Skip to main content

Calcitriol Uses, Side Effects, and More

 Calcitriol 

Brand name:- Caltrol, Rolsical ,Rocaltrol 0.25ùg cap. Calcibest 1ml aqueous inj;

Calcitriol is the active form of Vitamin D. It raises Vitamin D levels in your blood. This in turn raises calcium levels in your blood by helping you absorb more calcium from your intestine.

Pharmacodynamic:-

Calcitriol is a biologically active calcitrophic hormone with anti-osteoporotic, immunomodulatory, anticarcinogenic, antipsoriatic, antioxidant, and mood-modulatory activities. Its main sites of action are the intestine, bone, kidney and parathyroid hormone Label. Calcitriol is a ligand for the vitamin D nuclear receptor, which is expressed in, but not limited to, gastrointestinal (GI) tissues, bones, and kidneys . As an active form of vitamin D3, calcitriol elevates the plasma levels of calcium by stimulating intestinal calcium uptake, increasing reabsorption of calcium by the kidneys, and possibly increasing the release of calcium from skeletal stores. The duration of pharmacologic activity of a single dose of exogenous calcitriol is expected to be about 3 to 5 days Label.

In addition to its important role in calcium metabolism, other pharmacological effects of calcitriol have been studied in various conditions including cancer models. Various studies demonstrated expression of vitamin D receptors in cancer cell lines, including mouse myeloid leukemia cells . Calcitriol has been found to induce differentiation and/or inhibit cell proliferation in vitro and in vivo in many cell types, such as malignant cell lines carcinomas of the breast, prostate, colon, skin, and brain, myeloid leukemia cells, and others 2. In early human prostate cancer trials, administration of 1.5 µg/d calcitriol in male participants resulted in a reduction in the rate of PSA rise in most participants, however it was coincided with dose-limiting hypercalcemia in most participants 1. Hypercalcemia and hypercalcuria were evident in numerous initial trials, and this may be due to these trials not testing the drug at concentrations that are active in preclinical systems 2. Findings from preclinical data show an additive or synergistic antineoplastic action of calcitriol when combined with agents including dexamethasone, retinoids, and radiation, as well as several cytotoxic chemotherapy drugs such as platinum compounds .

Vitamin D deficiency has long been suspected to increase the susceptibility to tuberculosis. The active form of calcitriol, 1,25-(OH)2-D3, has been found to enhance the ability of mononuclear phagocytes to suppress the intracellular growth of Mycobacterium tuberculosis. 1,25-(OH)2-D3 has demonstrated beneficial effects in animal models of such autoimmune diseases as rheumatoid arthritis. Vitamin D appears to demonstrate both immune-enhancing and immunosuppressive effects.


 Mechanism of action:-


The mechanism of action of calcitriol in the treatment of psoriasis is accounted for by their antiproliferative activity for keratinocytes and their stimulation of epidermal cell differentiation. The anticarcinogenic activity of the active form of Calcitriol appears to be correlated with cellular vitamin D receptor (VDR) levels. Vitamin D receptors belong to the superfamily of steroid-hormone zinc-finger receptors. VDRs selectively bind 1,25-(OH)2-D3 and retinoic acid X receptor (RXR) to form a heterodimeric complex that interacts with specific DNA sequences known as vitamin D-responsive elements. VDRs are ligand-activated transcription factors. The receptors activate or repress the transcription of target genes upon binding their respective ligands. It is thought that the anticarcinogenic effect of Calcitriol is mediated via VDRs in cancer cells. The immunomodulatory activity of calcitriol is thought to be mediated by vitamin D receptors (VDRs) which are expressed constitutively in monocytes but induced upon activation of T and B lymphocytes. 1,25-(OH)2-D3 has also been found to enhance the activity of some vitamin D-receptor positive immune cells and to enhance the sensitivity of certain target cells to various cytokines secreted by immune cells.

A study suggests that calcitriol plays an immunoregulatry role by suppressing the aryl hydrocarbon receptor (AhR) expression in human Th9, a pro-inflammatory CD4 T cell subset 9. This suppression subsequently leads to repressed expression of BATF, a transcription factor essential for Th9 9. Calcitriol has also been found to induce monocyte differentiation and to inhibit lymphocyte proliferation and production of cytokines, including interleukin IL-1 and IL-2, as well as to suppress immunoglobulin secretion by B lymphocytes.

 Used:- 

Used in the treatment of calcium deficiency and post menopausal osteoporosis.

Side effects:- 

Calcitriol does not usually have side effects.
Headache, Abdominal pain, Nausea, Increased calcium level in blood, Rash, Urinary tract infection, Itching, Erythema (skin redness)

Dose:- As directed by your doctor.

Comments

Popular posts from this blog

BOTULINUM TOXIN Uses, Side Effects, and More

 BOTULINUM TOXIN ( A or B ) BRAND NAME:- BOTOX ,DYSPORT  BOTULINUM TOXIN  A and B are highly potent exotoxins produced by Clostridium botulinum that are responsible for ' botulism' ( a type of food poisoning). These neurotoxic proteins cause long- lasting loss of cholinergic transmission by interacting with axonal proteins involved in exocytotic release of Ach. Localized injection of minute quantity of botulinum toxin.  PHARMACODYNAMIC :- Botulinum toxin A inhibits the release of acetylcholine, relieving muscle contraction and spasm associated with many conditions, such as incontinence and dystonia. Cosmetically, botulinum toxin A paralyses muscles in the face to temporarily treat wrinkles. The maximum effects of muscle paralysis occur four to seven days after a dose.When injected at therapeutic doses, botulinum toxin A causes partial chemical denervation of muscle tissue, causing local reduction of muscle activity. Muscle atrophy may result, axonal sprouting may beg...

Clonazepam used, Side effects, Dose, & more

Clonazepam  Brand name:- Lonazepam , Clonapax , Rivotril 0.5, 1.0, 2.0 mg tab. Clonazepam is a benzodiazepine. It works by increasing the action of a chemical messenger (GABA) which suppresses the abnormal and excessive activity of the nerve cells in the brain. Pharmacodynamic:- The pharmacodynamic properties of clonazepam are common among benzodiazepines and include anticonvulsive, sedative, muscle relaxing and anxiolytic effects . Animal data and electroencephalographic investigations in man have shown that clonazepam rapidly suppresses many types of paroxysmal activity including the spike and wave discharge in absence seizures (petit mal), slow spike wave, generalized spike wave, spikes with temporal or other locations, as well as irregular spikes and waves Label . Moreover, the agent can also decrease the frequency, amplitude, duration, and spread of discharge in minor motor seizures Label . Generalized EEG abnormalities are more readily suppressed by clonazepam than are focal ...

CLOMIPHENE CITRATE Uses, Side Effects, and More

 CLOMIPHENE CITRATE BRAND NAME:- CLOMIPHENE, FERTOMED, CLOFERT, CLOME 25,50,100mg tab.  Clomiphene is a selective estrogen receptor modulator (SERM) which treats female infertility. It works by promoting the release of reproductive hormones. This helps stimulate the release of eggs from the ovary (ovulation). PHARMACODYANIMCS:- Clomifene (previously clomiphene) is an orally administered, non steroidal, ovulatory stimulant that acts as a selective estrogen receptor modulator (SERM). Clomifene can lead to multiple ovulation, and hence increase the risk of conceiving twins. In comparison to purified FSH, the rate of ovarian hyperstimulation syndrome is low. There may be an increased risk of ovarian cancer and weight gain. Clomifene is capable of interacting with estrogen-receptor-containing tissues, including the hypothalamus, pituitary, ovary, endometrium, vagina, and cervix. It may compete with estrogen for estrogen-receptor-binding sites and may delay replenishment of intracel...