Estulic
Estulic - General Information
A centrally acting antihypertensive agent. The drug lowers both systolic and diastolic blood pressure by activating the central nervous system alpha-2 adrenoreceptors, which results in reduced sympathetic outflow leading to reduced vascular tone. Its adverse reactions include dry mouth, sedation, and constipation. [PubChem]
Pharmacology of Estulic
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.
Estulic for patients
Patients who receive guanfacine should be advised to exercise caution when operating dangerous machinery or driving motor vehicles until it is determined that they do not become drowsy or dizzy from the medication. Patients should be warned that their tolerance for alcohol and other CNS depressants may be diminished. Patients should be advised not to discontinue therapy abruptly.
Estulic Interactions
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 Noncardioselective beta-blockers (nadolol,porpranolol,timolol) may exacerbate rebound hypertension when guanfacine is withdrawn. The beta-blocker should be withdrawn first.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.
Estulic Contraindications
Guanfacine hydrochloride tablets are contraindicated in patients with known hypersensitivity to the drug.
Additional information about Estulic
Estulic Indication: For use in the management of hypertension.
Mechanism Of Action: Estulic 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Guanfacine
Synonyms: Guanfacina [Inn-Spanish]; Guanfacine HCl; Guanfacine Hydrochloride; Guanfacinum [Inn-Latin]
Drug Category: Adrenergic alpha-Agonists; Sympatholytics; Antihypertensive Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Guanfacine: Estulic; Tenex;
Absorption: Rapid and complete, with an oral bioavailability of approximately 80%.
Toxicity (Overdose): Symptoms of overdose include drowsiness, lethargy, bradycardia and hypotension. LD50=165mg/kg (orally in mice)
Protein Binding: Approximately 70% bound to plasma proteins, independent of drug concentration.
Biotransformation: Hepatic
Half Life: 17 hours (range 10-30 hours)
Dosage Forms of Estulic: Tablet Oral
Chemical IUPAC Name: N-(diaminomethylidene)-2-(2,6-dichlorophenyl)acetamide
Chemical Formula: C9H9Cl2N3O
Guanfacine on Wikipedia: https://en.wikipedia.org/wiki/Guanfacine
Organisms Affected: Humans and other mammals
