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

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Showing 81 - 90 of 129 results

Like other thiazides, chlorothiazide promotes water loss from the body (diuretics). It inhibits Na /Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue. Chlorothiazide affects the distal renal tubular mechanism of electrolyte reabsorption. At maximal therapeutic dosages, all thiazides are approximately equal in their diuretic efficacy. Chlorothiazide increases excretion of sodium and chloride in approximately equivalent amounts. Natriuresis may be accompanied by some loss of potassium and bicarbonate. After oral doses, 10-15 percent of the dose is excreted unchanged in the urine. Chlorothiazide crosses the placental but not the blood-brain barrier and is excreted in breast milk. As a diuretic, chlorothiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like chlorothiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of chlorothiazide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle. It is marketed under the brand name Diuril.
Dexamethasone is an anti-inflammatory agent that is FDA approved for the treatment of many conditions, including rheumatic problems, a number of skin diseases, severe allergies, asthma, chronic obstructive lung disease, croup, brain swelling and others. Dexamethasone is a glucocorticoid agonist. Unbound dexamethasone crosses cell membranes and binds with high affinity to specific cytoplasmic glucocorticoid receptors. Adverse reactions are: Glaucoma with optic nerve damage, visual acuity and field defects; cataract formation; secondary ocular infection following suppression of host response; and perforation of the globe may occur; muscle weakness; osteoporosis and others. Aminoglutethimide may diminish adrenal suppression by corticosteroids. Macrolide antibiotics have been reported to cause a significant decrease in corticosteroid clearance.
Dexamethasone is an anti-inflammatory agent that is FDA approved for the treatment of many conditions, including rheumatic problems, a number of skin diseases, severe allergies, asthma, chronic obstructive lung disease, croup, brain swelling and others. Dexamethasone is a glucocorticoid agonist. Unbound dexamethasone crosses cell membranes and binds with high affinity to specific cytoplasmic glucocorticoid receptors. Adverse reactions are: Glaucoma with optic nerve damage, visual acuity and field defects; cataract formation; secondary ocular infection following suppression of host response; and perforation of the globe may occur; muscle weakness; osteoporosis and others. Aminoglutethimide may diminish adrenal suppression by corticosteroids. Macrolide antibiotics have been reported to cause a significant decrease in corticosteroid clearance.
Status:
US Approved OTC
Source:
21 CFR 341.12(m) cough/cold:antihistamine triprolidine hydrochloride
Source URL:
First approved in 1958

Class (Stereo):
CHEMICAL (ACHIRAL)



Triprolidine is a first generation histamine H1 antagonist, which in combination with codeine phosphate and pseudoephedrine hydrochloride is sold under brand name TRIACIN-C. TRIACIN-C is indicated for temporary relief of coughs and upper respiratory symptoms, including nasal congestion, associated with allergy or the common cold.
Status:
US Approved OTC
Source:
21 CFR 341.12(m) cough/cold:antihistamine triprolidine hydrochloride
Source URL:
First approved in 1958

Class (Stereo):
CHEMICAL (ACHIRAL)



Triprolidine is a first generation histamine H1 antagonist, which in combination with codeine phosphate and pseudoephedrine hydrochloride is sold under brand name TRIACIN-C. TRIACIN-C is indicated for temporary relief of coughs and upper respiratory symptoms, including nasal congestion, associated with allergy or the common cold.
Status:
US Approved OTC
Source:
21 CFR 341.12(e) cough/cold:antihistamine dexchlorpheniramine maleate
Source URL:
First approved in 1958
Source:
Polaramine by Schering
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Dexchlorpheniramine, the d-isomer of the racemic compound chlorpheniramine, is two times more active than chlorpheniramine. Dexchlorpheniramine does not prevent the release of histamine, but rather, competes with free histamine for binding at the H1-receptor sites, and competitively antagonizes the effects of histamine on H1-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Blockade of H1-receptors also suppresses the formation of oedema, flare, and pruritus that result from histaminic activity. Since dexchlorpheniramine binds to central and peripheral H1-receptors, sedative effects are likely to occur. H1-antagonists are structurally similar to anticholinergic agents and therefore possess the potential to exhibit anticholinergic properties of varying degrees. They also have antipruritic effects. Dexchlorpheniramine has high antihistaminic activity, moderate anticholinergic effects and minimal sedative effects. The drug does not possess antiemetic properties.
Status:
US Previously Marketed
Source:
DEANER 100MG by RIKER
(1961)
Source URL:
First approved in 1958
Source:
Deaner by Riker
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

DEANOL is an inactive component of CERAVE® hydrocortisone anti-itch cream, which is used for temporarily relieve itching associated with minor skin irritations, inflammation, and rashes due to eczema, soaps, detergents, cosmetics, seborrheic dermatitis, psoriasis. DEANOL is also used as a food additive.
Status:
US Previously Marketed
Source:
Delvex by Lilly
(1958)
Source URL:
First approved in 1958
Source:
Delvex by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dithiazanine, 3-ethyl-2-[5-(3-ethyl-2-benzothiazolinylidene)-l, 3- pentadienyl] benzothiazolium iodide, is an old effective broad-spectrum human anthelmintic. In proper dosage, this polyvermicide is therapeutic for trichuriasis, strongyloidiasis, ascariasis, and enterobiasis. The drug also has significant anthelmintic activity against human hookworm, Necator americanus. It fulfills a need for an effective therapeutic for trichuriasis and strongyloidiasis. Dithiazanine is useful for the treatment of patients with either single or multiple intestinal helminth infections. It is effective for mass therapy for trichuriasis. Nowdays Dithiazanine is used only as a veterinary anthelmintic for dogs. It has being proved to be a highly toxic chemical, with a lethal dose for humans of about 4–16 mg/kg by oral ingestion.