CLONIDINE

brands

Class

• Neuroscience-based Nomenclature: norepinephrine receptor agonist (N-RA)
• Antihypertensive; centrally acting alpha 2 agonist hypotensive agent, nonstimulant for attention deficit hyperactivity disorder (ADHD)

CLONIDINE commonly prescribed for

(Bold for FDA approved)

How CLONIDINE works

• For ADHD, theoretically has central actions on postsynaptic alpha 2 receptors in the prefrontal cortex

• For hypertension, stimulates alpha 2 adrenergic receptors in the brain stem, reducing sympathetic outflow from the CNS and decreasing peripheral resistance, renal vascular resistance, heart rate, and blood pressure

• An imidazoline, so also interacts at imidazoline receptors

How long until CLONIDINE works

• For ADHD, can take a few weeks to see maximum therapeutic benefits

• Blood pressure may be lowered 30–60 minutes after first dose; greatest reduction seen after 2–4 hours

• May take several weeks to control blood pressure adequately

Notable Side Effects

• Dry mouth

• Dizziness, constipation, sedation

• Weakness, fatigue, impotence, loss of libido, insomnia, headache

• Major depression

• Dermatologic reactions (especially with transdermal clonidine)

• Hypotension, occasional syncope

• Tachycardia

• Nervousness, agitation

• Nausea, vomiting

Life Threatening Side Effects

• Sinus bradycardia, atrioventricular block

• During withdrawal, hypertensive encephalopathy, cerebrovascular accidents, and death (rare)

weight gain

unusual

sedation

common

What to do about CLONIDINE side effects

• Wait

• Take larger dose at bedtime to avoid daytime sedation

• Switch to another medication with better evidence of efficacy

• For withdrawal and discontinuation reactions, may need to reinstate clonidine and taper very slowly when stabilized

usual dosage range

• Extended-release for ADHD: 0.1–0.4 mg/ day in divided doses

• Immediate-release for hypertension: 0.2–0.6 mg/day in divided doses

• Opioid withdrawal: 0.1 mg 3 times daily (can be higher in inpatient setting)

Dosage Forms

• Extended-release tablet 0.1 mg, 0.2 mg

• Immediate-release tablet 0.1 mg scored, 0.2 mg scored, 0.3 mg scored

• Topical (7 day administration) 0.1 mg/24 hours, 0.2 mg/24 hours, 0.3 mg/24 hours

• Injection 0.1 mg/mL, 0.5 mg/mL

long term use

• Patients may develop tolerance to the antihypertensive effects

• Studies have not established the utility of clonidine for long-term CNS uses

• Be aware that forgetting to take clonidine or running out of medication can lead to abrupt discontinuation and associated withdrawal reactions and complications

habit forming

• Reports of some abuse by opiate addicts

• Reports of some abuse by non-opioiddependent patients

Renal Impairment

• Use with caution and possibly reduce dose

Hepatic Impairment

• Use with caution

Cardiac Impairment

• Use with caution in patients with recent myocardial infarction, severe coronary insufficiency, cerebrovascular disease

Elderly

• Elderly patients may tolerate a lower initial dose better

• Elderly patients may be more sensitive to sedative effects

Children and Adolescents

• Safety and efficacy not established for children under age 6

• Children may be more sensitive to hypertensive effects of withdrawing treatment

• Because children commonly have gastrointestinal illnesses that lead to vomiting, they may be more likely to abruptly discontinue clonidine and therefore be more susceptible to hypertensive episodes resulting from abrupt inability to take medication

• Children may be more likely to experience CNS depression with overdose and may even exhibit signs of toxicity with 0.1 mg of clonidine

• Injection may be used in pediatric cancer patients with severe pain unresponsive to other medications

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Controlled studies have not been conducted in pregnant women

• Some animal studies have shown adverse effects

• Use in women of childbearing potential requires weighing potential benefits to the mother against potential risks to the fetus

• For ADHD patients, clonidine should generally be discontinued before anticipated pregnancies

Breast Feeding

• Some drug is found in mother’s breast milk

• No adverse effects have been reported in nursing infants

• If irritability or sedation develop in nursing infant, may need to discontinue drug or bottle feed