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Guanfacine
drug data and news
Guanfacine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Guanfacine | ||
| Brand Names/Synonyms | CHEMBANK3368; Estulic; Guanfacina [Inn-Spanish]; Guanfacine; Guanfacine Hcl; Guanfacine Hydrochloride; Guanfacinum [Inn-Latin]; LON 798; Tenex | ||
| Indication | For management of High blood pressure | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Similar to clonidine, guanfacine is a centrally-acting, alpha(2)-adrenergic receptor agonist used alone or in combination with other drugs for the treatment of hypertension. | ||
| Mechanism Of Action | Guanfacine selectively stimulates central alpha(2)-adrenergic receptors, resulting in inhibition of sympathetic nervous system outflow, reduction of peripheral and renal vascular resistance, and lowering of blood pressure and heart rate. | ||
| Guanfacine News (When available) |
Myogen Reports 2005 Results 07 Mar 2006 Monoaminergic Treatment of Schizophrenia Feb 27, 2006 | ||
| Dosage Forms | 2 oral tablet strengths | ||
| Drug_Category | Sympatholytics; Antihypertensive Agents; ATC:C02AC02 | ||
| Absorption | Rapid and complete; bioavailability approximately 80% | ||
| Interactions |
-->Interactions for Guanfacine: The potential for increased sedation when guanfacine is given with other CNS-depressant drug should be appreciated. The administration of guanfacine concomitantly with known microsomal enzyme inducer (phenobarbital or phenytoin) to two patients with renal impairment reportedly resulted in significant reductions in elimination half-life and plasma concentration. In such cases, therefore, more frequent dosing may be required to achieve or maintain the desired hypotensive response. Further, if guanfacine is to be discontinued in such patients, careful tapering of the dosage may be necessary in order to avoid rebound phenomena. TCAs decrease the hypotensive effect of guanfacine. Noncardioselective beta-blockers (nadolol,porpranolol,timolol) may exacerbate rebound hypertension when guanfacine is withdrawn. The beta-blocker should be withdrawn first. The gradual withdrawal of guafacine or a cardioselective beta-blocker could be substituted. Anticoagulants Ten patients who were stabilized on oral anticoagulants were given guanfacine, 1-2 mg/day, for 4 weeks. No changes were observed in the degree of anticoagulation. In several well-controlled studies, guanfacine was administered together with diuretics with no drug interactions reported. In the long-term safety studies, guanfacine was given concomitantly with many drugs without evidence of any interactions. The principal drugs given (number of patients in parentheses) were: cardiac glycosides (115), sedatives and hypnotics (103), coronary vasodilators (52), oral hypoglycemics (45), cough and cold preparations (45), NSAIDs (38), antihyperlipidemics (29), antigout drugs (24), oral contraceptives (18), bronchodilators (13), insulin (10), and beta blockers (10). Laboratory Test In clinical trials, no clinically relevant laboratory test abnormalities were identified as causally related to drug during short-term treatment with guanfacine. Drug/Laboratory Test Interactions No laboratory test abnormalities related to the use of guanfacine have been identified. | ||
| Toxicity | Drowsiness, lethargy, bradycardia and hypotension; LD50=165mg/kg (orally in mice) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | N-(diaminomethylidene)-2-(2,6-dichlorophenyl)-ethanamide | ||
| Chemical Formula | C9H9Cl2N3O | ||
| Molecular Weight | 246.093 g/mol | ||
| Smiles String | C1=CC(=C(C(=C1)Cl)CC(=O)N=C(N)N)Cl | ||
| Melting Point | 225-227 °C | ||
| Water Solubility | 1892 mg/L | ||
| State | white to off-white powder | ||
| LogP/Hphobicity | 2.464 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 17 hr (range 10-30 hr) | ||
| Protein Binding [%] | 70% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Guanfacine.html http://www.rxlist.com/cgi/generic3/guanfacine.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00075 | ||
| CAS Registry Number | 29110-47-2 | ||
| KEGG Compound ID | C07037 | ||
| PubChem ID | SID:290562 | ||
| PharmGKB ID | PA449825 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | Not Available |
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