Transdermal Clonidine: Therapeutic Considerations

Sica, Domenic A.; Grubbs, Rebecca A.

doi:10.1111/j.1524-6175.2005.04133.x

Cited by 38 publications

(22 citation statements)

References 49 publications

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“…The current data, consistent with others (Mitchell et al 2005, Sica & Grubbs 2005, show clonidine to be an effective intervention for lowering blood pressure; however, long-term use may result in weight gain (Morrison et al 1990, Laurent & Safar 1992. Sympathoadrenal inhibition will lead to decreased b-AR stimulation, and hence decreased b-AR support of EE, creating a physiological environment favoring positive energy balance and weight gain (Spraul et al 1993).…”

Section: Women Basalsupporting

confidence: 85%

Short-term sympathoadrenal inhibition augments the thermogenic response to β-adrenergic receptor stimulation

Newsom

Richards²,

Johnson³

et al. 2010

Journal of Endocrinology

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Sedentary behavior is associated with an attenuated thermogenic response to b-adrenergic receptor (b-AR) stimulation, an important regulator of energy expenditure (EE) in humans. Chronic stimulation of b-ARs, via heightened activity of the sympathoadrenal system, leads to diminished b-AR function. We have investigated the hypothesis that the thermogenic response of sedentary adults to b-AR stimulation will be increased during short-term sympathoadrenal inhibition. Using a randomly ordered, repeated measures study design, resting EE (REE; indirect calorimetry, ventilated hood technique) and the % increase in EE above REE (%DEE) during acute i.v. isoproterenol administration (nonselective b-AR agonist; 6, 12, and 24 ng/kg fat-free mass per min) were determined in 16 sedentary adults (nine females and seven males, 25G1 years, body mass index: 26 . 1G0 . 9 kg/m 2 , maximal oxygen uptake: 40G2 ml/kg per min (meanGS.E.M.)) in the basal state and on the 6th day of transdermal clonidine administration (centrally acting a2-AR agonist; 0 . 2 mg/day).Relative to baseline, clonidine inhibited sympathoadrenal activity, as evidenced by decreased plasma norepinephrine concentration (1 . 04G0 . 13 vs 0 . 34G0 . 03 nmol/l; P!0 . 001), skeletal muscle sympathetic nerve activity (22 . 5G3 . 8 vs 8 . 5 G1 . 9 bursts/min; PZ0 . 003), and resting heart rate (63G2 vs 49G1 beats/min; P!0 . 001). Sympathoadrenal inhibition decreased REE (6510G243 vs 5857G218 kJ/day; P!0 . 001), increased respiratory exchange ratio (0 . 84G0 . 01 vs 0 . 86 G0 . 01; PZ0 . 03), and augmented the thermogenic response to b-AR stimulation (%DEE: 11G2, 16G2, and 24G2 vs 14G1, 20G2, and 31G2; PZ0 . 04). These data demonstrate that in sedentary humans, short-term inhibition of sympathoadrenal activity increases the thermogenic response to b-AR stimulation, an important determinant of EE and hence energy balance.

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Section: Women Basalsupporting

confidence: 85%

Short-term sympathoadrenal inhibition augments the thermogenic response to β-adrenergic receptor stimulation

Newsom

Richards²,

Johnson³

et al. 2010

Journal of Endocrinology

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“…Dexmedetomidine has a half-life of 2 hours and should be completely eliminated from the body in 12 hours, whereas a clonidine patch has a half-life of 21 hours [3, 15, 16]. The combination of clonidine and dexmedetomidine has become increasingly common, but clinically significant adrenal insufficiency has not been described before, most likely because the pharmacokinetics and dosing are different depending on age.…”

Section: Discussionmentioning

confidence: 99%

Dexmedetomidine Infusion Associated with Transient Adrenal Insufficiency in a Pediatric Patient: A Case Report

Tucker

Cooke²,

Kudchadkar³

et al. 2013

Case Reports in Pediatrics

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Dexmedetomidine is a highly selective α 2-adrenoceptor agonist used for sedation due to its anxiolytic and analgesic properties without respiratory compromise. Due to its structural similarity to etomidate, there has been concern that dexmedetomidine may cause adrenal insufficiency. This concern was initially supported by animal studies, but subsequent human studies demonstrated mixed results. We describe the case of transient adrenal insufficiency in a 1-year-old male who presented with 24% total body surface 2nd degree burns. He required sedation with a prolonged, high-dose dexmedetomidine infusion with a peak infusion dose of 2.7 mcg/kg/hr and duration of 6.5 days. The patient developed lethargy and hypotension four days after discontinuation of his infusion. He had a random cortisol level which was low at 0.4 mcg/dL, and the concern for adrenal suppression was confirmed with an ACTH stimulation test with the baseline cortisol of 0.4 mcg/dL and inappropriate 60 minute post-ACTH stimulation cortisol of 7.8 mcg/dL. While further studies will be needed to clarify the risk of adrenal suppression secondary to dexmedetomidine, this case suggests that caution should be taken when administering dexmedetomidine to pediatric patients and highlights the need for future studies to look at appropriate dosing and duration of dexmedetomidine infusions.

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“…Clonidine and α‐methyldopa are the only 2 drugs in this class, that are intravenously available. Clonidine is the only compound in this class that is offered in a transdermal delivery system 13 . Onset and duration of action are features that distinguish compounds in this class.…”

Section: Indications/contraindications and Objectives Of Therapymentioning

confidence: 99%

“…Transdermal clonidine is of particular utility for the management of the labile hypertensive patient who requires multiple medications, the hospitalized patient who cannot take oral medications, and the patient with prominent early morning BP surges. At equivalent doses, transdermal clonidine is more likely than oral clonidine to be accompanied by dose‐dependent salt and water retention 13 …”

Section: Indications/contraindications and Objectives Of Therapymentioning

confidence: 99%

“…Clonidine has also been used effectively in various diarrheal states including that associated with the short‐gut syndrome 27 . Clonidine has also been used in the perioperative period, as an adjuvant to general and/or regional anesthesia; to improve analgesia with systemic, spinal, or peripheral opioids; and to control postoperative sympathetic responses 13 . As a result, anesthesia and analgesia requirement can be reduced.…”

Section: Bp‐independent Usesmentioning

confidence: 99%

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Centrally Acting Antihypertensive Agents: An Update

Sica

2007

J of Clinical Hypertension

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Centrally acting agents stimulate α2 receptors and/or imadozoline receptors on adrenergic neurons situated within the rostral ventrolateral medulla and, in so doing, sympathetic outflow is reduced. Centrally acting agents also stimulate peripheral α2 receptors, which, for the most part, is of marginal clinical significance. Central a agonists have had a lengthy history of use, starting with α‐methyldopa, which has had a dramatic decline in use, in part, because of bothersome side effects. Patients who require multidrug therapy with otherwise resistant hypertension, such as diabetic and/or renal failure patients, are typically responsive to these drugs, as are patients with sympathetically driven forms of hypertension. Perioperative forms of hypertension respond well to clonidine, a circumstance where the additional anesthesia‐ and analgesia‐sparing effects of this drug may offer additional clinical benefits. Clonidine can be used adjunctively with other more traditional therapies in heart failure, particularly when hypertension is present. Sustained‐release moxonidine, however, is associated with early mortality and morbidity when used in patients with heart failure. Escalating doses of drugs in this class often give rise to salt and water retention, in which case diuretic therapy becomes a valuable adjunctive therapy.

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Transdermal Clonidine: Therapeutic Considerations

Abstract: Transdermal clonidine was approved by the US (J Clin Hypertens. 2005;7:558-562)

Cited by 38 publications

References 49 publications

Short-term sympathoadrenal inhibition augments the thermogenic response to β-adrenergic receptor stimulation

Short-term sympathoadrenal inhibition augments the thermogenic response to β-adrenergic receptor stimulation

Dexmedetomidine Infusion Associated with Transient Adrenal Insufficiency in a Pediatric Patient: A Case Report

Centrally Acting Antihypertensive Agents: An Update

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