Prednisolone Actions

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Actions of Prednisolone in details

infoThe action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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CCMD Prednisolone is a glucocorticosteroid (GCS). This medication inhibits the function of leukocytes and tissue macrophages. Prednisolone restricts the migration of leukocytes in the area of inflammation. This drug violates the ability of macrophages to phagocytosis and the formation of interleukin-1. CCMD Prednisolone contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in inflammation. This medicine decreases capillary permeability caused by histamine release. Prednisolone inhibits the activity of fibroblasts and collagen formation.

CCMD Prednisolone inhibits the activity of phospholipase A2 which leads to suppression of the synthesis of prostaglandins and leukotrienes. This medication inhibits the release of COX (especially COX-2), which also helps reduce the production of prostaglandins.

CCMD Prednisolone reduces the number of circulating lymphocytes (T-and B-cells), monocytes, eosinophils and basophils as a result of their displacement from the bloodstream into lymphoid tissue; suppresses the formation of antibodies.

Prednisolone inhibits the release of pituitary ACTH and beta-lipotropina but it does not reduces the level of circulating beta-endorphin. This drug also inhibits the secretion of TSH and FSH.

CCMD Prednisolone has a vasoconstrictor effect with direct application to the vessels.

Prednisolone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. It stimulates gluconeogenesis, amino acid contributes to the capture of the liver and kidneys and increases the activity of enzymes of gluconeogenesis. In the liver, Prednisolone enhances the deposition of glycogen by stimulating the activity of glikogensintetazy and synthesis of glucose from the products of protein metabolism. This medicine increases blood glucose activates the secretion of insulin.

Prednisolone inhibits glucose uptake by fat cells that leads to the activation of lipolysis. However, due to an increase in insulin secretion is stimulated lipogenesis which contributes to the accumulation of fat.

CCMD Prednisolone also has catabolic effects in lymphoid and connective tissue, muscle, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone Prednisolone affects the processes of water and electrolyte metabolism: promotes the excretion of potassium and calcium, delay in the body of sodium and water. Osteoporosis and Itsenko-Cushing's syndrome are the main factors limiting the long-term therapy with corticosteroids. As a result of the catabolic actions it may suppress growth in children.

In high doses prednisone can increase the excitability of brain tissue and contributes to lowering the threshold of convulsive readiness. This medication stimulates the excessive production of hydrochloric acid and pepsin in the stomach which leads to the development of peptic ulcers.

When systemic use the therapeutic activity of Prednisolone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.

For external and local application the therapeutic activity of Prednisolone is due to anti-inflammatory, antiallergic and antiexudative (due to vasoconstrictor effect) effect.

As compared with hydrocortisone the anti-inflammatory activity of Prednisolone is 4 times greater, the mineralocorticoid activity is 0.6 times smaller.

How should I take Prednisolone?

Use Prednisolone only as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so may increase the chance of too much medicine being absorbed into the body and the chance of side effects.

Prednisolone is available in 2 forms: Prednisolone 0.12% eye drops and Prednisolone 1% eye drops. Use only the brand of Prednisolone that your doctor prescribed. Different brands may not work the same way. Ask your doctor or pharmacist if you have any questions.

To use the eye drops:

  • Wash your hands first with soap and water.
  • Shake the bottle well before each use.
  • Tilt your head back and, pressing your finger gently on the skin just beneath the lower eyelid, pull the lower eyelid away from the eye to make a space. Drop the medicine into this space.
  • Let go of the eyelid and gently close your eye. Do not blink. Keep the eye closed and apply pressure to the inner corner of your eye with your finger for 1 or 2 minutes to allow the medicine to be absorbed by the eye.
  • If you think you did not get the drop of medicine into your eye properly, use another drop.
  • To keep the medicine as germ-free as possible, do not touch the applicator tip to any surface (including the eye). Keep the bottle tightly closed and upright when you are not using it.

If you are wearing contact lenses, remove them before putting the drops in your eyes. Wait at least 15 minutes after using Prednisolone before putting your contact lenses back in.

Dosing

The dose of Prednisolone will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Prednisolone. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For ophthalmic dosage form (eye drops):
    • For inflammation of the eye:
      • Adults—Use one or two drops in the affected eye 2 to 4 times a day. Your doctor may tell you to use the drops more often during the first two days of treatment.
      • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of Prednisolone, apply it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule.

Storage

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Pred Mild® eye drops may be stored in a cool, dry place.

Prednisolone administration

infoAdministration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Your doctor may occasionally change your dose to make sure you get the best results.

Your steroid medication needs may change if you have unusual stress such as a serious illness, fever or infection, or if you have surgery or a medical emergency. Tell your doctor about any such situation that affects you.

Measure the liquid form of Prednisolone with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

You may need to shake the oral suspension (liquid) well just before you measure a dose. Follow the directions on your medicine label.

Keep the disintegrating tablet in its blister pack until you are ready to take the medicine. Open the package using dry hands, and peel back the foil from the tablet blister (do not push the tablet through the foil). Remove the tablet and place it in your mouth.

Allow the disintegrating tablet to dissolve in your mouth without chewing. Swallow several times as the tablet dissolves. If desired, you may drink liquid to help swallow the dissolved tablet.

Steroids can cause you to have unusual results with certain medical tests. Tell any doctor who treats you that you are using Prednisolone.

Do not stop using Prednisolone suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to avoid withdrawal symptoms when you stop using Prednisolone.

Wear a medical alert tag or carry an ID card stating that you take Prednisolone. Any medical care provider who treats you should know that you take steroid medication.

Store at room temperature away from moisture and heat.

Prednisolone pharmacology

infoPharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Mechanism of Action

Naturally occurring glucocorticoids (hydrocortisone and cortisone), which also have salt-retaining properties, are used as replacement therapy in adrenocortical deficiency states. Their synthetic analogs such as Prednisolone are primarily used for their potent anti-inflammatory effects in disorders of many organ systems.

Glucocorticoids such as Prednisolone cause profound and varied metabolic effects. In addition, they modify the body's immune responses to diverse stimuli.

Prednisolone is a synthetic adrenocortical steroid drug with predominantly glucocorticoid properties. Some of these properties reproduce the physiological actions of endogenous glucocorticosteroids, but others do not necessarily reflect any of the adrenal hormones' normal functions; they are seen only after administration of large therapeutic doses of the drug. The pharmacological effects of Prednisolone which are due to its glucocorticoid properties include: promotion of gluconeogenesis; increased deposition of glycogen in the liver; inhibition of the utilization of glucose; anti-insulin activity; increased catabolism of protein; increased lipolysis; stimulation of fat synthesis and storage; increased glomerular filtration rate and resulting increase in urinary excretion of urate (creatinine excretion remains unchanged); and increased calcium excretion.

Depressed production of eosinophils and lymphocytes occurs, but erythropoiesis and production of polymorphonuclear leukocytes are stimulated. Inflammatory processes (edema, fibrin deposition, capillary dilatation, migration of leukocytes and phagocytosis) and the later stages of wound healing (capillary proliferation, deposition of collagen, cicatrization) are inhibited.

Prednisolone can stimulate secretion of various components of gastric juice. Suppression of the production of corticotropin may lead to suppression of endogenous corticosteroids. Prednisolone has slight mineralocorticoid activity, whereby entry of sodium into cells and loss of intracellular potassium is stimulated. This is particularly evident in the kidney, where rapid ion exchange leads to sodium retention and hypertension.

Pharmacokinetics

Absorption

The maximum serum concentration of Prednisolone occurs within 1 to 2 hrs following a single dose of oral administration. Food intake prolongs the time to peak concentration, but does not affect the extent of absorption significantly.

Distribution

Prednisolone is reported to be 70-90% protein-bound in the plasma and the volume of distribution is reported as 0.22 - 0.7 L/kg.

Metabolism

Prednisolone is reported to be metabolized mainly in the liver and excreted in the urine as sulfate and glucuronide conjugates.

Excretion

Prednisolone is eliminated from the plasma with a half-life of 2 to 3 hours.

Oral administration of single dose of 15 mg/5 mL of Prednisolone, 15 mg/5 mL Prednisolone USP syrup, and 3× 5 mg Prednisolone USP tablets in 24 adult volunteers yielded comparable pharmacokinetic data:

Table 1. Comparison of Mean Pharmacokinetic Parameters (%CV) in Healthy Volunteers Following a Single Dose of 15 mg/5 mL of Prednisolone, 15 mg/5 mL Prednisolone USP Syrup, and 3× 5 mg Prednisolone USP Tablets
Dose*

(15 mg Prednisolone base equivalent)

AUC0-∞ (ng∙hr/mL)

(%CV)

Cmax (ng∙hr/mL)†

(%CV)

*
Administered under fasting conditions.
Mean values of 24 normal volunteers.
Prednisolone Suspension 1999.4 (60.0) 321.1 (52.0)
Prednisolone Syrup 1872.7 (50.4) 362.4 (37.8)
Prednisolone Tablet 1968.4 (54.6) 326.9 (43.5)

The systemic availability, metabolism and elimination of Prednisolone after administration of single weight-based doses (0.8 mg/kg) of intravenous (IV) Prednisolone and oral prednisone were reported in a study of 19 younger adult (aged 23 to 34 years) and 12 geriatric (65 to 89 years) subjects. Results showed that the systemic availability of total and unbound Prednisolone, as well as interconversion between Prednisolone and prednisone were independent of age. The mean unbound fraction of Prednisolone was higher, and the steady-state volume of distribution (Vss) of unbound Prednisolone was reduced in elderly patients. Plasma Prednisolone concentrations were higher in elderly subjects, and the higher AUCs of total and unbound Prednisolone were most likely reflective of an impaired metabolic clearance, evidenced by reduced fractional urinary clearance of 6b-hydroxyprednisolone. Despite these findings of higher total and unbound Prednisolone concentrations, elderly subjects had higher AUCs of cortisol, suggesting that the elderly population is less sensitive to suppression of endogenous cortisol or their capacity for hepatic inactivation of cortisol is diminished.



References

  1. DailyMed. "PREDNISOLONE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. NCIt. "Prednisolone: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
  3. EPA DSStox. "Prednisolone: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

Reviews

The results of a survey conducted on ndrugs.com for Prednisolone are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Prednisolone. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

User reports

2 consumers reported administration

When best can I take Prednisolone, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Prednisolone should be taken After food. In any case, this may not be the right description on how you ought to take this Prednisolone. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Prednisolone can be taken.
Users%
After food1
50.0%
With a meal1
50.0%


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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