Precobal

Therapeutic indications

Precobal is indicated in: Neuropathic pain of central or peripheral origin, associated or not with diabetic neuropathy, post-herpetic neuralgia, fibromyalgia, paresthetic states, neuritic and neuralgic disorders in general.

Properties

Precobal effectively combines the analgesic-neuroleptic action of pregabalin with the antineuritic action of mecobalamin.

Pregabalin is an analogue of gamma aminobutyric acid (GABA), which binds to an auxiliary subunit (protein 2-α) of voltage-regulated calcium channels in the central nervous system, strongly displacing H-gabapentin.

Precobal Prevents neuropathic pain and postsurgical pain, including hyperalgesia and allodynia, improves sensory and motor disturbances, decreases the degree of pain and improves quality of life.

The mechanism of action of pregabalin is not exactly known, since it does not interact with GABA-A or B receptors, nor does it affect GABA reuptake. The pharmacological profile of pregabalin is similar to that of gabapentin: it shows an antihyperalgesic and antiallodynic activity 4 times higher than gabapentin. Both pregabalin and gabapentin modulate the release of sensory neuropeptides (substance P and calcitonin gene-related peptide) from rat spinal tissues, but only under conditions involving inflammation of the spinal cord. Mecobalamin is vitamin B12 of the coenzyme type, existing in the blood and brain spinal fluid. Improves disturbances in nucleic acid and protein metabolism in nervous tissue. Compared to cyanocobalamin, it is the only vitamin B12 homologous compound that participates in transmethylation. Facilitates the transfer methylation of RNAs in nerve cells, which play an important role in protein synthesis; and it also stimulates the synthesis of methionine in glial cells.

Increases uridine intake when vitamin B12 and folic acid deficiency are present, and helps restore normal levels of RNAs in nerve cells. It also elevates the incorporation of leucine into the crushed nerves. Facilitates the synthesis of nucleic acids and proteins in nerve cells.

Repairs nerve tissues: Exhibits an inhibitory effect on nerve cell degeneration in nerve disorders induced in rats and rabbits by experimental acrylamide, adriamycin, or vincristine poisoning. Mecobalamin improves sensory disturbances such as numbness and paresthesia, and motor disturbances.


Pharmacokinetics

Pregabalin is rapidly absorbed when administered fasting, with peak plasma concentrations occurring within one hour after single and multiple dose administration. Oral bioavailability is estimated at 90% and is independent of dose. After repeated administration, steady state is achieved in 24-48 hours. Absorption rate decreases when administered with food. The apparent volume of distribution, after oral administration, is approximately 0.56 l / kg. It does not bind to plasma proteins. It is eliminated from the systemic circulation mainly by renal excretion as an unmodified drug. The elimination half-life is 6.3 hours. Plasma and kidney clearance is directly proportional to creatinine clearance.

Once absorbed, mecobalamin binds to a plasma betaglobulin called transcobalamin II to transport it to the tissues. It is rapidly removed from plasma and stored in liver cells, such that up to 90% of the body’s vitamin B12 stores in the normal adult, that is, 1 to 10 mg are in the liver. Mecobalamin is stored as an active coenzyme, with a turnover rate of 0.5 to 0.8 mcg per day, depending on the capacity of body deposits.

Contraindications

Known hypersensitivity to the active substance or to any of the excipients, pregnancy and lactation.

Side  Effects

 

The most commonly reported undesirable effects with pregabalin are: dizziness and drowsiness; they are of mild to moderate intensity.

On the part of mecobalamin, exceptionally, allergic reactions that may include anaphylactic shock, polycythemia and peripheral thrombosis in the treatment of pernicious anemia.

Composition

Each coated tablet contains:

Pregabalin     75 mg

Mecobalamin     500 mcg

C.S.P Excipients     1 coated tablet


Posology and  administration 

 

Route of administration: Oral.

Dosage:

Except for medical criteria, 1 capsule every 12 hours.

Administer preferably 1 or 2 hours after food intake.


Presentation

Box containing 3 blisters with 10 coated tablets each.

Box containing 1 blister with 10 coated tablets each.


Storage Recommendations

Store below 30 °C. Protect  from light and moisture.

 

Cautions and Warnings

Safety and efficacy in children under 12 years of age have not been established. Precobal usually causes drowsiness, which is why it is recommended to observe special care when using machinery and motor vehicles.

Drug interactions

Precobal can enhance the neurodepressant effect of ethanol, lorazepan and oxycodone on cognitive or motor functions.

Co-administration with norestisterone and / or ethinyl estradiol oral contraceptives does not influence the steady state pharmacokinetics of any of the drugs.

Concomitant administration of neomycin and colchicine increases mecobalamin malabsorption; Ascorbic acid can destroy significant amounts of mecobalamin and intrinsic factor, therefore this possibility should be considered when large doses of ascorbic acid are administered concomitantly with mecobalamin orally.