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Drug Interactions between Exxua and propofol

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Moderate

propofol gepirone

Applies to: propofol and Exxua (gepirone)

MONITOR: Treatment with propofol may lead to prolongation of the QT interval; however, the extent of prolongation and its clinical impact is difficult to determine. A retrospective single-center cohort study in patients treated at the Mayo clinic over 17 years (n=628,784) concluded that torsade de pointes (TdP) after propofol administration occurred at an annual incidence of 1.93 per million; however, it was often associated with other risk factors, including concomitant QT-prolonging medications, low serum potassium levels (<3.5 mmol/L), and low serum magnesium levels (<1.8 mg/dL). Other studies have reported that propofol has no effect or that it decreases the QTc interval and may offset QTc prolongation due to other coadministered anesthetic medications. Theoretically, concurrent use of two or more drugs that can cause QT interval prolongation may result in additive effects and increased risk of ventricular arrhythmias including TdP and sudden death. The risk of an individual agent or a combination of these agents causing ventricular arrhythmia in association with QT prolongation is largely unpredictable but may be increased by certain underlying risk factors such as congenital long QT syndrome, cardiac disease, and electrolyte disturbances (e.g., hypokalemia, hypomagnesemia). In addition, the extent of drug-induced QT prolongation is dependent on the particular drug(s) involved and dosage(s) of the drugs. Data from formal QT/QTc studies on propofol are lacking.

MANAGEMENT: Caution and clinical monitoring is recommended if propofol is used concomitantly with other agents associated with QT interval prolongation. Patients should be advised to seek prompt medical attention if they experience symptoms that could indicate the occurrence of torsade de pointes such as dizziness, lightheadedness, fainting, palpitation, irregular heart rhythm, shortness of breath, or syncope.

References (10)
  1. Whyte SD, Booker PD, Buckley DG (2005) "The Effects of Propofol and Sevoflurane on the QT Interval and Transmural Dispersion of Repolarization in Children." Anesth Analg, 100, p. 71-77
  2. Staikou C, Stamelos M, Stavroulakis E (2014) "Impact of anaesthetic drugs and adjuvants on ECG markers of torsadogenicity." Br J Anaesth, 112, p. 217-30
  3. Toyoda T, Terao Y, Oji M, Okada M, Fukusaki M, Sumikawa K (2013) "The interaction of antiemetic dose of droperidol with propofol on QT interval during anesthetic induction." J Anesth, 27, p. 885-9
  4. Wutzler A, De Asmundis C, Matsuda H, et al. (2018) "Effects of propofol on ventricular repolarization and incidence of malignant arrhythmias in adults." J Electrocardiol, 51, p. 170-4
  5. Kim DH, Kweon TD, Nam SB, Han DW, Cho WY, Lee JS (2008) "Effects of target concentration infusion of propofol and tracheal intubation on QTc interval." Anaesthesia, 63, p. 1061-4
  6. Scalese MJ, Herring HR, Rathburn RC, Skrepnek GH, Ripley TL (2016) "Propofol-associated QTc prolongation." Ther Adv Drug Saf, 7, p. 68-78
  7. Hanci V, Aydin M, Yurtlu BS, et al. (2010) "Anesthesia induction with sevoflurane and propofol: evaluation of P-wave dispersion, QT and corrected QT intervals." Kaohsiung J Med Sci, 26, p. 470-7
  8. Kleinsasser A, Kuenszberg E, Loeckinger A, et al. (2000) "Sevoflurane, but not propofol, significantly prolongs the Q-T interval." Anesth Analg, 90, p. 25-7
  9. Paventi S, Santevecchi A, Ranieri R (2001) "Effects of sevoflurane versus propofol on QT interval." Minerva Anestesiol, 67, p. 637-40
  10. Kleinsasser A, Loeckinger A, Lindner KH, Keller C, Boehler M, Puehringer F (2001) "Reversing sevoflurane-associated Q-Tc prolongation by changing to propofol." Anaesthesia, 56, p. 248-50

Drug and food interactions

Moderate

propofol food

Applies to: propofol

GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents. Use in combination may result in additive central nervous system depression and/or impairment of judgment, thinking, and psychomotor skills.

MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol. Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

References (4)
  1. Warrington SJ, Ankier SI, Turner P (1986) "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology, 15, p. 31-7
  2. Gilman AG, eds., Nies AS, Rall TW, Taylor P (1990) "Goodman and Gilman's the Pharmacological Basis of Therapeutics." New York, NY: Pergamon Press Inc.
  3. (2012) "Product Information. Fycompa (perampanel)." Eisai Inc
  4. (2015) "Product Information. Rexulti (brexpiprazole)." Otsuka American Pharmaceuticals Inc
Moderate

gepirone food

Applies to: Exxua (gepirone)

GENERALLY AVOID: Grapefruit and/or grapefruit juice may increase the plasma concentrations and effects of gepirone. The proposed mechanism is inhibition of CYP450 3A4 mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. Inhibition of hepatic CYP450 3A4 may also contribute. The interaction has not been studied with grapefruit juice, but has been reported for other CYP450 3A4 inhibitors. For example, when subjects who were at steady state on the strong CYP450 3A4 inhibitor ketoconazole (200 mg twice daily) received a single dose of gepirone (36.3 mg), the maximum plasma concentration (Cmax) and systemic exposure (AUC) of gepirone increased by approximately 5-fold. Similarly, when subjects who were at steady state on the moderate CYP450 3A4 inhibitor verapamil (80 mg three times daily) received a single dose of gepirone (18.2 mg), the maximum plasma concentration (Cmax) and systemic exposure (AUC) of gepirone increased by approximately 2.6-fold. In general, the effects of grapefruit products are concentration-, dose-, and preparation-dependent and can vary widely among both brands and individual patients. Some preparations have demonstrated strong CYP450 3A4 inhibition, while others have demonstrated moderate inhibition.

ADJUST DOSING INTERVAL: Food enhances the bioavailability of gepirone and its major active metabolites (3'-OH-gepirone and 1-PP). The magnitude of the effect is dependent on the fat content of the meal, but the systemic exposure of gepirone and its major metabolites was consistently higher under fed conditions as compared to the fasted state. The peak plasma concentration (Cmax) of gepirone after intake of a low-fat (about 200 calorie) breakfast was 27% higher, after a medium-fat (about 500 calorie) breakfast was 55% higher, and after a high-fat (about 850 calorie) breakfast was 62% higher than the Cmax achieved in the fasted state. Likewise, the systemic exposure (AUC) of gepirone was about 14% higher after a low-fat breakfast, 22% higher after a medium-fat breakfast, and 32% to 37% higher after a high-fat breakfast when compared to the AUC achieved in the fasted state. The effect of varying amounts of fat on the AUC and Cmax of 3'-OH-gepirone and 1-PP were similar to that of gepirone.

MANAGEMENT: Coadministration of gepirone with grapefruit products should be avoided. If grapefruit juice is consumed, monitoring for adverse effects (e.g., QT prolongation, serotonin syndrome, dizziness, nausea, insomnia, abdominal pain, and/or dyspepsia) should be considered. Gepirone should be taken orally with food at the approximately the same time each day. Tablets should be swallowed whole.

References (4)
  1. (2023) "Product Information. Exxua (gepirone)." Mission Pharmacal Company, 1
  2. FDA. U.S. Food and Drug Administration (2024) Grapefruit juice and some drugs don't mix. https://www.fda.gov/consumers/consumer-updates/grapefruit-juice-and-some-drugs-dont-mix
  3. Chen M, Zhou S, Fabriaga E, Zhang P, Zhou Q (2024) Food-drug interactions precipitated by fruit juices other than grapefruit juice: an update review. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9326888/
  4. Kiani J, Imam SZ (2024) Medicinal importance of grapefruit juice and its interaction with various drugs. https://nutritionj.biomedcentral.com/articles/10.1186/1475-2891-6-33

Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

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