Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin Pharmacology

Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin

About Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Mechanism of Action of Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Pharmacokinets of Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Onset of Action for Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Duration of Action for Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Half Life of Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Side Effects of Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Contra-indications of Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Special Precautions while taking Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
N/A
Pregnancy Related Information
Use with caution
Old Age Related Information
N/A
Breast Feeding Related Information
Contraindicated
Children Related Information
N/A
Indications for Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
1.Diabetic neuropathy
2.Peripheral neuropathy
Interactions for Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Typical Dosage for Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Schedule of Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Storage Requirements for Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Effects of Missed Dosage of Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Effects of Overdose of Alpha-lipoic acid + Mecobalamin + Vit B6 + Folic Acid + Gabapentin
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Alpha-Lipoic acid

About Alpha-Lipoic acid
Naturally occurring dithiol compound , antioxidant, Agent for neuropathies.
Mechanism of Action of Alpha-Lipoic acid
Alpha-lipoic acid and its reduced metabolite, Dihydrolipoic acid (DHLA), form a redox couple and may scavenge a wide range of reactive oxygen species. Alpha-lipoic acid has been found to decrease urinary isoprostanes, O-LDL and plasma protein carbonyls, markers of oxidative stress. Further, alpha-lipoic acid and its redox couple DHLA have been found to have antioxidant activity in aqueous, as well as in lipophilic regions, and in extra cellular and intracellular environments. Alpha-lipoic acid participates in the recycling of other important biologic antioxidants, such as vitamins E and C, Ubiquinone and glutathione.
Both alpha-lipoic acid and DHLA can scavenge hydroxyl radicals, the nitric oxide radical, peroxynitrite, hydrogen peroxide and hypochlorite. Alpha-lipoic acid may scavenge singlet oxygen, and DHLA may scavenge super oxide and peroxyl reactive oxygen species.
Pharmacokinets of Alpha-Lipoic acid
Absorption: Alpha-lipoic acid is absorbed from the small intestine. The natural R-entantiomer is more readily absorbed than the L-entantiomer and is the more active form.
Distribution:It is distributed to the liver via the portal circulation and to various tissues in the body via the systemic circulation. . Alpha-lipoic acid readily crosses the blood-brain barrier. It is found, after its distribution to the various body tissues, intracellularly, intramitochondrialy and extracellularly.Metabolism: Alpha-lipoic acid is metabolized to its reduced form, dihydrolipoic acid (DHLA), by mitochondrial lipoamide dehydrogenase enzyme. DHLA, together with lipoic acid, form a redox couple. It is also metabolized to lipoamide, which functions as the lipoic acid cofactor in the multienzyme complexes that catalyze the oxidative decarboxylations of pyruvate and alpha-ketoglutarate. Alpha-lipoic acid may be metabolized to dithiol octanoic acid, which can undergo catabolism.
Onset of Action for Alpha-Lipoic acid
N/A
Duration of Action for Alpha-Lipoic acid
N/A
Half Life of Alpha-Lipoic acid
N/A
Side Effects of Alpha-Lipoic acid
1.Nausea
2.Vomiting
Contra-indications of Alpha-Lipoic acid
1.Contraindicated during radiotherapy
Special Precautions while taking Alpha-Lipoic acid
Patient with diabetes and problems with glucose intolerance
Pregnancy Related Information
Use with caution
Old Age Related Information
N/A
Breast Feeding Related Information
Use with caution
Children Related Information
N/A
Indications for Alpha-Lipoic acid
1.Diabetic neuropathy
2.It may help prevent the oxidation of LDL cholesterol and may be protective, generally, against oxidative stress and, specifically, against atherosclerosis, ischemia-reperfusion injury and various radiologic and chemical toxins.
3.It may also be useful in some inborn metabolic disorders
Interactions for Alpha-Lipoic acid
N/A
Typical Dosage for Alpha-Lipoic acid
Adult: up to 600 milligrams daily
Diabetic neuropathy: 300 milligrams daily taken in divided doses.
Schedule of Alpha-Lipoic acid
N/A
Storage Requirements for Alpha-Lipoic acid
Store at room temperature away from moisture and heat.Keep out of the reach of children. Keep the medicine from freezing. Do not refrigerate.
Effects of Missed Dosage of Alpha-Lipoic acid
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose.Continue the regular schedule.Do not double the dose.
Effects of Overdose of Alpha-Lipoic acid
Give supportive measures and symptomatic treatment.

Mecobalamin

About Mecobalamin
Water soluble, Form of Vitamin B12
Mechanism of Action of Mecobalamin
Mecobalamin is the neurologically active form of vitamin B12 and occurs as a water-soluble vitamin in the body. It is a cofactor in the enzyme methionine synthase, which functions to transfer methyl groups for the regeneration of methionine from homocysteine. In anaemia, it increases erythrocyte production by promoting nucleic acid synthesis in the bone marrow and by promoting maturation and division of erythrocytes.
Pharmacokinets of Mecobalamin
Absorption: Absorbed after oral, sublingual, injection
Excretion: Excretion via urine
Onset of Action for Mecobalamin
N/A
Duration of Action for Mecobalamin
N/A
Half Life of Mecobalamin
N/A
Side Effects of Mecobalamin
1.Oral: Anorexia, nausea, vomiting and diarrhea
2.Parenteral: Rash, headache, hot sensation, diaphoresis and pain/induration at IM inj site
Contra-indications of Mecobalamin
N/A
Special Precautions while taking Mecobalamin
N/A
Pregnancy Related Information
May be used
Old Age Related Information
May be used
Breast Feeding Related Information
May be used
Children Related Information
N/A
Indications for Mecobalamin
1.Peripheral neuropathies
2.Megaloblastic anaemia
Interactions for Mecobalamin
1.Decreased GI tract absorption with neomycin, aminosalicylic acid, H2-blockers and colchicines
2.Reduced serum concentrations with oral contraceptives
3.Reduced effects in anaemia with parenteral chloramphenicol
Typical Dosage for Mecobalamin
Peripheral neuropathies
Oral: Adult: 1500 mcg/day in 3 divided doses
Parenteral: 500 mcg daily IM/IV 3 times/wk

Megaloblastic anaemia caused by vitamin B12 deficiency
Parenteral: Adult: 500 mcg daily IM/IV 3 times/wk. Maintenance dose: After about 2 mth of therapy, reduce dose to single admin of 500 mcg every 1-3 mth.
Schedule of Mecobalamin
N/A
Storage Requirements for Mecobalamin
Oral: Store at room temperature. Protect from moisture and light.
Parenteral: Store at room temperature. Do not expose to direct light.


Effects of Missed Dosage of Mecobalamin
N/A
Effects of Overdose of Mecobalamin
N/A

Vit B6

About Vit B6
Physiological functions: It is involved as a coenzyme (Pyridoxal phosphate) in metabolism of tryptophan, in several metabolic transformations of amino acids including transamination, decarboxylation & racemization.
Deficiency symptoms: Peripheral neuritis, seizures, stomatitis, glossitis, anaemia, seborrhea like lesions.
Mechanism of Action of Vit B6
Vitamin B6 is a collective term for Pyridoxine, Pyridoxal, Pyridoxamine and their phosphorylated derivatives such as Pyridoxine phosphate, Pyridoxal phosphate and Pyridoxamine derivatives respectively. Vitamin B6 is essential for the metabolism of amino acid, glycogen and fatty acids, for nerve functions, for the formation of red blood cells and also helps the skin healthy. Vitamin B6 is also used for the synthesis of nucleic acid, Haemoglobin, Sphingomyelin, other Sphingolipids, Serotonin, Dopamine, Noradrenaline and GABA.
Pharmacokinets of Vit B6
Absorption: Vitamin B6 is readily absorbed after oral administration.
Distribution: It is mainly distributed in the body in protein bound form. It is stored primarily in the liver and to a lesser extent muscle and brain.
Metabolism: It is metabolised in the liver
Onset of Action for Vit B6
N/A
Duration of Action for Vit B6
N/A
Half Life of Vit B6
15-20 days
Side Effects of Vit B6
1. Neuropathy
2. Unstable gait
3. Drowsiness
4. Perioral numbness
5. Paresthesia
6. Numbness of feet
7. Somnolence
8. Sensory neuropathy
9. Ataxia
Contra-indications of Vit B6
1. Hypersensitivity to Vitamin B6
Special Precautions while taking Vit B6
N/A
Pregnancy Related Information
May be used
Old Age Related Information
May be used
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
NEONATES: Contraindicated
Indications for Vit B6
1. Vitamin B6 deficiency including inadequate diet and drug induced causes
2. Neuropathy
3. Premenstrual syndrome
4. Hyperoxaluria type 1
5. Metabolic disorder
6. Isoniazid poisoning
Interactions for Vit B6
Cycloserine, Hydralazine, Isoniazide, Oral contraceptive, Penicillamine: Increase Pyridoxine requirement.
Levodopa: Pyridoxine reverses the therapeutic effect of Levodopa.
Phenobarbital, Phenytoin: Pyridoxine decreases serum level of these anticonvulsants.
Typical Dosage for Vit B6
Adult: 10 - 20 mg / day
Dietary deficiency: 2.5 -10 mg / day for effective therapeutic response is obtained.
Maintenance dose: 2 - 5 mg / day for several weeks.
Drug induced deficiency: 100 - 200 mg / day for 3 weeks.
Maintenance dose: 25 - 100 mg / day
Neuropathy: 50 - 200 mg /day
Premenstrual syndrome: 40 - 500 mg / day
Hyperoxaluria type 1: 25 - 300 mg / day
Metabolic disorder: 100-500 mg /day.
Isoniazid poisoning: Initial dose: 1 - 4 g as IV administration, then 1 g IM every 30 minute until Pyridoxine dose is equal to the Isoniazid dose has been given.
Schedule of Vit B6
N/A
Storage Requirements for Vit B6
Store it at 15 - 30 degree C. Protect from moisture and heat.
Effects of Missed Dosage of Vit B6
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Vit B6
Give supportive measures and symptomatic treatment. The signs of Pyridoxine overdose can be resolved by discontinuation (withdrawal) of Pyridoxine.

Folic Acid

About Folic Acid
Dietary supplement, Folate derivative( B9 ), Water Soluble Vitamin.
Mechanism of Action of Folic Acid
Folic acid reduced by enzymes folate reductase and dihydrofolate reductase and forms dihydrofolic acid tetrahydrofolic acid respectively. Tetrahydrofolic acid acts as a coenzyme which mediates a number of one carbon transfer reactions by carrying a methyl group as an adduct. It involves a number of reactions such as 1).conversion of homocysteine to methionine. 2).synthesis of thymidylate which is an essential constituent of DNA from methylene-tetrahydrofolic acid. 3). Conversion of serine to glycine by tetrahydrofolic acid and forms methylene-tetrahydrofolic acid. 4).to introduce carbon units at position 2 and 8 during de novo purine synthesis requires formyl-tetrahydrofolic acid and methenyl-tetrahydrofolic acid.5).generation and utilization of "formate pool". 6).For mediating formino group transfer in histidine metabolism. Folic acid is required to maintain normal erythropoiesis and nucleoprotein synthesis.
Pharmacokinets of Folic Acid
Absorption: Well absorbed orally
Distribution: Widely distributed in the body and highest concentration is seen in liver. It appears in the CSF and breast milk
Metabolism: Metabolized in to N-methyl tetrahydrofolic acid in liver
Excretion: Extra drug is excreted unchanged in urine. A small portion of folate is lost by a combination of urinary and fecal excretion and oxidative cleavage of molecule.
Onset of Action for Folic Acid
Oral: 20 to 30minutes
I.V.: 5 minutes
I.M.:10 to 20minutes
Duration of Action for Folic Acid
Oral: 3 to 6 hours
I.V.:3 to 6minutes
I.M.:3 to 6hours
Half Life of Folic Acid
N/A
Side Effects of Folic Acid
N/A
Contra-indications of Folic Acid
N/A
Special Precautions while taking Folic Acid
1. In patients with undiagnosed anaemia; because it may mask pernicious anaemia
2. In pernicious anaemia and other megaloblastic where vitamin B12 is deficient
Pregnancy Related Information
May be used
Old Age Related Information
May be used
Breast Feeding Related Information
May be used
Children Related Information
May be used
Indications for Folic Acid
1. Megaloblastic anaemia
2. Folic acid deficiency
3. Anaemias of pregnancy
4. Nutritional anaemia
5. Alcoholism
6. Tropical sprue
7. Non tropical sprue
Interactions for Folic Acid
1. Hypersensitivity reactions with injection form
2. Bronchospasm
Typical Dosage for Folic Acid
Oral: 5mg 1 to 4 times daily; depending up on the severity of deficiency.
Maintenance dosage: Half of the therapeutic dosage.
Children: 2.5 to 5mg 1 to 2 times daily.
Schedule of Folic Acid
C1 (Oral)
C (Parenteral)
Storage Requirements for Folic Acid
Store at controlled room temperature at a range of 15 to 25 degree C in a well closed container. Protect from excess heat, light and moisture.
Effects of Missed Dosage of Folic Acid
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Folic Acid
Relatively non toxic. Provide symptomatic treatment and supportive measures.

Gabapentin

About Gabapentin
A GABA analogue, Anticonvulsant, Mood stabilizer.
Mechanism of Action of Gabapentin
Gabapentin is a GABA derivative and it bounds to lipophilic molecule. The mechanism of action of Gabapentin is not exactly known. It crosses blood brain barrier and enhances release of GABA.
Pharmacokinets of Gabapentin
Absorption: It is not well absorbed after oral administration. The bioavailability is not dose dependent. Distribution: Gabapentin is distributed in the body in unbound form. Drug crosses blood brain barrier. Metabolism: Gabapentin undergoes insignificant metabolism. Excretion: Drug is excreted mainly in urine.
Onset of Action for Gabapentin
Within few weeks
Duration of Action for Gabapentin
6 - 8 hours
Half Life of Gabapentin
5 -8hours
Side Effects of Gabapentin
1.Dizziness
2.Somnolence
3.Tremor
4.Ataxia
5.Nausea
6.Vomiting
7.Convulsions
8.Dyspepsia
9.Headache
10.Fatigue
11.Diplopia
12.Nystagmus
13.Anorexia
14.Leukopenia
Contra-indications of Gabapentin
1.Hypersensitivity to Gabapentin
Special Precautions while taking Gabapentin
1.Renal impairment
2.Slowly withdraw the drug with caution
3.Use caution when driving vehicle, operating machine or performing other hazardous activities.
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution.
Breast Feeding Related Information
Use with caution.
Children Related Information
Use with caution.
NEONATES: contraindicated
Indications for Gabapentin
1.Antiepileptic(Treatment of partial seizure)
2.Treatment of neuropathic pain
Interactions for Gabapentin
N/A
Typical Dosage for Gabapentin
Adult: Initial dose: 300 mg / day increase the dose by 300 mg/day for next 2 days (up to 900 mg / day in 3 divided doses). Thereafter increase the dose until sufficient therapeutic response is obtained.
Maintenance dose: 900-1800mg /day in 3 divided doses
Maximum dose: 3.6 g /day
Children above 12 years: 10mg / kg / day in 3 divided doses, then gradually increase the dose until sufficient therapeutic response is obtained.

Schedule of Gabapentin
N/A
Storage Requirements for Gabapentin
Store at 15 - 30 degree C. Protect from heat and moisture.Store the Gabapentin solution at refrigerator.
Effects of Missed Dosage of Gabapentin
Take the missed dose as soon as noticed. If it the time for next dose then skips the missed dose and continue the regular schedule. Do not double the dose
Effects of Overdose of Gabapentin
Give supportive measures and symptomatic treatment. Haemodialysis can be done if needed

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