Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 100mcg/mL
- 500mcg/mL
patch, extended-release
- 0.1mg/day
- 0.2mg/day
- 0.3mg/day
tablet, immediate-release
- 0.1mg
- 0.2mg
- 0.3mg
tablet, extended-release
- 0.1mg
Hypertension
Immediate-release tablets
- 0.1 mg PO q12hr
- Range: 0.1-0.2 mg/day q12hr; not to exceed 2.4 mg/day
Transdermal
- Apply 1 patch q7Days; start with 0.1 mg; increase by 0.1 mg after q1-2Week interval; usual dose range is 0.1-0.3 mg qWeek
Cancer Pain
Epidural infusion
- Severe pain in patients with cancer not adequately relieved by opioid analgesics alone
- Initial: 30 mcg/hr
- Titrate as required for pain relief or presence of side effects
- Limited data on doses exceeding 40 mcg/hr
Acute Hypertension (Off-label)
0.1-0.2 mg PO; may follow with additional doses of 0.1 mg qhr PRN to maximum 0.6 mg total dose
EtOH Withdrawal (Off-label)
0.3-0.6 mg PO q6hr
Smoking Cessation (Off-label)
PO administration: 0.1 mg qDay; increase by 0.1 mg/day to 0.15-0.75 mg/day if required
TD administration: 100-200 mcg/day patch q7Days
Restless Legs Syndrome (Off-label)
100-300 mcg PO 2 hours befor bedtime, up to 900 mcg/day
Tourette's Syndrome (Off-label)
0.0025-0.015 mg/kg/day PO for 6 weeks to 3 months
Cyclosporine Nephrotoxicity (Off-label)
100-200 mcg/day transdermal patch; change q7Days
Menopausal Flushing (Off-label)
Apply 100 mcg/day patch; change q7Days, OR
50 mcg PO q12hr initially; may increase up to 400 mcg q12hr
Dysmenorrhea (Off-label)
PO administration: 0.025 mg q12hr for 2 weeks prior to menstruation
Opioid Withdrawal (Off-label)
PO administration: 0.1-0.3 mg q4-6hr; increase by 0.1 mg/day to 0.15-0.75 mg/day if required; do not exceed 2.4 mg/day
TD administration: 100-200 mcg/day patch q7Days; initiate 0.1-0.3 mg PO q4-6hr for first 2 days to allow for adequate drug levels
Postherpetic Neuralgia (Off-label)
PO administration: 0.1 mg q12hr
Psychosis (Off-label)
PO administration: 0.4-1.4 mg/day in divided doses
Pheochromocytoma Diagnosis (Off-label)
Clonidine suppression testing: 0.3 mg PO for 60-80 kg patient; obtain blood sample 3 hours after administration to supine patient
Dosing Considerations
Extended-release is not to be used interchangeably with immediate-release tablets
Conversion from oral to transdermal
- Day 1: Place Catapress-TTS-1; administer 100% of oral dose
- Day 2: Administer 50% of oral dose
- Day 3: Administer 25% of oral dose
- Day 4: Patch remains, no further oral supplement needed
Cancer pain
- Dilute 500 mcg/mL to 100 mcg/mL with 0.9% NaCl before administration
- Epidural infusion considered as adjunct to intraspinal opiate therapy; epidural administration (Duraclon) is indicated in combination with opiates for the treatment of severe pain in patients with cancer not adequately relieved by opioid analgesics alone
- More likely to be effective in patients with neuropathic pain than in those with somatic or visceral pain
Dosing Modifications
Renal Impairment
- Impact of renal impairment not assessed
- Initial dose should be based on amount of renal impairment
- Monitor carefully for hypotension and bradycardia
- Removed minimally during hemodialysis; no need to redose following dialysis
Dosage Forms & Strengths
injectable solution
- 100mcg/mL
- 500mcg/mL
patch
- 0.1mg/day
- 0.2mg/day
- 0.3mg/day
tablet, immediate-release
- 0.1mg
- 0.2mg
- 0.3mg
tablet, extended-release
- 0.1mg
Hypertension
>12 years old
- Immediate-release tablets: 0.2 mg/day PO divided q12hr; increase qWeek; maintenance dose range, 0.2-0.6 mg/day q12hr; not to exceed 2.4 mg/day
- Transdermal patch: 0.1 mg patch q7Day initially; may increase by weekly 0.1-mg increments after 1-2 weeks if desired blood pressure reduction not achieved; not to exceed 0.6 mg/week (ie, 2 clonidine 0.3 mg patches)
<12 years old
- Immediate-release tablets and transdermal patch: Safety and efficacy not established
<18 years old
- Extended-release tablets (Jenloga, Nexiclon XR): Safety and efficacy not established
ADHD
<6 years old: Not established
≥6 years old (extended-release tablets, Kapvay): 0.1 mg PO qHS initially; may adjust dose by increments of 0.1 mg/day at weekly intervals until desired response; not to exceed 0.4 mg/day
When discontinuing, taper gradually by decrements not to exceed 0.1 mg q3-7Days
Dosing considerations
- May be given as monotherapy or as adjunctive therapy with stimulants
- Extended-release not interchangeable with immediate-release product
Cancer Pain
Severe pain in patients with cancer not adequately relieved by opioid analgesics alone
Epidural infusion: 0.5 mcg/kg/hr initially; adjust according to clinical response
Dosing considerations
- Epidural administration (Duraclon) is indicated in combination with opiates for the treatment of severe pain in patients with cancer not adequately relieved by opioid analgesics alone
- Restrict use to pediatric patients with severe, intractable pain from malignancy that is unresponsive to epidural or spinal opiates or to other, more conventional analgesic techniques
- More likely to be effective in patients with neuropathic pain than in those with somatic or visceral pain
- Safety and effectiveness of epidural administration in this limited indication and clinical population have been established in patients old enough to tolerate placement and management of an epidural catheter; these conclusions are based on evidence from adequate and well-controlled studies in adults and through experience with the use of clonidine in the pediatric age group for other indications
Administration
ADHD
- Doses 0.2 mg/day or greater should be divided BID, with either an equal or higher split dosage being given at bedtime
- Swallow tablet whole; do not crush, chew, or split
Dosing Modifications
Renal Impairment
- Impact of renal impairment not assessed
- Initial dose should be based on amount of impairment
- Monitor carefully for hypotension and bradycardia
- Removed minimally during hemodialysis, so no need to redose following dialysis
Hypertension
Immediate-release tablets: 0.1 mg PO qHS
Dosing considerations
Not recommended as routine treatment for hypertension (Beers criteria)
Potential for orthostatic hypotension and adverse CNS effects
May cause bradycardia
Immediate release: Lower initial doses than for nongeriatric adult dosing, as well as gradual adjustments, are recommended
Extended release: May require lower initial dose than for nongeriatric adult dosing
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Skin reactions; patch (15-50%)
Dry mouth (40%)
Somnolence (19-38%)
Headache (19-29%)
Fatigue (13-24%)
Drowsiness (33%)
Dizziness (13-16%)
Hypotension, epidural (45%)
Postural hypotension, epidural (32%)
Anxiety (11%)
1-10%
Constipation (10%)
Sedation (10%)
Nausea/vomiting, PO (5%)
Malaise (3%)
Orthostatic hypotension (3%)
Anorexia, PO (1%)
Abnormal LFTs (1%)
Rash (1%)
Weight gain, PO (1%)
Frequency Not Defined
Children with ADHD
- Upper respiratory tract infection
- Irritability
- Throat pain
- Nightmares
- Insomnia
- Emotional disorder
- Constipation
- Nasal congestion
Postmarketing Reports
Hallucinations
AV block
Warnings
Black Box Warnings
Epidural clonidine is not recommended for obstetric postpartum or perioperative pain management because the risk of hemodynamic instability (eg, hypotension, bradycardia) may be unacceptable in this population
Dilute product with strength of 500 mcg/mL prior to use
Contraindications
Hypersensitivity
Epidural
- Concurrent anticoagulants, bleeding diathesis
- Presence of injection site infections
- Administration above C4 dermatome, due to lack of adequate safety data
- Obstetric/perioperative pain
Cautions
Epidural: Hemodynamically unstable patients (risk of severe hypotension)
Do not discontinue suddenly (risk of rebound hypertension)
Patch: May need to remove if severe erythema and/or localized vesicle formation develop at application site or generalized rash; consult physician
Severe coronary insufficiency
May cause xerostomia
Recent MI
Cerebrovascular disease
Chronic renal failure
Raynaud's disease
Thromboangiitis obliterans
History of depression (may exacerbate depression in cancer patients)
May impair ability to perform hazardous tasks
Remove patch before MRI (may cause burns)
Hypotension may occur; usually responsive to IV fluids and, if necessary, appropriate parenterally administered pressor agents
Cardiac conduction abnormalities: Sympatholytic action may worsen sinus node dysfunction and atrioventricular (AV) block, especially if coadministered with other sympatholytic drugs
Titrate slowly and monitor vital signs frequently in patients at risk for hypotension, heart block, bradycardia, syncope, cardiovascular disease, vascular disease, cerebrovascular disease or chronic renal failure; measure heart rate and blood pressure prior to initiation of therapy, following dose increases, and periodically while on therapy; avoid concomitant use of drugs with additive effects unless clinically indicated; advise patients to avoid becoming dehydrated or overheated
Epidural administration may result in mild respiratory depression (usually with higher than recommended dose)
Use with caution in cerebrovascular disease
Avoid as first line antihypertensive in the elderly due to high risk for adverse side effects
Children may be particularly susceptible to hypertensive episodes when experiencing GI illnesses that lead to vomiting
Discontinue oral immediate release formulations within 4 hr of surgery; restart as soon as possible following surgery
Due to different pharmacokinetic profiles, oral formulations are not interchangeable with extended release on a mg-mg basis due to different pharmacokinetic profiles
Pregnancy & Lactation
Pregnancy category: C
Lactation: Distributed in breast milk; caution advised
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Central sympatholytic via stimulation of central alpha receptors; results in reduced sympathetic outflow, causing decreased PVR, HR, BP, and renal vascular resistance; produces presynaptic and postjunctional alpha-2 adrenoreceptor analgesia by preventing pain signal transmission to brain
Postsynaptic alpha2-agonist stimulation may regulate subcortical activity in the prefrontal cortex, which may regulate the area of the brain responsible for attention, emotions, and behaviors, and thereby reduces hyperactivity, distractibility, and impulsiveness
Absorption
Bioavailability: Immediate release (75-85%); extended release (89%)
Onset: <1 hr (2-4 hr peak effect in blood pressure)
Duration: 6-10 hr
Peak plasma time: 1-3 hr (immediate release); 7-8 hr (extended release)
Distribution
Protein bound: 20-40%
Vd: 2.9 L/kg
Metabolism
Liver
Elimination
Half-life: 12-16 hr
Excretion: Urine (40-60%)
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Patient Handout
Formulary
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