NEURACALM 75 Pregabalin (75 mg) & Methylcobalamin (750 mcg) Capsules
The description of the drug, Active ingredient, Mechanism of action, Pharmacokinetics and metabolism, Indication and usage, Contraindications, Drug interactions, Warnings, Precautions, Adverse reactions, Drug abuse and dependence, Symptoms of overdose and antidote, Dosage and administration, Preparation for use, Presentation, Storage condition, Manufacturer and Marketer of Neuracalm 75 Capsule Medicine for Pains.
THE DESCRIPTION OF THE DRUG
Brand Name: NEURACALM-75
Generic Name: PREGABALIN (75 MG) & METHYLCOBALAMIN (750 MCG) CAPSULES
Dosage Form And Strength: Solid Oral Dosage Form; Capsule 75mg/750mcg
Net Content 75mg/750mcg
Mechanism Of Action:
Pregabalin is an oral medication that is chemically related to gabapentin (Neurontin, Gabarone). It is used for treating pain caused by neurologic diseases such as postherpetic neuralgia as well as seizures. It also is used for treating fibromyalgia. The mechanism of action of pregabalin is unknown. Pregabalin binds to calcium channels on nerves and may modify the release of neurotransmitters (chemicals that nerves use to communicate with each other). Reducing communication between nerves may contribute to pregabalin’s effect on pain and seizures.
Methylcobalamine: Vitamin B12 normally plays a significant role in the metabolism of every cell of the body, especially affecting the DNA synthesis and regulation but also fatty acid synthesis and energy production. However, many (though not all) of the effects of functions of B12 can replaced by sufficient quantities of folic acid (vitamin B9), since B12 is used to regenerate folate in the body. Most vitamin B12 deficiency symptoms are actually folate deficiency symptoms, since they include all the effects of pernicious anemia and megaloblastosis, which are due to poor synthesis of DNA when the body does not have a proper supply of folic acid for the production of thymine. When sufficient folic acid is available, all known B12 related deficiency syndromes normalize, save those narrowly connected with the vitamin B12-dependent enzymes Methylmalonyl CoenzymeAmutase, and 5-methyltetrahydrofolate-homocystein methyltransferase (MTR), also known as methionine synthase; and the buildup of their respective substrates (methylmalonic acid, MMA) and homocysteine.
Pharmacokinetics And Metabolism
Pregabalin Absorption: Pregabalin is rapidly absorbed when administered on an empty stomach, with peak plasma concentrations occurring within one hour. Pregabalin oral bioavailability is estimated to be greater than or equal to 90% and is independent of dose. The rate of pregabalin absorption is decreased when given with food resulting in a decrease in Cmax by approximately 25 to 30% and a delay in Tmax to approximately 2.5 hours. Administration with food, however, has no clinically significant effect on the extent of absorption.
Distribution: Pregabalin has been shown to cross the blood-brain barrier in mice, rats, and monkeys. Pregabalin has been shown to cross the placenta in rats and is present in the milk of lactating rats. In humans, the volume of distribution of pregabalin for an orally administered dose is approximately 0.56 L/kg and is not bound to plasma proteins.
Metabolism: Pregabalin undergoes negligible metabolism in humans. Approximately 98% of the radioactivity recovered in the urine was unchanged pregabalin. The major metabolite is N-methyl pregabalin.
Excretion: Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug. Renal clearance of pregabalin is 73mL/minute
Methylcobalamine: methylcobalamin as adenosylcobalamin and hydroxocobalamin. These act as co-enzymes in the trans methylation of homocysteine to methionine; in the isomerisation of methylmalonyl co-enzyme to succinyl co-enzyme and with folate in several metabolic pathways respectively. Deficiency of Vitamin B12 interferes with haemopoiesis and produces megaloblastic anaemia.
INDICATIONS AND USAGE
• Possesses anxiolytic, analgesic and anticonvulsant activity.
• Possess high bioavailability (90% vs 33-66%) compared to gabapentin.
• Highly effective in relieving the neuropathic pain.
• Improves mood and reduces sleep disturbance.
• Acts as neuroprotective, promotes myelination in neurons.
• Relieves burning sensation, numbness, loss of sensation & muscle cramps in diabetic neuropathy.
• Peripheral Neuropathy.
• Diabetic Neuropathy.
• Drug Induced Neuropathy
Hypersensitivity. Pregnancy, lactation. Driving or working with machines or do other dangerous activities.
Concurrent use with oxycodone, lorazepam and ethanol may increase the CNS effects.
• May cause peripheral oedema.
• Regular vision check is recommended.
• May decrease platelet count and prolong PR interval.
• Discontinue treatment if patients develop severe angioedema.
• Withdraw treatment gradually over at least 1 week.
Dizziness, drowsiness, visual disturbance (including blurred vision, diplopia), ataxia, dysarthria, tremor, lethargy, memory impairment, euphoria, weight gain, constipation, dry mouth, peripheral edema, depression, confusion, agitation, hallucinations, myoclonus, hypoaesthesia, hyperaesthesia, tachycardia, excessive salivation, sweating, flushing, rash, muscle cramp, myalgia, arthralgia, urinary incontinence, dysuria, thrombocytopenia, neutropenia, 1st heart block, hypotension, hypertension, pancreatitis, dysphagia, oliguria, rhabdomyolysis.
DRUG ABUSE AND DEPENDANCE
SYMPTOMS OF OVERDOSE AND ANTIDOTE
Pregabalin: In overdoses up to 15g, no unexpected adverse reactions were reported. In the post-marketing experience, the most commonly reported adverse reactions observed when pregabalin was taken in overdose included somnolence, confusional state, agitation, and restlessness. Treatment of pregabalin overdose should include general supportive measures and may include haemodialysis if necessary.
Methyl cobalamine: Most nutrients have an established tolerable upper intake level, helping you identify the maximum amount you can safely consume. Since Methyl cobalamine is generally safe, even at high doses, there is no UL set for the vitamin.
DOSAGE AND ADMINISTRATION
One capsule two or three times daily or as directed by physician.
PREPARATION FOR USE
3 x 10 Capsule Alu-Alu Pack
Store in a dry place at a temperature below 30oC.
Name and Address of Manufacturer
WEST-COAST Pharmaceutical Works Ltd.
FP No. 17 & 16/5, Medi Estate, B/S Meidi Mata Temple
Near Gota Railway Crossing, At & post Gota, Ahmeddabad – 382 481
OSBIL PHARMACY LIMITED
23 Buba Marwa Road Ijegun
Satelite Town Lagos, Nigeria.