Alimta

Alimta is an antimetabolite and has a strong antitumor effect. Its main active component is pemetrexed, a multi-target antifolate that can inhibit the activity of elements such as DHFR, TS and GARFT (they are the main folate-dependent enzymes involved in the biosynthesis of thymidine purine nucleotides).

The active element enters the cells with the participation of protein folate-synthesizing structures that have the function of movement, as well as a transporter of previously restored folates. At this time, pemetrexed is transformed under the action of the enzyme FPGS, acquiring a polyglutamate form. [ 1 ]

Indications Alimta

It is used in the treatment of the following tumors of a malignant nature:

• pleural mesothelioma;
• locally advanced pulmonary carcinoma;
• non-small cell and non-squamous cell lung carcinoma that has a metastatic form (adenocarcinoma or large cell carcinoma).

[ 2 ]

Release form

The release of the therapeutic substance is realized in the form of infusion powder, inside vials. In a box - 1 vial.

[ 3 ]

Pharmacodynamics

Because polyglutamated metabolic elements have an extended half-life, the duration of the therapeutic effect of the drug also increases.

The use of Alimta in combination with cisplatin leads to the development of synergistic antitumor activity.

[ 4 ], [ 5 ], [ 6 ], [ 7 ]

Pharmacokinetics

Intraplasmic protein synthesis is approximately 81%; synthesis processes do not change even in patients with renal insufficiency. Only limited pemetrexed metabolism processes are observed within the liver.

After 24 hours from the moment of drug administration, 70-90% of the unchanged component is excreted via the kidneys. The systemic values of intraplasmic clearance of pemetrexed are 92 ml per minute. The plasma half-life in individuals with healthy renal function is 3.5 hours.

[ 8 ]

Dosing and administration

The prepared medicinal liquid is administered through a dropper, intravenously (the procedure lasts 10 minutes). Often the medication is used in combination with cisplatin - to increase the therapeutic effect.

The duration of the treatment cycle and the size of the dosage portion are selected by the attending physician, who takes into account the stage of development of the pathology. Before the start of therapy, dexamethasone should be used (4 mg 2 times a day (the day before the start of treatment, on the day of the start of the course, and also the next day after)) - to reduce the frequency and intensity of epidermal reactions to the action of the drug.

[ 11 ]

Use Alimta during pregnancy

You cannot use Alimta during breastfeeding or pregnancy.

Contraindications

Contraindicated for use in people with a history of hypersensitivity to pemetrexed or any of the excipients of the drug.

[ 9 ]

Side effects Alimta

Side effects that occur when administering infusion fluid include:

• damage to the hematopoietic function: leuko-, thrombocyto- or neutropenia, as well as anemia;
• problems with the epidermis and skin appendages: rashes, erythema multiforme, peeling, alopecia and itching;
• disorders of the PNS: neuropathy of a motor or sensory nature;
• gastrointestinal disorders: vomiting, abdominal pain, diarrhea or constipation, anorexia, stomatitis, nausea, increased AST or ALT levels, pharyngitis and colitis (rarely);
• signs from the cardiovascular system: tachycardia of a supraventricular nature;
• urinary dysfunction: increased creatinine levels;
• other disorders: conjunctivitis, urticaria, severe fatigue, neutropenic fever, interstitial forms of pneumonitis, increased temperature and dehydration.

[ 10 ]

Overdose

Poisoning with the drug can lead to bone marrow suppression, the symptoms of which are neutro- and thrombocytopenia, as well as anemia. Along with this, diarrhea, secondary infections, and inflammation affecting the mucous membranes can develop.

Symptomatic measures are taken, and in addition, immediate administration of leucovorin or thymidine is prescribed.

[ 12 ], [ 13 ], [ 14 ]

Interactions with other drugs

The clearance rate of pemetrexed may be significantly reduced when the drug is combined with substances that are nephrotoxic and excreted through the kidneys.

The drug demonstrates minimal interaction with drugs whose metabolic processes are realized with the participation of these enzymes: CYP3A and CYP2D6 with CYP2C9, as well as CYP1A2.

For people with healthy kidney function, the drug can be prescribed in combination with ibuprofen.

People with moderate or mild renal impairment should use Alimta in combination with NSAIDs with extreme caution.

Pemetrexed should not be mixed with liquids such as Ringer's or Ringer's lactate solutions.

[ 15 ], [ 16 ]

Storage conditions

Alimta should be stored in a place closed to small children. Temperature indicators are in the range of 15-25°C. The prepared liquid can be stored for 24 hours at temperatures in the range of 2-8°C.

[ 17 ]

Shelf life

Alimta can be used within a 3-year period from the date of manufacture of the pharmaceutical product.

Application for children

There is no relevant information regarding the use of the drug in pediatrics for the treatment of malignant pleural mesothelioma and non-small cell lung carcinoma.

[ 18 ], [ 19 ], [ 20 ]

Analogues

The analogs of the drug are Navelbine, Taxotere, Paclitaxel with Tarceva, and also Taxol, Photoditazine and Lastet with Iressa.

[ 21 ], [ 22 ], [ 23 ], [ 24 ]