Dosing & Uses
Dosage Forms & Strengths
Spasticity associated with multiple sclerosis and spinal cord injury
Initial: 2 mg PO q6-8hr PRN; no more than 3 doses q24hr
Maintenance: Titrate in 2-4 mg/day increments to optimum effect with minimum 1-4 days between dose increments
Not to exceed 36 mg/day; single doses >16 mg not studied
To discontinue taper gradually; decrease by 2-4 mg daily
- CrCl <25 mL/min: Use caution; clearance reduced >50%
- CrCl >25 mL/min: Not studied; use caution
- Close monitoring of ADRs (eg, hypotension); avoid in severe impairment
Serious - Use Alternative
Significant - Monitor Closely
Dry mouth (46-50%)
Blurred vision (3%)
LFT abnormalities (3-5%)
Speech disorder (3%)
Urinary frequency (3%)
Frequency Not Defined
Concomitant ciprofloxacin or fluvoxamine, or other potent CYP1A2 inhibitors
Potential for hypotension
Caution in renal/hepatic impairment
Women on oral contraceptives
Hepatotoxicity may occur; monitor aminotransferases prior to and during use
Sedation may occur (dose related); may potentiate effect of sedative drugs or ethanol
Visual hallucinations may occur
CYP1A2 inducers may decrease levels
Rebound hypertension, tachycardia, and hypertonia reported upon abrupt discontinuation; decrease doses slowly in patients taking concomitant narcotics or high doses (20-28 mg/day) for prolonged periods
Pregnancy & Lactation
Pregnancy category: C
Lactation: May be excreted in breast milk due to lipophilic nature; use caution
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.
Mechanism of Action
Alpha-2 adrenergic receptor agonist structurally related to clonidine; increases presynaptic inhibition of motor neurons
Peak serum time: 1-4 hr
Protein bound: 30%
Vd: 2.4 L/kg
Extensively metabolized in the liver
Half-life: 2.5 hr
Excretion: Feces (20%); urine (60%)
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.
|1||This drug is available at the lowest co-pay. Most commonly, these are generic drugs.|
|2||This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.|
|3||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.|
|NC||NOT COVERED – Drugs that are not covered by the plan.|
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.