Zolpidem Drug Interactions
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The majority of drug interactions with zolpidem include those that increase CNS depression. CNS depressant drugs that are given concurrently may increase the risk of respiratory depression, sedation, impaired psychomotor ability, and cognitive impairment.
Contents |
Drugs That Lead to Increased CNS Depression
1. Anxiolytics, sedatives, and hypnotics such as: barbiturates[1], benzodiazepines[1]
- These drugs are CNS depressants and may have cumulative sedative effects when administered concurrently.
2. Anti-parkinson drugs such as: entacapone [1], pramipexole [1], ropinirole [1], tolcapone [1]
- These drugs are CNS depressants and may have cumulative sedative effects when administered concurrently.
3. Anti-psychotics such as: Haloperidol[1], Clozapine[1], Molindone[1]
- May have additive CNS depressant effects with multiple doses
4. Atypical anti-psychotics such as: Olanzapine[1], Pimozide[1], Quetiapine[1], Risperidone[1]
5. Azole anti-fungals[2] such as: Itraconazole[1], Voriconazole[3], Ketoconazole[2]
- Itraconazole: May result in a 34% increase in zolpidem AUC. May reduce zolpidem clearance.
- Voriconazole: Increases in peak plasma concentrations of zolpidem by 1.23-fold and the AUC by 1.48-fold may occur.
- Ketoconazole: May reduce oral clearance of zolpidem by 41%, may prolong half-life by about 26%, and CNS activity or side effects of zolpidem may be increased.
6. General Anesthetics[1]
- These drugs are CNS depressants and may have cumulative sedative effects when administered concurrently.
7. Opiate agonists/antagonists such as: buprenorphine [1], butorphanol [1], nalbuphine [1], pentazocine [1]
- These drugs are CNS depressants and may have cumulative sedative effects when administered concurrently.
8. Sedating H1-blockers such as diphenhydramine[1]
- These drugs are CNS depressants and may have cumulative sedative effects when administered concurrently.
9. Tricyclic antidepressants such as: imipramine[4] and desipramine[4]
10. Miscellaneous: Chlorpromazine, [1], Tramadol[1]Trazodone[1], Pregabalin[1], Valproic acid[5]
- Valproic Acid: One case report of sleep walking
Drugs That Lead to Decreased Zolpidem Efficacy
1. Flumazenil
- Antagonizes the effects of zolpidem and can reverse the sedative/hypnotic effects seen with zolpidem.[6] [1]
Drugs That Interfere with CYP3A4 Metabolism
1. Anti-retroviral protease inhibitors such as: delavirdine (Link Here) Nevirapine (Link Here)
- May act by inhibiting CYP3A4 and increasing zolpidem concentrations. This may cause excessive sedation and possible respiratory depression.
- Nevirapine - Induces CYP450 enzymes and may decrease the plasma concentrations.
2. Miscellaneous such as: Imatinib, Aprepitant (Link Here), Conivaptan (Link Here), Ranolazine (Link Here), Rifamycins (Link Here), Rifabutin (Link Here), Rifapentine (Link Here), Rifampin[1]
- Imatinib: May potently inhibit cytochrome P450 3A4 and is expected to inhibit zolpidem CYP3A4 metabolism(Link Here).
- Aprepitant: Potentially increases serum concentrations of zolpidem by interfering with zolpidem metabolism by CYP3A4
- Conivaptan: Potently inhibits cytochrome P450 3A4, and may inhibit zolpidem CYP3A4 metabolism
- Ranolazine: May inhibit zolpidem CYP3A4 metabolism
- Rifamycins / Rifabutin / Rifapentine: May increase the clearance of zolpidem by inducing hepatic metabolism
- Rifampin: Reduces zolpidem AUC by ~73%, Cmax by ~58%, and T1/2 by ~36%. Significant reduction in zolpidem efficacy may also result.
Herbals/Food that May Increase CNS Depression
1. Herbals such as: Valerian[1], Kava Kava[7]
- Kava Kava: May increase CNS effects of zolpidem by disrupting GABAnergic action at the receptor site
2. Miscellaneous such as: Pramiprexole[1]
Medications/Herbals that Have Been Shown to Increase CNS Effects
1. Selective serotonin re-uptake inhibitors ([[SSRIs]) such as: Duloxetine[4] [8] and Venlafaxine[4] [8], Fluoxetine[1], Sertraline[1]
- Fluoxetine: Zolpidem half-life decreases by 17% after multiple doses of fluoxetine.
- Sertraline: Zolpidem Cmax increases by ~43% and Tmax decreases by ~53%.
- Disorientation, delusions, or hallucinations have rarely been reported.
2. Serotonin norepinephrine re-uptake inhibitors ([SNRIs]) such as: duloxetine[4] [8], venlafaxine .[4] [8]
3. Herbals such as: St. John’s Wort[4]
Back to Zolpidem
References
- ↑ 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 1.11 1.12 1.13 1.14 1.15 1.16 1.17 1.18 1.19 1.20 1.21 1.22 1.23 1.24 1.25 1.26 1.27 1.28 1.29 Sanofi-Aventis. Ambien (zolpidem) Package Insert. New York, N.Y., 2004 March.
- ↑ 2.0 2.1 Greenblatt DJ, von Moltke LL, Harmatz JS, et al. Kinetic and dynamic interaction study of zolpidem with ketoconazole, itraconazole, and fluconazole. Clin Pharmacol Ther 1998;64:661—71.
- ↑ Saari TI, Laine K, Leino K, et al Effect of voriconazole on the pharmacokinetics and pharmacodynamics of zolpidem in healthy subjects. Br J Clin Pharmacol 2007;63:116—20.
- ↑ 4.0 4.1 4.2 4.3 4.4 4.5 4.6 Elko CJ, Burgess JL, Robertson WO. Zolpidem-associated hallucinations and serotonin reuptake inhibition: a possible interaction. J Toxicol Clin Toxicol 1998;36:195—203.
- ↑ Sattar SP, Ramaswamy S, Bhatia SC, et al. Somnambulism due to probable interaction of valproic acid and zolpidem. Ann Pharmacother. 2003;37:1429—33
- ↑
- ↑ Sheree Cairney PMARCACJCBJC. Saccade and cognitive impairment associated with kava intoxication. Vol 18; 2003:525-533. (Link Here)
- ↑ 8.0 8.1 8.2 8.3 Richelson E. Pharmacokinetic Drug Interactions of New Antidepressants: A Review of the Effects on the Metabolism of Other Drugs. Vol 72; 1997:835-847.
