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Uses

Hypertension

Used alone or in combination with other classes of antihypertensive agents in the management of hypertension.

Thiazide diuretics are considered the preferred initial monotherapy for uncomplicated hypertension by JNC 7.

May be more effective when used with a diuretic.

Has been used in conjunction with thiazide diuretics, chlorthalidone, or furosemide, producing a greater reduction in BP than is obtained with either drug alone.

Use of a diuretic may aid in overcoming tolerance to clonidine and permit reduction of clonidine dosage.

May be useful in some patients unable to tolerate other adrenergic blocking agents because of severe postural hypotension; geriatric patients may not tolerate the adverse cognitive effects of central α₂-adrenergic agonists such as clonidine.

Has been used with other hypotensive agents such as hydralazine, reserpine, or methyldopa, permitting a reduction in the dosage of each drug and, in some patients, minimizing adverse effects while maintaining BP control.

Transdermal clonidine has been effective in many patients for the management of mild to moderate hypertension when used alone or in combination with an oral thiazide diuretic.

Transdermal clonidine has been successfully substituted for oral clonidine hydrochloride in mild to moderate hypertension.

Role of transdermal versus oral therapy remains to be more fully evaluated; transdermal therapy may prove to be convenient (e.g., in those in whom compliance with a daily dosing regimen may be a problem), but adverse dermatologic reactions occur frequently.

The principal goal of preventing and treating hypertension is to reduce the risk of cardiovascular and renal morbidity and mortality, including target organ damage. The higher the baseline BP, the more likely the development of MI, heart failure, stroke, and renal disease.

Effective antihypertensive therapy reduces the risk of stroke by about 34–40%, MI by about 20–25%, and heart failure by more than 50%.

Antihypertensive drug therapy is recommended for all patients with SBP/DBP ≥140/90 mm Hg who fail to respond to lifestyle/behavioral modifications.

Initial antihypertensive therapy with drugs generally is recommended for anyone with diabetes mellitus, chronic renal impairment, or heart failure having SBP ≥130 mm Hg or DBP ≥80 mm Hg.

Hypertensive Crises

Oral clonidine, including loading-dose regimens, has been effective in rapidly reducing BP in patients with severe hypertension when reduction of BP was considered urgent (i.e., hypertensive urgency†), but not requiring emergency treatment.

Hypertensive urgencies† are those situations in which it is desirable to reduce BP within a few hours.

Avoid excessive falls in BP since they may precipitate renal, cerebral, or coronary ischemia.

Recommended by some experts to be administered orally for rapidly reducing BP in pediatric patients 1–17 years of age when reduction of BP is considered a hypertensive urgency† or in some hypertensive emergencies.†

Has been used IV† in the management of acute hypertensive crisis† and in hypertensive episodes during labor†, as well as IM† or sub-Q† in the management of late-onset toxemia of pregnancy†, with satisfactory results; however, other antihypertensives are preferred.

Pain

Used epidurally as adjunctive therapy in combination with opiates in the management of severe cancer pain that is not relieved by opiate analgesics alone.

Epidural analgesia should be considered only when maximum tolerated doses of opiate and adjunct analgesics administered by other routes (e.g., oral, transdermal, sub-Q, IV) fail to relieve pain.

Epidural clonidine is more likely to be effective in patients with neuropathic pain rather than somatic or visceral pain.

Opiate Dependence

Has been used safely and effectively for rapid detoxification in the management of opiate withdrawal in opiate-dependent individuals†, in both inpatient and outpatient settings.

Exact role and its efficacy compared with other methods of detoxification (e.g., methadone) remain to be clearly determined.

Appears to be most useful as a transitional treatment between opiate dependence† and administration of the opiate antagonist naltrexone.

May be especially useful when detoxification using methadone is inappropriate, unsuccessful, or unavailable.

Alcohol Dependence

Has been used in conjunction with benzodiazepines for the management of alcohol withdrawal†.

May be effective in reducing symptoms of the hyperadrenergic state associated with alcohol withdrawal†, including elevated BP, increased heart rate, tremor, sweating, and anxiety.

Has not been shown to prevent delirium or seizures, and should be used only as an adjunct to benzodiazepines (not as monotherapy) for the management of alcohol withdrawal†.

Smoking Cessation

Used for the management of nicotine (tobacco) dependence†.

Nicotine dependence† is a chronic relapsing disorder that requires ongoing assessment and often repeated intervention.

US Public Health Service (USPHS) currently recommends clonidine as a second-line drug† for use under the supervision of a clinician.

Second-line pharmacotherapy (e.g., clonidine, nortriptyline, combined therapy with 2 forms of nicotine replacement) is of a more limited role than first-line pharmacotherapy (i.e., bupropion [as extended-release tablets], nicotine polacrilex gum, transdermal nicotine, nicotine nasal spray, nicotine nasal inhaler) in part because of more concerns about potential adverse effects with second-line drugs than with first-line drugs.

Use of second-line pharmacotherapy should be considered after first-line pharmacotherapy was attempted or considered and should be individualized based on patient considerations.

Attention Deficit Hyperactivity Disorder

Has been used for the treatment of attention deficit hyperactivity disorder† (ADHD).

Produces a moderate reduction in symptoms of ADHD†; stimulants (e.g., methylphenidate, amphetamines) remain the drugs of choice for the management of ADHD because of their greater efficacy compared with that of other drugs (e.g., clonidine).

Generally, has been shown to be more effective than placebo in the treatment of core symptoms of ADHD†, but the magnitude of its effects is lower than with stimulants and efficacy has been established mainly in children with ADHD and comorbid conditions (motor tics in patients with Tourette’s syndrome), especially sleep disturbances.

Use in pediatric patients for the treatment of ADHD† usually is not recommended without such comorbid psychiatric disorders due to current lack of evidence establishing safety and efficacy.

Pheochromocytoma

Not indicated in the treatment of pheochromocytoma†; however, unlike reserpine and guanethidine, it does not cause acute cardiovascular collapse in patients with this condition.

Has been used as an aid in the diagnosis of pheochromocytoma† in hypertensive patients with suggestive symptoms and borderline catecholamine values; plasma norepinephrine concentration generally is unchanged following administration of a single oral dose of clonidine in pheochromocytoma, while decrease in plasma norepinephrine concentration occurs with sympathetic hyperactivity.

Migraine Headaches

Has been used in the prophylaxis of migraine headaches†, but efficacy for this condition is questionable.

Dysmenorrhea

Has been used for the treatment of severe dysmenorrhea†.

Vasomotor Symptoms Associated with Menopause

Has been used orally and transdermally for the management of vasomotor symptoms† (e.g., hot flashes) associated with menopause.

May improve the severity and frequency of vasomotor symptoms†, albeit modestly; however, required dosages (exceeding the equivalent of 0.1 mg daily administered orally) may result in increased and, sometimes, intolerable adverse effects.

Use for management of vasomotor symptoms† mainly in postmenopausal women in whom estrogen replacement therapy is contraindicated or in those with preexisting hypertension.

Glaucoma

Has been used topically† to reduce IOP in the treatment of open-angle† (chronic simple) and secondary glaucoma† and hemorrhagic glaucoma associated with hypertension†.

Diarrhea

Has been used with some success in a limited number of patients for the management of diarrhea† of various etiologies (e.g., narcotic bowel syndrome, idiopathic diarrhea associated wtih diabetes).