Itrasec

Properties

Itrasec is a gynecological product for oral use, containing Itraconazole, a broad-spectrum antifungal and Secnidazole as a tricomonicide antiprotozoal. Itraconazole inhibits ergosterol synthesis in fungi; This is the reason for its antifungal effect. Itraconazole binds to plasma proteins by 99.8%, the concentration in the blood is 60% higher than the plasma concentration and in the skin it is five times higher than the plasma concentration.

Secnidazole is a derivative of 5-nitroimidazoles and, like these, it produces DNA degradation and inhibition of nucleic acid synthesis, being equally effective against cells that are in their division phase or that are not. Secnidazole is rapidly distributed in the body and reaches good concentrations in organs and soft tissues. It is very well absorbed orally, but it does not do so quickly, so very high serum concentrations appear after 48 and 72 hours after administration.

Therapeutic indications

Itrasec is an oral anti-infective for gynecological treatments such as vaginosis caused by any of the Candida and Trichomonas vaginalis species and vaginosis caused by Gardnerella vaginalis, Anaerobic bacteria and Mobiluncus sp.

Cautions

Itrasec should not be administered during pregnancy and lactation. It is contraindicated during the second half of the menstrual cycle, unless an adequate contraceptive is used or the pregnancy detection test is negative. It has the ability to interact with other medications of clinical importance; it is contraindicated in hypersensitivity to the components of the formulation.

Decreased gastric acidity

When gastric acidity is decreased, the absorption of Itrasec is disturbed, as well as in patients receiving acidity-reducing medications (aluminum hydroxide); This must be administered at least 2 hours before the administration of Itrasec.

In certain AIDS patients suffering from achlorhydria and in patients with suppressors of acid secretion (example H2 antagonist) it is advisable to administer the drug with cola drinks.

Renal insufficiency

The oral bioavailability of Itraconazole may be lower in patients with renal failure.


Side effects

Itrasec, despite being generally well tolerated, can produce a bad taste in the mouth, nausea, vomiting, heartburn, epigastric burning, gastralgias and vertigo. All these effects have been of a slight and transitory nature in a general sense.

Drug and other interactions

Itrasec should not be administered at the same time with disulfiran and alcoholic beverages because they produce intolerance and phenobarbital apparently decreases the serum half-life of Itrasec. When associated with lithium, it can cause lithium toxicity. Medicines that affect the metabolism of Itraconazole: Enzyme-inducing drugs such as rifampin, rifabutin, carbamazepine, isoniazid and phenytoins, significantly reduce the bioavailability of Itraconazole. As it is metabolized through CYP3A4, powerful inhibitors of this enzyme can increase the bioavailability of Itraconazole such as: ritonovir, indinavir and clarithromycin.

Effects of Itraconazole on the metabolism of other drugs

Itraconazole can inhibit the metabolism of drugs metabolized by the cytochrome 3A family. This may result in an increase or prolongation of its effects, including adverse effects.

  • Medicines not to be used during treatment with Itraconazole: terfenadine, astemizole, cisapride, triazolam, oral midazolam, quinidine, pimozide, HMG-CoA reductase inhibitors metabolized by CYP3A4 such as Simvastatin.
  • Medicines for monitoring plasma levels or side effects: Its dosage, if co-administered with Itraconazole, should be reduced if necessary.
  • Anticoagulants.
  • Inhibitors of anti-HIV proteases, such as ritonavir, indinavir, saquinavir.
  • Certain antineoplastic agents such as vinca alkaloids, busulfan, docetaxel, and trimetrexate.
  • Calcium channel blockers metabolized by CYP3A4 such as dihydropyridines and verapamil.
  • Certain immunosuppressive agents: Cyclosporine, tacrolimus, rapamycin.
  • Others: Digoxin, carbamazepine, buspirone, alfentanil, alprazolam, midazolam IV, rifabutin, methylprednisolone.
  • No interactions of Itraconazole with AZT (Zidovudine) and fluvastatin have been observed.

No interactions of Itraconazole with the metabolism of ethinyl estradiol and norestisterone (oral contraceptives) have been observed.

Protein binding effect: In vitro studies show that there is no interaction in plasma protein binding between Itraconazole and propanolol, imipramine, diazepam, cimetidine, indomethacin, tolbutamide and sulfametazine.

Posology

 

Two oral caplets, every 12 hours together with food, for three days.

Composition

Each coated caplet contains:

Itraconazole     33.3 mg

Secnidazole     166.6 mg

C.S.P. excipients     1 caplet


Administration route

Oral


Presentation

Box containing 2 blisters with 6 caplets each.


Storage recommendations

Keep in a cool dry place below 30 °C.


Alterations in the results of laboratory tests

Itrasec can interfere with liver enzyme measurements in the blood, producing abnormally low results. It can also interfere with the hexokinase method of measuring blood glucose concentrations. It has been reported to interfere with assays for procainamide blood concentrations.

Precautions and relationship with effects of carcinogenesis, mutagenesis, teratogenesis and fertility

Itrasec is metabolized mainly in the liver, although in short treatments it has not been associated with liver failure or in those who have shown hepatotoxicity to other compounds. ITRASEC has not been studied in children; therefore use in pediatric patients should be avoided unless the benefits outweigh the risks.

ITRASEC can be used without carcinogenic or mutagenic risk. It is apparently free of teratogenic potential.

Warnings

Delicate medicine. Sale under prescription.

Keep out of reach of children.