Guanabenz

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

North America

USA: Guanabenz.

Latin America

Brazil: Lisapres.

Asia

Japan: Wytensin.

Drug combinations

Chemistry

Guanabenz Acetate: C~8~H~8~Cl~2~N~4~ C~2~H~4~O~2~. Mw: 291.13. (1) Hydrazinecarboximidamide, 2-[(2,6-dichlorophenyl)methylene]-, monoacetate; (2) [(2,6-Dichlorobenzylidene)amino]guanidine monoacetate. CAS-23256-50-0 (1981).

Pharmacologic Category

Sympathomimetic (Adrenergic) Agents; α-Adrenergic Agonists. Hypotensive Agents; Central α-Agonists. (ATC-Code: N06BA).

Mechanism of action

Guanabenz is a centrally active hypotensive agent, structurally and pharmacologically related to clonidine. Stimulates α~2~-adrenoreceptors in brain stem, thus activating an inhibitory neuron, resulting in reduced sympathetic outflow, producing a decrease in vasomotor tone and heart rate.

Therapeutic use

Guanabenz is used alone or in combination with other classes of antihypertensive agents in management of hypertension.

Pregnancy and lactiation implications

Teratogenic effects observed in animal studies. There are no adequate, well-controlled studies in pregnant women. Guanabenz should be used during pregnancy only when potential benefits justify possible risks to fetus. Unknown whether drug is excreted in breast milk, and therefore should be used with caution in nursing women.

Unlabeled use

Contraindications

Hypersensitivity to guanabenz or any component of the formulation.

Warnings and precautions

CNS effects (sedation and drowsiness) possible (avoid use in CNS disease). May cause significant orthostasis. Use with caution in severe coronary insufficiency or recent MI. Use with caution in cerebrovascular disease, and in severe hepatic or renal impairment. Avoid use with other CNS depressants (effects may be potentiated). Avoid use in the elderly. Avoid abrupt withdrawal (can result in nervousness, anxiety and rarely, rebound hypertension).

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