Seremax Forte

Each hard gelatin capsule contains: Pregabalin 75 mg, Mecobalamin 750 mcg, Alpha Lipoic Acid USP 100 mg.
Pregabalin is y-aminobutyric acid analogue ((S)-3-(aminomethyl-5-methylhexanoic acid). It is an anticonvulsant drug use for neuropathic pain and as an adjunct therapy for partial seizures with or without secondary generalization in adults. It has also been found effective for generalized anxiety disorder. It was designed as more potent successor to gabapentin.
Mecobalamin is a cobalamin used in the treatment of peripheral neuropathy, diabetic, and as preliminary treatment for amyotrophic lateral sclerosis.
Chemically it is carbamide; cobalt (3+).
Alpha Lipoic Acid is an organosulfur compound derived from octanoic acid. Chemically it is (R)-5-(1,2-dithiolan-3-yl) pentonic acid.

Pharmacology: Pregabalin binds to an auxiliary subunit (a₂-δprotein) voltage-gated Calcium channels in the central nervous system.
Mecobalamin: The exact mechanism of action is not yet elucidated, it is possible that mecobalamin is needed for the synthesis of melatonin, since the biosynthetic formation of melatonin requires the donation of a methyl group.
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 biological antioxidant activity, antioxidant recycling activity and activity in enhancing biological energy production.
Pharmacokinetics: Pregabalin is well absorbed after oral administration, is eliminated largely by renal excretion, and has an elimination half-life about 6 hours.
Absorption and Distribution: Following oral administration of seremax capsule under fasting conditions, peak plasma concentrations occur within 1.5 hours. Pregabalin oral bioavailability is ≥90% and is independent of dose. Following single (25-300mg) and multiple-dose (75 to 900 mg/day) administration, maximum plasma concentration (Cmax) and area under plasma concentration-time curve (AUC) values increase linearly. Following repeated administration, steady state is achieved within 24 to 28 hours. Multiple-dose pharmacokinetics can be predicted from single-dose data.
The rate of pregabalin absorption is decreased when given with food, resulting in decreasing in (max of approximately 25% to 30% and an increase in Tmax approximately 3 hours. However, administration of pregabalin with food has no clinically relevant effect on the total absorption of pregabalin. Therefore, pregabalin can be taken with or without food. Pregabalin does not bind to plasma protein. The apparent volume of distribution of pregabalin following oral distribution is approximately 0.5 L/kg.
Pregabalin is a substance for system L transporter for the transport of large amino acids across the blood brain barrier. Although there are no data in human, pregabalin has been shown to cross the blood brain barrier in mice, rats, and monkey. In addition, pregabalin has been shown to cross the placenta in rats and is presented in the milk of lactating rats.
Metabolism and Elimination: Pregabalin undergoes negligible metabolism in humans. Following a dose of radiolabeled pregabalin, approximately 90% of the administered dose recovered in the uterine as unchanged pregabalin. The N-methylated derivative of pregabalin, the major metabolite of pregabalin found in the urine, accounted for 0.9% of the dose. In preclinical studies, pregabalin (S-enantiomer) did not undergo racemisation to the R-enantiomer in mice, rats, rabbits, or monkeys.
Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug with a mean elimination half-life of 6.3 hours in subjects with normal renal function. Mean renal clearance was estimated to be 67.0 to 80.9 mL/min in young healthy subjects. Because pregabalin is not found to plasma proteins this clearance rate indicates that renal tubular reabsorption is involved. Pregabalin elimination is nearly proportional to creatinine clearance (ClCr).
Mecobalamin: Absorption of Mecobalamin following oral administration. The quantity of cobalamin detected following a small oral dose of mecobalamin but significantly more cobalamin accumulates in liver tissue following administration of mecobalamin. Human urinary excretion of mecobalamin is about one third, indicating substantially greater tissue retention.
Alpha Lipoic Acid: Alpha Lipoic Acid is absorbed from the small intestine and distributed to the liver via the portal circulation and to various tissues in the body via 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.

Drug used to treat epileptic seizures, an anticonvulsant.

The dose range is 150 mg to 600 mg per day given in either two or three divided doses.
Neuropathic Pain: Pregabalin treatment can be started at a dose of 150 mg per day given as two or three divided doses. Based on individual patient response and tolerability, the dose may increased to 300 mg per day after an interval of 3 to 7 days, and if needed, to a maximum dose of 600 mg per day after additional 7-day interval.
Mecobalamin: Oral administration of Mecobalamin (500 mcg three times daily for four months) resulted in subjective improvement in burning sensations, numbness, loss of sensation, and muscle cramps.
Alpha Lipoic Acid: In diabetic neuropathy dose is 300 milligrams daily of the oral preparation, should be taken in divided dose.
Method of administration: Seremax Forte is for oral use only. May be taken with or without food.
Hepatic Impairment: No dosage adjustment is required for patients with hepatic impairment (see Pharmacokinetics under Actions). Administration: SEREMAX FORTE may be taken with or without food. (See table.)

Click on icon to see table/diagram/image

In overdoses up to 15 g, no unexpected adverse reactions were reported. In the post-marketing experience, the most commonly reported adverse events observed when pregabalin was taken in overdose included affective disorder, somnolence, confusional state, depression, agitation and restlessness. Treatment of pregabalin overdose should include general supportive measures and may include haemodialysis if necessary.

Hypersensitivity to the active substances to any of excipients.

Diabetic Patients: In accordance with current clinical practice, some diabetic patients who gain weight on pregabalin treatment may need to adjust hypoglycaemic medications.
Hypersensitivity Reactions: There have been reports in the post-marketing experience of hypersensitivity reactions, including cases of angioedema. Pregabalin should be discontinued immediately if symptoms of angioedema eg. facial, perioral or upper airway swelling occur.
Pregabalin treatment has been associated with dizziness and somnolence, which could increase the occurrence of accidental injury (fall) in the elderly population. There have also been post-marketing reports of loss consciousness, confusion and mental impairment. Therefore, Patients should be advised to exercise caution until they are familiar with the potential effects of the medications.
Renal Failure: Cases of renal failure have been reported and in some cases discontinuation of pregabalin did show reversibility of this adverse reaction.
Galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. Renal impairment, diabetes, discontinue if symptoms of angioedema occurs. CHF. Monitor patients for signs of suicidal ideation & behaviours. May impair ability to drive or operate machinery. Pregnancy & lactation, Adolescent 12-17 yr & children <12 yr. Elderly >65 yr.
Use in Pregnancy: There are no adequate data on the use of pregabalin in pregnant women, Studies in animals have shown reproductive toxicity. The potential risk for humans is unknown. Pregabalin should not be used during pregnancy unless clearly necessary (if the benefit to the mother clearly outweighs the potential risk to the fetus). Effective contraception must be used in women of childbearing potential.
Use in Lactation: It is known if pregabalin is excreted in the breast milk of humans; however, it is present in the milk of rats. Therefore, breastfeeding is not recommended during treatment with pregabalin.

Use in Pregnancy: There are no adequate data on the use of pregabalin in pregnant women, Studies in animals have shown reproductive toxicity. The potential risk for humans is unknown. Pregabalin should not be used during pregnancy unless clearly necessary (if the benefit to the mother clearly outweighs the potential risk to the fetus). Effective contraception must be used in women of childbearing potential.
Use in Lactation: It is known if pregabalin is excreted in the breast milk of humans; however, it is present in the milk of rats. Therefore, breastfeeding is not recommended during treatment with pregabalin.

Dizziness, somnolence. Increased appetite & weight; euphoria, confusion, irritability, decreased libido, disorientation, insomnia, ataxia, abnormal, coordination, balance disorder, amnesia, tremor, dysarthria, memory impairment, attention disturbance, paraesthesia, sedation, lethargy, blurred vision, diplopia, vertigo; vomiting, dry mouth, constipation, flatulence, abdominal distension, erectile dysfunction, abnormal gait, drunk feeling, fatigue, peripheral oedema, abnormal feeling.
Mecobalamin: has excellent tolerability and no toxicity.
Alpha Lipoic Acid: Alpha Lipoic Acid in doses up to 600 milligrams daily has been well tolerated.

Since pregabalin is predominantly excreted unchanged in the urine, undergoes in the urine, undergoes negligible metabolism in human (<2% of a dose recovered in urine as metabolites), does not inhibit drug metabolite in vitro, and is not bound to plasma proteins, it is unlikely to produce, or be subject to pharmacokinetic interactions. Accordingly, in in vivo studies, no clinically relevant pharmacokinetic interactions were observed between pregabalin and phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone or ethanol. Population pharmacokinetic analysis indicated that oral antidiabetics, diuretics, insulin, Phenobarbital, tiagabine and topiramate has no clinically significant effect on pregabalin clearance. Co-administration of pregabalin with the oral contraceptives norethisterone and/or ethinyl oestradiol does not influence the steady-state pharmacokinetics of either substance.
Pregabalin may potentiate the effects of ethanol and lorazepam. In controlled clinical trials, multiple oral doses of pregabalin co-administered with oxycodone, lorazepam or ethanol did not result in clinically important effects on respiration. Pregabalin appears to be additive in the impairment of cognitive and gross motor function caused by oxycodone.
In the post marketing experience, there are reports of respiratory failure and coma in patients taking pregabalin and other central nervous system depressant medications. There are post-marketing reports of events related to reduce lower gastrointestinal tract function (eg, intestinal obstruction, paralytic ileus, constipation) when pregabalin was co-administered with medications that have the potential to produce constipation eg. Opioid analgesic. No specific pharmacodynamic interaction studies were conducted in elderly volunteers. Interaction studies have only been performed in adults.
Mecobalamin: There is no known adverse reactions when taken in conjunction with medication.
Alpha Lipoic Acid: Supplemental alpha lipoic acid any lower blood glucose levels.

Store at temperatures not exceeding 30°C.

Anticonvulsants / Drugs for Neuropathic Pain / Vitamins &/or Minerals

N02BF02 - pregabalin ; Belongs to the class of gabapentinoids. Used to relieve pain and other conditions.

Rx