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Status:
US Approved Rx
(1983)
First approved in 1983
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Hemin (trade name Panhematin) is a protoporphyrin IX containing a ferric iron ion (heme B) with a chloride ligand, which is is indicated for the amelioration of recurrent attacks of acute intermittent porphyria temporally related to the menstrual cycle in susceptible women. Manifestations such as pain, hypertension, tachycardia, abnormal mental status and mild to progressive neurologic signs may be controlled in selected patients with this disorder. the therapy for the acute porphyrias is not curative. Heme acts to limit the hepatic and/or marrow synthesis of porphyrin. This action is likely due to the inhibition of δ-aminolevulinic acid synthetase, the enzyme which limits the rate of the porphyrin/heme biosynthetic pathway. The exact mechanism by which hematin produces symptomatic improvement in patients with acute episodes of the hepatic porphyrias has not been elucidated.
Status:
US Approved Rx
(1991)
Source:
NDA019998
(1991)
Source URL:
First approved in 1982
Source:
NDA214993
Source URL:
Class (Stereo):
CHEMICAL (MIXED)
Targets:
Conditions:
Succimer is an analogue of dimercaprol, and has replaced dimercaprol as one of the main antidotes used in the management of poisoning by lead and other heavy metals. The advantages of succimer are that it is effective by oral administration because it is soluble in water, it is well-tolerated, has relatively low toxicity and can be given at the same time as iron supplements to treat iron deficiency anaemia. It does not cause significant increase in urinary excretion of essential minerals unlike the other widelyused lead chelating agent, sodium calcium EDTA.
Status:
US Approved Rx
(2020)
Source:
ANDA206997
(2020)
Source URL:
First approved in 1982
Source:
NDA018602
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Diltiazem is a nondihydropyridines calcium channel blocker used in the treatment of hypertension, angina pectoris, and some types of arrhythmia. Diltiazem produces its antihypertensive effect primarily by relaxation of vascular smooth muscle and the resultant decrease in peripheral vascular resistance.
Status:
US Approved Rx
(2014)
Source:
ANDA204605
(2014)
Source URL:
First approved in 1982
Source:
ZOVIRAX by GLAXOSMITHKLINE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Acyclovir is a synthetic antiviral nucleoside analogue. A screening program for antiviral drugs begun at Burroughs Wellcome in the 1960s resulted in the discovery of acyclovir in 1974. Preclinical investigation brought the drug to clinical trials in 1977 and the first form of the drug (topical) was available to physicians in 1982. Activity of acyclovir is greatest against herpes 1 and herpes 2, less against varicella zoster, still less against Epstein-Barr, and very little against cytomegalovirus. Acyclovir is an antiviral agent only after it is phosphorylated in infected cells by a viral-induced thymidine kinase. Acyclovir monophosphate is phosphorylated to diphosphate and triphosphate forms by cellular enzymes in the infected host cell where the drug is concentrated. Acyclovir triphosphate inactivates viral deoxyribonucleic acid polymerase.
Status:
US Approved Rx
(2017)
Source:
ANDA206136
(2017)
Source URL:
First approved in 1982
Source:
NDA018147
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Piroxicam is in a class of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). It was originally brought to market by Pfizer under the tradename Feldene in 1980, became generic in 1992, and is marketed worldwide under many brandnames. Piroxicam works by reducing hormones that cause inflammation and pain in the body. Piroxicam is used to reduce the pain, inflammation, and stiffness caused by rheumatoid arthritis and osteoarthritis. The antiinflammatory effect of Piroxicam may result from the reversible inhibition of cyclooxygenase, causing the peripheral inhibition of prostaglandin synthesis. The prostaglandins are produced by an enzyme called Cox-1. Piroxicam blocks the Cox-1 enzyme, resulting into the disruption of production of prostaglandins. Piroxicam also inhibits the migration of leukocytes into sites of inflammation and prevents the formation of thromboxane A2, an aggregating agent, by the platelets. Piroxicam is used for treatment of osteoarthritis and rheumatoid arthritis.
Status:
US Approved Rx
(2020)
Source:
ANDA214219
(2020)
Source URL:
First approved in 1982
Source:
NDA017892
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Triazolam is a short-acting benzodiazepine used as a hypnotic agent in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. Triazolam has a shorter half-life than chlordiazepoxide, flurazepam, and prazepam and does not generate active metabolites. Benzodiazepines bind nonspecifically to bezodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. Triazolam is used for the short-term treatment of insomnia. Triazolam`s original brand name is Halcion. Triazolam is withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions. This drug continues to be available in the U.S. Internationally, triazolam is a Schedule IV drug under the Convention on Psychotropic Substances.
Status:
US Approved Rx
(2017)
Source:
ANDA203547
(2017)
Source URL:
First approved in 1982
Source:
DOLOBID by MERCK
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Diflunisal is a salicylic acid derivative with analgesic and anti-inflammatory activity. It was developed by Merck Sharp & Dohme in 1971 after showing promise in a research project studying more potent chemical analogs of aspirin. Diflunisal is an aspirin-like nonsteroidal anti-inflammatory drug that inhibits cyclooxygenase-2 (COX-2), an enzyme involved in prostaglandin synthesis.In animals, prostaglandins sensitize afferent nerves and potentiate the action of bradykinin in inducing pain. Since prostaglandins are known to be among the mediators of pain and inflammation, the mode of action of diflunisal may be due to a decrease of prostaglandins in peripheral tissues.
Status:
US Approved Rx
(1994)
Source:
ANDA074063
(1994)
Source URL:
First approved in 1982
Source:
VISKEN by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Pindolol was developed at Sandoz at 1960s. Pindolol is a nonselective beta-adrenergic antagonist (beta-blocker) which possesses intrinsic sympathomimetic activity (partial agonist activity) in therapeutic dosage ranges but does not possess quinidine-like membrane stabilizing activity. The partial beta-adrenergic agonistic activity of pindolol in the heart appears to be completely restricted to the sinoatrial pacemaker. In standard pharmacologic tests in man and animals, Pindolol attenuates increases in heart rate, systolic blood pressure, and cardiac output resulting from exercise and isoproterenol administration, thus confirming its beta-blocking properties. In addition to beta-adrenergic activity pindolol demonstrates mixed agonist-antagonist activity at central 5-HT receptors. Although in accordance with the hypothesis that pindolol increases the antidepressant effects of selective serotonin reuptake inhibitors by antagonism of 5-HT at inhibitory 5-HT1A autoreceptors, pindolol possesses partial agonist activity at 5-HT1A receptors. Pindolol tablets are indicated in the management of hypertension.
Status:
US Approved Rx
(2012)
Source:
ANDA091559
(2012)
Source URL:
First approved in 1982
Source:
OVIDE by TARO
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Malathion is an organophosphate insecticide, an inhibitor of cholinesterase. In low doses (0.5%) malathion is used for treatment of pediculosis and scabies.
Status:
US Approved Rx
(2002)
Source:
ANDA076005
(2002)
Source URL:
First approved in 1982
Source:
SPECTAZOLE by ALVOGEN
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Econazole (commonly used as the nitrate salt) is an antifungal medication of the imidazole class. It is a broad spectrum antimycotic with some action against Gram positive bacteria. It is used topically in dermatomycoses also orally and parenterally. Sold under the brand name Ecoza among others, it is indicated for the treatment of interdigital tinea
pedis caused by Trichophyton rubrum, Trichophyton mentagrophytes, and
Epidermophyton floccosum in patients 12 years of age and older. Econazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Econazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.