DCSIMG
AMBIEN CR® (zolpidem tartrate) Pharmacokinetics
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AMBIEN CR (Zolpidem Tartrate Extended Release) Sleep Aid

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Pharmacokinetics

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Plasma concentration

The controlled-release characteristics of AMBIEN CR reflect the makeup of the dual-layer tablet and the resultant biphasic absorption characteristics2,4-6,8:

  • A rapid initial absorption from the gastrointestinal tract similar to the immediate-release formulation of zolpidem tartrate4
  • Extended plasma concentrations lasting beyond 3 hours postdose4

Mean Plasma Concentration

Pharmacokinetic Characteristics of AMBIEN CR 12.5 mg

Half-Value Duration

Higher levels beyond 3 hours postdose 4

A study in 24 healthy male subjects compared the mean zolpidem plasma concentration-time profiles obtained after single oral administration of
AMBIEN CR (12.5 mg) and the immediate-release formulation of zolpidem tartrate (10 mg).4

Both formulations showed an initial rapid absorption with maximal zolpidem concentrations reached between 0.9 and 1.5 hours after dosing (P=NS).7

However, as shown below, plasma concentrations were consistently higher for the CR formulation beyond 3 hours postdose.7

Comparison of zolpidem plasma concentrations following a single dose of 12.5 mg of the controlled-release formulation (AMBIEN CR) and 10 mg of the immediate-release formulation.7

Half-value duration

AMBIEN CR is approved at doses of 12.5 mg for healthy adults and 6.25 mg for elderly (≥65 years) or debilitated patients who might be more sensitive to the medication and for patients with hepatic insufficiency who do not clear the medication as rapidly as normal individuals.4

The pharmacokinetic characteristics of
AMBIEN CR 12.5 mg in healthy adult subjects are shown at right in comparison to zolpidem tartrate immediate-release 10 mg.4,9

The peak plasma concentration (Cmax) and half-life (t1/2) of AMBIEN CR are comparable to those of immediate-release zolpidem.2,7,11

However, AMBIEN CR has a greater half-value duration (HVD), which is defined as the time during which plasma concentrations equal or exceed 50% of the peak plasma concentration.7

The mean HVD, as shown below for AMBIEN CR, was determined to be almost 2-fold greater than that of immediate-release zolpidem in healthy adult subjects: AMBIEN CR, 4.6 hours; immediate-release zolpidem, 2.3 hours (90% confidence interval: 1.8 to 2.2 hours).7

In other words, circulating plasma concentrations are maintained for a longer duration with
AMBIEN CR.2,7,11

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* Maximum benefit is $240 off, up to $20 off each prescription (up to 12 prescriptions), depending on your out-of-pocket costs. Not valid for patients participating in Medicare, Medicaid, government (public insurance) programs, or any private payor in the state of Massachusetts and where prohibited by law.

AMBIEN CR is indicated for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance.

AMBIEN® (zolpidem tartrate) is indicated for the short-term treatment of insomnia characterized by difficulties with sleep initiation.

IMPORTANT SAFETY INFORMATION

In elderly or debilitated patients, or in patients with hepatic insufficiency or dysfunction, the recommended dose of AMBIEN CR is 6.25 mg and the recommended dose of AMBIEN is 5 mg. These patients should be closely monitored.

AMBIEN CR and AMBIEN both have rapid onset of action; therefore, patients should ingest right before going to bed and when ready for sleep. To avoid residual effects, patients should not take AMBIEN CR or AMBIEN unless they are prepared to get a full night’s sleep (7 to 8 hours). Until they know how it will affect their physical or mental performance upon awakening, patients should not drive or operate hazardous machinery after taking AMBIEN CR, AMBIEN, or any other sleep medication. Complex behaviors such as somnambulism, including driving or eating while not fully awake, with amnesia for the event, as well as abnormal behaviors such as being more outgoing or aggressive than normal, confusion, agitation, and hallucinations may occur. AMBIEN CR or AMBIEN should not be taken with alcohol as they may increase these abnormal behaviors. Discontinuation of AMBIEN CR or AMBIEN should be strongly considered for patients reporting such complex behaviors. Angioedema may occur in patients taking AMBIEN CR or AMBIEN and in rare cases may be fatal. Patients who develop angioedema should not be rechallenged. In primarily depressed patients, worsening of depression, including risk of suicidal thoughts or actions, including completed suicides, have been reported. The most commonly observed adverse effects in controlled clinical trials of AMBIEN CR were headache, somnolence, and dizziness. During short-term treatment with AMBIEN, the most commonly observed adverse effects in controlled clinical trials were drowsiness, dizziness, and diarrhea. Because individuals with a history of addiction or substance abuse are at increased risk of habituation and dependence, they should be under careful surveillance when receiving
AMBIEN CR, AMBIEN, or any other hypnotic. Both AMBIEN CR and AMBIEN are Schedule IV controlled substances. Sedative hypnotics have produced withdrawal symptoms following abrupt discontinuation.

Please refer to the full prescribing information for AMBIEN CR.

Please refer to the full prescribing information for AMBIEN.