Alfacalcidol (One alpha)- a partially activated vitamin D

Alfacalcidol (One alpha) is a partially activated form of vitamin D. Although it is relatively less potent than calcitriol, it has a longer half-life and is available as oral drops, tablets, and injections. It was first produced by Leo Pharma in 1973 and was first made available in Denmark in 1974 as an oral and inexpensive vitamin D.

Alfacalcidol tablet uses:

It is used in the treatment of:

Alfacalcidol has also been found to reduce the arterial stiffness, improve systolic blood pressure, and reduce left ventricular mass index. It has got immune-modulatory effects and has been found beneficial in patients with multiple sclerosis [Ref]. In another retrospective study, alfacalcidol plus denosumab demonstrated a significantly higher bone mineral density in non-CKD patients compared to denosumab plus inactivated vitamin D [Ref].

Alfacalcidol vs Cholecalciferol:

 

Alfacalcidol

Cholecalciferol
Activation status Partially activated (1-hydroxylated) Inactivated Vitamin D
Activation by PTH Does not require PTH for activation Requires PTH for activation
Formulations available Oral drops, Tablets, and injections Capsules, Gels, Tablets, Injections (Oral and Parenteral), Creams and ointments
Dosage strengths 0.25 mcg, 0.5 mcg 400 units, 800 units, 50,000 units, and 200,000 units.
Usual dose 0.25 mcg – 2 mcg per day 400 – 800 units daily OR 50,000 units weekly OR 200,000 units monthly
Half-life elimination 3 hours 2 – 3 weeks
Onset of action 6 hours 24 hours or more
Pregnancy category "C" “A” in usual doses
Efficacy in Renal failure effective ineffective
Efficacy in hypoparathyroidism effective ineffective

Alfacalcidol Contraindications

  • Hypersensitivity to vitamin D, its analogs or derivatives, or any component in the formulation
  • Hypercalcemia;
  • Hyperphosphatemia
  • Vitamin D toxicity

Warnings and Precautions

  • Vitamin D supplementation may cause over stimulation of parathyroid hormones (PTH), progressive hypercalcemia, hypercalciuria and hyperphosphatemia as well as a dynamic bone disease.
  • Hypermagnesemia can be avoided by avoiding magnesium-containing antacids
  • Digoxin-treated patients may experience hypercalcemia, which can lead to cardiac arrhythmias.

Alfacalcidol Dose in Adults

Alfacalcidol (One alpha) oral dose:

·         Predialysis patients:

Note: Limit supplemental calcium to less than 500 mg/day of elemental calcium

  • The initial dose is 0.25 mcg/day for 2 months.
  • The dose may be increased if required.
  • The maintenance usual dose is 0.5 mcg/day

Dialysis patients:

  • For up to 4 weeks, a starting dose of 1 mcg per day is administered.
  • The dose may be increased if required every 2-4 weeks in increments of 0.5 mcg/day.
  • The recommended daily dose is 1-2 mcg.
  • Some people may need up to 3 mcg each day.
  • 0.25 to 1 mcg per day is the typical maintenance dose.
  • The dosing interval may be increased (every other day) in patients who develop hypercalcemia

Alfacalcidol (One alpha) intravenous dose:

Dialysis patients:

  • One mcg per dialysis is the starting dose (2-3 times weekly).
  • After one week, if there is still insufficient improvement, the dose may be increased in weekly increments of 1 mcg per dialysis.
  • The weekly dosage cap is 12 mcg.
  • The total titration period should not exceed 6 weeks.

Maintenance dose:

  • 1.5 to 12 mcg each week (divided equally between hemodialysis sessions).
  • 6 mcg/week is the typical effective dosage.

 

Alfacalcidol Dose in Chlidrens

Alfacalcidol dose in hypophosphatemic rickets, persistent hypocalcemia due to hypoparathyroidism or pseudohypoparathyroidism:

  • Child 1 month–11 years:

    • 25–50 nanograms/kg once daily, the dose to be adjusted as necessary. (maximum 1 microgram per day)

  • Child 12–17 years:

    • 1 microgram once daily, the dose is adjusted as necessary.

Alfacalcidol dose in the prevention of vitamin D deficiency in renal or cholestatic liver disease

  • Child 1 month–11 years (body-weight up to 20 kg):

    • 15–30 nanograms/kg once daily (max. per dose 500 nanograms)

  • Child 1 month–11 years (body-weight 20 kg and above):

    • 250–500 nanograms once daily, the dose is adjusted as necessary

  • Child 12–17 years:

    • 250–500 nanograms once daily, the dose is adjusted as necessary.

Alfacalcidol dose equivalence and conversion:

  • One drop of alfacalcidol 2 microgram/mL oral drops contains approximately 100 nanograms alfacalcidol.

Alfacalcidol Dose in kidney disease:

  • The manufacturer's labelling makes no mention of adjusting the dosage.

Alfacalcidol Dose in hepatic impairment:

  • The manufacturer's labelling makes no mention of adjusting the dosage.

Dose adjustment for toxicity:

Predialysis patients:

  • Reduce the dose to 0.25 mcg every other day if hypercalcemia appears within the first two months of treatment.
  • If hypercalcemia develops at any other time during therapy, reduce the dose by 50% and discontinue all calcium supplements until serum calcium levels normalize.

Dialysis patients:

  • (Oral and intravenous) Discontinue immediately in patients with hypercalcemia.
  • After the serum calcium levels normalize, the drug may be reinitiated at a lower dose.

How to administer Alfacalcidol?

  • Administer oral solution, oral drops, and capsules with food.

Intravenous injection:

  • Shake injection solution well prior to use and administer as bolus intravenous injection over 30 seconds at the end of each dialysis. 

Pregnancy category C

  • Safety has not been established in pregnant women.
  • Alfacalcidol enters breast milk. It is therefore not recommended during breastfeeding

Alfacalcidol Side effects:

  • Cardiovascular:

      • hypertension
      • Cardiac arrhythmia,

  • Central nervous system:

    • hyperthermia,
    •  Headache,
    • somnolence
    • psychosis (rare),

  • Dermatologic:

    • Pruritus

  • Genitourinary:

    • Nocturia

  • Endocrine & metabolic: 

    • hypercholesterolemia
    • libido decreased
    • hyperphosphatemia
    • polydipsia
    • Hypercalcemia,

  • Gastrointestinal:

    • weight loss
    • constipation
    • pancreatitis
    • vomiting
    • taste abnormal
    • nausea
    • xerostomia
    • Anorexia

  • Hepatic:

    • AST increased
    • ALT increased

  • Neuromuscular & skeletal: 

    • muscle pain
    • Bone pain
    • weakness

  • Ocular:

    • corneal calcification
    • Conjunctivitis
    • photophobia

  • Renal:

    • Polyuria
    • BUN increased

  • Respiratory:

    • Rhinorrhea

Mechanism of action of Alfacalcidol:

  • Alfacalcidol successfully avoids renal metabolic conversion by being converted quickly in the liver to the active vitamin D metabolite (1,25-dihydroxyvitamin D 3).
  • It can encourage renal reabsorption as well as intestinal absorption and resorption of calcium and/or phosphorus.

The Onset o action is about 6 hours

1,25-(OH) 2 D 3's effect on intestinal calcium absorption levels lasts for 48 hours.

Protein binding: It is extensively bound to vitamin D-binding protein.

Metabolism: Hepatic to 1,25-(OH) 2 D 3

Half-life elimination is 3 hours in renal insufficiency

Time to the peak of active vitamin D levels after oral administration is 12 hours and after intravenous administration is 4 hours.

Alfacalcidol Brand names in Pakistan

A-BONE (EVERGREEN PHARMACEUTICALS PVT LIMITED)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 0.00

ADELA (GETZ PHARMA PAKISTAN (PVT) LTD)

Tablets : 0.25 mcg :

10 tablets pack : Rs. 70.00

Tablets : 1 mcg :

10 tablets pack : 200.00

Tablets : 0.5 mcg]

10 tablets pack : Rs. 150.00 20 tablets pack :Rs.  300.00 30 tablets pack : Rs. 400.00 60 tablets pack : Rs. 600.00

ALBONE D (ALLIANCE PHARMACEUTICALS (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 127.00

Tablets : 0.25 mcg :

10 tablets pack : Rs. 70.00

ALCIDOL (EVEREST PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

Tablets : 1 mcg :

10 tablets pack : Rs. 200

Tablets : 0.25 mcg :

10 tablets pack : Rs. 70

ALCIDOL (MIRACLE PHARMACEUTICALS(PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

ALFA-D (PLATINUM PHARMACEUTICALS (PVT.) LTD)

Drops : 0.2 mcg/ml

20 ml pack : Rs. 550.00

Syrup : 0.5 mcg/5ml

60 ml pack : Rs. 156.00

Tablets : 0.25 mcg

10 tablets pack : Rs. 80.0

Tablets : 0.5 mcg

10 tablets pack : Rs. 150.00

Tablets  : 1 mcg :

10 tablets pack : Rs. 200.00

ALFABONE (RAKAPOSHI PHARMACEUTICAL (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

ALFACAL  (ZESION PHARMACEUTICAL (PVT) LTD)

Tablets : 0.5 mcg :

20 tablets pack : Rs. 300.00

ALFADAL (SHAHEEN AGENCIES)

Tablets : 0.5 mcg :

30 tablets pack : Rs. 350.00

Syrup : 0.5 mcg/ml :

60 ml pack : Rs. 156

ALFADIX (NEO MEDIX)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

ALFADOX (SWAN PHARMACEUTICALS(PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

20 tablets pack : Rs. 300

ALFAGOOD (GOODMAN LABORATORIES)

Tablets : 0.5 mcg :

20 tablets pack : Rs. 300.00

ALFAMAK (MAKSON PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

ALFAS (FASSGEN PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

ALPHA-PLUS (ROTEX MEDICA PAKISTAN (PVT) LTD)

Capsules : 0.25 mcg :

10 capsules pack : Rs. 70.00

Capsules : 1 mcg :

10 capsules pack : Rs. 200.00

Capsules : 1 mcg

20 capsules pack : Rs. 380.00

Tablets : 0.5 mcg

10 tablets pack : Rs. 150.00 30 tablets pack : Rs. 400.00 60 tablets pack : Rs. 600.00

BIO D3 (BIO LABS (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

BIOALFA (BIO LABS (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

BIOALFA (SURGE LABORATORIES (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 120.00

BIODOL TAB (BROOKES PHARMACEUTICAL LABORATORIES (PAK.) LTD)

Tablets : 0.5 mcg :

30 tablets pack : Rs. 400.00

BONAFIDE INJECTION (S.J & G. FAZUL ELLAHIE (PVT)LTD)

Injection : 2 mcg/ml :

ten 0.5 ml injecctions pack : Rs. 500

BON-ONE (MARTIN DOW PHARMACEUTICALS (PAK) LTD)

Tablets : 0.5 mcg :

40 tablets pack : Rs. 753.90

BONCID (SAYDON PHARMACEUTICAL INDUSTRIES (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs.150.00

BONE-CARE (SCHAZOO ZAKA)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 100.00

BONEDOL (PHARMEVO (PVT) LTD)

Tablets : 0.25 mcg :

10 tablets pack : Rs. 60.0

Tablets : 0.5 mcg :

10 tablets pack : Rs. 120.00

Tablets  : 1 mcg :

10 tablets pack : Rs. 150.00

BONEHEEL (GRAY`S PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

30 tablets pack : Rs. 400

BONEX (LOTUS PHARMACEUTICALS (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

BONIDOL (BIOGEN PHARMA)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

20 tablets pack : Rs. 300

30 tablets pack : Rs. 400

40 tablets pack : Rs. 600

BONION (OBSONS PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

20 tablets pack : Rs. 300

30 tablets pack : Rs. 400

BONREX (BIOREX PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

Tablets  : 1 mcg :

10 tablets pack : Rs. 200.00

CADLA ( MACTER INTERNATIONAL (PVT) LTD)

Tablets : 0.5 mcg :

20 tablets pack : Rs. 278.00

CALSAF (SAAAF PHARMACEUTICALS)

Tablets : 0.5 mcg :

20 tablets pack : Rs. 300.00

CARACAL (CARAWAY PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

Tablets  : 1 mcg :

10 tablets pack : Rs. 200.00

DENS (FARM AID GROUP PAK LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

ELCICAL (CREST PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

20 tablets pack : Rs. 300

30 tablets pack : Rs. 400

40 tablets pack : Rs. 600

ELSEDOL (BLOOM PHARMACEUTICALS (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

20 tablets pack : Rs. 300

30 tablets pack : Rs. 400

ENGBONE (ENGLISH PHARMACEUTICALS INDUSTRIES)

Injection : 0.5 mcg/ml :

10 injections pack : Rs. 200

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

ERGOKET-D (BLOOM PHARMACEUTICALS (PVT) LTD)

Tablets : 0.5 mcg :

20 tablets pack : Rs. 300.00

EVER-ALFA (EVEREST PHARMACEUTICALS)

Tablets : 1 mcg :

10 tablets pack : Rs. 200

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

EVERALFA (MAARK PHARMA)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

GROWELL (POLYFINE CHEMPHARMA (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

HANCIDOL (HANSEL PHARMACUEUTICAL PVT (LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 148.00

HIBONE (OLIVE PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

HYPOCAL (MEDICRAFT PHARMACEUTICALS (PVT) LTD)

Tablets : 0.5 mcg :

30 tablets pack : Rs. 400.00

HELPHA (HYGEI PHARMACEUTICALS)

Injection : 2 mcg/ml :

10 x 5 ml pack : Rs. 300.00 5 x 5 ml pack : Rs. 150.00

INDROP ALPHA (NEUTRO PHARMA (PVT) LTD)

Tablets : 0.5 mcg :

30 tablets pack : Rs. 400.00

KELFA (MEDERA PHARMACEUTICALS (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

MAXI-ALFA (MAX PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

20 tablets pack : Rs. 300

30 tablets pack : Rs. 400

60 tablets pack : Rs. 600

Tablets : 1 mcg :

10 tablets pack : Rs. 200

MEDCIDOL (MEDLEY PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

20 tablets pack : Rs. 300

30 tablets pack : Rs. 400

Tablets : 0.25 mcg :

10 tablets pack : Rs. 80

MYALFA (WELMARK PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150.00

NENALFA (NENZA PHARMACEUTICALS (PVT) LIMITED)

Tablets : 0.25 mcg :

10 tablets pack : Rs. 70

Tablets : 0.5 mcg :

30 tablets pack : Rs. 390.00

NEXBONE (HIRANIS PHARMACEUTICALS PVT LTD)

Tablets : 0.25 mcg :

10 tablets pack : Rs. 70

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

ORTHODOL (GLOBAL PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

OSIVITOL (ARIES PHARMACEUTICALS (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

OSTEDOL (HANSEL PHARMACUEUTICAL PVT (LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 148

OSTEO-D (GILLMAN PHARMACEUTICALS)

Tablets : 0.5 mcg :

20 tablets pack : Rs. 300

OSTEODOL (PARAMOUNT PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

OSTIBON (GENIX PHARMA (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 140

QUNJI PLUS (NIMRALL LABORATORIES)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

REBONE (ANCHOR PHARMA)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

Tablets : 0.25 mcg :

10 tablets pack : Rs. 70

REBOOST (ELKO ORGANIZATION (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

20 tablets pack : Rs. 300

30 tablets pack : Rs. 400

60 tablets pack : Rs. 600

Tablets : 1 mcg :

10 tablets pack : Rs. 180

Drops : 0.2 mcg/ml :

20 ml pack : Rs. 500

RECALBON (SAMI PHARMACEUTICALS (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

SERL ALPHA (SEARLE PAKISTAN (PVT.) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

Tablets : 0.25 mcg :

10 tablets pack : Rs. 70

Tablets : 1 mcg :

10 tablets pack : Rs. 200

TASOCAL (TAS PHARMACEUTICAL)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

UNI-DOL (UNISON CHEMICAL WORKS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

UNIDOL (GT PHARMA )

Tablets : 0.5 mcg :

10 tablets pack : Rs. 139

VITALPHA-D (RAY PHARMA (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

VONE (AMBROSIA PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

Tablets : 1 mcg :

10 tablets pack : Rs. 200

WINDOL (WNS FIELD PHARMACEUTICALS)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

20 tablets pack : Rs. 300

X-BONE (WILSHIRE LABORATORIES (PVT) LTD)

Tablets : 0.5 mcg :

10 tablets pack : Rs. 150

Tablets : 0.25 mcg :

10 tablets pack : Rs. 70

Tablets : 1 mcg :

10 tablets pack : Rs. 200

XONE-ONE (XENON PHARMACEUTICALS (PVT) LTD)

Capsules : 1 mcg :

10 capsules pack : Rs. 333.00

Capsules : 0.25 mcg :

100 capsules pack : Rs. 1223.00

Capsules : 0.5 mcg :

30 capsules pack : Rs. 600.00

10 tablets pack : Rs. 150

LFACARE (CHERWEL PHARMACEUTICALS (PVT) LTD)

Capsule : 0.5 mcg :

10 capsules pack : Rs. 150

ALFAGEN (GENOME PHARMACEUTICALS (PVT) LTD)

Capsule : 0.5 mcg :

10 capsules pack : Rs. 135

BIODOL (BIO LABS (PVT) LTD)

Capsule : 0.5 mcg :

10 capsules pack : Rs. 135

CAL-BONE (GOODMAN INTERNATIONAL)

Capsule : 0.5 mcg :

30 capsules pack : Rs. 600

FADOL (MIRACLE PHARMACEUTICALS(PVT) LTD)

Capsule : 0.5 mcg :

10 capsules pack : Rs. 150

ONE ALPHA ( ZAM ZAM CORPORATION)

Capsules : 1 mcg :

10 capsules pack : Rs. 333.00

Capsules : 0.25 mcg :

100 capsules pack : Rs. 1223.00

Capsules : 0.5 mcg :

30 capsules pack : Rs. 600.00

Drops : 0.2 mcg/ml :

20 ml pack : Rs. 1285.00

Injections : 0.5 mcg/ml :

10 injections pack : Rs. 1334.00

TRYLOC (CSH PHARMACEUTICALS-NORTH (PVT) LTD)

Capsules : 1 mcg :

10 capsules pack : Rs. 200.00

Capsules : 0.25 mcg :

10 capsules pack : Rs. 70.00

Capsules : 0.5 mcg :

30 capsules pack : Rs. 600.00

Alfacalcidol brand names (International):

  • 1 Alpha Leo
  • Alfa Caps
  • Alfacan
  • Alfadiol
  • Alfarol
  • Alpha D3
  • Alphacal
  • Bon-One
  • Bondiol
  • EinsAlpha
  • Etalpha
  • Gr-Alfa
  • Innosfen
  • One-Alpha
  • Onealfa
  • Ostidil-D3
  • QTR-Alfa
  • Tevacidol
  • Un Alfa
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