Drug Interactions between gepirone and Hydroxy Compound

Both smoking and excessive caffeine consumption can alter the blood levels of theophylline, which may affect the dosing. Tobacco and marijuana smoke (including secondhand exposure) generally reduces, while caffeine increases, blood levels. In addition, caffeine is a stimulant and may add to the side effects of theophylline such as headache, insomnia, and increases in blood pressure and heart rate. It is best to avoid smoking and to limit caffeine consumption during theophylline therapy. Talk to a healthcare professional if you have any questions or concerns. If you start smoking or undergo smoking cessation, your doctor may need to monitor your blood levels more closely to determine if you need a dose adjustment of theophylline. You should stop taking theophylline and seek medical attention if you experience potential signs and symptoms of excessive drug levels such as nausea, vomiting, persistent headache, insomnia, and rapid heartbeat. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

When theophylline is given with enteral (tube) feedings, blood levels may be decreased due to interference with its absorption. This may reduce the effectiveness of the medication. To minimize potential for interaction, you may interrupt the feeding for one hour before and one hour after the theophylline dose. You may need more frequent blood tests to monitor theophylline levels.

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Alcohol can increase the nervous system side effects of hydrOXYzine such as dizziness, drowsiness, and difficulty concentrating. Some people may also experience impairment in thinking and judgment. You should avoid or limit the use of alcohol while being treated with hydrOXYzine. Do not use more than the recommended dose of hydrOXYzine, and avoid activities requiring mental alertness such as driving or operating hazardous machinery until you know how the medication affects you. Talk to your doctor or pharmacist if you have any questions or concerns.

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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.

Ask your doctor before using theophylline together with caffeine. Using these medications together may increase some of the side effects of theophylline. This can cause nausea, vomiting, insomnia, tremors, restlessness, uneven heartbeats, and seizure (convulsions). Avoid drinks or foods that contain caffeine, such as coffee, tea, cola, and chocolate. You may need a dose adjustment or special test if you use both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

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MONITOR: Coadministration of two or more sympathomimetic agents may increase the risk of adverse effects such as nervousness, irritability, and increased heart rate. Central nervous system (CNS) stimulants, particularly amphetamines, can potentiate the adrenergic response to vasopressors and other sympathomimetic agents. Additive increases in blood pressure and heart rate may occur due to enhanced peripheral sympathetic activity.

MANAGEMENT: Caution is advised if two or more sympathomimetic agents are coadministered. Pulse and blood pressure should be closely monitored.