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Clonidine

    Brands

    DEA Class;  Rx

    Common Brand Names; Catapres, Catapres-TTS, Duraclon, Jenloga, Kapvay, Nexiclon XR

    • Alpha2 Agonists, Central-Acting; 
    • ADHD Agents

    Centrally-acting alpha2-agonist
    Oral and transdermal drug for HTN and autonomic hyperactivity (e.g., drug withdrawal syndromes); also used orally for ADHD
    Epidural product is used for refractory pain

    Indicated for the treatment of hypertension.

    For the treatment of attention-deficit hyperactivity disorder (ADHD) in pediatric patients as monotherapy or as adjunctive therapy to a psychostimulant.

    For the treatment of severe pain.
    For the treatment of hypertensive urgency or hypertensive emergency.
    For the treatment of opiate agonist withdrawal and/or benzodiazepine withdrawal.
    For the treatment of neonatal abstinence syndrome.
    For the symptomatic treatment of diabetic neuropathy.
    For the treatment of diabetic diarrhea.
    For use as an adjunct to psychosocial interventions in the management of tobacco cessation (smoking cessation).
    For the treatment of hypertension and the subsequent decline in renal function associated with scleroderma renal crisis (SRC).
    For minimization of nephrotoxicity in patients receiving cyclosporine (i.e., cyclosporine nephrotoxicity prophylaxis) and low-dose methotrexate for allogeneic bone marrow transplant.
     

    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
    • 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%)
    • 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%)

    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

    There is pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ADHD medications, during pregnancy

    Based on published lactation studies, clonidine hydrochloride is present in human milk at relative infant doses ranging from 4.1 to 8.4% of maternal weight-adjusted dosage

    Adults

    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

    Pediatric

    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

    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

    Clonidine hydrochloride

    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