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.

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
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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
Approximately 770 patients will be randomized to darusentan, active control (guanfacine, an antihypertensive drug that acts as a central alpha agonist) or ... - Business Wire (press release),

Monoaminergic Treatment of Schizophrenia  Feb 27, 2006
Guanfacine (Tenex), by enhancing signals at postsynaptic α 2 -adrenergic receptors, has been shown to improve working memory performance in animal models ... - Psychiatric Times,

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
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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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