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Kaletra Oral Solution and Tamsulosin Capsules

Determining the interaction of Kaletra Oral Solution and Tamsulosin Capsules and the possibility of their joint administration.

Check result:
Kaletra Oral Solution <> Tamsulosin Capsules
Relevance: 05.01.2023 Reviewer: Shkutko P.M., M.D., in

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Consumer:

Using tamsulosin together with ritonavir is not recommended. Combining these medications may significantly increase the blood levels and effects of tamsulosin. This may cause blood pressure to fall excessively and heart rate to increase, especially when you rise from a sitting or lying position. The risk of other side effects such as dizziness, lightheadedness, fainting, headache, flushing, nasal congestion, heart palpitation, and priapism (prolonged and painful erection unrelated to sexual activity) may also increase. Let your doctor know if you develop these symptoms while using tamsulosin and they do not go away on their own or they become troublesome. Avoid driving or operating hazardous machinery until you know how the medication affects you, and use caution when getting up from a sitting or lying position. 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.

Professional:

GENERALLY AVOID: Coadministration with potent inhibitors of CYP450 3A4 may significantly increase the plasma concentrations of tamsulosin, which is primarily metabolized by the hepatic microsomal isoenzymes CYP450 3A4 and 2D6. Severe hypotension and priapism may occur. In 24 healthy volunteers, administration of a single 0.4 mg dose of tamsulosin with the potent CYP450 3A4 inhibitor ketoconazole (400 mg once daily for 5 days) resulted in a 2.2-fold increase in tamsulosin peak plasma concentration (Cmax) and 2.8-fold increase in systemic exposure (AUC). The magnitude of interaction may be increased further in individuals who have genetic polymorphisms of CYP450 2D6 resulting in reduced or absent enzyme activity, or so-called CYP450 2D6 poor metabolizers (approximately 7% of Caucasians and less than 2% of Asians and individuals of African descent). When a single 0.4 mg dose of tamsulosin was given to 24 healthy volunteers with the potent CYP450 2D6 inhibitor paroxetine (20 mg once daily for 9 days), tamsulosin Cmax and AUC increased by a factor of 1.3 and 1.6, respectively. A similar increase in exposure is expected in CYP450 2D6 poor metabolizers as compared to extensive metabolizers, hence a potentially greater impact of CYP450 3A4 inhibition.

MANAGEMENT: Since CYP450 2D6 poor metabolizers cannot be readily identified, concomitant use of tamsulosin with potent CYP450 3A4 inhibitors should generally be avoided. If tamsulosin administration is discontinued for several days or more at either the 0.4 or 0.8 mg dose, therapy should be reinitiated with the 0.4 mg once-daily dose and titrated gradually as needed.

References
  • "Product Information. Flomax (tamsulosin)." Boehringer-Ingelheim, Ridgefield, CT.
  • Franco-Salinas G, de la Rosette JJ, Michel MC "Pharmacokinetics and pharmacodynamics of tamsulosin in its modified-release and oral controlled absorption system formulations." Clin Pharmacokinet 49 (2010): 177-88
  • Kamimura H, Oishi S, Matsushima H, et al. "Identification of cytochrome P450 isozymes involved in metabolism of the alpha1-adrenoceptor blocker tamsulosin in human liver microsomes." Xenobiotica 28 (1998): 909-22
Kaletra Oral Solution

Generic Name: lopinavir / ritonavir

Brand name: Kaletra

Synonyms: Kaletra

Tamsulosin Capsules

Generic Name: tamsulosin

Brand name: Flomax

Synonyms: Tamsulosin

In the course of checking the drug compatibility and interactions, data from the following reference sources was used: Drugs.com, Rxlist.com, Webmd.com, Medscape.com.

Interaction with food and lifestyle