflex response to blood pressure. Also, during intravenous administration, ritodrine transiently increases maternal and fetal blood glucose and maternal plasma insulin concentrations. Other metabolic changes include increased cAMP, lactic acid, and free fatty acids, and decreased serum potassium concentration. Most side effects of β2 agonists result from their concurrent β1 activity and include the increase in heart rate, rise in systolic pressure, decrease in diastolic pressure, chest pain secondary to myocardial infarction, and arrhythmia. Beta-agonists may also cause fluid retention secondary to decrease in water clearance, which when added to the tachycardia and increased myocardial work, may result in heart failure. In addition, they increase gluconeogenesis in the liver and muscle resulting in hyperglycemia, which increases insulin requirements in diabetic patients. The passage of β agonists through the placenta does occur and may be responsible for fetal tachycardia, as well as hypoglycemia or hyperglycemia at birth.
Status:
First approved in 1980
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Sisomicin is a new broad-spectrum aminoglycoside most closely related structurally to gentamicin C1a. In vitro and in experimental infections, sisomicin has been found to be more potent than or nearly as potent as the most active of the other available aminoglycosides. Although susceptible to many (but not all) aminoglycoside-inactivating enzymes, sisomicin is active against many microorganisms that are resistant to other aminoglycosides by nonenzymatic mechanisms. Sisomicin has been shown to interact synergistically with various beta-lactam antibiotics against enterococci, staphylocicci, Enterobacteriaceae, and nonfermentative gram-negative bacilli. The pharmacokinetics and toxicity of sisomicin in humans appear to be similar to those of gentamicin, despite earlier reports of greater acute toxicity in animals. Sisomicin binds to 30s and 50s ribosomal subunits of susceptible bacteria disrupting protein synthesis, thus rendering the bacterial cell membrane defective.
Status:
US Previously Marketed
Source:
DIPIVEFRIN HYDROCHLORIDE by FALCON PHARMS
(1994)
Source URL:
First approved in 1980
Source:
PROPINE by ALLERGAN
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Dipivefrin is a prodrug with little or no pharmacologically activity until it is hydrolyzed into epinephrine inside the human eye. The liberated epinephrine, an adrenergic agonist, appears to exert its action by stimulating α -and/or β2-adrenergic receptors, leading to a decrease in aqueous production and an enhancement of outflow facility. The dipivefrin prodrug delivery system is a more efficient way of delivering the therapeutic effects of epinephrine, with fewer side effects than are associated with conventional epinephrine therapy. Dipivefrin is used as initial therapy for the control of intraocular pressure in chronic open-angle glaucoma.