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Steadfast MediShield Pvt. Ltd

Noida, Uttar Pradesh

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Pharmaceutical Products

Offering you a complete choice of products which include AB-lol Tablets, Adferol Capsules, Aplazar Tablets, Awaytox Capsules, Costead Capsules and Deflazacort Tablets.

AB-lol Tablets
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AB-lol Tablets

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Description

AB-lol is Labetalol HCl Tablet which is an adrenergic receptor blocking agent having both selective alpha1-adrenergic and nonselective beta-adrenergic receptor blocking actions in a single substance.

Composition

Each film coated tablet of AB-lol Tablets contains Labetalol HCl 50 mg.

Pharmacology

Labetalol HCl combines both selective, competitive, alpha1-adrenergic blocking and nonselective, competitive, betaadrenergic blocking activity in a single substance. In man, the ratios of alpha- to beta-blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. Beta2-agonist activity has been demonstrated in animals with minimal beta1-agonist (ISA) activity detected. In animals, at doses greater than those required for alpha- or beta-adrenergic blockade, a membrane stabilizing effect has been demonstrated.

Pharmacodynamics

The alpha- and beta-blocking actions of orally administered Labetalol HCl contribute to a decrease in blood pressure in hypertensive patients. Labetalol HCl consistently, in dose-related fashion, blunted increases in exercise-induced blood pressure and heart rate, and in their double product. The pulmonary circulation during exercise was not affected by Labetalol HCl dosing.

Single oral doses of Labetalol HCl administered to patients with coronary artery disease had no significant effect on sinus rate, intraventricular conduction, or QRS duration. The atrioventricular (A-V) conduction time was modestly prolonged in two of seven patients. In another study, IV Labetalol HCl slightly prolonged A-V nodal conduction time and atrial effective refractory period with only small changes in heart rate. The effects on A-V nodal refractoriness were inconsistent.

Labetalol HCl produces dose-related falls in blood pressure without reflex tachycardia and without significant reduction in heart rate, presumably through a mixture of its alpha- and beta-blocking effects. Hemodynamic effects are variable, with small, nonsignificant changes in cardiac output seen in some studies but not others, and small decreases in total peripheral resistance. Elevated plasma renins are reduced.

Doses of Labetalol HCl that controlled hypertension did not affect renal function in mildly to severely hypertensive patients with normal renal function. Due to the alpha1-receptor blocking activity of Labetalol HCl, blood pressure is lowered more in the standing than in the supine position, and symptoms of postural hypotension (2%), including rare instances of syncope, can occur. Following oral administration, when postural hypotension has occurred, it has been transient and is uncommon when the recommended starting dose and titration increments are closely followed. Symptomatic postural hypotension is most likely to occur 2 to 4 hours after a dose, especially following the use of large initial doses or upon large changes in dose.

 

The peak effects of single oral doses of Labetalol HCl occur within 2 to 4 hours. The duration of effect depends upon dose, lasting at least 8 hours following single oral doses of 100 mg and more than 12 hours following single oral doses of 300 mg. The maximum, steady-state blood pressure response upon oral, twice-a-day dosing occurs within 24 to 72 hours.

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Adferol Capsules
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Adferol Capsules

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Description

Cholecalciferol is an amber crystalline solid compound. It is a secosterol that is a natural precursor of the calcium-regulating hormone — Calcitriol (1, 25-dihydroxyvitamin).

Composition

Adferol is available as soft-gel capsules containing 60,000 IU of cholecaliciferol.

Pharmacology

Pharmacodynamics

Cholecalciferol (vitamin D3) is a steroid hormone that has long been known for its important role in regulating body levels of calcium and phosphorus, in mineralization of bone and for the assimilation of Vitamin A. The classical manifestation of vitamin D deficiency is rickets, which is seen in children and results in bony deformities including bowed long bones. Deficiency in adults leads to the disease osteomalacia. Both rickets and osteomalacia reflect impaired mineralization of newly synthesized bone matrix and usually result from a combination of inadequate exposure to sunlight and decreased dietary intake of vitamin D. Common causes of vitamin D deficiency include genetic defects in the vitamin D receptor, severe liver or kidney disease and insufficient exposure to sunlight. Vitamin D plays an important role in maintaining calcium balance and in the regulation of parathyroid hormone (PTH). It promotes renal reabsorption of calcium, increases intestinal absorption of calcium and phosphorus and increases calcium and phosphorus mobilization from bone to plasma.

Cholecalciferol is generated in the skin of animals when light energy is absorbed by a precursor molecule, 7-dehydrocholesterol. Vitamin D, as either D3 or D2, does not have significant biological activities. Rather, it must be metabolized within the body to the hormonally active form known as 1, 25-dihydroxycholecalciferol. This transformation occurs in two steps, as depicted below:

Within the liver, cholecalciferol is hydroxylated to 25-hydroxycholecalciferol by the enzyme 25-hydroxylase.

Within the kidney, 25-hydroxycholecalciferol serves as a substrate for 1-alpha-hydroxylase, yielding 1, 25-dihydroxycholecalciferol, the biologically active form. Adferol increases the serum calcium concentrations by increasing GI absorption of phosphorus and calcium, increasing osteoclastic reabsorption and increasing distal renal tubular reabsorption of calcium. Adferol appears to promote intestinal absorption of calcium through binding to the vitamin D receptor in the mucosal cytoplasm of the intestine. Subsequently, calcium is absorbed through formation of a calcium-binding protein.

Pharmacokinetics

Absorption: Well absorbed from the GI tract. The presence of bile is essential for adequate intestinal absorption. Hence, absorption may be decreased in patients with decreased fat absorption.

Distribution: Bound to a specific α-globulin. Cholecalciferol can be stored in adipose and muscle tissue for long periods of time. It is slowly released from storage sites and skin where it is formed in the presence of sunlight or UV light. Cholecalciferol may distribute through breast milk.

Metabolism: Hydroxylated in the liver by the enzyme vitamin D 25-hydroxylase to form 25-hydroxycholecalciferol (calcifediol). It is further hydroxylated in the kidneys by the enzyme Vitamin D1-hydroxylase to form the active metabolites 1, 25-dihydroxycholecalciferol (calcitriol). Further metabolism also occurs in the kidneys, including the formation of the 1, 24, 25-trihydroxy derivatives.

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Aplazar Tablets
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Aplazar Tablets

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Description

APLAZAR contains all amino acids essential for uremic patients, five out of them are keto or hydroxyanalogue in the form of calcium salts. Therefore it allows reduction in the nitrogen supply and provides calcium. It is a medication for the treatment of chronic kidney disease patients on Conservative management therapy (CKD stage I, II, III). In combination with very low protein diet / low protein diet, it helps in delaying the progression of kidney disease in the Predialysis period.

Composition

One film-coated tablet contains:

    • Calcium-3-methyl-2-oxovalerate (α-ketoanalogue of isoleucine,Calcium salt)67 mg
    • Calcium-4-methyl-2-oxovalerate (α-ketoanalogue of leucine,Calcium-salt)101 mg
  • 101 mg Calcium-2-oxo-3-phenylpropionate (α-ketoanalogue of phenylalanine,Calcium-salt) 68 mg
  • Calcium-3-methyl-2-oxobutyrate (α-ketoanalogue of valine,Calcium-salt) 86 mg
  • Calcium-DL-2-hydroxy-4-(methylthio)-butyrate α-hydro xyanalogue of methionine,Calcium salt)59mg
  • L-lysine 75 mg
  • L-threonine 53 mg
  • L-tryptophan 23 mg
  • L-histidine 38 mg
  • L-tyrosine 30 mg
Indications

Prevention and therapy of damages due to faulty or deficient protein metabolism in chronic renal insufficiency in connection with limited protein in food of 40 g per day (for adults) and less; i.e. generally in patients with a glomerular filtration rate (GFR) below 25 ml/min.

Contraindications

Hypercalcemia, disturbed amino acid metabolism. In case of hereditary phenylketonurie it has to be taken into account that this product contains phenylalanine.

Precautions and Warnings

No experience has been made so far with the application in pregnancy and pediatrics. APLAZAR should be taken during meals to allow proper absorption and metabolism into the corresponding amino acids. The serum calcium level should be monitored regularly. An adequate supply of calories should be ensured.

Undesirable effects

Hypercalcemia may develop. In this case, it is recommended to decrease vitamin D intake. If the hypercalcaemia persists, reduce the dosage of APLAZAR as well as any other source of calcium.

Drug Interactions

Simultaneous administration of medicinal products that contain calcium (e.g. acetolyte) may trigger, or worsen, a pathological increase in the serum calcium level.

As the uremic symptoms improve under therapy with APLAZAR tablets, the dose of aluminum hydroxide administered should be reduced, as appropriate. The patient should be monitored for reduced levels of serum phosphate.

In order not to interfere with absorption, an appropriate interval should be observed between administration of APLAZAR tablets and medicinal products which form poorly soluble compounds with calcium (e.g. tetracyclines, quinolones such as ciprofloxacin and norfloxacin, preparations that contain iron, fluoride and estramustin). An interval of at least 2 hours should be observed between the intake of APLAZAR tablets and such preparations.

If administration of APLAZAR tablets leads to increased blood levels of calcium, the sensitivity to medicinal products which increase heart action (cardiac glycosides) and thus also the risk of cardiac arrhythmia is increased

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Awaytox Capsules
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Awaytox Capsules

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Description

Awaytox is a Pre-Probiotic combination, a blend of probiotic Lactobacillus and Bifidobacterium species, the two most important genuses associated with the human intestinal tract and oral adsorbent Lactitol monohydrate.

Patients with chronic disease have abnormal microbiota when compared to healthy individuals. Diet and impaired protein absorption, increased intestinal transit time, medications, and uremia may all contribute to unfavorable changes in microbiota. Probiotic is used to maintain a friendly bacterial balance for support to healthy digestion. Probiotics are used to eliminate uremic toxics in CKD patients and in patients undergoing dialysis.

Composition
Bifidobacterium longum5 Billion CFU
Lactobacillus acidophilus5 Billion CFU
Streptococcus thermophilus5 Billion CFU
Total Count15 Billion CFU
Lactitol monohydrate USP (Prebiotic)100 mg
Pharmacodynamics

Awaytox Pre-Probiotic is a blend of probiotic Lactobacillus and Bifidobacterium species, the two most important genuses associated with the human intestinal tract and oral adsorbent Lactitol monohydrate. Each capsule supplies 15 billion active cells, otherwise called colony forming units (CFU).

Lactobacillus acidophilus 5 billion CFU

Studies have shown that dialysis patients, who were given freeze-dried Lactobacillus acidophilus, have reduced concentration of toxins (methylamine, demethylmine, nitrosamines and several other carcinogenic amines) in the bloodstream. In addition, it also helps to prevent the growth of pathogenic bacteria in the small bowel.

Bifidobacterium longum 5 billion CFU

These bacteria utilize various phenolic and indole metabolic toxic compounds in the colonic region as its nutrients for growth.

Streptococcus thermophilus 5 billion CFU

This bacterium actually utilizes urea/Creatinine/uric acid as nutrients for its increased growth and survival and thus help cleanse the bloodstream of urea and uric acid.

Our extensive research provides strong evidence that the three power Probiotics help the human gastrointestinal tract function as a pseudo kidney to filter out waste products that are usually the responsibility of kidney.

Indication

Awaytox is indicated in Renal Impairment for reducing the burden on impaired kidney.

Dosage and Administration

The recommended dosage of Awaytox in CKD is 1-2 capsules with every meal. The dose should be adjusted to suit the requirements of the individual patients.

Adverse Side Effects

Probiotic bacteria are indigenous to the human intestinal tract and their introduction into the alimentary tract is not associated with adverse side effects or considered a risk to health.

The daily recommended dose, or exceeding the recommended daily dose, may cause irritation and possibly a change in stool characteristics. Dose adjustments will resolve overuse problems.

Interactions

Probiotics used too soon after an antibiotic dosing could result in a loss of antibiotic efficacy. Follow standard pharmacy recommendations for dosing separation of probiotic and antibiotic substances.

Probiotic gains in friendly bacteria populations will be reduced by antibiotic therapy. Patients should be encouraged to support and maintain probiotic populations during and after an antibiotic course.

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Costead Capsules
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Costead Capsules

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Description

Coenzyme Q10 is the active antioxidant nutrient ingredient. The term ‘Coenzyme’ denotes it as an organic, non-protein molecule. The ‘Q’ refers to the quinone chemical group and the ‘10’ refers to the 10 isoprenyl chemical subunits. This oil-soluble, vitamin-like substance is present in most eukaryotic cells, primarily in the mitochondria.

It is a component of the electron transport chain and participates in aerobic cellular respiration, generating energy in the form of ATP. 95% of a human body’s energy is generated in this manner. Therefore, those organs with the highest energy requirements — such as the heart, liver and kidney — have the highest CoQ concentrations.

CoQ10 is naturally present in small amounts in a wide variety of foods, but the levels are particularly high in organ meats such as heart, liver and kidney as well as beef, soy oil, sardines, mackerel and peanuts.

Coenzymes help enzymes work to digest food and perform other body processes and they help protect the heart and skeletal muscles.

Pharmacokinetics

Some reports have been published on the pharmacokinetics of CoQ10. The plasma peak can be observed 2–6 hours after oral administration, mainly depending on the design of the study. In some studies, a second plasma peak was also observed at about 24 hours after administration, probably due to both entero-hepatic recycling and redistribution from the liver to circulation. Tomono et al. used deuterium-labelled crystalline CoQ10 to investigate pharmacokinetics in human and determined an elimination half-time of 33 hours.

Absorption

  • CoQ10 is a crystalline powder that is insoluble in water.
  • Absorption follows the same process as that of lipids and the uptake mechanism appears to be similar to that of Vitamin E, another lipid-soluble nutrient.
  • This process in the human body involves the secretion into the small intestines of pancreatic enzymes and bile that facilitate emulsification and micelle formation required for the absorption of lipophilic substances.
  • Food intake (and the presence of lipids) stimulates bodily biliary excretion of bile acids and greatly enhances the absorption of CoQ10.
  • Exogenous CoQ10 is absorbed from the small intestinal tract and is best absorbed when taken with a meal.

Metabolism

Data on the metabolism of CoQ10 in animals and humans are limited. A study with C-14 labelled CoQ10 in   showed most of the radioactivity in the liver 2 hours after oral administration when the peak plasma radioactivity was observed, but it should be noted that CoQ9 is the predominant form of coenzyme Q in  . It appears that CoQ10 is metabolised in all tissues, while a major route for its elimination is biliary and fecal excretion. After the withdrawal of CoQ10 supplementation, the levels return to normal within a few days, irrespective of the type of formulation used.

Mechanism of Action
  • The highest concentrations are found in the heart, liver, kidney and pancreas. The lowest concentrations are found in the lungs.
  • The human body produces the coenzyme Q10. Humans can replenish coenzyme Q10 from dietary sources including meats and seafood.
  • Within the cell, coenzyme Q-10 is mostly present in the mitochondria (40- 50%). It is the electron acceptor for the mitochondrial electron transport chain.

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Deflazacort Tablets
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Deflazacort Tablets

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Description

Defstead is Deflazacort, a glucocorticoid and an oxazoline derivative of prednisolone with anti-inflammatory and immunosuppressive activity.

Indication and Usage

This medication is a glucocorticoid, prescribed for anti-inflammatory conditions and used as an immunosuppressant. It is a prodrug. Deflazacort is indicated in a wide variety of conditions viz. Nephrotic Syndrome, Transplantation, Systemic Lupus Erythematosus, Uveitis, Duchhene and Dystrophy.

Dose and Administration

Defstead tablets should be taken with food.

Adult: Initially, up to 120 mg daily

Maintenance: 3-18 mg/day

Child: 0.25-1.5 mg/kg/day on alternate days

In cases of hepatic impairment, dose reductions may be needed.

Conversion of dose from Prednisolone to Deflazacort

6 mg of Deflazacort has approximately the same anti-inflammatory potency as 5 mg Prednisolone

Side Effects

Long-term use of high doses of Deflazacort may cause ‘Cushing’s syndrome’. These side-effects usually return to normal once the treatment has been stopped.

Pharmacology

Deflazacort is an inactive prodrug, which is converted rapidly to the active metabolite 21-desacetyldeflazacort. Maximum concentrations of 21-desacetyldeflazacort averaged 116 ng/ml and were observed after 1.3 hours. The terminal half-life was 1.3 hours. 21-Desacetyldeflazacort was cleared significantly faster than both Methylprednisolone and Prednisolone.

Pharmacokinetics

Pharmacokinetics of deflazacort in renal transplanted and hemodialyzed children:

Deflazacort (DFZ) pharmacokinetics was evaluated in fifteen pediatric patients on chronic hemodialysis or after renal transplantation and in three normal children. After overnight fasting, oral DFZ 0.26+/-0.01 mg/kg (mean +/- SEM) was given. Serial blood samples were collected for 360 min and analyzed by HPLC for 21-hydroxy-DFZ (21-HO-DFZ). Serum concentration profiles and pharmacokinetic parameters were similar in patients on hemodialysis, renal transplant recipients and normal children. Elimination of half-life was longer in the 9 cyclosporine-treated subjects (108.0+/-13.6 min) than in the other nine (71.2+/-8.3 min; p <0.02). The finding suggests that from a pharmacokinetic point of view, DFZ dose adjustment for renal function is not necessary in children with chronic renal failure or after renal transplantation.

Contraindications

The medicine is contraindicated in patients who are receiving immunosuppressive vaccines, who have infections and hypersensitivity.

Warnings and Precautions

Caution should be exercised in patients with history of adrenal suppression, infections (ex-chickenpox, shingles, measles) children, elderly, tuberculosis, muscle pain, recent heart attack, high blood pressure, heart failure, liver failure, kidney impairment, sugar, increased eye pressure, osteoporosis, corneal damage, epilepsy, peptic ulcer, under active thyroid, during pregnancy and breastfeeding.

Presentation

Defstead-6 is available as a blister of 10 uncoated tablets in a strip and 10 such blisters in a box.

Defstead-30 is available as a blister of 10 uncoated tablets in a strip and 10 such blisters in a box.

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Dilminox Tablets
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Dilminox Tablets

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Description

Minoxidil (Dilminox) is an orally active peripheral vasodilator. The pure compound is soluble in water to the extent of approximately 2 mg/ml and is readily soluble in propylene glycol or ethanol. Chemically, Minoxidil (Dilminox) is 2.4-diamino-6-piperidino-pyrimidine-3-oxide. The Molecular Weight is 209.25.

Composition

Each uncoated tablet of Dilminox contains Minoxidil I.P. 5 mg

Pharmacology

Minoxidil (Dilminox) selectively relaxes the arteriolar smooth muscle, which reduces peripheral vascular resistance and lowers systemic blood pressure. This is accomplished without a diminution of nutritional flow to body tissues or interference with normal vasomotor reflexes.

Minoxidil (Dilminox) does not directly stimulate the heart or electrolyte reabsorption of the kidney. However, Minoxidil’s (Dilminox) administration elicits a reflex mediated increase in cardiac output, salt and water retention, and a rise in plasma renin activity. These effects are diminished by the simultaneous administration of diuretics and beta-adrenergic blocking agents.

Gastrointestinal absorption is rapid and amounts to at least 95% of the administered dose. Serum levels of the parent drug peak within the first hour. The plasma elimination half-life of Minoxidil (Dilminox) is approximately 4-4.5 hours, but the duration of its hypotensive action may exceed 24 hours. This disparity between blood level and pharmacological effect and the large volume of distribution indicated extensive tissue localization of the drug. However, on chronic treatment, accumulation does not occur and the pharmacological effect is slowly reversible.

With an effective oral dose, blood pressure usually starts to decline within one — half hour, reaches a minimum between 2 and 3 hours and recovers at a rate of approximately 30%/day.

During daily administration, there is a cumulative effect which reaches a steady state after 3 to 7 days. The magnitude of the blood pressure response is related to the extent of the original diastolic elevation above 85 mm Hg and is proportional to the logarithmic function of the dose administered. When the desired diastolic reduction is greater than 30 mm Hg, twice a day dosing is advised to keep the diurnal variation within 10 mm Hg.

Minoxidil does not bind to plasma proteins, enter the central nervous system or accumulate in body tissues. Metabolism is predominantly by glucuronic acid conjugation. Metabolites are excreted principally in the urine and can be removed by hemodialysis in anephric patients. Hemodialysis does not, however, rapidly reverse the pharmacological effect of Minoxidil.

Indications

It is indicated as adjunctive therapy in adults with severe refractory hypertension, which has failed to respond to extensive multiple therapies. When used in combination with an accompanying diuretic and beta-blocker, Minoxidil (Dilminox) has been shown to reverse encephalopathy and retinopathy in severe hypertensives.

Contraindications

Minoxidil (Dilminox) is contraindicated in phaeochromocytoma and pulmonary hypertension secondary to mitral stenosis.

Warnings

If used alone, Minoxidil (Dilminox) can cause a significant retention of salt and water, producing dependent oedema, puffiness of face, eyes or hands, neck vein distention and hepatojugular reflux. Chest X-rays may show evidence of pulmonary vascular engagement.

 

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Magmaxx Tablets
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Magmaxx Tablets

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Description:

It has an empirical formula of MgO and consists of a lattice of Mg2+ ions and O2− ions held together by ionic bonding.Magnesium (Mg) is the fourth most abundant cation in the body and the second most important intracellular cation.

In recent years, Mg has gained much importance with the growing awareness that Mg is required as a cofactor in multiple enzymatic reactions and that it plays an important role in neuromuscular processes . Mg also has a role in mineral bone metabolism, adenosine triphos- phate metabolism, neurotransmitter release and in the regulation of vascular tone, heart rhythm and platelet- activated thrombosis .

In patients with chronic kidney disease (CKD) and end-stage renal disease (ESRD), changes in Mg homeo- stasis may occur. An understanding of the physiology in Mg handling is therefore of relevance for those taking care of patients with CKD and ESRD.

Composition:

Each film coated tablet contains light Magnesium Oxide 400mg which is equivalent to elemental magnesium 241.2mg or 19.6 mEq.

Indication:

Magmaxx is indicated in the management of Hypomagnesemia associated with Acute kidney injury, NODAT/ PTDM, Post Renal Transplant & Tacrolimus use.

Hypomagnesemia is usually defined as serum Magnesium,<0.7 mmol/L, <1.4 mEq/L, or <1.7 mg/dl.

Treatment with magnesium salts is indicated when magnesium deficiency is symptomatic or the magnesium concentration is persistently < 1.25 mg/dL (< 0.50 mmol/L).

Dosage & Administration:

Oral 1 to 2 tabs daily of Magmaxx can be taken until serum magnesium concentration reaches 2.5-3.0 mg/dL.

Treatment is indicated when Magnesium concentration is <1.25mg/l (<0.50mmol/l).

Warnings:

This medication contains magnesium oxide. Do not take Magmaxx if allergic to magnesium oxide or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help immediately.

Precautions:

Pregnancy and Lactation

Use of Magnesium oxide during pregnancy is generally acceptable.Controlled studies in pregnant women show no evidence of foetal risk.350-400 mg/ day elemental magnesium is recommended during pregnancy.

Magnesium oxide is distributed in breast milk; 310-360 mg/day elemental magnesium is recommended during breastfeeding.

Contraindications:

Patients with renal impairment (creatinine clearance of less than 30 mL per minute [0.5 mL per second]) may be at risk of heart block or hypermagnesemia

Adverse Reactions:

Oral supplementation generally is safe and well-tolerated; some reports of nausea, vomiting, diarrhoea; overdose may lead to hypotension & muscle weakness.

Storage:

Keep in a dry place at a temperature not exceeding 30°C. Protected from light.

Presentation:

Magmaxx is available as tablets in a strip of 10 tablets and 5 such strips in a box.

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ActiveD Capsules
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ActiveD Capsules

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Description

Calcitriol is a synthetic vitamin D analog which is active in the regulation of the absorption of calcium from the gastrointestinal tract and its utilization in the body. Calcitriol is a white, crystalline compound which occurs naturally in humans. It has a calculated molecular weight of 416.65 and is soluble in organic solvents but relatively insoluble in water.

Composition

ActiveD is available as soft gelatin capsules containing 0.25 micrograms of Calcitriol.

Pharmacology Pharmacodynamics

Calcitriol is the most important active metabolite of Vitamin D3. It is normally formed in the kidney from its precursor 25-hydroxycholecalciferol (25-HCC). Physiological daily production is normally 0.5 – 1.0µg and is somewhat higher during periods of increased bone synthesis (e.g., growth or pregnancy). The natural supply of Vitamin D in humans depend mainly on exposure to ultraviolet rays of the sun for conversion of 7-dehydrocholesterol in the skin to Vitamin D3 (cholecalciferol). Vitamin D3 must be metabolically activated in the liver and the kidney before it is fully active as a regulator of calcium and phosphorus metabolism at target tissues. The initial transformation of Vitamin D3 is catalysed by a Vitamin D3-25-hydroxylase enzyme (25-OHase) present in the liver and the product of this reaction is 25-hydroxyvitamin D3 [25-(OH) D3]. Hydroxylation of 25-(OH) D3 occurs in the mitochondria of kidney tissue, activated by the renal 25-hydroxyvitamin D3-1 alpha-hydroxylase (alpha-OHase), to produce 1,25-(OH)2 D3 (Calcitriol), the active form of Vitamin D3.

Calcitriol binds to an intracellular receptor, a member of the steroid receptor superfamily. The calcitriol receptor complex interacts with specific DNA sequences that regulate transcription and protein synthesis in a variety of cells including osteoblasts, mucosal cells of the intestine, renal tubular cells and parathyroid cells. The changes in protein synthesis induced in these cells by Calcitriol are responsible for its profound physiological effects. A Vitamin D-resistant state exists in uremic patients because of the failure of the kidney to convert precursors to the active compound. The uremic state may also inhibit the binding of the Calcitriol receptor to its specific DNA responsive elements. The key role of Calcitriol in the regulation of bone and calcium homeostasis, which includes stimulating effects on osteoblastic activity in the skeleton, provides a sound pharmacological basis for its therapeutic effects in osteoporosis. The treatment of established osteoporosis with Calcitriol is associated with an increase in bone density and a reduction in new vertebral fractures. Established osteoporosis is defined as the finding of bone mineral density measurements of 2 or more standard deviations below the gender specific peak bone mass; or the presence or history of osteoporotic fracture. Calcitriol also reduces bone loss associated with corticosteroid therapy.

In patients with marked renal impairment, synthesis of endogenous Calcitriol is correspondingly limited or may even cease altogether. This deficiency plays a key role in the development of renal osteodystrophy.

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