Alimta

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

Inside the cells, the active element passes with the participation of protein folate synthesizing structures that have the function of movement, as well as the transporter of previously restored folates. At this time, pemetrexed under the action of the enzyme FPGS transformed, acquiring polyglutamate form.

Indications Alimta

It is used in the treatment of such malignant tumors:

• pleural mesothelioma ;
• pulmonary carcinoma locally common;
• non-small cell and non-lung carcinoma of the lung, having a metastatic form (adenocarcinoma or large cell carcinoma).

[1]

Release form

The release of the therapeutic substance is realized in the form of an infusion powder, inside the flasks. In the box - 1 bottle.

[2]

Pharmacodynamics

Therefore, since polyglutamine metabolic elements have an extended half-life term, the duration of therapeutic effect of drugs also increases.

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

[3], [4], [5], [6], [7]

Pharmacokinetics

Protein intraplasma synthesis is approximately 81%; synthesis processes do not change even in case of insufficiency of the kidneys in a patient. Inside the liver, only limited pemetrexed metabolism is observed.

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

[8]

Dosing and administration

The finished medicinal fluid is injected through an IV drip, in / in the method (the procedure lasts 10 minutes). Often the drug 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 treating doctor, who takes into account the stage of development of the pathology. Before starting therapy, dexamethasone should be used (4 mg 2 times a day (one day before the start of treatment, the day the course starts, and the next day after)) in order to reduce the frequency and intensity of epidermal reactions regarding the effect of the drug.

[15], [16]

Use Alimta during pregnancy

You can not use Alimtoy for HB or pregnancy.

[9]

Contraindications

It is contraindicated to prescribe to people with a history of intolerance to pemetrexed or any of the auxiliary components of the drug.

[10], [11], [12]

Side effects Alimta

Among the side effects that occur with the introduction of an infusion fluid:

• lesions of the hematopoietic function: leuko-, thrombocyto- or neutropenia, as well as anemia;
• problems with the epidermis and skin appendages: rash, erythema multiforme, peeling, alopecia and itching;
• Violations in the PNS: neuropathy with a motor or sensory nature;
• disorders of the gastrointestinal tract: vomiting, pain in the abdomen, diarrhea or constipation, anorexia, stomatitis, nausea, increased AST or ALT, pharyngitis and colitis (occasionally);
• signs from the cardiovascular system: tachycardia with supraventricular character;
• urinary function disorders: an increase in creatinine;
• other disorders: conjunctivitis, urticaria, severe fatigue, neutropenic fever, interstitial forms of pneumonitis, fever and dehydration.

[13], [14]

Overdose

Drug poisoning can lead to bone marrow suppression, the symptoms of which are neutro-and thrombocytopenia, and also anemia. At the same time, diarrhea, secondary infections, and inflammations that affect the mucous membranes can develop.

Symptomatic actions are carried out, and in addition they prescribe the immediate administration of leucovorin or thymidine.

[17], [18], [19]

Interactions with other drugs

The level of clearance of pemetrexed can significantly decrease when the drug is combined with substances that have nephrotoxicity and are excreted through the kidneys.

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

It is allowed to prescribe medication for people with healthy kidney activity in combination with ibuprofen.

People with kidney failure (in moderate or mild form) should be extremely careful to use Alimta in combination with NSAIDs.

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

[20], [21], [22]

Storage conditions

Alimta should be kept in a closed place for small children. Temperature indicators - in the range of marks 15-25 ° C. It is allowed to keep the prepared liquid within 24 hours at temperature values in the range of 2-8 ° C.

[23], [24]

Shelf life

Alimta can be applied within a 3-year period from the moment the pharmaceutical is manufactured.

Application for children

There is no relevant information regarding the use of drugs in pediatrics for the treatment of pleural mesothelioma of a malignant nature, as well as non-small cell pulmonary carcinoma.

[25], [26], [27]

Analogs

Analogues of the drug are substances Navelbin, Taxotere, Paclitaxel with Tarceva, and in addition, Taxol, Photoditazin and Lastet with Iressa.

 

[28], [29], [30], [31], [32]