TENEX

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TENEX (TENEX).

How it works

Selective alpha-2A adrenergic receptor agonist in the brainstem, reducing sympathetic outflow from the CNS, leading to decreased peripheral vascular resistance and heart rate.

What the body does with it

Metabolism	Primarily hepatic via CYP3A4; approximately 60% metabolized, with the remainder excreted unchanged in urine.
Excretion	Renal (40-60% unchanged), fecal (40-50% as metabolites, <5% unchanged).
Half-life	Terminal elimination half-life is 12-17 hours; requires dose adjustment in renal impairment (CrCl <30 mL/min).
Protein binding	70-75% bound to albumin.
Volume of Distribution	2-4 L/kg; indicates extensive tissue distribution.
Bioavailability	Oral: 80-90%.
Onset of Action	Oral: 1-2 hours for peak antihypertensive effect.
Duration of Action	24 hours; once-daily dosing is effective due to sustained plasma concentrations.

Classification & Brands

Action Class	DPP-4 inhibitors
Brand Substitutes	Ecoglip-T Tablet, Dynaglipt Tablet, Tenlimac Tablet, Megagliptin Tablet, Glipon 20mg Tablet

Dosing & administration

1 mg orally once daily, titrated by 1 mg increments at weekly intervals; maximum 2 mg/day.

Dosage form	TABLET
Renal impairment	CrCl 30-59 mL/min: administer 50% of normal dose; CrCl 15-29 mL/min: administer 25% of normal dose; CrCl <15 mL/min: administer 12.5% of normal dose; hemodialysis: administer 12.5% of normal dose post-dialysis.
Liver impairment	No specific guidelines; use with caution in severe hepatic impairment (Child-Pugh C).
Pediatric use	Not established for children <12 years; off-label: 0.05-0.1 mg/kg/day divided every 6-8 hours, titrate slowly.
Geriatric use	Start at 0.5 mg orally once daily, titrate slowly, monitor for hypotension and sedation.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TENEX (TENEX).

Breastfeeding	Excreted in breast milk; M/P ratio approximately 0.8; limited data suggest infant doses <5% maternal weight-adjusted dose; consider risk-benefit.
Teratogenic Risk	No evidence of teratogenicity in human studies; animal studies showed no malformations at clinically relevant doses. First trimester: no known risk; second and third trimesters: maternal hypertension treatment may be preferred over methyldopa.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

No black box warning.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to guanfacine or any component","Concomitant use with potent CYP3A4 inhibitors (e.g., ketoconazole)"]

Clinical Precautions

Precautions

["Rebound hypertension upon abrupt discontinuation","Sedation and dizziness","Bradycardia and heart block","Renal impairment requires dose adjustment"]

Clinical Tips & Counseling

Drug interactions

Loading safety data…

TENEX

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TENEX (TENEX).

How it works

Selective alpha-2A adrenergic receptor agonist in the brainstem, reducing sympathetic outflow from the CNS, leading to decreased peripheral vascular resistance and heart rate.

What the body does with it

Metabolism	Primarily hepatic via CYP3A4; approximately 60% metabolized, with the remainder excreted unchanged in urine.
Excretion	Renal (40-60% unchanged), fecal (40-50% as metabolites, <5% unchanged).
Half-life	Terminal elimination half-life is 12-17 hours; requires dose adjustment in renal impairment (CrCl <30 mL/min).
Protein binding	70-75% bound to albumin.
Volume of Distribution	2-4 L/kg; indicates extensive tissue distribution.
Bioavailability	Oral: 80-90%.
Onset of Action	Oral: 1-2 hours for peak antihypertensive effect.
Duration of Action	24 hours; once-daily dosing is effective due to sustained plasma concentrations.

Classification & Brands

Action Class	DPP-4 inhibitors
Brand Substitutes	Ecoglip-T Tablet, Dynaglipt Tablet, Tenlimac Tablet, Megagliptin Tablet, Glipon 20mg Tablet

Dosing & administration

1 mg orally once daily, titrated by 1 mg increments at weekly intervals; maximum 2 mg/day.

Dosage form	TABLET
Renal impairment	CrCl 30-59 mL/min: administer 50% of normal dose; CrCl 15-29 mL/min: administer 25% of normal dose; CrCl <15 mL/min: administer 12.5% of normal dose; hemodialysis: administer 12.5% of normal dose post-dialysis.
Liver impairment	No specific guidelines; use with caution in severe hepatic impairment (Child-Pugh C).
Pediatric use	Not established for children <12 years; off-label: 0.05-0.1 mg/kg/day divided every 6-8 hours, titrate slowly.
Geriatric use	Start at 0.5 mg orally once daily, titrate slowly, monitor for hypotension and sedation.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TENEX (TENEX).

Breastfeeding	Excreted in breast milk; M/P ratio approximately 0.8; limited data suggest infant doses <5% maternal weight-adjusted dose; consider risk-benefit.
Teratogenic Risk	No evidence of teratogenicity in human studies; animal studies showed no malformations at clinically relevant doses. First trimester: no known risk; second and third trimesters: maternal hypertension treatment may be preferred over methyldopa.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

No black box warning.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to guanfacine or any component","Concomitant use with potent CYP3A4 inhibitors (e.g., ketoconazole)"]

Clinical Precautions

Precautions

["Rebound hypertension upon abrupt discontinuation","Sedation and dizziness","Bradycardia and heart block","Renal impairment requires dose adjustment"]

Clinical Tips & Counseling

Drug interactions

Loading safety data…